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Identification
NameTiclopidine
Accession NumberDB00208  (APRD01257)
TypeSmall Molecule
GroupsApproved
Description

Ticlopidine is an effective inhibitor of platelet aggregation. It is a prodrug that is metabolised to an active form, which blocks the ADP receptor that is involved in GPIIb/IIIa receptor activation leading to platelet aggregation. Ticlopidine is marketed under the brand name Ticlid and is indicated for patients who cannot take aspirin or in whom aspirin has not worked to prevent a thrombotic stroke. The FDA label includes a black-box warning of neutropenia, aplastic anemia, thrombotic thrombocytopenia purpura, and agranulocytosis, so it is necessary to monitor patients’ WBC and platelets when they are taking ticlopidine.

Structure
Thumb
Synonyms
Ticlopidina
Ticlopidinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alti-ticlopidine - Tab 250mgtablet250 mgoralAltimed Pharma Inc.1996-12-312005-05-27Canada
Dom-ticlopidinetablet250 mgoralDominion Pharmacal2001-05-23Not applicableCanada
Mylan-ticlopidinetablet250 mgoralMylan Pharmaceuticals Ulc1999-03-04Not applicableCanada
Nu-ticlopidine 250 mgtablet250 mgoralNu Pharm Inc1998-06-092012-09-04Canada
PMS-ticlopidinetablet250 mgoralPharmascience Inc2001-02-23Not applicableCanada
Sandoz Ticlopidinetablet250 mgoralSandoz Canada Incorporated2001-05-142011-10-21Canada
Teva-ticlopidinetablet250 mgoralTeva Canada Limited2002-07-30Not applicableCanada
Ticlid 250mg Tabletstablet250 mgoralHoffmann La Roche Limited1995-12-312006-07-25Canada
Ticlid Tab 250mgtablet250 mgoralSyntex Inc.1992-12-311996-09-30Canada
Ticlopidinetablet250 mgoralSanis Health Inc2010-02-162014-08-01Canada
Ticlopidine-250tablet250 mgoralPro Doc Limitee1999-11-182010-07-13Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-ticlopidine Tabletstablet250 mgoralApotex Inc1998-03-30Not applicableCanada
Ticlopidine Hydrochloridetablet, film coated250 mg/1oralTeva Pharmaceuticals USA Inc1999-09-072016-02-25Us
Ticlopidine Hydrochloridetablet, film coated250 mg/1oralCarilion Materials Management1999-09-07Not applicableUs
Ticlopidine Hydrochloridetablet, film coated250 mg/1oralApotex Corp.1999-07-01Not applicableUs
Ticlopidine Hydrochloridetablet, film coated250 mg/1oralCaraco Pharmaceutical Laboratories, Ltd.2002-09-26Not applicableUs
Ticlopidine Hydrochloridetablet, film coated250 mg/1oralEon Labs, Inc.1999-08-20Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TiclidROCHE PALO
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Ticlopidine Hydrochloride
53885-35-1
Thumb
  • InChI Key: MTKNGOHFNXIVOS-UHFFFAOYSA-N
  • Monoisotopic Mass: 299.030225589
  • Average Mass: 300.247
DBSALT000179
Categories
UNIIOM90ZUW7M1
CAS number55142-85-3
WeightAverage: 263.786
Monoisotopic: 263.05354785
Chemical FormulaC14H14ClNS
InChI KeyInChIKey=PHWBOXQYWZNQIN-UHFFFAOYSA-N
InChI
InChI=1S/C14H14ClNS/c15-13-4-2-1-3-11(13)9-16-7-5-14-12(10-16)6-8-17-14/h1-4,6,8H,5,7,9-10H2
IUPAC Name
5-[(2-chlorophenyl)methyl]-4H,5H,6H,7H-thieno[3,2-c]pyridine
SMILES
ClC1=CC=CC=C1CN1CCC2=C(C1)C=CS2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as thienopyridines. These are heterocyclic compounds containing a thiophene ring fused to a pyridine ring. Thiophene is 5-membered ring consisting of four carbon atoms and one sulfur atom. Pyridine is a 6-membered ring consisting of five carbon atoms and one nitrogen center.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassThienopyridines
Sub ClassNot Available
Direct ParentThienopyridines
Alternative Parents
Substituents
  • Thienopyridine
  • Phenylmethylamine
  • Benzylamine
  • Aralkylamine
  • Halobenzene
  • Chlorobenzene
  • Benzenoid
  • Pyridine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Thiophene
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed in patients, who have had a stroke or stroke precursors and who cannot take aspirin or aspirin has not worked, to try to prevent another thrombotic stroke.
