Dostinex (cabergoline) is a prescription medication specifically designed to address hyperprolactinemia, a condition characterized by abnormally high levels of the hormone prolactin. As a dopamine receptor agonist, it works by mimicking the action of dopamine in the brain, effectively suppressing prolactin secretion from the pituitary gland. This targeted mechanism makes it a first-line treatment for various prolactin-related disorders, offering precise hormonal control with a favorable pharmacokinetic profile. Clinical studies demonstrate its efficacy in normalizing prolactin levels, restoring reproductive function, and reducing prolactinoma tumor size when present. Its long half-life allows for convenient dosing schedules, enhancing patient compliance and treatment outcomes.

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: Primarily hepatic via hydrolysis
• Excretion: Mainly fecal (72%) with urinary elimination (18–20%)
• Pregnancy category: B (AU)/N (US) - use with caution
• Manufacturer: Originally developed by Pharmacia & Upjohn, now available as generic

Benefits

• Effectively normalizes elevated prolactin levels within 2–4 weeks of treatment initiation
• Restores ovulation and fertility in women with hyperprolactinemic amenorrhea
• Reduces galactorrhea (inappropriate lactation) in both men and women
• Shrinks prolactin-secreting pituitary adenomas (prolactinomas) with demonstrated efficacy in microadenomas and macroadenomas
• Improves testosterone levels and sexual function in men with hyperprolactinemia
• Offers convenient twice-weekly dosing due to extended half-life, improving adherence

Common use

Dostinex is primarily indicated for the treatment of hyperprolactinemia disorders, including idiopathic hyperprolactinemia and prolactin-secreting adenomas. It is prescribed for the management of amenorrhea and/or galactorrhea associated with hyperprolactinemia in women who do not seek pregnancy. For women desiring conception, it effectively induces ovulation while monitoring for potential pregnancy. In men, it addresses hypogonadism and infertility secondary to elevated prolactin levels. Off-label uses include Parkinson’s disease treatment (at higher doses) and prevention of physiological lactation postpartum, though these applications require careful medical supervision.

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. The therapeutic dosage typically ranges from 0.5 mg to 2 mg per week, administered in divided doses (e.g., 1 mg twice weekly). Maximum dosage should not exceed 4.5 mg per week. Tablets should be taken orally with food to minimize gastrointestinal discomfort. Dose titration must be guided by regular assessment of prolactin levels, with adjustments made no more frequently than every 4 weeks. For postpartum lactation prevention, a single 1 mg dose is administered within the first day after delivery.

Precautions

Patients should undergo comprehensive cardiovascular evaluation before initiation, including echocardiography to rule out valvular heart disease. Regular monitoring of blood pressure is essential, particularly during dose escalation. Hepatic and renal function should be assessed periodically, with dosage adjustments necessary in impairment. Patients should be cautioned about potential drowsiness that may impair driving or operating machinery. Ophthalmologic examinations are recommended for long-term therapy to monitor for retinal changes. Women of childbearing potential must use reliable contraception during treatment unless seeking pregnancy under medical supervision.

Contraindications

Dostinex is contraindicated in patients with hypersensitivity to cabergoline or any ergot derivatives. It should not be used in individuals with uncontrolled hypertension, history of cardiac valvular disorders, or fibrotic conditions including pericarditis, pleuritis, or retroperitoneal fibrosis. Contraindications extend to patients with severe hepatic impairment (Child-Pugh C) and those taking medications with potent CYP3A4 inhibitory effects. It is not recommended for patients with psychotic disorders due to potential exacerbation of symptoms. Use is prohibited in pregnancy unless clearly necessary and under strict medical supervision.

Possible side effect

Common adverse reactions (≥5%) include nausea (27–29%), headache (26%), dizziness (15–19%), and fatigue (8–12%). Gastrointestinal disturbances such as constipation, dyspepsia, and abdominal pain occur in approximately 5–8% of patients. Orthostatic hypotension affects 4–6% of users, particularly during initial therapy. Less frequent side effects (1–4%) include hot flashes, breast pain, depression, and paresthesia. Serious but rare adverse events (<1%) include valvular heart disorders, pleural effusion, pulmonary fibrosis, and psychotic reactions. Dosage reduction or discontinuation may be necessary based on severity and persistence of side effects.

Drug interaction

Strong CYP3A4 inhibitors (ketoconazole, ritonavir, clarithromycin) significantly increase cabergoline exposure, requiring dosage reduction or avoidance. Antipsychotics (haloperidol, phenothiazines) may antagonize Dostinex’s prolactin-lowering effects. Concurrent use with antihypertensive agents may potentiate hypotensive effects. Ergot alkaloids and other dopamine agonists should be avoided due to additive effects. Macrolide antibiotics and serotonin antagonists may interact unpredictably. Always review the patient’s complete medication profile, including over-the-counter products and herbal supplements, before prescribing.

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 that case, skip the missed dose and resume the regular dosing schedule. Doubling doses to compensate for missed administration is not recommended due to the risk of excessive dopaminergic stimulation and side effects. Patients should maintain their regular twice-weekly schedule and contact their healthcare provider if multiple doses are missed or if uncertainty exists about proper dosing resumption.

Overdose

Symptoms of overdose may include severe nausea, vomiting, hypotension, syncope, hallucinations, and psychotic reactions. Management involves immediate gastric lavage if ingestion occurred within 2 hours, followed by activated charcoal administration. Cardiovascular monitoring is essential, with supportive measures including IV fluids for hypotension. Dopamine antagonists are not recommended for managing overdose due to theoretical risk of exacerbating hyperprolactinemia. There is no specific antidote; treatment remains symptomatic and supportive. Hospitalization may be required for severe cases, particularly with cardiovascular manifestations.

Storage

Store at controlled room temperature (20–25°C or 68–77°F) in the original blister packaging to protect from light and moisture. Keep tightly closed and away from excessive heat and humidity. Do not store in bathroom cabinets or near kitchen sinks where moisture levels fluctuate. Keep out of reach of children and pets. Do not use beyond the expiration date printed on packaging. Properly dispose of unused medication through take-back programs or following FDA-recommended disposal methods.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Dostinex is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to therapy may vary, and treatment decisions should be based on comprehensive medical evaluation. Always follow your healthcare provider’s instructions regarding dosage, monitoring, and duration of therapy. Report any adverse effects or concerns to your prescribing physician promptly.

Reviews

Clinical studies demonstrate Dostinex’s efficacy with 80–85% of patients achieving normalized prolactin levels within 4–8 weeks of treatment. Patient satisfaction surveys indicate high rates of symptom improvement, particularly in restoration of menstrual regularity and reduction of galactorrhea. Long-term studies (up to 4 years) show maintained efficacy with stable dosing in most patients. Medical professionals appreciate its favorable side effect profile compared to older ergot derivatives and convenient dosing schedule that enhances compliance. However, some patients report persistent nausea or dizziness requiring dose adjustment or adjunctive therapy.