Cabergoline

Brand Names: Dostinex

Drug Class: Dopamine agonist

Overview

Cabergoline is a dopamine agonist used to treat hyperprolactinemic disorders, including those caused by pituitary adenomas. It works by inhibiting prolactin secretion from the pituitary gland. Treatment requires careful cardiovascular monitoring due to potential valvular heart disease risks.

Mechanism of Action

Cabergoline is a long-acting dopamine D2 receptor agonist that directly inhibits prolactin secretion from the anterior pituitary gland. It has high affinity and selectivity for dopamine receptors, resulting in sustained suppression of prolactin levels.

Indications

  • Treatment of hyperprolactinemic disorders
  • Idiopathic hyperprolactinemia
  • Hyperprolactinemia due to pituitary adenomas

Common Doses

  • 0.25 mg
  • 0.5 mg
  • 1 mg

Dosage

Initial dose: 0.25 mg twice weekly. May increase by 0.25 mg twice weekly every 4 weeks based on serum prolactin response, up to maximum of 1 mg twice weekly. Requires pre-treatment cardiovascular evaluation and periodic cardiac monitoring during long-term therapy.

Contraindications

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

Side Effects

  • Nausea
  • Headache
  • Dizziness
  • Fatigue
  • Constipation
  • Postural hypotension
  • Valvular heart disease with long-term use

Interactions

  • Contraindicated with dopamine antagonists (phenothiazines, butyrophenones, thioxanthenes, metoclopramide)
  • May potentiate hypotensive effects of antihypertensive medications
  • Use caution with other medications affecting dopamine pathways

Counseling Points

  • Take exactly as prescribed, typically twice weekly
  • Report symptoms of dizziness, fainting, or shortness of breath immediately
  • Regular cardiac monitoring is required during treatment
  • Avoid sudden position changes to prevent dizziness
  • Do not take with dopamine-blocking medications
  • Use effective contraception during treatment