eprosartan indications/contra

Stem definitionDrug idCAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic) 1037 133040-01-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • SKF-108566
  • eprosartan
  • eprosartan mesylate
  • eprosartan mesilate
angiotensin II receptor antagonist; structure given in first source
  • Molecular weight: 424.52
  • Formula: C23H24N2O4S
  • CLOGP: 4.80
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 92.42
  • ALOGS: -4.69
  • ROTB: 10

Drug dosage:

DoseUnitRoute
0.60 g O

Approvals:

DateAgencyCompanyOrphan
Dec. 22, 1997 FDA ABBVIE

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
ATC C09CA02 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, PLAIN
Angiotensin II antagonists, plain
ATC C09DA02 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and diuretics
FDA MoA N0000000070 Angiotensin 2 Receptor Antagonists
FDA EPC N0000175561 Angiotensin 2 Receptor Blocker
MeSH PA D057912 Angiotensin II Type 2 Receptor Blockers
MeSH PA D057911 Angiotensin Receptor Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
CHEBI has role CHEBI:61016 angiotensin receptor antagonist
CHEBI has role CHEBI:35674 antihypertensive agent

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Azotemia contraindication 445009001
Chronic heart failure off-label use 48447003
Atrial fibrillation off-label use 49436004 DOID:0060224
Diabetic renal disease off-label use 127013003
Diastolic heart failure off-label use 418304008 DOID:9775
Nondiabetic Proteinuric Nephropathy off-label use

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.12 acidic
pKa2 4.83 acidic
pKa3 7.22 Basic

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
Type-1 angiotensin II receptor GPCR ANTAGONIST IC50 8.70 CHEMBL CHEMBL
Angiotensin II receptor GPCR IC50 9 CHEMBL
Type-1B angiotensin II receptor GPCR IC50 9 CHEMBL
Type-2 angiotensin II receptor GPCR IC50 9 CHEMBL
Angiotensin II receptor (AT-1) type-1 GPCR IC50 9 CHEMBL

External reference:

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IDSource
588 IUPHAR_LIGAND_ID
4021199 VUID
N0000148645 NUI
C0287041 UMLSCUI
D02082 KEGG_DRUG
2KH13Z0S0Y UNII
7223 INN_ID
DB00876 DRUGBANK_ID
CHEMBL813 ChEMBL_ID
4021199 VANDF
N0000006926 NDFRT
N0000148645 NDFRT
d04266 MMSL
83515 RXNORM
318990002 SNOMEDCT_US
396044005 SNOMEDCT_US
007065 NDDF
144143-96-4 SECONDARY_CAS_RN
5281037 PUBCHEM_CID
CHEMBL1200987 ChEMBL_ID
C068373 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:4814 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Eprosartan Mesylate HUMAN PRESCRIPTION DRUG LABEL 1 0378-6629 TABLET, FILM COATED 600 mg ORAL ANDA 13 sections
Teveten HCT HUMAN PRESCRIPTION DRUG LABEL 2 54868-5281 TABLET 600 mg ORAL NDA 13 sections