Note: Safety: Use the lowest effective dose; periodic monitoring for cardiac valve abnormalities (eg, echocardiogram) is suggested in patients receiving doses >2 mg/week (Ref).
Acromegaly (off-label use): Oral: Initial: 0.25 to 0.5 mg two times per week; titrate as needed every 4 to 6 weeks based on insulin-like growth factor 1 (IGF-1) and growth hormone levels; usual dosage range: 0.5 to 3.5 mg/week (mean dose: ~2 mg/week) (Ref). Note: Doses up to 7 mg/week have been studied in a small number of patients; doses >2 mg/week may not be more efficacious in suppressing IGF-1 levels (Ref).
Cushing disease (off-label use): Oral: Initial: 0.5 mg administered once or twice weekly; may increase by 0.5 to 1 mg/week every 1 to 2 months until urinary free cortisol levels normalize; usual dosage range: 1 to 7 mg/week (median dose: ~2 to 3.5 mg/week) (Ref).
Hyperprolactinemic disorders:
Oral: Initial: 0.25 to 0.5 mg/week administered in 1 or 2 divided weekly doses (Ref).
Dosage adjustment: May increase dose by 0.25 to 0.5 mg/week no sooner than every 4 weeks if needed based on serum prolactin levels (Di Sarno 2001; manufacturer's labeling); usual dosage range: 0.25 to 3 mg/week administered in 1 or 2 divided weekly doses (Ref). If higher doses are used, may administer in as many as 3 to 4 divided weekly doses (Ref).
Duration of therapy: Although the US labeling states that therapy may be discontinued after 6 months, treatment for ≥2 years has been recommended to reduce the risk of recurrence. Ensure that prolactin levels are normal and there is no visible tumor on MRI (in patients with prolactinoma) prior to tapering and discontinuing; maintenance of normal prolactin levels after tapering dosage to ≤0.5 mg/week may predict a lower risk of recurrence following discontinuation (Ref).
Lactation inhibition (off-label use): Oral: 1 mg as a single dose within 48 hours postpartum (Ref).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; however, cabergoline pharmacokinetics are not altered in patients with moderate to severe renal impairment.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution and monitor carefully in patients with severe hepatic impairment (Child-Pugh class C) (extensive hepatic metabolism).
Cardiac valvulopathy: Discontinue if an echocardiogram reveals new valvular regurgitation, valvular restriction, or valve leaflet thickening.
Refer to adult dosing. Start at the low end of the dosage range.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.
>10%:
Gastrointestinal: Nausea (27% to 29%)
Nervous system: Dizziness (15% to 17%), headache (26%)
1% to 10%:
Cardiovascular: Dependent edema (1%), hypotension (≤1%), orthostatic hypotension (4%), palpitations (≤1%), peripheral edema (1%), syncope (≤1%)
Dermatologic: Acne vulgaris (≤1%), pruritus (≤1%)
Endocrine & metabolic: Hot flash (3%)
Gastrointestinal: Abdominal pain (5%), anorexia (≤1%), constipation (7% to 10%), diarrhea (≤2%), dyspepsia (2% to 5%), flatulence (≤2%), toothache (1%), vomiting (2% to 4%), xerostomia (≤2%)
Genitourinary: Dysmenorrhea (≤1%), mastalgia (1% to 2%)
Nervous system: Anxiety (≤1%), asthenia (6%), depression (3%), drowsiness (≤2%), fatigue (5% to 7%), insomnia (≤1%), lack of concentration (1%), malaise (≤1%), nervousness (≤2%), pain (2%), paresthesia (≤2%), vertigo (1% to 4%)
Neuromuscular & skeletal: Arthralgia (1%)
Ophthalmic: Periorbital edema (1%), visual disturbance (≤1%)
Respiratory: Flu-like symptoms (≤1%), rhinitis (1%), throat irritation (1%)
<1%:
Endocrine & metabolic: Increased libido (including hypersexuality), weight gain, weight loss
Hypersensitivity: Facial edema
Respiratory: Epistaxis, nasal congestion
Postmarketing:
Cardiovascular: Acquired valvular heart disease (Cawood 2009), constrictive pericarditis (Townsend 2004), coronary artery dissection (Mehta 2012)
Dermatologic: Alopecia (Miwa 2003)
Hematologic & oncologic: Autoimmune hemolytic anemia (Gürbüz 2014)
Nervous system: Aggressive behavior, impulse control disorder (Bulwer 2017), pathological gambling (Falhammar 2009), psychosis (Gupta 2018)
Respiratory: Interstitial pneumonitis (Frank 1999), pleural effusion (Belmonte 2009)
Miscellaneous: Fibrosis (extracardiac; including pericardial fibrosis, pleuropulmonary fibrosis, pulmonary fibrosis [Townsend 2004], retroperitoneal fibrosis)
Known hypersensitivity to cabergoline, ergot derivatives, or any component of the formulation; uncontrolled hypertension; history of cardiac valvular disorders (indicated by valvulopathy of any valve, thickening of valve leaflet, valve restriction, or mixed valve restriction stenosis); history of pulmonary, pericardial, or retroperitoneal fibrotic disorders.
