Mexiletine

Abstract

Mexiletine is a new local anaesthetic antiarrhythmic agent whose chemical structure and electrophysiological properties closely resemble those of lignocaine although its anticonvulsant and pharmacokinetic properties differ from that drug. Unlike lignocaine (lidocaine) it is active following oral administration with a plasma half-life varying between 8 and 20 hours so that it can be administered twice or three times daily to sustain therapeutic plasma levels. The drug is effective when given intravenously or by the oral route in controlling ventricular arrhythmias especially following acute myocardial infarction but the side effects are greater during parenteral administration. Side effects during chronic oral therapy with mexiletine have not posed a serious problem. Mexiletine has the pharmacodynamic and pharmacokinetic properties of an agent suitable for the chronic oral prophylaxis of serious ventricular arrhythmias in patients with ischaemic heart disease.

Interactions of rosiglitazone and anti-arrhythmic drugs in animal model

“…[13] Mexiletine is not metabolized by the same enzyme as of Rosiglitazone but is believed to increase insulin release. [1415] Rosiglitazone produces hypoglycemic action by way of release of insulin from β cells of pancreas and also by increase in glucose uptake at cellular level. [16]…”

Mexiletine as a treatment for primary erythromelalgia: normalization of biophysical properties of mutant L858F NaV1.7 sodium channels

“…The non-selective sodium channel inhibitor mexiletine hydrochloride [1-methyl-2-(2,6-xylyloxy)ethylamine hydrochloride] has been extensively studied and used clinically for decades because of its antiarrhythmic effects (Chew et al ., 1979; Woosley et al ., 1984; Fenster and Comess, 1986; Monk and Brogden, 1990). More recently, it has also been found to be effective in several animal models of chronic pain and it has been suggested as a third-line treatment instead of systemic lidocaine for neuropathic pain syndromes (Jarvis and Coukell, 1998; Kuhnert et al ., 1999; Mao and Chen, 2000; Challapalli et al ., 2005; Tremont-Lukats et al ., 2005; Ebell, 2006; Marmura, 2010).…”

Gas chromatographic determination of mexiletine in human plasma with flame ionization detection after reaction with carbon disulphide

“…The effective plasma concentration falls in the range 0.75-2.0 yg/mL (Campbell et al, 1978;Follath, Ganziner and Schuetz, 1982); an unacceptable frequency of serious side-effects occurs at plasma concentrations higher than 2.0 pg/mL (Talbot, Julian and Prescott, 1976). Since it has a low therapeutic index, routine monitoring of plasma levels of mexiletine will be helpful to obtain effective arrhythmia suppression without toxicity.…”