Cilostazol

Intermittent Claudication (Peripheral Artery Disease)

• Indication: Cilostazol is FDA-approved for treating intermittent claudication, a condition caused by peripheral artery disease (PAD) that leads to pain, cramping, and muscle fatigue in the legs during walking or exercise.
• Dosing Information:
• Initial and Maintenance Dose: The recommended dose is 100 mg taken twice daily.
• Administration: Cilostazol should be taken at least 30 minutes before or 2 hours after meals, as food can increase the drug's concentration in the bloodstream, potentially leading to side effects.
• Duration: Improvement may take 2-4 weeks of consistent use, and the full effect is usually seen within 12 weeks.

Cerebral Ischemia (Prevention of Stroke or Mini-Strokes)

• Off-label Use: Cilostazol is sometimes used to reduce the risk of strokes or transient ischemic attacks (TIAs) in patients with cerebral ischemia, particularly in patients who cannot tolerate aspirin or clopidogrel.
• Dosing Information: Typically, 100 mg twice daily, similar to the dosage for intermittent claudication.

Secondary Prevention of Coronary Artery Disease (CAD) after Angioplasty or Stenting

• Off-label Use: Cilostazol may prevent restenosis (re-narrowing of blood vessels) after angioplasty or stent placement in coronary arteries. It is often combined with other antiplatelet medications.
• Dosing Information: The usual dose is 100 mg twice daily, along with other blood-thinning agents.

Buerger's Disease (Thromboangiitis Obliterans)

• Off-label Use: Cilostazol has been used to improve circulation and reduce symptoms like pain and ulcers in patients with Buerger's disease, where small blood vessels become inflamed and blocked.
• Dosing Information: 100 mg twice daily, taken at least 30 minutes before or 2 hours after meals.

Prevention of Stent Thrombosis

• Off-label Use: Cilostazol may be prescribed to reduce the risk of stent thrombosis (blood clots forming in a stent) in patients undergoing percutaneous coronary intervention (PCI).
• Dosing Information: Typically, 100 mg twice daily is taken, often in combination with other antiplatelet medications like clopidogrel.

Raynaud's Phenomenon

• Off-label Use: Cilostazol can improve blood flow and reduce symptoms of Raynaud's phenomenon, which causes decreased blood flow to the fingers and toes.
• Dosing Information: 100 mg twice daily, similar to the treatment for intermittent claudication.

Heart Failure (any severity):

• Cilostazol is contraindicated in patients with congestive heart failure of any severity. It can increase mortality in these patients due to its effects on the heart, as it may increase heart rate and cause arrhythmias.

Active Bleeding:

• Patients with active bleeding disorders (e.g., peptic ulcer, intracranial hemorrhage) should not use Cilostazol, as it can increase the risk of bleeding due to its blood-thinning effects.

Hypersensitivity to Cilostazol:

• Individuals who are allergic or have had a previous hypersensitivity reaction to Cilostazol or any of its components should avoid taking the medication.

Severe Renal Impairment:

• Cilostazol is contraindicated in patients with severe kidney disease (creatinine clearance less than 25 mL/min), as the drug may accumulate in the body and cause harmful effects.

Concurrent Use of Certain CYP3A4 and CYP2C19 Inhibitors:

• Strong inhibitors of the CYP3A4 enzyme (e.g., ketoconazole, itraconazole) or the CYP2C19 enzyme (e.g., omeprazole) can significantly increase Cilostazol levels in the blood, increasing the risk of side effects. Dose adjustments or avoiding these combinations are recommended.

Monitor for heart symptoms: If you experience chest pain, rapid heartbeat, or palpitations while taking Cilostazol, contact your doctor immediately. Cilostazol can increase heart rate and may not be suitable for individuals with heart conditions.

Be patient with results: It may take 2-4 weeks to notice an improvement in symptoms like leg pain, and up to 12 weeks for full effects. Continue taking the medication as prescribed and follow up with your doctor if needed.

