Pergolide, a potent long-acting dopamine-receptor agonist

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Abstract
After single doses (100-400 .mu.g orally), pergolide, a synthetic ergot, reduced basal plasma prolactin levels in normal human subjects in a dose-related manner. This effect persisted for more than 24 h. Multiple doses of pergolide (150-250 .mu.g daily for 7 days) resulted in a plasma prolactin decrease of more than 80%. A single dose of pergolide (150 .mu.g orally) suppressed plasma prolactin and abolished the plasma prolactin diurnal rhythm, i.e., suppression of sleep-induced elevation in plasma prolactin during a 40-h period. Perphenazine (5 mg i.m.)-induced plasma prolactin elevation was inhibited by pergolide; the effect was dose-dependent. After single or multiple doses, pergolide had no effect on plasma follicle-stimulating hormone, luteinizing hormone, cortisol, growth hormone and thyroid-stimulating hormone. Pergolide appears to have specificity at the pituitary level for the dopamine receptors that mediate prolactin secretion.