oxyphenonium

Summary

Summary: A quaternary ammonium anticholinergic agent with peripheral side effects similar to those of ATROPINE. It is used as an adjunct in the treatment of gastric and duodenal ulcer, and to relieve visceral spasms. The drug has also been used in the form of eye drops for mydriatic effect.

Top Publications

  1. Vlek J, Feitsma K, van der Mark T, Drenth B, Paans A, Vaalburg W. Synthesis of d-[11C]oxyphenonium iodide, a potential radioligand for in vivo visualization of human cholinergic muscarinic receptor-sites by positron emission tomography. Int J Rad Appl Instrum A. 1990;41:453-6 pubmed
    Carbon-11 labeled d-oxyphenonium iodide, a cholinergic antagonist is synthesized for in vivo visualization of muscarinic receptor-sites on airway tissue by positron emission tomography (PET)...
  2. Kirkova M, Alexandova A, Kesiova M, Todorov S. In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems. Comparison with non-selective and COX-2 selective NSAIDs. Auton Autacoid Pharmacol. 2007;27:99-104 pubmed
    ..3. It is suggested that the lack of pro-oxidant effects in vivo associated with amtolmetin guacyl treatment contribute improved gastric tolerability...
  3. Berezina T, Ovsiannikov V. [Mechanisms of inhibition of the contractile activity in the ileo-caecal zone in rabbits under psychogenic stress]. Ross Fiziol Zh Im I M Sechenova. 2005;91:893-902 pubmed
  4. Funasaki N, Kawaguchi R, Hada S, Neya S. Ultraviolet spectroscopic estimation of microenvironments and bitter tastes of oxyphenonium bromide in cyclodextrin solutions. J Pharm Sci. 1999;88:759-62 pubmed
    The UV absorbance and bitter taste of oxyphenonium bromide (OB), an antiacetylcholine drug, in cyclodextrin (CD) solutions are measured, and the local environment of the binding site and the reduction of the bitter taste intensity are ..
  5. Michal P, Lysíková M, Tucek S. Dual effects of muscarinic M(2) acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: dependence on time, receptor density and receptor agonists. Br J Pharmacol. 2001;132:1217-28 pubmed
    ..The stimulatory components disappeared after the density of receptors had been lowered with oxyphenonium mustard. 3. All agonists stimulated the synthesis of cyclic AMP in cells pretreated with pertussis toxin. 4...
  6. Nezhinskaya G, Sapronov N, Vladykin A, Shepeleva V. Effects of cholinotropic and cytostatic drugs on the development of Arthus reaction. Bull Exp Biol Med. 2008;146:747-9 pubmed
    ..Apoptosis of tumor cell and inhibition of inflammation can be essential for chemotherapy of malignant and autoimmune diseases...
  7. el Gindy A, Emara S, Shaaban H. Stability-indicating method for determination of oxyphenonium bromide and its degradation product by high-performance liquid chromatography. J AOAC Int. 2007;90:1250-7 pubmed
    A high-performance liquid chromatographic (HPLC) method was developed for determination of oxyphenonium bromide (OX) and its degradation product...
  8. Nezhinskaya G, Vladykin A, Sapronov N. Cholinergic modulation of anaphylactic shock: plasma proteins influence. Life Sci. 2007;80:2342-6 pubmed
    ..At the pathochemical stage of shock IgG increases the antianaphylactic activity of methacine, but albumin and CRP abolish it...
  9. Funasaki N, Uratsuji I, Okuno T, Hirota S, Neya S. Masking mechanisms of bitter taste of drugs studied with ion selective electrodes. Chem Pharm Bull (Tokyo). 2006;54:1155-61 pubmed
    The masking mechanisms of the bitter taste of propantheline bromide (PB) and oxyphenonium (OB) bromide by native and modified cyclodextrins, saccharides, surfactants, organic acids, nonionic and anionic polymers, and other compounds were ..

