2ND SEMESTER, A.Y.

2023 – 2024 (PRELIMS)

PHARMACOLOGY
 replenisher: supplement insufficient
INTRODUCTION TO PHARMACOLOGY
endogenous compounds
I. Overview
o Hypothyroidism = kulang sa Iodine (T1
II. Branches / Fields of Study
& T4)
III. Pharmacokinetics
o Diabetes Mellitus (Type 1)
IV. Pharmacodynamics
 Dependent
 binibigyan ng insulin
I. OVERVIEW (HISTORY)
 Babylonians  kasi kulang ang insulin na
 Greeks nirerelease ng pancreas
 Egyptians  replenisher = ROA, SQ
o Diabetes Mellitus (Type 2)
 Chinese
 Non-insulin dependent
= used plants to relieve symptoms of disease
o INSULIN = lowers the level of glucose
in the blood
PAPYRUS EBERS
 opium > opium poppy plant (can be addictive)
 DIAGNOSTIC AGENT
o DOBUTAMINE
MORPHINE
 pampapagod ng heart
 papaver somniferum
 Pharmacologic Stress Test:
 analgesic/pain reliver papagurin ng isang drug ang
puso na katumbas ng isang
DIGOXIN activity na kelangan gawin ni
 for Heart Failure patient. (example: para
 powerful inotropic agent (papatibukin ng mapagod yung heart ni patient
malakas) kelangan mag threadmill pero
 increase contractility of the heart dahil walang limbs si patient,
gagamit ng dobutamine para
PHARMACOLOGY mapagod yung heart ni patient
 a distinct discipline when the first department since hindi applicable kay
of Pharmacology patient mag threadmill)
 first established in Estonia in 1847 – Northern o METACHOLINE
Europe  cholinergic agent
 parasympathetic
JOHN JACOB ABEL  mnemonics:
 Father of American Pharmacology DUMBBELLS/DUMBELS
 Founded the 1st Pharmacology department in  diagnostic agent for Asthma
US in the University Michigan in 1890  to confirm, bibigyan ng
metacholine, since it causes
bronchoconstriction = liliit
CONCEPTS yung air passage which
PHARMACOLOGY causes SOB
 Greek words: ‘Pharmakon’ (drugs or
medicine), ‘logos’ (study)  CHEMOTHERAPEUTIC AGENT
o ‘kill’ (-cidal) or inhibit (-static) the
 study of chemical drugs on living tissues
growth of foreign cells in the body
(humans/animals) and how these chemicals
o ANTI bacteria, fungi, virus, cancer
help diagnose, treat, cure, and prevent
cells
disease (prophylaxis) or correct the
o usually listed in United States
pathophysiology of living tissues
Pharmacopeia or British
 effects, fate/disposition, clinical uses
Pharmacopeia
o may mga gamot na tinatawag na
 to check the drugs if it is
diagnostic and prophylactic agents
clinically effective and safe
DRUG
 any article that is used in the diagnosis,
mitigation, treatment, cure of diseases
 functional modifier (common function of
drug): alter the biochemical and physiological
processes/activities of the cell