PharmacodynamicsTiclopidine is a prodrug that is metabolised to an as yet undetermined metabolite that acts as a platelet aggregation inhibitor. Inhibition of platelet aggregation causes a prolongation of bleeding time. In its prodrug form, ticlopidine has no significant in vitro activity at the concentrations attained in vivo.
Mechanism of actionThe active metabolite of ticlopidine prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. It is proposed that the inhibition involves a defect in the mobilization from the storage sites of the platelet granules to the outer membrane. No direct interference occurs with the GPIIb/IIIa receptor. As the glycoprotein GPIIb/IIIa complex is the major receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation. By blocking the amplification of platelet activation by released ADP, platelet aggregation induced by agonists other than ADP is also inhibited by the active metabolite of ticlopidine.
Related Articles
AbsorptionAbsorption is greater than 80%. Food increases absorption by approximately 20%.
Volume of distribution

The volume of distribution was not quantified.

Protein bindingBinds reversibly (98%) to plasma proteins, mainly to serum albumin and lipoproteins. The binding to albumin and lipoproteins is nonsaturable over a wide concentration range. Ticlopidine also binds to alpha-1 acid glycoprotein (about 15% or less).
Metabolism

Ticlopidine is metabolized extensively by the liver with only trace amounts of intact drug detected. At least 20 metabolites have been identified.

SubstrateEnzymesProduct
Ticlopidine
2-ChloroticlopidineDetails
Ticlopidine
2-OxoticlopidineDetails
Ticlopidine
ThienodihydropyridiniumDetails
Ticlopidine
Ticlopidine S-oxideDetails
Ticlopidine
Dehydrogenated ticlopidineDetails
Ticlopidine
Ticlopidine N-oxideDetails
Ticlopidine
di-HydroxyticlopidineDetails
Ticlopidine
Not Available
7-HydroxyticlopidineDetails
2-Oxoticlopidine
Not Available
Active metabolite of TiclopidineDetails
Ticlopidine S-oxide
Not Available
Ticlopidine S-oxide dimerDetails
Thienodihydropyridinium
ThienopyridiniumDetails
Thienodihydropyridinium
Ticlopidine lactam analog (M8)Details
Route of eliminationTiclopidine is eliminated mostly in the urine (60%) and somewhat in the feces (23%).
Half lifeHalf-life following a single 250-mg dose is approximately 7.9 hours in subjects 20 to 43 years of age and 12.6 hours in subjects 65 to 76 years of age. With repeated dosing (250 mg twice a day), half-life is about 4 days in subjects 20 to 43 years of age and about 5 days in subjects 65 to 76 years of age.
Clearance

Ticlopidine clearance was not quantified, but clearance decreases with age.

