Rocuronium Bromide

A non-depolarizing muscle relaxant

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Background

Rocuronium Bromide (ORG 9426 Bromide) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal musclerelaxation during surgery or mechanical ventilation.

Rocuronium reduced the indirectly elicited twitch tensions in normal (50% inhibitory concentration [IC(50)], 9.84 [9.64-10.04] μM, mean [95% confidence interval]) and all pretreated diaphragms (P < .01, n = 6) in a concentration-dependent fashion [1]. The ED95 of rocuronium is essentially the same for children as for adults. Its duration of action is similar to vecuronium, and it is shorter for children than for adults. Rocuronium is readily reversed with conventional doses of cholinesterase-inhibiting drugs [2]. Onset time until maximum block, duration until 25% recovery of twitch height, and recovery from 25 until 75% of twitch height were 1.7 (32), 53 (19) and 20 (37) min, respectively [3].

Only 8.7±5.7% (SD) and 6.0±2.8% of an injected dose of ORG 9426 and ORG 9616 was excreted into the urine, respectively. Conversely, 54.4±9.2% and 52.4±9.2% of an injected dose of ORG 9426 and 35.7±12.2% and 46.8±9.7% of ORG 9616 were excreted into the bile in cats without and with renal pedicle ligation, respectively [4].

参考文献:
[1]. Narimatsu E, Niiya T, Takahashi K, Pralidoxime inhibits paraoxon-induced depression of rocuronium-neuromuscular block in a time-dependentfashion. Am J Emerg Med. 2012 Jul;30(6):901-7.
[2]. Wicks TC. The pharmacology of rocuronium bromide (ORG 9426). AANA J. 1994 Feb;62(1):33-8.
[3]. Wierda JM, Kleef UW, Lambalk LM, The pharmacodynamics and pharmacokinetics of Org 9426, a new non-depolarizing neuromuscular blocking agent, in patients anaesthetized with nitrous oxide, halothane and fentanyl. Can J Anaesth. 1991 May;38(4 Pt 1):430-5.
[4]. Khuenl-Brady K, Castagnoli KP, Canfell PC, The neuromuscular blocking effects and pharmacokinetics of ORG 9426 and ORG 9616 in the cat. Anesthesiology. 1990 Apr;72(4):669-74.