Brands, Medical Use, Clinical Data
- Antihypertensive Agents
- Angiotensin II Receptor Antagonists
Brands / Synonyms
Diovan; Diovan HCT; Exforge; Exforge HCT; Valsarran; Valsartan [Usan:Inn]
For the treatment of hypertension.
Valsartan, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. Unlike the angiotensin receptor antagonist losartan, Valsartan does not have an active metabolite or possess uricosuric effects.
Mechanism of Action
Valsartan competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance.
Biotrnasformation / Drug Metabolism
Diovan® (valsartan) is contraindicated in patients who are hypersensitive to any
component of this product.
No clinically significant pharmacokinetic interactions were observed when valsartan was coadministered
with amlodipine, atenolol, cimetidine, digoxin, furosemide, glyburide, hydrochlorothiazide, or indomethacin. The
valsartan-atenolol combination was more antihypertensive than either component, but it did not lower the heart rate
more than atenolol alone.
Coadministration of valsartan and warfarin did not change the pharmacokinetics of valsartan or the
time-course of the anticoagulant properties of warfarin.
CYP 450 Interactions: The enzyme(s) responsible for valsartan metabolism have not been
identified but do not seem to be CYP 450 isozymes. The inhibitory or induction potential of valsartan on CYP 450 is
As with other drugs that block angiotensin II or its effects, concomitant use of potassium sparing
diuretics (e.g. spironolactone, triamterene, amiloride), potassium supplements, or salt substitutes containing
potassium may lead to increases in serum potassium and in heart failure patients to increases in serum