INTRODUCTION TO

PHARMACOLOGY

By
Sindhu Priya E S
Asst. Professor
YPCRC
SPECIFIC LEARNING OBJECTIVES
At the end of this session, you will be able to
 Define Pharmacology and classify different
branches of Pharmacology
 Describe the history and scope of pharmacology

 Explain different sources of drug

 Explain the concept of essential drugs

 Describe different routes of administration

 Explain Agonists, antagonists( competitive and

non competitive),spare receptors, addiction,
tolerance, dependence, tachyphylaxis,
idiosyncrasy, allergy 2
 INTRODUCTION

Pharmacology (Greek)
 Pharmacon – Drug / Active principle

 Logos - discourse in / study

Pharmacology means

“THE SCIENCE OF DRUGS”

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 DEFINITION
 Pharmacology is the study of substances that
interact with living systems through chemical
process, especially by binding to regulatory
molecules & activating or inhibiting normal body
process

 It deals with the interaction of exogenously

administered chemical molecule (Drug) with
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living system
 DIVISIONS OF PHARMACOLOGY
 Pharmacodynamics
 What the drug does to the body
 It includes physiological and biochemical effects of
drugs
 Explains mechanism of action at molecular level

 Pharmacokinetics
 What the body does to the drug
 It includes movement and alteration of the drug in
the body
 Absorption, Distribution, Metabolism and Excretion
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 HISTORY

Rudolf Buchheim – 1847 Oswald Schmiedeberg

First institute of pharmacology Father of Pharmacology
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DRUG DISCOVERY AND DEVELOPMENT
PROCESS

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 SCOPE OF PHARMACOLOGY
 It provides the rational basis for therapeutic use
of the drug
 Scientific understanding of the drug enables us to
predict pharmacological effect of new chemical
that will produce a specific therapeutic effect
 The scope of pharmacology has expanded to new
approaches to CADD, gentic screening, protein
engineering, use of novel drug delivery vehicles
including viruses and artificial cells.

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DRUG
 Derived from french word “Drogue” which
means “Dry herb”

 Any substance that brings change in biological

function through its chemical action

 It alters state of the body-

➢ Can’t create new function but alters existing function

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WHO DEFINITION OF DRUG

 Drug is any substance or product that is used or

is intended to be used to modify or explore
physiological systems or pathological states for
the benefit of the recipient

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RECEPTORS

 Specialized target macromolecules present on

the cell surface or intracellularly

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OTHER BRANCHES OF PHARMACOLOGY
1. Pharmacotherapeutics
It is the application of pharmacological information
together with knowledge of the disease for its prevention,
mitigation or cure

2. Clinical pharmacology
It is the scientific study of drugs in man

3. Chemotherapy
It is the treatment of systemic infection/malignancy with
specific drugs that have selective toxicity for the infecting
organism malignant cell with no/minimal effects on the 12
host cells.
OTHER BRANCHES OF PHARMACOLOGY CONT…

4. 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.

5. Toxicology
It is the study of poisonous effect of drugs and other
chemicals (household, environmental pollutant,
industrial, agricultural, homicidal) with emphasis on
detection, prevention and treatment of poisonings.

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 APPLICATION OF PHARMACOLOGY
 To control speed of onset, intensity of drug effect and
duration of action

 To identify the possible side effect and withdrawl

symptoms of the drugs

 To avoid adverse effects, drug interactions and

contraindications of drugs

 To avoid treatment failure due to tolerance and

resistance
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 To control misuse of drugs
 NATURE AND SOURCE OF DRUGS

Drugs will be obtained from different sources

1. Natural

2. Semisynthetic

3. Synthetic

4. Biosynthetic

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1. NATURAL DRUGS
a. Plants: -Digoxin from Digitalis purpurea
-Atropine from Atropa belladona
-Quinine from Cinchona officinalis
b. Animals: -Insulin from pork/beef
-Cod liver oil from Cod fish liver
c. Minerals: -Iron, Iodine, Potassium salts
d. Microorganisms:
-Penicillin from Penicillium notatum
-Chloramphenicol from Streptomyces
venezulae (Actinomycetes)
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2. Semi synthetic drugs: These are prepared by
chemical modification of natural drugs
Eg: Ampicillin from Penicillin G

