Lindberg R, Sellman R, Iisalo E
Eur J Drug Metab Pharmacokinet. 1985 Jan-Mar;10(1):21-5. doi: 10.1007/BF03189693.
Nomifensine (1 and 5 mg/kg) was administered to dogs orally and intravenously. The pharmacokinetics of the drug was evaluated. Nomifensine was rapidly absorbed from the gastro-intestinal tract reaching maximum concentration at 0.5-1 h. The peak levels were directly proportional to the doses administered. The elimination half-life was 6 h and only very small amounts were found in blood at 24 h after administration. The apparent volume of distribution (Vd) was 120-149 1, suggesting an extensive distribution of the drug throughout body fluids and tissues. The area under the serum concentration-time curve (AUC) obtained after oral administration was significantly smaller than that after intravenous administration indicating incomplete bioavailability of the drug in oral form. The conjugation of nomifensine after the two different administration routes was also studied: the conjugation reaction was in equilibrium at 15 min after oral administration, while after intravenous administration, equilibrium was not reached until 1-1.5 h. The metabolism of nomifensine occurred in the gastrointestinal membranes and or in the liver during the absorption process; the first-pass effect was marked.
将诺米芬辛（1毫克/千克和5毫克/千克）经口和静脉注射给予犬类。对该药物的药代动力学进行了评估。诺米芬辛从胃肠道迅速吸收，在0.5 - 1小时达到最高浓度。峰值水平与给药剂量成正比。消除半衰期为6小时，给药后24小时血液中仅发现极少量药物。表观分布容积（Vd）为120 - 149升，表明该药物在全身体液和组织中广泛分布。口服给药后获得的血清浓度 - 时间曲线下面积（AUC）显著小于静脉给药后的AUC，表明该药物口服剂型的生物利用度不完全。还研究了两种不同给药途径后诺米芬辛的结合情况：口服给药后15分钟结合反应达到平衡，而静脉给药后，直到1 - 1.5小时才达到平衡。诺米芬辛的代谢在吸收过程中发生于胃肠道膜或肝脏；首过效应明显。
