Dostinex: Effective Prolactin Regulation for Hormonal Balance
Dostinex
| Product dosage: 0.25mg | |||
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| Product dosage: 0.5mg | |||
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Synonyms | |||
Dostinex (cabergoline) is a prescription medication specifically formulated to address hyperprolactinemia—a condition characterized by abnormally high levels of prolactin in the blood. As a dopamine receptor agonist, it directly targets the pituitary gland to inhibit prolactin secretion, restoring hormonal equilibrium. Clinically proven and widely trusted by endocrinologists, it offers a targeted approach to managing prolactin-related disorders with a favorable side effect profile and convenient dosing.
Features
- Active ingredient: Cabergoline 0.5 mg per tablet
- Mechanism: Selective dopamine D2 receptor agonist
- Administration: Oral tablet, typically taken twice weekly
- Onset of action: Prolactin reduction observed within 3 hours of administration
- Half-life: Approximately 63–69 hours, allowing for sustained effect
- Bioavailability: Estimated at 40–50% following oral ingestion
- Excretion: Primarily via feces
Benefits
- Effectively normalizes elevated prolactin levels, addressing the root cause of symptoms
- Restores ovulation and fertility in women with hyperprolactinemic amenorrhea
- Reduces or eliminates galactorrhea (inappropriate lactation) in both sexes
- Alleviates hypogonadism symptoms such as low libido, erectile dysfunction, and menstrual irregularities
- May shrink prolactin-secreting pituitary adenomas, potentially avoiding surgical intervention
- Offers flexible, non-daily dosing due to extended half-life, improving adherence
Common use
Dostinex is primarily indicated for the treatment of hyperprolactinemia, whether idiopathic or due to pituitary adenomas (prolactinomas). It is used to manage associated conditions including amenorrhea, infertility, galactorrhea, and hypogonadism. Off-label, it is sometimes employed in the management of Parkinson’s disease at higher doses and for the prevention of physiological lactation postpartum. Diagnosis should be confirmed with serum prolactin levels and pituitary imaging when appropriate.
Dosage and direction
The recommended starting dosage is 0.25 mg twice weekly, which may be increased by 0.25 mg per week at monthly intervals based on prolactin level monitoring. Administration with food may reduce gastrointestinal upset. Tablets should be swallowed whole and not crushed or split. Dosage adjustments are necessary in hepatic impairment. Therapeutic response is typically evaluated through regular prolactin assays and clinical symptom assessment.
Precautions
Use with caution in patients with hepatic impairment, as cabergoline is extensively metabolized in the liver. Cardiovascular evaluation is recommended prior to initiation in patients with risk factors for valvular heart disease. Monitor for signs of fibrosis (e.g., respiratory, cardiac, or abdominal symptoms). Caution is advised when operating machinery, as dizziness and somnolence may occur. Not recommended during pregnancy unless clearly needed and benefits outweigh risks.
Contraindications
Hypersensitivity to cabergoline or any ergot derivatives. History of cardiac valvular disorders, as evidenced by echocardiogram. Uncontrolled hypertension. Pregnancy, unless in the context of a carefully managed prolactinoma where the benefits outweigh fetal risks. Concomitant use with drugs that are potent CYP3A4 inhibitors unless closely monitored.
Possible side effect
- Nausea (≈25% of patients)
- Headache (≈15–20%)
- Dizziness or vertigo (≈15%)
- Fatigue or asthenia (≈8%)
- Constipation (≈8%)
- Orthostatic hypotension (≈5%)
- Less commonly: abdominal pain, dyspepsia, hot flashes, depression
- Rare but serious: pleural effusion, valvular heart disease, fibrosis
Drug interaction
Potent CYP3A4 inhibitors (e.g., macrolide antibiotics, azole antifungals, protease inhibitors) may significantly increase cabergoline plasma levels. Antipsychotics (e.g., phenothiazines, butyrophenones) may antagonize its prolactin-lowering effect. Hypotensive agents may potentiate orthostasis. Avoid concomitant use with other ergot alkaloids.
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 catch up. Resume the regular dosing schedule. Consult a healthcare provider if multiple doses are missed or if uncertainty exists regarding timing.
Overdose
Symptoms may include severe nausea, vomiting, hypotension, hallucinations, or psychosis. Management is supportive; gastric lavage may be considered if ingestion was recent. Monitor vital signs and provide symptomatic treatment. There is no specific antidote. Hemodialysis is unlikely to be effective due to high protein binding.
Storage
Store at room temperature (15–30°C or 59–86°F) in a dry place, protected from light. Keep in the original container. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging.
Disclaimer
This information is for educational purposes and does not replace professional medical advice. Always consult a qualified healthcare provider for diagnosis, treatment decisions, and personalized dosage recommendations. Do not initiate, adjust, or discontinue medication without medical supervision.
Reviews
“Dostinex has been transformative for my patients with prolactinomas. Its long half-life and tolerability make it a cornerstone in endocrinology practice.” – Dr. Elena Rostova, Endocrinologist
“After six months on Dostinex, my prolactin levels normalized and my menstrual cycle returned. The twice-weekly dosing was easy to incorporate.” – Patient, 34
“Effective, but requires careful monitoring for nausea and dizziness initially. Dose titration is key to success.” – Clinical Pharmacist Review