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There Are No Useful CYP3A Probes that Quantitatively Predict the In Vivo Kinetics of Other CYP3A Substrates and No Expectation that One Will Be Found
Table 1.
Comparison of Published Mean Pharmacokinetic1 and Metabolic Pathway2 Parameters for Alprazolam, Midazolam, and Triazolam with Mean Experimental Values3
| Drug | Oral Availability F % | Urinary Excretion % | Clearance ml/min/kg | Vol. Dist. L/kg | Half-Life (hr) | 4-OH Metabolite % | 1′-OH Metabolite % |
|---|---|---|---|---|---|---|---|
| 1 Mean pharmacokinetic parameters were derived from (11). 2 Metabolic pathway parameters were derived from (12, 13). | |||||||
| 3 Mean experimental values as derived from (2) are given in parentheses. | |||||||
| Alprazolam | 88 | 20 | 0.74 | 0.72 | 12 (14) | 20 | 60 |
| Midazolam | 44 (30) | < 1 | 6.6 (5.5) | 1.1 | 1.9 (1.3) | 5 | 95 |
| Triazolam | 44 (55) | 2 | 5.6 (3.2) | 1.1 | 2.9 (2.8) | 49 | 49 |
