ValtensinHCT ValsartanHCT是什么中国药品电子监管网

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DrugBank. IdentificationNameValsartanAccession NumberDB00177& (APRD00133) TypeSmall MoleculeGroupsApproved, InvestigationalDescriptionValsartan 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.StructureSynonymsSynonymLanguage(S)-N-Valeryl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]-methyl}-valineNot AvailableDiovanNot AvailableN-(P-(O-1H-Tetrazol-5-ylphenyl)benzyl)-N-valeryl-L-valineNot AvailableN-Pentanoyl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-L-valineNot AvailableExternal Identifiers Not AvailablePrescription ProductsNameDosageStrengthRouteLabellerMarketing StartMarketing EndAct Valsartantablet40 mgoralActavis Pharma CompanyNot applicableCanadaAct Valsartantablet80 mgoralActavis Pharma CompanyNot applicableCanadaAct Valsartantablet160 mgoralActavis Pharma CompanyNot applicableCanadaAct Valsartantablet320 mgoralActavis Pharma CompanyNot applicableCanadaAuro-valsartantablet40 mgoralAuro Pharma IncNot applicableCanadaAuro-valsartantablet80 mgoralAuro Pharma IncNot applicableCanadaAuro-valsartantablet160 mgoralAuro Pharma IncNot applicableCanadaAuro-valsartantablet320 mgoralAuro Pharma IncNot applicableCanadaAva-valsartantablet80 mgoralAvanstra IncCanadaAva-valsartantablet160 mgoralAvanstra IncCanadaAva-valsartantablet40 mgoralAvanstra IncCanadaAva-valsartantablet320 mgoralAvanstra IncCanadaDiovantablet80 mgoralPd Rx Pharmaceuticals, Inc.Not applicableUSDiovantablet320 mgoralRebel Distributors CorpNot applicableUSDiovantablet40 mgoralPhysicians Total Care, Inc.Not applicableUSDiovantablet40 mgoralNovartis Pharmaceuticals CorporationNot applicableUSDiovantablet160 mgoralREMEDYREPACK INC.Not applicableUSDiovantablet160 mgoralbryant ranch prepackNot applicableUSDiovantablet320 mgoralPd Rx Pharmaceuticals, Inc.Not applicableUSDiovantablet320 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLCNot applicableUSDiovantablet80 mgoralCardinal HealthNot applicableUSDiovantablet40 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLCNot applicableUSDiovantablet80 mgoralAphena Pharma Solutions
Tennessee, LlcNot applicableUSDiovantablet80 mgoralbryant ranch prepackNot applicableUSDiovantablet80 mgoralREMEDYREPACK INC.Not applicableUSDiovantablet160 mgoralAphena Pharma Solutions
Tennessee, LlcNot applicableUSDiovantablet160 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLCNot applicableUSDiovantablet80 mgoralCarilion Materials ManagementNot applicableUSDiovantablet80 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLCNot applicableUSDiovantablet160 mgoralCardinal HealthNot applicableUSDiovantablet160 mgoralPhysicians Total Care, Inc.Not applicableUSDiovantablet40 mgoralNovartis Pharmaceuticals Canada IncNot applicableCanadaDiovantablet80 mgoralNovartis Pharmaceuticals CorporationNot applicableUSDiovantablet40 mgoralCarilion Materials ManagementNot applicableUSDiovantablet80 mgoralRebel Distributors CorpNot applicableUSDiovantablet320 mgoralCardinal HealthNot applicableUSDiovantablet80 mgoralPhysicians Total Care, Inc.Not applicableUSDiovantablet320 mgoralNovartis Pharmaceuticals Canada IncNot applicableCanadaDiovantablet160 mgoralNovartis Pharmaceuticals CorporationNot applicableUSDiovantablet160 mgoralPd Rx Pharmaceuticals, Inc.Not applicableUSDiovantablet160 mgoralRebel Distributors CorpNot applicableUSDiovantablet320 mgoralPhysicians Total Care, Inc.Not applicableUSDiovantablet320 mgoralNovartis Pharmaceuticals CorporationNot applicableUSDiovan 160mgcapsule160 mgoralNovartis Pharmaceuticals Canada IncNot applicableCanadaDiovan 160mg Tabletstablet160 mgoralNovartis Pharmaceuticals Canada IncNot applicableCanadaDiovan 80mgcapsule80 mgoralNovartis Pharmaceuticals Canada IncNot applicableCanadaDiovan 80mg Tabletstablet80 mgoralNovartis Pharmaceuticals Canada IncNot applicableCanadaDom-valsartantablet160 