Roge J, Baumer P, Berard H, Schwartz J C, Lecomte J M
Policlinic, Kremlin Bicêtre University Hospital Centre, Paris, France.
Scand J Gastroenterol. 1993 Apr;28(4):352-4. doi: 10.3109/00365529309090255.
The antidiarrhoeal properties of acetorphan, an inhibitor of enkephalinase (EC 3.4.24.11) that prevents endogenous enkephalin degradation, and loperamide, a mu opiate receptor agonist, were compared. The double-blind study included 69 patients with acute diarrhoea of presumed infectious origin, allocated at random to two parallel groups. Acetorphan and loperamide were both rapidly and similarly effective, diarrhoea resolving in both cases in nearly 2 days. With acetorphan, however, abdominal distension vanished significantly more rapidly, and reactive constipation was less frequent (8% versus 31% with loperamide). These differences can be accounted for by the distinct mechanisms of antidiarrhoeal activity of the two drugs--that is, primary antitransit effect for loperamide and antisecretory activity for acetorphan.
比较了乙酰氧肟酸（一种脑啡肽酶抑制剂，可防止内源性脑啡肽降解）和洛哌丁胺（一种μ阿片受体激动剂）的止泻特性。这项双盲研究纳入了69例推测为感染性病因的急性腹泻患者，随机分为两个平行组。乙酰氧肟酸和洛哌丁胺的起效都很快且效果相似，两种药物治疗的患者腹泻均在近2天内缓解。然而，使用乙酰氧肟酸时，腹胀消失得明显更快，且反应性便秘的发生率更低（分别为8%和洛哌丁胺组的31%）。这些差异可由两种药物不同的止泻活性机制来解释，即洛哌丁胺主要是抗转运作用，而乙酰氧肟酸是抗分泌活性。
