Cabergoline
生产企业：Impax laboratories inc, Ivax pharmaceuticals inc sub teva pharmaceuticals usa，另有 3 家
Cabergoline is a dopamine receptor agonist used for the treatment of hyperprolactinemic conditions due to various causes.
Cabergoline is a dopamine receptor agonist used for the treatment of hyperprolactinemic conditions due to various causes.
The dopamine D receptor is a 7-transmembrane G-protein coupled receptor associated with G proteins. In lactotrophs, stimulation of dopamine D causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α,- and α- adrenergic, and 5-HT- and 5-HT-serotonin receptors.
For the treatment of hyperprolactinemic disorders, either idiopathic or due to prolactinoma (prolactin-secreting adenomas). May also be used to manage symptoms of Parkinsonian Syndrome as monotherapy during initial symptomatic management or as an adjunct to levodopa therapy during advanced stages of disease.
