Cabergoline

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Generic Name of Cabergoline - Learn More

Cabergoline

Cabergoline Precaution - What You Need to Know

Cabergoline is a dopamine agonist primarily used to treat hyperprolactinemia (high levels of prolactin in the blood) and associated disorders, such as prolactinomas. While it is generally well-tolerated, there are several important precautions to consider before using cabergoline. Patients with a history of cardiovascular disease, including heart valve disorders, should be carefully monitored, as cabergoline has been associated with the potential development of valvular heart disease, particularly with long-term or high-dose use. It should be used cautiously in patients with psychiatric disorders such as psychosis, as the medication may exacerbate these conditions. Cabergoline is contraindicated in individuals with hypersensitivity to ergot derivatives or any component of the formulation. Pregnant women should avoid using cabergoline unless prescribed by a healthcare provider, as the drug can cross the placenta and affect fetal development. Additionally, the medication can be excreted in breast milk, so it should be avoided in breastfeeding mothers unless absolutely necessary. Patients with hepatic or renal impairment should be monitored closely when using cabergoline, and dose adjustments may be required. Regular follow-up appointments should be scheduled to monitor for potential side effects, such as dizziness, nausea, or signs of heart valve problems.

Cabergoline Indication - Uses and Benefits

Cabergoline is mainly indicated for the treatment of hyperprolactinemia and its associated conditions, including prolactinomas (benign tumors of the pituitary gland that produce excessive prolactin) and conditions like galactorrhea (inappropriate milk production), amenorrhea (absence of menstruation), and infertility related to high prolactin levels. The medication works by stimulating dopamine receptors in the brain, specifically in the pituitary gland, to decrease the secretion of prolactin. Lowering prolactin levels can help alleviate symptoms such as irregular menstrual cycles and fertility issues in women, as well as decrease breast milk production in non-lactating women or men with hyperprolactinemia. Cabergoline is often preferred over other treatments, like bromocriptine, due to its lower side-effect profile and longer half-life, which allows for less frequent dosing. Cabergoline may also be used off-label in some cases to treat other conditions associated with excess prolactin or to manage symptoms of Parkinson’s disease, though its use for Parkinson’s is more common with higher doses in clinical settings.

Cabergoline Contraindications - Important Warnings

Cabergoline is contraindicated in patients with a known hypersensitivity to the drug or any of its components, particularly ergot alkaloids, as it may provoke allergic reactions such as skin rashes, itching, or more severe systemic reactions. It is also contraindicated in individuals with a history of cardiovascular disorders such as heart valve disease or fibrosis, as the medication has been linked to an increased risk of valvular heart disease, especially with long-term use. Patients with uncontrolled high blood pressure should not use cabergoline, as it may exacerbate these conditions. Additionally, cabergoline is not recommended for use during pregnancy unless the potential benefit outweighs the risk to the fetus, as there is a possibility of harm to fetal development. The drug is also contraindicated in breastfeeding women, as it can pass into breast milk, potentially affecting the infant. In patients with severe hepatic or renal impairment, caution is necessary, and the drug may be contraindicated depending on the level of dysfunction, with dosage adjustments required. For patients with psychiatric conditions like schizophrenia, the medication should be avoided or used with caution, as it may worsen these disorders.

Cabergoline Side Effects - What to Expect

Cabergoline is generally well-tolerated, but some side effects may occur. Common side effects include dizziness, nausea, and fatigue, especially when starting the medication. These effects are often mild and transient but should be monitored. Other potential side effects include headache, abdominal discomfort, constipation, and dry mouth. Some individuals may experience psychiatric symptoms such as mood changes, depression, or confusion, particularly at higher doses. In rare cases, cabergoline has been associated with severe cardiovascular side effects, including heart valve abnormalities, pericardial effusion (fluid around the heart), and heart failure, particularly with long-term or high-dose use. If any symptoms such as shortness of breath, chest pain, or swelling of the legs or abdomen occur, medical attention should be sought immediately. Cabergoline has also been linked to a risk of compulsive behaviors, including gambling or hypersexuality, and these symptoms should be reported to a healthcare provider. In some cases, patients may develop a tolerance to the medication, and its efficacy may decrease over time. It is important to follow up with a healthcare provider regularly to monitor for any adverse effects, especially during long-term treatment.