More Information

Publications29

  1. Funasaki N, Sumiyoshi T, Ishikawa S, Neya S. Solution structures of 1:1 complexes of oxyphenonium bromide with beta- and gamma-cyclodextrins. Mol Pharm. 2004;1:166-72 pubmed
    The solution structures of complexes of oxyphenonium bromide (OB) with beta- and gamma-cyclodextrins (beta- and gamma-CDs, respectively) in deuterium oxide have been investigated by 500 MHz proton NMR spectroscopy and molecular mechanics ..
  2. Smisterová J, Ensing K, de Zeeuw R. Effect of purification followed by solubilization of receptor material on quantitative receptor assays for anticholinergic drugs. J Pharm Biomed Anal. 1996;14:1425-33 pubmed
    ..for two chemically different anticholinergics, the tertiary amine scopolamine and the quaternary amine oxyphenonium, were calculated from inhibition studies of 3H-NMS binding in buffer and plasma...
  3. Hoener B, Tzika A, Englestad B, White D. Hepatic transport of the magnetic resonance imaging contrast agent Fe(III)-N-(3-phenylglutaryl)desferrioxamine B. Magn Reson Med. 1991;17:509-15 pubmed
    ..In animals pretreated with a saturating dose of taurocholate, oxyphenonium, or bromosulfophthalein (BSP), 25 +/- 6%, 23 +/- 1%, or 1.6 +/- 0...
  4. Ovsiannikov V, Berezina T. [Mechanism of the serotonin effect on motility of the duodenum, ileum, and jejunum in awake rabbits]. Ross Fiziol Zh Im I M Sechenova. 2002;88:1017-27 pubmed
    ..The initial suppression of the motility is caused by participation of nonadrenergic noncholinergic inhibitory mechanism, and the secondary inhibition of contractile activity of a small bowel with serotonin has an adrenergic nature...
  5. Shi W, Hoganson C, Espe M, Bender C, Babcock G, Palmer G, et al. Electron paramagnetic resonance and electron nuclear double resonance spectroscopic identification and characterization of the tyrosyl radicals in prostaglandin H synthase 1. Biochemistry. 2000;39:4112-21 pubmed
    ..Our ENDOR data also indicate that the catalytically active, wide-doublet species is not hydrogen bonded, which may enhance its reactivity toward the fatty-acid substrate bound nearby...
  6. Kuznetsova N, Ovsiannikov V. [Myoelectrical activity in the stomach during ulcerogenic exposure in rabbits]. Ross Fiziol Zh Im I M Sechenova. 1999;85:1560-6 pubmed
    ..Bensohexonium prevented the changes as well as ulceration. Metacin combined with proserin accelerated healing of the ulcer and the rate of stomach myoelectrical activity...
  7. Feitsma K, Postma D, Koeter G, Nossent G, Brenth B, de Zeeuw R. Comparative study of the bronchodilating effects of (-)- and (+)-oxyphenonium bromide. Br J Clin Pharmacol. 1988;25:683-7 pubmed
    1. Racemic oxyphenonium bromide, its enantiomers and placebo were inhaled by eight adult patients with chronic airflow obstruction, in a four-way double-blind cross-over study. 2...
  8. Feitsma K, Drenth B, de Zeeuw R, Oosting R, Meijer D. Unequal disposition of enantiomers of the organic cation oxyphenonium in the rat isolated perfused liver. J Pharm Pharmacol. 1989;41:27-31 pubmed
    ..describes the results of pharmacokinetic experiments in the rat isolated perfused liver with enantiomers of oxyphenonium. The study was performed with the [14C]methyl labelled compounds...
  9. Funasaki N, Ishikawa S, Neya S. Stoichiometric and microenvironmental effects on hydrolysis of propantheline and oxyphenonium bromides in cyclodextrin solutions. J Pharm Sci. 2001;90:740-8 pubmed
    ..of alpha-, beta-, and gamma-cyclodextrins (CDs) on the basic hydrolysis of propantheline bromide (PB) and oxyphenonium bromide (OB) are analyzed in terms of the stoichiometry and microenvironments of their complexes...
  10. Luft W, Ming Y, Stell W. Variable effects of previously untested muscarinic receptor antagonists on experimental myopia. Invest Ophthalmol Vis Sci. 2003;44:1330-8 pubmed
