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Chemical Compound Review

BIDISOMIDE     2-(2-chlorophenyl)-2-[2- (ethanoyl-propan-2...

Synonyms: Bidisomida, Bidisomidum, CHEMBL305745, SureCN120852, AC1L1RYW, ...
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Disease relevance of BIDISOMIDE


High impact information on BIDISOMIDE

  • Bidisomide (SC-40230), a new antiarrhythmic agent: initial study of tolerability and pharmacokinetics [4].
  • Bioavailability was studied in 12 male volunteers, with each receiving 2.0 mg/kg of bidisomide, both orally and intravenously, in an open-label crossover trial [4].
  • The cardiac and general haemodynamic effects of SC-40230, a newly developed anti-arrhythmic agent with both class 1a and 1b properties, were assessed in two different types of experiments using anaesthetised dogs, and in experiments using isolated cat papillary muscles [5].
  • At the canine anti-arrhythmic dose (9 intravenously), SC-40230 decreased the maximum rate of rise of the left ventricular pressure (LV dP/dtmax) by 20% [5].
  • In the converse series of experiments after treatment with isoproterenol, which caused a 20 to 30% reduction in APD and ERP, only bidisomide completely reversed the effect of 1 microM isoproterenol [6].

Biological context of BIDISOMIDE

  • RESULTS: Bidisomide plasma AUC was significantly reduced following oral drug co-administration with breakfast compared to fasted-state controls in human subjects and in dogs independent of the composition of the solid cooked breakfast [7].
  • Reduced systemic availability of an antiarrhythmic drug, bidisomide, with meal co-administration: relationship with region-dependent intestinal absorption [7].
  • 2. The mass spectra of bidisomide metabolites indicate that the two major metabolic pathways of bidisomide were hydroxylation of the piperidine ring and N-dealkylation [8].
  • Our results indicate that bidisomide binds to rat cardiac sodium channels and that the dissociation kinetics of bidisomide from the inactivated sodium channel is slower than that of disopyramide [9].

Anatomical context of BIDISOMIDE


Associations of BIDISOMIDE with other chemical compounds


Gene context of BIDISOMIDE


Analytical, diagnostic and therapeutic context of BIDISOMIDE


  1. Rapid infusions of bidisomide or disopyramide in conscious dogs: effect of myocardial infarction on acute tolerability. Schmidt, J.J., Frederick, L.G., Garthwaite, S.M. J. Cardiovasc. Pharmacol. (1992) [Pubmed]
  2. Effect of diet and gavage on the dose- and dose-mode-dependent absorption and metabolism of bidisomide in rat. Cook, C.S., Lonien, M., Hribar, J. Xenobiotica (2000) [Pubmed]
  3. Effects of bidisomide (SC-40230), a new class I antiarrhythmic agent, on ventricular arrhythmias induced by coronary artery occlusion and reperfusion in anesthetized rats; comparison with mexiletine and disopyramide. Komori, S., Sano, S., Li, B.H., Matsumura, K., Naitoh, A., Mochizuki, S., Ishihara, T., Watanabe, A., Umetani, K., Ijiri, H. Heart and vessels. (1995) [Pubmed]
  4. Bidisomide (SC-40230), a new antiarrhythmic agent: initial study of tolerability and pharmacokinetics. Page, R.L., Wharton, J.M., Wilkinson, W.E., Friedman, I.M., Claypool, W.D., Karim, A., Kowalski, K.G., McDonald, S.J., Gardiner, P., Pritchett, E.L. Clin. Pharmacol. Ther. (1992) [Pubmed]
  5. Cardiovascular profile of a new anti-arrhythmic agent, SC-40230. Frederick, L.G., McDonald, S.J., Garthwaite, S.M. Cardiovasc. Res. (1989) [Pubmed]
  6. Comparison of bidisomide, flecainide and dofetilide on action potential duration in isolated canine atria: effect of isoproterenol. Martin, C.L., Palomo, M.A., Mcmahon, E.G. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  7. Reduced systemic availability of an antiarrhythmic drug, bidisomide, with meal co-administration: relationship with region-dependent intestinal absorption. Pao, L.H., Zhou, S.Y., Cook, C., Kararli, T., Kirchhoff, C., Truelove, J., Karim, A., Fleisher, D. Pharm. Res. (1998) [Pubmed]
  8. Metabolism of a novel antiarrhythmic agent, bidisomide, in man: use of high resolution mass spectrometry to distinguish desisopropyl bidisomide from desacetyl bidisomide. Cook, C.S., Ames, G.B., Hribar, J.D., Liu, N.W., Sweeney, D.L., Schoenhard, G.L., Karim, A. Xenobiotica (1995) [Pubmed]
  9. Electrophysiologic effects of an antiarrhythmic agent, bidisomide, on sodium current in isolated rat ventricular myocytes: comparison with mexiletine and disopyramide. Homma, N., Tsujimoto, G., Hashimoto, K. Jpn. J. Pharmacol. (2001) [Pubmed]
  10. Absorption and disposition of a new antiarrhythmic agent bidisomide in man. Cook, C.S., Ames, G.B., Smith, M.E., Kowalski, K.G., Karim, A. Pharm. Res. (1993) [Pubmed]
  11. Importance of pharmacokinetic and physicochemical data in the discovery and development of novel anti-arrhythmic drugs. Cook, C.S., McDonald, S.J., Karim, A. Xenobiotica (1993) [Pubmed]
  12. Effect of folate supplementation on clinical chemistry and hematologic changes related to bidisomide administration in the rat. Vandenberghe, Y., Masson, M., Palate, B., Roba, J. Drug and chemical toxicology. (1995) [Pubmed]
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