TABLE 2

Recommended in vivo substrates for P450 induction studies


Probe Substrate to Evaluate NME As an Inducer
P450 Isoform
Substratea
Recommended Dose and Route
CYP1A2 Theophylline, caffeine 200 mg oral
CYP2B6 Bupropion,b efavirenz 150 mg oral
CYP2C8 Rosiglitazone, repaglinide 8 mg oral
CYP2C9 Warfarin, tolbutamide 2 to 5 mg oral
CYP2C19 Omeprazole, esomeprazole, lansoprazole, pantoprazole 20 mg oral
CYP2E1b Chlorzoxazone 500 mg oral
CYP3A4/3A5
Midazolam, buspirone, felodipine, lovastatin, eletriptan, sildenafil, simvastatin, triazolam
10 mg oral
  • a Substrates in bold are preferred substrates.

  • b Assessment of hydroxybupropion exposure.