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Studies on absorption, excretion, and metabolism of 3 H‐reserpine in man
Author(s) -
Maass Alfred R.,
Jenkins Bernard,
Shen Yvonne,
Tannenbaum Philip
Publication year - 1969
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/cpt1969103366
Subject(s) - reserpine , excretion , urine , chemistry , excretory system , absorption (acoustics) , feces , tritium , metabolism , endocrinology , medicine , radiochemistry , biochemistry , biology , paleontology , physics , acoustics , nuclear physics
Following oral administration of 0.25 mg. of 3 H‐reserpine, dissolved in water, to 6 normal male volunteers, tritium was rapidly absorbed into the blood, reaching a peak in approximately one to 2 hours. Radioactivity was found in both the red blood cell and plasma, with a greater concentration in the plasma. Tritium was tightly bound to the red cells; a fixed concentration of radioactivity was found in the red blood cell during 96 hours of observation, while the plasma concentration continued to fall. The rate of plasma disappearance gave two biological half‐lives of 4.5 and 271 hours. Initial urinary excretion averaged approximately 6 per cent of the dose in 24 hours; the major excretory product was trimethoxybenzoic acid. Urinary excretion averaged 8 per cent of the dose in 4 days, but radioactivity was still detectable in plasma, urine, and feces 11 to 12 days after administration of 3 H‐reserpine, indicating the very slow release of radioactivity from the body. The major portion of radioactivity appearing in the feces was identified as reserpine by paper chromatography.