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健康志愿者体内吗啡-6-葡萄糖醛酸苷和吗啡的处置情况。

Disposition of morphine-6-glucuronide and morphine in healthy volunteers.

作者信息

Hanna M H, Peat S J, Knibb A A, Fung C

机构信息

Pain Relief Research Unit, Kings College Hospital, School of Medicine and Dentistry, London.

出版信息

Br J Anaesth. 1991 Jan;66(1):103-7. doi: 10.1093/bja/66.1.103.

DOI:10.1093/bja/66.1.103
PMID:1997044
Abstract

The pharmacokinetics and subjective side effects of i.v. morphine sulphate 120 micrograms kg-1 and morphine-6-glucuronide (M6G) 30 micrograms kg-1 were determined in six healthy volunteers, using a placebo-controlled, single-blind randomized crossover design. Five of these volunteers underwent an additional (non-randomized) study of M6G 60 micrograms kg-1. Subjective side effects were similar following both drugs, but of shorter duration following M6G. Morphine was not detected after administration of M6G. For M6G 30 micrograms kg-1 the mean (SD) volume of distribution, elimination half-life and clearance were 29.38 (18.36) litre, 2.05 (1.2) h and 187.81 (37.41) litre h-1, respectively. These values were not significantly different from those obtained for M6G 60 micrograms kg-1. In all subjects the volumes of distribution and clearances were significantly smaller for M6G than for morphine, but the elimination half-lives were similar.

摘要

采用安慰剂对照、单盲随机交叉设计,在6名健康志愿者中测定了静脉注射120微克/千克硫酸吗啡和30微克/千克吗啡-6-葡萄糖醛酸苷(M6G)的药代动力学及主观副作用。其中5名志愿者还接受了一项额外的(非随机)60微克/千克M6G的研究。两种药物后的主观副作用相似,但M6G后的持续时间较短。给予M6G后未检测到吗啡。对于30微克/千克的M6G,平均(标准差)分布容积、消除半衰期和清除率分别为29.38(18.36)升、2.05(1.2)小时和187.81(37.41)升/小时。这些值与60微克/千克M6G获得的值无显著差异。在所有受试者中,M6G的分布容积和清除率均显著低于吗啡,但消除半衰期相似。

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