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Brand Name: Caberlin
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Generic Name: Cabergoline
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Therapeutic Class: Ergot-derived dopamine D2 receptor agonist
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Dosage Form: 0.5 mg scored tablets
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Key Feature:
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Long half-life (63-69 hours) → twice-weekly dosing
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Highly selective for pituitary lactotrophs
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2. COMPOSITION
Component | Role |
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Cabergoline | Active ingredient |
Lactose monohydrate | Filler |
Leucine | Flow agent |
(Contains ergot alkaloid derivative – monitor for fibrosis risk)
3. MECHANISM OF ACTION
✔ Inhibits prolactin secretion via:
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Direct D2 receptor stimulation on lactotrophs
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Downregulation of prolactin gene expression
✔ Additional Effects: -
Mild GH suppression (useful in acromegaly adjunct therapy)
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Parkinsonian symptom relief (high doses)
4. DOSAGE & ADMINISTRATION
By Indication
Condition | Starting Dose | Maintenance Dose | Max Dose |
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Hyperprolactinemia | 0.25 mg 2x/week | 0.5-1 mg 2x/week | 4.5 mg/week |
Parkinson’s Disease | 0.5 mg daily | 2-3 mg/day in divided doses | 6 mg/day |
Key Notes:
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Take with food to reduce nausea
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Titrate slowly (increase every 4 weeks for prolactin disorders)
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For macroprolactinomas: Start low (0.25 mg/week) to avoid tumor shrinkage complications
5. INDICATIONS
✅ Hyperprolactinemic disorders:
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Prolactinomas (micro/macro)
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Idiopathic hyperprolactinemia
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Medication-induced (e.g., antipsychotics)
✅ Parkinson’s disease (2nd line)
✅ Acromegaly adjunct therapy
✅ Infertility with hyperprolactinemia
6. STORAGE CONDITIONS
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Temperature: Below 30°C
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Humidity: Keep in original blister
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Light Protection: Required
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Shelf Life: 2-3 years
7. KEY RECOMMENDATIONS
✔ Monitoring Protocol:
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Prolactin levels every 4-6 weeks until normalized
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MRI for macroprolactinomas (3-6 months post-initiation)
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Echocardiogram baseline + annually (fibrosis risk)
✔ For Antipsychotic-Induced Hyperprolactinemia:
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Coordinate with psychiatrist
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Consider alternative antipsychotics (e.g., aripiprazole) first
✔ In Pregnancy:
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Discontinue once pregnancy confirmed
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Monitor for tumor growth in macroprolactinomas
8. IMPORTANT SAFETY NOTES
Black Box Warnings
⚠ Valvular Heart Disease:
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Risk increases with cumulative dose (>3 mg/day for Parkinson’s)
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Contraindicated in fibrotic cardiac/retroperitoneal disorders
Contraindications
❌ Uncontrolled hypertension
❌ History of pericardial/pleural fibrosis
❌ Hypersensitivity to ergot derivatives
Adverse Effects
Common (≥10%) | Serious (<1%) |
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Nausea | Valvulopathy |
Headache | Psychosis |
Dizziness | Pulmonary fibrosis |
9. COMPARISON WITH OTHER DOPAMINE AGONISTS
Parameter | Cabergoline | Bromocriptine | Quinagolide |
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Dosing Frequency | 2x/week | Daily | Daily |
GI Tolerance | Better | Poor | Moderate |
Fibrosis Risk | Higher | Lower | Moderate |
Cost | $$ | $ | $$$ |
10. PATIENT COUNSELING
✔ Take evening doses to minimize dizziness
✔ Report immediately:
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Shortness of breath (cardiac fibrosis)
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Hallucinations (especially in Parkinson’s patients)
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Leg swelling/pain (DVT risk)
✔ Fertility patients:
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May resume menses within 4-6 weeks
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Use contraception until prolactin normalized
CONCLUSION
Caberlin 0.5 mg is the most potent/longest-acting prolactin-lowering agent, ideal for:
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Rapid prolactin normalization
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Macroprolactinoma shrinkage
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Patients intolerant to bromocriptine
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