Cabgolin: Advanced Dopamine Agonist for Hyperprolactinemia Management
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Cabgolin (cabergoline) is a potent, long-acting dopamine receptor agonist specifically formulated for the treatment of hyperprolactinemic disorders. It demonstrates high selectivity for D2 dopamine receptors, resulting in sustained suppression of prolactin secretion from the pituitary lactotroph cells. Its extended half-life and favorable tolerability profile make it a first-line pharmacologic option for both microprolactinomas and macroprolactinomas, as well as idiopathic hyperprolactinemia. Clinical use extends to the inhibition of physiological lactation and, in some cases, off-label management of Parkinson’s disease symptoms.
Features
- Active ingredient: Cabergoline 0.5mg per tablet
- Mechanism: Selective dopamine D2 receptor agonist
- Pharmacokinetics: Extended half-life (~63–69 hours), allowing for less frequent dosing
- Bioavailability: Approximately 40–50% following oral administration
- Metabolism: Primarily hepatic via CYP3A4 isoenzyme
- Excretion: Mainly fecal (72%), with renal elimination accounting for 18–20%
Benefits
- Effectively normalizes elevated prolactin levels, restoring gonadal function and fertility
- Reduces prolactinoma tumor size in a significant proportion of patients with pituitary adenomas
- Convenient twice-weekly dosing regimen improves patient adherence and quality of life
- Lower incidence of side effects such as nausea and hypotension compared to older ergot-derived agonists
- Provides symptomatic relief from galactorrhea, amenorrhea, and hypogonadism
- Non-teratogenic profile allows for use in women seeking pregnancy under careful supervision
Common use
Cabgolin is primarily indicated for the treatment of hyperprolactinemia, whether due to prolactin-secreting pituitary adenomas (prolactinomas) or idiopathic causes. It is employed to restore ovulation and fertility in women with anovulatory cycles secondary to hyperprolactinemia, and to ameliorate hypogonadism in affected men. Additionally, it is used for the prevention of physiological lactation postpartum when breastfeeding is not desired. Off-label applications include adjunctive treatment in Parkinson’s disease and management of certain cases of acromegaly or cyclic Cushing’s disease.
Dosage and direction
The initial dosage for hyperprolactinemia is typically 0.25 mg twice weekly, which may be increased by 0.25 mg increments at 4-week intervals based on prolactin level monitoring. The therapeutic dosage usually ranges from 0.5 mg to 2 mg per week, administered in divided doses (e.g., Monday and Thursday). Tablets should be taken orally with or without food, though administration with meals may reduce potential gastrointestinal discomfort. Dosage titration should be performed gradually to minimize adverse effects, and maintenance therapy should continue until prolactin normalization is sustained.
Precautions
Patients should be monitored for signs of cardiac valvulopathy, particularly with long-term use or higher cumulative doses. Baseline echocardiogram is recommended before initiation and periodically during treatment. Use with caution in patients with hepatic impairment, as cabergoline is extensively metabolized in the liver. Caution is advised when prescribing to patients with a history of psychiatric disorders, as dopamine agonists can exacerbate or precipitate impulse control disorders. Blood pressure should be monitored, especially during initial dose titration.
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, toxemia of pregnancy, or a history of cardiac valvular disease. Concomitant use with other medications known to cause fibrosis (e.g., pergolide) is contraindicated. Use is contraindicated in patients with pre-existing respiratory or cardiac fibrotic disorders.
Possible side effect
Common adverse reactions include nausea (27%), headache (26%), dizziness (15%), and fatigue (8%). Less frequently reported effects include constipation, abdominal pain, and nasal congestion. Serious but rare side effects include cardiac valvulopathy, pleural effusion, pulmonary fibrosis, and retroperitoneal fibrosis. Neuropsychiatric effects such as somnolence, impulse control disorders (pathological gambling, hypersexuality), and hallucinations may occur, particularly at higher doses.
Drug interaction
Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, clarithromycin) may significantly increase cabergoline plasma concentrations, necessitating dose reduction. Concomitant use with antipsychotics (e.g., phenothiazines, butyrophenones) may antagonize the prolactin-lowering effect of cabergoline. Hypotensive agents may potentiate orthostatic hypotension. Use with other dopamine antagonists should be avoided due to potential therapeutic interference.
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 that case, the missed dose should be skipped, and the regular dosing schedule resumed. Doubling of doses is not recommended. Patients should contact their healthcare provider if multiple doses are missed to discuss potential adjustments to the treatment regimen.
Overdose
Symptoms of overdose may include severe nausea, vomiting, hypotension, hallucinations, and psychosis. Management is supportive and symptomatic. Gastric lavage may be considered if ingestion was recent. Blood pressure should be monitored closely, and vasopressors may be required for severe hypotension. There is no specific antidote for cabergoline overdose.
Storage
Store at room temperature (15–30°C or 59–86°F) in a dry place, protected from light and moisture. Keep in the original blister packaging until use. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made in consultation with a qualified healthcare professional based on individual patient characteristics. Dosage and administration may vary based on clinical context. Regular monitoring and follow-up are essential during cabergoline therapy.
Reviews
Clinical studies demonstrate cabergoline’s efficacy in normalizing prolactin levels in 80–90% of patients with microprolactinomas and 70–80% of those with macroprolactinomas. Long-term studies show sustained efficacy with maintenance of normoprolactinemia in most patients. Patient-reported outcomes indicate high satisfaction with the dosing schedule and improvement in quality of life measures. Specialist reviews highlight its position as a first-line therapy for hyperprolactinemia due to its efficacy and tolerability profile compared to bromocriptine.