Cabgolin: Effective Dopamine Agonist for Hyperprolactinemia Management
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Cabgolin (cabergoline) is a potent, long-acting dopamine receptor agonist specifically indicated for the treatment of hyperprolactinemic disorders. With its high affinity for D2 dopamine receptors, it effectively suppresses pathological prolactin secretion from the pituitary lactotroph cells. The medication offers superior tolerability and a convenient twice-weekly dosing regimen, making it a first-line pharmacological intervention for prolactinomas and idiopathic hyperprolactinemia. Its selective action and extended half-life provide sustained prolactin normalization with minimal side effects compared to older ergot-derived agonists.
Features
- Active ingredient: Cabergoline 0.5 mg per tablet
- Pharmacological class: Dopamine D2 receptor agonist
- Administration: Oral tablet formulation
- Half-life: Approximately 63–69 hours
- Bioavailability: 40–50% following oral administration
- Metabolism: Hepatic via CYP3A4 isoenzyme
- Excretion: Primarily fecal (72%) with minor renal elimination
- Storage: Room temperature (15–30°C) in original packaging
Benefits
- Rapid normalization of elevated prolactin levels within 2–3 weeks of initiation
- Restoration of gonadal function and fertility in both male and female patients
- Reduction of prolactinoma size with demonstrated tumor shrinkage in macroprolactinomas
- Convenient twice-weekly dosing regimen enhances treatment adherence
- Lower incidence of nausea and vomiting compared to bromocriptine therapy
- Effective management of galactorrhea and menstrual cycle irregularities
Common use
Cabgolin is primarily prescribed for the treatment of hyperprolactinemia, whether idiopathic or due to pituitary microadenomas and macroadenomas. It is indicated for the management of associated clinical manifestations including galactorrhea, amenorrhea, infertility, and hypogonadism. The medication is also utilized off-label for Parkinson’s disease symptoms and restless legs syndrome, though these applications require careful specialist supervision. In endocrine practice, it serves as the pharmacological cornerstone for prolactin-secreting adenomas, often obviating the need for surgical intervention in appropriately selected cases.
Dosage and direction
The initial recommended dosage is 0.25 mg twice weekly, which may be increased gradually by 0.25 mg increments at monthly intervals based on prolactin level monitoring. Most patients achieve prolactin normalization with 0.5–1.0 mg administered weekly in divided doses (e.g., Monday and Thursday). Tablets should be taken with food to minimize gastrointestinal discomfort. Dosage titration should proceed cautiously, with regular assessment of prolactin levels and clinical response. Maximum recommended dosage is 4.5 mg per week, though most hyperprolactinemia cases respond to lower doses. Treatment duration is typically long-term, with periodic reevaluation of continuing necessity.
Precautions
Cardiac monitoring is advised before and during treatment due to potential valvular fibrosis risk, particularly at higher doses. Baseline echocardiogram is recommended for patients requiring prolonged therapy. Blood pressure should be monitored regularly, especially during dose escalation. Caution is warranted in patients with hepatic impairment, requiring dosage adjustment and close monitoring. Patients should be advised about potential dizziness and sedation, particularly when initiating therapy or increasing dosage. Regular ophthalmological examinations are recommended for patients on long-term therapy to monitor for retinal changes. Pregnancy testing should be performed before initiation in women of childbearing potential.
Contraindications
Cabgolin is contraindicated in patients with hypersensitivity to ergot derivatives or any component of the formulation. It should not be used in patients with uncontrolled hypertension, history of cardiac valvular disorders, or pericardial/fibrotic conditions. Contraindications include concomitant use with medications that may cause hypotension. Patients with severe hepatic impairment (Child-Pugh Class C) should not receive cabergoline therapy. The medication is contraindicated in patients with a history of pulmonary fibrosis or retroperitoneal fibrosis. Concomitant administration with potent CYP3A4 inhibitors is contraindicated due to increased cabergoline exposure.
Possible side effect
Common adverse reactions (≥5%) include nausea (27%), headache (26%), dizziness (15%), and fatigue (8%). Less frequent side effects comprise constipation (5%), abdominal pain (4%), and dyspepsia (3%). Serious but rare adverse effects include cardiac valvulopathy (particularly with higher cumulative doses), pleural effusion, and pulmonary fibrosis. Postural hypotension occurs in approximately 4% of patients, typically during initial therapy. Psychiatric effects including impulse control disorders (pathological gambling, hypersexuality) have been reported in approximately 3% of patients. Transient asymptomatic increases in liver enzymes may occur in 2% of cases.
Drug interaction
Potent CYP3A4 inhibitors (ketoconazole, ritonavir, clarithromycin) significantly increase cabergoline plasma concentrations, requiring dosage reduction or avoidance. Antipsychotics (phenothiazines, butyrophenones) may antagonize the prolactin-lowering effect of cabergoline. Concomitant use with antihypertensive agents may potentiate hypotensive effects. Macrolide antibiotics and protease inhibitors may increase cabergoline exposure. Dopamine antagonists including metoclopramide and domperidone may diminish therapeutic efficacy. Serotonin agonists (triptans) used concomitantly may increase risk of serotonin syndrome. MAO inhibitors may potentiate hypotensive effects.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In such cases, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Given the long half-life of cabergoline, occasional missed doses are unlikely to significantly affect prolactin control, though consistent adherence is important for optimal therapeutic outcomes. If multiple doses are missed, consultation with the prescribing physician is recommended before resuming therapy.
Overdose
Symptoms of overdose may include severe nausea, vomiting, hypotension, syncope, and hallucinations. Management involves supportive care including gastric lavage if ingestion occurred within recent hours. Blood pressure should be monitored closely with intravenous fluids and vasopressors if significant hypotension occurs. Symptomatic treatment for nausea and vomiting may be indicated. There is no specific antidote for cabergoline overdose. Hemodialysis is unlikely to be effective due to high protein binding and extensive tissue distribution. Cardiac monitoring is recommended in cases of significant overdose, particularly for arrhythmias.
Storage
Store at room temperature between 15–30°C (59–86°F) in the original container to protect from light and moisture. Keep tightly closed and out of reach of children. Do not transfer tablets to other containers as they are sensitive to moisture. Do not use if the blister pack is damaged or tablets show signs of deterioration. Protect from excessive heat and humidity. Properly discard any unused medication after the expiration date printed on the packaging. Do not flush medications down the toilet or pour into drains unless instructed to do so.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient characteristics. Dosage and administration should be determined by a physician familiar with the patient’s medical history. The prescribing information provided here may not include all possible uses, directions, precautions, or interactions. Patients should consult their healthcare provider for complete information about their medication. Never discontinue or change dosage without medical supervision.
Reviews
Clinical studies demonstrate cabergoline’s efficacy with 80–90% of patients achieving normal prolactin levels within 4 weeks of treatment. Long-term studies show maintained efficacy in 85% of patients at 2-year follow-up. Patient satisfaction surveys indicate preference over bromocriptine due to reduced side effects and convenient dosing. Meta-analyses confirm superior tolerability profile with discontinuation rates of only 3% compared to 12% with bromocriptine. Endocrine specialists report excellent response in microprolactinomas with 95% success rate in restoring menses and fertility. Macroadenoma patients show significant tumor volume reduction (30–50%) in 70% of cases within 6–12 months of therapy.