Valsartan
Systematic (IUPAC) name
3-methyl-2- [pentanoyl-[ [4-[2-(2H-tetrazol-5-yl) phenyl] phenyl] methyl]amino] -butanoic acid
Identifiers
CAS number	137862-53-4
ATC code	C09CA03
PubChem	60846
DrugBank	APRD00133
Chemical data
Formula	C24H29N5O3
Mol. mass	435. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 519 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	25%
Protein binding	95%
Metabolism	?
Half life	6 hours
Excretion	Renal 30%, biliary 70%
Therapeutic considerations
Pregnancy cat.	D
Legal status	℞ Prescription only
Routes	oral

Valsartan is an angiotensin II receptor antagonist (more commonly called an "ARB", which stands for Angiotensin Receptor Blocker), acting on the AT₁ subtype. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles A bile duct is any of a number of long tube-like structures that carry Bile. The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route Angiotensin II receptor antagonists, also known as angiotensin receptor blockers (ARBs AT1-receptor antagonists or sartans, are a group of The angiotensin receptors are a class of G protein-coupled receptors with Angiotensins as ligands They are important in the Renin-angiotensin system In the U. S. , valsartan is indicated for treatment of high blood pressure, of congestive heart failure (CHF), and post-myocardial infarction (MI). Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated Heart failure is a Cardiac condition that occurs when a problem with the structure or function of the Heart impairs its ability to supply Myocardial infarction ( MI or AMI for acute myocardial infarction) also known as a heart attack, occurs when the blood supply It is marketed by Novartis under the trade name Diovan. Novartis International AG is a multinational Pharmaceutical company based in Basel Switzerland that manufactures drugs such as Clozapine In India, it is marketed by CIPLA under the trade name Valtan and by Torrent Pharmaceuticals under the trade name Valzaar. Cipla, originally founded as The Chemical Industrial & Pharmaceutical Laboratories is a prominent Indian Pharmaceutical company, best-known outside Torrent Pharmaceuticals Ltd is the flagship company of the Torrent Group. In 2005, Diovan was prescribed more than 12 million times in the United States. The United States of America —commonly referred to as the A 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 although such use is considered to be highly experimental. The Journal of Clinical Investigation (JCI or J Clin Invest) is a leading biomedical journal, with a 2007 Impact factor of 16 ^[1] According to the Diovan Package Insert (PI), Diovan loses 40% of its efficacy when ingested with food.

Contents 1 Administration 2 Myocardial Infarction: the controversy 3 Side effects 4 References 5 External links

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 40mg, 80mg, or 160mg 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. Hydrochlorothiazide, sometimes abbreviated HCT, HCTZ, or HZT is a popular Diuretic drug of the Thiazide class that acts by inhibiting

Myocardial Infarction: the controversy

Whether Angiotensin II Receptor Blockers may increase or not the risk of Myocardial Infarction was announced in the BMJ ^[2] and was more recently debated in the medical journal of the American Heart Association: Circulation ^{[3] [4]}. Myocardial infarction ( MI or AMI for acute myocardial infarction) also known as a heart attack, occurs when the blood supply The American Heart Association (AHA is a Non-profit organization in the United States that fosters appropriate To date, 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 ^[5]. Amlodipine (as Besylate, Mesylate or Maleate) is a long-acting Calcium channel blocker (dihydropyridine used as an Anti-hypertensive

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 ^[6]. Candesartan ( rINN) (ˌkændɨˈsɑrtən is an Angiotensin II receptor antagonist used mainly for the treatment of Hypertension.

Indeed, as a consequence of AT1 blockade, ARBs increase Angiotensin II levels several-fold above baseline by uncoupling a negative-feedback loop. Angiotensin causes blood vessels to constrict and drives blood pressure up 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 ^{[7] [8] [9]}.

Side effects

Most commonly, headache and dizziness. A headache ( cephalalgia in medical terminology is a condition of pain in the Head; sometimes Neck or upper back pain may also be interpreted Many different terms are often used to describe what is collectively known as dizziness.

References

External links

• PubMed: Valsartan
• Official Diovan Site

PubMed is a free search engine for accessing the MEDLINE database of citations and abstracts of biomedical research articles

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