Cabergoline acts as an agonist at D2 dopamine receptors and inhibits prolactin secretion. It is indicated for the treatment of Parkinson's disease and conditions associated with elevated prolactin levels. What guidelines should be followed when administering Cabergoline?
1. What is Cabergoline?
What is Cabergoline? Cabergoline is a Dopaminergic Ergoline derivative with strong and prolonged agonist activity on D2 dopamine receptors. It improves motor deficiency in Parkinson's disease animal models, with a daily oral dose of 1-2.5 mg/kg in mice and a subcutaneous dose of 0.5-1 mg/kg in monkeys.
In humans, a single oral dose of 0.3-2.5 mg of Cabergoline is associated with significantly reducing serum prolactin levels. This effect is dose-dependent, with both the degree and duration varying according to the dose. The pharmacodynamic effect of Cabergoline is not associated with blood pressure reduction, which usually occurs within the first 6 hours after taking the medication and is dose-dependent.
Cabergoline is available in tablet strengths of 1 mg and 2 mg.
2. What are the effects of Cabergoline?
Cabergoline is indicated for the following conditions:
- Parkinson's disease: As a second-line monotherapy or in combination with Levodopa/dopamine decarboxylase inhibitors.
- Hyperprolactinemia: Caused by pituitary tumors or idiopathic origins.
Cabergoline is contraindicated in patients with:
- An allergy to Cabergoline, Ergot derivatives, or any drug components;
- A history of heart valve disease, pulmonary fibrosis, or pericardial disease;
- Uncontrolled hypertension.
3. Dosage and administration of Cabergoline
Dosage of Cabergoline for adults and elderly patients:
- Parkinson's Disease Treatment: The starting dose is 1 mg, taken once daily. Depending on the patient’s response, the dose can be increased by 0.5-1 mg/day weekly or biweekly until the optimal dose is reached. The maintenance dose for Parkinson’s disease treatment is 2-6 mg/day.
- Hyperprolactinemia Treatment: The initial dose is 0.25 mg twice a week, gradually increasing by 0.25 mg until the dose reaches 1 mg twice a week, depending on prolactin levels. Consider reducing the Cabergoline dose once serum prolactin levels have normalized for at least 24 months, and when the tumor size has decreased by more than 50%.
- In certain patients, a reduction in the dose of Cabergoline may be necessary in cases of severe liver impairment.
How to use Cabergoline:
- Patients should take Cabergoline with meals.
- Note that treatment with Cabergoline should begin at a low dose, with gradual increases every 1 to 2 weeks, until the optimal therapeutic effect is achieved.
4. Side effects of Cabergoline
Very common side effects of Cabergoline include:
- Valve abnormalities, inflammation and/or pericardial effusion;
- Peripheral edema.
Other common side effects of Cabergoline include:
- Angina;
- Headache, dizziness, and movement disorders;
- Drowsiness and sleep disturbances;
- Hallucinations;
- Increased libido;
- Confusion;
- Orthostatic hypotension;
- Constipation, dyspepsia, gastritis, vomiting;
- Weakness;
- Decreased levels of hemoglobin, hematocrit, and red blood cell count.
Uncommon and rare side effects of Cabergoline include:
- Pleural effusion, pulmonary fibrosis (pulmonary pleura fibrosis);
- Allergic reactions;
- Delusions or psychiatric disorders;
- Neuropathic muscle pain;
- Edema, fatigue;
- Abnormal liver function tests;
- Rash;
- Respiratory failure, pleuritis;
- Hyperkinesia;
- Sudden sleep episodes, fainting, or tremors;
- Aggression, excitability;
- Alopecia;
- Muscle cramps;
- Elevated creatine phosphokinase levels.
5. Interactions of Cabergoline
Cabergoline should not be used together with drugs that have dopamine antagonistic properties (e.g., Phenothiazines, Butyrophenones, Thioxanthenes, Metoclopramide), as they may reduce its effectiveness.
Similarly, like other ergot derivatives, Cabergoline should not be taken with macrolide antibiotics (e.g., erythromycin) because they may increase its systemic bioavailability.
Alcohol may increase the side effects of Cabergoline on the nervous system, such as dizziness, drowsiness, and difficulty concentrating. Therefore, patients should avoid or limit alcohol consumption during treatment.
6. Precautions when using Cabergoline
Caution should be exercised when prescribing Cabergoline to patients with a history of severe cardiovascular diseases, Raynaud's syndrome, peptic ulcer, gastrointestinal bleeding, or severe psychiatric disorders (especially psychosis).
Patients with genetic disorders, including galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption, should not use Cabergoline.
Patients with severe hepatic impairment should use Cabergoline at a reduced dose. Studies comparing normal volunteers with patients having hepatic impairment have shown an increased AUC in those with severe impairment (Child-Pugh C), even after a single 1mg dose.
Postural hypotension may occur after taking Cabergoline, particularly during the initial phase of treatment. Caution is advised when combining Cabergoline with other antihypertensive drugs.
Fibrotic and serosal inflammation, including pleuritis, pleural effusion, pleural fibrosis, pulmonary fibrosis, pericarditis, pericardial effusion, valvular heart disease (involving one or more valves, such as the aortic, mitral, and tricuspid valves), or retroperitoneal fibrosis, has been observed in patients using ergot derivatives with serotonin 5-HT2B receptor agonists, including Cabergoline. In some cases, symptoms or manifestations of valvular heart disease improve upon discontinuation of Cabergoline.
Before initiating long-term treatment with Cabergoline, all patients should undergo a cardiovascular evaluation, including echocardiography, to detect any underlying asymptomatic valvular heart disease.
Fibrotic disorders associated with Cabergoline may develop insidiously, so patients should be regularly monitored for early signs of progressive fibrosis, including:
- Pleural and pulmonary conditions: shortness of breath, persistent cough, or chest pain;
- Renal failure, urinary tract or abdominal vascular obstruction, with symptoms such as back pain, leg swelling, or the appearance of abdominal masses, which may indicate retroperitoneal fibrosis.
Cabergoline has been associated with drowsiness and sudden sleep episodes in patients with Parkinson's disease.
Patients receiving Cabergoline should be closely monitored for the development of impulse control disorders, particularly for behavioral symptoms such as gambling addiction, increased sexual desire, hypersexuality, compulsive spending or shopping, and overeating, as these may occur in patients treated with dopamine agonists. Dose reduction of Cabergoline should be considered if these symptoms develop.
There is insufficient data on the safety of Cabergoline use during pregnancy. While animal studies have not shown teratogenic effects, Cabergoline may reduce fertility or pose a risk of fetal toxicity. Therefore, if indicated, Cabergoline should only be used during pregnancy, with a thorough benefit-risk assessment.
Cabergoline and its metabolites may be excreted in breast milk in rodents. Although no studies have been conducted on human breast milk excretion, Cabergoline may inhibit or suppress lactation. Therefore, women receiving Cabergoline treatment should refrain from breastfeeding.
Cabergoline may cause side effects such as drowsiness and sudden sleep episodes in Parkinson's disease patients. Therefore, patients treated with Cabergoline who experience drowsiness should exercise caution when driving or operating machinery.
In summary, Cabergoline is a dopamine agonist ergoline derivative with a potent and prolonged effect on D2 dopamine receptors. It is indicated for the treatment of Parkinson's disease and conditions associated with hyperprolactinemia.
Reference source: drugs.com
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