Valsartan

Angiotensin II receptor blockers (ARBs)

ATC code: C09CA03 (Valsartan)

Mechanism of action

Selective AT1 angiotensin II receptor antagonist. Blocks vasoconstriction, aldosterone secretion, and proliferative effects of angiotensin II. Does not cause dry cough, unlike ACE inhibitors, because it does not affect bradykinin degradation. Half-life is about 6 hours, but the clinical effect lasts 24 hours.

Indications

Hypertension

First line

First-line antihypertensive. Starting dose 80 mg once daily, maximum 320 mg. Prescribed as an ACE inhibitor alternative or when ACEi is not tolerated (cough). Frequently included in fixed-dose combinations with amlodipine and/or hydrochlorothiazide. Antihypertensive effect develops over 2-4 weeks.

Sources

Heart failure

Second line

Valsartan is a proven ACE inhibitor alternative in HFrEF. The Val-HeFT trial showed a 27% reduction in hospitalizations when valsartan was added to background therapy. Sacubitril/valsartan (Entresto) is a separate drug that outperformed enalapril in PARADIGM-HF and is now preferred in HFrEF.

Prescribed when ACE inhibitors are not tolerated. Per 2021, sacubitril/valsartan (Entresto) is preferred over valsartan monotherapy in HFrEF.

Sources

N Engl J Med: A randomized trial of the angiotensin-receptor blocker valsartan in chronic heart failure. (2001)

Post-myocardial infarction heart failure

Second line

Valsartan is an alternative to captopril in post-MI heart failure. The VALIANT trial (over 14,000 patients) showed that valsartan 160 mg twice daily was as effective as captopril for mortality and cardiovascular events. Prescribed for patients who do not tolerate ACE inhibitors.

Sources

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

Anti-aging and longevity

Not recommended

Valsartan is an angiotensin II receptor blocker. It is prescribed for hypertension, heart failure, and after myocardial infarction ( 2023, SEH-LELHA, 2017). In anti-aging regimens, valsartan is given to healthy normotensives for general vessel protection. In people with normal blood pressure, no clinical studies of prophylactic use exist. The drug can cause dizziness, hyperkalemia, angioedema in predisposed people, and teratogenicity. If valsartan was prescribed to a healthy person, consider seeking a second opinion.

Sources

Practical notes

Timing and administration

Take once daily at any time, with or without food. In heart failure, titration starts at 40 mg twice daily, increased to 160 mg twice daily. In hypertension, 80-320 mg once daily. Full antihypertensive effect in 2-4 weeks.

Monitoring

Check potassium and creatinine 1-2 weeks after initiation and each dose increase, same as other ARBs and ACE inhibitors. A creatinine rise up to 30% is acceptable. Larger rises warrant investigation for renal artery stenosis, hypovolemia, or concurrent NSAID use. Absence of cough is the key clinical differentiator from ACE inhibitors.

Drug–drug interactions

6 pairs found. Sorted from critical to minor.

Major

Captopril

ACE inhibitor

Mechanism

Dual RAAS blockade (ACE-I + ARB). Additive hyperkalaemia, hypotension, and acute kidney injury risk without added benefit.

Symptoms

Weakness, postural dizziness, syncope. Reduced urine output, rising creatinine. Weakness and paraesthesia from hyperkalaemia.

Management

The combination is not prescribed. Choose one: ACE-I if tolerated, ARB if there is a dry cough or intolerance.

Sources

KDIGO: KDIGO 2024 Clinical Practice Guideline for the Evaluation and Management of CKD (2024)

Pair details →

Major

Co-trimoxazole

Sulfonamide-trimethoprim combination

Mechanism

Trimethoprim blocks collecting duct sodium channels (amiloride-like mechanism) and reduces potassium secretion. Valsartan (ARB) additionally retains potassium through aldosterone suppression.

Symptoms

Muscle weakness, paraesthesia in the limbs, slowed pulse, arrhythmias. ECG shows peaked T waves and widened QRS. Severe cases progress to cardiac arrest. Symptoms typically appear within 1–2 weeks of starting the combination.

Management

During co-trimoxazole therapy, check potassium 3–5 days after start. In older patients and chronic kidney disease, prefer alternative antibiotics: nitrofurantoin or fosfomycin.

Sources

PubMed: Trimethoprim-sulfamethoxazole and risk of sudden death among patients taking spironolactone or ACE inhibitors (2014)

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Major

Enalapril

Angiotensin-converting enzyme inhibitors (ACEi)

Mechanism

Dual RAAS blockade (ACE-I + ARB). Proven in ONTARGET and VA NEPHRON-D trials: increased hyperkalaemia, hypotension, and acute kidney injury without cardioprotection.

Symptoms

Muscle weakness, paraesthesia, slowed pulse, arrhythmias. ECG: peaked T waves, widened QRS. Severe cases progress to cardiac arrest.

Management

The combination is not prescribed. Choose one: ACE-I (enalapril) if tolerated, ARB (valsartan) if there is a dry cough or intolerance.

