Identification

Name
Cilostazol
Accession Number
DB01166  (APRD00155)
Type
Small Molecule
Groups
Approved
Description

Cilostazol is a medication used in the alleviation of the symptom of intermittent claudication in individuals with peripheral vascular disease. It is manufactured by Otsuka Pharmaceutical Co. under the trade name Pletal. Although drugs similar to cilostazol have increased the risk of death in patients with congestive heart failure, studies of significant size have not addressed people without the disease. [Wikipedia]

Structure
Thumb
Synonyms
  • 3,4-dihydro-6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinone
  • 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone
  • 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydrocarbostyril
  • 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-1H-quinolin-2-one
  • Cilostazole
  • Cilostazolum
External IDs
OPC-13013 / OPC-21
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PletalTablet100 mg/1OralOtsuka Pharmaceutical Co., Ltd.1999-01-152016-06-30Us
PletalTablet50 mg/1OralOtsuka Pharmaceutical Co., Ltd.1999-01-152017-11-30Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CilostazolTablet100 mg/1OralGolden State Medical Supply2011-10-18Not applicableUs
CilostazolTablet50 mg/1OralBio Key, Inc.2014-04-01Not applicableUs
CilostazolTablet100 mg/1OralAvera Mc Kennan Hospital2015-04-01Not applicableUs
CilostazolTablet50 mg/1OralEon Labs, Inc.2005-11-08Not applicableUs00185 0123 60 nlmimage10 714438b1
CilostazolTablet50 mg/1OralNucare Pharmaceuticals, Inc.2012-04-24Not applicableUs
CilostazolTablet100 mg/1OralTeva2012-10-24Not applicableUs
CilostazolTablet100 mg/1OralPhysicians Total Care, Inc.2005-09-09Not applicableUs
CilostazolTablet50 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-06-26Not applicableUs00093 2065 06 nlmimage10 8b27c5ee
CilostazolTablet100 mg/1OralCarilion Materials Management2005-05-17Not applicableUs00054 0044 21 nlmimage10 c83fe45f
CilostazolTablet50 mg/1OralGolden State Medical Supply2011-10-18Not applicableUs
International/Other Brands
Pletaal
Categories
UNII
N7Z035406B
CAS number
73963-72-1
Weight
Average: 369.4607
Monoisotopic: 369.216475133
Chemical Formula
C20H27N5O2
InChI Key
RRGUKTPIGVIEKM-UHFFFAOYSA-N
InChI
InChI=1S/C20H27N5O2/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16/h10-11,14,16H,1-9,12-13H2,(H,21,26)
IUPAC Name
6-[4-(1-cyclohexyl-1H-1,2,3,4-tetrazol-5-yl)butoxy]-1,2,3,4-tetrahydroquinolin-2-one
SMILES
O=C1CCC2=C(N1)C=CC(OCCCCC1=NN=NN1C1CCCCC1)=C2

Pharmacology

Indication

For the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).

Structured Indications
Pharmacodynamics

Cilostazol is a quinolinone derivative indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs.

Mechanism of action

Cilostazol and several of its metabolites are cyclic AMP (cAMP) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.

TargetActionsOrganism
AcGMP-inhibited 3',5'-cyclic phosphodiesterase A
inhibitor
Human
Absorption

Cilostazol is absorbed after oral administration. A high fat meal increases absorption, with an approximately 90% increase in Cmax and a 25% increase in AUC. Absolute bioavailability is not known.

Volume of distribution
Not Available
Protein binding

95-98%

Metabolism

Hepatic. Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Two metabolites are active, with one metabolite appearing to account for at least 50% of the pharmacologic (PDE III inhibition) activity after administration of cilostazol.

Route of elimination

Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Cilostazol is eliminated predominately by metabolism and subsequent urinary excretion of metabolites. The primary route of elimination was via the urine (74%), with the remainder excreted in feces (20%). No measurable amount of unchanged cilostazol was excreted in the urine, and less than 2% of the dose was excreted as 3,4-dehydro-cilostazol. About 30% of the dose was excreted in urine as 4'-trans-hydroxy-cilostazol.

Half life

11-13 hours.

