Tegaserod is a 5-HT4 agonist manufactured by Novartis and sold under the names Zelnorm and Zelmac for the management of irritable bowel syndrome and constipation.
Mechanism of action
The drug functions as a
motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT
4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the
peristalsis reflex, and allegedly reduces abdominal pain.
Additionally, tegaserod is a 5-HT
2B receptor antagonist.
Withdrawal from market
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.
