Cabergoline: How It Lowers Prolactin, What the Trials Found and Its Heart-Valve Warning

Cabergoline is a prescription tablet that lowers prolactin, the pituitary hormone that drives breast-milk production. Too much prolactin can stop periods, cause milk to leak from the breasts, lower sex drive and cause infertility in both women and men. The most common cause is a prolactinoma, a benign tumor of the pituitary gland. Cabergoline is the medicine most often used for it, and in many people it shrinks the tumor as well as lowering the hormone.

This page covers how the medicine works, why it is taken only twice a week, what the main trials found, its other uses, the heart-valve story that changed how it is monitored, and the other safety findings reported in the research and in the United States label. The Prolactinoma page describes the tumor itself, its symptoms and how it is diagnosed.

Table of Contents

  1. What Cabergoline Is
  2. How Dopamine Holds Prolactin Down and How Cabergoline Copies It
  3. A Long Half-Life and a Twice-Weekly Schedule
  4. The 1994 Trial Against Bromocriptine
  5. The 1999 Belgian Series of 455 Patients
  6. Stopping the Medicine and How Often Prolactin Stays Normal
  7. The 2023 Pituitary Society Consensus
  8. Acromegaly
  9. Stopping Breast-Milk Production After Childbirth
  10. The Parkinson's Disease Years
  11. The Heart-Valve Findings at Parkinson's Doses
  12. Heart Valves at the Lower Doses Used for Prolactin
  13. What the United States Label Requires and Who It Excludes
  14. Impulse-Control Disorders
  15. Fibrosis, Low Blood Pressure and the Common Side Effects
  16. Pregnancy Data as Reported
  17. What Is Not Yet Known
  18. Key Research Papers
  19. Connections
  20. Featured Videos

What Cabergoline Is

Cabergoline is a dopamine agonist: a medicine that switches on the same receptors that the brain chemical dopamine switches on. Chemically it is an ergot derivative. Ergot is a fungus that grows on rye, and its natural compounds were the starting point for a whole family of medicines in the twentieth century, including the older prolactin-lowering drug bromocriptine. The Albert Hofmann page tells part of that ergot story.

The United States label lists the medicine’s first United States approval as 1996 and its approved use as “the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas in adults.” In plain words: high prolactin with no tumor found (idiopathic), or high prolactin caused by a pituitary tumor. The label describes 0.5 mg tablets.

Three dopamine agonists are used for high prolactin: cabergoline, bromocriptine (also ergot-derived, taken daily) and quinagolide (not ergot-derived). Most of the research on this page compares cabergoline with bromocriptine, the older standard.

How Dopamine Holds Prolactin Down and How Cabergoline Copies It

Most pituitary hormones are pushed up by signals from the brain. Prolactin is the exception: it is held down. Nerve cells in the hypothalamus, just above the pituitary, release dopamine into the small blood vessels that run to the gland. The dopamine lands on dopamine type 2 (D2) receptors on the prolactin-making cells, called lactotrophs, and acts as a brake on them. When the brake weakens — because a tumor grows, a stalk is pressed, or a medicine blocks the receptors — prolactin rises.

Cabergoline puts the brake back on. The label describes it as a dopamine receptor agonist “with a high affinity for D2 receptors,” and reports that in laboratory studies it directly reduced prolactin release from rat pituitary cells. The same label says it has low affinity for the D1 dopamine receptor and for several adrenaline-type and serotonin receptors.

The prolactinoma cells themselves carry D2 receptors. When those receptors are switched on, the cells make less hormone and, in many people, shrink. This is why a tablet can shrink a tumor without surgery: in the 1999 Belgian series described below, the tumor shrank in 67% of patients.

Dopamine also acts in other parts of the brain, including the reward system, which is the background to the impulse-control findings described further down. Medicines that do the opposite job — blocking D2 receptors — work against cabergoline. The label states that cabergoline “is not recommended for concomitant use with D2-antagonists, such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide.”

