Cabergoline is a synthetic ergoline derivative and a long-acting dopamine receptor agonist with high affinity for the dopamine D2 receptor. Cabergoline exerts an inhibitory effect on prolactin secretion by acting on dopamine receptors present in pituitary lactotrophs. This drug also binds to dopamine D2 receptors in the corpus striatum, thereby mimicking the actions of dopamine on motor control. Cabergoline also possesses antioxidant and neuroprotective properties due to its free radical scavenging activity. Cabergoline is used in the treatment of Parkinson’s disease and in the treatment of hyperprolactinemia.
Cabergoline, sold under the brand name Dostinex among others, is a dopaminergic medication used in the treatment of high prolactin levels, prolactinomas, Parkinson’s disease, and for other indications. It is taken by mouth.
Cabergoline is an ergot derivative and a potent dopamine D2 receptor agonist.
Cabergoline was patented in 1980 and approved for medical use in 1993.
This medication is used to treat high levels of prolactin hormone in your body. High levels of prolactin in women can cause symptoms such as unwanted breast milk and missed periods and can cause difficulty becoming pregnant. High levels of prolactin in men can cause symptoms such as enlarged breasts and decreased sexual ability/desire. Cabergoline is an ergot medication and works by blocking the release of prolactin from the pituitary gland.
Side effects are mostly dose dependent. Much more severe side effects are reported for treatment of Parkinson’s disease and (off-label treatment) for restless leg syndrome which both typically require very high doses. The side effects are considered mild when used for treatment of hyperprolactinemia and other endocrine disorders or gynecologic indications where the typical dose is one hundredth to one tenth that for Parkinson’s disease.
Cabergoline requires slow dose titration (2–4 weeks for hyperprolactinemia, often much longer for other conditions) to minimise side effects. The extremely long bioavailability of the medication may complicate dosing regimens during titration and require particular precautions.
Cabergoline is considered the best tolerable option for hyperprolactinemia treatment although the newer and less tested quinagolide may offer similarly favourable side effect profile with quicker titration times.
As with other ergot derivatives, pleuritis, exudative pleura disease, pleura fibrosis, lung fibrosis, and pericarditis are seen. These side effects are noted in less than 2% of patients. They require immediate termination of treatment. Clinical improvement and normalization of X-ray findings are normally seen soon after cabergoline withdrawal. It appears that the dose typically used for treatment of hyperprolactinemia is too low to cause this type of side effects.
Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following.
Scarring of tissues in your organs, such as your heart, lungs, and kidneys. Symptoms can include:
- trouble breathing
- shortness of breath
- a cough that doesn’t go away
- chest pain that doesn’t go away
- stomach pain
- swelling in your legs, ankles, or feet
Heart valve problems. Symptoms can include:
- swelling in your arms, legs, hands, or feet
- trouble breathing
- changes in your heart rhythm
- chest pain
Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
The more common side effects of cabergoline oral tablet can include:
- weakness or lack of energy
If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.
Call your doctor at once if you have:
- shortness of breath (even while lying down);
- chest pain, dry cough or hack;
- a light-headed feeling, like you might pass out;
- pain in your side or lower back;
- little or no urination; or
- swelling in your ankles or feet.
You may have increased sexual urges, unusual urges to gamble, or other intense urges while taking cabergoline. Talk with your doctor if this occurs.