Definitions of Analgesics o Opioid overdose.

o Respiratory depression.
1. General Definition: Pain relief without inducing o Low-dose use for opioid-induced constipation.
unconsciousness.  Contraindications:
2. Clinical Definition: Inhibition or modulation of pain o Hypersensitivity.
signals in the CNS. o Precipitation of acute withdrawal.
 Side Effects:
o Tachycardia, nausea, withdrawal symptoms.

Classification of Analgesics Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)

1. Non-Opioid Analgesics Classifications by Mechanism of Action

 Definition: Drugs for mild-to-moderate pain, acting 1. Non-Selective COX Inhibitors: Inhibit both COX-1 and
outside the opioid system. COX-2 enzymes (e.g., aspirin, ibuprofen).
 Examples: NSAIDs, Acetaminophen. 2. Preferential COX-2 Inhibitors: Primarily inhibit COX-
2 but retain some COX-1 activity (e.g., meloxicam,
 Mechanism:
nimesulide).
o NSAIDs: Inhibit COX-1 and/or COX-2
3. Selective COX-2 Inhibitors: Exclusively inhibit COX-2
enzymes → ↓ Prostaglandins → ↓
enzyme (e.g., celecoxib, etoricoxib).
Pain/Inflammation.
4. Analgesic Antipyretics with Poor Anti-inflammatory
o Acetaminophen: Central prostaglandin
Action: Provide pain relief and fever reduction but
inhibition (weak anti-inflammatory effects).
limited anti-inflammatory activity (e.g., paracetamol).
2. Opioid Analgesics
Subclassifications by Chemical Structure

 Definition: Drugs for moderate-to-severe pain, acting on

1. Subsalicylates
opioid receptors.
o Example: Aspirin
 Examples: Morphine, Fentanyl. o Explanation: Irreversible COX-1 and COX-2
 Mechanism: inhibitor with anti-inflammatory, analgesic, and
o Bind to μ, δ, and κ receptors → Inhibit pain antipyretic effects.
signal transmission in CNS. 2. Propionic Acid Derivatives
o Examples: Ibuprofen (Brufen), Ketoprofen
3. Co-Analgesics (Adjuvant Analgesics) (Ketoprin)
o Explanation: Reversible inhibitors of COX
 Definition: Drugs not primarily for pain but enhance or enzymes; commonly used for mild-to-moderate
manage specific pain types. pain and inflammation.
 Examples: 3. Enolic Acid Derivatives
o Antidepressants (e.g., Amitriptyline for o Examples: Piroxicam, Tenoxicam
neuropathic pain). o Explanation: Long-acting NSAIDs that
o Anticonvulsants (e.g., Gabapentin for nerve preferentially inhibit COX-2.
pain). 4. Phenamate Derivatives
 Mechanism: o Example: Mefenamic Acid
o Antidepressants: Serotonin/norepinephrine o Explanation: Used for dysmenorrhea and
modulation. inflammatory pain.
o Anticonvulsants: Stabilize nerve membranes. 5. Acetic Acid Derivatives
o Examples: Ketorolac, Indomethacin,
Diclofenac, Aceclofenac
o Explanation: Potent NSAIDs with anti-
inflammatory and analgesic properties.
Epidural Analgesia 6. Selective COX-2 Inhibitors
o Examples: Celecoxib (Celebrex), Etoricoxib,
 Definition: Delivery of analgesics into the epidural Parecoxib
space for acute/chronic pain. o Explanation: Designed to minimize
 Mechanism: gastrointestinal side effects associated with
o Local Anesthetics: Sodium channel blockade COX-1 inhibition.
→ ↓ Nerve conduction. 7. Para-Aminophenol Derivatives
o Opioids: Spinal opioid receptor binding → ↓ o Example: Paracetamol
Pain transmission. o Explanation: Centrally acting analgesic and
antipyretic with minimal anti-inflammatory
effects.
8. Pyrazolone Derivatives
o Example: Metamizole
Pure Opioid Antagonists
o Explanation: Analgesic and antipyretic often
used for severe pain or fever.
 Examples: Naloxone, Naltrexone. 9. Benzoxazocine Derivatives
 Mechanism: Block μ receptors → Reverse opioid o Example: Nefopam
effects.
 Indications:
 o Explanation: Centrally acting non-opioid Max
analgesic with minimal anti-inflammatory Drug Class Dosage
Dose/Day
effects.
500–1000 mg
Pyrazolone
Metamizole every 6–8 4g
derivative
hours
30–90 mg
Opioid Analgesics Benzoxazocine
Nefopam every 6–8 120 mg
derivative
hours
Classifications by Source 10–30 mg
No defined
Morphine Natural opioid every 4 hours
1. Natural Opium Alkaloids upper limit
(oral)
o Examples: Morphine, Codeine 15–60 mg
o Explanation: Derived directly from the opium Codeine Natural opioid every 4–6 240 mg
poppy; used for severe pain. hours
2. Semi-Synthetic Opioids
o Examples: Diacetylmorphine (Heroin), 25–100 Based on
Synthetic
Ethylmorphine, Pholcodine Fentanyl mcg/hour patient
opioid
o Explanation: Chemically modified natural (transdermal) response
alkaloids with potent analgesic effects. 50–100 mg
Synthetic
3. Synthetic Opioids Tramadol every 4–6 400 mg
opioid
o Examples: Pethidine, Fentanyl, Tramadol, hours
Methadone 2.5–10 mg
o Explanation: Fully synthetic compounds Synthetic
Methadone every 8–12 Individualized
designed to mimic natural opioid effects with opioid
hours
varying potency and duration.
Indications & Contraindications (Mnemonic: ANALGESIC)

Indications:
Dosage Table for Mentioned Drugs
 A: Acute pain (e.g., surgery, trauma).
Drug Class Dosage
Max  N: Neuropathic pain.
Dose/Day  A: Arthritis.
325–650 mg  L: Labor pain.
Aspirin Subsalicylate
every 4–6 4g  G: Gout.
hours  E: Endometriosis.
Propionic acid
200–400 mg  S: Sickle cell crisis.
Ibuprofen
(Brufen) derivative
every 4–6 3200 mg  I: Inflammatory conditions.
hours  C: Cancer pain.
50–100 mg
Ketoprofen Propionic acid
every 6–8 300 mg Contraindications:
(Ketoprin) derivative
hours

Piroxicam
Enolic acid 10–20 mg once
20 mg  A: Allergy to the drug.
derivative daily  N: NSAID-induced asthma.
Enolic acid 20 mg once  A: Active peptic ulcer disease.
Tenoxicam 20 mg
derivative daily  L: Liver failure (paracetamol).
500 mg  G: GI bleeding.
Mefenamic Phenamate initially, then  E: End-stage renal disease.
1500 mg
Acid derivative 250 mg every 6  S: Severe respiratory depression (opioids).
hrs  I: Intracranial pressure elevation.
Acetic acid 10 mg every 4–  C: Coagulopathy (NSAIDs).
Ketorolac 40 mg (oral)
derivative 6 hours
Acetic acid 25–50 mg 2–3
Indomethacin 200 mg
derivative times daily
Acetic acid 50 mg 2–3 Side Effects/Adverse Effects
Diclofenac 150 mg
derivative times daily
Acetic acid 100 mg twice System-Wise Examples:
Aceclofenac 200 mg
derivative daily
Selective COX- 100–200 mg  CNS: Sedation, dizziness (opioids).
Celecoxib 400 mg  GI: Gastritis, ulcers (NSAIDs).
2 inhibitor twice daily
Selective COX- 60–120 mg  Renal: Nephrotoxicity (NSAIDs).
Etoricoxib
2 inhibitor once daily
120 mg  Hepatic: Hepatotoxicity (paracetamol overdose).
Para- 500–1000 mg
Paracetamol aminophenol every 4–6 4g
derivative hours
Antidotes
  Paracetamol: N-acetylcysteine. o NSAIDs and Paracetamol inhibit COX enzymes
 Opioids: Naloxone. → ↓ Prostaglandin E2 (PGE2) production.
o Reduced hypothalamic set-point → ↓ Fever.

Drug Interactions
Dosage Table for Antipyretics
A table can detail:
Max
Drug Class Dosage
 NSAIDs: Risk of GI bleeding with anticoagulants. Dose/Day
 Opioids: Enhanced sedation with CNS depressants. Non-selective 325–650 mg
Aspirin 4g
 Acetaminophen: Hepatotoxicity risk with alcohol or NSAID every 4–6 hours
enzyme inducers. Non-selective 200–400 mg
Ibuprofen 3200 mg
NSAID every 4–6 hours
Definitions of Antipyretics 500–1000 mg
Paracetamol Para-aminophenol 4g
every 4–6 hours
1. General Definition: Antipyretics are medications used Pyrazolone 500–1000 mg
to reduce fever by lowering the body’s hypothalamic set- Metamizole 4g
derivative every 6–8 hours
point.
30–90 mg every
2. Clinical Definition: Antipyretics are drugs that Nefopam Benzoxazocine 120 mg
6–8 hours
modulate the production or action of pyrogenic
cytokines, thereby reducing fever without affecting 100–200 mg
Celecoxib Selective COX-2 400 mg
normal body temperature. twice daily
60–120 mg once
Etoricoxib Selective COX-2 120 mg
daily

Classification and Subclassification of Antipyretics

Indications (Mnemonic: ANTYPYRETICS)
1. NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)
 A: Acute infections (e.g., viral or bacterial).
 Definition: Reduce fever, pain, and inflammation by  N: Non-inflammatory fever.
inhibiting cyclooxygenase enzymes.  T: Temperature management in post-operative patients.
 Subclassification and Examples:  I: Influenza and common cold-related fever.
o Non-Selective COX Inhibitors: Aspirin,  P: Pain-associated fever (e.g., arthritis).
Ibuprofen.  Y: Young children with febrile seizures (e.g.,
o Selective COX-2 Inhibitors: Celecoxib, paracetamol).
Etoricoxib.  R: Rheumatic fever.
 E: Emergency fever reduction (e.g., metamizole in high
2. Para-Aminophenol Derivatives fever).
 T: Travel-related fever (e.g., malaria-induced fever).
 Definition: Primarily act as antipyretics and analgesics  I: Immunization-related fever.
with minimal anti-inflammatory effects.  C: Cancer-related fever (e.g., NSAIDs).
 Examples: Paracetamol (Acetaminophen).  S: Severe febrile illness (e.g., meningitis).

3. Pyrazolone Derivatives

 Definition: Provide antipyretic and analgesic effects, Contraindications (Mnemonic: ANTYPYRETICS)

often used for severe pain or fever.
 Examples: Metamizole.  A: Allergy to the drug.
 N: NSAID-induced asthma.
4. Benzoxazocine Derivatives  T: Thrombocytopenia (aspirin).
 I: Impaired renal or liver function (e.g., NSAIDs,
 Definition: Centrally acting antipyretics and analgesics. paracetamol overdose).
 Examples: Nefopam.  P: Peptic ulcer disease (NSAIDs).
 Y: Young children with viral infections (aspirin →
Reye's syndrome).
 R: Risk of bleeding disorders.
 E: Elderly with multiple comorbidities.
Mechanism of Action of Antipyretics (Flowchart)
 T: Third trimester of pregnancy (NSAIDs).
 I: Interactions with anticoagulants.
1. Fever Triggers: Infections or inflammation → Release
 C: Chronic alcohol use (paracetamol).
of pyrogens (e.g., IL-1, IL-6, TNF-α).
 S: Severe dehydration.
2. Effect on Hypothalamus: Pyrogens stimulate PGE2
synthesis in the hypothalamus → Raise set-point.
3. Antipyretic Action:
Side Effects (Body System Wise)  Mechanism of Action: Potentiates
GABA-A receptor activity, inhibiting
1. Central Nervous System: neuronal firing.
o Dizziness, headache, drowsiness (paracetamol, o Intravenous Anesthetics: Administered IV for
NSAIDs). rapid induction.
2. Gastrointestinal:  Example: Propofol.
o Gastritis, ulcers, nausea, vomiting, bleeding  Mechanism of Action: Enhances
(NSAIDs). GABAergic inhibition in the CNS,
3. Renal: causing sedation and hypnosis.
o Acute kidney injury (high doses of NSAIDs).
4. Hepatic: 2. Local Anesthetics
o Hepatotoxicity (paracetamol overdose).
5. Hematologic:  Subtypes:
o Bleeding tendency (aspirin). o Amide Local Anesthetics: Longer duration of
6. Hypersensitivity: action, metabolized by the liver.
o Rash, anaphylaxis (rare).  Example: Lidocaine.
 Mechanism of Action: Blocks sodium
channels, preventing nerve impulse
transmission.
Antidotes for Antipyretics o Ester Local Anesthetics: Shorter duration of
action, metabolized by plasma esterases.
1. Paracetamol: N-Acetylcysteine (NAC) → Restores  Example: Procaine.
glutathione and prevents liver damage.  Mechanism of Action: Similar
2. NSAIDs: Activated charcoal (early ingestion) or sodium channel blockade.
supportive care.
3. Aspirin: Sodium bicarbonate for alkalinizing urine or 3. Regional Anesthetics
hemodialysis in severe cases.
 Subtypes:
o Spinal Anesthesia: Injected into cerebrospinal
fluid, used for lower body surgeries.
Definitions of Anesthetics  Example: Bupivacaine.
 Mechanism of Action: Sodium
channel blocker causing sensory and
1. General Definition: Anesthetics are drugs that induce a
motor block.
reversible loss of sensation or consciousness, used
o Epidural Anesthesia: Injected into the epidural
during surgical or diagnostic procedures.
space for continuous pain relief.
2. Clinical Definition: Anesthetics are medications that
 Example: Ropivacaine.
modulate neural activity to suppress pain perception and
 Mechanism of Action: Similar
other sensory responses through central or peripheral
sodium channel blockade with
nervous system depression.
localized effects.

4. Dissociative Anesthetics

Stages of Anesthesia
 Subtype:
o NMDA Receptor Antagonists: Produce
1. Stage I – Analgesia: Induction of anesthesia with mild dissociative anesthesia, preserving airway
sedation, reduced pain, and maintained consciousness. reflexes.
2. Stage II – Excitement/Delirium: Loss of  Example: Ketamine.
consciousness, irregular breathing, and potential  Mechanism of Action: Blocks NMDA
agitation or involuntary movements. receptors, preventing excitatory
3. Stage III – Surgical Anesthesia: Regular breathing, neurotransmission.
muscle relaxation, and the absence of reflexes, suitable
for surgery.
4. Stage IV – Medullary Paralysis: Overdose stage
leading to respiratory and cardiac arrest, requiring
immediate intervention. Indications and Contraindications (Mnemonic:
ANESTHETIC)

Indications (Mnemonic: ANESTHETIC)

Types of Anesthetics
 A: Analgesia during surgery.
1. General Anesthetics  N: Neurological procedures (e.g., craniotomy).
 E: Emergency trauma surgeries.
 S: Sedation in ICU or diagnostic procedures.
 Subtypes:
 T: Targeted regional blocks (e.g., labor pain).
o Inhalational Anesthetics: Delivered via
inhalation; act on CNS to induce  H: Hypnosis induction for major surgeries.
unconsciousness.  E: Endoscopy and minor outpatient surgeries.
 Example: Isoflurane.  T: Tumor resection requiring extensive anesthesia.
  I: Intractable pain (e.g., nerve blocks). Drug Dosage Table
 C: Cardiovascular surgeries requiring bypass.
Max
Contraindications (Mnemonic: ANESTHETIC) Drug Type Dosage
Dose/Day
Inhalational Titrated to effect
Isoflurane NA
 A: Allergy to anesthetic agents. General (MAC 1-2%)
 N: Neuromuscular disorders (e.g., myasthenia gravis). 2–2.5 mg/kg
 E: Elevated intracranial pressure (e.g., ketamine Propofol IV General NA
(induction)
contraindicated).
1–5 mg/kg (with
 S: Severe respiratory compromise. Lidocaine Amide Local
epinephrine)
7 mg/kg
 T: Toxicity risks in liver failure (amide anesthetics).
Procaine Ester Local 7 mg/kg 800 mg
 H: Heart block or arrhythmias (local anesthetics).
 E: Epilepsy (caution with certain agents). 15–20 mg (spinal
Bupivacaine Spinal/Regional NA
 T: Third-trimester pregnancy (caution with some block)
anesthetics). 1–2 mg/kg (IV
Ketamine Dissociative NA
 I: Infection at the injection site (regional anesthesia). induction)
 C: Coagulopathy (spinal/epidural anesthesia). 20–30 mg
Ropivacaine Epidural/Regional NA
(epidural bolus)

Classification and Subclassification of General Anesthetics

Side Effects and Adverse Effects (Body System Wise)
1. Inhalation Anesthetics
1. Central Nervous System:
o Confusion, drowsiness, seizures, hallucinations  Definition: Delivered through inhalation; induce
(ketamine). unconsciousness by acting on the CNS.
2. Cardiovascular:  Subclassification:
o Hypotension, bradycardia, arrhythmias (local o Halogenated: Include volatile agents with
anesthetics, propofol). halogen atoms, ensuring high potency and
3. Respiratory: stability.
o Respiratory depression, airway obstruction  Halothane: Potent volatile anesthetic
(opioid anesthetics). with smooth induction and
4. Gastrointestinal: maintenance.
o Nausea, vomiting (common with inhalational  Isoflurane: Volatile anesthetic with
anesthetics). minimal cardiac depression.
5. Renal:  Enflurane: Causes muscle relaxation
o Reduced urine output with prolonged and has anticonvulsant properties.
anesthesia. o Non-Halogenated: Lack halogen atoms;
6. Allergic Reactions: include gaseous anesthetics.
o Urticaria, anaphylaxis (rare with local  Nitrous Oxide: Weak anesthetic but
anesthetics). excellent analgesic.
 Ether: Effective but rarely used due to
flammability.
 Cyclopropane: Rarely used, with
Drug Interactions good cardiovascular stability.

 Benzodiazepines: Potentiate CNS depression when 2. Intravenous Anesthetic Agents

combined with general anesthetics.
 Opioids: Additive respiratory depression with  Definition: Administered intravenously for rapid onset
anesthetics. of anesthesia.
 Beta-Blockers: Exaggerated hypotension.  Subclassification:
 Neuromuscular Blockers: Enhanced muscle relaxation o Barbiturates: Induce rapid unconsciousness by
when used with general anesthetics. potentiating GABA activity.
 Thiopental: Short-acting; used for
induction.
 Methohexital: Ultra-short-acting;
Antidotes for Anesthetics preferred for electroconvulsive therapy
(ECT).
o Propofol: Rapid induction and recovery; causes
 Local Anesthetics Toxicity: Intralipid Emulsion sedation and hypnosis.
(binds and neutralizes the drug). o Ketamine: Dissociative anesthetic preserving
 Benzodiazepine-Induced Sedation: Flumazenil airway reflexes.
(GABA receptor antagonist). o Benzodiazepines: Sedative and anxiolytic
 Opioid Anesthetic Overdose: Naloxone (opioid properties.
receptor antagonist).  Diazepam: Preoperative sedation.
 Lorazepam: Prolonged sedation and
amnesia.
 o Ethyl Alcohol: Historical anesthetic with Max
minimal use today. Drug Type Dosage
Dose/Day
Benzoic
Cocaine 1–3 mg/kg 200 mg
Acid Ester
Para-Amino
Drug Dosage Table for General Anesthetics Procaine 5–8 mg/kg 800 mg
Ester
Para-Amino Topical use (5–20%
Max Benzocaine NA
Drug Type Dosage Ester concentration)
Dose/Day
Halogenated
Halothane 0.5–1% MAC NA
Inhalation Gaseous Anesthetics
Halogenated
Isoflurane 1–2% MAC NA
Inhalation 1. Oxygen
Nitrous 50–70% in
Non-Halogenated NA
Oxide oxygen  Definition: Supports cellular respiration; essential for
Thiopental Barbiturate (IV) 3–5 mg/kg NA life.
2–2.5 mg/kg  Storage: Stored in high-pressure cylinders, dry and cool
Propofol Intravenous NA conditions.
(induction)
Ketamine Dissociative (IV) 1–2 mg/kg NA  Dosage: Delivered at 21–100% concentration, depending
on need.
Benzodiazepine
Diazepam 0.1–0.2 mg/kg 20 mg
(IV)
2. Nitrous Oxide

 Definition: Weak anesthetic with strong analgesic

Classification and Subclassification of Local Anesthetics properties.
 Storage: Stored in liquid form under high pressure.
1. Amides  Dosage: Typically 50–70% in oxygen.

 Definition: Longer acting and metabolized by the liver. 3. Carbon Dioxide

o Lidocaine: Commonly used for infiltration and
nerve blocks.
 Definition: Rarely used in anesthesia; included in
o Prilocaine: Low toxicity, suitable for regional
respiratory mixtures to stimulate breathing.
anesthesia.
o Mepivacaine: Intermediate-acting; used for  Storage: Stored in compressed gas cylinders.
epidural blocks.  Dosage: Delivered at 5–7% concentration mixed with
o Bupivacaine: Long-acting; suitable for labor oxygen.
pain and post-op analgesia.

2. Benzoic Acid Esters

Drug Dosage Table for Gaseous Anesthetics
 Definition: Short-acting and metabolized by plasma
esterases. Gas Purpose Dosage Storage Conditions
o Cocaine: Used for topical anesthesia; 21– High-pressure
vasoconstrictive properties. Oxygen Life support
100% cylinders, dry area
o Fiprocaine: Limited use in modern practice.
Nitrous Liquid form under high
Analgesia 50–70%
Oxide pressure
3. Para-Amino Benzoic Esters
Carbon Respiratory Compressed gas
5–7%
Dioxide stimulant cylinders
 Definition: Older class; associated with higher allergy
rates.
o Procaine: Used for infiltration and nerve
blocks. Antidotes for Anesthetics
o Methocaine: Rarely used; short-acting.
o Benzocaine: Used for topical anesthesia.  Local Anesthetic Toxicity: Intralipid Emulsion (binds
lipid-soluble anesthetics).
 Benzodiazepine Overdose: Flumazenil (GABA
receptor antagonist).
Drug Dosage Table for Local Anesthetics  Opioid-Induced Sedation: Naloxone (opioid receptor
antagonist).
 Inhalation Anesthetic Overdose: Ventilatory support
Max and oxygen administration.
Drug Type Dosage
Dose/Day
3–5 mg/kg (7 mg/kg Definitions
Lidocaine Amide 7 mg/kg
with epinephrine)
Prilocaine Amide 6–8 mg/kg 8 mg/kg Sedatives:
 1. Sedatives are drugs that calm or soothe the central Bind to GABA-A receptor → Increase Cl⁻ channel frequency →
nervous system (CNS) without inducing sleep, though Hyperpolarization → CNS depression.
they may facilitate it in higher doses.
2. They reduce irritability or agitation in the patient by Non-benzodiazepine Hypnotics
depressing CNS activity.
Bind selectively to GABA-A receptor α1 subunit → Induce sleep
Hypnotics: → Minimal anxiolytic effects.

1. Hypnotics are drugs primarily used to induce and Miscellaneous

maintain sleep by depressing the CNS.
2. They are often prescribed to treat insomnia and other
 Chloral Hydrate: Metabolized to trichloroethanol →
sleep disorders by promoting drowsiness.
Enhances GABAergic inhibition → Sedation.
 Glutethimide: Acts on GABA receptor sites → CNS
depression.

Classification of Sedatives and Hypnotics

1. Urea Derivatives Indications and Contraindications (Mnemonic Format)

 Diureates: Using "SEDATIVE" for sedatives:

o Short-acting barbiturates: Rapid onset and
short duration of action.
 S: Sleep induction.
 Examples: Butobarbitone,
Cecobarbitone, Pentobarbitone.  E: Epilepsy.
o Intermediate-acting barbiturates: Moderate  D: Drowsiness (to calm).
onset and duration.  A: Anxiety disorders.
 Examples: Amobarbitone,  T: Tremors.
Butabarbitone.  I: Insomnia.
o Long-acting barbiturates: Slower onset but  V: Ventilation control (in ICU).
prolonged action.  E: Eclampsia.
 Examples: Phenobarbitone,
Mifobarbital. Contraindications: "SEDATIVE" reversed:
o Ultra-short-acting barbiturates: Very rapid
onset with ultra-short duration.
 E: Elderly with respiratory issues.
 Examples: Thiopentone,
 V: Ventilation-impaired conditions.
Hexobarbitone.
 I: Intracranial hypertension.
 T: Toxic hepatic conditions.
2. Benzodiazepines
 A: Alcohol intoxication.
 D: Depression (severe).
 Hypnotics: Used for sleep induction.  E: Epilepsy without proper monitoring.
o Examples: Diazepam, Clonazepam,
Flurazepam.
Using "HYPNOTIC" for hypnotics:
 Anti-anxiety agents: Used to treat anxiety disorders.
o Examples: Diazepam, Chlordiazepoxide,
Lorazepam.  H: Hypnosis induction (for sleep).
 Anticonvulsants: Used for seizure control.  Y: Yawning insomnia (chronic insomnia).
o Examples: Diazepam, Clonazepam, Oxazepam.  P: Preoperative sedation.
 N: Non-organic sleep disorders.
3. Non-benzodiazepine Hypnotics  O: Onset of acute stress.
 T: Temporary insomnia.
 Examples: Zopiclone, Zolpidem.  I: Irritability reduction.
 C: Chronic anxiety with sleep disturbance.
4. Miscellaneous
Contraindications: "HYPNOTIC" reversed:
 Examples: Chloral Hydrate, Glutethimide, Thalidomide.
 C: Chronic respiratory disease.
 I: Insufficient hepatic function.
 T: Toxic CNS depression.
 O: Organic brain syndromes.
Mechanism of Action (Flowchart Format)
 N: Narrow-angle glaucoma.
 P: Pregnancy (category-specific).
Urea Derivatives (Barbiturates)  Y: Youth (children—caution).
 H: Hypersensitivity to drugs.
Enhance GABAergic activity → Prolong Cl⁻ channel opening →
Hyperpolarization of neurons → CNS depression.

