Valsartan

Brand Names: Valsartan

Drug Class: Angiotensin 2 Receptor Blocker

Overview

11 DESCRIPTION Valsartan tablets, USP are a nonpeptide, orally active, and specific angiotensin II receptor blocker acting on the AT 1 receptor subtype. Valsartan is chemically described as N -(1-oxopentyl)- N -[[2′-(1 H -tetrazol-5-yl) [1,1′-biphenyl]-4-yl]methyl]-L-valine. Its molecular formula is C 24 H 29 N 5 O 3 , its molecular weight is 435.

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Valsartan tablets blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis.

Indications

  • 1 INDICATIONS AND USAGE Valsartan tablets are an angiotensin II receptor blocker (ARB) indicated for: Hypertension ,to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions ( 1.1 ) Heart failure (NYHA class II-IV); valsartan tablets significantly reduced hospitalization for heart failure ( 1.2 ) Post-myocardial infarction ; for the reduction of cardiovascular mortality in clinically stable patients with left ventricular failure or left ventricular dysfunction following myocardial infarction ( 1.

Common Doses

  • 160 mg
  • 320 mg
  • 1 mg
  • 40 mg

Dosage

2 DOSAGE AND ADMINISTRATION Indication Starting Dose Dose Range * Adult Hypertension ( 2.2 ) 80 or 160 mg once daily 80-320 mg once daily 6-16 years ( 2.3 ) 1mg/kg once daily (up to 40 mg total) 1-4mg/kg once daily (up to 160 mg total) Heart Failure ( 2.4 ) 40 mg twice daily 40-160 mg twice daily Post-Myocardial Infarction ( 2.5 ) 20 mg twice daily 20-160 mg twice daily * As tolerated by patient 2.1 Important Dosage and Preparation Information Valsartan tablets and oral suspension are not substitutable on a milligram-per-milligram basis.

Black Box Warning

WARNING: FETAL TOXICITY When pregnancy is detected, discontinue valsartan tablets as soon as possible. ( 5.1 ) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. ( 5.1 ) WARNING: FETAL TOXICITY See full prescribing information for complete boxed warning. When pregnancy is detected, discontinue valsartan tablets as soon as possible. ( 5.1 ) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. ( 5.1 )

Contraindications

  • 4 CONTRAINDICATIONS Do not use in patients with known hypersensitivity to any component. Do not coadminister aliskiren with valsartan tablets in patients with diabetes [See Drug Interactions (7.3) ]. Known hypersensitivity to any component. Do not coadminister aliskiren with valsartan tablets in patients with diabetes ( 4 )

Side Effects

  • 6 ADVERSE REACTIONS Hypertension: Most common adverse reactions are headache, dizziness, viral infection, fatigue and abdominal pain ( 6.1 ) Heart Failure :Most common adverse reactions are dizziness, hypotension, diarrhea, arthralgia, back pain, fatigue and hyperkalemia ( 6.1 ) Post-Myocardial Infarction : Most common adverse reactions which caused patients to discontinue therapy are hypotension, cough and increased blood creatinine ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact RK Pharma Inc at 1-844-757-4276 (1-844-RKPHARMA) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.

Interactions

  • 7 DRUG INTERACTIONS Potassium-sparing diuretics, potassium supplements or salt substitutes may lead to increases in serum potassium, and in heart failure patients, increases in serum creatinine ( 7.1 ) NSAID use may lead to increased risk of renal impairment and loss of antihypertensive effect ( 7.2 ) Dual inhibition of the renin-angiotensin system : Increased risk of renal impairment, hypotension, and hyperkalemia ( 7.3 ) Lithium : Increases in serum lithium level and lithium toxicity ( 7.4 ) 7.