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Identification
NameValsartan
Accession NumberDB00177  (APRD00133)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Valsartan is an angiotensin-receptor blocker (ARB) that may be used to treat a variety of cardiac conditions including hypertension, diabetic nephropathy and heart failure. Valsartan lowers blood pressure by antagonizing the renin-angiotensin-aldosterone system (RAAS); it competes with angiotensin II for binding to the type-1 angiotensin II receptor (AT1) subtype and prevents the blood pressure increasing effects of angiotensin II. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of dry cough. Valsartan may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction and coronary artery disease.

Structure
Thumb
Synonyms
(S)-N-Valeryl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]-methyl}-valine
Diovan
N-(P-(O-1H-Tetrazol-5-ylphenyl)benzyl)-N-valeryl-L-valine
N-pentanoyl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-L-valine
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Valsartantablet320 mgoralActavis Pharma Company2011-02-16Not applicableCanada
Act Valsartantablet160 mgoralActavis Pharma Company2011-02-16Not applicableCanada
Act Valsartantablet80 mgoralActavis Pharma Company2011-02-16Not applicableCanada
Act Valsartantablet40 mgoralActavis Pharma Company2011-02-16Not applicableCanada
Auro-valsartantablet80 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-valsartantablet40 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-valsartantablet320 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Auro-valsartantablet160 mgoralAuro Pharma Inc2014-02-06Not applicableCanada
Ava-valsartantablet320 mgoralAvanstra Inc2011-08-182014-08-21Canada
Ava-valsartantablet160 mgoralAvanstra Inc2011-08-182014-08-21Canada
Ava-valsartantablet80 mgoralAvanstra Inc2011-08-182014-08-21Canada
Ava-valsartantablet40 mgoralAvanstra Inc2011-08-182014-08-21Canada
Diovantablet80 mg/1oralCarilion Materials Management2001-07-012016-04-05Us
Diovantablet320 mg/1oralCardinal Health2001-07-012016-04-05Us
Diovantablet160 mg/1oralPhysicians Total Care, Inc.2008-02-282016-04-05Us
Diovantablet40 mg/1oralCarilion Materials Management2001-07-012016-04-05Us
Diovantablet80 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-282016-04-05Us
Diovantablet80 mg/1oralRebel Distributors Corp2001-07-012016-04-05Us
Diovantablet80 mg/1oralNovartis Pharmaceuticals Corporation2001-07-012016-04-23Us
Diovantablet160 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-282016-04-05Us
Diovantablet160 mg/1oralAphena Pharma Solutions Tennessee, Llc2001-07-012016-04-05Us
Diovantablet160 mg/1oralCardinal Health2001-07-012016-04-05Us
Diovantablet320 mgoralNovartis Pharmaceuticals Canada Inc2007-02-14Not applicableCanada
Diovantablet40 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-152016-04-05Us
Diovantablet80 mg/1oralAphena Pharma Solutions Tennessee, Llc2001-07-012016-04-05Us
Diovantablet40 mgoralNovartis Pharmaceuticals Canada Inc2005-11-01Not applicableCanada
Diovantablet160 mg/1oralREMEDYREPACK INC.2013-09-112016-04-05Us
Diovantablet160 mg/1oralbryant ranch prepack2001-07-012016-04-05Us
Diovantablet80 mg/1oralREMEDYREPACK INC.2014-01-092016-04-05Us
Diovantablet80 mg/1oralbryant ranch prepack2001-07-012016-04-05Us
Diovantablet80 mg/1oralCardinal Health2001-07-012016-04-05Us
Diovantablet320 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-02-282016-04-05Us
Diovantablet40 mg/1oralNovartis Pharmaceuticals Corporation2001-07-012016-04-23Us
Diovantablet320 mg/1oralPd Rx Pharmaceuticals, Inc.2001-07-012016-04-05Us
Diovantablet40 mg/1oralPhysicians Total Care, Inc.2009-01-022016-04-05Us
Diovantablet320 mg/1oralRebel Distributors Corp2001-07-012016-04-05Us
Diovantablet320 mg/1oralNovartis Pharmaceuticals Corporation2001-07-012016-04-23Us
Diovantablet80 mg/1oralPd Rx Pharmaceuticals, Inc.2001-07-012016-04-05Us
Diovantablet320 mg/1oralPhysicians Total Care, Inc.2007-09-172016-04-05Us
Diovantablet160 mg/1oralPd Rx Pharmaceuticals, Inc.2001-07-012016-04-05Us
Diovantablet80 mg/1oralPhysicians Total Care, Inc.2010-01-062016-04-05Us
Diovantablet160 mg/1oralRebel Distributors Corp2001-07-012016-04-05Us
Diovantablet160 mg/1oralNovartis Pharmaceuticals Corporation2001-07-012016-04-23Us
Diovan 160mgcapsule160 mgoralNovartis Pharmaceuticals Canada Inc1997-12-15Not applicableCanada
Diovan 160mg Tabletstablet160 mgoralNovartis Pharmaceuticals Canada Inc2003-01-24Not applicableCanada
Diovan 80mgcapsule80 mgoralNovartis Pharmaceuticals Canada Inc1997-12-15Not applicableCanada
Diovan 80mg Tabletstablet80 mgoralNovartis Pharmaceuticals Canada Inc2003-01-24Not applicableCanada
Dom-valsartantablet40 mgoralDominion PharmacalNot applicableNot applicableCanada
Dom-valsartantablet80 mgoralDominion Pharmacal2014-02-03Not applicableCanada
Dom-valsartantablet320 mgoralDominion PharmacalNot applicableNot applicableCanada
Dom-valsartantablet160 mgoralDominion PharmacalNot applicableNot applicableCanada
Mylan-valsartantablet40 mgoralMylan Pharmaceuticals Ulc2012-04-27Not applicableCanada
Mylan-valsartantablet320 mgoralMylan Pharmaceuticals Ulc2012-04-27Not applicableCanada