mgoralDominion PharmacalNot applicableNot applicableCanadaDom-valsartantablet80 mgoralDominion PharmacalNot applicableCanadaDom-valsartantablet320 mgoralDominion PharmacalNot applicableNot applicableCanadaDom-valsartantablet40 mgoralDominion PharmacalNot applicableNot applicableCanadaMylan-valsartantablet80 mgoralMylan Pharmaceuticals UlcNot applicableCanadaMylan-valsartantablet160 mgoralMylan Pharmaceuticals UlcNot applicableCanadaMylan-valsartantablet40 mgoralMylan Pharmaceuticals UlcNot applicableCanadaMylan-valsartantablet320 mgoralMylan Pharmaceuticals UlcNot applicableCanadaNovo-valsartantablet80 mgoralTeva Canada LimitedNot applicableNot applicableCanadaNovo-valsartantablet160 mgoralTeva Canada LimitedNot applicableNot applicableCanadaNovo-valsartantablet320 mgoralTeva Canada LimitedNot applicableNot applicableCanadaNovo-valsartantablet40 mgoralTeva Canada LimitedNot applicableNot applicableCanadaPMS-valsartantablet80 mgoralPharmascience IncNot applicableCanadaPMS-valsartantablet160 mgoralPharmascience IncNot applicableCanadaPMS-valsartantablet320 mgoralPharmascience IncNot applicableCanadaPMS-valsartantablet40 mgoralPharmascience IncNot applicableCanadaQ-valsartantablet40 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanadaQ-valsartantablet80 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanadaQ-valsartantablet160 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanadaQ-valsartantablet320 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanadaRan-valsartantablet160 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableCanadaRan-valsartantablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableCanadaRan-valsartantablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableCanadaRiva-valsartantablet160 mgoralLaboratoire Riva IncNot applicableCanadaRiva-valsartantablet320 mgoralLaboratoire Riva IncNot applicableCanadaRiva-valsartantablet40 mgoralLaboratoire Riva IncNot applicableCanadaRiva-valsartantablet80 mgoralLaboratoire Riva IncNot applicableCanadaSandoz Valsartantablet40 mgoralSandoz Canada IncorporatedNot applicableCanadaSandoz Valsartantablet80 mgoralSandoz Canada IncorporatedNot applicableCanadaSandoz Valsartantablet160 mgoralSandoz Canada IncorporatedNot applicableCanadaSandoz Valsartantablet320 mgoralSandoz Canada IncorporatedNot applicableCanadaTeva-valsartantablet40 mgoralTeva Canada LimitedNot applicableCanadaTeva-valsartantablet320 mgoralTeva Canada LimitedNot applicableCanadaTeva-valsartantablet80 mgoralTeva Canada LimitedNot applicableCanadaTeva-valsartantablet160 mgoralTeva Canada LimitedNot applicableCanadaValsartantablet160 mgoralPro Doc LimiteeNot applicableCanadaValsartantablet320 mgoralPro Doc LimiteeNot applicableCanadaValsartantablet40 mgoralSandoz IncNot applicableUSValsartantablet40 mgoralSanis Health IncNot applicableCanadaValsartantablet40 mgoralActavis Pharma CompanyNot applicableNot applicableCanadaValsartantablet160 mgoralCardinal HealthNot applicableUSValsartantablet80 mgoralSandoz IncNot applicableUSValsartantablet80 mgoralSanis Health IncNot applicableCanadaValsartantablet160 mgoralSanis Health IncNot applicableCanadaValsartantablet160 mgoralActavis Pharma CompanyNot applicableNot applicableCanadaValsartantablet80 mgoralCardinal HealthNot applicableUSValsartantablet160 mgoralSandoz IncNot applicableUSValsartantablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanadaValsartantablet40 mgoralSivem Pharmaceuticals UlcNot applicableCanadaValsartantablet320 mgoralSandoz IncNot applicableUSValsartantablet320 mgoralSanis Health IncNot applicableCanadaValsartantablet80 mgoralActavis Pharma CompanyNot applicableNot applicableCanadaValsartantablet80 mgoralSivem Pharmaceuticals UlcNot applicableCanadaValsartantablet80 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanadaValsartantablet40 mgoralPro Doc LimiteeNot applicableCanadaValsartantablet320 