Clinical profiles of newer class I antiarrhythmic agents--tocainide, mexiletine, encainide, flecainide and lorcainide.
New class I antiarrhythmic drugs differ in potency, adverse effects and pharmacokinetics. Encainide and flecainide can totally suppress arrhythmias in some patients, but arrhythmia induction can also occur. At effective dose levels, neurologic and gastrointestinal adverse effects are uncommon. Flecainide pharmacokinetics are suitable for oral use but encainide disposition is complex with variable bioavailability and active metabolites that contribute substantially to activity. Lorcainide is also potent, but neurologic adverse effects are common and dose-dependent bioavailability and an active metabolite may complicate long-term oral therapy. Tocainide and mexiletine can suppress arrhythmias in acute myocardial infarction, during convalescence from myocardial infarction and in patients with arrhythmias resistant to other therapy. Dose-related neurologic and gastrointestinal adverse effects are common, but hemodynamic effects are minor and arrhythmia induction is rare. Tocainide disposition is reasonably predictable and stable in patients, but mexiletine disposition is less so because of variation in distribution and clearance. Although all of the newer agents have some disadvantages, their availability should increase the likelihood of success in the high-risk patient.
D000284:Administration, Oral; D000813:Anilides / Q000008:administration & dosage / Q000378:metabolism / Q000494:pharmacology; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000378:metabolism / Q000494:pharmacology*; D044482:Benzeneacetamides; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology; D016700:Encainide; D005424:Flecainide; D006439:Hemodynamics; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008012:Lidocaine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D008801:Mexiletine / Q000008:administration & dosage / Q000378:metabolism / Q000494:pharmacology; D010880:Piperidines / Q000008:administration & dosage / Q000378:metabolism / Q000494:pharmacology; D016677:Tocainide
D000813:Anilides; D000889:Anti-Arrhythmia Agents; D044482:Benzeneacetamides; D010880:Piperidines; D008801:Mexiletine; D016677:Tocainide; D008012:Lidocaine; D005424:Flecainide; C015970:lorcainide; D016700:Encainide