A Long Half-Life and a Twice-Weekly Schedule

A medicine’s half-life is the time the body takes to clear half of it. The United States label reports that the half-life of cabergoline, estimated from urine data in 12 healthy volunteers, ranged from 63 to 69 hours — close to three days. Bromocriptine, by comparison, is taken every day. The label also reports the following:

The long half-life is what allows a twice-weekly schedule. The label states a starting dosage of 0.25 mg by mouth twice weekly. It describes raising the dose by 0.25 mg twice weekly, at intervals of no less than 4 weeks, until prolactin is normal, and gives 1 mg twice weekly as the maximum recommended dosage. In the label’s 4-week dose-finding trial in 188 women, prolactin became normal in 0% on placebo and in 76%, 74% and 95% of the three groups given the higher cabergoline doses.

The 1994 Trial Against Bromocriptine

The trial that set cabergoline apart was published in the New England Journal of Medicine in 1994 by Webster and colleagues. It enrolled 459 women whose periods had stopped because of high prolactin. Of them, 279 had a small prolactinoma (a microprolactinoma), 167 had high prolactin with no tumor seen, and a few had other causes.

The women were randomly given cabergoline or bromocriptine. The trial gave cabergoline at 0.5 to 1.0 mg twice weekly and bromocriptine at 2.5 to 5.0 mg twice daily. Neither the women nor their doctors knew which tablet was which for the first 8 weeks; after that the trial continued openly for 16 more weeks. The results:

The authors concluded that cabergoline was more effective and better tolerated than bromocriptine in these women. Nausea was the most common complaint in both groups. In the label’s table from the first 8 weeks of this trial, nausea was reported by 29% on cabergoline and 43% on bromocriptine.

The 1999 Belgian Series of 455 Patients

A trial shows what happens under controlled conditions. Verhelst and colleagues looked instead at ordinary practice: they went back through the records of 455 patients (102 men and 353 women) treated with cabergoline at 9 Belgian hospitals. Unlike the 1994 trial, this group included many large tumors: 42% had a macroadenoma (10 mm or more), 41% a microadenoma and 16% high prolactin with no tumor seen. Of the 455, 292 had taken bromocriptine before.

Because it was a look back at records, without a comparison group, this study shows how the medicine performed in practice rather than proving it beat anything else.

Stopping the Medicine and How Often Prolactin Stays Normal

An important question for anyone on a dopamine agonist is whether the tablets can ever stop. In 2010 Dekkers and colleagues pooled 19 studies with 743 patients in whom a dopamine agonist had been stopped and prolactin was then measured.

The authors wrote that the probability of success was highest when cabergoline had been used for at least 2 years. The results of the individual studies varied a great deal, so these averages hide a wide spread. The Prolactinoma page describes when a supervised trial off the medicine is considered.

The 2023 Pituitary Society Consensus

In 2023 the Pituitary Society published an international consensus statement on prolactinomas, with 36 authors, from first author Stephan Petersenn to last author Shlomo Melmed. It gives graded recommendations on diagnosis and treatment. According to its summary, it covers the following:

The statement concluded that resistance to treatment is rare, but that more treatment options and international patient registries are needed.

Acromegaly

Acromegaly is caused by a pituitary tumor that makes too much growth hormone. The hormone’s effects are measured with a blood test for insulin-like growth factor 1 (IGF-1), which the liver makes in response to growth hormone. Cabergoline has been tried in acromegaly for years, although, as the meta-analysis below notes, it was widely considered poorly effective there.

In 2011 Sandret, Maison and Chanson pooled 15 studies with 237 patients. None of the studies was randomized or compared with placebo, which limits how firm the findings are.

Cabergoline is not approved in the United States for acromegaly; its label covers high-prolactin disorders only.

Stopping Breast-Milk Production After Childbirth

Because prolactin drives milk production, cabergoline has also been studied for stopping milk after childbirth, in women who do not wish to breastfeed. The How Breast Milk Is Made animation shows the hormone loop involved.

A randomized, double-blind trial of 272 women in European hospitals, published in 1991, gave one group a single 1 mg dose of cabergoline within 27 hours of delivery and the other group bromocriptine 2.5 mg twice daily for 14 days.