Sources

KDIGO: KDIGO 2024 Clinical Practice Guideline for the Evaluation and Management of CKD (2024)

Pair details →

Major

Spironolactone

Potassium-sparing diuretics (mineralocorticoid receptor antagonists)

Mechanism

Valsartan (ARB) suppresses the RAAS, while spironolactone blocks aldosterone receptors. Dual aldosterone blockade raises hyperkalaemia risk.

Symptoms

Management

The combination is appropriate in heart failure with reduced ejection fraction. Check potassium and creatinine 1 week after start, then monthly. If potassium exceeds 5.5 mmol/L, reduce the spironolactone dose.

Sources

ESC: ESC Guidelines for the diagnosis and treatment of acute and chronic heart failure (2021)

Pair details →

Moderate

Acetylsalicylic acid

Antiplatelet agents (low dose) / NSAIDs (analgesic dose)

Mechanism

Analgesic aspirin doses weaken the ARB's antihypertensive effect via vasodilator prostaglandin suppression. Cardioprotective doses are clinically minor.

Symptoms

Gradual blood pressure rise at high aspirin doses. At cardioprotective doses, no significant changes.

Management

Cardioprotective aspirin doses (75–100 mg) are acceptable without adjustment. At high doses, monitor blood pressure and increase valsartan if needed. Alternative analgesic: paracetamol.

Sources

ESH: 2023 ESH Guidelines for the management of arterial hypertension (2023)

Pair details →

Moderate

Bisoprolol

Selective beta-adrenergic blockers

Mechanism

Standard combination in heart failure with reduced ejection fraction. Additive antihypertensive effect and complementary neurohormonal blockade.

Symptoms

On starting, in older or hypovolaemic patients: symptomatic hypotension, dizziness. Bisoprolol bradycardia is amplified.

Management

Start both at minimal doses with up-titration every 2 weeks to target. Check standing/sitting BP, heart rate, creatinine and potassium at 2 weeks. In heart failure, target maximum tolerated doses (bisoprolol up to 10 mg, valsartan up to 320 mg). Outcome evidence base is extensive.

Sources

ESC: ESC Guidelines for the diagnosis and treatment of acute and chronic heart failure (2021)

Pair details →

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Official sources

Direct links to regulator labels. Open in a new tab.

AEMPS / CIMA

Spanish Medicines Information Centre (CIMA)

Label dated: 03/14/2026

FDA / DailyMed

FDA — DailyMed Drug Labels

Label dated: 03/13/2026

Safety

Contraindications

Pregnancy (all trimesters) – FDA category D
Severe hyperkalemia
Bilateral renal artery stenosis or stenosis of a single functioning kidney
Concurrent aliskiren in patients with diabetes or CKD
Severe hepatic impairment, biliary cirrhosis, cholestasis

Serious adverse effects

Angioedema (much less common than with ACEi, but possible)
Acute renal failure (in bilateral renal artery stenosis)
Life-threatening hyperkalemia (with potassium-sparing diuretics or aliskiren)

Common adverse effects

Dizziness
Hyperkalemia
Hypotension (more common with hypovolemia and in heart failure)
Creatinine elevation
Headache

PregnancyFDA D

FDA category D. Drugs acting on the renin-angiotensin system cause fetal renal injury, oligohydramnios, pulmonary and skeletal hypoplasia. Discontinue when pregnancy is planned.

Breastfeeding

No data on valsartan excretion in breast milk. Not recommended during breastfeeding. Alternative antihypertensives are chosen if therapy is needed.

Calculate RID Full profile on NIH LactMed ↗

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Frequently asked

What is Valsartan used for?

Valsartan is evaluated for the following indications with varying evidence strength: Hypertension (evidence tier A), Post-myocardial infarction heart failure (evidence tier B), Heart failure (evidence tier B). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Valsartan?

Common side effects of Valsartan (≥ 1 in 100): Dizziness, Hyperkalemia, Hypotension (more common with hypovolemia and in heart failure), Creatinine elevation, Headache. See the Safety section for uncommon and serious reactions.

Is Valsartan safe during pregnancy?

FDA category D. FDA category D. Drugs acting on the renin-angiotensin system cause fetal renal injury, oligohydramnios, pulmonary and skeletal hypoplasia. Discontinue when pregnancy is planned.

Is Valsartan compatible with breastfeeding?

No data on valsartan excretion in breast milk. Not recommended during breastfeeding. Alternative antihypertensives are chosen if therapy is needed.

Who should not take Valsartan?

Valsartan is contraindicated in: Pregnancy (all trimesters) – FDA category D; Severe hyperkalemia; Bilateral renal artery stenosis or stenosis of a single functioning kidney; Concurrent aliskiren in patients with diabetes or CKD; Severe hepatic impairment, biliary cirrhosis, cholestasis. Full list in the Safety section.

Mechanism of action

Practical notes

Timing and administration

Monitoring

Drug–drug interactions

6 pairs found. Sorted from critical to minor.

Major

Captopril

ACE inhibitor

Mechanism

Dual RAAS blockade (ACE-I + ARB). Additive hyperkalaemia, hypotension, and acute kidney injury risk without added benefit.

