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Pharmacology D Pharma Second year

In Easy English
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Contents
S.N. Chapters P.N.
1 General Pharmacology 3

2 Drugs Acting On The Peripheral Nervous 11

System
3 Drugs Acting On Eyes 26

4 Drugs Acting on the Central Nervous System 29

5 Drugs Acting On Cardiovascular System 42

6 Drugs Acting on blood and Blood forming 59

Organs
7 Drugs Acting On The Respiratory System 63

8 Drugs Acting on the gastrointestinal Tract 69

9 Drugs Acting On Kidney 76

10 Hormones and Hormones antagonist 79

11 Autocoids 90
12 Chemotherapeutic Agents 96

13 Biologicals 112

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Chapter 1 Pharmacology
General Pharmacology

Introduction:
Pharmacology is derived from Greek word Pharmacon means drug and logos means to
study. So we can say Pharmacology means to study about drug and its action.
Definition :
Pharmacology is a branch of science in which we study about drugs and their Interaction
with the living organism.
Or it can be defined as " Pharmacology is a branch of science in which we study about
Pharmacokinetic and Pharmacodynamics " .
Pharmacokinetics :
It is a Greek word which means the " the action of body on the drugs ".
Pharmacokinetic Involves the study of drug's absorption, distribution, metabolism, and
excretion .

Pharmacodynamic : -
It is also a Greek word which means " the action of drugs on the body ".
Pharmacodynamics involves the study of concentration of drugs on the site of action ,
result of effect , timing of drug's action , adverse effect etc.
Scope Of Pharmacology

1) Pharmacotherapeutics :
A person who has knowledge of Pharmacology can treat the patients , because he
Knows selection of appropriate drugs , their dosage , and half life .

2) Preclinical Clinical trails :

A pharmacologist can work in the field of preclinical trails .
3) Clinical Trails :
A pharmacologist can work in the field of clinical trails .
4) Drug discovery :
A pharmacologist can go in the field of research and discover many of new drugs .
5) Toxicology :-
A pharmacologist can reduce the toxicity effect, and turn adverse effects .

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Routes Of Administration Of Drugs

Introduction:
Route of drug administration is the path or way by which the drug is introduced ( taken)
into body .
There are different types of route of administration , and the choice of route for the
drug administration depends on :
a) properties of drug like water or lipid solubility , ionisation etc.
b) therapeutic objectives i.e. rapid onset of action or long term administration or for
effect to a local site .

Classification Of route of administration of drugs

Oral rout sublingual route Parental route

(in buccal cavity ) ( below the tongue ) (other than GIT )

Parental Route

Injection Inhalation local application

1) Intradermal 1) External preparation

2) Intravenous e.g. ointment , cream
3) Intramuscular 2)Enema
4) subcutaneous etc.

Oral Route

In this route the drug is placed in oral cavity and is swallowed along with water or milk
etc.
Advantages
1) It is safe route of drug administration .

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2) No special skill is required for administration of drug .
3) It is very convenient route .
4) there are low possibilities of adverse effect reaction .
5) sterilisation is not required for drug taken orally .
6) Large amount of drugs can be administrated by this route .
7) This route is painless .
8) this route is economical .
Disadvantages
1) Onset of action is slow .
2) This route is note useful in clinical emergencies .
3) This route is not useful in unconscious and uncooperative patients .
4) This route is not useful in pre-vomiting and diarrhoea patients .
5) the presence of food in GIT may interfere with absorption of drug.
6) low gastric pH , digestive and liver enzymes destroy drug, before its distribution into
circulation .
7) It may cause irritation in GIT.
Sublingual Route

In this route , tablet is placed below the tongue and dissolved in mouth
cavity. The active drug gets absorbed through the sublingual mucus membrane
directly into blood circulation .
Examples of drugs :
Isoprenaline tablet : used in bronchial asthma
Glyceryl trinitrite : used angina pectoris .
Advantages
1) Rapid onset of action .
2) Degradation of drug does not take place in stomach .
3) Inactivation of drug avoided in liver .
4) Drug can be administered easily .
5) This route is painless .
6) No special skill is required for administration of drug .
7) It is very convenient route .

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Disadvantage
1) This route is not suitable for large dosage and frequent use of drug .
2) Some drugs may cause irritation to buccal mucosa .
3) the drugs having high molecular weight can't be absorbed .( insulin)
4) Unpleasant , distasteful , and irritant drugs can not be administered through this
route .

Parental Route

The routes of administration of drug other than alimentary canal are called
Parental routes .
Advantages
1) Rapid onset of action .
2) The drugs irritate GIT , can given by this route .
3) This route is useful in case of vomiting and diarrhoea .
4) This route is useful in unconscious and incooperative patients .
5) In this route drugs are not destroyed like GIT .
6) This route is useful in clinical emergencies .
7) 100% bioavailability is possible by this route .
8) Those drugs are also can given by this route which are not absorbable fairly
by GIT.

Disadvantage
1) Skilled person required for administration of drug in this route .
2) Possibility of pain at site of application .
3) self medication is difficult by this route .
4) sterilization of syringe and needle is required .
5) once the drug is absorbed in blood circulation , the adverse effect can not
be reversed or controlled easily .

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Intradermal Route
In this route , the drug is injected in the dermis layer of the skin . Only a small
quantity of drug can administered through this route , and the injection is
painful .
Note
a) this route is used for detection of drug allergy ,e.g. penicillin is injected
intradermally to observe allergic reaction to it .
b) Vaccines are given by this route such as BCG, smallpox etc.
Intramuscular Route
In this route drug is administered directly into the muscular tissue .

Advantage
1) mild irritant , suspension , injections with insoluble oily bases can be
administered by this route .
2) The drugs are administered by this route depots in tissue and releases
slowly slowly which provides prolonged duration of action .

Disadvantages
1) sterilization of syringe and needle is required .
2) skilled person required .
3) some drugs may cause irritation , and pain in this route.
4) more than 10ml volume is restricted by IM route.

Absorption Of Drugs

The movement of drug from the site of administration into blood circulation is called
Absorption of drug.

Types Of Absorption
1) Passive diffusion /simple diffusion
2) Filtration / Pore transport
3) Endocytosis .
4) Facilitated diffusion .
5) Active Transport

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1) Passive diffusion /simple diffusion
In this type of absorption the drug is transported from higher concentration to low
concentration .
2) Filtration / Pore transport : In this type of absorption the drug molecules are pass
through the space between tow cells .

3) Endocytosis .
In this type of absorption the cell membrane engulfs the drug molecule and take inside
the cell .

4) Facilitated diffusion .
In this type of absorption a carrier protein helps in the entering of drug inside the cell or
membrane from higher concentration to low concentration , and no energy required in
this process .

5) Active Transport
In this type of absorption the carrier molecule combines with drug molecule and
transports it inside the membrane , and energy is required in this process.

Factors Affecting The Absorption Of Drugs

1)Physical State of Drug

the liquids are betterly absorbed than solid medicaments .
2) Particle Size
Smaller Particle size of drug absorbed easily .
3) Surface area of absorbing site
Larger absorbing surface area provides greater absorption of drug .
4) Physical and mental state of the patient
abnormal / disturbed physiological conditions affect the absorption of drugs like infection ,
fever ,emotional upset etc.
5) Functional condition of GIT
Increased peristaltic movement of GIT decreases the absorption of drugs .
6) pH of drug
Acidic drugs are rapidly absorbed in stomach while basic drugs are rapidly absorbed in
intestine .

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7) Presence of food and other things in GIT.
The presence of food in GIT may reduce the absorption of drugs , because no direct
connation with walls of GIT .
Vitamin C increases the absorption of drugs .

Distribution Of Drug

Distribution of drug means delivery/transportation of drug to body's tissues .

Factors Affecting Drug distribution
1) Age ( fat content , skeletal muscles , Plasma protein )
2) Pregnancy .
3) Obesity
4) Disease conditions .
5) Drug interaction

Metabolism Of drugs

The chemical alteration of the drug in the body , in which nonpolar drugs are converted
into polar form and lipid soluble compounds are converted into lipid insoluble form .
These processes may be used for Biotransformation of drugs .
1) Oxidation 2) Reduction 3)Hydrolysis
4) conjugation .
Factors Affecting drug Metabolism
1) inhibitors : certain drugs like omeprazole , ciprofloxacin inhibit enzymes that
metabolise a drug .
2) Stimulators : certain drugs like phenobarbitone , rifampicin can increase the activity
of enzymes that metabolise a drug .
3) Age : Young children show poor drug metabolism because metabolic enzymes are not
developed properly in them .
4) Sex : In comparison to males , females have lesser ability for drug metabolise .
5) Body Temperature : High temperature of body provides fast metabolism of drugs .

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Excretion / elimination of Drugs

It is a process of body in which drugs or metabolites are removed from the body .
There are two types of excretion :
1) Renal Excretion : Kidneys are main organs for excretion , and the excretion is done
through kidneys is called renal excretion .
2) Non- Renal Excretion : The excretions by all other organs except kidneys are called
Non renal excretion . (lungs , intestine , salivary glands , sweat glands ).

General Mechanism of Drug Action And Factors Modifying Drug

Action

Majority of drug produce their action / effect by interacting with a target site / molecule,
which is usually a protein . These protein can be Receptor , enzyme , carrier and ion
channel .

Factors Modifying drug action

1) Body Weight
2) Age
3) Sex
4) Route of administration
5) Time of administration
6) Diet and environmental factors
7) Genetic Factors
8) Emotional Factors
9) Presence of disease
10) Metabolic disturbance
11) cumulative effect
12) additive effect
13) synergism
14) antagonism
15) tolerance
16) dependence

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Pharmacology Chapter 2
Drugs Acting On The Peripheral Nervous System

CNS : Includes the brain and spinal cord .

PNS : It consists of the nerves branched out from the brain and spinal cord .
These nerves form the communication network between the CNS and body
parts .
PNS

Somatic Nervous System Autonomic Nervous System

Somatic Nervous System : It is a part of PNS and associated with the
voluntary control of body movement via skeletal muscles . sensory and motor
neurons found in it .
Autonomic Nervous System : It is a part of PNS also, and associated with
Involuntary Physiological Process e.i. Heart rate , blood pressure , digestion
etc.

Neurotransmitters
These are specific chemicals allowing communication between nerve cell and
effector cell or organs .
Steps Involved In Neurohumoral Transmission
1) Initiation Of an Action Potential and Axonal Conduction
2) Arrival of an AP at nerve terminal , resulting in the release of the transmitter
3) Events at the synaptic cleft and post - junctional sites .
4) Termination of effect of released Transmitter .

Cholinergic Drugs ( Parasympathomimeticts )

Cholinergic Drugs are those drugs which give action similar to acetylcholine .
They give their action by directly binding to the cholinergic receptors or by
indirect process .

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Classification
1) Direct Acting Cholinergic Agonist
these drugs produced actions similar to ACh by directly interacting with
cholinergic receptors .
Acetylcholine , Methacholine , Carbachol , Bethanechol. Pilocarpine .
2) Indirect Acting Agents ( Anticholinestrase )
These drugs inhibit the enzyme cholinestrase , this enzyme inactivates the
Acetylcholine . Physostigmine ( this can cross blood brain barrier )
Neostigmine ( this can't cross blood brain barrier ) .
Pharmacological Actions
1) Muscarinic Action
a) Heart : bradycardia ( slow down heart rate )
b) Blood Vessels : dilates blood vessels , lowers blood pressure
c) Respiratory System : bronchocon striction
d) smooth muscles : contracts smooth muscles
e) Exocrine Gland : Increase secretion ( saliva ,HCL , Pancreatic Juice )
f) GI Tract : Increase peristalsis Movement .
g) Urinary Bladder : Contraction
h) Eye : Contraction of Pupils

2) Nicotinic Action
a) Skeletal Muscle : contraction
b) CNS : ACh does not cross BBB , but if injected directly into brain and
stimulates initially and then depresses.
Indication
Acetylcholine is mainly used in experimental studies , and has limited clinical value because
of following reasons .
1) It is rapidly hydrolysed by the Pseudocholinesterases .
2) It spread widely and diffuses in easily and thus does not produce a selective
pharmacological action .
3) It can not be administered orally as it immediately hydrolysed and degraded by gastric
enzymes .
Methacoline is not used nowadays .

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Carbachol shows action on M and N receptors non selectively , so no longer in use .
Bethanechol Is in use as
1) In case of gastroparesis , postoperative abdominal distension .
2) In case of urinary bladder retention .
Dose
Bethanechol : 5 or 10 mg tablets , 10-30 mg 3-4 times in a day .
Contraindications
1) Hyperthyroidism : choline ester may precipitate cardiac arrhythmias .
2) Bronchial Asthma : choline ester may precipitate bronchospasm .
3) Peptic ulcer : choline ester may increase gastric acid secretion .
4) Myocardial Infarction : choline ester may cause hypotension and form conduction block .

Pilocarpine
It is a alkaloid cholinergic drug , and it is a selective muscarinic agonist , therefore most of
muscarinic effects can be predicted .
Pharmacological action
Eye : miosis
CVS : when administered intravenously a brief fall in blood pressure is seen .
Sweat Glands : Excessive amount of sweat secret . ( termed as diaphoresis )
Indication
Pilocrpine is commonly used in glaucoma as eye drops .
Dose
It is used 1-4 % pilocarpine nitrate in eye drops .
Contraindications
1) during pregnancy and lactation
2) In children because its safety and efficacy is not clear .
3) In older people may cause diarrhoea , urinary frequency and dizziness .

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Anticholinergic Drugs

These are the drugs which occupy the ACh receptors and do not allow ACh to
bind to the receptors .
Anticolinergic Drugs are also called " Parasympatholytic " Anti -
Parasympathetic Agents " Cholinergic blocking Agents " Cholinergic antagonist
"

Classification
1) Anti Muscarinic Agents : Atropine , Ipratropium , Tropicamide .
2) Anti Nicotinic Agents : Trimethaphan , Pentolinium .

Anti-muscarinic Agents
The anticholinergic drugs that block the action of ACh on muscarinic receptors
are called Anti-muscarinic agents . example . Atropine

Atropine
It is most common anti muscarinic agent . It is an alkaloid and blocks the all
types of muscarinic receptors .
Pharmacological Action
1) CNS : mild stimulation
2) Eye : Mydriasis
3) CVS : It cause bradycardia initially and then tachycardia .
4) Respiratory System : bronchodilation
5) secretion : secretions of sweat , saliva , and gastric are reduced .
6) GIT : relaxation , decrease peristaltic movement so it used as antispasmodic
and anti diarrhoeal drug .
Indication
1) for dilation of pupil .
2) Pre - Anaesthetic
3) in bronchial Asthma and COPD .
4) in hypersalivation .
5) to treat diarrhoea
6) as antidote for organophosphorus poisoning .
7) to treat parkinsonism .

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Dose : It is given IV , IM and SC, routes .
0.4-0.6mg for preoperative and pre anaesthetic ,
1% solution in eye drop for mydriasis .
Contraindication
1) in glaucoma condition
2) in infants suffering from Down' syndrome ( delay in development of body
and brain )
3) in patients are hypertensive with atropine .

Adrenergic Drugs
Adrenergic drugs are those drugs which stimulate the adrenergic receptors
and gives sympathetic action . e.g. epinephrine , norepinephrine . they work
on α 1 α 2 ß 1 ß 2 receptors .
they also called adrenergic agonist , sympathomimetic agents .

Classification
1) Direct Acting Adrenergic agents : Epinephrine Norepinephrine
2) Indirect Acting Adrenergic Agents : Amphetamine
3) Mixed Acting Adrenergic Agents : Ephedrine

Location Of adrenergic receptors

α1 : smooth muscles = Heart , , Bladder , spleen , Ureters, ( contraction ) eye ( mydriasis )
α2 : Pancreas ( decrease insulin )
ß 1 : Heart ( Increase heart rate )
ß 2 : smooth muscles = heart , bronchi , uterus , GIT , ( relaxation )

1) Direct Acting Adrenergic agents

these are drugs which directly bind to adrenergic receptors and activate them
to give their actions .
Pharmacological Action of Epinephrine and norepinephrine .
1) cardiovascular system : stimulate the α 1 receptor and increase the
contraction force of heart and then output of blood .

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2) Respiratory system : stimulate ß 2 receptor and dilate the bronchi smooth
muscles .
3) pancreas : bind to α 2 receptor of pancreas and decrease the release of
insulin ,so give hyperglycemic effect .
Indication
1) it bind to alpha 1 receptor and cause vasoconstriction and epinephrine is
used :
a) to control bleeding
b) to slow the absorption of local anaesthetics .
c) to increase blood pressure .
2) epinephrine is useful in asthmatic patient because it promote
bronchodilation .
Contraindication
1) α 1 receptor agonist is contraindicated in hypertension .
2) α 2 receptor agonist is contraindicated in low blood pressure .
Dose : in acute asthma 0.01ml/ml
in cardiac arrest 0.01ml/ml

2) Indirect Acting Adrenergic Agents

Indirect Acting Adrenergic agents stimulate the release of a stored
neurotransmitter from adrenergic nerve terminals . The main
neurotransmitter involved here is noradreneline . Example , Amphetamine
Pharmacological Action of Amphetamine
1) Cardiovascular Action : systolic and diastolic BP is increase
2) smooth muscle relaxation .
Dose : 5-10mg tablet in the morning and midday

3)Mixed Acting adrenergic Agents

These are the drugs which act directly and indirectly on both α and ß
adrenergic rectors .examples : Ephedrine . metaraminol .
Pharmacological Action and other things just like direct acting adrenergic
drugs .
Dose : Ephedrine Hydrochloride tablet 30mg , to be administered in doses of
15-30 mg TDS .

