Fasudil [Neurosurgery Wiki]

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====== Fasudil ======


===== Mechanism, Clinical Uses, and Therapeutic Potential  =====
 

#### **1. What is Fasudil?**  
Fasudil is a **selective [[ROCK inhibitor]]**, an enzyme involved in cytoskeletal regulation, smooth muscle contractility, and vascular function. Initially developed for treating **cerebral vasospasm** after subarachnoid hemorrhage (SAH), it has shown potential for various **neurological and cardiovascular** conditions.  

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### **2. Mechanism of Action**  
Fasudil inhibits **Rho-kinase (ROCK)**, leading to several beneficial effects:  
✅ **Vasodilation:** Reduces smooth muscle contractility, improving blood flow.  
✅ **Neuroprotection:** Decreases apoptosis and promotes neuronal regeneration.  
✅ **Cytoskeletal modulation:** Prevents fibrosis and pathological tissue stiffening.  
✅ **Anti-inflammatory effects:** Reduces immune cell activation and oxidative stress.  

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### **3. Clinical Indications**  

#### **3.1. Approved Uses (Japan & China)**  
🔹 **Cerebral vasospasm after SAH** → Approved in Japan & China. Improves cerebral perfusion and reduces secondary ischemia.  

#### **3.2. Investigational Uses**  
🔹 **Ischemic stroke** → Potential neuroprotective and recovery-enhancing effects.  
🔹 **Pulmonary hypertension** → Reduces pulmonary vascular resistance.  
🔹 **Neurodegenerative diseases (Parkinson’s, Alzheimer’s, ALS)** → Anti-apoptotic and anti-inflammatory effects in experimental models.  
🔹 **Spinal cord injury & axonal regeneration** → Inhibition of the RhoA-ROCK pathway promotes neuronal growth.  
🔹 **Glaucoma** → Reduces intraocular pressure by improving aqueous humor drainage.  

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### **4. Side Effects & Limitations**  
✅ Generally well-tolerated.  
🚨 **Possible adverse effects:**  
- Hypotension  
- Nausea and vomiting  
- Headache  
- Rare liver enzyme elevation  

📌 **Limitations:**  
- **Intravenous administration**, limiting outpatient use.  
- **Not yet approved** in the U.S. or Europe for broader indications.  

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### **5. Future Perspectives**  
🔹 **Development of oral formulations** to enhance accessibility.  
🔹 **Clinical trials for neurodegenerative and fibrotic diseases.**  
🔹 **Combination therapies** to optimize effects in nerve injury and vascular diseases.  

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### **6. Conclusion**  
Fasudil is a promising drug with **vasodilatory, neuroprotective, and anti-inflammatory** properties. While currently approved mainly in Asia for **cerebral vasospasm**, its potential applications in **neuroprotection, pulmonary hypertension, and nerve regeneration** make it a key candidate for future therapeutic advancements.  

📌 Would you like more details on recent studies or its mechanism in a specific disease?