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The implications of procainamide metabolism to its induction of lupus.

Authors
  • Uetrecht, J P
  • Freeman, R W
  • Woosley, R L
Type
Published Article
Journal
Arthritis and rheumatism
Publication Date
Aug 01, 1981
Volume
24
Issue
8
Pages
994–1003
Identifiers
PMID: 6169352
Source
Medline
License
Unknown

Abstract

The principal metabolic pathway of procainamide leads to formation of the less toxic N-acetyl-procainamide and the rapid acetylator phenotype is associated with a lower incidence of procainamide-induced lupus. Another metabolic pathway forms a reactive metabolite which causes revertants in the Ames test and covalently binds to microsomal protein. A study of the metabolism of procainamide revealed three metabolites that have not been previously described. A comparison of the metabolites of N-acetylprocainamide with those of procainamide suggests possibilities for the identity of the reactive metabolite. The hypotheses to be discussed explore the relationships between the formation of a reactive metabolite and the induction of lupus.

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