DRUG METABOLISM

PRESENTED BY

Piyali Dey
ID: 192015033
Department: Biochemistry.
Primeasia University.
PRESENTED TO

Dr. M. Hafizur Rahman

Designation: Professor
Department : Biochemistry
Primeasia University
INTRODUCTION
 Metabolism = biotransformation
 Essential pharmacokinetic process which converts lipid soluble and non polar
compounds to water soluble and polar compounds, so that they are easily
excreted.
 Chemical alteration of drug in the body.
Advantages:
 Decrease toxicity
 Reduced lipophilicity
 Increase renal excretion
SITE OF DRUG METABOLISM
 The major site of drug metabolism is the liver ( microsomal enzyme system of hepatocytes ).
 Secondary organ are kidney, plasma ,lungs etc.
Fast pass metabolism:
 Metabolism of a drug before it reaches the systemic circulation.
 The route of administration would be subject to first pass metabolism.
Bioavailability:
 is the fraction of a drug that reaches systemic circulation.
 If the rate of first pass metabolism is increase the rate of bioavailability is decrease.
Outcome of first pass metabolism:
 Active molecule become inactive (pro drug) and it’s a reversible process.
 Toxic become non toxic
PRO DRUG
The inactive drug being active inside the cell.
TYPES OF BIOTRANSFORMATION
Types:
=> Phase 1 :
 A functional group is generated
 Metabolite Active or inactive
=> Phase 1 reactions :
 Oxidation
 Reduction
 Hydrolysis
 Cyclization
 De cyclization
TYPES OF BIOTRANSFORMATION
=> Phase 2 :
 An endogenous radical is conjugated
 Metabolite is usually inactive
=> Phase 2 reactions :
 Glucuronide conjugation
 Acetylation
 Methylation
 Sulfate conjugate
 Glycine conjugate
THANK
YOU