SUBJECT

OF
PHARMACOLOGY & THERAPEUTICS
 Lecture topic:
Definition of drug, sources and active
principals of drugs, structure activity
relationship of drugs and drug
nomenclature.
 Learning objectives
1. Describe the sources and active
principles of drugs.
2. Explain the structure-activity
relationship of drugs.
 Sources of Drugs
Drugs may be obtained from:
■ Plants
■ Animals
■ Mineral / Earth sources
■ Synthetic / Semi-synthetic sources
■ Microbiological sources
■ Recombinant DNA technology /
Genetic engineering.
 Plant / Vegetable Sources
■ The oldest natural source
■ Even now some drugs are obtained
from the plant source.
■ Drugs can be obtained from all parts
of the plants.
 Plant / Vegetable Sources…
LEAVES
■ Digitalis purpura …….. Digoxin, Digitoxin
■ Euclaptus …….. Euclaptus oil
■ Tobacco leaves …….. Nicotine
■ Atropa Belladona …….. Atropine

FLOWERS
■ Papaver Somniferum …….. Morphine
■ Vinca rosea …….. Vincristine, Vinbastine
■ Rose …….. Rose water
Nicotine, the
active principles
of tobacco
Morphine (opioid analgesic)
Heroin
codeine
unripe capsules papaver
somniferum (Opium Poppy).
 Plant / Vegetable Sources…

FRUITS
■ Senna pod ….. Anthracene
■ Calabar beans …..
Physostigmine

Calabar beans
 Plant / Vegetable Sources…

Castor Oil Seeds Calabar Beans

 Plant / Vegetable Sources…

Rouwolfia sepentina root

 Plant / Vegetable Sources…
BARKS
■ Cinchona bark ……. Quinine, Quinidine
■ Atropa Belladona ……. Atropine
■ Hyoscyamus niger ……. Hyoscine

Cinchona bark Atropa Belladona

 Plant / Vegetable Sources…

STEM
■ Chondrodendron tomentosum ….. D-
tubocurarine
■ Atropa Belladona ….. Atropine

Chondrodendron tomentosum
 Animal Sources
■ Various organs & tissue of animals are
used as source of drug.
■ Active principles of animal drugs are
proteins, oils, fat, enzymes and hormones.

Pancreas → Insulin
Cod liver → Cod liver oil (contains Vit A
& D)
Blood of animals → Anti toxins,
Vaccines
Stomach tissues → Pepsin, Trypsin
 Mineral / Earth Sources
Many drugs are mineral substances &
their compounds.
■ Metals: Iron , Zinc, Gold salts

■ Non - metallic element: Iodine

■ Miscellaneous: Fluorine, Selenium

 Synthetic & Semi-synthetic
Sources
■ The drugs are prepared in
pharmaceutical laboratories. They
may be organic or inorganic
compounds or combination of both.
■ 90% drugs in use are prepared
synthetically.
Diazepam.
Diacetyl morphine.
Ethinyl estradiol.
 Microbiological Sources

These are prepared from bacteria &

moulds.
Examples:
■ Antibiotics: Penicillin ,
Erythromycin
■ Vitamins
 Recombinant DNA Technology
/ Genetic Engineering
The new technique for preparing certain
drugs e.g. Human insulin, insulin analogs ,
Erythropoietin, Plasminogen Activators,
Interferons

Human Insulin & insulin analogs may be

prepared by inserting human or modified
pro-insulin gene into E-coli or yeast &
treating the extracted pro-insulin to form
the insulin or insulin analogs.
 Method- Recombinant DNA
Technology / Genetic Engineering
■ In terms of genetic modification,
recombinant DNA is produced through the
addition of relevant DNA into an existing
organismal genome, such as the plasmid of
bacteria, to code for or alter different traits for a
specific purpose.

■ Plasmids are extra-chromosomal self-replicating

circular forms of DNA present in most bacteria,
such as Escherichia coli (E. Coli), containing genes
related to catabolism and metabolic activity,
and allowing the carrier bacterium to survive
and reproduce in conditions present within
 Recombinant DNA Technology / Genetic
Engineering…

Advantages:
■ Mass production.
■ Cost effective
■ Less immunological reactions

Disadvantages
■ Complex technique
■ Need a well trained staff
■ Well equipped lab
Active Principles Of Crude
Drugs
 Active Principles Of Crude Drugs..

Definition

The chemical constituents present in

crude animal/vegetable preparations,
responsible for their biological activity are
called active principles.