Symptoms

Weakness, postural dizziness, syncope. Reduced urine output, rising creatinine. Weakness and paraesthesia from hyperkalaemia.

Management

The combination is not prescribed. Choose one: ACE-I if tolerated, ARB if there is a dry cough or intolerance.

Sources

KDIGO: KDIGO 2024 Clinical Practice Guideline for the Evaluation and Management of CKD (2024)

Pair details →

Major

Co-trimoxazole

Sulfonamide-trimethoprim combination

Mechanism

Trimethoprim blocks collecting duct sodium channels (amiloride-like mechanism) and reduces potassium secretion. Valsartan (ARB) additionally retains potassium through aldosterone suppression.

Symptoms

Management

During co-trimoxazole therapy, check potassium 3–5 days after start. In older patients and chronic kidney disease, prefer alternative antibiotics: nitrofurantoin or fosfomycin.

Sources

PubMed: Trimethoprim-sulfamethoxazole and risk of sudden death among patients taking spironolactone or ACE inhibitors (2014)

Pair details →

Major

Enalapril

Angiotensin-converting enzyme inhibitors (ACEi)

Mechanism

Dual RAAS blockade (ACE-I + ARB). Proven in ONTARGET and VA NEPHRON-D trials: increased hyperkalaemia, hypotension, and acute kidney injury without cardioprotection.

Symptoms

Muscle weakness, paraesthesia, slowed pulse, arrhythmias. ECG: peaked T waves, widened QRS. Severe cases progress to cardiac arrest.

Management

The combination is not prescribed. Choose one: ACE-I (enalapril) if tolerated, ARB (valsartan) if there is a dry cough or intolerance.

Sources

KDIGO: KDIGO 2024 Clinical Practice Guideline for the Evaluation and Management of CKD (2024)

Pair details →

Major

Spironolactone

Potassium-sparing diuretics (mineralocorticoid receptor antagonists)

Mechanism

Valsartan (ARB) suppresses the RAAS, while spironolactone blocks aldosterone receptors. Dual aldosterone blockade raises hyperkalaemia risk.

Symptoms

Management

Sources

ESC: ESC Guidelines for the diagnosis and treatment of acute and chronic heart failure (2021)

Pair details →

Moderate

Acetylsalicylic acid

Antiplatelet agents (low dose) / NSAIDs (analgesic dose)

Mechanism

Analgesic aspirin doses weaken the ARB's antihypertensive effect via vasodilator prostaglandin suppression. Cardioprotective doses are clinically minor.

Symptoms

Gradual blood pressure rise at high aspirin doses. At cardioprotective doses, no significant changes.

Management

Cardioprotective aspirin doses (75–100 mg) are acceptable without adjustment. At high doses, monitor blood pressure and increase valsartan if needed. Alternative analgesic: paracetamol.

Sources

ESH: 2023 ESH Guidelines for the management of arterial hypertension (2023)

Pair details →

Moderate

Bisoprolol

Selective beta-adrenergic blockers

Mechanism

Standard combination in heart failure with reduced ejection fraction. Additive antihypertensive effect and complementary neurohormonal blockade.

Symptoms

On starting, in older or hypovolaemic patients: symptomatic hypotension, dizziness. Bisoprolol bradycardia is amplified.

Management

Sources

ESC: ESC Guidelines for the diagnosis and treatment of acute and chronic heart failure (2021)

Pair details →

Safety

Contraindications

Pregnancy (all trimesters) – FDA category D
Severe hyperkalemia
Bilateral renal artery stenosis or stenosis of a single functioning kidney
Concurrent aliskiren in patients with diabetes or CKD
Severe hepatic impairment, biliary cirrhosis, cholestasis

Serious adverse effects

Angioedema (much less common than with ACEi, but possible)
Acute renal failure (in bilateral renal artery stenosis)
Life-threatening hyperkalemia (with potassium-sparing diuretics or aliskiren)

Common adverse effects

Dizziness
Hyperkalemia
Hypotension (more common with hypovolemia and in heart failure)
Creatinine elevation
Headache

PregnancyFDA D

FDA category D. Drugs acting on the renin-angiotensin system cause fetal renal injury, oligohydramnios, pulmonary and skeletal hypoplasia. Discontinue when pregnancy is planned.

Breastfeeding

No data on valsartan excretion in breast milk. Not recommended during breastfeeding. Alternative antihypertensives are chosen if therapy is needed.

Calculate RID Full profile on NIH LactMed ↗

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Frequently asked

What is Valsartan used for?

What are the side effects of Valsartan?

Is Valsartan safe during pregnancy?

FDA category D. FDA category D. Drugs acting on the renin-angiotensin system cause fetal renal injury, oligohydramnios, pulmonary and skeletal hypoplasia. Discontinue when pregnancy is planned.

Is Valsartan compatible with breastfeeding?

No data on valsartan excretion in breast milk. Not recommended during breastfeeding. Alternative antihypertensives are chosen if therapy is needed.

Who should not take Valsartan?