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Disposition of bretylium in man and rat; A sensitive chemical method for its estimation in plasma and urine
Author(s) -
Kuntzman R.,
Tsai I.,
Chang R.,
Conney A. H.
Publication year - 1970
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/cpt1970116829
Subject(s) - urine , bretylium , chemistry , liter , feces , excretion , endocrinology , intramuscular injection , plasma levels , medicine , pharmacology , chromatography , biology , biochemistry , paleontology , receptor , adrenergic
A gas chromatographic method is described which allows estimation of bretylium, a quarternary ammonium compound, in plasma and urine at drug concentrations as low as 0.07 μg per milliliter. This sensitivity allows the measurement of plasma levels of bretylium in patients receiving therapeutic doses. The plasma level of bretylium in man does not decrease as a first‐order function. During the first 24 hours after drug administration the half‐life increased from 1 to 5.5 hours. In man, 70 to 80 per cent of an intramuscular dose of bretylium was excreted unchanged in the urine within 24 hours and an additional 10 per cent was excreted during the next 3 days. In the rat, 63 per cent of an intramuscular dose was excreted unchanged in the urine; 31 per cent was excreted unchanged in the feces. Excretion into the bile probably accounts for the bretylium found in rat feces.