|Trade names||Zelnorm, Zelmac|
|Main uses||Irritable bowel syndrome with constipation|
|Side effects||Headache, abdominal pain, diarrhea, heart attacks, stroke, suicide|
|Typical dose||6 mg BID|
|Metabolism||Stomach and liver|
|Elimination half-life||11 ± 5 hours|
|Excretion||Fecal and Kidney|
|Chemical and physical data|
|Molar mass||301.394 g·mol−1|
|3D model (JSmol)|
Common side effects include headache, abdominal pain, diarrhea, and dizziness. Other side effects may include heart attacks, stroke, and suicide. It is a 5-HT4 activator which stimulates both contraction and increased fluid release by the intestines.
Tegaserod was approved for medical use in the United States in 2002. It was removed from the market in 2007 due to concerns related to the heart but than re-allowed in 2019. In Europe it was refused approval in both 2005 and 2006. In the United States it costs about 360 USD per month as of 2021. It was withdrawn from the market due to commercial reasons in 2022.
It is generally taken as 6 mg twice per day.
Mechanism of action
The drug functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist.
On 30 March 2007, the United States Food and Drug Administration requested that Novartis withdraw tegaserod from shelves. The FDA alleged a relationship between prescriptions of the drug and increased risks of heart attack or stroke. An analysis of data collected on over 18,000 patients demonstrated adverse cardiovascular events in 13 of 11,614 patients treated with tegaserod (a rate of 0.11%) as compared with 1 of 7,031 patients treated with placebo (a rate of 0.01%). Novartis alleged all of the affected patients had preexisting cardiovascular disease or risk factors for such, and further alleged that no causal relationship between tegaserod use and cardiovascular events has been demonstrated. On the same day as the FDA announcement, Novartis Pharmaceuticals Canada announced that it was suspending marketing and sales of the drug in Canada in response to a request from Health Canada. In a large cohort study based on a US health insurance database, no increase in the risk of cardiovascular events were found under tegaserod treatment. In 2019, tegaserod was reintroduced as for use in irritable bowel syndrome with constipation (IBS-C) in women under 65.
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