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Identification
NameCilostazol
Accession NumberDB01166  (APRD00155)
TypeSmall Molecule
GroupsApproved
DescriptionCilostazol 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 Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PletalTablet100 mg/1OralOtsuka America Pharmaceutical, Inc.1999-01-152016-06-30Us
PletalTablet50 mg/1OralOtsuka America Pharmaceutical, Inc.1999-01-15Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CilostazolTablet100 mg/1OralLake Erie Medical DBA Quality Care Products LLC2011-10-18Not applicableUs
CilostazolTablet50 mg/1OralCorepharma LLC.2006-09-062016-10-13Us
CilostazolTablet50 mg/1OralEon Labs, Inc.2005-11-08Not applicableUs
CilostazolTablet100 mg/1OralGolden State Medical Supply, Inc.2011-10-18Not applicableUs
CilostazolTablet50 mg/1OralTeva Pharmaceuticals USA Inc2012-04-24Not applicableUs
CilostazolTablet100 mg/1OralPhysicians Total Care, Inc.2005-09-09Not applicableUs
CilostazolTablet50 mg/1OralAvera Mc Kennan Hospital2015-03-23Not applicableUs
CilostazolTablet100 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-03-23Not applicableUs
CilostazolTablet100 mg/1OralApotex Corp.2011-10-18Not applicableUs
CilostazolTablet50 mg/1OralAv Pak2016-10-18Not applicableUs
CilostazolTablet100 mg/1OralLake Erie Medical DBA Quality Care Products LLC2012-10-24Not applicableUs
CilostazolTablet100 mg/1OralCorepharma LLC.2006-09-062016-10-13Us
CilostazolTablet100 mg/1OralEon Labs, Inc.2004-11-23Not applicableUs
CilostazolTablet50 mg/1OralGolden State Medical Supply, Inc.2006-09-06Not applicableUs
CilostazolTablet50 mg/1OralCarilion Materials Management2005-05-17Not applicableUs
CilostazolTablet100 mg/1OralCardinal Health2011-10-18Not applicableUs
CilostazolTablet50 mg/1OralWest Ward Pharmaceuticals Corp.2005-05-17Not applicableUs
CilostazolTablet100 mg/1OralAv Pak2016-10-18Not applicableUs
CilostazolTablet100 mg/1OralSTAT Rx USA LLC2006-09-06Not applicableUs
CilostazolTablet50 mg/1Oralbryant ranch prepack2005-05-17Not applicableUs
CilostazolTablet50 mg/1OralBreckenridge Pharmaceutical, Inc.2009-09-28Not applicableUs
CilostazolTablet50 mg/1OralAmerican Health Packaging2014-07-30Not applicableUs
CilostazolTablet100 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-03-23Not applicableUs
CilostazolTablet100 mg/1OralGolden State Medical Supply, Inc.2006-09-06Not applicableUs
CilostazolTablet100 mg/1OralCarilion Materials Management2005-05-17Not applicableUs
CilostazolTablet100 mg/1OralWest Ward Pharmaceuticals Corp.2005-05-17Not applicableUs
CilostazolTablet50 mg/1OralCardinal Health2011-02-18Not applicableUs
CilostazolTablet50 mg/1OralBIOKEY INC.2014-04-012016-04-05Us
CilostazolTablet100 mg/1Oralbryant ranch prepack2004-11-23Not applicableUs
CilostazolTablet100 mg/1OralBio Key, Inc.2014-04-01Not applicableUs
CilostazolTablet100 mg/1OralBreckenridge Pharmaceutical, Inc.2009-09-28Not applicableUs
CilostazolTablet100 mg/1OralAvera Mc Kennan Hospital2015-04-01Not applicableUs
CilostazolTablet50 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-06-26Not applicableUs
CilostazolTablet50 mg/1OralApotex Corp.2011-10-18Not applicableUs
CilostazolTablet100 mg/1OralPreferred Pharmaceuticals, Inc.2014-07-28Not applicableUs
CilostazolTablet50 mg/1OralGolden State Medical Supply, Inc.2011-10-18Not applicableUs
CilostazolTablet100 mg/1OralTeva Pharmaceuticals USA Inc2012-10-24Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PletaalNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIN7Z035406B
CAS number73963-72-1
WeightAverage: 369.4607
Monoisotopic: 369.216475133
Chemical FormulaC20H27N5O2
InChI KeyRRGUKTPIGVIEKM-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
IndicationFor the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
Structured Indications
PharmacodynamicsCilostazol 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 actionCilostazol 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
cGMP-inhibited 3',5'-cyclic phosphodiesterase AProteinyes
inhibitor
HumanQ14432 details
Related Articles
AbsorptionCilostazol 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 distributionNot Available
Protein binding95-98%
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 eliminationCilostazol 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 life11-13 hours.