mgoralActavis Pharma CompanyNot applicableNot applicableCanadaValsartantablet160 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanadaValsartantablet160 mgoralSivem Pharmaceuticals UlcNot applicableCanadaValsartantablet80 mgoralPro Doc LimiteeNot applicableCanadaValsartantablet320 mgoralSivem Pharmaceuticals UlcNot applicableCanadaGeneric Prescription ProductsNameDosageStrengthRouteLabellerMarketing StartMarketing EndApo-valsartantablet40 mgoralApotex IncNot applicableCanadaApo-valsartantablet80 mgoralApotex IncNot applicableCanadaApo-valsartantablet160 mgoralApotex IncNot applicableCanadaApo-valsartantablet320 mgoralApotex IncNot applicableCanadaValsartantablet160 mgoralLupin Pharmaceuticals, Inc.Not applicableUSValsartantablet, film coated160 mgoralActavis Pharma, Inc.Not applicableUSValsartantablet, film coated160 mgoralOhm Laboratories Inc.Not applicableUSValsartantablet, film coated320 mgoralAv Kare, Inc.Not applicableUSValsartantablet, film coated160 mgoralAmerican Health PackagingNot applicableUSValsartantablet, film coated320 mgoralTeva Pharmaceuticals USA IncUSValsartantablet80 mgoralAlembic Pharmaceuticals LimitedNot applicableUSValsartantablet, film coated40 mgoralCamber Pharmaceuticals, Inc.Not applicableUSValsartantablet, film coated320 mgoralPhysicians Total Care, Inc.Not applicableUSValsartantablet, film coated160 mgoralAv Kare, Inc.Not applicableUSValsartantablet80 mgoralQualitest PharmaceuticalsNot applicableUSValsartantablet320 mgoralLupin Pharmaceuticals, Inc.Not applicableUSValsartantablet, film coated320 mgoralActavis Pharma, Inc.Not applicableUSValsartantablet, film coated320 mgoralOhm Laboratories Inc.Not applicableUSValsartantablet, film coated40 mgoralAv Kare, Inc.Not applicableUSValsartantablet, film coated40 mgoralAurobindo Pharma LimitedNot applicableUSValsartantablet, film coated40 mgoralMylan Pharmaceuticals Inc.Not applicableUSValsartantablet160 mgoralAlembic Pharmaceuticals LimitedNot applicableUSValsartantablet, film coated80 mgoralCamber Pharmaceuticals, Inc.Not applicableUSValsartantablet160 mgoralQualitest PharmaceuticalsNot applicableUSValsartantablet, film coated80 mgoralPhysicians Total Care, Inc.Not applicableUSValsartantablet, film coated320 mgoralAv Kare, Inc.Not applicableUSValsartantablet40 mgoralQualitest PharmaceuticalsNot applicableUSValsartantablet, film coated160 mgoralPhysicians Total Care, Inc.Not applicableUSValsartantablet, film coated80 mgoralAv Kare, Inc.Not applicableUSValsartantablet, film coated80 mgoralAurobindo Pharma LimitedNot applicableUSValsartantablet, film coated80 mgoralMylan Pharmaceuticals Inc.Not applicableUSValsartantablet320 mgoralAlembic Pharmaceuticals LimitedNot applicableUSValsartantablet, film coated160 mgoralCamber Pharmaceuticals, Inc.Not applicableUSValsartantablet320 mgoralQualitest PharmaceuticalsNot applicableUSValsartantablet40 mgoralJubilant Cadista Pharmaceuticals Inc.Not applicableUSValsartantablet40 mgoralSolco Healthcare US, LLCNot applicableUSValsartantablet, film coated320 mgoralCamber Pharmaceuticals, Inc.Not applicableUSValsartantablet, film coated160 mgoralAurobindo Pharma LimitedNot applicableUSValsartantablet, film coated160 mgoralMylan Pharmaceuticals Inc.Not applicableUSValsartantablet, film coated80 mgoralNorthwind Pharmaceuticals, LLCNot applicableUSValsartantablet40 mgoralTorrent Pharmaceuticals LimitedNot applicableUSValsartantablet80 mgoralJubilant Cadista Pharmaceuticals Inc.Not applicableUSValsartantablet80 mgoralSolco Healthcare US, LLCNot applicableUSValsartantablet, film coated40 mgoralAv Kare, Inc.Not applicableUSValsartantablet, film coated320 mgoralAurobindo Pharma LimitedNot applicableUSValsartantablet, film coated320 mgoralMylan Pharmaceuticals Inc.Not applicableUSValsartantablet, film coated160 mgoralNorthwind PharmaceuticalsNot applicableUSValsartantablet, film coated40 mgoralTeva Pharmaceuticals USA