By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

SOURCES & NATURE OF DRUGS

Drug is a substance which is used for the following purposes:
Diagnosis of the disease
Prevention of the disease
Treatment or palliation (relief of symptoms) of disease
Prevention of pregnancy (i.e. contraception)
Maintenance of optimal health
1: Symptomatic:
 Relieve disease symptoms. Aspirin, Tylenol.
2: Preventative:
 To avoid getting a disease. Hepatitis B vaccine, Flu vaccine.
3: Diagnostic:
 Help determine disease presence. Radioactive dyes.
4: Curative:
 Eliminate the disease. Antibiotics.
5: Health Maintenance:
 Help keep the body functioning normally. Insulin.
6: Contraceptive:
Preventative

Sources of Drugs
Drug- (fr. Drogue- dried herbs), medication, and medicament: Substance administered to
humans and animals for diagnosis or treatment of diseases.
Sources of drugs are as follows:

THERE ARE FOUR SOURCES OF DRUG:

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NSHM COLLEGE OF PHARMACETICAL TECHNOLOGY, NSHM KNOWLEDGE CAMPUS, KOLKATA
By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

I. NATURAL SOURCES

Most primitive and abundant.

Drugs are obtained from the following natural sources:

A) PLANTS, B) ANIMAL SOURCES, C) MINERAL & D) MICROORGANISMS

A- PLANTS:
Following categories of drugs are derived from roots, leaves or barks of plants:

a) Alkaloids

These are nitrogenous heterocyclic bases, which are pharmacologically active principles
of plants.
They are composed of carbon, hydrogen, nitrogen and oxygen.
They are bitter in taste and are often poisonous. These are, therefore, used in small doses.
They are insoluble in water. However, they form salts with acids which are soluble in
water.

Some examples of alkaloids and their sources are listed in the table:

ALKALOID SOURCE

Atropine Atropa belladonna

Quinine Cinchona bark

Morphine Papavarum somniferum

Reserpine Rauwolfia serpentina

Nicotine Tobacco

Digoxin Digitalis lanata

Caffeine Coffee, Tea, Cocoa

b) Glycosides

They are ether-like combination of sugar moiety with non-sugar moiety.

They are called glycosides, if the sugar moiety is glucose.
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By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

Sugar moiety is not essential for the pharmacological activity but it governs the
pharmacokinetic properties of the glycoside. In the body it may be removed to liberate
aglycone.
Pharmacological activity resides in the non-sugar moiety that is called aglycone (or
genin).
Some examples are digitoxin, digoxin and ouabain.

c) Oils

They are liquids which are insoluble in water. They are of three types and are used for various
medicinal purposes.

i) Essential Oils (or volatile oils): Essential oils are obtained from leaves or flower petals by
steam distillation, and have an aroma.

They have no caloric or food value.

They do not form soaps with alkalis.

They do not leave greasy stain after evaporation.

On prolonged stay, they do not become rancid (foul smell).

They are frequently used as carminatives and astringents in mouth-washes.

Some of these oils are solid at room temperature and sublime on heating e.g. menthol and
camphor.

Other examples are clove oil, peppermint oil, eucalyptus oil and ginger oil.

ii) Fixed oils are glycerides of stearic, oleic and palmitic acid.

They are obtained from the seeds that are present within the cells as crystals or droplets.
They are non-volatile and leave greasy stains on evaporation.
They have caloric or food value.
They form soaps with alkalies.
On prolonged stay, they become rancid.
They do not have marked pharmacological activity and have little pharmacological use
except castor oil (purgative) or arachis oil (demulcent).
They may be of vegetable origin e.g. olive oil, castor oil, croton oil and peanut oil or of
animal origin e.g. cod liver oil, shark liver oil and lard.

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NSHM COLLEGE OF PHARMACETICAL TECHNOLOGY, NSHM KNOWLEDGE CAMPUS, KOLKATA
By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

iii) Mineral Oils are mostly petroleum products and extracted by fractional distillation.

