A type III phosphodiesterase inhibitor that inhibits platelet aggregation and increases vasodilation and is effective for treatment of intermittent claudication.
Used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease.
Has a therapeutic focus on cAMP with main effects being the dilation of the arteries supplying blood to the legs and decreasing platelet coagulation.
Increased cAMP results in an increase in the active form of PKA, which is directly related with an inhibition in platelet aggregation.
Dosage is 100 mg twice a day.
Pletal may take as long as 3 months to be clinically apparent and has been shown to improve pain-free walking distance by 50%.
Adverse effects include: headache, diarrhea, abnormal stools, tachycardia, and palpitations.
Metabolized by CYP3A4 and CYP2C19, two isoenzymes of the cytochrome P450 system.
Drugs that inhibit CYP3A4, such as itraconazole, erythromycin, ketoconazole, and diltiazem, are known to interact with cilostazol, and the proton pump inhibitor omeprazole, a potent inhibitor of CYP2C19, increases exposure to the active metabolite of cilostazol.
Grapefruit juice, a CYP3A4 inhibitor, increases the drug’s maximum concentration by around 50%.