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肥胖患者中吗啡的药理学:临床意义

Pharmacology of morphine in obese patients: clinical implications.

作者信息

Lloret Linares Célia, Declèves Xavier, Oppert Jean Michel, Basdevant Arnaud, Clement Karine, Bardin Christophe, Scherrmann Jean Michel, Lepine Jean Pierre, Bergmann Jean François, Mouly Stéphane

机构信息

Unit of Therapeutic Research, Department of Internal Medicine, Hôpital Lariboisière, Assistance Publique-Hôpitaux de Paris, Paris, France.

出版信息

Clin Pharmacokinet. 2009;48(10):635-51. doi: 10.2165/11317150-000000000-00000.

Abstract

Morphine is an analgesic drug used to treat acute and chronic pain. Obesity is frequently associated with pain of various origins (e.g. arthritis, fibromyalgia, cancer), which increases the need for analgesic drugs. Obesity changes drug pharmacokinetics, and for certain drugs, specific modalities of prescription have been proposed for obese patients. However, scant data are available regarding the pharmacokinetics and pharmacodynamics of morphine in obesity. Prescription of morphine depends on pain relief but the occurrence of respiratory adverse effects correlates with obesity, and is not currently taken into account. Variations in the volume of distribution, elimination half-life and oral clearance of morphine, as well as recent advances in the respective roles of drug-metabolizing enzymes, catechol-O-methyltransferase and the mu opioid receptor in morphine pharmacokinetics and pharmacodynamics, may contribute to differences between obese and non-obese patients. In addition, drug-drug interactions may alter the disposition of morphine and its glucuronide metabolites, which may either increase the risk of adverse effects or reduce drug efficacy.

摘要

吗啡是一种用于治疗急慢性疼痛的镇痛药。肥胖常与各种原因引起的疼痛(如关节炎、纤维肌痛、癌症)相关,这增加了对镇痛药的需求。肥胖会改变药物的药代动力学,对于某些药物,已针对肥胖患者提出了特定的处方方式。然而,关于肥胖患者中吗啡的药代动力学和药效学的数据却很少。吗啡的处方取决于疼痛缓解情况,但呼吸不良反应的发生与肥胖相关,目前并未将其考虑在内。吗啡的分布容积、消除半衰期和口服清除率的变化,以及药物代谢酶、儿茶酚 - O - 甲基转移酶和μ阿片受体在吗啡药代动力学和药效学中各自作用的最新进展,可能导致肥胖患者与非肥胖患者之间存在差异。此外,药物相互作用可能会改变吗啡及其葡萄糖醛酸代谢物的处置,这可能会增加不良反应的风险或降低药物疗效。

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