cilostazol (Rx)

Brand and Other Names:Pletal
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 50mg
  • 100mg

Intermittent Claudication

100 mg PO q12hr 30 minutes before or 2 hours after meals

Discontinue if symptoms not improved after 3 months of therapy

Dosing considerations

  • CYP2C19 or CYP3A4 inhibitors: Reduce dosage to 50 mg PO q12hr

Thrombotic Complications of Coronary Angioplasty (Off-label)

100 mg q12hr 30 minutes before or 2 hours after meals

Dosing considerations

  • May be administered alone or in combination with aspirin 81 mg/day

Renal Impairment

CrCl< 25 mL/min: Use caution

Hepatic Impairment

Moderate to severe: Use caution

Safety and efficacy not established

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Interactions

Interaction Checker

and cilostazol

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            Contraindicated (1)

            • abrocitinib

              abrocitinib and cilostazol both increase anticoagulation. Contraindicated. Antiplatelet drugs, except for low-dose aspirin (=81 mg qDay), during the first 3 months of treatment are contraindicated.

            Serious - Use Alternative (46)

            • abametapir

              abametapir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

            • antithrombin alfa

              antithrombin alfa, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • antithrombin III

              antithrombin III, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • apalutamide

              apalutamide will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • apixaban

              cilostazol and apixaban both increase anticoagulation. Avoid or Use Alternate Drug.

            • argatroban

              argatroban, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • aspirin rectal

              aspirin rectal increases effects of cilostazol by pharmacodynamic synergism. Avoid or Use Alternate Drug. Enhanced risk of hemorrhage.

            • bivalirudin

              bivalirudin, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • caplacizumab

              caplacizumab, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug.

            • carbamazepine

              carbamazepine will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ceritinib

              ceritinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • cimetidine

              cimetidine will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • clarithromycin

              clarithromycin will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • dalteparin

              dalteparin, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • enoxaparin

              enoxaparin, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • enzalutamide

              enzalutamide will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erythromycin base

              erythromycin base will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Dose reduction to 50 mg twice daily should be considered

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Dose reduction to 50 mg twice daily should be considered

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Dose reduction to 50 mg twice daily should be considered

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Dose reduction to 50 mg twice daily should be considered

            • esomeprazole

              esomeprazole increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; 3,4-dehydrocilostazol, an active metabolite, increased by 69% as a result of omeprazole inhibition of CYP2C19.

            • fexinidazole

              fexinidazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • fluconazole

              fluconazole increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; serum levels of 3,4-dehydrocilostazol (active metabolite) increased by strong CYP2C19 inhibitors.

            • fluvoxamine

              fluvoxamine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; serum levels of 3,4-dehydrocilostazole (active metabolite) increased by strong CYP2C19 inhibitors.

            • fondaparinux

              fondaparinux, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • gemfibrozil

              gemfibrozil increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; serum levels of 3,4-dehydrocilostazol (active metabolite) increased by strong CYP2C19 inhibitors.

            • heparin

              heparin, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • idelalisib

              idelalisib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • isoniazid

              isoniazid increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; serum levels of 3,4-dehydrocilostazol (active metabolite) increased by strong CYP2C19 inhibitors.

            • ivosidenib

              ivosidenib will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternate therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

            • ketoconazole

              ketoconazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Dose reduction to 50 mg twice daily should be considered

            • levoketoconazole

              levoketoconazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Dose reduction to 50 mg twice daily should be considered

            • lonafarnib

              lonafarnib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

            • lopinavir

              lopinavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • mifepristone

              mifepristone will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • modafinil

              modafinil increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; serum levels of 3,4-dehydrocilostazol (active metabolite) increased by strong CYP2C19 inhibitors.

            • nefazodone

              nefazodone will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • omeprazole

              omeprazole will increase the level or effect of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug.

            • protamine

              protamine, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Enhanced risk of hemorrhage.

            • rifabutin

              rifabutin will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • rifampin

              rifampin will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • saquinavir

              saquinavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • St John's Wort

              St John's Wort will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ticlopidine

              ticlopidine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; serum levels of 3,4-dehydrocilostazol (active metabolite) increased by strong CYP2C19 inhibitors.

