[Type text] [Type text] TYBSc Drugs

© Dr Dasgupta

SEMESTER V
UNIT I
Definition
The term ‘drug’ is derived from the French word ‘drogue’ meaning ‘dry herb’.
A drug may be defined as a substance used in the prevention, diagnosis,
treatment or cure of disease in man or other animals.
REQUIREMENTS OF AN IDEAL DRUG
1. Localised site of action
2. Efficient and safe
3. Non- toxic
4. Non-injurious to host tissues or physiological processes
5. Minimum side-effects
6. Ability to overcome tolerance or resistance by cell

CLASSIFICATION OF DRUGS
Drugs can be classified either on the basis of their therapeutic action
or on the basis of their chemical structure. A rigid classification tends to
overlap a number of categories. Hence drugs are first classified on the basis
of their therapeutic action and then on the basis of their chemical action.
On the basis of their therapeutic action, drugs are classified as:
1. Functional or pharmacodynamic agents:
These act upon various physiological systems of the body. They are
further sub-divided as:
a. CNS stimulants
b. CNS depressants
c. Tranquilizers
d. Diuretics
e. Cardiovascular agents
f. Anti-inflammatory agents
g. Anti-diabetic agents
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h. Analgesics and Antipyretics

i. Antihistaminic agents
j. Anti-parkinsonism agents, etc

2. Chemotherapeutic agents:
Treatment of infectious diseases caused by parasitic micro-organisms in
such a way that the disease-producing organism is destroyed without
causing any harmful effect to the host cell is called chemotherapy and
the drugs used in this manner are called chemotherapeutic drugs.
They are further sub-divided into:
a. Anthelmintic
b. Anti-malarial
c. Anti-fungal
d. Anti-protozoal
e. Anti-viral
f. Antiseptics, etc

3. Vitamins:
These are organic compounds required by the host in minute quantities
for its normal health and growth, but are not synthesized by the host.
They are of two types:
a. Water-soluble eg. Vitamin B and C
b. Fat-soluble eg. Vitamin A,D,E and K

4. Hormones:
These are organic compounds secreted by the endocrine or ductless
glands into the blood stream and are synthesized by the host. They are
required in very minute quantities for metabolism, growth and
reproduction.
They are:
a. Thyroid hormones
b. Pituitary hormones
c. Sex hormones, etc
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1.1.2Nomenclature of Drugs
Chemical name or Systematic name
The systematic name of a drug is given on the basis of its chemical
structure in accordance with the IUPAC rules of nomenclature. As such
names are generally very elaborate, it is not recommended for routine use.
E.g. Paracetamol
Systematic name: 4- Hydroxyacetanilide

Trade Name or Brand name

Also called trivial name. It is the individual name selected and used by the
manufacturer. In case the same drug is manufactured by more than one
manufacturer, each assigns its own trade name. The first alphabet in the
name of the drug is always capital.
E.g. trade name of ibuprofen is Brufen, Ibugesic

Generic name
Also called official name or common name. It is the common established
name of the drug by which it is known as an isolated substance, irrespective
of its manufacturer. The first alphabet in the name is not in capital. WHO
selects, approves and designates the generic name of the drug.
E.g. paracetamol is the generic name of the drug which is marketed under
various trade names such as Crocin, Metacin

Definition of the following medicinal terms:

Pharmacophore
The specific functional group in a drug which is responsible for its
therapeutic activity is called pharmacophore. These groups interact with
specific receptors at the site of action. Any slight change in their structural
feature may result in a major change in the pharmacological activity of
drugs. They play an important role in the search for newer drugs, and in
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improving the therapeutic activity and/or reducing the toxicity of existing

drugs.

Prodrug
It is a suitable derivative of a biologically active drug which undergoes
certain changes in vivo on reacting with enzymes, to release the parent
drug.
This concept is mainly used to improve certain therapeutic effects of the drug
such as: duration of action, localisation, drug distribution, toxicity. Eg.
Prontosil which is a dye is metabolised into a sulphonamide.

Half-life efficiency or Half-life efficacy

It is the time required for 50% of the drug to be eliminated from the
bloodstream.
Half-life (t1/2) follows first order kinetics i.e. a constant fraction of the drug
disappears in equal intervals of time. The rate of drug elimination is
proportional to its plasma concentration.
A drug with a large half-life e.g. Digitoxin requires less frequent dosage
whereas those with short half-life require frequent dosage. An ideal drug
should have an optimum half-life.

LD50
Also called Lethal Dose 50 or Threshold Dose or Median Lethal Dose.
It is the maximum amount of drug required (in mg/kg) to cause death to 50%
of a test population of the same species or strain. An ideal drug should have
a high LD50

ED50
Also called Effective Dose 50 or Median Effective Dose.
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It is the minimum amount of drug required (in mg/kg) to effect the desired
therapeutic activity in 50% of a test population of the same species or strain.
An ideal drug should have a low ED50

Therapeutic Index (T.I.)

It is the ratio of the median lethal dose (LD50) to the median effective dose
(ED50)
Therapeutic Index (T.I.) = LD50/ ED50
The larger the therapeutic index, the safer is the drug.

1.1.3 Brief idea of the following terms:

Receptor
Receptors are target molecules in the host, with which the drug combines so
as to bring about its therapeutic effects. They are essentially proteins
present either in the cell membrane, or on the surface, or inside the cell.
Receptors determine the quantitative relationship between the dosage of a
drug and its therapeutic effects.

