INTRODUCTION TO

PHARMACOLOGY
BY
DR MOHAMMED O.H
 PHA 311
• Pharmacology can be defined as the study of
the effects of drugs on the function of living
systems
• Subdivision of Pharmacology include
 Neuropharmacology
 Immunopharmacology
 Cardiovascular pharmacology
 Respiratory pharmacology
 Gastrointestinal pharmacology
 Pharmacogenomics
 CON’T
• Pharmacology encompasses all aspects of
knowledge about drugs, but most importantly
those that are relevant to effective and safe
use for medicinal purposes.
• Drug is any chemical substance that can
produce effect in a biological system
• Oswald Schmiedeberg, regarded as the father
of pharmacology.
• The two main divisions of pharmacology are
pharmacodynamics and pharmacokinetics.
 BASIC PHARMACOLOGY TERMS
• Pharmacology: Pharmacology is the study of
interaction of drugs with living organisms.
• It also includes history, source, physicochemical
properties, dosage forms, methods of
administration, absorption, distribution
mechanism of action, biotransformation,
excretion, clinical uses and adverse effects of
drugs.
• Clinical Pharmacology: It evaluate the
pharmacological action of drug preferred route of
administration and safe dosage range in human
by clinical trails.
 CONT’D
• Drugs: Drugs are chemicals that alter
functions of living organisms.
• Drugs are generally given for the diagnosis,
prevention, control or cure of disease.
• Pharmacy: It is the science of identification,
selection, preservation, standardisation,
compounding and dispensing of medical
substances.
• Pharmacodynamics: The study of the
biological and therapeutic effects of drugs (i.e,
“what the drug does to the body”).
 CONT’D
• Pharmacokinetics: Study of the absorption,
distribution metabolism and excretion (ADME) of
drugs (“i.e what the body does to the drug”).
• Pharmacotherapeutics: It deals with the proper
selection and use of drugs for the prevention and
treatment of disease
• Toxicology: It’s the science of poisons. Many
drugs in larger doses may act as poisons.
• Poisons are substances that cause harmful,
dangerous or fatal symptoms in living substances.
 CONT’D
• Chemotherapy: It’s the effect of drugs upon
microorganisms, parasites and neoplastic cells
living and multiplying in living organisms.
 SOURCES OF DRUGS
• Drugs are obtained from various sources which includes

1. Minerals: Liquid paraffin, magnesium sulfate, magnesium

trisilicate, kaolin, etc.
2. Animals: Insulin, thyroid extract, heparin and antitoxin sera, etc.
3. Plants: Morphine, digoxin, atropine, castor oil, etc.
4. Synthetic source: Aspirin, sulphonamides, paracetamol,
zidovudine, etc.
5. Micro organisms: Penicillin, streptomycin and many other
antibiotics.
6. Genetic engineering: Human insulin, human growth hormone
etc.
• Out of all the above sources, majority of the drugs currently used
in therapeutics are from synthetic source.
 DRUG NAMING
• A drug generally has three categories of
names
(a) Chemical name : It describes the substance
chemically, e.g. 1-(Isopropylamino)-3-(1-
naphthyloxy) propan-2-ol for propranolol.
This is cumbersome and not suitable for use
in prescribing.
(b) Non-proprietary name or generic name : It is
the name accepted by a competent scientific
body/authority, e.g. the United States Adopted
Name (USAN) by the USAN council.
 CONT’D
(c) Proprietary (Brand) name : It is the name
assigned by the manufacturer(s) and is his
property or trade mark. One drug may have
multiple proprietary names, e.g. ALTOL,
ATCARDIL, ATECOR, ATEN, BETACARD, LONOL,
TENOLOL, TENORMIN for atenolol from different
manufacturers
• Brand names are designed to be catchy, short,
easy to remember and often suggestive, e.g.
LOPRESOR suggesting drug for lowering blood
pressure.
 Prescription Vs Over the counter drugs
• Prescription drugs are drugs retailed only
against a prescription issued to a patient by a
registered medical practitioner
• Majority of drugs fall into this category
including antibiotics
• Over The Counter Drugs : few drugs like
simple analgesics (paracetamol aspirin),
antacids, laxatives (senna, lactulose), vitamins,
ferrous salts, etc. are considered relatively
harmless, and can be procured without a
prescription.
 HOW DRUGS ACT
• One of the basic tenets of pharmacology is
that drug molecules must exert some chemical
influence on one or more constituents of cells
in order to produce a pharmacological
response.
• Paul Ehrlich stipulates that ‘drug molecules
must be ‘bound’ to particular constituents of
cells and tissues in order to produce an effect’
• There are four main kinds of regulatory
protein involved as primary drug targets,
namely
 CONT’D
 Receptors
 Enzymes
 Carrier molecules (transporters)
 Ion channels.

