TABLE 4

Percentage of circulating metabolites of zoniporide and their estimated exposure in healthy male volunteers, Sprague-Dawley rats, and Beagle dogs after intravenous administration of [14C]zoniporide

Healthy male volunteers were administered [14C]zoniporide by intravenous infusion for 1 h at a dose of 80 mg (100 μCi). The rats were administered a bolus of [14C]zoniporide at a dose of 10 mg/kg (50 μCi). The dogs were administered a bolus of [14C]zoniporide at a dose of 3 mg/kg (150 μCi). The estimated exposures were determined by multiplying percent circulating radioactivitymetabolite and AUC(0–tlast)radioactivity. The AUC(0–tlast)radioactivity is depicted in Table 2.

MetabolitesHumanRatDog
Circulating RadioactivityEstimated AUC(0–tlast)Circulating RadioactivityEstimated AUC(0–tlast)Circulating RadioactivityEstimated AUC(0–tlast)
%ng-Eq-h/ml%ng-Eq-h/ml%ng-Eq-h/ml
M1601755461642
M36.41879.03213.7117
M42.373
M6
M88.53035.4171
M923727
M103.198
Zoniporide30878361285621959