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Anti- Adrenergic Drugs

The drugs block the effect or actions that occur by release of adrenaline are called anti-
Adrenergic Drugs .
these drugs are also called " Adrenergic Blocking Agents " " Adrenoceptor antagonist " .
Classification Of Anti-Adrenergic Drugs
1) α Adrenoceptor blocking Agents : Prazosin , Yohimbine , Phenoxybenzamine .
2) ß Aderenoceptor blocking agents : Atenolol , Butoxamine , propranonol
3) α & ß Blockers : Labetalol , Carvedilol

Alpha Blocking Agents

a) α1 Selective blocker : Prazosin
b) α2 Selective blocker : Yohimbine
c) α1 & α2 Non selective blocker : Phenoxybenzamine , Phentolamine
Pharmacological Actions
1) Effect on CVS : Hypotension , fall in BP
2) on Eye : miosis
3) nasal congestion
4) Inhibit ejaculation
5) increase intestinal motility .
Indication
1) to treat hypertension
2) In congestive heart failure .
3) In migraine
Contraindication
Alpha blockers are contraindicated in
1) Hepatic and renal disease
2) peptic ulcer
3) any drug allergy
4) coronary artery disease
Alpha 2 blocking agent
yohimbine : increases the insulin secretion and down the blood glucose level .

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Beta Blockers
1) Selective ß1 Blocker : Atenolol , Bisoprolol ( cardioselective ) , esmolol , Binoprolol
2) selective ß2 Blockers : Butoxamine , ICI 118551
3) Non selective ß1 & ß2 blockers : Propranolol

1) Beta 1 Cardioselective blockers

Atenolol , Bisoprolol : these are used to treat Hypertension

2) Non selective beta 1 beta 2 Blockers

Propranolol :
Pharmacological action
1) decrease the heart rate
2) Bronchodilation
3) Vasodilation .
4) Lower blood pressure
Indication
To treat :
1) Hypertension 2) Angina pectoris
3) Cardiac arrhythmias 4) Migraine
5) Anxiety 6 ) parkinson's disease

α & ß Blockers

Labetalol , Carvedilol are non selective α & ß blockers .

these are used to treat high blood pressure .

Doses
Atenolol : 25 - 100mg daily
Propanolol : 80 - 240 mg 12 hourly
labetalol : 200 -600 mg 12 hourly

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Neuromuscular Blocking Agents ( Skeletal Muscle Relaxant )

Definition
The drugs are used to block the transmission of nerve impulses at the skeletal
neuromuscular junction and cause skeletal muscle relaxation are called Neuromuscular
Blocking Agent .
They are used to reduce spasm and pain in skeletal muscles .
Classification
Drugs Acting Peripherally at the Neuromuscular Junction

1) Non Depolarising Agents

a) long acting ( 60 - 120 minutes ) e.g. tubocuratine ,Dexacurium
b) Intermediate acting ( 20 -50 minutes ) e.g. Atracurium
c) short Acting ( 10 -20 ) e.g. Mivacurium
2) Depolarising Agents : Succinyl Choline

Pharmacological Action of Non depolarising Agents

1) Skeletal muscle : parental Administration of Tubocurarine results in weakness of Motor
Impulses .
2) CVS : No significant effect show on CVS .
Pharmacological Action of Depolarising Agents
1) Skeletal Muscle : parental Administration of " Succinyl Choline "results in muscle
relaxation .
2) CVS : These agents produce Hypotention and cardiac arrhythmia ( increase or decrease
in heart rate )
Indications
1) Adjuvant ( helping ) to general Anaesthesia : Neuromuscular Blocking Agents are use with
general anaesthesia to achieve adequate ( as need ) muscle relaxation .
2) In Convulsant : these drugs are used for muscle relaxation in epileptic condition .
3) In sever tetanus : tetanus cause a painful muscle contraction , these drug are used only in
severe case of tetanus .
Contraindications
1) Heart patients : these are contraindicated in heart patients .
2) Asthma patients ; these are contraindicated in asthma patients .

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Dose
d -tubocurarine 0.5 - 0.6 mg/kg
Dexacurium 0.03 -0.05 mg / kg
Atracurium 0.4 -0.5 mg / kg
mivacurium 0.15 -0.2 mg/kg
Succinyl Choline 1.0 -1.5

Myasthenia Gravis

Myasthenia Gravis (MG) is an autoimmune disorder , in which antibodies

attack on M & N receptors , and then number of M &N receptors decrease ,
and Acetylcholine faces difficulty in binding with them .
In this disease muscle become weak and unable to contract relax .

Drugs used In Myasthenia Gravis

1) Anticolinesterases: Pridostigmine
2) Immunosuppression : Cyclosporine , Azthioprine

3) Intravenous Immune Globulin ( IVIG )

4) Immunoabsorption : this procedure helps to remove anti AChR ABs (
Acetycholine Receptor Antibodies )
5) Plasma Exchange : It helps to remove the abnormal antibodies .

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Local Anaesthetic

Definition
The drugs are used to block the sensation in a limited area are call Local
anaesthetics .
or we say The drugs are used to abolish the sensory perception over a local
area are called local anesthetics.
Classification Of Local anaesthetics
1) Injectable Anaesthetics
a) short duration : procaine
b) Intermediate duration : Lignocaine ( lidocaine )
c) Long duration : Tetracaine
2) Surface Anaesthetics : Cocaine , Lignocaine
Pharmacological Action Of Local Anaesthetics
The local anaesthetic have the following two types of actions :
1) Local Action 2 ) systemic action

1) Local Action
a) they block the nerve ending
b) They block the neuromuscular junction
c) They delay the release of acetylcholine from motor neuron .
2) Systemic Action
a) CNS Ⅰ) they stimulate the CNS in starting and then depress
Ⅱ) They produce restlessness , mental confusion .

B) CVS
Ⅰ) Heart : Cardiac depression
Ⅱ) Blood Vessels : Vasodilation Ⅲ ) Lower Blood pressure
Indications
1) these are used for infiltration anae sthetics ( anaesthetic of an operative
site by local injection )
2) ) these are used as antiarrhythmic agents .
3) ) these are used to treat status epilepsy .

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Contraindications ( Lignocaine IV )
1) These are contraindicated in coronary disease .
2) These are contraindicated in heart failure .
3) These are contraindicated in heart block .
4) These are contraindicated in liver disease .
Dose
1) Lignocaine : 4mg/ kg and should not exceed 300 mg or 500mg
2) procaine : 12mg/kg and should exceed 1000mg

Non-Steroidal Anti-Inflammatory Drugs ( NSAIDs)

The drugs are used to treat Inflammation , and mild to moderate Pain and fever are called
Non steroidal anti Inflammatory drugs .
Inflammation : It is a condition in which part of the body becomes reddened , swollen , hot,
and painful , especially as a reaction to injury or infection .
Classification of (NSIADs)
1) Non -Selective COX inhibitors
a) Salicylates : Aspirin
b) pyrazolone Derivatives : Phenylbutazone
c) Indole Derivatives : Indomethacin
d) Propionic Acid Derivatives : Ibuprofen
e) Aril Acetic Acid Derivatives : Diclofenac
f) oxycame Derivatives : Piroxicam
2) Preferential COX 2 inhibitors : Nimesulide , meloxicam
3) Selective COX - 2 inhibitors : selecoxib , Rofecoxib

4) Analgesic Antipyretics with poor Anti inflammatory Action :

a) Paraaminophenol Derivatives : Paracetamol ( acetaaminophen )
b) Pyrazolone Derivatives : metamizol .
Indications
1) Analgesia : NSIADs are used to eliminate or treat mild to moderate pain like :
a) headache b) toothaches c) muscle aches
d) arthritis e) migraine f) Dysmenorrhea

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2) Antipyresis : NSIADs are used to treat fever / to normalize body temperature .
3) Anti Inflammation : NSIADs are used to stop inflammation and pain like :
a) Rheumatoids
b) osteoarthritis
c) Ankylosing spondylitis d) bursitis
Adverse Effects
1) In Stomach : NSIADs block the biosynthesis of PG ( prostaglandins ) , which inhibit the
acid secretion and promote the secretion of cytoprotective mucus in the GIT . If these PGs
are inhibited there are more chances to damage the inner layer of stomach , and may cause
the gastric ulcer .
2) In Platelets : The function of platelets are disturbed because NSIADs prevent the
formation of TXA2 ( thromboxane A2 ) , which helps in blood clotting .
3) In Uterus : prostaglandins help to open the cervix because of contraction , but in the case
of inhibition of PGs cause difficulty in labor .(child birth )
4) In Kidneys : NSIADs decrease the renal blood flow and the glomerular filtration rate .
Contraindication Of non NSIADs
1) with NSIADs hypersensitivity ( an exaggerated response by immune to a drug ) .
2) In peptic Ulcer ,
3) In children suffering from chicken pox or influenza .
4) In chronic liver disease
5) In during pregnancy .
6) in breastfeeding mother .
Detail study of some drugs
1) Aspirin :
It is a non selective anti- inflammatory drug .
Indications : It is used as
1) an analgesic , in headache , in primary dysmenorrhoea , muscle pain etc .
2) an antipyretic for fever .
3) an anti- inflammatory : In Rheumatoids, osteoarthritis , Ankylosing spondylitis .
Contraindications
1) with NSIADs hypersensitivity ( an exaggerated response by immune to a drug ) .
2) In peptic Ulcer ,

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3) In children suffering from chicken pox or influenza .
4) In chronic liver disease
5) In during pregnancy .
6) in breastfeeding mother .
7) in stomach bleeding

Dose
Adults : 325 -650mg orally 4 -6 Hours as need and should not exceed 3.9 g/day
children under 12 years : 10-15mg/kg
2) Ibufrofen :
It is a non steroidal anti inflammatory drug , it is marketed as Brufen .

Indications :
a) headache b) toothache
c) Menstrual cramps d) muscle aches
e) Arthritis f) fever
g) in common cold and flu .

Contraindications
1) with NSIADs hypersensitivity ( an exaggerated response by immune to a drug ) .
2) In peptic Ulcer ,
3) In children suffering from chicken pox or influenza .
4) In chronic liver disease
5) In during pregnancy .
6) in breastfeeding mother .
7) asthma
8) kidney or liver problems
9) in stomach bleeding
10 ) in hypertension
3) Diclofenac :
It is a Non steroidal anti inflammatory drug .

(same aspirin)

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4) paracetamol
It is a non steroidal anti inflammatory drug , it is just like the aspirin but has weak anti
inflammatory effects .

Indications :
a) headache b) toothache
c) Menstrual cramps d) muscle aches
e) Arthritis f) fever
g) in common cold and flu .

Adverse Effects
1) allergic reactions .
2) bloody or black stools .
3) bloody or black urine
4) pine in lower back
5) small red spots on the skin
6) ulcer on lips or in mouth
7) unusual tiredness or weakness
8) sudden decrease in the amount of urine .

Contraindications
1) in liver problems
2) In a condition where the body is unable to maintain adequate blood flow .

Dose
Adults : 500- 650 mg , duration 4-6 hours , and should not exceed 4000mg/day
children under 18 years : 15mg/kg duration 6 hours .
Pharmacology chapter 3

Pharmacology Chapter 3

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Drugs Acting on Eye

Introduction
These are the drugs which used to treat eye problems , like inflammation , Infection and
reduction of intraocular pressure .

Miotics
The drugs are used to produce miosis / constriction of pupils are called Miotics .
Classification Of miotics
1) Muscarinic Agents : pilocarpine , carbachol and other cholinergic drugs .
2) α adrenergic blockers( relaxation of dilator muscle ) : tolazoline and other alpha blocker
. pupil get constricted when iris dilated .
Indications
1) These drugs are used to treat glaucoma .
2) To control mydratic effect .
3) To prevent or break adhesion ( attachment ) between iris and lens .
Contraindications
1) These are contraindicated during pregnancy .
2) These are contraindicated during lactation .
3) These are contraindicated during in children because its safety is not clear .
4) These are contraindicated in patients are above 65 years .
5) These are contraindicated in patients are suffering from cataract .
Dose
Pilocarpine : 1-4% pilocarpine nitrate in eye drops .
tolazoline ; 1-2mg/kg intravenously over 10 minutes .

Mydriatics
The drug are used to dilate the pupil to perform easier and detailed examination .
Classification Of mydriatics
1) Adrenergic agonist : - adrinaline , Phenylephrine .
2) Cholinergic Antagonist : Tropicamide , Atropine , cyclopentolet .

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Indications
1) These are used to dilate the pupil .
2) These are used for examination of retina and optic nerves .
3) These are used for diagnosis of iris problems .
4) These are used to determine refractive error ( it is a disease in which eye can not focus
the image clearly and result in blurred vision .
Contraindications
1) it is contraindicated in hypertension . 2) in Glaucoma .
3) In intraocular pressure .
Doses
Tropicamide : 0.5% solution dilate for 30 minutes nearly .
atropine : 1% solution 7-12 days
cyclopentolate : 1-2 % 24 hours

Glaucoma
Glaucoma is a ocular ( eye ) Disease in which intraocular pressure is increased and damage
the optic nerves which causes visual loss .
when drainage canal of aqueous humorous get blocked , the intraocular pressure increases
.
There are two types of glaucoma :
1) Open Angle glaucoma
2) narrow / closed angle Glaucoma .
Classification of drugs used in Glaucoma ( they reduce intraocular pressure ( IOP )

decrease the production of aqs.hum Increase the out flow of fluid

1) ß Blockers : Timolol topical ( 0.5% ) 1) Miotics : Pilocarpine topi.(2%)

2)Carbonic Anhydrase inhibiter : 2) osmotic agents : mannitol i.v. 20%
Acetazolamide oral 500mg 3) prostaglandin : topical ( 0.005% )
Dorzolamide : eye drop

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Indications Of Mannitol
1) It is used to reduce intraocular pressure .
2) It is used to reduce intracranial pressure .
3) It is used to reduce as diuretics .
4) It is used to reduce to lower BP .
Contraindications
1) It is contraindicated in renal diseases
2) In pulmonary edema
3) in severe dehydration .
4) heart failure .
5) in hypertension .

Indications Of Prostaglandin
1) it is used in glaucoma .
2) to treat peptic ulcer .
3) to induce labor
4) in pulmonary hypertension .
5) to treat erectile dysfunction
Contraindications
1) in bronchial asthma .
2) in renal disease

3 ) in hypersensitivity person .

4) in hypertension

5) in epilepsy

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Pharmacology Chapter 4
Drugs Acting on the Central Nervous System

General Anaesthetics
Definition
The drugs which produce reversible loss of all sensation , conscious ness and
Movement .
there are three component of anaesthesia :
1) Analgesia ( pain killer )
2) Amnesia ( loss of memory )
3) Immobolisation ( loss of movement )

Types of Anaesthetics
1) Local Aneasthetics : they produce action at a local ( specific ) area .
2) General Anaesthetics : they produce action on whole body .

Stages of Anaesthesia
Stage -1 : Analgesia :
* It starts with administration of anaesthetics
* beginning of loss of consciousness , reflexes and respiration remain normal
, and feel dream like condition .
* loss of pain sensation .
Stage -2 : Excitement or Delirium :
* It starts with unconsciousness to beginning of irregular respiration .
* Patient may shout , struggle for movement , jaws are tightly closed .
* Heart rate and BP may rise , and pupils dilate
* involuntary Urination , and defecation .
* No operative procedure carried out in this stage .
Stage -3 : Surgical Anaesthesia : all t he surgical procedures are done in this
stage.
plane 1 : respiration becomes regular , and eyes become fixed .
plane 2: loss of corneal and laryngeal reflexes
plane 3 : pupils start dilating and light reflexes
plane 4: Dilated pupils , decrease muscle t one , BP falls .

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Stage 4: Medullary paralysis :
This stage must be avoided , otherwise patient may be died . In this stage
medulla depresses and leads to stop respiration and then death .
Classification of General Anaestheics
1) Inhalation Anaestheics
1) Enflurane 2) Desflurane
3) Halothane 4) Ether

2) Intravenous Anaestheics
1)Thoipental sodium 2) ketamine hydrochloride
3) Diazepam
3) Gaseous Anaestheics
Nitrous Oxide
Pharmacological Action Of general anaestheics
These drugs work on central nervous system and depress it , and induce sleep
, loss of pain sensation and unconsciousness.

Indication , Contraindication and doses of some commonly used general

anaesthetics
1) Inhalation Anaestheics
Halotane Indication : It is used for general Anaesthesia in combination with
other anaesthetic agents .
contraindication : It should not be used in patient having intracranial
hemorrhage .
Dose : 2-3 % in oxygen vapor .
2) Intravenous Anaestheics
Thiopental sodium
Indication : It is used for general Anaesthesia in combination with other
anaesthetic agents .
Contraindication : 1) It is contraindicated in myasthenia gravis .
2) in Prolonged asthma
3) in low blood pressure
4) in porphyria

Dose:
2.5 % solution for IV
3) Gaseous Anaestheics

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Nitrous Oxide
Indication : It is used to maintain surgical anaesthesia in combination with
other anaesthetic agents .
Contraindication :
1) It is contraindicated in patients suffering from chronic respiratory
problems.
2) in pregnancy
3) in vitamin B12 deficiency patients

Dose :
It should be mixed with at least 30% oxygen .

Sedative & Hypnotics

Definition
Sedatives : sedatives are those drugs which reduce excitement,emotions,
tension and induce calmness . It is also used as antianxiety .
Hypnotics : hypnotics are those drugs which produce sleep , just like natural
sleep.
when we increase sedative drugs dose then th ey produce hypnotics effects .
Classification
1) Urea derivatives : Barbiturate
a) Long acting Barbiturate : Phenobarbitone , Mephobarbitone .
b) Short acting barbiturate : Butobarbitone , secobarbitone .
c) Ultra short acting barbiturate : Thiopentone , hexobarbitone

2) Benzodiazepines :
a) sedative and hypnotics : diazepam , clonazepam , Alprazolam , flurazepam .
3) Newer Non Benzodiazepine Hypnotics : Zopiclone , zolpidem .
Pharmacological Action
1) CNS Depression : They depress the CNS and cause sedation and hypnotic
effects . over dose can cause death when respiratory and vasomotor center
depressed .
2) CVS : they lower blood pressure , reduce cardiac output , and induce
vasodilatation .

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Indications
1) they are used as sedative and hypnoti cs .
2) they are as anticovusant .
3) They are used as anaesthetics in combination of other anaesthetic drugs .
Contraindications
1 ) they are contraindicated in porphyria.
2) they are contraindicated in Liver and kidney diseases
3) They are contraindicated in pulmonary diseases .

