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Cabergoline

Cabergoline is a synthetic ergoline derivative and long-acting dopamine D₂ receptor agonist that inhibits prolactin secretion from the anterior pituitary gland.^[1]^[2] It is primarily indicated for the treatment of hyperprolactinemic disorders, including those caused by prolactin-secreting pituitary adenomas (prolactinomas) or idiopathic origins, where elevated prolactin levels can lead to symptoms such as infertility, irregular menstrual cycles, galactorrhea, and reduced libido.^[1]^[3]^[4] Administered orally as tablets, cabergoline is typically started at a low dose of 0.25 mg twice weekly, with adjustments made no more frequently than every four weeks based on serum prolactin levels, up to a maximum of 1 mg twice weekly.^[1]^[3] Beyond hyperprolactinemia, it is sometimes used off-label at higher doses in the management of Parkinson's disease symptoms due to its dopaminergic effects.^[3] Treatment duration varies, but for hyperprolactinemia, it may continue for six months or longer if prolactin levels normalize, with periodic monitoring to assess the need for ongoing therapy.^[4] Common side effects include nausea, headache, dizziness, and constipation, while serious risks involve cardiac valvulopathy, pulmonary or retroperitoneal fibrosis, and hypotensive episodes, necessitating baseline and periodic echocardiographic evaluations in long-term users.^[1]^[4] Contraindications include uncontrolled hypertension, hypersensitivity to ergot derivatives, and a history of fibrotic or valvular heart disorders; it should be used cautiously in patients with liver impairment or during pregnancy due to potential risks.^[1]^[3]^[5]

Medical uses

Hyperprolactinemia

Hyperprolactinemia is a condition characterized by elevated levels of prolactin in the blood, which can arise from various causes including idiopathic origins or pathological conditions such as pituitary adenomas, particularly prolactinomas, which are benign tumors of the pituitary gland that overproduce prolactin.^[6] Prolactinomas represent the most common pathological etiology of hyperprolactinemia, accounting for a significant proportion of cases once physiological and pharmacological factors are excluded.^[7] Cabergoline exerts its therapeutic effect in hyperprolactinemia primarily through its action as a potent dopamine D2 receptor agonist, which inhibits prolactin secretion from lactotroph cells in the anterior pituitary gland by mimicking the tonic inhibitory influence of endogenous dopamine on prolactin release.^[8] This mechanism leads to rapid suppression of serum prolactin levels and, in cases involving prolactinomas, promotes tumor volume reduction by inducing apoptosis and inhibiting cell proliferation within the adenoma.^[9] The standard dosing regimen for cabergoline in treating hyperprolactinemia begins with an initial dose of 0.25 mg orally twice weekly, with subsequent titration in increments of 0.25 mg twice weekly every 4 weeks based on serum prolactin levels, up to a maximum of 1 mg twice weekly to achieve normalization.^[5] Clinical studies have demonstrated high efficacy, with prolactin normalization achieved in approximately 80-90% of patients with microprolactinomas and 60-80% with macroprolactinomas, alongside significant tumor shrinkage observed in up to 90% of responsive cases after 12 months of therapy.^[10] For instance, long-term treatment has been associated with greater than 75% reduction in tumor volume in the majority of patients.^[11] Long-term management of hyperprolactinemia with cabergoline involves regular monitoring of serum prolactin levels, typically every 3-6 months once normalized, to assess treatment response and guide dose adjustments or potential withdrawal in stable cases.^[12] For patients with visible prolactinomas, magnetic resonance imaging (MRI) of the pituitary is recommended at baseline, 3-6 months after initiating therapy, and periodically thereafter (e.g., annually) to evaluate tumor size and detect any residual or recurrent mass effects.^[13] This approach ensures sustained control of hyperprolactinemia while minimizing risks associated with prolonged dopamine agonist use.

Parkinson's disease

Cabergoline has been used off-label as an adjunct therapy to levodopa in Parkinson's disease (PD), particularly in countries where it is approved for this indication (e.g., as second-line therapy in the EU), to control motor symptoms and reduce the duration of "off" periods, during which patients experience symptom re-emergence due to waning levodopa effects.^[14] However, it is not approved by the FDA for PD in the US. By acting as a selective dopamine D2 receptor agonist, it enhances dopaminergic activity in the basal ganglia, helping to stabilize motor function without the need for frequent administration.^[15] Clinical trials have demonstrated that adding cabergoline to levodopa regimens can decrease daily "off" time by approximately 9-42%, depending on dosage and patient response, while allowing modest reductions in levodopa requirements.^[16]^[17] Dosing for PD (off-label in the US) begins at 0.5 mg once daily, with gradual titration every 3-7 days based on tolerability and efficacy, up to a maximum of 4.5-6 mg daily.^[18]^[15] This once-daily schedule is facilitated by cabergoline's long plasma half-life of about 65 hours, which provides sustained receptor stimulation and differentiates it from shorter-acting dopamine agonists requiring multiple doses.^[19] Efficacy is evidenced by improvements in Unified Parkinson's Disease Rating Scale (UPDRS) motor scores, with reductions of 30% or more in parkinsonian disability observed in early-stage patients treated with cabergoline monotherapy or adjunctively, comparable to other dopamine agonists like bromocriptine.^[20]^[14]^[21] Historically, cabergoline was considered for first-line monotherapy in early Parkinson's disease, showing efficacy similar to levodopa in delaying motor complications over five years.^[22] However, concerns over cardiac valvulopathy risks with ergot-derived agonists led to restrictions and a shift away from its use. As of 2025, due to these serious risks including valvular heart disease and fibrosis, cabergoline is no longer recommended for PD treatment and has been largely supplanted by safer non-ergot dopamine agonists such as pramipexole and ropinirole.^[23]^[24] It may occasionally be considered in limited scenarios under close monitoring, but current guidelines prioritize alternatives to minimize cardiac risks.^[25]^[22]

