PHARMACOLOGY

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 INTRODUCTION TO PHARMACOLOGY
Definitions of terms
Pharmacology is the science that deals
with study of drugs and their interaction
with the living system.
A drug is a substance used in the diagnosis,
prevention and treatment of disease.
“WHO definition, a drug is any substance
or product that is used or intended to be
used to modify or explore physiological
systems or pathological states for the
benefit of recipient”. 2
Medications are drugs give for therapeutic
purposes.
Therapeutics deals with the use of drugs
in the prevention and treatment of disease.
Toxicology is the study of the adverse
effects of the drugs on the living system.
Chemotherapy is the use of chemical
agents or drugs to treat cancer or other
diseases caused by bacteria, fungi, viruses
or parasites
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Pharmacokinetics is the study of what body
does to the drug.
Pharmacodynamics is the study what the
drug does to the body.
Pharmacy is the science of identification,
compounding and dispensing of drugs. It also
includes collection, isolation, purification,
synthesis and standardization of medicinal
substances.

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Importance of studying pharmacology
•Understand drugs and how they affect living
things (human)
•Know the right dosage of drugs
•Identify and respond to interactions, reactions and
side effects and treat accordingly
•Know when to use drugs because some
conditions do not need drug therapy.
•Understand the process of drug intake,
absorption, distribution, metabolism and
elimination.
•Identify the properties of ideal drugs 5
•Know the application of pharmacology in
regard to the 5 right drug administration:
Use right drug
Give to right patient
 give right dose
Give by right route
Give at right t4ime
Right duration
•To be able to explain to clients about the
medications, dosages and possible side effects.
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Importance of pharmacology to patient
education
Promote active participation of patient in
drug therapy
Promote therapeutic effect
Minimize adverse effects
Minimize adverse interactions

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Sources of drugs

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The sources of drugs could be natural or synthetic
Natural sources
Plants, e.g. atropine, morphine, quinine, digoxine,
pilocarpine, physiostigmine
Animals, e.g. Insulin, adrenaline, heparin,
gonadotrophins and antitoxic sera
Minerals, e.g. magnesium sulphate, aluminium
hydroxide, iron, sulphur and radioactive isotopes.
Microorganisms, antibacterial agents are obtained
from some bacteria and fungi. E.g. penicillin,
cephalosporin, tetracycline and other antibiotics.
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Cont. sources of drugs
Human: e.g. immunoglobulin from blood,
growth hormone from anterior pituitary and
chorionic gonadotrophins from the urine of a
pregnant woman.
Synthetic sources
Most drugs are now synthesized e.g. quinolones,
omeprazole, sulfonamides, pancuronium,
neostigmine.

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Naming of drugs

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 Naming of drugs
The drug can have three names;
Chemical name
The name gives the chemical description or make up of the
drug. The name is length, complex and unsuitable for
prescribing, e.g. propionic acid
Non- proprietary or generic name
The name is given by an official agency like WHO and is
internationally accepted. Drugs have same generic names all
over the world, e.g. Ibuprofen, propranol, atenolol, esmolol and
metoprolol all ᵝ-blockers
Proprietary or brand name
The name is given by the manufacturer. Each drug may have
brand names, e.g. brufen®, crocin, metacin, pacemol, kamadol12
THE NATIONAL DRUG POLICY
AND AUTHORITY ACT.
An Act to establish a national drug policy and a
national drug authority to ensure the availability,
at all times, of essential, efficacious and cost-
effective drugs to the entire population of
Uganda, as a means of providing satisfactory
health care and safeguarding the appropriate use
of drugs. (established in 1993)
 National drug policy
A National Drug Policy
Comprehensive strategies assuring supply & essential
drugs use & supported by laws.
Strategies of the Uganda national drug policy,
include:
(a) to ensure that essential, safe, efficacious and
cost-effective drugs are made available to the
entire population of Uganda to provide satisfactory
health care.
(b) to make a continuous review of the needs,
knowledge and resources of essential drugs.
(c) to promote the rational use of drugs both
in the public and private sector.
(d) to improve Government regulation and
control on manufacture, production,
importation, exportation, marketing and use
of drugs.
e) to provide systematic public information
and professional training and retraining of
health workers.
(f) to improve the registration of drugs and
licensing of pharmaceutical premises.
(g) to intensify research in all types of
drugs, including traditional medicines.
(h) to comply with the international
regulations on drugs, including the
conventions on narcotic drugs and
psychotropic substances under international
control.
(i) to fight against drug and substance
abuse.
 The National Drug Authority.
Is a board of members of persons of high
integrity that implement the national drug
policy.
Functions of the national drug authority.
(a) deal with the development and regulation
of the pharmacies and drugs in the country;
(b) approve the national list of essential drugs
and supervise the revisions of the list in a
manner provided by the Minister;
(C) estimate drug needs to ensure that the
needs are met as economically as possible;
(D) control the importation, exportation and
sale of pharmaceuticals;
(E) control the quality of drugs;
(F) promote and control local production of
essential drugs;
(G) encourage research and development of
herbal medicines;
(H) promote rational use of drugs through
appropriate professional training;
(i) establish and revise professional
guidelines and disseminate information to
health professionals and the public;
(j) provide advice and guidance to the
Minister and bodies concerned with drugs
on the implementation of the national drug
policy; and
(k) perform any other function that is
connected with the above or that may be
accorded to it by law.
National list of essential drugs.
(1) There shall be a national list of
essential drugs which shall be revised
from time to time.
(2) There shall be a national formulary
made of the national list of essential drugs
and such other drugs as the authority may,
from time to time, approve.
.
ESSENTIAL DRUGs