Benzodiazepines
Side Effects (Body System-Wise)
1. CNS: Drowsiness, dizziness, headache, sedation, ataxia. Usual
2. Respiratory: Respiratory depression (especially barbiturates). Drug Classification Route
Dose
3. Cardiovascular: Hypotension, bradycardia.
15-30 mg
4. Gastrointestinal: Nausea, vomiting, constipation.
three
5. Musculoskeletal: Weakness, fatigue. Intermediate-acting
Butabarbitone times Oral
6. Skin: Rashes, urticaria. barbiturate
daily or at
bedtime
Adverse Effects
5-10 mg
before
 Dependence and withdrawal symptoms. Benzodiazepine Oral/I
Diazepam bedtime
 Rebound insomnia or anxiety. (Hypnotic/Anxiolytic) V
or as
 Overdose leading to coma or death. needed
1-2 mg at
Benzodiazepine
bedtime
Clonazepam (Hypnotic/Anticonvulsant Oral
or divided
)
Drug Interactions doses
Benzodiazepine 15-30 mg
Flurazepam Oral
 Potentiation with alcohol, opioids, and other CNS (Hypnotic) at bedtime
depressants. 5-25 mg
 Reduced efficacy with enzyme inducers (e.g., rifampicin, Chlordiazepoxid Benzodiazepine (Anti- three
phenytoin). Oral
e anxiety) times
 Altered metabolism when combined with cimetidine or daily
erythromycin. 10-20 mg
two or
Benzodiazepine (Anti-
Chlorazepam three Oral
anxiety)
times
Antidotes daily
10-30 mg
 Benzodiazepines: Flumazenil (competitive antagonist). Oxazepam
Benzodiazepine (Anti- three
Oral
 Barbiturates: alkalinization of urine. anxiety) times
 Others: Symptomatic management daily
3.75-7.5
Non-benzodiazepine
Drug Dosage Table Zopiclone mg at Oral
hypnotic
bedtime
Usual Non-benzodiazepine 5-10 mg
Drug Classification Route Zolpidem Oral
Dose hypnotic at bedtime
50-100 500-1000
Butobarbitone Short-acting barbiturate mg at Oral Chloral Hydrate Miscellaneous (Hypnotic) mg for Oral
bedtime sedation
100-200 250-500
Cicobarbitone Short-acting barbiturate mg at Oral Glutethimide Miscellaneous (Hypnotic) mg at Oral
bedtime bedtime
100 mg at
bedtime Oral/I
Pentobarbitone Short-acting barbiturate
or 2-5 V
mg/kg IV Definitions of Skeletal Muscle Relaxants
30-120
mg/day in Oral/I 1. Skeletal muscle relaxants are drugs that reduce muscle
Phenobarbitone Long-acting barbiturate tone, spasm, or hyperactivity, improving mobility and
divided V
doses reducing discomfort in various musculoskeletal
50-100 conditions.
mg once 2. They work by either depressing the CNS or directly
Mefobarbital Long-acting barbiturate Oral targeting skeletal muscle fibers to relax them.
or twice
daily
Ultra-short-acting Induction:
Thiopentone IV
barbiturate 3-5 mg/kg
100-200 Classification of Skeletal Muscle Relaxants
mg
Ultra-short-acting 1. Centrally Acting Muscle Relaxants
Hexobarbitone (anestheti IV/IM
barbiturate
c
induction)  Act on the central nervous system to inhibit reflexes and
65-200 reduce muscle tone.
Intermediate-acting Oral/I  Examples: Baclofen, Cyclobenzaprine, Carisoprodol,
Amobarbitone mg at
barbiturate V Tizanidine.
bedtime
2. Directly Acting Muscle Relaxants  E: Elderly patients (use caution).
 L: Lethargy or severe CNS depression.
 Act directly on skeletal muscles to interfere with  E: Epilepsy without monitoring (Baclofen).
excitation-contraction coupling.  K: Kidney dysfunction (Tizanidine).
 Example: Dantrolene.  S: Severe hypotension or bradycardia (Tizanidine).

Mechanism of Action Side Effects (Body System-Wise)

Centrally Acting Muscle Relaxants 1. CNS: Drowsiness, dizziness, sedation, headache.

2. Respiratory: Respiratory depression in overdose
1. Baclofen: Activates GABA-B receptors → Inhibits (Carisoprodol).
excitatory neurotransmitter release → Muscle relaxation. 3. Cardiovascular: Hypotension, bradycardia (Tizanidine).
2. Cyclobenzaprine: Reduces tonic somatic motor activity 4. Gastrointestinal: Nausea, constipation, diarrhea.
at brainstem → Decreases muscle hyperactivity. 5. Musculoskeletal: Muscle weakness.
3. Carisoprodol: Modulates interneuronal activity in spinal
cord and reticular formation → CNS depression.
4. Tizanidine: α2-adrenergic receptor agonist → Reduces
presynaptic neurotransmitter release → Muscle Adverse Effects (Body System-Wise)
relaxation.
1. CNS: Confusion, hallucinations, seizures (rare).
Directly Acting Muscle Relaxants 2. Hepatic: Hepatotoxicity (Dantrolene, Tizanidine).
3. Cardiovascular: Severe hypotension (Tizanidine).
1. Dantrolene: Inhibits calcium release from sarcoplasmic 4. Renal: Acute kidney injury (rare with Tizanidine).
reticulum → Prevents muscle contraction.

Drug Interactions
Drug Dosage Table
Drug Interacting Drug Effect of Interaction
Drug Classification Usual Dose Route CNS depressants (e.g., Enhanced CNS
Baclofen
Centrally acting 5-20 mg three alcohol) depression.
Baclofen Oral
muscle relaxant times daily Risk of serotonin
Cyclobenzaprine MAO inhibitors
Centrally acting 10-30 mg daily syndrome.
Cyclobenzaprine Oral
muscle relaxant in divided doses Increased risk of
Benzodiazepines,
Centrally acting 250-350 mg Carisoprodol sedation and
Carisoprodol Oral opioids
muscle relaxant three times daily overdose.
Centrally acting 2-4 mg up to Increased plasma
Tizanidine Oral CYP1A2 inhibitors
muscle relaxant three times daily Tizanidine concentration →
(e.g., ciprofloxacin)
Directly acting 25-100 mg once toxicity.
Dantrolene Oral
muscle relaxant or twice daily Risk of
Calcium channel
Dantrolene cardiovascular
blockers
collapse.
Indications and Contraindications

Mnemonic for Indications: SKELETAL Antidotes

 S: Spasticity from multiple sclerosis or spinal cord 1. Baclofen: in severe overdose, hemodialysis may help.
injuries (Baclofen). 2. Cyclobenzaprine: manage with activated charcoal and
 K: Kinks in muscles (acute muscle spasms - supportive care.
Cyclobenzaprine, Tizanidine). 3. Carisoprodol: Symptomatic treatment; manage CNS
depression with airway support.
 E: Epileptic muscle spasms.
4. Tizanidine: ; atropine may be used for bradycardia.
 L: Lower back pain or strain.
 E: Exertion-related muscle stiffness (Carisoprodol).
 T: Tetanus-related muscle stiffness (Dantrolene). Definitions of Antipsychotic Drugs
 A: Antidote for malignant hyperthermia (Dantrolene).
 L: Long-term spastic conditions like cerebral palsy. 1. Antipsychotic drugs are medications used to manage
psychosis, including disorders like schizophrenia,
bipolar disorder, and severe depression.
Mnemonic for Contraindications: SKELETAL (Reversed)
2. They primarily work by modulating dopamine pathways
in the brain, reducing symptoms like delusions,
 L: Liver dysfunction (Dantrolene, Tizanidine). hallucinations, and disorganized thinking.
 A: Alcohol or drug abuse history (Carisoprodol).
 T: Tachyarrhythmias (Cyclobenzaprine).
Classification of Antipsychotic Drugs  Atypical Antipsychotics: Dopamine and serotonin
receptor modulation; fewer motor side effects.
1. Typical (First-Generation) Antipsychotics (FGAs) o Dibenzodiazepines: Effective for refractory
schizophrenia; requires monitoring (e.g.,
Clozapine).
 Subclassification: Based on chemical structure
o Dibenzothiazepines: Better tolerability for
o Phenothiazines: Dopamine D2 receptor
antagonists. long-term use.
 Examples: Chlorpromazine, o Benzisoxazoles: Effective for both positive and
negative symptoms.
Thioridazine, Fluphenazine.
o Benzothiazoles: Effective for mood and
o Thioxanthenes: Similar to phenothiazines with
cognitive symptoms.
structural differences.
o Dihydroindoles: Limited use due to safety
 Examples: Thiothixene.
o Butyrophenones: Potent D2 antagonists. concerns.
 Examples: Haloperidol, Droperidol.  Mood Stabilizers: Modulate neurotransmitters to
o Diphenylbutylpiperidines: Long-acting D2 stabilize mood swings in bipolar disorder.
receptor antagonists.
 Examples: Pimozide. Here’s a drug dosage table for the drugs you’ve listed:

2. Atypical (Second-Generation) Antipsychotics (SGAs) Drug Classification Usual Dose Route

Thioxanthen Typical Antipsychotic 10-50 mg/day in
Oral
 Subclassification: Based on receptor affinity and e (Thioxanthene) divided doses
structure Benzisoxazo Atypical Antipsychotic
o Dibenzodiazepines: Dual action on dopamine 1-6 mg/day Oral
le (Benzisoxazole)
and serotonin receptors.
Butyrophen Typical Antipsychotic 1-15 mg/day in Oral/I
 Examples: Clozapine, Quetiapine.
one (Butyrophenone) divided doses M
o Dibenzothiazepines: Serotonin-dopamine
antagonists. Dibenzoxaze Atypical Antipsychotic 300-900 mg/day
Oral
 Examples: Olanzapine. pine (Dibenzodiazepine) in divided doses
o Benzisoxazoles: High affinity for serotonin Dihydroindo Atypical Antipsychotic
12-24 mg/day Oral
receptors. le (Dihydroindole)
 Examples: Risperidone, Paliperidone. Dibenzodiaz Atypical Antipsychotic
o Benzothiazoles: Modulate both serotonin and 25-900 mg/day Oral
epine (Dibenzodiazepine)
dopamine.
 Examples: Lurasidone. Typical Antipsychotic
Diphenylbut
o Dihydroindoles: Dopamine and serotonin (Diphenylbutylpiperidi 2-10 mg/day Oral
ylpiperidine
receptor modulation. ne)
 Examples: Sertindole. Thienobenz
Atypical Antipsychotic
(Thienobenzodiazepine 5-20 mg/day Oral
odiazepine
3. Mood Stabilizers )
Dibenzothia Atypical Antipsychotic
10-20 mg/day Oral
 Used for bipolar disorder and mood stabilization. zepine (Dibenzothiazepine)
o Lithium Carbonate: Reduces excitatory Benzothiazo
Atypical Antipsychotic
neurotransmitters and increases GABA. le- 20-120 mg/day Oral
(Benzothiazole)
o Anticonvulsants: Valproic acid, piperazine
Carbamazepine, Lamotrigine, Gabapentin. Phenothiazi Typical Antipsychotic 100-1000 mg/day Oral/I
ne (Phenothiazine) in divided doses M
4. Calcium Channel Blockers Lithium
Carbonate 900-1200 mg/day
Mood Stabilizer Oral
 Used as adjunctive therapy in bipolar disorder. (Eskalith, in divided doses
o Example: Verapamil. Lithane)
Clonazepam Benzodiazepine 0.5-4 mg/day in
Oral
(Klonopin) (Anxiolytic) divided doses
Carbamaze
Anticonvulsant/Mood
One-Line Explanation pine 200-600 mg/day Oral
Stabilizer
(Tegretol)
 Typical Antipsychotics: Primarily D2 receptor Valproic
antagonists; effective for positive symptoms of Acid Anticonvulsant/Mood
10-15 mg/kg/day Oral
schizophrenia. (Depakene; Stabilizer
o Phenothiazines: Reduce psychotic symptoms Depakote)
but cause extrapyramidal side effects. Lamotrigine Anticonvulsant 25-200 mg/day Oral
o Thioxanthenes: Similar efficacy to
900-1800 mg/day
phenothiazines with fewer side effects. Gabapentin Anticonvulsant Oral
in divided doses
o Butyrophenones: High potency; used for acute
psychosis and agitation. Calcium Channel
Verapamil 80-160 mg/day Oral
o Diphenylbutylpiperidines: Long-acting Blocker
antipsychotics for chronic schizophrenia.
Indications and Contraindications (Mnemonic: Genitourinary Effects
ANTIPSYCHOTIC)
 Urinary retention, erectile dysfunction.
Indications
Other Effects
 A: Acute psychosis.
 N: Negative symptoms of schizophrenia (atypicals).  Weight gain, hyperprolactinemia, metabolic syndrome.
 T: Tourette syndrome.
 I: Insomnia in refractory cases.
 P: Positive symptoms of schizophrenia.
 S: Schizoaffective disorders. Drug Interactions
 Y: Youth aggression (severe).
 C: Chronic bipolar disorder.
 H: Hyperactivity (severe cases). Interacting Drug Effect
 O: OCD (adjunctive therapy). CNS depressants (e.g., Increased sedation and respiratory
 T: Treatment-resistant depression (adjunct). alcohol) depression.
 I: Irritability in autism. Increased risk of cognitive
Anticholinergics
 C: Catatonia. impairment.
Lithium with NSAIDs Increased lithium toxicity.
Contraindications QT-prolonging drugs Increased risk of torsades de pointes.
Carbamazepine with SGAs Reduced antipsychotic efficacy.
 A: Alcohol intoxication.
 N: Neuroleptic malignant syndrome history.
 T: Tardive dyskinesia.
Antidotes
 I: Intolerance to antipsychotics.
 P: Parkinson’s disease (typicals worsen symptoms).
1. Antipsychotic Overdose: Symptomatic management;
 S: Severe liver impairment.
activated charcoal for early ingestion.
 Y: Young children (caution).
2. Extrapyramidal Symptoms: Anticholinergics (e.g.,
 C: Cardiac arrhythmias. benztropine, diphenhydramine).
 H: Hypersensitivity to drugs. 3. Neuroleptic Malignant Syndrome: Stop antipsychotics;
 O: Obesity-related metabolic syndrome risk. administer dantrolene or bromocriptine.
 T: Thyroid dysfunction. 4. Lithium Toxicity: Hydration and hemodialysis for
 I: Insufficient renal function (lithium). severe cases.
 C: Coma or severe CNS depression.
Definitions of Antidepressants:

1. Medical Definition: Antidepressants are medications

Adverse Effects (Body System-Wise) prescribed to treat depressive disorders by altering
chemical imbalances of neurotransmitters in the brain.
Extrapyramidal Effects (EPEs) 2. Pharmacological Definition: Antidepressants are a
class of drugs that modulate serotonergic, noradrenergic,
 Definition: Motor side effects due to D2 receptor or dopaminergic pathways to alleviate symptoms of
depression.
blockade in the nigrostriatal pathway.
 Symptoms:
o Acute dystonia (muscle spasms).
o Akathisia (restlessness).
o Parkinsonism (rigidity, bradykinesia). Classification and Subclassification of Antidepressants:
o Tardive dyskinesia (involuntary movements).
1. Monoamine Oxidase Inhibitors (MAOIs):
CNS Effects o Subclassifications: Non-selective MAOIs,
Selective MAO-B inhibitors.
 Sedation, cognitive dulling, seizures (rare). 2. Tricyclic Antidepressants (TCAs):
o Subclassifications: Secondary amines, Tertiary
amines.
Cardiovascular Effects
3. Selective Serotonin Reuptake Inhibitors (SSRIs):
o Subclassifications: None.
 QT prolongation, orthostatic hypotension, tachycardia. 4. Serotonin-Norepinephrine Reuptake Inhibitors
(SNRIs):
Liver Effects o Subclassifications: None.
5. Atypical Antidepressants:
 Elevated liver enzymes, rare hepatotoxicity. o Subclassifications: Noradrenergic and specific
serotonergic antidepressants (NaSSAs),
Dopamine-norepinephrine reuptake inhibitors
Gastrointestinal Effects
(DNRIs).

 Dry mouth, constipation, nausea.

Mechanism of Action in Flowchart Format: Typical Dose
Drug Name Class/Subclass Route
(mg/day)
1. Monoamine Oxidase Inhibitors (MAOIs): MAOI (Non-
Phenelzine sulfate 15-90 Oral
selective)
 Action: Inhibit monoamine oxidase → Decreased Tranylcypromine MAOI (Non-
breakdown of monoamines (serotonin, norepinephrine, 10-60 Oral
sulfate selective)
dopamine) → Increased neurotransmitter availability →
Selegiline MAOI (Selective
Improved mood. 6-12 Oral
(Eldepryl) MAO-B)
Mianserin Atypical (NaSSA) 30-90 Oral
2. Tricyclic Antidepressants (TCAs):
TCA (Tertiary
Amitriptyline 50-300 Oral
amine)
 Action: Block reuptake of serotonin and norepinephrine
→ Increased neurotransmitter levels in synaptic cleft → Mirtazapine Atypical (NaSSA) 15-45 Oral
Enhanced mood. Maprotiline TCA-like 75-150 Oral
TCA (Secondary
Desipramine 25-300 Oral
3. Selective Serotonin Reuptake Inhibitors (SSRIs): amine)
TCA (Tertiary
Imipramine 75-200 Oral
 Action: Selectively inhibit serotonin reuptake → amine)
Increased serotonin concentration in synaptic cleft → TCA (Secondary
Improved emotional state. Nortriptyline 25-150 Oral
amine)
Fluoxetine SSRI 20-80 Oral
4. Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs):
Fluvoxamine SSRI 50-300 Oral
 Action: Block serotonin and norepinephrine reuptake → Paroxetine SSRI 20-50 Oral
Dual increase in neurotransmitter levels → Enhanced Sertraline SSRI 50-200 Oral
mood.

5. Atypical Antidepressants: Indications and Contraindications (Mnemonic:

ANTIDEPRESSANTS):
 NaSSAs: Block alpha-2 receptors → Increased release
of serotonin and norepinephrine.  A: Anxiety disorders.
 DNRIs: Inhibit reuptake of dopamine and  N: Neuropathic pain.
norepinephrine → Enhanced neurotransmitter activity.  T: Tinnitus (off-label).
 I: Insomnia (specific agents).
 D: Depression.
 E: Eating disorders (contraindication for some).
Explanation of Classifications and Subclassifications:  P: Pregnancy (SSRIs preferred).
 R: Risk of suicidal ideation (monitor).
 MAOIs: Used for treatment-resistant depression.  E: Epilepsy (contraindication for bupropion).
o Non-selective: Inhibit both MAO-A and MAO-  S: Serotonin syndrome (caution in combinations).
B (e.g., phenelzine).  S: Stimulant abuse disorders (contraindicated for
o Selective MAO-B inhibitors: Target dopamine MAOIs).
metabolism (e.g., selegiline).
 TCAs: Potent antidepressants targeting serotonin and
norepinephrine.
o Secondary amines: Preferentially increase Adverse Effects (Body System-Wise):
norepinephrine (e.g., desipramine).
o Tertiary amines: More effect on serotonin
 CNS: Sedation, agitation, insomnia, dizziness.
(e.g., amitriptyline).
 Cardiovascular: Orthostatic hypotension, arrhythmias
 SSRIs: Most commonly prescribed for depression due to
(especially TCAs).
fewer side effects.
 GI: Nausea, vomiting, dry mouth, constipation.
 SNRIs: Dual-action antidepressants enhancing serotonin
and norepinephrine.  Endocrine: Weight gain, sexual dysfunction.
 Atypical Antidepressants: Have unique mechanisms or  Hematologic: Rare agranulocytosis (e.g., mirtazapine).
receptor targets, e.g., mirtazapine (NaSSA), bupropion
(DNRI).

Drug Interactions:

Drug Dosage Table: 1. MAOIs + SSRIs → Serotonin syndrome.

2. TCAs + Antihistamines → Enhanced sedation.
3. SSRIs + NSAIDs → Increased bleeding risk.
Typical Dose 4. Bupropion + Alcohol → Seizure risk.
Drug Name Class/Subclass Route
(mg/day) 5. Fluoxetine + Warfarin → Prolonged INR.
MAOI (Non-
Isocarboxazid 20-60 Oral
selective)
Antidote for Toxicity: o Non-selective: Block both beta-1 and beta-2
receptors (e.g., propranolol).
 Supportive Care: Activated charcoal for recent  Antihistamines: Sedating antihistamines reduce anxiety
ingestion. as a secondary effect.
 Specific Antidotes: Cyproheptadine for serotonin o First-generation: Cross BBB for sedation (e.g.,
syndrome, sodium bicarbonate for TCA-induced hydroxyzine).
cardiotoxicity. o Second-generation: Less sedating (less
commonly used).
Definitions of Anxiolytics:

1. Medical Definition: Anxiolytics are medications

designed to alleviate symptoms of anxiety by calming Mechanisms of Action for Each Classification:
the central nervous system.
2. Pharmacological Definition: Anxiolytics are a class of 1. Benzodiazepines:
drugs that target neurotransmitter systems such as
GABA or serotonin to reduce excessive nervousness,  Enhance GABA-A receptor activity → Increased
fear, or worry. chloride ion influx → CNS depression → Anxiolysis.

