Ballicules › Drugs › Tegaserod
Pronunciation: te-GAS-a-rod (ZEL-norm)
Mechanism of action: Tegaserod ballicule
What it is 5-HT4 partial agonist; IBS with constipation in women under 65.
Why this one It accelerates transit and relieves pain in constipation-predominant IBS.
What limits it Withdrawn in 2007 for ischemic cardiovascular events, then reintroduced with restriction to low-risk women.
Molecular structure: Tegaserod
FDA-approved for
IBS with constipation (2002 — withdrawn 2007, reintroduced 2019)
FDA label
Read the full label on DailyMed ↗
FDA dosing Population Start Target Max
IBS with constipation (IBS-C) Women <65 yr 6 mg BID 6 mg BID 6 mg BID
Renal Contraindicated if severe (eGFR <15) or ESRD; no adjustment for mild-moderate (eGFR ≥30)
Hepatic Contraindicated if moderate-severe (Child-Pugh B or C); no adjustment for mild
Instructions Take orally ≥30 minutes before meals Discontinue if inadequate symptom control after 4–6 weeks
Available strengths
Contraindications History of MI, stroke, TIA, or angina History of ischemic colitis or other intestinal ischemia Severe renal impairment (eGFR <15) or ESRD Moderate/severe hepatic impairment (Child-Pugh B or C) History of bowel obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, or abdominal adhesions
Cautions Cardiovascular ischemic events including MACE — assess CV history/risk before use; discontinue if MI/stroke/TIA/angina Ischemic colitis — discontinue if rectal bleeding, bloody diarrhea, or new/worsening abdominal pain; do not reinitiate Volume depletion from diarrhea (hypovolemia, hypotension, syncope) — avoid in patients with diarrhea Suicidal ideation and behavior — monitor for worsening depression
Adverse reactions Headache, abdominal pain, nausea, diarrhea, flatulence, dyspepsia, dizziness
Pregnancy Available data have not identified a drug-associated risk of major birth defects or miscarriage
Lactation Breastfeeding not recommended during treatment (present in rat milk; tumorigenicity concern)
Cost Tegaserod (ZELNORM)
Strength #/mo generic $/mo CostPlus 6 mg tab 60 BID not offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Tegaserod is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.
Principal risk Withdrawn in 2007 for ischemic cardiovascular events, then reintroduced with restriction to low
Classes and tags
Clinical profile
Therapeutic safety burden 2 / 4
Overdose danger 1 / 4
QT / Torsades 0 / 4
Direct muscarinic antagonism 0 / 4
Embryofetal risk 2 / 4
Legacy pregnancy category B
Defining liability Cardiovascular ischemia and ischemic colitis
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