Cabergoline (cabergoline)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Cabergoline is an ergot-derivative dopamine receptor agonist and prolactin inhibitor.

Cabergoline, a long-acting dopamine receptor agonist, has high binding affinity for dopamine D2 receptors and lesser affinity for D1, alpha1- and alpha2-adrenergic, and serotonin (5-HT1 and 5-HT2) receptors. Cabergoline reduces serum prolactin concentrations by inhibiting release of prolactin from the anterior pituitary gland. This effect on hypothalamic/pituitary function is attributed to the drug's agonist activity at D2 receptors.

USES: This medication is used to treat high levels of prolactin hormone in your body. High levels of prolactin in women can cause symptoms such as unwanted breast milk and missed periods and can cause difficulty becoming pregnant. High levels of prolactin in men can cause symptoms such as enlarged breasts and decreased sexual ability/desire.

Cabergoline is an ergot medication and works by blocking the release of prolactin from the pituitary gland.

Generic name: cabergoline
Pronunciation: (ka-BER-goe-leen)

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Cabergoline:

  • Hyperprolactinemia

Dosing

Cabergoline therapy should be initiated with a low dosage and increased slowly (at intervals of at least 4 weeks) until therapeutic response is achieved.

An initial adult cabergoline dosage of 0.25 mg twice weekly is recommended for the treatment of hyperprolactinemic disorders; dosage may be increased in increments of 0.25 mg twice weekly up to 1 mg twice weekly based on the patient's serum prolactin concentrations; the lowest effective dosage should be used.

Patients receiving long-term treatment with the drug should be periodically evaluated to determine continued need for therapy. Some patients (e.g., those with normal prolactin concentrations for 6 months) may be able to discontinue the drug with periodic monitoring of serum prolactin concentrations to determine whether or when cabergoline therapy should be reinstituted; discontinuance of therapy in those with macroadenomas should be undertaken with extreme caution. The manufacturer states that efficacy of cabergoline beyond 24 months has not been established.

Drug interactions

There is no enhanced messaging for this drug.

Contraindications

Known hypersensitivity to cabergoline or other ergot derivatives.

Uncontrolled hypertension.

History of cardiac valvular disorders (e.g., valve leaflet thickening, valve restriction, mixed valve restriction-stenosis).

History of pulmonary, pericardial, or retroperitoneal fibrotic disorders.

Adverse reactions

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

Precautions

No enhanced messaging available.

ICD codes

No ICD codes are available for this drug.

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data