alosetron

Also known as GR68755, Lotronex®, 2,3,4,5-Tetrahydro-5-methyl-2-((5-methyl-1H-imidazol-4-yl)methyl)-1H-pyrido(4,3-b)indol-1-one

Alosetron, sold under the brand name Lotronex among others, is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in females only.

Key facts

Drug.image: Alosetron.svg
Drug.image_class: skin-invert-image
Drug.width: 222
Drug.image2: Alosetron ball-and-stick model.png
Drug.image_class2: bg-transparent
Drug.tradename: Lotronex
Drug.MedlinePlus: a601230
Drug.DailyMedID: Alosetron
Drug.routes_of_administration: By mouth
Drug.ATC_prefix: A03
Drug.ATC_suffix: AE01
Drug.legal_US: Rx-only
Drug.bioavailability: 50–60%
Drug.protein_bound: 82%
Drug.metabolism: Liver (including CYP2C9, CYP3A4 and CYP1A2)
Drug.elimination_half life: 1.5–1.7 hours
Drug.excretion: Kidney 73%, feces 24%
Drug.CAS_number: 122852-42-0

via Wikipedia infobox

Research

383 papers

Alosetron.Drugs · 2000
Alosetron.2006
Alosetron.2026
Alosetron and irritable bowel syndrome.Expert opinion on pharmacotherapy · 2003
Alosetron for severe diarrhea-predominant irritable bowel syndrome: improving patient outcomes.Current medical research and opinion · 2011

via PubMed

Wikidata facts

Mass: 294.148061

Show 5 more facts

chemical formula: C₁₇H₁₈N₄O
Commons category: Alosetron
canonical SMILES: CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C
World Health Organisation international non-proprietary name: alosetron
defined daily dose: 1

Sources (6)

via Wikidata · CC0

~7 min read

Article

8 sections

Contents

Medical uses
Efficacy
Contraindications
Adverse effects
Mechanism of action
History
Criticism of the FDA
References

Alosetron, sold under the brand name Lotronex among others, is a 5-HT3 antagonist used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in females only.

It was patented in 1987 and approved for medical use in 2002. It is currently marketed by Prometheus Laboratories Inc. (San Diego). Alosetron was withdrawn from the market in 2000 owing to the occurrence of serious life-threatening gastrointestinal adverse effects, but was reintroduced in 2002 with availability and use restricted.