Dose
Diazepam : Tablets 2 , 5, and 10mg and slow releasing capsule 15 mg
Alprazolam : Tablets ( 0.25 , 0.5 , 1 , and 2 mg )
Clonazepam : Injection and tablets ( 0.25 , 0.5 , 1 , and 2 mg )

Anti-Convusant Drugs / antiepileptic / antiseizure drug

Definition
The drugs are used to treat convulsion are called anticovulsant drugs .
Convulsion is a nervous system disorder , due to abnormal electrical activity
in brain cells .
this disorder may result involuntary muscle movement , uncontrolled shaking
of the body .
Classification
1) Hydantoin Derivatives : Phenytoin
2) barbiturates : Phenobarbiturate
3) GABA Transaminase Inhibitors : Sodium Valproate
4) GABA agonist : Gabapentin
5) Benzodiazepines : Diazepam , clonazepam
6) Iminostilbenes : Carbamazepine

Pharmacological Action Of Anticonvulsant drugs

These drugs stabilize cell membranes and suppress the abnormal electric
impulses in the cerebral cortex . They mainly work on GABA receptors ,
sodium and calcium channels .

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Indications
These drugs are used to treat various types of Epilepsy .
1) Generalised ( Tonic clonic , pettimal )
2) partial seizure ( simple , complex )
3) Status
Contraindications
1) These are contraindicated in liver diseases .
2) These are contraindicated in certain blood diseases.
3) These are contraindicated in narrow angle glaucoma .

Doses
Phenytoin : 50 mg and 100mg tablets , 50 mg IV , and it should not exceed
50mg / minute .
Phenobarbitone : 60mg 1-3 times a day . 3-6 mg /kg / day in children .
It is the first effective antiepileptic drug was introduced in 1912 . and it
broad spectrum antiseizure drug .
Sodium Valproate : 100mg and 200 mg tablets and 200mg/5ml syrup.
and in children 10mg/kg in tow divided doses .
Carbamazepine : 100mg initial dose and gradually increased to 600 -1200mg
/day in divided dose . it is available as 100 ,200, 400 mg tablets .

Anti-Anxiety Drugs / Anxiolytic Drugs

Definition
The drugs are used to treat anxiety are called antianxiety drugs .
Anxiety is a CNS disorder . some symptoms of anxiety are below :
1) too much worry and fear about everyday situation .
2) feeling nervous and restlessness
3) Tension , panic
4) Increased heart rate and breathing
5) sweating

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Classification of Anti- anxiety Drugs
1) Benzodiazepines : Diazepam , clonazepam , alprazolam , lorazepam ,
oxazepam , Clobazam , chlordiazepoxide .
2) Non Benzodiazepines anxiolytics : meprobamate , tybamate , zopiclon ,
zolpidem .
Pharmacological Action Of anti-anxiety drugs
These drugs show anxiolytic , sedative & hypnotic , anticonvulsant , and
central muscle relaxant actions .
Indications of Bezodiazepines
1) In Anxiety : they are used to treat anxiety .
2) In depression : alprazolam is used to treat mild depression
3) In Insomnia : they are used to treat insomnia .
4) In convulsant : they are used to treat convulsant .
5) In drug withdrawal : diazepam and chlordiazepoxide are used to reduce
alcohol withdrawal symptoms .
Contraindications
1) These are contraindicated in liver diseases .
2) These are contraindicated in certain blood diseases.
3) These are contraindicated in narrow angle glaucoma .
Doses
Diazepam : Tablets 2 , 5, and 10mg and slow releasing capsule 15 mg
Alprazolam : Tablets ( 0.25 , 0.5 , 1 , and 2 mg )
Clonazepam : Injection and tablets ( 0.25 , 0.5 , 1 , and 2 mg )
Lorazepam : 1-4mg /day
Chlordiazepoxide : 10-30mg /day .
Indications of Non-Bezodiazepines
Meprobamate : It is used for managing anxiety . ( 400 mg/ 3 times a day )
Buspirone ( anxipar ) : It is used to treat general anxiety .( 15 -30mg/day )
Contraindication of Non-Bezodiazepines
1) in liver diseases
2) Kidney disorder
3) alcoholism 4) suicidal thoughts

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Anti-Depressant drugs
Definition :
The drugs are used to treat depression are called antidepressant drugs .
Depression : According to WHO Depression is a mental disorder presents with
depressed mood , loss of interest or pleasure , feeling of guilt or low self
confidence , disturbed seep and appetite , low energy , and poor
concentration .
Types of Depression
1) unipolar depression : In this type of depression mood swings always in the
same direction .
2) Bipolar depression : In this type of depression mood swings in two
directions depression and mania . In mania condition the affected person feel
more energetic , and exaggerated self confidence .

Classification Of Antidepressant drugs

1) Monoamine Oxidase Inhibitors (MAOIs): Phenelzine , Isocarboxazid
2) Tricyclic Antidepressant ( Reuptake ( reabsorb) Inhibitor ) : Imipramine ,
Amitiptyline .
3) Selective Serotonin Reuptake Inhibitors(SSRIs) : Fluoxetine , setraline
4) Atypical Antidepressant : Trazodone , Venlafexine .
Monoamine Oxidase Inhibitors (MAOIs): Phenelzine , Isocarboxazid

Pharmacological Actions
These drugs uplift the patient's mood , and he feels more energetic and fresh
after therapy
Indications
these are used to treat unipolar depression , but they are second line drugs
when tricyclic antidepressant fails to manage the condition .
Contraindications
1) MAOI are contraindicated with foods having high level of tyramine like aged cheese , and
topical fruits when ripened e.g. banana , pineapple etc.

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Dose
Phenelzine Sulphate ( Nardil ) : 45-60mg/day . upto 75 mg
Isocarboxazid : 10-30 mg /day , upto 50 mg

Tricyclic Antidepressant ( Reuptake Inhibitor ) : Imipramine , Amitiptyline .

Pharmacological Action
1) ANS : They cause blurred vision , dry mouth , and constipation .
2) CVS : they cause Hypotension ( due to α blocking effect ) and toxic effect
on myocardium .
3) They inhibit the reuptake ( reabsorption ) of neurotransmitter Like
Dopamine , Norepinephrine , serotonin .
Indications
1) they are used to treat depression .
2) they are used to treat migraine, and panic disorder .
Contraindications
1) in having a history of myocardial infarction , heart failure ,
2) narrow angle glaucoma .
Dose
Imipramine :75 mg tablet daily , upto 150 mg a day .
Amitriptyline : same Imipramine .
Selective Serotonin Reuptake Inhibitors(SSRIs) : Fluoxetine , setraline
Pharmacological Action
Its pharmacological action is just like Tricyclic antidepressant but less them .
And it is selective inhibitor of serotonin .
Indications
1) these are given to them who are not able to tolerate TCAs .
2) have a high risk of suicide .
Contraindications
1) in manic phase of Bipolar depression
2) together with anti depressant drugs
Dose
Fluoxetine : initial dose is 20mg /day , up to 30 -40 a day .
Setraline : 50mg / day

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Antipsychotics / neuroleptics
Definition
The drugs are used to treat schizophrenia ( mood -altering ) are called
antipsychotics . It may be called mood stabilizing agents also.
symptoms of schizophrenia hallucination ( in which a person hears , sees,
smell , taste ,or feel things that seems to real but only exit in his mine ) and
delusions.
Classification of Antipsychotics
1) Phenothiazine derivatives : Chlorpromazine
2) Butyrophenones : Haloperidol
3) Rauwolfia Alkaloids : Reserpine
4) Atypical Neuroleptics : Clozapnie , Risperidone
5) substituted Benzamide : Sulpiride
Pharmacological Actions
1) they prevent the excess of dopamine in the brain .
2) In normal individuals , chlorpromazine makes them to loss interest from
surroundings.
3) they act as α adrenergic blocking agents .
4) they cause hypotension.
Indications
1) They are used to treat Schizophrenia .
2) They are used to treat manic depression
3) They are used for controlling aggressive and destructive behavior in
children
4) they are used to control vomiting and Hiccups
Contraindications
1) these are contraindicated in severe allergy .
2) In severe cardiac diseases
3) in narrow angle glaucoma
4) In History of seizure disorder
Doses
Chlorpromazine : 10-100 mg TDS ( thrice a day) Max 800 mg a day )
Haloperidol : 2-20mg/day
clozapnie : 100-300mg/day
Risperidone : 2-8mg/day

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Nootropic Agents / Cognitive Enhancer / Smart drugs

Definition
Nootropics are those substances which incre ase mental functions including :
* Memory * Motivation
*Concentration *Attention
Classification
1) Cholinergic Activators : Piracetam
2) Seratonergics : Theamine
3) Dopaminergic : L- Dopa
Some other examples
Aniracetam , Oxiracetam , Hydergine , Vincamine Meclofenoxate .
How do nootropics work
1) They increase Metabolism in brain .
2) They increase cerebral circulation .
3) They protect brain from Chemical damage .
Indications
1) They are used to treat alzheimer's disease .
2) They are used in those who are suffering from learning and attention
problems,.
3) they are used to increase intelligence , smartness .
4) they are used to treat amnesia .
5) they are used to treat dementia ( abnormalities in to remember , think ,
and decision )
Contraindications
They are contraindicated :
1) in Hypersensitivity 2) In pregnancy 3) in lactation
Dose
Piracetam : 2-3mg /day in divided dose
Hydergine : 4.5- 9 mg / day

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Centrally Acting Muscle Relaxant

Definition
The drugs are used to relax the skeletal muscle by acting on central nervous
system are called " centrally acting muscle relaxants .
They are used to treat spasm and pain in muscles .
Classification
1) Barbiturates : phenobarbitone .
2) Benzodiazepines : Diazepam .
3) GABA derivatives : Baclofen .
4) Mephenesin Congeners : Mephenesin , Meprobamate ,Chlormezanone .
Pharmacological actions
1) Voluntary Muscles : They relax the voluntary muscles by depressing the
CNS.
2) CNS : They depress the CNS , Show sedative effects .
Indications
1) Muscles Spasm : They are used to treat spasm and pain of muscles , and
rheumatic disorders .
2) anxiety and Tension : They are used in treatment of anxiety and tension .
3) Tetanus : They are used in treatment of tetanus in combination with other
medicines .
4) Convulsion : They are also used in treatment of convulsion .
Contraindication
Mephenesin Congeners and Baclofen are contraindicated in hypersensitivity .
Doses
Diazepam : : Tablets 2 , 5, and 10mg and slow releasing capsule 15 mg
Phenobarbitone : 30-120 mg /day in divided dose .
Mephenesin : Ointment as required .
Baclofen : 10-15 mg/day orally

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Opioid ( Narcotic ) Analgesics

Definition
Analgesics are those substances which reduce pain by acting on central
nervous system .
and Opioid Analgesics are pain killers that obtained from opioids .
They reduce pain without disturbing other sensory functions , or without
causing unconsciousness .
Opioid Analgesics may be natural , semi synthetic , or synthetic .
Classification
1) Morphine Analogue : Morphine , dimorphine , Codeine .
2) Synthetic : Pethidine , tramadol Methadone , pentazoci ne , cyclazocine .

Morphine
It is a potent analgesic drug .It is also called gold standard drug for treating
severe pain .It has a high potential for addiction .

Pharmacological Action
1) CNS : It interacts with different types of brain receptors and produces
following actions
a) Analgesia : It reduces pain sensation .
b) Euphoria : It produces a feeling of excitement and happiness .
c) sedation : it causes sleep .
d) vomiting : It stimulates Chemoreceptor Trigger Zone in medulla and
causes
vomiting .
e) respiratory depression : It depresses the respiratory volume , and may
cause death .
f) antitussive : It suppresses the cough reflex by depressing cough center in
medulla .
2) Action on GIT : It causes constipation , It inhibits peristaltic movement .
3) CVS : it causes Vasodilatation .
4) It causes pain in bile duct .
5) it causes urine urgency and difficulty in urination .
6) It prolongs labours .
Indications
1) Analgesia : they are used to relief severe pain .
2) They are used to treat Diarroea .

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3) They are used to relief cough .
4) They are used as pre anaesthetic .
Contraindications
They are contraindicated :
1) In head injury .
2) In Bronchial Asthma .
3) undiagnosed abdominal pain .
4) Chronic lungs disease s
5) in Hypothyrodism .
6) In Hepatic failure.
Doses :
Morphine : (10-15mg oral ) 0.1 - 0.2 mg /kg (4 hours ) as need to manage
pain
codeine : 30 -60 mg
Pethidine : 50-100 mg oral
Tramadol: 50-100 mg oral
Methadone : 2.5-10mg oral
pentazocine : 50-100 mg oral

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Pharmacology Chapter 5
Drugs Acting On Cardiovascular System

Anti-Hypertensive Drugs
Definition
The drugs are used to treat High Blood Pressure are called Anti -hypertensive
Drugs .
Classification
1) Diuretics :
a) Thiazides : Chlorothiazide , Hydrochlorothiazide . chlorthalidone .
b) Potassium Sparing Diuretics : Spironolectone , Amiloride .
c) Loop Diuretics : Furosemide , Bumetanide
2) Angiotensin Converting Enzyme Inhibitors : Coptopril , Ramipril .
3) angiotensin 2nd Receptor Blocker : Losartan , Valsartan .

4) Adrenergic drugs :
a) α blocker : Prazosin , Doxazosin .
b) ß Blockers : Atenolol , Propranolol .
c) α& ß blockers : Labetalol , Carvedilol .
5) Calcium Channel Blockers : Verapamil , Amlodipine , Nifedipine .
6) Vasodilators : Hydralazine .

Diuretics
Diuretics are drugs which promote urination or water loss . these are used as
first line drug for treating Hypertension .
Pharmacological action
a) Thiazides : Chlorothiazide ( 125- 500 mg/ d ) Hydrochlorothiazide ( 12.5 -
50 mg/d)
They work on kidney at PCT of nephron and reduce reabsorption of Sodium
, Potassium and chloride , thus promote the excretion of body fluid and blood
volume .
Excretion of sodium relax the blood vessels also . and lower the blood
pressure .

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b) Potassium Sparing Diuretics : Spironolectone ( 25-50 mg/d) Amiloride ( 5-
10 mg/d)
They work on kidney at DCT of ( nephron ) and reduce reabsorption of
Sodium and chloride , thus promote the excretion of body fluid and blood
volume .
It prevent excretion of Potassium , and correct the potassium loss caused by
Other diuretics .
c) Loop Diuretics : Furosemide ( 20-80mg/d) Bumetanide(0.5- 2 mg/d ) .
They work on kidney at Loop of Henle of nephron and reduce reabsorption
of Sodium , Potassium and chloride , thus promote the excretion of body fluid
and blood volume .
Indication
1) Hypertension 2) Oedema
3) Diabetes 4) Congestive Heart fail ure
5) Hypercalcemia 6) Certain Kidney disease
7) Liver cirrhosis ( damage )
contraindication
1) Hypokalemia 2) Hypotension 3) Hyponatremia
Doses
Chlorothiazide ( 125- 500 mg/ d )
Hydrochlorothiazide ( 12.5 -50 mg/d)
chlorthalidone .( 12.5 -50 mg/d)
Angiotensin Converting Enzyme Inhibitors : Coptopril ( Ramipril .
These are commonly used as first line antihypertensive drugs .
Pharmacological action :
1) Vasodilation , and lower SBP and DBP .
2) Increase Blood Flow ( Renal , Coronary etc. )
3) It prevent the enzyme from converting angiotensin to angiotensin 2nd .
Indications :
They are used to treat following disease
1) Hypertension 2) congestive Heart failure .
3) Myocardial Infarction .
4) Diabetic nephropathy ( Nerve Damage due to Diabetes )

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Contraindication
They are contraindicated in :
1) angioedema ( painless swelling in mouth ,lips , throat , nose etc. )
2) Hypersensitivity to ACE Inhibitors .
3) in single kidney person .

Doses
Coptopril ( 25-100 mg /d )
Ramipril ( 2.5 -20 mg/d )
Losartan ( 25- 100 mg/ d)
Valsartan ( 80 -320 mg/ d )
Note : angiotensin 2nd Receptor Blocker are just like Angiotensin Converting Enzyme
Inhibitors in respect to Indication , contraindication s .
Adrenergic drugs
a) α blocker : Prazosin , Doxazosin .
These are not preferred for normal Hypertension , they are used to treat
special conditions .
Pharmacological Actions
1) Effect on CVS : Hypotension , fall in BP
2) on Eye : miosis
3) nasal congestion
4) Inhibit ejaculation
5) increase intestinal motility .
Indication
1) to treat hypertension
2) In congestive heart failure .
3) In migraine
Contraindication
Alpha blockers are contraindicated in
1) Hepatic and renal disease
2) peptic ulcer
3) any drug allergy
4) coronary artery disease

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Doses
Prazosin ( 1-15 mg/d )
Doxazosin .( 1-20 mg/d )
b) ß Blockers : Atenolol , Propranolol .
They are effective in all grades of Hypertension
Pharmacological action
1) decrease the heart rate
2) Bronchodilation
3) Vasodilation .
4) Lowers Blood pressure .
Indication
To treat :
1) Hypertension 2) Angina pectoris
3) Cardiac arrhythmias 4) Migraine
5) Anxiety 6 ) parkinson's disease
Contraindication
They are Contraindicated in :
1) nasal Congestion 2) headache
3) depression 4) Hepatitis
Doses
Atenolol : ( 25 - 100mg daily )
Propanolol : ( 80 - 240 mg 12 hourly )

c) α& ß blockers : Labetalol , Carvedilol .

Pharmacological action
1) Lower heart rate
2) vasodilation
3) Erectile dysfunction
4) Lower BP .