Mylan-valsartantablet160 mgoralMylan Pharmaceuticals Ulc2012-04-27Not applicableCanada
Mylan-valsartantablet80 mgoralMylan Pharmaceuticals Ulc2012-04-27Not applicableCanada
Novo-valsartantablet80 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Novo-valsartantablet40 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Novo-valsartantablet320 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Novo-valsartantablet160 mgoralTeva Canada LimitedNot applicableNot applicableCanada
PMS-valsartantablet80 mgoralPharmascience Inc2012-05-22Not applicableCanada
PMS-valsartantablet40 mgoralPharmascience Inc2012-05-22Not applicableCanada
PMS-valsartantablet320 mgoralPharmascience Inc2012-05-22Not applicableCanada
PMS-valsartantablet160 mgoralPharmascience Inc2012-05-22Not applicableCanada
Q-valsartantablet320 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-valsartantablet160 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-valsartantablet80 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-valsartantablet40 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Ran-valsartantablet160 mgoralRanbaxy Pharmaceuticals Canada Inc.2011-02-16Not applicableCanada
Ran-valsartantablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.2011-02-16Not applicableCanada
Ran-valsartantablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.2011-02-16Not applicableCanada
Riva-valsartantablet320 mgoralLaboratoire Riva Inc2014-12-03Not applicableCanada
Riva-valsartantablet160 mgoralLaboratoire Riva Inc2014-12-03Not applicableCanada
Riva-valsartantablet80 mgoralLaboratoire Riva Inc2014-12-03Not applicableCanada
Riva-valsartantablet40 mgoralLaboratoire Riva Inc2014-12-03Not applicableCanada
Sandoz Valsartantablet320 mgoralSandoz Canada Incorporated2011-01-27Not applicableCanada
Sandoz Valsartantablet160 mgoralSandoz Canada Incorporated2011-01-27Not applicableCanada
Sandoz Valsartantablet80 mgoralSandoz Canada Incorporated2011-01-27Not applicableCanada
Sandoz Valsartantablet40 mgoralSandoz Canada Incorporated2011-01-27Not applicableCanada
Teva-valsartantablet80 mgoralTeva Canada Limited2011-02-16Not applicableCanada
Teva-valsartantablet160 mgoralTeva Canada Limited2011-02-16Not applicableCanada
Teva-valsartantablet40 mgoralTeva Canada Limited2011-02-16Not applicableCanada
Teva-valsartantablet320 mgoralTeva Canada Limited2011-02-16Not applicableCanada
Valsartantablet320 mgoralPro Doc Limitee2011-05-30Not applicableCanada
Valsartantablet160 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Valsartantablet160 mgoralPro Doc Limitee2011-05-30Not applicableCanada
Valsartantablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Valsartantablet320 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Valsartantablet320 mg/1oralSandoz Inc2014-07-072016-04-05Us
Valsartantablet80 mgoralPro Doc Limitee2011-05-30Not applicableCanada
Valsartantablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Valsartantablet160 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Valsartantablet160 mg/1oralSandoz Inc2014-07-072016-04-05Us
Valsartantablet320 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Valsartantablet80 mg/1oralCardinal Health2014-07-072016-04-05Us
Valsartantablet40 mgoralPro Doc Limitee2011-05-30Not applicableCanada
Valsartantablet80 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Valsartantablet80 mg/1oralSandoz Inc2014-07-072016-04-05Us
Valsartantablet80 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Valsartantablet160 mg/1oralCardinal Health2014-07-072016-04-05Us
Valsartantablet320 mgoralSanis Health Inc2012-07-20Not applicableCanada
Valsartantablet40 mgoralSivem Pharmaceuticals Ulc2012-06-10Not applicableCanada
Valsartantablet40 mg/1oralSandoz Inc2014-07-072016-04-05Us
Valsartantablet160 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Valsartantablet40 mgoralActavis Pharma CompanyNot applicableNot applicableCanada
Valsartantablet160 mgoralSanis Health Inc2012-07-20Not applicableCanada
Valsartantablet80 mgoralSanis Health Inc2012-07-20Not applicableCanada
Valsartantablet40 mgoralSanis Health Inc2012-07-20Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-valsartantablet40 mgoralApotex Inc2012-07-12Not applicableCanada
Apo-valsartantablet320 mgoralApotex Inc2012-07-12Not applicableCanada
Apo-valsartantablet160 mgoralApotex Inc2012-07-12Not applicableCanada
Apo-valsartantablet80 mgoralApotex Inc2012-07-12Not applicableCanada
Valsartantablet40 mg/1oralTorrent Pharmaceuticals Limited2015-01-052016-04-05Us
Valsartantablet, film coated40 mg/1oralActavis Pharma, Inc.2015-01-052016-04-23Us
Valsartantablet, film coated40 mg/1oralTeva Pharmaceuticals USA Inc2015-01-052017-05-31Us
Valsartantablet80 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-12-232016-04-05Us
Valsartantablet, film coated40 mg/1oralOhm Laboratories Inc.2014-07-072016-04-05Us
Valsartantablet320 mg/1oralAmneal Pharmaceuticals of New York, LLC2016-01-172016-04-05Us
Valsartantablet160 mg/1oralSolco Healthcare US, LLC2015-08-312016-04-05Us
Valsartantablet40 mg/1oralLupin Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet160 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-12-232016-04-05Us
