From the Guidelines
Yes, cilostazol is an anti-platelet agent, as it works by inhibiting phosphodiesterase type 3 (PDE3), which increases cyclic adenosine monophosphate (cAMP) levels in platelets and blood vessels, preventing platelets from clumping together and forming blood clots, while also causing vasodilation of blood vessels 1.
Mechanism of Action
Cilostazol's mechanism of action is unique, as it not only prevents platelet aggregation but also causes vasodilation, which helps improve blood flow to the legs in peripheral artery disease. This is particularly beneficial for patients with intermittent claudication, a condition characterized by leg pain during walking due to poor circulation.
Clinical Use
Cilostazol is primarily used to treat intermittent claudication, with a typical dosage of 100 mg taken twice daily, at least 30 minutes before or 2 hours after meals, as food can increase absorption and potentially cause side effects 1.
- Common side effects include:
- Headache
- Diarrhea
- Palpitations
- Dizziness It should not be used in patients with heart failure, as it may increase mortality risk in this population 1.
Benefits and Risks
Unlike some other anti-platelet medications, cilostazol has the added benefit of dilating blood vessels, which helps improve blood flow to the legs in peripheral artery disease. However, its use is contraindicated in patients with congestive heart failure, and it may cause side effects such as headache, diarrhea, palpitations, and dizziness 1.
- The benefits of cilostazol include:
- Improved symptoms and increased walking distance in patients with claudication
- Vasodilation of blood vessels, which helps improve blood flow to the legs
- The risks of cilostazol include:
- Increased mortality risk in patients with heart failure
- Common side effects such as headache, diarrhea, palpitations, and dizziness
Recommendation
Cilostazol is a recommended therapy for patients with intermittent claudication, as it improves symptoms and increases walking distance, with a typical dosage of 100 mg taken twice daily 1.
From the FDA Drug Label
Cilostazol and several of its metabolites are cyclic AMP (cAMP) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing cAMP degradation with a resultant increase in cAMP in platelet and blood vessels, leading to inhibition of platelet aggregation and vasodilation, respectively Cilostazol reversibly inhibits platelet aggregation induced by a variety of stimuli, including thrombin, ADP, collagen, arachidonic acid, epinephrine, and shear stress. Cilostazol tablets inhibit platelet aggregation in a reversible manner.
Yes, cilostazol is an anti-platelet agent because it inhibits platelet aggregation in a reversible manner, as stated in the drug labels 2 and 2.
- The mechanism of action of cilostazol involves the inhibition of phosphodiesterase III, which leads to an increase in cAMP in platelets and blood vessels.
- This increase in cAMP results in the inhibition of platelet aggregation and vasodilation.
- Cilostazol has been shown to reversibly inhibit platelet aggregation induced by various stimuli.
From the Research
Cilostazol's Mechanism of Action
- Cilostazol is a selective inhibitor of phosphodiesterase-III with antiplatelet, antithrombotic, and vasodilating properties 3, 4, 5, 6, 7
- It inhibits platelet aggregation induced by ADP, collagen, and arachidonic acid 3
- Cilostazol also acts as a vascular vasodilator by inhibiting calcium-induced contractions while having no direct effect on contractile proteins 3
Clinical Applications
- Cilostazol has been used in the treatment of patients with peripheral ischemia, such as intermittent claudication 3, 4, 6, 7
- It has been shown to improve walking distances and quality of life in patients with intermittent claudication 3, 4, 6
- Cilostazol may also be useful in preventing thrombosis and restenosis following percutaneous coronary interventions 6
- It is potentially useful after ischemic stroke and is an alternative in those who are allergic or intolerant to classical antithrombotic agents 7
Safety and Tolerability
- Cilostazol has been well tolerated, with the most common adverse events being headache, diarrhea, abnormal stools, and dizziness 3, 4
- Significant drug interactions are observed when cilostazol is coadministered with other agents that inhibit cytochrome P450 (CYP) 3A4 or CYP2C19 4
- Cilostazol is contraindicated in several subpopulations of patients, particularly those with congestive heart failure and severe hepatic or renal impairment 4