valsartan indications/contra

Stem definitionDrug idCAS RN
angiotensin II receptor antagonists, antihypertensive (non-peptidic) 2806 137862-53-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • diovan
  • cardopan
  • valsartanin
  • valsartan
  • CGP 48933
  • CGP-48933
A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.
  • Molecular weight: 435.53
  • Formula: C24H29N5O3
  • CLOGP: 4.86
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 2
  • TPSA: 112.07
  • ALOGS: -4.28
  • ROTB: 10

Drug dosage:

DoseUnitRoute
80 mg O

Approvals:

DateAgencyCompanyOrphan
Dec. 23, 1996 FDA

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
Hypotension 4468.34 26.31 1558 14479 47956 3321866
Dizziness 1903.71 26.31 967 15070 75545 3294277
Blood pressure increased 1653.52 26.31 611 15426 21619 3348203
Blood creatinine increased 1583.28 26.31 589 15448 21229 3348593
Hyperkalaemia 1440.41 26.31 465 15572 10829 3358993
Cardiac failure 1284.81 26.31 495 15542 19610 3350212
Acute kidney injury 1192.40 26.31 615 15422 49068 3320754
Dyspnoea 1191.67 26.31 793 15244 102141 3267681
Angioedema 1112.30 26.31 413 15624 14722 3355100
Malaise 1065.03 26.31 626 15411 64551 3305271
Blood pressure inadequately controlled 1017.48 26.31 229 15808 1191 3368631
Blood pressure decreased 1003.38 26.31 374 15663 13462 3356360
Hypertension 929.56 26.31 479 15558 37987 3331835
Cough 922.09 26.31 482 15555 39376 3330446
Renal failure 856.01 26.31 431 15606 32509 3337313
Hyponatraemia 718.87 26.31 319 15718 18040 3351782
Death 718.78 26.31 694 15343 151630 3218192
Renal impairment 714.06 26.31 317 15720 17944 3351878
Blood urea increased 672.95 26.31 238 15799 7322 3362500
Oedema peripheral 660.84 26.31 368 15669 33993 3335829
Fall 609.37 26.31 425 15612 58458 3311364
Blood potassium increased 607.81 26.31 189 15848 3847 3365975
Diabetes mellitus 593.77 26.31 247 15790 11886 3357936
Fatigue 558.29 26.31 517 15520 106723 3263099
Contraindicated product administered 523.16 26.31 124 15913 836 3368986
Pruritus 488.54 26.31 340 15697 46493 3323329
Syncope 488.10 26.31 273 15764 25360 3344462
Asthenia 475.83 26.31 383 15654 65282 3304540
Feeling abnormal 469.97 26.31 273 15764 27252 3342570
Loss of consciousness 443.33 26.31 265 15772 27882 3341940

Pharmacologic Action:

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SourceCodeDescription
ATC C09CA03 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, PLAIN
Angiotensin II antagonists, plain
ATC C09DA03 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and diuretics
ATC C09DB01 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DB08 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists and calcium channel blockers
ATC C09DX01 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists, other combinations
ATC C09DX02 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists, other combinations
ATC C09DX04 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ANGIOTENSIN II ANTAGONISTS, COMBINATIONS
Angiotensin II antagonists, other combinations
ATC C10BX10 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, COMBINATIONS
HMG CoA reductase inhibitors, other combinations
MeSH PA D047228 Angiotensin II Type 1 Receptor Blockers
MeSH PA D057911 Angiotensin Receptor Antagonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:61016 angiotensin receptor antagonist
FDA MoA N0000000070 Angiotensin 2 Receptor Antagonists
FDA EPC N0000175561 Angiotensin 2 Receptor Blocker

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Chronic heart failure indication 48447003
Left ventricular cardiac dysfunction indication 429589006
Anuria contraindication 2472002 DOID:2983
Hypercholesterolemia contraindication 13644009
Hyperkalemia contraindication 14140009
Secondary angle-closure glaucoma contraindication 21571006
Hypovolemia contraindication 28560003
Obstruction of bile duct contraindication 30144000 DOID:13580
Dehydration contraindication 34095006
Hyperuricemia contraindication 35885006 DOID:1920
Angioedema contraindication 41291007 DOID:1558
Hypokalemia contraindication 43339004
Low blood pressure contraindication 45007003
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
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
Chronic idiopathic constipation contraindication 82934008
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Hypomagnesemia contraindication 190855004
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Renal artery stenosis contraindication 302233006
Neutropenic disorder contraindication 303011007 DOID:1227
Azotemia contraindication 445009001
Severe Aortic Valve Stenosis contraindication
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 3.8 acidic
pKa2 4.44 acidic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
160MG VALTURNA NOVARTIS N022217 Sept. 16, 2009 DISCN TABLET ORAL 5559111 July 21, 2018 TREATMENT OF HYPERTENSION
320MG VALTURNA NOVARTIS N022217 Sept. 16, 2009 DISCN TABLET ORAL 5559111 July 21, 2018 TREATMENT OF HYPERTENSION
103MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL 8796331 Jan. 14, 2023 TREATMENT OF HEART FAILURE
26MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL 8796331 Jan. 14, 2023 TREATMENT OF HEART FAILURE
51MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL 8796331 Jan. 14, 2023 TREATMENT OF HEART FAILURE
103MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL 9388134 Nov. 8, 2026 TREATMENT OF HEART FAILURE
26MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL 9388134 Nov. 8, 2026 TREATMENT OF HEART FAILURE
51MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL 9388134 Nov. 8, 2026 TREATMENT OF HEART FAILURE
80MG BYVALSON ALLERGAN SALES LLC N206302 June 3, 2016 RX TABLET ORAL 7838552 Oct. 4, 2027 METHOD OF TREATING HYPERTENSION

