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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
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.1999-01-15Not applicableUs
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 LLC2012-10-24Not applicableUs
Cilostazoltablet100 mg/1oralCorepharma LLC.2006-09-06Not applicableUs
Cilostazoltablet50 mg/1oralRoxane Laboratories, Inc2005-05-17Not applicableUs
Cilostazoltablet50 mg/1oralCarilion Materials Management2005-05-17Not applicableUs
Cilostazoltablet100 mg/1oralBreckenridge Pharmaceutical, Inc.2009-09-28Not applicableUs
Cilostazoltablet100 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-03-23Not applicableUs
Cilostazoltablet50 mg/1oralGolden State Medical Supply, Inc.2006-09-06Not applicableUs
Cilostazoltablet100 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-10-18Not applicableUs
Cilostazoltablet50 mg/1oralCorepharma LLC.2006-09-06Not applicableUs
Cilostazoltablet100 mg/1oralEon Labs, Inc.2004-11-23Not applicableUs
Cilostazoltablet100 mg/1oralGolden State Medical Supply, Inc.2011-10-18Not applicableUs
Cilostazoltablet100 mg/1oralBIOKEY INC.2014-04-012016-04-05Us
Cilostazoltablet100 mg/1oralbryant ranch prepack2004-11-23Not applicableUs
Cilostazoltablet50 mg/1oralEon Labs, Inc.2005-11-08Not applicableUs
Cilostazoltablet50 mg/1oralAvera Mc Kennan Hospital2015-03-23Not applicableUs
Cilostazoltablet50 mg/1oralGolden State Medical Supply, Inc.2011-10-18Not applicableUs
Cilostazoltablet50 mg/1oralBIOKEY INC.2014-04-012016-04-05Us
Cilostazoltablet50 mg/1oralbryant ranch prepack2005-05-17Not applicableUs
Cilostazoltablet50 mg/1oralTeva Pharmaceuticals USA Inc2012-04-24Not applicableUs
Cilostazoltablet100 mg/1oralAvera Mc Kennan Hospital2015-04-01Not applicableUs
Cilostazoltablet50 mg/1oralCardinal Health2011-02-18Not applicableUs
Cilostazoltablet100 mg/1oralSTAT Rx USA LLC2006-09-06Not applicableUs
Cilostazoltablet100 mg/1oralApotex Corp.2011-10-18Not applicableUs
Cilostazoltablet100 mg/1oralTeva Pharmaceuticals USA Inc2012-10-24Not applicableUs
Cilostazoltablet100 mg/1oralPreferred Pharmaceuticals, Inc.2014-07-28Not applicableUs
Cilostazoltablet100 mg/1oralCardinal Health2011-10-18Not applicableUs
Cilostazoltablet100 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-03-23Not applicableUs
Cilostazoltablet50 mg/1oralApotex Corp.2011-10-18Not applicableUs
Cilostazoltablet50 mg/1oralBreckenridge Pharmaceutical, Inc.2009-09-28Not applicableUs
Cilostazoltablet50 mg/1oralAmerican Health Packaging2014-07-30Not applicableUs
Cilostazoltablet100 mg/1oralRoxane Laboratories, Inc2011-01-05Not applicableUs
Cilostazoltablet100 mg/1oralCarilion Materials Management2011-01-05Not applicableUs
Cilostazoltablet100 mg/1oralPhysicians Total Care, Inc.2005-09-09Not applicableUs
Cilostazoltablet50 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs2012-06-26Not applicableUs
Cilostazoltablet100 mg/1oralGolden State Medical Supply, Inc.2006-09-06Not 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 KeyInChIKey=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
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.
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
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
SpectraNot Available
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)
Interactions
Drug Interactions
Drug
AbciximabCilostazol may increase the anticoagulant activities of Abciximab.
AbirateroneThe serum concentration of Cilostazol can be increased when it is combined with Abiraterone.
