Related Subjects:
| Prolactin
| Prolactinoma
⚠️ Key Safety Warning: Cabergoline is associated with fibrotic reactions — particularly cardiac valvulopathy, pleural, pericardial, and retroperitoneal fibrosis.
💡 Monitoring: Baseline and periodic echocardiogram, chest X-ray, ESR, U&Es are essential for long-term use.
Always 🔗 check the BNF entry for up-to-date prescribing advice.
🧠 About
- Cabergoline is a potent, long-acting ergot-derived dopamine D₂ receptor agonist.
- Used in the treatment of hyperprolactinaemia (prolactinoma) and as adjunct therapy in Parkinson’s disease.
- Inhibits prolactin release from the anterior pituitary lactotroph cells, suppressing lactation and normalising menstrual cycles.
- Compared with bromocriptine, cabergoline has greater selectivity, longer half-life, and fewer gastrointestinal effects.
⚙️ Mode of Action
- Dopamine D₂ receptor agonist: mimics dopamine activity in the hypothalamus and pituitary.
- Suppresses prolactin secretion by inhibiting adenylate cyclase activity and reducing cAMP in lactotrophs.
- In Parkinson’s disease, stimulates striatal dopamine receptors to enhance dopaminergic transmission, improving motor symptoms.
- Ergot-derived structure explains its association with fibrotic complications (valvular and serosal).
💊 Indications & Typical Doses
- Parkinson’s Disease:
- Start with 1 mg once daily, increasing by 500 mcg/week until symptom control (max 3 mg/day).
- Always introduce gradually to reduce nausea and hypotension.
- Prolactinoma / Hyperprolactinaemia:
- 500 mcg once per week, titrated up to 2 mg/week in divided doses as required.
- Postpartum Lactation Suppression:
- To prevent lactation: 1 mg single dose on day 1 postpartum.
- To suppress established lactation: 250 mcg twice daily for 2 days.
🧪 Pharmacology
- Class: Ergot-derived dopamine D₂ agonist.
- Half-life: ~65 hours (allows once or twice weekly dosing).
- Metabolism: hepatic (CYP3A4); excreted mainly in bile.
- Onset: Prolactin suppression within 3 hours; effect lasts 7–14 days.
🤝 Interactions
- Antipsychotics (especially typical agents) antagonise dopamine effects and reduce efficacy.
- Antihypertensives — additive hypotensive effect; monitor closely.
- Macrolide antibiotics (e.g., erythromycin) inhibit CYP3A4 and can raise cabergoline levels.
- See BNF for full list of drug interactions.
⚠️ Cautions
- Abrupt cessation can precipitate a neuroleptic malignant–like syndrome (rigidity, pyrexia, autonomic instability).
- Postural hypotension — advise slow position changes and caution when driving.
- Drowsiness or sudden sleep attacks may occur — particularly in Parkinson’s therapy.
- Acute porphyria and fibrotic risk require extra vigilance.
- Impulse control disorders (hypersexuality, gambling, compulsive shopping/eating) — monitor patients and carers.
- Baseline and annual cardiac echo, CXR, ESR, U&E when used chronically.
⛔ Contraindications
- History of pulmonary, pericardial, or retroperitoneal fibrosis.
- Valvular heart disease.
- Severe hepatic impairment.
- Uncontrolled hypertension or pre-eclampsia.
- See BNF for full contraindication list.
💢 Side Effects
- Common: nausea, vomiting, headache, dizziness, constipation, postural hypotension.
- Neuropsychiatric: hallucinations, confusion, depression, sleep attacks.
- Fibrotic reactions: pericardial, pleural, retroperitoneal fibrosis; cardiac valvulopathy.
- Cardiac: chest pain, vasospasm, arrhythmia.
- Other: peripheral oedema, fatigue, Raynaud’s phenomenon, epistaxis.
🧠 Clinical Pearls
- Cabergoline is highly effective in normalising prolactin and shrinking micro- and macroprolactinomas.
- In Parkinson’s disease, consider it as adjunctive therapy in fluctuating motor symptoms or as monotherapy in younger patients.
- Always screen for cardiac valvulopathy before initiating — fibrotic risk is cumulative and dose-related.
- Patients should be advised to report dyspnoea, chest pain, flank pain, or ankle swelling promptly — signs of fibrosis.
- Monitor behaviour — dopamine agonists can unmask or worsen impulse-control disorders.
📚 References
- BNF: Cabergoline
- NICE CKS: Prolactinoma
- UpToDate: “Dopamine agonists in Parkinson’s disease and hyperprolactinaemia.”
- MHRA Drug Safety Update: “Ergot-derived dopamine agonists and fibrotic reactions.”
