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DRUG METABOLISM

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Tam metin

(1)

DRUG METABOLISM

(BIOTRANSFORMATION)

and

PRODRUGS

INTRODUCTION TO

PHARMACEUTICAL CHEMISTRY

(2)

Drug metabolism

is the

metabolic breakdown

/

chemical changes

of

drugs

by living

organisms

,

usually through specialized

enzymatic

systems.

• Metabolite

is the product of a drug after

metabolic reactions.

(3)

Metabolism is a very important

mechanism for the elimination of

drugs from the body.

(4)

PRO DRUG

• While not exhibiting any activity in vitro, they give the active

compounds metabolically in vivo. These are called

pro drugs

.

(5)
(6)

PHASES OF METABOLISM

Phase I Reactions

(7)

1. OXIDATION REACTIONS

 Aromatic oxidation (Aromatic hydroxylation)  Alken epoxidation

 Oxidation of aliphatic and alicyclic carbon atoms  Oxidation of carbons adjacent to an sp2 center

(Oxidation of carbon atoms in benzyl, allylic and carbonyl or imine - position)  Oxidation of carbon-nitrogen systems

(Oxidative dealkylation, oxidative deamination, oxide formation, N-hydroxylation)

 Oxidation of carbon-oxygen systems (Oxidative O-dealkylation)  Oxidation of carbon-sulfur systems

(Oxidative S-dealkylation, S-oxidation, desulfurization)  Alcohol and aldehyde oxidation

(8)

2. REDUCTION REACTIONS

 Carbonyl (aldehyde, ketone) reduction

 Nitro reduction

 Azo reduction

3. HYDROLYSIS REACTIONS

(9)

Phase II Reactions

(10)

• glucuronic acid

• sulfate

• acetate

Referanslar

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