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Tegaserod

From Wikipedia, the free encyclopedia
Medication
Pharmaceutical compound
Tegaserod
Clinical data
Trade namesZelnorm, Zelmac
AHFS/Drugs.comMonograph
Pregnancy
category
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability10%
Protein binding98%
MetabolismGastric andhepatic
Eliminationhalf-life11 ± 5 hours
ExcretionFecal andrenal
Identifiers
  • (2E)-2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.158.793Edit this at Wikidata
Chemical and physical data
FormulaC16H23N5O
Molar mass301.394 g·mol−1
3D model (JSmol)
  • CCCCCNC(=N)NN=Cc1c[nH]c2ccc(OC)cc12
  • InChI=1S/C16H23N5O/c1-3-4-5-8-18-16(17)21-20-11-12-10-19-15-7-6-13(22-2)9-14(12)15/h6-7,9-11,19H,3-5,8H2,1-2H3,(H3,17,18,21)/b20-11+ checkY
  • Key:IKBKZGMPCYNSLU-RGVLZGJSSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Tegaserod is a5-HT4agonist manufactured byNovartis and sold under the namesZelnorm andZelmac for the management ofirritable bowel syndrome andconstipation.[1] Approved by the FDA in 2002, it was subsequently removed from the market in 2007 due to FDA concerns about possible adverse cardiovascular effects. Before then, it was the only drug approved by theUnited StatesFood and Drug Administration to help relieve theabdominal discomfort,bloating, and constipation associated with irritable bowel syndrome. Its use was also approved to treat chronicidiopathic constipation.[2]

Mechanism of action

[edit]

The drug functions as amotility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of theenteric nervous system in thegastrointestinal tract. It also stimulates gastrointestinal motility and theperistaltic reflex, and allegedly reduces abdominal pain.[3] Additionally, tegaserod is a5-HT2B receptor antagonist.[4]

Withdrawal from market

[edit]

On 30 March 2007, the United StatesFood and Drug Administration requested that Novartis withdraw tegaserod from shelves.[5] 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.[6] On the same day as theFDA announcement, Novartis Pharmaceuticals Canada announced that it was suspending marketing and sales of the drug in Canada in response to a request fromHealth Canada.[7] 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.[8] In 2019, tegaserod was reintroduced as for use in irritable bowel syndrome with constipation (IBS-C) in women under 65.[9]

References

[edit]
  1. ^"New Data for Zelnorm". Archived fromthe original on December 9, 2007. RetrievedMarch 30, 2007.
  2. ^"FDA approves first treatment for women with irritable-bowel syndrome".Food and Drug Administration. Archived fromthe original on February 5, 2007. RetrievedMarch 30, 2007.
  3. ^Rossi, S. (2004).Australian Medicines Handbook. Adelaide: Health Communication Network.ISBN 0-9578521-4-2.
  4. ^Beattie DT, Smith JA, Marquess D, et al. (November 2004)."The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo".Br. J. Pharmacol.143 (5):549–60.doi:10.1038/sj.bjp.0705929.PMC 1575425.PMID 15466450.
  5. ^"FDA Announces Discontinued Marketing of GI Drug, Zelnorm, for Safety Reasons". FDA Press Release. 30 March 2007. Archived fromthe original on July 10, 2009.
  6. ^"Zelnorm"(PDF).Novartis. Archived fromthe original(PDF) on 2007-04-10. Retrieved2007-03-30.
  7. ^"Novartis suspends Canadian marketing and sales of Zelnorm in response to request from Health Canada". Retrieved2007-03-30.
  8. ^Loughlin J, Quinn S, Rivero E, Wong J, Huang J, Kralstein J, Earnest DL, Seeger JD (2010)."Tegaserod and the Risk of Cardiovascular Ischemic Events: An Observational Cohort Study".J Cardiovasc Pharmacol Ther.15 (2):151–7.doi:10.1177/1074248409360357.PMID 20200325.S2CID 37964792.
  9. ^WorldMeds, U. S."FDA approves the reintroduction of Zelnorm™ (tegaserod) for Irritable Bowel Syndrome with Constipation (IBS-C) in women under 65".www.prnewswire.com (Press release). Retrieved2019-09-17.
Drugs for constipation (laxatives andcathartics) (A06)
Stool softeners
Stimulant laxatives
Bulk-forming laxatives
Lubricant laxatives
Osmotic laxatives
Enemas
Opioid antagonists
Others
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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