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Comparative physiological disposition of two nitrofuran anti‐microbial agents
Author(s) -
Labaune J. P.,
Moreau J. P.,
Byrne R.
Publication year - 1986
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510070504
Subject(s) - nitrofuran , urine , pharmacology , feces , oral administration , chemistry , drug , antimicrobial , excretion , metabolite , diarrhea , medicine , microbiology and biotechnology , biology , genetics , organic chemistry
The physiological disposition of two nitrofuran derivatives used as antimicrobial agents for the treatment of acute infectious diarrhea was evaluated in humans and animals. Upon administration of a single oral dose (600mg) of nifurzide or nifuroxazide, no unchanged parent drug was detected in human blood or urine. In rats given 14 C‐nifurzide and 14 C‐nifuroxazide at a dose of 10mg kg −1 , 5 per cent and 17 per cent of the dose of nifurzide and nifuroxazide, respectively, were excreted in urine over a 48‐hour period. None of this radioactivity was present as unchanged drug, indicating that renal excretion of both drugs occurs as metabolites. In the feces 20 per cent of the radioactivity recovered was associated with unchanged nifuroxazide as compared with 100 per cent for nifurzide. Whole body autoradiography using rats showed that after oral administration of 14 C‐nifurzide and 14 C‐nifuroxazide, most of the radioactivity remained in the gastrointestinal lumen.