Pharmacology · Dopamine agonists
Cabergoline !
A long-acting ergot dopamine agonist that lowers prolactin and shrinks prolactinomas. Valve disease and fibrosis are the key risks.
Updated 2026-11-01
The figure shows bromocriptine, another ergot dopamine agonist, in the human D2 receptor; cabergoline binds the same dopamine site.
Mechanism of action
Cabergoline is an ergot derivative with high affinity for D2 receptors. On pituitary lactotroph cells, D2 stimulation directly inhibits prolactin secretion; prolactin falls and prolactin-secreting adenomas shrink. It has low affinity for D1, adrenergic and some serotonin receptors.
- Cabergoline binds D2 receptors on pituitary lactotrophs
- Prolactin synthesis and release are switched off
- Prolactin falls and the adenoma shrinks
- Periods, fertility and libido can return
Pharmacokinetics
- Metabolism
- Extensive first-pass metabolism in the liver
- Half-life
- Very long: about 63 to 69 hours, allowing doses once or twice a week
Indications
- Hyperprolactinaemic disorders, idiopathic or due to a pituitary adenoma (prolactinoma) Prolactinoma (hyperprolactinaemia) →
- Parkinson disease: little used today because of the risk of valve disease Parkinson disease →
Adverse effects
Common
- Nausea and vomiting
- Headache and dizziness
- Orthostatic hypotension
- Constipation
Contraindications
- Uncontrolled hypertension
- Hypersensitivity to ergot derivatives
- History of cardiac valve disease or pericardial fibrosis
- History of pleural, pulmonary or retroperitoneal fibrosis
Key interactions
- Dopamine antagonists (antipsychotics, metoclopramide)
- Oppose its prolactin-lowering effect
- Antihypertensives
- Additive fall in blood pressure
What is monitored
- Echocardiogram before starting and periodically during treatment
- Serum prolactin and, for adenomas, pituitary imaging
- Blood pressure and orthostatic symptoms
- Breathlessness, chest pain, oedema or flank pain (fibrosis)
Administration and safety
- Given by mouth, usually once or twice a week
- Not used to suppress normal postpartum lactation because of serious cardiovascular and neurological risks
- Taking it with food can reduce nausea
Nursing care
- Confirm a baseline echocardiogram has been done
- Check blood pressure lying and standing at the start
- Ask about gambling, shopping or sexual urges
- Teach to report breathlessness, cough, chest pain or swelling
Pregnancy and breastfeeding
Fertility can return quickly as prolactin falls; if pregnancy occurs, continuation is weighed by the specialist.
Test yourself
Think of the answer, then tap the question to see it.
What is the first-line medical treatment of a prolactinoma?
A dopamine agonist, usually cabergoline (bromocriptine is the alternative).
Which test is done before and during cabergoline treatment, and why?
An echocardiogram, because ergot dopamine agonists can cause cardiac valve disease.
Why can cabergoline be given only once or twice a week?
Its elimination half-life is very long, around 63 to 69 hours.
Related drugs
Related conditions
← Back to the class: Dopamine agonists
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - CABERGOLINE tablet (DailyMed (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 46 (McGraw Hill, 2023); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 15 (McGraw Hill, 2023); eEML - Electronic Essential Medicines List (World Health Organization, 2025).
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Representative model, for educational purposes only.