IncUSValsartantablet160 mgoralSolco Healthcare US, LLCNot applicableUSValsartantablet80 mgoralTorrent Pharmaceuticals LimitedNot applicableUSValsartantablet160 mgoralJubilant Cadista Pharmaceuticals Inc.Not applicableUSValsartantablet, film coated40 mgoralActavis Pharma, Inc.Not applicableUSValsartantablet, film coated40 mgoralOhm Laboratories Inc.Not applicableUSValsartantablet, film coated80 mgoralAv Kare, Inc.Not applicableUSValsartantablet40 mgoralLupin Pharmaceuticals, Inc.Not applicableUSValsartantablet320 mgoralJubilant Cadista Pharmaceuticals Inc.Not applicableUSValsartantablet, film coated80 mgoralTeva Pharmaceuticals USA IncUSValsartantablet320 mgoralSolco Healthcare US, LLCNot applicableUSValsartantablet160 mgoralTorrent Pharmaceuticals LimitedNot applicableUSValsartantablet, film coated80 mgoralActavis Pharma, Inc.Not applicableUSValsartantablet, film coated80 mgoralOhm Laboratories Inc.Not applicableUSValsartantablet, film coated160 mgoralAv Kare, Inc.Not applicableUSValsartantablet80 mgoralLupin Pharmaceuticals, Inc.Not applicableUSValsartantablet, film coated80 mgoralAmerican Health PackagingNot applicableUSValsartantablet, film coated160 mgoralTeva Pharmaceuticals USA IncUSValsartantablet40 mgoralAlembic Pharmaceuticals LimitedNot applicableUSValsartantablet320 mgoralTorrent Pharmaceuticals LimitedNot applicableUSOver the Counter ProductsNot AvailableInternational BrandsNot AvailableBrand mixturesNameLabellerIngredientsAmlodipine and ValsartanTeva Pharmaceuticals USA IncValsartanAmlodipine Besylate and ValsartanMylan Pharmaceuticals Inc.ValsartanAmlodipine, Valsartan and HydrochlorothiazideTorrent Pharmaceuticals LimitedValsartanAmlodipine, Valsartan, and HydrochlorothiazideTeva Pharmaceuticals USA IncValsartanAmlodipine, Valsartan, HydrochlorothiazideSandoz IncValsartanApo-valsartan/hctzApotex IncValsartanAuro-valsartan HctAuro Pharma IncValsartanAva-valsartan HctAvanstra IncValsartanDiovan HctNovartis Pharmaceuticals CorporationValsartanDiovan-hctNovartis Pharmaceuticals Canada IncValsartanEntrestoNovartis Pharmaceuticals Canada IncValsartanExforgeNovartis Pharmaceuticals CorporationValsartanExforge HctNovartis Pharmaceuticals CorporationValsartanMylan-valsartan HctzMylan Pharmaceuticals UlcValsartanNovo-valsartan/hctzTeva Canada LimitedValsartanPMS-valsartan-hctzPharmascience IncValsartanQ-valsartan HctzQd Pharmaceuticals UlcValsartanSandoz Valsartan HctSandoz Canada IncorporatedValsartanTeva-valsartan/hctzTeva Canada LimitedValsartanValsartan and HydrochlorothiazideMylan Pharmaceuticals Inc.ValsartanValsartan HctSanis Health IncValsartanValsartan HctzNorthwind PharmaceuticalsValsartanValsartan-hctzPro Doc LimiteeValsartanSaltsNot AvailableCategoriesCAS number-4WeightAverage: 435.5188 Monoisotopic: 435. Chemical FormulaC24H29N5O3InChI KeyInChIKey=ACWBQPMHZXGDFX-QFIPXVFZSA-NInChIInChI=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/s1IUPAC Name(2S)-3-methyl-2-[N-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)pentanamido]butanoic acidSMILESCCCCC(=O)N(CC1=CC=C(C=C1)C1=CC=CC=C1C1=NNN=N1)[C@@H](C(C)C)C(O)=OTaxonomyDescriptionThis 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.KingdomSuper ClassClassSub ClassDirect ParentAlternative Parents
SubstituentsBiphenyltetrazole
N-acyl-aliphatic-alpha amino acid
N-acyl-alpha amino acid or derivatives
N-acyl-alpha-amino acid
N-acyl-l-alpha-amino acid
Alpha-amino acid or derivatives
Phenylmethylamine
Benzylamine
N-acyl-amine
Monocyclic benzene moiety
Heteroaromatic compound
Tertiary carboxylic acid amide
Tertiary amine
Carboxamide group
Monocarboxylic acid or derivatives
Carboxylic acid
Carboxylic acid derivative
Hydrocarbon derivative
Organooxygen compound
Organonitrogen compound
Carbonyl group
Aromatic heteromonocyclic compoundMolecular FrameworkAromatic heteromonocyclic compoundsExternal Descriptorsbiphenylyltetrazole ()PharmacologyIndicationMay 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. AbsorptionAbsolute bioavailability = 23% with high variabilityVolume of distribution