• Receptors In pharmacology are protein

molecules whose function is to recognise and
respond to endogenous chemical signals
• RECEPTORS are specific to individual drugs
• Enzyme such as dihydrofolate reductase is the
‘receptor’ for methotrexate
• Ion channel such as the voltage-sensitive
sodium channel is sometimes referred to as
the ‘receptor’ for local anaesthetics
ROUTE OF DRUG ADMINISTRATION
• These are the means by which administered
drugs gets into the circulation or place of
action.
• The RODA depends on so many factors and
eac route has its own advantages and
disadvantages.
• Basically RODA can be broadly divided into
 Local RODA
 Systemic RODA
 LOCAL RODA
• In the local RODA, the administered drugs are
basically not been absorbed into the systemic
circulation. They act at site of administration.
Example include
 Dermal patches
 Intravaginal pessaries
 Eye/ear drops
 Ointments
• Absorption through mucous membrane may be rapid.
• Absorption through skin generally slow; enhanced by
increased lipophilicity, by damage to stratum
corneum, and by increased blood flow.
 SYSTEMIC RODA
• These methods leads to systemic circulation of
the administered drugs

• It can be classified into

 Enteral (oral and rectal)

 Parenteral ( IV,IM,IT,SC,ID,SL,SB,Inhalational)
 Advantages of ORAL RODA
• It is not invasive
• It doesn’t require expertise administration
• Drugs can be recalled in case of wrong drug
administration
• Easy means of administration
• It has less serious complication in cases of
overdose
 Disadvantages of ORAL RODA
• Patients are usually poorly compliant
• It undergoes first pass effect thereby reducing
the administered dosage
• Onset of action is slow
• It cannot be use for an emergency or for an
unconscious patient
 Advantages of IV RODA
• Onset of drug action is rapid(fast)
• Patient compliance is high as it cant be self
administered mostly
• It can be use in cases of emergency and
unconscious patient
• It bypass the first pass effect
 Disadvantages of IV RODA
• Severe complications if drugs are wrongly
administered or doses exceeded
• The need of an expertise for administration
• It is invasive
• Complications such as thromphlebitis is
common
• Drugs cannot be recalled
• Insoluble drugs cannot be administered
 OTHERS
• Sublingual(SL): Good absorption through capillary
bed under tongue. Drugs are easily self-
administered. Because the stomach is bypassed, and
lability and gut-permeability need not be
considered.
• Rectal: Useful for unconscious or vomiting patients
or small children. Absorption is unreliable.
• Intramuscular (IM): Drug passes through capillary
walls to enter the blood stream. Rate of absorption
depends on formulation (oil-based preparations are
absorbed slowly, aqueous preparations are absorbed
rapidly). May be used for self-administration by
trained patients.
 CON’T
• Subcutaneous (SubQ, SC): Drug is injected
beneath the skin and permeates capillary walls to
enter the blood stream. Absorption can be
controlled by drug formulation.
• Inhalation : Generally rapid absorption. Some
agents, marketed in de vices which deliver
metered. Suitable for self-administration. Rapid
absorption of drugs in gaseous, vaporized or
aerosol form. Absorption of particulates/aerosols
depends on particle/droplet size which influences
depth of entry in pulmonary tree; 1-5 uM
particles reach alveolus
 PHARMACOKINETICS
• Pharmacokinetics (PK) is defined as the action of the
body on the drugs.
• Pharmacokinetics is the study of drug absorption,
distribution within body, biotransformation and drug
elimination over time
• It involves the following
 Absorption
 Distribution
 Metabolism(Biotransformation)
 Excretion
• Other terms of note include BIOAVAILABILITY ,
VOLUME OF DISTRIBUTION AND FIRST PASS EFFECT.
 ABSORPTION
• Absorption : This is the process by which
administered drugs get to the systemic circulation.
Its dependent on a host of factors
• The process by which drug proceeds from the site
of administration to the site of measurement (blood
stream) within the body.
• Necessary for the production of a therapeutic effect.

• Most drugs undergo gastrointestinal absorption.

This is extent to which drug is absorbed from gut
lumen into portal circulation
• Exception: IV drug administration
 Factors affecting absorption
• Broadly divided into 2
1 Pharmaceutical factors
Physicochemical properties of drug
Dosage form characteristics
2 Patients related Factors

