From the Guidelines
Cabergoline should be initiated at a dose of 0.25 mg twice weekly and gradually increased as needed, with some patients requiring up to 3.5 mg per week or even 7 mg per week in exceptional cases for the treatment of hyperprolactinemia. The dose titration should be based on prolactin level monitoring and symptom response, with increments of 0.25 mg every 4 weeks 1.
Key Considerations
- Patients who are resistant to standard doses of cabergoline may benefit from graduated dose increments of up to 3.5 mg per week or up to 7 mg per week in exceptional cases 1.
- High-dose cabergoline is reportedly well tolerated, and doses of up to 7 mg per week have been used to successfully treat patients with prolactinoma 1.
- However, some studies suggest that there may be little benefit of cabergoline doses above 3.5 mg per week in adults 1.
Monitoring and Treatment Duration
- Regular prolactin level monitoring is essential, typically every 4-8 weeks during dose adjustments and then every 6-12 months once levels normalize.
- Treatment duration varies, with microadenomas often requiring 2-3 years of therapy before attempting withdrawal, while macroadenomas typically need longer treatment.
Mechanism of Action and Side Effects
- Cabergoline works by activating dopamine D2 receptors on lactotroph cells in the pituitary gland, inhibiting prolactin secretion.
- Side effects may include nausea, headache, dizziness, and rarely cardiac valve fibrosis with long-term high-dose use, though this is uncommon at doses used for hyperprolactinemia.
From the Research
Cabergoline Dosage for Hyperprolactinemia
The dosage of cabergoline for hyperprolactinemia can vary depending on the individual patient and the severity of their condition.
- The median dose of cabergoline at the start of therapy was 1.0 mg/week, but could be reduced to 0.5 mg/week once control was achieved 2.
- Patients with a macroprolactinoma needed a higher median cabergoline dose, compared with those with idiopathic hyperprolactinemia or a microprolactinoma: 1.0 mg/week vs. 0.5 mg/week 2.
- In another study, cabergoline was given to 48 hyperprolactinemic women for 3-18 months at doses varying between 0.2-3 mg/week administered one to three times weekly 3.
- A study comparing the effects of cabergoline and bromocriptine on prolactin levels in hyperprolactinemic patients used a dose of 0.5 mg twice weekly for cabergoline 4.
- Another study used a dose of 1-2 mg weekly doses of cabergoline, given on a twice weekly schedule, for the treatment of hyperprolactinemic amenorrhoea 5.
Effective Dose Range
The effective dose range of cabergoline for hyperprolactinemia can vary, but most patients can achieve normalization of prolactin levels with doses ranging from 0.25 mg to 2 mg per week.
- In one study, the final treatment doses ranged from 0.25 mg fortnightly to 2 mg twice weekly, with most patients finishing the study taking 0.5 mg once or twice weekly 6.
- The majority of patients (85%) achieved stable normalization of PRL levels with doses less than 1 mg per week 6.
Tolerability and Efficacy
Cabergoline has been shown to be well tolerated and effective in the treatment of hyperprolactinemia, with a high rate of normalization of prolactin levels and few adverse events.
- In one study, side effects were noted in 13% of patients, but only 3.9% discontinued therapy because of side effects 2.
- Another study found that adverse events were reported in 39.5% of patients, but most were mild or moderate and occurred during the first few weeks of therapy 6.
- Cabergoline has been compared to bromocriptine in several studies, and has been shown to have a higher efficacy and better tolerability profile 4, 5.