Cilostazol
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Generic Name of Cilostazol - Learn More
Cilostazol
Cilostazol Precaution - What You Need to Know
When using cilostazol, several important precautions need to be observed to ensure safe and effective therapy:
- Pregnancy and breastfeeding:
- Cilostazol is classified as Category C by the FDA, meaning it should only be used during pregnancy if the potential benefits justify the potential risks to the fetus. Limited data on its safety in pregnant women suggests that the drug may not be safe during pregnancy.
- Breastfeeding: The use of cilostazol in breastfeeding mothers is not well studied, and it is excreted in small amounts in breast milk. Caution is advised if cilostazol is prescribed to breastfeeding women, and it should be considered only if the potential benefit to the mother outweighs any potential risk to the infant.
- Cardiovascular concerns:
- Cilostazol should be used cautiously in patients with heart failure, particularly those with class III or IV heart failure, as it may worsen the condition. It has been associated with an increased risk of cardiac events in this patient group.
- Bleeding risks:
- Cilostazol is an antiplatelet drug, and as such, it increases the risk of bleeding. Caution is needed when using cilostazol in patients with a history of bleeding disorders, those who are on anticoagulants, or those who have undergone surgical procedures. Monitoring for signs of excessive bleeding (e.g., bruising, hematuria) is recommended.
- Renal function:
- Cilostazol is metabolized by the liver and excreted by the kidneys. It should be used with caution in patients with renal impairment, particularly in those with severe renal dysfunction (creatinine clearance < 25 mL/min). Dose adjustment may be necessary in these patients.
- Hepatic concerns:
- Cilostazol is metabolized by the liver, and in patients with liver disease, especially severe liver impairment, its use should be avoided due to potential accumulation and increased risk of adverse effects.
Cilostazol Indication - Uses and Benefits
Cilostazol is primarily indicated for the treatment of intermittent claudication, which is a condition commonly associated with peripheral arterial disease (PAD). It helps to improve walking distance and reduce symptoms of claudication.
- Peripheral arterial disease (PAD):
- Cilostazol is used to improve symptoms of intermittent claudication, which is characterized by leg pain and cramping due to inadequate blood flow. The drug works by improving blood flow and increasing walking distance in patients with PAD.
- Off-label uses:
- Cilostazol is sometimes used off-label for conditions where improving blood flow might be beneficial, such as cerebral ischemia or other vascular diseases. However, the evidence for its efficacy in these conditions is less robust than for PAD.
Cilostazol Contraindications - Important Warnings
There are several conditions in which cilostazol should not be used due to safety concerns:
- Heart failure (moderate to severe):
- Cilostazol is contraindicated in patients with heart failure of class III or IV (moderate to severe), as it can worsen the condition. The drug may increase the risk of cardiac events in patients with heart failure.
- Hypersensitivity:
- Cilostazol is contraindicated in patients who have a known hypersensitivity or allergy to the drug. An allergic reaction may include rash, swelling, or difficulty breathing, and immediate medical attention should be sought if any of these symptoms occur.
- Active bleeding disorders:
- Since cilostazol is an antiplatelet agent, it is contraindicated in patients with a history of active bleeding disorders, such as peptic ulcer disease, intracranial hemorrhage, or any condition that predisposes to bleeding. It should also be avoided in patients undergoing recent surgery or trauma where there is a high risk of bleeding.
- Liver impairment:
- Cilostazol is contraindicated in patients with severe hepatic impairment, as it can accumulate in the body, leading to an increased risk of adverse effects.
Cilostazol Side Effects - What to Expect
Cilostazol is generally well-tolerated, but some patients may experience side effects. These range from mild to severe:
- Common side effects:
- Headache: One of the most common side effects, occurring in approximately 10% of patients.
- Diarrhea: Mild gastrointestinal upset, including diarrhea or loose stools, can occur.
- Dizziness or lightheadedness: Especially when standing up quickly, which may be due to vasodilation.
- Palpitations: Some patients report rapid or irregular heartbeats, particularly those with pre-existing cardiovascular conditions.