Clearance
Not Available
Toxicity

Information on acute overdosage with cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The oral LD50 of cilostazol is >5.0 g/kg in mice and rats and >2.0 g/kg in dogs.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Cilostazol Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabCilostazol may increase the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Cilostazol can be increased when it is combined with Abiraterone.Approved
AcenocoumarolCilostazol may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Cilostazol is combined with Acetylsalicylic acid.Approved, Vet Approved
AloxiprinThe risk or severity of adverse effects can be increased when Cilostazol is combined with Aloxiprin.Experimental
AlprostadilAlprostadil may increase the anticoagulant activities of Cilostazol.Approved, Investigational
AlteplaseCilostazol may increase the anticoagulant activities of Alteplase.Approved
ALX-0081Cilostazol may increase the anticoagulant activities of ALX-0081.Investigational
AminophenazoneThe serum concentration of Cilostazol can be increased when it is combined with Aminophenazone.Approved, Withdrawn
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Cilostazol is combined with Aminosalicylic Acid.Approved
AmiodaroneThe serum concentration of Cilostazol can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Cilostazol can be increased when it is combined with Amitriptyline.Approved
AmprenavirThe serum concentration of Cilostazol can be increased when it is combined with Amprenavir.Approved
AnagrelideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Cilostazol.Approved
AncrodCilostazol may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideAndrographolide may increase the anticoagulant activities of Cilostazol.Investigational
AnistreplaseCilostazol may increase the anticoagulant activities of Anistreplase.Approved
AntipyrineThe serum concentration of Cilostazol can be increased when it is combined with Antipyrine.Approved
Antithrombin III humanCilostazol may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Cilostazol is combined with Apixaban.Approved
AprepitantThe serum concentration of Cilostazol can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe therapeutic efficacy of Cilostazol can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinCilostazol may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanCilostazol may increase the anticoagulant activities of Argatroban.Approved, Investigational
ArmodafinilThe serum concentration of Cilostazol can be increased when it is combined with Armodafinil.Approved, Investigational
ArtemetherThe metabolism of Cilostazol can be decreased when combined with Artemether.Approved
AstaxanthinCilostazol may increase the anticoagulant activities of Astaxanthin.Investigational
AtazanavirThe serum concentration of Cilostazol can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Cilostazol can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Cilostazol can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Cilostazol can be increased when it is combined with Azelastine.Approved
AzithromycinThe metabolism of Cilostazol can be decreased when combined with Azithromycin.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Cilostazol is combined with Balsalazide.Approved, Investigational
BatroxobinCilostazol may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminCilostazol may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinCilostazol may increase the anticoagulant activities of Bemiparin.Approved
BenzbromaroneThe serum concentration of Cilostazol can be increased when it is combined with Benzbromarone.Investigational, Withdrawn
BeraprostCilostazol may increase the anticoagulant activities of Beraprost.Investigational
BetaxololThe metabolism of Cilostazol can be decreased when combined with Betaxolol.Approved
BicalutamideThe serum concentration of Cilostazol can be increased when it is combined with Bicalutamide.Approved
BifonazoleThe serum concentration of Cilostazol can be increased when it is combined with Bifonazole.Approved
BivalirudinCilostazol may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BoceprevirThe serum concentration of Cilostazol can be increased when it is combined with Boceprevir.Withdrawn
BortezomibThe serum concentration of Cilostazol can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Cilostazol can be decreased when it is combined with Bosentan.Approved, Investigational
BrinaseCilostazol may increase the anticoagulant activities of Brinase.Experimental
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Cilostazol.Approved, Investigational
BuflomedilBuflomedil may increase the anticoagulant activities of Cilostazol.Experimental
BuprenorphineThe serum concentration of Cilostazol can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Cilostazol can be decreased when combined with Bupropion.Approved
ButylphthalideButylphthalide may increase the anticoagulant activities of Cilostazol.Investigational
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Cilostazol.Approved
CaffeineThe metabolism of Cilostazol can be decreased when combined with Caffeine.Approved
CangrelorCilostazol may increase the anticoagulant activities of Cangrelor.Approved
CarbamazepineThe serum concentration of Cilostazol can be increased when it is combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Cilostazol is combined with Carbaspirin calcium.Experimental
CelecoxibThe metabolism of Cilostazol can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Cilostazol can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cilostazol can be increased when it is combined with Cerivastatin.Withdrawn
CertoparinCilostazol may increase the anticoagulant activities of Certoparin.Approved
ChloramphenicolThe serum concentration of Cilostazol can be increased when it is combined with Chloramphenicol.Approved, Vet Approved
ChloroquineThe metabolism of Cilostazol can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe metabolism of Cilostazol can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe serum concentration of Cilostazol can be increased when it is combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe serum concentration of Cilostazol can be increased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Cilostazol can be decreased when combined with Cinacalcet.Approved
CitalopramThe serum concentration of Cilostazol can be increased when it is combined with Citalopram.Approved
Citric AcidCilostazol may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClarithromycinThe serum concentration of Cilostazol can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Cilostazol can be increased when it is combined with Clemastine.Approved
ClevidipineThe serum concentration of Cilostazol can be increased when it is combined with Clevidipine.Approved
ClobazamThe metabolism of Cilostazol can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Cilostazol can be decreased when combined with Clomipramine.Approved, Vet Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Cilostazol.Approved, Nutraceutical
CloricromenCilostazol may increase the anticoagulant activities of Cloricromen.Experimental
ClorindioneCilostazol may increase the anticoagulant activities of Clorindione.Experimental