Valsartantablet80 mg/1oralSolco Healthcare US, LLC2015-08-312016-04-05Us
Valsartantablet, film coated80 mg/1oralAv Kare, Inc.2015-11-122016-04-05Us
Valsartantablet80 mg/1oralTorrent Pharmaceuticals Limited2015-01-052016-04-05Us
Valsartantablet40 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-12-232016-04-05Us
Valsartantablet, film coated160 mg/1oralNorthwind Pharmaceuticals2015-01-072016-04-05Us
Valsartantablet160 mg/1oralAmneal Pharmaceuticals of New York, LLC2016-01-172016-04-05Us
Valsartantablet, film coated320 mg/1oralAurobindo Pharma Limited2015-01-052016-04-05Us
Valsartantablet40 mg/1oralSolco Healthcare US, LLC2015-08-312016-04-05Us
Valsartantablet, film coated40 mg/1oralAv Kare, Inc.2015-11-122016-04-05Us
Valsartantablet320 mg/1oralQualitest Pharmaceuticals2015-01-062016-04-23Us
Valsartantablet, film coated320 mg/1oralMylan Pharmaceuticals Inc.2015-01-052016-04-23Us
Valsartantablet, film coated80 mg/1oralPhysicians Total Care, Inc.2015-01-052016-04-05Us
Valsartantablet, film coated80 mg/1oralNorthwind Pharmaceuticals, LLC2014-11-132016-04-05Us
Valsartantablet80 mg/1oralAmneal Pharmaceuticals of New York, LLC2016-01-172016-04-05Us
Valsartantablet, film coated160 mg/1oralAurobindo Pharma Limited2015-01-052016-04-05Us
Valsartantablet, film coated320 mg/1oralAv Kare, Inc.2015-01-292016-04-05Us
Valsartantablet, film coated320 mg/1oralCamber Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet160 mg/1oralQualitest Pharmaceuticals2015-01-062016-04-23Us
Valsartantablet, film coated160 mg/1oralMylan Pharmaceuticals Inc.2015-01-052016-04-23Us
Valsartantablet, film coated320 mg/1oralPhysicians Total Care, Inc.2015-01-052016-04-05Us
Valsartantablet320 mg/1oralAlembic Pharmaceuticals Limited2015-01-062016-04-05Us
Valsartantablet40 mg/1oralAmneal Pharmaceuticals of New York, LLC2016-01-172016-04-05Us
Valsartantablet, film coated80 mg/1oralAurobindo Pharma Limited2015-01-052016-04-05Us
Valsartantablet, film coated160 mg/1oralAv Kare, Inc.2015-01-292016-04-05Us
Valsartantablet, film coated160 mg/1oralCamber Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet80 mg/1oralQualitest Pharmaceuticals2015-01-062016-04-23Us
Valsartantablet, film coated80 mg/1oralMylan Pharmaceuticals Inc.2015-01-052016-04-23Us
Valsartantablet, film coated80 mg/1oralAvera Mc Kennan Hospital2015-05-202016-04-05Us
Valsartantablet, film coated40 mg/1oralAurobindo Pharma Limited2015-01-052016-04-05Us
Valsartantablet, film coated80 mg/1oralAv Kare, Inc.2015-01-292016-04-05Us
Valsartantablet320 mg/1oralProficient Rx LP2015-08-312016-04-05Us
Valsartantablet, film coated80 mg/1oralCamber Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet40 mg/1oralQualitest Pharmaceuticals2015-01-062016-04-23Us
Valsartantablet, film coated40 mg/1oralMylan Pharmaceuticals Inc.2015-01-052016-04-23Us
Valsartantablet, film coated160 mg/1oralPhysicians Total Care, Inc.2015-01-052016-04-05Us
Valsartantablet160 mg/1oralAlembic Pharmaceuticals Limited2015-01-062016-04-05Us
Valsartantablet, film coated40 mg/1oralAv Kare, Inc.2015-01-292016-04-05Us
Valsartantablet, film coated40 mg/1oralCamber Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet, film coated320 mg/1oralActavis Pharma, Inc.2015-01-052016-04-23Us
Valsartantablet, film coated320 mg/1oralTeva Pharmaceuticals USA Inc2015-01-052016-10-31Us
Valsartantablet, film coated320 mg/1oralOhm Laboratories Inc.2014-07-072016-04-05Us
Valsartantablet80 mg/1oralAlembic Pharmaceuticals Limited2015-01-062016-04-05Us
Valsartantablet320 mg/1oralLupin Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet, film coated160 mg/1oralAmerican Health Packaging2015-02-202016-04-05Us
Valsartantablet, film coated320 mg/1oralAv Kare, Inc.2015-11-122016-04-05Us
Valsartantablet320 mg/1oralTorrent Pharmaceuticals Limited2015-01-052016-04-05Us
Valsartantablet, film coated160 mg/1oralActavis Pharma, Inc.2015-01-052016-04-23Us
Valsartantablet, film coated160 mg/1oralTeva Pharmaceuticals USA Inc2015-01-052017-07-31Us
Valsartantablet, film coated160 mg/1oralOhm Laboratories Inc.2014-07-072016-04-05Us
Valsartantablet40 mg/1oralAlembic Pharmaceuticals Limited2015-01-062016-04-05Us
Valsartantablet160 mg/1oralLupin Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet, film coated80 mg/1oralAmerican Health Packaging2015-02-202016-04-05Us
Valsartantablet, film coated80 mg/1oralActavis Pharma, Inc.2015-01-052016-04-23Us
Valsartantablet, film coated80 mg/1oralTeva Pharmaceuticals USA Inc2015-01-052017-05-31Us
Valsartantablet, film coated80 mg/1oralOhm Laboratories Inc.2014-07-072016-04-05Us
Valsartantablet320 mg/1oralSolco Healthcare US, LLC2015-08-312016-04-05Us
Valsartantablet80 mg/1oralLupin Pharmaceuticals, Inc.2015-01-052016-04-05Us
Valsartantablet320 mg/1oralJubilant Cadista Pharmaceuticals Inc.2014-12-232016-04-05Us
Valsartantablet, film coated160 mg/1oralAv Kare, Inc.2015-11-122016-04-05Us
Valsartantablet160 mg/1oralTorrent Pharmaceuticals Limited2015-01-052016-04-05Us
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Amlodipine and ValsartanTeva Pharmaceuticals USA Inc
Amlodipine Besylate and ValsartanMylan Pharmaceuticals Inc.
