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Acetylation of procainamide in man and its relationship to isonicotinic acid hydrazide acetylation phenotype
Author(s) -
Gibson Thomas P.,
Matusik Jean,
Matusik Edward,
Nelson Howard A.,
Wilkinson Joanne,
Briggs William A.
Publication year - 1975
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1975174395
Subject(s) - procainamide , chemistry , hydrazide , acetylation , urine , napa , isonicotinic acid , isoniazid , pharmacology , biochemistry , medicine , organic chemistry , tuberculosis , pathology , gene
To assess the extent of the acetylation of procainamide (PA) to N‐acetylprocainamide (NAPA) in man, and its relation to isonicotinic acid hydrazide (INH) acetylation phenotype, the following study was done. Fourteen subjects received 500 mg of PA . HCI orally. INH acetylation phenotype was determined by the serum half‐life of INH after 4 mg/kg of INH orally. Each urine voided for 96 hr after procainamide was saved and levels of procainamide and NAPA measured by gas‐liquid chromatography. The 14 subjects eliminated 52 ± 4% ofthe dose as procainamide and 16 ± 2% ofthe dose as NAPA. Four fast INH acetylators eliminated 23 ± 3% ofthe dose as NAPA compared to 12 ± 1% by the slow acetylators (p < 0.05). The amount of unaltered procainamide excreted by thefast and slow INH acetylators was not significantly different, 50 ± 4% and 53 ± 4%, respectively. Ofthe total amount of drug recovered in the urine ofthefast and slow INH acetylators, NAPA accountedfor 32% and 19%, respectively (p < 0.01). There appears to be a positive correlation between the ability to acetylate INH and the ability to acetylate procainamide.