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 67.87 30.47 48 1287 229083 63258604
Sopor 52.05 30.47 19 1316 22145 63465542
Hyponatraemic syndrome 44.28 30.47 8 1327 547 63487140
Hyperkalaemia 41.48 30.47 21 1314 54182 63433505
Apraxia 40.21 30.47 9 1326 1812 63485875
Hypochloraemia 39.33 30.47 9 1326 2000 63485687
Hypercreatininaemia 37.61 30.47 7 1328 564 63487123
Cerebral haemorrhage 36.08 30.47 16 1319 30713 63456974
Melaena 33.07 30.47 15 1320 30350 63457337

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 56.34 28.00 57 1385 225889 34729600
Sopor 50.71 28.00 19 1423 12117 34943372
Slow speech 48.51 28.00 11 1431 1191 34954298
Intentional self-injury 41.44 28.00 17 1425 13754 34941735
Alcohol interaction 38.85 28.00 11 1431 2902 34952587
Melaena 36.59 28.00 21 1421 35359 34920130
Electrocardiogram QT prolonged 31.24 28.00 20 1422 40932 34914557
Hyponatraemia 30.40 28.00 26 1416 82665 34872824
Mechanical urticaria 29.90 28.00 5 1437 108 34955381
Anaemia 29.87 28.00 42 1400 233293 34722196
Coombs negative haemolytic anaemia 28.14 28.00 5 1437 156 34955333

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 110.29 24.98 104 2890 415079 79326315
Sopor 93.54 24.98 38 2956 32972 79708422
Melaena 65.72 24.98 36 2958 60854 79680540
Intentional self-injury 54.92 24.98 26 2968 32393 79709001
Anaemia 53.39 24.98 74 2920 444941 79296453
Cerebral haemorrhage 51.15 24.98 30 2964 57643 79683751
Hyponatraemic syndrome 48.38 24.98 10 2984 770 79740624
Hyperkalaemia 45.00 24.98 36 2958 114362 79627032
Hyponatraemia 43.99 24.98 43 2951 177805 79563589
Slow speech 41.61 24.98 11 2983 2467 79738927
Drug abuse 35.92 24.98 37 2957 162654 79578740
Alcohol interaction 34.26 24.98 11 2983 4863 79736531
Hypertensive crisis 33.16 24.98 16 2978 20754 79720640
Hypochloraemia 32.12 24.98 9 2985 2506 79738888
Apraxia 30.96 24.98 9 2985 2858 79738536
Electrocardiogram QT prolonged 30.42 24.98 26 2968 90360 79651034
Hypoglycaemia 29.75 24.98 27 2967 101567 79639827
Subdural haematoma 26.93 24.98 16 2978 31418 79709976
Rectal haemorrhage 25.78 24.98 22 2972 76278 79665116
Haematidrosis 24.99 24.98 4 2990 72 79741322

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 2 Enzyme IC50 4.33 WOMBAT-PK
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
Cytochrome P450 2C19 Enzyme IC50 6.18 DRUG MATRIX
Cytochrome P450 2B6 Enzyme INHIBITOR IC50 6.70 IUPHAR
Bile salt export pump Transporter IC50 4.13 CHEMBL
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
DB00208 DRUGBANK_ID
CHEMBL1717 ChEMBL_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