Tegaserod irritable bowel syndrome

In the periphery, 5-HT4 receptor mRNA is found in vascular smooth muscle. Newly developed drugs that activate 5-HT4 receptors are of interest for their potential in treating cardiac arrhythmia. The 5-HT4 receptor is also located on neurons of the alimentary tract, for example the myenteric plexus of the ileum, and on smooth muscle cells and secretory cells of the gastrointestinal tract, where they evoke secretions and the peristaltic reflex. 5-HT4 receptor agonists (e.g. cisapride, prucalopride, tegaserod) are used therapeutically in the treatment of constipation-predominant irritable bowel syndrome and in functional motility disorders of the upper gastrointestinal tract. 

Evans BW, Clark WK, Moore DJ, Whorwell PJ. Tegaserod for the treatment of irritable bowel syndrome and chronic constipation. Cochrane Database Syst Rev 2007. 

Cisapride, a 5-HT4 agonist, was used in the treatment of gastroesophageal reflux and motility disorders. Because of toxicity, it is now available only for compassionate use in the USA. Tegaserod, a 5-HT4 partial agonist, is used for irritable bowel syndrome with constipation. These drugs are discussed in Chapter 62. 

Tegaserod was recently approved for the treatment of patients with irritable bowel syndrome with... 

A subclass of serotonin receptors dubbed 5-HT4 are involved in regulation of intestinal motility. The partial agonist tegaserod (22) has proven useful in treating conditions characterized by decreased motility, such as irritable bowel syndrome. The drug is interestingly prescribed specifically for use in women, since results from clinical trials indicated poor response in men. Alkylation of thiosemicarbazone (18) with methyl iodide proceeds on sulfur to the thioether (19). Treatment of intermediate 19 with pentyl-1-amine leads to addition of the amine to the thioether function followed by... 

Tougas G, Snape WJ, Otten MH, et al. Long-term safety of tegaserod in patients with constipation-predominant irritable bowel syndrome. AUment PUarmacol TUer 2002 16 1701-1708. 

Muller-Lissner SA, EumagalU I, BardUan KD, et al. Tegaserod, a 5-HT4 receptor partial agonist, relieves symptoms in irritable bowel syndrome patients with abdominal pain, bloating and constipation. AUment Pharmacol Ther 2001 15 1655-1666. 

Tegaserod maleate is a GI agent that binds with high affinity to human 5-HT4 receptors, acting as an agonist at neuronal 5-HT4 receptors to trigger the release of neurotransmitters. Activation of 5-HT4 receptors in the GI tract stimulates peristaltic reflex and intestinal secretion, and inhibits visceral sensitivity. It is used for short-term treatment of women with irritable bowel syndrome (IBS) whose primary symptom is constipation and in treatment of patients younger than 65 years of age with chronic idiopathic constipation. 

In clinical trials, tegaserod also reduced bloating (a prominent symptom in patients with irritable bowel syndrome) and pain, but it is not clear whether this represents an independent effect on sensory nerves or simply a consequence of decreased fecal or air distention of the colon. As yet, there is no evidence for significant modulation of nociceptive signaling by 5-HT4 receptors. 

Tegaserod is available for oral administration in 2-mg and 6-mg tablets and approved for use in women with constipation-dominant irritable bowel syndrome at a dose of 6 mg twice daily. Tegaserod also has been approved for the treatment of chronic constipation. Higher doses have been suggested for other prokinetic effects (e.g., stimula-... 

The female client is diagnosed with irritable bowel syndrome (IBS). The health-care provider prescribes tegaserod (Zelnorm), a gastrointestinal agent. Which assessment data indicates the medication is effective ... 

Wagstaff AJ, Frampton JE, Croom KF. Tegaserod a review of its use in the management of irritable bowel syndrome with constipation in women. Drugs 2003 63 1101-20. 

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