Valsartan is used in adults and in children 1 year of age and older alone or in combination with other medications to treat high blood pressure.
Valsartan is also used in adults to treat heart failure (condition in which the heart is unable to pump enough blood to the rest of the body) and to improve survival after a heart attack.
Valsartan works by relaxing blood vessels, which decreases the amount of work the heart has to do.
CAS Number: 137862‑53‑4
EC Number (EINECS): 604‑045‑2
Chemical Name (IUPAC): 2S)‑3‑methyl‑2‑[pentanoyl‑[[4‑[2H‑tetrazol‑5‑yl]biphenyl]‑4‑yl]methyl]amino]butanoic acid
Molecular Formula: C₄H₂₉N₅O₃
Molecular Weight: 435.52 g/mol
SYNONYMS:
Valsartan, DIOVAN, Nisis, Valsratan, Varsartan, Tareg, CGP-48933, VALSARTAN, Valsatarn, Valsartane, L-Valsartan, N-(1-Oxopentyl)-N-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine, Valsartan Impurity 113, valsartan, 137862-53-4, Diovan, CGP 48933, CGP-48933, Prexxartan, (2S)-3-methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid, N-(p-(o-1H-Tetrazol-5-ylphenyl)benzyl)-N-valeryl-L-valine, NSC-758927, 80M03YXJ7I, L-Valine, N-(1-oxopentyl)-N-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-, CHEBI:9927, DTXSID6023735, DAFIRO COMPONENT VALSARTAN, COPALIA COMPONENT VALSARTAN, EXFORGE COMPONENT VALSARTAN, IMPRIDA COMPONENT VALSARTAN, ENTRESTO COMPONENT VALSARTAN, VALTURNA COMPONENT VALSARTAN, DAFIRO-HCT COMPONENT VALSARTAN, COPALIA-HCT COMPONENT VALSARTAN, IMPRIDA-HCT COMPONENT VALSARTAN, (S)-N-valeryl-N-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]-methyl}-valine, (2S)-3-Methyl-2-(pentanoyl-((4-(2-(2H-tetrazol-5-yl)phenyl)phenyl)methyl)amino)butanoic acid, valsartanum, (S)-N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)-methyl)-valine, N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)valine, (2S)-3-methyl-2-(N-((4-(2-(2H-1,2,3,4-tetrazol-5-yl)phenyl)phenyl)methyl)pentanamido)butanoic acid, (2S)-3-methyl-2-[N-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)pentanamido]butanoic acid, 48933, CGP, RefChem:6344, C09CA03, DTXCID801508574, (2S)-3-Methyl-2-(N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)pentanamido)butanoic acid, N-pentanoyl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-L-valine, Tareg, Provas, (S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, MFCD00865840, L-Valine, N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, L-Valsartan, CHEMBL1069, N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine, 137863-60-6, C24H29N5O3, Nisis, Kalpress, Miten, Vals, N-pentanoyl-N-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-L-valine, Valzaar, Valtan, [3H]valsartan, (2S)-3-Methyl-2-(pentanoyl{[2?-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}amino)butanoic acid, N-(1-OXOPENTYL)-N-[[2'-(2H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-L-VALINE, (2~{S})-3-methyl-2-[pentanoyl-[[4-[2-(2~{H}-1,2,3,4-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid, SMR000466318, Diovan (TN), UNII-80M03YXJ7I, Valpression, Valsartana, Varexan, Valsartan RS, Valsartan CRS, Valtan, HSDB 7519, Valsartan [USAN:USP:INN:BAN], N-(1-Oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine, CGP 48933, Diovan, U35, valsartan (Diovan), Valsartan (Standard), Spectrum_001796, VALSARTAN [INN], VALSARTAN [JAN], VALSARTAN [MI], VALSARTAN [HSDB], VALSARTAN [USAN], Spectrum2_001120, Spectrum3_001831, Spectrum4_000749, Spectrum5_001582, VALSARTAN [VANDF], VALSARTAN [MART.], EC 604-045-2, SCHEMBL2542, VALSARTAN [USP-RS], VALSARTAN [WHO-DD], BSPBio_003501, GTPL593, KBioGR_001078, KBioSS_002289, VALSARTAN [EMA EPAR], MLS000759423, MLS001424088, BIDD:GT0345, SCHEMBL678231, SPECTRUM1505209, SPBio_001260, Valsartan - Bio-X trade mark, Valsartan (JP18/USP/INN), GTPL3937, orb1300528, VALSARTAN [EP IMPURITY], VALSARTAN [ORANGE BOOK], SCHEMBL29406387, VALSARTAN [EP MONOGRAPH], Valsartan, >=98% (HPLC), KBio2_002287, KBio2_004855, KBio2_007423, KBio3_003006, EZR-104, VAL-489, VALSARTAN [USP MONOGRAPH], GLXC-05207, HMS1922L21, HMS2051L12, HMS2093K22, HMS2232F05, HMS3651E04, HMS3715P12, Pharmakon1600-01505209, (2R)-3-Methyl-2-[pentanoyl[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]amino]butanoic Acid (Valsartan (R)-Enantiomer), ALBB-038653, BB_SC-02163, MSK10065, AGSAV301 COMPONENT VALSARTAN, BDBM50049186, EBC-11260, HY-18204R, NSC758927, s1894, Valsartan for system suitability CRS, DIOVAN HCT COMPONENT VALSARTAN, Valsartan for peak identification CRS, AKOS015914315, AKOS015994698, EXFORGE HCT COMPONENT VALSARTAN, AC-4543, CCG-101028, CCG-221275, CS-1967, DB00177, DS-1248, FV28662, KS-1194, NC00278, NSC 758927, (s)-2-(n-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)pentanamido)-3-methylbutanoic acid, N-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-N-pentanoyl-L-valine, NCGC00178027-08, NCGC00178027-11, NCGC00178027-19, (2S)-3-methyl-2-(N-{[2'-(1H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}pentanamido)butanoic acid, BV164506, HY-18204, SBI-0206738.P001, SW197658-2, V0112, 62V534, D00400, AB00639940-06, AB00639940-08, AB00639940_09, AB00639940_11, EN300-6482022, F036602, Q155472, SR-05000001928, SR-05000001928-1, BRD-K45158365-001-02-3, BRD-K45158365-001-05-6, BRD-K45158365-001-10-6, BRD-K45158365-001-11-4, Z1379303659, Valsartan Working Standard (Secondary Reference Standard), Valsartan, European Pharmacopoeia (EP) Reference Standard, Valsartan, United States Pharmacopeia (USP) Reference Standard, N-Valeryl-N-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-L-valine, Valsartan, Pharmaceutical Secondary Standard, Certified Reference Material, (5)-2-{N-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]pentanamido}-3-methylbutanoic acid, (S)-3-Methyl-2-{pentanoyl-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butyric acid, 3-Methyl-2-{pentanoyl-[2''-(1H-tetrazol-5-yl)-biphenyl-4-yl]-amino}-butyric acid, L-Valine,N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-3-yl]methyl]-(9ci), N-(1-oxopentyl)-N-[[2'-(1h-tetrazol-5-yl) [1,1'-bi-phenyl]-4-yl]methyl]-l-valine, N-(1-Oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-(L)-valine, N-pentanoyl-N-{[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl}-L-valine, Valsartan for peak identification, European Pharmacopoeia (EP) Reference Standard, Valsartan for system suitability, European Pharmacopoeia (EP) Reference Standard, (2S)-3-Methyl-2-{N-pentanoyl-N'-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butanoic acid, (2S)-3-Methyl-2-{pentanoyl-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butyric acid, (S)-2-(N-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoicacid, (S)-2-(N-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, (s)-3-methyl-2-[N-({4-[2-(2h-1,2,3,4-tetrazol-5-yl) phenyl]phenyl}methyl)pentanamido]butanoic acid, (s)-3-methyl-2-{pentanoyl-[-2'-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butyric acid, (S)-3-Methyl-2-{pentanoyl-[2''-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butyric acid, (S)-3-Methyl-2-{pentanoyl-[2''-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butyric acid, (S)-N-(1-carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[2'(1H-tetrazol-5-yl)biphenyl-4-yl-methyl]amine, (S)-N-(1-carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amine, (S)-N-(1-Carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-amine, 2-{[2''-(2,3-Dihydro-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-pentanoyl-amino}-3-methyl-butyric acid, 3-Methyl-2-{((S)-pentanoyl)-[2''-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amino}-butyric acid, L-Valine, N-(1-oxopentyl)-N-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, (S)-2-(N-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid
Valsartan is a synthetic small molecule that belongs to the class of angiotensin II receptor blockers (ARBs), designed to modulate the renin‑angiotensin‑aldosterone system (RAAS).
