# Cabergoline
**Cabergoline**, sold under the brand name Dostinex, is a synthetic ergoline derivative and long-acting dopamine receptor agonist with high affinity for the dopamine D2 receptor, used to treat hyperprolactinemia (elevated blood prolactin) and, at higher doses, [Parkinson's disease](https://www.edgepedia.org/parkinsons-disease)[1](https://www.cancer.gov/publications/dictionaries/cancer-drug/def/cabergoline) • [2](https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=c9f0b576-d5e5-4e3e-bb5c-3574d75d9907). It was first approved in the United States in 1996[2](https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=c9f0b576-d5e5-4e3e-bb5c-3574d75d9907).
| Key fact | Detail |
|---|---|
| Drug class | Synthetic ergoline derivative; long-acting dopamine receptor agonist with high affinity for D2 receptors[1](https://www.cancer.gov/publications/dictionaries/cancer-drug/def/cabergoline) |
| Chemistry | Chemical name 1-[(6-allylergolin-8β-yl)-carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea; formula C₂₆H₃₇N₅O₂; molecular weight 451.62[3](https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020664s011lbl.pdf) |
| Elimination half-life | 63 to 109 hours estimated from urinary data in healthy subjects[4](https://pubmed.ncbi.nlm.nih.gov/12844325/) |
| Dosing schedule | Twice weekly for hyperprolactinemia; once daily for Parkinson's disease[4](https://pubmed.ncbi.nlm.nih.gov/12844325/) |
| First-line status | Recommended over other dopamine agonists for prolactinoma for higher efficacy in normalizing prolactin and shrinking tumors[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false) • [6](https://www.nature.com/articles/s41574-023-00886-5) |
| Resistance rates | Approximately 10% of prolactinoma patients resistant to cabergoline versus approximately 25% to bromocriptine[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false) |
| Main safety concern | Cardiac valve regurgitation and fibrotic disorders, chiefly at high Parkinson's disease doses (at least 3 mg/day)[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false) • [7](https://www.ema.europa.eu/en/medicines/human/referrals/ergot-derived-dopamine-agonists) |
## Mechanism and pharmacology
Prolactin secretion by the anterior pituitary is mainly under hypothalamic inhibitory control, exerted through dopamine released by tuberoinfundibular neurons. Cabergoline mimics this signal: it is a long-acting agonist with high affinity for D2 receptors, and in vitro studies show a direct inhibitory effect on prolactin secretion by pituitary lactotroph cells[3](https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020664s011lbl.pdf). Receptor-binding studies indicate low affinity for dopamine D1, α1- and α2-adrenergic, and 5-HT1 and 5-HT2 serotonin receptors[3](https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020664s011lbl.pdf).
The pharmacokinetic profile explains its dosing schedule. Cabergoline is extensively metabolized by the liver, predominantly by hydrolysis of the acylurea bond, with minimal cytochrome P450-mediated metabolism; less than 4% is excreted unchanged in the urine, and it is about 40% bound to plasma proteins[4](https://pubmed.ncbi.nlm.nih.gov/12844325/). The elimination half-life of 63 to 109 hours allows twice-weekly administration in hyperprolactinemia and once-daily administration in Parkinson's disease, an advantage for adherence and symptom control over other dopaminergic agents[4](https://pubmed.ncbi.nlm.nih.gov/12844325/). Mild to moderate renal or hepatic impairment, food, and concomitant levodopa or selegiline do not alter its pharmacokinetics, though severe hepatic insufficiency (Child-Pugh score above 10) substantially increases exposure and requires caution[4](https://pubmed.ncbi.nlm.nih.gov/12844325/) • [8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf).
## Clinical use in hyperprolactinemia and prolactinoma
Cabergoline tablets are indicated for hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas[8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf). In the placebo-controlled registration study (placebo n=20; cabergoline n=168), prolactin normalized after 4 weeks in 29%, 76%, 74%, and 95% of patients receiving 0.125, 0.5, 0.75, and 1.0 mg twice weekly respectively[8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf). In an 8-week double-blind comparison with bromocriptine, prolactin normalized in 77% of patients on cabergoline 0.5 mg twice weekly versus 59% on bromocriptine 2.5 mg twice daily; menses returned in 77% versus 70%, and [galactorrhea](https://www.edgepedia.org/galactorrhea) resolved in 73% versus 56%[8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf).
**Guideline position.** The Endocrine Society clinical practice guideline recommends dopamine agonist therapy to lower prolactin, reduce tumor size, and restore gonadal function in patients with symptomatic prolactin-secreting microadenomas or macroadenomas, and recommends cabergoline in preference to other dopamine agonists because of higher efficacy in normalizing prolactin levels and a higher frequency of tumor shrinkage[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false). The Pituitary Society's 2023 international consensus statement likewise names cabergoline the preferred agonist, citing its long half-life, high efficacy, and good tolerability[6](https://www.nature.com/articles/s41574-023-00886-5). Patients resistant to or intolerant of other dopamine agonists should be switched to cabergoline[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false) • [6](https://www.nature.com/articles/s41574-023-00886-5).
Quantitatively, about 10% of patients are resistant to cabergoline versus about 25% to bromocriptine, and roughly 80% of bromocriptine-resistant patients may achieve prolactin normalization on cabergoline[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false). Bromocriptine shrinks pituitary tumors by about 50% in roughly two thirds of those treated, while cabergoline produces tumor reduction in over 90% of patients[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false). The guideline also suggests not treating asymptomatic microprolactinomas, and notes that cabergoline appears safe for infertility treatment in women with hyperprolactinemia, though published experience is smaller[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false).
