Cabergoline (cabergoline)
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.
Today’s intelligence on Cabergoline
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.
Cabergoline is administered orally without regard to meals.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions 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.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Patients with hyperprolactinemia: Nausea, constipation, abdominal pain, headache, dizziness, asthenia, fatigue, and somnolence.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of cabergoline have not been established in pediatric patients.
There are no adequate and well-controlled studies of cabergoline in pregnant women. Animal reproduction studies revealed some evidence of maternal toxicity and postimplantation embryofetal loss, but developmental malformations were not consistently observed. (See Hypertension during Pregnancy under Cautions.)
It is not known whether cabergoline is distributed into milk; however, the drug is expected to interfere with lactation. A decision should be made whether to discontinue nursing or the drug, taking into account the importance of cabergoline to the mother. Use of cabergoline for the inhibition or suppression of lactation is not recommended.
Dosage should be selected carefully in geriatric patients, starting at the low end of the dosage range. (See Cautions: Geriatric Use.)
There is 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.
The effect of age on the pharmacokinetics of cabergoline has not been studied.
The greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or drug therapy in geriatric patients should be considered.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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