3. Synthetic drugs: These are synthesized drugs

in pharmaceutical laboratory
Eg: Sulphonamides, Quinolones, Barbiturates

4. Biosynthetic drugs:
These are prepared by cloning of human DNA
into the bacteria like E.coli
Eg: Human Insulin (Humilin), human Gh,
monoclonal antibodies
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DRUG NOMENCLATURE

A drug has 3 categories of names

1. Chemical name (IUPAC ) / Scientific name:
 Based on molecular structure of the drug
 Very long, too complex to use in common practice
Eg:1-(lsopropylamino)-3-(1-naphthyloxy) prop an-2 -ol for
propranolol

2. Non-proprietary name / Generic name:

 Given by approval authorities
 Short hand version of chemical name
 Recommended in Rx
Eg: Meperidine (Pethidin), Lidocaine (lignocaine),
paracetamol 18
DRUG NOMENCLATURE

3. Proprietary name / Brand name:

 Given by pharmaceutical companies

 It will be costly
Eg: ALTOL, ATCARDIL, ATECOR, ATEN, BETACARD,
LONOL, TENOLOL, TENORMIN for atenolol, DISPRIN

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ESSENTIAL DRUGS

WHO Definition:
Essential drugs are the drugs which satisfy the
priority healthcare needs of the population

They are selected with due

 regard to public health relevance

 efficacy and safety

 comparative cost effectiveness

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NEED FOR ESSENTIAL DRUG LIST

They should be available within the context of

functioning health systems

 At all times

 In adequate amounts

 In appropriate dosage forms

 With assured quality and adequate information

 At an affordable price
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 WHO prepared its first Model List of Essential
Drugs in 1977

 This has been revised from time to time and the

current is the 20th list (2017) with 433 medicines

 India produced its National Essential Drugs List

in 1996

 It has been revised in 2015 with the title

"National List of Essential Medicines"

 This includes 376 medicines in which 20 are

FDCs 22
ORPHAN DRUGS

 These are drugs or biological products for

diagnosis/treatment/prevention of a rare disease
or condition

Eg: sodium nitrite, fomepizole, liposomal

amphotericin, ancrod, rifabutin, succimer,
somatropin, digoxin immune Fab (digoxin

antibody), liothyronine (T3)

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 ROUTES OF ADMINISTRATION
1. Local: Topical (skin & mucous membrane),
Deeper tissues, arterial supply

2. Systemic
a. Enteral: Oral, Sublingual, Rectal
b. Parenteral – inhalational, injections
(intradermal, subcutaneous, intravenous,
intramuscular, intrathecal), Transdermal

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25
Different routes of
administration and
first pass metabolism

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FACTORS GOVERNING CHOICE OF ROUTE
 Drug characteristics (state, solubility, stability, pH)
 Site of action (localized or generalized)

 Effect of digestive juices and first pass metabolism

 Onset of action (slow or fast)

 Rapidity of response (routine or emergency)

 Accuracy of dose required (i.v. and inhalational)

 Liver and kidney diseases

 Patient condition (unconscious, vomiting)

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 A. LOCAL - TOPICAL

1. Skin
A. Dermal- Drugs applied as ointment, cream, lotion,
paste, powder, spray, oil, gels etc
B. Transdermal – absorption of drug through skin

2. Mucous membrane
 The dosage form depends on the site of application

 Eye drops, eardrops, nasal drops, antiseptics, sunscreen,

jellys etc…

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 B. SYSTEMIC ROUTE
I. ENTERIC – ORAL ROUTE (P.O)
It is oldest and commonest mode of drug administration

Advantages Disadvantages
 Convenient mode  Slow absorption
 Noninvasive  Slow action
 Painless  Irritable and unpalatable
 Economical  Cannot be used for
 Safe uncooperative/ unconciuos
patients
 Can be self administered
 May cause nausea /
 Both solids and liquids can
vomiting
be taken
 First pass effect
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 ORAL DOSAGE FORMS

