Kárpáti E, Bíró K
Richter Gedeon Vegyészeti Gyár Rt., Budapest.
Acta Pharm Hung. 1992 May;62(3):121-6.
The experimental results in animals suggest that pipecuronium bromide offers the possibility of a neuromuscular blocking agent without side effects for surgical procedures of long duration. Its mechanism of action is twofold: 1. antagonism of acetylcholine effect at neuromuscular junction (postsynaptic nicotine receptors), 2. inhibition of acetylcholine release (presynaptic nicotine receptors). Its neuromuscular blocking potency is somewhat greater (2.0-3.0) than that of pancuronium in all species studied, and the duration of action is twice of that. It has no remarkable cumulative effect. Neostigmine rapidly and completely antagonises the neuromuscular blockade caused by pipecuronium. Certain structural properties (e.g. pipecuronium has no acetylcholine-like fragments in contrast with pancuronium and the interonium distance is also considerably larger than in pancuronium) may predict advantages. This has been proved by low vagal blocking--and ganglion--blocking potencies. On the basis of these a wide margin of safety can be expected in humans as well in preventing cardiovascular side effects. Pipecuronium is also characterized by interactions--only slight interactions--with other drugs used mainly in perioperative period.
动物实验结果表明,哌库溴铵有可能成为一种用于长时间外科手术且无副作用的神经肌肉阻滞剂。其作用机制有两方面:1. 拮抗神经肌肉接头处乙酰胆碱的作用(突触后烟碱受体);2. 抑制乙酰胆碱的释放(突触前烟碱受体)。在所有研究的物种中,其神经肌肉阻滞效能比泮库溴铵略强(2.0 - 3.0),且作用持续时间是泮库溴铵的两倍。它没有明显的蓄积效应。新斯的明能迅速且完全地拮抗哌库溴铵引起的神经肌肉阻滞。某些结构特性(例如,与泮库溴铵相比,哌库溴铵没有类似乙酰胆碱的片段,且离子间距也比泮库溴铵大得多)可能预示着其优势。这已通过低迷走神经阻滞和神经节阻滞效能得到证实。基于这些,预计在人类中预防心血管副作用时也有很大的安全范围。哌库溴铵的另一个特点是,它与主要在围手术期使用的其他药物仅有轻微相互作用。