Active Principles have been purified and

synthetic/ semi- synthetic derivatives can
be prepared and used in therapeutics.
 Important Active principles
• Alkaloids Glycosides
• Saponins Fixed oils
• Volatile oils Fats
• Waxes Gums
• Resins Oleoresins
• Gum resins Balsams
• Tannins
 Alkaloids
Characteristics:
• Found in plants.
• Nitrogenous compounds of complex
structure.
• Intensely bitter.
• Insoluble in water, soluble in alcohol.
• Very active biologically, alkaline in
reaction.
• Mostly solids, only a few are liquids.
• English names end in ----“INE”.
 Alkaloids…
Examples:
Solid Alkaloids:
■ Morphine, Papaverine
■ Atropine , Hyoscine
■ Quinine
■ Ephedrine
■ Strychnine
Liquid Alkaloids:
■ Nicotine , Pilocarpine , Lobeline
 Glycosides
Characteristics
■ Found in plants.
■ Non nitrogenous, containing carbon,
hydrogen & oxygen
■ Complex structure & very active
biologically
■ Hydrolyzed by acid / enzymes.
■ English names end in letter “IN”
 Glycosides…

Examples:

Cardiac Glycosides:
■ Digoxin Digitoxin
■ Gitoxin Gitalin
 Fixed Oils
■ Obtained from various plants or animals.
■ Esters of higher fatty acid.
■ Insoluble in water, soluble in ether,
chloroform, alcohol.
■ Bland + non irritating.
■ Leave greasy mark on paper.
■ Form soaps with alkalies.
Used as: Nutrient, Emollient, Purgative.
Examples: Castor oil, Cod liver oil,
Olive oil.
 Volatile Oils
(Essential Oils / Ethereal Oil)
■ Obtained from various parts of plants.
■ Mostly contain liquid hydrocarbons
which are monoterpenes.
 Volatile Oils
(Essential Oils / Ethereal Oil)…

In addition most contain oxidized

hydrocarbons.
■ They are usually crystalline solids,
called stearoptenes.
■ Highly aromatic, slightly water soluble
– impart smell & taste.
Used as: Volatile Oils…
■ Carminative e.g. cardamon oil
■ Diuretic e.g. oil of sandal wood
■ Antiseptic e.g. clove oil
Examples
Usually Solids:
Camphor Thymol Menthol
Some Liquids: Eucalyptol
 Fats
■ Source Plants
Animals
■ Fixed oils solid at room temperature
■ Natural ester of glycerol & fatty acids. All
the three OH groups of glycerol are
estrified, so called Triglycerides
■ Examples: Theobroma (cocoabutter) ,
Lard, Wool fat (Lanolin)
 Waxes
■ Esters of fatty acids with monohydric
alcohols
■ Complex mixtures

■ Used in ointments & other topical

preparations used on skin.
Examples: White bee’s wax (cera alba)
 Gums
■ Plant exudations
■ Carbohydrate in nature Starch
Cellulose
■ Amorphous (shapeless), Transparent
 Gums..
■ Used as suspending/emulsifying
agents in preparation of suspensions
& emulsions.

Examples: Gum Acacia, Gum

Tragacanth
 Structure-activity relationship of
drug
■ Structure-activity relationship (SAR) is the
relationship between the chemical or
three-dimensional structure of a molecule
and its biological activity.

■ The analysis of SAR facilitates the

determination of the new chemical
groups responsible for evoking a target
biological effect in the organism.
 Structure-activity relationship of drug…

■ The biological effects of a new chemical

compound can often be predicted from
its molecular structure using data about
other similar compounds
■ This is because similar compounds may
have similar physical and biological
properties
■ There is a relationship between
molecular structures and their biological
activity, and this principle is referred to
as Structure Activity Relationship (SAR)
 Structure-activity relationship of drug…

■ Medicinal chemists use the techniques of

chemical synthesis & computational drug
design to insert new chemical groups
into the biomedical compound and test
the modifications for their biological
effects
 Pharmacology Books
Main Textbook:
th
■ Bertram. G. Katzung, Basic & Clinical Pharmacology ----14 Edition

Review Books: ( and for MCQs)

h
■ Katzung & Trevor’s Pharmacology Examination & Board Review 10t Edition

■ Lippincott’s Illustrated Reviews (Pharmacology) Edition-7 th

Reference Books:
th
■ Essentials of Medical Pharmacology by KD Tripathi Edition – 6
th
■ Pharmacology By Rang, Dale, Ritter --- Edition-8

■ Multiauthor Textbook of Pharmacology & Therapeutics (Vol I) Latest Edition

th
■ Goodman & Gilman’s The Pharmacological Basis of Therapeutics Edition-12
th
■ Clinical Pharmacology By D.R. Laurance, P.N. Bennett, M.J. Brown Edition-11

Practical Notebook:
■ Pharmacology Practical Manual by Prof. Dr. Muhammad Akram
Randhawa, HBS Medical & Dental College, Islamabad.
The end