Cabgolin: Advanced Dopamine Agonist for Hyperprolactinemia Management
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Cabgolin, containing the active ingredient cabergoline, is a highly selective dopamine receptor agonist specifically engineered for the treatment of hyperprolactinemic disorders. It offers a sophisticated therapeutic approach by directly inhibiting prolactin secretion from the pituitary gland. With its long half-life and favorable tolerability profile, Cabgolin provides sustained hormonal control, making it a cornerstone in endocrinological and reproductive medicine practice for both men and women.
Features
- Active ingredient: Cabergoline 0.5mg per tablet
- Selective D2 dopamine receptor agonist with high affinity
- Extended half-life allowing for less frequent dosing
- High oral bioavailability and extensive tissue distribution
- Metabolized primarily via hydrolysis in the liver
- Excretion predominantly through fecal route
Benefits
- Effectively reduces elevated prolactin levels to within normal physiological range
- Restores gonadal function and fertility in both male and female patients
- Promotes regression of prolactin-secreting pituitary adenomas
- Alleviates symptoms associated with hyperprolactinemia including galactorrhea and menstrual irregularities
- Improves bone mineral density by normalizing estrogen/testosterone levels
- Enhances quality of life through symptom control and psychological well-being
Common use
Cabgolin is primarily indicated for the treatment of hyperprolactinemia, whether idiopathic or due to pituitary adenomas. It is prescribed for the management of associated conditions including amenorrhea, oligomenorrhea, galactorrhea, and infertility. In male patients, it addresses hypogonadism and sexual dysfunction related to elevated prolactin levels. Off-label uses include Parkinson’s disease therapy and prevention of physiological lactation.
Dosage and direction
The initial recommended dosage is 0.25mg twice weekly, which may be increased gradually by 0.25mg per week at monthly intervals until optimal therapeutic response is achieved. Administration should be taken with food to minimize gastrointestinal discomfort. Dosage titration should be based on periodic prolactin level measurements, with most patients responding to doses between 0.5mg and 2mg per week. Maximum recommended weekly dosage is 4.5mg.
Precautions
Regular monitoring of prolactin levels is essential during therapy. Cardiovascular evaluation including echocardiogram is recommended before initiation and during treatment, particularly at higher doses. Caution is advised in patients with hepatic impairment requiring dosage adjustment. Patients should be monitored for potential psychiatric effects including impulse control disorders. Abrupt discontinuation should be avoided; taper gradually under medical supervision.
Contraindications
Hypersensitivity to cabergoline or any ergot derivatives. History of cardiac valvular disorders as detected by echocardiography. Uncontrolled hypertension. Pregnancy unless clearly indicated and monitored by specialists. Concomitant use with other dopamine antagonists. Severe hepatic impairment without appropriate dosage adjustment. History of fibrotic disorders including pleural and retroperitoneal fibrosis.
Possible side effect
Common adverse reactions include nausea (25-30%), headache (15-20%), dizziness (10-15%), and fatigue (5-10%). Less frequently observed effects comprise orthostatic hypotension, constipation, and abdominal discomfort. Rare but serious side effects include cardiac valvulopathy, pleural effusion, and pulmonary fibrosis. Psychiatric manifestations may include impulse control disorders, depression, or hallucinations in susceptible individuals.
Drug interaction
Concomitant use with antipsychotics (phenothiazines, butyrophenones) may antagonize prolactin-lowering effects. Macrolide antibiotics may increase cabergoline concentrations. Hypotensive agents may potentiate orthostatic hypotension. Strong CYP3A4 inhibitors (ketoconazole, ritonavir) may significantly increase cabergoline exposure. Dopamine antagonists including metoclopramide should be avoided. MAO inhibitors may enhance hypertensive 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. Do not double the dose to make up for the missed administration. Maintain the regular dosing schedule thereafter. If multiple doses are missed, consult healthcare provider for dosage re-titration to avoid recurrence of hyperprolactinemic symptoms.
Overdose
Symptoms may include severe nausea, vomiting, hypotension, hallucinations, and psychotic episodes. Management involves immediate gastric lavage if ingestion occurred within recent hours, followed by activated charcoal administration. Cardiovascular support including vasopressors may be required for hypotension. Symptomatic treatment should be provided with continuous monitoring of vital signs. There is no specific antidote; hemodialysis is not effective due to high protein binding.
Storage
Store at controlled room temperature between 15-30°C (59-86°F). Protect from light and moisture. Keep in original packaging until time of administration. Do not store in bathroom or near kitchen sink. Keep out of reach of children and pets. Do not use beyond the expiration date printed on packaging. Discard any tablets showing signs of deterioration.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made exclusively by qualified healthcare professionals based on individual patient assessment. Always follow the prescribed dosage and instructions provided by your physician. Report any adverse effects or concerns to your healthcare provider promptly.
Reviews
Clinical studies demonstrate Cabgolin’s efficacy in normalizing prolactin levels in 80-90% of patients with microprolactinomas and 70-80% with macroprolactinomas. Long-term follow-up studies show maintained efficacy with continued therapy. Patient satisfaction surveys indicate significant improvement in quality of life measures. Medical professionals appreciate its favorable side effect profile compared to bromocriptine. Continued research supports its position as first-line therapy for hyperprolactinemia management.