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Indications
To treat :
1) Hypertension 2) Angina pectoris
3) Cardiac arrhythmias 4) Migraine
5) Anxiety 6 ) parkinson's disease
7) glaucoma 8) MI
Contraindication
They are contraindicated in :
1) Asthma 2) Bronchitis 3) Severe Liver disease
4) Slow heart rate
Doses
carvedilol (12.5- 50 mg/d )
Labetalol (200-800 mg/d )

Calcium Channel Blockers(CCBs) : Verapamil , Amlodipine , Nifedipine

They are commonly used to treat Hypertension as first line drug . They can be
used safely in patients having asthma , Hyperlipidemia , diabetes mellitus and
renal dysfunction .
Pharmacological Actions
1) relax blood vessels
2) Slows electrical activity in heart and slows heart rate .
Indications
1) They can be used in patients whom ß blockers are contraindicated .
2) Angina pectoris
3) Hypertension 4) arrhythmias
Contraindication
They are contraindicated in :
1) Severe Asthma
2) with beta blockers 3) in patients having hypersensitivity to it

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Doses
Verapamil ( 120-360 mg /d )
Amlodipine ( 2.5- 10 mg/d )
Nifedipine ( 30-60 mg/d )

Vasodilators : Hydralazine . Sodium Nitropruside

They may be used in emergency condition because of onset of action . They
are safe in pregnancy .
Pharmacological Actions
They relax the wall of blood vessels directly .
Indications
they are used hypertension .
contraindications
they are contraindicated in Heart failure and coronary artery diseases .
Doses
Hydralazine ( 25-100mg /d)
Sodium Nitropruside ( 0.25-1.5mcg/kg/min i.v. )

Anti Anginal Drugs

Definition
The Drugs are used to treat Angina pectoris are called anti anginal Drugs
Angina is referred to chest pain due to low or no blood supply to the Heart
muscles .
Classification
1) Vasodilators :
a) Nitrites and nitrates : Isosorbide dinitrate Nitro -glycerine .
b) Calcium Channel Blockers : Verapamil , amlodipine , Nifedipine
c) Potassium Channel Opener : Nicorandil
2) ß adrenoceptor antagonist ( ß blockers ) :
Atenolol , Prapranolol , Metoprolol .
Nitrites and nitrates : Isosorbide dinitrate Nitro -glycerine .
These are commonly used in angina pectoris .

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Pharmacological Actions
1) dilation : they dilate the coronary arteries .
2) Blood Flow : Reduce oxygen demand by increasing blood flow to the heart
muscles .
3) They dilate peripheral Blood vessels and decrease the load of heart .
Indications
1) They are used to angina
2) in MI
3) Chronic heart failure
Contraindications
they are contraindicated in
1) cardiomyopathy ( disease of heart muscles )
2) Close angle Glaucoma
Doses
Isosorbide dinitrate : ( 5-10 mg sublingual ) ( 20-40 mg sustained release oral
)
Nitro Glycerine : ( 0.5 mg sublingual ) ( 5 -15 mg oral ) ( 5-20 ug /min i.v. )
Potassium Channel Openers: Nicorandil (5-20mg/ BD)
It is used for preventing and treating chronic stable angina pectoris .
Pharmacological Actions
It Activates the Potassium Channels and cause Vasodilation of arteries and
large coronary arteries .
Indication
It is used for preventing and treating chronic sta ble angina pectoris .
Contraindication
They are contraindicated In :
1) hypotension
2) Low blood volume
3) pulmonary oedema
4) left ventricle failure

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Anti- Arrhythmic Drugs

Definition
The drugs are used to treat Arrhythmia are called Anti - Arrhythmic Drugs .
Arrhythmia is improper beating of heart , whether irregular , too fast ,or too
slow .
Classification
1) Sodium Channel Blocker : Quinidine , Procanamide , Lidocaine , Phenytoin .
2) beta blockers : Atenolol , Propranolol
3) potassium channel blockers : amiodaron , bretylium .
4) Calcium Channel Blockers : Verapamil , Nifedipine .

Sodium Channel Blocker : Quinidine , Procanamide , Lidocaine , Phenytoin .

Pharmacological Actions
1) They block mayocardial Na + Channels .
2) they slow down heart rate .
Indication
They are used to treat :
1) arrhythmia
2) quinidine is used to treat malaria .
Contraindications : They are contraindicated in :
1) Hypersensitivity 2) Coronary artery diseases
3) Cardiogenic shock )( sudden unability of heart to pump enough blood to
meet body 's need )
4) Severe hepatic disorder

Doses
Quinidine : ( 100-200mg/tds ) oral
procainamide : ( .5-1 g/d) oral

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Potassium Channel Blockers : amiodaron , bretylium .

Pharmacological Actions
1) They prolong the duration of action potential .
2) They decrease heart rate .
3) they block potassium channel in myocardium .
Indications
They are used to treat :
1) atrial fibrillation ( irregular or rapid heart rate )
2) Ventricular fibrillation .
Contraindications
1) Bradycardia 2) congestive heart failure .
3) Bronchospasm
Doses
Amiodaron ( 400-600mg/d) orally
Sotlol ( 40-80mg/bd ) orally .

Drugs Used In Atherosclerosis

Atherosclerosis is Formation of plaque inside the Arteries which reduce the supply of blood
, oxygen , and nutrients to other body parts .
Classification
1) HMG-CoA Reductase Inhibitors ( Satins ) : Atorvastatin , Lovastatin .
2) Bile Acid Sequestrants ( Resins ) : Cholestyramine , Colestipol .
3) Fibric Acid Derivatives ( Fibrates ) : Clofibrate , Fenofibrate .
4) Triglyceride Synthesis and lipolysis Inhibitors : Nicotinic Acid , Probucol .
5) Others : Omega 3 fatty acids .
HMG-CoA Reductase Inhibitors ( Satins ) : Atorvastatin , Lovastatin .
Statins are most effective and best drugs to treat Hyperlipidemia . They are usually given in
evening , Because cholesterol Biosynthesis occurs mainly in night . 10-20mg/d

Pharmacological Action
1) They slow or inhibit the production / synthesis of cholesterol .
2) They decrease cholesterol , LDL ,VLDL In plasma .
3) They increase HDL in plasma .

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4) They prevent deposition of lipids in blood vessels ( formation of plaque )

Indication
1) They are used to treat hyperlipidemia .
2) They are used to reduce the risk of MI .
3) They are used to remove plaque in blood vessels .

Contraindication
They are contraindicated in :
1) liver disease 2) In Pregnant and lactating woman .
3) in Whom is Hypersensitivity to it .

Doses :
Atorvastatin (10-20mg/d)
Lovastatin ( 20-80mg/d)
Bile Acid Sequestrants ( Resins ) : Cholestyramine , Colestipol .

Pharmacological Action
They bind with bile and prevent reabsorption of bile from GIT .
Indications
1) These are used to maintain or reduce cholesterol level .

Contraindication
they are contraindicated in patients have complete bile absorption

Dose
Cholestyramine ( 4 g / d in starting in divided dose )
Colestipol ( 2-16 g /d in divided dose )

Fibrates ( fibric Acid Derivatives ) : Clofibrate , Fenofibrate .

Pharmacological Actions
1) They reduce Blood LDL and triglyceride .
2) They increase HDL in blood .
3) they reduce cholesterol level .

Indication
1) These are used to treat Type 3 hyperlipidemia ( due to genetic disorder)
2) These are used with Statins in patients with high risk of CHD( coronary Heart Disorder )

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Contraindications
1) In Liver disorder 2 ) gall bladder disorder .

Doses :
Clofibrate ( 1.5 - 2 g /d in divided dose )
Fenofibrate ( 50-150mg/ d ) .
Triglyceride Synthesis and lipolysis Inhibitors : Nicotinic Acid , Probucol .

Pharmacological Actions
1) These agents inhibit either the synthesis of triglyceride or lipolysis ( break down of lipids )
2) They reduce the level of LDL and VLDL in blood .
3) They prevent deposition of lipids in blood vessels ( formation of plaque ) .

Indication
they are not used usually due to a lot of serious adverse effects .
Drugs used in congestive Heart failure

Congestive Heart Failure is inability of heart to pump enough B lood to meet

the minimum body needs .
Some causes :
1) Narrowing of arteries 2) Congenital Heart defects .
3) Infection or defect in heart valve 4) Myocarditis (Infection of
heart muscles )
5) cardiomyopathy ( disease of heart muscl es ) .
Classification
following drugs are used in the treatment of CHF :
1) drugs with Positive Inotropic Effects :
a) cardiac glycosides : Digoxin , Digitoxin , Oubain .
b) Bipyridines Or Phosphodiestrase Inhibitors : amrinone , Milrinone .
c) ß adrenergic agonist : Dobutamine , Dopamine .
2) Drugs without Positive Inotropic Effects :
a) Diuretics : Chlorothiazides , Furosemide , spironollectone .
b) ACEI : captopril , ramipril .
c) ß Blockers : Atenolol , propranolol .
d) vasodilators : nitrates , Hydralazine .

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Cardiac Glycosides : Digoxin , Digitoxin , Oubain .
Cardiac Glycosides also known as Digitalis , they strengthen the heart muscles
and increase the contraction force of heart .

Pharmacological Action
1) They increase the contraction force of heart .
2) Administration in low dose , increase the vagal tone , which cause
Bradycardia .
3) they Increase the blood circulation and increase the blood flow to the
kidney , this increase urination and relieves oedema in patients with cardiac
oedema .
4) They stimulate the chemoreceptor trigger zone in medulla and cause
Nausea , Vomiting .
5) They cause blurred vision
6) they cause Photophobia .

Indications : They are used to treat :

1) Congestive heart Failure . 2) cardiac arrhythmias .
Contraindications : They are contraindicated in
1) Hypokalamia 2) severe renal disease
3) severe hepatic disease 4) Vantricular Tachycardia
5) Thyrotoxicosis .

Doses
Digoxin ( 0.25-0.5 mg/d )
Bipyridines Or Phosphodiestrase Inhibitors : amrinone , Milrinone .

Pharmacological Action
1) They exert positive Inotropic Effect .
2) They cause Vasodilation
3) They Increase CO ( cardiac output )
4) They decrease Peripheral vascular resistance and After load .

Indications
1) They are used to treat severe CHF for short term .
contraindications :

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1) in hypersensitivity
2) pulmonic Valve disease 3) aortic disease .
Dose
Milrinone : ( 0.375mcg/kg/min ) maximum 1.13 mg kg /d .
Amrinone ( 5-15mcg /kg/min ) maximum 10mg /d .

ß adrenergic agonist : Dobutamine , Dopamine .

The heart has ß 1 and ß 2 adrenoceptors , when these receptors are activated
, heart beat , contractility of hear t muscles and cardiac output increased

Pharmacological Action :
1) Increase positive Inotropic
2) Increase heart rate
3) Increase cardiac Output .

Indications
1) They are used to treat Congestive heart failure .
2) circulatory Shock

contraindications
1) MI 2) Unstable Angina 3) severe Hypertension
4) Arrhythmias 5) myocarditis 6) Hypokalamia .

Doses
Dobutamine ( 2.5-10mcg/kg/min) maximum 40 mcg /kg In divided dose
Dopamine ( 0.2-1mg /kg/min ) maxm. 300-1200 mg in divided dose .

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Drug Therapy For Shock

Shock is a medical Condition in which blood perfusion to the tissues
decrease , and cause cell injury and improper function of cells .
Treatment of Involves :
1) primary therapy : By this therapy causes of Shock are corrected like
haemorrhage , Infection , MI , Allergic reaction etc.
2) Secondary therapy : This therapy is used to correct Hemodynamic( blood flow
and the system through it flows ) disturbance . Following type o f drugs are
used for correcting hemodynamic disorder :
1) Sympathomimetic amines 2) corticosteroids
3) Dextrans 4) Oxygen
5) Cardiac glycosides 6) glucagon

Sympathomimetic amines
Some Important Adrenergic Drugs used in Shock are
1)Nor- adrenaline 2)Adrenaline 3) Dopamine 4) Dobutamine .

Nor- adrenaline
Pharmacological Actions
1) It increase the perfusion pressure and Cardiac Output ( CO ) .
2) It stimulate α 1 receptor and cause peripheral Vasoconstriction ,
3) Increase blood pressure
4) It stimulates ß 1 receptor and produces Positive Inotropic Effect at higher
dose .
Indications
1) In patients suffering from low peripheral resistance shock .
2) in Acute Hypotension
Contraindication
No significant contraindication is found
Dose
( 2-4ug/min i.v. infusion )
Adrenaline
Pharmacological Action
1) it increase Cardiac Output
2) decrease renal blood flow
3) It increase Total Peripheral Resistance . ( TPR )

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Indications
1) to treat Anaphylactic shock ( Shock due to allergic reaction in which
blood pressure drops sudden )
Contraindication
1) In High peripheral resistance shock .
2) in cardiac dilation
Dose
( 0.2- 0.5mg s.c./i.m.)
Dobutamine
Pharmacological Action :
1) Increase positive Inotropic Effect
2) Increase heart rate
3) Increase cardiac Output .
Indications
1) it is used to treat shock due to Congestive heart failure .
contraindications
1) MI 2) Unstable Angina 3) severe Hypertension
4) Arrhythmias 5) myocarditis 6) Hypokalamia .
Doses
Dobutamine ( 2.5-10mcg/kg/min) maximum 40 mcg /kg In divided dose

Dopamine
Pharmacological Action :
1) Increase positive Inotropic Effect
2) Increase heart rate
3) Increase cardiac Output .
Indications
1) it is used to treat septic shock ( due to infection ) , Traumatic shock .

2) to teat Congestive heart failure .

contraindications
1) MI 2) Unstable Angina 3) severe Hypertension
4) Arrhythmias 5) myocarditis 6) Hypokalamia .
Doses
Dopamine ( 0.2-1mg /kg/min ) maxm. 300-1200 mg in divided dose .

Corticosteroids
Corticosteroids are Hormones produced by adrenal gland ,and also
synthesized ,

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Pharmacological Actions
1) Suppress all type of Allergy .
2) Induce Inotropic effects
3) decrease peripheral resistance
4) Prevent leakage of capillaries .
Indication
It is used in septic shock
It is used to treat allergic disorders
It is used in asthma .
it is used to treat inflammation .
Contraindication : they are contraindicated in
1) Live attenuated vaccine 2) In fungal Infection
3) Diabetes mellitus 4) Glaucoma
Dose
( 2.5-10mg/kg/d )
Oxygen
In shock condition the blood oxygen level should also be monitored It is called
The arterial PO 2 ( partial Pressure of oxygen ) It means amount of oxygen
dissolved in blood .
Oxygen supplementation is used fo r :
1) It increase cardiac output .
2) Oxygen level of tissues can be improves easily .
And it is used in following condition
1) in Hypoxia
2) in Carbon monoxide Poisoning .
3) in severe asthma .
4) when Arterial PO 2 falls below 60mm Hg .

Glucagon
It is a type of hormone produced by pancreas which convert Glycogen into
glucose in liver .

Pharmacological Action
1) It increase contraction force of heart and CO .
2) It improves the Hemodynamic condition of patients .

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Indications
1) In patients having shock due to heart failure .
2) in Hypoglycemia
Contraindication
1) cardiac arrhythmia
2) Hyperglycemia
Doses ( 0.1 ml . s.c. )

Dextrans
Dextrans are plasma volume Expanders . These are also called NS , saline , RL
etc.
High molecular weight Dextran ( 1,10,000 Mol.wt. ) is used in hypovolemic
Shock

Uses
1) it is used in shock , because it improves tissues perfusion .
2) it helps in flow .
3) To increase Blood volume .
4) In dehydration
5) diarrhea

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Pharmacology chapter 6
Drugs Acting on blood and Blood forming Organs

Haematologic System :
The system responsible for formation of blood is called Haematlogic System .
Haematopoiesis :
The process of blood forming is called Haematopoiesis .
Haemtinics
The drugs are used to treat Anaemia are called Haematinics . or the
substances are used to treat deficiency of Iron are called haematinics .
following Types f Drugs are used as Haematinics :
1) Iron :
Ferrous Sulphate , Ferrous Fumarate , Ferrous Gluconate , Ferric ammonium
Citrate .
2) Folic acid
3) Cobalamin .

1) Iron :
Ferrous Sulphate , Ferrous Fumarate , Ferrous Gluconate , Ferric ammonium
Citrate .
Pharmacological Action
1) It play an important role in formation of haemoglobin .
2) It involves in formation of some Hormone like Thyroid Hormone .
Indication
1) it is used to treat anaemia .
2) It is used to treat iron deficiency .
No Significant Contraindication is found .
Drugs Does
Ferrous Sulphate 0.3g Tds
Ferrous Fumarate 0.2g Tds
Ferrous Gluconate 0.6g tds .
Ferric Ammonium Citrate 1.0 g tds .

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2) Folic Acid 3) cobalamin
Function
1) B 9 helps the body in metabolism of proteins and in their uses .
2) B 9 and B 12 helps in formation of RBCs .
3) B 12 helps in maturation of RBCs .
Indication
1) they are used to treat anaemia .
2) they are used to treat megaloblastic anaemia .
3) they are used to treat Pernicious anaemia ( in this condition the body
can't absorb enough vitamin B12 and leads to low formation of RBCs )
Dose
Folic Acid : 0.1 -.08 mcg or 1 mg daily .
B12 : 1mg in pernicious anaemia .

Anticoagulants
The drugs prevent coagulation of blood are called anticoagulants .
Classification
1) Injectable Anticaogulants : Heparin , Ancrod , Lepirudin .
2) Oral Anticaogulants :
a) Coumarin : Bishydroxy Coumarin ., Warfarin Sodium , Acenocoumarin .
b) Indandione Derivatives : Phenindion .
Pharmacological Action
1) Heparin : It prevent blood clotting in vivo ( inside the body ) as well as in
Vitro .
It Activates antithrombin Ⅲ , which inactivates factors Ⅸ , and Ⅹ . in this
way coagulation is prevented .
2) Coumarin : Coagulation factors Ⅱ , Ⅶ , Ⅸ and Ⅹ are present in inactive
form , until they are carboxylated . These drugs act on Vitamin K and prevent
the synthesis of chemical that carboxylate these factors .

Indications
1) in unstable angina .
2) to prevent coagulation in Heart fa ilure .
3) to prevent pulmonary embolism .
4) to prevent clotting during open heart surgery .

