Yeo Q M, Crutchley R, Cottreau J, Tucker A, Garey K W
National University of Singapore, Singapore.
Drugs Today (Barc). 2013 Apr;49(4):239-52. doi: 10.1358/dot.2013.49.4.1947253.
Secretory diarrhea has a significant impact on morbidity and mortality worldwide and may be a predominant or minor component of pathogenesis in diarrhea of various etiologies. Crofelemer is a first-in-class antidiarrheal medication with unique inhibitory mechanisms at both the cystic fibrosis transmembrane conductance regulator and the calcium-activated chloride channels which are responsible for chloride secretion and subsequent luminal hydration. The efficacy of crofelemer has been investigated in patients with HIV-associated diarrhea, diarrhea of various infectious etiologies, as well as diarrhea-predominant irritable bowel syndrome. Crofelemer was approved by the FDA in December 2012 to treat diarrhea in HIV/AIDS patients on antiretroviral therapy. Crofelemer is not absorbed in the body and well-tolerated in small trials performed to date although long-term safety data is lacking. Crofelemer may be an important addition to the currently available drugs for the management of secretory diarrhea.
分泌性腹泻对全球的发病率和死亡率有重大影响，并且在各种病因引起的腹泻发病机制中可能是主要或次要组成部分。克罗felemer是一种一流的止泻药物，在囊性纤维化跨膜传导调节因子和钙激活氯离子通道上具有独特的抑制机制，这些通道负责氯离子分泌和随后的肠腔水合作用。已对克罗felemer在HIV相关腹泻、各种感染性病因引起的腹泻以及以腹泻为主的肠易激综合征患者中的疗效进行了研究。2012年12月，克罗felemer被美国食品药品监督管理局批准用于治疗接受抗逆转录病毒治疗的HIV/AIDS患者的腹泻。克罗felemer在体内不被吸收，在迄今为止进行的小型试验中耐受性良好，尽管缺乏长期安全性数据。克罗felemer可能是目前用于治疗分泌性腹泻的现有药物的重要补充。
