Literature DB >> 10493276

Tegaserod.

L J Scott1, C M Perry.   

Abstract

Tegaserod is a serotonin (5-hydroxytryptamine; 5-HT) receptor partial agonist which has been investigated for the treatment of irritable bowel syndrome (IBS). Specifically, it binds with high affinity to human 5-HT4 receptors, thereby stimulating the release of neurotransmitters and the peristaltic reflex in vitro. Small bowel transit (increased colonic filling over 6 hours) was accelerated in patients with constipation-predominant irritable bowel syndrome (IBS) receiving oral tegaserod 2mg twice daily for 1 week compared with those receiving placebo. In addition, there was a mean 20% increase of proximal colonic emptying in these patients. Oral tegaserod 2 (p < 0.05) or 6mg twice daily improved symptoms of abdominal discomfort, bloating and constipation (assessed using a Subjects' Global Assessment Scale) compared with placebo in patients with constipation-predominant IBS in a double-blind, dose-ranging study. The most frequent adverse events in patients with constipation-predominant IBS receiving oral tegaserod were transient diarrhoea and flatulence. No clinically relevant changes in blood pressure, pulse rate, QRS or QTc interval were reported with tegaserod doses of 25 to 100mg.

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Year:  1999        PMID: 10493276     DOI: 10.2165/00003495-199958030-00013

Source DB:  PubMed          Journal:  Drugs        ISSN: 0012-6667            Impact factor:   9.546


  12 in total

1.  Integrated modelling of the clinical pharmacokinetics of SDZ HTF 919, a novel selective 5-HT4 receptor agonist, following oral and intravenous administration.

Authors:  S Appel-Dingemanse; M O Lemarechal; A Kumle; M Hubert; E Legangneux
Journal:  Br J Clin Pharmacol       Date:  1999-05       Impact factor: 4.335

2.  High affinity of SDZ HTF-919 related molecules for calf and human caudate 5-HT4 receptors.

Authors:  D Hoyer; D Fehlmann; D Langenegger; J Kummer; R Giger; H Mattes; A Probst; H J Pfannkuche
Journal:  Ann N Y Acad Sci       Date:  1998-12-15       Impact factor: 5.691

3.  Clinical pharmacodynamics of SDZ HTF 919, a new 5-HT4 receptor agonist, in a model of slow colonic transit.

Authors:  S Appel; A Kumle; R Meier
Journal:  Clin Pharmacol Ther       Date:  1997-11       Impact factor: 6.875

Review 4.  Irritable bowel syndrome: a technical review for practice guideline development.

Authors:  D A Drossman; W E Whitehead; M Camilleri
Journal:  Gastroenterology       Date:  1997-06       Impact factor: 22.682

5.  American Gastroenterological Association medical position statement: irritable bowel syndrome.

Authors: 
Journal:  Gastroenterology       Date:  1997-06       Impact factor: 22.682

6.  First pharmacokinetic-pharmacodynamic study in humans with a selective 5-hydroxytryptamine4 receptor agonist.

Authors:  S Appel; A Kumle; M Hubert; T Duvauchelle
Journal:  J Clin Pharmacol       Date:  1997-03       Impact factor: 3.126

7.  The serotonin 5-HT4 receptor. 2. Structure-activity studies of the indole carbazimidamide class of agonists.

Authors:  K H Buchheit; R Gamse; R Giger; D Hoyer; F Klein; E Klöppner; H J Pfannkuche; H Mattes
Journal:  J Med Chem       Date:  1995-06-23       Impact factor: 7.446

8.  5-Hydroxytryptamine4 receptor agonists initiate the peristaltic reflex in human, rat, and guinea pig intestine.

Authors:  J R Grider; A E Foxx-Orenstein; J G Jin
Journal:  Gastroenterology       Date:  1998-08       Impact factor: 22.682

Review 9.  New drugs in the management of the irritable bowel syndrome.

Authors:  M J Farthing
Journal:  Drugs       Date:  1998-07       Impact factor: 9.546

10.  Diagnosis and treatment of irritable bowel syndrome.

Authors:  C B Dalton; D A Drossman
Journal:  Drugs Today (Barc)       Date:  1998-07       Impact factor: 2.245

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  12 in total

1.  What comes after macrolides and other motilin stimulants?

Authors:  J Tack; T Peeters
Journal:  Gut       Date:  2001-09       Impact factor: 23.059

Review 2.  Serotonin and neuroprotection in functional bowel disorders.

Authors:  M D Gershon; M-T Liu
Journal:  Neurogastroenterol Motil       Date:  2007-08       Impact factor: 3.598

Review 3.  Clinical pharmacokinetics of tegaserod, a serotonin 5-HT(4) receptor partial agonist with promotile activity.

Authors:  Silke Appel-Dingemanse
Journal:  Clin Pharmacokinet       Date:  2002       Impact factor: 6.447

Review 4.  Drug treatment options for irritable bowel syndrome: managing for success.

Authors:  R C Dunphy; G N Verne
Journal:  Drugs Aging       Date:  2001       Impact factor: 3.923

Review 5.  New developments in the treatment of functional dyspepsia.

Authors:  Vincenzo Stanghellini; Fabrizio De Ponti; Roberto De Giorgio; Giovanni Barbara; Cesare Tosetti; Roberto Corinaldesi
Journal:  Drugs       Date:  2003       Impact factor: 9.546

6.  Differences between the abilities of tegaserod and motilin receptor agonists to stimulate gastric motility in vitro.

Authors:  E M Jarvie; V J North Laidler; S Corcoran; A Bassil; G J Sanger
Journal:  Br J Pharmacol       Date:  2007-01-08       Impact factor: 8.739

Review 7.  Irritable bowel syndrome: new agents targeting serotonin receptor subtypes.

Authors:  F De Ponti; M Tonini
Journal:  Drugs       Date:  2001       Impact factor: 9.546

8.  Pharmacology and metabolism of renzapride : a novel therapeutic agent for the potential treatment of irritable bowel syndrome.

Authors:  Nicholas L Meyers; Roger I Hickling
Journal:  Drugs R D       Date:  2008

Review 9.  Tegaserod: a review of its use in the management of irritable bowel syndrome with constipation in women.

Authors:  Antona J Wagstaff; James E Frampton; Katherine F Croom
Journal:  Drugs       Date:  2003       Impact factor: 9.546

10.  Delayed Gastric Emptying in Functional Dyspepsia.

Authors:  Vincenzo Stanghellini; Roberto De Giorgio; Giovanni Barbara; Rosanna Cogliandro; Cesare Tosetti; Fabrizio De Ponti; Roberto Corinaldesi
Journal:  Curr Treat Options Gastroenterol       Date:  2004-08
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