            • tucatinib

              tucatinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • voxelotor

              voxelotor will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            Monitor Closely (119)

            • amobarbital

              amobarbital will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • anagrelide

              anagrelide, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor.

            • aprepitant

              aprepitant will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • armodafinil

              armodafinil will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              armodafinil increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • artemether/lumefantrine

              artemether/lumefantrine will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • aspirin

              aspirin, cilostazol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. The need for simultaneous use of low-dose aspirin and anticoagulant or antiplatelet agents are common for patients with cardiovascular disease; monitor closely.

            • aspirin/citric acid/sodium bicarbonate

              aspirin/citric acid/sodium bicarbonate, cilostazol. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. The need for simultaneous use of low-dose aspirin and anticoagulant or antiplatelet agents are common for patients with cardiovascular disease; monitor closely.

            • atazanavir

              atazanavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • azficel-T

              azficel-T, cilostazol. Other (see comment). Use Caution/Monitor. Comment: Coadministration with anticoagulants or antiplatelets may increase bruising or bleeding at biopsy and/or injection sites; concomitant use not recommended. Decisions regarding continued use or cessation of anticoagulants or antiplatelets should be made by a physician.

            • belzutifan

              belzutifan will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

            • betrixaban

              cilostazol, betrixaban. Either increases levels of the other by anticoagulation. Use Caution/Monitor.

            • bortezomib

              bortezomib increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • bosentan

              bosentan will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • budesonide

              budesonide will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • butabarbital

              butabarbital will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • butalbital

              butalbital will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • cimetidine

              cimetidine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • citalopram

              citalopram increases effects of cilostazol by pharmacodynamic synergism. Use Caution/Monitor. Combination may increase risk of bleeding.

            • cobicistat

              cobicistat will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce cilostazol dose to 50 mg twice daily when administered concomitantly; monitor for increase in cilostazole related adverse effects.

            • conivaptan

              conivaptan will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • cortisone

              cortisone will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • crizotinib

              crizotinib increases levels of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A.

            • crofelemer

              crofelemer increases levels of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • cyclosporine

              cyclosporine will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dabigatran

              dabigatran, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Both drugs have the potential to cause bleeding. Concomitant use may increase risk of bleeding.

            • dabrafenib

              dabrafenib will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • darifenacin

              darifenacin will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • darunavir

              darunavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dasatinib

              dasatinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • deferasirox

              deferasirox will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dexamethasone

              dexamethasone will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • DHEA, herbal

              DHEA, herbal will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • diltiazem

              diltiazem will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Consider reducing cilostazol dose to 50 mg PO BID when administered with diltiazem.

            • dronedarone

              dronedarone will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • duvelisib

              duvelisib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. will increase the level or effect of

            • efavirenz

              efavirenz will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              efavirenz increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • elagolix

              elagolix will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.

            • encorafenib

              encorafenib, cilostazol. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • etravirine

              etravirine will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              etravirine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • fedratinib

              fedratinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

            • fish oil

              fish oil, cilostazol. Other (see comment). Use Caution/Monitor. Comment: Patients taking fish oil and an anticoagulant or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding. .

            • fish oil triglycerides

              fish oil triglycerides will increase the level or effect of cilostazol by anticoagulation. Use Caution/Monitor. Prolonged bleeding reported in patients taking antiplatelet agents or anticoagulants and oral omega-3 fatty acids. Periodically monitor bleeding time in patients receiving fish oil triglycerides and concomitant antiplatelet agents or anticoagulants.

            • fluconazole

              fluconazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction to 50 mg twice daily should be considered

            • fludrocortisone

              fludrocortisone will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fluoxetine

              fluoxetine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • fluvoxamine

              fluvoxamine will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosamprenavir

              fosamprenavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • fosphenytoin

              fosphenytoin will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • grapefruit

              grapefruit will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • green tea

              green tea increases effects of cilostazol by pharmacodynamic synergism. Use Caution/Monitor. (Theoretical interaction). Combination may increase risk of bleeding.

