What is cabergoline?

From the Guidelines

Cabergoline is a dopamine agonist that is the first-line treatment for prolactinomas, offering superior effectiveness and a lower adverse effect profile compared to other dopamine agonists, as evidenced by a strong recommendation with moderate-quality evidence 1.

Key Points About Cabergoline

• Cabergoline is used to treat high levels of prolactin hormone in the body (hyperprolactinemia) and certain types of pituitary tumors called prolactinomas.
• It belongs to a class of drugs called dopamine agonists, which work by mimicking the action of dopamine in the brain.
• Typical dosing starts at 0.25 mg twice weekly, with gradual increases based on prolactin levels and patient response, usually not exceeding 1 mg twice weekly.
• Treatment duration varies depending on the condition but may continue for years or indefinitely for prolactinomas.
• Cabergoline effectively reduces prolactin by binding to dopamine D2 receptors in the pituitary gland, inhibiting prolactin secretion.
• Side effects may include nausea, dizziness, headache, and fatigue.
• Patients should be aware that cabergoline can also be used off-label for Parkinson's disease and to suppress lactation.

Monitoring and Adjustments

• Regular monitoring of prolactin levels and pituitary gland size (via MRI) is necessary during treatment to assess effectiveness and adjust dosing accordingly.
• For patients with prolactinomas, an echocardiogram should be offered at the start of treatment with a dopamine agonist, with yearly surveillance echocardiography for patients receiving >2 mg per week cabergoline and every 5 years if on ≤2 mg per week, as recommended with moderate-quality evidence 1.

Special Considerations

• In cases of resistance 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 offered, based on a strong recommendation with moderate-quality evidence 1.
• If the serum level of prolactin has been normalized for at least 2 years on medical therapy and there is no visible residual prolactinoma on MRI, consideration of gradual cabergoline dose reduction to maintain normoprolactinaemia and eventual treatment discontinuation, with continued serum prolactin monitoring for at least 2 more years, is recommended with moderate-quality evidence 1.

From the FDA Drug Label

Cabergoline tablets are indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. Cabergoline is a dopamine receptor agonist. The chemical name for cabergoline is 1-[(6-allylergolin-8β-yl)-carbonyl]-1-[3-(dimethylamino) propyl]-3-ethylurea.

Cabergoline is a dopamine receptor agonist used for the treatment of hyperprolactinemic disorders. It works by inhibiting the secretion of prolactin by the pituitary gland. The drug is available in oral form and contains 0.5 mg of cabergoline per tablet 2, 2, 2.

• Key characteristics:
  • Dopamine receptor agonist
  • Treats hyperprolactinemic disorders
  • Inhibits prolactin secretion
  • Available in 0.5 mg oral tablets
  • Chemical name: 1-[(6-allylergolin-8β-yl)-carbonyl]-1-[3-(dimethylamino) propyl]-3-ethylurea 2

From the Research

Definition and Mechanism of Action

• Cabergoline is a synthetic ergoline that shows high specificity and affinity for the dopamine D2 receptor 3.
• It is a potent and very long-acting inhibitor of prolactin secretion, with prolactin-lowering effects occurring rapidly and lasting up to 21 days after a single dose 3, 4.

Therapeutic Uses

• Cabergoline is used for the treatment of hyperprolactinemia, Parkinson's disease, and antipsychotic-induced prolactin elevation 4.
• It is effective in suppressing prolactin levels and restoring ovulatory cycles in women with hyperprolactinemic amenorrhea 3, 5.
• Cabergoline is also used for the prevention and suppression of puerperal lactation, with a single dose being as effective as bromocriptine for 14 days 3.

Efficacy and Tolerability

• Cabergoline has been shown to be more effective than bromocriptine in reducing prolactin levels and normalizing plasma prolactin levels in patients with hyperprolactinemia 3, 5, 6.
• It appears to offer considerable advantages over bromocriptine in terms of efficacy and tolerability, with fewer adverse events reported 3, 5, 7.
• Cabergoline has also been shown to have beneficial effects on metabolic and cardiovascular risk factors in patients with elevated prolactin levels, including reducing triglycerides, improving insulin sensitivity, and increasing HDL cholesterol 7.

Adverse Effects

• Cabergoline can cause adverse reactions consistent with other dopaminergic agonists, including cardiovascular, gastrointestinal, and neuropsychiatric effects 4.
• It has been associated with a risk of psychosis, and susceptible individuals may experience manic episodes 4.
• However, cabergoline is generally better tolerated than bromocriptine, with most patients intolerant of other ergot derivatives able to tolerate cabergoline 3.