Capacity-limited elimination of procainamide in man. 1978

W J Tilstone, and D H Lawson

Procainamide (PA) pharmacokinetics were studied at steady state in 19 patients. The PA was given as 1.0 or 1.5 g eight hourly (L and H dose groups) and acetylator phenotype determined from sulphadimidine acetylation was classified as Slow or Fast (S or F). Thus, four groups were categorized, HF, LF, HS and LS with 7, 5, 3, and 4 patients in each respective group. Overall the mean steady state plasma concentration of PA (Cpss) expressed as a fraction of dose did not depend on dose or on acetylator status, but the HS group had significantly higher Cpss per gram dose (6.3 mug/ml) than LS (2.7 mug/ml) or the HF (2.3 mug/ml) groups. Clearance of PA be acetylation (C1A) was 23.8% of the total in fast acetylators and 16.5% in slow acetylators. C1A was not dose-dependent in the HF or LF groups (mean 177.9 ml/min and 168.4 ml/min) but was dose-dependent in the HS group (mean 74.6 ml/min) which differed significantly from the LS group (mean 113.4 ml/min).

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D009203 Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION). Cardiovascular Stroke,Heart Attack,Myocardial Infarct,Cardiovascular Strokes,Heart Attacks,Infarct, Myocardial,Infarction, Myocardial,Infarctions, Myocardial,Infarcts, Myocardial,Myocardial Infarctions,Myocardial Infarcts,Stroke, Cardiovascular,Strokes, Cardiovascular
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
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

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