Drug-Receptor interaction
Drug receptor interaction is based on drug affinity which is the quantitative
ability of the drug to bind with the receptor through either ionic or non-ionic
bonds. Affinity determines how much of the drug-receptor complex is
formed and hence the biological response of the drug. The non-ionic
bonding may be H-bond, hydrophobic bond or van der Waals forces. The
drug effect is at its maximum when it is able to bind completely with its
receptors. The formation of the drug receptor complex is usually a reversible
reaction as most drugs have limited duration of action.
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Drug Potency
Drug potency is the amount of drug required to produce a biological
response. The potency of a drug depends upon drug-receptor interaction.
D + R → [DR] → Biological Response
Where D= Drug, R= Receptor, DR = Drug – Receptor Complex
The better the drug- receptor interaction, the better is the complex formed
and hence better is the biological response and therefore higher the drug
potency.

Bioavailability
The amount or percentage of the drug that is absorbed from the given
dosage form and reaches the circulatory system following non-vascular
administration is called bioavailability of the drug.
Only vascular administration gives 100% bioavailability of the drug.
Bioavailability depends upon:
a) Physical properties of the drug eg. nature and solubility
b) Nature of the dosage form including particle size
c) Physiological factors eg. emotional and psychological factors, metabolic
disturbances, presence of diseases, etc.

Drug Toxicity
When a drug causes certain adverse effects in the host, it is called drug
toxicity. Drug toxicity may be mild eg. a skin rash or, serious eg. liver
damage. It may be either short term (Acute) or long term (Chronic) in
nature. Chronic toxicity studies of drugs tell us how ‘safe’ the drug is.
Eg.
1. Overdose of insulin causes hypoglycaemia (lowering of blood sugar).
2. Long term use of morphine causes respiratory depression.

Drug Addiction
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Repeated administration of some drugs may lead to physical and

psychological dependence causing physical disturbances. This is called drug
addiction.
Characteristics of drug addiction:
1. Strong compulsion to continue taking the drug so as to avoid the
discomfort of its absence.
2. Tendency to increase the dose.
3. Relapse after withdrawal.

Examples of drugs which cause addiction are: Barbiturates, alcohols, opiates.

These drugs produce a feeling a euphoria leading to dependence.

Routes of Drug Administration and Dosage Forms

Route of Drug Administration

The route of drug administration is important as it determines the rate
of drug absorption in the body.
Oral < Subcutaneous < Intramuscular < Inhalation < Intravenous (Increasing
order of rapidity of absorption in man)
Different routes of drug administration produce quantitative as well as
qualitative difference in pharmacological response.
Factors governing the choice of route
1. Physical and chemical properties of the drug molecule
2. Site of desire action
3. Rate and extent of absorption of drug from different routes
4. Effect of digestive juices on the drug molecule
5. Rapidity with which the response is desired
6. Accuracy of dosage desired
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Different routes of drug administration:

1. Oral
2. Parenteral
3. Nasal
4. Rectal
5. Subcutaneous
6. Topical

Oral route
This is the oldest and commonest route of drug administration where
the drug is taken through the mouth.
Advantages
1. Safe and convenient to use
2. Does not require assistance
3. Painless
4. Economical
5. Medication need not be sterile
Disadvantages
1. As the onset of action is slow, it is not suitable in case of emergency
situations.
2. Unpalatable drugs cannot be administered by this route
3. It cannot be given to patients who are vomiting or having diarrhoea
4. It cannot be given to unconscious or uncooperative patients
5. Some drugs such as streptomycin or insulin cannot be given by this route
as they get metabolized in the liver.

Parenteral Route
This refers to those routes of drug administration which directly enter the
circulatory system. They are-
1. Intravenous
2. Intrathecal
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3. Intramuscular
4. Subcutaneous
5. Intracardiac
6. Intramedullary

Advantages
1. Action is very fast as the drug directly enters the circulatory system
2. It is suitable for emergencies
3. Can be given to vomiting or unconscious patients
4. As the liver is bypassed, the chances of the drug getting metabolized
into inactive product are not there.

Disadvantages
1. The medication should be sterile
2. It is expensive
3. Technique is invasive and hence skilled assistance is required
4. There are chances of local tissue injury

SUSTAINED RELEASE FORMULATION

In such cases where a high therapeutic concentration is required

at the site of action, either large dosage or frequent dosage is required.
This can lead to adverse effects especially in long-term therapy.
This problem is overcome with sustained release formulations which
release the drug slowly over an extended period of time, rather than
immediately after drug administration.

Types
1. Capsules coated with cellulose acetate or phthalate:
These release the drug only in specific physiological conditions eg.
Alkaline intestinal juices
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2. Coatings which dissolve at different time-intervals and release the

drug in a steady controlled manner over an extended period of time.
E.g. Ocusert placed under the eyelid

3. Transdermally implanted drugs using biocompatible polymers: these

are activated by osmotic pressure, magnetism, vapour pressure. E.g.
Levonorgestrel implant placed beneath the skin of the upper arm as a
contraceptive.

Formulation of sustained release drugs:

1. Embedding in matrix
2. Coating with ion-exchange resins
3. Increasing the particle size.
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