Valsartan

Valsartan
Valsartan
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. D
Legal status ℞ Prescription only
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
DrugBank APRD00133
ChemSpider 54833 YesY
UNII 80M03YXJ7I YesY
KEGG D00400 N
ChEBI CHEBI:9927 N
ChEMBL CHEMBL1069 YesY
Chemical data
Formula C24H29N5O3 
Mol. mass 435.519 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

Valsartan (Angiotan) 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. By blocking the action of angiotensin, valsartan dilates blood vessels and reduces blood pressure.[1] In the U.S., valsartan is indicated for treatment of high blood pressure, congestive heart failure (CHF), or post-myocardial infarction (MI).[2] In 2005, Angiotan was prescribed more than 12 million times in the United States and global sales were approximately $6.1 billion in 2010.[3]

A study released in 2010, based on 819,491 cases in U.S. Veteran's Administration database from 2002-2006, demonstrated a significant reduction in the incidence and progression of Alzheimer’s disease and dementia. [[2]]. An earlier study released by the Journal of Clinical Investigation in 2007 found some efficacy in the use of valsartan in the treatment and prevention of Alzheimer's disease (in a mouse model).[4]

Contents

Administration

Oral tablets, containing 40 mg (scored), 80 mg, 160 mg or 320 mg of valsartan. Usual dosage ranges from 40–320 mg daily.

In some markets available as a hard gelatin capsule, containing 40 mg, 80 mg, or 160 mg of valsartan.

Diovan HCT contains a combination of valsartan and hydrochlorothiazide but, unlike Diovan, is only indicated for hypertension, not for CHF or post-MI.[citation needed] Diovan HCT is available in oral tablets, containing (valsartan/HCTZ mg) 80/12.5, 160/12.5, 160/25, 320/12.5, and 320/25.

Myocardial infarction controversy

Whether angiotensin receptor blockers may or may not increase the risk of myocardial infarction (heart attack) was announced in BMJ[5] and was debated in 2006 in the medical journal of the American Heart Association.[6][7] To date[when?], there is no consensus on whether ARBs have a tendency to increase MI, but there is also no substantive evidence to indicate that ARBs are able to reduce MI.

In the VALUE trial, the angiotensin II receptor blocker valsartan produced a statistically significant 19% (p=0.02) relative increase in the prespecified secondary end point of myocardial infarction (fatal and non-fatal) compared with amlodipine.[8]

The CHARM-alternative trial showed a significant +52% (p=0.025) increase in myocardial infarction with candesartan (versus placebo) despite a reduction in blood pressure.[9]

Indeed, as a consequence of AT1 blockade, ARBs increase Angiotensin II levels several-fold above baseline by uncoupling a negative-feedback loop. Increased levels of circulating Angiotensin II result in unopposed stimulation of the AT2 receptors, which are, in addition upregulated. Unfortunately, recent data suggest that AT2 receptor stimulation may be less beneficial than previously proposed and may even be harmful under certain circumstances through mediation of growth promotion, fibrosis, and hypertrophy, as well as proatherogenic and proinflammatory effects.[10][11][12]

Diabetes

In patients with impaired glucose tolerance, valsartan may decrease the incidence of developing type 2 diabetes mellitus.[13] However, the absolute risk reduction is small (less than 1% 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.

Side effects

  • Most commonly, headache and dizziness.
  • Sensitivity to sun light and bright artificial light.(needs citation)
  • Significant weight gain and fatigue.(needs citation)

There is a case report of a stillbirth in which valsartan is implicated.[14]

Brands

In the US, valsartan is marketed by Novartis under the trade name Diovan. In Pakistan, it is marketed by Efroze under the trade name Angiotan. In India, it is marketed by Cipla under the trade name Valtan and by Torrent Pharmaceuticals under the trade name Valzaar. In Egypt it is marketed by Novartis under the name of Tareg.