AcenocoumarolCilostazol may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Cilostazol is combined with Acetylsalicylic acid.
AlteplaseCilostazol may increase the anticoagulant activities of Alteplase.
AnagrelideThe risk or severity of adverse effects can be increased when Anagrelide is combined with Cilostazol.
AnistreplaseCilostazol may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Cilostazol is combined with Apixaban.
AprepitantThe serum concentration of Cilostazol can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Cilostazol.
ArmodafinilThe serum concentration of Cilostazol can be increased when it is combined with Armodafinil.
AtazanavirThe serum concentration of Cilostazol can be increased when it is combined with Atazanavir.
BexaroteneThe serum concentration of Cilostazol can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Cilostazol can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Cilostazol can be increased when it is combined with Bortezomib.
BosentanThe serum concentration of Cilostazol can be decreased when it is combined with Bosentan.
CeritinibThe serum concentration of Cilostazol can be increased when it is combined with Ceritinib.
ChloramphenicolThe serum concentration of Cilostazol can be increased when it is combined with Chloramphenicol.
CimetidineThe serum concentration of Cilostazol can be increased when it is combined with Cimetidine.
Citric AcidCilostazol may increase the anticoagulant activities of Citric Acid.
ClarithromycinThe serum concentration of Cilostazol can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Cilostazol can be increased when it is combined with Cobicistat.
CollagenaseThe risk or severity of adverse effects can be increased when Cilostazol is combined with Collagenase.
ConivaptanThe serum concentration of Cilostazol can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Cilostazol can be increased when it is combined with Crizotinib.
Dabigatran etexilateCilostazol may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Cilostazol can be decreased when it is combined with Dabrafenib.
DalteparinCilostazol may increase the anticoagulant activities of Dalteparin.
DarunavirThe serum concentration of Cilostazol can be increased when it is combined with Darunavir.
DasatinibDasatinib may increase the anticoagulant activities of Cilostazol.
DeferasiroxThe serum concentration of Cilostazol can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Cilostazol can be increased when it is combined with Delavirdine.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Cilostazol is combined with Deoxycholic Acid.
DicoumarolCilostazol may increase the anticoagulant activities of Dicoumarol.
DiltiazemThe serum concentration of Cilostazol can be increased when it is combined with Diltiazem.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Cilostazol.
DronedaroneThe serum concentration of Cilostazol can be increased when it is combined with Dronedarone.
Edetic AcidCilostazol may increase the anticoagulant activities of Edetic Acid.
EfavirenzThe serum concentration of Cilostazol can be increased when it is combined with Efavirenz.
EnoxaparinCilostazol may increase the anticoagulant activities of Enoxaparin.
ErythromycinThe serum concentration of Cilostazol can be increased when it is combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Cilostazol can be increased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe serum concentration of Cilostazol can be increased when it is combined with Esomeprazole.
Ethyl biscoumacetateCilostazol may increase the anticoagulant activities of Ethyl biscoumacetate.
EtravirineThe serum concentration of Cilostazol can be increased when it is combined with Etravirine.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Cilostazol.
FluconazoleThe serum concentration of Cilostazol can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Cilostazol can be increased when it is combined with Fluoxetine.
FluvoxamineThe serum concentration of Cilostazol can be increased when it is combined with Fluvoxamine.
Fondaparinux sodiumCilostazol may increase the anticoagulant activities of Fondaparinux sodium.
FosamprenavirThe serum concentration of Cilostazol can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Cilostazol can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Cilostazol can be increased when it is combined with Fusidic Acid.
GemfibrozilThe serum concentration of Cilostazol can be increased when it is combined with Gemfibrozil.
GlucosamineGlucosamine may increase the antiplatelet activities of Cilostazol.
HeparinCilostazol may increase the anticoagulant activities of Heparin.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Cilostazol.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Cilostazol is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Cilostazol.
IdelalisibThe serum concentration of Cilostazol can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Cilostazol can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Cilostazol can be increased when it is combined with Indinavir.
