Tegaserod maleate

Tegaserod maleate (Zelnorm) is a partial serotonin (5-HT4) receptor agonist that causes an increase in peristaltic activity and intestinal secretion and moderation of visceral sensitivity. It increases the frequency of bowel movements and reduces abdominal discomfort, bloating, and straining. It is indicated for the treatment of patients younger than 65 years of age who experience chronic idiopathic constipation. The most common adverse effects include headache, abdominal pain, diarrhea, and nausea. 

Slow-transit constipation can be treated with chronic administration of osmotic laxatives. Tegaserod maleate 6 mg orally twice daily is an acceptable treatment. Senna, bisacodyl, and other stimulants should be used only when the others fail to deliver the desired effect. 

Tegaserod maleate (Zelnorm) stimulates 5-HT4 receptors in the GI tract, thereby increasing intestinal secretion, peristalsis, and small bowel transit. It also reduces sensitivity related to abdominal distention. It has been shown to be more effective than placebo in improving global IBS symptoms and altered bowel habits in constipation-predominant IBS.21 Diarrhea is a possible adverse effect. 

In March of 2007, the FDA announced that tegaserod maleate would be voluntarily withdrawn from the market because of information indicating an increased risk of serious cardiovascular events (myocardial infarction, unstable angina, and stroke). 

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. 

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