What is cabergoline? How does it work (mechanism of action)?
Cabergoline is a synthetic ergot derived medication that acts on dopamine receptors in the pituitary gland which is located at the base of the brain. Cabergoline stimulates D2 (a specific type of dopamine receptor) receptors in the anterior pituitary gland and prevents the production of the hormone prolactin.
The approval of cabergoline has gradually decreased the use of bromocriptine (Cycloset) for the treatment of hyperprolactinemias (abnormally high levels of prolactin in the blood). Cabergoline may be more effective than bromocriptine and has less bothersome side effects. Additionally, bromocriptine is given multiple times per day while cabergoline has a longer half-life which allows it to be given twice weekly. Cabergoline was first approved by the FDA for the treatment of hyperprolactinemic disorders (high levels of prolactin) on Dec. 23, 1996.
Is cabergoline available as a generic drug?
Yes, cabergoline is available in generic form.
Do I need a prescription for cabergoline?
Yes, you need a prescription from your doctor or other medical health care professional for cabergoline.
What are the uses for cabergoline?
Cabergoline is used for the treatment high levels of prolactin in the blood, a condition known as hyperprolactinemia.
What are cabergoline side effects?
The most common side effects are:
- nausea,
- headache,
- dizziness or vertigo,
- weakness,
- low blood pressure,
- constipation, and
- stomach pain.
Less commonly reported side effects are:
- abnormal heart rhythm changes,
- pain in the upper middle area of the stomach,
- nosebleeds, and
- temporary blindness in one half of the visual field in one or both eyes.
Rare (occurring in <1% of patients) side effects include:
- heart problems,
- movement disorders,
- duodenal ulcer,
- facial edema (swelling),
- gastric ulcer,
- hallucinations,
- increased libido,
- pathological gambling,
- psychosis,
- lung problems, and
- weight gain or loss.
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What is the dosage for cabergoline and how should I take it?
The recommended dosage of cabergoline tablets for initiation of therapy is 0.25 mg twice a week. Dosage may be increased by 0.25 mg twice weekly up to a dosage of 1 mg twice a week according to the patient’s serum prolactin level. Before initiating treatment, cardiovascular evaluation should be performed and echocardiography should be considered to assess for valvular disease.
Dosage increases should not occur more rapidly than every 4 weeks, so that the physician can assess the patient’s response to each dosage level. If the patient does not respond adequately, and no additional benefit is observed with higher doses, the lowest dose that achieved maximal response should be used and other therapeutic approaches considered.
Patients receiving long-term treatment with cabergoline should undergo periodic assessment of their cardiac status and echocardiography should be considered.
After a normal serum prolactin level has been maintained for 6 months, cabergoline may be discontinued, with periodic monitoring of the serum prolactin level to determine whether or when treatment with cabergoline should be reinstituted. The durability of efficacy beyond 24 months of therapy with cabergoline has not been established.
Cabergoline is better tolerated when administered with food.
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Which drugs or supplements interact with cabergoline?
Cabergoline is related to the ergot alkaloids. The use of cabergoline with other ergot alkaloids is not recommended due to the increased risk for adverse events. Ergot alkaloids are commonly used to treat migraine headaches. Therefore, patients receiving treatment for migraine headaches should discuss treatment with cabergoline with their doctor or pharmacist before using cabergoline.
Cabergoline works by stimulating dopamine receptors in the brain. It should not be used with dopamine antagonists or blockers which might decrease or cancel out the beneficial effects of cabergoline. Examples of dopamine antagonists are phenothiazines, butyrophenones, thioxanthenes, and metoclopramide (Reglan).
Is cabergoline safe to take if I’m pregnant or breastfeeding?
No adequate or well-controlled studies have been conducted in pregnant women. Due to the lack of conclusive safety data, cabergoline should only be used in pregnancy if clearly needed. Cabergoline is classified in FDA pregnancy risk category B.
Cabergoline should not be used in breastfeeding mothers because it interferes with the production of breast milk. It is not known whether cabergoline is excreted in human milk.
What else should I know about this drug?
What preparations of oral cabergoline are available?
Oral tablets: 0.5 mg
How should I keep oral cabergoline stored?
Tablets should be stored at room temperature, between 15 C to 30 C (59 F to 86 F).