2. Non-Benzodiazepine Sedative-Hypnotics:

Classification and Subclassification of Anxiolytics:  Bind selectively to GABA-A receptors → Sleep

induction without muscle relaxant effects.
1. Benzodiazepines
o Subclassifications: Short-acting, Intermediate- 3. Buspirone:
acting, Long-acting.
2. Non-Benzodiazepine Sedative-Hypnotics
 Partial agonist at 5-HT1A receptors → Modulates
o Subclassifications: Z-drugs (e.g., zolpidem),
serotonin activity → Reduces anxiety without sedation.
Other sedatives.
3. Buspirone
o Subclassifications: None. 4. Antidepressants (SSRIs/SNRIs):
4. Antidepressants (Used as Anxiolytics)
o Subclassifications: SSRIs, SNRIs.  SSRIs: Inhibit serotonin reuptake → Increased serotonin
5. Beta Blockers levels.
o Subclassifications: Selective, Non-selective.  SNRIs: Inhibit serotonin and norepinephrine reuptake →
6. Antihistamines Dual neurotransmitter elevation.
o Subclassifications: First-generation, Second-
generation. 5. Beta Blockers:

 Block beta-adrenergic receptors → Reduced heart rate,

tremors, and sweating → Symptom-focused anxiety
Explanation of Classification and Subclassification in One relief.
Line:
6. Antihistamines:
 Benzodiazepines: Act as GABA receptor modulators for
rapid anxiety relief.  Block histamine H1 receptors in the brain → Sedation
o Short-acting: Fast onset, shorter duration (e.g., and reduced anxiety.
alprazolam).
o Intermediate-acting: Moderate duration (e.g.,
lorazepam).
o Long-acting: Longer effects, slower clearance
(e.g., diazepam). Drug Dosage Table:
 Non-Benzodiazepine Sedative-Hypnotics: Similar to
benzodiazepines but with fewer side effects. Typical Dose
o Z-drugs: Target GABA-A receptors for sleep Drug Name Class/Subclass Route
(mg/day)
induction (e.g., zolpidem).
Benzodiazepine (Short-
o Other sedatives: Broader CNS depressants. Alprazolam 0.25-4 Oral
acting)
 Buspirone: A partial serotonin receptor agonist for
generalized anxiety. Benzodiazepine
Lorazepam 1-10 Oral/IV
 Antidepressants (Used as Anxiolytics): Act on (Intermediate)
serotonin or norepinephrine for chronic anxiety. Benzodiazepine (Long-
Diazepam 2-40 Oral/IV
o SSRIs: Selectively block serotonin reuptake acting)
(e.g., fluoxetine). Non-benzodiazepine Z-
o SNRIs: Inhibit serotonin and norepinephrine Zolpidem 5-10 Oral
drug
reuptake (e.g., venlafaxine). Buspirone Serotonin agonist 15-60 Oral
 Beta Blockers: Reduce physical anxiety symptoms by
Fluoxetine SSRI 20-80 Oral
blocking adrenergic receptors.
o Selective: Beta-1 selective (e.g., atenolol). Venlafaxine SNRI 37.5-225 Oral
 Typical Dose  Benzodiazepines: Flumazenil (GABA receptor
Drug Name Class/Subclass Route antagonist).
(mg/day)
Beta blocker (Non-  Beta Blockers: Atropine or glucagon for bradycardia.
Propranolol
selective)
10-80 Oral  SSRIs/SNRIs: Cyproheptadine for serotonin syndrome.
Antihistamine (First-
Hydroxyzine 25-100 Oral Definitions of Anticonvulsants:
gen)

1. Medical Definition: Anticonvulsants are drugs that

prevent or reduce the frequency and severity of epileptic
Indications and Contraindications (Mnemonic:
seizures by stabilizing neuronal activity in the brain.
ANXIOLYTICS):
2. Pharmacological Definition: Anticonvulsants are a
class of medications that modulate excitatory and
 A: Acute stress reactions. inhibitory neurotransmission to control abnormal
 N: Non-specific anxiety. electrical activity in the central nervous system.
 X: eXtreme fear (phobias).
 I: Insomnia (secondary use).
 O: Obsessive-compulsive disorder.
 L: Long-term generalized anxiety. Classification and Subclassification of Anticonvulsants:
 Y: Young adults (caution in dosing).
 T: Tremors and physical symptoms of anxiety.
1. Sodium Channel Blockers
 I: Intermittent panic attacks. o Subclassifications: Traditional (e.g., phenytoin),
 C: Chronic post-traumatic stress disorder. Newer generation (e.g., lamotrigine).
 S: Seizures (benzodiazepines). 2. GABA Modulators
o Subclassifications: Benzodiazepines (e.g.,
Contraindications: diazepam), Barbiturates (e.g., primidone).
3. T-Type Calcium Channel Blockers
 A: Addiction history (benzodiazepines). o Subclassifications: Succinimides (e.g.,
 N: Narrow-angle glaucoma. ethosuximide).
 X: Extreme sedation (elderly). 4. AMPA/Kainate Receptor Blockers
o Subclassifications: Topiramate.
 I: Impaired liver or renal function (dose adjustment).
5. Glutamate Modulators
 O: Obstructive sleep apnea (benzodiazepines).
o Subclassifications: Felbamate.
 L: Long-term use without review.
6. Broad-Spectrum Anticonvulsants
 Y: Young children (limited evidence). o Subclassifications: Levetiracetam, Valproate.
 T: Third trimester pregnancy (neonatal withdrawal). 7. Carbonic Anhydrase Inhibitors
 I: Interactions with alcohol or opioids. o Subclassifications: Sulfonamides (e.g.,
 C: CNS depression risk. sulfonamide derivatives).
 S: Severe respiratory depression. 8. Miscellaneous Agents
o Subclassifications: Gabapentin, Tiagabine.

Side Effects and Adverse Effects (Body System-Wise):

Explanation of Classification and Subclassification in One
 CNS: Sedation, dizziness, cognitive impairment, Line:
dependence (benzodiazepines).
 Cardiovascular: Hypotension (beta blockers).  Sodium Channel Blockers: Stabilize neuronal
 Respiratory: Depression (high-dose benzodiazepines). membranes by reducing repetitive firing.
 GI: Nausea, vomiting, constipation (buspirone, SSRIs). o Traditional: Well-established efficacy (e.g.,
 Endocrine: Weight gain (some SSRIs). phenytoin).
 Immune: Rare hypersensitivity reactions. o Newer generation: Fewer side effects (e.g.,
lamotrigine).
 GABA Modulators: Enhance inhibitory
neurotransmission.
o Benzodiazepines: Potentiate GABA-A receptor
Drug Interactions: activity.
o Barbiturates: Prolong GABA-mediated
1. Benzodiazepines + Alcohol → Severe CNS depression. chloride influx.
2. SSRIs + MAOIs → Risk of serotonin syndrome.  T-Type Calcium Channel Blockers: Reduce
3. Beta blockers + Calcium channel blockers → thalamocortical oscillations in absence seizures.
Bradycardia.  AMPA/Kainate Receptor Blockers: Inhibit excitatory
4. Buspirone + CYP3A4 inhibitors (e.g., ketoconazole) glutamate activity.
→ Increased buspirone levels.  Glutamate Modulators: Inhibit glutamatergic
5. Antihistamines + Sedatives → Excessive drowsiness. transmission (e.g., felbamate).
 Broad-Spectrum Anticonvulsants: Multiple
mechanisms targeting seizures of various types.
 Carbonic Anhydrase Inhibitors: Modulate ion balance
Antidote for Toxicity: to reduce neuronal excitability.
  Miscellaneous Agents: Unique mechanisms targeting Typical Dose
specific seizure types. Drug Name Class/Subclass Route
(mg/day)
GABA Modulator
Primidone 250-1000 Oral
(Barbiturate)
GABA Modulator
Mechanism of Action for Each Classification: Clonazepam 0.5-4 Oral
(Benzodiazepine)
GABA Modulator
1. Sodium Channel Blockers: Clorazepate 7.5-60 Oral
(Benzodiazepine)
GABA Modulator
 Block voltage-gated sodium channels → Decrease Diazepam
(Benzodiazepine)
2-40 Oral/IV
repetitive neuronal firing → Stabilize membrane
GABA Modulator
potential. Lorazepam 1-10 Oral/IV
(Benzodiazepine)
T-Type Calcium
2. GABA Modulators: Ethosuximide 500-1500 Oral
Blocker
T-Type Calcium
 Benzodiazepines: Enhance GABA-A receptor activity → Mitosuccimide 300-1200 Oral
Blocker
Increase chloride ion influx → Inhibit neuronal
excitability. Carbonic Anhydrase
Sulfonamide Varies Oral
 Barbiturates: Prolong GABA-A receptor opening → Inhibitor
Potentiate inhibitory signals. Sodium Channel
Carbamazepine 400-1600 Oral
Blocker
3. T-Type Calcium Channel Blockers: Felbamate Glutamate Modulator 1200-3600 Oral
Gabapentin Miscellaneous 900-3600 Oral
 Inhibit T-type calcium currents in thalamic neurons → Sodium Channel
Suppress rhythmic cortical discharges in absence Lamotrigine 100-500 Oral
Blocker
seizures.
Levetiracetam Broad-Spectrum 1000-3000 Oral
Sodium Channel
4. AMPA/Kainate Receptor Blockers: Oxcarbazepine 600-2400 Oral
Blocker
Tiagabine Miscellaneous 4-56 Oral
 Inhibit AMPA/kainate glutamate receptors → Decrease
excitatory neurotransmission. Topiramate AMPA/Kainate Blocker 25-400 Oral

5. Glutamate Modulators:
Indications and Contraindications (Mnemonic:
 Inhibit NMDA or AMPA receptors → Reduce ANTICONVULSANTS):
glutamatergic excitation.
Indications:
6. Broad-Spectrum Anticonvulsants:
 A: Absence seizures.
 Combination of sodium channel blockade, calcium  N: Neuropathic pain.
channel modulation, and GABA potentiation.  T: Tonic-clonic seizures.
 I: Infantile spasms.
7. Carbonic Anhydrase Inhibitors:  C: Complex partial seizures.
 O: Off-label uses (e.g., mood stabilization).
 Inhibit carbonic anhydrase → Alter ion homeostasis →  N: Non-epileptic myoclonus.
Decrease neuronal excitability.  V: Valproate for broad-spectrum needs.
 U: Uncontrolled epilepsy.
8. Miscellaneous Agents:  L: Lennox-Gastaut syndrome.
 S: Status epilepticus.
 A: Anxiety-associated seizures (benzodiazepines).
 Gabapentin: Modulates calcium channels to inhibit
 N: Nocturnal seizures.
neurotransmitter release.
 T: Trigeminal neuralgia (carbamazepine).
 Tiagabine: Inhibits GABA reuptake → Increases GABA
 S: Secondary epilepsy.
availability.

Contraindications:

Drug Dosage Table:  A: Alcohol use disorder.

 N: Narrow-angle glaucoma (benzodiazepines).
 T: Teratogenic risks (valproate).
Typical Dose  I: Impaired hepatic function (carbamazepine).
Drug Name Class/Subclass Route
(mg/day)  C: Cardiac conduction disorders (phenytoin).
Phenytoin
Sodium Channel
200-400 Oral/IV  O: Osteoporosis (long-term use).
Blocker  N: Neutropenia risk (felbamate).
Mifobarbital
GABA Modulator
60-200 Oral  V: Valproate in pregnancy.
(Barbiturate)  U: Uncontrolled hypertension (some agents).
  L: Liver disease. o Mechanism of Action: Levodopa crosses the
 S: Severe respiratory depression (benzodiazepines). blood-brain barrier and is converted to
dopamine, replenishing dopamine levels in the
brain.
2. Peripheral Decarboxylase Inhibitors
o Examples: Carbidopa, Benserazide
Side Effects and Adverse Effects (Body System-Wise): o Mechanism of Action: Inhibit peripheral
conversion of levodopa to dopamine, ensuring
 CNS: Sedation, dizziness, ataxia, cognitive impairment. more levodopa reaches the brain and reducing
 GI: Nausea, vomiting, weight changes. peripheral side effects.
 Hematologic: Aplastic anemia (felbamate), leukopenia 3. Dopamine Agonists
(carbamazepine). o Examples: Bromocriptine, Ropinirole,
 Hepatic: Liver enzyme elevation, hepatotoxicity. Pramipexole, Rotigotine, Apomorphine
 Dermatologic: Rash, Stevens-Johnson syndrome o Mechanism of Action: Mimic dopamine by
(lamotrigine). directly stimulating dopamine receptors in the
 Endocrine: Bone loss with long-term use. brain.
4. MAO-B Inhibitors
o Examples: Selegiline, Rasagiline
o Mechanism of Action: Inhibit monoamine
oxidase-B enzyme, reducing dopamine
Drug Interactions: breakdown and prolonging its action.
5. COMT Inhibitors
1. Phenytoin + Warfarin → Increased bleeding risk (CYP o Examples: Entacapone, Tolcapone
enzyme interaction). o Mechanism of Action: Inhibit catechol-O-
2. Valproate + Lamotrigine → Increased lamotrigine methyltransferase, reducing peripheral levodopa
toxicity (metabolic inhibition). metabolism and enhancing brain dopamine
3. Carbamazepine + Oral Contraceptives → Reduced levels.
contraceptive efficacy (enzyme induction). 6. Dopamine Facilitators
4. Topiramate + Alcohol → Excessive CNS depression. o Examples: Amantadine
5. Benzodiazepines + Opioids → Severe respiratory o Mechanism of Action: Increases dopamine
depression. release, inhibits dopamine reuptake, and has
NMDA receptor antagonist activity.

Antidotes:
II. Drugs Affecting the Brain Cholinergic System
 Benzodiazepines: Flumazenil (GABA antagonist).
 Valproate: L-carnitine for hepatotoxicity. 1. Central Anticholinergics
 Carbamazepine: Hemodialysis in severe overdose. o Examples: Trihexyphenidyl, Procyclidine,
 Barbiturates: Alkalinization of urine to enhance Benztropine, Biperiden
excretion. o Mechanism of Action: Block central
muscarinic receptors to reduce cholinergic
Anti-Parkinson Drugs overactivity, which contributes to tremors and
rigidity.
2. Antihistaminics with Anticholinergic Activity
Anti-Parkinson drugs are medications used to manage the
o Examples: Orphenadrine, Promethazine
symptoms of Parkinson's disease (PD), a progressive
o Mechanism of Action: Exhibit anticholinergic
neurodegenerative disorder primarily affecting movement.
and sedative properties to alleviate Parkinsonian
symptoms.
1. Definition 1: Medications designed to correct the
imbalance between dopamine and acetylcholine in the
brain to alleviate motor symptoms such as tremor,
rigidity, and bradykinesia.
2. Definition 2: A class of drugs aimed at enhancing Drug Dosage Table
dopaminergic activity or reducing cholinergic activity in
the central nervous system. Drug Class Dose Frequency
Dopamine 300-600 3-4 divided
Unique Name for Anti-Parkinson Drugs Levodopa
precursor mg/day doses
Peripheral
"Neuro-Movement Modifiers" (NMMs) 70-100 With
Carbidopa decarboxylase
mg/day levodopa
inhibitor
Dopaminergic 2.5-15
Bromocriptine Twice daily
agonist mg/day
Classification of Anti-Parkinson Drugs Dopaminergic 0.25-24
Ropinirole Once daily
agonist mg/day
I. Drugs Affecting the Brain Dopaminergic System Selegiline MAO-B inhibitor 5-10 mg/day Morning
200 mg with Max 8
1. Dopamine Precursors Entacapone COMT inhibitor
each doses/day
o Examples: Levodopa
 Drug Class Dose Frequency
levodopa
dose Drug Interactions
Dopamine 100-200 1-2 divided
Amantadine 1. Levodopa: Interacts with MAO inhibitors, increasing
facilitator mg/day doses
hypertensive crisis risk.
Central 3-4 divided
Trihexyphenidyl 2-15 mg/day 2. Selegiline: Avoid with SSRIs or TCAs to prevent
anticholinergic doses
serotonin syndrome.
Promethazine Antihistaminic 25-50 mg/day Once daily 3. Amantadine: Potentiates anticholinergic side effects
with central anticholinergics.

Indications and Contraindications (Mnemonic:

ANTIPARKINSON)
Antidotes for Overdose
Indications
 Levodopa: Discontinue and provide symptomatic
A: Akinesia management.
N: Neuroleptic-induced Parkinsonism  Anticholinergics: Use physostigmine for central
T: Tremors anticholinergic syndrome..
I: Idiopathic Parkinson's Disease
P: Postencephalitic Parkinsonism Anti-Alzheimer Drugs
A: Anticipated motor complications
R: Rigidity
Anti-Alzheimer drugs are medications used to manage symptoms
K: Kinetic slowing
of Alzheimer's disease (AD), a neurodegenerative disorder
I: Intolerable bradykinesia
characterized by progressive memory loss, cognitive decline, and
N: Non-motor symptoms in PD
behavioral disturbances.
S: Symptom management
O: Off-periods of motor fluctuations
N: Neuroprotection (hypothetical for MAO-B inhibitors)

Contraindications Classification of Anti-Alzheimer Drugs

A: Angle-closure glaucoma (anticholinergics) I. Cholinesterase Inhibitors

N: Narrow-angle glaucoma
T: Tachyarrhythmias Cholinesterase inhibitors work by increasing acetylcholine levels
I: Intestinal obstruction in the brain, compensating for the loss of cholinergic neurons in
P: Peptic ulcers (dopaminergic drugs) Alzheimer's disease.
A: Active psychosis
R: Recent myocardial infarction  Examples:
K: Kidney dysfunction (Amantadine caution) o Donepezil (D-O-N-E-P-E-Z-I-L)
I: Impulsive behaviors (dopamine agonists) o Rivastigmine
N: Neurotoxic effects (high MAO-B inhibitor doses) o Galantamine
S: Severe hepatic impairment (Tolcapone)  Explanation:
O: Orthostatic hypotension o Acetylcholine is critical for memory and
N: Non-compliance risks learning. By inhibiting the enzyme
acetylcholinesterase, these drugs prevent the
breakdown of acetylcholine, enhancing its
availability at synaptic junctions.
Side Effects and Adverse Effects

Body System-Wise
II. NMDA Receptor Antagonists
1. Central Nervous System:
o Hallucinations, confusion (dopaminergic NMDA receptor antagonists reduce excitotoxicity caused by
agonists) overstimulation of NMDA receptors by glutamate, which is
o Insomnia, anxiety (MAO-B inhibitors) implicated in neuronal damage in AD.
2. Cardiovascular System:
o Orthostatic hypotension (dopamine agonists,  Example:
levodopa) o Memantine (M-E-M-A-N-T-I-N-E)
3. Gastrointestinal System:
 Explanation:
o Nausea, vomiting (levodopa, dopamine
o Glutamate overstimulation can lead to calcium
agonists)
influx and neuronal damage. Memantine
o Diarrhea (COMT inhibitors)
regulates this by blocking excessive NMDA
4. Musculoskeletal System:
receptor activity without disrupting normal
o Dyskinesia (levodopa overuse)
synaptic transmission.
5. Hepatic:
o Hepatotoxicity (Tolcapone)
Drug Dosage Table o Nausea, vomiting, diarrhea (cholinesterase
inhibitors)
3. Cardiovascular System:
Drug Class Dose Frequency
o Bradycardia, hypotension (donepezil,
Cholinesterase rivastigmine)
Donepezil 5-10 mg/day Once daily
inhibitor 4. Respiratory System:
3-12 mg/day
Twice daily o Worsening of asthma or COPD (cholinesterase
Cholinesterase (oral) or 4.6- inhibitors)
Rivastigmine (oral) / Once
inhibitor 13.3 mg/24
daily (patch)
hours (patch)
Cholinesterase
Galantamine 16-24 mg/day Twice daily
inhibitor Drug Interactions
NMDA Once or twice
Memantine 5-20 mg/day
antagonist daily 1. Donepezil, Rivastigmine, Galantamine:
o Avoid anticholinergics (counteract therapeutic
effects).
Mechanism of Action of Each Drug o Increased risk of bradycardia with beta-
blockers.
2. Memantine:
1. Cholinesterase Inhibitors:
o Caution with other NMDA antagonists (e.g.,
o Inhibit acetylcholinesterase enzyme → Increase
amantadine, ketamine).
acetylcholine levels → Improve cognitive
function. o May interact with diuretics, altering drug
clearance.
2. NMDA Antagonists:
o Block excessive NMDA receptor activity →
Reduce excitotoxicity → Protect neurons from
damage.
Antidotes for Overdose

 Cholinesterase Inhibitors:
Indications and Contraindications (Mnemonic: o Atropine for cholinergic crisis.
ALZHEIMER)
Stimulants
Indications
Stimulants are drugs that enhance the activity of the central
A: Alzheimer's disease nervous system (CNS) and/or the cardiovascular system,
L: Late-stage cognitive decline increasing alertness, energy, and physiological functions such as
Z: Zoning out or apathy (addressing non-motor symptoms) heart rate and blood pressure.
H: Hallucinations in AD-related psychosis
E: Early memory loss
I: Impaired learning ability
M: Mild to moderate cognitive impairment Definitions of Stimulants
E: Executive dysfunction
R: Restlessness and irritability
1. Definition 1: Drugs that increase neural or muscular
activity by enhancing the release of excitatory
Contraindications neurotransmitters or inhibiting inhibitory pathways in the
body.
A: Allergy to the drug 2. Definition 2: Medications or substances that heighten
L: Liver dysfunction (dose adjustments for rivastigmine) physical or mental performance by stimulating the
Z: Zollinger-Ellison syndrome (cholinesterase inhibitors may central nervous system or cardiac system.
increase gastric acid secretion)
H: Heart conduction abnormalities (donepezil can prolong QT
interval)
E: Epilepsy (excess acetylcholine may lower seizure threshold)
Mechanism of Action
I: Intestinal obstruction
M: Muscle weakness (e.g., in myasthenia gravis)
E: Exacerbation of asthma or COPD CNS Stimulants
R: Renal impairment (dose adjustments for memantine)
Flowchart:
Stimulus → Activation of dopamine and norepinephrine release
in the synapse → Inhibition of reuptake by presynaptic neurons
→ Increased neurotransmitter levels in the CNS → Enhanced
Side Effects and Adverse Effects (Body System-Wise)
alertness, attention, and mood.
1. Central Nervous System:
Cardiac Stimulants
o Headache, dizziness (memantine)
o Confusion, agitation (dose-dependent in all
classes) Flowchart:
2. Gastrointestinal System: Stimulation of adrenergic receptors (β1 or β2) → Increased
intracellular cyclic AMP (cAMP) → Enhanced calcium influx o Hypertension (CNS and cardiac stimulants)
into cardiac myocytes → Increased force of contraction (positive 3. Gastrointestinal System:
inotropy) and heart rate (positive chronotropy). o Nausea, vomiting, diarrhea (common with
caffeine)
4. Respiratory System:
o Dyspnea (rare but possible with
overstimulation)
Drug Dosage Table
5. Other:
o Dependency and abuse potential
Drug Class Dose Frequency (amphetamines, methylphenidate)
CNS 1-3 divided
Amphetamine 5-40 mg/day
Stimulant doses
CNS 2-3 divided
Methylphenidate 10-60 mg/day
Stimulant doses Drug Interactions
CNS &
100-200 mg as Every 4-6
Caffeine Cardiac 1. CNS Stimulants:
needed hours
Stimulant o Interact with monoamine oxidase inhibitors
2.5-10 (MAOIs), causing hypertensive crises.
Cardiac Continuous o Potentiate the effects of SSRIs and TCAs,
Dobutamine mcg/kg/min
Stimulant infusion increasing serotonin syndrome risk.
(IV)
2. Cardiac Stimulants:
2-20
Cardiac Titrate to o Additive effects with beta-agonists (e.g.,
Dopamine mcg/kg/min
Stimulant response isoproterenol).
(IV) o Antagonized by beta-blockers.

Indications and Contraindications (Mnemonic:

STIMULANTS) Antidotes for Overdose

Indications 1. CNS Stimulants (e.g., amphetamines):

o Administer benzodiazepines for agitation or
S: Shock (e.g., cardiogenic shock for cardiac stimulants) seizures.
T: Tachyphylaxis of low blood pressure o Use acidification of urine (ammonium
I: Inattention disorders (e.g., ADHD for CNS stimulants) chloride) to enhance excretion.
M: Major depressive disorder (adjunct in treatment-resistant 2. Cardiac Stimulants (e.g., dobutamine):
cases) o Discontinue the infusion and administer beta-
U: Unresponsiveness (e.g., caffeine for apnea in neonates) blockers (e.g., propranolol) to counteract
L: Learning disorders (some CNS stimulants) excessive adrenergic activity.
A: Acute heart failure (e.g., dobutamine)
N: Narcolepsy
T: Temporary fatigue or drowsiness Chapter 5
S: Severe hypotension
Drugs Used for Pregnant Women
Contraindications
Drugs used during pregnancy are carefully selected to ensure
S: Seizure disorders (CNS stimulants) maternal and fetal safety, addressing common needs during the
T: Tachyarrhythmias (cardiac stimulants) antenatal, labor, and postnatal periods.
I: Increased intracranial pressure
M: Myocardial infarction (recent)
U: Uncontrolled hypertension
L: Liver dysfunction (dose adjustments)
A: Anxiety or agitation disorders 1. Tetanus Prophylaxis
N: Narrow-angle glaucoma
T: Thyrotoxicosis Definition
S: Stimulant abuse history
Tetanus prophylaxis during pregnancy involves administering
tetanus toxoid (TT) to prevent neonatal and maternal tetanus by
boosting maternal immunity, which passes to the fetus.
Side Effects and Adverse Effects

Body System-Wise
Mechanism of Action (Flowchart)
1. Central Nervous System:
o Anxiety, insomnia, tremors (CNS stimulants) Tetanus Toxoid → Stimulates immune system → Production of
o Agitation, hallucinations (high doses) anti-tetanus antibodies → Passive transfer of antibodies to the
2. Cardiovascular System: fetus → Protection against tetanus.
o Tachycardia, palpitations, arrhythmias (cardiac
stimulants)
Drug Dosage Table Oral/Parenteral Iron → Enters bloodstream → Absorbed in
duodenum → Incorporated into hemoglobin, myoglobin, and
enzymes → Improves oxygen transport and stores iron in tissues.
Drug Dose Timing Frequency
Two doses (1-month
First dose in early
0.5 interval) in first pregnancy.
Tetanus pregnancy, second
mL In subsequent pregnancies,
Toxoid dose at least 4 Drug Dosage Table
IM one booster if last dose
weeks later
given <3 years prior.
Drug Dose Route Frequency
200 mg (60 mg Once or twice
Ferrous Sulfate Oral
Indications and Contraindications elemental iron) daily
Ferrous 300 mg (99 mg
Oral Once daily
Indications (Mnemonic: IMMUNITY) Fumarate elemental iron)
200-1,000 mg Single dose or
I: Immunization against tetanus Ferric
(parenteral iron for IV divided doses
M: Maternal tetanus prevention Carboxymaltose
severe deficiency) over 1-2 weeks
M: Minimized neonatal tetanus risk
U: Universal prophylaxis in pregnancy
N: Non-immunized women during pregnancy
Indications and Contraindications
I: Inadequate prior tetanus immunization
T: Timely vaccination schedule
Y: Young maternal age with no prior vaccinations Indications (Mnemonic: ANEMIA)

Contraindications A: Anemia during pregnancy (Hb < 11 g/dL)

N: Nutritional deficiency of iron
E: Enhanced iron needs in pregnancy
1. Hypersensitivity to tetanus toxoid
M: Malabsorption syndromes (for IV iron)
2. History of severe allergic reactions (e.g., anaphylaxis)
I: Iron stores depleted
A: Antenatal anemia prevention

Contraindications
Side Effects and Adverse Effects (Body System-Wise)
1. Hypersensitivity to iron supplements
1. Local Reaction: 2. Hemochromatosis or other iron overload conditions
o Pain, redness, swelling at the injection site 3. Active gastrointestinal bleeding
2. Systemic Reaction:
o Mild fever, fatigue, headache
o Rare: Anaphylaxis

Side Effects and Adverse Effects (Body System-Wise)

1. Gastrointestinal System:
Drug Interactions
o Nausea, vomiting, constipation, black stools
(common with oral iron)
 No significant drug interactions. Tetanus toxoid can be 2. Allergic Reactions:
co-administered with other vaccines, such as the o Anaphylaxis (rare, associated with IV iron)
diphtheria-pertussis vaccine. 3. Cardiovascular System:
o Hypotension with rapid IV infusion

Antidote
Drug Interactions
 Administer epinephrine in case of anaphylaxis.
 Decreased absorption with antacids, calcium, and dairy
2. Iron Supplementation products.
 Reduced efficacy of tetracyclines and fluoroquinolones
when co-administered.
Definition

Iron supplementation during pregnancy is essential to prevent and

treat iron deficiency anemia, which can lead to maternal and fetal
complications such as preterm delivery and low birth weight. Antidote

 For iron toxicity: Administer deferoxamine (iron-

chelating agent).
Mechanism of Action (Flowchart)
3. Best Iron Supplementation During Pregnancy 1. Local Reaction:
o Pain, swelling at the injection site
Definition 2. Immune System:
o Rare allergic reactions, rash, or anaphylaxis (IV
route)
Combination iron formulations with folic acid and vitamin C are
considered optimal for pregnant women to enhance absorption
and address increased needs.