Off-label uses

Cabergoline, a dopamine receptor agonist, has been explored for various off-label applications leveraging its ability to modulate prolactin secretion and exert antiproliferative effects on certain tissues. These uses are typically supported by small-scale clinical studies, case series, or retrospective analyses rather than large randomized controlled trials, with response rates varying by indication. In polycystic ovary syndrome (PCOS), cabergoline has been investigated for its potential to address hyperprolactinemia and enhance ovulatory function, particularly in women with elevated prolactin levels. Chronic administration at doses of 0.5 mg twice weekly has been shown to normalize androgen levels and restore menstrual cyclicity in affected women, with ovulation rates improving in approximately 50-70% of cases across multiple small studies. For instance, when combined with metformin, cabergoline further augments hormonal balance and ovarian activity compared to metformin alone, as demonstrated in a meta-analysis of randomized trials. Similarly, adjunctive use with clomiphene citrate or letrozole has increased ovulation induction success in euprolactinemic PCOS patients, though evidence remains limited to pilot studies. For nonfunctioning pituitary adenomas (NFPAs), cabergoline is used off-label to potentially induce tumor shrinkage or prevent regrowth following surgery, capitalizing on dopamine-mediated antiproliferative effects. Clinical studies indicate modest tumor volume reduction in 20-30% of patients and stabilization or prevention of progression in 50-60% over 1-3 years of treatment at doses of 0.5-2 mg weekly. A single-center retrospective analysis reported tumor growth control in over two-thirds of NFPA cases, though 16% experienced escape from therapy, highlighting variable efficacy primarily from observational data. Cabergoline is also employed off-label at lower doses (typically 0.25-1 mg as a single administration) to inhibit lactation following stillbirth, neonatal death, or weaning, offering a more tolerable alternative to older agents like bromocriptine. Systematic reviews confirm its effectiveness in suppressing milk production and alleviating breast engorgement, with 80-90% of women reporting symptom resolution within 7 days and a favorable safety profile, including fewer adverse events than comparators. This application is supported by retrospective evaluations and small prospective trials, emphasizing its role in postpartum scenarios where lactation suppression is desired. Additional off-label uses include restless legs syndrome (RLS), where low-dose cabergoline (0.25-0.5 mg) has demonstrated symptom improvement in moderate-to-severe cases, with International Restless Legs Syndrome Study Group scores reducing by 50-70% in short-term trials, though long-term use is cautioned due to augmentation risks and cardiac concerns. In Cushing's disease, cabergoline serves as an adjunctive therapy for hypercortisolism control, achieving normalization of urinary free cortisol in 20-25% of patients at doses up to 3.5 mg weekly, based on multicenter retrospective data showing sustained responses in a subset unresponsive to surgery. For ovarian endometriomas, cabergoline has shown preliminary promise in reducing cyst size and pelvic pain, with one comparative study reporting volume decreases comparable to dienogest after 3 months, attributed to antiangiogenic effects in small cohorts. Overall, these applications rely on evidence from limited studies, underscoring the need for further research to establish optimal dosing and long-term outcomes.

Use during pregnancy and breastfeeding

Cabergoline has not been assigned a formal pregnancy category by regulatory authorities such as the FDA or EMA, as these categorical systems were phased out in favor of narrative risk summaries; however, extensive data from systematic reviews of over 1,600 pregnancies exposed to the drug show no increased risk of major congenital malformations (rates of 1.9–2.1%, comparable to the general population of 2–3%) or spontaneous abortions (rates of 8.6–13.3%, similar to the general population of 10–20%) compared to untreated controls or other dopamine agonists like bromocriptine.^[26]^[27] Guidelines recommend using the lowest effective dose of cabergoline for hyperprolactinemia treatment preconceptionally until pregnancy is confirmed, at which point the drug should be discontinued to minimize potential exposure, though inadvertent first-trimester exposure in more than 1,000 reported cases has not demonstrated adverse fetal outcomes.^[28]^[26] If possible, discontinuation one month prior to attempting conception is advised to prevent unplanned exposure, but continuation until confirmation is often necessary for effective prolactin control in patients with prolactinomas.^[29]^[5] During breastfeeding, cabergoline is contraindicated in women intending to nurse, as it potently suppresses prolactin secretion and lactation; the FDA labeling explicitly states it should not be administered postpartum to those planning to breastfeed due to this interference.^[5]^[30] However, cabergoline is safely and effectively used off-label as a single-dose regimen (typically 1 mg) to inhibit physiological lactation and alleviate associated breast symptoms following pregnancy loss, abortion, or when breastfeeding is not desired, with studies reporting high efficacy and minimal adverse effects.^[31]^[32] Monitoring for patients discontinuing cabergoline preconceptionally or upon pregnancy confirmation includes serial fetal ultrasounds to assess development and growth, alongside prolactin level measurements post-discontinuation to evaluate for hyperprolactinemia recurrence, particularly in those with underlying prolactinomas.^[28]^[26]