• Physicochemical properties of drug include

 Drug solubility and dissolution rate
 Particle size and surface area
 Lipophilicity of the drug
 pH of the drug
 Drug stability
 Patients related Factors
• Age
• Gastric emptying time
• Intestinal transit time
• Gastrointestinal pH
• Disease states
• Blood flow through the GIT
• Gastrointestinal contents (other drugs, food,
fluids)
• Presystemic metabolism (gut wall enzymes,
bacterial enzymes, hepatic enzymes)
 DISTRIBUTION
• Distribution is the process by which drugs in
systemic circulation moves to sites of
action(tissue)
• Factors affecting didtribution includes all
factors that affect absorption plus the following
 Blood flow:
 Capillary permeability:
 Plasma protein binding
 Nature of drug/Nature of tissue
 OTHERS :(Pregnancy,Obesity,Diet,Disease state,
Drug interaction)
 CONT’D
• Blood flow: Distribution occurs most rapidly
into tissues with high blood flow (lungs,
kidneys, liver, brain) and least rapidly in tissues
with low flow (fat).
• Capillary permeability: Permeability of
capillaries is tissue dependent; CNS capillaries
are less permeable to drugs because of the
blood brain barrier and other CNS efflux pump
• Plasma protein binding: some drugs binds
reversibly/irreversibly. Some have a higher
affinity for albumin and other plasma protein
 CONT’D
• Many drugs bind to plasma proteins in the
blood steam
• Plasma protein binding limits distribution.
• A drug that binds plasma protein diffuses less
efficiently, than a drug that doesn’t.
 METABOLISM/BIOTRANSFORMATION
• Biotransformation is the chemical modification
of drugs by hepatic and intestinal enzymes.
• Biotransformation could either lead to
I. Activation of prodrugs into active
pharmacological agents
II. Modification of lipid soluble drugs to water
soluble drugs to aid excretion
III. Lesser pharmacological agent from parent
drug
• Failure to remove the products of metabolism
reactions can lead to toxicity of conjugates to
 Drug Metabolism
 The chemical modification of drugs with the overall goal of getting rid of the drug
 Enzymes are typically involved in metabolism

Metabolism Excretion
More polar
Drug
(water soluble)
Drug

02/13/2024 32
 ENZYME INDUCERS AND INHIBITORS
• The most important enzyme of metabolism are the
microsomal cytochrome P450 monooxygenase family of
enzymes, which oxidize drugs.
• Act on structurally unrelated drugs
• Metabolize the widest range of drugs
• CYPs are found in liver, small intestine, lungs, kidneys and
placenta
• It’s been estimated that 90% or more of human drug
oxidation can be attributed to 6 main enzymes:
CYP1A2 CYP2D6
CYP2C9 CYP2E1
CYP2C19 CYP3A4
• Some drugs are classified as enzyme inducers while
others are enzymes inhibitors
 Participation of the CYP Enzymes in Metabolism of
Some Clinically Important Drugs

CYP Examples of substrates

Enzyme
1A1 Caffeine, Testosterone, R-Warfarin
1A2 Acetaminophen, Caffeine, Phenacetin, R-Warfarin
2A6 17-Estradiol, Testosterone
2B6 Cyclophosphamide, Erythromycin, Testosterone
2C-family Acetaminophen, Tolbutamide (2C9); Hexobarbital, S-
Warfarin (2C9,19); Phenytoin, Testosterone, R- Warfarin,
Zidovudine (2C8,9,19);
2E1 Acetaminophen, Caffeine, Chlorzoxazone, Halothane
2D6 Acetaminophen, Codeine, Debrisoquine
3A4 Acetaminophen, Caffeine, Carbamazepine, Codeine,
Cortisol, Erythromycin, Cyclophosphamide, S- and R-
Warfarin, Phenytoin, Testosterone, Halothane, Zidovudine

02/13/2024 34
 Proportion of Drugs Metabolized
by the Major CYPs

CYP 1A2
CYP 2C CYP 2E1

CYP 2D6 CYP 3A4

02/13/2024 35
 Cont’d
•Enzyme Inhibitors: Cimetidine, Isoniazid,

•Enzyme Inducers: Barbiturates,

carbamazepine, rifampicin, cyclophosphamide
 Risks associated with CYP enzyme inhibition or induction

Inhibition of CYP enzymes Induction of CYP enzymes

 
Decreased degradation Increased degradation
of comedicated drugs of comedicated drugs
 
Increased drug plasma Decreased drug plasma
concentrations concentrations
 
Risk of severe Loss of pharmacological
adverse events effect

Risk of therapeutic failure

02/13/2024 37
Factors affecting biotransformation
• All the mentioned factors that affect
absorption
• Induction of drug metabolizing enzymes
• Inhibition of drug metabolizing enzymes
• Biological Factors
Species/Strain differences Disease state
Sex differences (M F ) Circadian rhythm
Age
Diet
Pregnancy
02/13/2024 38
 EXCRETION
• It is the process by which metabolites of drugs
are eliminated from the systemic circulation
• Some drugs are excreted unchanged.
• Routes of excretion includes
Urine: Most drugs are eliminated through
urine
Bile: Excreted via the feaces
Others (sweat,tears,breastmilk)
NB: Importance of breastmilk drug excretion in
babies
 Factors affecting drug excretion
• All factors mentioned to affect absorption
• Plasma concentration of drug
• Distribution and binding characteristics of
drug
• Urine pH
• Blood flow to the kidneys
• Drug interaction
• Disease states

02/13/2024 40
 FIRST PASS EFFECT
• First-pass effect: absorbed drug passes via portal
circulation through liver which may clear substantial
fraction and thus decrease bioavailability (percent of
dose which reaches the systemic circulation).
• Bioavailability: the fraction of the administered dose
reaching the systemic circulation

• A drug given by the intravenous route will have an

absolute bioavailability of 1 (F=1 or 100%
bioavavailable)

• While drugs given by other routes usually have an

absolute bioavailability of less than one.
ANY QUESTION???

THANK YOU