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An ergot alkaloidderivative that exhibits potent dopamine agonist properties, particularlyat D2 dopamine receptors. Bromocriptine, like dopamine,inhibits prolactin release from the pituitary and so is used in endocrinedisorders, such as hyperprolactinemia. It is also used in thetreatment of Parkinson’s disease. A large “first-pass” effect is seenwith bromocriptine, and peak concentrations occur about 1.5-3 hafter ingestion, with a half-life of about 3 h. Nausea, vomiting, andorthostatic hypotension are among the acute adverse effects.Long-term use has been associated with dyskinesias, constipation,psychoses, digital spasm, and erythromelalgia. The LD50 in rabbitsexceeds 1 g/kg, p.o., and 12 mg/kg, i.v.
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