Tegaserod
💊 Brand Formulations & Prices
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📖 Official Clinical Monograph
DGDA Approved Prescribing GuidelinesTegazel tablet is indicated for the treatment of adult women less than 65 years of age with irritable bowel syndrome with constipation (IBS-C).
Tegaserod is contraindicated in patients with:
A history of myocardial infarction (MI), stroke, transient ischemic attack (TIA), or angina
A history of ischemic colitis or other forms of intestinal ischemia
Severe renal impairment (eGFR< 15 mL/min/1.73 m2) or end-stage renal disease
Moderate and severe hepatic impairment
A history of bowel obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, or abdominal adhesions
Hypersensitivity to tegaserod.
Most common adverse reactions (>2%) are headache, abdominal pain, nausea, diarrhea, flatulence, dyspepsia, and dizziness.
Cardiovascular Ischemic Events, Including Major Adverse Cardiovascular Events (MACE)
: The potential risks of treatment must be balanced with expectations in improvements in symptoms of IBS-C. Discontinue Tegazel treatment in patients who experience a myocardial infarction, stroke, transient ischemic attack or angina. Evaluate the risks and benefits of continued treatment in patients who develop clinical or other evidence of cardiovascular ischemic heart disease and/or experience changes in health status that could increase cardiovascular risk during treatment.
Ischemic Colitis
: Monitor for rectal bleeding, bloody diarrhea, and new or worsening abdominal pain and discontinue Tegazel if symptoms develop.
Volume Depletion Associated with Diarrhea
: Avoid use in patients with severe diarrhea. Instruct patients to discontinue Tegazel and contact their healthcare provider if severe diarrhea, hypotension or syncope occur.
Suicidal Ideation and Behavior
: Monitor patients for clinical worsening of depression and emergence of suicidal thoughts and behaviors, especially during the initial few months of treatment. Instruct patients to immediately discontinue Tegazel and contact their healthcare provider if their depression is persistently worse or they are experiencing emergent suicidal thoughts or behaviors.
Tegaserod is an agonist of serotonin type-4 (5-HT4) receptors that stimulates the peristaltic reflex and intestinal secretion, inhibits visceral sensitivity, enhances basal motor activity, and normalizes impaired motility throughout the gastrointestinal tract. Based on in vitro binding affinity and functional assessment, at clinically relevant plasma concentrations, tegaserod is an antagonist at 5-HT2B receptors in humans. It is expected to have minimal binding to 5-HT1 receptors. Tegaserod has no affinity for 5-HT3 or dopamine receptors. The main metabolite, M29, has negligible affinity for 5-HT4 receptors in vitro. In vivo studies showed that tegaserod enhanced basal motor activity and normalized impaired motility throughout the gastrointestinal tract. In addition, studies demonstrated that tegaserod moderated visceral sensitivity during colorectal distension in animals.