Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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.
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
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
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.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%)
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.
Formulary
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