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Chemical Compound Review

Mexitil     1-(2,6- dimethylphenoxy)propan-2- amine

Synonyms: Mexityl, Mexiletene, Mexiletina, Mexiletine, Mexilitine, ...
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Disease relevance of Mexiletine


Psychiatry related information on Mexiletine


High impact information on Mexiletine

  • The results provide insights for the selective suppression of the mutant phenotype by very low concentrations of drug and indicate that mexiletine equally suppresses the defect in all three known LQT3 mutants [7].
  • Finally, treatment with mexiletine altered only sodium channel number; the Kd for [3H]BTXB and the IC50 for mexiletine were not different for myocytes prepared from control and mexiletine-treated rats [8].
  • The administration of mexiletine to rats induced a dose-dependent increase in [3H]BTXB total specific binding (Bmax) on isolated cardiac myocytes [8].
  • In this report we show that in vivo administration of the class I antiarrhythmic drug mexiletine to rats induces sodium channel upregulation in isolated cardiac myocytes [8].
  • Mexiletine treatment had no effect on tendon reflexes, vibration threshold levels, beat-to-beat variation in heart rate during deep breathing, and postural blood pressure response [4].

Chemical compound and disease context of Mexiletine


Biological context of Mexiletine


Anatomical context of Mexiletine


Associations of Mexiletine with other chemical compounds


Gene context of Mexiletine

  • Involvement of CYP1A2 in mexiletine metabolism [28].
  • Mexiletine, a sodium channel blocker, is effective in shortening the QT interval corrected for heart rate (QTc) of patients with SCN5A mutations [29].
  • Mexiletine shortened significantly the QT interval among LQT3 patients but not among LQT2 patients [30].
  • High concentration (100 microM-1 mM) of mexiletine partially displaced the specific binding of [125I]cyanopindolol to human beta3-adrenoceptor [31].
  • A class IB sodium channel blocker, mexiletine, is most effective in abbreviating QT interval in LQT3, but effectively reduces transmural dispersion of repolarization (TDR) and prevents the development of Torsade de Pointes (TdP) in all 3 models, suggesting its potential as an adjunctive therapy in LQT1 and LQT2 [32].

