Efficacy of 5-HT3 Antagonists and 5-HT4 Agonists in Irritable Bowel Syndrome: Systematic Review and Meta-Analysis

  title={Efficacy of 5-HT3 Antagonists and 5-HT4 Agonists in Irritable Bowel Syndrome: Systematic Review and Meta-Analysis},
  author={Alexander Charles Ford and Lawrence J Brandt and Christine Young and William D. Chey and Amy E. Foxx-Orenstein and Paul Moayyedi},
  journal={The American Journal of Gastroenterology},
OBJECTIVES:Irritable bowel syndrome (IBS) is a chronic functional disorder. 5-Hydroxytryptamine (5-HT) is a key modulator of gastrointestinal sensorimotor function. Many patients have IBS that can be difficult to treat, which has led to the development of newer agents, such as 5-HT3 antagonists and 5-HT4 agonists. We conducted a systematic review and meta-analysis of randomized controlled trials (RCTs) to estimate the efficacy of all available 5-HT agents in IBS.METHODS:MEDLINE, EMBASE, and the… 

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Renzapride is not superior to placebo in relieving IBS symptoms and causes significant incidences of diarrhea and drop-outs due to adverse effects in treated patients vs. placebo, suggesting this medicine might be a cost burden to patients without providing good effectiveness.

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The authors concluded that the ramosetron 5 µg once daily was as effective as mebeverine 3 times daily in male patients with IBS-D.

CSTI-300 (SMP-100); a Novel 5-HT3 Receptor Partial Agonist with Potential to Treat Patients with Irritable Bowel Syndrome or Carcinoid Syndrome

Evidence is presented that treatment with a suitable 5-HT3 receptor partial agonist will alleviate some symptoms associated with these conditions yet, without fully inhibiting the receptor, predict a less pronounced side-effect profile associated with this therapeutic strategy.

Efficacy of Prebiotics, Probiotics, and Synbiotics in Irritable Bowel Syndrome and Chronic Idiopathic Constipation: Systematic Review and Meta-analysis

Probiotics are effective treatments for IBS, although which individual species and strains are the most beneficial remains unclear, and the efficacy of all three therapies in CIC is also uncertain.

Treatment of IBS‐D with 5‐HT3 receptor antagonists vs spasmolytic agents: similar therapeutical effects from heterogeneous pharmacological targets

  • P. Clavé
  • Medicine, Biology
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  • 2011
A pharmacologic strategy which uses different drugs for pain and dysmotility in the same patient and includes specific drugs acting on smooth muscle cells, neuromuscular transmission, synaptic transmission and intrinsic afferents is proposed.

Modern Management of Irritable Bowel Syndrome: More Than Motility

Antidepressants were found to be efficacious for abdominal pain, but their tolerance may be problematic and the therapeutic effect varied largely between trials, while meta-analyses suggest efficacy of probiotics as a group, the quality of the trials is often suboptimal and there is large variability.

The neurokinin-2 receptor antagonist ibodutant improves overall symptoms, abdominal pain and stool pattern in female patients in a phase II study of diarrhoea-predominant IBS

Ibodutant showed dose-dependent efficacy response in IBS-D, reaching statistical significance at the 10 mg dose in female patients, and the safety and tolerability profile of ibodutan was similar to placebo.

Treatment of Irritable Bowel Syndrome

The treatment strategies adequate for Korean patients with IBS are required and some probiotics, tricyclic antidepressants and selective serotonin reuptake inhibitors may have some benefits in relieving global IBS symptoms.



A randomized controlled clinical trial of the serotonin type 3 receptor antagonist alosetron in women with diarrhea-predominant irritable bowel syndrome.

Alosetron hydrochloride, 1 mg twice daily for 12 weeks, is effective in relieving pain and some bowel-related symptoms in diarrhea-predominant female patients with IBS.

Effect of renzapride on transit in constipation-predominant irritable bowel syndrome.

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  • Medicine
    Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association
  • 2004

Efficacy of alosetron in irritable bowel syndrome: a meta‐analysis of randomized controlled trials

The present analysis shows that alosetron 1 mg b.i.d. positively impacts global symptoms, and pain and discomfort in non‐constipated IBS female patients.

A randomised controlled trial assessing the efficacy and safety of repeated tegaserod therapy in women with irritable bowel syndrome with constipation

Tegaserod provides rapid and sustained relief of IBS-C symptoms both during first and repeated treatment and produced greater satisfaction, work productivity, and improved quality of life than placebo (p<0.05).

Identification of Patients with Non-D, Non-C Irritable Bowel Syndrome and Treatment with Renzapride: An Exploratory, Multicenter, Randomized, Double-Blind, Placebo-Controlled Clinical Trial

Renzapride was well tolerated and most adverse events were mild to moderate in intensity and further studies are warranted to determine whether renzapride is beneficial in this patient population.

Meta‐analysis: the treatment of irritable bowel syndrome

Evidence is weak to recommend the use of bulking agents in the treatment of irritable bowel syndrome with constipation, but antidepressants can be beneficial for patients with severe symptoms and loperamide can be recommended in painless diarrhoea.

Tegaserod for Female Patients Suffering From IBS With Mixed Bowel Habits or Constipation: A Randomized Controlled Trial

Tegaserod is effective in treating overall IBS symptoms in patients with IBS-Mixed and IBS with constipation and the most frequent adverse events leading to study discontinuation in tegaserod-treated patients were diarrhea and abdominal pain.