Tegaserod

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Tegaserod
Systematic (IUPAC) name
1-{[5-(hydroxymethyl)-1H-indol-3-yl]methylideneamino}- 2-pentyl-guanidine
Identifiers
CAS number	189188-57-6
ATC code	A03 AE02
PubChem	5487301
DrugBank	APRD00096
Chemical data
Formula	C₁₆H₂₃N₅O
Mol. weight	301.387 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 used for the management of constipation-predominant irritable bowel syndrome (IBS). Tegaserod is the only FDA approved drug to help relieve the abdominal discomfort, bloating and constipation of IBS. IT had also been FDA approved to treat Chronic Constipation (Idiopathic). It is currently marketed by Novartis under the trade names Zelnorm® (in the US) or Zelmac (outside the US).

A slow-moving digestive system may be the cause of Chronic Constipation or Irritable Bowel Syndrome with Constipation. It can result in the "ABC" symptoms:

Abdominal discomfort: Cramps, twinges or sharp aches that may be in several locations or change location.

Bloating: A full, tight feeling in the abdomen often caused by excessive gas in the intestines. The abdomen may appear distended, as if heavy and full.

Constipation: This bowel pattern is different for everyone, but could include infrequent bowel movements, hard or lumpy stools, difficulty in passing stools, inability to have a bowel movement, incomplete elimination, straining with a bowel movement or any of these in combination.

Tegaserod is a motility stimulant. Therapeutic effect is achieved through activation of 5-HT₄ receptors of the enteric nervous system in the gastrointestinal tract. Tegaserod stimulates gastrointestinal motility and the peristaltic reflex, and possibly also reduces abdominal pain (Rossi, 2004).

A recent press release by the manufacturing company (Novartis) has disclosed a positive preliminary pooled results of a mega trial to prove efficacy in Dyspepsia

[edit] References

Rossi, S (Ed.) (2004). Australian Medicines Handbook 2004 (AMH). Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2.
www.pharma.us.novartis.com/newsroom/pressReleases/releaseDetail.jsp?PRID=2004
http://www.fda.gov/bbs/topics/ANSWERS/2002/ANS01160.html