Tissue distribution of N-acetylprocainamide in rats.

The purpose of this study was to determine the distribution of N-acetylprocainamide (NAPA) in heart, kidney, and liver tissues of rats and their relationship to the plasma concentration after intravenous administration of the drug (100 mg/kg) to 24 Charles River rats. A specific HPLC procedure was used. The plasma and tissue concentrations of NAPA declined biexponentially in parallel, with an elimination half-life of about 1.8 hr. The equilibrium between plasma and the organs tested in this study was attained within 5 min. The tissue/plasma concentration ratio remained constant throughout the study. The tissue/plasma ratios for heart, kidney, and liver were 2.1, 7.9, and 2.4, respectively. The data indicate that: a) these organs have greater affinity to NAPA than do plasma proteins, and b) plasma concentrations may be reliable measures of the therapeutically effective concentrations at the site of action, i.e., the heart tissues.