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2ND SEMESTER, A.Y. 2023 – 2024 (PRELIMS)
ACTION OF DRUG
 chemical change or effects that a drug has on DRUG SIZE
the body cells or tissues  for specificity of action and mobility of drug in
the body
INDICATION  ALTEPLASE: Thrombolytic (intra-atrial) = for
 documented usefulness of a specific drug to treatment of MI/stroke
combat or treat certain diseases o ‘thrombo’ (platelets/blood clot), ‘lytic’
o THALIDOMIDE > pharmacovigilance (sira)
 sisirain ang blood clot ni
CONTRAINDICATION patient
 list of conditions for which a drug should not be  may malaking drug size
given
o WARFARIN = pantanggal ng clot / DRUG REACTIVITY and RECEPTOR BONDS
ididisolve yung clot  determine the duration of effect
 side effect: bleeding  Covalent: ASA = (Acetylsalicylic Aspirin)
 paano kung binigay sa o ASPIRIN (covalent COX 1 & 2 =
pregnant? magkakaroon ng irreversible)
nasal hypoplasia (hypoplastic  at risk of bleeding
nose/pango)  Electrotastic Bonding: H bonds and VDW
 is known to be Teratogenic:  Hydrophobic Bonding: for highly Iipophilic
affect the fetus, so drugs
contraindicated to pregnant o ‘lipo’ (fat), ‘philic’ (lover)
o GRISEOFULVIN = antifungal
SIDE EFFECTS  isasabay sa high fatty meal >
 additional effects of the drug that is not magfoform ng micelle kaya
necessarily the main purpose of giving the mas maabsorb ng katawan
drug
o side effects are not always bad, can DRUG SHAPE
also be beneficial  permits binding to the Receptor
o Diarrhea  “Lock-and-Key” Theory
MINOXIDIL o compliment each other
 for Hypertension o Conformational Changes:
 side effect: dadami ang buhok magbabago ng 2nd receptor para mag
 for hair growth to prevent hair fit yung drug sakanya/ nagc-change
baldness (alopecia) shape for the drug (Induced Fit
METFORMIN Theory)
 for Diabetes Mellitus  Chirality/Stereoisomer Carvedilol; Thalidomide
 pampapayat = for o CARVEDILOL
obese/obesity which may lead  Betablocker for Hypertension
to Lactic Acidosis  Isomers - S(atan) which is
masama
RECEPTOR
 molecule that is the target of
pharmacologically-active substances SOURCES OF DRUGS
 API (Active Pharmaceutical Ingredient) 1. Minerals
 Au (Gold) = ginagamit for Rheumatoid
Arthritis (oral)
PHYSICAL NATURE OF DRUGS 2. Salt of Inorganic Compounds
 Drug molecule must have the appropriate size,  Kremil S (antacids): orangey-antacid
electrical charge, shape and atomic o with Aluminum and
composition. Magnesium
 A drug is often administered at a location o If Aluminum lang, Constipation
distant from its intended site of action. (Ala Tae)
 Physical state of the drug often determines the o If Magnesium lang, Diarrhea
best route of administration. (Mag Tae)
o ROA = oral, topical, parenteral, rectal,  therefore, antacids
vaginal must be in a
combination
 Most of drugs enter into SYSTEMIC 3. Animals
CIRCULATION except TOPICAL  galing sa pig ang insulin before
 TOPICAL = action is ON the skin (history)
 TRANSDERMAL = action is THROUGH the
skin (ex: salonpas)

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2ND SEMESTER, A.Y. 2023 – 2024 (PRELIMS)
4. Plants Example drugs: gabapentin, amlodipine,
 BABYPLANTS (10 medicinal trazodone
plants) Category D There is positive evidence of human fetal
o Bawang risk based on adverse reaction data from
o Akapulko investigational or marketing experience or
o Bayabas studies in humans, but potential benefits
o Yerba Buena may warrant use of the drug in pregnant
o Pansit-Pansitan/Ulasimang women despite potential risks.
Bato Category X Studies in animals or humans have
o Lagundi demonstrated fetal abnormalities and/or
o Ampalaya there is positive evidence of human fetal risk
o Niyog-Niyogan based on adverse reaction data from
o Tsaang Gubat investigational or marketing experience, and
o Sambong the risks involved in use of the drug in
5. Synthetic Sources pregnant women clearly outweigh potential
benefits.
 Aspirin > Bark of Willow Tree Example drugs: atorvastatin, simvastatin,
methotrexate, finasteride

CLASSIFICATION OF DRUGS
1. Prescription Drugs Vs. OTC Drugs
 Rx = recipe
 Prescription Drugs: needs
prescription
 OTC Drugs: w/o Rx / Prescription
o ex: Paracetamol
o We must advocate the
responsible use of
antibiotics to
AMR (Antimicrobial
Resistance)
2. Investigational Drugs
 Drug development (Stages)
o Pre-clinical: animals
o Clinical: humans
3. Orphan Drugs
 mahal, wala gusto bumili kaya orphan)
 for rare diseases (too costly)
 hindi pa natatapos ang study kasi
masyadong mataas ang cost of
research
4. Illicit Drugs
 ex: Ecstasy
 RA 9165 Dangerous Drugs Act of