ClotrimazoleThe serum concentration of Cilostazol can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Cilostazol can be increased when it is combined with Clozapine.Approved
CobicistatThe serum concentration of Cilostazol can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Cilostazol can be decreased when combined with Cocaine.Approved, Illicit
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Cilostazol is combined with Collagenase clostridium histolyticum.Approved, Investigational
CrizotinibThe serum concentration of Cilostazol can be increased when it is combined with Crizotinib.Approved
CyclosporineThe serum concentration of Cilostazol can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Cilostazol can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateCilostazol may increase the anticoagulant activities of Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Cilostazol can be decreased when it is combined with Dabrafenib.Approved
DalteparinCilostazol may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidCilostazol may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanCilostazol may increase the anticoagulant activities of Darexaban.Investigational
DarifenacinThe metabolism of Cilostazol can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Cilostazol can be increased when it is combined with Darunavir.Approved
DasatinibDasatinib may increase the anticoagulant activities of Cilostazol.Approved, Investigational
DeferasiroxThe serum concentration of Cilostazol can be decreased when it is combined with Deferasirox.Approved, Investigational
DefibrotideCilostazol may increase the anticoagulant activities of Defibrotide.Approved, Investigational
DelavirdineThe serum concentration of Cilostazol can be increased when it is combined with Delavirdine.Approved
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Cilostazol is combined with Deoxycholic Acid.Approved
dersalazineThe risk or severity of adverse effects can be increased when Cilostazol is combined with dersalazine.Investigational
DesipramineThe serum concentration of Cilostazol can be increased when it is combined with Desipramine.Approved
DesirudinCilostazol may increase the anticoagulant activities of Desirudin.Approved
DesloratadineThe serum concentration of Cilostazol can be increased when it is combined with Desloratadine.Approved, Investigational
DesmoteplaseCilostazol may increase the anticoagulant activities of Desmoteplase.Investigational
DexfenfluramineThe serum concentration of Cilostazol can be increased when it is combined with Dexfenfluramine.Approved, Illicit, Withdrawn
DexlansoprazoleThe serum concentration of Cilostazol can be increased when it is combined with Dexlansoprazole.Approved
DextranCilostazol may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Cilostazol may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Cilostazol may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Cilostazol may increase the anticoagulant activities of Dextran 75.Approved
DiazepamThe serum concentration of Cilostazol can be increased when it is combined with Diazepam.Approved, Illicit, Vet Approved
DicoumarolCilostazol may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Cilostazol is combined with Diflunisal.Approved
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Cilostazol.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Cilostazol.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Cilostazol.Experimental
DihydroergotamineThe serum concentration of Cilostazol can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Cilostazol can be increased when it is combined with Diltiazem.Approved
Dimethyl sulfoxideThe serum concentration of Cilostazol can be increased when it is combined with Dimethyl sulfoxide.Approved, Vet Approved
DiphenadioneCilostazol may increase the anticoagulant activities of Diphenadione.Experimental
DiphenhydramineThe metabolism of Cilostazol can be decreased when combined with Diphenhydramine.Approved
DipyridamoleDipyridamole may increase the anticoagulant activities of Cilostazol.Approved
DitazoleCilostazol may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
DosulepinThe serum concentration of Cilostazol can be increased when it is combined with Dosulepin.Approved
DoxycyclineThe serum concentration of Cilostazol can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe serum concentration of Cilostazol can be increased when it is combined with Dronedarone.Approved
Drotrecogin alfaCilostazol may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
DuloxetineThe metabolism of Cilostazol can be decreased when combined with Duloxetine.Approved
Edetic AcidCilostazol may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanCilostazol may increase the anticoagulant activities of Edoxaban.Approved
EfavirenzThe serum concentration of Cilostazol can be increased when it is combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Cilostazol can be decreased when combined with Eliglustat.Approved
EnasidenibThe serum concentration of Cilostazol can be increased when it is combined with Enasidenib.Approved
EnoxaparinCilostazol may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe serum concentration of Cilostazol can be decreased when it is combined with Enzalutamide.Approved
EpinastineEpinastine may increase the anticoagulant activities of Cilostazol.Approved, Investigational
EplivanserinCilostazol may increase the anticoagulant activities of Eplivanserin.Investigational
eplivanserineCilostazol may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Cilostazol.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Cilostazol.Approved, Investigational
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Cilostazol.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Cilostazol.Approved
ErythromycinThe serum concentration of Cilostazol can be increased when it is combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Cilostazol can be increased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe serum concentration of Cilostazol can be increased when it is combined with Esomeprazole.Approved, Investigational
EthanolThe serum concentration of Cilostazol can be increased when it is combined with Ethanol.Approved
EthotoinThe serum concentration of Cilostazol can be increased when it is combined with Ethotoin.Approved
Ethyl biscoumacetateCilostazol may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtoricoxibThe serum concentration of Cilostazol can be increased when it is combined with Etoricoxib.Approved, Investigational
EtravirineThe serum concentration of Cilostazol can be increased when it is combined with Etravirine.Approved
FelbamateThe serum concentration of Cilostazol can be increased when it is combined with Felbamate.Approved
Ferulic acidCilostazol may increase the anticoagulant activities of Ferulic acid.Experimental
FibrinolysinCilostazol may increase the anticoagulant activities of Fibrinolysin.Investigational
FluconazoleThe serum concentration of Cilostazol can be increased when it is combined with Fluconazole.Approved
FluindioneCilostazol may increase the anticoagulant activities of Fluindione.Investigational
