Dr Bilal Ahmad MalikDr Bilal Ahmad Malik

Sources of DrugSources of Drug&&

Active principle of DrugActive principle of Drug

ObjectivesObjectives

After completing the discussion, the student will be able toAfter completing the discussion, the student will be able to

Define drug and medicineDefine drug and medicine

Describe different sources of drugDescribe different sources of drug

Identify the active principles of a drugIdentify the active principles of a drug

Select authorative sources of drug Select authorative sources of drug information.information.

Do Drugs play any role in our lives ?

MedicinesMedicines

Part of our way of Life Part of our way of Life

Birth DeathBirth Death..

Average family experiences illness on Average family experiences illness on one day in four.one day in four.

Between ages of 20-45 years a lower Between ages of 20-45 years a lower middle class man experiences approx. middle class man experiences approx.

one life endangering illness one life endangering illness 20 disabling (temporarily) illnesses20 disabling (temporarily) illnesses 200 non disabling illnesses200 non disabling illnesses 1000 symptomatic episodes1000 symptomatic episodes 12 years of bad health in an average life 12 years of bad health in an average life

span. span.

What is Drug ?What is Drug ?

What is Medicine ?

Drugs/MedicinesDrugs/Medicines WHO scientific group has defined a drug asWHO scientific group has defined a drug as

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.

A substance that changes the biological system by interacting with it

A medicine is a substance or a A medicine is a substance or a mixture of substances used in mixture of substances used in restoring or preserving health.restoring or preserving health.

A drug is a single chemical substance A drug is a single chemical substance that forms the active ingredient of a that forms the active ingredient of a medicine.medicine.

A medicine may contain many other A medicine may contain many other substances to deliver the drug in a substances to deliver the drug in a stable form, acceptable and convenient stable form, acceptable and convenient to the patient. to the patient.

Drug vs Medicine?

Why do we Why do we need/ Use need/ Use Drugs/Drugs/

Medicines?Medicines?

Uses of drugs/MedicinesUses of drugs/Medicines

To cure the disease

To suppress the disease

To prevent disease

To diagnose the disease

PharmacologyPharmacology

Study of pharmacology involves the study ofStudy of pharmacology involves the study of

origin of drugs origin of drugs Chemical and physical properties of drugsChemical and physical properties of drugs Physiologic effects and site of action in the Physiologic effects and site of action in the

bodybody Absorption, distribution, metabolism, and Absorption, distribution, metabolism, and

excretion.excretion. Safe/effective dosage regimen & route of Safe/effective dosage regimen & route of

administration.administration. Adverse reactions, toxic effects & drug-drug Adverse reactions, toxic effects & drug-drug

interactions interactions

Sources of DrugsSources of Drugs

Naturally occurringNaturally occurring Modified natural drugsModified natural drugs Mineral sourcesMineral sources Microbial sourcesMicrobial sources Human sources Human sources Synthetic sources Synthetic sources Genetic engineeringGenetic engineering

Active principles of drugActive principles of drug

A constituent of a A constituent of a drug, upon the, upon the

presence of which the presence of which the characteristic

therapeutic action of the of the substance

largely depends. largely depends.

Examples Examples Alkaloids Alkaloids

GlycodiesGlycodies

TanninsTannins

Oleo-resinsOleo-resins

Oils Oils

Gums Gums

Natural sources of drugsNatural sources of drugs

Animals

Plants

Plant SourcesPlant Sources

Plant SourcesPlant Sources

Earliest sourceEarliest source

GalenicalsGalenicals --- ---

Galen (Greek Galen (Greek physician)physician)

Active Principles Active Principles in in

Plants Plants

1. Alkaloids1. Alkaloids

organic organic nitrogenous substances bitter

insoluble in water insoluble in water

react with acids to form saltsreact with acids to form salts

salts are soluble in body fluidssalts are soluble in body fluidsExamples are Examples are

atropine, , caffeine,, ,, morphine, , nicotine, , quinine, ,

reserpine, emetine, codeine, tubocurarine.reserpine, emetine, codeine, tubocurarine.

Morphine (opioid analgesic)

Heroin

codeine

unripe capsules papaver somniferum (Opium Poppy).

Nicotine,Nicotine, the the

active principles active principles

of tobacco of tobacco

Caffeine (CNS Stimulant) Caffeine (CNS Stimulant) is the active is the active

principle in tea, coffee.principle in tea, coffee.

Cocaine Cocaine is the active principle of the is the active principle of the

coca leaf, which is chewed as a coca leaf, which is chewed as a

stimulant-narcoticstimulant-narcotic

Atropine (Anticholinergic) ---- from leaves of atropa belladona.

Ephedrine (bronchodilator) ---- from plant Ephedra Vulgaris

Quinine (Antimalarial) ---- from bark of Cinchona.

Reserpine (Antihypertensive) ---- from roots of Rauwalfia serpentia

2.2. GlycosidesGlycosides

Any Any compound that contains a that contains a carbohydrate molecule (sugar) molecule (sugar)

by hydrolytic cleavage, convertible into by hydrolytic cleavage, convertible into sugar and a nonsugar component (aglycone) sugar and a nonsugar component (aglycone)

glucoside (glucose), glucoside (glucose), pentosidepentoside (pentose), (pentose), fructoside (fructose) etc fructoside (fructose) etc

EXAMPLE:EXAMPLE:

Digoxin Digoxin (cardiac stimulant)(cardiac stimulant)------ leaves leaves

of digitalis purpurea or digitalis of digitalis purpurea or digitalis

lanatalanata

Anthraqinone glycosides Anthraqinone glycosides ((laxative laxative

action)action) ---------- senna,cascara,aloe senna,cascara,aloe

3. 3. OilsOils

Fixed oils

Volatile oils

Mineral oils

Fixed oils Fixed oils

Esters of fatty acid and glycerol Edible

Examples Coconut oil Mustard oil Olive oil Castor oil (Purgative) Cod liver oil (Vitamin A & D) Used in the preparation of ointments, suppositories, Soaps

Volatile OilsVolatile OilsEssential or flavoring oils.

