Buzello W, Agoston S
Anaesthesist. 1978 Jun;27(6):291-7.
Plasma concentration curves of patients with normal and impaired renal function are fitted to a tri-exponential function according to an open three compartment pharmacokinetic model. A detailed discussion of the relationship between theoretical distribution volumes, clinical pharmacodynamics and morphological or biochemical structures provides the basis for the concept of a central application and measuring compartment, a pharmacologically specific compartment and a non specific one. The distirbution of pancuronium from the application compartment to the specific compartment results in the onset of muscular paralysis. The recovery is governed by renal elimination of the unchanged drug as well as by its redistribution into the non specific compartment. In anuric patients the spontaneous recovery after 3--4 h is the effect of redistribution only. Neither metabolic degradation nor increased biliary elimination can sufficiently compensate for the lack of the renal pathway. The clinician should always keep in mind that after the recovery from pancuronium-induced muscular paralysis, both in patients with or without renal pathology, considerable residues of the active drug are stored at nonspecific and even specific receptor sites for many hours.
根据开放三室药代动力学模型,将肾功能正常和受损患者的血浆浓度曲线拟合为三指数函数。对理论分布容积、临床药效学与形态学或生化结构之间关系的详细讨论,为中央应用和测量隔室、药理特异性隔室和非特异性隔室概念提供了基础。泮库溴铵从给药隔室向特异性隔室的分布导致肌肉麻痹的开始。恢复过程受未变化药物的肾脏消除以及其重新分布到非特异性隔室的控制。在无尿患者中,3 - 4小时后的自发恢复仅是重新分布的结果。代谢降解和胆汁消除增加均不能充分弥补肾脏途径的缺失。临床医生应始终牢记,在泮库溴铵引起的肌肉麻痹恢复后,无论有无肾脏病变的患者,活性药物的相当一部分残留物会在非特异性甚至特异性受体部位储存数小时。