新的神经肌肉阻断剂:他们如何与代理商建立?

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波弗特TM, Sparr HJ Fuchs-Buder T

新的神经肌肉阻断剂:他们如何与代理商建立?

药。2001;61 (7):919 - 42。

PubMed ID

11434449 (在PubMed

]

文摘

Rapacuronium溴化(Rapacuronium;org - 9487)是一个nondepolarising肌肉松弛剂(NMBA)效力较低(90%有效剂量(ED90) 1毫克/公斤),在某种程度上负责其迅速开始行动。因为等离子体间隙高(5.3 - 11.1毫克/公斤/分钟)rapacuronium,其临床作用持续时间后单剂量2毫克/公斤成人是短暂的(例如< 20分钟)。Rapacuronium形成药物活性3-desacetyl代谢物,组织- 9488,这可能导致延迟重复剂量或注入后自然痊愈。rapacuronium 1.5毫克/公斤后临床可接受的患者条件达到60至90秒内大多数成人和老年病人择期麻醉。然而,在快速设置。患者条件不佳后rapacuronium比琥珀酰胆碱后1.5 - 2.5毫克/公斤。rapacuronium最突出的不利影响(心动过速、低血压和支气管痉挛)剂量相关,特别是肺不利影响是更频繁地观察条件下快速感应的成年人。因此,它似乎值得只考虑剂量的rapacuronium <或= 1.5毫克/公斤,以方便快速气管插管,并使用琥珀酰胆碱或rocuronium而不是rapacuronium快速设置。Rapacuronium,然而,是一个合适的替代氯化mivacurium (mivacurium)和琥珀酰胆碱短程序(例如动态麻醉)。 Rocuronium bromide (rocuronium) is a relatively low-potent, intermediateacting NMBA. Its main advantage is the rapid onset of neuromuscular block whereby good or excellent intubating conditions are achieved within 60 to 90 seconds after rocuronium 0.6 mg/kg (2 x ED95), and within 60 to 180 seconds after smaller doses (1 to 1.5 x ED95). Larger doses of rocuronium (> or = 1 mg/kg) seem to be suitable for rapid-sequence induction under relatively light anaesthesia. However, it is still a matter of controversy whether, in the case of an unanticipated difficult intubation, the long duration of rocuronium administered in such large doses outweighs the many adverse effects of succinylcholine. Rocuronium has mild vagolytic effects and does not release histamine, even when administered in large doses. Rocuronium is primarily eliminated via the liver and its pharmacokinetic profile is similar to that of vecuronium bromide (vecuronium). Unlike vecuronium, rocuronium has no metabolite. Cisatracurium besilate (cisatracurium), the IR-cis, 1'R-cis isomer of atracurium besilate (atracurium) is approximately 4 times more potent than atracurium. The onset time of cisatracurium is significantly slower than after equipotent doses of atracurium. The recommended intubating dose is 0.15 to 0.2 mg/kg (3 to 4 times ED95). Over a wide range of clinically relevant doses the recovery properties of cisatracurium are affected by neither the size of the bolus dose nor by the duration of infusion. Unlike atracurium, cisatracurium does not trigger histamine release. Like atracurium, cisatracurium undergoes Hofmann elimination. In contrast to atracurium, cisatracurium does not undergo hydrolysis by nonspecific plasma esterases. Moreover, about 77% of the drug is cleared by organ-dependent mechanisms.

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药物

Rocuronium