PROCAINAMIDE PHARMACOKINETICS IN BEAGLES - URINARY PH DEPENDENCY AND COMPARISON WITH N-ACETYLPROCAINAMIDE

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  • 1 January 1977
    • journal article
    • letter
    • Vol. 17  (2) , 333-336
Abstract
Male and female beagles received i.v. bolus injections of procainamide (PA) [a cardioactive agent] to study its pharmacokinetic behavior and to determine the effect of urinary pH upon renal excretion. Urinary alkalinization caused an increase in plasma disappearance half-life (t1/2) and decreases in renal clearance (ClR) and total body clearance (ClB), while the apparent volume of distribution remained unchanged. Acid hydrolysis of the urine collected caused a 17% increase in the amount of PA measured. This hydrolyzable substance was found not to be the N-acetylated metabolite of PA. When i.v. N-acetylprocainamide (NAPA) was administered in crossover fashion to some of the above animals, it exhibited a longer t1/2 than PA. Mean ClR and mean ClB values were smaller with NAPA while both compounds showed similar dependence upon renal and non-renal clearance mechanisms.

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