Valsartan

Generic Name
Valsartan
Brand Names
Dafiro, Diovan, Diovan Hct, Entresto, Exforge, Exforge Hct
Drug Type
Small Molecule
Chemical Formula
C24H29N5O3
CAS Number
137862-53-4
Unique Ingredient Identifier
80M03YXJ7I
Background

Valsartan belongs to the angiotensin II receptor blocker (ARB) family of drugs, which also includes telmisartan, candesartan, losartan, olmesartan, and irbesartan. ARBs selectively bind to angiotensin receptor 1 (AT1) and prevent the protein angiotensin II from binding and exerting its hypertensive effects, which include vasoconstriction, stimulation and synthesis of aldosterone and ADH, cardiac stimulation, and renal reabsorption of sodium, among others. Overall, valsartan's physiologic effects lead to reduced blood pressure, lower aldosterone levels, reduced cardiac activity, and increased excretion of sodium.

Valsartan also affects the renin-angiotensin aldosterone system (RAAS), which plays an important role in hemostasis and regulation of kidney, vascular, and cardiac functions. Pharmacological blockade of RAAS via AT1 receptor blockade inhibits negative regulatory feedback within RAAS, which is a contributing factor to the pathogenesis and progression of cardiovascular disease, heart failure, and renal disease. In particular, heart failure is associated with chronic activation of RAAS, leading to inappropriate fluid retention, vasoconstriction, and ultimately a further decline in left ventricular function. ARBs have been shown to have a protective effect on the heart by improving cardiac function, reducing afterload, increasing cardiac output and preventing ventricular hypertrophy and remodelling.

By comparison, the angiotensin-converting enzyme inhibitor (ACEI) class of medications (which includes drugs such as ramipril, lisinopril, and perindopril) inhibit the conversion of angiotensin I to angiotensin II through inhibition of the ACE enzyme. However, this does not prevent the formation of all angiotensin II within the body. The angiotensin II receptor blocker (ARB) family of drugs unique in that it blocks all angiotensin II activity, regardless of where or how it was synthesized.

Valsartan is commonly used for the management of hypertension, heart failure, and Type 2 Diabetes-associated nephropathy, particularly in patients who are unable to tolerate ACE inhibitors. ARBs such as valsartan have been shown in a number of large-scale clinical outcomes trials to improve cardiovascular outcomes including reducing risk of myocardial infarction, stroke, the progression of heart failure, and hospitalization. Valsartan also slows the progression of diabetic nephropathy due to its renoprotective effects. Improvements in chronic kidney disease with valsartan include both clinically and statistically significant decreases in urinary albumin and protein excretion in patients diagnosed with type 2 diabetes and in nondiabetic patients diagnosed with chronic kidney disease.

Valsartan was initially approved in 1996 in Europe for the treatment of hypertension in adults. Shortly after, in 1997, this drug was approved in the United States. Valsartan is generally well-tolerated with a side-effect profile superior to that of other antihypertensive drugs.

Indication

Valsartan is indicated for the treatment of hypertension to reduce the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. It is also indicated for the treatment of heart failure (NYHA class II-IV) and for left ventricular dysfunction or failure after myocardial infarction when the use of an angiotensin-converting enzyme inhibitor (ACEI) is not appropriate.

It is also used in combination with sacubitril.

Associated Conditions
Cardiovascular Mortality, Diabetic Nephropathy, Heart Failure, Hypertension, Moderate Essential Hypertension, Chronic heart failure with reduced ejection fraction (NYHA Class II), Chronic heart failure with reduced ejection fraction (NYHA Class III), Chronic heart failure with reduced ejection fraction (NYHA Class IV), Hospitalization due to cardiac failure
Associated Therapies
-

Pharmacokinetic Drug Interaction Study of Dapagliflozin and Valsartan or Simvastatin in Healthy Subjects

First Posted Date
2009-02-09
Last Posted Date
2016-10-17
Lead Sponsor
AstraZeneca
Target Recruit Count
24
Registration Number
NCT00839683
Locations
🇺🇸

Mds Pharma Services (Us) Inc., Neptune, New Jersey, United States

Reducing the Overall Risk Level in Patients Suffering From Metabolic Syndrome

First Posted Date
2009-01-13
Last Posted Date
2017-03-01
Lead Sponsor
Novartis
Target Recruit Count
144
Registration Number
NCT00821574

Efficacy and Safety of Aliskiren in Patients With Mild to Moderate Hypertension During Exercise

First Posted Date
2009-01-09
Last Posted Date
2011-06-28
Lead Sponsor
Novartis
Target Recruit Count
68
Registration Number
NCT00819767
Locations
🇬🇧

Investigative Site, Leicester, United Kingdom

8 Weeks Study to Evaluate the Efficacy and Safety of Valsartan in Combination With Aliskiren Compared to Valsartan Alone in Patients With Stage 2 Hypertension

First Posted Date
2008-12-17
Last Posted Date
2011-05-02
Lead Sponsor
Novartis
Target Recruit Count
451
Registration Number
NCT00809926
Locations
🇺🇸

Sites in USA, East Hanover, New Jersey, United States

Kagoshima Collaborate Trial in Metabolic Syndrome (KACT Study)

Phase 4
Conditions
Interventions
First Posted Date
2008-11-14
Last Posted Date
2010-06-03
Lead Sponsor
Kagoshima University
Target Recruit Count
250
Registration Number
NCT00790946
Locations
🇯🇵

Chuwa Tei,MD,FACC,FAHA, Kagoshima, Japan

Regression of Fatty Heart by Valsartan Therapy

First Posted Date
2008-09-03
Last Posted Date
2019-01-17
Lead Sponsor
University of Texas Southwestern Medical Center
Registration Number
NCT00745953
Locations
🇺🇸

University of Texas Southwestern Medical Center, Dallas, Texas, United States

Left Ventricular Hypertrophy Reduction With Statins in Hypertensives Patients (MK0653A-168)

First Posted Date
2008-08-21
Last Posted Date
2013-08-26
Lead Sponsor
Fundación Lindavista del Corazón AC
Target Recruit Count
12
Registration Number
NCT00738972

Ocsaar and CYP2C9 Ploymorphism, Is There a Connection Between Pharmacokinetics, Pharmacodynamics and Pharmacogenetics?

Not Applicable
Conditions
Interventions
First Posted Date
2008-08-12
Last Posted Date
2008-08-12
Lead Sponsor
Assaf-Harofeh Medical Center
Target Recruit Count
30
Registration Number
NCT00732966

Study of Inflammation and Oxidative Stress in Persons Undergoing Dialysis

First Posted Date
2008-08-11
Last Posted Date
2013-07-02
Lead Sponsor
Vanderbilt University
Target Recruit Count
19
Registration Number
NCT00732069
Locations
🇺🇸

Vanderbilt University Medical Center, Nashville, Tennessee, United States

Renal Protective Effects of Renin Angiotensin System (RAS) Inhibitor in Peritoneal Dialysis Patients

First Posted Date
2008-07-24
Last Posted Date
2015-05-20
Lead Sponsor
Sun Yat-sen University
Target Recruit Count
200
Registration Number
NCT00721773
Locations
🇨🇳

The 1st Affiliated Hospital, Sun Yet-sen University, GuangZhou, Guangdong, China

© Copyright 2024. All Rights Reserved by MedPath