Naloxone as part of a prolonged release oxycodone/naloxone combination reduces oxycodone-induced slowing of gastrointestinal transit in healthy volunteers

羟考酮 (+)-纳洛酮 安慰剂 医学 麻醉 药理学 吗啡 类阿片 内科学 病理 受体 替代医学
作者
Kevin J. Smith,Michael Hopp,Gill Mundin,Simon Bond,Paul Bailey,Jo Woodward,Karuppan Palaniappan,Ann Church,Marie C. Limb,Alyson Connor
出处
期刊:Expert Opinion on Investigational Drugs [Informa]
卷期号:20 (4): 427-439 被引量:53
标识
DOI:10.1517/13543784.2011.563236
摘要

This exploratory study in healthy volunteers investigated the effect of single doses of oxycodone on gastrointestinal (GI) transit time and the degree to which a single dose of naloxone reverses the oxycodone-induced effect.Fifteen healthy male volunteers received: oxycodone 10 and2 0 mg, oxycodone/naloxone 10/5 and 20/10 mg (all as prolonged release tablets) and placebo. Each dose was radiolabelled and administered with a capsule containing radiolabelled resin (surrogate for GI contents).Scintigraphic analysis showed that 20 mg oxycodone significantly increased colon arrival time (mean 7.19 vs 5.15 h for placebo, p = 0.0159). Mean colon arrival time for oxycodone/naloxone 20/10 mg (5.16 h) was similar to placebo, although the difference between oxycodone/naloxone 20/10 mg versus oxycodone 20 mg was not significant (p = 0.0653). Colonic geometric centre analysis showed a significant increase in mean time for the resin to reach the colon following oxycodone 10 and 20 mg compared with placebo (increases of 5.3 and 8.8 h). There was no significant effect of naloxone at the lower dose; however, oxycodone/naloxone 20/10 mg significantly reduced mean colonic transit time by 2.1 h (p = 0.0376).A single dose of oxycodone 20 mg significantly prolonged GI transit time but this effect was reduced by co-administration of naloxone.
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