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Contraindications
These are contraindicated In :
Recent trauma , recent surgery , recent abortion , recent stroke , severe
Hypertension , severe Diabetes , severe liver damage , peptic ulcer , and
bleeding disorder .
Doses
Drugs Name Does
Heparin 5000-10000 unit /ml i.v
Warfarin 5-10 mg /d

Anti Platelet Agents

The drugs prevent platelet aggregation are called Anti - Platelet drugs .
Classification
1) Thromboxan ( TxA2 ) synthesis Inhibitors : Low dose of Aspirin , Dazoxiben
.
2) Phosphodiesterase Inhibitors : Dipyridamol .
3) ADP - Induced Platelet Aggregation Inhibitors : Ticlopidine , Clopidogrel .
4) Glycoprotein Ⅱb / Ⅲa receptor Blockers : Tirofiban , Eptifibatide .
Pharmacological Action
1) Thromboxan ( TxA2 ) synthesis Inhibitors : Low dose of Aspirin . acts on
Cox 1 and reduces the production of TXA2 . ( this TxA2 causes platelet
aggregation )
2) Phosphodiesterase Inhibitors : Dipyridamol .
It increases the concentration of cyclic adenosine monophosphate ( cAMP)
levels and it prevents platelet aggregation .
3) ADP - Induced Platelet Aggregation Inhibitors : Ticlopidine , Clopidogrel . It
blocks the P 2 Y 1 2 receptor of platelet , which activates the platelets and
cause aggregation .
4) Glycoprotein Ⅱb / Ⅲa receptor Blockers : Tirofiban , Eptifibatide .
They block Glycoprotein Ⅱb / Ⅲa receptor of platelet which activates
platelet aggregation .
Indications
These are used to prevent arterial thromboembolis In following situations :

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1) unstable angina 2) Acute MI 3) in Post MI Patients
4) Cerebrovascular Diseases 5) Prosthetic heart valves ( artificial valve )
Contraindications
These are contraindicated In :
Recent trauma , recent surgery , recent abortion , recent stroke , severe
Hypertension , severe Diabetes , severe liver damage , peptic ulcer , and
bleeding disorder .
Dose
Aspirin 75-150mg /d oral
Dipyridamol 150-300 mg /d
Ticlopidine 250- 500 mg /d
Tirofiban 0.4mcg/kg/min i.v.

Thrombolytic Drugs ( Fibrinolytics)

Definition
The drugs are used to dissolve the blood clotting are called Thrombolytic
drugs .
Examples :
Alteplase , Streptokinase , Urokinase etc .
Pharmacological Actions
These drugs dissolve the blood clotting by activating or converting
plasminogen into plasmin ( an proteolytic enzyme ) which lyses ( breaks down)
the fibrin and fibrinogen , and dissolves the clots .
Indication
These are used for dissolving the clotting anywhere .
Contraindications
These are contraindicated In :
Recent trauma , recent surgery , recent abortion , recent stroke , severe
Hypertension , severe Diabetes , severe liver damage , peptic ulcer , and
bleeding disorder .
Dose
Alteplase For MI 15 mg i.v. For pulmonary embolism 100mg i.v.
Streptokinase 250,000 IU /2ml
Urokinase 4400 IU/kg

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Pharmacology Chapter 7
Drugs Acting On The Respiratory System

Bronchodilators
Definition
The drugs dilate ( widen ) the diameter of bronchi are called Bronchodilators .
Classification

1) sympathomimetic Agents ( ß 2 Blockers )

a) short acting agents : Salbutamol , Terbutaline .
b) Long acting agents : Salmeterol , fenoterol , Formeterol .
2) Xanthine derivatives : Thyeophyline , aminophyline .
3) Anti-Colinergic agents : Ipratropium Bromide , atropine .
Pharmacological Actions
1) sympathomimetic Agents ( ß2 Blockers ) : Salbutamol , Terbutaline .
Salmeterol , fenoterol , Formeterol .
1) they dilate the bronchi .
2) increase mucociliary clearance ( it is a defense mechanism of lungs in
which mucus and harmful foreign substances are moved out of lungs ) .
3) they inhibit the mediators , which are released by mast cells and cause
problems ( Histamine , PG ) .
Indications
1) They are used in acute bronchospasm .
2) they are used in the treatment of asthma .
3) they are used in bronchitis
4) they are used in emhysema .
Contraindications
1) Hypertension
2) Coronary arteries disease .
3) Uncontrolled arrhythmias .
4) previous history of stroke .
Does
Salbutamol 2-4 mg oral , 0.25-.5 mg i.m./s.c. 100-200 mcg
Terbutaline inhalation
5 mg oral .

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Salmeterol 50-100 mcg by inha.
Formeterol . 12-24 mcg by inhal. bd .

2) Xanthine derivatives : Thyeophyline , aminophyline .

Pharmacological .A .
1) CNS : they increase the CNS performance .
2) CVS : they have positive inotropic effect .
3) Smooth muscles : they relax smooth muscles .
4) Stomach : they increase the acid and pepsin i n the stomach .
5) they increase the contraction force of skeletal muscle .
6) They decrease the function of mast cells .

Indications
1) In acute attack of asthma .
2) in mild to moderate bronchspasm .
3) In COPD .
Contraindications
1) Hypertension 2) Cardiovascular Disease
3) In Cystic Fibrosis ( it affects the cells the produce mucus , sweat and
digestive juice .)
4) Hyperthyrodism . 5) Peptic ulcer . 6) Seizure disorder .
7) hepatic disorder 8) Pregnancy .
Doses
Thyeophyline 100-300mg TDS oral
aminophyline 250-500 mg / oral

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Anti-muscarinic Agents

The anticholinergic drugs that block the action of ACh on muscarinic receptors
are called Anti-muscarinic agents . example . Atropine , Apratropium
bromide .
It is most common anti muscarinic agent . And blocks the all types of
muscarinic receptors .
Pharmacological Action
1) CNS : mild stimulation
2) Eye : Mydriasis
3) CVS : It cause bradycardia initially and then tachycardia .
4) Respiratory System : bronchodilation
5) secretion : secretions of sweat , saliva , and gastric are reduced .
6) GIT : relaxation , decrease peristaltic movement so it used as antispasmodic
and anti diarrhoeal drug .

Indication
1) for dilation of pupil .
2) Pre - Anaesthetic
3) in bronchial Asthma and COPD .
4) in hypersalivation .
5) to treat diarrhoea
6) as antidote for organophosphorus poisoning .
7) to treat parkinsonism .
Contraindication
1) in glaucoma condition .
2) in infants suffering from Down' syndrome ( delay in development of body
and brain )
3) in patients are hypertensive with atropine .
Dose :
Atropine : It is given IV , IM and SC, routes .
0.4-0.6mg for preoperative and pre anaesthetic ,
1% solution in eye drop for mydriasis .
Ipratropium Bromide :
40-80 mcg by inhalation .

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Expectorant
The drugs are used to treat protuctive cough ( with sputum ) are called
expectorants .
Classification
1) Directly acting ( secretion enhancer / expectorant ) : Sodium citrate ,
sodium acetate , potassium citrate , potassium acetate , Potassium iodide ,
Guaiphensine , Tolu balsam , Vasaka , Terpine Hydrate , ammonium chloride ,
2)Mucolytics : Bromhexine , ambroxol , Acetyl Cystieine , carbocisteine .
Pharmacological Actions
1) Directly acting ( secretion enhancer ) : Sodium citrate , sodium acetate.
They increase the volume of bronchial secretion and decrease the viscosity of
sputum , and sputum removed out easily .

Indication
They are used to treat productive cough .

Contraindication
These drugs should be used carefully in pregnancy and lactation .
Dose
Sodium citrate , sodium acetate , 0.3-1.0 g TDs
potassium citrate , potassium acetate ,
Guaiphensine 100-200mg TDS
Tolu balsam 0.3-0.6 g TDS
Vasaka , 2-4ml TDS
ammonium chloride , 50-200mg TDS

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Mucolytics
Definition
The drugs dissolve the thick mucus ( sputum ) are called Mucolytics .
Examples : Bromhexine , ambroxol , Acetyl Cystieine , carbocisteine .
P.A .
These drugs break the thick , strong sputum and decrease the viscosity of
sputum , and sputum comes out easily .
Indication
1) they are used in patients having difficulty in coughing out the secretions .
2) They used for clearing secretions before diagnosis .
3) in Tb 4) Pneumonia 5) COP D
Contraindication
These drugs should be cautiously in acute bronchospasm , peptic ulcer ,
Esophageal varices .
Dose
Bromhexine , 8 mg TDS
ambroxol , 15-30 mg TDS
Acetyl Cystieine , 200-600 mg oral TDS
carbocisteine 250-750 mg TDS

Anti-Tussive Agents
Definition
The drugs are used to Non- Productive Cough are called anti -tussive drugs .
Classification
1) Centrally acting Anti- tussive
a) Opioids / Narcotics : Codeine , Pholcodine , Ethylmorphine .
b) Non- Opiods / Non- Narcotics : Noscapine , Dextromethophan ,
Chlophedianol .
2) Anti-Histaminics : Chlopheniramine , Diphenhydramine , Promethazine .
Pharmacological Action
Centrally acting Anti- tussive
1) They inhibit reflex by suppressing the cough center in CNS ( medu lla
2) Constipation
3) CNS depression

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Indication
1) In cough cold 2) In mild to moderate pain .
3) Diarrhoea .
Contraindication
No significant contraindications other than hypersensitivity .
Doses
Codeine 15-30 mg TDS
Pholcodine 10-15 mg BD
Ethylmorphine 10-30 mg TDS
Noscapine 15-30 mg TDS
Dextromethophan , 10-20 mg TDS
Chlophedianol .
10-20 mg TDS

2) Anti-Histaminics : Chlorpheniramine , Diphenhydramine , Promethazine .

Pharmacological Action
1) They cause CNS depression ,
2) sedation
2) they have anti- allergic action
3) They cause dryness of mouth , blurring of vision , constipation .
Indication
1) In Common Cold and cough
2) In Allergic Diseases
3) In Parkinson's disease
4) as antiemetic .
Contraindication
1) in Hypertension 2) Cardiovascular Diseases
3) Urinary retention . ( difficulty in urination and completely empting ) .

Doses
Chlorpheniramine 2-4 mg oral
Diphenhydramine 25-50 mg oral
Promethazine 25-50 mg oral

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Pharmacology Chapter 8
Drugs Acting on the gastrointestinal Tract

Anti- Ulcer Drugs

Definition : The Drugs are used to treat ulcer / Sore are called anti ulcer drugs .
Ulcer : A sore ( wound ) develops on the lining of the oesophagus , Stomach , or small
intestine .
If ulcer is in stomach it is called Gastric Ulcer , if in Duodenum it is called Duodenal Ulcer ,
and both type of ulcer is called Peptic Ulcer .
Classification
1) Anti-secretory Agents ( reduce gastric acid secretion )
a) H2 Antagonists : Cimetidine , Ranitidine .
b) Proton Pump inhibitors : Omeprazole , pantoprazole , Lansoprazole, raeprazole .
c) Anti-cholinergic drugs : pirenzepine .
d) prostaglandin Analogues : Misoprostol , Enprostil .

2) Antacids : ( Neutralize gastric acid)

a) Systemic : Sodium Bicarbonate , Sodium citrate .
b) Non- Systemic : Magnesium Hydroxide , aluminium Hydroxide Gel , Magaldrate ,
Calcium Carbonate .
3) Ulcer Protectives : Sucralfate and Colloidal Bismuth Subcitrate ( CBS)
4) Ulcer Healing Drugs : carbenoxolone sodium .
5) Anti- Helicobacter pylori Drugs : amoxicilin , Metronidazole , Clarithromycine .
H2 Antagonists : Cimetidine , Ranitidine
Pharmacological Action :
These drugs bind to Histamine H2 receptors on Gastric parietal cells and reduce the
histamine production . Histamine is a chemical which stimulate the stomach cells to
produce acid .
They reduce gastric acid secretion .
Indications
1) To treat peptic ulcer .
2) To treat dyspepsia ( indigestion )
3) Gasroesophageal Reflux Disease ( GERD)
4) With NSAIDs to prevent Ulcer .
Contraindication ( No Significant Contraindications )
Proton Pump inhibitors : Omeprazole , pantoprazole , Lansoprazole, raeprazole .

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Pharmacological Action :
PPIs reduces the acid production by blocking the enzyme in the wall of the stomach which
produce acids .
They reduce gastric acid secretion .
Indications
1) To treat peptic ulcer . 2) To treat dyspepsia ( indigestion )
3) Gasroesophageal Reflux Disease ( GERD)
4) With NSAIDs to prevent Ulcer .
5) In combination with antibiotics , to eradicate helicobacter pylori .
6) to relief Heart burn .
Contraindication
All PPIs are classified as Category B drugs by the US Food and Drug Administration ( FDA) ,
Which means that they are safe to use during pregnancy .
Anti-cholinergic drugs : pirenzepine .
Pharmacological Action :
It reduces gastric acid secretion and reduces muscle spasm .
Indication 1) it is used in peptic ulcer .
Contraindication In pregnancy .
prostaglandin Analogues : Misoprostol , Enprostil
Pharmacological action
Like gastric mucus they also provide a protection against gastric acids and inhibit the acid
secretion .
Contraindication
In pregnancy .
Antacids
Systemic : Sodium Bicarbonate , Sodium citrate .
Non- Systemic : Magnesium Hydroxide , aluminium Hydroxide Gel
Pharmacological Action
They neutralize the gastric acid .
Indications
1) they are used in peptic ulcer .
2) they used in GERD .
3) in Constipation 4) in Dyspepsia
Contraindication
should be given to patients with renal or heart failure .
Ulcer Protectives : Sucralfate and Colloidal Bismuth Subcitrate ( CBS) .
Pharmacological Action
They make a protective layer upon the ulcer and protect it from further damage of HCL .

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Indication
1) they are used in peptic ulcer.
Note : sucralfate is effective under acidic condition , thus an antacid should not taken 30
minutes before or after sucralfate dose .
Contraindication
1) Hypersensitivity to it
2) GI bleeding history .
Ulcer Healing Drugs : carbenoxolone sodium .
These drugs are used to heal the ulcer .
Indication
1) in peptic Ulcer 2) Gastric Ulcer
3) It is used along with antacids and alginic acid to treat GERD .
Anti- Helicobacter pylori Drugs : amoxicilin , Metronidazole , Clarithromycine
Pharmacological action
these are antibiotics , These drugs destroy the Helicobacter pylori
They are used to treat different types of bacterial infection .
Contraindication
Amoxicilin : In patients with previous history of allergic reaction . In hepatic dysfunction .
Dose
Cimetidine 0.02g tab.
Ranitidine 0.15 g tab.
Omeprazole 0.02g caps.
Lansoprazole 0.03 g caps
pantoprazole 0.04 g tab
Pirenzepine 0.25-0.50 g tab.
Sucralfate 10ml four time a day .
Carbenoxolone 20-50 mg 4 time a day

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Anti - Emetics
The drugs are used to treat vomiting and nausea are called anti-emetics
Classification
1) Anti Cholinergic drugs : Hyoscine , Dicyclomine .
2) H1 Anti-Histaminics : Promethazine , Diphenhydramine , Cyclizine .
3) Neuroleptics : Chlorpromazine , Haloperidol .
4) Prokinetic drugs : Metoclopramide , Domperidone .
5) 5-HT3 Antagonist : Ondansetron , Granisetron .
6) Adjuvant Anti-emetics : Dexamethasone , Benzodiazepines , Canabinoids .
Pharmacological Action
They work on nervous system and block the signaling to the vomiting center " Medulla " .
Indications
1) They are used to treat Vomiting
2) to treat nausea .
3) to treat Motion sickness .
4) To treat post anaesthetic nausea and vomiting .
5) Morning sickness ( vomiting during pregnancy , in first three months ) .
Contraindications
1) Hyoscine and dicyclomine are contraindicated in glaucoma , or tendency towards
glaucoma .
2) H1 Anti-Histaminics are contraindicated in those are suffering with lungs problem like
asthma .
3) Prokinetic Drugs should be used carefully in liver disease and in pakinson's disease .
Doses
Hyoscine 200-600mg ( SC)
Dicyclomine 40 mg
Promethazine 25 mg .
Clorpromazine 25 mg
Domperidone 10 mg
Ondansetron 8-16 mg in divided dose

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Laxative ( Purgative )
Definition : The drugs are used to treat constipation are called laxative .These drugs make
the stool soft and increase the bowel movement and ease to Defecate ( to pass stool) .
If the laxatives are taken in high dose and cause diarrhoea( watery stool) it is called
purgative .
Classification
1) Bulk Forming - Dietary fiber : Bran , Psyllium , Ispagula , Methylcelulose .
2) Stool softener : Docusates ( DOSS) , Liquid paraffin.
3) stimulant : Senna , Cascara sagrada , castor oil .
4) Osmotic Purgatives :Mag. sulphate . Mag. hydroxide
Pharmacological Action
1) Bulk Forming - Dietary fiber: Bran , Psyllium , Ispagula , Methylcelulose
These drugs increase the weight and size of stool by absorbing water, and make the stool
soft , so stool passes easily .

2) Stool softener : Docusates ( DOSS) , Liquid paraffin.

