Clinical Enteric Neuroscience Translational and Epidemiological Research (C.E.N.T.E.R.), Mayo Clinic, Rochester, MN, USA.
Aliment Pharmacol Ther. 2012 May;35(9):1088-96. doi: 10.1111/j.1365-2036.2012.05040.x. Epub 2012 Feb 21.
Tapentadol is a mu-opioid receptor agonist and norepinephrine reuptake inhibitor. In clinical trials, tapentadol provided somatic pain relief comparable to mu-opioids such as oxycodone, with significantly less gastrointestinal adverse effects. The acute effects of tapentadol on gastrointestinal and colonic transit are unclear.
To compare acute effects of oral tapentadol and oxycodone on gastric, small bowel and colonic transit of solids in 38 healthy human subjects.
In a randomised, parallel-group, double-blind, placebo-controlled study of the effects of identical-appearing tapentadol immediate release (IR), 75 mg t.d.s., or oxycodone IR, 5 mg t.d.s., for 48 h, we measured gastric (GE), small bowel (SBT measured as colonic filling at 6 h) and colonic transit by validated scintigraphy. Drug was commenced on the evening before the start of the transit test. The primary endpoints were overall colonic transit (geometric centre, GC) at 24 h and GE half-time (t1/2 ). ancova of transit data included gender or BMI as covariates. Adverse effects were summarised.
At the doses tested, oxycodone and tapentadol significantly delayed GE t1/2 and SBT, but not overall colonic transit, compared to placebo. Transit profiles in all regions were not significantly different between oxycodone and tapentadol at the doses tested. Both oxycodone and tapentadol were associated with nausea and central effects attributable to central opiate effects.
Tapentadol significantly delayed gastric emptying t1/2 and small bowel transit, similar to oxycodone. These data suggest that acute administration of tapentadol may not have significant advantages over standard mu-opioids, in terms of the potential to avoid upper gastrointestinal motor dysfunction.
曲马多是一种μ-阿片受体激动剂和去甲肾上腺素再摄取抑制剂。在临床试验中，曲马多提供的躯体疼痛缓解作用可与羟考酮等μ-阿片类药物相媲美，而胃肠道不良反应明显较少。曲马多对胃肠道和结肠转运的急性影响尚不清楚。
比较口服曲马多和羟考酮对 38 名健康人体固体胃、小肠和结肠转运的急性影响。
在一项随机、平行组、双盲、安慰剂对照研究中，观察了外观相同的曲马多即时释放（IR）75mg，每日 3 次，或羟考酮 IR，5mg，每日 3 次，共 48 小时，我们通过验证闪烁成像测量胃（GE）、小肠（SBT 测量为 6 小时时的结肠充盈）和结肠转运。药物在转运试验开始前的晚上开始服用。主要终点是 24 小时时的总体结肠转运（几何中心，GC）和 GE 半衰期（t1/2）。包括性别或 BMI 作为协变量的协方差分析用于转运数据。总结不良反应。
在所测试的剂量下，与安慰剂相比，羟考酮和曲马多显著延迟了 GE t1/2 和 SBT，但不延迟整体结肠转运。在测试剂量下，曲马多和羟考酮在所有区域的转运曲线均无显著差异。与标准阿片类药物相比，羟考酮和曲马多都与恶心和中枢作用相关，这些作用归因于中枢阿片类药物的作用。
曲马多显著延迟了胃排空 t1/2 和小肠转运，与羟考酮相似。这些数据表明，与标准μ-阿片类药物相比，曲马多急性给药可能没有明显的优势，在避免上胃肠道运动功能障碍方面可能没有明显优势。