Chemically, Valsartan is known by the molecular formula C₂₄H₂₉N₅O₃ and has a molecular weight of approximately 435.5 g/mol.
Its distinctive structure includes a biphenyl‑tetrazole group and an L‑valine derived side chain, which together facilitate high affinity for the angiotensin II type 1 (AT₁) receptor.
The biphenyl and tetrazole components serve as bioisosteres that help mimic the natural ligand while improving stability and receptor binding specificity.
Valsartan is typically supplied as a white to off‑white solid crystalline powder that is practically insoluble in water but soluble in several organic solvents, characteristics that are important for its pharmaceutical formulation.
In the human body, valsartan exerts its effect by selectively blocking the AT₁ receptor, one of the main receptors for angiotensin II, a potent regulator of vascular tone and fluid balance.
Angiotensin II normally binds to this receptor to induce vasoconstriction and promote the release of aldosterone, which contributes to increased blood pressure and fluid retention.
By preventing angiotensin II from interacting with the AT₁ receptor, valsartan effectively promotes vasodilation, supporting lower systemic blood pressure and a reduced workload on the cardiovascular system.
Importantly, valsartan does this without inhibiting the enzyme that generates angiotensin II, which means it interacts directly at the receptor level rather than altering enzyme activity.
Valsartan's affinity for the AT₁ receptor is many thousands of times greater than for the related AT₂ receptor, which has different physiological roles.
From a pharmacokinetic perspective, valsartan is rapidly absorbed after oral administration, with peak plasma concentrations typically reached within 2–4 hours.
Bioavailability after oral dosing is moderate, and Valsartan is highly bound to plasma proteins, which influences its distribution in the body.
The volume of distribution is relatively modest, indicating most of the drug remains in the vascular and interstitial compartments rather than extensively penetrating into tissues.
Valsartan is only minimally metabolized, with the majority of the unchanged molecule being excreted through feces and a smaller proportion via urine.
These characteristics support a dosing regimen that generally allows once‑daily administration in many patients.
In clinical practice, valsartan has become a staple in the management of hypertension, where it helps lower both systolic and diastolic blood pressure with a sustained effect over a 24‑hour dosing interval.
Valsartan's activity extends across diverse patient populations and can be enhanced when used in fixed‑dose combinations with other antihypertensive agents, such as hydrochlorothiazide, for more robust blood‑pressure control where needed.
Research spanning large outcome trials has also shown that valsartan contributes to improved cardiovascular outcomes — for example, reducing the likelihood of hospitalization due to heart failure and supporting cardiac performance in certain conditions.
Additionally, valsartan has demonstrated beneficial effects on markers associated with vascular health, such as reductions in circulating factors linked to endothelial dysfunction.
Given its unique mechanism of action, valsartan provides an alternative to other classes of blood pressure medications such as ACE inhibitors.