ToxicitySingle oral doses of ticlopidine at 1600 mg/kg and 500 mg/kg were lethal to rats and mice, respectively. Symptoms of acute toxicity were GI hemorrhage, convulsions, hypothermia, dyspnea, loss of equilibrium and abnormal gait. The FDA label includes a black-box warning of neutropenia, aplastic anemia, thrombotic thrombocytopenia purpura, and agranulocytosis, so it is necessary to monitor patients' WBC and platelets when they are taking ticlopidine.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Ticlopidine Metabolism PathwayDrug metabolismSMP00611
Ticlopidine Action PathwayDrug actionSMP00261
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9902
Blood Brain Barrier+0.9906
Caco-2 permeable+0.6062
P-glycoprotein substrateSubstrate0.6111
P-glycoprotein inhibitor IInhibitor0.8
P-glycoprotein inhibitor IIInhibitor0.8513
Renal organic cation transporterInhibitor0.8152
CYP450 2C9 substrateNon-substrate0.8234
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateNon-substrate0.5155
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.9209
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorNon-inhibitor0.8808
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9666
Ames testNon AMES toxic0.6773
CarcinogenicityNon-carcinogens0.9414
BiodegradationNot ready biodegradable0.9959
Rat acute toxicity2.2022 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6392
hERG inhibition (predictor II)Inhibitor0.6333
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Roche palo alto llc
  • Actavis elizabeth llc
  • Apotex inc
  • Caraco pharmaceutical laboratories ltd
  • Genpharm inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral250 mg
Tablet, film coatedoral250 mg/1
Prices
Unit descriptionCostUnit
Ticlid 30 250 mg tablet Bottle87.36USD bottle
Ticlid 250 mg tablet2.61USD tablet
Ticlopidine HCl 250 mg tablet2.1USD tablet
Ticlopidine 250 mg tablet1.86USD tablet
Apo-Ticlopidine 250 mg Tablet0.72USD tablet
Mylan-Ticlopidine 250 mg Tablet0.72USD tablet
Novo-Ticlopidine 250 mg Tablet0.72USD tablet
Nu-Ticlopidine 250 mg Tablet0.72USD tablet
Sandoz Ticlopidine 250 mg Tablet0.72USD tablet
Ticlopidine 250 mg Tablet0.72USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting pointapprox. 1 189°CFrom Remington: The Science and Practice of Pharmacy
water solubilityFreely solubleFrom Remington: The Science and Practice of Pharmacy
logP2.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0219 mg/mLALOGPS
logP4.25ALOGPS
logP4.2ChemAxon
logS-4.1ALOGPS
pKa (Strongest Basic)7.31ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area3.24 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity74.33 m3·mol-1ChemAxon
Polarizability27.99 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. FDA label.
External Links
ATC CodesB01AC05
AHFS Codes
  • 20:12.18
PDB EntriesNot Available
FDA labelDownload (916 KB)
MSDSDownload (106 KB)
Interactions
Drug Interactions
Drug
AbciximabTiclopidine may increase the anticoagulant activities of Abciximab.
AcenocoumarolTiclopidine may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Acetylsalicylic acid.
AlteplaseTiclopidine may increase the anticoagulant activities of Alteplase.
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Ticlopidine.
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Ticlopidine.
AmoxapineThe metabolism of Amoxapine can be decreased when combined with Ticlopidine.
AnistreplaseTiclopidine may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Apixaban.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Ticlopidine.
AtomoxetineThe metabolism of Atomoxetine can be decreased when combined with Ticlopidine.
BexaroteneThe serum concentration of Ticlopidine can be decreased when it is combined with Bexarotene.
BortezomibThe metabolism of Bortezomib can be decreased when combined with Ticlopidine.
BosentanThe serum concentration of Ticlopidine can be decreased when it is combined with Bosentan.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Ticlopidine.
BupropionThe serum concentration of Bupropion can be increased when it is combined with Ticlopidine.
CaptoprilThe metabolism of Captopril can be decreased when combined with Ticlopidine.
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Ticlopidine.
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Ticlopidine.
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Ticlopidine.
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Ticlopidine.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Ticlopidine.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Ticlopidine.
Citric AcidTiclopidine may increase the anticoagulant activities of Citric Acid.
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Ticlopidine.
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Ticlopidine resulting in a loss in efficacy.
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Ticlopidine.
CollagenaseThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Collagenase.
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Ticlopidine.
Dabigatran etexilateTiclopidine may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Ticlopidine can be decreased when it is combined with Dabrafenib.
