From the Guidelines
Cabergoline is the preferred dopamine agonist for the management of hyperprolactinemia, particularly in patients with prolactinomas, due to its superior effectiveness and lower adverse effect profile, as evidenced by a strong recommendation with moderate-quality evidence from the 2024 consensus guideline for the diagnosis and management of pituitary adenomas in childhood and adolescence 1. The role of cabergoline in hormone replacement therapy is primarily focused on managing hyperprolactinemia rather than traditional hormone replacement. It works by mimicking dopamine's action to inhibit prolactin secretion from the pituitary gland. Key points to consider in the management of hyperprolactinemia with cabergoline include:
- The typical starting dose is 0.25 mg twice weekly, which can be gradually increased if needed, with most patients requiring 0.5-1 mg twice weekly.
- Treatment duration varies based on the underlying cause, with microadenomas often requiring 2-5 years of therapy while idiopathic hyperprolactinemia may need shorter courses.
- Cabergoline is preferred over older bromocriptine due to its better side effect profile and twice-weekly dosing, as supported by a randomized controlled trial that showed cabergoline was superior to bromocriptine in normalizing prolactin levels and had fewer adverse events 1.
- Common side effects include nausea, headache, and dizziness, which can be minimized by taking it at bedtime with food.
- Patients should have regular prolactin level monitoring, with dose adjustments based on these results.
- Cabergoline helps restore normal reproductive function by normalizing prolactin levels, which can reverse symptoms like menstrual irregularities, infertility, decreased libido, and galactorrhea.
- For patients with prolactinomas, it can also reduce tumor size and relieve associated symptoms like headaches and visual disturbances, with studies showing that cabergoline can reduce tumor size by 80-88% and improve visual deficits 1.
From the FDA Drug Label
The secretion of prolactin by the anterior pituitary is mainly under hypothalamic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. The prolactin-lowering efficacy of cabergoline was demonstrated in hyperprolactinemic women in two randomized, double-blind, comparative studies, one with placebo and the other with bromocriptine Restoration of menses occurred in 77% of the women treated with cabergoline, compared with 70% of those treated with bromocriptine.
The role of cabergoline in hormone replacement is to decrease serum prolactin levels and restore menses in hyperprolactinemic women.
- Key benefits of cabergoline include:
- Prolactin lowering efficacy: demonstrated in hyperprolactinemic women
- Restoration of menses: occurred in 77% of women treated with cabergoline
- Galactorrhea disappearance: occurred in 73% of women treated with cabergoline Cabergoline is indicated for the treatment of hyperprolactinemic disorders 2.
From the Research
Role of Cabergoline in Hormone Replacement
- Cabergoline is a dopamine agonist that is effective in normalizing prolactin levels in patients with hyperprolactinemia, as shown in a study of 455 patients 3.
- The drug has been found to be more effective than bromocriptine in treating hyperprolactinemic amenorrhea, with a higher rate of normalization of serum prolactin levels and resumption of ovulatory cycles 4.
- Cabergoline has also been shown to be effective in inhibiting and suppressing puerperal lactation, with better efficacy and tolerability results compared to bromocriptine 5.
Efficacy and Tolerability
- A long-term study of cabergoline therapy in hyperprolactinemic disorders found that the drug was effective in normalizing prolactin levels and restoring gonadal function in 85% of patients, with a low rate of adverse events 6.
- A systematic review and meta-analysis of randomized controlled trials found that cabergoline was more effective than bromocriptine in normalizing serum prolactin levels and restoring menstruation, with a lower rate of adverse effects 7.
- The majority of patients with macroprolactinomas and microprolactinomas have been found to experience tumor shrinkage with cabergoline treatment 3, 5.
Comparison with Bromocriptine
- Cabergoline has been found to be more effective and better tolerated than bromocriptine in the treatment of hyperprolactinemia, with a lower rate of adverse effects and a higher rate of normalization of serum prolactin levels 4, 7.
- A study found that patients with bromocriptine intolerance or resistance were able to tolerate cabergoline and experience normalization of prolactin levels 3.