Pharmacology · Pathway 2
P450 Enzyme System
Key points
- Cytochrome P450: family of enzymes mainly in the liver, responsible for phase I metabolism; CYP3A4 and CYP2D6 are the most clinically important isoforms.
- Inducers (faster metabolism, ↓ drug effect): Rifampicin, Phenytoin, Carbamazepine, Phenobarbitone, Chronic alcohol, St John's Wort, Smoking (CYP1A2).
- Inhibitors (slower metabolism, ↑ drug effect/toxicity): Sodium valproate, Erythromycin/clarithromycin, Azole antifungals, Ciprofloxacin, Grapefruit juice, Acute alcohol, Omeprazole.
- Grapefruit juice inhibits intestinal CYP3A4 → ↑ levels of statins, CCBs, some benzodiazepines.
- Key interactions: P450 inhibitors ↑ warfarin effect; inducers ↓ warfarin effect and can cause contraceptive pill failure.
Decision points in this pathway
- Co-prescribed drug is an inhibitor or inducer?
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