Valsartan

Valsartan
Clinical data


Trade names	Diovan
AHFS/Drugs.com	Monograph
MedlinePlus	a697015
License data	US FDA: Valsartan
Pregnancy category	US: D (Evidence of risk)
Routes of administration	oral
ATC code	C09CA03 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	25%
Protein binding	95%
Biological half-life	6 hours
Excretion	Renal 30%, biliary 70%
Identifiers
IUPAC name (S)-3-methyl-2-(N-{[2'-(2H-1,2,3,4-tetrazol-5-yl)biphenyl-4-yl]methyl}pentanamido)butanoic acid
CAS Number	137862-53-4^Y
PubChem CID	60846
IUPHAR/BPS	3937 tritiated: 593
DrugBank	DB00177^Y
ChemSpider	54833^Y
UNII	80M03YXJ7I
KEGG	D00400^Y
ChEBI	CHEBI:9927^Y
ChEMBL	CHEMBL1069^Y
ECHA InfoCard	100.113.097
Chemical and physical data
Formula	C₂₄H₂₉N₅O₃
Molar mass	435.519 g/mol
3D model (Jmol)	Interactive image
SMILES O=C(O)[C@@H](N(C(=O)CCCC)Cc3ccc(c1ccccc1c2nnnn2)cc3)C(C)C
InChI InChI=1S/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m0/s1^Y Key:ACWBQPMHZXGDFX-QFIPXVFZSA-N^Y

Valsartan (trade name Diovan) is an angiotensin II receptor antagonist (commonly called an ARB, or angiotensin receptor blocker), that is selective for the type I (AT₁) angiotensin receptor. Valsartan is mainly used for treatment of high blood pressure, congestive heart failure, and to increase the chances of living longer after a heart attack.

Valsartan is used to treat high blood pressure, congestive heart failure, and to reduce death for people with left ventricular dysfunction after having had a heart attack.

There is contradictory evidence with regard to treating people with heart failure with a combination of an angiotensin receptor blocker like valsartan and an angiotensin-converting enzyme inhibitor, with two major clinical trials (CHARM-additive and ValHeFt) showing a reduction in death, and two others (VALIANT and ONTARGET) showing no benefits, and more adverse effects including heart attacks.

In people with type II diabetes and high blood pressure or albumin in the urine, valsartan is used to slow the worsening and the development end-stage renal disease.

The packaging for valsartan includes a warning stating the drug should not be used with the renin inhibitor aliskiren in people with diabetes mellitus. It also states the drug should not be used in people with kidney disease.

Valsartan falls in FDA pregnancy category D and includes a black box warning for fetal toxicity. Discontinuation of these agents is recommended immediately after detection of pregnancy and an alternative medication should be started. The US labeling makes no recommendation regarding continuation or discontinuation of valsartan for breast-feeding mothers. The Canadian labeling does not recommend use by nursing women.

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Wikipedia