Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

USA: Lotronex.

Drug combinations


Alosetron Hydrochloride: C~17~H~18~N~4~O.HCl. Mw: 330.81. (1) 1H-Pyrido[4,3-b]indol-1-one, 2,3,4,5-tetrahydro-5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-, monohydrochloride; (2) 2,3,4,5-Tetrahydro-5-methyl-2-[(5-methylimidazol-4-yl)methyl]-1H-pyrido[4,3-b]indol-1-one monohydrochloride. CAS-122852-69-1; CAS-122852-42-0 (alosetron)(1992).

Pharmacologic Category

Anti-Inflammatory Agents; Selective 5-HT~3~ Receptor Antagonist. (ATC-Code: A03AE01).

Mechanism of action

Potent and selective antagonist of the serotonin 5-HT~3~ receptor.

Therapeutic use

Treatment of severe diarrhea-predominant irritable bowel syndrome in women.

Pregnancy and lactiation implications

Should be used in pregnant women only if clearly needed. Caution if administered to a nursing woman.

Unlabeled use


Hypersensitivity to alosetron or any component of the formulation. Constipation. Ischemic colitis. Intestinal obstruction. Stricture. Toxic megacolon. Gastrointestinal perforation and/or adhesions. Diverticulitis. Crohn’s disease. Hepatic dysfunction. Ulcerative colitis. Impaired intestinal circulation, thrombophlebitis, or hypercoagulable state. Concomitant administration with fluvoxamine.

Warnings and precautions

Only indicated for women with severe diarrhea-predominant irritable bowel syndrome with inadequate response to conventional therapy. Risk of constipation. Acute ischemic colitis reported. Avoid use in severe hepatic impairment.



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