- Serious side effects:
- Bleeding: Cilostazol increases the risk of bleeding, which can result in easy bruising, nosebleeds, or more serious hemorrhagic events, such as gastrointestinal bleeding or intracranial hemorrhage.
- Heart problems: Although rare, cilostazol may cause issues like tachycardia or arrhythmias, particularly in patients with underlying heart conditions.
- Liver toxicity: Cilostazol can cause elevated liver enzymes in some individuals, potentially leading to liver injury. Monitoring of liver function is recommended during treatment.
- Mitigating side effects:
- Dose reduction or discontinuation of cilostazol is recommended if significant adverse effects occur, particularly bleeding or heart-related issues.
Cilostazol Pregnancy Category ID - Safety Information
3
Cilostazol Mode of Action - How It Works
Cilostazol exerts its therapeutic effects primarily by inhibiting platelet aggregation and promoting vasodilation.
- Platelet aggregation inhibition: Cilostazol is a phosphodiesterase-3 (PDE3) inhibitor, which increases cyclic AMP (cAMP) levels within platelets. This leads to the inhibition of platelet aggregation and reduces the likelihood of clot formation. This effect is beneficial in preventing the occlusion of blood vessels in patients with peripheral arterial disease (PAD).
- Vasodilation: In addition to its effects on platelets, cilostazol causes vasodilation by increasing cAMP levels in vascular smooth muscle cells. This results in the relaxation of blood vessels and improved blood flow, especially in the lower extremities of patients with PAD. This mechanism helps to reduce symptoms of intermittent claudication and improve walking distance.
Cilostazol Drug Interactions - What to Avoid
Cilostazol interacts with a variety of other drugs, potentially altering its effects or causing harmful side effects:
- CYP3A4 inhibitors:
- Cilostazol is metabolized by the CYP3A4 enzyme in the liver. Drugs that inhibit this enzyme, such as ketoconazole, itraconazole, and clarithromycin, can increase the levels of cilostazol in the blood, raising the risk of side effects. Dose adjustments or alternative therapies may be needed if these drugs are co-administered.
- Antiplatelet and anticoagulant drugs:
- The concurrent use of cilostazol with other antiplatelet agents (such as aspirin or clopidogrel) or anticoagulants (such as warfarin) increases the risk of bleeding. Careful monitoring of bleeding parameters (such as INR for warfarin) is essential.
- Other vasodilators:
- Cilostazol may have additive effects when taken with other vasodilators (e.g., nitrates), potentially leading to excessive hypotension. Blood pressure should be monitored in patients receiving both therapies.
- Grapefruit juice:
- Grapefruit or grapefruit juice can inhibit the CYP3A4 enzyme and increase blood levels of cilostazol, increasing the risk of side effects. It is recommended to avoid grapefruit products during cilostazol therapy.
Cilostazol Adult Dose - Recommended Dosage
- The standard adult dose of cilostazol for intermittent claudication is 100 mg twice daily. It should be taken on an empty stomach, ideally 30 minutes before or 2 hours after meals, as food can reduce its absorption.
- In patients with mild-to-moderate renal impairment (creatinine clearance ≥ 25 mL/min), the dose does not need to be adjusted. However, in patients with severe renal impairment (creatinine clearance < 25 mL/min), cilostazol should be avoided or used with caution.
- The maximum recommended dose is 100 mg twice daily.
Cilostazol Child Dose - Dosage for Children
- Cilostazol is not recommended for use in children, as safety and efficacy in pediatric populations have not been established. The drug is intended primarily for adult patients with peripheral arterial disease and intermittent claudication.
Cilostazol Renal Dose - Dosage for Kidney Conditions
- Cilostazol should be used with caution in patients with renal impairment. In those with severe renal dysfunction (creatinine clearance < 25 mL/min), the drug is generally avoided because the risk of side effects may be increased due to slower drug clearance.
- For mild-to-moderate renal impairment (creatinine clearance ≥ 25 mL/min), the standard dose of 100 mg twice daily is typically safe, but renal function should be monitored periodically.