See also

References

  1. ^ Marks JW (2007-02-15). "Valsartan". MedicineNet.com. MedicineNet, Inc. http://www.medicinenet.com/valsartan/article.htm. Retrieved 2010-03-04. 
  2. ^ "Diovan prescribing information". Novartis. http://www.pharma.us.novartis.com/product/pi/pdf/diovan.pdf. 
  3. ^ Novartis International AG @ul[1], accessed June 15, 2011.
  4. ^ Wang J, Ho L, Chen L, et al. (November 2007). "Valsartan lowers brain β-amyloid protein levels and improves spatial learning in a mouse model of Alzheimer disease". J. Clin. Invest. 117 (11): 3393–402. doi:10.1172/JCI31547. PMC 2040315. PMID 17965777. http://content.the-jci.org/articles/view/31547. Retrieved 2009-11-11. 
  5. ^ Verma S, Strauss M (November 2004). "Angiotensin receptor blockers and myocardial infarction: These drugs may increase myocardial infarction—and patients may need to be told". BMJ 329 (7477): 1248–9. doi:10.1136/bmj.329.7477.1248. PMC 534428. PMID 15564232. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=534428. 
  6. ^ Strauss MH, Hall AS (August 2006). "Angiotensin receptor blockers may increase risk of myocardial infarction: unraveling the ARB-MI paradox". Circulation 114 (8): 838–54. doi:10.1161/CIRCULATIONAHA.105.594986. PMID 16923768. 
  7. ^ Tsuyuki RT, McDonald MA (August 2006). "Angiotensin receptor blockers do not increase risk of myocardial infarction". Circulation 114 (8): 855–60. doi:10.1161/CIRCULATIONAHA.105.594978. PMID 16923769. 
  8. ^ Julius S, Kjeldsen SE, Weber M, et al. (June 2004). "Outcomes in hypertensive patients at high cardiovascular risk treated with regimens based on valsartan or amlodipine: the VALUE randomised trial". The Lancet 363 (9426): 2022–31. doi:10.1016/S0140-6736(04)16451-9. PMID 15207952. 
  9. ^ Granger CB, McMurray JJ, Yusuf S, et al. (September 2003). "Effects of candesartan in patients with chronic heart failure and reduced left-ventricular systolic function intolerant to angiotensin-converting-enzyme inhibitors: the CHARM-Alternative trial". The Lancet 362 (9386): 772–6. doi:10.1016/S0140-6736(03)14284-5. PMID 13678870. 
  10. ^ Levy BI (September 2005). "How to explain the differences between renin angiotensin system modulators". Am. J. Hypertens. 18 (9 Pt 2): 134S–141S. doi:10.1016/j.amjhyper.2005.05.005. PMID 16125050. 
  11. ^ Levy BI (January 2004). "Can angiotensin II type 2 receptors have deleterious effects in cardiovascular disease? Implications for therapeutic blockade of the renin-angiotensin system". Circulation 109 (1): 8–13. doi:10.1161/01.CIR.0000096609.73772.C5. PMID 14707017. 
  12. ^ Reudelhuber TL (December 2005). "The continuing saga of the AT2 receptor: a case of the good, the bad, and the innocuous". Hypertension 46 (6): 1261–2. doi:10.1161/01.HYP.0000193498.07087.83. PMID 16286568. 
  13. ^ McMurray JJ, Holman RR, Haffner SM, et al. (April 2010). "Effect of valsartan on the incidence of diabetes and cardiovascular events". The New England Journal of Medicine 362 (16): 1477–90. doi:10.1056/NEJMoa1001121. PMID 20228403. 
  14. ^ Briggs GG, Nageotte MP (2001). "Fatal fetal outcome with the combined use of valsartan and atenolol". The Annals of Pharmacotherapy 35 (7–8): 859–61. doi:10.1345/aph.1A013. PMID 11485133. 

External links

v · d · eAntihypertensives: agents acting on the renin-angiotensin system (C09)
ACE inhibitors
("-pril")
AIIRAs/
("-sartan")
Azilsartan • Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan§ • Telmisartan (+HCT) • Valsartan (+HCT)
Renin inhibitors/
("-kiren")
Aliskiren (+amlodipine) • Remikiren§
#WHO-EM. ‡Withdrawn from market. Clinical trials: †Phase III. §Never to phase III

M: VAS

anat(a:h/u/t/a/l,v:h/u/t/a/l)/phys/devp/cell/prot

noco/syva/cong/lyvd/tumr, sysi/epon, injr

proc, drug(C2s+n/3/4/5/7/8/9)

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