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Essential drugs (medicines) are those drugs that
satisfy the health care needs of the majority of
the population.
Characteristics of essential drugs
 Available at all times
adequate amounts
 assured quality
 appropriate dosage forms
Affordable - a price that individuals
and the community can afford."
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 Selection criteria of essential drugs
Essential medicines are selected with due
regard to;
disease prevalence
evidence on efficacy
Evidence of safety,
comparative cost-effectiveness
 meet the needs of the majority of the
population
sufficient proven scientific data regarding
effectiveness must be available 24
 a substantial safety and risk/benefit ratio
an acceptable quality, and must be tested
on a continuous basis
containing single pharmacologically
active ingredients
combination products, as an exception,
will be included where patient compliance
becomes an important factor, or when two
pharmacologically active ingredients are
synergistically active in a product
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RATIONAL USE OF DRUGS (MEDICINES

Rational use of medicine means that patients

receive medicines appropriate to their clinical
needs, in appropriate doses and for adequate
period of time at a cost affordable to them and the
community.

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Irrational use of medicines
Irrational use of medicine involves use of:
•Too many drugs per patient
•Wrong choice of drugs for particular
condition
•Inadequate dosages
•Unnecessary use of injections where oral
dosage form can be applicable
•Indiscriminate use of antibiotics in the
treatment of viral infections such as cough,
diarrhea among others. 27
Factors that contribute to irrational use of
drugs.
Heavy patient load
Poor communication skills among health care
providers
Lack of ethics among health care providers
Inappropriate interpretation of laboratory
results
Poor attitude towards work
Misleading beliefs by the patient (patients
believe they can only be cured by injections)
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Inconsistent drug supply
Lack of medicine formulary
Promotional misleading claims by drug
companies
Inadequate drug regulation

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Consequences of irrational use of drugs
Overuse of antibiotics lead to development
of resistance
Leads to wastage of scarce resources
Leads to the increased costs of drugs to
patients
Increases adverse drug reactions
(especially with poly-pharmacy)
May lead to loss of patient confidence in
the health system
May lead to poor patient outcome
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Classification of drugs

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Drugs may be classified by:
Prescription
Pharmacological action
Legislation (legal)
Prescription
Drugs are classified basing on whether they
are obtained using:
a prescription (prescription only medicine)
 without a prescription (Over the counter
drugs).
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Prescription drugs:
These drugs can only be obtained when the
patient presents a valid prescription to a
pharmacy. Examples of prescription drugs
include:- Amoxicillin, Ciprofloxacin,
Nifedipine.
Non prescription drugs (over the counter
drugs). These can obtained either from a
pharmacy or a drug shop without a prescription,
e.g. Panadol, Hedex, vitamins, etc.

