Valsartan

From Wikipedia, the free encyclopedia
  (Redirected from Diovan)
Jump to: navigation, search
Valsartan
Valsartan.svg
Valsartan ball-and-stick.png
Systematic (IUPAC) name
(S)-3-methyl-2-(N-{[2'-(2H-1,2,3,4-tetrazol-5-yl)biphenyl-4-yl]methyl}pentanamido)butanoic acid
Clinical data
Trade names Diovan
AHFS/Drugs.com monograph
MedlinePlus a697015
Licence data US FDA:link
Pregnancy cat.
Legal status
Routes oral
Pharmacokinetic data
Bioavailability 25%
Protein binding 95%
Half-life 6 hours
Excretion Renal 30%, biliary 70%
Identifiers
CAS number 137862-53-4 YesY
ATC code C09CA03
PubChem CID 60846
IUPHAR ligand 3937
DrugBank DB00177
ChemSpider 54833 YesY
UNII 80M03YXJ7I YesY
KEGG D00400 YesY
ChEBI CHEBI:9927 YesY
ChEMBL CHEMBL1069 YesY
Chemical data
Formula C24H29N5O3 
Mol. mass 435.519 g/mol
 YesY (what is this?)  (verify)

Valsartan (trade name Diovan) is an angiotensin II receptor antagonist (more commonly called an ARB, or angiotensin receptor blocker), with particularly high affinity for the type I (AT1) angiotensin receptor.

Medical uses[edit]

Valsartan is used to treat of high blood pressure, congestive heart failure, and to reduce death for people with left ventricular dysfunction after having had a heart attack.[1][2]

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.[1]

Contraindications[edit]

Valsartan should not be given with aliskiren to people with diabetes.[2]

Valsartan falls in FDA pregnancy category D with a black box warning for fetal toxicity.[2] Discontinuation of these agents is recommended immediately after detection of pregnancy and an alternative medication should be started.[2] The US labeling makes no recommendation regarding continuation or discontinuation of valsartan for breast-feeding mothers.[2] The Canadian labeling does not recommend use by nursing women.[3]

Side effects[edit]

Interactions[edit]

The US prescribing information lists the following drug interactions for valsartan:

  • Other inhibitors of the renin-angiotensin system may increase the risks of low blood pressure, kidney problems, and hyperkalemia
  • Potassium sparing diuretics, potassium supplements, salt substitutes containing potassium may increase the risk of hyperkalemia.
  • NSAIDs may increase the risk of kidney problems and may interfere with blood pressure-lowering effects.
  • Valsartan may increase the concentration of lithium.[2]

Mechanism of action[edit]

Valsartan blocks the actions of angiotensin II, which include constricting blood vessels and activating aldosterone, to reduce blood pressure. [5]

Economics[edit]

In 2005, valsartan was prescribed more than 12 million times in the United States[citation needed], and global sales were around $6.1 billion in 2010.[6] The patents for valsartan and valsartan/hydrochlorothiazide expired in September 2012.[7][8]

Research[edit]

In patients with impaired glucose tolerance, valsartan may decrease the incidence of developing diabetes mellitus type 2. However, the absolute risk reduction is small (less than 1 percent per year) and diet, exercise or other drugs, may be more protective. In the same study, no reduction in the rate of cardiovascular events (including death) was shown.[9]

A prospective study released in 2010, based on 819,491 cases in U.S. Department of Veterans Affairs database from 2002 to 2006, demonstrated a significant reduction in the incidence and progression of Alzheimer's disease and dementia.[10]

See also[edit]

References[edit]

  1. ^ a b Randa Hilal-Dandan "Renin and Angiotensin". Chapter 26 in Goodman & Gilman's The Pharmacological Basis of Therapeutics, 12e, eds. Laurence L. Brunton, Bruce A. Chabner, Björn C. Knollmann. The McGraw-Hill Companies, Inc. 2011. ISBN 978-0-07-162442-8
  2. ^ a b c d e f "Diovan prescribing information". Novartis. 
  3. ^ Lexi-Drugs Online. "Valsartan". Lexi-Comp. 
  4. ^ Haberfeld, H, ed. (2009). Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X. 
  5. ^ Marks JW (2007-02-15). "Valsartan, Diovan". MedicineNet. Retrieved 2010-03-04. 
  6. ^ "Novartis Annual Report". Novartis. 2010. Retrieved June 15, 2011.
  7. ^ Philip Moeller (April 29, 2011). "Blockbuster Drugs That Will Go Generic Soon". U.S.News & World Report. 
  8. ^ Eva Von Schaper (August 5, 2011). "Novartis's Jimenez Has Blockbuster Plans For Diovan After Patent Expires". Bloomberg. 
  9. ^ McMurray JJ, Holman RR, Haffner SM, et al. (April 2010). "Effect of valsartan on the incidence of diabetes and cardiovascular events" (PDF). The New England Journal of Medicine 362 (16): 1477–90. doi:10.1056/NEJMoa1001121. PMID 20228403. 
  10. ^ Li NC, Lee A, Whitmer RA, et al. (January 2010). "Use of angiotensin receptor blockers and risk of dementia in a predominantly male population: prospective cohort analysis". BMJ 340: b5465. doi:10.1136/bmj.b5465. PMC 2806632. PMID 20068258. 

External links[edit]