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Tegaserod
Systematic (IUPAC) name
(2E)-2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide
Identifiers
CAS number 189188-57-6
ATC code A03AE02
PubChem 6918369
DrugBank  (wrong structure) APRD00096  (wrong structure)
Chemical data
Formula C16H23N5O 
Mol. mass 301.39 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 10%
Protein binding 98%
Metabolism Gastric and hepatic
Half life 11 ± 5 hours
Excretion Fecal and renal
Therapeutic considerations
Pregnancy cat. B3(AU) B(US)
Legal status Withdrawn
Routes Oral

Tegaserod is a 5-HT4 agonist manufactured by Novartis and sold under the name Zelnorm for the management of irritable bowel syndrome and constipation.[1] It was removed from the market. Before then, it was the only drug approved by the United States Food and Drug Administration to help relieve the abdominal discomfort, bloating and constipation associated with irritable bowel syndrome. Its use was also approved to treat chronic idiopathic constipation.[2]

Contents

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.[3] Additionally, tegaserod is a 5-HT2B receptor antagonist.[4]

Withdrawal from market

On March 30, 2007, the U.S. Food and Drug Administration requested that Novartis withdraw Zelnorm from shelves. The FDA alleges a relationship between prescriptions of the drug and increased risks of heart attack or stroke.[5] An analysis of data collected on over 18,000 patients demonstrated adverse cardiovascular events in 13 of 11,614 patients treated with Zelnorm (a rate of 0.11%) as compared with 1 of 7,031 patients treated with placebo (a rate of 0.01%). Novartis alleges all of the affected patients had preexisting cardiovascular disease or risk factors for such, and further alleges that no causal relationship between tegaserod use and cardiovascular events has been demonstrated.[6] 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.[7] Some manufacturers in India, such as Cipla, seem to still have generic Tegaserod available in their listings[8] and some online merchants may be selling it. Large cohort study based on US health insurance database showed that tegaserod doesn't increase the risk of cardiovascular event.[9]

References

http://hc-sc.gc.ca/dhp-mps/medeff/advisories-avis/public/2007/zelnorm_pc-cp_2_e.html

External links








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