Analytical, diagnostic and therapeutic context of Mexiletine


  1. A comparison of seven antiarrhythmic drugs in patients with ventricular tachyarrhythmias. Electrophysiologic Study versus Electrocardiographic Monitoring Investigators. Mason, J.W. N. Engl. J. Med. (1993) [Pubmed]
  2. Mexiletine. Use in control of chronic drug-resistant ventricular arrhythmia. Abinader, E.G., Cooper, M. JAMA (1979) [Pubmed]
  3. Mexiletine after myocardial infarction. Gore, S.M. Lancet (1981) [Pubmed]
  4. Mexiletine for treatment of chronic painful diabetic neuropathy. Dejgard, A., Petersen, P., Kastrup, J. Lancet (1988) [Pubmed]
  5. Comparison of procainamide and mexiletine in prevention of ventricular arrhythmias after acute myocardial infarction. Campbell, R.W., Dolder, M.A., Prescott, L.F., Talbot, R.G., Murray, A., Julian, D.G. Lancet (1975) [Pubmed]
  6. Mexiletine in treatment-resistant bipolar disorder. Schaffer, A., Levitt, A.J., Joffe, R.T. Journal of affective disorders. (2000) [Pubmed]
  7. Pharmacological targeting of long QT mutant sodium channels. Wang, D.W., Yazawa, K., Makita, N., George, A.L., Bennett, P.B. J. Clin. Invest. (1997) [Pubmed]
  8. Upregulation of the rat cardiac sodium channel by in vivo treatment with a class I antiarrhythmic drug. Taouis, M., Sheldon, R.S., Duff, H.J. J. Clin. Invest. (1991) [Pubmed]
  9. Safe treatment of resistant ventricular arrhythmias with a combination of amiodarone and quinidine or mexiletine. Hoffmann, A., Follath, F., Burckhardt, D. Lancet (1983) [Pubmed]
  10. Combination of disopyramide and mexiletine for better tolerance and additive effects for treatment of ventricular arrhythmias. Kim, S.G., Mercando, A.D., Tam, S., Fisher, J.D. J. Am. Coll. Cardiol. (1989) [Pubmed]
  11. Mexiletine-quinidine combination: electrophysiologic correlates of a favorable antiarrhythmic interaction in humans. Duff, H.J., Mitchell, L.B., Manyari, D., Wyse, D.G. J. Am. Coll. Cardiol. (1987) [Pubmed]
  12. Propafenone-mexiletine combination for the treatment of sustained ventricular tachycardia. Yeung-Lai-Wah, J.A., Murdock, C.J., Boone, J., Kerr, C.R. J. Am. Coll. Cardiol. (1992) [Pubmed]
  13. Mexiletine antagonizes effects of sotalol on QT interval duration and its proarrhythmic effects in a canine model of torsade de pointes. Chézalviel-Guilbert, F., Davy, J.M., Poirier, J.M., Weissenburger, J. J. Am. Coll. Cardiol. (1995) [Pubmed]
  14. Pharmacokinetics and nondialyzability of mexiletine in renal failure. Wang, T., Wuellner, D., Woosley, R.L., Stone, W.J. Clin. Pharmacol. Ther. (1985) [Pubmed]
  15. Kinetics and bioavailability of mexiletine in healthy subjects. Häselbarth, V., Doevendans, J.E., Wolf, M. Clin. Pharmacol. Ther. (1981) [Pubmed]
  16. Differential interaction of R-mexiletine with the local anesthetic receptor site on brain and heart sodium channel alpha-subunits. Weiser, T., Qu, Y., Catterall, W.A., Scheuer, T. Mol. Pharmacol. (1999) [Pubmed]
  17. Cardiodepressant effects of mexiletine in patients with severe left ventricular dysfunction. Gottlieb, S.S., Weinberg, M. Eur. Heart J. (1992) [Pubmed]
  18. Short-term myocardial uptake of lidocaine and mexiletine in patients with ischemic heart disease. Horowitz, J.D., Dynon, M.K., Woodward, E., Sia, S.T., Macdonald, P.S., Morgan, D.J., Goble, A.J., Louis, W.J. Circulation (1986) [Pubmed]
  19. Molecular determinants of mexiletine structure for potent and use-dependent block of skeletal muscle sodium channels. De Luca, A., Natuzzi, F., Desaphy, J.F., Loni, G., Lentini, G., Franchini, C., Tortorella, V., Camerino, D.C. Mol. Pharmacol. (2000) [Pubmed]
  20. Cardiovascular profile of a new anti-arrhythmic agent, SC-40230. Frederick, L.G., McDonald, S.J., Garthwaite, S.M. Cardiovasc. Res. (1989) [Pubmed]
  21. Electrophysiological actions of mexiletine on isolated rabbit atria and canine ventricular muscle and purkinje fibres. Yamaguchi, I., Singh, B.N., Mandel, W.J. Cardiovasc. Res. (1979) [Pubmed]
  22. Effect of mexiletine on monophasic action potentials recorded from the right ventricle in man. Harper, R.W., Olsson, S.B., Varnauskas, E. Cardiovasc. Res. (1979) [Pubmed]
  23. Regulation of sodium channel gene expression by class I antiarrhythmic drugs and n - 3 polyunsaturated fatty acids in cultured neonatal rat cardiac myocytes. Kang, J.X., Li, Y., Leaf, A. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  24. Determinants of stereospecific binding of type I antiarrhythmic drugs to cardiac sodium channels. Hill, R.J., Duff, H.J., Sheldon, R.S. Mol. Pharmacol. (1988) [Pubmed]
  25. Possible mechanism for pharmacokinetic interaction between lidocaine and mexiletine. Maeda, Y., Funakoshi, S., Nakamura, M., Fukuzawa, M., Kugaya, Y., Yamasaki, M., Tsukiai, S., Murakami, T., Takano, M. Clin. Pharmacol. Ther. (2002) [Pubmed]
  26. Mexiletine. A review of its therapeutic use in painful diabetic neuropathy. Jarvis, B., Coukell, A.J. Drugs (1998) [Pubmed]
  27. Electrophysiological effects of the combination of mexiletine and flecainide in guinea-pig ventricular fibres. Delpón, E., Valenzuela, C., Tamargo, J. Br. J. Pharmacol. (1991) [Pubmed]
  28. Involvement of CYP1A2 in mexiletine metabolism. Nakajima, M., Kobayashi, K., Shimada, N., Tokudome, S., Yamamoto, T., Kuroiwa, Y. British journal of clinical pharmacology. (1998) [Pubmed]
  29. Genetics, molecular mechanisms and management of long QT syndrome. Wang, Q., Chen, Q., Towbin, J.A. Ann. Med. (1998) [Pubmed]
  30. Molecular biology of the long QT syndrome: impact on management. Priori, S.G., Napolitano, C., Paganini, V., Cantù, F., Schwartz, P.J. Pacing and clinical electrophysiology : PACE. (1997) [Pubmed]
  31. Characterization of mexiletine as an antagonist of beta-adrenoceptor in Chinese hamster ovary cells expressing cloned human beta-adrenoceptors. Sakamoto, K., Karikomi, Y., Kubota, Y., Nakahara, T., Ishii, K. Biochem. Pharmacol. (2004) [Pubmed]
  32. Specific therapy based on the genotype and cellular mechanism in inherited cardiac arrhythmias. Long QT syndrome and Brugada syndrome. Shimizu, W., Aiba, T., Antzelevitch, C. Curr. Pharm. Des. (2005) [Pubmed]
  33. Role of combination drug therapy with a class IC antiarrhythmic agent and mexiletine for ventricular tachycardia. Mendes, L., Podrid, P.J., Fuchs, T., Franklin, S. J. Am. Coll. Cardiol. (1991) [Pubmed]
  34. Effect of fluvoxamine on the pharmacokinetics of mexiletine in healthy Japanese men. Kusumoto, M., Ueno, K., Oda, A., Takeda, K., Mashimo, K., Takaya, K., Fujimura, Y., Nishihori, T., Tanaka, K. Clin. Pharmacol. Ther. (2001) [Pubmed]
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