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 63.21 32.43 46 1249 209709 56081063
Sopor 51.45 32.43 19 1276 20903 56269869
Hyponatraemic syndrome 43.72 32.43 8 1287 536 56290236
Hyperkalaemia 40.96 32.43 21 1274 50844 56239928
Hypochloraemia 39.96 32.43 9 1286 1703 56289069
Apraxia 39.92 32.43 9 1286 1710 56289062
Hypercreatininaemia 39.59 32.43 7 1288 386 56290386
Cerebral haemorrhage 35.81 32.43 16 1279 28590 56262182

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 56.14 27.06 57 1366 208486 31487435
Sopor 50.06 27.06 19 1404 11533 31684388
Slow speech 49.03 27.06 11 1412 1043 31694878
Intentional self-injury 43.99 27.06 18 1405 13297 31682624
Alcohol interaction 38.40 27.06 11 1412 2778 31693143
Melaena 36.50 27.06 21 1402 32633 31663288
Electrocardiogram QT prolonged 31.06 27.06 20 1403 37967 31657954
Hyponatraemia 31.06 27.06 26 1397 73773 31622148
Mechanical urticaria 30.51 27.06 5 1418 87 31695834
Anaemia 30.01 27.06 42 1381 213480 31482441
Drug abuse 29.10 27.06 27 1396 87731 31608190
Coombs negative haemolytic anaemia 27.90 27.06 5 1418 150 31695771

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 105.46 24.66 102 2831 381339 70544172
Sopor 91.99 24.66 38 2895 31229 70894282
Melaena 62.34 24.66 35 2898 56320 70869191
Intentional self-injury 56.14 24.66 27 2906 31623 70893888
Anaemia 51.99 24.66 73 2860 403350 70522161
Cerebral haemorrhage 50.37 24.66 30 2903 53834 70871677
Hyponatraemic syndrome 47.64 24.66 10 2923 753 70924758
Hyponatraemia 44.31 24.66 43 2890 160044 70765467
Hyperkalaemia 42.09 24.66 35 2898 106556 70818955
Slow speech 41.90 24.66 11 2922 2181 70923330
Drug abuse 41.58 24.66 40 2893 147216 70778295
Alcohol interaction 33.72 24.66 11 2922 4642 70920869
Hypertensive crisis 32.84 24.66 16 2917 19246 70906265
Hypochloraemia 32.66 24.66 9 2924 2142 70923369
Apraxia 30.69 24.66 9 2924 2674 70922837
Electrocardiogram QT prolonged 30.03 24.66 26 2907 83491 70842020
Hypoglycaemia 29.22 24.66 27 2906 94337 70831174
Rectal haemorrhage 26.76 24.66 22 2911 65809 70859702
Subdural haematoma 26.54 24.66 16 2917 29282 70896229
Hypercreatininaemia 24.96 24.66 6 2927 833 70924678
Haematidrosis 24.87 24.66 4 2929 67 70925444

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
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