Concerns related to adverse effects:
• Cardiac valvulopathy: Cardiac valvulopathy has been reported with use. Risk is increased with use of high doses (eg, >2 mg/day). Although some conflicting data exist, a majority of observational evidence suggests the risk of valvulopathy in patients receiving typical low dose regimens (eg, ≤2 mg/week) is minimal or absent (Budayr 2020; ES [Katznelson 2014]; ES [Melmed 2011]; Stiles 2021).
• Cardiovascular effects: Initial doses >1 mg may cause orthostatic hypotension; may be symptomatic. Use with caution in patients with cardiovascular disease; hypertension, stroke, and seizure have been reported with other dopamine agonists. Concurrent use with antihypertensives may increase risk.
• CNS depression: May cause somnolence, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).
• Pleural/retroperitoneal fibrosis: Cases of pleural, pericardial, and retroperitoneal fibrosis have been reported. Do not use in patients with a history of cardiac or extracardiac fibrotic disorders. Following diagnosis of fibrosis, discontinuation of cabergoline may result in improvement of condition.
• Psychiatric disorders: Aggression, psychotic behavior, and impulse control disorders such as pathological gambling, increased libido, hypersexuality, compulsive spending or buying, and binge-eating have been reported with use; generally reversible with dose reduction or discontinuation of treatment.
Disease-related concerns:
• Hepatic impairment: Use with caution and carefully monitor patients with hepatic impairment; extensive hepatic metabolism.
• Peptic ulcer disease: Use with caution in patients with peptic ulcer disease (PUD) or GI bleeding.
• Raynaud syndrome: Use with caution in patients with Raynaud syndrome.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Generic: 0.5 mg
Yes
Tablets (Cabergoline Oral)
0.5 mg (per each): $36.66
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Dostinex: 0.5 mg
Generic: 0.5 mg
Oral: Administer with meals (may increase tolerability).
Hazardous agent (NIOSH 2016 [group 3]).
Use appropriate precautions for receiving, handling, administration, and disposal. Gloves (single) should be worn during receiving, unpacking, and placing in storage. NIOSH recommends single gloving for administration of intact tablets or capsules (NIOSH 2016). Assess risk to determine appropriate containment strategy (USP-NF 2017).
Hyperprolactinemic disorders: Treatment of hyperprolactinemic disorders, either idiopathic or caused by pituitary adenomas.
