Pipecuronium bromide

Pipecuronium bromide 是一种有效的长效非去极化甾体神经肌肉阻滞剂 (NMBA)，是一种双季铵化合物。Pipecuronium bromide 是一种功能强大的竞争性 nAChR 拮抗剂，Kd 为 3.06 μM。

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Background

Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM[1][2][3][4][5].

Sugammadex has a high affinity for Pipecuronium bromide. As Pipecuronium bromide is about 6 to 7 times more potent than Rocuronium, fewer molecules are required to achieve a comparative blockade than in the case of Rocuronium[1].

The average ED95 is 0.045mg/kg (0.035-0.059 mg/kg) of Pipecuronium bromide, the onset of action varies between 2 and 6.3 minutes, depending on the dose and the background anesthesia. Pipecuronium bromide does not liberate histamine, it has no cardiovascular side effects even in doses of 3× ED95, and anaphylaxis does not appear to be a problem[2].Carboxymethylated γ-cyclodextrin shows efficient and complete reversal of the Pipecuronium bromide induced neuromuscular block in an ex vivo rat diaphragm experiment[3].

[1]. Tassonyi E, et al. Reversal of Pipecuronium-Induced Moderate Neuromuscular Block with Sugammadex in the Presence of a Sevoflurane Anesthetic: A Randomized Trial. Anesth Analg. 2015 Aug;121(2):373-80. [2]. Tassonyi E, et al. Reversal of Deep Pipecuronium-Induced Neuromuscular Block With Moderate Versus Standard Dose of Sugammadex: A Randomized, Double-Blind, Noninferiority Trial. Anesth Analg. 2018 Dec;127(6):1344-1350. [3]. Alánt O, et al. First clinical experience with a new neuromuscular blocker pipecurium bromide. Arzneimittelforschung. 1980;30(2a):374-9. [4]. T?r?csik A, et al. Characterization of somatodendritic neuronal nicotinic receptors located on the myenteric plexus. Eur J Pharmacol. 1991 Sep 24;202(3):297-302. [5]. Kárpáti E, et al. Investigation of neuromuscular blocking agents at Richter Ltd. Acta Pharm Hung. 2002;72(1):37-48.