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Pharmacological action
Drugs can be classified basing on:
Target body system, e.g. cardiovascular drugs
Activity on microorganisms, e.g. antibiotics, antivirals,
antifungal, etc.
Legal
Class A drugs or narcotics: They may only imported or
exported or manufactured or used under authority. They
may be sold by retail only on prescription of a duly
qualified medical practitioner, dentist, veterinary surgeon,
but only for medical, dental or veterinary purposes. May
be supplied only by a registered pharmacist or licensed
pharmacy. e.g. Codeine, fentanyl, Morphine, Pethidine,
Cocaine, Heroin.
Class B drugs or controlled drugs: May be
supplied by retail only on prescription of a duly
qualified medical practitioner, dentist or
veterinary surgeon, but only for medical, dental
or animal treatment respectively. e.g.
Phenobarbitone, Ciprofloxacin, amoxycillin,
diazepam, griseofulvin, metformin
Class C drugs or licensed drugs. They be sold
by retail only by a person operating a licensed
pharmacy or by a licensed drug seller in
accordance with the terms of his or her license
e.g. over the counter drugs 35
PHARMACOKINETICS

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 Why Study Pharmacokinetics (PK)?
• Pharmacokinetics is used to ;

1. to individualize therapy
2. to assess adherence to therapy
3. to diagnose toxicity
4. to guide withdrawal of therapy
5. to determine whether a patient is already taking a drug before starting
therapy (eg theophylline in an unconscious patient with asthma)
6. in research (eg to monitor for drug interactions in post-marketing
surveillance using population pharmacokinetics).
 What is pharmacokinetics?
It is the study of what the body does to the
drug
or is the study of the movement of drugs into,
within or out of the body
or the study of the absorption, distribution,
metabolism and excretion (ADME) of drugs.

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Pharmacokinetic Phases: absorption, distribution,
metabolism, & excretion

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 Pharmacokinetic properties of drug determine ;

• the route(s) of administration,

• dose
• latency of onset,
• time of peak action,
• duration of action
• and frequency of drug administration.
 Routes Of Administration

Routes Of Drug
Administration

Parenteral Enteral

Injection Topical Respiratory Rectal Oral

 Drug administration
This is the process of introducing drugs into the body. The
point of administration is referred to as the site of
administration.

Drug absorption:
Is the movement of a drug from the site of
administration into the blood stream (general
circulation).
Qn: 1.drug absorption occurs by which route of drug
administration.
2. Does not occur by which route of drug
administration. 42
 Absorption
• The passage of drug from the site of
administration into the general
circulation.
• Exception: Intravenous injections
I.V Drug Oral Drug
Immediately Delayed
completely incomplete
• Drug Absorption:

• Movement of a drug from its site of administration into the

bloodstream
– For solid dosage forms (tablet or capsule), dissolution
precedes absorption
Sites of absorption
a) Stomach
 Lipid-soluble drugs & weak acids are absorbed directly from the
stomach
 Weak bases & strong acids are not normally absorbed from this
site b ’se they exist as ions

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Sites of absorption cont’d
b) Small intestine
 is the primary site of absorption of most drugs b’se of very
large SA across which drugs, including partially ionized
weak acids & bases, may diffuse. (also SI is Highly
vascularized)

 Acids are normally absorbed more extensively from the small

intestine than from the stomach, even though the intestine
has a higher pH.

02/10/2025 PHA 2111 45

 The Process
• Absorption relies on
 Passage through membranes to reach the blood
 passive diffusion of lipid soluble species.
Mechanisms by which drugs move a cross the
cell membrane
Passive/simple diffusion of water and lipid
soluble drugs: movement of particles from an area
of high concentration to an area of low
concentration. (Good for small particles)
Facilitated diffusion: passive diffusion that uses
special carrier molecules (Good for big
molecules)
Passive filtration: involves the aqueous channels
or pores through hydrophilic drugs can pass.
Pinocytosis and phagocytosis: Molecules are
physically taken into the cell by engulfing. 47
Active transport: movement of
molecules against the concentration gradient
from areas of low concentration of
molecules to an area of high concentration
of molecules. It involves both a carrier
molecule and energy (good for
accumulation of a drug within a part of the
body)
Adsorption of drugs to cell content:
Passage via gap junction
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How does drug absorption occur?
Factor affecting absorption of a drug
Disintegration and dissolution time: The
drugs taken orally should break up as
individual particles to be absorbed; it then
has to dissolve in the gastrointestinal fluids.
In case of a drug given subcutaneously or
intramuscularly, the drug molecules have to
dissolve in tissue fluid.
Formulation of drug: substances added to a
drug as diluents like starch and lactose may
sometimes interfere with absorption.
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Particles size: some drugs are better
absorbed when they are of small particles,
e.g. corticosteroids, griseofulvin, digoxin,
Aspirin and tolbutamide. For some drugs
that must act on the gut and absorption is
not desired, the particle size should be
kept large.
Solubility of the drug: lipid soluble
drugs are absorbed faster and better by
dissolving in the phospholipids.
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PH levels: ionized drugs are poorly
absorbed while unionized drugs are lipid
soluble and are well absorbed. Acidic drugs
remain unionized in acidic medium of the
stomach and are rapidly absorbed, e.g.
aspirin and barbiturates. Basic drugs are
unionized when they reach the alkaline
medium of the intestine, e.g. pethidine and
ephedrine. Strong acids and bases are highly
ionized and therefore poorly absorbed, e.g.
heparin and streptomycin 52
Total surface area available for
absorption: the intestines is rich in microvilli,
this offers a large surface for absorption of
drugs.
Contact time at absorption site: if
the drug moves through the gastrointestinal
tract very quickly, as in severe diarrhea, it
will not be well absorbed or anything that
delays the transport of drugs from the
stomach to intestines delays the rate of
absorption of the drug. 53
Presence of food in GIT: delay gastric
emptying, dilutes the drug, delay absorption,
drugs may form complexes with food
constituents and such complexes are poorly
absorbed, e.g. tetracyclines chelate calcium
present in food. Certain drugs like
ampicillin and rifampicin will be absorbed
only on the empty stomach.

