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Chemical Compound Review

Bretylum     (2-bromophenyl)methyl-ethyl- dimethyl-azanium

Synonyms: Bretylium, CHEBI:3172, CHEMBL1199080, BSPBio_000904, CID2431, ...
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Disease relevance of Bretylol


High impact information on Bretylol


Chemical compound and disease context of Bretylol


Biological context of Bretylol

  • Inhibition of gastric emptying induced by central administration of CRF was completely abolished by pretreatment of the animals with either the ganglionic blocking agent chlorisondamine or the opioid antagonist naloxone, or by noradrenergic blockade with bretylium, but not by truncal vagotomy [14].
  • At the distal segment only Phe produced a vasodilatation of +23 +/- 1%; YO counteracted constriction (from -16 +/- 2% to +9 +/- 6%, P < .05 versus basal), whereas after Pro+Phe and Bre, the vasoconstriction persisted [15].
  • The use of different antiadrenergic drugs showed that Phe counteracts post-PTCA vasoconstriction, and the simultaneous use of alpha- and beta-receptor blocking agents (Pro+Phe and Bre) reveals the presence of a peripheral, predominant beta-mediated dilatation [15].
  • In adrenal demedullated rats, the systemic hemodynamic effects of i.c.v. TRH were diminished along with the decrease in renal blood flow and increase in renal vascular resistance; however, the increase in hindquarter blood flow was attenuated only in adrenal demedullated rats pretreated with the sympathetic blocker bretylium [16].
  • Administration of bretylium, an antihypertensive and anti-arrhythmic agent, resulted in reduction of blood pressure and the severities of glomerulonephritis, DVD, and MI; it also slightly reduced the levels of circulating immune complexes and leukocytosis [17].

Anatomical context of Bretylol

  • However, animals treated with bretylium had an improved outcome for a given amount of myocardium at risk [18].
  • Twenty-five dogs were given 10 mg/kg infusions of bretylium over 10 min, subjected to a 20 min proximal left anterior descending coronary artery ligation followed by sudden release, and compared with 25 animals given saline placebo [18].
  • To find out whether the active vasodilator system is under baroreceptor control, laser-Doppler velocimetry and the local iontophoresis of bretylium were combined to allow selective study of the active vasodilator system [10].
  • The first electrophysiologic action appears to depend on catecholamine release by bretylium, as hyperpolarization was not observed in reserpine-pretreated Purkinje fibers [19].
  • In aorta and vas deferens, about 45% and 65%, respectively, of the total [3H]XYL accumulation was blocked by 100 mumol/L desmethylimipramine (DMI), l-NA, or bretylium [20].

Associations of Bretylol with other chemical compounds

  • In contrast, the hindquarter vasodilation produced by the NO donor sodium nitroprusside (4 micrograms/kg i.v.) was markedly exaggerated in the bretylium- or L-NAME-treated rats [21].
  • When exercise was performed after brachial artery administration of bretylium (to block noradrenaline release) and phentolamine (an alpha-adrenergic antagonist), profound vasodilatation was seen in the resting forearm during both exercise and post-exercise ischaemia [22].
  • To determine whether ischaemic tissue is more sensitive than normal tissue to class III anti-arrhythmic agents, we studied the effects of the class III agents clofilium, d-sotalol and bretylium on normal and ischaemic Purkinje fibres one day after ligation of canine left anterior descending coronary artery [23].
  • Quinidine-induced long QT interval did not change after bretylium (358 +/- 37 vs 348 +/- 26 ms) when transiently elevated blood pressure returned to the pre-bretylium level [24].
  • Previous CPR studies from our laboratory have shown that a standard iv dose of lidocaine (2 mg/kg) has a rapid antifibrillatory effect, while a standard dose of bretylium (5 mg/kg) produces a delayed but more pronounced effect [25].

