Cabergoline (2 brand names, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- CABERGOLINE
- DOSTINEX
Indications and Usage
CABERGOLINE is an ergot derivative indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas in adults. Limitations of Use Avoid use of CABERGOLINE for the inhibition or suppression of postpartum physiologic lactation because of the risk of serious adverse reactions [see Warnings and Precautions (5.4)].
Contraindications
CABERGOLINE is contraindicated in patients with: •Uncontrolled hypertension. •Known hypersensitivity to ergot derivatives. •History of cardiac valvular disorders, as suggested by anatomical evidence of valvulopathy of any valve, determined by pre-treatment evaluation including echocardiographic demonstration of valve leaflet thickening, valve restriction, or mixed valve restriction-stenosis, or history of pericardial fibrosis [see Warnings and Precautions (5.1)]. •History of pleural, pulmonary, or retroperitoneal fibrotic disorders [see Warnings and Precautions (5.2)].
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: •Cardiac Valvulopathy and Pericardial Fibrosis [see Warnings and Precautions (5.1)]. •Pleural, Retroperitoneal, and Pulmonary Fibrosis [see Warnings and Precautions (5.2)]. •Orthostatic Hypotension [see Warnings and Precautions (5.3)]. •Impulse Control Disorders and Compulsive Behaviors [see Warnings and Precautions (5.5)].
Drug Interactions
CABERGOLINE, a dopamine receptor agonist, is not recommended for concomitant use with D2-antagonists, such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide.
Mechanism of Action
Cabergoline is an ergot derivative and 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.
Overdosage
Take measures to support blood pressure, if necessary. Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.