Inhibitor | Elimination of Buprenorphine | Formation of | ||||||
---|---|---|---|---|---|---|---|---|
Norbuprenorphine | M1 | M3 | M5 | |||||
% inhibition | ||||||||
A. HLM 452013: higher 2C8, lower 3A4/5 | ||||||||
Anti-3A4/5 | 12 | 7 | 14 | 74 | 87 | |||
Anti-2C8 | 77 | 83 | 67 | 14 | 12 | |||
Ketoconazole | 18 | 14 | 4 | 89 | 100 | |||
Trimethoprim | 28 | 32 | 14 | 38 | 0 | |||
B. HLM 452164: lower 2C8, higher 3A4/5 | ||||||||
Anti-3A4/5 | 76 | 60 | 48 | 95 | 94 | |||
Anti-2C8 | 3 | 18 | 18 | 0 | 0 | |||
Ketoconazole | 77 | 59 | 48 | 95 | 90 | |||
Trimethoprim | 7 | 13 | 16 | 38 | 7 |