Gene context of Bretylol

  • Therefore the interactions between bretylium and other drugs (including other antiarrhythmic drugs) is primarily through the pharmacodynamic mechanism.Dofetilide is metabolised by CYP3A4 and excreted by the renal cation transport system [26].
  • It has been demonstrated that bretylium, a quaternary ammonium ion, can significantly inhibit the first pathway at the same dose range that stimulates cell activation through the IL-2 receptor system [27].
  • Ganglionic blockade with chlorisondamine chloride, noradrenergic blockade with bretylium, or adrenalectomy abolished the gastric inhibitory action of CRF whereas truncal vagotomy or opiate blockade with naloxone did not [28].
  • During the application of LBNP in normothermia, cutaneous vascular conductance (CVC) fell at untreated sites by 22.7 +/- 4.7% (p less than 0.01) but was unaffected at bretylium-treated sites (p greater than 0.20) [10].
  • Hexamethonium (20 mg/kg) also prevented 3-h cold exposure-induced myenteric Fos expression by 76-80%, whereas atropine or bretylium had no effect [29].

Analytical, diagnostic and therapeutic context of Bretylol


  1. Pharmacokinetics of bretylium in renal insufficiency. Adir, J., Narang, P.K., Josselson, J., Sadler, J.H. N. Engl. J. Med. (1979) [Pubmed]
  2. Bretylium tosylate: a newly available antiarrhythmic drug for ventricular arrhythmias. Heissenbuttel, R.H., Bigger, J.T. Ann. Intern. Med. (1979) [Pubmed]
  3. Randomized, double-blind comparison of intravenous amiodarone and bretylium in the treatment of patients with recurrent, hemodynamically destabilizing ventricular tachycardia or fibrillation. The Intravenous Amiodarone Multicenter Investigators Group. Kowey, P.R., Levine, J.H., Herre, J.M., Pacifico, A., Lindsay, B.D., Plumb, V.J., Janosik, D.L., Kopelman, H.A., Scheinman, M.M. Circulation (1995) [Pubmed]
  4. Polymorphous ventricular tachycardia associated with acute myocardial infarction. Wolfe, C.L., Nibley, C., Bhandari, A., Chatterjee, K., Scheinman, M. Circulation (1991) [Pubmed]
  5. A nitric oxide-like factor mediates nonadrenergic-noncholinergic neurogenic relaxation of penile corpus cavernosum smooth muscle. Kim, N., Azadzoi, K.M., Goldstein, I., Saenz de Tejada, I. J. Clin. Invest. (1991) [Pubmed]
  6. Cerebroventricular calcitonin gene-related peptide inhibits rat duodenal bicarbonate secretion by release of norepinephrine and vasopressin. Lenz, H.J., Brown, M.R. J. Clin. Invest. (1990) [Pubmed]
  7. Psychological stress-induced accelerated colonic transit in rats involves hypothalamic corticotropin-releasing factor. Mönnikes, H., Schmidt, B.G., Taché, Y. Gastroenterology (1993) [Pubmed]
  8. Central action of recombinant interleukin-1 to inhibit acid secretion in rats. Saperas, E.S., Yang, H., Rivier, C., Taché, Y. Gastroenterology (1990) [Pubmed]
  9. Peptidergic (enkephalin) innervation of the mammalian esophagus. Uddman, R., Alumets, J., Håkanson, R., Sundler, F., Walles, B. Gastroenterology (1980) [Pubmed]
  10. Baroreflex control of the cutaneous active vasodilator system in humans. Kellogg, D.L., Johnson, J.M., Kosiba, W.A. Circ. Res. (1990) [Pubmed]
  11. Bethanidine sulfate: efficacy in prevention of ventricular tachyarrhythmias during programmed stimulation. Report of a multicenter study of 56 patients. Teichman, S.L., Waspe, L.E., Matos, J.A., Kim, S.G., Fisher, J.D. J. Am. Coll. Cardiol. (1985) [Pubmed]
  12. Changes in canine ventricular fibrillation threshold induced by verapamil, flecainide and bretylium. Quesada, A., Sanchis, J., Chorro, F.J., Burguera, M.A., Alberola, A., Such, L., Lopez-Merino, V. Eur. Heart J. (1993) [Pubmed]
  13. Broad sensitivity of rodent arrhythmia models to class I, II, III, and IV antiarrhythmic agents. Brooks, R.R., Miller, K.E., Carpenter, J.F., Jones, S.M. Proc. Soc. Exp. Biol. Med. (1989) [Pubmed]