FDA Pregnancy Categories

Category A Adequate and well-controlled studies have
failed to demonstrate a risk to the fetus in the
first trimester of pregnancy (and there is no
evidence of risk in later trimesters).
Example drugs or substances:
levothyroxine, folic acid, liothyronine
Category B Animal reproduction studies have failed to
demonstrate a risk to the fetus and there are
no adequate and well-controlled studies in
pregnant women.
Example drugs: metformin,
hydrochlorothiazide, cyclobenzaprine,
amoxicillin
Category C Animal reproduction studies have shown an
adverse effect on the fetus and there are no
adequate and well-controlled studies in
humans, but potential benefits may warrant
use of the drug in pregnant women despite
potential risks.

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2ND SEMESTER, A.Y. 2023 – 2024 (PRELIMS)
Drug Scheduling Guide (United States) PHARMACOGNOSY
Schedule I  Science that deals with the study of drugs
 Most potential abuse and dependence derived from natural sources
 No medicinal qualities o plants, microorganisms, animals
 Heroin, LSD, Marijuana, Ecstasy, Peyote  Antibiotic: bacteria fighting other bacteria

Schedule II PHARMACOVIGILANCE
 High potential for abuse and dependence  Science and activities relating to the detection,
 Some medicinal qualities assessment, understanding, and prevention of
 Vicodin, Cocaine, Meth, OxyContin, Adderall adverse effects, or any other medicine/vaccine
related problem (WHO).
Schedule III  Refers to the continuous monitoring of
 Moderate potential for abuse/dependence unwanted effects and other safety related
 Acceptable medicinal qualities aspects of marketed drugs.
 Doctor’s prescription required  THALIDOMIDE disaster nagkaroon ng PV
 Tylenol with Codeine, Ketamine, Steroids, o for morning sickness
Testosterone  side effects: lalabas na baby,
no limbs (phocomelia/amelia)
Schedule IV o for cancer (prototype)
 Low potential for abuse and dependence
PHARMACOEPIDEMIOLOGY
 Acceptable medicinal qualities
 Prescription required – fewer refill regulations  Study of both the beneficial and adverse
 Xanax, Darvon, Valium, Ativan, Ambien, effects of a drug on large number of people.
Tramadol
TOXICOLOGY
Schedule V  Branch of Pharmacology, which deals with the
 Lowest potential for abuse/dependence undesirable effects of chemicals on living
 Acceptable medicinal qualities systems
 Prescription required – fewest refill regulations o Narrow Therapeutic Index (konting
 Robitussin AC, Lomotil, Motofen, Lyrica kamali sa dose, pwedeng mamatay si
patient)
Source: United States Drug Enforcement Agency  Example: APAP:
Paracetamol (metabolism) –
once ma overdose or
DRUG NAMES magkaroon ng medication
I. Generic Name (Official Name) versus Trade Name error, it can lead to
II. Chemical Name HEPATOTOXICITY (chronic)
 Ax: Antidotes (N. Acetylcysteine-mucolytic):
paglagay mo sa tubig magb-bubbles
BRANCHES/FIELDS OF STUDY
PHARMACEUTICS PHARMACOKINETICS
 Science of medicine’s design: formulation,  What the body does to the drug; fate and
manufacturing stability, and effectiveness. disposition of drugs in the body
 ROA: oral, parenteral (IM, IV, SQ), vaginal,  ADME (Absorption, Distribution, Metabolism,
rectal, topical Elimination/Excretion)
 konti/maliit lang ang active ingredient sa drug o First Pass Effect (FPE) – Parenteral
but nagdadagdag ng diluent para maging 100%
appealing at maganda ang itsura ng tablets  LADMERT (Liberate, Absorb, Distribute,
o pero walang pagbabago o difference Metabolize, Excrete, Response, Toxic Effects)
sa effect (same na same parin)
 Film-coated drugs: DO NOT CRUSH!!

