What is cilostazol, and how does it work (mechanism of action)?

Cilostazol is a medication for the treatment of intermittent claudication, a condition caused by narrowing of the arteries that supply the legs with blood. Patients with intermittent claudication develop pain when they walk because not enough oxygen-containing blood reaches the active leg muscles. Cilostazol reduces the pain of intermittent claudication by dilating the arteries, thereby improving the flow of blood and oxygen to the legs. (It does this by decreasing the action of an enzyme, phosphodiesterase III.) It also reduces the ability of blood to clot. Cilostazol enables patients with intermittent claudication to walk longer and faster before developing pain. Cilostazol has a different mechanism of action than pentoxifylline (Trental), the other drug approved for intermittent claudication. (Pentoxifylline improves blood flow by making it easier for red blood cells to pass through vessels. It also decreases the viscosity of blood.). The FDA approved cilostazol in January 1999.

What brand names are available for cilostazol?

Pletal

Is cilostazol available as a generic drug?

Yes

Do I need a prescription for cilostazol?

Yes

What are the side effects of cilostazol?

The most common adverse effects of cilostazol are:

Other important side effects which have also been reported with cilostazol include a reduction in numbers of white blood cells and platelets. Severe skin reactions also have been reported.

Cilostazol inhibits the enzyme phosphodiesterase III. Other drugs that inhibit this enzyme have caused death in individuals with heart failure. Therefore, individuals with heart failure should not use cilostazol.

What is the dosage for cilostazol?

The dose is 100 mg twice daily. Cilostazol should be taken at least half an hour before or two hours after dinner and breakfast to prevent food from affecting its absorption.

Which drugs or supplements interact with cilostazol?

Erythromycin (E.E.S, Erythrocin), omeprazole (Prilosec) and diltiazem (Cardizem) increase the concentration of cilostazol by blocking the action of enzymes that destroy cilostazol. Though not specifically studied, a similar interaction could occur with ketoconazole (Nizoral), itraconazole (Sporanox), fluconazole (Diflucan), miconazole (Monistat), fluvoxamine (Luvox), fluoxetine (Prozac), nefazodone (Serzone) and sertraline (Zoloft). Diltiazem (Cardizem) and omeprazole (Prilosec) also increase concentrations of cilostazol.

Higher concentrations of cilostazol could increase the possibility of toxic effects. Therefore, a dose of 50 mg twice daily should be considered when drugs that may increase the concentration of cilostazol also are being used.

Combining pletal with other drugs that interfere with the blood clotting process may increase the likelihood of bleeding.

A high fat meal increases the absorption of cilostazol. Grapefruit juice could increase the concentration of cilostazol. Therefore, grapefruit juice should not be taken by patients on cilostazol.

Is cilostazol safe to take if I’m pregnant or breastfeeding?

The use of cilostazol in pregnancy has not been adequately studied.

Cilostazol has not been adequately studied in women who are breastfeeding.

What else should I know about cilostazol?

What preparations of cilostazol are available?

Tablets: 50 and 100 mg

How should I keep cilostazol stored?

Tablets should be stored below 25 C (77 F). Brief exposures to 30 C (86 F) are allowed.

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Medically Reviewed on 3/19/2019

References

Medically reviewed by John P. Cunha, DO, FACOEP; Board Certified Emergency Medicine

REFERENCE:

FDA Prescribing Information