Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Latin America

Brazil: Zelmac; Mexico: Zelmac.

Drug combinations


Tegaserod Maleate: C~16~H~23~N~5~O C~4~H~4~O~4~. Mw: 417.46. (1) Hydrazinecarboximidamide, 2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentyl-, (2Z)-2-butenedioate (1:1); (2) 3-(5-Methoxy-1H-indol-3-ylmethylene)-N-pentylcarbazimidamide hydrogen maleate. CAS-189188-57-6 (2002).

Pharmacologic Category

GI Drugs, Miscellaneous; Serotonin 5-HT~4~ Receptor Agonist. (ATC-Code: A03AE02).

Mechanism of action

A partial neuronal 5-HT~4~ receptor agonist. Its action at receptor site leads to stimulation of peristaltic reflex and intestinal secretion, and moderation of visceral sensitivity.

Therapeutic use

Emergency treatment of irritable bowel syndrome with constipation and chronic idiopathic constipation in women (<55 years of age) in which no alternative therapy exists.

Pregnancy and lactiation implications

Use during pregnancy only if clearly needed. Not recommended in nursing women.

Unlabeled use


Treatment should not be started with diarrhea or in patients who experience diarrhea frequently. Severe renal impairment. Moderate or severe hepatic impairment. History of intestinal obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, or abdominal adhesions. Known hypersensitivity to tegaserod or any ingredient in the formulation.

Warnings and precautions

Serious cardiovascular events (e.g. MI, stroke, unstable angina) may occur. Diarrhea may occur after start of treatment (serious consequences of diarrhea (hypovolemia, syncope) reported). Use associated with rare intestinal ischemic events. Use not permitted in the following situations: unstable angina, history of MI or stroke, hyperlipidemia, cigarette smoking, hypertension, or obesity, depression or anxiety, or any signs of suicidal ideation or behavior, and in diabetes. Use with caution in mild hepatic impairment. Not recommended with moderate or severe impairment.



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