Evigrade

Cabergoline

Long-acting dopamine D2 receptor agonist, ergot derivative

ATC code: N04BC06

Brand names: Dostinex, Cabaser

Updated · Methodology

Indications

A

Hyperprolactinemia

First line

Cabergoline is first-line dopamine agonist for hyperprolactinemia and pituitary micro- and macroprolactinomas. SEEN recommends cabergoline due to better tolerability and convenient dosing (once or twice weekly 0.25–0.5 mg). Effect over 2–4 weeks. Less used in Parkinson disease due to high-dose valvulopathy risk.

ICD-10: E22.1 · ICD-11: 5A60.1

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

Highly selective long-acting D2 agonist (T½ 65 hours), supporting once or twice weekly dosing. Pituitary prolactin suppression is 5-fold stronger than bromocriptine. Stimulates 5-HT2B serotonin receptors on heart valves, raising valvulopathy risk at high doses (>3 mg/week in Parkinson disease). CYP3A4 metabolism is less prominent than for bromocriptine.

Safety

Contraindications

  • Uncontrolled hypertension
  • Prior valvulopathy
  • Eclampsia, preeclampsia
  • Combination with erythromycin, clarithromycin, itraconazole
  • Prior psychosis

Serious adverse effects

  • Valvular regurgitation (at doses above 3 mg/week in Parkinson)
  • Retroperitoneal and pleuropulmonary fibrosis
  • Impulse control disorders (gambling, hypersexuality)

Common adverse effects

  • Nausea
  • Headache
  • Dizziness
  • Orthostatic hypotension

Pregnancy: can you take Cabergoline?

Can be used when planning pregnancy in prolactinoma; usually withdrawn once pregnancy confirmed. Registry data show no increase in birth defects.

Breastfeeding: can you take Cabergoline?

Suppresses lactation – not used in nursing mothers.

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Drug–drug interactions

1 pair found. Sorted from critical to minor.

CriticalItraconazoleAntifungal, triazole

Mechanism

Itraconazole is the strongest CYP3A4 inhibitor. Cabergoline rises 5-7 fold. Valvulopathy and pulmonary fibrosis risk.

Symptoms

Dyspnoea, cardiac murmurs, edema.

Management

Combination contraindicated.

Pair details →Itraconazole →

Label mentions3 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • «DRUG INTERACTIONS: CABERGOLINE, a dopamine receptor agonist, is not recommended for concomitant use with D2-antagonists, such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide.»

    FDA, section 7 · Open on DailyMed

From other drugs’ labels

  • «Historia de hemorragia cerebral o con factores de riesgo que puedan aumentar el riesgo de hemorragia cerebral. Esto se debe a la actividad alfa-mimética de pseudoefedrina, en asociación con otros…»

    AEMPS, section 4.3 · Open on CIMA

  • «Aparato respiratorio: otros medicamentos para el aparato respiratorio: Cabergolina, Dienogest, Ulipristal»

    AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Cabergoline used for?

Cabergoline is evaluated for the following indications with varying evidence strength: Hyperprolactinemia (evidence tier A). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Cabergoline?

Common side effects of Cabergoline (≥ 1 in 100): Nausea, Headache, Dizziness, Orthostatic hypotension. See the Safety section for uncommon and serious reactions.

Is Cabergoline safe during pregnancy?

Can be used when planning pregnancy in prolactinoma; usually withdrawn once pregnancy confirmed. Registry data show no increase in birth defects.

Is Cabergoline compatible with breastfeeding?

Suppresses lactation – not used in nursing mothers.

Who should not take Cabergoline?

Cabergoline is contraindicated in: Uncontrolled hypertension; Prior valvulopathy; Eclampsia, preeclampsia; Combination with erythromycin, clarithromycin, itraconazole; Prior psychosis. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

Other drugs in this group

Bromocriptine, Levodopa + Carbidopa + Entacapone, Pramipexole, Rasagiline, Ropinirole, Selegiline