Tegaserod
You don't need to be Editor-In-Chief to add or edit content to WikiDoc. You can begin to add to or edit text on this WikiDoc page by clicking on the edit button at the top of this page. Next enter or edit the information that you would like to appear here. Once you are done editing, scroll down and click the Save page button at the bottom of the page.
| Image:Tegaserod chemical structure.png | |
| Image:Tegaserod Zelnorm.gif | |
| Tegaserod
| |
| Systematic (IUPAC) name | |
| 2-((5-Methoxy-1H-indol-3-yl)methylene)-N-pentylhydrazinecarboximidamide | |
| Identifiers | |
| CAS number | |
| ATC code | A03 |
| PubChem | |
| DrugBank | |
| 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. | |
| Legal status | |
| 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.[1] It is currently marketed by Novartis under the trade names Zelnorm and Zelmac in the United States and abroad, respectively.
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.[1]
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.[1] 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.[1] 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.[1] Some manufacturers in India, such as Cipla, seem to still have generic Tegaserod available in their listings[1] and some online merchants may be selling it.
References
http://hc-sc.gc.ca/dhp-mps/medeff/advisories-avis/public/2007/zelnorm_pc-cp_2_e.html
External links
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 |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
