Cabergoline – Dosage

What is Cabergoline?

Cabergoline, an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor. It is used to treat hyperprolactinemic disorders and Parkinsonian Syndrome. Cabergoline possesses potent agonist activity on dopamine D2 receptors.

Properties and Characteristics of Cabergoline

Drug class	Ergot derivative and prolactine inhibitors
Brand Names	Dostinex, Cabaser, Cabaseril, Cabergolinum [Latin], Cabergolina [Spanish], Cabergolinum, Cabergolina, Galastop
Synonyms	Cabergolina, Cabergoline, Cabergolinum
Molecular Formula	C₂₆H₃₇N₅O₂
Molecular Weight	451.6 g/mol
IUPAC Names	(6aR,9R,10aR)-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)-7-prop-2-enyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide
Structural formula of main components
Pure active ingredient	Cabergoline
Appearance	Solid
Melting Point	102-104 °C
Solubility	Insoluble
Excretion	Excreted within 20 days in the urine
Available as	Tablet
Storage	Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Prescription	Prescription is required

Cabergoline Uses

This drug is used to treat the body with elevated levels of the hormone prolactin. Symptoms such as unwanted breast milk and missed periods can be caused by elevated levels of prolactin in women and can cause difficulties becoming pregnant. Symptoms such as enlarged breasts and diminished sexual ability/desire can be triggered by elevated levels of prolactin in men. Cabergoline is an ergot drug that functions by blocking the release of prolactin from the pituitary gland.

Cabergoline is also used to treat Parkinson’s disease in some cases (a disorder of the nervous system that causes difficulties with movement, muscle control, and balance). Speak to your doctor about the complications of your condition using this drug.

What side effects may I notice from receiving Cabergoline?

Side effects that you should report to your doctor or health care professional as soon as possible:

Allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
Breathing problems
Chest pain
Confusion
Hallucinations
New or increased gambling urges, sexual urges, uncontrollable spending, binge or compulsive eating, or other urges
Persistent cough
Swelling of the ankles, feet, hands
Unusually weak or tired

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):

Constipation
Dizziness
Headache
Nausea

This list may not describe all possible side effects. Call your doctor for medical advice about side effects.

Mechanism of Action

The dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca2+ from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D2 receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1,- and α2- adrenergic, and 5-HT1- and 5-HT2-serotonin receptors.

Drug Interactions

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

Sulpiride

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Haloperidol
Itraconazole
Metoclopramide
Olanzapine

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor’s orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For oral dosage form (tablets)

For disorders of high prolactin levels or pituitary tumors:

Adults—At first, 0.25 milligram (mg) 2 times a week. Your doctor may increase your dose every 4 weeks as needed, according to body prolactin levels, up to 1 mg two times a week.
Children—Use and dose must be determined by the doctor.

Overdose

Call a poison control center immediately if someone has overdosed and has severe signs such as passing out or difficulty breathing. Extreme dizziness, fainting, mental/mood changes can be signs of overdose (such as hallucinations).

Cabergoline warnings

This drug comes with several warnings.

Allergy warning

Cabergoline can cause a severe allergic reaction. Symptoms can include:

Trouble breathing
Swelling of your throat or tongue

If you have an allergic reaction, call your doctor or local poison control center right away. If your symptoms are severe, call your nearest emergency room. Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal (cause death).

Warnings for people with certain health conditions

For people with heart problems: If you have uncontrolled high blood pressure or heart valve problems, you should not use this drug. It can make your condition worse. If you have high blood pressure, ask your doctor if your blood pressure is under control.
For people with history of tissue scarring: If you have a history of scarred tissue in your lungs, heart, kidney, or abdomen (stomach area), you should not use this drug. It can make your condition worse.
For people with high blood pressure from pregnancy: If you’re currently pregnant and have high blood pressure from your pregnancy, you should not use this drug. It can make your condition worse.
For people with liver problems: You may not be able to process this drug well. This may increase the levels of the drug in your body and cause more side effects.

Warnings for other groups

For pregnant women: Cabergoline is a category B pregnancy drug. That means two things:

Research in animals has not shown a risk to the fetus when the mother takes the drug.
There aren’t enough studies done in humans to show if the drug poses a risk to the fetus.

Talk to your doctor if you’re pregnant or plan to become pregnant. Animal studies do not always predict the way humans would respond. Therefore, this drug should only be used in pregnancy if clearly needed.

Call your doctor right away if you become pregnant while taking this drug.

For women who are breastfeeding: It isn’t known if this drug passes into breast milk. If it does, it may cause side effects in a child who is breastfed. This drug may also keep you from making breast milk. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

For seniors: The kidneys and liver of older adults may not work as well as they used to. This can cause your body to process drugs more slowly. As a result, more of a drug stay in your body for a longer time. This raises your risk of side effects.

For children: This medication has not been studied in children. It should not be used in people younger than 18 years.

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