- Drug metabolism is the chemical transformation of pharmaceuticals, primarily in the liver, converting lipophilic compounds into water-soluble metabolites for easier excretion.
Key Goals of Drug Metabolism
- Detoxification: Converts toxic compounds into less harmful forms.
- Excretion: Enhances drug elimination via urine or bile.
- Regulation of Drug Activity: Activates prodrugs or inactivates drugs, influencing their effect.
Enzymatic Systems
- Cytochrome P450 (CYP450): Key enzymes in Phase I oxidation reactions.
- Conjugative Enzymes: UGTs and sulfotransferases mediate Phase II reactions.
Clinical Relevance
- Drug Interactions: Enzyme inhibition/induction affects drug levels.
- Genetic Polymorphisms: Variations impact metabolism, efficacy, and toxicity.
- First-Pass Metabolism: Liver metabolism of oral drugs reduces bioavailability.
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