Identification

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

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

Structure
Thumb
Synonyms
  • 3,4-dihydro-6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinone
  • 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone
  • 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydrocarbostyril
  • 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-1H-quinolin-2-one
  • Cilostazole
  • Cilostazolum
External IDs
OPC-13013 / OPC-21
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CilostazolTablet50 mg/1OralTEVA PHARMACEUTICALS USA2007-01-082007-01-08Us
PletalTablet100 mg/1OralOtsuka Pharmaceutical Co., Ltd.1999-01-152016-06-30Us
PletalTablet50 mg/1OralPhysicians Total Care, Inc.1999-01-152011-07-31Us
PletalTablet50 mg/1OralOtsuka Pharmaceutical Co., Ltd.1999-01-152017-11-30Us
PletalTablet100 mg/1OralPhysicians Total Care, Inc.1999-01-152011-07-31Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CilostazolTablet50 mg/1OralBioKey, Inc.2017-09-272017-09-27Us
CilostazolTablet100 mg/1OralCardinal Health2011-10-18Not applicableUs
CilostazolTablet50 mg/1OralCardinal Health2011-02-182018-05-25Us
CilostazolTablet100 mg/1OralCore Pharma, Llc2006-09-062012-11-01Us
CilostazolTablet50 mg/1OralNucare Pharmaceuticals, Inc.2012-04-24Not applicableUs
CilostazolTablet100 mg/1OralStat Rx USA2006-09-06Not applicableUs
CilostazolTablet50 mg/1OralCarilion Materials Management2005-05-17Not applicableUs68151 384420180907 15195 caq6w4
CilostazolTablet100 mg/1OralTeva Pharmaceuticals USA, Inc.2012-10-24Not applicableUs0093 206420180814 13942 16ufbi0
CilostazolTablet100 mg/1OralGolden State Medical Supply2011-10-182017-05-31Us
CilostazolTablet100 mg/1OralAvera McKennan Hospital2015-04-012018-05-22Us
International/Other Brands
Pletaal
Categories
UNII
N7Z035406B
CAS number
73963-72-1
Weight
Average: 369.4607
Monoisotopic: 369.216475133
Chemical Formula
C20H27N5O2
InChI Key
RRGUKTPIGVIEKM-UHFFFAOYSA-N
InChI
InChI=1S/C20H27N5O2/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16/h10-11,14,16H,1-9,12-13H2,(H,21,26)
IUPAC Name
6-[4-(1-cyclohexyl-1H-1,2,3,4-tetrazol-5-yl)butoxy]-1,2,3,4-tetrahydroquinolin-2-one
SMILES
O=C1CCC2=C(N1)C=CC(OCCCCC1=NN=NN1C1CCCCC1)=C2

Pharmacology

Indication

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

Associated Conditions
Pharmacodynamics

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

Mechanism of action

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

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

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

Volume of distribution
Not Available
Protein binding

95-98%

Metabolism

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

Route of elimination

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

Half life

11-13 hours.

Clearance
Not Available
Toxicity

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

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

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Cilostazol.
(S)-WarfarinThe risk or severity of bleeding can be increased when Cilostazol is combined with (S)-Warfarin.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Cilostazol.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Cilostazol.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Cilostazol.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Cilostazol.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Cilostazol.
6-Deoxyerythronolide BThe metabolism of Cilostazol can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe serum concentration of 6-O-benzylguanine can be increased when it is combined with Cilostazol.
7-DeazaguanineThe serum concentration of 7-Deazaguanine can be increased when it is combined with Cilostazol.
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment, grapefruit can significantly increase serum levels of this product.
  • Take on an empty stomach, a lipid rich meal will increase absorption.