Unlike ACE inhibitors, which target the enzyme responsible for converting angiotensin I to angiotensin II, valsartan’s receptor‑blocking strategy ensures that it can neutralize angiotensin II derived from all pathways.
This receptor‑level blockade offers complete antagonism of angiotensin II’s pressor actions regardless of its route of formation.
Furthermore, because valsartan does not influence cellular pathways related to bradykinin metabolism, certain side effects that are more common with other antihypertensive classes — such as cough — are typically not associated with its use, making it suitable for patients preferring or requiring this pharmacologic profile.
Pharmaceutical science also recognizes that valsartan’s poor water solubility and moderate bioavailability present challenges and opportunities for formulation improvement.
Researchers have explored advanced tablet formulations and drug‑delivery strategies — including solid dispersions and specialized carriers — to enhance dissolution properties and consistency of therapeutic effects.
These formulation innovations aim to optimize the medication’s performance in clinical settings, especially in populations where precise control of blood pressure is essential from the outset of treatment.
Overall, valsartan represents a well‑characterized and widely used member of the ARB family, supported by decades of clinical experience and pharmaceutical research.
Its development marked a significant advancement in cardiovascular therapeutics, offering effective blood‑pressure management with pharmacologic attributes tailored for sustained and selective angiotensin II receptor blockade.
Valsartan, sold under the brand name Diovan among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease.
Valsartan is an angiotensin II receptor blocker (ARB).
Valsartan is a reasonable initial treatment for high blood pressure.
Valsartan is taken by mouth.
Using Valsartan in pregnancy may harm the baby and use when breastfeeding is not recommended.
Valsartan is an angiotensin II receptor antagonist and works by blocking the effects of angiotensin II.
Valsartan was patented in 1990, and came into medical use in 1996.
Valsartan is available as a generic medication.
In 2023, Valsartan was the 85th most commonly prescribed medication in the United States, with more than 7 million prescriptions.
Valsartan is an angiotensin II receptor blocker (ARB) that may be used to treat high blood pressure or reduce the risk of being admitted to the hospital if you have heart failure.
Specifically, valsartan is FDA-approved to:
*Lower high blood pressure in adults and children aged 1 year and older, either alone or in combination with other blood pressure medicines.
*Decrease the need for hospitalization because of heart failure in adults with heart failure.
*Increase the chance of living longer after a heart attack (myocardial infarction) in adults with certain types of heart failure.
Valsartan is an Angiotensin 2 Receptor Blocker.
The mechanism of action of valsartan is as an Angiotensin 2 Receptor Antagonist.
Valsartan is an angiotensin II receptor blocker used alone or in combination with other agents to treat hypertension and reduce cardiovascular mortality after myocardial infarction.
Valsartan is an orally active nonpeptide triazole-derived antagonist of angiotensin (AT) II with antihypertensive properties.
Valsartan selectively and competitively blocks the binding of angiotensin II to the AT1 subtype receptor in vascular smooth muscle and the adrenal gland, preventing AT II-mediated vasoconstriction, aldosterone synthesis and secretion, and renal reabsorption of sodium, and resulting in vasodilation, increased excretion of sodium and water, a reduction in plasma volume, and a reduction in blood pressure.
Valsartan is a small molecule drug with a maximum clinical trial phase of IV (across all indications) that was first approved in 1996 and has 8 approved and 22 investigational indications.
Valsartan is a tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.
Valsartan is a monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group.
Valsartan exhibits antihypertensive activity.
Valsartan has a role as an antihypertensive agent, an angiotensin receptor antagonist, a xenobiotic and an environmental contaminant.
Valsartan is a biphenylyltetrazole, a monocarboxylic acid amide and a monocarboxylic acid.
Valsartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes telmisartan, candesartan, losartan, olmesartan, and irbesartan.
ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects, which include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium, among others.
Overall, valsartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.
Valsartan also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions.
Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease.
In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function.
ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.
