INTRODUCTION TO

PHARMACOLOGY 1
 Learning objectives
By the end of the unit the learners shall be able to:
• Define terms used in pharmacology
• Apply principles of pharmacodynamics and
pharmacokinetics in patient care
• Demonstrate an understanding of legislation
guiding drug use
• Classify common pharmaceutical agents in clinical
practice
• Administer drugs safely to clients/patients
 PHARMACOLOGICAL TERMS

Pharmacology is the study of effects of

chemical substances on the function of living
systems.
 pharmacology is the science of drugs which
includes their preparation, use and effects.
It is also the science that deals with the origin,
chemistry, effects and uses of drugs.
Pharmacy: Branch of health science that
deals with preparation and dispensing of
drugs.
pharmacotherapy: The study of therapeutic
uses and effects of drugs.
Pharmacognosy: the study of drugs that come
from natural sources e.g. plants, animals and
minerals as well as search for new drugs from
natural sources.
• Pharmacokinetics – What the body does to
the drug – study of absorption, distribution,
metabolism and excretion
– Greek: Kinesis
• Pharmacodynamics – What the drug does to
the body – Study of the effect of the drug and
their mechanism of action
Pharmacogenetics: the study of the effects that
genetics have on an individuals response to
drugs.
 Contra-indication: – a specific situation in
which a drug, procedure, or surgery should not
be used because it may be harmful to the person
Half life or half time (t1/2):Time taken for
plasma concentration to fall by half following its
elimination in the body.
• Drug interactions : - a change in the action or
side effects of a drug caused by concomitant
administration with a food, beverage,
supplement, or another drug
• Desired therapeutic effect: This should
indicate the mechanism of action of a drug
e.g.an analgesic is for pain relief.
• Toxicology:Study of poisons (detection,
prevention and treatment of poisons). Deals
with the adverse effect of drugs
• Placebo: Any component of therapy that is
without specific biological activity e.g.
inactive substance such as normal saline or
distilled water usually used in clinical trials
research and for psychological treatment.
Drug: Any substance used in diagnosis,
treatment and prevention of disease/condition
or any substance that brings a change in
biological functions through its chemical
actions
• Side effects: these are physiological effects
exerted by the chemical that are not related to
the desired therapeutic effects. you must
therefore be familiar with serious side effect
and commonly occurring effects.
• Adverse drug reaction:– unwanted or
harmful reaction experienced following the
administration of a drug or combination of
drugs under normal conditions of use and is
suspected to be related to the drug.
• Allergic reactions: This the body's
immunological response to a drug following
previous exposure to the same drug.
• Idiosyncratic reactions: unexpected, unusual
or abnormal response to a drug that is not
normally seen in the general population.
• Tolerance and dependence:
• Tolerance occurs when a person no longer
responds to the drug in the way that person
initially responded as a result of continued use
of the drug causing a need to increase dose of
a drug to achieve the same effect
Dependence: A state arising from repeated
periodic or continuous administration of a drug
that results in harm to the individual or sometimes
society.
• People feel desire or compulsion to continue
using the drug and feel ill if abruptly withdrawn
or an antidote is used. Substance that cause
dependence are taken to induce a good feelings
or avoid discomfort of their absence.
 SOURCES OF DRUGS
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.
 Naming drugs
Drugs often have several names.
When a drug is first discovered, it is given a
chemical name, which describes the atomic or
molecular structure of the drug e.g chemical
name for mefipristone is 11B-[p-
(Dimethylamino)phenyl]-17B-hydroxy-17-(1-
propynyl)estra-4,9-dien-3-one.
• The chemical name is usually too complex and
cumbersome for general use. Next, a
shorthand version of the chemical name or a
code name (such as RU 486) is developed for
easy reference among researchers
• When a drug is approved by the Food and
Drug Administration (FDA—the U.S.
government agency responsible for ensuring
that drugs marketed in the United States are
safe and effective), it is given a Generic
(official) name
• Brand (proprietary, trademark, or trade) name
• For example, phenytoin is the generic name
and Dilantin is a brand name for the same
drug, which is a commonly used antiseizure
drug.
• The generic name is assigned, in the United
States, by an official body—the United States
Adopted Names (USAN) Council.
• The brand name is developed by the
company requesting approval for the drug and
identifies it as the exclusive property of that
company.
Pharmacokinetics
pharmacokinetics
 Absorption
• Absorption –Process of movement of drugs
from the site of administration to the
bloodstream.
• Mechanism of drug absorption.
• simple diffusion/passive diffusion
• Active transport
• Facilitated diffusion
• Pinocytosis(Endocytosis)
1. Structure of biological membrane:
The outer surface of the cell covered by a very
thin structure known as plasma membrane. It is
composed of lipid and protein molecules.
The membrane proteins have many functions
like
Contributing structure to the membrane
Acting as enzyme
Acting as carrier for transport of substances
Acting as receptors.
The plasma membrane is a semipermeable
membrane allowing certain chemical substances
to pass freely e.g. it allows water, glucose, etc.
but it won’t allow sucrose until it is converted
into glucose and fructose.
 PASSAGE OF DRUG ACROSS
MEMBRANE.
Simple diffusion: Movement of a solute
through a biological barrier from the phase of
higher concentration to phase of lower
concentration. No need of energy e.g. highly
lipid soluble drugs.
Facilitated diffusion: It means the passage of
drug across the biological membrane along the
concentration gradient by the protein carrier
mediated system also called as carrier
mediated diffusion. It depends on number of
carrier e.g. tetracycline, pyrimidine.
Active transport: The process by which drugs
pass across the biological membrane most
often against their concentration gradient with
the help of carriers along with the expenditure
of energy e.g. alpha methyl dopa, levodopa, 5-
fluoro-uracil, 5 bromouracil.
Endocytosis: It is the process by which the
large molecules are engulfed by the cell
membrane and releases them intracellularly
e.g. protein, toxins (botulinum, diphtheria)
Endocytosis
 Bioavailability

