Azilsartan in Patients With Mild to Moderate Hypertension Using Clinic and Ambulatory Blood Pressure Measurements

Abstract

This was a phase 2, multicenter, randomized, parallel‐group, double‐blind dose‐ranging study. Hypertensive adults (n=555) received one of five doses of azilsartan (AZL; 2.5, 5, 10, 20, 40 mg), olmesartan medoxomil (OLM) 20 mg, or placebo once daily. The primary endpoint was change in trough clinic diastolic blood pressure (DBP) at week 8. Compared with placebo, all AZL doses (except 2.5 mg) provided statistically and clinically significant reductions in DBP and systolic blood pressure (SBP) based on both clinic blood pressure (BP) and 24‐hour ambulatory BP monitoring (ABPM). AZL 40 mg was statistically superior vs OLM. Clinic BP was associated with a pronounced placebo effect (−6 mm Hg), whereas this was negligible with ABPM (±0.5 mm Hg). Adverse event frequency was similar in the AZL and placebo groups. Based on these and other findings, subsequent trials investigated the commercial AZL medoxomil tablet at doses 20 to 80 mg/d using 24‐hour ABPM.

Pharmacokinetics of a Single Dose of Azilsartan in Pediatric Patients: A Phase 3, Open-Label, Multicenter Study

“…Furthermore, a single oral dose does not reflect the typical treatment course with antihypertensives, where patients are treated over a longer period of time. Although limited by the small number of patients and short treatment period, our results suggest that, similar to reported studies in adult patients [ 5 , 6 ], azilsartan is well tolerated in pediatric patients.…”

“…Azilsartan (TAK-536) is an angiotensin II receptor blocker (ARB) approved for the treatment of adult hypertension in Japan in January 2012. In adults, azilsartan is considered superior to the ARBs candesartan cilexetil and olmesartan medoxomil in terms of its ability to lower 24-h blood pressure, alongside a favorable safety profile [ 5 , 6 ]. Although there are some exceptions, previously reported clinical trials of ARBs indicate that their blood pressure (BP)-lowering effects in children are consistent with their effects in adults [ 7 , 8 ].…”

Hronotherapy Aspects of Efficiency Azilsartan Medoxomil in Combination Therapy in Patients With Hypertension and Metabolic Syndrome

“…Именно благодаря этим свойствам азил-сартан способен удерживать связь с АТ1 рецептором, несмотря на возрастающую концентрацию АТII в ситуациях, сопровождающихся подъемом АД. Высокая аффинность к АТ1 рецепторам, необрати-мость взаимодействия и обратный агонизм, скорее всего, ответственны за быстрый и стабильный эффект препарата и значительный потенциал в антигипер-тензивном действии [8,9]. По-видимому, именно этими эффектами могут быть обусловлены органо-протекторные и антифибротические свойства препа-рата [10].…”

Improvement of Diurnal Blood Pressure Variation by Azilsartan

“…In a prospective study comparing azilsartan (20 mg) with olmesartan (20 mg), the difference of office SBP/DBP was 4.0/2.3 mm Hg in favor of azilsartan [ 13 ]. When olmesartan (20 mg) was switched to azilsartan (20 mg) in the current study, office SBP was reduced from 155 to 140 mm Hg (a decrease of 15 mm Hg), so the antihypertensive effect of azilsartan was also more pronounced in this study.…”