In vitro degradation of atracurium in human plasma.
In vitro degradation of atracurium in human plasma.
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人血浆中阿曲库铵的体外降解。
DOI：
10.1093/bja/57.11.1085
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发表时间：
1985
影响因子：
9.8
通讯作者：
Chakravorti,S
中科院分区：
文献类型：
--
作者：
Stiller,RL;Cook,DR;Chakravorti,S
在Sorensen缓冲液和人血浆中，采用灵敏、特异的高压液相色谱法测定药物浓度，体外检测阿曲库铵的降解和劳丹诺新的形成。在正常生理pH和温度下，阿曲库铵在血浆中的降解速度是在缓冲液中的三倍。劳达新是阿曲库铵在缓冲液或血浆中降解的主要终产物;其在血浆中的产生比在缓冲液中更快。稀释血浆成分或使用二异丙基氟磷酸盐（一种强效酯酶抑制剂）可减缓阿曲库铵的降解和劳丹诺新的产生。我们的结论是，虽然酯水解是阿曲库铵降解的主要代谢途径。霍夫曼消除法在临床应用中提供了一个“安全网”。
The degradation of atracurium and the formation of laudanosine was examinedin vitroin both Sorensen buffer and human plasma using sensitive, specific high pressure liquid chromato-graphic assays to determine drug concentrations. At normal physiological pH and temperature, the degradation of atracurium was threefold more rapid in plasma than in buffer. Laudanosine is the major end-product of atracurium degradation in buffer or in plasma; its production is more rapid in plasma than in buffer. Dilution of plasma constituents or the use of diisopropylfluorophosphate (a potent esterase inhibitor), slows the degradation of atracurium and the production of laudanosine. We conclude that, although ester hydrolysis is the major metabolic pathway of atracurium degradation. Hofmann elimination provides a “safety net” in its clinical use.