Prolactin-Lowering Effect of Acute and Once Weekly Repetitive Oral Administration of Cabergoline at Two Dose Levels in Hyperprolactinemic Patients

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Abstract
To further evaluate the potency and time course of the PRL-lowering effect of single oral doses of cabergoline, two doses of the drug were given to 51 hyperprolactinemic patients who also received 2.5 mg bromocriptine according to a randomized cross-over design. On group (n=26) received 0.3 mg, and the other (n=25) received 0.6 mg. Both cabergoline doses induced a significant fall in serum PRL levels, which lasted, on the average, from 3 h to 5 days after 0.3 mg and from 3 h to 14 days after 0.6 mg; the mean maximum decrease after 0.3 mg was -65 .+-. 4% (.+-.SEM), significantly less than that after bromocriptine (group mean, -73 .+-. 4%), and it was -76 .+-. 3% after 0.6 mg, not significantly different from that induced by bromocriptine (group mean, -71 .+-. 4%). The effect of mg cabergoline was significantly greater than that of 0.3 mg (P50% of pretreatment values) occurred in all patients treated with 0.6 mg and in 13 treated with 0.3 mg weekly. Resumption of menses occurred during the treatment period in 15 of the 17 premenopausal women with amenorrhea. Six patients who had poor responses had better responses when given higher drug doses for 4 weeks, and serum PRL levels became normal in the 3 receiving 0,6 mg twice weekly. These data confirm that cabergoline is a long is long acting oral dopaminergic drug and suggest that it may be a useful agent for the treatment of patients with hyperprolactinemia.