EXAMPLES:

LIQUIDClove oil (toothache)Eucalyptus oilCoriander oilDill oilGinger oil ( Carminative)Terpentine oil ( counter irrritant )

SOLIDSCamphor Menthol (peppermint oil)

Mineral OilMineral Oil

Hydrocarbon

Obtained from petroleum

EXAMPLE: Liquid paraffin (Lubricant & Laxative)

4. 4. RESINSRESINS

Formed by :

Oxidation or polymerization of volatile oilsAmorphous, brittle, translucent, hard solids

Example:

Podophyllum (Purgative action),Jalap ( hydragogue)

Toxicological importance

5. OLIORESINS5. OLIORESINS

Mixtures of resins & volatile oils

Example:

Benzoin (Antiseptic)

6. GUMS6. GUMS

Inert ----- emulsifying agents -Gum acacia, Gum tragacanth

Active --------------------------------------- Agar (Purgative)

7. TANNINS7. TANNINS

Mixture of esters of Gallic acid + Glucose

Astringent action on MM Hemostatic

Animal SourcesAnimal Sources

Animal SourcesAnimal Sources

HormonesHormones Insulin Insulin (hypoglycemic)(hypoglycemic)

Oils and fatsOils and fats cod-liver oilcod-liver oil

EnzymesEnzymes Pancreatin, Pepsin Pancreatin, Pepsin

VaccinesVaccines killed, modified or killed, modified or

attenuated virusesattenuated viruses

Mineral Sources of DrugsMineral Sources of Drugs

Mineral Sources of DrugsMineral Sources of Drugs Eg:Eg:

• Iron (Anemia)Iron (Anemia)• Aluminum hydroxide (Antacid) Aluminum hydroxide (Antacid) • Iodine Iodine ( Lugol’s iodine for thyrotoxicosis, ( Lugol’s iodine for thyrotoxicosis,

tincture iodine as antiseptic )tincture iodine as antiseptic )

• Magnesium sulphate (Purgative)Magnesium sulphate (Purgative)• Sulphur (Scabies)Sulphur (Scabies)• Antimony salts (Kala Azar)Antimony salts (Kala Azar)• Bismuth Salts (peptic Ulcer )Bismuth Salts (peptic Ulcer )

Microbial Sources

Examples Examples

AntibioticAntibioticss

Penicillin -----Penicillin ----- Penicillium chrysogenumPenicillium chrysogenum

Streptomycin, neomycin ----Streptomycin, neomycin ----Actinomycetaceae.Actinomycetaceae.

EnzymesEnzymesStreptokinase Streptokinase (Fibrinolytic) ---- (Fibrinolytic) ---- streptococcusstreptococcus

HUMAN SOURCES

Immunoglobulins ------------ from blood

Growth hormones ---------- anterior pituitary

Chorionic gonadotropin-- urine of pregnant women

SYNTHETIC SOURCES

Organic

e.g.: penicillin

Inorganic

sulfonamide antibiotics oral contraceptives

GENETIC ENGINEERING

Laboratory Produced Drugs

Recombinant drugs

And what,” you ask, “is a And what,” you ask, “is a recombinantrecombinant drug?!” drug?!”

Recombinant DrugsRecombinant Drugs

These are drugs These are drugs produced by produced by means of means of recombinant recombinant DNA technologyDNA technology

It all starts with a It all starts with a gene that codes gene that codes for a specific for a specific protein ...protein ...

DNA

RNA

Protein(A drug)

How a recombinant drug is madeHow a recombinant drug is made ... ...

Plasmid(a circular bit o’ DNA)

cDNA(codes for a protein)

E.COLI

HUMAN INSULIN

Example of a Recombinant DrugExample of a Recombinant Drug::InsulinInsulin

Most insulin is Most insulin is now recombinantnow recombinant

Consists of two Consists of two chains (A and B)chains (A and B)

A and B chains A and B chains joined chemicallyjoined chemically

S

S

A

B

SOURCES OF DRUG INFORMATIONSOURCES OF DRUG INFORMATION

Sources of Drug InformationSources of Drug Information

The United States Pharmacopoeia (USP) and The United States Pharmacopoeia (USP) and National Formulary (NF) National Formulary (NF)

Physician's Desk Reference (PDR)Physician's Desk Reference (PDR) Drug Facts and Comparisons Drug Facts and Comparisons Textbook Textbook Journals Journals Continuing medical education programsContinuing medical education programs Drug company representativesDrug company representatives Advertisements ( medical/nonmedical journals) Advertisements ( medical/nonmedical journals) InternetInternet

Helpful Internet SitesHelpful Internet Sites

MedscapeMedscape (http:/www.medscape.com)(http:/www.medscape.com) Food and Drug Administration Food and Drug Administration

(http:/www.fda.gov)(http:/www.fda.gov) PharmInfo PharmInfo (http:/www.pharminfo.com)(http:/www.pharminfo.com) RxMed RxMed (http:/www.rxmed.com)(http:/www.rxmed.com)