Prolactin lowering effect of dihydroergokryptine in rat and in man

Abstract

The prolactin lowering activity of dihydroergokryptine was investigated both in rats and in humans. The drug was administered orally at the doses of 0.2, 1 and 5 mg/Kg to intact or reserpinized male rats. Nine male adult volunteers were given 300 mg cimetidine iv 90 min after receiving 2, 3 or 4.5 mg of dihydroergokryptine and 3, 4.5 and 6.75 mg of dihydroergocristine or placebo per os in a randomized, cross-over design. Eight young adult males were injected im with 10 mg sulpiride 120 min after randomly receiving dihydroergokryptine 2.5 and 5 mg or placebo in a cross-over manner. Finally, five healthy young women were given dihydroergokryptine 2.5 and 5 mg, bromocriptine 2.5 mg and placebo in a cross-over design. Dihydroergokryptine caused a strong, long-lasting, dose-dependent fall of plasma prolactin concentrations in both rats and humans. Moreover, it inhibited the reserpine-induced rise of plasma prolactin in rats, as well as the cimetidine-or sulpiride-induced hyperprolactinemia in humans. Dihydroergokryptine proved twice as potent as dihydroergocristine and about half as potent as bromocriptine. Effective doses of both dihydrogenated ergot alkaloids were much better tolerated than bromocriptine.

Dihydroergokryptine Versus Dihydroergotamine in Migraine Prophylaxis: A Double-Blind Clinical Trial

“…Alpha-dihydroergokryptine is a hydrogenated ergot alkaloid derivative endowed with dopaminergic activity. The dopaminergic activity of dihydroergokryptine has already been demonstrated with various methods, both in experimental animals and humans (1)(2)(3).…”

In VitroEffect and Mechanism of Action of Ergot Alkaloid Dihydroergocristine in Chemoresistant Prostate Cancer Cells

“…Dihydroergocristine (DHECS) is a dihydrogenated alkaloid of ergot (17) that mainly affects several neurological processes, including memory (18)(19)(20), cerebral hypoxia (21), sleepwakefulness cycle (22) and prolactin release (23,24). DHECS has been used, alone or combined with other ergot alkaloids, in the treatment of Parkinson's disease (25), peripheral vascular diseases (26), hypertension (27), hyperprolactinemia (28) and depression (29).…”