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
80MG BYVALSON ALLERGAN SALES LLC N206302 June 3, 2016 RX TABLET ORAL June 3, 2019 NEW COMBINATION
103MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL July 7, 2020 NEW CHEMICAL ENTITY
26MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL July 7, 2020 NEW CHEMICAL ENTITY
51MG ENTRESTO NOVARTIS PHARMS CORP N207620 July 7, 2015 RX TABLET ORAL July 7, 2020 NEW CHEMICAL ENTITY

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Type-1 angiotensin II receptor GPCR ANTAGONIST Ki 5.33 CHEMBL CHEMBL
Type-1B angiotensin II receptor GPCR IC50 8.72 CHEMBL
Type-1A angiotensin II receptor GPCR IC50 8.47 CHEMBL
Angiotensin II receptor (AT-1) type-1 GPCR IC50 8.57 CHEMBL

External reference:

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IDSource
DB00177 DRUGBANK_ID
3937 IUPHAR_LIGAND_ID
C0719949 UMLSCUI
D00400 KEGG_DRUG
80M03YXJ7I UNII
7016 INN_ID
4020986 VANDF
N0000006659 NDFRT
N0000148456 NDFRT
006279 NDDF
d04113 MMSL
5663 MMSL
69749 RXNORM
108581009 SNOMEDCT_US
386876001 SNOMEDCT_US
53010 MMSL
CHEMBL1069 ChEMBL_ID
60846 PUBCHEM_CID
D000068756 MESH_DESCRIPTOR_UI
CHEBI:9927 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Byvalson HUMAN PRESCRIPTION DRUG LABEL 2 0023-5874 TABLET, FILM COATED 80 mg ORAL NDA 18 sections
Diovan HCT HUMAN PRESCRIPTION DRUG LABEL 2 0078-0314 TABLET, FILM COATED 80 mg ORAL NDA 18 sections
Diovan HCT HUMAN PRESCRIPTION DRUG LABEL 2 0078-0315 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Diovan HUMAN PRESCRIPTION DRUG LABEL 1 0078-0358 TABLET 80 mg ORAL NDA 18 sections
Diovan HUMAN PRESCRIPTION DRUG LABEL 1 0078-0359 TABLET 160 mg ORAL NDA 18 sections
Diovan HUMAN PRESCRIPTION DRUG LABEL 1 0078-0360 TABLET 320 mg ORAL NDA 18 sections
Diovan HCT HUMAN PRESCRIPTION DRUG LABEL 2 0078-0383 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Diovan HUMAN PRESCRIPTION DRUG LABEL 1 0078-0423 TABLET 40 mg ORAL NDA 18 sections
Diovan HCT HUMAN PRESCRIPTION DRUG LABEL 2 0078-0471 TABLET, FILM COATED 320 mg ORAL NDA 18 sections
Diovan HCT HUMAN PRESCRIPTION DRUG LABEL 2 0078-0472 TABLET, FILM COATED 320 mg ORAL NDA 18 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0488 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0489 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0490 TABLET, FILM COATED 320 mg ORAL NDA 18 sections
Exforge HUMAN PRESCRIPTION DRUG LABEL 2 0078-0491 TABLET, FILM COATED 320 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0559 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0560 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0561 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0562 TABLET, FILM COATED 160 mg ORAL NDA 18 sections
Exforge HCT HUMAN PRESCRIPTION DRUG LABEL 3 0078-0563 TABLET, FILM COATED 320 mg ORAL NDA 18 sections
ENTRESTO HUMAN PRESCRIPTION DRUG LABEL 2 0078-0659 TABLET, FILM COATED 26 mg ORAL NDA 19 sections
ENTRESTO HUMAN PRESCRIPTION DRUG LABEL 2 0078-0696 TABLET, FILM COATED 103 mg ORAL NDA 19 sections
ENTRESTO HUMAN PRESCRIPTION DRUG LABEL 2 0078-0777 TABLET, FILM COATED 51 mg ORAL NDA 19 sections
Amlodipine, Valsartan, and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 3 0093-7037 TABLET, FILM COATED 160 mg ORAL ANDA 18 sections
Amlodipine, Valsartan, and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 3 0093-7038 TABLET, FILM COATED 160 mg ORAL ANDA 18 sections
Amlodipine and Valsartan HUMAN PRESCRIPTION DRUG LABEL 2 0093-7690 TABLET, FILM COATED 160 mg ORAL ANDA 18 sections
Amlodipine and Valsartan HUMAN PRESCRIPTION DRUG LABEL 2 0093-7691 TABLET, FILM COATED 160 mg ORAL ANDA 18 sections
Amlodipine and Valsartan HUMAN PRESCRIPTION DRUG LABEL 2 0093-7692 TABLET, FILM COATED 320 mg ORAL ANDA 18 sections
Amlodipine and Valsartan HUMAN PRESCRIPTION DRUG LABEL 2 0093-7693 TABLET, FILM COATED 320 mg ORAL ANDA 18 sections
Amlodipine, Valsartan, and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 3 0093-7807 TABLET, FILM COATED 160 mg ORAL ANDA 18 sections
Amlodipine, Valsartan, and Hydrochlorothiazide HUMAN PRESCRIPTION DRUG LABEL 3 0093-7809 TABLET, FILM COATED 320 mg ORAL ANDA 18 sections