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Metabolism (first pass metabolism): some
drugs may be degraded in the gut, e.g.
nitroglycerine, insulin; such drugs should be
given using alternative routes
Diseases: diseases of the gut like
malabsorption and achlorhydria result in
reduced absorption of drugs.
Blood flow to the absorption site: : blood
flow to the intestines is much greater than
blood flow to the stomach. Thus absorption
from the small intestines is much favoured
over that from the stomach 55
BIOAVAILABILITY
Is the extend and the rate at which a drug enters
the systemic circulation. Is the fraction of the
drug that reaches the systemic circulation
following administration by any route. Drugs
given intravenously their bioavailability is
100%.

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 actor that affect bioavailability
. First pass metabolism (presystemic
metabolism or first pass effect):
his is metabolism of a drug during its passage
rom the site of absorption to the systemic
irculation. Drugs given orally may be rapidly
metabolized in the gut wall or in the liver before
eaching the systemic circulation. Is an important
eature of oral route of drug administration. First
ass metabolism may result in partial to total
nactivation of a drug.
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 1. First-pass hepatic metabolism

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Drug Routes and First-Pass Effects
Examples of drugs that undergo first pass
metabolism include; nitroglycerin, propranol,
sulbutamol. Some drugs under complete first
pass metabolism, e.g. isoprenaline,
hydrocortisone, insulin undergo complete 1st
pass metabolism

2. Solubility of the drug:

Drugs that are very hydrophilic (water loving)
are poorly absorbed because of their inability
to cross the lipid rich cell membranes. 60
3.Chemical instability:
some drugs such as penicillin G and insulun
are unastable to pH of gastric juice;
degradative enzymes in the GIT.
4. Nature of formulation of the drug:
The size of the particles, salt form and
excipients such as binders, dispersing agents or
disintergrants can influence the ease of
dissolution and affect the rate of absorption of
the drug.

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 Activity

How does each of the following affect absorption?

– Acidity of a drug

– Tattoo on the skin

– Drug concentration

02/10/2025 PHA 2111 62

DRUG DISTRIBUTION
Is the movement of a drug from the blood
stream or general circulation into different
organs and fluid of the body. Once a drug
is injected or absorbed into the blood
stream, it is carried by blood and tissue
fluids to its site of pharmacological action,
metabolism and excretion.

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• Drugs move between body compartment plasma; extracellular
fluid; intracellular fluid; + special areas (fetus, brain). Drug
reaches the site of action

• The drug may be distributed to various organs ; first -liver, kidney,

brain, etc. Later-muscle, viscera, skin
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Drug distribution after absorption
Factors that determine the rate of drug
distribution.
1.Blood flow to tissues.
Drugs are distributed rapidly to organs
receiving large blood supply, such as the heart,
liver and kidneys. Distribution to other internal
organs, skin, fat and muscle is usually slow.

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2.Binding to plasma proteins and cellular proteins
Most drugs bind to plasma proteins.
Acidic drugs mainly bind to albumin and basic
drugs bind to alpha acid glycoprotein.
Protein binding prolongs the duration of action of
the drug
Only free or unbound portion of a drug act on the
cell of the body
Protein binding allows part of the drug dose to be
stored and released as needed.
The rest is bound to protein. Clients with low albumin levels will
have higher levels of circulating drugs, and are at risk for drug toxicity.