 Tablets

 Capsules

 Syrup

 Emulsions

 Suspensions

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 Elixirs
2. SUBLINGUAL / BUCCAL ROUTE

 The tablet or pellet containing drug is placed under the

tongue or crushed in the mouth and spread over the buccal
mucosa
 Lipid soluble and non-irritating drugs can be administered

Advantages Disadvantages
 Economical  Unpalatable & bitter drugs
 Quick termination  Irritation of oral mucosa
 First pass avoided  Large quantities can’t be
 Drug absorption is quick given
 Can be self administered  Few drugs are absorbed 31
 3. RECTAL ROUTE
Unpleasant and irritant drugs will be placed into rectum as
suppositories or enema. Eg: Aspirin, theophylline,
chlorpromazine

Advantages Disadvantages
 Used in children  Inconvenient
 Little or no first-pass effect  Irritation or inflammation
 Used in vomiting / of rectal mucosa can occur
unconscious conditions  Absorption is slow and
 Higher concentrations are erratic
achieved rapidly

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 VAGINAL ROUTE

Drugs may be

administered in the

vagina in the form of

pessaries

Eg: Antifungal vaginal

pessaries

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 II. PARENTERAL ROUTE
➢ The drug is injected directly into the tissue fluid or blood
without crossing intestinal mucosa.
➢ Derived from Greek word- para-outside; enteron-intestine
➢ It includes
1. Inhalations – absorption through lungs
2. Injections – administered using syringe needles
3. Transdermal drug delivery system

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 1. INHALATION
 The drug is inhaled into lungs directly
 Gaseous and Volatile drugs. Eg: Anesthetic agents

Advantages Disadvantages
 Rapid onset of action  Irritant vapours cause
 Absorption takes place inflammation of
from vast surface of alveoli respiratory tract
 First pass metabolism is
avoided

NASAL
 The drug is administered into nasal cavity in the form of
spray or nebulizer or drops
 Mucous membrane of nose can readily absorb many drugs
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 Digestive juices and liver bipassed
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 2. INJECTIONS
INTRAVENOUS (I.V.)
 The drug is injected as bolus / infused slowly in one of the
superficial veins
 Drug directly reaches blood stream

Advantages Disadvantages
 100% bioavailability  Cannot be self
 Precise, accurate and administered
immediate onset of action  High risk of adverse effects
 First pass avoided  High conc. Achieved

 Highly irritant drugs can rapidly

be injected  Risk of embolism

 Drugs which are not  Thrombophlebitis and

absorbed orally can be necrosis
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given
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 INTRAMUSCULAR (I.M.)

 The drug is injected in one of the large skeletal muscle-

deltoid, triceps, gluteus maximus, rectus femoris

Advantages Disadvantages
 Fast onset of action  Cannot be self
 First pass avoided administered
 Mild irritants can be
injected

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 INTRADERMAL

 The drug is injected in to the skin raising a bleb

 This route is employed for specific purpose only
 Eg: BCG Vaccine, small pox vaccine

SUBCUTANEOUS
 The drug is deposited in the loose subcutaneous tissue
rapidly supplied by nerves
 Irritants cannot be injected
 Tissue is less vascular. Hence absorption is slow

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 Subcutaneous injection
Intradermal injection

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 3. CUTANEOUS ROUTE

TRANSDERMAL DRUG DELIVERY SYSTEM

• The drug is delivered at the skin surface by diffusion for

percutaneous absorption into circulation

• Drug delivery at constant and predictable rate

Backing film
Drug reservoir
Rate controlling
micropore
membrane
Adhesive layer
with priming
dose
Capillary
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CASE STUDY

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 REFERENCES

 Essentials of Medical Pharmacology by K.D

Tripathi

 Pharmacology for Pharmacy students by

Padmaja Udaykumar

 Goodman and Gilman’s Manual of Pharmacology

and Therapeutics

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 THANK YOU

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