INTRODUCTION TO

PHARMACOLOGY & THERAPEUTICS

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 INTRODUCTION

 The role of pharmacology in medicine -

“Medicine is making the right diagnosis,
selecting and administering the right drug, in
the right dose, in the right form, for the right
intervals and over the right length of time”

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 Introduction Cont.

 “Poisons in small doses are the best medicines;

and useful medicines in too large doses are
poisons” – William Withering (discoverer of
digitalis - 1789).

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 Introduction Cont.

 Drug therapy involves a great deal more than

matching the name of the drug to the name of
a disease; it requires knowledge, judgement,
skill and wisdom, but above all a sense of
responsibility.

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 TERMINOLOGIES

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 Pharmacodynamics

 It is derived from a Greek word “dynamics”-

meaning power i.e. what the drug does to the
body; how drugs, alone and in combination,
affect the body (young, old, well, sick).

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 Pharmacodynamics Cont.

 It includes physiological and biochemical

effects of drugs and their mechanism of action
at organ /system/subcellular/ macromolecular
levels.

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 Pharmacokinetics

 It is derived from a Greek word “kinesis

“Meaning movement”.
 What the body does to the drug and alteration
of the drug by the body; how the body, well or
sick, affects drugs.

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 Pharmacokinetics Cont.

 It includes absorption, distribution, binding/

localization/ storage, biotransformation
(metabolism) and excretion of the drug.

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 Drug

 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 the recipient – WHO 1966
Technical Report Series No. 341;7 –
Definition by a WHO Scientific Group.
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 Pharmacotherapeutics

 It is the application of pharmacological

information together with the knowledge of
the disease for its prevention, mitigation or
cure.

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 Pharmacotherapeutics Cont.

 Selection of the most appropriate drug, dosage

and duration of treatment taking into account
the specific features of a patient are part of
pharmacotherapeutics.

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 Clinical pharmacology

 Is the science of drugs.

 It is the scientific study of drugs in man.

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 Clinical pharmacology Cont.

 It includes pharmacodynamic and

pharmacokinetic investigations in healthy
volunteers and in patients; evaluation of efficacy
and safety of drugs and comparative trials with
other forms of treatment; surveillance of patterns
of drug use and adverse effects.

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 Clinical pharmacology Cont.

 In a broader sense, it deals with interaction of

exogenously administered chemical molecules
(drugs) with living systems.

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 Chemotherapy

 It is the treatment of systemic infections

/malignancies with specific drugs that have
selective toxicity for the infecting
organism/malignant cell with no/minimal
effects on the host cells.

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 Pharmacy

 It is the art and science of compounding and

dispensing drugs or preparing suitable dosage
forms for administration of drugs to man or
animals.

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 Pharmacy Cont.

 It includes collection, identification,

purification, isolation, synthesis,
standardization and quality control of
medicinal substances.
 The large scale manufacture of drugs is called
pharmaceutics.
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 Toxicology

 It is the study of poisonous effects of drugs

and other chemicals (household,
environmental pollutant, industrial,
agricultural) with emphasis on detection,
prevention and treatment of poisoning.

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 Toxicology Cont.

 It also includes the study of adverse effects of

drugs, since the same substance can be a drug
or a poison, depending on the dose.

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 THE NATURE AND SOURCES OF
DRUGS

1.Mineral:
a)Liquid paraffin.
b)Magnesium sulfate.
c)Magnesium trisilicate.
d)Kaolin.
e)Epsom salts
f) arsenic
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 The Nature And Sources Of Drugs Cont.

2. Animal:
a)Insulin.
b)Thyroid extract.
c)Heparin.
d)Gonadotropins.
e)Antitoxic sera.

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 The Nature And Sources Of Drugs Cont.

3. Micro-organisms i.e. bacteria and fungi;

antibiotics e.g. penicillin and bacitracin.

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 The Nature And Sources Of Drugs Cont.

4. Vegetable Drugs:
The pharmacologically active principles in
vegetable drugs are:

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 The Nature And Sources Of Drugs Cont.

a) Alkaloids – Basic substances containing

cyclic nitrogen; insoluble in water but combine
with acids to form well-defined, water soluble
salts e.g. morphine, atropine and emetine.

