Full Prescribing Info
Pharmacotherapeutic Group: Antiplatelet Agent; Phos­phodiesterase Enzyme Inhibitor.
Pharmacology: Pharmacodynamics: Mechanism of Action: Cilostazol and its metabolites are inhibitors of phosphodiesterase III. As a result cyclic AMP is increased leading to inhibition of platelet aggregation, vasodila­tion and inhibi­tion of platelet aggregation,  vasodilation,  and inhibi­tion of vascular smooth muscle cell proliferation.
Pharmacodynamics/kinetics: Onset of action: 2-4 weeks; may require up to 12 weeks.
Protein binding: Cilostazol 95% to 98%; active metabolites 66% to 97%.
Metabolism: Hepatic via CYP3A4 (primarily), 1A2, 2C19, and 2D6; at least one metabolite has significant activity.
Half-life elimination: 11-13 hours.
Excretion: Urine (74%) and (20%) as metabolites.
Symptomatic management of peripheral vascular disease, primarily intermittent claudication; currently being investigated for the treatment of acute coronary syndromes and for graft patency improvement in percutaneous coronary interventions with or without stenting.
Dosage/Direction for Use
Adults: Oral: 100 mg twice daily.
Dosage adjustment to cilostazol with concomitant medications: CYP2C19 inhibitors (see Interactions): Dosage of cilostazol should be reduced to 50 mg twice daily. CYP3A4 inhibitors (see Interactions): Dosage of cilostazol should be reduced to 50 mg twice daily.
Dietary Considerations: It is best to take cilostazol 30 minutes before or 2 hours after meals.
Administration: Administer cilostazol 30 minutes before or 2 hours after meals.
Experience with overdosage in humans is limited. Headache, diar­rhea, hypotension, tachycardia and/or cardiac arrhythmias may occur. Treatment is sympto­matic and supportive. Hemodialysis is unlikely to be of value. In some animal models, high-dose or long-term administration was associated with a variety of cardiovascular lesions; including endocardial hemorrhage, hemosiderin deposition and left ventricular fibrosis, coronary arteritis, and periarteritis.
Hypersensitivity to cilostazol or any component of the formulation; heart failure (HF) of any severity; hemostatic disorders or active bleeding.
Special Precautions
Use with caution in patients receiving other platelet aggregation inhibitors or in patients with thrombocytopenia. Discontinue therapy if thrombocytopenia or leukopenia occur; progression to agranulocytosis (reversible) has been reported when cilostazol was not immediately stopped. When cilostazol and clopidogrel are used concurrently, manufacturer recommends checking bleeding times. Withhold for at least 4-6 half-lives prior to elective surgical procedures. Use with caution in patients receiving CYP3A4 inhibitors (eg, ketoconazole or erythromycin) or CYP2C19 inhibitors (eg, omeprazole). If concurrent use is warranted, consider dosage adjustment of cilostazol. Use with caution in severe underlying heart disease. Use caution in moderate-to-severe hepatic impairment. Use cautiously in severe renal impairment (Clcr <25 mL/minute). Safety and efficacy in pediatric patients have not been established.
Use In Pregnancy & Lactation
Pregnancy: Pregnancy Risk Factor: C.
In animal studies, abnor­malities of the skeletal, renal and cardiovascular system were increased. In addition, the incidence of stillbirth  and decreased birth weights were increased.
Excretion in breast milk unknown/not recommended.
Adverse Reactions
>10%: Central nervous system: Headache (27% to 34%).
Gastrointestinal: Abnormal stools (12% to 15%), diarrhea (12% to 19%).
Respiratory: Rhinitis (7% to 12%).
Miscellaneous: Infection (10% to 14%).
2% to 10%: Cardiovascular: Peripheral edema (7% to 9%), palpitation (5% to 10%), tachycardia (4%).
Central nervous system: Dizziness (9% to 10%), vertigo (up to 3%).
Gastrointestinal: Dyspepsia (6%), nausea (6% to 7%), abdominal pain (4% to 5%), flatulence (2% to 3%).
Neuromuscular and skeletal: Back pain (6% to 7%), myalgia (2% to 3%).
Respiratory: Pharyngitis (7% to 10%), cough (3% to 4%).
<2% (Limited to important or life-threatening): Agran­ulocytosis, anemia, aplastic anemia, asthma, atrial fibrillation, atrial flutter, blindness, blood pressure increased, bursitis, cardiac arrest, cerebral infarc­tion/ischemia, cerebrovascular accident, chest pain, CHF, cholelithiasis, colitis, coronary stent thrombosis, cystitis, diabetes mellitus, duodenal ulcer, duodenitis, esophageal hemorrhage, esoph­agitis, extradural hematoma, gastrointestinal hemorrhage, gout, granulocytopenia, hemorrhage, hepatic dysfunction, hot flashes, hyperglycemia, hypotension, interstitial pneumonia, intracranial hemorrhage, jaundice, leukopenia, myocardial infarction/ischemia, neuralgia, nodal arrhythmia, pain, periodontal abscess, peptic ulcer, pneumonia, polycythemia, postural hypotension, pulmonary hemorrhage, pruritus, QTc prolongation, rectal hemorrhage, retinal hemorrhage, retroperitoneal hemorrhage, Stevens-Johnson syndrome, subcutaneous hemorrhage, subdural hematoma, supraven­tricular tachycardia, syncope, thrombocytopenia, thrombosis, torsade de pointes, uric acid increased, ventricular tachycardia.
Drug Interactions
Cytochrome P450 Effect: Substrate of CYP1A2 (minor), 2C19 (minor), 2D6 (minor), 3A4 (major).
Increased Effect/Toxicity: Cilostazol serum concentrations may be increased by antifungal agents (midazole), macrolide antibiotics, and omeprazole. Increased concentrations of cilostazol may be anticipated during concurrent therapy with other inhibitors of CYP3A4 (eg, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil) or inhibitors of CYP2C19 (eg, delavridine, fluconazole, fluvoxamine, gemfibrozil, isoniazid, omeprazole, and ticlopidine). Aspirin-induced inhibition of platelet aggregation is potentiated by concurrent cilostazol. Concurrent use of anticoagulants, dasatinib, drotrecogin alfa, NSAIDs, or treprostinil may cause increased bleeding.
Decreased Effect: CYP3A4 inducers may decrease the levels/effects of cilostazol. Example inducers include aminoglutethimide, carbamaze­pine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.
Ethanol/Nutrition/Herb Interactions: Food: Taking cilostazol with a high-fat meal may increase peak concentration by 90%. Avoid concur­rent ingestion of grapefruit juice due to the potential to inhibit CYP3A4.
Herb/Nutraceutical: St. John's wort may decrease the levels/effects of cilostazol. Avoid alfalfa, anise, bilberry, bladderwrack, bromelain, cat's claw, chamomile, coleus, cordyceps, dong quai, evening primrose oil, fenugreek, feverfew, garlic, ginger, ginkgo biloba, ginseng (American), ginseng (Panax), ginseng (Siberian), grape seed, green tea, guggul, horse chestnut seed, horseradish, licorice, prickly ash, red clover, reishi, SAMe (S-adenosylmethionine), sweet clover, turmeric, white willow (all have additional antiplatelet activity).
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
ATC Classification
B01AC23 - cilostazol ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
Tab 50 mg x 1 x 10's, 1 x 10 x 10's. 100 mg x 1 x 10's, 10 x 10's.
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