Huighebaert S, Awouters F, Tytgat G N J
Consultant Pharmaceutical Sciences, La Hulpe, Belgium.
Dig Dis Sci. 2003 Feb;48(2):239-50. doi: 10.1023/a:1021989606317.
Racecadotril is an enkephalinase inhibitor, presented as a purely antisecretory agent with advantages over the opiate-receptor agonist loperamide in the treatment of diarrhea. A critical review of the literature and the models used was performed. Although pretreatment with high doses of racecadotril reduced cholera toxin-induced secretion and although clinical efficacy was demonstrated in young infants--a population characterized by 10-fold higher plasma enkephalin concentrations compared with adults, the analysis calls into question the peripheral antisecretory selectivity and relative clinical efficacy. Conversely, loperamide can be proposed as an antisecretory agent at therapeutic concentrations. Its efficacy is well established in acute and chronic diarrhea. Current experimental and clinical comparative studies of both drugs have problems with regard to the selection of the doses, the validity of models, and/or the trial design. The conclusion is that more research is needed before reliable conclusions can be drawn on the place of racecadotril in diarrhea treatment.
消旋卡多曲是一种脑啡肽酶抑制剂，作为一种单纯的抗分泌剂，在治疗腹泻方面比阿片受体激动剂洛哌丁胺更具优势。我们对相关文献和所使用的模型进行了批判性综述。尽管高剂量消旋卡多曲预处理可减少霍乱毒素诱导的分泌，并且在幼儿（与成人相比，该人群血浆脑啡肽浓度高10倍）中已证明其临床疗效，但该分析对其外周抗分泌选择性和相对临床疗效提出了质疑。相反，洛哌丁胺在治疗浓度下可作为抗分泌剂。其在急性和慢性腹泻中的疗效已得到充分证实。目前这两种药物的实验和临床对比研究在剂量选择、模型有效性和/或试验设计方面存在问题。结论是，在得出关于消旋卡多曲在腹泻治疗中地位的可靠结论之前，还需要更多研究。