• The proportion of unchanged drug reaching

the systemic circulation (thereby accessing its
site of action) following administration by any
route.
• Bioavailability of a drug may depend on:
1)Route of administration
2)Dosage form
– Drugs administered intravenously have
100% bioavailability
– Other routes of administration have less
than 100% bioavailability:
– Orally administered have lower
bioavailability because of extent of
absorption (incomplete absorption) and
first pass metabolism.
 FACTORS AFFECTING DRUG ABSORPTION
AND BIOAVAILABILITY

a) Physico-chemical properties of drug

b) Nature of the dosage form
c) Physiological factors
d) Pharmacogenetic factors
e) Disease states.
PHYSICO-CHEMICAL PROPERTIES OF DRUG:

Physical state: Liquids are absorbed better

than solids.
Lipid or water solubility: Drugs in aqueous
solution mix more readily than those in oily
solution. However at the cell surface, the lipid
soluble drugs penetrate into the cell more
rapidly than the water soluble drugs.
• Ionization: ionized drugs are poorly absorbed
while unionized drugs are lipid soluble and are
well absorbed
• Acidic drugs: rapidly absorbed from the
stomach e.g. salicylates and barbiturates.
• Basic drugs: Not absorbed until they reach to
the alkaline environment i.e. small intestine
when administered orally e.g. pethidine and
ephedrine.
 DOSAGE FORMS:
Particle size: Small particle size is important
for drug absorption. Drugs given in a
dispersed or emulsified state are absorbed
better e.g. vitamin D and vitamin A.
Disintegration time and dissolution rate.
Disintegration time: The rate of break up of the
tablet or capsule into the drug granules.
Dissolution rate: The rate at which the drug goes
into solution.
• Formulation: Usually substances like lactose,
sucrose, starch and calcium phosphate are used
as inert diluents in formulating powders or
tablets. Fillers may not be totally inert but may
affect the absorption as well as stability of the
medicament. Thus a faulty formulation can
render a useful drug totally useless
therapeutically.
 PHYSIOLOGICAL FACTORS
Gastrointestinal transit time: Rapid
absorption occurs when the drug is given on
empty stomach. However certain irritant drugs
like salicylates and iron preparations are
deliberately administred after food to
minimize the gastrointestinal irritation.
Presence of other agents: Vitamin C
enhances the absorption of iron from the G.I.T.
Area of the absorbing surface and local
circulation: Drugs can be absorbed better
from the small intestine than from the stomach
because of the larger surface area of the
former. Increased vascular supply can increase
the absorption.
Metabolism of drug/first pass effect:
Rapid degradation of a drug by the liver
during the first pass (propranolol) or by the gut
wall (isoprenaline) also affects the
bioavailability. Thus a drug though absorbed
well when given orally may not be effective
because of its extensive first pass metabolism.
Pharmacogenetic factors:
Individual variations occur due to the
genetically mediated reason in drug absorption
and response.
Disease states:
Absorption and first pass metabolism may be
affected in conditions like malabsorption and
liver cirrhosis.