Clinical Advantage of Valsartan

Abstract

Valsartan is a specific angiotensin II receptor antagonist with high selectivity for the AT₁ receptor subtype. After oral administration of single or repeated once-daily doses, valsartan 40–80 mg inhibits the pressor response to angiotensin II for 24 hours. In patients with mild-to-moderate hypertension, efficacy of valsartan appears to be independent of age, sex, and race, and is at least equivalent to that of calcium antagonists, ACE inhibitors, or thiazide diuretics. Response rate to valsartan 160 mg o.d. is significantly greater than after receiving losartan 100 mg o.d. Valsartan has additive effects with other antihypertensive drugs and combination therapy is effective in severe hypertension and in hypertension with renal insufficiency, where renal function is well maintained. Valsartan has good tolerability with a side-effect profile indistinguishable from placebo and superior to that of comparable drugs. Valsartan does not cause cough or adverse metabolic effects; first dose hypotension and rebound hypertension on abrupt withdrawal have not been encountered. Valsartan has clear clinical advantage in the management of hypertension. Its impact on prognosis in patients with a high risk of cardiovascular morbidity and mortality is under evaluation.

Valsartan ingestions among adults reported to Texas poison control centers, 2000 to 2005

“…The listing of hypertension as an adverse clinical effect may be due to recording errors by the poison control center staff when entering information into the TESS database. Aside from hypertension, the other specific adverse clinical effects reported in this study had generally been found in other studies [1,[3][4][5][6][7].…”

“…Valsartan is indicated for the treatment of hypertension and heart failure and for the reduction of cardiovascular mortality after myocardial infarction [1][2][3][4][5]. The drug's effects are dose-dependent [3].…”

“…Other adverse clinical effects reported with valsartan use include dizziness, diarrhea, arthralgia, fatigue, drowsiness, nausea, abdominal pain, blurred vision, syncope, headache, cough, rhinitis, sinusitis, and edema [1,[3][4][5][6][7]. The recommended treatment of adverse valsartan ingestions includes decontamination or increased elimination via such methods as lavage or activated charcoal and supportive care [4][5].…”

Transdermal delivery of angiotensin II receptor blockers (ARBs), angiotensin-converting enzyme inhibitors (ACEIs) and others for management of hypertension

“…When administrated orally in humans, VS is rapidly absorbed. It has a favorable log P (4.5) and mean halflife (7.5 h) (McInnes, 1999;Beg et al, 2012). Its C max occurs at 2 to 4 h, and it is then excreted into bile.…”

Determination of 4, 4′-Bis (Bromomethyl) Biphenyl Genotoxic Impurity in Valsartan Drug Substances by HPLC

“…The drug has more affinity about 20,000-fold for the angiotensin type 1 receptor than for the angiotensin type 2 receptor, through relaxing blood vessels and causing them to extend, leads to lowers blood pressure and improves the blood flow [6,7]. The drug is rapidly orally absorbed, the limited volume of distribution, extensively bound to plasma proteins, relaxes to control high blood pressure and congestive heart [8].…”