Amlodipine, Valsartan and HydrochlorothiazideTorrent Pharmaceuticals Limited
Amlodipine, Valsartan, and HydrochlorothiazideTeva Pharmaceuticals USA Inc
Amlodipine, Valsartan, HydrochlorothiazideSandoz Inc
Apo-valsartan/hctzApotex Inc
Auro-valsartan HctAuro Pharma Inc
Ava-valsartan HctAvanstra Inc
Diovan HctNovartis Pharmaceuticals Corporation
Diovan-hctNovartis Pharmaceuticals Canada Inc
EntrestoNovartis Pharmaceuticals Corporation
ExforgeNovartis Pharmaceuticals Corporation
Exforge HctNovartis Pharmaceuticals Corporation
Mylan-valsartan HctzMylan Pharmaceuticals Ulc
Novo-valsartan/hctzTeva Canada Limited
PMS-valsartan-hctzPharmascience Inc
Q-valsartan HctzQd Pharmaceuticals Ulc
Sandoz Valsartan HctSandoz Canada Incorporated
Teva-valsartan/hctzTeva Canada Limited
Valsartan and HydrochlorothiazideMylan Pharmaceuticals Inc.
Valsartan HctSanis Health Inc
Valsartan HctzNorthwind Pharmaceuticals
Valsartan-hctzPro Doc Limitee
SaltsNot Available
Categories
UNII80M03YXJ7I
CAS number137862-53-4
WeightAverage: 435.5188
Monoisotopic: 435.227039819
Chemical FormulaC24H29N5O3
InChI KeyInChIKey=ACWBQPMHZXGDFX-QFIPXVFZSA-N
InChI
InChI=1S/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m0/s1
IUPAC Name
(2S)-3-methyl-2-[N-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)pentanamido]butanoic acid
SMILES
CCCCC(=O)N(CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1)[C@@H](C(C)C)C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as biphenyltetrazoles and derivatives. These are organic compounds containing a biphenyl attached to a tetrazole. A carbon atom of the biphenyl moiety is boned to a carbon or the nitrogen atom of the tetrazole moiety.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassTetrazoles
Direct ParentBiphenyltetrazoles and derivatives
Alternative Parents
Substituents
  • Biphenyltetrazole
  • N-acyl-aliphatic-alpha amino acid
  • N-acyl-alpha amino acid or derivatives
  • N-acyl-alpha-amino acid
  • Biphenyl
  • N-acyl-l-alpha-amino acid
  • Alpha-amino acid or derivatives
  • Phenylmethylamine
  • Benzylamine
  • Benzenoid
  • N-acyl-amine
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationMay be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. May be used as a first line agent to delay progression of diabetic nephropathy. Losartan may be also used as a second line agent in the treatment of congestive heart failure, systolic dysfunction, myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors.
PharmacodynamicsValsartan belongs to a class of antihypertensive agents called angiotensin II receptor blockers (ARBs). Valsartan is a specific and selective type-1 angiotensin II receptor (AT1) antagonist which blocks the blood pressure increasing effects angiotensin II via the renin-angiotensin-aldosterone system (RAAS). RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from granular cells of the juxtaglomerular apparatus in the kidneys. Renin cleaves circulating angiotensinogen to angiotensin I, which is cleaved by angiotensin converting enzyme (ACE) to angiotensin II. Angiotensin II increases blood pressure by increasing total peripheral resistance, increasing sodium and water reabsorption in the kidneys via aldosterone secretion, and altering cardiovascular structure. Angiotensin II binds to two receptors: AT1 and type-2 angiotensin II receptor (AT2). AT1 is a G-protein coupled receptor (GPCR) that mediates the vasoconstrictive and aldosterone-secreting effects of angiotensin II. Studies performed in recent years suggest that AT2 antagonizes AT1-mediated effects and directly affects long-term blood pressure control by inducing vasorelaxation and increasing urinary sodium excretion. Angiotensin receptor blockers (ARBs) are non-peptide competitive inhibitors of AT1. ARBs block the ability of angiotensin II to stimulate pressor and cell proliferative effects. Unlike ACE inhibitors, ARBs do not affect bradykinin-induced vasodilation. The overall effect of ARBs is a decrease in blood pressure.
Mechanism of actionValsartan is an ARB that selectively inhibits the binding of angiotensin II to AT1, which is found in many tissues such as vascular smooth muscle and the adrenal glands. This effectively inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in a decrease in vascular resistance and blood pressure. Valsartan is selective for AT1 and has virtually no affinity for AT2. Inhibition of aldosterone secretion may inhibit sodium and water reabsorption in the kidneys while decreasing potassium excretion. The primary metabolite of valsartan, valeryl 4-hydroxy valsartan, has no pharmacological activity.
