| Product Name |
Cerebrolysin |
| Active Ingredient |
Cerebrolysin |
| Dosage Form |
Injection |
| Strength |
60mg/vial*6vials |
| Manufacturer |
Sinopharmatech Co., Ltd. |
Mechanism of Action
Cerebrolysin is a peptide-based neurotrophic agent derived from porcine brain proteins, containing a mixture of low molecular weight peptides (25%) and free amino acids (75%), including neurotrophic factors like BDNF, NGF, and GDNF. Its multimodal mechanism includes:
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Neuroprotection: Reduces ischemic neuronal death by inhibiting oxidative stress, inflammation, and excitotoxicity. It stabilizes the blood-brain barrier (BBB) by upregulating tight-junction proteins and reducing pro-inflammatory cytokines (e.g., IL-1β) released by microglia.
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Neurotrophic Support: Mimics endogenous neurotrophic factors, promoting neuronal survival, axonal growth, and synaptic plasticity. It enhances BDNF and NGF signaling, critical for cholinergic neuron preservation in Alzheimer's disease.
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Metabolic Enhancement: Increases GLUT1 glucose transporter expression in the BBB, improving cerebral glucose uptake and energy metabolism.
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Anti-Inflammatory Effects: Modulates neuroinflammation by reducing fibrin-induced endothelial damage and ICAM-1 expression, thereby limiting leukocyte adhesion and vascular leakage.
2. Therapeutic Applications and Future Prospects
Current Clinical Uses
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Stroke Recovery: Reduces infarct volume and improves neurological outcomes by protecting neurons from ischemic injury and promoting angiogenesis via VEGF and Angiopoietin-1 pathways.
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Neurodegenerative Diseases:
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Alzheimer's Disease (AD): Modulates amyloid precursor protein (APP) phosphorylation, reducing amyloid-beta accumulation, and enhances cholinergic function.
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Vascular Dementia: Improves cognitive scores (e.g., ADAS-cog) by enhancing synaptic connectivity and cerebral perfusion.
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Traumatic Brain Injury (TBI): Accelerates neuronal repair and reduces apoptosis through neurotrophic factor upregulation.
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Peripheral Neuropathies: Supports nerve regeneration in conditions like diabetic neuropathy.
Emerging Research Directions
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Parkinson's Disease: Investigated for its potential to protect dopaminergic neurons and improve motor symptoms.
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Multiple Sclerosis (MS): Explored for remyelination support and immune modulation.
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Cognitive Enhancement: Used off-label as a nootropic to improve memory and focus in healthy adults.
3. Dosage and Administration
Standard Protocols
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Route: Intramuscular (IM) or intravenous (IV) injection. IV is preferred for rapid CNS distribution, while IM is common for outpatient use.
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Dosing:
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Stroke/TBI: 20-50 mL/day IV for 7-21 days.
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AD/Vascular Dementia: 10-30 mL/day IV for 4 weeks, repeated 2-4 times annually.
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Nootropic Use: 5-10 mL/day IM for 10-20 days, with cycles repeated as needed.
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Cycling: Typically administered in 20-day cycles with 1-2 month breaks to prevent tolerance.
Individualization
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Elderly/Frail Patients: Lower initial doses (e.g., 5 mL/day) to minimize adverse effects.
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Combination Therapy: Often paired with cholinesterase inhibitors (e.g., donepezil) in AD for synergistic effects.
4. Storage and Stability
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Unopened Vials: Store at room temperature (15-25°C), protected from light and moisture.
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Reconstituted Solution: Use immediately; if necessary, refrigerate at 2-8°C for up to 24 hours.
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Avoid Freezing: Freezing may denature peptides, reducing efficacy.
5. Safety and Considerations
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Side Effects: Generally well-tolerated; mild reactions include headache, nausea, or injection-site pain. High doses (≥80 mL/day) may increase non-fatal adverse events.
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Contraindications: Hypersensitivity to porcine proteins, severe renal/hepatic impairment, or active malignancy.
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Monitoring: Regular cognitive assessments and metabolic panels during long-term use.
6. Conclusion
Cerebrolysin represents a unique therapeutic approach by combining neuroprotection, neurotrophic support, and metabolic enhancement. Its broad applicability in acute neurological injuries and chronic degenerative conditions underscores its potential as a disease-modifying agent. While robust clinical evidence supports its efficacy, ongoing research is critical to optimize dosing, clarify long-term safety, and expand its role in neuroregenerative medicine.
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References: International Peptide Society, Cochrane Reviews, and clinical trials published in European Journal of Neurology and Journal of Neural Transmission.
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