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 The Nature And Sources Of Drugs Cont.

b) Glycosides – Ether-like combinations of sugar with

other organic structures; do not form salts with acids but
when heated with mineral acids are hydrolysed to a sugar
and a non-sugar component called aglycone or genin e.g.
digoxigenin. A glycoside which yields glucose on acid
hydrolysis is called a glucoside e.g. strophanthin.

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 The Nature And Sources Of Drugs Cont.

c) Oils:
i. Fixed oils – Are glycerides of oleic, palmitic
and stearic acids. Castor oil acts as a purgative.

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 The Nature And Sources Of Drugs Cont.

ii. Volatile oils – Not fats; contain hydrocarbon

terpene or some polymer of it, which serves as a
diluent or solvent for a more active compound
e.g. menthol in peppermint oil. They are used as

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 The Nature And Sources Of Drugs Cont.

1. Carminatives for expulsion of gas from the

stomach, e.g. oil of eucalyptus, asafetida, ginger.
2. Antiseptics in mouth wash, pastes.
3. Counterirritants e.g. oil of wintergreen,
turpentine oil,
4. Flavouring agents e.g. oil of peppermint.
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 The Nature And Sources Of Drugs Cont.

5. Pain relieving agents e.g. oil of clove in

toothache.
6. NB: Mineral oil e.g. liquid paraffin is a
hydrocarbon derived from petroleum and is
commonly used as a lubricant purgative.

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 The Nature And Sources Of Drugs Cont.

d) Resins – Formed by oxidation or

polymerization of volatile oils and are insoluble
in water but soluble in alcohol
e) Oleoresins – Are mixtures of volatile oils and
resins.

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 The Nature And Sources Of Drugs Cont.

f) Gums – Secretory products of plants.

Dispersible in water and form thick,
mucilaginous colloids. Employed as suspending
and emulsifying agents e.g. gum acacia, gum
tragacanth. Agar, another gum, is used as a bulk
purgative.
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 The Nature And Sources Of Drugs Cont.

g) Tannins – Non-nitrogenous plant constituents

1. Digoxin. foxglove (digitalis
2. Quinine.
3. Atropine.
4. Reserpine.
5. poppy (opium)
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 The Nature And Sources Of Drugs Cont.

5. Synthetic:
a) Aspirin.
b) Sulfonamides.
c) Procaine.
d) Corticosteroids.

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 The Nature And Sources Of Drugs Cont.

6. The vitamins and endocrine hormones.

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 Traditional Cures, Modern Uses
Drug Source Condition Treated

Digitalis Purple foxglove Heart failure

Quinine Cinchona bark Malaria

Vinca alkaloids Periwinkle plant Cancer

Insulin Pig, cow and genetically Diabetes

engineered human insulin

Urokinase Cultures of human kidney cells Blood clots

Opium Poppy plant Pain

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 CLASSIFICATON OF DRUGS

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 There is no homogeneous system for classifying
drugs that suits the purpose of every user.
 Drugs are commonly categorized according to the
convenience of who is discussing them: clinicians,
pharmacologists or medicinal chemists.

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 Drugs may be classified by:
1. Therapeutic use, e.g. receptor blockers,
enzyme inhibitors, carrier molecules, ion
channels.
2. Molecular structure, e.g. glycoside, alkaloid
(cinchona/solonaceous), steroid.

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 Drugs may be classified by Cont.
3. Chemical structure of drugs e.g. barbiturates,
the organic nitrites, the phenothiazine, the
sulphonamides and the quaternary ammonium
bases
4. Body system/ Sites of action of drugs e.g.:
a) Alimentary
b) Central nervous system stimulants.
c) Cardiac /cardiovascular or oxytocic drugs.
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 Drugs may be classified by Cont.
d) Anti-inflammatory and
e) Haematopoietic drugs and
f) Ganglion-stimulant drugs.
g) Cellular site, e.g. loop diuretic, catecholamine
uptake inhibitor (imipramine)

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 Drugs may be classified by Cont.
• 5. Prototype drugs – A well-known drug taken
as a prototype of compounds possessing a
particular type of pharmacological activity.
• 6. Therapeutic use, e.g. antmicrobial,
antidiabetic, antihypertensive, analgesic.