It is a surfactant ingredient ( a substance when it is added to a liquid , reduces its surface
tension , so that increases its spreading and wetting property ) It mixes the water in bowel
with the stool and softens it .
3) stimulant : Senna , Cascara sagrada , castor oil .
They increase the peristalsis movement by direct acting on the enteric nervous system and
ease the stool passage .
4) Osmotic Purgatives : Mag. sulphate . Mag. hydroxide
These agents stimulate the intestine to absorb water in excess amount from the body and
pore the water into stool , so stool becomes soft and easier to pass out .
Indications
1) To treat constipation .
2) To empty and prepare the bowel for radiologic examination or for surgical procedure .
3) to empty the bowel after ingestion of Poison .
Contraindication
No significant Contraindications .
Dose
Psyllium 6-15g
Ispagula 3- 6 g
Docusates 100-400 mg /day
Liquid paraffin 15-30 ml /day
Senna 10-40 mg at bed time
Mag. sulphate 5-15 g in 150 ml water

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Anti Diarrhoeal Drugs
Definition
The drugs are used to treat diarrhoea are called anti- Diarrhoeal drugs .
Diarrhoea : it a condition in which patients pass loss and watery Stool more than three
times a day .
Acute Diarrhoea : If diarrhoea continues for 1-2 days it is called
Acute diarrhoea .
And if continues for more than 2 days it is called prolonged diarrhoea.
 In diarrhoea motility of GIT increased , fluid absorption decreased and causes a loss
of water and electrolytes in the body ( Na+)

Classification
1) Anti-Motility agents : Morphine , Codeine , Loperamide ,Bismuth subsalicylate .
2) Cannabinoids Receptor Agonist : tetrahydrocannabinol .
3) Adsorbents : Kaolin , Pectine, Chalk , Charcoal , methyl Cellulose .
4) Anti-spasmodic Agents : dicyclomine , Mebeverine .
5) Anti-Microbial drugs : refaximin , ciprofloxacin .
6) probiotics : Lactobacillus , Bifidobacterium .
Pharmacological Action
Anti-Motility agents : Morphine , Codeine , Loperamide ,Bismuth subsalicylate.
these drugs decrease the ability of intestine to contract .
Cannabinoids Receptor Agonist : tetrahydrocannabinol .
The drugs reduce the intestinal motility by decreasing the release of Acetylcholine from
enteric nerve ( The nervous system controls the function of GIT) .
Adsorbents : Kaolin , Chalk , Charcoal , methyl Cellulose .
They absorb water , toxin ,and bacteria from GIT , and give relief .
Anti-spasmodic Agents : dicyclomine , Mebeverine .
They relax the smooth muscles and rid from spasm and pain in bowel
Anti-Microbial drugs : refaximin , ciprofloxacin .
These drugs kill the microorganism or prevent their growth .
Probiotics : Lactobacillus , Bifidobacterium .
These are good bacteria of large intestine , if diarrhoea is due to lack of them , the use of
Probiotics treats the diarrhoea .
Indications
These are used to treat diarrhoea .
contraindication
they are contraindicated in abdominal pain of unknown reason .

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Doses
Codeine 60mg Tds
Loperamide 4 mg 2 mg after per motion
Probiotic ( Econorm ) 250 mg
Kaolin 26.2 mg after each loss motio
Methyl Cellulose 2 tabs .1000 mg with 8 oz of water .

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Pharmacology Chapter 9
Drugs Acting On Kidney

Diuretics
Definition
Diuretics are drugs which promote urination or water loss . They act on
kidney and increase the excretion of water and Ions ( Na + , cl - HCO 3 - ) .
Classification
1) Thiazides : Chlorothiazide , Hydrochlorothiazide . chlorthalidone .
2) Potassium Sparing Diuretics : Spironolectone , Amiloride .
3) Loop Diuretics : Furosemide , Bumetanide
4) Osmotic Diuretics : isosorbide , Manitol .
5) Carbonic Anhydrase inhibitors : Acetazolamide , Methazolamide .
6) Xanthine : Theophyline

Pharmacological Action
1) Thiazides : Chlorothiazide ( 125- 500 mg/ d ) Hydrochlorothiazide ( 12.5 -
50 mg/d)
They work on kidney at PCT of nephron and reduce reabsorption of Sodium
, Potassium and chloride , thus promote the excretion of body fluid and
Decrease blood volume .
Because with the absorption of Sodium , Potassium and chloride water is
absorbed .
Excretion of sodium relax the blood vessels also . and lower the blood
pressure . Volume of fluid decreased and lower the blood pressure .
2) Potassium Sparing Diuretics : Spironolectone ( 25-50 mg/d) Amiloride ( 5-
10 mg/d)
They work on kidney at DCT of ( nephron ) and reduce reabsorption of
Sodium and chloride , thus promote the excretion of body fluid and blood
volume .
It prevent excretion of Potassium , and correct the potassium loss caused by
Other diuretics .
3) Loop Diuretics : Furosemide ( 20-80mg/d) Bumetanide(0.5- 2 mg/d )

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They work on kidney at Loop of Henle of nephron and reduce reabsorption
of Sodium , Potassium and chloride , thus promote the excreti on of body fluid
and blood volume .
Indication
1) Hypertension 2) Oedema
3) Diabetes 4) Congestive Heart failure
5) Hypercalcemia 6) Certain Kidney disease
7) Liver cirrhosis ( damage ) 8) Poisoning
contraindication
1) Hypokalemia 2) Hypotension 3) Hyponatremia
Doses
Chlorothiazide ( 125- 500 mg/ d )
Hydrochlorothiazide ( 12.5 -50 mg/d)
Spironolectone ( 25-50 mg/d)
Amiloride ( 5 -10 mg/d)
Furosemide ( 20 -80mg/d)
Bumetanide (0.5- 2 mg/d )
4) Osmotic Diuretics : isosorbide , Manitol .
These drugs increase plasma volume and increase blood flow to kidney and
prevent normal reabsorption of water .
* They can be used to reduce intracranial and intra -ocular pressure (glaucoma
).
5) Carbonic Anhydrase inhibitors : Acetazolamide , Methazolamide .
Carbonic Anhydrase is an enzyme which convert CO 2 and H 2 O into HCO 3 (
Bicarbonate ) and protons ( H + ) . if they present in blood and increase blood
volume .
so the Carbonic anhydrase inhibitors prevent the enzyme from this conversion
. But they produce acidosis and other adverse effects , thus they are not in
use as diuretics .
6) Xanthine : Theophyline
This drug increase the glomerular filtration . in this way increase the urine volume .

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Antidiuretics

Definition
the drugs decrease the volume of urine are called antidiuretics .
these drugs inhibit urine formation by increasing the reabsorption of water in
the kidney .
Classification
1) Antidiuretic hormones and its Analogues : Vasopressin ( ADH) ,
Desmopressin , Lypressin , Terlipressin . ( these last 3 are analogues of
Vasopressin)
2) Thiazides ( in patients with Diabetes insipidus ) : Amiloride
3) Miscellaneous : Carbamazepine , Chlorpropamide , Indomethacin .

Antidiuretic hormones
antiduretic hormone is a hormone of pituitary gland . It is also called Arginine
Vasopessin (AVP ) or vasopressin .
Pharmacological Actions
These drugs act on kidney and increase the reabsorption of water .
Indications
1) to treat bedwetting .
2) thiazides are used to treat Diabetes Insipidus ( increased urine volume due
to problem in hypothalamus or in pituitary or in kedney )
Contraindication
1) in Ischemic heart disease
2) in hypertension
3) chronic nephritis
4) psychogenic polydipsia ( a mental disorder in which patient urge to drink
water and drink all day , although he doesn't need )
Doses
Vasopressin 5-10 U injection
Lypressin 10 U i.m. or s.c.

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Pharmacology Chapter 10
Hormones and Hormones antagonist
Hormones are substances which are secreted by special type of cells ( Gland )
and are poured into bloodstream directly and transported to the action
tissues .
Thyroid Hormones
Thyroid hormones are released by thyroid gland and regulated by TSH (
Thyroid stimulating hormone ) which is released by anterior pituitary .
thyroid hormones :
1) T3 ( Triiodothyronine )
2) T4 ( Thyroxine )
3) Calcitonin
Physiological Functions
1) Increase Basal Metabolic Rate ( BMR ) ( The rate at which body uses energy
for maintaining vital functions like breathing , body temperature etc.
 In hyperthyroidism BMR increase by about 60 % to 100% above the
normal level .
 In Hypothyroidism BMR decrease by 20% to 40% below the normal range
.
3) growth and Development of body and brain

4) Action On Protein Metabolism : they increase Protein synthesis working on

DNA
 They increase Enzyme Activity
 They also cause catabolism of protein .
5) Action On Carbohydrates Metabolism : They increase metabolism of
carbohydrates . especially Thyroxine increases :
 Absorption of Glucose from GIT .
 Glucose Uptake by cells
 Glycogenesis
 gluconeogenesis ( formation of glucose from non carbohydrate
substances like fat , protein )
6) Action On Fat metabolism : They decrease the fat storage and convert the
fat into free fatty acids .
7) Action On Plasma and Liver fats :
 decrease the cholesterol level in plasma .
 In hypothyroidism the level of cholesterol increase and causes
Athreosclerosis .
 low level of thyroxine increase deposition of fats in lever and leads to
fatty lever .

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8) Action On Vitamins Metabolism :
 Thyroxine Increase the formation of enzymes and vitamins are essential
parts of enzyme , so vitamins are used during formation of enzymes .
 In case of hyperthyroidism vitamins deficiency is possible .
9) Action On Body temperature :
 they increase heat production in the body
 In case of hyperthyroidism increase body temperature and results
excess sweating .
10) Action On Growth :
 Thyroxine is necessary for growth and development of body and brain
 In case of Hypothyroidism during childhood causes dwarfism and mental
retardation .
11) Action On Body Weight :
 Increase in thyroxine decrease the body weight and fat storage
 decrease in thyroxine increase the body weight .
12) Action On Sexual func tions :
 normal thyroxine level is essential for normal sexual function .
 In men , Hypothyroidism leads to complete loss of libido ( sexual desire
) . and hyperthyroidism leads to impotence .
 In women ,hypothyroidism causes Manorrhagia and polymanorrhaea
and hyperthyroidism leads to irregular MC ( oligomanorrhea ) and some
time leads to amanorrhea ( loss of fertility ) .

Pathological Roles
1) High Level of Thyroid hormone indicates Hyperthyrodism , Symptoms of
Hyperthyrodism includes :
1) Constipation 2) depression 3) feeling tiredness
4) high blood cholesterol level
5) dry skin
6) excessive forgetfulness
7) heavy and frequent menstrual cycle
8) Tingling in hands
9) loss of sexual desire
10) weight Loss

2 ) Low level of Thyroid Hormone Indicates Hypothyrodism , its symptoms

includes :
1) Weight gain

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2) Increased appetite
3) changes in menstrual
4) Restless
5) diarrhoea
6) excess sweating
7) sleep problems
8) swollen in thyroid gland etc.
Clinical Uses
thyroid hormones natural and synthetic ( Livothyroxine ) are used to treat :
1) Hypothyroidism
2) Hypothyroid Coma ( it is a extreme condition of hypothyrodism in which
multiple organ abnormalities occurs )
3) Cretinism ( stopped mental and physica l growth )

Anti-thyroid Drugs
Definition
Anti-thyroids are the drugs which block the formation of thyroid hormone or
prevent their secretion .
It is also called Thyroid Antagonist or Thionamide drugs .
Examples
Propylthiouracil , methimazole , ca rbimazole , Perchlorates , radioactive
iodine ( 131,125,123 )
Indications
these are used to treat overactive thyroid gland ( Hyperthyrodism /
thyrotoxicosis ) .

Parathormone
Definition
It is a hormone released by parathyroid gland , which regulates the calcium
level of blood .
parathormone aslo called Parathyroid hormone ( PTH)
Physiological Role
1) Regulation of blood calcium level : - when blood calcium level decreases
parathyroid gland releases parathormone , and causes release of calcium
from bone into blood circulation .

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2) It increases the vitamin D production , which increases the absorption of
calcium from intestine to maintain blood calcium level .
3) It prevents calcium loss in urine .
Pathological Role
1) Low level of parathormone indicates the Hypoparathyroidism , and it
increases the phosphorus level in blood .
2) High Production of parathormone indicates Hyperparathyroidism which
causes Increase blood calcium level , th at can lead to kidney stone , bone
thinning , ( osteoporosis ) and causes weakness of body and fatigue.
Symptoms acute Hypoparathyroidism
1) Hypocalcaemia 2) Tetany 3) tingling of lips , hands and muscles 4)
Convulsion .
Symptoms Chronic Hypoparathyroidism
1) Loss of Hair 2) Brittle Finger nails 3) carries of Teeth 4) Cataract
Clinical Uses
1) Parathormone is used to treat Hypoparathyroidism .
2) Cinacalcet and Teriparatide are used as antagonist to treat
Hyperparathyroidism .

Calcitonin
Definition
Calcitonin is a hormone , secreted by thyroid gland , and acts just opposite to
PTH ( parathyroid Hormone ) and reduces Plasma calcium level .
Physiological Role
1) It decreases the bone resorption ( the absorption into blood ) . It prevents
action of Osteoclast ( osteoclasts are cells which break down the bone matrix
and release calcium and phosphorus into blood stream ).
2) It decrease blood calcium level working on kidney and prevents
reabsorption of calcium and phosphorus .
Pathological Roles
1) If too much calcitonin found in blood it may be a sign of thyroid cancer ,
which is called MTC ( Medullary Thyroid Cancer )
2) Low level of Calcitonin during or after thyroid cancer treatment means
that your cancer treatment is effective . or may be due to a problem in
thyroid gland , pituitary or in hypothalamus .
Clinical Uses
1) It is used in Hypercalcaemia .
2) In Paget's Disease of bone ( a disease that Disrupt /Prevent the
replacement of old bone tissue with new bone ti ssues )
Note : anti-thyroid Drugs are its antagonist

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Vitamin D
Definition
Vitamin D is a fat Soluble Vitamin . It is a prohormone , which is converted in
the body into a number of biologically active metabolites , and they
function as true hormone .
Sources of vitamin D are foods and exposure to sun light , but it biologically
inactive , and by hydrolisation process of the body becomes active .
Vitamin D3 and D 2 are most essential for Human body .
Pathological Roles
 It increases the intestinal absorption of calcium , magnesium , iron , zinc
and phosphorus
 It promotes the reabsorption of calcium and phosphorus in the kidney
 It increases blood calcium level
 It promotes mineralisation of bone
Pathological role
1. Vitamin D deficiency causes rickets in children and osteomalacia in
adults.
2. Acute large amount or long term use of vitamin D causes
hypervitaminosis .
Clinical Uses
o it is used for prevention and treatment of rickets and osteomalacia .
o It is used to treat hypoparathyroidism.
Note : 6-fluoro-vitamin D3 is a antagonist of vitamin D 3

Insulin
Definition
Insulin is a hormone secreted by pancreas and control the glucose level in
blood stream and helps in utilisation of glucose by body tissues .
Physiological roles
1) In liver :
a) insulin promotes glucose entry in liver .
b) It promotes glucose storage in the form of glycogen
c) It inhibits glucogenolysis , and gluconeogenesis .
d) It Inhibits phosphorylation .
2) In Skeletal Muscles :-
a) It increases Protein synthesis.
b) increases glycogen synthesis and increases utilisation of glucose .
c) It inhibits phosphorylation .
d) and decreases glucose plasma level .
3) In adipose tissues :
1) it promotes glucose entry into adipose tissues .
2) It increase triglyceride storage .

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3) It inhibit lipolysis .
4) and decrease plasma glucose level .
Pathological roles
1) Low secretion of insulin or Complete absence Or resistance to insulin
action , indicates hyperglycemia
And causes many of biological problems
a) diabetes mellitus type 2
b) myocardial infection c) kidney failure
d) abnormal blood level of lipids
e) hypertension f) non alcoholic fatty liver g) blindness
h) weakness of immune system and weakness
2) High secretion of Insulin
High secretion of insulin indicate and pancreatic cancer and because of this
hypoglycemia occurs . And causes many of biological problems like excess
sweating , Excessive hunger , shakiness , nausea ,vomiting ,mental
confusion trembling lips, and blurred vision .
Clinical Uses
1) To treat Type 1 Diabetes .
2) To Treat Diabetes Ketoacidosis
3) Diabetic Coma .
Insulin Antagonists : Glucagon , Adrenaline , Cortisol ,

Oral Hypoglycemic agents

Definition
The Oral drugs are used to treat Diabetes Mellitus are called oral
Hypoglycemic agents .
Classification
1) Sulfonylurea : Tolbutamide , Glibenclamide , Glimepiride .
They stimulate release of insulin .
2) Biguanides : Metformin , Phenformin , Buformine .
they increase the insulin action
3) Meglitinide analogues : Repaglinide , Nateglinide .
They directly stimulate the pancreas to release the insuline
4) Thiazolidinediones : Rosiglitazne , Pioglitazone .
They decreases the blood sugar level without increasing the insu lin secretion .
5) α -Glucosidase Inhibitors : Miglitol , Voglibose .
They inhibit the digestion of carbohydrates and decrease blood sugar level .

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Estrogen
Definition
Estrogen or Oestrogen is a female sex hormone produce by the ovary ,
adrenal gland and placenta ( During pregnancy ) .
This is responsible for development and control of reproductive system and
secondary sex characteristic in females .
Note : any natural or synthetic substance which mimics the effect of natural
hormone is called estrogen .
Physiological roles
1) Structural :
 it helps in growth and development of sex organs in females
 it helps in development of secondary sex characteristics in females
 it Increases uterine growth and breast development
 increase vaginal lubrication
 it makes vaginal secretion thin , watery , and alkaline which facilitated
the entry of sperm
 it helps in synthesis of progesterone receptor .
2) Metabolic Functions
 It decrease the resorption rate of bone by inhibiting the activity of
osteoclast
 It is increases HDL level of plasma and decrease LDL level
 It causes sodium and water retention .
3) Coagulation
It increases clotting ability of blood by increasing the clotting factors( 2nd ,
7th 9th and 10th ) and decrease ant i-thrombin 3rd .
Pathological roles
high plasma level of estrogen associated with
1) ovarian cancer or adrenal gland cancer
2) Breast cancer
3) Polycystic ovarian syndrome ( a hormonal disorder causing enlarged
ovaries with small cyst on outer edges ) .
4) Heavy menstruation
Low level of estrogen associated with

1 )stopped or irregular menstruation

2) Infertility in male and female
3) osteoporosis and bone fracture
4) libido
5) erectile dysfunction

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6) cholesterol level increase in blood
7) coronary arteries problems developed.
Clinical Uses
1) Oral contraceptives : this is used in combination with progesterone
( progestin ) for contraception.
2) Menopause symptoms treatment :( Menopause is a stage of life when a
menstrual cycle stopped and ovaries stopped releasing eggs and estrogen
which causes many problems like hot flushing( sudden feeling of warmth in
the upper body ) Pain during sexual intercourse , osteoporosis , insomnia ,
dry skin etc.
3) To treat premature ovarian failure( loss of normal function of the ovaries
before the age 40)
4) To treat vaginal atrophy( it is the condition in which the walls of vagina
becomes dry and thiner in sometime inflamed )
5) To treat osteoporosis.
antagonists of Estrogen are : Tamoxifene , toremifene , and raloxifene

Progesterone / Progestin

Definition
Progesterone is a hormone secreted by Ovaries , adrenal gland and placenta (
During pregnancy ) .
Physiological functions
o It prepares the uterus ( Endometrium ) for pregnancy means for
development and growth of fertilized egg .
o Its Secretion causes menstruation in absence of pregnancy .
o It prevents the contraction of myo -metrium( smooth muscles layer )and
counter the effect of oxytocin on contraction
o It helps the breast for milk production on childbirth
o It promotes the glycogen storage in liver
o It acts as antagonist of estrogen inhibits the estrogen receptor
Pathological role
 High level of progesterone maybe a sign of pregnancy and it rise during
menstrual cycle also
 Level of progesterone maybe high due to ovarian cancer or cyst or
adrenal cancel
 Low level of progesterone can cause irregular menstrual
 Low level of progesterone is unable to prevent contraction of myo -
metrium and premature labour maybe occurs
 low level of progesterone can disturb fertilization
 low level of progesterone can cause infertility .