            • griseofulvin

              griseofulvin will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • hydrocortisone

              hydrocortisone will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ibrutinib

              ibrutinib will increase the level or effect of cilostazol by anticoagulation. Use Caution/Monitor. Ibrutinib may increase the risk of hemorrhage in patients receiving antiplatelet or anticoagulant therapies and monitor for signs of bleeding.

            • icosapent

              icosapent, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Icosapent may prolong bleeding time; monitor periodically if coadministered with other drugs that affect bleeding.

            • iloperidone

              iloperidone increases levels of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • indinavir

              indinavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • isoniazid

              isoniazid will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

            • itraconazole

              itraconazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Consider a dose reduction to 50 mg BID in patient who are concurrenlt receiving strong CYP3A4 inhibitors.

            • ketoconazole

              ketoconazole increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite); dose reduction to 50 mg twice daily should be considered.

            • lapatinib

              lapatinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • letermovir

              letermovir increases levels of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • levoketoconazole

              levoketoconazole increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite); dose reduction to 50 mg twice daily should be considered.

            • lomitapide

              cilostazol increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.

            • loratadine

              loratadine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • lorlatinib

              lorlatinib will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • lumefantrine

              lumefantrine will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • marijuana

              marijuana will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • melatonin

              melatonin increases effects of cilostazol by anticoagulation. Use Caution/Monitor. Melatonin may decrease prothrombin time.

            • methylprednisolone

              methylprednisolone will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • metronidazole

              metronidazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • miconazole vaginal

              miconazole vaginal will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • milrinone

              milrinone, cilostazol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor.

            • mitotane

              mitotane decreases levels of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • nelfinavir

              nelfinavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nevirapine

              nevirapine will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nicardipine

              nicardipine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • nifedipine

              nifedipine will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • nilotinib

              nilotinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • omega 3 carboxylic acids

              omega 3 carboxylic acids, cilostazol. Other (see comment). Use Caution/Monitor. Comment: Patients taking omega-3 acids and an anticoagulant or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding.

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • pantoprazole

              pantoprazole increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • pentobarbital

              pentobarbital will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenobarbital

              phenobarbital will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • phenytoin

              phenytoin will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • piracetam

              piracetam increases effects of cilostazol by pharmacodynamic synergism. Use Caution/Monitor.

            • porfimer

              cilostazol decreases effects of porfimer by pharmacodynamic antagonism. Use Caution/Monitor.

            • posaconazole

              posaconazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • prednisone

              prednisone will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • primidone

              primidone will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • propofol

              propofol increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • quinupristin/dalfopristin

              quinupristin/dalfopristin will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rabeprazole

              rabeprazole increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • ribociclib

              ribociclib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • rifapentine

              rifapentine will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • riociguat

              riociguat, cilostazol. Either increases toxicity of the other by additive vasodilation. Modify Therapy/Monitor Closely. Riociguat is contraindicated with specific PDE-5 inhibitors (eg sildenafil, tadalafil, vardenafil) and nonspecific PDE-5 inhibitors (eg theophylline, dipyridamole) due to risk of hypotension; data are limited with other PDE inhibitors (eg, milrinone, cilostazol, roflumilast).

            • ritonavir

              ritonavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rivaroxaban

              rivaroxaban, cilostazol. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Avoid concurrent use of rivaroxaban with other anticoagulants due to increased bleeding risk other than during therapeutic transition periods where patients should be observed closely. Monitor for signs/symptoms of blood loss.

            • rucaparib

              rucaparib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

            • rufinamide

              rufinamide will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • secobarbital

              secobarbital will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • selumetinib

              cilostazol and selumetinib both increase anticoagulation. Modify Therapy/Monitor Closely. An increased risk of bleeding may occur in patients taking a vitamin-K antagonist or an antiplatelet agent with selumetinib. Monitor for bleeding and INR or PT in patients coadministered a vitamin-K antagonist or an antiplatelet agent with selumetinib.

            • sertraline

              sertraline increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • stiripentol

              stiripentol, cilostazol. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

            • tazemetostat

              tazemetostat will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tecovirimat

              tecovirimat will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • ticagrelor

              ticagrelor, cilostazol. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Increased risk of bleeding during concomitant use of medications that increase potential for bleeding.

