title: Bioavailability and saturation of the presystemic metabolism of oral lorcainide therapy initiated in three different dose regimens.
abstract: The feasibility of giving a supplementary starting dose of the antiarrhythmic drug lorcainide, in order to minimalize the impact of the extensive, but saturable first-pass metabolism, was evaluated. Twenty-five adult patients were given 100 mg lorcainide tablets according to one of 3 different dosage schedules: Eight patients took one tablet at 0, 12 and 24 h, 8 took 1 tablet at 0, 1, 12 and 24 h and 9 took 1 tablet at 0, 2, 12 and 24 h. Levels of lorcainide and its metabolite, nor-lorcainide, during treatment were determined by gas-liquid chromatography. The results show that giving a second tablet 1 or 2 h after the first may produce faster saturation of the pre-systemic metabolism of lorcainide in the liver.
mesh_terms: D000368:Aged; D044482:Benzeneacetamides; D001682:Biological Availability; D001711:Biotransformation; D004334:Drug Administration Schedule; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D010880:Piperidines / Q000008:administration & dosage* / Q000378:metabolism
chemical_list: D044482:Benzeneacetamides; D010880:Piperidines; C015970:lorcainide