17 L (low tissue distribution)
Protein binding94 - 97% bound to serum proteins, primarily serum albuminMetabolismValsartan 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. SubstrateEnzymesProductValsartan Route of elimination83% of absorbed valsartan is excreted in feces and 13% is excreted in urine, primarily as unchanged drugHalf lifeThe initial phase t1/2 & is < 1 hour while the terminal phase t1/2 & 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 AvailableAffected organismsHumans and other mammalsPathwaysPathwayCategorySMPDB IDValsartan Action PathwayDrug actionSNP Mediated EffectsNot AvailableSNP Mediated Adverse Drug ReactionsNot AvailableADMETPredicted ADMET featuresPropertyValueProbabilityHuman Intestinal Absorption+0.9956Blood Brain Barrier-0.8032Caco-2 permeable-0.6912P-glycoprotein substrateSubstrate0.685P-glycoprotein inhibitor INon-inhibitor0.5548P-glycoprotein inhibitor IINon-inhibitor0.5966Renal organic cation transporterNon-inhibitor0.8646CYP450 2C9 substrateNon-substrate0.7722CYP450 2D6 substrateNon-substrate0.9116CYP450 3A4 substrateNon-substrate0.5073CYP450 1A2 substrateNon-inhibitor0.8707CYP450 2C9 inhibitorNon-inhibitor0.5398CYP450 2D6 inhibitorNon-inhibitor0.8816CYP450 2C19 inhibitorInhibitor0.5539CYP450 3A4 inhibitorNon-inhibitor0.5521CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5618Ames testNon AMES toxic0.6384CarcinogenicityNon-carcinogens0.645BiodegradationNot ready biodegradable1.0Rat acute toxicity2.6518 LD50, mol/kg Not applicablehERG inhibition (predictor I)Weak inhibitor0.9766hERG inhibition (predictor II)Non-inhibitor0.7388 ADMET data is predicted using , a free tool for evaluating chemical ADMET properties. () PharmacoeconomicsManufacturersNovartis pharmaceuticals corp
Novartis CorporationPackagersAdvanced Pharmaceutical Services Inc.
Heartland Repack Services LLC
Lake Erie Medical and Surgical Supply
Prepackage Specialists
Promex Medical Inc.
Resource Optimization and Innovation LLC
Vangard Labs Inc.Dosage formsFormRouteStrengthTabletoralTabletoral320 mgTabletoral40 mgCapsuleoral160 mgTabletoral160 mgCapsuleoral80 mgTabletoral80 mgTablet, film coatedoralTabletoral12.5 mgTabletoral25 mgTabletoral102.8 mgTabletoral25.7 mgTabletoral51.4 mgTablet, film coatedoral160 mgTablet, film coatedoral320 mgTablet, film coatedoral40 mgTablet, film coatedoral80 mgPricesUnit descriptionCostUnitDiovan hct 320-25 mg tablet4.63USD tabletDiovan hct 320-12.5 mg tablet4.1USD tabletDiovan hct 160-25 mg tablet3.66USD tabletDiovan hct 160-12.5 mg tablet3.27USD tabletDiovan 320 mg tablet3.17USD tabletDiovan hct 80-12.5 mg tablet3.0USD tabletDiovan 160 mg tablet2.42USD tabletDiovan 80 mg tablet2.33USD tabletDiovan 40 mg tablet2.32USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. PatentsCountryPatent NumberApprovedExpires (estimated)Canada2036427Canada2259148United States5399578United States6294197PropertiesStateSolidExperimental PropertiesSourcemelting point116-117 °CNot AvailablelogP5.8Not AvailablePredicted PropertiesSourceWater Solubility0.0234 mg/mLlogP3.68logP5.27logS-4.3pKa (Strongest Acidic)4.37pKa (Strongest Basic)-0.11Physiological Charge-1Hydrogen Acceptor Count6Hydrogen Donor Count2Polar Surface Area112.07 ?2Rotatable Bond Count10Refractivity134.77 m3·mol-1Polarizability47.27 ?3Number of Rings3Bioavailability1Rule of FiveYesGhose FilterYesVeber's RuleYesMDDR-like RuleYesSpectraMass Spec (NIST)Not AvailableSpectraNot AvailableReferencesSynthesis ReferenceZvi Harel, Igor Rukhman, &#8220;Process for the preparation of valsartan.&#8221; U.S. Patent US, issued January 13, 2005.General References
Bader, M. (2004). Renin-angiotensin-aldosterone system. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 810-814). Berlin, Germany: Springer.
