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DR. RAHUL KUNKULOL

ASSO.PROF. PHARMACOLOGY

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Pharmacology

A Very Basic

Intro…..

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Introduction

What is Pharmacology? Why do we need to take

Pharmacology?

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What is Pharmacology?

It is the science that deals with the study of drugs and its effect on biological system.

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What is a drug?

WHO definition….Drug is any substance or product used or intended to be used to modify or explore the physiological state or pathological condition for the well being of the recipient

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PharmacologyPharmacokinetics

Pharmacodynamics What the body does to drug What the drug does to

body

Pharmacotherapeutics Pharmacocognosy

The study of the use of drugs Identifying crude materials as drugs

Pharmacology

Toxicology

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PHARMACOKINETICSIs what the body does to the

drug ?......

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Pharmacokinetics

The magnitude of the pharmacological effect of a drug depends on its concentration at the site of action.

Absorption Distribution Metabolism Elimination

PharmacokineticsWhat the body does to the drug

t1/2 (Half-Life)- the time required for the plasma concentration of a drugto be reduced by 50%

ED50 (effective dose)- The dose of a drug that is effective for 50% of the population exposed to the drug

LD50 (lethal dose)- the dose at which death occurs in 50% of subjects

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PHARMACODYNAMICSIs what the drug does to the

body ?...

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Pharmacodynamics

Interaction of drugs with cellular proteins, such as receptors or enzymes, to control changes in physiological function of particular organs.

Drug-Receptor Interactions› Binding

Signal Transduction› Mechanism of action, Pathways

Dose-Response› Effect

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- Based on the chemical structure  - Based on the main effect (e.g.

analgesics).- Based on the therapeutic use (e.g.

antidepressant).- Based on mechanism of action (e.g.

serotonin agonist). 

DRUG CLASSIFICATION

- Chemical name - *Generic name - Trade name

Chemical Name: 2-(4-isobutylphenyl)-propionic acid

Generic Name: ibuprofen

Trade Names: Advil, Aches-N-Pain, Brufen, Emodin, Haltran, Medipren, Midol 200, Motrin, Nuprin, Rufen, Trendar, Wal-Profen

*preclinical nomenclature = company abbrev-123456 (e.g. WAY-100635, MK-869)

Drug Nomenclature

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15Sources of DrugsPlants

AnimalsMineralsMicrobes Synthetics

Genetic engineering

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Sources of Drugs (cont.)Sources Details Examples

Plants Berries (seeds) , bark, LeavesResin from trees, roots

MorphineQunineDigitalis / Digoxin Gum acacia

Minerals Earth & soil Iron, sulfur, potassium, silver & even gold

Animals Glands, organs & tissues Pork insulin

Synthetic Man made Meperidine, sulphonamides

Microbes Fungus StreptomycetsBacteria

PenicillinsErythromycinBacitracin

Plants Alkaloids : Nitrogenous bases

derived from plant. There names end with ‘ne'.

Examples :Morphine, Quinine

Glycosides : Are plant products with sugar moiety attached to non-sugar with ether linkage. Examples : Digoxin

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Plants Gums :Exudates of plants. used as emulsifying agents

› Ex. Gum acacia Resins :Polymers of volatile oil

› Ex. Benzoin

Tannins :Nonphenolic nitrogenous derivatives. Used as astrigents.

› Ex. Tinc,. Catechu

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PlantsPurple foxglove, Digitalis purpurea

From the leaves of this plant was isolated the cardiac glycoside Digitalis, a drug still used today to treat heart failure.

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Papaverous somniferum Morphine was isolated from the opium

poppy

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Artemisia annua L. (wormwood),

The eastern herb used in China since antiquity to treat fevers, is the source of the modern drug qinghaosu, which shows great promise as a modern anti-malarial compound.

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Cinchona : Qunine

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Atropa belladonna :Atropine

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Erythroxylon coca :cocaine

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PlantsPlant Part Drug Use

Chinchona Bark Quinine Anti malarialPurple Foxglove

Leaves Digitallis Congestive cardiac failure

Pappaverous somniferous

Poppy seeds(opium)

Morphine Codeine

Opioid Analgesicantitussive

Artimisia annua

Quinghousu Artimisinin derivatives

Antimalarial

Atropa belladona

Leaves Atropine OPPs

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AnimalsAnimal Part Drug Use

Cow Pancreas Insulin Antidiabetic hormone

Fish Sperms Protamine sulphate

Antidote of heparin

Pig intestine Heparin anticoagulants

Ox lungs Heparin anticoagulants

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Synthetic Pethidine

Cotrimoxazole

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Minerals

Minerals Drugs Uses

Magnesium Milk of magnesia

constipation

Iron Ferrous sulphate

Anaemia

Zinc Zinc oxide ointment

Calamine lotion

Calcium Calcium sulphate

Osteoporosis

Gold Gold salts Rheumatoid arthritis

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Microbes

Microbes Name Drug

Fungi Penicillium notataum Penicillin

Actinomycetes

Streptomyces VenezuelaStreptomyces aurefaciens

ChloramphenicolTetracycline

Bacteria Bacillus subtilis Bacitracin

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Genetically engineered Recombinax HB (hepatitis B

Vaccine) Human erythropoetin Human Insulin Abciximab

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Drug Formulation

Dosage: Amount of drug to be administered usually based on weight. Example: mg/kg

Concentration: How the drug is formulated into a solution . Example: mg/ml

Injection Volume: A liquid measurement based on weight . Example: ml/kg

Drug Formulation

Drug Formulationexamples……

VERY SIMPLE FORMULATION:

A rat needs to be administered a dosage of 50mg.

The drug is in a liquid form of concentration 25 mg/ml.

What volume of the solution needs to be injected?

Drug Formulationexamples……

SIMPLE FORMULATION:

The rat weighs 350 g.

The maximum volume to be injected IP in a rat is 1ml/kg.

The dose to be administered is 10mg/kg.

The dose is in a liquid concentration of 10mg/ml.

What volume of the solution will be injected into the rat?

Drug Formulationexamples……

SIMPLE FORMULATION:

The rat weighs 350 g.

The maximum volume to be injected IP in a rat is 1ml/kg.

The dose to be administered is 10mg/kg.

The dose is in a liquid concentration of 10mg/ml.

SIMPLE ANSWER:

1. Transform weight: A 350 g. rat = 0.35 kg.

2. Determine max. vol.: 0.35 kg X 1ml/kg = 0.35 ml volume

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Thank you