Clinical pharmacology of adriamycin (NSC 123127)

In clinical pharmacology studies using adriamycin, initial plasma levels declined rapidly after intravenous administration suggesting rapid uptake into tissues. In our own studies, plasma levels decreased at an intermediate rate until 12 hr after drug administration at which time the drug disappeared with a half life of approximately 1 day, reflecting the tissue half life. There was extensive metabolism to adriamycinol and several aglycone metabolites. In our study, where urinary excretion was reproducible, such excretion rarely accounted for more than 10% of the administered dose in 5 days. The drug was not detected in the cerebrospinal fluid, and in one patient with an indwelling T tube, biliary excretion of fluorescent material accounted for 40% of the administered dose, explaining the elevated and prolonged levels of adriamycin and its metabolites seen in patients with liver disease.