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

Stem definitionDrug idCAS RN
4839 9087-70-1

Description:

MoleculeDescription

Synonyms:

  • aprotinin
  • trasylol
A single-chain polypeptide derived from bovine tissues consisting of 58 amino-acid residues. It is an inhibitor of proteolytic enzymes including CHYMOTRYPSIN; KALLIKREIN; PLASMIN; and TRYPSIN. It is used in the treatment of HEMORRHAGE associated with raised plasma concentrations of plasmin. It is also used to reduce blood loss and transfusion requirements in patients at high risk of major blood loss during and following open heart surgery with EXTRACORPOREAL CIRCULATION. (Reynolds JEF(Ed): Martindale: The Extra Pharmacopoeia (electronic version). Micromedex, Inc, Englewood, CO, 1995)
  • Molecular weight: 6511.51
  • Formula: C284H432N84O79S7
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 2645.74
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
500 TU P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 29, 1993 FDA BAYER HLTHCARE

FDA Adverse Event Reporting System (Female)

None

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
Product use in unapproved indication 266.70 233.51 69 126 117430 34839306

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
Product use in unapproved indication 315.48 153.35 85 204 250274 79493825
Off label use 179.57 153.35 77 212 907138 78836961

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B02AB01 BLOOD AND BLOOD FORMING ORGANS
ANTIHEMORRHAGICS
ANTIFIBRINOLYTICS
Proteinase inhibitors
MeSH PA D003029 Coagulants
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006401 Hematologic Agents
MeSH PA D006490 Hemostatics
MeSH PA D011480 Protease Inhibitors
MeSH PA D015842 Serine Proteinase Inhibitors
MeSH PA D014361 Trypsin Inhibitors
FDA PE N0000175632 Decreased Fibrinolysis
FDA EPC N0000175634 Antifibrinolytic Agent

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

DiseaseRelationSNOMED_IDDOID
Hemorrhage indication 50960005




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Plasminogen Enzyme INHIBITOR IC50 6.80 IUPHAR CHEMBL
Plasma kallikrein Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
04XPW8C0FL UNII
4020852 VUID
N0000148360 NUI
4020852 VANDF
C0003641 UMLSCUI
CHEMBL1201619 ChEMBL_ID
16130295 PUBCHEM_CID
DB06692 DRUGBANK_ID
D007611 MESH_DESCRIPTOR_UI
2481 INN_ID
6570 IUPHAR_LIGAND_ID
1056 RXNORM
1439 MMSL
4215 MMSL
d03185 MMSL
003455 NDDF
109008002 SNOMEDCT_US
386961008 SNOMEDCT_US

Pharmaceutical products:

None