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GREENSTONE LLC.
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59762100501

cabergoline 0.5 mg tablet

Generic
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Uses

Hyperprolactinemic Disorders

Cabergoline is used in the treatment of hyperprolactinemic disorders due to prolactinoma (prolactin-secreting adenomas) or idiopathic hyperprolactinemia. The drug suppresses prolactin secretion, restores gonadal function, and reduces the size of prolactinomas.

Cabergoline is 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, were reported in cabergoline-treated women than in bromocriptine-treated women. Bromocriptine is 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

Cabergoline has been used for the symptomatic management of parkinsonian syndrome.

Cabergoline has been used as monotherapy for the 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 or younger.

Cabergoline 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.

Parkinsonian syndrome: Administer once daily.

Dosage

Adults

Hyperprolactinemic Disorders

Oral:

Initiate at low dosage and increase slowly (at intervals of at least 4 weeks) 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 by at least 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 beyond 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 Cautions: Hepatic Impairment.)

Renal Impairment

No specific dosage recommendations at this time.

Geriatric Patients

Select dosage carefully; start at low dosage.(See Cautions: Geriatric Use.)

Cautions

Contraindications

Known hypersensitivity to cabergoline or other ergot derivatives.

Uncontrolled hypertension.

Warnings/Precautions

Warnings

Hypertension during Pregnancy

Should not be used in patients with pregnancy-induced hypertension (e.g., preeclampsia, eclampsia) unless potential benefits outweigh possible risks.

Fibrotic Effects

Pleural effusion, pulmonary fibrosis, and cardiac valvulopathy reported. Signs and symptoms have improved after discontinuance.

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 exceeding 1 mg are used. Exercise care in patients currently receiving drugs known to lower blood pressure.

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 Cautions: Hypertension during Pregnancy.)

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 or older 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 is extensively metabolized in liver; use with caution and monitor carefully.

Common Adverse Effects

Patients with hyperprolactinemia: Nausea, constipation, abdominal pain, headache, dizziness, asthenia, fatigue, somnolence.

Patients with parkinsonian syndrome: Dyskinesia, hallucinations, confusion, peripheral edema.

Drug Interactions

Dopamine Antagonists (e.g., phenothiazines, butyrophenones, thioxanthenes, metoclopramide)

Possible reduced efficacy of cabergoline. Generally should not be used concomitantly.

Levodopa

Additive therapeutic and/or adverse (e.g., dyskinesia) effects. 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.

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