ticlopidine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
2657 55142-85-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ticlopidine
  • ticlop
  • ticlid
  • tiklyd
  • ticlopidine hydrochloride
  • ticlopidine HCl
An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.
  • Molecular weight: 263.78
  • Formula: C14H14ClNS
  • CLOGP: 4.39
  • LIPINSKI: 0
  • HAC: 1
  • HDO: 0
  • TPSA: 3.24
  • ALOGS: -4.08
  • ROTB: 2
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.50 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 15.81 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 80 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Oct. 31, 1991 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 61.38 30.64 46 1233 199575 50404270
Sopor 50.66 30.64 19 1260 19860 50583985
Hyponatraemic syndrome 42.97 30.64 8 1271 536 50603309
Hyperkalaemia 40.21 30.64 21 1258 48068 50555777
Apraxia 40.03 30.64 9 1270 1536 50602309
Hypercreatininaemia 39.15 30.64 7 1272 374 50603471
Cerebral haemorrhage 35.22 30.64 16 1263 27036 50576809
Hypochloraemia 34.13 30.64 8 1271 1639 50602206

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 56.07 26.30 57 1348 197328 29375794
Sopor 50.03 26.30 19 1386 10915 29562207
Slow speech 49.94 26.30 11 1394 905 29572217
Intentional self-injury 40.77 26.30 17 1388 12444 29560678
Alcohol interaction 38.13 26.30 11 1394 2692 29570430
Melaena 36.30 26.30 21 1384 31155 29541967
Hyponatraemia 31.76 26.30 26 1379 67607 29505515
Electrocardiogram QT prolonged 30.94 26.30 20 1385 36117 29537005
Mechanical urticaria 30.39 26.30 5 1400 84 29573038
Anaemia 28.66 26.30 41 1364 200910 29372212
Coombs negative haemolytic anaemia 27.62 26.30 5 1400 150 29572972

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug interaction 102.83 24.36 102 2795 361981 64133854
Sopor 90.89 24.36 38 2859 29623 64466212
Melaena 61.31 24.36 35 2862 53513 64442322
Intentional self-injury 53.21 24.36 26 2871 29018 64466817
Cerebral haemorrhage 49.55 24.36 30 2867 51060 64444775
Anaemia 49.43 24.36 72 2825 378608 64117227
Hyponatraemic syndrome 46.81 24.36 10 2887 753 64495082
Hyponatraemia 44.07 24.36 43 2854 148296 64347539
Slow speech 41.80 24.36 11 2886 2026 64493809
Hyperkalaemia 41.17 24.36 35 2862 101094 64394741
Drug abuse 34.93 24.36 36 2861 132338 64363497
Alcohol interaction 33.43 24.36 11 2886 4390 64491445
Hypertensive crisis 32.40 24.36 16 2881 18232 64477603
Apraxia 30.60 24.36 9 2888 2486 64493349
Electrocardiogram QT prolonged 29.29 24.36 26 2871 79422 64416413
Hypoglycaemia 28.43 24.36 27 2870 89865 64405970
Hypochloraemia 27.78 24.36 8 2889 2053 64493782
Subdural haematoma 25.96 24.36 16 2881 28038 64467797
Hypercreatininaemia 24.64 24.36 6 2891 809 64495026
Haematidrosis 24.60 24.36 4 2893 66 64495769

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B01AC05 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Platelet aggregation inhibitors excl. heparin
FDA PE N0000008832 Decreased Platelet Aggregation
FDA EPC N0000175578 Platelet Aggregation Inhibitor
MeSH PA D002317 Cardiovascular Agents
MeSH PA D065689 Cytochrome P-450 CYP2C19 Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005343 Fibrinolytic Agents
MeSH PA D006401 Hematologic Agents
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010975 Platelet Aggregation Inhibitors
MeSH PA D058914 Purinergic Antagonists
MeSH PA D058919 Purinergic P2 Receptor Antagonists
MeSH PA D058921 Purinergic P2Y Receptor Antagonists
CHEBI has role CHEBI:48676 fibrin modulating agent
CHEBI has role CHEBI:50248 hematologic agents
CHEBI has role CHEBI:50249 anticoagulants
CHEBI has role CHEBI:50427 platelet aggregation inhibitors
CHEBI has role CHEBI:68563 ADP receptor subtype P2Y12 antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Percutaneous coronary intervention indication 415070008
Cerebrovascular Occlusion indication
Subacute Stent Thrombosis Prevention indication
Prevention of Cerebral Thrombosis indication
Obstruction of bile duct contraindication 30144000
Gastrointestinal ulcer contraindication 40845000
Hyperlipidemia contraindication 55822004 DOID:1168
Acute nephropathy contraindication 58574008
Blood coagulation disorder contraindication 64779008 DOID:1247
Gastrointestinal hemorrhage contraindication 74474003
Ascorbic acid deficiency contraindication 76169001
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Congenital hypoplastic anemia contraindication 88854002 DOID:1339
Leukemia, disease contraindication 93143009 DOID:1240
Procedure on central nervous system contraindication 118679007
Bleeding contraindication 131148009
Arterial aneurysm contraindication 233981004
Cerebral hemorrhage contraindication 274100004
Lumbar puncture contraindication 277762005
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Surgical procedure contraindication 387713003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.18 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
P2Y purinoceptor 12 GPCR ANTAGONIST WOMBAT-PK CHEMBL
Prostaglandin G/H synthase 1 Enzyme IC50 4.28 WOMBAT-PK
Alpha-2A adrenergic receptor GPCR Ki 6.85 DRUG MATRIX
Sigma non-opioid intracellular receptor 1 Membrane receptor Ki 6.75 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.86 DRUG MATRIX
Alpha-2C adrenergic receptor GPCR Ki 6.77 DRUG MATRIX
Cytochrome P450 2D6 Enzyme IC50 5.20 DRUG MATRIX
Cytochrome P450 2A6 Enzyme Ki 6.70 WOMBAT-PK
Bile salt export pump Transporter IC50 4.13 CHEMBL
Cytochrome P450 2C19 Enzyme IC50 6.18 DRUG MATRIX
Cytochrome P450 2B6 Enzyme INHIBITOR IC50 6.70 IUPHAR
Prostaglandin G/H synthase 2 Enzyme IC50 4.33 WOMBAT-PK
Membrane-associated progesterone receptor component 1 Membrane receptor Ki 5.70 DRUG MATRIX
Bile salt export pump Transporter IC50 4.31 CHEMBL

External reference:

IDSource
4020513 VUID
N0000148235 NUI
D01028 KEGG_DRUG
53885-35-1 SECONDARY_CAS_RN
4020458 VANDF
4020513 VANDF
C0040207 UMLSCUI
CHEBI:9588 CHEBI
TIC PDB_CHEM_ID
CHEMBL833 ChEMBL_ID
CHEMBL1717 ChEMBL_ID
DB00208 DRUGBANK_ID
D013988 MESH_DESCRIPTOR_UI
5472 PUBCHEM_CID
7307 IUPHAR_LIGAND_ID
3908 INN_ID
OM90ZUW7M1 UNII
10594 RXNORM
2177 MMSL
31069 MMSL
5582 MMSL
d00514 MMSL
003610 NDDF
003611 NDDF
108971003 SNOMEDCT_US
386950000 SNOMEDCT_US
395904008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ticlopidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68151-0079 TABLET, FILM COATED 250 mg ORAL ANDA 25 sections