Enzyme Induction and Inhibition

Enzyme induction and inhibition alter drug metabolism, affecting drug activity, duration, and interactions.

Enzyme Induction:

  • Certain drugs increase the activity of CYP450 enzymes.
  • Leads to faster metabolism of the drug and/or other drugs.
  • Effect: Reduced plasma levels and therapeutic effect.

Examples of Enzyme Inducers:

  • Rifampin
  • Phenobarbital
  • Carbamazepine
  • Phenytoin

Enzyme Inhibition:

  • Some drugs inhibit CYP450 enzymes.
  • Leads to slower metabolism → increased drug levels → possible toxicity.
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Examples of Enzyme Inhibitors:

  • Cimetidine
  • Ketoconazole
  • Erythromycin
  • Grapefruit juice

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