Valsartan Drug Classification
Valsartan is an angiotensin II receptor blocker (ARB), also known as an angiotensin II receptor antagonist, that selectively blocks the AT1 receptor subtype. 1
Mechanism of Action
Valsartan is a nonpeptide, orally active, specific angiotensin II receptor blocker acting on the AT1 receptor subtype, with no affinity for the AT2 receptor. 1, 2
The drug selectively blocks the binding of angiotensin II to the AT1 receptor, thereby inhibiting angiotensin II-mediated effects including vasoconstriction, aldosterone release, and cell growth promotion. 3, 4
After oral administration, valsartan inhibits the pressor response to angiotensin II for 24 hours, making it suitable for once-daily dosing in hypertension. 5
Clinical Classification Context
ARBs as a drug class are positioned as alternatives to ACE inhibitors in major cardiovascular guidelines, particularly for patients intolerant to ACE inhibitors due to cough or angioedema. 6
The European Society of Cardiology and American College of Cardiology classify valsartan alongside other ARBs (candesartan, losartan, irbesartan, telmisartan) as inhibitors of the renin-angiotensin-aldosterone system. 6
Valsartan demonstrates dose-dependent efficacy over the range of 80-320 mg once daily for blood pressure reduction, with higher doses providing greater cardiovascular benefits. 7, 3
Key Distinguishing Features from ACE Inhibitors
Unlike ACE inhibitors, valsartan does not inhibit kininase, which explains its significantly lower incidence of cough (a common ACE inhibitor side effect caused by bradykinin accumulation). 6
The side effect profile of ARBs including valsartan is comparable to placebo in most studies, with significantly fewer adverse effects than ACE inhibitors. 6, 8
Angioedema occurs in fewer than 1% of patients on ACE inhibitors but is even rarer with ARBs, though extreme caution is advised when substituting an ARB in patients with prior ACE inhibitor-associated angioedema. 6