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Drug Metabolism

  • Drug metabolism involves the biochemical modification of drugs, primarily through enzymatic processes, to facilitate their excretion from the body.

A.Biotransformation

Drugs can undergo transformation through various pathways, resulting in:

  • Inactive Compounds: Metabolites ready for excretion.

  • Active Metabolites: Compounds with their own therapeutic or toxic effects.

  • Prodrugs: Inactive forms that become active only after metabolic conversion.

B.Metabolic Pathways

  1. Cytochrome P450 Enzymes

    • A key family of enzymes involved in drug metabolism. Individual variability in these enzymes can significantly influence drug response.

  2. Phase I Reactions

    • Involve oxidation, reduction, or hydrolysis to increase polarity of the compound, preparing it for further modification or excretion.

  3. Phase II Reactions

    • Conjugation of Phase I metabolites with larger molecules (e.g., glucuronic acid), making them more water-soluble for easier excretion.

C.Metabolite Profiling in Drug Metabolism

  • Techniques such as mass spectrometry help in identifying and quantifying drug metabolites, aiding in the prediction of potential drug interactions and side effects.

  • Drug metabolism is crucial in determining a drug’s duration of action, potential interactions, and side effects, all of which influence therapeutic effectiveness and safety.


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