Related Articles
AbsorptionAbsolute bioavailability = 23% with high variability
Volume of distribution
  • 17 L (low tissue distribution)
Protein binding94 - 97% bound to serum proteins, primarily serum albumin
Metabolism

Valsartan is excreted largely as unchanged drug (80%) and is minimally metabolized in humans. The primary circulating metabolite, 4-OH-valsartan, is pharmacologically inactive and produced CYP2C9. 4-OH-valsartan accounts for approximately 9% of the circulating dose of valsartan. Although valsartan is metabolized by CYP2C9, CYP-mediated drug-drug interactions between valsartan and other drugs is unlikely.

SubstrateEnzymesProduct
Valsartan
4-HydroxyvalsartanDetails
Route of elimination83% of absorbed valsartan is excreted in feces and 13% is excreted in urine, primarily as unchanged drug
Half lifeThe initial phase t1/2 α is < 1 hour while the terminal phase t1/2 β is 5-9 hours.
Clearance
  • 2 L/h [IV administration]
  • 4.5 L/h [heart Failure patients receiving oral administration 40 to 160 mg twice a day]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Valsartan Action PathwayDrug actionSMP00165
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9956
Blood Brain Barrier-0.8032
Caco-2 permeable-0.6912
P-glycoprotein substrateSubstrate0.685
P-glycoprotein inhibitor INon-inhibitor0.5548
P-glycoprotein inhibitor IINon-inhibitor0.5966
Renal organic cation transporterNon-inhibitor0.8646
CYP450 2C9 substrateNon-substrate0.7722
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5073
CYP450 1A2 substrateNon-inhibitor0.8707
CYP450 2C9 inhibitorNon-inhibitor0.5398
CYP450 2D6 inhibitorNon-inhibitor0.8816
CYP450 2C19 inhibitorInhibitor0.5539
CYP450 3A4 inhibitorNon-inhibitor0.5521
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5618
Ames testNon AMES toxic0.6384
CarcinogenicityNon-carcinogens0.645
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6518 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9766
hERG inhibition (predictor II)Non-inhibitor0.7388
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
  • Novartis Corporation
Packagers
Dosage forms
FormRouteStrength
Tabletoral
Tabletoral160 mg/1
Tabletoral320 mg/1
Tabletoral320 mg
Tabletoral40 mg
Tabletoral40 mg/1
Tabletoral80 mg/1
Capsuleoral160 mg
Tabletoral160 mg
Capsuleoral80 mg
Tabletoral80 mg
Tablet, film coatedoral
Tablet, film coatedoral160 mg/1
Tablet, film coatedoral320 mg/1
Tablet, film coatedoral40 mg/1
Tablet, film coatedoral80 mg/1
Prices
Unit descriptionCostUnit
Diovan hct 320-25 mg tablet4.63USD tablet
Diovan hct 320-12.5 mg tablet4.1USD tablet
Diovan hct 160-25 mg tablet3.66USD tablet
Diovan hct 160-12.5 mg tablet3.27USD tablet
Diovan 320 mg tablet3.17USD tablet
Diovan hct 80-12.5 mg tablet3.0USD tablet
Diovan 160 mg tablet2.42USD tablet
Diovan 80 mg tablet2.33USD tablet
Diovan 40 mg tablet2.32USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2036427 No1998-12-292011-02-15Canada
CA2259148 No2009-09-292017-06-18Canada
US5399578 No1995-03-212012-03-21Us
US5559111 No1998-07-212018-07-21Us
US5972990 Yes1997-04-262017-04-26Us
US6294197 Yes1997-12-182017-12-18Us
US6395728 No1999-07-082019-07-08Us
US7468390 No2003-11-272023-11-27Us
US8101599 No2003-05-162023-05-16Us
US8101659 No2003-01-142023-01-14Us
US8168616 No2006-07-032026-07-03Us
US8404744 No2003-01-142023-01-14Us
US8475839 Yes2003-11-162023-11-16Us
US8796331 No2003-01-142023-01-14Us
US8877938 No2007-05-272027-05-27Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point116-117 °CNot Available
logP5.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0234 mg/mLALOGPS
logP3.68ALOGPS
logP5.27ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)4.37ChemAxon
pKa (Strongest Basic)-0.11ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area112.07 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity134.77 m3·mol-1ChemAxon
Polarizability47.27 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Zvi Harel, Igor Rukhman, “Process for the preparation of valsartan.” U.S. Patent US20050010053, issued January 13, 2005.

US20050010053
General References
  1. Bader, M. (2004). Renin-angiotensin-aldosterone system. In Encyclopedic reference of molecular pharmacology (pp. 810-814). Berlin: Springer. [ISBN:9783540298328 ]
External Links
ATC CodesC09CA03C09DA03C09DB01C09DB08C09DX01C09DX02C09DX04C10BX10
AHFS Codes
  • 24:32.08
PDB EntriesNot Available
FDA labelDownload (237 KB)
MSDSDownload (36.2 KB)
Interactions
Drug Interactions
Drug
AcebutololThe risk or severity of adverse effects can be increased when Valsartan is combined with Acebutolol.
AcetaminophenAcetaminophen may increase the hypotensive activities of Valsartan.
AcetazolamideThe risk or severity of adverse effects can be increased when Valsartan is combined with Acetazolamide.
AldesleukinThe risk or severity of adverse effects can be increased when Valsartan is combined with Aldesleukin.
AlfuzosinAlfuzosin may increase the hypotensive activities of Valsartan.