By comparison, the angiotensin-converting enzyme inhibitor (ACEI) class of medications (which includes drugs such as ramipril, lisinopril, and perindopril) inhibit the conversion of angiotensin I to angiotensin II through inhibition of the ACE enzyme.
However, this does not prevent the formation of all angiotensin II within the body.
The angiotensin II receptor blocker (ARB) family of drugs is unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized.
Valsartan is commonly used for the management of hypertension, heart failure, and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors.
ARBs such as valsartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization.
Valsartan also slows the progression of diabetic nephropathy due to its renoprotective effects.
Improvements in chronic kidney disease with valsartan include both clinically and statistically significant decreases in urinary albumin and protein excretion in patients diagnosed with type 2 diabetes and in nondiabetic patients diagnosed with chronic kidney disease.
Valsartan was initially approved in 1996 in Europe for the treatment of hypertension in adults.
Shortly after, in 1997, this drug was approved in the United States.
Valsartan is generally well-tolerated with a side-effect profile superior to that of other antihypertensive drugs.
USES and APPLICATIONS of VALSARTAN:
Medical uses: Valsartan is used to treat high blood pressure, heart failure, and to reduce death for people with left ventricular dysfunction after having a heart attack.
Valsartan should not be used to treat high blood pressure in children less than 1 year of age and it is not known if it is safe and effective in children with certain kidney problems.
Valsartan works by blocking angiotensin II, a powerful blood pressure regulator that narrows blood vessels (vasoconstriction), affects the production and release of aldosterone, stimulates the heart, and promotes sodium reabsorption by the kidneys.
Valsartan blocks angiotensin II from binding to the AT1 receptor in many tissues such as blood vessel smooth muscle and the adrenal gland, lowering blood pressure.
Valsartan is used in adults and in children 1 year of age and older alone or in combination with other medications to treat high blood pressure.
Valsartan is also used in adults to treat heart failure (condition in which the heart is unable to pump enough blood to the rest of the body) and to improve survival after a heart attack.
Valsartan is in a class of medications called angiotensin II receptor antagonists.
Valsartan works by blocking the action of certain natural substances that tighten the blood vessels, allowing the blood to flow more smoothly and the heart to pump more efficiently.
High blood pressure is a common condition and when not treated, can cause damage to the brain, heart, blood vessels, kidneys and other parts of the body.
Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems.
In addition to taking medication, making lifestyle changes will also help to control your blood pressure.
These changes include eating a diet that is low in fat and salt, maintaining a healthy weight, exercising at least 30 minutes most days, not smoking, and using alcohol in moderation.
Valsartan comes as a tablet and a suspension (liquid) to take by mouth.
For the treatment of high blood pressure, the tablet or suspension is usually taken once a day with or without food.
For the treatment of heart failure or heart attack, Valsartan is usually taken twice a day with or without food.
To help you remember to take valsartan, take it at around the same time(s) every day.
Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.
Take valsartan exactly as directed.
Do not take more or less of Valsartan or take it more often than prescribed by your doctor.
Shake the suspension well for at least 10 seconds before each use to mix the medication evenly.
Each valsartan product releases the medication differently in your body and cannot be used interchangeably.
Only take the valsartan product prescribed by your doctor and do not switch to a different valsartan product unless your doctor says that you should.
Your doctor will probably only tell you to take valsartan suspension if you are younger than 5 years of age or unable to swallow tablets.
Your doctor may start you on a low dose of valsartan and gradually increase your dose.
Valsartan controls high blood pressure and heart failure but does not cure them.
Your blood pressure may decrease during the first 2 weeks of your treatment, but it may take 4 weeks for you to notice the full benefit of valsartan.
Continue to take valsartan even if you feel well.
Do not stop taking valsartan without talking to your doctor.
Ask your pharmacist or doctor for a copy of the manufacturer's information for the patient.
Valsartan is also sometimes used to treat diabetic nephropathy (kidney disease in people with diabetes and high blood pressure).
Talk to your doctor about the risks of using this medication for your condition.