FluoxetineThe serum concentration of Cilostazol can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FluvastatinThe serum concentration of Cilostazol can be increased when it is combined with Fluvastatin.Approved
FluvoxamineThe serum concentration of Cilostazol can be increased when it is combined with Fluvoxamine.Approved, Investigational
FondaparinuxCilostazol may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumCilostazol may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FosamprenavirThe serum concentration of Cilostazol can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Cilostazol can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Cilostazol can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Cilostazol can be increased when it is combined with Fusidic Acid.Approved
GabexateCilostazol may increase the anticoagulant activities of Gabexate.Investigational
GefitinibThe serum concentration of Cilostazol can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilThe serum concentration of Cilostazol can be increased when it is combined with Gemfibrozil.Approved
GliclazideThe serum concentration of Cilostazol can be increased when it is combined with Gliclazide.Approved
GlucosamineGlucosamine may increase the antiplatelet activities of Cilostazol.Approved
GuacetisalThe risk or severity of adverse effects can be increased when Cilostazol is combined with Guacetisal.Experimental
HaloperidolThe metabolism of Cilostazol can be decreased when combined with Haloperidol.Approved
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Cilostazol is combined with Hemoglobin crosfumaril.Experimental
HeparinCilostazol may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineCilostazol may increase the anticoagulant activities of Higenamine.Investigational
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Cilostazol.Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Cilostazol is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Cilostazol.Approved
IbudilastIbudilast may increase the anticoagulant activities of Cilostazol.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Cilostazol.Approved, Nutraceutical
IdraparinuxCilostazol may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Cilostazol.Approved, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Cilostazol.Investigational
IloprostIloprost may increase the antiplatelet activities of Cilostazol.Approved, Investigational
ImatinibThe serum concentration of Cilostazol can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Cilostazol can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Cilostazol can be increased when it is combined with Indinavir.Approved
IndobufenCilostazol may increase the anticoagulant activities of Indobufen.Investigational
IndomethacinThe serum concentration of Cilostazol can be increased when it is combined with Indomethacin.Approved, Investigational
IsavuconazoniumThe serum concentration of Cilostazol can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsoniazidThe serum concentration of Cilostazol can be increased when it is combined with Isoniazid.Approved
IsradipineThe serum concentration of Cilostazol can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Cilostazol can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Cilostazol can be increased when it is combined with Ivacaftor.Approved
KetanserinKetanserin may increase the anticoagulant activities of Cilostazol.Investigational
KetoconazoleThe serum concentration of Cilostazol can be increased when it is combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Cilostazol can be increased when it is combined with Lansoprazole.Approved, Investigational
LepirudinCilostazol may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanCilostazol may increase the anticoagulant activities of Letaxaban.Investigational
LidocaineThe metabolism of Cilostazol can be decreased when combined with Lidocaine.Approved, Vet Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Cilostazol.Approved
LinsidomineLinsidomine may increase the anticoagulant activities of Cilostazol.Experimental
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Cilostazol.Approved
LobeglitazoneThe serum concentration of Cilostazol can be increased when it is combined with Lobeglitazone.Approved
LopinavirThe serum concentration of Cilostazol can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Cilostazol can be increased when it is combined with Loratadine.Approved
LorcaserinThe metabolism of Cilostazol can be decreased when combined with Lorcaserin.Approved
LosartanThe serum concentration of Cilostazol can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Cilostazol can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Cilostazol can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Cilostazol can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Cilostazol can be decreased when combined with Lumefantrine.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Cilostazol.Illicit, Withdrawn
ManidipineThe serum concentration of Cilostazol can be increased when it is combined with Manidipine.Approved
MelagatranCilostazol may increase the anticoagulant activities of Melagatran.Experimental
MemantineThe serum concentration of Cilostazol can be increased when it is combined with Memantine.Approved, Investigational
MephenytoinThe serum concentration of Cilostazol can be increased when it is combined with Mephenytoin.Investigational, Withdrawn
MesalazineThe risk or severity of adverse effects can be increased when Cilostazol is combined with Mesalazine.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Cilostazol.Experimental
MethadoneThe metabolism of Cilostazol can be decreased when combined with Methadone.Approved
MethazolamideThe serum concentration of Cilostazol can be increased when it is combined with Methazolamide.Approved
MethimazoleThe serum concentration of Cilostazol can be increased when it is combined with Methimazole.Approved
MethotrimeprazineThe metabolism of Cilostazol can be decreased when combined with Methotrimeprazine.Approved
MethsuximideThe serum concentration of Cilostazol can be increased when it is combined with Methsuximide.Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Cilostazol.Approved
MethylphenobarbitalThe serum concentration of Cilostazol can be increased when it is combined with Methylphenobarbital.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Cilostazol.Approved
MetoprololThe metabolism of Cilostazol can be decreased when combined with Metoprolol.Approved, Investigational
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Cilostazol.Experimental
MexiletineThe metabolism of Cilostazol can be decreased when combined with Mexiletine.Approved
MiconazoleThe serum concentration of Cilostazol can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidostaurinThe serum concentration of Cilostazol can be increased when it is combined with Midostaurin.Approved
MifepristoneThe serum concentration of Cilostazol can be increased when it is combined with Mifepristone.Approved, Investigational
MilrinoneMilrinone may increase the anticoagulant activities of Cilostazol.Approved
MirabegronThe metabolism of Cilostazol can be decreased when combined with Mirabegron.Approved
MitotaneThe serum concentration of Cilostazol can be decreased when it is combined with Mitotane.Approved
