Treatment of hyperprolactinemic disorders due to prolactinoma (prolactin-secreting adenomas) or idiopathic hyperprolactinemia. Suppresses prolactin secretion, restores gonadal function, and reduces the size of prolactinomas.
At least as effective as bromocriptine in normalizing serum prolactin concentrations and restoring gonadal function in women with hyperprolactinemic amenorrhea. Fewer adverse effects, especially adverse GI effects, reported in cabergoline-treated women than in bromocriptine-treated women. Bromocriptine preferred when restoration of fertility is the goal of therapy; this recommendation is based on the safety record of bromocriptine in pregnant women.
Parkinsonian Syndrome
Has been used for the symptomatic management of parkinsonian syndrome†.
Has been used as monotherapy for initial symptomatic management of parkinsonian syndrome†. Most clinicians would use levodopa for initial therapy in individuals >70 years of age (less likely than younger individuals to develop levodopa-related motor complications and because of concerns about cognitive dysfunction), in patients with cognitive impairment, and in those with severe disease. A dopamine receptor agonist may be preferred for initial therapy in patients ≤70 years of age.
Has been used as an adjunct to levodopa for the symptomatic management of parkinsonian syndrome† in patients with advanced disease.
Dosage and Administration
Administration
Oral Administration
Administer orally without regard to meals.
Hyperprolactinemic disorders: Administer twice weekly.
Initiate at low dosage and increase slowly (at ≥4 week intervals) until therapeutic response is achieved.
Initially, 0.25 mg twice weekly; increase in increments of 0.25 mg twice weekly up to 1 mg twice weekly. Base dosage adjustments on serum prolactin concentrations; use lowest effective dosage.
Consider decreasing the dosage if normal serum prolactin concentrations maintained for 24 months and size of tumor decreased ≥50%; periodically monitor to determine whether retreatment is needed. Some patients (e.g., those with microadenomas) may be able to discontinue the drug; discontinuance in those with macroadenomas should be undertaken with extreme caution. The manufacturer states that efficacy >24 months not established.
Parkinsonian Syndrome
Oral
Initiate at low dosage and increase slowly (at intervals of 7 or 14 days) until the maximum therapeutic response is achieved.†
2–6 mg daily has been used.†
Therapy has been initiated with 1 mg once daily, then increased in increments of 0.5–1 mg at 7 or 14 day intervals until control of symptoms obtained.†
When cabergoline is used as an adjunct to levodopa, the levodopa dosage may be decreased gradually as tolerated.†
When therapy with a dopamine receptor agonist is discontinued, the drug is discontinued gradually.†
Prescribing Limits
Adults
Hyperprolactinemic Disorders
Oral
Dosages >1 mg twice weekly have not been systematically evaluated.
Special Populations
Hepatic Impairment
No specific dosage recommendations at this time; use with caution in patients with severe hepatic impairment. (See Hepatic Impairment under Cautions and also see Absorption: Special Populations, under Pharmacokinetics.)
Renal Impairment
No specific dosage recommendations at this time.(See Elimination: Special Populations, under Pharmacokinetics.)
Geriatric Patients
Select dosage carefully; start at low dosage.(See Geriatric Use under Cautions.)
Use with caution in patients with history of, or current signs and/or symptoms of, respiratory or cardiac disorders linked to fibrotic tissue.
General Precautions
When used for parkinsonian syndrome, observe the usual precautions associated with dopamine receptor agonist therapy in this patient population. Usual dosage for parkinsonian syndrome exceeds dosage used for hyperprolactinemia.
Symptomatic Hypotension
Orthostatic hypotension reported, especially if initial doses >1 mg are used. Exercise care in patients currently receiving drugs known to lower BP.
Postpartum Breast Engorgement
Not indicated for the inhibition or suppression of lactation. Hypertension, cerebrovascular accidents, and seizures reported rarely when another dopamine receptor agonist (i.e., bromocriptine) was used for this indication.
Specific Populations
Pregnancy
Category B. (See Hypertension during Pregnancy under Cautions.)
Lactation
Not known whether cabergoline is distributed into milk; drug is expected to interfere with lactation. Discontinue nursing or the drug.
Pediatric Use
Safety and efficacy not established.
Geriatric Use
Insufficient experience from clinical studies to determine whether patients ≥65 years of age respond differently than younger adults. Other clinical experience has not identified age-related differences in responses.
Select dosage carefully, generally initiating therapy at low dosage. Consider the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or drug therapy in geriatric patients.
Hepatic Impairment
Cabergoline extensively metabolized in liver; use with caution and monitor carefully.(See Absorption: Special Populations, under Pharmacokinetics.)
Consider a reduction in levodopa dosage when cabergoline is added to levodopa therapy
Pharmacokinetics
Absorption
Bioavailability
Peak plasma concentrations usually attained within 1–2 hours.
Absolute bioavailability unknown.
Onset
Following oral administration of a single 0.6-mg dose of cabergoline, time to maximum prolactin-lowering effect was 48 hours.
Duration
Prolactin-lowering effect persists for 14 days.
Food
Food does not alter the pharmacokinetics of cabergoline.
Special Populations
Peak plasma concentrations and AUC not altered in patients with mild to moderate hepatic impairment (Child Pugh score ≤10). Peak plasma concentrations and AUC substantially increased in patients with severe impairment (Child Pugh score >10).
Distribution
Extent
Extensively distributed throughout the body, including the CNS.
Plasma Protein Binding
40–42%.
Elimination
Metabolism
Metabolized in the liver (minimal CYP involvement), mainly by hydrolysis of the acylurea bond; undergoes substantial first-pass metabolism.
Elimination Route
Excreted in feces (72%) and in urine (18% as metabolites and unchanged drug).
Half-life
63–109 hours.
Special Populations
Pharmacokinetic values not altered in patients with moderate to severe renal impairment.
Stability
Storage
Oral
Tablets
20–25°C.
Actions
A long-acting dopamine receptor agonist; has high binding affinity for dopamine D2 receptors and lesser affinity for D1, α1- and α2-adrenergic, and serotonin (5-HT1 and 5-HT2) receptors.
Reduces serum prolactin concentrations by inhibiting release of prolactin from the anterior pituitary gland. This effect on hypothalamic/pituitary function attributed to the drug's agonist activity at D2 receptors.
Advice to Patients
Potential for hypotension.
Importance of patients informing clinicians if cough or dyspnea develop.
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., respiratory or cardiac disorders associated with fibrosis).
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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