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Valsartan

Valsartan structure

CAS No:
137862-53-4
Formula:
C24H29N5O3
Chemical Name:
Valsartan
Synonyms:
L-Valine,N-(1-oxopentyl)-N-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-;L-Valine,N-(1-oxopentyl)-N-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-;N-(1-Oxopentyl)-N-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine;Valsartan;CGP 48933;Diovan;Tareg;Nisis;Valsartanin;Cardopan;Valsarect;Vazar;(2S)-3-Methyl-2-[pentanoyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid;186597-74-0
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

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Description

Valsartan (CGP-48933) is an angiotensin II receptor antagonist for treatment of high blood pressure and heart failure.

3-methyl-2-[1-oxopentyl-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]amino]butanoic acid is a N-acyl-amino acid.

Valsartan Basic Attributes

Molecular Weight：

435.52

Exact Mass：

435.52

EC Number：

1592732-453-0

HScode：

2933990090

Characteristics

PSA：

112

XLogP3：

4.4

Appearance：

white to tan

Density：

1.2±0.1 g/cm3

Melting Point：

116-117 °C

Boiling Point：

684.9ºC at 760 mmHg

Flash Point：

368.0±34.3 °C

Refractive Index：

1.587

Water Solubility：

DMSO: ≥20mg/mL

Storage Conditions：

-20°C Freezer, Under inert atmosphere

Vapor Pressure：

8.18X10-16 mm Hg at 25 deg C (est)

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

36/37/38

safety instructions：

26-37/39

RTECS Number：

YV9455000

Marks：

Stability/Shelf Life：

Hygroscopic

Precautionary statement(s)：

P201, P202, P273, P281, P308+P313, P405, P501

Hazard Statements：

H413

Valsartan Use and Manufacturing

May 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

Computed Properties

Molecular Weight:435.5
XLogP3:4.4
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:10
Exact Mass:435.22703980
Monoisotopic Mass:435.22703980
Topological Polar Surface Area:112
Heavy Atom Count:32
Complexity:608
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Price Analysis

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Drug Function and Efficacy

Valsartan is an orally effective specific angiotensin (AT) II receptor antagonist that selectively acts on the AT1 receptor subtype and produces all known effects. The AT2 receptor subtype is not related to cardiovascular effects. Valsartan does not have any partial agonist activity on the AT1 receptor. The affinity of valsartan for the AT1 receptor is 20,000 times stronger than that for the AT2 receptor. Valsartan has no inhibitory effect on ACE and does not cause retention of bradykinin or substance P, so it does not cause coughing.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Valsartan Dispersible Tablets
Ingredients	Valsartan
Indication	No obvious drug interactions have been found clinically. The following drugs have been studied: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide. Since valsartan is almost not metabolized, no clinical interactions with drugs that induce valsartan dispersible tablets or inhibit the cytochrome P450 system have been found. Although valsartan is mostly bound to plasma proteins, in vitro experiments have not found that it interacts with other plasma protein-bound drugs (such as diclofenac, furosemide, and warfarin) at this level. When used in combination with potassium-sparing diuretics (such as spironolactone, triamterene, and amiloride), potassium supplementation or the use of potassium-containing preparations can lead to increased blood potassium concentrations. Therefore, caution is required when using combined medications.
Specifications	40mg
Manufacturer	Lunan BETTER Pharmaceutical Co., Ltd.

Valsartan Hydrochlorothiazide Tablets
Ingredients	This product is a compound preparation, its components are: valsartan 80mg, hydrochlorothiazide 12.5mg.
Indication	The antihypertensive effect of this product can be enhanced by co-administration with other antihypertensive drugs. It is necessary to be cautious and monitor the serum potassium level when co-administered with potassium-sparing diuretics, potassium supplements or potassium-containing salt substitutes, or other drugs that increase serum potassium (such as heparin). It has been reported that the simultaneous use of lithium, ACE inhibitors and/or thiazide diuretics can cause a reversible increase in serum potassium concentration and lithium poisoning. There is no experience of the simultaneous use of valsartan and lithium. Therefore, it is recommended to regularly monitor serum lithium levels when lithium and this product are used in combination. No clinically significant interactions have been observed between valsartan alone and any of the following drugs, including: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide. Because this product contains thiazide diuretic components, the following interactions may occur: Co-administration with nonsteroidal anti-inflammatory drugs (such as salicylic acid derivatives, indomethacin) may weaken the diuretic and antihypertensive activity of the thiazide components in this product. Acute renal failure may occur if volume depletion is present. Concomitant administration with potassium-wasting diuretics (e.g. furosemide), corticosteroids, adrenocorticotropic hormone (ACTH), amphotericin B, carbenoxolone, penicillin G, or salicylic acid derivatives may exacerbate potassium and/or magnesium loss. Hypokalemia or hypomagnesemia caused by thiazides may increase the risk of arrhythmias in patients taking cardiac glycosides. Thiazide diuretics increase the effect of curare-like muscle relaxants. Adjustment of the dose of insulin or oral antidiabetic drugs may be necessary. Concomitant use with thiazide diuretics may increase the incidence of hypersensitivity reactions to allopurinol. May increase the risk of adverse reactions caused by amantadine. Thiazides may also enhance the blood glucose-raising effect of diazoxide. Thiazides may reduce the renal excretion of cytotoxic drugs (e.g. cyclophosphamide, methotrexate), thereby increasing their bone marrow suppressive effects. The bioavailability of thiazide diuretics may increase when anticholinergic drugs (e.g., atropine, biperiden) are given simultaneously, probably as a result of decreased gastrointestinal motility and slower gastric emptying. There are isolated reports of hemolytic anemia caused by the combined use of hydrochlorothiazide and methyldopa. Cholestyramine and colestipol reduce the absorption of thiazide diuretics. The combined use of thiazide diuretics and vitamin D or calcium salts can enhance the effect of raising blood calcium. The combined use of cyclosporine may increase the risk of hyperuricemia causing symptoms of gout.
Specifications	Each tablet contains 80 mg of valsartan and 12.5 mg of hydrochlorothiazide
Manufacturer	Changzhou Siyao Pharmaceuticals Co., Ltd.

Valsartan
Manufacturer	Second PHARMA Co., Ltd.

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Registered Holders

Ningbo Menovo Pharmaceutical Co., Ltd.

China
Active
BIOPHORE INDIA PHARMACEUTICALS PVT LTD

United States
Active
SECOND PHARMA CO LTD

United States
Active

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