Diovan. (2009). [Electronic version]. e-CPS. Retrieved December 28, 2009.
Stanfield, C.L., & Germann, W.J. (2008). Principles of human physiology (3 rd ed.). San Francisco, CA: Pearson Education, Inc.
External LinksResourceLinkKEGG DrugPubChem CompoundPubChem SubstanceChemSpiderBindingDBChEBIChEMBLTherapeutic Targets DatabasePharmGKBIUPHARGuide to PharmacologyDrug Product DatabaseRxList<WikipediaATC CodesC09CA03AHFS Codes24:32.08PDB EntriesNot AvailableFDA label (237 KB) MSDS (36.2 KB) InteractionsDrug InteractionsThe risk or severity of adverse effects can be increased when Valsartan is combined with Acebutolol.Acetaminophen may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Acetazolamide.The risk or severity of adverse effects can be increased when Valsartan is combined with Aldesleukin.Alfuzosin may increase the hypotensive activities of Valsartan.Aliskiren may increase the hyperkalemic activities of Valsartan.Valsartan may increase the hypotensive activities of Amifostine.Valsartan may increase the hyperkalemic activities of Amiloride.The risk or severity of adverse effects can be increased when Valsartan is combined with Amlodipine.Amobarbital may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Amyl Nitrite.The risk or severity of adverse effects can be increased when Valsartan is combined with Apraclonidine.Ardeparin may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Atenolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Azilsartan medoxomil.The risk or severity of adverse effects can be increased when Valsartan is combined with Benazepril.The risk or severity of adverse effects can be increased when Valsartan is combined with Bendroflumethiazide.The risk or severity of adverse effects can be increased when Valsartan is combined with Betaxolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Bisoprolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Bretylium.Brimonidine may increase the antihypertensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Bumetanide.Butabarbital may increase the hypotensive activities of Valsartan.Butalbital may increase the hypotensive activities of Valsartan.Butethal may increase the hypotensive activities of Valsartan.Caffeine may increase the hypotensive activities of Valsartan.Canagliflozin may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Candesartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Captopril.Valsartan may increase the orthostatic hypotensive activities of Carbidopa.The risk or severity of adverse effects can be increased when Valsartan is combined with Carteolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Carvedilol.The risk or severity of adverse effects can be increased when Valsartan is combined with Celecoxib.The risk or severity of adverse effects can be increased when Valsartan is combined with Chlorothiazide.The risk or severity of adverse effects can be increased when Valsartan is combined with Chlorthalidone.The risk or severity of adverse effects can be increased when Valsartan is combined with Cilazapril.Valsartan may increase the arrhythmogenic activities of Ciprofloxacin.The risk or severity of adverse effects can be increased when Valsartan is combined with Clevidipine.The risk or severity of adverse effects can be increased when Valsartan is combined with Clonidine.Valsartan may increase the hyperkalemic activities of Cyclosporine.Dalteparin may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Dapagliflozin.Dapoxetine may increase the orthostatic hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Dexmedetomidine.Diazoxide may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Diclofenac.The risk or severity of adverse effects can be increased when Valsartan is combined with Diclofenamide.The risk or severity of adverse effects can be increased when Valsartan is combined with Diflunisal.The risk or severity of adverse effects can be increased when Valsartan is combined with Diltiazem.The risk or severity of adverse effects can be increased when Valsartan is combined with Dinutuximab.The risk or severity of adverse effects can be increased when Valsartan is combined with Dipyridamole.The risk or severity of adverse effects can be increased when Valsartan is combined with Doxazosin.Valsartan may increase the hyperkalemic activities of Drospirenone.Valsartan may increase the orthostatic hypotensive activities of Duloxetine.The serum concentration of Valsartan can be increased when it is combined with Eltrombopag.The risk or severity of adverse effects can be increased when Valsartan is combined with Empagliflozin.The risk or severity of adverse effects can be increased when Valsartan is combined with Enalapril.The risk or severity of adverse effects can be increased when Valsartan is combined with Enalaprilat.Enoxaparin may increase the hyperkalemic activities of Valsartan.Valsartan may increase the orthostatic hypotensive activities of Entacapone.Eplerenone may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Eprosartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Esmolol.Valsartan may increase the hyperkalemic activities of Estradiol.The risk or severity of adverse effects can be