Otilonium bromide - CAS 26095-59-0

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Otilonium bromide
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CAS 26095-59-0 Otilonium bromide
Reference Reading
1.Antimuscarinic, calcium channel blocker and tachykinin NK2 receptor antagonist actions of otilonium bromide in the circular muscle of guinea-pig colon
Paolo Santicioli • Vladimir Zagorodnyuk, Anna Rita Renzetti • Carlo Alberto Maggi. Naunyn-Schmiedeberg’s Arch Pharmacol (1999) 359:420–427
Otilonium bromide is a quaternary ammonium derivative used for the treatment of hypermotility and hypersensitivity disorders of the intestine, in particular for treatment of irritable bowel syndrome (IBS; Camilleri and Choi 1997; Poynard et al. 1994 for review). In humans, orally administered otilonium bromide causes a dose-dependent increase of the whole gut transit time and eliminates the exaggerated colonic motor responses produced by physiological stimuli in IBS patients (Narducci et al. 1985; Sutton et al. 1997). A double-blind placebo-controlled study in a large number of IBS patients has established that otilonium bromide is es-pecially effective in relieving abdominal pain/discomfort (Battaglia et al. 1998).
2.IBS and the role of otilonium bromide
Guy Boeckxstaens & Enrico S. Corazziari & Fermín Mearin & Jan Tack. Int J Colorectal Dis (2013) 28:295–304
Antispasmodic agents are a heterogeneous class of agents that decrease the tone and contractility of intestinal smooth muscle. Mechanisms of action vary but divide broadly into those directly affecting intestinal smooth muscle contractility by acting on calcium channels (musculotropic spasmolytics such as otilonium bromide (OB), peppermint oil, pinaverium bromide, and mebeverine) and those with anticholinergic/anti-muscarinic properties such as dicyclomine, hyoscyamine, cimetropium bromide, and prifinium bromide. Unlike musculotropic spasmolytics, which are usually devoid of action outside of the gastrointestinal tract, anticholinergic agents not only act on gastrointestinal smooth muscle (causing constipation), but also bind to muscarinic receptors in other body tissues leading to other anticholinergic effects such as dry mouth, tachycardia, and impaired vision.
3.New and Investigational Agents for Irritable Bowel Syndrome
Akhilesh Wadhwa & Michael Camilleri & Madhusudan Grover. Curr Gastroenterol Rep (2015) 17: 46
Otilonium Bromide Otilonium is a spasmolytic agent that blocks L-type calcium channels in colonic smooth muscle in humans. In a 15-week, double blind, placebo-controlled trial of 356 IBS-D patients, otilonium bromide (40 mg thrice daily) was well tolerated and improved abdominal pain frequency and severity of abdominal bloating. In another 4-week, dose-ranging study, 80mg dose thrice daily dosing of otilonium bromide reduced the frequency of diarrheal episodes while intensity and frequency of abdominal pain or bloating were improved with both 40- and 80-mg thrice daily doses.
4.Oral Bioavailability and Enterohepatic Recirculation of Otilonium Bromide in Rats
Beom Soo Shin, Jung Jun Kim, John Kim, Sul Ki Hu, Han Kyung Kim, Hye Suk Lee, and Sun Dong Yoo. Arch Pharm Res Vol 31, No 1, 117-124, 2008
Otilonium bromide, diethylmethyl{[(octyloxy-2 benzamido)-4 benzoyloxy] 2 ethyl]}ammonium bromide, is a quaternary ammonium derivative possessing potent spasmolytic activity in the gastrointestinal tract (Evangelista, 1999). It has been used to treat abdominal discomfort symptoms accompanied by irritable bowel syndrome (Battaglia et al., 1998; Glende et al., 2002; Evangelista, 2004). Various studies have been conducted to examine the pharmacological action mechanism and therapeutic outcomes of otilonium bromide (Gandia et al., 1996; Sutton et al., 1997; Battaglia et al., 1998; Lindqvist et al., 2002). The spasmolytic action of otilonium bromide has been shown to be mediated by inhibition of calcium ion flux in colonic smooth muscles (Giachetti, 1991; Evangelista, 1999S 2004). When orally administered at doses that produce spasmolytic effects (40-240 mg), otilonium bromide was well tolerated without central and peripheral atropine-like adverse reactions (Sutton et al., 1997). In studies of C-otilonium bromide in rats, high accumulation of radioactivity was found in intestinal tissues (Amenta et al., 1991; Evangelista et al., 2000). A trace amount of radioactivity was found only in the liver among various tissues including kidney, lung and muscle (Evangelista et al., 2000). The systemic absorption of otilonium bromide was suggested to be low after oral administration (Signorini et al., 1984; Evangelista et al., 2000). Information on the extent of systemic absorption and pharmacokinetic disposition of otilonium bromide is limited, primarily due to a lack of sensitive assay for the determination of otilonium in biological samples. To date, several assay methods are available for the determination of otilonium, including first-derivative spectroscopy (Mannucci et al., 1992), HPLC (Signorini et al., 1984; Mannucci et al., 1992, 1993), spectrophotometry (El-Kousy and Bebawy 1999) and capillary zone electrophoresis (Furlanetto et al., 2001).
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