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説明

Chronic constipation is an affliction affecting 4–5 million Americans alone. When no specific cause is identified, it is classified as idiopathic. Dietary and lifestyle modifications are the first-line conventional approaches followed by the administration of laxatives. Unfortunately, chronic idiopathic constipation is frequently refractory to traditional therapy; thus, the need for novel agents exists. Lubiprostone is a bicyclic fatty acid with a novel mechanism of action. Without affecting sodium and potassium ion concentrations, lubiprostone activates intestinal chloride ion channels, thereby, increasing intestinal water secretion and intestinal fluid chloride ion concentration. In basolateral membranepermeabilized T84 gastrointestinal epithelial cells under chloride gradient conditions, lubiprostone concentration-dependently increased short-circuit current with an EC50 of approximately 20 nM.