Valsartan may be prescribed for other uses; ask your doctor or pharmacist for more information.
Valsartan treats high blood pressure and heart failure.
Valsartan may also be used to prevent further damage after a heart attack.
Valsartan works by relaxing blood vessels, which decreases the amount of work the heart has to do.
Valsartan belongs to a group of medications called ARBs.
Valsartan is used alone or together with other medicines to treat high blood pressure (hypertension).
High blood pressure adds to the workload of the heart and arteries.
If it continues for a long time, the heart and arteries may not function properly.
This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure.
Lowering blood pressure can reduce the risk of strokes and heart attacks.
Valsartan is also used to treat heart failure and left ventricular failure after a heart attack.
Left ventricular failure occurs when the left side of the heart (the main pumping chamber) becomes stiff and enlarged or swollen.
This causes pooling of blood in the lungs because the heart is not pumping properly.
Valsartan is an angiotensin II receptor blocker (ARB).
Valsartan works by blocking a substance in the body that causes blood vessels to tighten.
Valsartan relaxes the blood vessels and lowers blood pressure.
A lower blood pressure will increase the supply of blood and oxygen to the heart.
-High blood pressure uses of Valsartan:
Valsartan (and other ARBs) are an appropriate initial treatment option for most people with high blood pressure and no other coexisting conditions, as are ACE inhibitors, thiazide diuretics and calcium channel blockers.
If patients have coexisting diabetes or kidney disease, ARBs or ACE inhibitors may be considered over other classes of blood pressure medicines.
-Heart failure uses of Valsartan:
Valsartan has reduced rates of mortality and heart failure hospitalisations when used alone or in combination with beta blockers in the treatment of heart failure.
Importantly, the combination of valsartan and ACE inhibitors has not shown morbidity or mortality benefits but rather increases mortality risk when added to combination beta blocker and ACE inhibitor therapy, and increases the risk of adverse events like hyperkalaemia, hypotension and renal failure.
As shown in the PARADIGM-HF study, valsartan combined with sacubitril for the treatment of heart failure, significantly reduced all cause and cardiovascular mortality and hospitalisations due to heart failure.
-Diabetic kidney disease uses of Valsartan:
In people with type 2 diabetes, antihypertensive therapy with valsartan decreases the rate of progression of albuminuria (albumin in urine), promotes regression to normoalbuminuria and may reduce the rate of progression to end-stage kidney disease.
-Medical (Pharmaceutical) Uses of Valsartan:
*Antihypertensive Drug:
Valsartan treats essential hypertension (high blood pressure).
*Heart Failure Management:
Valsartan is used in mild to moderate heart failure, often when ACE inhibitors are unsuitable.
*Post‑Myocardial Infarction:
Valsartan reduces morbidity and mortality after heart attack with left ventricular dysfunction.
*Diabetic Nephropathy:
Valsartan protects kidney function in type 2 diabetes with kidney disease.
Valsartan is often combined with other agents (e.g., hydrochlorothiazide, amlodipine, or sacubitril) for enhanced cardiovascular effects.
MECHANISM OF ACTION of VALSARTAN:
Valsartan acts as an angiotensin II receptor blocker (ARB) — selectively inhibits the AT₁ receptor.
This reduces vasoconstriction, sodium and water retention, aldosterone release, and helps lower blood pressure.
PHARMACOLOGICAL CHARACTERISTICS of VALSARTAN:
Competitive antagonist of angiotensin II type 1 receptors.
High affinity and selectivity over other angiotensin receptor subtypes.
Valsartan reduces blood pressure and cardiovascular strain by vasodilation and increased sodium excretion.
CHARACTERISTICS & BENEFITS of VALSARTAN:
*Pharmacodynamic Benefits
Effective blood‑pressure reduction with a generally favorable side‑effect profile vs. some other antihypertensives.
*Clinical Benefits
Valsartan improves survival after certain cardiac events.
Renoprotective effects in diabetic nephropathy.
