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维库溴铵抑制组胺N-甲基转移酶。

Vecuronium inhibits histamine N-methyltransferase.

作者信息

Futo J, Kupferberg J P, Moss J, Fahey M R, Cannon J E, Miller R D

机构信息

Department of Anesthesia and Critical Care, University of Chicago, Illinois 60637.

出版信息

Anesthesiology. 1988 Jul;69(1):92-6. doi: 10.1097/00000542-198807000-00014.

Abstract

Although there have been clinical reports of significant hypotension and flushing associated with the use of vecuronium, it produces minimal cardiovascular effects in the vast majority of patients. In addition, there is no evidence that vecuronium stimulates the release of histamine. The authors performed in vitro kinetic studies to determine the effect of vecuronium on histamine N-methyltransferase (HNMT), the primary catabolic enzyme for histamine in humans. They also examined plasma from patients who had received vecuronium (0.1 or 0.2 mg/kg) to determine whether clinically used concentrations of the drug could inhibit HNMT. It was determined that vecuronium is a strong inhibitor of HNMT; apparent Ki = 1 microM. The inhibition is competitive with respect to methyl-donor and noncompetitive with respect to histamine. Vecuronium, in doses greater than or equal to 0.1 mg/kg, may delay the metabolism of histamine by HNMT in vitro.

摘要

尽管有临床报告称使用维库溴铵会出现显著低血压和潮红,但在绝大多数患者中它对心血管系统的影响极小。此外,没有证据表明维库溴铵会刺激组胺释放。作者进行了体外动力学研究,以确定维库溴铵对组胺N -甲基转移酶(HNMT)的影响,HNMT是人体内组胺的主要分解代谢酶。他们还检测了接受维库溴铵(0.1或0.2 mg/kg)患者的血浆,以确定该药物的临床使用浓度是否能抑制HNMT。结果确定维库溴铵是HNMT的强效抑制剂;表观抑制常数(Ki)= 1微摩尔。这种抑制作用对甲基供体而言是竞争性的,对组胺而言是非竞争性的。在体外,剂量大于或等于0.1 mg/kg的维库溴铵可能会延迟HNMT对组胺的代谢。

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