MoclobemideThe serum concentration of Cilostazol can be increased when it is combined with Moclobemide.Approved
ModafinilThe serum concentration of Cilostazol can be increased when it is combined with Modafinil.Approved, Investigational
NadroparinCilostazol may increase the anticoagulant activities of Nadroparin.Approved
NafamostatCilostazol may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Cilostazol.Investigational
NaloxegolThe serum concentration of Cilostazol can be increased when it is combined with Naloxegol.Approved
NefazodoneThe serum concentration of Cilostazol can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Cilostazol can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Cilostazol can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Cilostazol can be increased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Cilostazol can be increased when it is combined with Nicardipine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Cilostazol.Approved
NilotinibThe serum concentration of Cilostazol can be increased when it is combined with Nilotinib.Approved, Investigational
NilutamideThe serum concentration of Cilostazol can be increased when it is combined with Nilutamide.Approved
NilvadipineThe serum concentration of Cilostazol can be increased when it is combined with Nilvadipine.Approved
NimesulideNimesulide may increase the anticoagulant activities of Cilostazol.Approved, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Cilostazol is combined with Nitroaspirin.Investigational
ObinutuzumabThe risk or severity of adverse effects can be increased when Cilostazol is combined with Obinutuzumab.Approved
OlanzapineThe serum concentration of Cilostazol can be increased when it is combined with Olanzapine.Approved, Investigational
OlaparibThe serum concentration of Cilostazol can be increased when it is combined with Olaparib.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Cilostazol is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Cilostazol.Approved, Nutraceutical
OmeprazoleThe serum concentration of Cilostazol can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Cilostazol can be increased when it is combined with Osimertinib.Approved
OtamixabanCilostazol may increase the anticoagulant activities of Otamixaban.Investigational
OxcarbazepineThe serum concentration of Cilostazol can be increased when it is combined with Oxcarbazepine.Approved
OxymetholoneThe serum concentration of Cilostazol can be increased when it is combined with Oxymetholone.Approved, Illicit
OzagrelCilostazol may increase the anticoagulant activities of Ozagrel.Investigational
PalbociclibThe serum concentration of Cilostazol can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Cilostazol can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe serum concentration of Cilostazol can be increased when it is combined with Pantoprazole.Approved
ParnaparinCilostazol may increase the anticoagulant activities of Parnaparin.Approved
ParoxetineThe metabolism of Cilostazol can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Cilostazol can be decreased when it is combined with Peginterferon alfa-2b.Approved
PegvisomantThe serum concentration of Cilostazol can be increased when it is combined with Pegvisomant.Approved
PentobarbitalThe metabolism of Cilostazol can be increased when combined with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Cilostazol.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Cilostazol.Approved, Investigational
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Cilostazol.Approved, Vet Approved, Withdrawn
PhenelzineThe serum concentration of Cilostazol can be increased when it is combined with Phenelzine.Approved
PhenindioneCilostazol may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe metabolism of Cilostazol can be increased when combined with Phenobarbital.Approved
PhenprocoumonCilostazol may increase the anticoagulant activities of Phenprocoumon.Approved
PhensuximideThe serum concentration of Cilostazol can be increased when it is combined with Phensuximide.Approved
PhenytoinThe metabolism of Cilostazol can be increased when combined with Phenytoin.Approved, Vet Approved
PicotamideCilostazol may increase the anticoagulant activities of Picotamide.Experimental
PimozideThe serum concentration of Cilostazol can be increased when it is combined with Pimozide.Approved
PioglitazoneThe serum concentration of Cilostazol can be increased when it is combined with Pioglitazone.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Cilostazol.Approved
PosaconazoleThe serum concentration of Cilostazol can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrasugrelCilostazol may increase the anticoagulant activities of Prasugrel.Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Cilostazol.Approved
PrimidoneThe metabolism of Cilostazol can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Cilostazol can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Cilostazol can be increased when it is combined with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Cilostazol can be decreased when combined with Promazine.Approved, Vet Approved
Protein CCilostazol may increase the anticoagulant activities of Protein C.Approved
Protein S humanCilostazol may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeCilostazol may increase the anticoagulant activities of Protocatechualdehyde.Approved
QuinidineThe metabolism of Cilostazol can be decreased when combined with Quinidine.Approved
QuinineThe serum concentration of Cilostazol can be increased when it is combined with Quinine.Approved
RabeprazoleThe serum concentration of Cilostazol can be increased when it is combined with Rabeprazole.Approved, Investigational
RamatrobanRamatroban may increase the anticoagulant activities of Cilostazol.Investigational
RanolazineThe serum concentration of Cilostazol can be increased when it is combined with Ranolazine.Approved, Investigational
RegorafenibThe serum concentration of Cilostazol can be increased when it is combined with Regorafenib.Approved
ResveratrolResveratrol may increase the anticoagulant activities of Cilostazol.Experimental, Investigational
ReteplaseCilostazol may increase the anticoagulant activities of Reteplase.Approved
ReviparinCilostazol may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Cilostazol.Approved
RifabutinThe metabolism of Cilostazol can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Cilostazol can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Cilostazol can be increased when combined with Rifapentine.Approved
RilpivirineThe serum concentration of Cilostazol can be increased when it is combined with Rilpivirine.Approved
RiociguatCilostazol may increase the hypotensive activities of Riociguat.Approved
RitonavirThe serum concentration of Cilostazol can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanCilostazol may increase the anticoagulant activities of Rivaroxaban.Approved
RolapitantThe metabolism of Cilostazol can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Cilostazol can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneThe serum concentration of Cilostazol can be increased when it is combined with Rosiglitazone.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Cilostazol.Approved