AliskirenAliskiren may increase the hyperkalemic activities of Valsartan.
AmifostineValsartan may increase the hypotensive activities of Amifostine.
AmilorideValsartan may increase the hyperkalemic activities of Amiloride.
AmlodipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Amlodipine.
AmobarbitalAmobarbital may increase the hypotensive activities of Valsartan.
Amyl NitriteThe risk or severity of adverse effects can be increased when Valsartan is combined with Amyl Nitrite.
ApraclonidineThe risk or severity of adverse effects can be increased when Valsartan is combined with Apraclonidine.
ArdeparinArdeparin may increase the hyperkalemic activities of Valsartan.
AtenololThe risk or severity of adverse effects can be increased when Valsartan is combined with Atenolol.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Valsartan is combined with Azilsartan medoxomil.
BenazeprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Benazepril.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Valsartan is combined with Bendroflumethiazide.
BetaxololThe risk or severity of adverse effects can be increased when Valsartan is combined with Betaxolol.
BisoprololThe risk or severity of adverse effects can be increased when Valsartan is combined with Bisoprolol.
BretyliumThe risk or severity of adverse effects can be increased when Valsartan is combined with Bretylium.
BrimonidineBrimonidine may increase the antihypertensive activities of Valsartan.
BumetanideThe risk or severity of adverse effects can be increased when Valsartan is combined with Bumetanide.
ButabarbitalButabarbital may increase the hypotensive activities of Valsartan.
ButalbitalButalbital may increase the hypotensive activities of Valsartan.
ButethalButethal may increase the hypotensive activities of Valsartan.
CaffeineCaffeine may increase the hypotensive activities of Valsartan.
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Valsartan.
CandesartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Candesartan.
CaptoprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Captopril.
CarbidopaValsartan may increase the orthostatic hypotensive activities of Carbidopa.
CarteololThe risk or severity of adverse effects can be increased when Valsartan is combined with Carteolol.
CarvedilolThe risk or severity of adverse effects can be increased when Valsartan is combined with Carvedilol.
CelecoxibThe risk or severity of adverse effects can be increased when Valsartan is combined with Celecoxib.
ChlorothiazideThe risk or severity of adverse effects can be increased when Valsartan is combined with Chlorothiazide.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Valsartan is combined with Chlorthalidone.
CilazaprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Cilazapril.
CiprofloxacinValsartan may increase the arrhythmogenic activities of Ciprofloxacin.
ClevidipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Clevidipine.
ClonidineThe risk or severity of adverse effects can be increased when Valsartan is combined with Clonidine.
CyclosporineValsartan may increase the hyperkalemic activities of Cyclosporine.
DalteparinDalteparin may increase the hyperkalemic activities of Valsartan.
DapagliflozinThe risk or severity of adverse effects can be increased when Valsartan is combined with Dapagliflozin.
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Valsartan.
DexmedetomidineThe risk or severity of adverse effects can be increased when Valsartan is combined with Dexmedetomidine.
DiazoxideDiazoxide may increase the hypotensive activities of Valsartan.
DiclofenacThe risk or severity of adverse effects can be increased when Valsartan is combined with Diclofenac.
DiclofenamideThe risk or severity of adverse effects can be increased when Valsartan is combined with Diclofenamide.
DiflunisalThe risk or severity of adverse effects can be increased when Valsartan is combined with Diflunisal.
DiltiazemThe risk or severity of adverse effects can be increased when Valsartan is combined with Diltiazem.
DinutuximabThe risk or severity of adverse effects can be increased when Valsartan is combined with Dinutuximab.
DipyridamoleThe risk or severity of adverse effects can be increased when Valsartan is combined with Dipyridamole.
DoxazosinThe risk or severity of adverse effects can be increased when Valsartan is combined with Doxazosin.
DrospirenoneValsartan may increase the hyperkalemic activities of Drospirenone.
DuloxetineValsartan may increase the orthostatic hypotensive activities of Duloxetine.
EltrombopagThe serum concentration of Valsartan can be increased when it is combined with Eltrombopag.
EmpagliflozinThe risk or severity of adverse effects can be increased when Valsartan is combined with Empagliflozin.
EnalaprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Enalapril.
EnalaprilatThe risk or severity of adverse effects can be increased when Valsartan is combined with Enalaprilat.
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Valsartan.
EntacaponeValsartan may increase the orthostatic hypotensive activities of Entacapone.
EplerenoneEplerenone may increase the hyperkalemic activities of Valsartan.
EprosartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Eprosartan.
EsmololThe risk or severity of adverse effects can be increased when Valsartan is combined with Esmolol.
EstradiolValsartan may increase the hyperkalemic activities of Estradiol.
Etacrynic acidThe risk or severity of adverse effects can be increased when Valsartan is combined with Ethacrynic acid.
EtodolacThe risk or severity of adverse effects can be increased when Valsartan is combined with Etodolac.
FelodipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Felodipine.
FenoprofenThe risk or severity of adverse effects can be increased when Valsartan is combined with Fenoprofen.
FloctafenineThe risk or severity of adverse effects can be increased when Valsartan is combined with Floctafenine.
FlurbiprofenThe risk or severity of adverse effects can be increased when Valsartan is combined with Flurbiprofen.
FosinoprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Fosinopril.
FurosemideThe risk or severity of adverse effects can be increased when Valsartan is combined with Furosemide.
GuanfacineThe risk or severity of adverse effects can be increased when Valsartan is combined with Guanfacine.
HeparinHeparin may increase the hyperkalemic activities of Valsartan.
HeptabarbitalHeptabarbital may increase the hypotensive activities of Valsartan.
