Acecainide

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John J. Lima - One of the best experts on this subject based on the ideXlab platform.

  • Acecainide pharmacokinetics in normal subjects of known acetylator phenotype
    Biopharmaceutics & Drug Disposition, 1991
    Co-Authors: James D Coyle, Harisios Boudoulas, John J. Lima
    Abstract:

    The purpose of this study was to determine the pharmacokinetics of Acecainide (formerly N-acetylprocainamide) in six normal subjects of known acetylator phenotype. Three subjects were fast acetylators and three slow acetylators by sulfapyridine phenotyping criteria. Each subject received a 20-min, 3 mg kg−1 intravenous Acecainide infusion. Concentrations of Acecainide, procainamide, and their deethylated metabolites were measured in serum and urine samples using HPLC. Acecainide renal clearance, nonrenal clearance, steady-state volume of distribution, and other pharmacokinetic parameters were estimated using standard approaches. Acecainide renal clearance and steady-state volume of distribution were (mean ± SD) 13·6 ± 1·581 h−1 and 135 ± 20·31, respectively, and were not significantly different in fast and slow acetylators. Acecainide nonrenal clearance in the six subjects was 3·0 ± 1·01 h−1, however, nonrenal clearance in slow acetylators was 1·8 times that in fast acetylators (3·9 vs 2·21 h−1, p = 0·012) with clear separation of the subjects into two groups when the data were grouped by acetylator phenotype. The nonrenal clearance of Acecainide was inversely correlated with percentage sulfapyridine acetylation. Computer simulations were conducted to explore possible explanations for the observed difference in nonrenal clearance.

John Fawcett Wilson - One of the best experts on this subject based on the ideXlab platform.

  • Acecainide n acetylprocainamide
    1995
    Co-Authors: John Fawcett Wilson
    Abstract:

    The drug Acecainide or N-acetylprocainamide is also the principal active metabolite of the class la anti-arrhythmic procainamide. It has less pharmacological activity, a longer duration of action, and produces less frequent cardiac complications and hypersensitivity reactions than procainamide. The acetylation of procainamide is subject to genetic polymorphism with 30-40% being converted in fast acetylators. Up to 85% of a dose of Acecainide is excreted unchanged in urine. The half-life in plasma is 6-9 hours (procainamide 2.5-4 hours), increasing with renal impairment. Therapeutic concentrations in plasma have been proposed to be 10-30 μg/ ml for the sum of both procainamide and Acecainide, or 4-10 μg/ml for procainamide and 6-20 μg/ml for Acecainide.

James D Coyle - One of the best experts on this subject based on the ideXlab platform.

  • Acecainide pharmacokinetics in normal subjects of known acetylator phenotype
    Biopharmaceutics & Drug Disposition, 1991
    Co-Authors: James D Coyle, Harisios Boudoulas, John J. Lima
    Abstract:

    The purpose of this study was to determine the pharmacokinetics of Acecainide (formerly N-acetylprocainamide) in six normal subjects of known acetylator phenotype. Three subjects were fast acetylators and three slow acetylators by sulfapyridine phenotyping criteria. Each subject received a 20-min, 3 mg kg−1 intravenous Acecainide infusion. Concentrations of Acecainide, procainamide, and their deethylated metabolites were measured in serum and urine samples using HPLC. Acecainide renal clearance, nonrenal clearance, steady-state volume of distribution, and other pharmacokinetic parameters were estimated using standard approaches. Acecainide renal clearance and steady-state volume of distribution were (mean ± SD) 13·6 ± 1·581 h−1 and 135 ± 20·31, respectively, and were not significantly different in fast and slow acetylators. Acecainide nonrenal clearance in the six subjects was 3·0 ± 1·01 h−1, however, nonrenal clearance in slow acetylators was 1·8 times that in fast acetylators (3·9 vs 2·21 h−1, p = 0·012) with clear separation of the subjects into two groups when the data were grouped by acetylator phenotype. The nonrenal clearance of Acecainide was inversely correlated with percentage sulfapyridine acetylation. Computer simulations were conducted to explore possible explanations for the observed difference in nonrenal clearance.

Harisios Boudoulas - One of the best experts on this subject based on the ideXlab platform.

  • Acecainide pharmacokinetics in normal subjects of known acetylator phenotype
    Biopharmaceutics & Drug Disposition, 1991
    Co-Authors: James D Coyle, Harisios Boudoulas, John J. Lima
    Abstract:

    The purpose of this study was to determine the pharmacokinetics of Acecainide (formerly N-acetylprocainamide) in six normal subjects of known acetylator phenotype. Three subjects were fast acetylators and three slow acetylators by sulfapyridine phenotyping criteria. Each subject received a 20-min, 3 mg kg−1 intravenous Acecainide infusion. Concentrations of Acecainide, procainamide, and their deethylated metabolites were measured in serum and urine samples using HPLC. Acecainide renal clearance, nonrenal clearance, steady-state volume of distribution, and other pharmacokinetic parameters were estimated using standard approaches. Acecainide renal clearance and steady-state volume of distribution were (mean ± SD) 13·6 ± 1·581 h−1 and 135 ± 20·31, respectively, and were not significantly different in fast and slow acetylators. Acecainide nonrenal clearance in the six subjects was 3·0 ± 1·01 h−1, however, nonrenal clearance in slow acetylators was 1·8 times that in fast acetylators (3·9 vs 2·21 h−1, p = 0·012) with clear separation of the subjects into two groups when the data were grouped by acetylator phenotype. The nonrenal clearance of Acecainide was inversely correlated with percentage sulfapyridine acetylation. Computer simulations were conducted to explore possible explanations for the observed difference in nonrenal clearance.

Babić Dragan - One of the best experts on this subject based on the ideXlab platform.

  • Electrical conductivity of the acetamide-acetate salt melts
    2001
    Co-Authors: Babić Dragan, Nikolic R, Gadžurić Slobodan
    Abstract:

    Specific conductivity of molten mixtures of acetamide with following acetate salts was measured at 83 +/- 0.1degreesC : a) acetamide - anhydrous sodium acetate (up to 0.051 mole fraction), b) acetainide sodium acetate trihydrate (entire concentration range) and c) acetamide - zinc acetate dihydrate ( up to 0.24 mole fraction). Selected composition of all three mixtures, with low melting points were chosen for the studies of the changes of conductance with temperature. The mixtures: with sodium acetate both anhydrous and hydrated showed fairly high specific conductivity (approximate to10(-2) S/cm), nearly two orders of magnitude higher than the mixture with hydrated zinc acetate. Molar conductivity was also calculated. The results were discussed in terms of acetamide-salt-water interactions. Attempts were made to calculate the degree of dissociation of the salts in molten acetamide. The results were compared with the data obtained from earlier thermochemical studies of the same melt systems