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Introduction
Enzymatic conversion of one chemical compound to another is called drug metabolism
Aim :Make drug water soluble
Mostly in liver (importance)
Phases of drug metabolismPhase I:
Non-synthetic reactions such as cleavage
e.g. oxidation, reduction, hydrolysis
Formation or modification of a function group.
More hydrophilic molecules are produces
Phase II
Synthetic reactions such as conjugation with an endogenous substance
e.g. sulfate, glycine, glucuronicacid
More lipophobic molecules are produced
Hydrolysis
Introduce water molecule
For phase II
Esters,amides,hydrazides and carbamates are hydrolysed
Opposite to oxidation and reduction
Takes a water molecule to cleave the drug
Enzymes also found in kidney,intestine,plasma,etc
Drugs : cholinesters,procaine,procainamide.
Atropine = tropine + tropic acid
Cocaine = benzoic acid + ecgoninemethyl ester.
Procaine = p-amino acid (PABA) + diethyl amino ethanol.
Acetylcholine = acetic acid + choline.
Reaction R-COO-R' + H2O ⇒ R-COOH + R'-OH
R-CO-NH-R' + H2O ⇒ R-COOH + R'-NH2
Examples:cocaine to benzoylecognine
ecognine methyl ester
References
https://youtu.be/ztsBn8gsfHw
https://www.news-medical.net/amp/health/Drug-Metabolism.aspx
https://www.slideshare.net/suniu/drug-metabolism-16091624
https://www.unaab.edu.ng/attachments/484_PRINCIPLES%20OF%20DRUG%20METABOLISM%201Dr%20Saba.pdf