Otilonium bromide

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Otilonium bromide
Otilonium bromide.png
Clinical data
Trade names Spasmoctyl 40, Doralin
AHFS/Drugs.com International Drug Names
ATC code
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, sold under the trade name Spasmomen among others, is an antimuscarinic and calcium channel blocker used to relieve spasmodic pain of the gut, especially in irritable bowel syndrome. [1] 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.

Contents

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.

Related Research Articles

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Irritable bowel syndrome (IBS) is a "disorder of gut-brain interaction" characterized by a group of symptoms that commonly include abdominal pain, abdominal bloating and changes in the consistency of bowel movements. These symptoms may occur over a long time, sometimes for years. IBS can negatively affect quality of life and may result in missed school or work or reduced productivity at work. Disorders such as anxiety, major depression, and chronic fatigue syndrome are common among people with IBS.

An antispasmodic is a pharmaceutical drug or other agent that suppresses muscle spasms.

Chronic functional abdominal pain (CFAP) or functional abdominal pain syndrome (FAPS) is the ongoing presence of abdominal pain for which there is no known medical explanation, and has the potential to interfere with all aspects of daily functioning. It is quite similar to, but less common than, irritable bowel syndrome (IBS), and many of the same treatments for IBS can also be of benefit to those with CFAP. The fundamental difference between IBS and CFAP is that in CFAP, unlike in IBS, there is no change in bowel habits such as constipation or diarrhea. Bowel dysfunction is a necessary diagnostic criterion of IBS.

Functional gastrointestinal disorders (FGID), also known as disorders of gut–brain interaction, include a number of separate idiopathic disorders which affect different parts of the gastrointestinal tract and involve visceral hypersensitivity and motility disturbances.

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T-type calcium channels are low voltage activated calcium channels that become inactivated during cell membrane hyperpolarization but then open to depolarization. The entry of calcium into various cells has many different physiological responses associated with it. Within cardiac muscle cell and smooth muscle cells voltage-gated calcium channel activation initiates contraction directly by allowing the cytosolic concentration to increase. Not only are T-type calcium channels known to be present within cardiac and smooth muscle, but they also are present in many neuronal cells within the central nervous system. Different experimental studies within the 1970s allowed for the distinction of T-type calcium channels from the already well-known L-type calcium channels. The new T-type channels were much different from the L-type calcium channels due to their ability to be activated by more negative membrane potentials, had small single channel conductance, and also were unresponsive to calcium antagonist drugs that were present. These distinct calcium channels are generally located within the brain, peripheral nervous system, heart, smooth muscle, bone, and endocrine system.

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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 and Motility. 16 (2): 175–83. doi:10.1111/j.1365-2982.2004.00518.x. PMID   15086871. S2CID   7315438.
  5. 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): G706-13. doi:10.1152/ajpgi.00437.2009. PMC   2867415 . PMID   20203058.
  6. 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): 117–24. doi:10.1007/s12272-008-1129-2. PMID   18277617. S2CID   25727036.