Tegaserod

• Irritable Bowel Syndrome with Constipation (IBS-C): Approved for adult women under 65 years with IBS-C characterized by abdominal pain and constipation.
• Chronic Idiopathic Constipation (CIC): Indicated for adults with CIC who have not responded adequately to laxatives.

• Adults: 6 mg orally twice daily, 30 minutes before meals.
• Elderly: Use with caution; no specific dose adjustment recommended.
• Pediatrics: Safety and efficacy not established.
• Renal/Hepatic impairment: Use cautiously; no clear dose adjustments.
• Administration: Oral tablets; taken 30 minutes prior to meals.

Tegaserod acts as a selective partial agonist at 5-HT4 receptors in the gastrointestinal tract, stimulating peristalsis by enhancing acetylcholine release. It promotes gastrointestinal motility and secretion, leading to accelerated transit and relief from constipation and abdominal discomfort.

• Absorption: Rapid, peak plasma concentration within 1.5 hours.
• Bioavailability: ~10%, reduced by first-pass metabolism.
• Distribution: Extensive tissue binding.
• Metabolism: Hepatic glucuronidation and oxidation.
• Half-life: Approximately 11 hours.
• Elimination: Mainly feces (~65%) and urine (~30%) as metabolites.

• Pregnancy: Limited data; use only if benefits outweigh risks.
• Lactation: Unknown if excreted in milk; caution advised, breastfeeding not recommended.

• Gastrointestinal agent; selective 5-HT4 receptor agonist.

• Hypersensitivity to tegaserod.
• History of myocardial infarction, stroke, transient ischemic attack, or angina.
• Severe renal or hepatic impairment.
• GI obstruction, perforation, adhesions.
• History of intestinal ischemia or significant cardiovascular disease.

·         Increased cardiovascular risk; avoid in patients with known heart disease.

·         Risk of severe diarrhea and ischemic colitis.

·         Monitor for hypersensitivity reactions.

·         Not recommended for men or women over 65.

·         Use cautiously in hepatic or renal impairment.

• Common: Diarrhea, abdominal pain, flatulence, nausea.
• Serious: Ischemic colitis, cardiovascular events (rare).
• Side effects usually appear early and are dose-dependent.

·         Caution with serotonergic drugs.

·         Possible additive effects with other prokinetics.

·         Metabolized by CYP enzymes; interactions rare but possible.

·         No significant food or alcohol interactions.

• FDA re-approved in 2019 with restricted use.
• Indicated only for women under 65 without cardiovascular risk.
• Emphasis on cardiovascular risk assessment prior to therapy.

• Store at 20°C to 25°C.
• Protect from moisture and light.
• Keep container tightly closed.
• No refrigeration needed.