            • tipranavir

              tipranavir will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • topiramate

              topiramate will decrease the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tranylcypromine

              tranylcypromine increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider decreasing cilostazol dose; moderate CYP2C19 inhibitors may increase serum levels of 3,4-dehydrocilostazol (active metabolite).

            • verapamil

              verapamil will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Consider decreasing the cilostazol dose to 50 mg twice a day.

            • vorapaxar

              cilostazol, vorapaxar. Either increases effects of the other by anticoagulation. Use Caution/Monitor. Coadministration of anticoagulants, antiplatelets, or other drug affecting coagulation should be monitored periodically due to potential increased risk of bleeding.

            • voriconazole

              voriconazole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • vortioxetine

              cilostazol, vortioxetine. Either increases effects of the other by anticoagulation. Use Caution/Monitor.

            • warfarin

              cilostazol, warfarin. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Drugs with antiplatelet properties may increase anticoagulation effect of warfarin.

            • zafirlukast

              zafirlukast will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            Minor (18)

            • acetazolamide

              acetazolamide will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • anastrozole

              anastrozole will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • cigarette smoking

              cigarette smoking decreases levels of cilostazol by increasing metabolism. Minor/Significance Unknown.

            • clozapine

              clozapine increases levels of cilostazol by decreasing metabolism. Minor/Significance Unknown.

            • cyclophosphamide

              cyclophosphamide will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • devil's claw

              devil's claw, cilostazol. pharmacodynamic synergism. Minor/Significance Unknown. May prolong bleeding time. Conflicting evidence.ÿ Use with caution.

            • ginger

              ginger, cilostazol. pharmacodynamic synergism. Minor/Significance Unknown. May prolong bleeding time. Conflicting evidence. Use with caution.

            • ginkgo biloba

              ginkgo biloba, cilostazol. pharmacodynamic synergism. Minor/Significance Unknown. May prolong bleeding time. Conflicting evidence.ÿ Use with caution.

            • horse chestnut seed

              horse chestnut seed, cilostazol. pharmacodynamic synergism. Minor/Significance Unknown. May prolong bleeding time. Theoretical. Use with caution.

            • larotrectinib

              larotrectinib will increase the level or effect of cilostazol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • lopinavir

              lopinavir increases levels of cilostazol by decreasing metabolism. Minor/Significance Unknown.

            • midazolam

              midazolam increases levels of cilostazol by decreasing metabolism. Minor/Significance Unknown.

            • saquinavir

              saquinavir increases levels of cilostazol by decreasing metabolism. Minor/Significance Unknown.

            • smoking

              smoking decreases levels of cilostazol by increasing metabolism. Minor/Significance Unknown.

            • theophylline

              theophylline increases levels of cilostazol by decreasing metabolism. Minor/Significance Unknown.

            • tobacco use

              tobacco use decreases levels of cilostazol by increasing metabolism. Minor/Significance Unknown.

            • triazolam

              triazolam increases levels of cilostazol by decreasing metabolism. Minor/Significance Unknown.

            • verteporfin

              cilostazol decreases effects of verteporfin by pharmacodynamic antagonism. Minor/Significance Unknown.

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            Adverse Effects

            >10%

            Headache (27-34%)

            Diarrhea (12-19%)

            Abnormal stools (12-15%)

            Infection (10-14%)

            Rhinitis (7-12%)

            Pharyngitis (7-10%)

            1-10%

            Dizziness (9-10%)

            Palpitations (5-10%)

            Peripheral edema (7-9%)

            Back pain (6-7%)

            Dyspepsia (6%)

            Abdominal pain (4-5%)

            Tachycardia (4%)

            Increased cough (3-4%)

            Myalgia (2-3%)

            Atrial fibrillation (<2%)

            CHF (<2%)

            MI (<2%)

            Hematemesis (<2%)

            Ecchymosis (<2%)

            Blood in eye (<2%)

            Epistaxis (<2%)

            Hemoptysis (<2%)

