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洛哌丁胺:其药理学特性及对腹泻治疗效果的综述

Loperamide: a review of its pharmacological properties and therapeutic efficacy in diarrhoea.

作者信息

Heel R C, Brogden R N, Speight T M, Avery G S

出版信息

Drugs. 1978 Jan;15(1):33-52. doi: 10.2165/00003495-197815010-00003.

Abstract

Loperamide, a butyramide derivative is a new agent for use in symptomatic control of acute non-specific diarrhoea and chronic diarrhoea. Unlike diphenoxylate or codeine, loperamide does not appear to exert opiate activity in man at normal therapeutic doses. In acute diarrhoea, loperamide provides more rapid control of symptoms than diphenoxylate when given in a flexible dosage according to unformed bowel movements, and in single dose studies 4mg loperamide has a much longer duration of effect than 5mg diphenoxylate. Loperamide is probably superior to diphenoxylate in providing symptomatic control of chronic diarrhoea such as that associated with chronic inflammatory bowel disease or following gastrointestinal surgery. It has been used for up to 3 years in such conditions without evidence of tolerance. The possibility of once daily dosage of loperamide in chronic diarrhoea is an advantage. Side-effects have not proved a problem.

摘要

洛哌丁胺是一种丁酰胺衍生物,是用于急性非特异性腹泻和慢性腹泻症状控制的新药。与地芬诺酯或可待因不同,洛哌丁胺在正常治疗剂量下似乎不会在人体中发挥阿片样活性。在急性腹泻中,根据不成形的排便情况灵活给药时,洛哌丁胺比地芬诺酯能更快地控制症状,并且在单剂量研究中,4毫克洛哌丁胺的作用持续时间比5毫克地芬诺酯长得多。在提供慢性腹泻(如与慢性炎症性肠病或胃肠道手术后相关的腹泻)的症状控制方面,洛哌丁胺可能优于地芬诺酯。在这种情况下,它已被使用长达3年,没有耐受性的证据。在慢性腹泻中每日一次服用洛哌丁胺的可能性是一个优点。尚未证明副作用是一个问题。

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