Pharmacokinetic studies of procainamide (PA) and N-acetylprocainamide (NAPA) in healthy subjects. 1980

M Wierzchowiecki, and D Michałowska, and Z Lowicki, and R Ochotny, and A Grześkowiak, and T Tomaszkiewicz

Pharmacokinetic studies after a single oral dose of 750 mg of PA in 10 normal subjects were performed. In 6 of them, pharmacokinetics of NAPA were also determined after a single oral dose of 900 mg of NAPA. Substantial differences in pharmacokinetic parameters of PA depending on acetylation phenotype were found. In fast acetylators (sulphadimidine phenotyping), half-life was shorter (2.4 +/- 0.7 hr) and 24 hr urine NAPA excretion was larger (22.5 +/- 5.8% of dose) than in slow acetylators (3.6 +/- 1.0 hr and 8.8 +/- 5.4% respectively). NAPA was characterized by different pharmacokinetic parameters (t 1/2 7.0 +/- 1.0 hr, 24 hr urine elimination - 58.5% of dose). Clinical implications of these findings are discussed.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D010641 Phenotype The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment. Phenotypes
D011342 Procainamide A class Ia antiarrhythmic drug that is structurally-related to PROCAINE. Procaine Amide,Apo-Procainamide,Biocoryl,Novocainamide,Novocamid,Procainamide Hydrochloride,Procamide,Procan,Procan SR,Procanbid,Pronestyl,Rhythmin,Amide, Procaine,Hydrochloride, Procainamide
D005260 Female Females
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000107 Acetylation Formation of an acetyl derivative. (Stedman, 25th ed) Acetylations
D000120 Acecainide A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure. Acetylprocainamide,Acecainide Hydrochloride,Acecainide Monohydrochloride,N-Acetylprocainamide,Hydrochloride, Acecainide,Monohydrochloride, Acecainide,N Acetylprocainamide

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