Drug Dose Frequency Drug Interactions

Ferrous Sulfate + Folic 200 mg iron + 400 mcg
Acid folic acid
Once daily  Reduced efficacy with warfarin (antagonizes its action).
 Enhanced clotting risk when combined with prothrombin
100 mg iron + 500 mg complex concentrates.
Ferrous Ascorbate Once daily
vitamin C

4. Vitamin K1 Supplementation
Antidote
Definition
 For excessive bleeding due to warfarin: Administer
Vitamin K1 supplementation is used to prevent hemorrhagic vitamin K1 (phytonadione) IM/IV.
disease of the newborn by promoting blood clotting through
activation of coagulation factors.

5. Oxytocin
Mechanism of Action (Flowchart)
Definition
Vitamin K1 (Phytonadione) → Activates liver gamma-glutamyl
Oxytocin is a uterotonic agent used to induce labor, augment
carboxylase enzyme → Converts inactive clotting factors II, VII,
uterine contractions, and prevent or treat postpartum hemorrhage.
IX, X to active forms → Improves coagulation → Prevents
bleeding.

Mechanism of Action (Flowchart)

Drug Dosage Table
Oxytocin → Binds to oxytocin receptors on uterine myometrium
→ Increases intracellular calcium → Stimulates uterine
Drug Dose Route Frequency contractions → Facilitates labor and reduces postpartum bleeding.
Vitamin K1 1 mg IM (newborns) Single dose at birth
10-20 mg/day Oral (maternal) Daily (if deficient)

Drug Dosage Table

Indications and Contraindications
Indication Dose Route Frequency
Indications (Mnemonic: K-CLOTTING) IV Increase by 1-2 mU
Labor induction 0.5-2 mU/min
infusion every 15-30 mins
K: K deficiency bleeding (prevention in neonates) Postpartum 10-20 units in IV
C: Coagulopathy correction in pregnant women Continuous infusion
hemorrhage 500 mL NS/LR infusion
L: Low intake of vitamin K during pregnancy
10 units IM Single dose
O: Obstetric hemorrhage risk
T: Trauma-induced bleeding
T: Thrombocytopenia with bleeding
I: Infant prophylaxis at birth Indications and Contraindications
N: Neonatal jaundice risk reduced (controversial, but bleeding
prevention outweighs risk) Indications (Mnemonic: UTERINE)
G: General maternal deficiency
U: Uterine atony prevention or treatment
Contraindications T: Term labor induction or augmentation
E: Elective induction for medical reasons
1. Hypersensitivity to vitamin K1 R: Retained placenta expulsion aid
2. Use with caution in conditions like G6PD deficiency I: Incomplete miscarriage management
(risk of hemolysis with high doses) N: Non-progressive labor (dysfunctional labor)
E: Emergency postpartum hemorrhage

Contraindications
Side Effects and Adverse Effects (Body System-Wise)
 1. Fetal distress or malpresentation Indications (Mnemonic: CONTRACTION)
2. Previous uterine rupture or major surgery
3. Hypertonic uterine contractions C: Cervical ripening for labor induction
4. Placenta previa or vasa previa O: Obstetric hemorrhage (PPH)
N: Non-progressive labor (second-line after oxytocin)
T: Termination of pregnancy (first or second trimester)
R: Retained placenta expulsion
Side Effects and Adverse Effects (Body System-Wise) A: Augmentation of uterine contractions
C: Cervical priming before surgical abortion
T: Treatment of incomplete abortion
1. Uterine:
I: Intrauterine fetal demise (induction)
o Hyperstimulation, rupture (rare)
2. Cardiovascular System: O: Obstetric emergencies for uterine atony
N: Non-surgical uterine evacuation
o Hypotension, tachycardia
3. Fetal Effects:
o Bradycardia or distress due to uterine Contraindications
hyperstimulation
1. Hypersensitivity to prostaglandins
2. Uterine rupture risk (e.g., prior uterine surgery)
3. Active fetal distress in labor
Drug Interactions

 Enhanced effects with prostaglandins (e.g., misoprostol).

 Antagonized by beta-adrenergic tocolytics (e.g., Side Effects and Adverse Effects (Body System-Wise)
terbutaline).
1. Uterine:
o Hyperstimulation, rupture (rare in high doses)
2. Gastrointestinal System:
o Nausea, vomiting, diarrhea
Antidote 3. Cardiovascular System:
o Fever, chills, flushing
 For hyperstimulation: Discontinue oxytocin and
administer tocolytics (e.g., terbutaline).

6. Misoprostol Drug Interactions

Definition  Additive effects with oxytocin (risk of uterine rupture).

 Reduced efficacy with NSAIDs due to prostaglandin
Misoprostol is a synthetic prostaglandin E1 (PGE1) analog used inhibition.
to induce labor, manage postpartum hemorrhage (PPH), and treat
incomplete or missed abortions.

Antidote
Mechanism of Action (Flowchart)
 For hyperstimulation: Discontinue misoprostol and
administer a tocolytic (e.g., terbutaline).
Misoprostol → Activates prostaglandin E1 receptors in uterine
myometrium → Increases intracellular calcium → Stimulates
uterine contractions → Facilitates cervical ripening and bleeding
control.
7. Ergometrine

Definition
Drug Dosage Table
Ergometrine is an ergot alkaloid that induces strong, sustained
uterine contractions, primarily used in the management of
Indication Dose Route Frequency postpartum hemorrhage and uterine atony.
Labor induction 25 mcg Vaginal/oral Every 4-6 hours
Postpartum 600-
hemorrhage 800 Sublingual/oral Single dose
(PPH) mcg Mechanism of Action (Flowchart)
400- Single dose or
Incomplete
800 Vaginal/oral repeat after 24 Ergometrine → Binds to alpha-adrenergic and serotonin
miscarriage
mcg hours receptors in uterine smooth muscle → Increases intracellular
calcium → Induces tonic uterine contractions → Reduces
bleeding.
Indications and Contraindications
Drug Dosage Table Mechanism of Action (Flowchart)

Indication Dose Route Frequency Methyl Prostaglandin F2-alpha → Binds to prostaglandin F2-
alpha receptors on uterine smooth muscle → Increases
Postpartum 0.2 Single dose, may repeat
IM intracellular calcium → Stimulates uterine contractions →
hemorrhage (PPH) mg after 2-4 hours
Reduces postpartum bleeding or facilitates pregnancy
0.2 IV termination.
Uterine atony Single dose
mg (slow)

Indications and Contraindications Drug Dosage Table

Indications (Mnemonic: HEMORRHAGE)

Indication Dose Route Frequency
Postpartum 250 Every 15-90 minutes
H: Hemorrhage prevention postpartum IM
hemorrhage (PPH) mcg (max 2 mg)
E: Emergency uterine atony management
M: Management of excessive bleeding post-abortion Termination of 250 Repeat every 1.5-3.5
IM
O: Obstetric surgeries with high hemorrhage risk pregnancy mcg hours as needed
R: Retained placenta expulsion (in some cases)
R: Rapid control of postpartum bleeding
H: Hypotonic uterus causing blood loss Indications and Contraindications
A: Augmentation of uterine tone postpartum
G: General uterine atony or atonic PPH
Indications (Mnemonic: BLEED)
E: Emergency uterine evacuation support
B: Bleeding postpartum (PPH due to uterine atony)
Contraindications L: Late second-trimester pregnancy termination
E: Emergency PPH not responsive to first-line agents
1. Hypertension or pre-eclampsia E: Evacuation of retained products of conception
2. Severe cardiac disease D: Dysfunctional uterine atony in high-risk cases
3. Hypersensitivity to ergot alkaloids
Contraindications

1. Hypersensitivity to prostaglandins
Side Effects and Adverse Effects (Body System-Wise) 2. Severe cardiac, hepatic, or renal disease
3. Active pelvic infection
1. Cardiovascular System: 4. Asthma (bronchospasm risk)
o Hypertension, coronary vasospasm
2. Gastrointestinal System:
o Nausea, vomiting
3. Uterine:
Side Effects and Adverse Effects (Body System-Wise)
o Excessive contractions, risk of rupture
1. Gastrointestinal System:
o Nausea, vomiting, diarrhea
2. Respiratory System:
Drug Interactions o Bronchospasm, dyspnea (in asthmatics)
3. Cardiovascular System:
 Enhanced vasoconstriction with sympathomimetics (e.g., o Hypertension, flushing
epinephrine). 4. Uterine:
 Risk of hypertension with oxytocin co-administration. o Hypertonic uterine contractions

Antidote Drug Interactions

For ergot toxicity: Administer nitroprusside or phentolamine  Additive effects with oxytocin (risk of uterine
(alpha-adrenergic blocker) f8. Methyl Prostaglandin F2-alpha hyperstimulation).
(Carboprost)  Antagonized by NSAIDs (prostaglandin synthesis
inhibitors).
Definition

Methyl prostaglandin F2-alpha (Carboprost) is a synthetic

prostaglandin analog used for the management of postpartum Antidote
hemorrhage (PPH) and the termination of pregnancy.
 For bronchospasm: Administer a beta-agonist (e.g.,
salbutamol).
 For hypertension: Use antihypertensives as appropriate.
9. Magnesium Sulfate Antidote

Definition  For magnesium toxicity: Administer calcium gluconate

(1 g IV slowly).
Magnesium sulfate is a tocolytic and anticonvulsant drug used to
prevent and treat eclampsia and manage preterm labor. 10. Calcium Gluconate

Definition

Mechanism of Action (Flowchart) Calcium gluconate is a calcium supplement used as an antidote

for magnesium sulfate toxicity and to treat hypocalcemia.
Magnesium Sulfate → Competes with calcium at voltage-gated
channels → Reduces intracellular calcium in smooth muscle →
Relaxes uterine smooth muscle (tocolysis) and decreases CNS
excitability (anticonvulsant effect). Mechanism of Action (Flowchart)

Calcium Gluconate → Increases extracellular calcium →

Enhances calcium influx into cells → Counters magnesium’s
Drug Dosage Table inhibitory effects on neuromuscular and cardiac conduction →
Restores muscle and cardiac function.
Maintenance
Indication Loading Dose Route
Dose
Eclampsia (seizure 4-6 g over 15- IV
1-2 g/hour Drug Dosage Table
prevention) 20 min infusion
Preterm labor 4-6 g over 15- IV
1-2 g/hour
(tocolysis) 20 min infusion Indication Dose Route Frequency
Magnesium 1 g (10 mL of IV As needed, over
toxicity antidote 10% solution) (slow) 5-10 minutes
Indications and Contraindications IV or Divided doses as
Hypocalcemia 1-2 g/day
Oral needed
Indications (Mnemonic: CALM)

C: Control of seizures in eclampsia/preeclampsia Indications and Contraindications

A: Anticonvulsant in obstetric emergencies
L: Labor delay in preterm cases (tocolysis) Indications (Mnemonic: CALCIUM)
M: Management of severe hypertension-related seizures
C: Counteracts magnesium toxicity
Contraindications A: Acute hypocalcemia treatment
L: Low calcium disorders (e.g., hypoparathyroidism)
1. Myasthenia gravis (risk of muscle weakness) C: Cardiac arrest with hypocalcemia or hypermagnesemia
2. Severe renal impairment I: Ionized calcium replenishment in critical care
3. Hypocalcemia U: Uterine contractility dysfunction due to magnesium overdose
4. Heart block M: Muscle weakness (calcium-related)

Contraindications

Side Effects and Adverse Effects (Body System-Wise) 1. Hypercalcemia

2. Digitalis toxicity (risk of arrhythmias)
1. CNS: 3. Severe ventricular fibrillation
o Drowsiness, dizziness
2. Respiratory System:
o Respiratory depression (with overdose)
3. Cardiovascular System: Side Effects and Adverse Effects (Body System-Wise)
o Hypotension, bradycardia
4. Musculoskeletal System:
1. Cardiovascular System:
o Weakness, decreased reflexes
o Hypotension, bradycardia (if infused too
quickly)
2. Gastrointestinal System:
o Nausea, constipation (oral forms)
Drug Interactions 3. Musculoskeletal System:
o Muscle rigidity (rare with rapid infusion)
 Additive CNS depression with sedatives or opioids.
 Potentiated hypotensive effects with antihypertensives.
Drug Interactions Indicati
Drug Class Drug Dose Route
on
 Precipitation occurs when mixed with ceftriaxone. 0.2
 Risk of severe arrhythmias with digitalis glycosides. mg
PPH,
Ergot IM
Ergometrine uterine IM or IV
Alkaloids (max
atony
3
Antidote doses)
0.2
 Overdose or hypercalcemia: Administer loop diuretics Postpart mg
and adequate hydration. Methylergome um IM/IV
IM or IV
trine hemorrh (singl
age e
dose)

Uterine Stimulants (Oxytocics)

Brief Explanation of Each Subclassification
Definition
1. Oxytocin and Its Analogs: Stimulate rhythmic uterine
Uterine stimulants are drugs that enhance uterine contractions for contractions to facilitate labor and reduce bleeding
labor induction, postpartum hemorrhage control, and pregnancy postpartum.
termination. 2. Prostaglandins: Ripen the cervix, induce uterine
contractions, and manage uterine atony in hemorrhage.
3. Ergot Alkaloids: Cause strong, tonic uterine
contractions to reduce postpartum bleeding.
Classification and Subclassification 4. SPRMs: Induce abortion or labor by blocking
progesterone support for pregnancy.
1. Oxytocin and Its Analogs 5. Beta-2 Sympathomimetics: Rarely used to augment
o E.g., Oxytocin: Stimulates uterine smooth uterine contractility.
muscle contractions.
2. Prostaglandins
o E.g., Misoprostol, Dinoprostone: Induce labor
and manage postpartum hemorrhage. Indications (Mnemonic: UTERINE)
3. Ergot Alkaloids
o E.g., Ergometrine, Methylergometrine: Cause U: Uterine atony (postpartum hemorrhage)
tonic uterine contractions to prevent or treat T: Termination of pregnancy (induction of abortion)
postpartum hemorrhage. E: Evacuation of retained products (missed abortion or
4. Selective Progesterone Receptor Modulators incomplete miscarriage)
(SPRMs) R: Ripening of cervix for labor induction
o E.g., Mifepristone: Induces abortion by I: Induction of labor (preterm rupture or medical indication)
blocking progesterone. N: Non-progressive labor (augmentation of uterine contractions)
5. Beta-2 Sympathomimetics (Reverse Action) E: Emergency control of bleeding in postpartum hemorrhage
o Rarely used to enhance uterine tone.

Contraindications (Mnemonic: UTERINE)

Drug Dosage Table for Uterine Stimulants
U: Uterine rupture risk (previous C-section or uterine surgery)
Indicati T: Tachysystole or fetal distress (hyperstimulation risk)
Drug Class Drug Dose Route
on E: Ectopic pregnancy (contraindicated in prostaglandins and
0.5-2 oxytocin)
Labor mU/m R: Renal or liver dysfunction (ergot alkaloids contraindicated)
Oxytocin Oxytocin inductio in IV IV or IM I: Infection in pelvic area (prostaglandins contraindicated)
n, PPH infusi N: Non-vertex presentation (breech or transverse)
on E: Extreme hypertension or pre-eclampsia (ergot alkaloids
10 contraindicated)
Postpart
units
um
IM/IV IM or IV
hemorrh
infusi
age
on Side Effects and Adverse Effects (Body System-Wise)
Labor 25-
Prostaglan Vaginal/Oral/Subli
Misoprostol inductio 800 1. Central Nervous System (CNS):
dins ngual
n, PPH mcg o Headache, dizziness, agitation (ergot alkaloids)
10 mg o Fever (prostaglandins like misoprostol)
Cervical vagin 2. Cardiovascular System:
Dinoprostone Vaginal o Hypertension, tachycardia (ergot alkaloids,
ripening al
insert oxytocin overdose)
 o Hypotension, flushing (oxytocin infusion) o Estradiol (E2)
3. Gastrointestinal System: o Estrone (E1)
o Nausea, vomiting, diarrhea (common with o Estriol (E3)
prostaglandins) 2. Synthetic Oestrogens
4. Respiratory System: o Steroidal Synthetic Estrogens
o Bronchospasm (prostaglandins in asthmatic  Ethinyl Estradiol
patients)  Mestranol
5. Reproductive System: o Non-Steroidal Synthetic Estrogens
o Hypertonic uterine contractions, uterine rupture  Diethylstilbestrol (DES)
(oxytocin or prostaglandin overdose)  Dienestrol
6. Other:  Hexestrol
o Chills, shivering, and transient fever 3. Conjugated Oestrogens
(misoprostol) o Premarin
o Synthetic Conjugates
4. Selective Estrogen Receptor Modulators (SERMs)
o Raloxifene
o Tamoxifen
Drug Interactions

1. Oxytocin:
o Additive effects with prostaglandins, increasing
risk of uterine hyperstimulation and rupture. Mechanism of Action Flowchart
o Interaction with anesthetic agents may reduce
uterine contractility. 1. Natural Estrogens
2. Prostaglandins:
o Antagonized by NSAIDs (e.g., ibuprofen).  Estradiol, Estrone, Estriol
o Additive effects with oxytocin or ergometrine, o Bind estrogen receptors (ERα and ERβ) →
leading to hyperstimulation. Hormone-receptor complex → Translocates to
3. Ergot Alkaloids: nucleus → Modulates gene transcription →
o Potentiated by vasopressors or beta-blockers Physiological effects (menstrual cycle,
(exacerbates hypertension). secondary sexual characteristics).
o Interaction with nitrates may lead to excessive
vasodilation and hypotension.
2. Synthetic Estrogens

 Steroidal (Ethinyl Estradiol, Mestranol)

o Same as natural estrogens but have higher
Antidotes for Uterine Stimulant Toxicity potency due to slower metabolism.
 Non-Steroidal (Diethylstilbestrol, Dienestrol,
1. Oxytocin Overdose: Hexestrol)
o Discontinue oxytocin infusion. o Mimic estradiol → Bind ERs → Activate
o Administer tocolytics like terbutaline or transcription pathways → Elicit estrogenic
magnesium sulfate to counter effects.
hyperstimulation.
2. Prostaglandin Overdose: 3. Conjugated Estrogens
o Discontinue prostaglandin administration.
o Treat bronchospasm with beta-agonists (e.g.,
salbutamol).  Premarin, Synthetic Conjugates
o Manage hyperstimulation with tocolytics. o Hydrolyzed to active estrogens → Act on ERs
3. Ergot Alkaloid Toxicity: → Target reproductive and bone health.
o For hypertensive crisis: Use alpha-adrenergic
blockers (e.g., phentolamine). 4. SERMs
o For peripheral vasospasm: Administer
nitroprusside or nitroglycerin.  Raloxifene, Tamoxifen
o Agonist at bone/liver; antagonist in breast tissue
Oestrogen → Modulate estrogen activity selectively.

Introduction

Oestrogen is a group of steroid hormones critical for the Dosage Table

development and regulation of the female reproductive system
and secondary sexual characteristics. They are used in drugs to Drug Name Dosage Route
treat hormonal disorders, menopausal symptoms, contraception,
and osteoporosis prevention. Estradiol 1–2 mg daily Oral, patch
Conjugated Estrogens 0.3–1.25 mg daily Oral, IV
50 µg (as in combined
Mestranol Oral
OCP)
Classification of Oestrogens Estriol 0.5–2 mg daily Oral, topical
Dienestrol 0.01% cream Vaginal
1. Natural Oestrogens
 Drug Name Dosage Route Introduction
Oestrogel 2.5 g gel daily Transdermal
Progesterone is a steroid hormone essential for the menstrual
Estetrol 15–20 mg daily Oral
cycle, implantation, and pregnancy maintenance. Used
Estramustine therapeutically for contraception, hormone replacement, and
140–280 mg daily Oral
Phosphate gynecological disorders.
Polyestradiol
40 mg IM every 2–4 weeks IM
Phosphate
Hexestrol 1 mg daily Oral
Classification of Progestins

Indications and Mnemonic 1. Natural Progesterone

o Progesterone
Mnemonic: OESTROGEN 2. Synthetic Progestins
o First-Generation: Norethindrone, Ethynodiol
o Second-Generation: Levonorgestrel,
 Osteoporosis
Norgestrel
 Estrogen deficiency (menopause) o Third-Generation: Desogestrel, Dienogest
 Secondary hypogonadism o Fourth-Generation: Drospirenone
 Tumors (breast cancer adjunct therapy) 3. Antiprogestins
 Reproductive health (IVF support) o Mifepristone
 Oral contraceptives o Ulipristal
 Gynecomastia
 Endometrial atrophy
 Neuroprotection
Mechanism of Action Flowchart

1. Natural Progesterone
Side Effects
 Binds progesterone receptor (PR) → Hormone-receptor
System-Wise complex → Translocates to nucleus → Modulates gene
transcription → Maintains endometrium, inhibits LH
1. Cardiovascular surge.
o Increased risk of thromboembolism, stroke.
2. Reproductive 2. Synthetic Progestins
o Endometrial hyperplasia, breast tenderness.
3. Gastrointestinal
 Same as natural but more receptor specificity and
o Nausea, abdominal cramps.
potency.
4. Neurological
o Headaches, mood swings.
5. Others 3. Antiprogestins
o Weight gain, fluid retention.
 Bind PR but do not activate it → Block progesterone
action → Endometrial shedding or ovulation
suppression.
Drug Interactions

 Increased effects with: CYP450 inhibitors (e.g.,

grapefruit juice). Dosage Table
 Decreased effects with: CYP450 inducers (e.g.,
rifampin, carbamazepine). Drug Name Dosage Route
 Interaction with anticoagulants: Reduces anticoagulant Medroxyprogesterone Acetate 150 mg every 3 months IM
efficacy.
Megestrol Acetate 40–320 mg daily Oral
Norethindrone 0.35 mg daily Oral
Levonorgestrel 1.5 mg single dose Oral
Antidote for Oestrogen Overdose Desogestrel 0.15 mg daily Oral
Drospirenone 3 mg daily Oral
 Supportive care.
 Activated charcoal for recent ingestion.
 Symptom management (e.g., antiemetics, IV fluids). Indications and Mnemonic

Mnemonic: PROGESTIN

Progesterone  Pregnancy support

 Regulation of menstrual cycles
  Ovarian suppression (endometriosis)
 Gynecological cancers (adjunct)
 Emergency contraception Dosage Table
 Supportive therapy (HRT)
 Threatened miscarriage Drug Name Dosage Route
 In vitro fertilization support
Mifepristone 200 mg single dose (abortion) Oral
 Non-hormonal uses (appetite stimulation).
Ulipristal 30 mg single dose (emergency
Oral
Acetate contraception)

Side Effects
Indications and Mnemonic
1. Metabolic: Weight gain, glucose intolerance.
2. Reproductive: Breakthrough bleeding, amenorrhea. Mnemonic: ANTIPROGESTIN
3. Psychological: Mood changes, depression.
4. Cardiovascular: Thromboembolism (rare).  Abortion (medical termination of pregnancy).
 Neoplastic conditions (progesterone-sensitive tumors).
 Third-trimester induction (intrauterine fetal death).
 Infertility treatments (controlled ovarian stimulation).
Drug Interactions  Post-coital contraception.
 Reproductive health (fibroids).
 Enhanced metabolism with CYP450 inducers.  Ovarian suppression (endometriosis).
 May decrease efficacy of antiepileptics, anticoagulants.  Gynecological bleeding disorders.
 Endometrial thinning.
 Surgical preparation (cervical ripening).
Antiprogestins
 Tubal ectopic pregnancy adjunct (limited use).
 Incomplete abortion (management).
Introduction
 Non-hormonal use (investigational).
Antiprogestins are a class of drugs that block the effects of
progesterone by inhibiting its binding to the progesterone receptor
(PR). They are used for medical abortion, emergency
contraception, and treatment of specific gynecological conditions Side Effects and Adverse Effects
like endometriosis and uterine fibroids.
1. Reproductive System
o Vaginal bleeding, uterine cramps.
2. Gastrointestinal
o Nausea, vomiting, diarrhea.
Classification of Antiprogestins
3. Neurological
o Dizziness, headache.
1. Competitive Progesterone Receptor Antagonists 4. Systemic
o Mifepristone (RU-486) o Fatigue, fever.
o Ulipristal Acetate
2. Selective Progesterone Receptor Modulators
(SPRMs)
o Ulipristal Acetate (dual agonist-antagonist
activity). Drug Interactions

1. Mifepristone
o Increased effects with: CYP3A4 inhibitors
(e.g., ketoconazole).
Mechanism of Action Flowchart
o Decreased effects with: CYP3A4 inducers
(e.g., rifampin, phenytoin).
1. Competitive PR Antagonists o Anticoagulants may increase bleeding risk.
2. Ulipristal Acetate
 Mifepristone o Reduced efficacy with hormonal
o Binds to PR → Blocks progesterone action → contraceptives.
Endometrial degeneration → Decidual necrosis o Interaction with CYP3A4-modulating drugs.
→ Myometrial contraction → Cervical
softening → Pregnancy termination. Oral Contraceptives (OCs)

2. Selective PR Modulators (SPRMs) Definitions of Oral Contraceptives

 Ulipristal Acetate 1. General Definition: Oral contraceptives are medications

o Partial agonist-antagonist at PR → Inhibits taken orally to prevent pregnancy by inhibiting
ovulation (delays follicular rupture) → Alters ovulation, altering the endometrium, or affecting sperm
endometrial receptivity → Emergency motility and penetration.
contraception.
 2. Pharmacological Definition: Oral contraceptives are
drugs containing hormones (estrogens and/or progestins)
or non-hormonal agents that modulate the hypothalamic- Indications and Contraindications (Mnemonic:
pituitary-ovarian axis or cervical mucus to prevent CONTRACEPTIVE)
fertilization and implantation.
Indications

 Control of pregnancy (prevention).

