Which medications in the drug class IBS Agents are used in the treatment of Irritable Bowel Syndrome (IBS)?

Updated: Dec 11, 2019
  • Author: Jenifer K Lehrer, MD; Chief Editor: BS Anand, MD  more...
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IBS Agents

Linaclotide and lubiprostone enhance chloride-rich intestinal fluid secretions without altering the sodium and potassium concentrations in the serum. Linaclotide was approved by the FDA in August 2012 to treat chronic idiopathic constipation and irritable bowel syndrome with constipation (IBS-C) in adults. [60]

The safety and efficacy of linaclotide in the treatment of IBS-C were evaluated in 2 double-blind, placebo-controlled phase III clinical trials in which linaclotide met all four primary endpoints for changes in abdominal pain and constipation in each trial. The trials involved 1,605 patients aged 18-87 years, of which 807 were treated with linaclotide 290 mcg. Both trials showed a significantly higher proportion of responders in the linaclotide group compared with the placebo group. [60, 61, 62]

Tenapanor, an inhibitor of sodium-hydrogen exchange (NHE3) transporter, was approved in September 2019 for IBS-C. Approval was based on two phase III trials (N = 1226) that showed a statistically significant improvement in stool frequency and abdominal pain compared with those who received placebo. [6]

Lubiprostone (Amitiza)

This agent activates chloride channels on the apical part of the small bowel epithelium. As a result, chloride ions are secreted and sodium and water passively diffuse into the lumen to maintain isotonicity. This medication is FDA approved for use in idiopathic constipation and in irritable bowel syndrome with constipation.

Linaclotide (Linzess)

Guanylate cyclase agonist; activation of guanylate cyclase receptors in the intestinal neurons leads to increased cyclic guanosine monophosphate (cGMP), anion secretion, fluid secretion, and intestinal transit; it appears to work topically rather than systemically; when administered PO, linaclotide activates chloride channels in intestinal epithelial cells to increase intestinal fluid secretion; indicated to treat chronic idiopathic constipation and for IBS-C in adults.

Plecanatide (Trulance)

Plecanatide is a guanylate cyclase C (GC-C) agonist. Plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of intestinal epithelial cells. GC-C activation leads to increased cyclic guanosine monophosphate (cGMP), which, in turn, stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly by activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. It is indicated for IBS-C in adults.

Alosetron (Lotronex)

Alosetron is a 5-HT3 receptor antagonist. This agent controls irritable bowel syndrome symptoms through its potent and selective antagonism of serotonin 5-HT3 receptor type. These receptors are extensively located on the enteric neurons of the GI tract, and stimulation causes hypersensitivity and hyperactivity of the intestine. It is indicated only for women with severe diarrhea-predominant IBS who have: chronic IBS symptoms (generally lasting 6 months or longer), had anatomic or biochemical abnormalities of the GI tract excluded, and have not responded adequately to conventional therapy.

Limiting its use to this severely affected population is intended to maximize the benefit-to-risk ratio. The drug was previously removed from the US market but was reintroduced with new restrictions approved by the FDA on June 7, 2002. Restrictions are because of reports of infrequent but serious GI adverse reactions (eg, ischemic colitis, serious complications of constipation), including some that resulted in hospitalization and, rarely, blood transfusion, surgery, or death. In order to prescribe, physicians must be enrolled in the Prescribing Program for Lotronex.

Under the new management plan, serious adverse events have been few. [28]

Tegaserod (Zelnorm)

Tegaserod is a serotonin type-4 (5-hydroxytryptamine-4 [5-HT4]) receptor partial agonist. It stimulates the peristaltic reflex and intestinal secretions, inhibits visceral sensitivity, enhances basal motor activity, and normalizes impaired motility throughout the gastrointestinal tract. It is indicated for adult women younger than 65 years who have irritable bowel syndrome with constipation (IBS-C). Its use is further restricted to women without a history of cardiovascular risk.

Eluxadoline (Viberzi)

Eluxadoline is a mu opioid receptor agonist. It also is a delta opioid receptor antagonist and a kappa opioid receptor agonist. The multiple opioid activity is designed to treat the symptoms of IBS-D while reducing the incidence of constipation that can occur with unopposed mu opioid receptor agonists. It is indicated for IBS-D in adult men and women.

Tenapanor (Ibsrela)

Tenapanor is a locally acting inhibitor of the sodium/hydrogen exchanger 3 (NHE3), an antiporter expressed on the apical surface of the small intestine and colon primarily responsible for absorption of dietary sodium. NHE3 inhibition reduces sodium absorption from the small intestine and colon, resulting in an increase in water secretion into the intestinal lumen, which accelerates intestinal transit time and results in a softer stool consistency. It is indicated for adults with IBS-C.

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