title: Pharmacokinetics and pharmacodynamics in man of the dopamine antagonist ergot derivative, bromerguride.
abstract: The plasma levels and urinary excretion of the dopamine antagonist, bromerguride, were measured by radioimmunoassay in healthy male volunteers given 50 micrograms i.v. and oral doses of 1 and 2 mg. Plasma prolactin was also measured by radioimmunoassay. Following i.v. injection, the concentration of bromerguride declined biphasically, with half-lives of 7 min and 1.2 h. The total clearance was 32 ml X min-1 X kg-1 and the apparent volume of distribution was 3.61/kg. The bioavailability of oral bromerguride was 29% after 1 mg and 25% after 2 mg. The drug was almost totally metabolized and less than 0.05% of the dose was excreted in urine in 24 h after oral administration. Plasma prolactin levels were increased in a dose-dependent manner for about 8 h. Side-effects were minimal, mainly being tiredness and headache in some of the volunteers.
mesh_terms: D000284:Administration, Oral; D000328:Adult; D001682:Biological Availability; D018492:Dopamine Antagonists; D004873:Ergolines / Q000494:pharmacology*; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008090:Lisuride / Q000031:analogs & derivatives / Q000494:pharmacology*; D008297:Male; D011388:Prolactin / Q000097:blood
chemical_list: D018492:Dopamine Antagonists; D004873:Ergolines; D011388:Prolactin; D008090:Lisuride; C039667:bromerguride