Salicylic acidThe risk or severity of adverse effects can be increased when Cilostazol is combined with Salicylic acid.Approved, Vet Approved
SaquinavirThe serum concentration of Cilostazol can be increased when it is combined with Saquinavir.Approved, Investigational
SarpogrelateCilostazol may increase the anticoagulant activities of Sarpogrelate.Investigational
SaruplaseCilostazol may increase the anticoagulant activities of Saruplase.Experimental
SelexipagCilostazol may increase the anticoagulant activities of Selexipag.Approved
SeratrodastThe serum concentration of Cilostazol can be increased when it is combined with Seratrodast.Approved
SertralineThe serum concentration of Cilostazol can be increased when it is combined with Sertraline.Approved
SevofluraneSevoflurane may increase the anticoagulant activities of Cilostazol.Approved, Vet Approved
SildenafilThe serum concentration of Cilostazol can be increased when it is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Cilostazol can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Cilostazol can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Cilostazol can be increased when it is combined with Simvastatin.Approved
SitaxentanThe serum concentration of Cilostazol can be increased when it is combined with Sitaxentan.Approved, Investigational, Withdrawn
SorafenibThe serum concentration of Cilostazol can be increased when it is combined with Sorafenib.Approved, Investigational
SRT501SRT501 may increase the anticoagulant activities of Cilostazol.Investigational
St. John's WortThe serum concentration of Cilostazol can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Cilostazol can be increased when it is combined with Stiripentol.Approved
StreptokinaseCilostazol may increase the anticoagulant activities of Streptokinase.Approved
SulfanilamideThe serum concentration of Cilostazol can be increased when it is combined with Sulfanilamide.Approved
SulfisoxazoleThe serum concentration of Cilostazol can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SulodexideCilostazol may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TelaprevirThe serum concentration of Cilostazol can be increased when it is combined with Telaprevir.Withdrawn
TelithromycinThe serum concentration of Cilostazol can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Cilostazol can be increased when it is combined with Telmisartan.Approved, Investigational
TenecteplaseCilostazol may increase the anticoagulant activities of Tenecteplase.Approved
Tenofovir disoproxilThe metabolism of Cilostazol can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Cilostazol can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Cilostazol.Experimental
TeriflunomideThe serum concentration of Cilostazol can be decreased when it is combined with Teriflunomide.Approved
TesmilifeneTesmilifene may increase the anticoagulant activities of Cilostazol.Investigational
ThalidomideThe serum concentration of Cilostazol can be increased when it is combined with Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Cilostazol can be decreased when combined with Theophylline.Approved
ThioridazineThe metabolism of Cilostazol can be decreased when combined with Thioridazine.Withdrawn
TicagrelorCilostazol may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineThe serum concentration of Cilostazol can be increased when it is combined with Ticlopidine.Approved
TinzaparinCilostazol may increase the anticoagulant activities of Tinzaparin.Approved
TioclomarolCilostazol may increase the anticoagulant activities of Tioclomarol.Experimental
TioconazoleThe serum concentration of Cilostazol can be increased when it is combined with Tioconazole.Approved
TipranavirThe serum concentration of Cilostazol can be increased when it is combined with Tipranavir.Approved, Investigational
TirofibanTirofiban may increase the anticoagulant activities of Cilostazol.Approved
TocilizumabThe serum concentration of Cilostazol can be decreased when it is combined with Tocilizumab.Approved
TopiramateThe serum concentration of Cilostazol can be increased when it is combined with Topiramate.Approved
TopiroxostatThe serum concentration of Cilostazol can be increased when it is combined with Topiroxostat.Approved
TorasemideThe serum concentration of Cilostazol can be increased when it is combined with Torasemide.Approved
TositumomabThe risk or severity of adverse effects can be increased when Cilostazol is combined with Tositumomab.Approved
TranilastTranilast may increase the anticoagulant activities of Cilostazol.Approved, Investigational
TranylcypromineThe serum concentration of Cilostazol can be increased when it is combined with Tranylcypromine.Approved
TrapidilTrapidil may increase the anticoagulant activities of Cilostazol.Approved
TreprostinilTreprostinil may increase the antiplatelet activities of Cilostazol.Approved, Investigational
TriflusalCilostazol may increase the anticoagulant activities of Triflusal.Approved
TroglitazoneThe serum concentration of Cilostazol can be increased when it is combined with Troglitazone.Withdrawn
TroleandomycinThe serum concentration of Cilostazol can be increased when it is combined with Troleandomycin.Approved
TroxerutinCilostazol may increase the anticoagulant activities of Troxerutin.Investigational
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Cilostazol.Experimental
UrokinaseCilostazol may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
ValdecoxibThe serum concentration of Cilostazol can be increased when it is combined with Valdecoxib.Investigational, Withdrawn
Valproic AcidThe serum concentration of Cilostazol can be increased when it is combined with Valproic Acid.Approved, Investigational
VemurafenibThe serum concentration of Cilostazol can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Cilostazol can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Cilostazol can be increased when it is combined with Verapamil.Approved
VismodegibThe serum concentration of Cilostazol can be increased when it is combined with Vismodegib.Approved
Vitamin EVitamin E may increase the antiplatelet activities of Cilostazol.Approved, Nutraceutical, Vet Approved
VorapaxarCilostazol may increase the anticoagulant activities of Vorapaxar.Approved
VoriconazoleThe serum concentration of Cilostazol can be increased when it is combined with Voriconazole.Approved, Investigational
WarfarinThe serum concentration of Cilostazol can be increased when it is combined with Warfarin.Approved
XimelagatranCilostazol may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
ZafirlukastThe serum concentration of Cilostazol can be increased when it is combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe serum concentration of Cilostazol can be increased when it is combined with Ziprasidone.Approved
ZonisamideThe serum concentration of Cilostazol can be increased when it is combined with Zonisamide.Approved, Investigational
ZucapsaicinThe serum concentration of Cilostazol can be increased when it is combined with Zucapsaicin.Approved
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment, grapefruit can significantly increase serum levels of this product.
  • Take on an empty stomach, a lipid rich meal will increase absorption.