    ..The mechanisms and sites of action of these drugs against myopia are not clear. To shed further light on whether this mechanism is muscarinic, several other muscarinic antagonists were tested...
  11. Kovalenko N, Matsievskii D. Role of cholinergic structures in individual resistance of rat circulatory system to posthemorrhagic hypoxia. Bull Exp Biol Med. 2005;140:177-80 pubmed
    ..Preliminary blockade of peripheral muscarinic cholinoceptors with methacin prevented the decrease in the cardiac output in low resistant animals during the posthemorrhagic period...
  12. Martan A, Sindlar M, Halaska M, Koleska T, Stulc B. [The atropine test in patients with stress incontinence and their treatment with a combination of diltiazem and oxyphenonium]. Cesk Gynekol. 1990;55:406-12 pubmed
    ..were subsequently treated by a combination of dilthiazem (Diacordin), 3 X 30 mg by the oral route per day and oxyphenonium (Oxyphenon dupl.) 2 X 10 mg by the oral route per day...
  13. Nezhinskaya G, Vladykin A, Sapronov N. Blood plasma proteins modulate the broncholytic effects of a muscarinic receptor antagonist. Bull Exp Biol Med. 2008;145:55-7 pubmed
    ..The concentration of serotonin in mesenteric lymph nodes was high during shock...
  14. Ivanov AYa -, Skok V. Neuronal mechanisms responsible for ongoing activity of rabbit superior cervical ganglion neurons. J Auton Nerv Syst. 1992;41:61-6 pubmed
    ..This effect is probably due to the increase in the duration of after-hyperpolarization observed after the application of methacine.(ABSTRACT TRUNCATED AT 250 WORDS)..
  15. Berezina T, Ovsyannikov V. Mechanism for the inhibition of contractile activity of the gastric antrum and pylorus in rabbits during psychogenic stress. Bull Exp Biol Med. 2009;147:296-300 pubmed
    ..It resulted from the influence of a hormonal stress factor on the stomach, which was probably realized through nonadrenergic inhibitory neurons of the enteric nervous system...
  16. Berezina T, Ovsyannikov V. Changes in contractile activity of the large intestine in rabbits during the poststress period before and after blockade of muscarinic and nicotinic receptors. Bull Exp Biol Med. 2013;155:729-33 pubmed
    ..These changes were not observed under conditions of blockade of muscarinic and nicotinic receptors. This state can be considered as dyskinesia impairing large intestinal transit of chyme. ..
  17. Joseph T, Venkataraman V, Nagarani A, David J, Bhatt A, Vaidya A. Safety pharmacology of a combination of tinidazole and oxyphenonium bromide. Arzneimittelforschung. 1997;47:869-72 pubmed
    The effect of a combination of 150 mg tinidazole (CAS 19387-91-8) and 1 mg oxyphenonium bromide (CAS 50-10-2), referred to as the combination, was examined in various animal species to assess its safety...
  18. Martan A, Voigt R, Halaska M. [Drug therapy of urge incontinence in the female]. Zentralbl Gynakol. 1993;115:205-9 pubmed
    ..The results showed that the patients treated by spasmolytics (Oxyphenonium bromatum/Hexasonium jodatum/Papaverin) had the lowest rate of side effects in comparison with the women treated ..
  19. Tripathi S, Griyappanavar C, Lal A, Biswas K, Biswas N, Sankaranarayanan A, et al. Evaluation of antimuscarinic activity in human volunteers: a teaching aid in clinical pharmacology. Indian J Physiol Pharmacol. 1995;39:163-5 pubmed
    The antimuscarinic activity of oxyphenonium bromide, diphenhydramine hydrochloride and astemizole were evaluated in six volunteers. The parameters used were salivary secretion, heart rate and pupillary size...
  20. Scholtmeijer R, van Mastrigt R. The effect of oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux in children with vesicoureteral reflux and detrusor instability. J Urol. 1991;146:660-2 pubmed
    In a prospective study the effects of the anticholinergic drugs oxyphenonium bromide and oxybutynin hydrochloride on detrusor contractility and reflux were studied...