- Cabergoline
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, an ergot derivative, is a potent dopamine receptor agonist on D2 receptors. There are some basic informations about this crude drug: (1)CAS No.: ; (2)Formula: C26H37N5O2; (3)Mol. mass: 451.604 g/mol; (4)PubChem: CID 54746; (5)IUPHAR: ligand 37; (6)DrugBank: APRD00836; (7)ChemSpider: 49452.
Cabergoline is frequently used as a first-line agent in the management of prolactinomas due to higher affinity for D2 receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine. Farmitalia filed for patent protection of Cabergoline in 1982, and U.S. Patent 4,526,892 was granted in July 1985.
Uses of Cabergoline:
♦ Hyperprolactinemia.
♦ Adjunctive therapy of prolactin-producing pituitary gland tumors (prolactinomas).
♦ Monotherapy of Parkinson's disease in the early phase.
♦ Combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson's disease.
♦ In some countries also: ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovulation, nonpuerperal mastitis and galactorrhea).
♦ Treatment of uterine fibroids.
♦ Adjunctive or second line therapy of acromegaly, cabergoline has low efficacy in suppressing growth hormone levels and is highly efficient in suppressing hyperprolactinemia that is present in 20-30% of acromegaly cases. Growth hormone and prolactin are similar structurally and have similar effects in many target tissues, therefore targeting prolactin may help symptoms when growth horomone secretion can not be sufficiently controlled by other methods.
♦ Cushing's disease - cabergoline may be used to lower ACTH levels and cause regression of ACTH producing pituitary adenomas.
♦ Other pituitary adenomas - cabergoline has demonstrated certain efficacy in controlling or reducing other kinds of pituitary adenomas, as well as silent or non-fucntional adenomas.
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