Brands, Medical Use, Clinical Data
- Antineoplastic Agents
- Antiparkinson Agents
- Dopamine Agonists
- Tablets for oral administration (0.5 mg)
Brands / Synonyms
Cabaser; Cabergolina [Spanish]; Cabergoline; Cabergoline [USAN:BAN:INN]; Cabergolinum [Latin]; Dostinex; Dostinex
For the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.
Cabergoline is a dopamine receptor agonist and uncategorized drug which suppresses the production of prolactin in pituitary gland. It is an ergot-derivative. It has at times been used as an adjunct to SSRI antidepressants as there is some evidence that it counteracts certain side effects of those drugs such as reduced libido and anorgasmia. It also has been suggested online that it has a possible recreational use in reducing or eliminating the male refractory period.
Mechanism of Action
The secretion of prolactin by the anterior pituitary is mainly under hypothalmic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. Cabergoline decreased serum prolactin levels in reserpinized rats. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1,- and α2- adrenergic, and 5-HT1- and 5-HT2-serotonin receptors.
First-pass effect is seen, however the absolute bioavailability is unknown.
Overdosage might be expected to produce nasal congestion, syncope, or hallucinations.
Biotrnasformation / Drug Metabolism
Hepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond or the urea moiety. Cytochrome P-450 mediated metabolism appears to be minimal.
DOSTINEX Tablets are contraindicated in patients with uncontrolled hypertension or known hypersensitivity to ergot
DOSTINEX should not be administered concurrently with D2-antagonists, such as phenothiazines,
butyrophenones, thioxanthines, or metoclopramide.