increased when Valsartan is combined with Ethacrynic acid.The risk or severity of adverse effects can be increased when Valsartan is combined with Etodolac.The risk or severity of adverse effects can be increased when Valsartan is combined with Felodipine.The risk or severity of adverse effects can be increased when Valsartan is combined with Fenoprofen.The risk or severity of adverse effects can be increased when Valsartan is combined with Floctafenine.The risk or severity of adverse effects can be increased when Valsartan is combined with Flurbiprofen.The risk or severity of adverse effects can be increased when Valsartan is combined with Fosinopril.The risk or severity of adverse effects can be increased when Valsartan is combined with Furosemide.The risk or severity of adverse effects can be increased when Valsartan is combined with Guanfacine.Heparin may increase the hyperkalemic activities of Valsartan.Heptabarbital may increase the hypotensive activities of Valsartan.Hexobarbital may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Hydralazine.Hydrochlorothiazide may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Ibuprofen.The risk or severity of adverse effects can be increased when Valsartan is combined with Indapamide.The risk or severity of adverse effects can be increased when Valsartan is combined with Indomethacin.The risk or severity of adverse effects can be increased when Valsartan is combined with Infliximab.The risk or severity of adverse effects can be increased when Valsartan is combined with Irbesartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Isosorbide.The risk or severity of adverse effects can be increased when Valsartan is combined with Isosorbide Dinitrate.The risk or severity of adverse effects can be increased when Valsartan is combined with Isosorbide Mononitrate.The risk or severity of adverse effects can be increased when Valsartan is combined with Isoxsuprine.The risk or severity of adverse effects can be increased when Valsartan is combined with Isradipine.The risk or severity of adverse effects can be increased when Valsartan is combined with Ketoprofen.The risk or severity of adverse effects can be increased when Valsartan is combined with Ketorolac.The risk or severity of adverse effects can be increased when Valsartan is combined with Labetalol.The risk or severity of adverse effects can be increased when Valsartan is combined with Levobunolol.Valsartan may increase the orthostatic hypotensive activities of Levodopa.The risk or severity of adverse effects can be increased when Valsartan is combined with Lisinopril.The serum concentration of Lithium can be increased when it is combined with Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Losartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Mannitol.The risk or severity of adverse effects can be increased when Valsartan is combined with Mecamylamine.The risk or severity of adverse effects can be increased when Valsartan is combined with Mefenamic acid.The risk or severity of adverse effects can be increased when Valsartan is combined with Meloxicam.Metformin may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Methazolamide.Methohexital may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Methyclothiazide.The risk or severity of adverse effects can be increased when Valsartan is combined with Methyldopa.Methylphenidate may decrease the antihypertensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Metipranolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Metolazone.The risk or severity of adverse effects can be increased when Valsartan is combined with Metoprolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Minoxidil.The risk or severity of adverse effects can be increased when Valsartan is combined with Moexipril.Molsidomine may increase the hypotensive activities of Valsartan.Moxonidine may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Nabumetone.The risk or severity of adverse effects can be increased when Valsartan is combined with Nadolol.Nadroparin may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Naproxen.The risk or severity of adverse effects can be increased when Valsartan is combined with Nebivolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Nesiritide.The risk or severity of adverse effects can be increased when Valsartan is combined with Nicardipine.Nicorandil may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Nifedipine.The risk or severity of adverse effects can be increased when Valsartan is combined with Nimodipine.The risk or severity of adverse effects can be increased when Valsartan is combined with Nisoldipine.The risk or severity of adverse effects can be increased when Valsartan is combined with Nitroglycerin.The risk or severity of adverse effects can be increased when Valsartan is combined with Nitroprusside.Valsartan may increase the hypotensive activities of Obinutuzumab.The risk or severity of adverse effects can be increased when Valsartan is combined with Olmesartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Oxaprozin.The risk or severity of adverse effects can be increased when Valsartan is combined with