TABLE 2

Urinary excretion of midazolam and metabolites (n = 8 subjects)

Geometric Mean (90% Confidence Interval)
ControlTreatmentTreatment/Control
Midazolam
 Ae,0–12h (nmol)7.7 (5.9–10)15 (11–21)*2 (1.3–2.9)
 % of total amount recovered0.14 (0.11–0.18)0.53 (0.34–0.81)*NA
 ClR (l/h)0.12 (0.10–0.15)0.02 (0.02–0.04)*0.2 (0.13–0.31)
Midazolam N-glucuronide
 Ae,0–12h (nmol)53 (43–66)230 (130–400)*4.3 (2.1–8.9)
 % of total amount recovered0.98 (0.78–1.2)8.1 (4.6–14)*NA
 ClR (l/h)13 (6.2–28)4.3 (2.1–8.7)*0.32 (0.14–0.72)
1′-Hydroxymidazolam
 Ae,0–12h (nmol)5.7 (4.7–7.0)NQNA
 % of total amount recovered0.11 (0.09–0.13)NQNA
 ClR (l/h)0.2 (0.14–0.27)NQNA
Midazolam 1′-O-glucuronide
 Ae,0–12h (nmol)5400 (5100–5700)2600 (2100–3100)*0.48 (0.39–0.59)
 % of total amount recovered99 (98–99)89 (86–93)*NA
 ClR (l/h)13 (11–15)14 (12–17)1.1 (0.82–1.5)
Total amount recovered (nmol)5400 (5200–5700)2856 (2400–3400)0.53 (0.43–0.64)
  • Ae,0–12h, amount recovered over 12 hours postdose; ClR, renal clearance; NA, not applicable; NQ, not quantifiable.

  • * P < 0.05 compared with control group.