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安乃近的药理学及相关药物相互作用

Pharmacology and relevant drug interactions of metamizole.

作者信息

Brinkman David J, Hendriksen Linda C, Rigter Irma M, Hollmann Markus W

机构信息

Department of Anaesthesiology, Amsterdam UMC, Amsterdam, Netherlands.

Department of Internal Medicine, Pharmacotherapy Unit, Amsterdam UMC, Amsterdam, Netherlands.

出版信息

Br J Clin Pharmacol. 2025 Jul;91(7):2095-2102. doi: 10.1002/bcp.70101. Epub 2025 May 15.

Abstract

Metamizole is a frequently prescribed analgesic because of its favourable benefit/risk ratio compared with classic NSAIDs. However, increasing research shows that metamizole displays several drug interactions that are relevant to clinical practice. We reviewed the literature to summarize the pharmacology and most clinically relevant drug interactions of metamizole. Metamizole has a fast analgesic effect but a short half-life and duration of action. The exact mechanism of action of metamizole is currently not fully known. Studies showed that metamizole appears to be a moderate to strong inductor of the enzymes CYP3A4, CYP2B6 and CYP2C19; a weak inductor of CYP2C9; and a moderate inhibitor of CYP1A2. Furthermore, metamizole inhibits the effect of acetylsalicylic acid when taken simultaneously. Metamizole should be cautiously used together with other drugs that can cause agranulocytosis. If metamizole is prescribed in a high dosage (1000 mg three or four times daily) for more than 1 day, these pharmacokinetic and dynamic interactions should be taken into account.

摘要

与传统非甾体抗炎药相比,由于其良好的效益/风险比,安乃近是一种常用的镇痛药。然而,越来越多的研究表明,安乃近存在几种与临床实践相关的药物相互作用。我们回顾了文献,以总结安乃近的药理学及最与临床相关的药物相互作用。安乃近具有快速镇痛作用,但半衰期和作用持续时间较短。安乃近的确切作用机制目前尚不完全清楚。研究表明,安乃近似乎是细胞色素P450 3A4(CYP3A4)、细胞色素P450 2B6(CYP2B6)和细胞色素P450 2C19(CYP2C19)酶的中度至强诱导剂;细胞色素P450 2C9(CYP2C9)的弱诱导剂;以及细胞色素P450 1A2(CYP1A2)的中度抑制剂。此外,同时服用时,安乃近会抑制阿司匹林的作用。安乃近应谨慎与其他可导致粒细胞缺乏症的药物合用。如果安乃近以高剂量(每日三四次,每次1000毫克)给药超过1天,则应考虑这些药代动力学和药效学相互作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d9ec/12199094/f5dc1fc3cbf6/BCP-91-2095-g001.jpg

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