HexobarbitalHexobarbital may increase the hypotensive activities of Valsartan.
HydralazineThe risk or severity of adverse effects can be increased when Valsartan is combined with Hydralazine.
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Valsartan.
IbuprofenThe risk or severity of adverse effects can be increased when Valsartan is combined with Ibuprofen.
IndapamideThe risk or severity of adverse effects can be increased when Valsartan is combined with Indapamide.
IndomethacinThe risk or severity of adverse effects can be increased when Valsartan is combined with Indomethacin.
InfliximabThe risk or severity of adverse effects can be increased when Valsartan is combined with Infliximab.
IrbesartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Irbesartan.
IsosorbideThe risk or severity of adverse effects can be increased when Valsartan is combined with Isosorbide.
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Valsartan is combined with Isosorbide Dinitrate.
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Valsartan is combined with Isosorbide Mononitrate.
IsoxsuprineThe risk or severity of adverse effects can be increased when Valsartan is combined with Isoxsuprine.
IsradipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Isradipine.
KetoprofenThe risk or severity of adverse effects can be increased when Valsartan is combined with Ketoprofen.
KetorolacThe risk or severity of adverse effects can be increased when Valsartan is combined with Ketorolac.
LabetalolThe risk or severity of adverse effects can be increased when Valsartan is combined with Labetalol.
LevobunololThe risk or severity of adverse effects can be increased when Valsartan is combined with Levobunolol.
LevodopaValsartan may increase the orthostatic hypotensive activities of Levodopa.
LisinoprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Lisinopril.
LithiumThe serum concentration of Lithium can be increased when it is combined with Valsartan.
LosartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Losartan.
MannitolThe risk or severity of adverse effects can be increased when Valsartan is combined with Mannitol.
MecamylamineThe risk or severity of adverse effects can be increased when Valsartan is combined with Mecamylamine.
Mefenamic acidThe risk or severity of adverse effects can be increased when Valsartan is combined with Mefenamic acid.
MeloxicamThe risk or severity of adverse effects can be increased when Valsartan is combined with Meloxicam.
MetforminMetformin may increase the hyperkalemic activities of Valsartan.
MethazolamideThe risk or severity of adverse effects can be increased when Valsartan is combined with Methazolamide.
MethohexitalMethohexital may increase the hypotensive activities of Valsartan.
MethyclothiazideThe risk or severity of adverse effects can be increased when Valsartan is combined with Methyclothiazide.
MethyldopaThe risk or severity of adverse effects can be increased when Valsartan is combined with Methyldopa.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Valsartan.
MetipranololThe risk or severity of adverse effects can be increased when Valsartan is combined with Metipranolol.
MetolazoneThe risk or severity of adverse effects can be increased when Valsartan is combined with Metolazone.
MetoprololThe risk or severity of adverse effects can be increased when Valsartan is combined with Metoprolol.
MinoxidilThe risk or severity of adverse effects can be increased when Valsartan is combined with Minoxidil.
MoexiprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Moexipril.
MolsidomineMolsidomine may increase the hypotensive activities of Valsartan.
MoxonidineMoxonidine may increase the hypotensive activities of Valsartan.
NabumetoneThe risk or severity of adverse effects can be increased when Valsartan is combined with Nabumetone.
NadololThe risk or severity of adverse effects can be increased when Valsartan is combined with Nadolol.
NadroparinNadroparin may increase the hyperkalemic activities of Valsartan.
NaproxenThe risk or severity of adverse effects can be increased when Valsartan is combined with Naproxen.
NebivololThe risk or severity of adverse effects can be increased when Valsartan is combined with Nebivolol.
NesiritideThe risk or severity of adverse effects can be increased when Valsartan is combined with Nesiritide.
NicardipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Nicardipine.
NicorandilNicorandil may increase the hypotensive activities of Valsartan.
NifedipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Nifedipine.
NimodipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Nimodipine.
NisoldipineThe risk or severity of adverse effects can be increased when Valsartan is combined with Nisoldipine.
NitroglycerinThe risk or severity of adverse effects can be increased when Valsartan is combined with Nitroglycerin.
NitroprussideThe risk or severity of adverse effects can be increased when Valsartan is combined with Nitroprusside.
ObinutuzumabValsartan may increase the hypotensive activities of Obinutuzumab.
OlmesartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Olmesartan.
OxaprozinThe risk or severity of adverse effects can be increased when Valsartan is combined with Oxaprozin.
PapaverineThe risk or severity of adverse effects can be increased when Valsartan is combined with Papaverine.
PenbutololThe risk or severity of adverse effects can be increased when Valsartan is combined with Penbutolol.
PentobarbitalPentobarbital may increase the hypotensive activities of Valsartan.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Valsartan.
PerindoprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Perindopril.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Valsartan.
PhenobarbitalPhenobarbital may increase the hypotensive activities of Valsartan.
PindololThe risk or severity of adverse effects can be increased when Valsartan is combined with Pindolol.
PiroxicamThe risk or severity of adverse effects can be increased when Valsartan is combined with Piroxicam.
Potassium ChloridePotassium Chloride may increase the hyperkalemic activities of Valsartan.
Potassium CitratePotassium Citrate may increase the hyperkalemic activities of Valsartan.
Potassium IodidePotassium Iodide may increase the hyperkalemic activities of Valsartan.
PrazosinThe risk or severity of adverse effects can be increased when Valsartan is combined with Prazosin.
PrimidonePrimidone may increase the hypotensive activities of Valsartan.
PropranololThe risk or severity of adverse effects can be increased when Valsartan is combined with Propranolol.