A 2020 systematic review of 25 studies, covering 757 women given cabergoline to stop or suppress milk, found 108 adverse events in 96 women (14.2%). The most common were dizziness (35 women), headache (30) and nausea or vomiting (19), described as short-lived and dose-dependent. One drug-safety study it included reported 29 serious events among 175 events in 72 case reports, including blood clots and neurological events, and half of 4 case studies in people with psychiatric illness reported psychiatric symptoms after the medicine.

The United States label lists this use under “Limitations of Use,” citing “the risk of serious adverse reactions,” and states that bromocriptine used for the same unapproved purpose “has been associated with cases of hypertension, stroke, myocardial infarction, seizures, and death.” It also states that cabergoline “is not recommended in postpartum women who are breastfeeding or who are planning to breastfeed.”

The Parkinson's Disease Years

In Parkinson’s disease, the brain loses the nerve cells that make dopamine, and dopamine agonists can stand in for some of the missing signal. Through the 1990s cabergoline was studied for this at much higher daily doses than those used for prolactin.

That use largely ended after the heart-valve findings described next. The United States label states plainly that cabergoline “is not approved for the treatment of PD” (Parkinson’s disease). A 2018 meta-analysis wrote that high-dose use in Parkinson’s disease “has largely been abandoned” because of the valve problem.

The Heart-Valve Findings at Parkinson's Doses

Heart valves are thin flaps that keep blood flowing one way. When a valve becomes thickened and stiff it may not close fully, and blood leaks backward. This is called regurgitation. Two studies published together in the New England Journal of Medicine in January 2007 linked ergot-derived dopamine agonists to this kind of valve damage.

The leading explanation involves a serotonin receptor called 5-HT2B, which sits on the cells inside heart valves. A 2011 laboratory study in pig tissue found that cabergoline acted as a potent full activator of this receptor, and traced that action to one part of the molecule. The authors described activation of this receptor as the most likely cause of the valve disease. This sits beside the label’s summary of low affinity for serotonin type 2 receptors, which shows the question is not fully settled.

The United States label reports that valve cases “have generally occurred during administration of high doses of CABERGOLINE (>2 mg/day) for the treatment of Parkinson’s disease” and that cases “have also been reported in patients who received lower dosages.” It also cites a 12-year study in several countries in which valve leakage in people with Parkinson’s disease occurred at 68 per 10,000 person-years on cabergoline, compared with 10 on non-ergot dopamine agonists and 11 on levodopa. The Valvular Heart Disease page describes valve disease from all causes.

Heart Valves at the Lower Doses Used for Prolactin

The doses used for prolactin are much lower. In the Belgian series above, the median dose was 1.0 mg per week, while the Parkinson’s trial gave up to 4 mg every day. So the question after 2007 was whether the low doses also harm valves.

In 2018 Stiles and colleagues pooled 13 case-control studies of people who had taken cabergoline for at least 6 months for high prolactin, comparing their heart scans with people who had not.

The authors wrote that low-dose cabergoline “appears to be associated with an increased prevalence of tricuspid regurgitation,” and that “the clinical significance of this is unclear and requires further investigation.”

What the United States Label Requires and Who It Excludes

The United States label turns these findings into firm instructions. Before treatment, it states: “Before initiating CABERGOLINE evaluate for valvular heart disease, including with an echocardiogram. If valvular disease is detected, do not administer CABERGOLINE.” An echocardiogram is an ultrasound scan of the heart.

During treatment, the label calls for monitoring “for the development of valvulopathy with a cardiac echocardiogram at intervals of 6 to 12 months or as clinically indicated with new onset edema, cardiac murmur, dyspnea, or heart failure.” It also calls for stopping the medicine “if the patient has a new diagnosis of valvular regurgitation, valvular restriction, valve leaflet thickening, or pericarditis.” The label notes that valve and pericardial scarring “have often manifested as heart failure.”

The label lists these contraindications, word for word:

Pericardial fibrosis is scarring of the sac around the heart. Pleural, pulmonary and retroperitoneal fibrosis are scarring of the lining of the lungs, the lungs themselves, and the tissue at the back of the abdomen. The label also lists severe liver disease (Child-Pugh class C) as a group in which use is “not recommended.”

Impulse-Control Disorders

Medicines that boost dopamine signalling in the brain can, in some people, produce urges that are hard to control. These problems are well documented in Parkinson’s disease and have since been studied at prolactinoma doses.