Watch for bleeding: Cilostazol can increase your risk of bleeding, especially if you are also taking blood thinners or antiplatelet medications. Report any unusual bruising, bleeding, or black, tarry stools to your healthcare provider right away.

Headache: One of the most frequently reported side effects.

Diarrhea: Some people experience loose stools or diarrhea while taking Cilostazol.

Dizziness: Feeling lightheaded or dizzy is common, especially when starting the medication.

Palpitations: Some patients report feeling a faster or irregular heartbeat.

Nausea: Mild nausea can occur, especially if the medication is not taken as directed (e.g., on an empty stomach).

Abdominal pain: Stomach discomfort or pain may develop in some patients.

Swelling in legs or feet (edema): Mild swelling in the lower limbs, particularly in the ankles or feet, can occur.

Fast or irregular heartbeat (arrhythmia): Cilostazol can cause heart rhythm problems, which may lead to dizziness, fainting, or chest pain.

Severe chest pain (angina): If you experience intense chest pain, it may be a sign of a serious heart issue, especially in patients with a history of heart disease.

Shortness of breath: Difficulty breathing or shortness of breath may indicate a serious reaction or worsening of an underlying condition.

Unusual bleeding or bruising: Cilostazol can increase the risk of bleeding, so any unexplained or prolonged bleeding (nosebleeds, gum bleeding) or large, unexplained bruises should be reported to a healthcare provider.

Black, tarry stools or blood in urine: These symptoms could indicate internal bleeding and require immediate medical attention.

Severe dizziness or fainting: While mild dizziness is common, severe dizziness or fainting can indicate low blood pressure or heart-related issues.

Increased Risk of Heart-Related Events in Certain Patients:

Cilostazol is not recommended for individuals with a history of heart failure. Studies have shown that patients with heart failure who take Cilostazol may have an increased risk of serious cardiovascular events, including heart failure worsening and death.

Risk of Fluid Retention:

Cilostazol may cause fluid retention, which can lead to or worsen swelling in the legs or feet (edema). Patients with a history of heart or kidney issues should be cautious and report any signs of swelling to their doctor.

Interaction with Antiplatelet or Anticoagulant Medications:

Patients taking blood thinners (like warfarin) or antiplatelet medications (like aspirin or clopidogrel) are at an increased risk of bleeding when using Cilostazol. Careful monitoring by a healthcare provider is necessary to avoid excessive bleeding.

Pentoxifylline (Trental):

• Another medication used to treat intermittent claudication improves blood flow and reduces muscle pain in the legs. It decreases blood viscosity (thickness) and increases oxygen delivery to tissues.

Aspirin:

• The antiplatelet medication prevents blood clots and improves circulation in patients with peripheral artery disease (PAD). While not as effective for intermittent claudication as Cilostazol, aspirin helps reduce the risk of cardiovascular events.

Clopidogrel (Plavix):

• An antiplatelet drug that helps prevent blood clots in patients with PAD, reducing the risk of heart attacks and strokes. It is not explicitly indicated for intermittent claudication but can improve circulation and prevent cardiovascular events.

Exercise Therapy:

• A supervised exercise program, particularly walking therapy, can improve symptoms of intermittent claudication by encouraging better blood flow to the legs. Exercise is highly recommended as a first-line treatment alongside medication.

Surgical or Endovascular Procedures:

• For patients with severe peripheral artery disease (PAD) or those who do not respond to medications, surgical options like angioplasty, stenting, or bypass surgery may be recommended to restore blood flow to the legs.

Statins (e.g., Atorvastatin, Rosuvastatin):

• Although statins are primarily used to lower cholesterol, they also improve blood vessel health and reduce the risk of cardiovascular events in patients with PAD. Statins can be used in combination with other treatments for intermittent claudication.

Vasodilators (e.g., Naftidrofuryl):

• Naftidrofuryl is a vasodilator used in some countries (though not widely available in the U.S.) to treat intermittent claudication by improving blood flow to the legs.