Contraindications and precautions

Absolute contraindications

Cabergoline is absolutely contraindicated in patients with uncontrolled hypertension, as the drug can exacerbate the condition and increase the risk of serious cardiovascular events such as stroke or myocardial infarction.^[5] It is also contraindicated in individuals with known hypersensitivity to ergot derivatives, which may provoke severe allergic reactions including anaphylaxis or other hypersensitivity manifestations.^[5] Patients with a history of valvular heart disease or any form of fibrosis, including cardiac valvular disorders, pericardial fibrosis, pleural, pulmonary, or retroperitoneal fibrotic disorders, must avoid cabergoline due to the established link between the drug and the development or progression of these conditions, potentially leading to heart failure or regurgitation.^[5]^[33]

Relative precautions and monitoring

Patients with pre-existing cardiovascular disease should undergo a baseline echocardiogram prior to initiating cabergoline therapy to assess for valvular abnormalities, as the drug has been associated with potential cardiac risks in such individuals.^[5] For long-term use, routine echocardiographic monitoring every 6 to 12 months is recommended to detect any new or worsening valvular issues, with discontinuation considered if significant changes occur.^[29] Blood pressure should also be checked at baseline and periodically during treatment, given the risk of orthostatic hypotension, particularly in those with underlying cardiovascular conditions.^[5] Individuals with a history of psychosis or impulse control disorders require careful surveillance during cabergoline treatment, as the dopamine agonist properties may exacerbate psychiatric symptoms or induce behaviors such as pathological gambling, hypersexuality, or compulsive shopping.^[5] Clinicians should inquire about emerging impulse control issues at regular intervals and consider dose reduction or discontinuation if worsening occurs.^[29] In patients with hepatic impairment, cabergoline should be used with caution due to its extensive hepatic metabolism; for moderate impairment (Child-Pugh class B), enhanced monitoring is advised, while severe impairment (Child-Pugh class C) warrants dose reduction and close observation, as plasma exposure may increase significantly.^[5] For renal impairment, no specific dose adjustment is required based on pharmacokinetics, but caution is still recommended with monitoring for potential fibrotic complications.^[29] Elderly patients may exhibit increased sensitivity to cabergoline owing to age-related declines in hepatic, renal, or cardiac function, necessitating a cautious approach with initiation at the lowest effective dose and gradual titration.^[4] Limited clinical data in this population underscore the need for individualized monitoring to mitigate risks.^[34] Safety and effectiveness of cabergoline have not been established in pediatric patients, and its use is not recommended.^[5]^[35]^[33] Cabergoline is not recommended for the prevention of physiological lactation postpartum due to the risk of serious adverse reactions such as hypertension, stroke, myocardial infarction, seizures, and death. It should be avoided in postpartum patients with preeclampsia or eclampsia unless the potential benefits outweigh the risks.^[5]^[30] Overall, routine monitoring for long-term cabergoline therapy includes periodic echocardiograms every 6 to 12 months and regular blood pressure assessments to ensure safety, particularly in at-risk groups.^[5] Prolactin levels should be evaluated every 4 weeks initially and then as needed to guide dosing, with adjustments made in increments of 0.25 mg twice weekly up to a maximum of 1 mg twice weekly.^[29]

Adverse effects

Common adverse effects

Common adverse effects of cabergoline, occurring in more than 10% of patients in clinical trials, are typically mild and transient. Gastrointestinal disturbances are prominent, with nausea affecting 27-29% of users, constipation in about 10%, and abdominal pain in approximately 5%.^[36] Neurological side effects include headache, reported in 26% of patients, dizziness in 15-17%, and somnolence in around 5%.^[36] Additional common complaints encompass fatigue (7%), and orthostatic hypotension, often linked to the drug's dopaminergic action.^[3]^[36] These effects exhibit dose-dependency, with higher incidences at elevated doses, and frequently resolve spontaneously over time or upon dose adjustment in clinical studies.^[36] To mitigate symptoms, particularly nausea, administration with meals is recommended, alongside antiemetics if needed, and gradual dose titration starting at 0.25 mg twice weekly.^[37]

