Key takeaways:
Dopamine agonists are the most common medications used to treat hyperprolactinemia.
The two FDA-approved medications for treating hyperprolactinemia are cabergoline and bromocriptine (Parlodel).
Cabergoline may be better than bromocriptine at lowering prolactin levels. It also causes fewer side effects.
Prolactin is a natural hormone made by the pituitary gland, which is below the brain. Under normal conditions, we all have a small amount of it in our bodies. It’s an important hormone because it regulates our estrogen and testosterone levels. And, it helps mothers produce breast milk after giving birth.
But, having extra prolactin can be a problem. Hyperprolactinemia is when there’s too much prolactin in nonpregnant women and men. Common causes include pituitary tumors, hypothyroidism, and certain medications like antipsychotics. Too much prolactin can cause problems. These include infertility, loss of sex drive, and gynecomastia (when men develop breasts).
When symptoms of hyperprolactinemia are bothersome, certain medications can help lower prolactin levels. Here, we’ll learn more about the medications used to treat hyperprolactinemia.
Dopamine agonists are the most common medications for treating hyperprolactinemia. These medications work like dopamine (a chemical messenger) does in the body. Dopamine has many functions, including controlling levels of prolactin. When there’s more dopamine in the blood, the body makes less prolactin.
Dopamine agonists attach to dopamine “D2” receptors in the pituitary gland. By attaching to these binding sites, dopamine agonists act like natural dopamine. The body is “tricked” into thinking there is more dopamine around. This stops prolactin production. As prolactin levels lower, hyperprolactinemia symptoms improve.
Currently, two dopamine agonists are FDA-approved to treat hyperprolactinemia. They are bromocriptine (Parlodel) and cabergoline.
Bromocriptine is a tablet or capsule that you take once daily. You’ll start by taking 1.25 mg to 2.5 mg every day. Your healthcare provider may raise your dose every 2 to 7 days. The goal is to find a dose that works well and doesn’t have too many side effects. Most people will end up taking somewhere between 2.5 mg to 15 mg daily. Take bromocriptine with food to prevent an upset stomach.
Cabergoline is a tablet that you take twice a week. The usual starting dose is 0.25 mg twice a week. Your healthcare provider will check your prolactin levels while you take cabergoline. If your levels remain high, your provider may raise your dose. The dose shouldn’t be raised more often than every 4 weeks. The maximum dose of cabergoline is 1 mg twice a week. You can take it with or without food.
Prolactinomas (pituitary tumors) are a common cause of hyperprolactinemia. If your hyperprolactinemia is caused by a prolactinoma, you’ll likely take dopamine agonists for at least 2 years. Your healthcare provider will check your prolactin levels and see if your tumor shrank during treatment. After 2 years, your provider will help you decide if you should continue on a dopamine agonist.
Cabergoline usually has fewer side effects than bromocriptine. But, cabergoline has been linked with valvular regurgitation. This is a fancy term for when a heart valve doesn’t close well. This can cause blood to flow backwards through the heart.
Either medication can cause the following side effects:
Nausea
Vomiting
Low blood pressure when standing
Headache
Dizziness
Abnormal heart rhythm
Using these medications for a long time can also lead to issues with your mental health. This includes depression and hallucinations.
If you have high blood pressure, talk to your healthcare provider before starting a dopamine agonist. This is especially important if you’re pregnant. And if you have health conditions affecting your heart, kidney, or liver, your provider can discuss the pros and cons of taking a dopamine agonist.
Studies have compared bromocriptine and cabergoline to see which works best. Cabergoline appears more effective than bromocriptine at lowering prolactin levels. It also has fewer side effects. And, it may be better at treating other issues associated with hyperprolactinemia. These include things like irregular periods and high blood sugar.
One review looked at over 700 women with hyperprolactinemia. The researchers found that cabergoline was better at lowering prolactin levels compared to bromocriptine. Women taking cabergoline also had fewer side effects.
Another review compared cabergoline to bromocriptine in people with hyperprolactinemia caused by prolactinomas. This review of 12 studies found that cabergoline caused fewer side effects. And it was better than bromocriptine at treating some symptoms of hyperprolactinemia. These include irregular periods and galactorrhea (breast milk production in a non-breastfeeding person). But, cabergoline wasn’t more effective than bromocriptine at shrinking prolactinomas.
Remember that hyperprolactinemia can cause infertility, loss of sex drive, and gynecomastia. Hyperprolactinemia can also affect how fats and glucose are broken down in the body. A small study looked at 20 women with hyperprolactinemia. They evaluated whether bromocriptine or cabergoline was better at normalizing prolactin, lipid, and blood sugar levels in the body.
The study found that cabergoline and bromocriptine were similar in reducing prolactin levels. But cabergoline lowered triglycerides and blood sugar more than bromocriptine. It also raised HDL (the good cholesterol) more than bromocriptine. This study was small, so more studies are needed to confirm these results.
The cost of dopamine agonists will vary depending on the dose you’re taking and the pharmacy you use. With a GoodRx coupon, 30 tablets of 2.5 mg of bromocriptine could cost less than $35. And 0.5 mg Cabergoline could cost around $25 for eight tablets.
If you have a large prolactinoma causing your hyperprolactinemia, medications are usually necessary. This is also true if you have symptoms that affect your daily life. But if you have few or no symptoms, treatment may not be necessary.
