Effects of allisartan isoproxil on blood pressure and target organ injury in patients with mild to moderate essential hypertension

Abstract

Evidence has shown that angiotensin II type 1 receptor antagonists have lower blood pressure and have target organ protective effects, but this is not the case for the drug allisartan isoproxil. The aim of this study was to evaluate the effects of allisartan isoproxil on blood pressure and target organ injury in patients with mild to moderate essential hypertension. In total, 80 essential hypertensive participants were randomly divided into an allisartan group and a nifedipine group (n = 40 per group), and their blood pressure was measured once per month for 6 months. A 2-dimensional echocardiogram was performed at baseline and at the end of the study. The serum levels of renal injury indexes, endothelial function markers, inflammatory factors, blood biochemical assays and urinary measurements were determined at baseline and at 6 months. At the end of the study, both systolic and diastolic blood pressure were significantly decreased in the allisartan group compared with baseline and showed the same antihypertensive effect as the nifedipine group. Meanwhile, the left ventricular remodeling, 24-hours levels of urinary microalbumin, endothelial dysfunction, and arterial stiffness were all significantly improved compared with that of the baseline and the nifedipine group (all P < .05). The present study showed that allisartan isoproxil had favorable blood pressure lowering and heart, renal, and endothelial protective effects in patients with mild to moderate essential hypertension.

Allisartan isoproxil attenuates oxidative stress and inflammation through the SIRT1/Nrf2/NF‑κB signalling pathway in diabetic cardiomyopathy rats

“…Allisartan isoproxil is a new nonpeptide angiotensin II receptor blocker precursor drug. Compared with losartan, allisartan isoproxil has higher absorption efficiency, better blood pressure lowering effect and lower adverse reactions ( 25 , 26 ). In the present study, it was revealed that treatment of DCM with allisartan isoproxil in diabetic rats alleviated inflammation and oxidative stress injury.…”

“…Briefly, increased levels of Ang II have been reported to regulate the production of ROS and lead to cardiac hypertrophy, left ventricular dysfunction, and myocardial insulin resistance ( 22 , 23 ). Allisartan isoproxil is a new nonpeptide angiotensin II receptor blocker (ARB) precursor drug that can produce a carboxylic acid derivative (EXP3174) during absorption in vivo ( 24 , 25 ). Compared with losartan, allisartan isoproxil can be completely hydrolysed by esterase into the active metabolite EXP3174 after being absorbed into the small intestine and stomach ( 26 ).…”

Allisartan ameliorates vascular remodeling through regulation of voltage-gated potassium channels in hypertensive rats

“…It stimulates cellular hypertrophy [ 12 ], protein synthesis, activation of NADPH oxidase system to generate ROS [ 13 ] and synthesize collagen in the vascular smooth muscle cells [ 14 ]. Reduction of cardiovasular events was reported with blockade of the RAS [ 15 , 16 ]. Several antihypertensive agents including angiotensin II receptor blockers (ARBs) and angiotensin-converting enzyme (ACE) inhibitors acts by blocking the RAS and are widely used in the management of hypertension [ 17 ].…”

“…Losartan, an orally active ARB is widely used due to its well-established efficacy and safety profile in hypertensive patients [ 15 , 23 ]. In humans, cytochrome P450 (CYP450) metabolizes losartan to various metabolites along with an active carboxylic acid metabolite, EXP3174 that includes around 14 % of losartan [ 24 ].…”

“…In humans, cytochrome P450 (CYP450) metabolizes losartan to various metabolites along with an active carboxylic acid metabolite, EXP3174 that includes around 14 % of losartan [ 24 ]. EXP3174 is an selective angiotensin II type 1 receptor antagonist and was reported to be more potent than losartan both in vitro (15 times) and in vivo (30 times) [ 15 , 25 ].…”