Miller R D, Agoston S, Booij L H, Kersten U W, Crul J F, Ham J
J Pharmacol Exp Ther. 1978 Nov;207(2):539-43.
To determine the potency of pancuronium and its metabolites, 3-OH-, 17-OH- and 3,17-OH-pancuronium, cumulative dose-response curves were determined in five anesthetized patients with each drug. Pancuronium (ED50 = 0.041 mg/kg) was 2 times more potent than 3-OH-pancuronium (ED50 = 0.082 mg/kg), 50 times more potent than 17-OH-pancuronium (ED50 = 2.0 mg/kg) and 54 times more potent than 3,17-OH--pancuronium (ED50 = 2.15 mg/kg). In 21 other patients, one equipotent dose of either pancuronium or one of its metabolites was given as an i.v. bolus. Onset time and duration of neuromuscular blockade from 3-OH- and 3,17-OH-pancuronium did not differ significantly from that of pancuronium; 17-OH-pancuronium had a shorter duration of action than did pancuronium. Although pancuronium tended to have a slightly longer elimination half-life, the pharmacokinetics of the four drugs did not differ significantly. The elimination half-lifes were 110, 68, 73 and 71 min for pancuronium and its 3-OH, 17-OH and 3,17-OH derivatives, respectively. We conclude that although pancuronium is more potent than its 3-OH, 17-OH and 3,17-OH metabolites, the pharmacokinetics of these three metabolites do not differ from each other and from that of pancuronium.
为测定泮库溴铵及其代谢产物3-羟基泮库溴铵、17-羟基泮库溴铵和3,17-二羟基泮库溴铵的效价，对5例麻醉患者分别给予上述每种药物，测定累积剂量-效应曲线。泮库溴铵（ED50 = 0.041 mg/kg）的效价比3-羟基泮库溴铵（ED50 = 0.082 mg/kg）强2倍，比17-羟基泮库溴铵（ED50 = 2.0 mg/kg）强50倍，比3,17-二羟基泮库溴铵（ED50 = 2.15 mg/kg）强54倍。在另外21例患者中，静脉推注给予一剂等效剂量的泮库溴铵或其一种代谢产物。3-羟基泮库溴铵和3,17-二羟基泮库溴铵的神经肌肉阻滞起效时间和持续时间与泮库溴铵相比无显著差异；17-羟基泮库溴铵的作用持续时间比泮库溴铵短。尽管泮库溴铵的消除半衰期往往略长，但这四种药物的药代动力学无显著差异。泮库溴铵及其3-羟基、17-羟基和3,17-二羟基衍生物的消除半衰期分别为110、68、73和71分钟。我们得出结论，尽管泮库溴铵比其3-羟基、17-羟基和3,17-二羟基代谢产物更有效，但这三种代谢产物的药代动力学彼此之间以及与泮库溴铵的药代动力学并无差异。
