Cabergoline exerts its therapeutic effects by selectively stimulating dopamine D2 receptors in the brain. Its mechanism of action includes:

1. Inhibition of Prolactin Secretion:
   • Cabergoline activates dopamine D2 receptors on lactotroph cells in the anterior pituitary gland.
   • This inhibits the synthesis and release of prolactin, a hormone responsible for milk production and reproductive function.
2. Reduction of Tumor Size:
   • In patients with prolactinomas (prolactin-secreting pituitary tumors), cabergoline reduces tumor size by inhibiting prolactin secretion and decreasing cell proliferation.
3. Dopaminergic Effects:
   • By stimulating dopamine receptors, cabergoline can improve motor symptoms in Parkinson’s disease and restless legs syndrome.

Cabergoline is primarily used for the following conditions:

1. Hyperprolactinemia:
   • Used to treat elevated prolactin levels caused by prolactinomas or idiopathic hyperprolactinemia.
2. Prolactinomas:
   • Reduces prolactin levels and shrinks pituitary tumors in patients with prolactin-secreting adenomas.
3. Infertility and Menstrual Disorders:
   • Restores normal ovulation and menstrual cycles in women with hyperprolactinemia-related infertility or amenorrhea (absence of menstruation).
4. Galactorrhea:
   • Treats abnormal milk production not associated with childbirth or nursing.
5. Off-Label Uses:
   • Parkinson’s Disease: Used as an adjunct therapy to manage motor symptoms.

Restless Legs Syndrome: Helps alleviate symptoms in some patients.

The dosage of cabergoline varies depending on the condition being treated. Always follow the prescribing physician's instructions.

Common Dosages:

• Hyperprolactinemia and Prolactinomas:
  • Initial dose: 0.25 mg twice weekly, taken orally with or without food.
  • Dose adjustments: The dose may be increased by 0.25 mg every 4 weeks based on prolactin levels and tolerability.
  • Maintenance dose: Typically 0.5–2 mg per week, divided into 1–2 doses.
• Parkinson’s Disease (Off-Label):
  • Initial dose: 0.5 mg once daily.
  • Dose adjustments: Gradually increased based on response and tolerability.

Administration Tips:

• Take the medication with food to reduce the risk of gastrointestinal side effects.
• Do not crush or chew the tablet; swallow it whole with water.
• Regular monitoring of prolactin levels and pituitary imaging (if applicable) is recommended during treatment.

Cabergoline is generally well-tolerated, but some patients may experience side effects. These can include:

Common Side Effects:

• Nausea
• Headache
• Dizziness
• Fatigue
• Constipation
• Abdominal pain

Rare but Serious Side Effects:

• Cardiac Valvulopathy: Long-term use of high doses may increase the risk of fibrotic heart valve damage.
• Psychiatric Effects: Hallucinations, confusion, or impulse control disorders (e.g., gambling addiction).
• Hypotension: Low blood pressure, especially when standing up (orthostatic hypotension).
• Pleural or Pericardial Fibrosis: Rare cases of fibrosis in the lungs or heart lining.

If any severe side effects occur, discontinue use and seek medical attention immediately.

Before using cabergoline, inform your healthcare provider if you have:

• A history of heart valve disorders or fibrosis
• Liver or kidney disease
• Psychiatric disorders
• Allergies to cabergoline or any of its components

Special Populations:

• Pregnancy: Cabergoline is generally considered safe during pregnancy if the benefits outweigh the risks. However, it should only be used under strict medical supervision.
• Breastfeeding: Cabergoline inhibits prolactin and may reduce milk production. Consult your doctor before use.
• Elderly Patients: Use with caution due to the potential for increased side effects, particularly hypotension and cardiac issues.

Cabergoline may interact with other medications, altering their effectiveness or increasing the risk of side effects. Notable interactions include:

1. Antihypertensive Medications:
   • Cabergoline may enhance the blood pressure-lowering effects of antihypertensive drugs, increasing the risk of hypotension.
2. Dopamine Antagonists:
   • Drugs like metoclopramide and antipsychotics (e.g., haloperidol) may reduce the efficacy of cabergoline.
3. Macrolide Antibiotics:
   • Drugs like erythromycin may increase cabergoline levels by inhibiting its metabolism.
4. Serotonin Agonists:
   • Concurrent use with serotonin agonists (e.g., sumatriptan) may increase the risk of serotonin syndrome.

Always inform your healthcare provider about all medications, supplements, and herbal products you are taking.

Generic Names in Pharmacy

• Cabergoline (the active ingredient in Dostinex)