These are mixtures of hydrocarbons of the methane and related aliphatic series.
These are extracted in various consistencies - hard paraffin, soft paraffin and liquid
paraffin.
Hard and soft paraffins are used as vehicles for preparation of ointments while liquid
paraffin is employed as a purgative.
d) Gums are colloidal exudates from plants which are polysaccharides chemically and yield
simple sugars on hydrolysis.

Upon addition of water, some of them swell or dissolve or form adhesive mucilage or
remain unchanged.

Uses:
In gut agar and psyllium seeds act as hydrophilic colloids and function as bulk
purgatives.
Gum acacia and gum tragacanth are used as suspending agents in making emulsions and
mixtures.
e) Resins are ill-defined solid substances found in plants, and are polymers of volatile oil.

They are produced by oxidation and polymerization of volatile oils.

They are insoluble in water but soluble in alcohol, chloroform and ether.
Examples: oleoresins (aspidium); gum resins (asafoetida); oleogum resin (myrrh);
balsams (benzoin, tolu, peru); benzoin shellac, podophyllum.

Uses:
o Benzoin is used as inhalation in common cold.
o Tincture benzoin is applied as antiseptic protective sealing over bruises.
o Colophony (an oleoresin) is used as an ingredient in various plasters.
o Shellac (from Lucifer lacca) is used for enteric coating of tablets.
o Balsams are used in the treatment of cough and bronchitis for their antiseptic and
protective properties.
o Podophyllum is used as an irritant purgative.
f) Tannins are non-nitrogenous phenolic plant constituents which have an astringent action.

Pyrogallol tannins are glycosides of glucose that occur in oak galls.

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NSHM COLLEGE OF PHARMACETICAL TECHNOLOGY, NSHM KNOWLEDGE CAMPUS, KOLKATA
By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

Pyrocatechol tannins are sugar-free derivatives of catechol that are present in catechu and
eucalyptus.

Tannic acid is tannin that is obtained from oak galls and is used for treating burns and
diarrhoea.

B-ANIMAL SOURCES

Some animal sources continue to be used to procure some modern drugs because of cumbersome
and expensive procedures for the synthesis of such chemicals.

For example:

Insulin, extracted from pork and beef pancreas, is used for the treatment of diabetes
mellitus.
Thyroid powder for treating hypothyroidism.
Heparin is used as an anticoagulant.
Hormones and vitamins are used as replacement therapy.
Vaccines (cholera, T.B., smallpox, polio and antirabic) and sera (antidiptheria and
antitetanus) are used for prophylaxis/treatment.

C-MICROBIOLOGICAL SOURCES

Many life-saving drugs are obtained from fungi, moulds and bacteria e.g. penicillin from
Penicillium notatum, chloramphenicol from Streptomyces venezuelae, grisofulvin (an anti-
fungal drug) from Penicillium griseofulvum, neomycin from Streptomyces fradiae and
streptomycin from Streptomyces griseus.

D-MINERAL SOURCES

Minerals or their salts are useful pharmacotherapeutic agents.

For example:
Ferrous sulfate is used in iron deficiency anaemia.
Magnesium sulfate is employed as purgative.
Magnesium trisilicate, aluminium hydroxide and sodium bicarbonate are used as antacids
for hyperacidity and peptic ulcer.
Kaolin (aluminium silicate) is used as adsorbent in antidiarrheal mixtures.
Radioactive isotopes of iodine, phosphorus, gold are employed for the diagnosis/
treatment of diseases particularly malignant conditions.
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NSHM COLLEGE OF PHARMACETICAL TECHNOLOGY, NSHM KNOWLEDGE CAMPUS, KOLKATA
By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

II. SEMISYNTHETIC SOURCES

Sometimes semi-synthetic processes are used to prepare drugs when the synthesis of drugs
(complex molecules) may be difficult, expensive and uneconomical or when the natural sources
may yield impure compounds. In these situation this methods plays an important role.

Some examples are semi synthetic human insulin and 6-aminopenicillanic acid derivatives.

Prepared by chemically modifying substances that are available from natural source improve to
improve its potency, efficacy and also reduce side effects.