Serious adverse effects

Serious adverse effects of cabergoline, though infrequent, can impact multiple organ systems and necessitate prompt medical intervention. Psychiatric manifestations include hallucinations and impulse control disorders, such as pathological gambling, hypersexuality, and compulsive shopping, which are recognized as class effects of dopamine agonists. In patients with Parkinson's disease treated with cabergoline, the prevalence of these impulse control disorders ranges from 5% to 15%, often emerging after prolonged use and resolving upon dose reduction or discontinuation.^[38]^[39] Respiratory complications, such as pleural effusion, occur rarely (less than 1% of cases) and are typically identified through postmarketing surveillance. These effusions may present with dyspnea or chest pain and require immediate discontinuation of cabergoline, with symptoms often improving after cessation.^[5]^[40] Dermatological effects like erythromelalgia or Raynaud's phenomenon are uncommon but documented in case reports, manifesting as episodic burning pain, redness, or vasospasm in the extremities. These vascular symptoms, potentially linked to cabergoline's dopaminergic action, usually abate upon drug withdrawal.^[41]^[42] Hematologic abnormalities, including leukopenia or thrombocytopenia, are exceedingly rare and primarily reported in isolated cases, possibly exacerbated by concurrent conditions or therapies. Monitoring of blood counts is advised in patients with predisposing factors.^[43]^[44] For any suspected serious adverse reaction, immediate reporting to the FDA via MedWatch is recommended, and cabergoline should be discontinued under medical supervision to mitigate risks.^[5]

Cardiac and fibrotic risks

Cabergoline, an ergot-derived dopamine agonist, is associated with cardiac valvulopathy primarily through its agonism at the 5-HT_2B serotonin receptor, which promotes fibroblast proliferation and extracellular matrix deposition on cardiac valve leaflets, leading to fibrosis and regurgitation.^[45] This mechanism mirrors that of other ergot alkaloids like pergolide and fenfluramine derivatives, resulting in thickened, retracted valves that impair function, most commonly affecting the tricuspid and mitral valves.^[46]^[47] The risk of valvular regurgitation is dose-dependent, with higher daily doses exceeding 2-3 mg—typically used in Parkinson's disease—increasing the incidence of moderate or severe regurgitation to approximately 20-30% in affected patients, compared to 2-3% in untreated controls.^[48]^[49] In contrast, lower weekly doses (0.5-2 mg) for hyperprolactinemia carry a much lower risk, with meta-analyses showing only a slight elevation in mild tricuspid regurgitation (prevalence around 15-25%) but no significant increase in clinically meaningful valve disease.^[50]^[51] Beyond cardiac valves, cabergoline can induce fibrotic reactions in serosal tissues, including retroperitoneal, pleural, and pericardial fibrosis, which may lead to organ dysfunction such as renal impairment or constrictive pericarditis.^[5] These extracardiac fibroses are linked to cumulative exposure, with postmarketing reports indicating onset after prolonged use, though incidence remains rare (less than 1% in large cohorts) and often reversible upon discontinuation.^[52]^[53] As of 2025, the FDA label for cabergoline (Dostinex) reinforces warnings on these risks, emphasizing baseline echocardiographic screening and highlighting that lower doses for hyperprolactinemia are generally safer than high-dose regimens for Parkinson's disease.^[5] To mitigate these effects, clinical guidelines recommend limiting cumulative doses where possible, performing serial echocardiograms every 6-12 months in at-risk patients, and promptly discontinuing therapy if fibrosis is detected.^[5]^[54]

Drug interactions

Pharmacokinetic interactions

Cabergoline undergoes partial metabolism via the cytochrome P450 3A4 (CYP3A4) enzyme, making it susceptible to pharmacokinetic interactions with CYP3A4 modulators that alter its plasma concentrations.^[55] Strong CYP3A4 inhibitors, such as ketoconazole, decrease the metabolism of cabergoline, leading to elevated plasma levels and an increased risk of toxicity, including adverse effects like nausea, hypotension, and cardiac valvulopathy.^[55] Similarly, erythromycin, another potent CYP3A4 inhibitor, significantly increases cabergoline blood levels and potentiates its effects; coadministration is generally not recommended, or if unavoidable, requires dose reduction and close monitoring.^[56] In clinical studies, coadministration with clarithromycin (a moderate CYP3A4 inhibitor) resulted in approximately a 2.7-fold increase in cabergoline's maximum plasma concentration (Cmax) and area under the curve (AUC) in both healthy volunteers and patients with Parkinson's disease, highlighting the potential for substantial exposure changes with strong inhibitors.^[57] Conversely, CYP3A4 inducers accelerate cabergoline metabolism, reducing its serum concentrations and potentially diminishing therapeutic efficacy, such as in prolactin suppression.^[55] For instance, rifampin increases cabergoline's metabolic clearance, necessitating monitoring of prolactin levels and possible dose adjustments to maintain efficacy.^[55] Regarding absorption, cabergoline's bioavailability is not significantly affected by food, though a single-dose study in healthy volunteers showed a modest, non-statistically significant reduction in Cmax (from 54 pg/mL fasting to 44 pg/mL fed) and AUC (from 6392 pg·h/mL to 5331 pg·h/mL) when administered with a mixed meal, suggesting minimal impact overall.^[58] High-fat meals similarly do not alter pharmacokinetics, allowing administration with or without food.^[5] Cabergoline exhibits moderate protein binding (40-42%) to plasma proteins, resulting in minor displacement interactions with highly bound drugs like warfarin (99% bound).^[55] Predicted increases in warfarin serum concentrations may occur upon coadministration, potentially affecting international normalized ratio (INR); monitoring of INR is advised in patients receiving both agents.^[59]