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Clinical Uses
1) Contraception : It is used in combination with est rogen or alone for
contraception . It prevents ovulation ( it prevent development of egg and
release from Ovary )
2) To treat Uterine Bleeding .
3) to treat menstrual disorder .
4) To treat endometriosis ( abnormal growth of uterus to outside )
5) It is used as HRT ( Hormone replacement therapy ) In postmenopause
female .
6) to treat endometrium Carcinoma ( a type of uterus cancer )
Antagonist : Mefipristone is an antagonist of Progesterone . It is used for
abortion up to 10 weeks of pregnancy .
Oxytocin

Definition
Oxytocin is a natural hormone synthesized by the hypothalamus and posterior
pitutory gland Stores it and release it into blood stream.

Physiological role
I. Uterus: it increase the frequency and force of uterine contraction which
facilitates childbirth .
II. Breast : it helps in milk production and ejection .
III. Heart : it causes vasodilation by relaxing the vascular smooth muscles
and decrease blood pressure .
IV. Kidney: it causes retention of water

Pathological Roles
1) High level of oxytocin : Oxytocin level increase at the time of childbirth in
female and rarely increases in normal condition .
High level of oxytocin increases the contraction of uterus which prevent
pregnancy .
2) Low level of oxytocin:
o It may be due to damage of hy pothalamus or pituitary gland
o Low level of oxytocin at the time of childbirth may prolong the labour
time
o Low level of oxytocin can cause autism spectrum disorder( a type of
mental disfunction in which patient face communication problem and
depression)

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Clinical uses
o It is used at the time of childbirth for induction of labour
o For Augmentation of labour ( a process of stimulating the uterus to
increase the contraction frequency)
o To treat postpartum hemorrhage ( excessive bleeding after) childbirth
Antagonist : Atosiban is an antagonist of Oxytocin . It is commonly used
prevent premature labour.

Corticosteroids

Definition
Corticosteroids are a class of steroid hormone that are released by the
adrenal cortex there are two main types of corticoster oids glucocoticoids (
Cortisol) and mineralocorticoids ( Aldosterone ) .

Physiological roles
 Metabolism : glucocorticoids help in gluconeogenesis by increasing
entry of amino acid in liver and kidney .
 Stress Management : glucocorticoids provide energy to overcome on stress
caused due to trauma , fright , infection , bleeding through increasing
the plasma glucose level .
 Anti inflammatory action: it suppress immune system and reduce
inflammatory response
 Ant-Allergic reaction : it to reduces electric reaction by separation the
immune response .
 Mineralocorticoids : It Promotes Sodium reabsorption and Potassium
excretion .

Pathological Role
1) High level of Corticosteroids may cause Cushing 's Syndrome .( Obesity ,
high Blood pressure , diabetes and osteoporosis )
 It may be due to over dose of steroids
 Light increase may be due to inflammation
2) Low Level of Corticosteroids is called Hypocortisolism and can cause
Addison's disease (dehydration, dizziness, fatigue , loss of appetite, low blood
pressure, low blood sugar, water-electrolyte imbalance , absence of
menstruation, craving salty foods, excess urination, muscle weakness,r weight
loss etc )

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 It may be due to autoimmune disorder that damage adrenal gland or
pituitary gland .
Clinical Uses
 In eye disease : allergic conjunctivitis
 Hematological disorder: haemolytic anaemia
 In neurological disorder : cerebral edema
 In pulmonary disorders : bronchial asthma , in infant for prevention of
respiratory problems .
 In gastrointestinal disorder : inflammatory bowel disease
 Bone and joints disorders : bursitis , arthritis
 Skin disorders : Atopic dermatitis ( and itchy inflammation of the skin ) it
is also called Eczema .
Antagonist : Mifepristone is an antagonist of corticosteroids and progesterone .

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Pharmacology Chapter 11
Autocoids

Definition
Autocoids are chemical substances produced by different cells of the body .
They act as local hormones at the site where they are synthesised and
released , and change the function of the other cells .
e.g. histamines , Serotonin( 5-HT) , Prostaglandin ( PG)
Autocoids

amines Polypeptides Lipids

Histamine* kinins Prostaglandines*

Serotonin* angiotensin Leukotriens
Thromboxanes

1) Histamine : Histamines are Organic compounds belonging to amines Group .

They are produced in almost all the cells , but it is released in large amount
when immune system is defending against an antigen .
They show their action when they binds with their receptors

Histamine

H1 receptor H2 receptor H3 receptor H4 receptor

1) smooth Increases Gastric Stimulates It makes allergy
muscles acid secretion sensory nerves and inflammation
Contraction worst .
2) increases Increases Itching in skin
permeability of contractility of
capillaries heart muscles
Airways
obstruction

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Physiological Roles
1) On CNS : Stimulates sensory neuron and give a feeling of itching , and other
senses .

2) On CVS :
 Dilation of blood vessels .
 Increases permeability of capillaries .
 Histamine shock : large amount of histamine causes too much
vasodilation and causes death .
 Increases contraction force of heart .
3) Inflammation and Allergic reaction : when antigen interacts with IGE
antibody present on the mast cell surface , the mast cell releases histamine
which causes inflammation and allergic reaction .
4) Gastric Acid Secretion : H2 receptor present in gastric mucosa and when
histamine binds with it , it stimulates acid secretion .

Clinical Uses
Histamine has no valid clinical use .

Anti-Hisamines
Definition
The Drugs prevent action of histamine are called anti -histamines or histamine
antagonists .
Classification
1) H1 Antagonists: Diphenhydramine Hydrochloride , Cyclizine hydrochloride
2) H2 Antagonists : Cimetidine , Rantidine .
3) H3 Antagonist : Thioperamide , Clobenpropit .
H1 Antagonists
H1 antagonist inhibit function of H1 receptors

First Generation H1 antagonist :

Diphenhydramine Hydrochloride , Cyclizine hydrochloride , Pyrilamine maleate
, Promethazine hydrochloride etc.
They cross blood Brain Barrier easily and produce laziness .
Second generation H1 antagonists : Cetirizine , Levocetirizine , acrivastine ,
Azelastine hydrochloride etc.
They don't cross blood Brain Barrier easily and don't produce laziness .

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Clinical Uses
1) Allergic disorders : H1 antihistamines are used to treat and prevent
symptoms of allergic reactions , like Dermatitis , Conjuctivitis , Pruritus (
Itching ) , urticaria ( skins rash ) .
2) Common Cold : they are used to relief common cold symptoms .
3) Preanaesthetic Medication : it is used for its sedative and anticholinergic
actions .
4) As anti- emetics : Promethzine , diphenhydramine etc . are used for
prophylaxis of motion sickness .
5) Parkinson's disease : it is used to treat Parkinson's disease .
6) Sedative and Hypnotics : it is used for sedative and hypnotic effects .
Adverse Effects
1) feeling of sleep 2) Dryness of mouth and nose 3) blurred vision
4) over dose cause Central Excitation , Convulsion , respiratory and cardiac
failure , and death .

H2 -Antagonists
These drugs prevent the action of H2 receptors
Examples Cimetidine , Rantidine , Famotidine .

Clinical Uses
They are used to prevent Gastric secretion in diseases like Hyperacidity ,
Gastric ulcer , GRD etc.
Adverse Effects
1) Headache 2) Constipation 3) Vomiting 4) Gynacomastia ( man boobs
)
5) Impotency in males

H3 and H4 Antagonists
Thioperamide and Clobenpropit are H3 receptor antagonists but H3 and H4
antagonists are not used usually , because their usefulness is still not clear .

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5HT ( Serotonin )

Definition
5HT ( 5HydroxyTryptamine is an important neurotransmitter , it is
synthesised by amine acid Tryptophan . It is widely found in animal and plant
, High concentration of 5HT is found in intestine , platelets and brain .
Physiological Roles
1) On CVS : It shows a complex action on CVS which depends on dose injected
.
a) On blood vessels : in starting induces vasoconstriction but later induces
vasodialation .
b) On Heart : It induces a positive chronotropic effect ( Increases heart rate )
and positive inotropic effect is also seen .
c) on blood pressure : its action on BP is complex . It may either cause
hypotension or hypertension .
2) Action on Smooth Muscles : It causes contraction of intestine bronchi , and
uterus .
3) On Digestive System : It increases intestinal motility , and induces Emesis
( vomiting )
4) On Lungs : it causes contraction of bronchi .
5) Uterus : it increases contraction of Uterus .
6) On CNS : a) It regulates the sleep , mood and appetite .
b) Migraine : contraction and relaxation of brain vessels due to 5 -HT causes
a repeated and severe pain .
7) Allergic and Inflammatory actions : it involves in allergic and
Inflammatory reactions.
5-HT Antagonists
Cyproheptadine , ketanserin , Ondansetron , Granisetron , Clozapine ,
olenzapine etc.
Clinical uses
1) Cyproheptadine
It is used in skin allergy like pruritis and urticaria .
It is used to treat Carcinoid tumor( slow growing tumor at any part of the
body) it is used to treat Migraine

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2) Ketanserin : it is used as antihypertensive drug , it dilates blood vessels .

3) Ondansetron and Granisetron

these are used as anti-emetics

4) Clozapine , olenzapine , resperidone

these are used as antipsychotics .
Adverse effects
1) Dry mouth 2) Drowsiness 3) weight gain .

Prostaglandins
Definition
prostaglandins ( PGs) are lipid compounds . Arachidonic acid is the precusor
for biosynthesis of all PGs , and COX ( Cyclooxygenase ) enzyme involves in
formation of PGs when phospholipid membrane is damage due to any reason .
Physiological Roles
1) GI Tract : PGE 2 and PGI 2 reduce acid secretion and increase the secretion of
mucus in the stomach . Misoprostol , Rantidine are used to prevent ulcer due
to NSAIDs .
2) Cardiovascular System : PGD 2 , PGE 2 and PGI 2 cause vasodilation , PGF 2 α
Constricts pulmonary veins and arteries . TXA 2 is a Vasoconstrictor .
3) Platelets : PGI 2 inhibits platelet aggregation . It is used during
Haemodialysis to prevent platelets aggregation .
4) Eye: PGF 2 α decreases the ocular pressure . Its analogues are used in
glaucoma e.g. Latanoprost , Bimatoprost etc.
5) Uterus : PGE 2 ( low concentration ) and PGF 2 α Contract Pregnant Uterus ,
PGs are commonly used for abortion .
They can used for Induction of labour .
6) Male reproductive system : PGE 1 is useful in the treatment of erectile
dysfunction . e.g. alprostadil .

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Clinical Uses
1) abortion 2) Induction of labour
3) PPH : To treat postpartum hemorrhage ( excessive bleeding after
childbirth ) e.g. Carboprost ( i.m.) Misoprost ( oral)
Adverse effects
Nausea , Vomiting , diarrhoea , fever , flushing ( reddening of skin )
hypotension etc.

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Pharmacology Chapter 12
Chemotherapeutic Agents

Introduction
I. The Chemical substances ( Drugs ) used for treatment of diseases
caused by microorganism and tumor Cell are called Chemotherapeutic
Agents .
II. Nowadays it refers to treatment of cancer usually .
III. The Chemical substances used as Chemotherapeutic agents are also
called antibiotics and anti-neoplastic Agents .
IV. Now antibiotics can further classified into Bactericidal ( kil ls the
Bacteria ) and Bacteriostatic ( Prevents the growth of Bacteria ) .
V. Even though Antibiotics are referred to bactericidal and Bacteriostatic
, But antiviral , antifungal anthelmintic , antiprotozoal are also called
antibiotics .
VI. The Chemotherapeutic agents that are used to treat infection and
infestation may be other than antibiotics also

Basic Principle of Chemotherapy of Infections and Infestations

1) Diagnosis : Before Chemotherapy diagnosis should be performed for
determination of type of microorganism and site of infection .
2) Selection of drug : drug should be select according to the type of pathogen
, and should consider which is required whether Narrow or broad spectrum .
3) frequency and duration of administration : low dose can develop resistance
, intermediate dose may not cure infection , so optimum dose should be used
.
4) Continue therapy : acute infection treated for 5-10 days , but some takes a
long time like Tuberculosis , thyroid .
5) Prophylactic Chemotherapy : Chemotherapy is also used as prophylaxis to
avoid surgical site infection .

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Classification of Chemotherapeutic agents
1) Antibiotics
a) a) B-Lactam Antibiotics : Penicillins. Monobactams,
Cephalosporins, Carbapenems etc.
b) Aminoglycosides : Streptomycin, Gentamycin, Framycetin, Neomycin,
etc.
c) Macrolides : Erythromycine , Roxithromycin, Erythromycin,
Clarithromycin,
d) d) Tetracyclines: Oxytetracycline, Doxycycline, Minocycline, etc.
e) Nitrobenzene Derivatives: Chloramphenicol, etc.
f) Polypeptide Antibiotics: Polymyxin-B, Colistin, Bacitracin,
Tyrothricin, etc.
g) Polyene Antibiotics : Nystatin, Hamycin, Amphotericin -B, etc.
h) Miscellaneous Agents: Rifampicin, Lincomycin, Vancomycin, Fusidic
acid, Cycloserine, Viomycin, Gri seofulvin, etc.

2) Chemotherapeutic Agents other than Antibiotics :

a) Sulphonamides and Related Agents: Sulfadiazine, Sulfamethoxazole,
Sulfones (Dapsone) , Para aminosalicylic acid (PAS), etc.
b) Diaminopyrimidines: Pyrimethamine.
c) Quinolones and Fluoroquinolones: Nalidixic acid, Norfloxacin,
Ciprofloxacin, ofloxacin, etc.
d) Nitrofuran Derivatives: Nitrofurantoin, Furazolidone, etc.
e) Nitroimidazoles: Metronidazole, Tinidazole etc.
f) Imidazole Derivatives: Miconazole, Clotrimazole, Ketoconazole, Fluconazole,
etc.
g) Nicotinic Acid Derivatives: Isoniazid, Pyrazinamide, Ethionamide, etc.
h) Miscellaneous Agents: Ethambutol, Thiacetazone, Clofazimine, etc.
3) Chemotherapeutic Agents According to the Types of Organisms Against
which they are Primarily Active:
i) Antibacterial : Penicillins, Aminoglycosides (Streptomycin, Gentamycin,
Framycetin, Neomycin) , Erythromycin, etc.
ii) Antifungal: Griseofulvin, Amphotericin B, Ketoconazole, etc.
iii) Antiviral: Acyclovir, Amantadine, Zidovudine, etc.

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iv) Antiprotozoal : Chloroquine, Pyrimethamine, Metronidazole, Diloxanide,
etc. v) Anthelmintic: Mebendazole, Niclosamide, Diethylcarbamazine, etc.
4) Classification of Chemotherapeutic Agents According to their Range of
Action:
i) Broad Spectrum Antibiotics: Those effective against Gram +ve, Gram -ve,
rickettsia and chlamydia. For example, Tetracycline,Chloramphenicol etc.

ii) Narrow Spectrum Antibiotics

a) Those effective only against gram +ve bacteria, e.g., Penicillin,
Erythromycin group, Vancomycin.
b) Those effective only against gram -ve bacteria, e.g., Streptomycin and
other aminoglycoside antibiotics, Colistin, Polymyxin -B.
iii) Relative Broad Spectrum Antibiotics: Those effective against +ve and gram -
ve bacteria. For example, Ampicillin group, Cephalosporins, Rifamycins, etc.

Penicillin

Introduction
Penicillin is the first antibiotics which was clinically used in 1941 firstly it was
obtained from fungus penicillium notatum , but presently it is obtained from
P. Chrysogenum .
Classification
1) Penicillin G : penicillin G ( Benzyl Penicillin ) , Procaine Penicillin G ,
Benzathine penicillin G .
2) Acid resistant penicillin : Phenoxymethylpenicillin ( Penicillin V)
3) penicillin With ß lactamse inhibitor : Amoxycilin , Clavulanic acid .
4) penicillin effective against Gram + and gram Negative Organism : Ampicillin
, Talampicillin .

Indications
penicillin G (PnG) is used for treatment of :
1) Streptococcal Infection : Normally it is used for 7 -10 days to treat
Pharyngitis , endocarditis , rheumatic Fever ( a type of fever which causes
inflammation of heart , blood vessels and joints ) etc.
2) Pneumococcal infection : Like pneumonia , Pericarditis , Meningitis etc.

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3) Syphilis
4) Diphtheria
5) tetanus
Contraindications
It is contraindicated in
1) previous history of allergic reactions
2) In Stevens johnson syndrome
3) In lactation
Dose
penicillin G : 0.5-5 MU im/iv

Cephalosporins

Introduction
Cephalosporins are largest group of Beta lactam antibiotics , Five generation
of cephalosporin are available . It is a broad spectrum antimicrobial agent
and used to treat infection gram positive and gram negative bacteria .
classification
1) first generation : Ampicillin , Cephalexin
2) Second generation : Cefazolin , Cefeclor
3) Third generation : Cefexime , Ceftizoxime
4) fourth generation : Cefepime
5) fifth generation : Ceftaroline
Indications They are used to treat :
 skin or soft tissue infections.
 urinary tract infections (UTIs)
 strep throat.
 ear infections.
 pneumonia.
 sinus infections.
 meningitis.
 gonorrhea.

