Otilonium bromide

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Otilonium bromide
Otilonium bromide.png
Clinical data
Trade names Spasmoctyl 40, Doralin, Menoctyl
AHFS/Drugs.com International Drug Names
ATC code
Pharmacokinetic data
Bioavailability 1.1% [1] [ unreliable source? ]
Identifiers
  • N,N-Diethyl-N-methyl-2-(4-[2-(octyloxy)benzamido]benzoyloxy)ethanaminium bromide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard 100.043.128 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C29H43BrN2O4
Molar mass 563.577 g·mol−1
3D model (JSmol)
  • CCCCCCCCOC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)OCC[N+](C)(CC)CC.[Br-]
  • InChI=1S/C29H42N2O4.BrH/c1-5-8-9-10-11-14-22-34-27-16-13-12-15-26(27)28(32)30-25-19-17-24(18-20-25)29(33)35-23-21-31(4,6-2)7-3;/h12-13,15-20H,5-11,14,21-23H2,1-4H3;1H X mark.svgN
  • Key:VWZPIJGXYWHBOW-UHFFFAOYSA-N X mark.svgN
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Otilonium bromide is a drug used to treat abdominal pain caused by irritable bowel syndrome. It is an antispasmodic, which is useful to treat the symptoms of irritable bowel syndrome by reducing abdominal spasms (colic), bloating, pain, and gut motility.

Contents

It is an antimuscarinic and calcium channel blocker used to relieve spasmodic pain of the gut, especially in irritable bowel syndrome. [2] This means it works in the gut themselves, by relaxing the small muscles of the intestines, which results in relieving cramps and therefore reduces pain.

Medical uses

A pooled analysis of three clinical trials suggest that otilonium bromide is more effective than placebo for the treatment of irritable bowel syndrome. [3]

Pharmacology

Otilonium bromide binds to both muscarinic receptors and tachykinin NK2 receptors. [4] 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. [5] [6]

When taken orally, very little of the drug is absorbed into the rest of the body, [7] which means that most of its actions remain confined to the gastrointestinal system.

Adverse effects

Otilonium bromide is generally well tolerated and does not have the side-effects observed with similar classes of drugs. [8] A case of cardiovascular toxicity was reported due to an overdose. [9] [10]

References

  1. ↑ Shin BS, Kim JJ, Kim J, Hu SK, Kim HJ, Hong SH, et al. (January 2008). "Oral bioavailability and enterohepatic recirculation of otilonium bromide in rats". Archives of Pharmacal Research. 31 (1): 117–124. doi:10.1007/s12272-008-1129-2. PMID   18277617.
  2. ↑ "Dismox" (PDF). Archived from the original (PDF) on 4 March 2016.
  3. ↑ 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.
  4. ↑ Evangelista S (1999). "Otilonium bromide: a selective spasmolytic for the gastrointestinal tract". The Journal of International Medical Research. 27 (5): 207–222. doi: 10.1177/030006059902700501 . PMID   10689627.
  5. ↑ Martin MT, Hove-Madsen L, Jimenez M (April 2004). "Otilonium bromide inhibits muscle contractions via L-type calcium channels in the rat colon". Neurogastroenterology and Motility. 16 (2): 175–183. doi:10.1111/j.1365-2982.2004.00518.x. PMID   15086871. S2CID   7315438.
  6. ↑ Strege PR, Sha L, Beyder A, Bernard CE, Perez-Reyes E, Evangelista S, et al. (May 2010). "T-type Ca(2+) channel modulation by otilonium bromide". American Journal of Physiology. Gastrointestinal and Liver Physiology. 298 (5): G706 –G713. doi:10.1152/ajpgi.00437.2009. PMC   2867415 . PMID   20203058.
  7. ↑ Shin BS, Kim JJ, Kim J, Hu SK, Kim HJ, Hong SH, et al. (January 2008). "Oral bioavailability and enterohepatic recirculation of otilonium bromide in rats". Archives of Pharmacal Research. 31 (1): 117–124. doi:10.1007/s12272-008-1129-2. PMID   18277617. S2CID   25727036.
  8. ↑ Evangelista S (November 2004). "Quaternary ammonium derivatives as spasmolytics for irritable bowel syndrome". Current Pharmaceutical Design. 10 (28): 3561–3568. doi:10.2174/1381612043382972. PMID   15579053.
  9. ↑ Zaki SA, Helal ME, Rashid A (March 2022). "Cardiovascular Toxicity Due to Otilonium Bromide Overdose: A Case Report". The Journal of Emergency Medicine. 62 (3): e47 –e50. doi:10.1016/j.jemermed.2021.10.025. PMID   35031171.
  10. ↑ "Submission for the classification of Otilonium bromide 40 mg film-coated tables (10 and 30 tablet pack) as Pharmacist Only" (PDF). Arai BioFarma Limited.
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