|Systematic (IUPAC) name|
|Excretion||Renal 30%, biliary 70%|
|(what is this?)|
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.
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.
Valsartan falls in FDA pregnancy category D with 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.
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.
Mechanism of action
Valsartan blocks the actions of angiotensin II, which include constricting blood vessels and activating aldosterone, to reduce blood pressure.
In 2005, valsartan was prescribed more than 12 million times in the United States, and global sales were around $6.1 billion in 2010. The patents for valsartan and valsartan/hydrochlorothiazide expired in September 2012.
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.
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.
- Angiotensin II receptor antagonist
- Discovery and development of angiotensin receptor blockers
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- PubMed Valsartan
- Diovan official website Novartis
- U.S. Valsartan National Library of Medicine: Drug Information Portal
- Diovan Prescribing information Novartis
- Diovan HCT Prescribing information Novartis