Lubiprostone: chronic constipation and irritable bowel syndrome with constipation.

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Lacy BE, Chey WD

Lubiprostone: chronic constipation and irritable bowel syndrome with constipation.

Expert Opin Pharmacother. 2009 Jan;10(1):143-52. doi: 10.1517/14656560802631319 .

PubMed ID

19236188 [ View in PubMed

]

Abstract

Lubiprostone is a bicyclic fatty acid metabolite analogue of prostaglandin E1. The FDA has approved lubiprostone for the treatment of chronic constipation in men and women and the treatment of women with irritable bowel syndrome with constipation (IBS-C). Lubiprostone specifically activates type-2-chloride channels on the apical membrane of epithelial cells. Lubiprostone acts locally within the intestinal tract, is rapidly metabolized and has very low systemic bioavailability. Animal studies have demonstrated that lubiprostone increases gastrointestinal fluid secretion in a dose-dependent manner. Clinical studies performed in men and women with chronic constipation using 24 microg of lubiprostone twice-daily demonstrated objective improvement in stool frequency and consistency, as well as symptoms of straining and incomplete evacuation. A multi-center study of patients with IBS-C found that 8 microg of lubiprostone twice-daily improved both global and individual symptoms of irritable bowel syndrome. Lubiprostone is generally well tolerated and serious adverse events are rare. The most common reported side effects are nausea, headache and diarrhea. This monograph provides a brief overview on chloride channel function in the gastrointestinal tract, describes the structure, function, and pharmacokinetics of lubiprostone, and discusses the safety and efficacy of this new medication for the treatment of chronic constipation and IBS-C.

DrugBank Data that Cites this Article

Drugs

Lubiprostone

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Lubiprostone	Chloride channel protein 2	Protein	Humans	Yes	Inducer	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Lubiprostone	Carbonyl reductase [NADPH] 1	Protein	Humans	Unknown	Substrate	Details