Angiotensin II receptor blockers (ARBs)
ATC code: C09CA03 (Valsartan)
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.
First 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.
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.
First 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 non-inferior to captopril for mortality and cardiovascular events. Prescribed for patients who do not tolerate ACE inhibitors.
FDA category D. Drugs acting on the renin-angiotensin system cause fetal renal injury, oligohydramnios, pulmonary and skeletal hypoplasia. Discontinue when pregnancy is planned.
No data on valsartan excretion in breast milk. Not recommended during breastfeeding. Alternative antihypertensives are chosen if therapy is needed.
valsartan is evaluated for the following indications with varying evidence strength: Hypertension (evidence tier A), Heart failure (evidence tier A), Post-myocardial infarction heart failure (evidence tier A). See the full indication matrix with dosing and citations above on this page.
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.
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.
No data on valsartan excretion in breast milk. Not recommended during breastfeeding. Alternative antihypertensives are chosen if therapy is needed.
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.