Lorcainide disposition kinetics in arrhythmia patients

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Abstract
Lorcainide [a new antiarrythmic] disposition kinetics were studied after i.v. and oral administration to patients with ventricular arrhythmias. After i.v. doses ranging from 100-200 mg, blodo samples were drawn and plasma was analyzed for lorcainide concentration by high-pressure liquid chromatography. A 3-compartment model was used to fit the data. The model-independent calculated values for clearance, steady-state volume of distribution and terminal half-life [t1/2] were 14.4 .+-. 3.28 ml/min per kg, 6.33 .+-. 2.23 l/kg and 7.8 .+-. 2.2 h, respectively. After 9 doses of oral lorcainide (100 mg every 12 h) blood samples were drawn and analyzed for lorcainide and its active metabolite, norlorcainide. The lorcainide and norlorcainide t1/2 were 9.6 .+-. 2.8 and 26.8 .+-. 8.2 h, respectively. Mean steady-state level of norlorcainide was 2.2 .+-. 0.9 times the level of lorcainide. The clearance of lorcainide evidently decreases with time during long-term dosing.