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Identification
NameCilostazol
Accession NumberDB01166  (APRD00155)
TypeSmall Molecule
GroupsApproved
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
SynonymLanguageCode
3,4-dihydro-6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinoneNot AvailableNot Available
6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinoneNot AvailableNot Available
6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydrocarbostyrilNot AvailableNot Available
6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-1H-quinolin-2-oneNot AvailableNot Available
CilostazoleNot AvailableNot Available
CilostazolumLatinINN
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pletaltablet100 mgoralOtsuka America Pharmaceutical, Inc.1999-01-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pletaltablet50 mgoralOtsuka America Pharmaceutical, Inc.1999-01-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cilostazoltablet50 mgoralRoxane Laboratories, Inc2005-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralRoxane Laboratories, Inc2011-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralTeva Pharmaceuticals USA Inc2012-10-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralTeva Pharmaceuticals USA Inc2012-04-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralEon Labs, Inc.2005-11-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralEon Labs, Inc.2004-11-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-03-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-06-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-03-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralSTAT Rx USA LLC2006-09-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralBIOKEY INC.2014-04-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralBIOKEY INC.2014-04-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralLake Erie Medical DBA Quality Care Products LLC2011-10-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralLake Erie Medical DBA Quality Care Products LLC2012-10-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralBreckenridge Pharmaceutical, Inc.2009-09-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralBreckenridge Pharmaceutical, Inc.2009-09-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralPhysicians Total Care, Inc.2005-09-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralCardinal Health2011-10-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralCardinal Health2011-02-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralGolden State Medical Supply, Inc.2011-10-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralGolden State Medical Supply, Inc.2011-10-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralGolden State Medical Supply, Inc.2006-09-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralGolden State Medical Supply, Inc.2006-09-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralApotex Corp.2011-10-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralApotex Corp.2011-10-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralbryant ranch prepack2005-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralbryant ranch prepack2004-11-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralCorepharma LLC.2006-09-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralCorepharma LLC.2006-09-06Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralAmerican Health Packaging2014-07-30Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet50 mgoralCarilion Materials Management2005-05-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralCarilion Materials Management2011-01-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cilostazoltablet100 mgoralPreferred Pharmaceuticals, Inc.2014-07-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
PletaalNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
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
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
Pharmacology
IndicationFor the reduction of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
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.
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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
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 substrateNon-inhibitor0.9071
CYP450 2D6 substrateNon-inhibitor0.9231
CYP450 2C19 substrateNon-inhibitor0.9026
CYP450 3A4 substrateInhibitor0.7959
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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg
Tabletoral50 mg
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
SpectraNot Available
References
Synthesis Reference

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

US20020099213
General ReferenceNot Available
External Links
ATC CodesB01AC23
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (35.9 KB)
Interactions
Drug Interactions
Drug
AbciximabAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
AbirateroneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
AcenocoumarolAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
Acetylsalicylic acidAgents with Antiplatelet Properties may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result.
AlteplaseAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
AnagrelideAnagrelide may enhance the adverse/toxic effect of Cilostazol.
AnistreplaseAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
ApixabanAgents with Antiplatelet Properties may enhance the adverse/toxic effect of Apixaban. Specifically, the risk for bleeding may be increased.
AprepitantCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
armodafinilCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
AtazanavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
BicalutamideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
BiotinCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
BoceprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
BortezomibCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
BosentanMay decrease the serum concentration of CYP3A4 Substrates.
ChloramphenicolCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
CimetidineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
Citric AcidAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
ClarithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
ClotrimazoleCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
ConivaptanMay increase the serum concentration of CYP3A4 Substrates.
CrizotinibCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
Dabigatran etexilateAgents with Antiplatelet Properties may enhance the anticoagulant effect of Dabigatran Etexilate. Agents with Antiplatelet Properties may increase the serum concentration of Dabigatran Etexilate. This mechanism applies specifically to clopidogrel.
DabrafenibMay decrease the serum concentration of CYP3A4 Substrates.
DalteparinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
DarunavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
DasatinibMay enhance the anticoagulant effect of Agents with Antiplatelet Properties.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DelavirdineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
Deoxycholic AcidAgents with Antiplatelet Properties may enhance the adverse/toxic effect of Deoxycholic Acid. Specifically, the risk for bleeding or bruising in the treatment area may be increased.
DesipramineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
DicoumarolAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
DiltiazemCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
DronedaroneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
Edetic AcidAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
EnoxaparinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
EsomeprazoleCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
Ethyl biscoumacetateAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
EtravirineCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
FluconazoleCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
FluoxetineCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
FluvoxamineCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
Fondaparinux sodiumAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
FosamprenavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
FosaprepitantCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
GemfibrozilCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
GlucosamineMay enhance the antiplatelet effect of Agents with Antiplatelet Properties.
HeparinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
IbritumomabAgents with Antiplatelet Properties may enhance the adverse/toxic effect of Ibritumomab. Both agents may contribute to impaired platelet function and an increased risk of bleeding.
IndinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
IsavuconazoniumCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
IsoniazidCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
ItraconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
IvacaftorMay increase the serum concentration of CYP3A4 Substrates.
LomitapideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
LopinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
LULICONAZOLEMay increase the serum concentration of CYP2C19 Substrates.
MifepristoneMay increase the serum concentration of CYP3A4 Substrates.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
MoclobemideCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
ModafinilCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
NefazodoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
NelfinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
NilotinibCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
NorfloxacinCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
ObinutuzumabAgents with Antiplatelet Properties may enhance the adverse/toxic effect of Obinutuzumab. Specifically, the risk of serious bleeding-related events may be increased.
OmeprazoleCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
PentoxifyllineMay enhance the antiplatelet effect of Agents with Antiplatelet Properties.
PhenindioneAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
PhenprocoumonAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
PosaconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
ReteplaseAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
RidogrelAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
RiociguatCilostazol may enhance the hypotensive effect of Riociguat.
RitonavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
RivaroxabanAgents with Antiplatelet Properties may enhance the anticoagulant effect of Rivaroxaban.
Salicylate-sodiumAgents with Antiplatelet Properties may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result.
SaquinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
SertralineCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay increase the serum concentration of CYP3A4 Substrates.
StreptokinaseAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
SulfisoxazoleCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
SulodexideAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
TelaprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
TelithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
TenecteplaseAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
TetracyclineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol.
TiclopidineCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
TipranavirMay enhance the antiplatelet effect of Agents with Antiplatelet Properties.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
TranylcypromineCYP2C19 Inhibitors may increase the serum concentration of Cilostazol.
TreprostinilAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
UrokinaseAgents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents.
Vitamin EMay enhance the antiplatelet effect of Agents with Antiplatelet Properties.
VoriconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cilostazol.
WarfarinAgents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants.
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.

Targets

1. cGMP-inhibited 3',5'-cyclic phosphodiesterase A

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
cGMP-inhibited 3',5'-cyclic phosphodiesterase A Q14432 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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
  3. Schror K: The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9. Pubmed
  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
  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. Epub 2007 Nov 22. Pubmed

Enzymes

1. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

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

2. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. Pubmed

3. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. Pubmed

4. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Suri A, Forbes WP, Bramer SL: Effects of CYP3A inhibition on the metabolism of cilostazol. Clin Pharmacokinet. 1999;37 Suppl 2:61-8. Pubmed

5. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

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

6. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

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

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:13