Acromegaly; Cushing disease; Lactation inhibition
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Antipsychotic Agents: Cabergoline may diminish the therapeutic effect of Antipsychotic Agents. Risk X: Avoid combination
Bromocriptine: Ergot Derivatives may enhance the adverse/toxic effect of Bromocriptine. Risk X: Avoid combination
Clarithromycin: May increase the serum concentration of Cabergoline. Risk C: Monitor therapy
Dihydroergotamine: Ergot Derivatives may enhance the vasoconstricting effect of Dihydroergotamine. Risk X: Avoid combination
Lisuride: May enhance the adverse/toxic effect of Ergot Derivatives. Risk X: Avoid combination
Lorcaserin (Withdrawn From US Market): May enhance the adverse/toxic effect of Ergot Derivatives. Specifically, use of these drugs together may increase the risk of developing valvular heart disease. Lorcaserin (Withdrawn From US Market) may enhance the serotonergic effect of Ergot Derivatives. This could result in serotonin syndrome. Risk X: Avoid combination
Methysergide: Ergot Derivatives may enhance the vasoconstricting effect of Methysergide. Risk X: Avoid combination
Metoclopramide: Cabergoline may diminish the therapeutic effect of Metoclopramide. Metoclopramide may diminish the therapeutic effect of Cabergoline. Risk X: Avoid combination
Nefazodone: Ergot Derivatives may enhance the serotonergic effect of Nefazodone. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Pipamperone [INT]: Cabergoline may diminish the therapeutic effect of Pipamperone [INT]. Pipamperone [INT] may diminish the therapeutic effect of Cabergoline. Risk X: Avoid combination
Serotonergic Agents (High Risk): Ergot Derivatives may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Sulpiride: Cabergoline may diminish the therapeutic effect of Sulpiride. Sulpiride may diminish the therapeutic effect of Cabergoline. Risk X: Avoid combination
Cabergoline is approved for the treatment of hyperprolactinemic disorders. Increased prolactin concentrations due to a prolactinoma may cause galactorrhea, amenorrhea, oligomenorrhea or luteal phase insufficiency. Treatment with cabergoline may restore ovulatory cycles; fertility may return prior to regular menses (ES [Melmed 2011]; ESE [Luger 2021]). Cabergoline is also used off-label for the treatment of acromegaly; normalization of insulin-like growth factor 1 and growth hormone may also restore fertility in premenopausal patients with acromegaly.
Treatment with a dopamine agonist such as cabergoline is recommended for patients with a prolactinoma who are trying to conceive (ES [Melmed 2011]; ESE [Luger 2021]). Patients should be treated with the lowest dose possible until pregnancy is confirmed (ESE [Luger 2021]). Cabergoline may be used for patients with acromegaly who are trying to conceive; discontinue once pregnancy is confirmed (ESE [Luger 2021]).
Normalizing prolactin concentrations during dopamine agonist treatment for a micro- or macroadenoma also improves fertility by restoring nocturnal penile tumescence, sperm count and sperm motility (ES [Melmed 2011]).
Cabergoline is approved for the treatment of hyperprolactinemic disorders. Data related to the use of cabergoline for the treatment of hyperprolactinemia during pregnancy are available but limited compared to the use of other agents (Almistehi 2018; Auriemma 2013; Colao 2008; Lebbe 2010; Moltich 2015; Ricci 2002; Robert 1996; Stalldecker 2010). Although available evidence suggests cabergoline use early in pregnancy does not cause harm to the fetus, it is recommended that dopamine agonist therapy be discontinued once pregnancy is discovered (ES [Melmed 2011]; ESE [Luger 2021]).
If treatment of a prolactinoma during pregnancy is required, a dopamine agonist such as cabergoline may be used. Serum prolactin concentrations are increased during pregnancy; monitoring prolactin levels may not be reliable for tumor progression (ES [Melmed 2011]; ESE [Luger 2021]).
If treatment for acromegaly (off-label use) is required during pregnancy for worsening symptoms (such as headache) or evidence of tumor growth, use of cabergoline may be considered (ES [Katznelson 2014]). Monitoring of insulin-like growth factor 1 and/or growth hormone (GH) are not recommended during pregnancy as an active placental GH variant present in maternal blood limits the usefulness of the results (ES [Katznelson 2014]; ESE [Luger 2021]).
Data related to cabergoline for the treatment of Cushing disease (off-label use) during pregnancy are limited. Medication may be considered for patients when surgery is not an option or for symptomatic control at initial diagnosis; agents other than cabergoline may be preferred (ES [Nieman 2015]; ESE [Luger 2021]; Nakhleh 2016; Sek 2017).