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 NOMENCLATURE (NAMES)

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•Any drug may have names in all three of the
following classes:

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 1. Chemical name
 It describes the (atomic or molecular structure of the drug)
substances chemically for chemists.
 Although the chemical name describes and identifies the product
precisely, it is usually too complex and cumbersome for general use,
not suitable for use in prescribing, except in the case of some
simple, inorganic drugs such as sodium bicarbonate.

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 1. Chemical name Cont.
 For example 1-(Isopropylamino)-3-(1-naphthyloxy) Propan-2-01 for
Propanol; 3-(10, 11-dihydro-5H-dibenz[b,f]-azepin-5-yl)propyl-
dimethylamin for imipriamine.
 It is cumbersome and not suitable for use in prescribing.

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 2. Non-Proprietary

• It is the name accepted by a competent

scientific body/Authority e.g. The United
States Adopted Name.
• Generic, approved, official name is given by
an official (pharmacopoeia) agency, e.g.
WHO.
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 2. Non-Proprietary Cont.

Three principles remain supreme and

unchallenged in importance:
 The need for distinction in sound and spelling
especially when the name is handwritten.
 The need for freedom from confusion with existing
names, both non-proprietary and proprietary

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 2. Non-Proprietary Cont.

 The desirability of indicating relationships

between similar substances.
 The generic names diazepam, nitrazepam,
flurazepam are all benzodiazepines.
 Their proprietary names are Valium, Mogodon,
and Dalmane respectively.

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 2. Non-Proprietary Cont.

 Names ending in –olol are adrenoceptor blockers;

those ending in –pril are angiotensin-converting
enzyme (ACE) inhibitors and those in -floxacin are
quinolone antimicrobials

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 2. Non-Proprietary: Advantages

•The principal reasons for advocating the

habitual use of non-proprietary (generic) names
in prescribing are:

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 2. Non-Proprietary: Advantages

a)Clarity
 Non-proprietary names give information on
the class of drug, e.g. nortriptyline and
amitriptyline are plainly related, but their
proprietary names, Allegron and Triptafen/
Lentizol, are not.
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 2. Non-Proprietary: Advantages

 It is not unknown for prescribers, when one

drug has failed, unwittingly to add or
substitute another drug of the same group (or
even the same drug), thinking that different
proprietary names must mean different classes
of drugs.
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 2. Non-Proprietary: Advantages

 Such occurrence underline the wisdom of

prescribing generically, so that group
similarities are immediately apparent, but
highlight the requirement for brand names to
be as distinct from one another as possible.

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 2. Non-Proprietary: Advantages

 Relationships cannot and should not, be shown

by brand names.

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 2. Non-Proprietary: Advantages

b) Economy:
 Drugs sold under non-proprietary names are
usually, but not always, cheaper than those
sold under proprietary names.

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 2. Non-Proprietary: Advantages

c) Convenience
 Pharmacists may supply whatever version they
stock, whereas if a proprietary name is used
they are normally obliged to supply that
preparation alone.

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 2. Non-Proprietary: Advantages
•NB:
 The generic name is now widely accepted as being
synonymous with non-proprietary name.
 Strictly, ‘generic’ (L. genus, race, a class of objects) should
refer to a group or class of drug, e.g. benzodiazepines, but by
common usage the word is now taken to mean the non-
proprietary name of individual members of a group, e.g.
diazepam.

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 3. Proprietary (Brand) name

 The proprietary name is a trademark applied to

particular formulation(s) of a particular
substance by a particular manufacturer
 Manufacture is confined to the owner of the
trade mark or to others licensed by the owner.

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 3. Proprietary (Brand) name Cont.

 It is designed to maximize the difference

between the names of similar drugs marketed
by rivals for obvious commercial reasons.

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 3. Proprietary (Brand) name Cont.

 To add confusion, some companies give

proprietary names to their generic products in
an attempt to capture the prescription market,
both proprietary and generic and some market
lower-priced generics of their own
proprietaries.
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 3. Proprietary (Brand) name Cont.
 When a prescription is written for a proprietary pharmacists
must, under law, dispense that product only, unless they
persuade the doctor to alter the prescription or, under law,
they have the right to substitute a generic product (this is
called generic substitution) or a drug of different molecular
structure deemed to be pharmacologically and therapeutically
equivalent (this is called therapeutic substitution).