Types of Oral Contraceptives  Ovarian cyst prevention.
 Normalization of menstrual cycles.
1. Hormonal Contraceptives  Treatment of endometriosis.
 Regulation of hormonal acne.
1. Combined Hormonal Contraceptives (CHCs)  Amenorrhea secondary to hormonal imbalances.
o Contain both estrogen (ethinyl estradiol) and  Conditions like PCOS.
progestin (e.g., norethindrone).  Emergency contraception.
o Prevent ovulation by suppressing follicle-  Premenstrual syndrome (PMS) management.
stimulating hormone (FSH) and luteinizing  Treatment of anemia (reduces menstrual blood loss).
hormone (LH).
 IVF adjunct.
o Subclassifications:
 Vaginal bleeding irregularities.
 Monophasic Birth Control Pills
 Fixed doses of estrogen and  Extra protection for lactating women (mini-pill).
progestin in each active pill.
 Further classification: Contraindications
 Low-dose pills: ≤20
µg ethinyl estradiol.  Cardiovascular disorders (DVT, stroke).
 Regular-dose pills:  Older age (≥35 years) + smoking.
21–35 µg ethinyl  Neurological disorders (migraines with aura).
estradiol.  Thromboembolic conditions.
 High-dose pills: ≥50  Renal or liver impairment.
µg ethinyl estradiol.  Altered lipid metabolism.
 Biphasic Birth Control Pills
 Current pregnancy.
 Two different doses of
 Endometrial/breast cancer.
hormones to mimic natural
cycle variations.  Physical immobility (post-surgery).
 Triphasic Birth Control Pills  Tumor of the liver.
 Three varying doses of  Idiopathic vaginal bleeding.
hormones across the cycle.  Vascular complications of diabetes.
2. Progestin-Only Contraceptives (Mini-Pills)  Elevated blood pressure.
o Contain only progestins (e.g., norethindrone,
desogestrel).
o Thicken cervical mucus and inhibit sperm
penetration. Side Effects (System-Wise)
3. Post-Coital Pills (Emergency Contraceptives)
o High-dose pills taken after unprotected
1. Cardiovascular: Thromboembolism, hypertension.
intercourse to prevent pregnancy.
2. Reproductive: Breakthrough bleeding, amenorrhea.
o Examples: Levonorgestrel, Ulipristal acetate.
3. Gastrointestinal: Nausea, abdominal cramps.
4. Neurological: Headache, mood changes.
5. Dermatological: Acne, skin darkening.

2. Non-Hormonal Contraceptives

 Centchroman (Ormeloxifene) Drug Interactions

o Selective estrogen receptor modulator (SERM).
o Works by delaying ovulation and implantation.
 CYP450 inducers (e.g., rifampin, phenytoin) reduce
efficacy.
 Antibiotics (e.g., rifampin) alter gut flora and hormone
absorption.
Drug Dosage Table  Anticoagulants: Decreased efficacy.

Type Drug Name Dosage Route Antidote for Overdose

Ethinyl estradiol + 30 µg + 150 µg
Combined Pills Oral
Norgestrel daily  Supportive care.
Mini-Pills Norethindrone 0.35 mg daily Oral  Symptomatic management for nausea or vomiting.
1.5 mg single
Post-Coital Pills Levonorgestrel Oral
dose
Non-Hormonal 30 mg twice
Centchroman Oral Hormone Replacement Therapy (HRT)
Pills weekly
Definitions of HRT  Mood stabilization.
 Enhanced quality of life.
1. General Definition: HRT is the therapeutic  Normalization of urogenital atrophy.
administration of hormones (estrogens, progestins, or  Treatment of vaginal dryness.
both) to alleviate symptoms associated with hormonal
deficiencies, particularly in menopause. Contraindications
2. Pharmacological Definition: HRT involves the
replacement of endogenous hormones to mimic
 Recent DVT or PE.
physiological levels and functions for managing
menopausal or surgical-induced hormone insufficiencies.  Estrogen-sensitive cancers.
 Pregnancy.
 Liver disease.
 Abnormal uterine bleeding (unexplained).
 Coronary artery disease.
Classification of HRT
 Endometrial hyperplasia.
 Migraine with aura.
1. Estrogen Replacement Therapy (ERT)  Elevated blood pressure.
o Natural Estrogens: Estradiol, estriol.
 Neurological conditions (stroke risk).
o Conjugated Estrogens: Premarin.
 Thromboembolic disorders.
2. Combined Estrogen-Progestin Therapy (EPT)
o Sequential therapy (progestin added
intermittently).
o Continuous therapy (progestin given daily).
3. Androgen Replacement Therapy Side Effects (System-Wise)
o For specific androgen deficiencies in women.
1. Cardiovascular: Thrombosis, stroke.
2. Reproductive: Endometrial hyperplasia, breast
tenderness.
Mechanism of Action Flowchart 3. Neurological: Headaches, mood swings.
4. Gastrointestinal: Nausea, bloating.
1. Estrogen Replacement Therapy

 Binds estrogen receptors (ER) → Modulates gene

transcription → Alleviates menopausal symptoms, Drug Interactions
maintains bone density.
 CYP450 inhibitors/inducers affect hormone
2. Combined Estrogen-Progestin Therapy metabolism.
 Anticoagulants and anti-epileptics may have altered
efficacy.
 Estrogen → Relieves vasomotor symptoms, improves
bone density.
 Progestin → Protects endometrium from hyperplasia Vaginal Contraceptives
caused by unopposed estrogen.
Definitions of Vaginal Contraceptives

1. General Definition: Vaginal contraceptives are

Drug Dosage Table contraceptive methods or devices applied intravaginally
to prevent pregnancy by creating a physical or chemical
barrier, altering cervical mucus, or releasing hormones.
Type Drug Name Dosage Route 2. Pharmacological Definition: Vaginal contraceptives are
Oral, preparations or devices containing active agents
ERT Estradiol 1 mg daily
patch (hormonal or non-hormonal) that inhibit sperm motility,
EPT Estradiol + 1 mg + 2.5 fertilization, or implantation when inserted into the
Oral vaginal canal.
(Sequential) Medroxyprogesterone mg daily

Indications and Contraindications (Mnemonic:

REPLACEMENT) Types of Vaginal Contraceptives

Indications 1. Hormonal Vaginal Contraceptives

 Relief of vasomotor symptoms.  Contain estrogens and/or progestins that prevent

 Estrogen deficiency states (menopause). ovulation and thicken cervical mucus.
 Prevention of osteoporosis.
 Long-term hypoestrogenism. Examples:
 Amenorrhea management.
 Cardiovascular risk reduction (controversial).  Vaginal Ring:
 Endometriosis management.
 o Etonogestrel + Ethinyl Estradiol Ring  Intolerance to vaginal devices.
(NuvaRing): A flexible ring inserted  Vaginal trauma.
intravaginally for 3 weeks.  Elevated clotting risk with hormonal rings.
o Segesterone acetate + Ethinyl Estradiol Ring
(Annovera): Reusable for 1 year.

Side Effects (System-Wise)

2. Non-Hormonal Vaginal Contraceptives 1. Reproductive System: Vaginal irritation, discharge,

dryness.
 Act as spermicides or physical barriers to sperm 2. Gastrointestinal: Nausea (hormonal rings).
penetration. 3. Systemic: Hormonal side effects (rings).

Examples:

 Spermicides: Nonoxynol-9 gel, foam, suppository, or Drug Interactions

film.
 Vaginal Contraceptive Film: A dissolvable film  Hormonal rings: Affected by CYP3A4 inducers (e.g.,
releasing spermicide upon insertion. rifampin, phenytoin).
 Nonoxynol-9 efficacy reduced by certain vaginal
lubricants.

Drug Dosage Table for Vaginal Contraceptives Antidote for Overdose

Type Drug/Device Name Dosage Route  Hormonal ring: Symptomatic care for nausea, vomiting.
Etonogestrel + Insert for 3  Spermicides: Rinse and symptomatic care for irritation.
Hormonal (Ring) Vaginal
Ethinyl Estradiol weeks
Segesterone acetate Insert for 21
Hormonal (Ring) Vaginal
+ Ethinyl Estradiol days/cycle
Non-Hormonal Apply prior to Drugs Used in Infertility
Nonoxynol-9 Vaginal
(Spermicide) intercourse
Definition of Infertility Drugs

Indications and Contraindications (Mnemonic: 1. General Definition: Drugs used in infertility are agents
CONTRACEPTIVE) designed to enhance ovulation, improve implantation, or
support early pregnancy to treat male or female
infertility.
Indications
2. Pharmacological Definition: Infertility drugs act by
modulating the hypothalamic-pituitary-ovarian axis,
 Contraception for women desiring non-daily options. improving sperm quality, or enhancing uterine
 Ovulation suppression. receptivity.
 Normalization of menstrual cycles (hormonal ring).
 Temporary contraception post-delivery.
 Regulation of hormonal acne (hormonal ring).
 Amenorrhea with ovulation. Classification of Infertility Drugs
 Conditions requiring spermicide use for added
protection.
1. Ovulation Induction Drugs
 Effective contraception during lactation.
 Prevention of fertilization.
 Temporary contraception in emergencies.  Clomiphene Citrate: Selective estrogen receptor
modulator (SERM) stimulating ovulation.
 IVF preparation.
 Letrozole: Aromatase inhibitor stimulating follicular
 Vaginal barrier contraceptive needs.
development.
 Enhanced compliance due to low maintenance.
 Gonadotropins: FSH, LH, or hCG for ovulation
induction.
Contraindications
2. Drugs for Luteal Support
 Cervical or vaginal infections.
 Obstruction or anatomical abnormalities.
 Progesterone: Supports luteal phase and implantation.
 Non-compliance with insertion.
 hCG: Maintains corpus luteum function.
 Thromboembolic disorders (hormonal rings).
 Recurrent UTI risk (spermicides).
3. Hyperprolactinemia Treatment
 Allergy to components.
 Concurrent use of oil-based lubricants (nonoxynol-9).
 Endometriosis or suspected carcinoma.  Bromocriptine: Dopamine agonist reducing prolactin.
 Pregnancy.  Cabergoline: Long-acting dopamine agonist.
 Tampon use concurrently.
4. Insulin Sensitizers for PCOS 2. Cardiovascular: Thrombosis (gonadotropins).
3. Neurological: Dizziness, headache (clomiphene).
 Metformin: Improves ovulation by reducing insulin 4. Gastrointestinal: Bloating, nausea (letrozole).
resistance.

5. Male Infertility Drugs

Drug Interactions
 Clomiphene: Improves spermatogenesis.
 Antioxidants: Coenzyme Q10, vitamin E.  Clomiphene: May potentiate gonadotropins' effects.
 Metformin: Risk of lactic acidosis with alcohol.

Medical Termination of Pregnancy (MTP)

Drug Dosage Table for Infertility Drugs
Definitions of Medical Termination of Pregnancy
Drug Name Dosage Indication Route
1. General Definition: Medical termination of pregnancy
Clomiphene 50 mg daily (5
Ovulation induction Oral is the intentional termination of a pregnancy through the
Citrate days/cycle)
use of medications or surgical methods under medical
2.5–5 mg daily (5 supervision.
Letrozole Ovulation induction Oral
days/cycle) 2. Pharmacological Definition: Medical termination of
5,000–10,000 IU pregnancy involves the administration of drugs to induce
hCG Ovulation trigger IM/SC
once uterine contractions, cervical dilation, or fetal expulsion
500–1,500 PCOS-related to terminate an unwanted or non-viable pregnancy
Metformin Oral within a defined gestational age.
mg/day infertility
Bromocriptine 2.5–7.5 mg/day Hyperprolactinemia Oral

Drugs Used in Medical Termination of Pregnancy

Indications and Contraindications (Mnemonic:
INFERTILITY)
1. Mifepristone (Antiprogestin)
Indications
 Mechanism: Progesterone receptor antagonist that blocks
the action of progesterone, leading to detachment of the
 Induction of ovulation.
gestational sac.
 Normalization of menstrual cycles in PCOS.
 Failure to conceive due to ovulatory issues.
2. Misoprostol (Prostaglandin E1 Analog)
 Endocrine dysfunction (hyperprolactinemia).
 Repeated pregnancy losses (luteal support).
 Treatment of male factor infertility.  Mechanism: Stimulates uterine contractions and softens
 Improvement of implantation rates. the cervix to expel pregnancy tissue.
 Low ovarian reserve.
 IVF protocols. 3. Methotrexate (Antimetabolite)
 Tubal factor infertility adjunct.
 Young couples with unexplained infertility.  Mechanism: Inhibits folate-dependent DNA synthesis,
affecting rapidly dividing trophoblastic cells.
Contraindications
4. Gemeprost (Prostaglandin E1 Analog)
 Idiopathic ovarian failure.
 Non-responsive ovaries to stimulation.  Mechanism: Induces uterine contractions to facilitate
 Failure of earlier ART protocols. fetal expulsion.
 Existing pregnancy.
 Recent thromboembolic events. 5. Carboprost (Prostaglandin F2α Analog)
 Tumors (hormone-sensitive).
 Intracranial prolactinoma (contraindicates  Mechanism: Potent uterotonic agent that causes uterine
bromocriptine). contractions and reduces blood loss.
 Liver dysfunction (contraindicates clomiphene).
 Infection or active pelvic pathology.
 Thyroid or adrenal disease untreated.
 Young age with premature ovarian insufficiency. Drug Dosage Table for Medical Termination of Pregnancy

Drug Name Dosage Indication Route

Pregnancy
Side Effects (System-Wise) 200 mg orally
Mifepristone termination (≤9 Oral
once
weeks)
1. Reproductive System: Ovarian hyperstimulation,
multiple pregnancies.
 Drug Name Dosage Indication Route  Misoprostol: Interactions with antacids containing
800 µg Expulsion of magnesium.
Misoprostol vaginally/200 µg pregnancy Vaginal/Oral
orally tissue
Ectopic
Methotrexate 50 mg/m² IM pregnancy or IM Antidote for Overdose.
MTP
1 mg vaginally Second-  Misoprostol: Activated charcoal for recent ingestion,
Gemeprost every 3 hours trimester Vaginal symptomatic care for diarrhea or dehydration.
(max 5 mg) abortion  Methotrexate: Leucovorin (folinic acid) rescue therapy.
250 µg IM every Late first-
Carboprost 15–90 min (max 2 trimester IM Uterine Stimulants
mg) abortion
Definitions of Uterine Stimulants

Indications and Contraindications (Mnemonic: 1. General Definition: Uterine stimulants are drugs that
TERMINATION) enhance the contractility of the uterus to facilitate labor,
induce abortion, or manage postpartum hemorrhage.
Indications 2. Pharmacological Definition: Uterine stimulants are
pharmacological agents that act on uterine smooth
muscle by stimulating oxytocin, prostaglandin, or
 Termination of early pregnancy. adrenergic receptors, promoting uterine contractions.
 Ectopic pregnancy (methotrexate).
 Rape or incest-related pregnancies.
 Malformations incompatible with life.
 Illnesses threatening maternal health.
Classification of Uterine Stimulants
 Non-viable pregnancy.
 Avoidance of surgical intervention.
 Therapeutic abortion. 1. Oxytocics
 Incomplete abortion management.
 Overpopulation control policies (where applicable).  Stimulate uterine smooth muscle contraction through
 Need for privacy (medical vs. surgical). oxytocin receptors.
o Oxytocin: Induces labor and controls
postpartum hemorrhage.
Contraindications
2. Prostaglandins
 Thrombocytopenia or coagulation disorders.
 Ectopic pregnancy (contraindicates misoprostol).
 Promote uterine contractions by increasing intracellular
 Recent uterine surgery (scar dehiscence risk).
calcium.
 Multiple gestations (higher risk of complications).
o PGE1 (Misoprostol): Used for labor induction
 Intrauterine infection or sepsis. and abortion.
 Non-compliance with follow-up visits. o PGE2 (Dinoprostone): Ripens the cervix and
 Advanced gestational age (>10 weeks for medication). induces labor.
 Tumors (hormone-sensitive, avoid mifepristone). o PGF2α (Carboprost): Treats postpartum
 Intolerance to prostaglandins. hemorrhage.
 Ongoing anticoagulation therapy.
 Neurological disorders aggravated by medications. 3. Ergot Alkaloids

 Act on serotonin and α-adrenergic receptors to increase

uterine tone.
Side Effects (System-Wise) o Methylergometrine: Used for postpartum
hemorrhage.
1. Reproductive System: Heavy bleeding, uterine cramps.
2. Gastrointestinal: Nausea, vomiting, diarrhea 4. Antiprogestins
(misoprostol).
3. Neurological: Headache, dizziness.  Block progesterone action, leading to uterine
4. Systemic: Fever, chills (misoprostol side effect). contractions.
o Mifepristone: Induces abortion.

5. Miscellaneous
Drug Interactions
 Promote uterine contractions via varying mechanisms.
 Mifepristone: Efficacy reduced by CYP3A4 inducers o Tranexamic Acid: Stabilizes clotting during
(e.g., rifampin, phenytoin). postpartum hemorrhage.
 Methotrexate: Potentiates hepatotoxicity with alcohol
or NSAIDs.
Drug Dosage Table for Uterine Stimulants 5. Hematologic: Coagulopathy (prolonged use).

Drug Name Dosage Indication Route

Labor
5–10 IU IV Drug Interactions
Oxytocin induction, PPH IV/IM
infusion
control
25–50 µg Labor  Oxytocin: Synergistic effects with prostaglandins; avoid
Misoprostol every 4–6 induction, Oral/Vaginal combined use.
hours abortion  Methylergometrine: Contraindicated with vasopressors
10 mg Cervical (risk of severe hypertension).
Dinoprostone vaginal insert ripening, labor Vaginal  Tranexamic Acid: Increased risk of thrombosis with
(1 dose) induction anticoagulants.
250 µg IM
every 15–90 Postpartum
Carboprost IM
min (max 2 hemorrhage
mg) Antidotes for Toxicity
0.2 mg IM/IV
Postpartum  Oxytocin: Stop infusion; administer tocolytics if uterine
Methylergometrine every 2–4 IM/IV
hemorrhage rupture risk.
hours
200 mg orally Medical  Methylergometrine: Alpha-blockers for severe
Mifepristone Oral hypertension.
once abortion
 Misoprostol/Carboprost: Supportive care for GI
1 g IV every PPH distress.
Tranexamic Acid IV
6–8 hours management

Indications and Contraindications (Mnemonic:

Uterine Relaxants (Tocolytics)
STIMULANTS)
Definitions of Uterine Relaxants
Indications
1. General Definition: Uterine relaxants are drugs used to
 Stimulation of uterine contractions during labor. suppress premature uterine contractions to delay preterm
 Treatment of postpartum hemorrhage. labor.
 Induction of labor in overdue pregnancies. 2. Pharmacological Definition: Tocolytics are agents that
 Management of incomplete abortions. inhibit uterine smooth muscle activity by blocking
 Uterine atony correction. calcium influx, reducing prostaglandin synthesis, or
 Late-term pregnancy complications. activating adrenergic receptors.
 Abortions (medical).
 Normalizing uterine bleeding postpartum.
 Termination of abnormal pregnancies.
 Softening of the cervix pre-delivery. Classification of Uterine Relaxants

Contraindications 1. Beta-Adrenergic Agonists

 Severe preeclampsia or eclampsia.  Stimulate β2 receptors, relaxing uterine smooth muscle.

