Bioactivity | 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]. |
Target | nAChR |
Invitro | 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]. |
In Vivo | 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]. |
Name | Pipecuronium bromide |
CAS | 52212-02-9 |
Formula | C35H62Br2N4O4 |
Molar Mass | 762.70 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [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]. Töröcsik 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. |