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Tegaserod



Tegaserod
Systematic (IUPAC) name
2-((5-Methoxy-1H-indol-3-yl)methylene)-N-pentylhydrazinecarboximidamide
Identifiers
CAS number	189188-57-6
ATC code	A03AE02
PubChem	6918369
DrugBank	APRD00096 (wrong structure)
Chemical data
Formula	C₁₆H₂₃N₅O
Mol. mass	301.39 g/mol
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	℞-only(US)
Routes	Oral

Tegaserod is a 5-HT₄ agonist manufactured by Novartis and used for the management of irritable bowel syndrome and constipation.^[1] Its use 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] It is currently marketed by Novartis under the trade names Zelnorm and Zelmac in the United States and abroad, respectively.

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The drug functioned 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]

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.^[4] 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 states all of the affected patients had preexisting cardiovascular disease or risk factors for such, and further states that no causal relationship between tegaserod use and cardiovascular events has been demonstrated.^[5] 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.^[6] Some manufacturers in India, such as Cipla, seem to still have generic Tegaserod available in their listings^[7] and some online merchants may be selling it.

References

^ New Data for Zelnorm®. Retrieved on March 30, 2007.
^ FDA approves first treatment for women with irritable-bowel syndrome. Retrieved on March 30, 2007.
^ Rossi, S. (2004). Australian Medicines Handbook. Adelaide: Health Communication Network. ISBN ISBN 0-9578521-4-2.
^ Constipation drug pulled at FDA request. Retrieved on March 30, 2007.
^ Zelnorm. Novartis. Retrieved on 2007-03-30.
^ Novartis suspends Canadian marketing and sales of Zelnorm® in response to request from Health Canada. Retrieved on 2007-03-30.
^ http://www.cipla.com/ourproducts/productlist/t.htm

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

v • d • e

Drugs for functional gastrointestinal disorders (A03)

Drugs for functional bowel disorders

antimuscarinics: Mebeverine - Dicycloverine - Propantheline

papaverine and derivatives: Papaverine - Drotaverine - Moxaverine

acting on serotonin receptors: 5-HT₃ antagonists (Alosetron, Cilansetron) - 5HT₄ agonists (Mosapride, Tegaserod)

other: Diisopromine - Isometheptene - Phloroglucinol - Proglumide - Tridihexethyl

Belladonna and derivatives
(antimuscarinics)

Atropine - Hyoscyamine - Butylscopolamine - Methylscopolamine

Propulsives

primarily dopamine antagonists (Metoclopramide/Bromopride, Domperidone, Alizapride) - serotonin agonists (Cisapride) - Clebopride

Categories: Motility stimulants | Serotonin receptor agonists | Withdrawn drugs

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Tegaserod". A list of authors is available in Wikipedia.