Cabgolin: Effective Prolactin Regulation for Hormonal Balance
Cabgolin
| Product dosage: 0.5mg | |||
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Cabgolin (cabergoline) is a potent dopamine receptor agonist specifically formulated for the management of hyperprolactinemic disorders. It directly inhibits prolactin secretion from the anterior pituitary gland, offering a targeted therapeutic approach for conditions characterized by elevated prolactin levels. With its long half-life and selective mechanism of action, Cabgolin provides sustained biochemical control and symptomatic relief, making it a cornerstone in endocrinological and neurological therapeutics for appropriate patient populations.
Features
- Active ingredient: Cabergoline 0.5 mg per tablet
- Pharmacological class: Dopamine D2 receptor agonist
- High selectivity for pituitary lactotroph dopamine receptors
- Extended half-life (63–69 hours) allowing for less frequent dosing
- Rapid absorption with peak plasma concentrations within 2–3 hours
- Extensive liver metabolism primarily via CYP3A4
- Excretion primarily through feces (72%) with minor renal elimination
Benefits
- Normalizes elevated prolactin levels through targeted dopamine receptor activation
- Restores gonadal function and fertility in hyperprolactinemic patients
- Reduces prolactinoma tumor size with sustained therapy
- Alleviates galactorrhea and associated symptoms
- Improves libido and sexual function in hypogonadal states
- Offers convenient twice-weekly dosing regimen for improved compliance
Common use
Cabgolin is primarily indicated for the treatment of hyperprolactinemia, including idiopathic hyperprolactinemia and prolactin-secreting adenomas (prolactinomas). It is employed in the management of associated manifestations such as galactorrhea, amenorrhea, infertility, and hypogonadism in both male and female patients. Off-label uses include Parkinson’s disease therapy (though not first-line) and prevention of physiological lactation.
Dosage and direction
Initiate treatment at 0.25 mg twice weekly, preferably with meals to minimize gastrointestinal discomfort. Titrate gradually by 0.25 mg increments at 4-week intervals based on prolactin level monitoring. Maintenance doses typically range from 0.5–2 mg weekly, divided into two administrations. Maximum recommended dose is 4.5 mg weekly for hyperprolactinemia. Administer tablets orally with water; do not crush or chew.
Precautions
Monitor cardiac function regularly, particularly echocardiograms for valvular fibrosis. Assess prolactin levels monthly during dose titration and quarterly during maintenance. Exercise caution in patients with hepatic impairment due to extensive hepatic metabolism. Monitor for signs of impulse control disorders. Use cautiously in patients with psychiatric history. Pregnancy testing recommended before initiation in women of childbearing potential.
Contraindications
Hypersensitivity to ergot derivatives or any component of the formulation. Uncontrolled hypertension. History of cardiac valvular disorders as detected by echocardiography. History of pericarditis, pleuropulmonary fibrosis, or retroperitoneal fibrosis. Concomitant use with potent CYP3A4 inhibitors. Severe hepatic impairment (Child-Pugh C).
Possible side effect
- Nausea (25–30%)
- Headache (15–20%)
- Dizziness (10–15%)
- Constipation (8–10%)
- Fatigue (5–8%)
- Orthostatic hypotension (5–7%)
- Nasal congestion (3–5%)
- Cardiac valvular regurgitation (dose-dependent)
- Impulse control disorders (pathological gambling, hypersexuality)
- Pulmonary fibrosis (rare, with long-term high doses)
Drug interaction
Potent CYP3A4 inhibitors (ketoconazole, ritonavir) significantly increase cabergoline exposure. Antipsychotics (especially D2 antagonists) may antagonize therapeutic effects. Hypotensive agents may potentiate orthostatic effects. Ergot derivatives may increase risk of fibrosis. Macrolide antibiotics may moderately increase concentrations. Serotonin agonists may theoretically increase risk of serotonin syndrome.
Missed dose
Take the missed dose as soon as remembered unless it is nearly time for the next scheduled dose. Do not double the dose to make up for a missed administration. Maintain regular twice-weekly schedule. Contact healthcare provider if multiple doses are missed for dosage re-titration guidance.
Overdose
Symptoms may include severe nausea, vomiting, hypotension, hallucinations, and psychosis. Management involves gastric lavage if presented early, activated charcoal, and vigorous supportive care including blood pressure support with intravenous fluids and vasopressors if needed. There is no specific antidote; hemodialysis is not effective due to high protein binding.
Storage
Store at controlled room temperature (20–25°C/68–77°F). Protect from light and moisture. Keep in original container with tight closure. Keep out of reach of children. Do not use after expiration date printed on packaging. Do not transfer to alternative containers as this may compromise stability.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Treatment decisions must be made by qualified healthcare professionals based on individual patient characteristics. Always follow prescribed dosage and monitoring recommendations. Report any adverse effects to your healthcare provider promptly.
Reviews
Clinical studies demonstrate 80–90% normalization of prolactin levels with cabergoline therapy. Long-term data shows sustained efficacy with 70–80% of microprolactinomas showing significant size reduction. Patient-reported outcomes indicate improved quality of life measures particularly in restoration of menstrual function and fertility. Cardiology monitoring studies indicate valvular changes occur primarily at doses exceeding 3 mg weekly for Parkinson’s disease, with hyperprolactinemia doses generally showing favorable safety profile.