  14. Central nervous system effects of corticotropin-releasing factor on gastrointestinal transit in the rat. Lenz, H.J., Burlage, M., Raedler, A., Greten, H. Gastroenterology (1988) [Pubmed]
  15. Coronary vasoconstriction after percutaneous transluminal coronary angioplasty is attenuated by antiadrenergic agents. Gregorini, L., Fajadet, J., Robert, G., Cassagneau, B., Bernis, M., Marco, J. Circulation (1994) [Pubmed]
  16. Hemodynamic and neural mechanisms of action of thyrotropin-releasing hormone in the rat. Sirén, A.L., Lake, C.R., Feuerstein, G. Circ. Res. (1988) [Pubmed]
  17. The role of hypertension in the vascular disease and myocardial infarcts associated with murine systemic lupus erythematosus. Hang, L., Stephens-Larson, P., Henry, J.P., Dixon, F.J. Arthritis Rheum. (1983) [Pubmed]
  18. A method for quantitating antifibrillatory effects of drugs after coronary reperfusion in dogs: improved outcome with bretylium. Wenger, T.L., Lederman, S., Starmer, C.F., Brown, T., Strauss, H.C. Circulation (1984) [Pubmed]
  19. Membrane action and catecholamine release action of bretylium tosylate in normoxic and hypoxic canine Purkinje fibers. Nishimura, M., Watanabe, Y. J. Am. Coll. Cardiol. (1983) [Pubmed]
  20. [3H]Xylamine accumulation by two sympathetically innervated tissues. Ransom, R.W., Waggaman, L.A., Cho, A.K. J. Neurochem. (1984) [Pubmed]
  21. Nitrosyl factors mediate active neurogenic hindquarter vasodilation in the conscious rat. Davisson, R.L., Johnson, A.K., Lewis, S.J. Hypertension (1994) [Pubmed]
  22. Evidence for nitric oxide-mediated sympathetic forearm vasodiolatation in humans. Dietz, N.M., Engelke, K.A., Samuel, T.T., Fix, R.T., Joyner, M.J. J. Physiol. (Lond.) (1997) [Pubmed]
  23. The differential response of normal and ischaemic Purkinje fibres to clofilium, d-sotalol and bretylium. Gough, W.B., el-Sherif, N. Cardiovasc. Res. (1989) [Pubmed]
  24. Effects of bretylium tosylate on inhomogeneity of refractoriness and ventricular fibrillation threshold in canine hearts with quinidine-induced long QT interval. Inoue, H., Toda, I., Nozaki, A., Matsuo, H., Sugimoto, T. Cardiovasc. Res. (1985) [Pubmed]
  25. Antifibrillatory effects of high dose bretylium and a lidocaine-bretylium combination during cardiopulmonary resuscitation. Hanyok, J.J., Chow, M.S., Kluger, J., Fieldman, A. Crit. Care Med. (1988) [Pubmed]
  26. Potentially significant drug interactions of class III antiarrhythmic drugs. Yamreudeewong, W., DeBisschop, M., Martin, L.G., Lower, D.L. Drug safety : an international journal of medical toxicology and drug experience. (2003) [Pubmed]
  27. Bretylium differentiates between distinct signal transducing pathways in human lymphocytes. Pieri, C., Bacsó, Z., Recchioni, R., Moroni, F., Balázs, M., Gáspár, R., Damjanovich, S. Biochem. Biophys. Res. Commun. (1993) [Pubmed]
  28. Pathways mediating CRF-induced inhibition of gastric acid secretion in rats. Drüge, G., Raedler, A., Greten, H., Lenz, H.J. Am. J. Physiol. (1989) [Pubmed]
  29. Acute cold exposure induces vagally mediated Fos expression in gastric myenteric neurons in conscious rats. Yuan, P.Q., Taché, Y., Miampamba, M., Yang, H. Am. J. Physiol. Gastrointest. Liver Physiol. (2001) [Pubmed]
  30. Drug therapy: bretylium. Koch-Weser, J. N. Engl. J. Med. (1979) [Pubmed]
  31. Paradoxical ventricular tachycardia and fibrillation after intravenous bretylium therapy. Report of two cases. Anderson, J.L., Popat, K.D., Pitt, B. Arch. Intern. Med. (1981) [Pubmed]
  32. Bretylium kinetics in renal insufficiency. Josselson, J., Narang, P.K., Adir, J., Yacobi, A., Sadler, J.H. Clin. Pharmacol. Ther. (1983) [Pubmed]
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