*Chemical Characteristics
Biphenylyltetrazole structure — typical motif for ARBs.
Moderate lipophilicity, acidity, and solid crystalline nature suitable for oral tablet formulations.
WHAT SHOULD I TELL MY CARE TEAM BEFORE I TAKE VALSARTAN?
They need to know if you have any of these conditions:
*Heart failure
*Kidney disease
*Liver disease
*An unusual or allergic reaction to valsartan, other medications, foods, dyes, or preservatives
*Pregnant or trying to get pregnant
*Breastfeeding
HOW SHOULD I USE VALSARTAN?
Take Valsartan by mouth.
Take Valsartan as directed on the prescription label at the same time every day.
You can take Valsartan with or without food.
If it upsets your stomach, take Valsartan with food.
Keep taking Valsartan unless your care team tells you to stop.
WHAT IS VALSARTAN USED FOR?
Valsartan is commonly used for the following conditions.
*To lower high blood pressure (hypertension)
*To lower the risk of hospitalization for heart failure in people with heart failure
*To lower the risk of death in people whose heart is not pumping blood as well as it should after a heart attack
Valsartan may also be used for other conditions as determined by your healthcare provider.
Valsartan blocks receptors in your body that normally bind to a hormone called angiotensin II.
When angiotensin II binds to these receptors, it causes your blood vessels to constrict and body to release a hormone that tells your kidneys to keep sodium.
Blocking these receptors help your blood vessels relax so that blood can move through them more easily.
These effects can help your heart work better, lower blood pressure, and may reduce your risk for heart attack and stroke.
Angiotensin II is a substance that causes the blood vessels to become narrower and this causes an increase in blood pressure.
Valsartan lowers blood pressure by blocking the effects of a substance called Angiotensin II at the blood vessel walls.
Valsartan can also be used for patients who have protein in their urine and other heart conditions.
Do not stop taking your medicine without checking with your healthcare provider.
Valsartan may be taken with or without food.
If you miss a dose, take the missed dose as soon as you remember.
If Valsartan is almost time for your next dose, take only the usual dose.
Do not double your dose or use extra medicine to make up for the missed dose.
Valsartan is an antihypertensive drug from the group of AT1 receptor antagonists (sartans), used to treat arterial hypertension, heart failure and diabetic nephropathy in type 2 diabetes mellitus.
The exact chemical name (IUPAC name) of valsartan is (S)-3-methyl-2-{N-[2'- (1H-tetrazol-5-yl)biphenyl-4-ylmethyl]pentanamido}butyric acid or (S)-3-methyl-2-{N-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]pentanamido}-butyric acid.
The molecular formula of Valsartan is C24H29N5O3.
The molecular mass (molecular weight) of Valsartan is 435.52 g·mol⁻¹.
Valsartan works by competitively and non-competitively blocking AT1 receptors, which act as binding sites for angiotensin II.
High-affinity blockade of AT1 receptors reduces the contractility of smooth muscle cells, leading to a decrease in peripheral vascular resistance and consequently a reduction in blood pressure.
Simultaneously, the release of aldosterone from the adrenal cortex is reduced.
Unlike antihypertensive drugs from the ACE inhibitor group, valsartan does not affect the breakdown of kinins (especially bradykinin) and substance P, thus avoiding the characteristic side effects of ACE inhibitors (e.g., ACE inhibitor cough).
Valsartan is administered orally and, after absorption in the small intestine, achieves a bioavailability of approximately 25% in the body.
Valsartan is eliminated 30% via the kidneys and 70% metabolized in the liver.
The plasma half-life of valsartan is 6 to 9 hours.
Due to its antihypertensive effect, Valsartan is primarily used in the treatment of arterial hypertension when the administration of alternative ACE inhibitors causes side effects or is contraindicated.
Other areas of application of Valsartan include chronic heart failure.
Other areas of application of Valsartan include diabetic nephropathy in type 2 diabetes mellitus.