Pharmacodynamic interactions

Cabergoline, as a dopamine D2 receptor agonist, can exhibit pharmacodynamic interactions with other dopamine agonists such as levodopa, leading to additive effects on dopaminergic activity. This combination may enhance therapeutic efficacy in conditions like Parkinson's disease but also increases the risk of adverse effects, including hypotension and dyskinesia. Dose adjustments are often necessary to mitigate these risks, with clinical monitoring recommended to balance benefits and side effects.^[60] Concomitant use with antipsychotics, such as haloperidol, which act as D2 receptor antagonists, results in pharmacodynamic antagonism that can reduce cabergoline's efficacy in suppressing prolactin or managing Parkinson's symptoms. This interaction is particularly concerning in patients requiring dopamine agonism, and coadministration is generally not recommended unless benefits outweigh risks, with close clinical evaluation required.^[5]^[61] Cabergoline, an ergot-derived agent, may interact additively with other ergot alkaloids or triptans like sumatriptan, potentiating vasoconstriction through shared serotonergic and adrenergic receptor effects. This can elevate the risk of fibrotic reactions, including valvular heart disease, due to prolonged activation of pathways involved in tissue proliferation. Such combinations should be avoided, with alternative therapies preferred for migraine management in cabergoline-treated patients.^[62]^[55] When combined with antihypertensives, cabergoline's hypotensive effects—mediated via dopamine receptor stimulation—can be potentiated, leading to enhanced orthostatic hypotension. Blood pressure monitoring is essential, particularly in patients with cardiovascular risk factors, and dose titration may be required to prevent symptomatic drops.^[5]^[63] Serotonergic drugs that agonize 5-HT2B receptors, such as certain triptans or ergot derivatives, can amplify cabergoline's partial agonism at this receptor, heightening the risk of valvular fibrosis and related cardiac complications. Cabergoline's affinity for 5-HT2B contributes to this concern, and concurrent use warrants echocardiographic screening and risk-benefit assessment to avoid cumulative serotonergic exposure.^[5]^[64]

Pharmacology

Pharmacodynamics

Cabergoline is a potent dopamine D₂ receptor agonist with high affinity, exhibiting a K_i value of approximately 0.6 nM at the D₂ receptor, which underlies its primary therapeutic effects.^[65] It also binds with low affinity to dopamine D₁ receptors (K_i ≈ 7000 nM), though its affinity for D₁ is lower relative to D₂ compared to other ergoline agonists.^[30]^[66] This receptor interaction potently inhibits prolactin release from lactotroph cells in the anterior pituitary by activating inhibitory D₂ autoreceptors, leading to suppression of hyperprolactinemia.^[55] In addition to its dopaminergic actions, cabergoline acts as an agonist at serotonin 5-HT_2A and 5-HT_2B receptors, with K_i values ranging from 1.2 to 20 nM, which may contribute to adverse effects such as cardiac valvulopathy. It also exhibits weak antagonism at α₂-adrenergic receptors due to low binding affinity.^[55] Physiologically, cabergoline's D₂ agonism results in significant prolactin suppression, with low weekly doses (0.5–1 mg) normalizing serum prolactin levels in the majority of hyperprolactinemic patients within 3–6 months.^[67] Its dopaminergic stimulation enhances motor control in conditions like Parkinson's disease by mimicking endogenous dopamine effects on basal ganglia pathways. Compared to bromocriptine, cabergoline demonstrates greater selectivity for D₂ over D₁ receptors, contributing to improved tolerability and efficacy profiles.^[66]

Pharmacokinetics

Cabergoline is rapidly absorbed following oral administration, with mean peak plasma concentrations of 30 to 70 pg/mL achieved within 2 to 3 hours after single doses of 0.5 to 1.5 mg in healthy volunteers.^[30] The drug exhibits linear pharmacokinetics over the dose range of 0.5 to 7 mg, and food does not significantly affect its absorption or peak levels.^[30] Absolute bioavailability has not been determined due to substantial first-pass metabolism.^[30] Cabergoline is extensively distributed in the body and demonstrates moderate binding to plasma proteins, ranging from 40% to 42%, in a concentration-independent manner.^[30] The drug undergoes extensive hepatic metabolism, primarily through hydrolysis of the acylurea bond or the urea moiety, yielding metabolites that lack prolactin-lowering activity.^[30] Cytochrome P450-mediated metabolism plays a minimal role in its biotransformation.^[30] Elimination of cabergoline occurs slowly, with an estimated half-life of 63 to 69 hours based on urinary excretion data from healthy subjects, supporting dosing regimens such as twice weekly.^[30] Over 20 days, approximately 60% of the dose is excreted in feces and 22% in urine, with less than 4% eliminated unchanged in the urine.^[30] Nonrenal clearance accounts for the majority of elimination at about 3.2 L/min, compared to renal clearance of 0.08 L/min.^[30] In special populations, pharmacokinetics remain unchanged in patients with moderate to severe renal insufficiency compared to healthy individuals.^[30] For hepatic impairment, maximum plasma concentration and area under the curve are unaffected in mild to moderate cases (Child-Pugh score ≤10), but exposure is substantially increased in severe hepatic impairment (Child-Pugh score >10), requiring dose adjustments and monitoring.^[30]

