Otilonium bromide

Otilonium bromide is an antimuscarinic and calcium channel blocker used to relieve spasmodic pain of the gut, especially in irritable bowel syndrome.[1]

Otilonium bromide
Clinical data
Trade namesSpasmoctyl 40, Doralin
AHFS/Drugs.comInternational Drug Names
ATC code
Identifiers
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.043.128
Chemical and physical data
FormulaC29H43BrN2O4
Molar mass563.57 g/mol g·mol−1
3D model (JSmol)
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Medical uses

A pooled analysis of three clinical trials suggest that otilonium is more effective than placebo for the treatment of irritable bowel syndrome.[2]

Pharmacology

Otilinium binds to both muscarinic receptors and tachykinin NK2 receptors.[3] It has been shown to inhibit L-type and T-type calcium channels, actions which may contribute to or determine its effects in the gut.[4][5]

When taken orally, very little of the drug is absorbed into the rest of the body,[6] which means that most of its actions remain confined to the gastrointestinal system.

References
  1. "Dismox" (PDF). Archived from the original (PDF) on 4 March 2016.
  2. Clavé, P; Tack, J (March 2017). "Efficacy of otilonium bromide in irritable bowel syndrome: a pooled analysis". Therapeutic advances in gastroenterology. 10 (3): 311–322. doi:10.1177/1756283X16681708. PMC 5305018. PMID 28246548.
  3. Evangelista, S (1999). "Otilonium bromide: a selective spasmolytic for the gastrointestinal tract". The Journal of international medical research. 27 (5): 207–22. doi:10.1177/030006059902700501. PMID 10689627.
  4. Martin, MT; Hove-Madsen, L; Jimenez, M (April 2004). "Otilonium bromide inhibits muscle contractions via L-type calcium channels in the rat colon". Neurogastroenterology & Motility. 16 (2): 175–83. doi:10.1111/j.1365-2982.2004.00518.x. PMID 15086871.
  5. Strege, PR; Sha, L; Beyder, A; Bernard, CE; Perez-Reyes, E; Evangelista, S; Gibbons, SJ; Szurszewski, JH; Farrugia, G (May 2010). "T-type Ca(2+) channel modulation by otilonium bromide". American Journal of Physiology. Gastrointestinal and Liver Physiology. 298 (5): G706–13. doi:10.1152/ajpgi.00437.2009. PMC 2867415. PMID 20203058.
  6. Shin, BS; Kim, JJ; Kim, J; Hu, SK; Kim, HJ; Hong, SH; Kim, HK; Lee, HS; Yoo, SD (January 2008). "Oral bioavailability and enterohepatic recirculation of otilonium bromide in rats". Archives of Pharmacal Research. 31 (1): 117–24. doi:10.1007/s12272-008-1129-2. PMID 18277617.


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