If a medical condition is causing hyperprolactinemia, treating the underlying condition can help. For example, hypothyroidism (an underactive thyroid) can cause hyperprolactinemia. Taking thyroid medication to treat hypothyroidism may resolve hyperprolactinemia. If hyperprolactinemia resolves, a dopamine agonist isn't needed.
If a medication you take causes hyperprolactinemia, talk to your healthcare provider. They may be able to help you find an alternative medication that doesn’t raise prolactin levels. The medications that most commonly cause hyperprolactinemia are antipsychotic medications. These include haloperidol (Haldol) and risperidone (Risperdal).
A large pituitary tumor left untreated can cause vision problems and headaches. And, high levels of prolactin can cause infertility and lowered bone density (osteoporosis).
When medication doesn’t shrink a prolactinoma, surgery or radiation are alternative options. And, surgery or radiation might be better treatment options if you have unbearable side effects from dopamine agonists.
Dopamine agonists are first-choice medications for treating hyperprolactinemia. The two dopamine agonists that are FDA-approved for hyperprolactinemia are bromocriptine and cabergoline. Both medications cause similar side effects, like nausea, vomiting, and headache. But, studies suggest that cabergoline causes fewer side effects. It's also better at treating hyperprolactinemia.
If you think you need medication for hyperprolactinemia, talk to your healthcare provider. They can help you decide if medication is needed, and which one is best for you.
American Academy of Optometry. (2004). Ocular manifestations of prolactinoma.
Ansari, M. S., et al. (2016). Primary hypothyroidism with markedly high prolactin. Frontiers in Endocrinology.
A-S. Medical Solutions. (2021). Cabergoline.
Auriemma, R. S., et al. (2018). The effects of hyperprolactinemia and its control on metabolic diseases. Expert Review of Endocrinology & Metabolism.
Brue, T., et al. (2016). The risks of overlooking the diagnosis of secreting pituitary adenomas. Orphanet Journal of Rare Diseases.
Budayr, A., et al. (2020). Cardiac valvular abnormalities associated with use and cumulative exposure of cabergoline for hyperprolactinemia: The CATCH study. Biomedical Central Endocrine Disorders.
Chanson, P., et al. (2007). Drug treatment of hyperprolactinemia. Annals of Endocrinology.
Choi, J., et al. (2021). Dopamine Agonists. StatPearls.
Dimarki, E., et al. (2022). Hyperprolactinemia. Endocrine Society
dos Santos Nunes, V. et al., (2011). Cabergoline versus bromocriptine in the treatment of hyperprolactinemia: A systematic review of randomized controlled trials and meta-analysis. Pituitary.
Fish, S. (2022). Brain Hormones. Endocrine Society.
Fitzgerald, P., et al. (2008). Prolactin and dopamine: What is the connection? A review article. Journal of Psychopharmacology.
Food and Drug Administration. (2012). Parlodel.
Food and Drug Administration. (2018). Understanding unapproved use of approved drugs "off label."
Kaiser, U. B. (2012). Hyperprolactinemia and infertility: New insights. The Journal of Clinical Investigation.
Klibanski, A., et al. (1980). Decreased bone density in hyperprolactinemic women. The New England Journal of Medicine.
Krysiak, R., et al. (2014). Different effects of cabergoline and bromocriptine on metabolic and cardiovascular risk factors in patients with elevated prolactin levels. Basic & Clinical Pharmacology & Toxicology.
Liu, X., et al. (2019). The mechanism and pathways of dopamine and dopamine agonists in prolactinomas. Frontiers in Endocrinology.
Melmed, S., et al. (2011). Diagnosis and treatment of hyperprolactinemia: An endocrine society clinical practice guideline. The Journal of Clinical Endocrinology & Metabolism.
Molitch, M.E., et al. (2005). Drug-induced hyperprolactinemia. Mayo Clinic Proceedings.
Mylan Pharmaceuticals Inc. (2021). Bromocriptine Mesylate.
Navy, H., et al. (2018). Strategies for managing medication-induced hyperprolactinemia. Current Psychiatry.
National Health Service. (2021). Why must some medicines be taken with or after food?
National Institute of Diabetes and Digestive and Kidney Diseases. (2019). Prolactinoma.
Nunes-Nogueira, V. S., et al. (2018). Dopamine agonists for idiopathic hyperprolactinemia and prolactinoma in adults. Cochrane Database of Systematic Reviews.
Prescribers’ Digital Reference. (n.d.). Bromocriptine mesylate - drug summary.
Public Library of Science. (2017). Dopamine control of prolactin secretion: hierarchy is the key!
Helena, C. (2017). Dopamine control of prolactin secretion: Hierarchy is the key! Public Library of Science Blog.
Reproductive Facts.org. (2014). Hyperprolactinemia (high prolactin levels).
Society for Endocrinology. (2014). Prolactinoma.
Thapa, S., et al. (2021). Hyperprolactinemia. StatPearls.
Triantafilo, N., et al. (2016). Cabergoline or bromocriptine for prolactinoma? Medwave.
Wang, A., et al. (2012). Treatment of hyperprolactinemia: a systematic review and meta-analysis. Systematic Reviews.
Wand, G. S. (2003). Diagnosis and management of hyperprolactinemia. The Endocrinologist.
Webster, J., et al. (1994). A comparison of cabergoline and bromocriptine in the treatment of hyperprolactinemic amenorrhea. The New England Journal of Medicine.
Yale Medicine. (n.d.). Hyperprolactinemia.
Zygourakis, C.C., et al. (2017). Cost-effectiveness analysis of surgical versus medical treatment of prolactinomas. Journal of Neurological Surgery.