Cabergoline

Long-acting dopamine D2 receptor agonist, ergot derivative

ATC code: N04BC06 (Cabergoline)

Brand names

Dostinex, Cabaser

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.

Indications

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.

Sources

Drug–drug interactions

1 pair found. Sorted from critical to minor.

Critical

Itraconazole

Antifungal, 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.

Sources

AEMPS: Ficha tecnica de Dostinex (cabergolina) (2023)

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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

PregnancyFDA B

Can be used when planning pregnancy in prolactinoma; usually withdrawn once pregnancy confirmed.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

Breastfeeding

Suppresses lactation – not used in nursing mothers.

Calculate RID

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

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?

FDA category B. 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.

Mechanism of action

Drug–drug interactions

1 pair found. Sorted from critical to minor.

Critical

Itraconazole

Antifungal, 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.

Sources

AEMPS: Ficha tecnica de Dostinex (cabergolina) (2023)

Pair details →

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

PregnancyFDA B

Can be used when planning pregnancy in prolactinoma; usually withdrawn once pregnancy confirmed.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

Breastfeeding

Suppresses lactation – not used in nursing mothers.

Calculate RID

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

Frequently asked

What is Cabergoline used for?

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?

FDA category B. 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?