bivalirudin indications/contra

Stem definitionDrug idCAS RN
hirudin derivatives 385 128270-60-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • bivalirudin
  • angiomax
  • angiox
  • hirulog
designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition
  • Molecular weight: 2180.32
  • Formula: C98H138N24O33
  • CLOGP: 0
  • LIPINSKI: 3
  • HAC: 57
  • HDO: 28
  • TPSA: 901.57
  • ALOGS: -4.67
  • ROTB: 66

Drug dosage:

DoseUnitRoute
0.25 g P

Approvals:

DateAgencyCompanyOrphan
Dec. 15, 2000 FDA MEDICINES CO

FDA Adverse Event Reporting System

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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
Thrombosis in device 1184.51 115.61 180 1099 1578 3383002
Coronary artery thrombosis 1099.91 115.61 154 1125 694 3383886
Coagulation time abnormal 846.85 115.61 101 1178 56 3384524
Thrombosis 463.40 115.61 115 1164 13975 3370605
Device occlusion 421.37 115.61 73 1206 1458 3383122
Haemorrhage 367.89 115.61 103 1176 19818 3364762
Procedural complication 280.14 115.61 55 1224 2205 3382375
Coronary artery dissection 238.08 115.61 34 1245 171 3384409
Coronary artery perforation 199.72 115.61 25 1254 31 3384549
Myocardial infarction 195.62 115.61 78 1201 44055 3340525
Coronary artery occlusion 194.78 115.61 43 1236 3052 3381528
Chest pain 191.82 115.61 75 1204 40200 3344380
Cardiac procedure complication 187.03 115.61 27 1252 148 3384432
Hypotension 173.47 115.61 74 1205 49440 3335140
Vascular pseudoaneurysm 168.76 115.61 29 1250 541 3384039
Cardiac arrest 155.36 115.61 58 1221 27261 3357319
Vascular stent thrombosis 153.34 115.61 26 1253 446 3384134
Retroperitoneal haemorrhage 151.13 115.61 29 1250 1019 3383561
Coagulation time prolonged 142.86 115.61 25 1254 520 3384060
International normalised ratio increased 140.74 115.61 46 1233 14569 3370011
Ventricular fibrillation 139.55 115.61 35 1244 4298 3380282
Post procedural complication 134.46 115.61 35 1244 4982 3379598
Cardio-respiratory arrest 130.29 115.61 44 1235 15396 3369184
Haematoma 129.28 115.61 37 1242 7502 3377078
Haemorrhage intracranial 118.08 115.61 32 1247 5307 3379273

Pharmacologic Action:

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SourceCodeDescription
ATC B01AE06 BLOOD AND BLOOD FORMING ORGANS
ANTITHROMBOTIC AGENTS
ANTITHROMBOTIC AGENTS
Direct thrombin inhibitors
FDA EPC N0000175980 Anti-coagulant
FDA EPC N0000175518 Direct Thrombin Inhibitor
FDA MoA N0000009963 Thrombin Inhibitors
MeSH PA D000925 Anticoagulants
MeSH PA D000991 Antithrombins
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006401 Hematologic Agents
MeSH PA D011480 Protease Inhibitors
MeSH PA D015842 Serine Proteinase Inhibitors
CHEBI has role CHEBI:50249 anticoagulant

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Percutaneous coronary intervention indication 415070008
Unstable Angina Pectoris during PTCA indication
Intracranial hemorrhage contraindication 1386000
Bleeding contraindication 131148009
Acute coronary syndrome off-label use 394659003

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Prothrombin Enzyme INHIBITOR Ki 8.60 IUPHAR CHEMBL

External reference:

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IDSource
DB00006 DRUGBANK_ID
4021268 VUID
N0000148708 NUI
C0168273 UMLSCUI
6470 IUPHAR_LIGAND_ID
D03136 KEGG_DRUG
N0000148708 NDFRT
N0000010076 NDFRT
009031 NDDF
d04744 MMSL
15879 MMSL
60819 RXNORM
4021268 VANDF
129498009 SNOMEDCT_US
400610005 SNOMEDCT_US
234768 MMSL
CHEMBL2103749 ChEMBL_ID
16129704 PUBCHEM_CID
TN9BEX005G UNII
7282 INN_ID
C074619 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:59173 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Bivalirudin in 0.9% Sodium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 0338-9572 INJECTION 250 mg INTRAVENOUS NDA 16 sections
Bivalirudin in 0.9% Sodium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 0338-9576 INJECTION 500 mg INTRAVENOUS NDA 16 sections
Bivalirudin HUMAN PRESCRIPTION DRUG LABEL 1 0409-8300 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS ANDA 17 sections
bivalirudin HUMAN PRESCRIPTION DRUG LABEL 1 0781-3158 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS NDA authorized generic 17 sections
bivalirudin HUMAN PRESCRIPTION DRUG LABEL 1 0781-9158 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS NDA authorized generic 17 sections
Bivalirudin HUMAN PRESCRIPTION DRUG LABEL 1 55111-652 INJECTION 250 mg INTRACAVERNOUS ANDA 17 sections
Bivalirudin HUMAN PRESCRIPTION DRUG LABEL 1 60505-6101 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS ANDA 17 sections
Bivalirudin HUMAN PRESCRIPTION DRUG LABEL 1 63323-562 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS ANDA 18 sections
Angiomax HUMAN PRESCRIPTION DRUG LABEL 1 65293-001 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 250 mg INTRAVENOUS NDA 17 sections