The relationship between the metabolism of procainamide and sulfamethazine.

Abstract

The metabolism of sulfamethazine (SMZ), which is acetylated by a binodally distributed enzyme, and procainamide (PA) was compared in 21 normal volunteers, each given a single oral dosted metabolites, N-acetyl-procainamide (NAPA) and Ac-SMZ, were measured. Subjects with less than 64% Ac-SMZ in the 0-8 hour collection were termed "slow" and those with more than 64% were termed "fast" SMZ acetylators. Slow SMZ acetylators had 9.8 to 43.8% (24.1 +/- 10.13) NAPA recovered, and fast SMZ acetylators, 22.0 to 42.6% (33.7 +/- 7.29) NAPA, P less than 0.01. In addition, the calculated half-life of PA metabolism for slow SMZ acetylators was 9.0 to 33.8 hours (18.4 +/- 8.82) and for fast SMZ acetylators was 8.1 to 14.4 hours (10.9 +/- 2.19), P less than 0.01. For four subjects, SMZ acetylation phenotype did not correlate with the half-life of SMZ or PA metabolism; and in two, SMZ acetylation phenotype and half-life of metabolism did not correlate with the same PA indices. Even though slow SMZ acetylators have less NAPA recovered than fast SMZ acetylators, it is not yet clear that procainamide is metabolized by a bimodally distributed enzyme as is sulfamethazine.

Effect of Coadministration of Procainamide and Isoniazid on Each Other’s Acetylation Pathway

“…1975. In contrast, recent studies by Giardina et al (1977) revealed a poor correlation between the t'/2 of PA metabolism and the t'/2 o f sul famethazine metabolism. These workers feel that t*/2 o f PA metabolism is the most precise method o f measuring acetylator phenotype using PA as the test dnig.…”

Fluorescence photometric quantitation of procainamide and N-acetylprocainamide in plasma after separation by thin-layer chromatography

“…A number of gas chromatographic (GC) procedures have been described (2,(8)(9)(10)(11). All are more specific but are slow.…”