## Safety: valvulopathy and fibrosis
Cabergoline shares with other ergot derivatives a risk of fibrotic and serosal inflammatory disorders, including pleuritis, pulmonary fibrosis, pericarditis, cardiac valvulopathy, and retroperitoneal fibrosis, after prolonged use[9](https://www.ema.europa.eu/en/documents/referral/cabergoline-and-pergolide-article-31-referral-annex-iii_en.pdf). A [European Medicines Agency](https://www.edgepedia.org/european-medicines-agency) review concluded that the risk of heart valve fibrosis is well established for cabergoline and pergolide, and restricted their use: in Parkinson's disease they are second-line therapy, and they are contraindicated in patients with evidence of heart valve problems[7](https://www.ema.europa.eu/en/medicines/human/referrals/ergot-derived-dopamine-agonists) • [10](https://ec.europa.eu/health/documents/community-register/2008/2008111462792/anx_62792_en.pdf).
The risk is dose-dependent. When cabergoline is taken at a daily dose of 3 mg or more, those treated for Parkinson's disease face a danger of heart valve regurgitation ranging from moderate to severe.[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false) By contrast, six of seven studies analyzing cardiac valves in over 500 patients with prolactinomas receiving standard doses showed no evidence of clinically significant valvular disease; the single study reporting a 57% incidence of tricuspid regurgitation also found significant regurgitation in its control group[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false). The Endocrine Society notes that patients receiving typical doses of 1 to 2 mg per week likely will not require regular echocardiographic screening, while echocardiography may be needed for those on very high doses for prolonged periods[5](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false). The FDA label advises using the lowest effective dose for hyperprolactinemia and periodically reassessing cardiac status during long-term treatment[8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf).
**Other adverse effects and interactions.** Postmarketing reports describe pathological gambling, [increased libido](https://www.edgepedia.org/increased-libido), and hypersexuality in patients treated with dopamine agonists including cabergoline, generally reversible on dose reduction or discontinuation[8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf). Cabergoline is contraindicated in uncontrolled hypertension, hypersensitivity to ergot derivatives, and a history of pulmonary, pericardial, cardiac valvular, or retroperitoneal fibrotic disorders, and it should not be given concurrently with D2-antagonists such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide[8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf) • [11](https://www.dailymed.nlm.nih.gov/dailymed/getFile.cfm?setid=8562f94f-a59a-4893-aefc-ea6547b01e92&type=pdf). It is not indicated for inhibition or suppression of physiologic postpartum lactation[8](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf).
## Use in Parkinson's disease
Cabergoline is one of the ergot-derived dopamine agonists, a group that also includes bromocriptine, dihydroergocryptine, lisuride, and pergolide[7](https://www.ema.europa.eu/en/medicines/human/referrals/ergot-derived-dopamine-agonists). Following the EMA safety review, cabergoline-containing products are indicated only as second-line therapy in Parkinson's disease, for patients who have already taken or cannot take other treatments[7](https://www.ema.europa.eu/en/medicines/human/referrals/ergot-derived-dopamine-agonists). Its long half-life permits once-daily dosing in this indication[4](https://pubmed.ncbi.nlm.nih.gov/12844325/).
## References
1. [Cabergoline, NCI Drug Dictionary, National Cancer Institute](https://www.cancer.gov/publications/dictionaries/cancer-drug/def/cabergoline)
2. [Cabergoline tablets highlights, DailyMed (Initial U.S. Approval: 1996)](https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=c9f0b576-d5e5-4e3e-bb5c-3574d75d9907)
3. [Dostinex (cabergoline) tablets label, FDA](https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020664s011lbl.pdf)
4. [Clinical pharmacokinetics of cabergoline, PubMed](https://pubmed.ncbi.nlm.nih.gov/12844325/)
5. [Diagnosis and Treatment of Hyperprolactinemia: An Endocrine Society Clinical Practice Guideline, Journal of Clinical Endocrinology & Metabolism](https://academic.oup.com/jcem/article/96/2/273/2709487?login=false)
6. [Diagnosis and management of prolactin-secreting pituitary adenomas: a Pituitary Society international Consensus Statement, Nature Reviews Endocrinology](https://www.nature.com/articles/s41574-023-00886-5)
7. [Ergot-derived dopamine agonists – referral, European Medicines Agency](https://www.ema.europa.eu/en/medicines/human/referrals/ergot-derived-dopamine-agonists)
8. [Cabergoline Tablets, 0.5 mg, ANDA 78-035 approval package, FDA](https://www.accessdata.fda.gov/drugsatfda_docs/anda/2008/078035Orig1s000.pdf)
9. [Cabergoline and pergolide Article 31 referral, Annex III, EMA](https://www.ema.europa.eu/en/documents/referral/cabergoline-and-pergolide-article-31-referral-annex-iii_en.pdf)
10. [Ergot-Cabergoline-Pergolide Annex, European Commission](https://ec.europa.eu/health/documents/community-register/2008/2008111462792/anx_62792_en.pdf)
11. [Cabergoline tablets prescribing information, DailyMed](https://www.dailymed.nlm.nih.gov/dailymed/getFile.cfm?setid=8562f94f-a59a-4893-aefc-ea6547b01e92&type=pdf)
---
*Topic: Encyclopedia › Life and health › Microorganisms and fungi › Fungi and mycology › Ascomycete taxa › Other sac fungus lineages › Ergot and Claviceps › Ergot-derived pharmaceuticals (Claviceps-tied treatment)*
*Initially written Sep 17, 2026 · Reviewed: Oct 21, 2026 · Edited: Oct 15, 2026; Oct 21, 2026 · Last review: Oct 21, 2026*
*Copyright 2026 EdgeChat AI, a subsidiary of Biostate AI.*
License: Edgepedia Community License 1.0, https://www.edgepedia.org/edgepedia/license