From the Guidelines
The treatment for elevated prolactin levels should start with cabergoline as the 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. This approach is based on the most recent and highest quality evidence available, as indicated in the consensus guideline for the diagnosis and management of pituitary adenomas in childhood and adolescence 1.
Key Considerations for Treatment
- Dopamine agonists, such as cabergoline, are the mainstay of treatment for prolactinomas and idiopathic hyperprolactinemia.
- Cabergoline has a longer half-life and greater affinity for the dopamine receptor than other dopamine agonists, making it the preferred choice 1.
- The initial dose of cabergoline can be started at 0.25mg twice weekly and gradually increased to 0.5-1mg twice weekly as needed, with careful monitoring of prolactin levels and tumor size.
- For patients resistant to standard doses of cabergoline, graduated dose increments of up to 3.5 mg per week or up to 7 mg per week in exceptional cases may be considered 1.
- Surgery and radiotherapy are reserved for patients who do not respond to or cannot tolerate medication, or for those with large tumors causing significant compression symptoms 1.
Monitoring and Follow-Up
- Regular monitoring of prolactin levels and tumor size is essential to assess the effectiveness of treatment and adjust the dose as needed.
- Patients should be monitored for potential side effects of dopamine agonists, such as nausea, dizziness, and headache, which can be minimized by taking medication with food and starting at low doses.
- In cases where surgery is considered, careful multidisciplinary discussion is necessary to weigh the benefits and risks of surgical intervention 1.
Diagnosis and Evaluation
- A single prolactin measurement taken at any time of the day is sufficient to assess hyperprolactinemia, but serial measurements over time may be necessary to exclude the effect of stress and prolactin pulsatility 1.
- Age-specific and sex-specific prolactin reference ranges should be used, and confounding conditions such as hypothyroidism, renal and/or hepatic impairment, and use of medications that cause hyperprolactinemia should be excluded 1.
From the FDA Drug Label
The dopaminergic neurons in the tuberoinfundibular process modulate the secretion of prolactin from the anterior pituitary by secreting a prolactin inhibitory factor (thought to be dopamine); in the corpus striatum the dopaminergic neurons are involved in the control of motor function Clinically, bromocriptine mesylate significantly reduces plasma levels of prolactin in patients with physiologically elevated prolactin as well as in patients with hyperprolactinemia.
The treatment for elevated prolactin levels is bromocriptine mesylate, a dopamine receptor agonist that activates post-synaptic dopamine receptors and reduces plasma levels of prolactin.
- Key benefits:
- Significantly reduces plasma levels of prolactin
- Inhibits the secretion of prolactin from the anterior pituitary
- Can be used to treat hyperprolactinemia and physiologically elevated prolactin
- Important considerations:
- Should be taken with food to minimize vomiting
- May interact with other medications, such as CYP3A4 inhibitors
- Requires periodic monitoring of blood pressure and other potential side effects 2
- Cabergoline is another option for treating hyperprolactinemic disorders, and it should be used with caution in patients with a history of cardiac or extracardiac fibrotic disorders 3.
From the Research
Treatment Options for Elevated Prolactin Levels
- Dopamine agonists are the primary treatment for hyperprolactinemia, with cabergoline being the most commonly used due to its favorable profile 4, 5, 6
- The goal of treatment is to normalize prolactin levels, restore gonadal function, and reduce the effects of chronic hyperprolactinemia 6
- For patients with prolactinomas, treatment with dopamine agonists can lead to normalization of prolactin secretion and gonadal function, as well as significant tumor shrinkage 4
Resistance to Dopamine Agonists
- A subset of patients may not respond to dopamine agonists, with a prevalence of 20-30% for bromocriptine and around 10% for cabergoline 7
- Predictive factors for dopamine agonist resistance include male gender and tumor invasiveness 7
- For patients resistant to dopamine agonists, options include switching to a different dopamine agonist, dose escalation, or considering alternative treatments such as temozolomide or surgery 5, 7
Alternative Treatments
- Surgery is typically reserved for patients who are intolerant of or resistant to dopamine agonists, or when hyperprolactinemia is caused by non-prolactin-secreting tumors compressing the pituitary stalk 4, 6
- Radiotherapy may be considered for patients with aggressive prolactinomas 7
- Other experimental treatments, such as aromatase inhibitors, somatostatin receptor ligands, and immune-checkpoint inhibitors, may be effective in some patients with refractory prolactinomas, but more research is needed 5