The United States label states that patients “can experience intense urges to gamble or to spend money, increased sexual urges, binge eating, and/or other intense urges, and the inability to control these urges.” It notes that people may not recognise these behaviours as abnormal, which is why the label asks health care providers to ask specifically about “new or increased gambling urges, sexual urges, uncontrolled spending, or other urges.” It reports that in some cases the urges stopped when the dose was reduced or the medicine was stopped. Reports after approval also list psychotic disorder and aggression.

A 2025 meta-analysis by Penchev and colleagues pooled 8 observational studies with 858 people with prolactinoma, 483 of whom were treated with dopamine agonists.

The authors noted that because all the studies were observational, the links are associations and need cautious reading.

Fibrosis, Low Blood Pressure and the Common Side Effects

Scarring (fibrosis) can also occur outside the heart. The United States label reports cases after approval of pleural, pulmonary and retroperitoneal fibrosis following cabergoline, some in people who had taken other ergot dopamine agonists before. It reports that people who developed fluid around the lungs or lung scarring and then stopped cabergoline had improvement in their lung symptoms. The signs it lists for monitoring include shortness of breath, a persistent cough, chest pain, pain in the loin or flank, and swelling of the legs.

The label also describes a drop in blood pressure on standing up (orthostatic hypotension). In its 4-week placebo-controlled trial, this occurred in 4% on cabergoline and 0% on placebo, and the label states the risk is greater alongside other medicines that lower blood pressure.

The label gives nausea, headache and dizziness as the most common side effects, each above 10%. In that 4-week trial in women with high prolactin:

Hair loss is also listed among reports after approval.

Pregnancy Data as Reported

Because cabergoline often restores fertility, many women become pregnant while taking it. Studies compare women who stopped the medicine when pregnancy was diagnosed with women who continued it.

A 2025 systematic review and meta-analysis by Chakraborty and Rastogi pooled 12 studies covering 1,387 pregnancies in women with prolactinoma.

The United States label states that published case reports “have not reported a clear association” between cabergoline used in early pregnancy and major birth defects, miscarriage or harm to the baby, but that these reports “cannot definitely establish the absence of CABERGOLINE-associated risk.” For comparison it gives the background risk in the United States population: 2% to 4% for major birth defects and 15% to 20% for miscarriage in recognised pregnancies. It also states that the risks of the medicine rise in women with pregnancy-induced high blood pressure, preeclampsia and eclampsia. In the Belgian series, 25 of 27 women who became pregnant on cabergoline delivered a healthy child. The Female Infertility page covers high prolactin as a cause of infertility.

What Is Not Yet Known

Decisions about starting, monitoring or stopping a prescription medicine belong with the clinician who prescribes it.