IsavuconazoniumThe serum concentration of Cilostazol can be increased when it is combined with Isavuconazonium.
IsoniazidThe serum concentration of Cilostazol can be increased when it is combined with Isoniazid.
ItraconazoleThe serum concentration of Cilostazol can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Cilostazol can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Cilostazol can be increased when it is combined with Ketoconazole.
LimaprostLimaprost may increase the antiplatelet activities of Cilostazol.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Cilostazol.
LuliconazoleThe serum concentration of Cilostazol can be increased when it is combined with Luliconazole.
MifepristoneThe serum concentration of Cilostazol can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Cilostazol can be decreased when it is combined with Mitotane.
MoclobemideThe serum concentration of Cilostazol can be increased when it is combined with Moclobemide.
ModafinilThe serum concentration of Cilostazol can be increased when it is combined with Modafinil.
NefazodoneThe serum concentration of Cilostazol can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Cilostazol can be increased when it is combined with Nelfinavir.
NicardipineThe serum concentration of Cilostazol can be increased when it is combined with Nicardipine.
NilotinibThe serum concentration of Cilostazol can be increased when it is combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Cilostazol.
ObinutuzumabThe risk or severity of adverse effects can be increased when Cilostazol is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Cilostazol.
OmeprazoleThe serum concentration of Cilostazol can be increased when it is combined with Omeprazole.
PalbociclibThe serum concentration of Cilostazol can be increased when it is combined with Palbociclib.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Cilostazol.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Cilostazol.
PhenindioneCilostazol may increase the anticoagulant activities of Phenindione.
PhenprocoumonCilostazol may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe metabolism of Cilostazol can be increased when combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Cilostazol.
PosaconazoleThe serum concentration of Cilostazol can be increased when it is combined with Posaconazole.
ReteplaseCilostazol may increase the anticoagulant activities of Reteplase.
RidogrelCilostazol may increase the anticoagulant activities of Ridogrel.
RiociguatCilostazol may increase the hypotensive activities of Riociguat.
RitonavirThe serum concentration of Cilostazol can be increased when it is combined with Ritonavir.
RivaroxabanCilostazol may increase the anticoagulant activities of Rivaroxaban.
SaquinavirThe serum concentration of Cilostazol can be increased when it is combined with Saquinavir.
SertralineThe serum concentration of Cilostazol can be increased when it is combined with Sertraline.
SiltuximabThe serum concentration of Cilostazol can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Cilostazol can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Cilostazol can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Cilostazol can be increased when it is combined with Stiripentol.
StreptokinaseCilostazol may increase the anticoagulant activities of Streptokinase.
SulodexideCilostazol may increase the anticoagulant activities of Sulodexide.
TelaprevirThe serum concentration of Cilostazol can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Cilostazol can be increased when it is combined with Telithromycin.
TenecteplaseCilostazol may increase the anticoagulant activities of Tenecteplase.
TiclopidineThe serum concentration of Cilostazol can be increased when it is combined with Ticlopidine.
TipranavirTipranavir may increase the antiplatelet activities of Cilostazol.
TocilizumabThe serum concentration of Cilostazol can be decreased when it is combined with Tocilizumab.
TositumomabThe risk or severity of adverse effects can be increased when Cilostazol is combined with Tositumomab.
TranylcypromineThe serum concentration of Cilostazol can be increased when it is combined with Tranylcypromine.
TreprostinilCilostazol may increase the anticoagulant activities of Treprostinil.
UrokinaseCilostazol may increase the anticoagulant activities of Urokinase.
VerapamilThe serum concentration of Cilostazol can be increased when it is combined with Verapamil.
Vitamin EVitamin E may increase the antiplatelet activities of Cilostazol.
VoriconazoleThe serum concentration of Cilostazol can be increased when it is combined with Voriconazole.
WarfarinCilostazol may increase the anticoagulant activities of Warfarin.
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

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