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3.Tissue binding/ localization of a drug
Some drugs bind to certain tissue constituents
because of special affinity(liking) for them.
 For example, lipid soluble drugs, like
thiopentone sodium bind to adipose tissue and
Iodine bind to thyroid tissues.
Tissue binding serves as a reservoir of the drug
4.Lipid solubility:
lipid soluble drugs are easily distributed in the
body
5.Ionization:
unionized lipid soluble drugs are widely
distributed throughout the body. 68
6. Barriers to drug distribution
Blood brain barrier (BBB):
Only lipid soluble, unionized drugs cross
the BBB.
During inflammation of the meninges,
the barrier becomes more permeable to
drugs, e.g. penicillin readily penetrates
the BBB during meningitis.
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Placenta barrier
Lipid soluble, unionized drugs
readily cross the placenta
Lipid insoluble drugs cross to a
much lesser extend.
These drugs may affect the
fetus during pregnancy. 70
Metabolism of drugs
Drug metabolism or biotransformation is
the process of biochemical alteration of the
drug in the body.
Sites of drug metabolism
The most important organ of metabolism is
the liver. Also some drugs are metabolized
by the kidneys, gut mucosa, lungs, blood
and skin

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Results of drug metabolism
Promotion of renal excretion of the
drug
Activation of inactive drugs (pro-drugs)
Enhancement of therapeutic action of
the drug
Alteration of toxicity of the drug
Inactivation of the drug

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Importance of metabolism
To convert fat soluble drugs into water
soluble compounds that are easily eliminated
Detoxification of drugs
 Activation of pro-drugs. A pro-drug is an
inactive drug which gets converted into an
active form in the body, e.g. levodopa
(inactive) is converted to dopamine (active
drug), prednisone (inactive) is converted to
prednisolone (active)
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Enzymes involved in biotransformation
of drugs
Most drugs are metabolized by enzymes
located in the liver cells (hepatocytes),
called cytochrome 450 (CYP) or
microsomal enzymes or mono-oxygenases.
The three groups that metabolize drugs are
labeled CYP1,CYP2 CYP3

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The red blood cells, plasma, kidneys, lungs
and GI mucosa also contain drug
metabolizing enzymes.

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Qn.What are the factors that infleunce
individual drug metabolism
Genetics
Co-existing disorders e.g. chronic
liver disorders
Drug interaction

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Enzyme induction:
Some drugs stimulate the liver cell to
produce (synthesis) larger amounts of the
drug metabolizing enzymes, a process called
enzyme induction.
This process speeds the metabolism of the
inducing drug itself and other drugs
metabolized by microsomal enzymes and
endogenous steroid hormones such as
cortisol, estrogens, testosterone and vitamin
D 77
Examples of enzyme inducers,
phenobarbitone, rifampicin, griseofluvin,
carbamazepine, phenytion, alcohol,
cigarette smoke, DDT
Clinical importance of microsomal
enzyme induction
Drug interactions: Enzyme induction
may result in therapeutic failure of some
drugs due to reduced duration of action,
e.g. failure of oral contraceptives in
patients taking rifampicin. 78
Toxicity: Is adverse drug reaction due to
enhanced activity of the drug.
Tolerance: is a gradual decrease in
response to a drug. Tolerance may occur
through a decrease of a drug at receptor site,
e.g. carbamazepine induces its own
metabolism.

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Enzyme inhibition: Is a process by which
metabolism of a drug is delayed or
decreased. It occurs in cases when drugs
inhibit microsomal enzyme activity; drugs
like cimetidine and ketaconazole bind to
these enzymes and competitively inhibit the
metabolism of substances like testosterone.
Enzyme inhibitors: chloramphenical,
erythromycin, cimetidine, kateconazole,
ciprofloxacin and verapamil
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Drug excretion (drug elimination)
This is the removal of a drug from the body.
The major organs of excretion are the kidneys,
intestines, biliary system and lungs. Renal
elimination is the most important.
Drugs can also be excreted in small amounts in
the saliva, sweat and milk.

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The excretion of drugs in the milk is in small
amounts and is of no significance to the
mother. But for the suckling infant, it may
sometimes be important, especially of the
infant’s immature metabolic or excretory
mechanisms.
Examples of drugs that could be toxic to
suckling infants when taken by the mother
Theophylline, anticancer drugs, salicylates,
chloramphenical, nalidixic acid,
phenobarbitone, Beta blocker
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Drugs may be excreted through any of the
following ways
Urine
Bile
Faeces
Breast milk
Sweat
Saliva
Expired air
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