Papaverine.The risk or severity of adverse effects can be increased when Valsartan is combined with Penbutolol.Pentobarbital may increase the hypotensive activities of Valsartan.Pentoxifylline may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Perindopril.Phenelzine may increase the orthostatic hypotensive activities of Valsartan.Phenobarbital may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Pindolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Piroxicam.Potassium Chloride may increase the hyperkalemic activities of Valsartan.Potassium Citrate may increase the hyperkalemic activities of Valsartan.Potassium Iodide may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Prazosin.Primidone may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Propranolol.The risk or severity of adverse effects can be increased when Valsartan is combined with Quetiapine.The risk or severity of adverse effects can be increased when Valsartan is combined with Quinapril.Quinine may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Ramipril.The risk or severity of adverse effects can be increased when Valsartan is combined with Reserpine.The risk or severity of adverse effects can be increased when Valsartan is combined with Riociguat.Valsartan may increase the hypotensive activities of Risperidone.Valsartan may increase the hypotensive activities of Rituximab.Secobarbital may increase the hypotensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Sotalol.Valsartan may increase the hyperkalemic activities of Spironolactone.Sulfamethoxazole may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Sulindac.Tadalafil may increase the antihypertensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Telmisartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Terazosin.The serum concentration of Valsartan can be increased when it is combined with Teriflunomide.The risk or severity of adverse effects can be increased when Valsartan is combined with Tiaprofenic acid.The risk or severity of adverse effects can be increased when Valsartan is combined with Timolol.Tinzaparin may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Tizanidine.The risk or severity of adverse effects can be increased when Valsartan is combined with Tolmetin.Tolvaptan may increase the hyperkalemic activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Torasemide.The risk or severity of adverse effects can be increased when Valsartan is combined with Trandolapril.Tranylcypromine may increase the orthostatic hypotensive activities of Valsartan.Treprostinil may increase the hypotensive activities of Valsartan.Valsartan may increase the hyperkalemic activities of Triamterene.Trimethoprim may increase the hyperkalemic activities of Valsartan.Vardenafil may increase the antihypertensive activities of Valsartan.The risk or severity of adverse effects can be increased when Valsartan is combined with Verapamil.Yohimbine may decrease the antihypertensive activities of Valsartan.Food InteractionsNot AvailableTargets
Kind: Protein
Organism: Human
Pharmacological action:
antagonist
Components
Type-1 angiotensin II receptor
References:
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
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. ):3126-33.
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. ):761-71.
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. ):1087-91.
de Gasparo M, Whitebread S: Binding of valsartan to mammalian angiotensin AT1 receptors. Regul Pept. 1995 Nov 10;59(3):303-11.
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. ):1157-63.
Kind: Protein
Organism: Human
Pharmacological action:
Components
Cytochrome P450 2C9
References:
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. ):. Epub 2009 Sep 1.
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. ):589-602.
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 J38(Database issue):D237-43. Epub 2009 Nov 24.
Kind: Protein
Organism: Human
Pharmacological action:
Components
Serum albumin
References:
Diovan. (2009). [Electronic version]. e-CPS. Retrieved September 15, 2011.
Transporters
Kind: Protein
Organism: Human
Pharmacological action:
Components
Solute carrier organic anion transporter family member 1B3
References:
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. ):585-611. Epub 2009 Nov 20.
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. ):1975-87.
Kind: Protein
Organism: Human
Pharmacological action:
Components
Solute carrier organic anion transporter family member 1B1
References:
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. ):585-611. Epub 2009 Nov 20.
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. ):1975-87.
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Drug created on June 13,
/Updated on September 16, This project is supported by the
(award #111062), , and by , a nationally-funded research and core facility that supports a wide range of cutting-edge metabolomic studies. TMIC is funded by , , and , a not-for-profit organization that is leading Canada's national genomics strategy with $900 million in funding from the federal government.DrugBank Version}

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