Chemistry

Chemical structure

Cabergoline is a synthetic derivative of ergot alkaloids, featuring a tetracyclic ergoline backbone characteristic of this class of compounds. The core structure consists of four fused rings: an indole system (rings A and B), a cyclohexene ring (C), and a piperidine ring (D), with a double bond between carbons 9 and 10. At the nitrogen atom in position 6 (the piperidine nitrogen), there is an allyl substitution, which contributes to its pharmacological profile.^[2]^[55] The defining feature at position 8 is a β-carboxamide group modified into an N-acylurea moiety, specifically (8β)-6-allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide. This includes a propylamide side chain—3-(dimethylamino)propyl attached to the nitrogen. The molecular formula of cabergoline is C₂₆H₃₇N₅O₂, with a molecular weight of 451.62 g/mol.^[2]^[33]^[68] Textually, the structure can be represented as an ergoline core with N⁶-allyl and at C⁸: -C(O)-N(CH₂CH₂CH₂N(CH₃)₂)-C(O)-NHCH₂CH₃, where the amide-urea linkage provides stability and prolonged activity compared to bromocriptine, another ergoline derivative lacking this specific substitution. This structural modification results in cabergoline's longer duration of action.^[2]^[69]

Physical and chemical properties

Cabergoline is a white to off-white crystalline powder.^[70]^[71] It is insoluble in water, soluble in ethanol, chloroform, and N,N-dimethylformamide (DMF), slightly soluble in 0.1 N hydrochloric acid, and very slightly soluble in n-hexane.^[71]^[70] The compound exhibits pKa values of approximately 6.4 and 9.3, corresponding to its basic nitrogen groups, with a pH of 9.2 in aqueous suspension, influencing its ionization state under physiological conditions.^[70] This ionization profile contributes to its absorption characteristics in pharmacokinetic studies.^[70] Cabergoline is light-sensitive and requires protection from light and moisture during storage, which should occur at room temperature (15–30°C) in tight, light-resistant containers to maintain stability.^[72]^[73] In pharmaceutical formulations, cabergoline is typically presented as 0.5 mg tablets containing excipients such as lactose monohydrate and leucine to aid in tablet integrity and bioavailability.^[71]^[70]

History

Development and discovery

The development of cabergoline originates from the study of ergot alkaloids, which were first isolated in chemically pure form in 1918 by Arthur Stoll at Sandoz Laboratories in Switzerland; Stoll extracted ergotamine from sclerotia of the fungus Claviceps purpurea growing on rye, marking the beginning of systematic research into these compounds' pharmacological properties. Ergot alkaloids served as scaffolds for semisynthetic derivatives that emerged as dopamine agonists in the 1970s, with bromocriptine—introduced clinically around 1974—demonstrating efficacy in suppressing prolactin secretion and treating conditions like hyperprolactinemia through its agonism at dopamine D2 receptors.^[74] In the early 1980s, scientists at the Italian pharmaceutical company Farmitalia Carlo Erba synthesized cabergoline (initially coded as FCE 21336) as a semisynthetic ergoline derivative, specifically engineered as a longer-acting alternative to bromocriptine to provide sustained dopamine D2 receptor stimulation with reduced dosing frequency.^[75] Preclinical studies in the early 1980s, including experiments in rats, confirmed cabergoline's enhanced affinity for D2 receptors and its potent, prolonged inhibition of prolactin release compared to bromocriptine, with effects lasting up to several days after a single dose.^[76] A key milestone was the filing of a patent application by Farmitalia in Italy on August 11, 1982, for the compound and its preparation method, with the corresponding U.S. patent (No. 4,526,892) granted on July 2, 1985.^[77] Early clinical evaluation began in the mid-1980s, with the first human studies reported in 1986 demonstrating cabergoline's superior efficacy and tolerability in hyperprolactinemic patients; a single 300 μg oral dose normalized prolactin levels for 7–14 days in most participants, including those with acromegaly or pituitary tumors, outperforming shorter-acting agents like bromocriptine in duration and side effect profile.^[78] These initial trials, conducted on 15 patients, established cabergoline's potential as a once- or twice-weekly therapy, paving the way for further development focused on its prolactin-lowering mechanism.^[79]

