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Valsartan

Basic information Indications and Usage Mechanisms of Action Pharmacokinetics Clinical Research Safety Related Supplier
Valsartan Basic information
Valsartan Chemical Properties
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Valsartan Usage And Synthesis
  • Indications and UsageValsartan is a type of specific angiotensin I (AT1) receptor antagonist and a clinical non-dermal AT1 receptor antagonist following losartan that has important effects in adjusting bodily blood pressure and maintaining electrolyte-body fluid balance. Valsartan’s antihypertensive effects are stronger than those of enalapril and is suitable for treating hypertension, mild to moderate primary hypertension, and especially secondary hypertension caused by renal damage. It can significantly reduce proteinuria for hypertension patients with diabetes or normal liver functions, and it can promote uric acid and urinary sodium to protect the kidney. Valsartan is also suitable for reducing the cardiovascular mortality for high risk patients (left ventricular failure or dysfunction) after experiencing a heart attack.
  • Mechanisms of ActionValsartan selectively affects the AT1 receptor subtype and prevents AT1 from binding with AT1 receptors (its selective AT1 receptor antagonizing effect is about 20000 times greater than its effects on AT2 receptors), thus inhibiting vasoconstriction and aldosterone release, producing an antihypertensive effect, but it cannot inhibit the release of aldosterone caused by potassium ions (K+). Valsartan does not affect angiotensin-converting enzymes (ACE) or renin and its receptors, and it does not inhibit ion channels related to blood pressure regulation and sodium balance. Valsartan does not inhibit ACE and does not affect bodily bradykinin levels, thus causing less coughing side effects than ACE inhibitors. Valsartan does not affect heart rate when lowering blood pressure. Sudden ceasing in Valsartan use will not cause rebound hypertension or other side effects. Valsartan does not affect hypertension patients’ overall cholesterol, triglyceride, blood glucose, or uric acid levels.
  • PharmacokineticsFor most patients, a single oral dose will have antihypertensive effects that occur within 2 hours, peak at 4-6 hours, and continue for over 24 hours. 2-4 weeks of treatment will result in maximum hypertensive curative effects, which will last throughout long-term treatment. It can be used with thiazide diuretics to further strengthen antihypertensive effects.
  • Clinical ResearchA clinical trial showed that Valsartan has very noticeable effects on mild to moderate hypertension. A daily dose of ≥80 mg can effectively control systolic and diastolic blood pressure while not affecting blood pressure’s circadian rhythm; a daily 160mg dose has more noticeable effects than a daily 100mg dose of losartan. Moderate hypertension patients with intact renal functions have a good tolerance towards Valsartan, Valsartan’s curative effects are significantly superior to those of ACE inhibitors, and there are minimal adverse reactions. Effective in treating severe hypertension when combined with other antihypertensive drugs.
  • DescriptionDiovan was launched in Germany and the UK as an angiotensin Ⅱ antagonist for use as an antihypertensive agent. Biphenylbromomethyl nitrite serves as the starting material for a three step synthesis of the compound, in which the (S)- enantiomer is more active than the (R)-enantiomer. Valsartan is a nonpeptide drug which is a highly specific antagonist of the AT1 receptor and is potent and orally active. This receptor is responsible for angiotensin Ⅱ cardiovascular effects (aldosterone and catecholamine secretion, vascular constriction, positive inotropic response and renal effects). Unlike losartan, it is not a prodrug and a single daily dose is comparible in activity to the ACE drug enalapril. It also did not exhibit the coughing side effect observed with ACE inhibitors. Diovan is slowly metabolized (long lasting) with its main metabolite being significantly less active. There was no evidence of rebound hypertension when drug treatment was terminated and was as effective as the dihydropyridine Ca antagonist anlodipine.
  • Chemical PropertiesWhite Crystalline Powder
  • OriginatorNorvartis (Switzerland)
  • UsesA nonpeptide angiotensin II AT1-receptor antagonist. Antihypertensive.
  • UsesAngiotensin II inhibitor, antihypertensive
  • UsesMay 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 l
  • DefinitionChEBI: 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. It exhibits antihypertensive activity.
  • Manufacturing Process0.5 g of 2'-cyanobiphenyl-4-carbaldehyde, 2.5 g of molecular sieve 5 A in tetrahydrofuran with stirring at room temperature for 36 hours; then the reaction mixture was cooled to 0°-5°C, 0.815 g of (L)-valine methyl ester hydrochloride and 180 mg of sodium cyanoborohydride dissolved in 4.8 ml of methanol are added. The mixture is stirred at room temperature for 24 hours and then concentrated in vacuo yields N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)- valine methyl ester after flash chromatography.
    1.15 g of N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester, 0.625 ml of triethylamine in 9 ml of dichloromethane are treated 0.56 ml of n-valeryl chloride at 0°C and stirred at room temperature overnight and then evaporated to dryness. The residue is taken up in diethyl ether and the diethyl ether mixture is washed with sodium hydrogencarbonate solution and brine.
    Flash chromatography (180 g of silica gel; ethyl acetate/petroleum ether 1:1) yields N-valeryl-N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester. (S)-N-(1-Carboxy-2-methyl-prop-1-yl)-N-pentanoyl-N-[2'-(1H-tetrazol-5- yl)biphenyl-4-ylmethyl]-amine. The product can be prepared starting from 1.40 g of N-valeryl-N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester and 2.25 g of tributyltin azide with subsequent flash chromatography; melting interval 105°-115°C (from ethyl acetate).
  • brand nameDiovan (Novartis).
  • Therapeutic FunctionAntihypertensive
  • General DescriptionValsartan, N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-L-valine (Diovan), likelosartan, possesses the acidic tetrazole system, which mostlikely plays a role, similar to that of the acidic groups of angiotensinII, in binding to the angiotensin II receptor. In addition,the biphenyl system that serves to separate the tetrazolefrom the aliphatic nitrogen is still present. In addition, there isa carboxylic acid side chain in the valine moiety that alsoserves to bind to the angiotensin II receptor.
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