User:Mr. Ibrahem/Alosetron

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Mr. Ibrahem/Alosetron
Clinical data
Pronunciational oh’ se tron
Trade namesLotronex
AHFS/Drugs.comMonograph
MedlinePlusa601230
Routes of
administration
By mouth (tablets)
Drug class5-HT3 receptor blocker[1]
Legal status
Legal status
Pharmacokinetic data
Bioavailability50–60%
Protein binding82%
MetabolismLiver (including CYP2C9, CYP3A4 and CYP1A2)
Elimination half-life1.5–1.7 hours
ExcretionRenal 73%, faecal 24%
Identifiers
  • 5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-1-one
Chemical and physical data
FormulaC17H18N4O
Molar mass294.358 g·mol−1
3D model (JSmol)
  • Cc1nc[nH]c1CN2CCc4c(C2=O)c3ccccc3n4C
  • InChI=1S/C17H18N4O/c1-11-13(19-10-18-11)9-21-8-7-15-16(17(21)22)12-5-3-4-6-14(12)20(15)2/h3-6,10H,7-9H2,1-2H3,(H,18,19) checkY
  • Key:JSWZEAMFRNKZNL-UHFFFAOYSA-N checkY
  (verify)

Alosetron, sold under the brand name Lotronex among others, is a medication used for diarrhea-predominant irritable bowel syndrome (IBS) in women.[1] It should only be used in those with severe disease who cannot be managed with other treatments.[3] It is taken by mouth.[3]

Common side effects include constipation, abdominal pain, and nausea.[2] Other side effects may include bowel obstruction and ischemic colitis.[2] Safety in pregnancy is unclear.[2] It is a 5-HT3 receptor blocker.[1]

Alosetron was patented in 1987 and came into medical use in the 1990s.[4][1] It was temporarily withdrawn in 2000 due to isssues with constipation but was reintroduced in 2002.[1] It is available as a generic medication.[5] In the United States a month costs about 240 USD as of 2022.[5]

References[edit]

  1. ^ a b c d e f "Serotonin 5-HT3 Receptor Antagonists". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Archived from the original on 8 May 2021. Retrieved 14 January 2022.
  2. ^ a b c d "DailyMed - ALOSETRON HYDROCHLORIDE tablet". dailymed.nlm.nih.gov. Archived from the original on 21 April 2021. Retrieved 14 January 2022.
  3. ^ a b "Alosetron Monograph for Professionals". Drugs.com. Archived from the original on 25 January 2021. Retrieved 14 January 2022.
  4. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 448. ISBN 9783527607495. Archived from the original on 2021-09-30. Retrieved 2021-10-11.
  5. ^ a b "Alosetron Prices, Coupons & Savings Tips - GoodRx". GoodRx. Archived from the original on 24 January 2016. Retrieved 14 January 2022.