Eg. i) Semi synthetic drugs from plant sources

Heroine from Morphine

Bromoscopolamine from scopolamine
Homoatropine from atropine.

ii) Semi synthetic drugs from animal sources:

Animal insulin changed to be like human insulin

6-aminopenicillanic acid derivatives.

III. SYNTHETIC SOURCES

At present majority of drugs used in clinical practice are prepared synthetically, such as aspirin,
oral antidiabetics, antihistamines, amphetamine, chloroquine, chlorpromazine, general and local
anaesthetics, paracetamol, phenytoin, synthetic corticosteroids, sulphonamides and thiazide
diuretics.

Most of the synthetic drugs are prepared synthetically i.e. by chemical process ( reaction) with
the help of the knowledge of phytochemical investigation.

Alterations are made on the naturally found structure of the drug to improve its effect and
to improve the finances of pharmaceutical companies.

Advantages of synthetic drugs are:

They are chemically pure.

The process of preparing them is easier and cheaper.
Control on the quality of the drug is excellent.

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NSHM COLLEGE OF PHARMACETICAL TECHNOLOGY, NSHM KNOWLEDGE CAMPUS, KOLKATA
 By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

Since the pharmacological activity of a drug depends on its chemical structure and
physical properties, more effective and safer drugs can be prepared by modifying the
chemical structure of the prototype drug.

IV. BIOSYNTHETIC SOURCES (genetically engineered drugs)

This is relatively a new field which is being developed by mixing discoveries from molecular
biology, recombinant DNA technology, DNA alteration, gene splicing, immunology and
immunopharmacology.

Some of the recent developments are genetically engineered novel vaccines (Recombinex HB - a
hepatitis-B vaccine), recombinant DNA engineered insulins (Humulin- human insulin) for
diabetes and interferon-alpha-2a and interferon-alpha-2b for hairy cell leukaemia.

For instance: genetically engineered Hepatitis-B vaccine formation:

Genetic material (DNA) The responsible gene that This gene is removed
extracted from Hepatitis directs the surface protein from virus DNA and
virus. production is then located. inserted into
“plasmid”.

Yeast is then grown by These Plasmids are

fermentation. Cells reproduce then inserted into
and generate large amounts of yeast cells.
surface protein.

Large quantity of surface

After 48 hours yeast cells are protein thus produced is
ruptured to free the surface protein stabilized with preserving
which is then extracted and agents and other ingredients
purified. to make the vaccine.

Hepatitis B Vaccine is ready

for use.
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NSHM COLLEGE OF PHARMACETICAL TECHNOLOGY, NSHM KNOWLEDGE CAMPUS, KOLKATA
 By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

Genetic manipulation of nonpathogenic, rapidly growing bacteria, such a E. Coli, to enable them
to manufacture complex biological compounds that would be extremely difficult or costly to
prepare by conventional means.

Recently chemists have developed computer programs to facilitate the design of new drugs.
These programs help design chemicals that fit to the 3-D conformation of the receptor……

-led to the discovery of HIV protease inhibitors, ACE inhibitors etc.

Drug Preparations- What are the differences?

Crude-

Pure- ?

Pharmaceuticals-

Drug Preparations

Crude drug preparations

Drying, pulverizing

Extraction; Alcohol, hot

water>Coffee, Tea, Opium

Pure drug compounds

Morphine, Insulin

Pharmaceutical preparations

Figure 1 Types of drug preparations.

A crude drug preparation retains most or all of the active and inactive compounds contained in the
natural source from which it was derived. After a pure drug compound (e.g., morphine) is extracted
from a crude drug preparation (in this case, opium), it is possible to manufacture pharmaceutical
preparations that are suitable for administration of a particular dose to the patient.

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NSHM COLLEGE OF PHARMACETICAL TECHNOLOGY, NSHM KNOWLEDGE CAMPUS, KOLKATA
 By Somnath Mondal, 2010 Pharmacology 5th semester, Sources of Drugs

Expected Question??

Write a note about the sources of drugs with example.

Why are synthetic drugs used most widely?

Write a note about biosynthetic sources of drug along with example.

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