 Threatened uterine rupture. o Terbutaline: Commonly used in preterm labor.
 Improper fetal position (breech/transverse).
 Maternal cardiovascular disease. 2. Calcium Channel Blockers
 Uterine scarring or cesarean history (relative).
 Low fetal heart rate or distress.
 Reduce calcium influx, relaxing uterine smooth muscle.
 Allergy to prostaglandins or ergot derivatives. o Nifedipine: Preferred tocolytic agent.
 Non-viable fetus in advanced pregnancy.
 Thromboembolism (avoid ergot alkaloids).
3. Prostaglandin Synthesis Inhibitors (NSAIDs)
 Severe asthma (carboprost).
 Inhibit prostaglandin production, reducing uterine
contractions.
o Indomethacin: Effective for short-term use.
Side Effects (System-Wise)
4. Oxytocin Receptor Antagonists
1. Reproductive System: Hyperstimulation of the uterus,
uterine rupture.
 Block oxytocin binding to its receptor, reducing uterine
2. Cardiovascular System: Hypertension
contractility.
(methylergometrine), hypotension (oxytocin).
o Atosiban: Used in preterm labor.
3. Gastrointestinal System: Nausea, vomiting, diarrhea
(prostaglandins).
4. Central Nervous System: Headache, dizziness. 5. Magnesium Sulfate
  Competes with calcium, reducing uterine contractility. o Headache, dizziness, flushing (nifedipine).
o Magnesium Sulfate: Also neuroprotective for o Drowsiness, lethargy (magnesium sulfate).
the fetus. 5. Gastrointestinal System: Nausea, vomiting
(indomethacin).
6. Renal System: Oligohydramnios with prolonged
NSAID use (indomethacin).
7. Metabolic System:
Drug Dosage Table for Uterine Relaxants
o Hyperglycemia, hypokalemia (terbutaline).
o Hypocalcemia (magnesium sulfate).
Drug Name Dosage Indication Route 8. Fetal Effects:
0.25 mg every o Premature closure of ductus arteriosus, renal
Terbutaline 20–30 min (max Preterm labor SC dysfunction, and oligohydramnios
0.5 mg) (indomethacin).
10 mg every 6– o Reduced fetal movements or tone (magnesium
Nifedipine Preterm labor Oral sulfate).
8 hours
25–50 mg every
Indomethacin 6 hours (max 48 Preterm labor Oral/Rectal
hours)
Drug Interactions – Uterine Relaxants
IV bolus 6.75
Atosiban mg, then 18 Preterm labor IV
mg/hour 1. Terbutaline: Increased risk of tachycardia when
combined with other beta-agonists or adrenergic drugs.
Magnesium 4–6 g IV bolus, Preterm labor,
IV 2. Nifedipine: Additive hypotensive effects with other
Sulfate then 1–2 g/hour neuroprotection
antihypertensives.
3. Indomethacin: Increased risk of GI bleeding with
anticoagulants or aspirin.
Indications and Contraindications (Mnemonic: 4. Atosiban: No significant drug interactions reported.
TOCOLYTICS) 5. Magnesium Sulfate:
o Enhanced CNS depression with sedatives or
Indications anesthetics.
o Risk of hypotension with nifedipine or other
calcium channel blockers.
 Treatment of preterm labor.
 Overactive uterine contractions in preterm pregnancy.
 Cervical shortening prevention.
 Organ preservation (fetal lung development).
 Labor delay for steroid administration. Antidotes for Toxicity
 Young fetal gestation requiring delay.
 Treatment of hypertonic uterine contractions. 1. Terbutaline: Discontinue drug, administer beta-blockers
 Increased risk of preterm delivery. (e.g., propranolol) for tachycardia or arrhythmias.
 Control of preterm uterine contractions. 2. Nifedipine: Stop drug, provide IV fluids, and administer
 Short-term pregnancy prolongation. calcium gluconate for severe hypotension.
3. Indomethacin: Discontinue; supportive care for renal or
GI toxicity.
Contraindications 4. Magnesium Sulfate:
o Stop infusion.
 Term pregnancy. o Administer calcium gluconate (10 mL of 10%
 Ongoing infection (chorioamnionitis). solution IV) as an antidote for magnesium
 Compromised fetal condition. toxicity.
 Overt uterine rupture. 5. Atosiban: Symptomatic care; severe side effects are
 Liver or kidney dysfunction (magnesium sulfate). rare.
 Young gestation (<20 weeks).
 Threat to maternal life (severe preeclampsia). Definitions of Antimicrobials
 Intrauterine fetal demise.
 Concurrent use of contraindicated drugs. 1. General Definition: Antimicrobials are agents that kill
 Severe maternal cardiovascular disease. or inhibit the growth of microorganisms, including
bacteria, fungi, viruses, and protozoa.
2. Pharmacological Definition: Antimicrobials are
chemical substances derived from microorganisms,
synthetic sources, or semi-synthetic processes used to
Side Effects (System-Wise) – Uterine Relaxants (Tocolytics)
treat or prevent infections caused by pathogenic
microorganisms.
1. Reproductive System: Reduced uterine tone, delayed
labor, uterine atony postpartum.
2. Cardiovascular System:
o Hypotension (nifedipine, magnesium sulfate).
o Tachycardia, palpitations (terbutaline). General Principles of Antimicrobial Use
3. Respiratory System: Pulmonary edema (terbutaline,
magnesium sulfate with prolonged use). 1. Selective Toxicity: Antimicrobials should target
4. Central Nervous System: microorganisms specifically without harming the host.
 2. Role of Pharmaceuticals: Ensure the production of 1. Penicillin binds to penicillin-binding proteins (PBPs) on
high-quality, pure drugs with appropriate bacterial cell walls.
pharmacokinetic properties. 2. Inhibits transpeptidase enzyme, preventing cross-linking
3. Post-Antimicrobial Effect (PAE): Persistence of of peptidoglycan chains.
antimicrobial activity after drug levels fall below the 3. Weakens cell wall integrity, causing osmotic lysis.
minimum inhibitory concentration (MIC). 4. Result: Bactericidal effect.
4. Combination Therapy: Using two or more
antimicrobials to enhance efficacy, reduce resistance, or
broaden the spectrum of activity.
5. Spectrum of Action: Dosage Table
o Narrow-spectrum: Effective against specific
types of microorganisms.
o Broad-spectrum: Effective against a wide Drug Dosage Route
range of pathogens. Penicillin G 1.2–2.4 million units daily IV/IM
6. Prophylactic Therapy: Preventing infections in high- Penicillin V 250–500 mg every 6–8 hours Oral
risk scenarios (e.g., surgeries, immunosuppressed
patients). Amoxicillin 500–1000 mg every 8–12 hours Oral
7. Empirical Therapy: Starting treatment based on clinical Ampicillin 1–2 g every 4–6 hours IV/IM
judgment before lab results. Methicillin 1 g every 4–6 hours IV
8. Microbial Sensitivity: Choosing antimicrobials based Ticarcillin 3 g every 4–6 hours IV
on laboratory tests like culture and sensitivity.
9. Mechanism of Resistance: Understanding how
microorganisms develop resistance (e.g., enzymatic
degradation, efflux pumps) to select appropriate drugs. Indications and Contraindications (Using "PENICILLIN"
10. Host Factors: Considering age, organ function, immune Mnemonic)
status, and allergies before prescribing.
11. Adverse Effects: Monitoring for side effects that may  Pharyngitis (streptococcal infections)
harm the patient.  Endocarditis
12. Drug Interactions: Assessing interactions with other  Neonatal infections
drugs to avoid reduced efficacy or toxicity.  Infections caused by Streptococcus pneumoniae
 Cellulitis
 Infective syphilis
 Listeria infections
Penicillin  Leptospirosis
 Inflammatory bacterial infections
1. Definition: Penicillin is a group of β-lactam antibiotics  Not indicated in penicillin allergy.
used to treat bacterial infections by inhibiting cell wall
synthesis.
2. Inventor: Alexander Fleming (1928).
3. Source: Initially obtained from the fungus Penicillium
Side Effects and Adverse Effects (System-Wise)
notatum; now primarily sourced from Penicillium
chrysogenum and semi-synthetic processes.
4. Chemical Composition: Core structure is a β-lactam 1. Gastrointestinal: Diarrhea, nausea, vomiting.
ring fused with a thiazolidine ring, with variable side 2. Hematological: Hemolytic anemia, thrombocytopenia.
chains. 3. Neurological: Seizures (high doses).
4. Renal: Interstitial nephritis.
5. Allergic Reactions: Anaphylaxis, rash, urticaria.
Types of Penicillin

 Natural Penicillins:
o Penicillin G (parenteral)
o Penicillin V (oral) Drug Interactions
o Narrow-spectrum, effective against Gram-
positive bacteria. 1. Reduced efficacy with tetracyclines.
 Semi-Synthetic Penicillins: 2. Increased nephrotoxicity with aminoglycosides.
o Acid-Resistant: Penicillin V (oral use due to 3. Prolonged bleeding time with anticoagulants.
acid stability).
o Penicillinase-Resistant: Methicillin, oxacillin,
nafcillin (resistant to β-lactamase enzymes).
o Amino-Penicillins: Amoxicillin, ampicillin Antidote for Penicillin Toxicity
(broader spectrum; effective against Gram-
negative bacteria). 1. Discontinue the drug.
o Carboxy-Penicillins: Carbenicillin, ticarcillin 2. Administer antihistamines or epinephrine for allergic
(effective against Pseudomonas and other reactions.
Gram-negative organisms). 3. Dialysis in severe toxicity.

Cephalosporins

Mechanism of Action of Penicillin (Flowchart Format) Definition:

Cephalosporins are β-lactam antibiotics that inhibit bacterial cell Drug Dosage Route
wall synthesis and are effective against a wide range of bacterial
Cefuroxime 500–1000 mg every 8–12 hours Oral/IV
infections.
Ceftriaxone 1–2 g once daily IV/IM
Inventor: Ceftazidime 1–2 g every 8 hours IV
Cefepime 1–2 g every 8–12 hours IV
Discovered by Giuseppe Brotzu in 1945.

Source: Indications and Contraindications (Using "CEPHALO"

Mnemonic)
Originally derived from the fungus Acremonium (formerly known
as Cephalosporium); now synthesized semi-synthetically.  Cellulitis.
 Endocarditis prophylaxis.
Chemical Composition:  Pyelonephritis.
 Hospital-acquired infections.
The core structure consists of a β-lactam ring fused to a  Acute otitis media.
dihydrothiazine ring, with side chain variations determining  Lower respiratory tract infections.
pharmacological properties.  Organism-specific therapy (e.g., MRSA with
ceftaroline).

Classification of Cephalosporins
Side Effects and Adverse Effects (System-Wise)
1. First Generation:
o Examples: Cephalexin, cefazolin. 1. Gastrointestinal: Nausea, diarrhea, pseudomembranous
o Spectrum: Gram-positive cocci, limited Gram- colitis.
negative coverage. 2. Hematological: Neutropenia, hemolytic anemia.
o Uses: Skin infections, surgical prophylaxis. 3. Renal: Interstitial nephritis.
2. Second Generation: 4. Hypersensitivity: Rash, anaphylaxis, cross-reactivity
o Examples: Cefuroxime, cefaclor. with penicillin.
o Spectrum: Better Gram-negative coverage than
first generation.
o Uses: Respiratory tract infections, UTIs.
3. Third Generation: Drug Interactions
o Examples: Ceftriaxone, ceftazidime.
o Spectrum: Broad-spectrum, enhanced Gram-
negative activity. 1. Increased nephrotoxicity when combined with
o Uses: Meningitis, sepsis. aminoglycosides.
4. Fourth Generation: 2. Decreased efficacy of oral contraceptives.
o Example: Cefepime.
o Spectrum: Broad-spectrum with Pseudomonas
activity.
o Uses: Nosocomial infections. Antidote for Cephalosporin Toxicity
5. Fifth Generation:
o Example: Ceftaroline. 1. Supportive care.
o Spectrum: Effective against MRSA and 2. Discontinue the drug.
multidrug-resistant organisms. 3. Antihistamines or epinephrine for hypersensitivity
o Uses: Skin infections, pneumonia. reactions.

Mechanism of Action (Flowchart Format) Aminoglycosides

1. Cephalosporin binds to penicillin-binding proteins Definition:

(PBPs).
2. Inhibits transpeptidase, disrupting peptidoglycan
Aminoglycosides are bactericidal antibiotics that inhibit bacterial
synthesis.
protein synthesis by binding to the 30S ribosomal subunit.
3. Weakens bacterial cell walls.
4. Causes osmotic lysis of bacteria (bactericidal effect).
Source:

Originally derived from Streptomyces and Micromonospora

species.
Dosage Table

Examples:
Drug Dosage Route
Cephalexin 250–500 mg every 6–12 hours Oral
  Streptomycin, gentamicin, amikacin, tobramycin, 1. Macrolides are a class of antibiotics characterized by a
neomycin. macrocyclic lactone ring, effective against gram-positive
bacteria and certain gram-negative pathogens, primarily
by inhibiting bacterial protein synthesis.
2. Macrolides are bacteriostatic antibiotics that bind to the
50S ribosomal subunit, preventing translocation of
Mechanism of Action (Flowchart Format)
peptides during protein synthesis.
1. Aminoglycoside enters bacterial cell via oxygen-
Discovery
dependent transport.
2. Binds irreversibly to the 30S ribosomal subunit.
3. Causes misreading of mRNA and inhibits protein  Macrolides were discovered in 1952 from Streptomyces
synthesis. erythraeus.
4. Leads to bacterial death (bactericidal).  Erythromycin was the first macrolide identified and is
still in use today.

Mechanism of Action (Flowchart Format)

Dosage Table
1. Drug enters bacterial cell.
2. Binds to the 50S ribosomal subunit of bacterial
Drug Dosage Route ribosomes.
Gentamicin 5–7 mg/kg/day (divided) IV/IM 3. Prevents translocation of the growing polypeptide
Amikacin 15 mg/kg/day (divided) IV/IM chain.
Tobramycin 3–5 mg/kg/day (divided) IV/IM 4. Inhibits bacterial protein synthesis.
5. Results in bacteriostatic action (bactericidal in high
Neomycin 500 mg 4 times daily Oral/Topical concentrations against some organisms).

Indications and Contraindications (Using "AMINO"

Mnemonic) Broad-Spectrum Antibiotics

 Aerobic Gram-negative infections. Definitions

 Meningitis (adjunct therapy).
 Intra-abdominal infections.
1. Broad-spectrum antibiotics are agents effective against a
 Nosocomial infections. wide variety of bacteria, including gram-positive, gram-
 Ophthalmic infections (topical use). negative, and some anaerobic organisms.
2. These antibiotics work by targeting fundamental
bacterial processes such as cell wall synthesis, DNA
replication, or protein synthesis.
Side Effects and Adverse Effects (System-Wise)
Discovery
1. Ototoxicity: Hearing loss, tinnitus, vestibular
dysfunction.  Broad-spectrum antibiotics, such as tetracyclines and
2. Nephrotoxicity: Acute tubular necrosis. chloramphenicol, were developed during the 1940s and
3. Neuromuscular: Paralysis (high doses). 1950s.
4. Hypersensitivity: Rare rashes.
Mechanism of Action (Flowchart Format)

1. Targets essential bacterial processes:

Drug Interactions o Cell wall synthesis (e.g., carbapenems,
cephalosporins).
1. Increased nephrotoxicity with cephalosporins or o Protein synthesis (e.g., tetracyclines).
diuretics. o DNA replication (e.g., fluoroquinolones).
2. Potentiates neuromuscular blockade with muscle 2. Inhibits bacterial growth or kills bacteria.
relaxants. 3. Affects both gram-positive and gram-negative bacteria.

Antidote for Aminoglycoside Toxicity Classification and Subclassification

1. Discontinue the drug. Macrolides Classification

2. Hemodialysis or peritoneal dialysis for rapid clearance.
3. Calcium gluconate for neuromuscular blockade. 1. Natural Macrolides
o Erythromycin
Macrolides 2. Semi-Synthetic Macrolides
o Clarithromycin, Azithromycin
Definitions 3. Ketolides (derivative of macrolides)
o Telithromycin
Broad-Spectrum Antibiotics Classification Broad-Spectrum
System Macrolides
Antibiotics
1. Cell Wall Inhibitors Nausea, diarrhea, Nausea,
o Penicillins (Amoxicillin, Ampicillin), Gastrointestinal
abdominal pain pseudomembranous colitis
Cephalosporins (Ceftriaxone).
QT interval
2. Protein Synthesis Inhibitors Cardiovascular Hypotension (rare)
prolongation
o Tetracyclines (Doxycycline), Macrolides
(Clarithromycin). Photosensitivity (e.g.,
Dermatological Rash, urticaria
3. DNA Gyrase Inhibitors tetracyclines)
o Fluoroquinolones (Ciprofloxacin, Dizziness, confusion
Neurological Headache, dizziness
Levofloxacin). (fluoroquinolones)
4. Miscellaneous Elevated liver
o Chloramphenicol, Metronidazole. Hepatic Hepatotoxicity (rare)
enzymes, jaundice

Drug Interactions
Examples of Subclassifications
Macrolides
1. Macrolides
o Natural: Erythromycin
 Increased toxicity with warfarin, digoxin.
o Semi-synthetic: Azithromycin, Clarithromycin
o Ketolides: Telithromycin  Prolonged QT with antiarrhythmics (e.g., amiodarone).
2. Broad-Spectrum Antibiotics
o Tetracyclines: Doxycycline, Minocycline Broad-Spectrum Antibiotics
o Fluoroquinolones: Ciprofloxacin, Norfloxacin
 Reduced absorption with antacids (fluoroquinolones).
 Increased nephrotoxicity with aminoglycosides.

Dosage Table

Drug Name Class Dosage Frequency Antidotes for Toxicity

Every 6
Erythromycin Macrolide 250-500 mg 1. Macrolides
hours
o Supportive care (e.g., gastric lavage).
500 mg (Day 1), 250
Azithromycin Macrolide Once daily o QT prolongation: Administer magnesium or
mg (Days 2-5)
antiarrhythmics if needed.
Clarithromycin Macrolide 250-500 mg Twice daily 2. Broad-Spectrum Antibiotics
Broad- o Activated charcoal for acute overdose.
Doxycycline 100 mg Twice daily o Hemodialysis for severe cases (e.g.,
spectrum
Broad- aminoglycosides).
Ciprofloxacin 250-750 mg Twice daily
spectrum
Sulfonamides

Indications and Contraindications Definitions

Indications 1. Sulfonamides are synthetic bacteriostatic antibiotics that

inhibit bacterial folic acid synthesis, essential for DNA
replication and growth.
 Macrolides: Respiratory tract infections, skin infections, 2. These antibiotics act as structural analogs of para-
Helicobacter pylori infections. aminobenzoic acid (PABA), competitively inhibiting
 Broad-spectrum antibiotics: Urinary tract infections, dihydropteroate synthase.
gastrointestinal infections, sepsis.
Discovery
Contraindications
 Discovered in 1935 from Prontosil, a red dye with
 Macrolides: Known hypersensitivity, hepatic antibacterial properties, by Gerhard Domagk, marking
dysfunction. the beginning of the antibiotic era.
 Broad-spectrum antibiotics: Severe renal impairment,
pregnancy (some classes).

Mechanism of Action (Flowchart Format)

Side Effects and Adverse Effects (System-Wise)
1. Sulfonamide enters the bacterial cell.
2. Competes with PABA for binding to dihydropteroate
synthase.
3. Blocks synthesis of dihydrofolic acid.
 4. Prevents formation of tetrahydrofolic acid, a precursor
for purine and pyrimidine synthesis.
5. Inhibits bacterial DNA synthesis, leading to Side Effects and Adverse Effects (System-Wise)
bacteriostatic action.
System Side/Adverse Effects
Gastrointestinal Nausea, vomiting, diarrhea
Classification and Subclassification Dermatological Rash, Stevens-Johnson syndrome (rare)
Hematological Hemolysis in G6PD deficiency, anemia
Classification Renal Crystalluria (encourage hydration)
Neurological Headache, dizziness
1. Short-acting Sulfonamides
o Sulfadiazine, Sulfamethoxazole
2. Intermediate-acting Sulfonamides
Drug Interactions
o Sulfamethoxazole (combined with
trimethoprim)
3. Long-acting Sulfonamides  Increased risk of bleeding with warfarin (due to protein-
o Sulfadoxine binding displacement).
4. Topical Sulfonamides  Potentiates effects of sulfonylureas and phenytoin.
o Silver sulfadiazine, Mafenide acetate  Antagonized by PABA-containing drugs (e.g., local
anesthetics like procaine).
Examples of Subclassifications

Type Examples Uses

Antidotes for Toxicity
Urinary tract infections
Short-acting Sulfadiazine
(UTIs)
 For crystalluria: Increase fluid intake and alkalinize
Combined with trimethoprim
Intermediate- urine with sodium bicarbonate.
Sulfamethoxazole for UTIs, respiratory
acting  For severe allergic reactions: Administer antihistamines
infections
or corticosteroids.
Used with pyrimethamine for
Long-acting Sulfadoxine
malaria
Quinolones
Silver
Topical Burns and wound infections
sulfadiazine
Definitions

1. Quinolones are a class of synthetic, broad-spectrum

Dosage Table antibacterial agents that inhibit bacterial DNA gyrase
and topoisomerase IV, essential for DNA replication.
Drug Name Class Dosage Frequency 2. These drugs are bactericidal, disrupting bacterial DNA
synthesis and leading to cell death.
Every 6
Sulfadiazine Short-acting 1-2 g
hours
Intermediate- 800 mg (with 160
Sulfamethoxazole Twice daily
acting mg trimethoprim)
Discovery
500 mg (with
Sulfadoxine Long-acting pyrimethamine Single dose
25 mg)  Quinolones were first introduced in the 1960s with
nalidixic acid, which was discovered as a byproduct of
Silver Once or
Topical Apply thin layer chloroquine synthesis. Later generations like
sulfadiazine twice daily
ciprofloxacin enhanced activity against gram-negative
and gram-positive organisms.

Indications and Contraindications

Indications Mechanism of Action (Flowchart Format)

 UTIs, respiratory infections, toxoplasmosis, burns 1. Quinolone enters the bacterial cell through porins.
(topical). 2. Binds to DNA gyrase (in gram-negative bacteria) or
topoisomerase IV (in gram-positive bacteria).
Contraindications 3. Prevents relaxation of supercoiled DNA, blocking
replication and transcription.
 Hypersensitivity to sulfonamides. 4. Leads to bacterial DNA fragmentation and cell death.
 G6PD deficiency (risk of hemolysis).
 Pregnancy (especially near term due to risk of
kernicterus).
 Severe liver or kidney disease. Classification and Subclassification
Classification Drug Interactions

1. First Generation: Limited activity against gram-  Antacids and iron supplements reduce absorption.
negative bacteria.  Increased risk of QT prolongation with other QT-
o Example: Nalidixic acid. prolonging drugs (e.g., amiodarone).
2. Second Generation: Improved gram-negative coverage  Potentiates the effects of warfarin.
and some gram-positive activity.
o Examples: Ciprofloxacin, Ofloxacin.
3. Third Generation: Enhanced gram-positive activity.
o Examples: Levofloxacin.
4. Fourth Generation: Broad-spectrum activity including Antidotes for Toxicity
anaerobes.
o Examples: Moxifloxacin, Gemifloxacin.  Discontinue the drug.
 For QT prolongation: Administer magnesium or correct
Examples of Subclassifications electrolyte imbalances.
 For seizures: Use benzodiazepines.
Generation Examples Uses
Nalidixic
First UTIs (rarely used now)
acid
Miscellaneous Antimicrobials
UTIs, gastroenteritis, respiratory
Second Ciprofloxacin
infections
Definitions
Community-acquired pneumonia,
Third Levofloxacin
skin infections
1. Miscellaneous antimicrobials include various
Respiratory infections, intra- antibiotics that do not belong to conventional classes and
Fourth Moxifloxacin
abdominal infections have unique mechanisms of action.
2. These drugs are used for resistant or atypical infections.

Dosage Table

Drug Name Class Dosage Frequency Mechanism of Action (Example: Linezolid)

Nalidixic acid First-generation 1g Every 6 hours
1. Binds to the 23S ribosomal RNA of the 50S subunit.
Ciprofloxacin Second-generation 500 mg Twice daily
2. Inhibits the formation of the initiation complex for
Levofloxacin Third-generation 500-750 mg Once daily protein synthesis.
Moxifloxacin Fourth-generation 400 mg Once daily 3. Prevents bacterial translation, leading to bacteriostatic or
bactericidal effects.

Indications and Contraindications

Indications Classification and Examples

 UTIs, respiratory infections, skin infections, intra- Drug Name Mechanism of Action Uses
abdominal infections, sexually transmitted infections Inhibits bacterial protein MRSA, VRE
(e.g., gonorrhea). Linezolid
synthesis infections
Inhibits bacterial cell wall MRSA, Clostridium
Contraindications Vancomycin
synthesis difficile
Causes depolarization of Skin infections,
 Hypersensitivity to quinolones. Daptomycin
bacterial membrane endocarditis
 Children and adolescents (due to cartilage damage).
 Pregnant and breastfeeding women.
 Patients with a history of tendon disorders related to
Dosage Table
quinolone use.

Drug Name Class Dosage Frequency

Linezolid Oxazolidinones 600 mg Twice daily
Side Effects and Adverse Effects (System-Wise) Vancomycin Glycopeptides 15-20 mg/kg IV Every 12 hours
Daptomycin Lipopeptides 4-6 mg/kg IV Once daily
System Side/Adverse Effects
Gastrointestinal Nausea, vomiting, diarrhea
Musculoskeletal Tendonitis, tendon rupture Indications and Contraindications
Neurological Headache, dizziness, seizures
Indications
Dermatological Photosensitivity, rash
Cardiovascular QT prolongation
  Severe gram-positive infections, multidrug-resistant 1. Drug is reduced by anaerobic bacteria into active
bacteria (e.g., MRSA, VRE). metabolites.
2. Metabolites interact with DNA.
Contraindications 3. Induces strand breaks and inhibits nucleic acid synthesis.
4. Results in bacterial death.
 Hypersensitivity to the specific drug.
 For Linezolid: Avoid in patients taking monoamine Clindamycin
oxidase inhibitors (risk of serotonin syndrome).
1. Binds to the 50S ribosomal subunit.
2. Inhibits bacterial protein synthesis.
3. Blocks elongation of the peptide chain.
4. Leads to bacteriostatic or bactericidal effects.
Side Effects and Adverse Effects (System-Wise)

System Side/Adverse Effects

Hematological Thrombocytopenia (Linezolid) Classification and Examples
Gastrointestinal Diarrhea, nausea (Vancomycin)
Neurological Peripheral neuropathy (Linezolid) Classification
Renal Nephrotoxicity (Vancomycin)
1. Nitroimidazoles: Metronidazole, Tinidazole.
2. Lincosamides: Clindamycin.
3. Beta-lactams with beta-lactamase inhibitors:
Drug Interactions Piperacillin-tazobactam.
4. Others: Chloramphenicol.
 Linezolid: Avoid with SSRIs and tyramine-rich foods
(risk of serotonin syndrome). Examples of Subclassifications
 Vancomycin: Increased risk of nephrotoxicity with
aminoglycosides.
Class Examples Uses
Abscesses, bacterial
Nitroimidazoles Metronidazole
vaginosis, C. difficile
Antidotes for Toxicity Skin infections, dental
Lincosamides Clindamycin
infections
 Linezolid: Supportive care for serotonin syndrome. Beta-lactams
Piperacillin-
Intra-abdominal infections
 Vancomycin: Discontinue drug and manage renal failure tazobactam
if present. Severe anaerobic
Others Chloramphenicol
infections
Drugs Used in Anaerobic Infections

Definitions Dosage Table

1. Drugs used in anaerobic infections target bacteria that Drug Name Class Dosage Frequency
thrive in low-oxygen environments, such as those Every 8
causing abscesses, intra-abdominal, and pelvic Metronidazole Nitroimidazoles 500 mg
hours
infections.
2. These drugs are effective against anaerobic gram- 300-450 Every 6
Clindamycin Lincosamides
positive and gram-negative organisms by interfering mg hours
with bacterial protein synthesis, DNA replication, or cell Piperacillin- Every 8
Beta-lactams 4.5 g IV
wall integrity. tazobactam hours
Tinidazole Nitroimidazoles 2 g Once daily

Discovery Indications and Contraindications

 Metronidazole, one of the most commonly used drugs Indications

in anaerobic infections, was developed in 1959 for the
treatment of parasitic infections before its efficacy  Anaerobic infections (e.g., intra-abdominal infections,
against anaerobes was discovered. abscesses, pelvic inflammatory disease).
 Clindamycin, derived from lincomycin in the 1960s,  Clostridium difficile infections (Metronidazole).
expanded the arsenal against anaerobic infections.  Dental infections (Clindamycin).

