Plasma levels and myocardial content of verapamil, norverapamil and two N-dealkyl-metabolites in man.
The plasma levels and myocardial content of verapamil and its metabolites norverapamil, N-dealkylverapamil and N-dealkylnorverapamil were determined in 15 patients with valvular [3] or ischaemic [12] heart disease. The mean myocardial plasma concentration ratio (M/P) was 7.05 for verapamil, 11.45 for norverapamil, 8.93 for N-dealkylverapamil, and 11.33 for N-dealkylnorverapamil, with great interpatient variability. The highest M/P ratios of verapamil were generally found in patients with the lowest plasma levels, suggesting that saturable tissue uptake may occur.
D000328:Adult; D000368:Aged; D002851:Chromatography, High Pressure Liquid; D003327:Coronary Disease / Q000188:drug therapy; D005260:Female; D006349:Heart Valve Diseases / Q000188:drug therapy; D006801:Humans; D008297:Male; D008433:Mathematics; D008875:Middle Aged; D008954:Models, Biological; D009206:Myocardium / Q000378:metabolism*; D009570:Nitriles; D014700:Verapamil / Q000031:analogs & derivatives / Q000097:blood / Q000378:metabolism*
D009570:Nitriles; C016906:alpha-(3-aminopropyl)-3,4-dimethoxy-alpha-(1-methylethyl)benzeneacetonitrile; C482241:2-(3,4-dimethoxyphenyl)-5-amino-2-isopropylvaleronitrile; C016904:norverapamil; D014700:Verapamil