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 3. Proprietary (Brand) name Cont.

 Both these substitutions are designed to reduce

cost.
 The company tries to choose a unique name
that’s short and easy to remember so doctors
will prescribe it and consumers will look for it
by name.
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 3. Proprietary (Brand) name Cont.

 For this reason, trade names sometimes link

the drug to its intended use, for example,
Diabinese for diabetes and Fexeril for muscle
cramps.

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 3. Proprietary (Brand) name Cont.

 One drug may have many/multiple proprietary

names e.g. Unimol, Pacimol, Hedex, Action,
Ethymol for paracetamol.

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 3. Proprietary (Brand) name Cont.

 They often indicate a particular characteristic

of the drug.

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 3. Proprietary (Brand) name Cont.

 For example, Lopressor lowers blood pressure,

Vivactil is an antidepressant that might make a
person more vivacious, Glucotrol controls
high blood sugar (glucose), and Skelexin is a
skeletal muscle relaxant.

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 3. Proprietary (Brand) name Cont.

 The trade name Minocin, on the other hand, is

simply a shortened version of minocycline, the
drug’s generic name.

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 3. Proprietary (Brand) name: Advantage.

 Consistency: The principal non-commercial reason for

advocating the use of proprietary names in prescribing
is consistency of the product, so that problems of
quality, especially of bioavailability are reduced.
 There is substance in this argument, though it is often
exaggerated.

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 3. Proprietary (Brand) name: Advantage.

 It is reasonable to use proprietary names when dosage,

and therefore pharmaceutical bioavailability, is critical,
so that small variations in the amount of drug available
for absorption can have big effects on the patient, e.g.
drugs with low therapeutic ratio, digoxin, hormone
replacement therapy, adrenocortical steroids (oral),
antiepileptics, cardiac antiarrhythmics, warfarin.
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 3. Proprietary (Brand) name: Advantage.

 In addition, with introduction of complex

formulations, e.g. sustained-release, it is
important clearly to identify these, and use of
proprietary names has a role.

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 Confusing Names

•The need for both clear thought and clear

handwriting is shown by medicines of totally
different class that have similar names.
•Serious events have occurred as a result of the
confusion of names and dispensing the wrong
drug, e.g.:
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 Confusing Names Cont.

 Lasix (frusemide) for Losec (omeprazole)

(death).
 AZT (intending zidovudine) was
misinterpreted in the pharmacy and
azathioprine was dispensed (do not use
abbreviations for drug names).
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 Confusing Names Cont.

 Daonil (glibenclamide) for De-nol (bismuth

chelate) and for Danol (danazol).

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 Confusing Names Cont.

 Authorities must be certain that trade and

generic names are unique and can’t be
mistaken for other drugs.
 Names too similar to those of other drugs can
lead to mistakes in drug prescribing or
dispensing.
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 Confusing Names Cont.

 It will be noted that non-proprietary names are

less likely to be confused with other classes of
drugs.

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Example: One drug – three names
1.3-(10,11-dihydro-5H-dibenz[b,f]-
azepin-5yl)propyldimethylamine
2.Imipramine.
3.Tofranil (UK), Melipramine,
Novopramine, Pryleugan, Surplix, etc.
(various countries.
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 More examples
Chemical Name Generic Name Trade Name
N-(4-Hydroxyphenyl)acetamide Acetaminophen Tylenol
1-(Isopropylamino)-3-(1-naphthyloxy) Propan-2-01 Propanol Inderal
3-(10, 11-dihydro-5H-dibenz [b,f]-azepin-5-yl)propyl- Imipriamine  
dimethylamin
7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4- Diazepam Valium
benzodiazepin-2-one
4-[4-(p-chlorophenyl)-4-hydrixpiperidino]-4- Haloperidol Haldol
fluorobutyrophenone
DL-threo-2-(methylamino)-phenylpropan-1-o Pseudoephedrine Sudafed
hydrochloride
N-cyano-N-methyl-N-[2-[[(5-methyl-1H-imidazol-4- Cimetidine Tagamet
y)methyl]thio]ethyl]guanidine
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