Abstract
Chronic constipation affects up to 27% of the population and negatively impacts health-related quality-of-life. Prescription medications targeting chronic constipation currently include polyethylene glycol, lactulose and tegaserod, a serotonin type 4 receptor partial agonist. The most recent addition is lubiprostone (Amitiza), a type-2 chloride channel (ClC-2) activator which is a member of a new class of compounds known as prostones. Lubiprostone is a bicyclic fatty acid that acts locally on ClC-2 channels located in the apical membrane of intestinal epithelial cells. This stimulation of chloride secretion induces the passive movement of sodium and water into the intestinal lumen, yielding a net increase in isotonic fluid, which results in improved bowel function. In double-blind, placebo-controlled clinical trials, lubiprostone increased the number of spontaneous bowel movements compared with placebo and was generally well tolerated. The predominant adverse effects were nausea and diarrhea. Lubiprostone represents a new therapeutic class of compounds for the treatment of chronic constipation and will be the focus of this review.
Original language | English (US) |
---|---|
Pages (from-to) | 66-70 |
Number of pages | 5 |
Journal | Current Opinion in Investigational Drugs |
Volume | 8 |
Issue number | 1 |
State | Published - Jan 2007 |
Keywords
- Chloride channel
- Clinical trial
- Constipation
- Lubiprostone
- Type-2 chloride channel
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery