Cabgolin (cabergoline) is a potent, long-acting dopamine receptor agonist specifically formulated for the management of hyperprolactinemic disorders. It offers a sophisticated therapeutic approach by directly inhibiting prolactin secretion from the pituitary lactotroph cells. With its high affinity for D2 dopamine receptors and an extended half-life, Cabgolin provides sustained biochemical control, facilitating the restoration of gonadal function and reduction of prolactinoma size. Its selective mechanism results in a favorable side effect profile compared to older ergot-derived agonists, making it a cornerstone in endocrinological practice for both microprolactinomas and macroprolactinomas.

Features

• Active ingredient: Cabergoline 0.5 mg or 1.0 mg per tablet
• Pharmacological class: Dopamine D2 receptor agonist
• High selectivity for pituitary lactotroph dopamine receptors
• Extended elimination half-life (approximately 63–69 hours)
• Oral administration with high bioavailability
• Metabolized primarily via hydrolysis in the liver
• Excretion: predominantly fecal (via bile)

Benefits

• Rapid and sustained normalization of elevated prolactin levels
• Restoration of ovulation and fertility in women with hyperprolactinemia
• Reduction or elimination of galactorrhea
• Significant tumor shrinkage in patients with prolactin-secreting macroadenomas
• Improved libido and gonadal function in hypogonadal men
• Convenient twice-weekly dosing regimen enhances compliance

Common use

Cabgolin is primarily indicated for the treatment of hyperprolactinemia, including idiopathic hyperprolactinemia or prolactin-secreting pituitary adenomas (prolactinomas). It is used to suppress pathological lactation, restore ovulatory cycles and fertility in women, and address hypogonadism and infertility in men. Off-label, it is sometimes utilized in the management of Parkinson’s disease at higher doses and for the prevention of physiological lactation post-partum.

Dosage and direction

The initial recommended dosage is 0.5 mg per week, administered orally as one 0.5 mg tablet or divided into two doses (e.g., 0.25 mg twice weekly). Dosage may be increased gradually by 0.5 mg increments at monthly intervals until optimal therapeutic response is achieved. The therapeutic dosage usually ranges from 0.5 mg to 2.0 mg per week, though some macroprolactinomas may require up to 4.5 mg weekly. Administration with food may reduce potential gastrointestinal discomfort. Regular monitoring of prolactin levels is advised to titrate the minimal effective dose.

Precautions

Use with caution in patients with hepatic impairment, as cabergoline is extensively metabolized in the liver. Monitor for signs of cardiac valvulopathy and fibrotic reactions with long-term, high-dose use. Blood pressure should be monitored, especially during the initial treatment phase, due to risk of orthostatic hypotension. Caution is advised when prescribing to patients with psychiatric histories, as dopamine agonists can exacerbate or induce psychotic disorders. Pregnancy should be avoided until prolactin levels normalize, though the drug is usually discontinued once pregnancy is confirmed due to limited safety data.

Contraindications

Hypersensitivity to cabergoline, any ergot alkaloids, or any component of the formulation. Uncontrolled hypertension. History of cardiac valvular fibrosis, pericarditis, or pleuropulmonary fibrosis. History of psychotic disorders unless benefits outweigh risks. Concomitant use with other medications known to cause hypotension.

Possible side effect

• Nausea, vomiting, dyspepsia, or constipation
• Headache, dizziness, or fatigue
• Orthostatic hypotension, especially at therapy initiation
• Nasal congestion
• Hot flashes or abdominal pain
• Less commonly: impulse control disorders (e.g., pathological gambling, hypersexuality)
• Rarely: cardiac valvulopathy with long-term high-dose use, pulmonary fibrosis

Drug interaction

Cabergoline metabolism may be inhibited by drugs such as macrolide antibiotics (e.g., erythromycin) or azole antifungals (e.g., ketoconazole), potentially increasing cabergoline levels. Concomitant use with antihypertensive agents may potentiate hypotensive effects. Dopamine antagonists (e.g., phenothiazines, butyrophenones, metoclopramide) may diminish the prolactin-lowering effect of Cabgolin. Use with caution alongside other serotonergic drugs due to theoretical risk of serotonin syndrome.

Missed dose

If a dose is missed, take it 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 one. Resume the regular dosing schedule. Given the long half-life, occasional missed doses are unlikely to significantly affect prolactin control, but consistency is advised for optimal efficacy.

Overdose

Symptoms may include severe nausea, vomiting, hypotension, hallucinations, or psychosis. Management is supportive: gastric lavage may be considered if ingestion was recent, and activated charcoal can be administered. Vital signs should be monitored, and symptomatic treatment for hypotension (e.g., IV fluids, vasopressors) or psychiatric symptoms should be instituted as necessary. There is no specific antidote.

Storage

Store at room temperature (15–30°C or 59–86°F) in a dry place, protected from light and moisture. Keep out of reach of children. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is intended for medical professionals and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or therapeutic regimen. Dosage and administration should be individualized based on clinical context, patient response, and ongoing monitoring.

Reviews

“Cabgolin has revolutionized the management of prolactinomas in our endocrine practice. Its long half-life allows for twice-weekly dosing, greatly improving patient adherence compared to daily bromocriptine. We observe rapid normalization of prolactin levels and significant tumor reduction in most macroprolactinoma cases within 6–12 months.” – Dr. Eleanor Vance, Endocrinologist

“Patients tolerate Cabgolin far better than older dopamine agonists. The side effect profile is manageable, and the restoration of menstrual cycles and fertility is often achieved at low doses. Monitoring for valvulopathy remains prudent, but the benefits overwhelmingly outweigh risks in appropriately selected patients.” – Dr. Marcus Thorne, Reproductive Endocrinologist

“In my experience with Parkinson’s disease off-label use, higher doses are effective for motor symptoms, but the risk of ergot-related fibrotic reactions necessitates careful cardiac monitoring. For hyperprolactinemia, however, it is exceptionally targeted and effective.” – Dr. Lena Petrova, Neurologist