Table 1

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, fluvoxamineMethoxsalen, mexiletine, oral contraceptives, phenylpropanolamine, thiabendazole, vemurafenib, zileutonAcyclovir, 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-smokersMoricizine, omeprazole, phenobarbital
Substrates of CYP1A2
Sensitive substratesSubstrates with narrow therapeutic range2
Alosetron, caffeine, duloxetine, melatonin, ramelteon, tacrine, tizanidineTheophylline, tizanidine, warfarin
  • AUC, area under the curve; CL, drug clearance.