Plasma concentrations of flecainide acetate, a new antiarrhythmic agent, in humans.
Flecainide, a new antiarrhythmic agent, was given to eight healthy men to ascertain plasma drug levels and to assess tolerance for the drug. Each subject received a single intravenous (IV) dose (0.5, 1, 1.5, or 2 mg/kg) of flecainide, and plasma levels of unchanged flecainide were measured by gas-liquid chromatography. After an initial rapid distribution phase, the drug's plasma half-life (terminal elimination phase) ranged from seven to 15 hours (mean, 11 hours); half-life was apparently independent of dose level. Immediately after IV administration, the relatively high plasma drug levels seen during the short distribution phase were associated with minor and transient side effects in some subjects receiving the two higher doses; overall, the drug was well tolerated. Plasma flecainide levels 60 minutes after administration (after distribution) ranged from 52 to 300 ng/ml and were reasonably proportional to dose level. The drug's relatively long plasma half-life in humans indicates that plasma levels will be maintained for prolonged periods; thus flecainide should provide sustained therapeutic activity in patients with cardiac arrhythmias.
D000328:Adult; D000889:Anti-Arrhythmia Agents / Q000097:blood* / Q000633:toxicity; D002849:Chromatography, Gas; D004244:Dizziness / Q000139:chemically induced; D004361:Drug Tolerance; D004562:Electrocardiography; D005424:Flecainide; D006207:Half-Life; D006801:Humans; D008297:Male; D010880:Piperidines / Q000097:blood* / Q000633:toxicity; D014785:Vision, Ocular / Q000187:drug effects; D014987:Xerostomia / Q000139:chemically induced
D000889:Anti-Arrhythmia Agents; D010880:Piperidines; D005424:Flecainide