Cabergoline Pregnancy Category ID - Safety Information

2

Cabergoline Mode of Action - How It Works

Cabergoline exerts its therapeutic effects by selectively stimulating dopamine D2 receptors in the brain. These receptors are located in the pituitary gland, where they regulate the secretion of prolactin. By activating dopamine receptors, cabergoline inhibits prolactin production, which helps reduce elevated levels of prolactin in the bloodstream. The suppression of prolactin is beneficial for managing conditions such as hyperprolactinemia, prolactinomas, and other prolactin-related disorders. In addition to its effect on prolactin, cabergoline has a moderate affinity for other dopamine receptors in the brain, including D1 and D3 receptors, although its primary action remains in the inhibition of prolactin. This selective mechanism of action helps minimize side effects compared to other dopamine agonists. Cabergoline’s long half-life allows for less frequent dosing, providing patients with convenience and improved adherence to the treatment regimen.

Cabergoline Drug Interactions - What to Avoid

Cabergoline has several known interactions with other medications that may impact its effectiveness or increase the risk of adverse effects. When used in combination with other dopamine agonists, such as bromocriptine, there may be an increased risk of side effects, such as hypotension, dizziness, and hallucinations. Cabergoline may also interact with antipsychotic medications, as these drugs block dopamine receptors and may reduce the effectiveness of cabergoline in lowering prolactin levels. Additionally, the use of cabergoline with antihypertensive drugs may result in an additive hypotensive effect, leading to a significant drop in blood pressure, particularly when standing up (orthostatic hypotension). Alcohol can enhance the sedative effects of cabergoline, leading to increased drowsiness and dizziness, so it should be consumed cautiously. Some antifungal medications, such as ketoconazole, may inhibit the metabolism of cabergoline, increasing the risk of toxicity, so close monitoring is required when these drugs are used together. It is essential to inform a healthcare provider of all medications, including over-the-counter drugs and supplements, to ensure the safe use of cabergoline and avoid potential interactions.

Cabergoline Adult Dose - Recommended Dosage

The typical adult dose of cabergoline for the treatment of hyperprolactinemia starts at 0.25 mg twice weekly, with gradual dose increases based on patient response and tolerance. The dose may be increased by 0.25 mg every 4 weeks, up to a maximum of 1 mg twice weekly. The usual maintenance dose ranges from 0.5 mg to 1 mg twice weekly, though some patients may require lower or higher doses based on individual factors. Cabergoline is usually taken with food to reduce the likelihood of gastrointestinal side effects, such as nausea. Doses are typically administered on the same days each week, and the medication should be taken consistently to maintain steady prolactin suppression. If doses are missed, the next dose should be taken as soon as remembered, but two doses should not be taken at once. Regular follow-up appointments are necessary to monitor prolactin levels and assess for any side effects, especially cardiovascular health.

Cabergoline Child Dose - Dosage for Children

Cabergoline is not generally recommended for use in children under the age of 16, as its safety and efficacy in pediatric populations have not been fully established. In certain cases, it may be prescribed off-label to treat specific conditions, such as hyperprolactinemia or prolactinomas, but this should only be done under the supervision of a healthcare provider with experience in pediatric endocrinology. Dosing in children would likely require careful adjustment based on the individual’s response and the severity of the condition being treated. For adolescents, the starting dose is typically lower, and careful monitoring is essential to ensure proper titration and minimize the risk of side effects. The medication should be used cautiously, and frequent follow-ups with healthcare professionals are necessary to monitor growth, development, and any potential side effects.

Cabergoline Renal Dose - Dosage for Kidney Conditions

For patients with renal impairment, dose adjustments may be necessary, although cabergoline’s minimal systemic absorption generally reduces the risk of renal-related complications. There is limited data on the precise pharmacokinetics of cabergoline in patients with renal impairment, but caution is advised. In patients with moderate to severe renal dysfunction (creatinine clearance <30 mL/min), the dose should be carefully adjusted, and more frequent monitoring of renal function and prolactin levels is recommended. In cases of severe renal impairment, cabergoline should be used with particular caution, and the potential for side effects, such as fluid retention or cardiac issues, should be closely monitored. If renal function deteriorates, discontinuation or dose adjustment may be required, but these decisions should be made in consultation with a healthcare provider.