Cabergoline is contraindicated in patients with uncontrolled hypertension; use is not recommended by the manufacturer in patients with pregnancy-induced hypertension (eg, preeclampsia, eclampsia, postpartum hypertension) unless benefit outweighs potential risk.
It is not known if cabergoline is present in breast milk.
Cabergoline interferes with lactation. When used for the treatment of hyperprolactinemic disorders (idiopathic or caused by pituitary adenomas), cabergoline should not be given to patients postpartum who are breastfeeding or who are planning to breastfeed.
Cabergoline has been studied for maternal use immediately postpartum when the inhibition of physiologic lactation is needed for medical reasons (eg, stillbirth, death of the newborn, severe or acute maternal medical conditions) (Boucoiran 2021; Buhendwa 2008; Humphrey 2018; Nisha 2009). The Health and Human Services perinatal HIV guidelines suggest use of cabergoline may be considered for lactation inhibition in select patients with HIV infection (HHS [perinatal] 2023).
Cabergoline has also been studied for use in breastfeeding patients with an overabundant milk supply (hypergalactia) who do not respond to preferred therapies to reduce milk production. When used for this indication, breast milk should be discarded for ~5 days after using cabergoline (ABM [Johnson 2020]; Eglash 2014).
Due to the potential for serious adverse reactions in the breastfeeding infant, the manufacturer recommends a decision be made whether to discontinue breastfeeding or to discontinue the drug, considering the importance of treatment to the mother.
Take with food.
Blood pressure (both sitting/supine and standing); serum prolactin level (monthly until normalized); erythrocyte sedimentation rate, chest x-ray, and serum creatinine (at baseline and during therapy as needed); signs and symptoms of pleuropulmonary disease, renal insufficiency, ureteral/abdominal vascular obstruction, and cardiac failure.
Echocardiogram: Monitor as clinically indicated. Although the US labeling states that an echocardiogram should be done at baseline and every 6 to 12 months during therapy, current guidelines suggest that patients receiving doses ≤2 mg/week may not require routine echocardiography to monitor for cardiac valve abnormalities (ES [Katznelson 2014]; ES [Melmed 2011]).
Acromegaly (off-label use): Insulin-like growth factor 1 (IGF-1), growth hormone, and prolactin every 4 to 6 weeks after dose adjustment then every 4 to 6 months after normalization of IGF-1 (AACE [Katznelson 2011]; Abs 1998; ACG [Melmed 2018]).
Cushing disease (off-label use): Urinary free cortisol (24-hour) every 1 to 2 months during dose titration, then periodically (Godbout 2010; Pivonello 2009).
Acromegaly (off-label use): Age-normalized serum insulin-like growth factor 1 (IGF-1) and a random growth hormone (GH) <1 ng/mL (SI: <1 mcg/L) correlate with disease control; consider targeting postoperative GH level <0.4 ng/mL (SI: <0.4 mcg/L) if ultra-sensitive GH assay is available; use of the same IGF-1 and GH assay in the same patient throughout management is suggested (ES [Katznelson 2014]; ACG [Melmed 2018]).
Cabergoline is a long acting dopamine receptor agonist with a high affinity for D2 receptors; prolactin secretion by the anterior pituitary is predominantly under hypothalamic inhibitory control exerted through the release of dopamine. It is a potent 5-HT2B-receptor agonist, which may contribute to observed fibrotic/valvulopathic events.
Distribution: Extensive, particularly to the pituitary
Protein binding: 40% to 42%
Metabolism: Extensively hepatic via hydrolysis; minimal CYP mediated metabolism
Half-life elimination: 63 to 69 hours
Time to peak, plasma: 2 to 3 hours
Excretion: Primarily feces (~60%); urine (~22%, <4% as unchanged drug)
Hepatic function impairment: Patients with severe insufficiency (Child-Pugh score >10) show a substantial increase in the mean cabergoline Cmax and AUC.
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