Regulatory approvals and milestones

Cabergoline received initial marketing authorization in Europe in 1992 under the brand name Dostinex for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas.^[80] In the United States, the Food and Drug Administration (FDA) approved cabergoline on December 23, 1996, also as Dostinex, specifically for the management of hyperprolactinemia associated with conditions such as prolactinomas.^[81] Regulatory expansions followed in the late 1990s, with approval for Parkinson's disease in Europe granted in 1997 as an adjunct therapy to levodopa, reflecting its role as a long-acting dopamine agonist.^[82] However, cabergoline was never approved by the FDA for Parkinson's disease in the US, limiting its use there to off-label applications despite early studies.^[83] In the 2000s, label updates addressed emerging safety concerns related to cardiac risks. Following reports of valvular heart disease linked to ergot-derived dopamine agonists, the FDA issued warnings in 2007 and updated the Dostinex label in 2011 to include precautions for cardiac valvulopathy and pericardial fibrosis, recommending echocardiographic monitoring for patients on higher cumulative doses.^[84] These changes were prompted by post-marketing surveillance and studies primarily in Parkinson's patients using high doses. Post-2007 fibrosis alerts led to restrictions on high-dose cabergoline for Parkinson's disease in several countries, including European nations, where regulatory bodies like the EMA revised product information in April 2007 to limit its use to cases where benefits outweigh the risks of fibrotic reactions such as pleuropulmonary or retroperitoneal fibrosis.^[85] As of 2025, a systematic review and meta-analysis found no increased risk of congenital malformations with cabergoline use in pregnancy but noted a lower live birth rate when continued compared to discontinuation upon prolactinoma diagnosis. The FDA's 2025 label describes risks during pregnancy, advising avoidance of dopamine agonists including cabergoline during pregnancy and postpartum unless the potential benefit justifies the potential risk.^[27]^[5]

Society and culture

Brand names and formulations

Cabergoline is marketed under the primary brand name Dostinex by Pfizer, available as 0.5 mg oral tablets for the treatment of hyperprolactinemic disorders.^[86]^[55] Generic versions of cabergoline became available following the expiry of key patents in 2005, with the first FDA approval granted to Par Pharmaceutical in December 2005. Subsequent approvals were granted to manufacturers such as Barr Laboratories in 2007.^[87]^[88] These generics are formulated as oral tablets in 0.25 mg and 0.5 mg strengths, matching the original brand's dosage options.^[71] In various international markets, cabergoline is sold under other brand names, including Cabaser primarily in Europe and Dostinex in multiple regions worldwide.^[89]^[90] Cabergoline is exclusively available in oral tablet formulations, with no approved injectable, extended-release, or other dosage forms.^[55]^[91] Major manufacturers include Pfizer for the branded Dostinex, and for generics, companies such as Teva Pharmaceutical Industries and Mylan (now part of Viatris), which produce equivalent 0.5 mg tablets.^[92]^[93]

Legal status and availability

Cabergoline is classified as a prescription-only medication (Rx-only) in the United States and is available by prescription worldwide, requiring medical supervision due to its dopaminergic effects and potential side effects. It is not designated as a controlled substance under the U.S. Controlled Substances Act or equivalent international regulations.^[5]^[94]^[55] The drug is approved and widely available in major markets including the United States (FDA-approved since 1996), the European Union (EMA-authorized), Canada (Health Canada-approved), and Australia (TGA-approved), where it is indicated primarily for hyperprolactinemic disorders. Availability is more restricted in some developing countries, where regulatory approvals, import challenges, and supply chain limitations can limit access despite its inclusion on the World Health Organization's List of Essential Medicines.^[5]^[89]^[95]^[96] In the United States, cabergoline carries an FDA-mandated warning for the risk of cardiac valvulopathy and pericardial fibrosis, particularly with long-term use or higher doses (e.g., >2 mg/day, though not approved for Parkinson's disease), following postmarketing reports and studies published in 2007 that linked it to heart valve damage similar to that seen with other ergot-derived dopamine agonists. Prescribers are advised to perform baseline echocardiograms and monitor patients every 6-12 months for valvular regurgitation or restriction.^[5]^[97] Generic cabergoline typically costs $20-50 per month for standard doses (e.g., 0.5-1 mg twice weekly, or 4-8 tablets), based on U.S. pharmacy pricing with discounts; brand-name formulations like Dostinex (now discontinued in many markets) were historically more expensive, often exceeding $200 monthly. Occasional drug shortages have occurred due to manufacturing disruptions, including a reported U.S. shortage of tablets starting in May 2023 and resolved Canadian supply issues in late 2023 and early 2024.^[98]^[99]^[100]