            Nausea

            Frequency Not Defined

            Decreased platelet aggregation

            Agranulocytosis

            Aplastic anemia

            Leukopenia

            Thrombocytopenia

            Stevens-Johnson syndrome

            Postmarketing Reports

            Blood and lymphatic system disorders: Agranulocytosis, aplastic anemia, granulocytopenia, thrombocytopenia, leukopenia, bleeding tendency

            Cardiovascular: Torsades de pointes, QTc prolongation, left ventricular outflow tract obstruction

            GI: GI hemorrhage

            General: Pain, chest pain, hot flushes, extradural or subdural hematoma, hyperglycemia, hyperuricemia, increased BUN, elevated BP, decreased platelet or white blood cell (WBC) count

            Hepatic: Hepatic dysfunction, abnormal liver function tests, jaundice

            Neurologic: Intracranial or cerebral hemorrhage, cerebrovascular accident (CVA)

            Respiratory: Pulmonary hemorrhage, interstitial pneumonia

            Skin: Subcutaneous hemorrhage, pruritus, skin eruptions such as Stevens-Johnson syndrome, skin drug eruption (dermatitis medicamentosa)

            Vascular: Subacute thrombosis

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            Warnings

            Black Box Warnings

            Cilostazol and metabolites are inhibitors of phosphodiesterase III; such activity has been shown to decrease survival of patients with class III-IV CHF; contraindicated in patients with CHF of any severity

            Contraindications

            Congestive heart failure of any severity

            Hypersensitivity

            Cautions

            Use with caution in liver and renal disease

            Leukopenia that progresses to agranulocytosis may occur (in which case, discontinue therapy); monitor white blood cell counts periodically

            Discontinue therapy if thrombocytopenia occurs; monitor platelets periodically

            Use with caution in patients taking platelet aggregation inhibitors

            Avoid use in patients with hemostatic disorders or active pathologic bleeding (eg, bleeding peptic ulcer, intracranial bleeding) due to reversible platelet aggregation

            Do not administer for at least 4-6 half-lives before elective surgical procedures

            Avoid grapefruit juice

            Response may be seen as early as 2-4 weeks after initiation, but treatment may be needed for up to 12 weeks

            Left ventricular outflow tract obstruction reported in patients with sigmoid shaped interventricular septum; monitor patients for development of new systolic murmur or cardiac symptoms after initiating therapy

            Dosage can be reduced or discontinued without rebound effects (eg, platelet hyperaggregability)

            Cilostazol may induce tachycardia, palpitation, tachyarrhythmia and/or hypotension; patients with history of ischemic heart disease may be at risk for exacerbations of angina pectoris or myocardial infarction

            Plasma concentrations and overall pharmacological activity are increased when cilostazol is administered with strong or moderate CYP3A4 inhibitors (eg, ketoconazole, itraconazole, erythromycin, diltiazem) and strong CYP2C19 inhibitors (eg, ticlopidine, fluconazole, omeprazole); dose reduction to 50 mg twice daily should be considered

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Excretion in milk unknown; not recommended

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Inhibits phosphodiesterase III, causing cyclic adenosine monophosphate (cAMP) to increase, which in turn inhibits platelet aggregation; causes homogeneous vasodilation, especially in femoral vascular beds

            Absorption

            Onset: 2-12 weeks

            Distribution

            Protein bound: 95-98% (especially albumin)

            Metabolism

            Metabolized by CYP3A4 (major), CYP2C19

            Metabolites: 4'-trans-hydroxy-cilostazol, 3,4-dehydro-cilostazol

            Elimination

            Half-life: 11-13 hr

            Dialyzable: No

            Excretion: Urine (74%), feces (20%)

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            cilostazol oral
            -
            100 mg tablet
            cilostazol oral
            -
            50 mg tablet
            cilostazol oral
            -
            100 mg tablet
            cilostazol oral
            -
            50 mg tablet
            cilostazol oral
            -
            100 mg tablet
            cilostazol oral
            -
            100 mg tablet
            cilostazol oral
            -
            50 mg tablet
            cilostazol oral
            -
            100 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

            FormularyPatient Discounts

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            Tier Description
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.