| Toxicity: |
An ergot alkaloid
derivative that exhibits potent dopamine agonist properties, particularly
at D2 dopamine receptors. Bromocriptine, like dopamine,
inhibits prolactin release from the pituitary and so is used in endocrine
disorders, such as hyperprolactinemia. It is also used in the
treatment of Parkinson’s disease. A large “first-pass” effect is seen
with bromocriptine, and peak concentrations occur about 1.5-3 h
after ingestion, with a half-life of about 3 h. Nausea, vomiting, and
orthostatic hypotension are among the acute adverse effects.
Long-term use has been associated with dyskinesias, constipation,
psychoses, digital spasm, and erythromelalgia. The LD50 in rabbits
exceeds 1 g/kg, p.o., and 12 mg/kg, i.v. |