Research directions

Emerging therapeutic applications

Cabergoline, a dopamine D₂ receptor agonist, has shown promise in preclinical and early clinical studies for diabetes management, particularly in improving glycemic control among patients with prediabetes and type 2 diabetes through modulation of dopamine pathways that influence insulin sensitivity and hepatic glucose production. A 2024 case report referenced studies in which cabergoline administration led to a mean HbA_1c reduction of approximately 0.6% after three months in type 2 diabetes patients, suggesting its potential as an adjunct therapy via enhanced peripheral insulin action.^[101] Further, a randomized trial demonstrated that twice-weekly dosing of cabergoline improved glucose metabolism in prediabetic individuals, with reductions in fasting plasma glucose and insulin resistance indices observed over 16 weeks.^[102] Recent 2025 analyses confirm these effects, noting cabergoline's role in lowering postprandial glucose excursions without significant adverse events, though phase II data indicate HbA_1c decreases of 0.5-1% that have not yet translated to regulatory approval.^[103] In the context of Parkinson's disease, cabergoline exhibits neuroprotective potential by exerting anti-apoptotic effects on dopaminergic neurons, potentially delaying disease progression beyond its symptomatic relief. Preclinical models from 2014 demonstrated that cabergoline prevented neuronal death in cortical cultures by repressing ERK1/2 activation and reducing extracellular glutamate release, mechanisms linked to apoptosis inhibition.^[104] Earlier studies also supported this through activation of the glutathione antioxidant system, which mitigates oxidative stress in Parkinson's models.^[105] These findings suggest cabergoline could serve as a disease-modifying agent, but clinical translation remains limited to early-phase investigations without established progression-delaying efficacy in humans. For Cushing's syndrome, cabergoline is being explored as an adjunct therapy to reduce adrenocorticotropic hormone (ACTH) hypersecretion from pituitary corticotroph adenomas, offering an alternative to surgery in select cases. A large multicenter study reported that 20-25% of patients with Cushing's disease achieved long-term biochemical control of hypercortisolism with cabergoline at low doses (up to 3.5 mg/week), normalizing urinary free cortisol levels in responsive individuals.^[106] This dopamine-mediated inhibition of ACTH release has shown sustained efficacy in combination regimens, with remission rates improving when paired with other agents like pasireotide, though it is not yet a standard frontline option.^[107] Emerging research on endometriosis investigates cabergoline's anti-angiogenic properties for ovarian ablation and pain relief, targeting vascular endothelial growth factor to suppress lesion growth without hormonal disruption. A 2021 randomized placebo-controlled trial found cabergoline (0.5 mg twice weekly) reduced pelvic pain severity comparably to norethisterone acetate, with improved quality-of-life scores after six months in adolescents and young adults.^[108] Ongoing phase II trials report decreased endometriosis-associated pain and inflammatory markers with cabergoline, while maintaining menstrual regularity, positioning it as a nonhormonal alternative though approval for this indication is pending.

Ongoing clinical trials

As of November 2025, ongoing clinical trials for cabergoline primarily explore its potential in endocrine disorders, pain management, and comparative efficacy against other dopamine agonists, building on its established role in treating hyperprolactinemia and related conditions. These studies aim to expand therapeutic applications or optimize treatment protocols, with phases ranging from early interventional to phase III. Additional investigations include trials for novel indications such as migraine prophylaxis and lactation inhibition. A key area of investigation involves cabergoline's utility in pituitary adenomas. For instance, one trial is evaluating cabergoline's effectiveness in reducing tumor volume and normalizing hormone levels in patients with nonfunctioning pituitary adenomas, where traditional surgery or radiation may not be ideal.^[109] This study, currently enrolling by invitation, involves oral administration of cabergoline over several months and is monitoring outcomes such as adenoma size via MRI and endocrine function. Similarly, another active trial assesses dopamine agonists like cabergoline for tumor control in nonfunctioning pituitary adenomas, with a focus on long-term remission rates post-treatment.^[110] In the realm of gynecological conditions, cabergoline is being tested as an adjunct therapy for chronic pelvic pain associated with endometriosis. An ongoing phase II trial examines whether adding cabergoline to standard hormonal treatments, such as gonadotropin-releasing hormone agonists, can further alleviate pain and inflammation by targeting dopamine pathways in endometriotic lesions.^[111] Participants receive cabergoline at doses of 0.5 mg twice weekly, with primary endpoints including pain scores on validated scales like the Visual Analog Scale; the study is active but not recruiting, with an estimated completion in 2026. Comparative studies are also underway to affirm cabergoline's advantages over alternatives. A phase III multicenter trial in China is recruiting approximately 382 patients with hyperprolactinemia to compare the efficacy and safety of cabergoline tablets against bromocriptine mesylate tablets, measuring prolactin normalization rates, tolerability, and adverse events over 24 weeks.^[112] This randomized, double-blind design highlights cabergoline's potentially lower dosing frequency and fewer side effects, such as nausea, compared to bromocriptine. Additionally, bioequivalence trials ensure generic formulations match the reference drug's pharmacokinetics, supporting broader access. One such active, not recruiting study compares a new cabergoline tablet to the branded version in healthy volunteers under fasting conditions.^[113] Other ongoing efforts include a trial evaluating cabergoline as a preventive treatment for chronic migraine (NCT05525611, available via expanded access) and a study on reduced-dose cabergoline for lactation inhibition after second-trimester abortion or pregnancy loss (NCT06909123, not yet recruiting as of April 2025).^[114] ^[115] These efforts underscore cabergoline's continued relevance in clinical research, with active trials for novel indications like migraine prophylaxis but none identified for diabetes management at present.

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If a study with a recruitment status of recruiting; not yet recruiting; or active, not recruiting has not been confirmed within the past 2 years, the ...
[113]
A Study on Bioequivalence of Cabergoline Tablets in Human Body
Treatment IND/Protocol: Allows a large, widespread population access to a drug or biological product that has not been approved by the FDA. This type of ...