PHARMACOTHERAPEUTICS
 Concerned with the clinical uses of drugs
 Therapeutic Duplication:
o To reduce cost sa px
o To reduce drug interaction
 the more interaction, the more
pwedeng lumala ang sakit ni
patient

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2ND SEMESTER, A.Y. 2023 – 2024 (PRELIMS)
PHARMACODYNAMICS
 What the drug does to the body; how the
drugs produce its effects on the effect on the
body
 Molecular Mechanism of Action (MOA), drug
receptor interaction, dose response curve

Pharmacokinetics and Pharmacodynamics

Drug Administration
Distribution
Absorption Tissues and Other
Extravascular Sites
Blood Pharmacokinetics

Distribution
Drug Metabolism
Drug Target Site and Excretion
Elimination

Pharmacologic Effect

Pharmacodynamics

Clinical Response

Adverse Benefit

PHARMACOKINETICS
 The study of the fate/disposition of a drug
 What the body does to the drug BIOAVAILABILITY (F)
 It is the fraction of administered drug in a
ABSORPTION chemically unchanged form that reaches the
 Transfer of a drug from its site of systemic circulation.
administration to the bloodstream  Parenteral = 100%
 Oral < 100% (FPE)
Physical Factors affecting Absorption  Other routes < 100%
1. Blood flow to the absorption site
2. Total surface area available for absorption How much of a 500mg dose is bioavailable if the
o in the small intestine (contains administered drug has an F of 75%?
microvillis) Formula: 500mg x 0.75
3. Contact time at the absorption surface
Factors that Influences Bioavailability
1. First-Pass Hepatic Metabolism
Difference Active Passive Transport 2. Solubility of a Drug
Transport goes along 3. Chemical Instability
goes against concentration gradient 4. Nature of Drug Formulation
concentration
gradient DISTRIBUTION
Energy Simple Diffusion:  Process by which a drug reversibly leaves the
Facilitated Diffusion: bloodstream and enters the interstitium
Carrier Simple Diffusion:
(extracellular fluid) and/or the cells of the
Mediated Facilitated Diffusion:
tissue
Saturable Simple Diffusion:
 Once a drug is injected or absorbed in the
Facilitated Diffusion:
bloodstream; it is carried by the blood and
tissue fluids to its sites of pharmacologic
action, metabolism, and excretion.

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2ND SEMESTER, A.Y. 2023 – 2024 (PRELIMS)
Factors affecting Distribution BIOTRANSFORMATION
1. Blood Flow  Process by which chemical reactions carried
2. Capillary Structure out by the body convert a drug into a
3. Binding of drugs to CHON compound different from that administered
4. Relative hydrophobicity of the drug originally
o HIPE

Why should a drug undergo biotransformation?

 To convert a drug into a more excretable form
 To convert a pharmacologically active drug to
LUNA HIPE inactive metabolite
 lipophilic  hydrophilic  To convert an active drug to an active
 unionized  ionized metabolite
 non-polar  poplar  To convert an inactive drug to an active
 absorbed  excreted metabolite
example: example:  To convert a drug into a more toxic metabolite
absorbed - stomach “ihi” – naging water
soluble yung drug PRODRUGS
 Drugs that are inactive are converted to active
 Drug distribution during pregnancy and forms
lactation is also unique o CHLORAMPHENICOL
 During pregnancy, most drugs cross the  Dati drug of choice sa typhoid
placenta and may affect the fetus fever pero super pait
 During lactation, many drugs enter breast milk Reasons:
and may affect the nursing infant 1. To improve unfavorable physical properties
o MORPHINE 2. To improve unfavorable pharmacokinetic
 pwede magcross sa placenta properties
at makaapekto kay baby 3. Prodrug approach is more efficient and
 pwede mag-cause ng cheaper
withdrawal effects kay baby =
diarrhea 2 ACE inhibitors (-pril)
 All ACEi are prodrugs except CEL (Captopril,
Which is preferred? Enalaprilat, Lisinopril)
Molecular size High MW Low MW
Lipid solubility Highly lipid Lowly lipid
soluble soluble
Drug half-life Longer t50 Shorter t50
Protein Free Bound
pKa Low pKa High pKa

METABOLISM
 Metabolism is the method by which drugs are
inactivated or biotransform by the body.
 Most often, an active drug is changed into one
or more inactive metabolites, which are then
excreted.

