Cabergoline

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Cabaseril, Cabergolin, Dostinex; Belgium: Cabergoline, Dostinex, Sostilar; Bulgaria: Dostinex; Cyprus: Dostinex; Czech Republic: Cabera, Cabergolin, Dostinex; Denmark: Cabaser, Cabergolin, Dostinex; Finland: Cabaser, Dostinex; France: Cabergoline, Dostinex; Germany: Cabaser, Cabaseril, Caber-Q, Cabergolin, Dostinex; Greece: Cabergoline, Dostinex; Ireland: Cabaser, Caberex, Cabergoline, Dalzior, Dostinex, Eflavex; Italy: Actualene, Cabaser, Cabergolina, Dostinex; Latvia: Dostinex; Luxembourg: Cabergoline, Dostinex; Malta: Cabergoline, Dostinex; Netherlands: Cabergoline, Dostinex; Poland: CabergoLek, Cabergoline, Dostinex; Portugal: Dostinex; Romania: Dostinex; Slovakia: Cabest; Spain: Cabergolina, Dostinex, Sogilen; Sweden: Cabaser, Cabergoline, Cabergonicht, Dostinex, Kabergolin, Kabergostad; UK: Cabaser, Dostinex.

North America

Canada: Dostinex; USA: Cabergoline.

Latin America

Argentina: Cabaser, Caberpar, Cabertrix, Dostinex, Lac Stop, Lactamax, Triaspar; Brazil: Dostinex; Mexico: Dostinex.

Asia

Japan: Cabaser, Cabergoline, Dostinex.

Drug combinations

Chemistry

Cabergoline: C~26~H~37~N~5~O~2~. Mw: 451.60. (1) Ergoline-8β-carboxamide, N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-; (2) 1-[(6-Allylergolin-8β-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea. CAS-81409-90-7 (1996).

Pharmacologic Category

Antiparkinsonian Agents; Ergot-derivative Dopamine Receptor Agonists. (ATC-Code: G02CB03; N04BC06).

Mechanism of action

A long-acting dopamine receptor agonist. Has high binding affinity for dopamine D~2~ receptors and lesser affinity for D~1~, α~1~- and α~2~-adrenergic, and serotonin (5-HT~1~ and 5-HT~2~) receptors. Reduces serum prolactin concentrations by inhibiting release of prolactin from the anterior pituitary gland (agonist activity at D~2~ receptors).

Therapeutic use

Hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.

Pregnancy and lactiation implications

Not recommended for use in patients with pregnancy-induced hypertension unless benefit outweighs potential risk. Interferes with lactation and should not be given to women postpartum who are breast-feeding or who are planning to breast-feed. Not indicated for inhibition or suppression of physiologic lactation.

Unlabeled use

Symptomatic management of parkinsonian syndrome (adjunct to levodopa).

Contraindications

Hypersensitivity to ergot derivatives. Uncontrolled hypertension. History of pulmonary, pericardial, cardiac valvular or retroperitoneal fibrotic disorders.

Warnings and precautions

Cardiac valvular disease (mitral, aortic, tricuspid regurgitation) has been associated with cabergoline. Initial doses >1 mg may cause orthostatic hypotension (concurrent use with antihypertensives may increase risk). Rare cases of pleural effusion, pulmonary/retroperitoneal fibrosis reported with prolonged daily use. Pathological gambling, increased libido, and hypersexuality reported with use (reversible with dose reduction or discontinuation). Should not be used in pregnancy-induced hypertension unless benefit outweighs potential risk. Antipsychotics may decrease the therapeutic effects of cabergoline (avoid combination).

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