References

Synthesis Reference

Marioara Mendelovici, "Processes for preparing cilostazol." U.S. Patent US20020099213, issued July 25, 2002.

US20020099213
General References
Not Available
External Links
Human Metabolome Database
HMDB15297
KEGG Drug
D01896
PubChem Compound
2754
PubChem Substance
46506317
ChemSpider
2652
BindingDB
50070490
ChEBI
31401
ChEMBL
CHEMBL799
Therapeutic Targets Database
DAP000191
PharmGKB
PA164746334
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cilostazol
ATC Codes
B01AC23 — Cilostazol
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Download (35.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceMigraine With Aura / Strokes1
1CompletedNot AvailableHealthy Volunteers3
1CompletedNot AvailableTherapeutic Equivalency, Healthy1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceTherapeutic Equivalency1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentIntermittent Claudication1
1CompletedTreatmentPain1
1RecruitingTreatmentDyslipidemias / Peripheral Artery Disease (PAD)1
1RecruitingTreatmentHealthy Volunteers1
2CompletedBasic ScienceContraception1
2CompletedTreatmentIntermittent Claudication1
2RecruitingPreventionCerebral Small Vessels Disease / Cognitive Impairments / Strokes1
2RecruitingTreatmentMild Cognitive Impairment (MCI)1
2Unknown StatusTreatmentPeripheral Artery Disease (PAD)1
3CompletedPreventionCerebral Infarctions2
3CompletedTreatmentCerebrovascular Disorders1
3CompletedTreatmentCoronary Artery Disease1
3CompletedTreatmentVasospastic Angina2
3RecruitingPreventionNoncardioembolic Cerebral Infarction1
3RecruitingPreventionPeripheral Arterial Disease (PAD)1
3Unknown StatusTreatmentAtherosclerosis / Cardiovascular Disease (CVD) / Peripheral Vascular Disease (PVD)1
3Unknown StatusTreatmentCoronary Artery Stenosis / High Post-Treatment Platelet Reactivity / Late Platelet Aggregation / Maximal Platelet Aggregation1
4Active Not RecruitingPreventionIntracranial Hemorrhages / Ischemia, Brain1
4Active Not RecruitingTreatmentCerebral Small Vessels Disease1
4Active Not RecruitingTreatmentClaudication (Finding) / Peripheral Arterial Disease (PAD)1
4Active Not RecruitingTreatmentIntracranial Hemorrhages / Ischemia, Brain1
4CompletedNot AvailableIntermittent Claudication / Peripheral Arterial Disease (PAD) / Peripheral Vascular Disease (PVD)1
4CompletedPreventionCerebral Infarctions1
4CompletedTreatmentAcute Coronary Syndromes (ACS)1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / Clopidogrel Low Responsiveness / Percutaneous Coronary Intervention1
4CompletedTreatmentAlzheimer Dementia (AD)1
4CompletedTreatmentArteriosclerosis Obliterans / Type 2 Diabetes Mellitus1
4CompletedTreatmentAtherosclerosis Cerebral Infarction1
4CompletedTreatmentAtherosclerosis / Cerebral Infarctions1
4CompletedTreatmentCardiovascular Disease (CVD)1
4CompletedTreatmentCerebral Infarctions3
4CompletedTreatmentChronic Kidney Disease (CKD) / Stable Angina (SA)1
4CompletedTreatmentCoronary Artery Disease3
4CompletedTreatmentDementia, Vascular / Strokes1
4CompletedTreatmentDiabetes Complications / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetic Nephropathies1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHemodialysis Patients / Peripheral Vascular Disease (PVD)1
4CompletedTreatmentMyocardial Infarction (MI)1
4CompletedTreatmentPeripheral Arterial Disease (PAD)1
4CompletedTreatmentPolyneuropathies1
4CompletedTreatmentRaynaud's Disease2
4CompletedTreatmentStroke, Ischemic1
4Not Yet RecruitingPreventionType 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentCritical Limb Ischemia (CLI)1
4RecruitingHealth Services ResearchPeripheral Artery Disease (PAD) / Stroke, Ischemic / Type 2 Diabetes Mellitus1
4RecruitingTreatmentCoronary Artery Disease2
4RecruitingTreatmentSevere Hypercholesterolemia1
4TerminatedTreatmentCoronary Artery Disease1
4Unknown StatusPreventionArteriosclerosis Obliterans1
4Unknown StatusPreventionType 2 Diabetes Mellitus1
4Unknown StatusTreatmentAngioplasty, Transluminal, Percutaneous Coronary1
4Unknown StatusTreatmentMetabolic Syndromes / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableAPT(Antiplatelet Therapy) / HOTPR(High on Treat Platelet Reactivity) / PRU(Platelet Reactivity Unit)1
Not AvailableCompletedHealth Services ResearchDrug Interactions1
Not AvailableCompletedHealth Services ResearchMigraines1
Not AvailableCompletedTreatmentClopidogrel Non-Responsiveness1
Not AvailableCompletedTreatmentCoronary Heart Disease (CHD)1
Not AvailableCompletedTreatmentIntermittent Claudication2
Not AvailableCompletedTreatmentMigraines1
Not AvailableCompletedTreatmentTinnitus1
Not AvailableRecruitingNot AvailableMigraine Without Aura / Migrainous Headache1
Not AvailableUnknown StatusNot AvailableTreatment of Ischemic Symptom and Prevention of Recurrence of Cerebral Infarction1
Not AvailableUnknown StatusTreatmentMild Cognitive Impairment (MCI)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
TabletOral100 mg/1
TabletOral50 mg/1
Prices
Unit descriptionCostUnit
Pletal 100 mg tablet2.51USD tablet
Pletal 50 mg tablet2.39USD tablet
Cilostazol 100 mg tablet1.86USD tablet
Cilostazol 50 mg tablet1.86USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)160 °CPhysProp
logP2.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0324 mg/mLALOGPS
logP3.38ALOGPS
logP3.31ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)14.42ChemAxon
pKa (Strongest Basic)-0.51ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area81.93 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity117.13 m3·mol-1ChemAxon
Polarizability41.15 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9909
Caco-2 permeable-0.5666
P-glycoprotein substrateNon-substrate0.5361
P-glycoprotein inhibitor IInhibitor0.7886
P-glycoprotein inhibitor IIInhibitor0.8387
Renal organic cation transporterNon-inhibitor0.5794
CYP450 2C9 substrateNon-substrate0.7887
CYP450 2D6 substrateNon-substrate0.7734
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9486
Ames testNon AMES toxic0.5436
CarcinogenicityNon-carcinogens0.9085
BiodegradationNot ready biodegradable0.9636
Rat acute toxicity1.9002 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7518
hERG inhibition (predictor II)Non-inhibitor0.7075
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00dr-1698000000-05ddf5c1a046516bae11
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01t9-3920000000-86a7d65313952e9a8d3f