Key Research Papers

  1. Webster J, Piscitelli G, Polli A, Ferrari CI, Ismail I, Scanlon MF. A comparison of cabergoline and bromocriptine in the treatment of hyperprolactinemic amenorrhea. Cabergoline Comparative Study Group. N Engl J Med. 1994;331(14):904-9. PubMed PMID: 7915824
  2. Verhelst J, Abs R, Maiter D, van den Bruel A, Vandeweghe M, Velkeniers B, Mockel J, Lamberigts G, Petrossians P, Coremans P, Mahler C, Stevenaert A, Verlooy J, Raftopoulos C, Beckers A. Cabergoline in the treatment of hyperprolactinemia: a study in 455 patients. J Clin Endocrinol Metab. 1999;84(7):2518-22. PubMed PMID: 10404830
  3. Dekkers OM, Lagro J, Burman P, Jørgensen JO, Romijn JA, Pereira AM. Recurrence of hyperprolactinemia after withdrawal of dopamine agonists: systematic review and meta-analysis. J Clin Endocrinol Metab. 2010;95(1):43-51. PubMed PMID: 19880787
  4. Petersenn S, Fleseriu M, Casanueva FF, Giustina A, Biermasz N, Biller BMK, Bronstein M, Chanson P, Fukuoka H, Gadelha M, Greenman Y, Gurnell M, Ho KKY, Honegger J, Ioachimescu AG, Kaiser UB, Karavitaki N, Katznelson L, Lodish M, Maiter D, Marcus HJ, McCormack A, Molitch M, Muir CA, Neggers S, Pereira AM, Pivonello R, Post K, Raverot G, Salvatori R, Samson SL, Shimon I, Spencer-Segal J, Vila G, Wass J, Melmed S. Diagnosis and management of prolactin-secreting pituitary adenomas: a Pituitary Society international Consensus Statement. Nat Rev Endocrinol. 2023;19(12):722-740. PubMed PMID: 37670148
  5. Sandret L, Maison P, Chanson P. Place of cabergoline in acromegaly: a meta-analysis. J Clin Endocrinol Metab. 2011;96(5):1327-35. PubMed PMID: 21325455
  6. European Multicentre Study Group for Cabergoline in Lactation Inhibition. Single dose cabergoline versus bromocriptine in inhibition of puerperal lactation: randomised, double blind, multicentre study. BMJ. 1991;302(6789):1367-71. PubMed PMID: 1676318
  7. Harris K, Murphy KE, Horn D, MacGilivray J, Yudin MH. Safety of Cabergoline for Postpartum Lactation Inhibition or Suppression: A Systematic Review. J Obstet Gynaecol Can. 2020;42(3):308-315.e20. PubMed PMID: 31285168
  8. Hutton JT, Koller WC, Ahlskog JE, Pahwa R, Hurtig HI, Stern MB, Hiner BC, Lieberman A, Pfeiffer RF, Rodnitzky RL, Waters CH, Muenter MD, Adler CH, Morris JL. Multicenter, placebo-controlled trial of cabergoline taken once daily in the treatment of Parkinson's disease. Neurology. 1996;46(4):1062-5. PubMed PMID: 8780092
  9. Rinne UK, Bracco F, Chouza C, Dupont E, Gershanik O, Marti Masso JF, Montastruc JL, Marsden CD. Early treatment of Parkinson's disease with cabergoline delays the onset of motor complications. Results of a double-blind levodopa controlled trial. The PKDS009 Study Group. Drugs. 1998;55 Suppl 1:23-30. PubMed PMID: 9483167
  10. Zanettini R, Antonini A, Gatto G, Gentile R, Tesei S, Pezzoli G. Valvular heart disease and the use of dopamine agonists for Parkinson's disease. N Engl J Med. 2007;356(1):39-46. PubMed PMID: 17202454
  11. Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E. Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med. 2007;356(1):29-38. PubMed PMID: 17202453
  12. Kekewska A, Hübner H, Gmeiner P, Pertz HH. The bulky N6 substituent of cabergoline is responsible for agonism of this drug at 5-hydroxytryptamine 5-HT2A and 5-HT2B receptors and thus is a determinant of valvular heart disease. J Pharmacol Exp Ther. 2011;338(1):381-91. PubMed PMID: 21518772
  13. Stiles CE, Tetteh-Wayoe ET, Bestwick J, Steeds RP, Drake WM. A meta-analysis of the prevalence of cardiac valvulopathy in hyperprolactinemic patients treated with Cabergoline. J Clin Endocrinol Metab. 2018 Sep 11. doi: 10.1210/jc.2018-01071. PubMed PMID: 30215804
  14. Penchev P, Milanova-Ilieva D, Gaydarski L, Husain N, Chenkov Y, Petrov PP, Kirovakov Z, Stanchev P. Impulse control disorders in prolactinoma patients treated with dopamine agonists: a systematic review and meta-analysis with trial sequential analysis. J Clin Neurosci. 2025;138:111363. PubMed PMID: 40480033
  15. Chakraborty AM, Rastogi A. Safety of Cabergoline for Prolactinoma in Pregnancy: A Systematic Review and Meta-Analysis. Clin Endocrinol (Oxf). 2025;103(5):633-640. PubMed PMID: 40629810
  16. U.S. National Library of Medicine, DailyMed. Cabergoline tablets, prescribing information (indications, dosage, contraindications, warnings and precautions, pregnancy, clinical pharmacology). DailyMed label

PubMed Topic Searches

  1. Cabergoline and prolactinoma
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  4. Cabergoline and impulse-control disorders
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  6. Cabergoline and acromegaly

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