Pharmacology · Angiotensin II receptor blockers (ARBs)

Valsartan !

An angiotensin II receptor blocker (ARB). Used for high blood pressure, heart failure and after a heart attack, without the ACE-inhibitor cough.

Updated 2026-11-01

Class: Angiotensin II receptor blockers (ARBs)
Receptor: Angiotensin II type 1 (AT1) receptor
ATC code: C09CA03

Angiotensin II type 1 (AT1) receptorValsartan

The figure shows olmesartan, another ARB, in the same binding pocket of the human AT1 receptor; no structure with valsartan bound is available.

Target in 3D: Angiotensin II type 1 (AT1) receptor. PDB structure 4ZUD (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Valsartan blocks the AT1 receptor, so angiotensin II cannot constrict arterioles, release aldosterone or drive remodelling of the heart and vessels. Blood pressure falls and less sodium is retained. ACE keeps working, so bradykinin does not build up and cough is rare.

Valsartan blocks the AT1 receptor of angiotensin II
Arterioles dilate and aldosterone falls
Blood pressure falls; bradykinin is not raised

Pharmacokinetics

Absorption: Low and variable oral bioavailability
Metabolism: Barely metabolised
Elimination: Mainly in bile and faeces
Half-life: About 6 hours

Indications

High blood pressure Arterial hypertension →
Heart failure Heart failure →
Left ventricular dysfunction after myocardial infarction Myocardial Infarction (Heart Attack) →

Adverse effects

Common

Dizziness and hypotension
Hyperkalaemia
Rise in creatinine
Fatigue

Contraindications

Pregnancy
Hypersensitivity to the drug
Use with aliskiren in people with diabetes

Key interactions

Potassium-sparing diuretics, potassium supplements or salt substitutes: Hyperkalaemia
NSAIDs, including COX-2 inhibitors: Weaker effect and risk of kidney injury
Lithium: Higher lithium levels and toxicity

What is monitored

Blood pressure
Potassium and creatinine

Administration and safety

Given by mouth, with or without food
Valsartan alone and the sacubitril/valsartan combination are different products and are not swapped

Nursing care

Check blood pressure, potassium and creatinine when starting and after changes
Watch for dizziness, especially in patients on diuretics
Ask women of childbearing age about pregnancy plans
Teach the patient to avoid potassium salt substitutes unless prescribed

Pregnancy and breastfeeding

Contraindicated: drugs acting on the renin-angiotensin system can injure and kill the developing fetus; it is stopped as soon as pregnancy is detected.

Test yourself

Think of the answer, then tap the question to see it.

Why do ARBs like valsartan rarely cause cough?

They block the AT1 receptor and leave ACE working, so bradykinin is not raised.

Which electrolyte is checked after starting valsartan?

Potassium, because lower aldosterone reduces potassium excretion.

Which ARB is part of the ARNI combination used in heart failure?

Valsartan, combined with the neprilysin inhibitor sacubitril.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - VALSARTAN tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.