Contraindications

Mechanism of Action (Flowchart Format)

 Metronidazole: Pregnancy (first trimester), alcohol
consumption (disulfiram-like reaction).
Metronidazole  Clindamycin: History of colitis or severe diarrhea.
 1. Binds to bacterial RNA polymerase.
2. Inhibits transcription of bacterial DNA to RNA.
Side Effects and Adverse Effects (System-Wise) 3. Suppresses protein synthesis.
4. Results in bacterial death.
System Side/Adverse Effects
Nausea, vomiting, metallic taste
Gastrointestinal
(Metronidazole)
Classification and Subclassification
Peripheral neuropathy
Neurological
(Metronidazole)
Classification
Hematological Neutropenia, thrombocytopenia
Gastrointestinal 1. First-line drugs: Isoniazid, Rifampin, Ethambutol,
Diarrhea, pseudomembranous colitis
(Clindamycin) Pyrazinamide.
2. Second-line drugs: Streptomycin, Cycloserine,
Capreomycin.
Drug Interactions
Examples of Subclassifications
 Metronidazole: Avoid with alcohol (disulfiram-like
reaction). Enhances warfarin’s anticoagulant effect. Line Examples Uses
 Clindamycin: Increases neuromuscular blockade with Isoniazid,
muscle relaxants. First-line Primary TB treatment
Rifampin
Second- Multi-drug resistant TB (MDR-
Streptomycin
line TB)

Antidotes for Toxicity

Dosage Table
 Metronidazole: Supportive care, discontinue drug.
 Clindamycin: Discontinue drug; treat
pseudomembranous colitis with vancomycin or Drug Name Class Dosage Frequency
fidaxomicin. Isoniazid First-line 300 mg Once daily
Rifampin First-line 600 mg Once daily
Ethambutol First-line 15-25 mg/kg Once daily
Streptomycin Second-line 15 mg/kg IV Once daily
Anti-Tubercular Drugs

Definitions
Indications and Contraindications

1. Anti-tubercular drugs target Mycobacterium

Indications
tuberculosis by disrupting cell wall synthesis, protein
synthesis, or other essential bacterial functions.
2. These are classified into first-line and second-line drugs  Active and latent tuberculosis.
based on efficacy and toxicity.  Multi-drug resistant tuberculosis (second-line drugs).

Contraindications

Discovery  Rifampin: Hypersensitivity, concurrent protease

inhibitor use.
 Streptomycin, discovered in 1944, was the first  Isoniazid: Severe liver disease.
antibiotic effective against tuberculosis.
 Isoniazid and Rifampin revolutionized TB treatment in
the mid-20th century.
Side Effects and Adverse Effects (System-Wise)

System Side/Adverse Effects

Mechanism of Action (Flowchart Format) Hepatic Hepatotoxicity (Isoniazid, Rifampin)
Neurological Peripheral neuropathy (Isoniazid)
Isoniazid (INH)
Nausea, orange discoloration of urine
Gastrointestinal
(Rifampin)
1. Activated by the bacterial enzyme KatG.
2. Inhibits the synthesis of mycolic acids.
3. Leads to disruption of the bacterial cell wall.
4. Causes bacterial death. Drug Interactions

Rifampin  Isoniazid: Inhibits CYP enzymes; interacts with

phenytoin.
  Rifampin: Induces CYP enzymes; reduces effectiveness Class Examples Uses
of oral contraceptives. Adjunctive
Thalidomide Erythema nodosum leprosum
drugs

Antidotes for Toxicity Dosage Table

 Isoniazid: Pyridoxine (Vitamin B6) for peripheral

Drug
neuropathy and toxicity. Class Dosage Frequency
Name
 Rifampin: Supportive care; discontinue if hepatotoxicity
occurs. Dapsone Sulfone 100 mg Once daily
Once monthly (in
Rifampin Rifamycin 600 mg
Anti-Leprosy Drugs MDT)
Phenazine 50 mg daily + 300
Clofazimine Daily/monthly
Definitions dye mg once monthly

1. Anti-leprosy drugs are medications specifically

designed to treat infections caused by Mycobacterium Indications and Contraindications
leprae and Mycobacterium lepromatosis.
2. These drugs aim to reduce bacterial load, prevent Indications
transmission, and treat associated nerve damage and
deformities.
 Paucibacillary leprosy: Dapsone + Rifampin for 6
months.
 Multibacillary leprosy: Dapsone + Rifampin +
Clofazimine for 12 months.
Discovery  Erythema nodosum leprosum (ENL): Clofazimine,
Thalidomide.
 Dapsone, discovered in the 1940s, was the first effective
drug for leprosy. Contraindications
 Rifampin, discovered later, became a cornerstone due to
its potent bactericidal activity.  Dapsone: Severe G6PD deficiency (causes hemolysis).
 Clofazimine: Hypersensitivity, severe liver disease.

Mechanism of Action (Flowchart Format)

Side Effects and Adverse Effects (System-Wise)
Dapsone
System Side/Adverse Effects
1. Competitively inhibits dihydropteroate synthase.
2. Blocks folic acid synthesis in bacteria. Dermatological Skin discoloration (Clofazimine)
3. Disrupts DNA and RNA synthesis. Hematological Hemolytic anemia (Dapsone)
4. Leads to bacteriostatic effect. Gastrointestinal Diarrhea, abdominal pain (Dapsone)
Neurological Peripheral neuropathy (Dapsone)
Clofazimine

1. Binds to bacterial DNA. Drug Interactions

2. Inhibits bacterial replication.
3. Has anti-inflammatory properties.
4. Results in bactericidal and anti-inflammatory effects.  Dapsone: Increases risk of methemoglobinemia when
combined with certain drugs (e.g., primaquine).
 Rifampin: Induces CYP450 enzymes, reducing
effectiveness of oral contraceptives.
Classification and Subclassification

Classification
Antidotes for Toxicity
1. Primary anti-leprosy drugs: Dapsone, Rifampin,
Clofazimine.  Dapsone: Methylene blue for methemoglobinemia.
2. Adjunctive drugs: Thalidomide, Corticosteroids.

Examples of Subclassifications
Anti-Malarial Drugs
Class Examples Uses
Definitions
Primary anti- Dapsone, Multibacillary and
leprosy Rifampin paucibacillary leprosy
 1. Anti-malarial drugs are medications used to prevent Drug Name Class Dosage Frequency
and treat infections caused by Plasmodium species (e.g.,
Tissue Once daily
P. falciparum, P. vivax). Primaquine 30 mg
schizonticide (14 days)
2. These drugs work by targeting different stages of the
parasite's life cycle in humans.

Indications and Contraindications

Discovery Indications

 Quinine, the first anti-malarial, was derived from the  Chloroquine-sensitive malaria: Chloroquine.
bark of the cinchona tree in the 17th century.  Chloroquine-resistant malaria: Artemether-
 Chloroquine was developed in the 1940s and became Lumefantrine.
the mainstay for decades.  Radical cure: Primaquine for P. vivax and P. ovale.

Contraindications

Mechanism of Action (Flowchart Format)  Primaquine: G6PD deficiency (risk of hemolysis).

 Artemether-Lumefantrine: Severe liver or kidney
Chloroquine disease.

1. Concentrates in parasitic food vacuoles.

2. Inhibits heme polymerase.
3. Accumulation of toxic heme derivatives. Side Effects and Adverse Effects (System-Wise)
4. Leads to parasite death.
System Side/Adverse Effects
Artemisinin Gastrointestinal Nausea, vomiting (Chloroquine)
Neurological Tinnitus, dizziness (Chloroquine)
1. Activated by iron in infected red blood cells.
2. Produces reactive oxygen species (ROS). Hematological Hemolysis (Primaquine in G6PD deficiency)
3. Damages parasite proteins and membranes. Cardiovascular QT prolongation (Artemether-Lumefantrine)
4. Causes rapid parasite clearance.

Drug Interactions

Classification and Subclassification  Chloroquine: Increases risk of QT prolongation with

other QT-prolonging drugs.
Classification  Primaquine: Enhanced toxicity with other oxidative
drugs (e.g., sulfonamides).
1. Blood schizonticides: Chloroquine, Artemether,
Lumefantrine.
2. Tissue schizonticides: Primaquine.
3. Gametocidal drugs: Primaquine. Antidotes for Toxicity

Examples of Subclassifications  Chloroquine: Supportive care, diazepam for seizures.

 Primaquine: Blood transfusion in case of hemolysis.
Class Examples Uses
Blood Artemether, Anti-Retroviral Drugs
Acute malaria
schizonticides Chloroquine
Tissue Radical cure of P. Definitions
Primaquine
schizonticides vivax
Prevents 1. Anti-retroviral drugs are medications used to manage
Gametocidal drugs Primaquine infections caused by retroviruses, particularly Human
transmission
Immunodeficiency Virus (HIV).
2. These drugs suppress viral replication, improve immune
function, and reduce transmission risk.
Dosage Table

Drug Name Class Dosage Frequency

600 mg Discovery
Blood Once daily (3
Chloroquine initially, then
schizonticide days)
300 mg  Zidovudine (AZT), the first FDA-approved anti-
Artemether- Twice daily retroviral drug, was developed in 1987.
Combination 20/120 mg
Lumefantrine (3 days)
  Subsequent discoveries introduced combination therapy, Indications
now standard as Highly Active Anti-Retroviral Therapy
(HAART).  HIV infection: All stages.
 Prevention of mother-to-child transmission:
Zidovudine during pregnancy.

Mechanism of Action (Flowchart Format) Contraindications

Zidovudine (NRTI - Nucleoside Reverse Transcriptase  Zidovudine: Severe anemia, neutropenia.

Inhibitor)  Efavirenz: Pregnancy (teratogenic), severe psychiatric
disorders.
1. Converts to active triphosphate form in cells.
2. Competitively inhibits reverse transcriptase.
3. Blocks viral RNA conversion to DNA.
4. Prevents viral replication. Side Effects and Adverse Effects (System-Wise)

Efavirenz (NNRTI - Non-Nucleoside Reverse Transcriptase

Inhibitor) System Side/Adverse Effects
Gastrointestinal Nausea, vomiting (Zidovudine)
1. Directly binds to reverse transcriptase. Hematological Anemia, neutropenia (Zidovudine)
2. Induces conformational changes in the enzyme. Neurological Dizziness, vivid dreams (Efavirenz)
3. Blocks RNA-dependent DNA polymerase activity. Metabolic Lipodystrophy (Protease inhibitors)
4. Results in decreased viral replication.

Drug Interactions
Classification (One-Line Explanation for Each)
 Zidovudine: Enhanced hematotoxicity with ganciclovir.
 Efavirenz: Reduces effectiveness of oral contraceptives
1. Nucleoside Reverse Transcriptase Inhibitors
via CYP3A4 induction.
(NRTIs): Block HIV DNA synthesis by mimicking
nucleotides (e.g., Zidovudine).
2. Non-Nucleoside Reverse Transcriptase Inhibitors
(NNRTIs): Bind to reverse transcriptase and inhibit
enzyme activity (e.g., Efavirenz). Antidotes for Toxicity
3. Protease Inhibitors (PIs): Inhibit HIV protease,
preventing viral maturation (e.g., Ritonavir).  Zidovudine: Supportive care, blood transfusions for
4. Integrase Strand Transfer Inhibitors (INSTIs): Block severe anemia.
integration of viral DNA into host DNA (e.g.,  Efavirenz: Discontinue drug; symptomatic treatment for
Raltegravir). neurotoxicity.
5. Entry Inhibitors: Prevent viral entry into host cells
(e.g., Enfuvirtide).
6. CCR5 Antagonists: Block CCR5 co-receptor on host
cells (e.g., Maraviroc).
Anti-Viral Drugs

Definitions
Examples of Subclassifications
1. Anti-viral drugs are medications targeting viruses by
inhibiting their replication and spread.
Class Examples Uses 2. These drugs are used for various viral infections,
NRTIs Zidovudine HIV in combination therapy including influenza, herpes, and hepatitis.
NNRTIs Efavirenz HIV-1
Protease Inhibitors Ritonavir Advanced HIV
INSTIs Raltegravir First-line HIV therapy
Discovery
Entry Inhibitors Enfuvirtide Drug-resistant HIV

 Acyclovir, developed in the 1970s, was the first drug

specifically targeting viral DNA replication.
Dosage Table  The introduction of oseltamivir revolutionized influenza
management.
Drug Name Class Dosage Frequency
Zidovudine NRTI 300 mg Twice daily
Efavirenz NNRTI 600 mg Once daily (at bedtime)
Mechanism of Action (Flowchart Format)

Indications and Contraindications Acyclovir

 1. Phosphorylated by viral thymidine kinase. System Side/Adverse Effects
2. Forms acyclovir triphosphate (active form).
Gastrointestinal Nausea, vomiting (Oseltamivir)
3. Competitively inhibits viral DNA polymerase.
4. Terminates viral DNA chain elongation. Neurological Headache, dizziness (Acyclovir)

Oseltamivir
Drug Interactions
1. Inhibits neuraminidase enzyme.
2. Prevents release of progeny viruses from infected cells.  Acyclovir: Increased nephrotoxicity with nephrotoxic
3. Reduces viral spread. drugs (e.g., aminoglycosides).
4. Alleviates symptoms and shortens illness duration.

Anti-Fungal Drugs
Classification (One-Line Explanation for Each)
Definitions
1. Anti-herpes drugs: Inhibit viral DNA synthesis (e.g.,
Acyclovir). 1. Anti-fungal drugs are medications that inhibit the
2. Anti-influenza drugs: Inhibit neuraminidase enzyme growth of fungi or kill them, treating fungal infections in
(e.g., Oseltamivir). humans.
3. Anti-hepatitis drugs: Target viral polymerase or 2. They target fungal cell structures and processes, such as
replication (e.g., Tenofovir). ergosterol synthesis, to treat superficial or systemic
4. Broad-spectrum anti-virals: Inhibit multiple viral mycoses.
targets (e.g., Ribavirin).

Discovery
Examples of Subclassifications
 Amphotericin B, discovered in 1955, was the first
Class Examples Uses widely used systemic anti-fungal.
HSV-1, HSV-2, VZV  Azoles, such as fluconazole, were later developed for
Anti-herpes drugs Acyclovir less toxic and oral therapy.
infections
Anti-influenza
Oseltamivir Influenza A and B
drugs
Anti-hepatitis drugs Tenofovir Chronic Hepatitis B
Mechanism of Action (Flowchart Format)

Dosage Table Amphotericin B

1. Binds to ergosterol in fungal cell membranes.

Drug Name Class Dosage Frequency 2. Forms pores in the membrane.
Acyclovir Anti-herpes 400 mg 3–5 times daily 3. Causes leakage of ions and molecules.
Oseltamivir Anti-influenza 75 mg Twice daily (5 days) 4. Leads to fungal cell death.

Fluconazole
Indications and Contraindications
1. Inhibits fungal cytochrome P450 enzyme (lanosterol
Indications 14α-demethylase).
2. Prevents conversion of lanosterol to ergosterol.
3. Disrupts fungal cell membrane synthesis.
 Acyclovir: HSV and VZV infections, prophylaxis in 4. Inhibits fungal growth.
immunocompromised patients.
 Oseltamivir: Influenza treatment and prophylaxis.

Contraindications
Classification (One-Line Explanation for Each)
 Acyclovir: Severe dehydration (risk of nephrotoxicity).
1. Polyenes: Bind to ergosterol, disrupting fungal
 Oseltamivir: Hypersensitivity to the drug. membranes (e.g., Amphotericin B).
2. Azoles: Inhibit ergosterol synthesis (e.g., Fluconazole).
3. Echinocandins: Inhibit fungal cell wall synthesis (e.g.,
Caspofungin).
Side Effects and Adverse Effects (System-Wise) 4. Allylamines: Inhibit squalene epoxidase in ergosterol
synthesis (e.g., Terbinafine).
5. Miscellaneous: Include flucytosine and griseofulvin
System Side/Adverse Effects
with unique actions.
Renal Crystalluria, nephrotoxicity (Acyclovir)
 Anti-Helminthics

Examples of Subclassifications Definitions

Class Examples Uses 1. Anti-helminthic drugs are agents that expel or destroy
parasitic worms (helminths) from the body without
Amphotericin
Polyenes Systemic mycoses causing significant harm to the host.
B
2. These drugs target the metabolic processes of worms,
Candidiasis, Cryptococcal often disrupting their nervous or energy metabolism.
Azoles Fluconazole
meningitis
Echinocandins Caspofungin Invasive candidiasis
Dermatophytosis (e.g.,
Allylamines Terbinafine
ringworm) Discovery
Miscellaneous Griseofulvin Fungal skin infections
 Albendazole was developed in 1975 as a broad-
spectrum anti-helminthic.
Dosage Table  Diethylcarbamazine (DEC) was introduced in the
1940s for filarial infections.
Drug Name Class Dosage Frequency
Amphotericin 0.5–1
Polyene Intravenous, once daily
B mg/kg/day
Mechanism of Action (Flowchart Format)
Once weekly (vaginal
Fluconazole Azole 150 mg
candidiasis)
Albendazole

1. Inhibits polymerization of tubulin in helminths.

Indications and Contraindications 2. Disrupts microtubule function in cells.
3. Blocks glucose uptake.
Indications 4. Depletes energy stores, leading to parasite death.

 Amphotericin B: Cryptococcal meningitis, systemic Diethylcarbamazine (DEC)

fungal infections.
 Fluconazole: Candidiasis, fungal meningitis. 1. Inhibits arachidonic acid metabolism in parasites.
2. Alters surface membranes of microfilariae.
Contraindications 3. Makes parasites more susceptible to immune attacks.
4. Immobilizes and kills parasites.
 Amphotericin B: Severe kidney impairment.
 Fluconazole: Hypersensitivity to azoles.

Classification (One-Line Explanation for Each)

Side Effects and Adverse Effects (System-Wise) 1. Benzimidazoles: Disrupt microtubule function in
parasites (e.g., Albendazole, Mebendazole).
2. Avermectins: Bind to chloride channels, causing
System Side/Adverse Effects
paralysis of worms (e.g., Ivermectin).
Renal Nephrotoxicity (Amphotericin B) 3. Piperazines: Block neuromuscular transmission (e.g.,
Gastrointestinal Nausea, vomiting (Fluconazole) Diethylcarbamazine).
Hematological Anemia (Amphotericin B) 4. Quinolines: Target energy metabolism (e.g.,
Praziquantel).
Cardiovascular Arrhythmias (Amphotericin B)
Neurological Headache, dizziness (Fluconazole)

Examples of Subclassifications
Drug Interactions
Class Examples Uses
 Amphotericin B: Enhanced nephrotoxicity with
aminoglycosides or cyclosporine. Benzimidazoles Albendazole Roundworm, hookworm
 Fluconazole: Increases levels of warfarin, cyclosporine, Avermectins Ivermectin Strongyloidiasis, filariasis
and phenytoin (via CYP inhibition). Piperazines Diethylcarbamazine Filarial infections
Tapeworms,
Quinolines Praziquantel
schistosomiasis

Antidotes for Toxicity

Dosage Table
 Amphotericin B: Hydration and electrolyte correction
for nephrotoxicity.
 Drug Name Class Dosage Frequency  Lindane, an organochlorine, was introduced in the mid-
400 mg Single dose 20th century.
Albendazole Benzimidazole
(adult) (roundworm)  Ivermectin emerged later as a safer and effective oral
alternative.
6 Divided into 3
Diethylcarbamazine Piperazine
mg/kg/day doses

Mechanism of Action (Flowchart Format)

Indications and Contraindications
Lindane
Indications
1. Blocks gamma-aminobutyric acid (GABA) receptors in
 Albendazole: Roundworms, hookworms, hydatid mites.
disease. 2. Causes uncontrolled neuronal firing.
 Diethylcarbamazine: Filariasis, tropical eosinophilia. 3. Leads to paralysis and death of the mites.

Contraindications Ivermectin

 Albendazole: Pregnancy, liver dysfunction. 1. Binds to glutamate-gated chloride channels in mites.

 Diethylcarbamazine: Onchocerciasis (may cause severe 2. Increases chloride permeability.
inflammatory reaction). 3. Causes hyperpolarization of nerve and muscle cells.
4. Leads to paralysis and death.

Side Effects and Adverse Effects (System-Wise)

Classification (One-Line Explanation for Each)
System Side/Adverse Effects
Gastrointestinal Nausea, abdominal pain (Albendazole) 1. Topical agents: Directly applied to kill mites (e.g.,
Permethrin, Lindane).
Neurological Headache, dizziness (DEC)
2. Systemic agents: Oral drugs that kill mites from within
Hematological Bone marrow suppression (Albendazole) (e.g., Ivermectin).
Dermatological Rash, itching (DEC)

Drug Interactions Examples of Subclassifications

 Albendazole: Increased toxicity with corticosteroids. Class Examples Uses

 Diethylcarbamazine: Additive effects with Topical agents Permethrin First-line for scabies
antihistamines (used for allergy management).
Systemic agents Ivermectin Resistant or severe scabies

Dosage Table
Antidotes for Toxicity

 Albendazole: Supportive care for bone marrow Drug Name Class Dosage Frequency
suppression. Permethrin Topical Apply
Single application
 Diethylcarbamazine: Manage inflammatory reactions (5%) Agent overnight
with antihistamines or steroids. Systemic 200 mcg/kg Single dose, repeat in
Ivermectin
Agent (oral) 2 weeks

Anti-Scabies Drugs Indications and Contraindications

Definitions Indications

1. Anti-scabies drugs are medications used to eradicate  Permethrin: Mild to moderate scabies infestation.
Sarcoptes scabiei, the mite causing scabies, by targeting  Ivermectin: Crusted scabies or treatment failures.
its nervous or reproductive systems.
2. These agents relieve symptoms like itching and
Contraindications
eliminate the infestation.

 Permethrin: Hypersensitivity to the drug.

 Ivermectin: Pregnancy, breastfeeding.
Discovery
Side Effects and Adverse Effects (System-Wise) 5. Ultra-Long-Acting Insulin

System Side/Adverse Effects  Subtype: Degludec

Dermatological Burning, itching (Permethrin)  Explanation: Covers basal insulin needs for up to 42
hours, minimizing risk of hypoglycemia.
Neurological Drowsiness, dizziness (Ivermectin)
 Examples:
Gastrointestinal Nausea, abdominal pain (Ivermectin) o Degludec (Tresiba)

6. Pre-Mixed Insulin
Drug Interactions
 Subtypes: Mixtures of rapid- or short-acting insulin with
 Permethrin: Minimal systemic absorption; no major intermediate-acting insulin.
interactions.  Explanation: Combines basal and mealtime insulin in a
 Ivermectin: Enhanced sedation with CNS depressants. single injection.
 Examples:
Definitions of Insulin o Humalog Mix 75/25
o Novolog Mix 70/30
1. Biochemical Definition: Insulin is a peptide hormone
produced by the beta cells of the pancreas that regulates
glucose metabolism by promoting cellular uptake of
glucose, lipid synthesis, and protein synthesis. Mechanism of Action
2. Pharmacological Definition: Insulin is a therapeutic
agent used to manage diabetes mellitus by mimicking or 1. Rapid-Acting Insulin (Lispro, Aspart, Glulisine):
supplementing the action of endogenous insulin to
control blood glucose levels.
 Pro: Binds to insulin receptors on muscle and adipose
tissue.
1.  Con: Requires exact timing with meals.
 Chat: Promotes glucose uptake by GLUT-4 receptors,
Types of Insulin and Subtypes suppressing hepatic gluconeogenesis.

1. Rapid-Acting Insulin 2. Short-Acting Insulin (Regular Insulin):

 Subtypes: Lispro, Aspart, Glulisine  Pro: Mimics endogenous insulin secretion.