Taxonomy

Description
This compound belongs to the class of organic compounds known as hydroquinolones. These are compounds containing a hydrogenated quinoline bearing a ketone group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Quinolines and derivatives
Sub Class
Quinolones and derivatives
Direct Parent
Hydroquinolones
Alternative Parents
Hydroquinolines / Alkyl aryl ethers / Benzenoids / Tetrazoles / Heteroaromatic compounds / Secondary carboxylic acid amides / Lactams / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds
show 3 more
Substituents
Tetrahydroquinolone / Tetrahydroquinoline / Alkyl aryl ether / Benzenoid / Azole / Heteroaromatic compound / Tetrazole / Carboxamide group / Lactam / Secondary carboxylic acid amide
show 12 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tetrazoles, lactam (CHEBI:31401 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
Gene Name
PDE3A
Uniprot ID
Q14432
Uniprot Name
cGMP-inhibited 3',5'-cyclic phosphodiesterase A
Molecular Weight
124978.06 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Hong KW, Lee JH, Kima KY, Park SY, Lee WS: Cilostazol: therapeutic potential against focal cerebral ischemic damage. Curr Pharm Des. 2006;12(5):565-73. [PubMed:16472148 ]
  3. Schror K: The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9. [PubMed:12180353 ]
  4. Mokry J, Mokra D, Nosalova G, Beharkova M, Feherova Z: Influence of selective inhibitors of phosphodiesterase 3 and 4 on cough and airway reactivity. J Physiol Pharmacol. 2008 Dec;59 Suppl 6:473-82. [PubMed:19218671 ]
  5. Parkkonen J, Hasala H, Moilanen E, Giembycz MA, Kankaanranta H: Phosphodiesterase 4 inhibitors delay human eosinophil and neutrophil apoptosis in the absence and presence of salbutamol. Pulm Pharmacol Ther. 2008;21(3):499-506. doi: 10.1016/j.pupt.2007.11.003. Epub 2007 Nov 22. [PubMed:18282775 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. [PubMed:10702888 ]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. [PubMed:10702888 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. [PubMed:10702888 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. [PubMed:10702888 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. [PubMed:10702888 ]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. [PubMed:10702888 ]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:54