Cabgolin: Effective Prolactin Regulation for Hormonal Balance
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Cabgolin (cabergoline) is a potent dopamine receptor agonist specifically formulated for the management of hyperprolactinemic disorders. It offers a targeted mechanism of action, directly inhibiting prolactin secretion from the pituitary gland. This medication is indicated for both therapeutic and long-term management, providing a non-invasive alternative to surgical intervention in appropriate cases. Its extended half-life allows for convenient dosing, enhancing patient adherence and treatment consistency.
Features
- Active ingredient: Cabergoline 0.5mg per tablet
- Pharmacological class: Dopamine D2 receptor agonist
- Administration: Oral tablet formulation
- Half-life: Approximately 63–69 hours
- Bioavailability: 40–50% following oral administration
- Protein binding: 40–42%
- Metabolism: Hepatic via CYP3A4 isoenzyme
- Excretion: Primarily fecal (72%) with minor renal elimination (18–20%)
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 or elimination of galactorrhea in hyperprolactinemic individuals
- Effective tumor size reduction in prolactin-secreting pituitary adenomas
- Improved bone mineral density through restoration of normal estrogen/testosterone levels
- Convenient twice-weekly dosing regimen improves long-term compliance
Common use
Cabgolin is primarily prescribed for the treatment of hyperprolactinemia, whether idiopathic or associated with pituitary prolactinomas. It is indicated for the management of persistent galactorrhea, amenorrhea, infertility, and hypogonadism resulting from elevated prolactin levels. The medication is also utilized in the treatment of Parkinson’s disease at higher doses, though this application requires specialized neurological supervision. Off-label uses include the prevention of physiological lactation and management of certain menstrual disorders.
Dosage and direction
The initial recommended dosage is 0.25 mg twice weekly, which may be increased gradually by 0.25 mg increments at 4-week intervals based on prolactin level monitoring. Maximum therapeutic dosage typically does not exceed 1 mg twice weekly for hyperprolactinemia. Tablets should be administered orally with food to minimize gastrointestinal discomfort. Dosage titration should be performed under strict medical supervision with regular assessment of prolactin levels, clinical response, and potential adverse effects. For Parkinson’s disease management, significantly higher doses are employed under neurological guidance.
Precautions
Patients should undergo comprehensive cardiovascular evaluation before initiation and during treatment, including echocardiogram to assess valvular status. Regular monitoring of blood pressure is essential, particularly during dosage escalation. Hepatic and renal function should be assessed periodically. Patients should be cautioned about potential dizziness or syncope, especially during the initial treatment phase. Use with caution in patients with history of psychiatric disorders, as dopamine agonists may exacerbate these conditions. Pregnancy testing is recommended 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 other dopamine antagonists and in patients with history of pulmonary fibrosis. The medication is not recommended for patients with severe hepatic impairment without careful risk-benefit assessment.
Possible side effect
Common adverse reactions include nausea (25–30%), headache (15–20%), dizziness (10–15%), and fatigue (8–12%). Gastrointestinal disturbances such as constipation, dyspepsia, and abdominal pain may occur in approximately 5–10% of patients. Less frequently reported effects include orthostatic hypotension (3–5%), nasal congestion (2–4%), and hot flashes (1–3%). Serious but rare side effects include cardiac valvulopathy, pleural fibrosis, and psychiatric manifestations including impulse control disorders. Most side effects are dose-dependent and often diminish with continued therapy.
Drug interaction
Cabgolin demonstrates significant interactions with CYP3A4 inhibitors including macrolide antibiotics, antifungal agents, and protease inhibitors, which may increase cabergoline concentrations. Concomitant use with antihypertensive agents may potentiate hypotensive effects. Dopamine antagonists such as phenothiazines, butyrophenones, and metoclopramide may diminish therapeutic efficacy. Caution is advised with concomitant use of other ergot derivatives due to additive effects. Serotonin agonists and MAO inhibitors may potentially interact, though clinical significance requires further evaluation.
Missed dose
If a dose is missed, patients should take it 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. Doubling of doses is not recommended. Patients should maintain their established twice-weekly schedule without significant alteration. Healthcare providers should be consulted if multiple doses are missed to determine if dosage readjustment is necessary.
Overdose
Symptoms of overdose may include severe nausea, vomiting, hypotension, hallucinations, and psychosis. Management involves immediate gastric lavage if ingestion occurred within recent hours and administration of activated charcoal. Cardiovascular monitoring is essential, with supportive measures including IV fluids for hypotension. Dopamine antagonists may be considered for severe symptomatic cases, though this may exacerbate hyperprolactinemia. There is no specific antidote; treatment remains primarily supportive with symptomatic management.
Storage
Store at controlled room temperature between 20–25°C (68–77°F). Protect from light and moisture. Keep in original packaging until administration. Do not store in bathroom or other areas with high humidity. Keep out of reach of children and pets. Do not use beyond the expiration date printed on packaging. Proper disposal of unused medication should follow local regulations for pharmaceutical waste.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient assessment. Dosage and administration should follow prescribing physician instructions. Patients should not alter treatment regimens without medical consultation. The manufacturer and distributors assume no liability for improper use or interpretation of this information.
Reviews
Clinical studies demonstrate cabergoline’s efficacy in normalizing prolactin levels in 80–90% of patients with microprolactinomas and 70–80% with macroprolactinomas. Long-term studies show sustained efficacy with maintenance of normalized prolactin levels for up to 5 years in most patients. Patient-reported outcomes indicate significant improvement in quality of life measures, particularly regarding restoration of fertility and resolution of galactorrhea. The twice-weekly dosing regimen receives high patient satisfaction scores compared to daily alternatives. Specialist endocrinologists consistently rate cabergoline as first-line therapy for hyperprolactinemia management due to its favorable efficacy and safety profile.