DISTRIBUTION AND EXCRETION IN THE RAT AND MONKEY OF [BR-82] BROMOCRIPTINE

  • 1 January 1979
    • journal article
    • research article
    • Vol. 211  (1) , 31-35
Abstract
Radiolabeled bromocriptine, a dopaminergic agonist, was administered to rats and rhesus monkeys and its tissue distribution, rate of excretion and metabolism were determined. In both species, [82Br]bromocriptine is predominantly concentrated in the liver, metabolized and excreted through bile. Extractable free drug is undetectable in blood after 30 min. After 2 h, the estimated concentration of free drug in rat brain is 2 .times. 10-8 M. Terminal phase half-lives of radiolabel excretion were 2.9 days for the rat and 27.3 days for the monkey. The retained organically bound 82Br is present in a form more polar than bromocriptine.