Is Cabergoline (cabergoline) safe?

From the Guidelines

Cabergoline is generally safe when used as prescribed under medical supervision, but it does have potential risks and side effects. It's a dopamine agonist medication commonly used to treat conditions like hyperprolactinemia, Parkinson's disease, and sometimes off-label for conditions like restless leg syndrome. Typical dosing ranges from 0.25 to 2 mg weekly, often divided into two doses. Common side effects include nausea, dizziness, headache, and fatigue, which often improve with continued use. More serious concerns include potential heart valve problems with long-term, high-dose use, which is why regular cardiac monitoring may be recommended for patients on higher doses or extended treatment, as suggested by a study published in Nature Reviews Endocrinology 1.

Key Considerations

• Cabergoline may also cause orthostatic hypotension (blood pressure drop when standing), so patients should rise slowly from sitting or lying positions.
• It can interact with certain medications, particularly antipsychotics and medications that affect dopamine levels.
• Pregnant women or those planning pregnancy should discuss risks with their doctor as cabergoline affects hormone levels.
• The safety profile is favorable for most patients when used appropriately, as it works by normalizing prolactin levels by binding to dopamine receptors in the pituitary gland.
• A consensus guideline for the diagnosis and management of pituitary adenomas in childhood and adolescence recommends offering cabergoline as first-line therapy, even in the presence of visual disturbance and pituitary apoplexy, while carefully monitoring for any deterioration in vision, pituitary function or general status 1.

Monitoring and Precautions

• Regular echocardiograms are recommended for patients receiving >2 mg per week cabergoline and every 5 years if on ≤2 mg per week, as suggested by a study published in Nature Reviews Endocrinology 1.
• Patients should be monitored for signs of dopamine agonist resistance, escape or intolerance, and neurosurgical intervention should be considered if vision deteriorates or does not improve on medical therapy 1.
• The long-term cardiac safety of ergot-based dopamine agonists in children and adolescents requires a balanced judgement against the increasing background rate of cardiac valvulopathy that occurs with age and the often more aggressive nature of prolactinomas in the pediatric age group 1.

From the FDA Drug Label

The safety of cabergoline has been evaluated in approximately 1,200 patients with Parkinson's disease in controlled and uncontrolled studies at dosages of up to 11. 5 mg/day which greatly exceeds the maximum recommended dosage of cabergoline for hyperprolactinemic disorders. The safety of cabergoline tablets has been evaluated in more than 900 patients with hyperprolactinemic disorders. Most adverse events were mild or moderate in severity.

The safety of Cabergoline is a concern due to the potential for adverse events, including:

• Cardiac valvulopathy and extracardiac fibrotic reactions
• Impulse control/compulsive behavior symptoms, including hypersexuality, increased libido, and pathological gambling
• Other events such as alopecia, aggression, and psychotic disorder have been reported in patients taking cabergoline. It is essential to carefully evaluate the potential benefits and risks of cabergoline before initiating treatment, and to closely monitor patients for any adverse events 2 2.

From the Research

Safety of Cabergoline

The safety of cabergoline has been evaluated in several studies, with a focus on its potential impact on cardiac valvular status.

• Cabergoline is a dopamine agonist used to treat hyperprolactinemia, including prolactinomas and idiopathic hyperprolactinemia 3, 4, 5, 6, 7.
• Studies have investigated the association between cabergoline therapy and cardiac valvular abnormalities, with most finding no significant increase in valvular regurgitation or other cardiac valve problems at the doses typically used in endocrinology 3, 4, 5, 7.

Cardiac Valvular Status

Research on the cardiac valvular status of patients treated with cabergoline includes:

• A prospective, long-term study of 100 patients with prolactinoma or idiopathic hyperprolactinemia, which found no clinically relevant alterations in cardiac valve function or valvular calcifications after a median treatment duration of 124.5 months 3.
• A review of seven case-control studies, including 463 patients, which found no association between cabergoline therapy and clinically relevant valvular regurgitation, although one study reported an increased rate of moderate tricuspid regurgitation 4.
• A prospective, multicentric study of 70 patients with prolactinomas treated with cabergoline for at least 1 year, which found no significant difference in the prevalence of moderate valvular regurgitation compared to control subjects 5.

Tolerability and Efficacy

Cabergoline has been shown to be effective and well-tolerated in the treatment of hyperprolactinemic patients:

• A study of 30 female hyperprolactinemic patients treated with cabergoline for 6-12 months found significant reductions in prolactin levels and improvement in symptoms, with most patients experiencing no or mild side effects 6.
• Another study found that cabergoline was better tolerated than bromocriptine, with fewer patients requiring discontinuation of treatment due to side effects 6.