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Metabolism => Termination of Drug Action – Bioinactivation -and/or- – Detoxification -and/or-

Importance of Drug Metabolism. Metabolism => Termination of Drug Action – Bioinactivation -and/or- – Detoxification -and/or- – Elimination -and/or-. Glutathion and mercapturic acid synthesis.

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Metabolism => Termination of Drug Action – Bioinactivation -and/or- – Detoxification -and/or-

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  1. Importance of Drug Metabolism Metabolism => Termination of Drug Action – Bioinactivation -and/or- – Detoxification -and/or- – Elimination -and/or-

  2. Glutathion and mercapturic acid synthesis • Glutathion (GSH) is a thiol-containing tripeptide of great significance in the detoxification and toxification of drugs and other xenobiotics. • GSH conjugation is an important pathway by which chemical reactive electrophilic compounds are detoxified. • GSH protect vital cellular constituents against chemically reactive species by its nucleophilic sulfhydryl (SH) group.

  3. SH group reacts with electron-deficient compounds to form S-substituted GSH adducts. • Conjugation with glutathione (GSH) is catalyzed by glutathione S-transferases. • Degradation of GSH conjugates to mercapturic acids is carried by microsomal enzymes.

  4. Examples

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