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Tegaserod

ZELNORM

Pronunciation: te-GAS-a-rod (ZEL-norm)

Tegaserod ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Tegaserod ballicule

What it is5-HT4 partial agonist; IBS with constipation in women under 65.

Why this oneIt accelerates transit and relieves pain in constipation-predominant IBS.

What limits itWithdrawn in 2007 for ischemic cardiovascular events, then reintroduced with restriction to low-risk women.

Tegaserod molecular structure (skeletal formula)
Molecular structure: Tegaserod

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
IBS with constipation (IBS-C)Women <65 yr6 mg BID6 mg BID6 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

Available strengths

Contraindications

Cautions

Adverse reactions

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#/mogeneric $/moCostPlus
6 mgtab60 BIDnot 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.

NO BOXED WARNINGS

Principal riskWithdrawn in 2007 for ischemic cardiovascular events, then reintroduced with restriction to low

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryB

Defining liabilityCardiovascular ischemia and ischemic colitis

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