QuetiapineThe risk or severity of adverse effects can be increased when Valsartan is combined with Quetiapine.
QuinaprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Quinapril.
QuinineQuinine may increase the hypotensive activities of Valsartan.
RamiprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Ramipril.
ReserpineThe risk or severity of adverse effects can be increased when Valsartan is combined with Reserpine.
RiociguatThe risk or severity of adverse effects can be increased when Valsartan is combined with Riociguat.
RisperidoneValsartan may increase the hypotensive activities of Risperidone.
RituximabValsartan may increase the hypotensive activities of Rituximab.
SecobarbitalSecobarbital may increase the hypotensive activities of Valsartan.
SotalolThe risk or severity of adverse effects can be increased when Valsartan is combined with Sotalol.
SpironolactoneValsartan may increase the hyperkalemic activities of Spironolactone.
SulfamethoxazoleSulfamethoxazole may increase the hyperkalemic activities of Valsartan.
SulindacThe risk or severity of adverse effects can be increased when Valsartan is combined with Sulindac.
TadalafilTadalafil may increase the antihypertensive activities of Valsartan.
TelmisartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Telmisartan.
TerazosinThe risk or severity of adverse effects can be increased when Valsartan is combined with Terazosin.
TeriflunomideThe serum concentration of Valsartan can be increased when it is combined with Teriflunomide.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Valsartan is combined with Tiaprofenic acid.
TimololThe risk or severity of adverse effects can be increased when Valsartan is combined with Timolol.
TinzaparinTinzaparin may increase the hyperkalemic activities of Valsartan.
TizanidineThe risk or severity of adverse effects can be increased when Valsartan is combined with Tizanidine.
TolmetinThe risk or severity of adverse effects can be increased when Valsartan is combined with Tolmetin.
TolvaptanTolvaptan may increase the hyperkalemic activities of Valsartan.
TorasemideThe risk or severity of adverse effects can be increased when Valsartan is combined with Torasemide.
TrandolaprilThe risk or severity of adverse effects can be increased when Valsartan is combined with Trandolapril.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Valsartan.
TreprostinilTreprostinil may increase the hypotensive activities of Valsartan.
TriamtereneValsartan may increase the hyperkalemic activities of Triamterene.
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Valsartan.
VardenafilVardenafil may increase the antihypertensive activities of Valsartan.
VerapamilThe risk or severity of adverse effects can be increased when Valsartan is combined with Verapamil.
YohimbineYohimbine may decrease the antihypertensive activities of Valsartan.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name:
AGTR1
Uniprot ID:
P30556
Molecular Weight:
41060.53 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Azizi M, Menard J, Bissery A, Guyenne TT, Bura-Riviere A, Vaidyanathan S, Camisasca RP: Pharmacologic demonstration of the synergistic effects of a combination of the renin inhibitor aliskiren and the AT1 receptor antagonist valsartan on the angiotensin II-renin feedback interruption. J Am Soc Nephrol. 2004 Dec;15(12):3126-33. [PubMed:15579516 ]
  3. Criscione L, de Gasparo M, Buhlmayer P, Whitebread S, Ramjoue HP, Wood J: Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype. Br J Pharmacol. 1993 Oct;110(2):761-71. [PubMed:8242249 ]
  4. Shargorodsky M, Leibovitz E, Lubimov L, Gavish D, Zimlichman R: Prolonged treatment with the AT1 receptor blocker, valsartan, increases small and large artery compliance in uncomplicated essential hypertension. Am J Hypertens. 2002 Dec;15(12):1087-91. [PubMed:12460705 ]
  5. de Gasparo M, Whitebread S: Binding of valsartan to mammalian angiotensin AT1 receptors. Regul Pept. 1995 Nov 10;59(3):303-11. [PubMed:8577935 ]
  6. Siragy HM, El-Kersh MA, De Gasparo M, Webb RL, Carey RM: Differences in AT2 -receptor stimulation between AT1 -receptor blockers valsartan and losartan quantified by renal interstitial fluid cGMP. J Hypertens. 2002 Jun;20(6):1157-63. [PubMed:12023686 ]
  7. Stanfield, Cindy L.;Germann, William J. (2009). Principles of Human Physiology (3rd ed.). Benjamin-Cummings Publishing Company. [ISBN:978-0321556660 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Nakashima A, Kawashita H, Masuda N, Saxer C, Niina M, Nagae Y, Iwasaki K: Identification of cytochrome P450 forms involved in the 4-hydroxylation of valsartan, a potent and specific angiotensin II receptor antagonist, in human liver microsomes. Xenobiotica. 2005 Jun;35(6):589-602. [PubMed:16192110 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Diovan. (2009). [Electronic version]. e-CPS. Retrieved September 15, 2011.

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn. 2009 Dec;36(6):585-611. doi: 10.1007/s10928-009-9139-3. Epub 2009 Nov 20. [PubMed:19936896 ]
  2. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in humans based on in vitro uptake-transport data. Chem Biodivers. 2009 Nov;6(11):1975-87. doi: 10.1002/cbdv.200900116. [PubMed:19937834 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn. 2009 Dec;36(6):585-611. doi: 10.1007/s10928-009-9139-3. Epub 2009 Nov 20. [PubMed:19936896 ]
  2. Poirier A, Cascais AC, Funk C, Lave T: Prediction of pharmacokinetic profile of valsartan in humans based on in vitro uptake-transport data. Chem Biodivers. 2009 Nov;6(11):1975-87. doi: 10.1002/cbdv.200900116. [PubMed:19937834 ]
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Drug created on June 13, 2005 07:24 / Updated on April 29, 2016 03:10