Other areas of application of Valsartan include prophylaxis after heart attack.
PHYSICAL and CHEMICAL PROPERTIES of VALSARTAN:
Chemical Name (IUPAC):(2S)-3-methyl-2-[pentanoyl-[[4-[2H-tetrazol-5-yl]biphenyl]-4-yl]methyl]amino]butanoic acid
Common Name:Valsartan
CAS Number:137862-53-4
EC Number (EINECS):604-045-2
Molecular Formula:C₄H₂₉N₅O₃
Molecular Weight:435.52 g/mol
InChIKey:ACWBQPMHZXGDFX-QFIPXVFZSA-N
Appearance & Physical Form:White to tan solid / powder
Melting & Boiling
Melting Point:~116–117 °C
Boiling Point:~684.9 ± 65.0 °C (predicted)
Density & Solubility
Density:~1.212 ± 0.06 g/cm³
Water Solubility:~84.99 mg/L at 25 °C (moderately low)
Soluble:in organic solvents such as DMSO at high concentrations
Chemical Behavior
Hygroscopic (absorbs moisture from air)
pKa:~3.56–4.38 (acid dissociation, predicted experimental)
LogP:~1.2–2.8 (lipophilicity measure)
Structural Characteristics
Contains a tetrazole ring and biphenyl moiety — typical of “sartan” class angiotensin receptor blockers
Molecular Weight:435.5 g/mol
XLogP3-AA:4.4
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:10
Exact Mass:435.22703980 Da
Monoisotopic Mass:435.22703980 Da
Topological Polar Surface Area:112 Ų
Heavy Atom Count:32
Formal Charge:0
Complexity:608
Isotope Atom Count:0
Defined Atom Stereocenter Count:1
Undefined Atom Stereocenter Count:0
Defined Bond Stereocenter Count:0
Undefined Bond Stereocenter Count:0
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
FIRST AID MEASURES of VALSARTAN:
-Description of first-aid measures
*General advice:
Show this material safety data sheet to the doctor in attendance.
*If inhaled:
After inhalation:
Fresh air.
*In case of skin contact:
Take off immediately all contaminated clothing.
Rinse skin with
water/ shower.
*In case of eye contact:
After eye contact:
Rinse out with plenty of water.
Call in ophthalmologist.
Remove contact lenses.
*If swallowed:
After swallowing:
Immediately make victim drink water (two glasses at most).
Consult a physician.
-Indication of any immediate medical attention and special treatment needed.
No data available
ACCIDENTAL RELEASE MEASURES of VALSARTAN:
-Environmental precautions:
Do not let product enter drains.
-Methods and materials for containment and cleaning up:
Cover drains.
Collect, bind, and pump off spills.
Observe possible material restrictions.
Take up dry.
Dispose of properly.
Clean up affected area.
FIRE FIGHTING MEASURES of VALSARTAN:
-Extinguishing media:
*Suitable extinguishing media:
Carbon dioxide (CO2)
Foam
Dry powder
*Unsuitable extinguishing media:
For this substance/mixture no limitations of extinguishing agents are given.
-Further information:
Prevent fire extinguishing water from contaminating surface water or the ground water system.
EXPOSURE CONTROLS/PERSONAL PROTECTION of VALSARTAN:
-Control parameters:
--Ingredients with workplace control parameters:
-Exposure controls:
--Personal protective equipment:
*Eye/face protection:
Use equipment for eye protection.
Safety glasses
*Body Protection:
protective clothing
*Respiratory protection:
Recommended Filter type: Filter A
-Control of environmental exposure:
Do not let product enter drains.
HANDLING and STORAGE of VALSARTAN:
-Conditions for safe storage, including any incompatibilities:
*Storage conditions:
Tightly closed.
Dry.
STABILITY and REACTIVITY of VALSARTAN:
-Chemical stability:
The product is chemically stable under standard ambient conditions (room temperature).
-Possibility of hazardous reactions:
No data available