DETOXIFICATION
 Involves conversion of foreign agents into
substances of less potential toxicity
o foreign agents = XENOBIOTICS
o less potential toxicity = HIPE

METABOLISM (Biochem)
 Sum of chemical changes in living cells by
which energy is provided for vital processes
and activities and new materials are produced
and assimilated for growth and maintenance.

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KINETIC OF DRUG BIOTRANSFORMATION o Slow-Acetylators: African, American,
1. First-Order Kinetics Egyptians, Caucasians
o metabolic transformation of drugs is o Mabagal i-metabolize or i-
catalyzed by enzymes HIPE yung gamot; kaya
o the rate of drug metabolism is directly mababa yung dose
proportional to the concentration of o Fast-Acetylators: Asian, Eskimos,
free drug Filipino
o Examples: most drugs o mabilis i-metabolize; kaya
mataas yung dose
2. Zero-Order Kinetics
o the rate of drug metabolism remains GLYCINE CONJUGATION
constant over time o transformation of Benzoic Acid to
o a constant amount of drug is Hippuric Acid
metabolized per unit time
o Example: TAPES: Theophylline, ASA GLUTATHIONE CONJUGATION
(Aspirin), Phenytoin, Ethanol, o Enzyme: Glutathione-S-transferase
Suspension o antioxidant

SULFATION
REACTIONS OF DRUG BIOTRANSFORMATION o Present at birth (good news)
1. PHASE I o Enzyme: Sulfotransferase
o function to convert lipophilic molecules
into more polar molecules by METHYLATION
introducing or unmasking a polar o Enzyme: Methyltransferases
function group o Nonpolar, inductive
o FUNCTIONALIZATION – introduction o “fight and flight”
of a new functional group  Norepinephrine
o Phase 1 reactions are functionalization  Epinephrine
reactions, frequently adding a new  Dopamine
oxygen atom or exposing an existing
functional group CRASH CART
o NOREPINEPHRINE
OXIDATION  septic shock
 Addition of oxygen or removal of hydrogen  sepsis = infection
from the original compound o EPINEPHRINE
 Carried out by a group of monooxygenase  anaphylactic shock
(oxidative enzymes found in the hepatic ER),  too much stimulation
mainly CYP450 enzymes of histamine or lahat
ng nagc-cause ng
REDUCTION inflammation
 the removal of oxygen or the adding of ENZYME INDUCTION ENZYME INHIBITION
hydrogen to the original compound involves protein synthesis, decrease of the rate of
 enzymes responsible are usually located in the needs time up to 3 weeks metabolism of a drug by
cytoplasm to reach a maximal effect another one; leading to
toxicity
enzyme = metabolism enzyme = metabolism
2. PHASE II ( plasma concentration) ( plasma concentration)
GLUCURONIDATION Result: activity Result: activity
o most common and most important Example: St. John’s wort Example: Grapefruit juice
inducible, reduced activity in neonates
(1-30 days)
o Enzyme: Glucuronyltransferase
o CHLORAMPHENICOL =
babies
 fate of meta = gray
baby syndrome BIOTRANSFORMATION
 Most drugs are biotransformed before being
ACETYLATION eliminated
o Enzyme: N-Acetyltransferase  Drug metabolites are generally more polar
o ISONIAZID = treatment to TB than their parent compound
o RIPE/S (Rifampicin, Isoniazid,  Concurrent ingestion of two or more drugs can
Pyrazinamide, Ethambutol, affect the rate of metabolism of one or more of
Streptomycin) them

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