Active ingredient: Cabergoline - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Antineoplastic Agents
• Antiparkinson Agents
• Dopamine Agonists

Dosage Forms

• Tablets for oral administration (0.5 mg)

Brands / Synonyms

Cabaser; Cabergolina [Spanish]; Cabergoline; Cabergoline [USAN:BAN:INN]; Cabergolinum [Latin]; Dostinex; Dostinex

Indications

For the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.

Pharmacology

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.

Absorption

First-pass effect is seen, however the absolute bioavailability is unknown.

Toxicity

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.

Contraindications

DOSTINEX Tablets are contraindicated in patients with uncontrolled hypertension or known hypersensitivity to ergot derivatives.

Drug Interactions

DOSTINEX should not be administered concurrently with D₂-antagonists, such as phenothiazines, butyrophenones, thioxanthines, or metoclopramide.