Drug reference
tegaserod
5HT4 partial agonist · Prokinetic agent
5HT4 partial agonistProkinetic agentATC A03AE02
CDSCO approvedATC A03AE02
EXCRETION
—
not curated
INTERACTIONS
—
none in our sources
PREGNANCY
—
not curated
Mechanism
Tegaserod is an aminoguanidine indole that acts as a partial 5HT4 agonist. It stimulates motility and accelerates transit in the esophagus, stomach, small bowel, and ascending colon, and stimulates Cl– secretion.
Indications
Constipation-predominant IBS (in women under 65 who fail first-line therapies)IBS with mixed bowel habits (in female patients who fail other therapies)
Dosing
- Adult
- 6 mg orally, twice a day and 30 min before meals. Discontinue if adequate symptom control not obtained in 4 to 6 weeks.
Pharmacokinetics
Peak effect
About 1 h
Half-life
5 to 8 h
Metabolism
Hydrolysis and direct glucuronidation
Excretion
Primarily in feces as unchanged drug; remainder in urine as metabolites
Contraindications
- History of myocardial infarction
- Stroke
- Transient ischemic attacks
- Angina
- Ischemic colitis
- Severe renal impairment
- Moderate or severe hepatic impairment
- Bowel obstruction
- Gallbladder disease
Side effects
Common
DiarrheaHeadacheAbdominal painNauseaFlatulenceDyspepsiaDizziness
Serious
- Volume depletion, hypotension, and syncope associated with diarrhea
- Suicidal ideation (warning, based on clinical trials)
- Ischemic colitis
Related guidelines
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Sources: Goodman & Gilman 14e·Verified: 2026-05-10 · House clinical team