ClearanceNot Available
ToxicityInformation 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
PathwayCategorySMPDB ID
Cilostazol Action PathwayDrug actionSMP00263
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot 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
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
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
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Cilostazol.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
BeraprostCilostazol may increase the anticoagulant activities of Beraprost.Investigational
BetaxololThe metabolism of Cilostazol can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Cilostazol can be decreased when it is combined with Bexarotene.Approved, Investigational
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.Approved
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
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
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
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
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
CollagenaseThe risk or severity of adverse effects can be increased when Cilostazol is combined with Collagenase.Approved
ConivaptanThe serum concentration of Cilostazol can be increased when it is combined with Conivaptan.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
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
DexamethasoneThe serum concentration of Cilostazol can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexfenfluramineThe serum concentration of Cilostazol can be increased when it is combined with Dexfenfluramine.Approved, Illicit, Withdrawn
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
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
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
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Cilostazol.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
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
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
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
FibrinolysinCilostazol may increase the anticoagulant activities of Fibrinolysin.Approved
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Cilostazol.Approved
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
HaloperidolThe metabolism of Cilostazol can be decreased when combined with Haloperidol.Approved
HeparinCilostazol may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineCilostazol may increase the anticoagulant activities of Higenamine.Investigational
HirulogCilostazol may increase the anticoagulant activities of Hirulog.Experimental
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Cilostazol.Approved, Illicit
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
IdelalisibThe serum concentration of Cilostazol can be increased when it is combined with Idelalisib.Approved
idraparinuxCilostazol may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Cilostazol.Approved, Withdrawn
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
Kct 0809Cilostazol may increase the anticoagulant activities of Kct 0809.Investigational
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
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
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Cilostazol.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
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
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
MethylphenobarbitalThe serum concentration of Cilostazol can be increased when it is combined with Methylphenobarbital.Approved
MetoprololThe metabolism of Cilostazol can be decreased when combined with Metoprolol.Approved, Investigational
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
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.Investigational
NafcillinThe serum concentration of Cilostazol can be decreased when it is combined with Nafcillin.Approved
NaftopidilNaftopidil may increase the anticoagulant activities of Cilostazol.Investigational
NaloxegolThe serum concentration of Cilostazol can be increased when it is combined with Naloxegol.Approved
NCX 4016The risk or severity of adverse effects can be increased when Cilostazol is combined with NCX 4016.Investigational
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
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
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Cilostazol.Approved
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
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
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
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
PimozideThe serum concentration of Pimozide can be increased when it is combined with Cilostazol.Approved
PioglitazoneThe serum concentration of Cilostazol can be increased when it is combined with Pioglitazone.Approved, Investigational
PlasminCilostazol may increase the anticoagulant activities of Plasmin.Investigational
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
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
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
SCH-530348SCH-530348 may increase the anticoagulant activities of Cilostazol.Investigational
SelexipagCilostazol may increase the anticoagulant activities of Selexipag.Approved
SeratrodastThe serum concentration of Cilostazol can be increased when it is combined with Seratrodast.Approved, Investigational
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.Approved
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
TenofovirThe metabolism of Cilostazol can be decreased when combined with Tenofovir.Approved, Investigational
TerbinafineThe metabolism of Cilostazol can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
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.Approved
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
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
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
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
Ym150Cilostazol may increase the anticoagulant activities of Ym150.Investigational
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
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 ReferencesNot Available
External Links
ATC CodesB01AC23
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (35.9 KB)
ADMET
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 )
Pharmacoeconomics
ManufacturersNot 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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point160 °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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as hydroquinolones. These are compounds containing a hydrogenated quinoline bearing a ketone group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassQuinolones and derivatives
Direct ParentHydroquinolones
Alternative Parents
Substituents
  • Tetrahydroquinolone
  • Tetrahydroquinoline
  • Alkyl aryl ether
  • Benzenoid
  • Heteroaromatic compound
  • Tetrazole
  • Cyclic alcohol
  • Azole
  • Secondary carboxylic acid amide
  • Lactam
  • Carboxamide group
  • Azacycle
  • Ether
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

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
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
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
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23