Drugs metabolised by cytochrome P450 1A2
Inhibitors of CYP1A2 | ||
Strong ≥ fivefold increase in AUC or >80% decrease in CL | Moderate ≥ twofold but <5 fold increase in AUC or 50% to 80% decrease in CL | Weak ≥1.25 fold but <2 fold increase in AUC or 20% to 50% decrease in CL |
Ciprofloxacin, enoxacin, fluvoxamine | Methoxsalen, mexiletine, oral contraceptives, phenylpropanolamine, thiabendazole, vemurafenib, zileuton | Acyclovir, allopurinol, caffeine, cimetidine, daidzein, disulfiram, echinacea, famotidine, norfloxacin, propafenone, propranolol, terbinafine, ticlopidine, verapamil |
Inducers of CYP1A2 | ||
Strong 80% decrease in AUC | Moderate 50% to 80% decrease in AUC | Weak 20% to 50% decrease in AUC |
Montelukast, phenytoin, smokers vs non-smokers | Moricizine, omeprazole, phenobarbital | |
Substrates of CYP1A2 | ||
Sensitive substrates | Substrates with narrow therapeutic range2 | |
Alosetron, caffeine, duloxetine, melatonin, ramelteon, tacrine, tizanidine | Theophylline, tizanidine, warfarin |
AUC, area under the curve; CL, drug clearance.