Midazolam | | |
AUC0–12h (nM × h) | 63.5 (51.3–78.5) | 614 (499–756)* | 9.7 (7.6–12.3) |
Cmax (nM) | 23.2 (18.9–28.5) | 128 (108–153)* | 5.5 (4.3–7.1) |
t1/2 (h) | 2.96 (2.22–3.95) | 5.72 (4.75–6.89)* | NC |
tmax (h)a | 1.0 (0.5–1.0) | 1.0 (0.5–2.0) | NC |
Cl/F (l/h) | 113 (90.4–141) | 6.69 (4.42–10.1)* | 0.06 (0.04–0.09) |
Midazolam N-glucuronide | | |
AUC0–12h (nM × h) | 4.02 (1. 57–10.3) | 54.4 (42.2–70.3)* | 13.5 (5.8–32) |
Metabolic ratiob | 0.063 (0.027–0.15) | 0.088 (0.072–0.11) | 1.40 (0.72–2.73) |
Cmax (nM) | 1.31 (0.89–1.92) | 6.81 (5.18–8.94)* | 5.2 (4.0–6.8) |
t1/2 (h) | 5.35 (3.09–9.26) | NA | NC |
tmax (h)a | 4.0 (3.0–6.0) | 6.0 (4.0–10.0)* | NC |
1′-Hydroxymidazolam | | | |
AUC0–12h (nM × h) | 29.3 (22.0–39.0) | 13.5 (11.2–16.1)* | 0.46 (0.31–0.69) |
Metabolic ratiob | 0.46 (0.38–0.55) | 0.022 (0.016–0.030)* | 0.05 (0.03–0.07) |
Cmax (nM) | 11.1 (8.94–13.7) | 2.31 (1.90–2.81)* | 0.21 (0.14–0.30) |
t1/2 (h) | 2.05 (1.44–2.92) | NA | NC |
tmax (h)a | 1.0 (0.5–1.0) | 5.0 (2.0–6.0)* | NC |
Midazolam 1′-O-glucuronide | | |
AUC0–12h (nM × h) | 415 (362–475) | 180 (155–210)* | 0.43 (0.33–0.57) |
Metabolic ratiob | 6.53 (5.69–7.53) | 0.29 (0.21–0.41)* | 0.045 (0.032–0.064) |
Cmax (nM) | 163 (146–181) | 26.5 (21.2–33.0)* | 0.16 (0.12–0.21) |
t1/2 (h) | 3.58 (2.88–4.43) | NA | NC |
tmax (h)a | 1.0 (0.5–1.0) | 5.0 (2.0–6.0)* | NC |