DalteparinTiclopidine may increase the anticoagulant activities of Dalteparin.
DasatinibDasatinib may increase the anticoagulant activities of Ticlopidine.
DeferasiroxThe serum concentration of Ticlopidine can be decreased when it is combined with Deferasirox.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Deoxycholic Acid.
DesipramineThe metabolism of Desipramine can be decreased when combined with Ticlopidine.
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Ticlopidine.
DicoumarolTiclopidine may increase the anticoagulant activities of Dicoumarol.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Ticlopidine.
DoxepinThe metabolism of Doxepin can be decreased when combined with Ticlopidine.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Ticlopidine.
Edetic AcidTiclopidine may increase the anticoagulant activities of Edetic Acid.
EfavirenzThe metabolism of Efavirenz can be decreased when combined with Ticlopidine.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Ticlopidine.
EnoxaparinTiclopidine may increase the anticoagulant activities of Enoxaparin.
Ethyl biscoumacetateTiclopidine may increase the anticoagulant activities of Ethyl biscoumacetate.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Ticlopidine.
FlecainideThe metabolism of Flecainide can be decreased when combined with Ticlopidine.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Ticlopidine.
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Ticlopidine.
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Ticlopidine.
FluvoxamineThe metabolism of Fluvoxamine can be decreased when combined with Ticlopidine.
Fondaparinux sodiumTiclopidine may increase the anticoagulant activities of Fondaparinux sodium.
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Ticlopidine.
GefitinibThe metabolism of Gefitinib can be decreased when combined with Ticlopidine.
GlucosamineGlucosamine may increase the antiplatelet activities of Ticlopidine.
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Ticlopidine.
HeparinTiclopidine may increase the anticoagulant activities of Heparin.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Ticlopidine.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Ticlopidine.
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Ticlopidine.
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Ticlopidine.
ImipramineThe metabolism of Imipramine can be decreased when combined with Ticlopidine.
IrinotecanThe metabolism of Irinotecan can be decreased when combined with Ticlopidine.
KetamineThe metabolism of Ketamine can be decreased when combined with Ticlopidine.
LimaprostLimaprost may increase the antiplatelet activities of Ticlopidine.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Ticlopidine.
MaprotilineThe metabolism of Maprotiline can be decreased when combined with Ticlopidine.
MethadoneThe metabolism of Methadone can be decreased when combined with Ticlopidine.
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Ticlopidine.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Ticlopidine.
MexiletineThe metabolism of Mexiletine can be decreased when combined with Ticlopidine.
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Ticlopidine.
MitotaneThe serum concentration of Ticlopidine can be decreased when it is combined with Mitotane.
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Ticlopidine.
NefazodoneThe metabolism of Nefazodone can be decreased when combined with Ticlopidine.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Ticlopidine.
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Ticlopidine.
ObinutuzumabThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Ticlopidine.
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Ticlopidine.
ParoxetineThe metabolism of Paroxetine can be decreased when combined with Ticlopidine.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Ticlopidine.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Ticlopidine.
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Ticlopidine.
PhenindioneTiclopidine may increase the anticoagulant activities of Phenindione.
PhenprocoumonTiclopidine may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Ticlopidine.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Ticlopidine.
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Ticlopidine.
PrimaquineThe metabolism of Primaquine can be decreased when combined with Ticlopidine.
ProcainamideThe metabolism of Procainamide can be decreased when combined with Ticlopidine.
PromazineThe metabolism of Promazine can be decreased when combined with Ticlopidine.
PromethazineThe metabolism of Promethazine can be decreased when combined with Ticlopidine.
PropafenoneThe serum concentration of Ticlopidine can be increased when it is combined with Propafenone.
PropofolThe metabolism of Propofol can be decreased when combined with Ticlopidine.
PropranololThe metabolism of Propranolol can be decreased when combined with Ticlopidine.
ProtriptylineThe metabolism of Protriptyline can be decreased when combined with Ticlopidine.
ReteplaseTiclopidine may increase the anticoagulant activities of Reteplase.