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Contraindications
Allergic reaction history
Dose
Ampicillin : 250-500 mg / 6 hours
Cefexime : 400 mg /d

Aminoglycosides

Introduction
Aminoglycosides have a broad spectrum of activity against Gram negative and
mycobacterium . It is used to treat serious infection . aminoglycocides are
called Bactericidal antibiotics .
Classifications
1) first generation : Streptomycin , kanamycin , Neomycin .
2) Second generation : Gentamicin , tobramicin .
3) Third generation : amikacin , sisomicin .
Indications
They are used in the treatment of severe infections of the abdomen, urinary
tract, skin and soft tissue, bone, cervix, blood, eye ear, lungs, and heart.
tuberculosis , UTIs , gonorrhoea , etc.
Contraindications
renal and hepatic diseases and in pregnancy
dose
Streptomycin : 1-2 g /d
amikacin : different according to infections

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Fluoroquinolones

Introduction
Fluoroquinolones are active against a wide range of aerobic gram positive and
gram negative organism . They are commonly used to treat respiratory and
urinary tract infections .
Classification
1) first generation : Nalidixic acid , Cinoxacin
2) Second generation : Norfloxacin , Ofloxacin , ciprofloxacin
3) Third generation : Levofloxacin , Sparfloxacin .
4) fourth generation : trovafloxacin .
Indications
These are used to treat bacterial infections like
 urinary tract infections (UTIs)
 throat infection .
 ear infections.
 pneumonia.
 sinus infections.
 meningitis.
 gonorrhea.
Contraindication
in lactation
In Hypersensitivity
Dose
Ofloxacin : 250-750 / BD
Levofloxacin : 250 -500 /d

Macrolides
Introduction
Macrolides are naturally occurring compounds , they have broad spectrum
activity against gram positive and gram negative bacteria . these are used in
patients who were allergic to penicillin or whose infections were penicillin
resistant .
Examples
1) Erythromycin 2) Clarithromycin 3) Azithromycin 4) tylosin

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Indications
they are used to treat bacterial infections :
1) Pneumonia 2) inflammation of nasal cavity 3) Pertussis (Respiratory
tract infection ) 4) Diphtheria ( inflam mation of mucus membrane of
throat )
5) Pharyngitis 6) Covid-19 7) Syphilis and Gonorrhoea 8) tetanus 9)
Skin infection ointment .
Contraindication
In pregnancy
Dose
Erythromycin : 250 mg /d
Azithromycin : 500- 1500 mg /d

Tetacyclines

Introduction
Tetracyclines are a group of broad spectrum antibiotics , which are used to
treat a variety of infectious diseases .
classification
1) Short acting ( 6 hours half life ) : Chlortetracycline , Oxytetracycline
2) Intermediate Acting ( 16 hours half life ) : Demeclocycline .
3) long acting ( 18-24 hours ) : Doxycycline , minocycline .
Indications
Tetracycline is used to treat many different bacterial infections of the skin,
intestines, respiratory tract, urinary tract, genitals, lymph n odes, and other
body systems. It is often used in treating severe acne, or sexually transmitted
diseases such as syphilis, gonorrhea, or chlamydia.
Contraindications
1) pregnancy and lactation
2) Hypersensitivity
3) In renal and hepatic failure
Dose
Chlortetracycline : 250 mg /6 h
Doxycycline : 100 -200 mg /d

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Sulphonamides

Introduction
Sulphonamides were the first antimicrobial agents ( AMAs) , they are also
known as Sulfa Drugs .
Sulfonamides (sulphonamides) are a group of man -made (synthetic) medicines
that contain the sulfonamide chemical group . They are bacteriostatic .
Many people use the term sulfonamide only for antibiotics However, there
are several non-antibiotic sulfonamides that have been developed by
observations These are used for a range of conditions such as diabetes and
pain relief.

Classification
1) Short acting ( 4-8 hours ) : Sulfadiazine .
2) Intermediate acting ( 8-12 hours) : Sulfamethoxaole , Sulfamoxole .
3) Long acting ( 7 days ) : Sulfadoxine , sulfam ethopyrazine .

Indications
1) Bacterial infections: eg, sulfamethoxazole / trimethoprim, sulfisoxazole
2) Crohn’s disease: eg, sulfasalazine
3) Diabetes: eg, glyburide, tolbutamide
4) Fluid retention: eg, chlorothiazide, furosemide, hydrochlorothiazide
5) Gout: eg, probenecid
6) High blood pressure: eg, chlorothiazide, hydrochlorothiazide
7) Pain and inflammation: eg, celecoxib
8) Rheumatoid arthritis: eg, sulfasalazine
9) Ulcerative colitis: eg, sulfasalazine.
Contraindications
1) pregnancy and lactation
2) Hypersensitivity
Dose
Sulfamethoxazole / trimethoprim : 800 mg 160 mg / d
Sulfones (Dapsone) : 50-100 mg /d

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Anti-Tubercular Drugs

Introduction
The drugs are used to treat TB ( tuberculosis) are called anti tubercular agent
. TB is a Bacterial infection due to Mycobacterium tuberculosis .
Antibiotics are used to treat TB
Classification
Anti-tubercular drugs can be classified as follows:
1) First Line Drugs
i) Isoniazid (H), ii) Rifampin (R),
iii) Pyrazinamide (Z), iv) Ethambutol (E),
v) Streptomycin (S).
2) Second Line Drugs
i) Thiacetazone (Tzn), ii) Paraaminosalicylic acid (PAS),
iii) Ethionamide (Etm), iv) Cycl oserine (Cys),
v) Kanamycin (Kmc), vii) Capreomycin(Cpr).
vi) Amikacin (Am),
3) Newer Drugs
i) Ciprofloxacin, ii) Ofloxacin,
iii) Clarithromycin, v) Rifabutin.
iv) Azithromycin,
Indication
These are used to treat TB
They can be used to treat other bacterial infections
Contraindications
First line drugs are contraindicated in the following conditions:
i) Hypersensitivity,
ii) Acute and chronic alcoholism,
iii) Acute liver disease,
iv) People above 35 years,
v) Seizure disorders,
vi) Lactating women,

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vii) Patients with kidney disorders,
viii) Pregnancy
ix) Hepatitis
x) Pyridoxine deficiency (vitamin B6 supplements are thus given
simultaneously with isoniazid).

Anti Fungal Drugs

Introduction
The drugs are used to treat Fungal I nfections are called antifungal drugs .
Fungi most commonly affect Skin , hair and nails .
Fungi are neither plants nor animals, and are classified as their own kingdom.
Fungi grow either as yeasts (single round cells) or as moulds (many cells
forming long, thin threads called hyphae). Some fungi even go through both
the forms during their life cycle. Many fungi, including bread moulds and
mushrooms, can be seen with the naked eye. Fungal infections are often
caused by fungi present in the environment. Mo st fungi are not dangerous,
but some of them can be harmful.
Classification
i) Antibiotics: ( Systemic )
a) Polyenes: Amphotericin B (AMB), Nystatin, Hamycin, and Natamycin
(Pimaricin).
b) Heterocyclic Benzofuran: Griseofulvin.
ii) Antimetabolite : Flucytosine (5-FC).
iii) Azoles:
a) Imidazoles (Topical): Clotrimazole, Econazole, and Miconazole.
(Systemic): Ketoconazole.
b) Triazoles (Systemic): Fluconazole , Itraconazole.
c) Allylamine: Terbinafine.
Indications
These are to treat Fungal Infection caused by :
Candida, Cryptococcus, Histoplasma,
Blastomyces, Coccidioimyces, Aspergillos,
Sporotrichos, etc.
Contraindications
Acute or chronic renal and hepatic diseases

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Anti-Viral Drugs

Introduction
The drugs are used to treat viral infections are called antiviral drugs .
Viruses are tiny capsules (smaller than bacteria) containing genetic material.
They cause common infectious diseases like common cold, flu, and warts;
while they may also cause severe illnesses such as HIV/AIDS, smallpox, and
haemorrhagic.
Viruses invade (enter , attack and take control of ) the living, normal cells of
an individual, and use them to multiply. This ultimately kills the cells, and the
individual becomes sick.
Since the viruses live inside the body's cells, treatment of viral diseases is
hard. Antibiotics cannot cure viral diseases, and a few antiviral drugs are
available. However, vaccines can prevent the occurrence of many viral
diseases.
Classification
1) Anti-Herpes Virus : Idoxuridine, Acyclovir, Trifluridine, Ganciclovir, and
Foscarnet. Famciclovir, Valacyclovir, Penciclovir, Docosanol,

2) Anti-Retrovirus
i) Nucleoside Reverse Transcriptase Inhibitors (NRTIs): Zidovudine (AZT),
Stavudine, Lamivudine, and Abacavir.
ii) Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs): Nevirapine,
Efavirenz, and Delavirdine.
iii) Retroviral Protease Inhibitors: Ritonavir, Indinavir, Nelfinavir, Saquinavir,
Amprenavir, and Lopinavir.
3) Anti-Influenza Virus: Amantadine, and Rimantadine.
4) Non -Selective Anti -viral drugs : Ribavirin , Lamivudine,
Indications
To treat infections due to following viruses :
1) Influenza A viruses
2) Herpes viruses
3) Cytomegalovirus (CMV) Infection
4) HIV Infection
5) Hepatitis B and C viruses

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6) Some viruses cause warts and Eye infections.
Contraindications
1) Previous history of allergy to the drug
2) Renal impairment
3) Pregnancy and lactation
4) Severe CNS disorders
5) Hepatic dysfunction
6) Bone marrow suppression

Anti- Amoebic Agents

Introductions
The drugs are used to treat Amoebiasis Infection are called Anti - Amoebic
agent .
Amoeba is a Parasite which affects intestine and extraintestinal parts of the
body including lungs , liver and brai n .
classification
1) tissue amoebicides
A) For intestinal and Extraintestinal amoebiasis :
I. NItroimidazoles : *Metronidazole , Tinidazole , Ornidazole .
II. Alkaloids : *Emetine and Dehyroemetine .
B) For extraintestinal Aboebiasis only : *Chloroquine .
2) Luminal Amoebicides :
a) Amides : Diloxanide furomate , Nitazoxanide .
b) Antibiotics : Tetracycline , Paramomycin .
Indication :
To treat
1) Amoebiasis
2) Giardiasis
3) Trichomoniasis ( sexually T . D. )
4) Anaerobic bacterial Infection
5) H. Pylory Infection
Contraindication
Renal disease , Pregnancy , in children

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Anthelmintic Drugs
Introduction
Anthelmintics are a type of medicine that kills helminths. Helminths are
worm-like parasites such as flukes, roundworms, and tapeworms .
It is important that anthelmintics are selectively toxic to the parasite and not
the host. Some work by inhibiting metabolic processes that are vital to the
parasite but absent or not vital in the host.
Classification
1. Benzimidazoles : Albendazole , Mebendazole .Flubendazole .
2. Hetrocyclics : Oxamniquine .
3. piperazine derivatives : Piperazine citrate.
4. Amides : Niclosamide
5. Natural Product : Ivermectin
Indications
these are used to treat the Infections caused by :
1) Hookworm
2) Roundworm
3) Pinworm
4) Liver Fluke
5) Tapeworm
Contraindication
They should not be given in
pregnancy , renal and hepatic disease , severe diarrhea and malnourishment .

Anti- Malarial Agents

Introduction
The drugs are used to treat malaria are called anti - malarial drugs .
Malaria is a life-threatening disease, transmitted through the bite of an
infected female Anopheles mosquito, carrying the Plasmodium parasite. The
infected mosquito releases the parasite in the blood by biting an individual.

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Classification
1) 4-Aminoquinolines: Chloroquine, Amodiaquine, and Piperaquine.
2) Quinoline-Methanol : Mefloquine.
3) Cinchona Alkaloid : Quinine and Quinidine.
4) Biguanides: Proguanil (Chloroguanide) and Chloroproguanil.
5) Diaminopyrimidines: Pyrimethamine.
6) 8-Aminoquinolines: Primaquine and Bulaquine.
7) Sulfonamides and Sulfone: Sulfadoxine, Sulfamethopyrazine, and Dapsone.
8) Tetracyclines: Tetracycline and Doxycycline.
9) Sesquiterpene Lactones: Artesunate, Artemether, and Arteether.
10) Amino Alcohols: Halfofantrine and Lumefantrine.
Indications
To treat malaria :
1) Malaria
2) Chloroquine is used with metronidazole in amoebiasis .
3) It is used in giardiasis
4) Chloroquine is used in Arrhythmias
5) In rheumatoid arthritis
Contraindication
1) Pregnancy and Lactation
2) Bone marrow suppression .
3) severe renal impairment .

Anti -Neoplastic Agents

Introduction
The drugs are used to treat cancer are called anti -neoplastic agents . Cancer
is a disease characterised by abnormal and uncontrolled cell division attacking
the surrounding tissues and organs, and also the other body parts by
circulating with blood and lymph.

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classification

1) Alkylating agents
 Nitrogen mustards: Mechlorethamine (Mustine HCI), Ifosfamide,
Cyclophosphamide, Chlorambucil, and Melphalan
 Ethylenimine: Thio-TEPA
 Alkyl sulfonate: Busulfan
 Nitrosoureas: Carmustine (BCNU) and Lomustine (CCNU)
 Triazine : Dacarbazine (DTIC)

2. Antimetabolites
 Folate antagonist: Methotrexate (Mtx)
 Purine antagonist: 6-Mercaptopurine (6-MP), 6-Thioguanine (6 -TG), and
Azathioprine
 Pyrimidine antagonist: 5-Fluorouracil (5-FU) and Cytarabine (cytosine
arabinoside)

3. Natural Products
 Vinca alkaloids: Vincristine (Oncovin) and Vinblastine
 Taxanes : Paclitaxel and Docetaxel
 Epipodophyllo toxin: Etoposide
 Camptothecin analogues: Topotecan and Irinotecan

4. Antibiotics:
Actinomycin D, Dactinomycin, Doxorubicin, Daunorubicin, Rubidomycin,
Mitoxantrone, Bleomycin, Mitomycin C, and Mithramycin
5. Enzymes:
Asparaginase
6. Miscellaneous:
Hydroxyurea, Procarbazine ,L-Asparaginase, Cisplatin, and Carboplatin
7. Hormone Balance altering gents
 Glucocorticoids: Prednisolone
 Estrogens: Fosfestrol and Ethinylestradiol
 Antiestrogen: Tamoxifen
 Antiandrogen: Flutamide
 5-α reductase inhibitor: Finasteride
 GnRH (Gonadotropin Releasing Hormone) analogues: Nafarelin and
Goserelin

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 Progestins: Hydroxyprogesterone , Acetate
8. Radioactive Isotopes:
Sodium phosphate, Sodium iodide, and Radio gold solution
Indications
these are used to treat ,
1) Breast Cancer
2) Ovarian cancer
3) cervical cancer
4) blood cancer
5) Neck carcinomas ( cancer of epithelia tissues )
6) certain lymphomas
7) Bladder cancer
8) Mechlorethamine is used in Bone Marrow Cancer Like Polycythemia ,
Leukemia Thrombocythemia .
9) Cyclophosphamide is mostly used for treating different cancers .
10 ) Ifosfamide is used to treat , Neck carcinomas , certain lymphomas and
Bladder cancer .
11 ) Vinblastine sulphate is used to treat neuroblastoma( cancer of adrenal
gland ) , testicular cancer , kapsosi's sarcoma ( cancer of soft tissues with
lesions )
Contraindications
1) previous history of allergy
2) pregnancy and lactation
3) bone marrow suppression
4) Renal and hepatic disorders
5) GI ulceration

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Pharmacology chapter 12

Biologicals

Definition
Biological , biopharmaceuticals or biologics are substances (medicinal products) made from
a living organism or contain components of living organism . e.g. Vaccines , blood ,
hormones etc.
 Biologicals include a wide variety of products derived from human , animal or
microorganism by using biotechnology .
 Biological products may contain proteins that control the function of other proteins ,
cellular process and gene which regulate the production of vital proteins .
 Biologics may content modified human hormones or cells which produce the
substances that suppress or activate the immune system .
Types
Following are some of the common classes of biologics:
1) Blood or other blood products (platelets)
2) Steroid hormone therapies (oestrogen, testosterone) 3) Vaccines (for disease prevention)
4) Antitoxins (for a snakebite) 5) Recombinant proteins (insulin or erythropoietin)
6) Recombinant nucleic acids (developed for genetic hypercholesterolemia)
7) Interleukins (immune molecules used to treat certain infections and cancers)
8) Tendons, ligaments, or other materials used for transplantation
9) Monoclonal antibodies (used to treat autoimmune diseases and cancer)
10) Stem cell therapies (for certain cancers or genetic diseases)
11) Gene therapies (for genetic conditions).

Indications with Example

The recently-developed biologic have been used for the treatment of autoimmune
diseases, cancer, and certain genetic conditions. Examples
1) Rheumatoid arthritis
2) Psoriasis
3) Ankylosing spondylitis 4) Crohn's disease
5) Multiple
6) Diabetic retinopathy
7) Age-related macular degeneration

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8) Diabetes
9) Gastric cancer
10) Breast cancer
11) Colon cancer
12) Forms of leukaemia and lymphoma
13) Infertility
14) Osteoporosis
15) Cystic fibrosis
16) Haemophilia
Treatment of autoimmune disorder with biologicals
TNF Blockers or anti- TNF : TNF means Tumor Necrosis Factor , these drugs are used to
treat autoimmune disorders , they suppress the immune system , Examples :
1) Adalimumab 2) Golimumab 3) Infliximab 4) Abatacept .
These are used to treat : Rheumatoid Arthritis , Crohn's disease , Psoriasis etc.
Treatment of Cancer with Biologics
Biologic therapies are also very important for cancer treatment. Some of them are used as a
first-line treatment, some are used when other treatments have failed .
Biologic therapies are often used along with other treatments. Some of these treatments
are therapeutic antibodies. For example, pembrolizumab , Trastuzumab , rituximab . etc.
Treatment of Diabetes with Biologic
Insulin is used to treat Type 1 Diabetes .

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