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口服硫酸吗啡缓释片在志愿者体内的药代动力学及镇痛效果

Pharmacokinetics and analgesic effect of slow-release oral morphine sulphate in volunteers.

作者信息

Vater M, Smith G, Aherne G W, Aitkenhead A R

出版信息

Br J Anaesth. 1984 Aug;56(8):821-7. doi: 10.1093/bja/56.8.821.

Abstract

Sustained-release oral morphine sulphate (MST) 20 mg was administered to 11 healthy volunteers. Mean peak plasma morphine concentration was 14.8 ng ml-1, and occurred at a mean time of 142.5 min after ingestion. Analgesia assessed by an ischaemic forearm pain test increased to a maximum approximately 40 min after the calculated peak plasma concentration of morphine had been achieved, and remained greater than control values as plasma morphine concentration decayed. However, there was not a significant correlation between analgesia and plasma morphine concentration. This may result from delay in brain penetration by morphine. The mean systemic availability of morphine in the first 7 h after administration of MST was 18.3%.

摘要

对11名健康志愿者给予20毫克缓释口服硫酸吗啡(美施康定)。血浆吗啡平均峰值浓度为14.8纳克/毫升,在摄入后平均142.5分钟出现。通过缺血性前臂疼痛试验评估的镇痛效果在计算出的吗啡血浆峰值浓度达到后约40分钟增加到最大值,并在血浆吗啡浓度下降时仍高于对照值。然而,镇痛效果与血浆吗啡浓度之间没有显著相关性。这可能是由于吗啡进入大脑存在延迟。给予美施康定后最初7小时内吗啡的平均全身利用率为18.3%。

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