Lubiprostone: a chloride channel activator.
In January 2006 the Food and Drug Administration approved lubiprostone for the treatment of chronic constipation in men and women aged 18 and over. Lubiprostone is categorized as a prostone, a bicyclic fatty acid metabolite of prostaglandin E1. Lubiprostone activates a specific chloride channel (ClC-2) in the gastrointestinal (GI) tract to enhance intestinal fluid secretion, which increases GI transit and improves symptoms of constipation. This article reviews the role of chloride channels in the GI tract, describes the structure, function, and pharmacokinetics of lubiprostone, and discusses clinically important data on this new medication.
Lacy
Brian E
BE
Section of Gastroenterology and Hepatology, Dartmouth-Hitchcock Medical Center, Lebanon, NH 03756, USA. brian.lacy@hitchcock.org
Levy
L Campbell
LC
D000527:Alprostadil / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D002400:Cathartics / Q000494:pharmacology*; D018118:Chloride Channels / Q000187:drug effects* / Q000502:physiology; D002712:Chlorides / Q000378:metabolism; D002908:Chronic Disease; D003248:Constipation / Q000188:drug therapy*; D005227:Fatty Acids / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D005772:Gastrointestinal Transit / Q000187:drug effects; D006801:Humans; D000068238:Lubiprostone; D008297:Male
D002400:Cathartics; D018118:Chloride Channels; D002712:Chlorides; D005227:Fatty Acids; D000068238:Lubiprostone; D000527:Alprostadil