RidogrelTiclopidine may increase the anticoagulant activities of Ridogrel.
RisperidoneThe metabolism of Risperidone can be decreased when combined with Ticlopidine.
RivaroxabanTiclopidine may increase the anticoagulant activities of Rivaroxaban.
SelegilineThe metabolism of Selegiline can be decreased when combined with Ticlopidine.
SiltuximabThe serum concentration of Ticlopidine can be decreased when it is combined with Siltuximab.
St. John's WortThe serum concentration of Ticlopidine can be decreased when it is combined with St. John's Wort.
StreptokinaseTiclopidine may increase the anticoagulant activities of Streptokinase.
SulodexideTiclopidine may increase the anticoagulant activities of Sulodexide.
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Ticlopidine resulting in a loss in efficacy.
TenecteplaseTiclopidine may increase the anticoagulant activities of Tenecteplase.
TetrabenazineThe metabolism of Tetrabenazine can be decreased when combined with Ticlopidine.
TheophyllineThe metabolism of Theophylline can be decreased when combined with Ticlopidine.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Ticlopidine.
TimololThe metabolism of Timolol can be decreased when combined with Ticlopidine.
TipranavirTipranavir may increase the antiplatelet activities of Ticlopidine.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Ticlopidine.
TocilizumabThe serum concentration of Ticlopidine can be decreased when it is combined with Tocilizumab.
TolterodineThe metabolism of Tolterodine can be decreased when combined with Ticlopidine.
TositumomabThe risk or severity of adverse effects can be increased when Ticlopidine is combined with Tositumomab.
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Ticlopidine.
TreprostinilTiclopidine may increase the anticoagulant activities of Treprostinil.
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Ticlopidine.
UrokinaseTiclopidine may increase the anticoagulant activities of Urokinase.
VenlafaxineThe metabolism of Venlafaxine can be decreased when combined with Ticlopidine.
Vitamin EVitamin E may increase the antiplatelet activities of Ticlopidine.
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Ticlopidine.
WarfarinTiclopidine may increase the anticoagulant activities of Warfarin.
ZuclopenthixolThe metabolism of Zuclopenthixol can be decreased when combined with Ticlopidine.
Food Interactions
  • High fat meals will increase ticlopidine absorption. As well, food can help ticlopidine-induced stomach upset.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Required for normal platelet aggregation and blood coagulation.
Gene Name:
P2RY12
Uniprot ID:
Q9H244
Molecular Weight:
39438.355 Da
References
  1. Storey RF: The P2Y12 receptor as a therapeutic target in cardiovascular disease. Platelets. 2001 Jun;12(4):197-209. [PubMed:11454254 ]
  2. Boeynaems JM, van Giezen H, Savi P, Herbert JM: P2Y receptor antagonists in thrombosis. Curr Opin Investig Drugs. 2005 Mar;6(3):275-82. [PubMed:15816504 ]
  3. Gachet C: The platelet P2 receptors as molecular targets for old and new antiplatelet drugs. Pharmacol Ther. 2005 Nov;108(2):180-92. Epub 2005 Jun 13. [PubMed:15955565 ]
  4. Zhan C, Yang J, Dong XC, Wang YL: Molecular modeling of purinergic receptor P2Y12 and interaction with its antagonists. J Mol Graph Model. 2007 Jul;26(1):20-31. Epub 2006 Sep 26. [PubMed:17110146 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Peroxidase activity
Specific Function:
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production of hypohalous acids, primarily hypochlorous acid in physiologic situations, and other toxic intermediates that greatly enhance PMN microbicidal activity.
Gene Name:
MPO
Uniprot ID:
P05164
Molecular Weight:
83867.71 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Vitamin d 24-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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Walsky RL, Astuccio AV, Obach RS: Evaluation of 227 drugs for in vitro inhibition of cytochrome P450 2B6. J Clin Pharmacol. 2006 Dec;46(12):1426-38. [PubMed:17101742 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:08