References

Synthesis Reference

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

US20020099213
General References
Not Available
External Links
Human Metabolome Database
HMDB0015297
KEGG Drug
D01896
PubChem Compound
2754
PubChem Substance
46506317
ChemSpider
2652
BindingDB
50070490
ChEBI
31401
ChEMBL
CHEMBL799
Therapeutic Targets Database
DAP000191
PharmGKB
PA164746334
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cilostazol
ATC Codes
B01AC23 — Cilostazol
MSDS
Download (35.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceMigraine With Aura / Strokes1
1Active Not RecruitingTreatmentHealthy Volunteers1
1Active Not RecruitingTreatmentIntermittent Claudication1
1CompletedNot AvailableHealthy Volunteers3
1CompletedNot AvailableTherapeutic Equivalency, Healthy1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceTherapeutic Equivalency1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentIntermittent Claudication1
1CompletedTreatmentPain NOS1
1RecruitingTreatmentDyslipidemias / Peripheral Artery Disease (PAD)1
2CompletedBasic ScienceContraception1
2CompletedPreventionCerebral Small Vessels Disease / Cognitive Impairments / Strokes1
2CompletedTreatmentIntermittent Claudication1
2RecruitingTreatmentMild Cognitive Impairment (MCI)1
2Unknown StatusTreatmentPeripheral Artery Disease (PAD)1
2, 3RecruitingPreventionCerebral Small Vessels Disease / Stroke, Lacunar1
3CompletedPreventionCerebral Infarctions2
3CompletedTreatmentCerebrovascular Diseases / Cerebrovascular Disorders1
3CompletedTreatmentCoronary Artery Disease1
3CompletedTreatmentVasospastic Angina2
3RecruitingPreventionNoncardioembolic Cerebral Infarction1
3RecruitingPreventionPeripheral Arterial Disease (PAD)1
3Unknown StatusTreatmentAtherosclerosis / Cardiovascular Disease (CVD) / Peripheral Vascular Disease (PVD)1
3Unknown StatusTreatmentCoronary Artery Stenosis / High Post-Treatment Platelet Reactivity / Late Platelet Aggregation / Maximal Platelet Aggregation1
4Active Not RecruitingPreventionIntracranial Hemorrhages / Ischemia, Brain1
4Active Not RecruitingTreatmentCarotid Atherosclerosis / Type 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentCerebral Small Vessels Disease1
4Active Not RecruitingTreatmentIntracranial Hemorrhages / Ischemia, Brain1
4CompletedNot AvailableIntermittent Claudication / Peripheral Arterial Disease (PAD) / Peripheral Vascular Disease (PVD)1
4CompletedPreventionCerebral Infarctions1
4CompletedTreatmentAcute Coronary Syndromes (ACS)1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / Clopidogrel Low Responsiveness / Percutaneous Coronary Intervention1
4CompletedTreatmentAlzheimer Dementia (AD)1
4CompletedTreatmentArteriosclerosis Obliterans / Type 2 Diabetes Mellitus1
4CompletedTreatmentAtherosclerosis Cerebral Infarction1
4CompletedTreatmentAtherosclerosis / Cerebral Infarctions1
4CompletedTreatmentCardiovascular Disease (CVD)1
4CompletedTreatmentCerebral Infarctions3
4CompletedTreatmentChronic Kidney Disease (CKD) / Stable Angina (SA)1
4CompletedTreatmentClaudication (Finding) / Peripheral Arterial Disease (PAD)1
4CompletedTreatmentCoronary Artery Disease3
4CompletedTreatmentDementia, Vascular / Strokes1
4CompletedTreatmentDiabetes Complications / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetic Nephropathies1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHemodialysis Patients / Peripheral Vascular Disease (PVD)1
4CompletedTreatmentMyocardial Infarction1
4CompletedTreatmentPeripheral Arterial Disease (PAD)1
4CompletedTreatmentPolyneuropathies1
4CompletedTreatmentRaynaud's Disease2
4CompletedTreatmentStroke, Ischemic1
4Not Yet RecruitingPreventionType 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentCritical Limb Ischemia (CLI)1
4RecruitingHealth Services ResearchPeripheral Artery Disease (PAD) / Stroke, Ischemic / Type 2 Diabetes Mellitus1
4RecruitingTreatmentCoronary Artery Disease2
4RecruitingTreatmentSevere Hypercholesterolemia1
4TerminatedTreatmentCoronary Artery Disease1
4Unknown StatusPreventionArteriosclerosis Obliterans1
4Unknown StatusPreventionType 2 Diabetes Mellitus1
4Unknown StatusTreatmentAngioplasty, Transluminal, Percutaneous Coronary1
4Unknown StatusTreatmentMetabolic Syndromes / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableAPT(Antiplatelet Therapy) / HOTPR(High on Treat Platelet Reactivity) / PRU(Platelet Reactivity Unit)1
Not AvailableCompletedHealth Services ResearchDrug Drug Interaction (DDI)1
Not AvailableCompletedHealth Services ResearchMigraines1
Not AvailableCompletedTreatmentClopidogrel Non-Responsiveness1
Not AvailableCompletedTreatmentCoronary Heart Disease (CHD)1
Not AvailableCompletedTreatmentIntermittent Claudication2
Not AvailableCompletedTreatmentMigraines1
Not AvailableCompletedTreatmentTinnitus1
Not AvailableRecruitingOtherMigraine Without Aura / Migrainous Headache1
Not AvailableRecruitingTreatmentMigraines1
Not AvailableUnknown StatusTreatmentMild Cognitive Impairment (MCI)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Alphapharm Party Ltd.
  • Apotex Inc.
  • Breckenridge Pharmaceuticals
  • Corepharma LLC
  • Diversified Healthcare Services Inc.
  • Eon Labs
  • Heartland Repack Services LLC
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Otsuka America
  • Physicians Total Care Inc.
  • Prasco Labs
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Stat Rx Usa
  • Teva Pharmaceutical Industries Ltd.
  • UDL Laboratories
  • United Research Laboratories Inc.
  • Vangard Labs Inc.
Dosage forms
FormRouteStrength
TabletConjunctival; Oral100 mg/1
TabletOral100 mg/1
TabletOral50 mg/1
Prices
Unit descriptionCostUnit
Pletal 100 mg tablet2.51USD tablet
Pletal 50 mg tablet2.39USD tablet
Cilostazol 100 mg tablet1.86USD tablet
Cilostazol 50 mg tablet1.86USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

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

Spectra

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

Taxonomy

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

Targets

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

Enzymes

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

Drug created on June 13, 2005 07:24 / Updated on November 02, 2018 04:57