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Pharmacokinetics of guanazole in man
Author(s) -
Gerber Nicholas,
Seibert Richard,
Desiderio Dominic,
Thompson Richard M.,
Lane Montague
Publication year - 1973
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/cpt1973142264
Subject(s) - pharmacokinetics , metabolite , urine , pharmacology , drug , body surface area , plasma concentration , chemistry , medicine
Guanazole, 3,5‐diamino‐1,2,4‐triazole, synthesized nearly a century ago, has recently been shown to have antitumor properties. In patients with cancer, intravenous doses ranging from 3.5 to 10 gm per square meter of body surface area have been used. It was found that the 15 minute plasma level declines to one‐half in 1 to 2 hours. After 4 to 6 hours the plasma half‐life is 5 to 10 hours. The drug is eliminated almost quantitatively in the urine in 24 hours. No metabolites could be detected in the perfusate or bile of the isolated perfused rat liver preparation, suggesting that the drug itself rather than a metabolite is responsible for the antitumor activity.