 Explanation: These insulins act quickly to lower blood  Con: Requires pre-meal planning due to slower onset.
glucose and are often used right before meals to manage  Chat: Reduces blood glucose by stimulating cellular
postprandial glucose spikes. glucose uptake.
 Examples:
o Lispro (Humalog)
3. Intermediate-Acting Insulin (NPH Insulin):
o Aspart (NovoRapid)
o Glulisine (Apidra)
 Pro: Provides extended basal coverage.
2. Short-Acting Insulin  Con: Peaks can increase hypoglycemia risk.
 Chat: Combines insulin with protamine, delaying
absorption.
 Subtype: Regular insulin
 Explanation: Slower onset than rapid-acting insulin,
4. Long-Acting Insulin (Glargine, Detemir):
used 30 minutes before meals.
 Examples:
o Regular insulin (Humulin R, Novolin R)  Pro: Smooth and sustained action.
 Con: Cannot mix with other insulins.
3. Intermediate-Acting Insulin  Chat: Forms micro-precipitates or binds albumin for
prolonged action.
 Subtype: NPH (Neutral Protamine Hagedorn) insulin
5. Ultra-Long-Acting Insulin (Degludec):
 Explanation: Provides basal insulin coverage and peaks
at 4–8 hours.
 Examples:  Pro: Provides ultra-stable glucose control.
o NPH insulin (Humulin N, Novolin N)  Con: High cost.
 Chat: Forms multi-hexamer complexes, slowly releasing
4. Long-Acting Insulin insulin.

 Subtypes: Glargine, Detemir 6. Pre-Mixed Insulin:

 Explanation: Provides basal coverage with no
pronounced peak, lasting up to 24 hours.  Pro: Combines convenience and efficacy.
 Examples:  Con: Less flexible for individualized control.
o Glargine (Lantus, Toujeo)  Chat: Provides both basal and bolus coverage by mixing
o Detemir (Levemir) insulins with different absorption profiles.
 1. Chemical Definition: Oral hypoglycemic drugs are
synthetic compounds designed to lower blood glucose
Dosage Table levels by acting on various biochemical pathways.
2. Pharmacological Definition: Oral hypoglycemic drugs
are medications used to manage hyperglycemia in type 2
Type Subtype Drug Dosage diabetes mellitus by enhancing insulin secretion,
0.5–1 unit/kg/day improving insulin sensitivity, or reducing glucose
Rapid-Acting Lispro Humalog
(divided) absorption.
4–12 units before
Aspart NovoRapid
meals Classification of Oral Anti-Diabetic Drugs
0.2–0.5
Glulisine Apidra
units/kg/day 1. Sulfonylureas
Regular 0.1–0.2 units/kg 2. Biguanides
Short-Acting Humulin R 3. Thiazolidinediones (Glitazones)
Insulin before meals
4. Alpha-Glucosidase Inhibitors
Intermediate- 10–20 units twice
NPH Insulin Humulin N 5. DPP-4 Inhibitors (Gliptins)
Acting daily
6. SGLT2 Inhibitors (Gliflozins)
Long-Acting Glargine Lantus 10 units/day 7. Meglitinides
0.1–0.2 units/kg 8. Others: GLP-1 Receptor Agonists (oral formulations),
Detemir Levemir
once daily Amylin Analogs
Ultra-Long- 0.2 units/kg once
Degludec Tresiba
Acting daily
Humalog Mix Humalog 12–18 units before
Pre-Mixed Types and Subtypes
75/25 Mix breakfast

1. Sulfonylureas
Indications & Contraindications (Mnemonic: INSULIN)
 Subtypes: First-generation, Second-generation
 I: Indications  Explanation: Stimulate pancreatic beta-cells to release
o Insulin-dependent diabetes (Type 1 DM) insulin by closing ATP-sensitive K⁺ channels.
o Non-responsive Type 2 DM  Examples:
o Stress-induced hyperglycemia o First-generation: Tolbutamide, Chlorpropamide
o Uncontrolled gestational diabetes o Second-generation: Glimepiride, Glipizide,
 N: Contraindications Glyburide
o Insulinoma
o Non-diabetic hypoglycemia 2. Biguanides

 Subtypes: None
 Explanation: Decrease hepatic glucose production and
Side Effects and Adverse Effects (System-Wise) increase peripheral glucose uptake without causing
hypoglycemia.
 Central Nervous System: Confusion, dizziness,  Examples:
seizures (hypoglycemia). o Metformin (Glucophage)
 Cardiovascular System: Palpitations, tachycardia.
 Gastrointestinal System: Nausea, hunger. 3. Thiazolidinediones (Glitazones)
 Skin: Lipodystrophy at injection sites.
 Metabolic: Hypoglycemia, hypokalemia.  Subtypes: Rosiglitazone, Pioglitazone
 Explanation: Activate PPAR-γ receptors to increase
insulin sensitivity in peripheral tissues.
 Examples:
Antidote for Toxicity o Rosiglitazone (Avandia)
o Pioglitazone (Actos)
 Mild Hypoglycemia: Oral glucose (15 g).
4. Alpha-Glucosidase Inhibitors
 Severe Hypoglycemia: Glucagon injection or IV
dextrose (50%).
 Subtypes: Acarbose, Miglitol
 Explanation: Delay carbohydrate absorption in the
intestine, reducing postprandial hyperglycemia.
 Examples:
Drug Interactions o Acarbose (Precose)
o Miglitol (Glyset)
 Increased Hypoglycemia Risk: Sulfonylureas, alcohol,
beta-blockers. 5. DPP-4 Inhibitors (Gliptins)
 Decreased Effectiveness: Corticosteroids, diuretics,
thyroid hormones.
 Subtypes: Sitagliptin, Saxagliptin, Linagliptin
Definitions of Oral Hypoglycemic Drugs
  Explanation: Inhibit DPP-4 enzyme, increasing incretin  Pro: Targets postprandial glucose.
levels, which enhances insulin secretion and suppresses  Con: Causes gastrointestinal side effects.
glucagon.  Chat: Inhibits intestinal alpha-glucosidase enzymes,
 Examples: delaying carbohydrate digestion.
o Sitagliptin (Januvia)
o Saxagliptin (Onglyza) 5. DPP-4 Inhibitors (Gliptins):
o Linagliptin (Tradjenta)
 Pro: Weight-neutral, low hypoglycemia risk.
6. SGLT2 Inhibitors (Gliflozins)  Con: Expensive compared to older drugs.
 Chat: Blocks DPP-4 enzyme, prolonging incretin action,
 Subtypes: Canagliflozin, Dapagliflozin, Empagliflozin increasing insulin, and decreasing glucagon secretion.
 Explanation: Inhibit glucose reabsorption in the
proximal renal tubules, increasing urinary glucose 6. SGLT2 Inhibitors (Gliflozins):
excretion.
 Examples:
 Pro: Helps in weight loss and reduces cardiovascular
o Canagliflozin (Invokana)
risk.
o Dapagliflozin (Farxiga)
o Empagliflozin (Jardiance)  Con: Increases risk of genital infections.
 Chat: Inhibits SGLT2 transporters in the kidney,
promoting glucose excretion.
7. Meglitinides
7. Meglitinides:
 Subtypes: Repaglinide, Nateglinide
 Explanation: Stimulate insulin secretion from beta cells
by a mechanism similar to sulfonylureas.  Pro: Short-acting, lower hypoglycemia risk.
 Examples:  Con: Multiple daily doses needed.
o Repaglinide (Prandin)  Chat: Stimulates rapid insulin secretion by closing K⁺
o Nateglinide (Starlix) channels in beta cells.

8. Others

 Subtypes: GLP-1 Receptor Agonists (Oral Dosage Table

Formulations)
 Examples: Drug Class Drug Dosage
o Semaglutide (Rybelsus) Sulfonylureas Glimepiride 1–2 mg once daily
5–20 mg/day in divided
Glipizide
doses
500–2000 mg/day in
Mechanism of Action Biguanides Metformin
divided doses
Thiazolidinediones Pioglitazone 15–45 mg once daily
(Explained in ProChat format for each type and subtype)
Alpha-Glucosidase
Acarbose 50–100 mg thrice daily
Inhib.
1. Sulfonylureas:
DPP-4 Inhibitors Sitagliptin 100 mg once daily
 Pro: Stimulate sustained insulin secretion. SGLT2 Inhibitors Canagliflozin 100–300 mg once daily
 Con: Can cause hypoglycemia and weight gain. Meglitinides Repaglinide 0.5–4 mg before meals
 Chat: Close K⁺ channels in beta cells, leading to
depolarization and calcium influx, triggering insulin
release. Indications & Contraindications (Mnemonic: INSULIN)

2. Biguanides (Metformin):  I: Indications

o Improved glycemic control in Type 2 DM
 Pro: Does not cause hypoglycemia. o Secondary failure to lifestyle modification
 Con: Risk of lactic acidosis in renal failure. o Gestational diabetes (select drugs like
 Chat: Activates AMPK, reducing hepatic Metformin)
gluconeogenesis and improving insulin sensitivity.  N: Contraindications
o Impaired renal function (Metformin)
3. Thiazolidinediones (Glitazones): o Non-diabetic hypoglycemia

 Pro: Improves insulin sensitivity significantly.

 Con: May cause fluid retention and heart failure.
 Chat: Activates PPAR-γ, modulating genes involved in Side Effects and Adverse Effects (System-Wise)
glucose and lipid metabolism.
 CNS: Dizziness, headache (DPP-4 inhibitors)
4. Alpha-Glucosidase Inhibitors:  CVS: Edema, heart failure (Thiazolidinediones)
 GI: Nausea, diarrhea (Biguanides), flatulence (Alpha-
Glucosidase Inhibitors)
  Renal: UTI, genital infections (SGLT2 inhibitors)  Androgens: Activate androgen
receptors, promoting anabolic and
masculinizing effects.
 Progestogens: Bind to progesterone
receptors, modulating uterine function
Antidote for Toxicity
and menstrual cycle.
o One-line Explanation:
 Sulfonylureas & Meglitinides Toxicity: IV glucose or  Estrogens: Regulate female
glucagon. reproductive function.
 Biguanides Toxicity: Supportive therapy, bicarbonate  Androgens: Promote male reproductive
for lactic acidosis. and anabolic effects.
 Progestogens: Support pregnancy and
menstrual regulation.
o Examples:
Drug Interactions  Estrogens: Estradiol, Conjugated
estrogens
 Androgens: Testosterone, Oxandrolone
 Increased Risk of Hypoglycemia: Sulfonylureas with
 Progestogens: Progesterone,
alcohol or beta-blockers.
Medroxyprogesterone acetate
 Reduced Efficacy: Corticosteroids, thiazides, and
thyroid hormones.

Definitions of Steroids
Dosage Table
1. Chemical Definition: Steroids are organic compounds
characterized by a molecular structure of four fused Drug Classification Usual Dosage
carbon rings (three cyclohexane rings and one 5–60 mg orally daily
Prednisone Glucocorticoid
cyclopentane ring) arranged in a specific pattern. (based on condition)
2. Biological Definition: Steroids are biologically active 0.5–10 mg orally/IV
molecules derived from cholesterol, playing key roles in Dexamethasone Glucocorticoid daily (dose depends on
cellular signaling, metabolism, and as hormones severity)
regulating various physiological processes.
0.05–0.2 mg orally
Fludrocortisone Mineralocorticoid
daily
Estradiol Estrogen 1–2 mg orally daily
Classification of Steroids 50–100 mg
Testosterone Androgen intramuscularly every
1–2 weeks
1. Corticosteroids
o Sub-classification: 2.5–20 mg orally daily
Oxandrolone Androgen
 Glucocorticoids in divided doses
 Mineralocorticoids 100–200 mg orally
Progesterone Progestogen
o Mechanism of Action: daily or intravaginally
 Glucocorticoids: Bind to 2.5–10 mg orally daily
glucocorticoid receptors, modulating Medroxyprogesterone Progestogen (depending on
gene transcription to reduce indication)
inflammation, suppress immune
response, and increase
gluconeogenesis.
 Mineralocorticoids: Act on Indications and Contraindications Using STEROIDS as
mineralocorticoid receptors in renal Mnemonic
tubules to promote sodium retention
and potassium excretion. Indications (STEROIDS)
o One-line Explanation:
 Glucocorticoids: Anti-inflammatory  S: Shock (e.g., septic shock, adrenal crisis)
and immunosuppressive steroids.  T: Transplant rejection prevention
 Mineralocorticoids: Regulate  E: Endocrine disorders (e.g., Addison's disease)
electrolyte and fluid balance.  R: Rheumatologic conditions (e.g., lupus, arthritis)
o Examples:  O: Organ inflammation (e.g., asthma, IBD)
 Glucocorticoids: Prednisone,
 I: Immunosuppressive therapy
Dexamethasone
 D: Dermatological conditions (e.g., eczema, psoriasis)
 Mineralocorticoids: Fludrocortisone
 S: Severe allergies or anaphylaxis
2. Sex Steroids
o Sub-classification:
 Estrogens Contraindications (STEROIDS)
 Androgens
 Progestogens  S: Systemic infections (untreated)
o Mechanism of Action:  T: Tuberculosis (active)
 Estrogens: Bind to estrogen receptors,  E: End-stage heart failure
influencing reproductive tissues and  R: Recent surgery (wound healing interference)
secondary sexual characteristics.
  O: Osteoporosis (severe) Propylthiouracil additionally inhibits peripheral
 I: Immunosuppression sensitivity conversion of T4 to T3.
 D: Diabetes mellitus (uncontrolled) o One-line Explanation: Suppress thyroid
 S: Stomach ulcers (active peptic ulcer disease) hormone synthesis.
o Examples: Methimazole, Propylthiouracil
2. Iodine-Containing Compounds
o Sub-classification:
 Lugol's iodine solution
Side Effects and Adverse Effects by Body System  Potassium iodide
o Mechanism of Action: High doses of iodine
1. Endocrine: inhibit thyroid hormone release and reduce
o Side effects: Hyperglycemia, adrenal iodine organification (Wolff-Chaikoff effect).
suppression o One-line Explanation: Temporarily inhibit
o Adverse effects: Cushing's syndrome, adrenal thyroid hormone release.
crisis o Examples: Lugol's solution, Potassium iodide
2. Musculoskeletal: 3. Radioactive Iodine (I-131)
o Side effects: Osteoporosis, muscle wasting o Mechanism of Action: Selectively destroys
o Adverse effects: Avascular necrosis, myopathy overactive thyroid tissue through beta radiation.
3. Cardiovascular: o One-line Explanation: Destroys thyroid tissue
o Side effects: Hypertension to reduce hormone levels.
o Adverse effects: Heart failure exacerbation o Examples: Sodium iodide I-131
4. Gastrointestinal: 4. Beta-Blockers (Adjunct Therapy)
o Side effects: Gastric irritation o Examples: Propranolol, Atenolol
o Adverse effects: Peptic ulcers, GI bleeding o Mechanism of Action: Inhibit beta-adrenergic
5. Neurological: effects of excess thyroid hormones, providing
o Side effects: Mood changes, insomnia symptomatic relief (e.g., reducing heart rate and
o Adverse effects: Psychosis, depression tremors).
6. Immunological: o One-line Explanation: Control symptoms of
o Side effects: Increased infection risk hyperthyroidism without affecting hormone
o Adverse effects: Severe opportunistic infections synthesis.
7. Dermatological:
o Side effects: Acne, skin thinning
o Adverse effects: Delayed wound healing
Dosage Table

Drug Classification Usual Dosage

Drug Interactions
10–30 mg orally daily in
Methimazole Thioamide
divided doses
 Increased Risk:
o NSAIDs: Additive risk of GI bleeding. 100–150 mg orally every 8
Propylthiouracil
o Anticoagulants: Increased bleeding risk. Thioamide hours (initial), maintenance
(PTU)
o Antihyperglycemics: Reduced efficacy leading 50–100 mg daily
to hyperglycemia. Iodine-containing 5–10 drops (0.25–0.5 mL)
Lugol's Solution
 Decreased Efficacy: compound orally 3 times daily
o Barbiturates, phenytoin, and rifampin: Induce Iodine-containing
steroid metabolism, reducing levels. Potassium Iodide 50–150 mg orally daily
compound
Sodium Iodide I- Radioactive Dose individualized based
Definitions of Antithyroid Drugs 131 iodine on thyroid uptake and size
20–40 mg orally every 6–8
1. Chemical Definition: Antithyroid drugs are compounds Propranolol Beta-blocker
hours as needed
that interfere with the synthesis, secretion, or effects of
thyroid hormones.
2. Pharmacological Definition: Antithyroid drugs are
medications used to manage hyperthyroidism by Indications and Contraindications Using ANTITHYROID as
inhibiting thyroid hormone production or action. a Mnemonic

Indications (ANTITHYROID)

Classification of Antithyroid Drugs  A: Autoimmune hyperthyroidism (Graves' disease)

 N: Nodular goiter (to control hyperfunctioning nodules)
1. Thioamides  T: Thyroid storm (acute management)
o Sub-classification:  I: Iodine-induced hyperthyroidism
 Methimazole  T: Thyroid cancer (adjunct to radioactive iodine)
 Propylthiouracil (PTU)  H: Hyperthyroidism (primary treatment)
o Mechanism of Action: Inhibit thyroid  Y: Young patients (non-destructive treatment preferred)
peroxidase enzyme, blocking iodine  R: Refractory hyperthyroidism (as part of a combined
organification and coupling reactions, which approach)
decreases thyroid hormone synthesis.
  O: Ophthalmopathy management (Graves' disease  Thioamides: ; discontinue drug and provide supportive
adjunct therapy) care (e.g., granulocyte colony-stimulating factor for
 I: In preparation for thyroidectomy (pre-surgical control) agranulocytosis).
 D: Diagnostic tests (radioactive iodine uptake studies)  Iodine Toxicity: Sodium thiosulfate to neutralize iodine,
supportive therapy (hydration and diuretics).
Contraindications (ANTITHYROID)
Introduction to Thyroid Hormones T3 and T4
 A: Allergy to antithyroid drugs
 N: Non-compliance or irregular follow-up Triiodothyronine (T3) and Thyroxine (T4) are hormones
 T: Thyroiditis (not indicated) produced by the thyroid gland. T3 is the active form, while T4 is
 I: Iodine allergy (for iodine-based treatments) converted to T3 in peripheral tissues. Both hormones are essential
 T: T-cell lymphopenia (risk of agranulocytosis with for regulating metabolism, growth, and development.
thioamides)
 H: Hepatic dysfunction (for PTU) Functions of Thyroid Hormones
 Y: Young children (radioactive iodine generally
avoided) The following points can be represented in a flowchart format:
 R: Renal impairment (caution with iodine compounds)
 O: Overt hypothyroidism 1. Metabolic Regulation: Increase basal metabolic rate
 I: Immunosuppression (increased infection risk with and oxygen consumption.
agranulocytosis) 2. Growth and Development: Essential for normal brain
 D: During pregnancy (methimazole contraindicated in and skeletal development in children.
the first trimester; PTU is preferred early pregnancy) 3. Cardiovascular Effects: Increase heart rate and cardiac
output.
4. Thermoregulation: Maintain body temperature by
regulating heat production.
Side Effects and Adverse Effects by Body System

1. Endocrine:
o Side effects: Hypothyroidism Introduction to Calcitonin (Thyrocalcitonin)
o Adverse effects: Thyroid gland destruction
(radioactive iodine) Calcitonin is a hormone secreted by the parafollicular (C-cells) of
2. Hematological: the thyroid gland. It helps regulate calcium and phosphate levels
o Side effects: Mild leukopenia in the blood by opposing the action of parathyroid hormone
o Adverse effects: Agranulocytosis (thioamides) (PTH).
3. Hepatic:
o Side effects: Elevated liver enzymes Functions of Calcitonin
o Adverse effects: Hepatitis (PTU)
4. Dermatological: 1. Inhibits Osteoclast Activity: Reduces bone resorption
o Side effects: Rash, pruritus and calcium release.
o Adverse effects: Severe exfoliative dermatitis 2. Decreases Blood Calcium Levels: Promotes calcium
5. Neurological: deposition in bones.
o Side effects: Headache, drowsiness 3. Regulates Phosphate Levels: Enhances renal excretion
o Adverse effects: Peripheral neuropathy of phosphate.
6. Gastrointestinal: 4. Prevents Hypercalcemia: Maintains calcium
o Side effects: Nausea, vomiting homeostasis.
o Adverse effects: Hepatotoxicity

Stepwise Synthesis of Thyroid Hormones (Simplified)

Drug Interactions
1. Thyroglobulin Production: Synthesized by follicular
 Increased Risk: cells and released into the colloid.
o Anticoagulants: Thioamides can increase the 2. Iodide Uptake: Iodide ions are transported into
anticoagulant effect of warfarin. follicular cells via the sodium-iodide symporter.
o Iodine supplements: Reduce efficacy of 3. Iodide Oxidation: Iodide is oxidized to iodine by
radioactive iodine therapy. thyroid peroxidase.
 Decreased Efficacy: 4. Thyroglobulin Iodination: Iodine binds to tyrosine
o Lithium: Potentiates hypothyroidism. residues on thyroglobulin, forming MIT and DIT.
o Beta-blockers: Mask hyperthyroid symptoms, 5. MIT and DIT Coupling: MIT and DIT combine to
delaying diagnosis. form T3 and T4.
6. Thyroglobulin Proteolysis: T3 and T4 are released into
the bloodstream.

Antidote for Toxicity Key Steps of Thyroid Hormone Synthesis

1. Thyroglobulin Production: Formation of the precursor

protein.
 2. Iodide Uptake: Active transport of iodide into follicular  T: Tachycardia.
cells.  H: Headache.
3. Iodination and Coupling: Formation of MIT, DIT, T3,  Y: (Y)ielding insomnia.
and T4.  R: Restlessness.
4. Hormone Release: Proteolysis of thyroglobulin and  O: Osteoporosis (long-term use).
release of T3 and T4.  I: Irritability.
 D: Diarrhea.

Mechanism of Action of Thyroid Hormones

Adverse Effects (Mnemonic: THYROID)
1. Enter target cells through specific transporters.
2. Bind to nuclear receptors and regulate gene transcription.
 T: Thyrotoxicosis.
3. Increase protein synthesis, enhancing metabolic
 H: Hypertension.
activities.
4. Influence mitochondrial function and energy production.  Y: (Y)ellowish skin (rare).
 R: Rapid heart rate.
 O: Overstimulation of metabolism.
 I: Increased bone loss.
 D: Death (rare, from thyroid storm).
Thyroid Drugs
Steps of Thyroid Hormone Synthesis
1. Levothyroxine (T4)
o Dosage: 25–200 mcg/day orally.
o Group: Synthetic thyroid hormone. 1. TRH Release by Hypothalamus
2. Liothyronine (T3) o The hypothalamus releases Thyrotropin-
o Dosage: 5–25 mcg/day orally. Releasing Hormone (TRH) in response to low
o Group: Synthetic thyroid hormone. levels of thyroid hormones in the blood or other
physiological signals like cold stress.
o TRH stimulates the anterior pituitary gland to
produce and release Thyroid-Stimulating
Hormone (TSH).
Indications (Mnemonic: THYROID) 2. TSH Release by Anterior Pituitary Gland
o TRH binds to receptors on thyrotroph cells in
 T: Thyroid replacement therapy. the anterior pituitary, triggering the release of
 H: Hypothyroidism. Thyroid-Stimulating Hormone (TSH) into the
 Y: (Y) Suppression of TSH. bloodstream.
 R: Reduction of goiter. o TSH acts as the primary regulator of thyroid
 O: Overt hypothyroidism in pregnancy. gland activity, stimulating the production and
 I: Iodine-deficiency correction. secretion of thyroid hormones (T3 and T4).
 D: Depression adjunct therapy (off-label). 3. Thyroid Hormone Synthesis by Thyroid Gland
o TSH binds to TSH receptors on thyroid
follicular cells, initiating a cascade of steps for
thyroid hormone production:
 Iodide Uptake: Active transport of
Contraindications (Mnemonic: THYROID) iodide into the follicular cells.
 Iodide Oxidation and
 T: Thyrotoxicosis. Organification: Iodide is converted to
 H: Hypersensitivity to components. iodine, which binds to tyrosine
 Y: (Y) Recent myocardial infarction. residues on thyroglobulin to form MIT
 R: Risk of osteoporosis (long-term use). and DIT.
 O: Overactive thyroid nodules (autonomous).  Coupling Reaction: MIT and DIT
 I: Impaired adrenal function. combine to form T3 and T4.
 Storage: Hormones are stored in the
 D: Diabetes (caution advised).
colloid attached to thyroglobulin.
4. Thyroid Hormone Release
o When stimulated by TSH, the thyroid gland
takes up iodinated thyroglobulin from the
Drug Interactions colloid into follicular cells.
o Proteolysis of Thyroglobulin: Enzymatic
1. Warfarin: Increases anticoagulant effect. cleavage releases T3 and T4 into the
2. Beta-blockers: Reduced effectiveness. bloodstream.
3. Calcium supplements: Decrease absorption of thyroid o T3 and T4 are transported by binding proteins
drugs. like Thyroxine-Binding Globulin (TBG) to
4. Estrogens: Increase TBG, reducing free hormone levels. target tissues.
5. Amiodarone: May induce thyroid dysfunction.

Side Effects (Mnemonic: THYROID)