A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

Michel, Martin C.; Foster, Carolyn; Brunner, Hans R.; Liu, Lisheng

doi:10.1124/pr.112.007278

Cited by 249 publications

(248 citation statements)

References 426 publications

(553 reference statements)

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“…Although the renin-angiotensin system is indeed distributed throughout systemic tissues including the brain, the ability of ARBs, including azilsartan, to cross the blood-brain barrier (BBB) is minimally limited and not fully conclusive. 46,47) In previous studies regarding HT and dementia, ARBs and ACE inhibitors with a higher degree of BBB penetration could prevent the development of dementia; however, this preventative effect was not confirmed in randomized controlled trails. 48,49) Thus, the precise mechanisms by which ARBs and ACE inhibitors affect psychiatric and cognitive functions are yet unclear.…”

Section: Discussionmentioning

confidence: 99%

Association Between Blood Pressure Lowering and Quality of Life by Treatment of Azilsartan

et al. 2017

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SummaryThe authors assessed the effects of switching from a conventional angiotensin II receptor blocker (ARB) to azilsartan on blood pressure (BP) and health-related quality of life (HR-QOL) in patients with uncontrolled hypertension. Key eligibility criteria were uncontrolled hypertension treated for !1 month with an ARB, excluding azilsartan, that did not reach the target BP. We recruited 147 patients (64 males and 83 females; mean ± standard deviation age 73 ± 15 years). Azilsartan reduced both systolic and diastolic BP significantly, from 151 ± 16/82 ± 12 to 134 ± 17/73 ± 12 mm Hg, 3 months after switching. Although scores on the comprehensive QOL scale, the EuroQoL 5 dimensions (EQ5D), and the simplified menopausal index (SMI) did not change, the Geriatric Depression Scale (GDS) score improved significantly, and there was a significant association between the change in the GDS score and systolic BP lowering (r = 0.2554, P = 0.030). The Pittsburgh sleep quality index (PSQI) improved significantly only in the female subgroup. Besides sufficient BP lowering activity, antihypertensive treatment with azilsartan may have a favorable impact on depression in geriatric patients with uncontrolled hypertension.(Int Heart J 2017; 58: 752-761)

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Section: Discussionmentioning

confidence: 99%

Association Between Blood Pressure Lowering and Quality of Life by Treatment of Azilsartan

et al. 2017

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“…In addition, eprosartan mesylate is poorly water soluble with slow dissolution rate which contributes to its low bioavailability after oral administration [8]. The drug thus exhibits low and variable bioavailability with the recorded absolute oral bioavailability being approximately 13% [6]. To date, the intestinal membrane transport parameters of this drug have not been identified.…”

Section: Introductionmentioning

confidence: 99%

“…The latter corresponds to the water flux effect. The actual amount of drug absorbed per unit time can be expressed using equation (6).…”

Section: Expmentioning

confidence: 99%

“…It differs from other angiotensin receptor blockers (ARBs) in achieving its action via competitive inhibitory effect [4,5]. Eprosartan is not substrate for cytochrome P450 (CYP450) and is mainly excreted unchanged by biliary or renal routes with no active metabolite being detected after oral or intravenous administration [6]. The drug is characterised by a relatively long elimination halflife which can reach 20 h but no accumulation was recorded after repeated dosing [6].…”

Section: Introductionmentioning

confidence: 99%

“…Eprosartan is not substrate for cytochrome P450 (CYP450) and is mainly excreted unchanged by biliary or renal routes with no active metabolite being detected after oral or intravenous administration [6]. The drug is characterised by a relatively long elimination halflife which can reach 20 h but no accumulation was recorded after repeated dosing [6]. Eprosartan is an amphiphilic molecule containing allylic and phenylic carboxylic groups and one imidazole (basic) functional group.…”

Section: Introductionmentioning

confidence: 99%

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Intestinal Absorption of Eprosartan Mesylate From Self Emulsifying System and Cyclodextrin Complex

Quader

Osman

Maghraby

2017

Int J Pharm Pharm Sci

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Objective: The aim of this work was to determine the intestinal membrane transport parameters of eprosartan mesylate (EM) and to investigate self-nano emulsifying drug delivery systems (SNEDDS) and inclusion complexation with hydroxypropyl β cyclodextrin (HPβCD) for enhanced intestinal absorption of eprosartan mesylate. Methods:The intestinal absorption was monitored using the in situ rabbit intestinal perfusion technique. SNEDDS was developed using labrafil, Lauroglycol with a tween in the presence of ethanol. Inclusion complexation was achieved by construction of phase solubility diagram in the presence of HPβCD. The prepared complex was evaluated using Fourier Transform Infrared Spectroscopy (FTIR) and differential scanning calorimetry (DSC). Results:The drug was found to be poorly absorbed from the jejuno-ileum and the colon with the absorption being mainly through paracellular pathway. An inclusion complex was developed between the drug and HPβCD. Perfusion of the drug in the nanoemulsion formulation or as an inclusion complex resulted in a significant increase in the intestinal absorption of the drug compared with the control.Conclusion: SNEDDS and inclusion complexation are promising strategies for enhanced intestinal absorption of eprosartan mesylate.

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Hypertension Treatment Modality and Suicide Risk Among Veterans in Veterans Health Administration Care From 2015 to 2017

et al. 2020

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IMPORTANCE The Veterans Health Administration (VHA) serves a population of veterans with a high prevalence of comorbid health conditions and increased risk for suicide. OBJECTIVE To replicate the findings of a previous study and assess whether exposure to angiotensin receptor blockers (ARBs) is associated with differential suicide risk compared with angiotensin-converting enzyme inhibitors (ACEIs) among veterans receiving VHA care. DESIGN, SETTING, AND PARTICIPANTS This nested case-control design included all suicide decedents from 2015 to 2017 with a VHA inpatient or outpatient encounter in the prior year and with either an active ACEI or ARB prescription in the 100 days prior to death. Using a 4:1 ratio, controls were matched to cases by age, sex, and hypertension and diabetes diagnoses. Controls were alive at the time of the death of the matched case, had a VHA encounter within the previous year, and had either an active ACEI or ARB medication fill within 100 days before the death of the matched case. EXPOSURES An active ACEI or ARB prescription within 100 days before the death of the case. MAIN OUTCOMES AND MEASURES Cases were suicide decedents from 2015 to 2017 per National Death Index search results included in the Veteran Affairs/Department of Defense Mortality Data Repository. RESULTS Among 1309 cases, the median (interquartile range [IQR]) age was 68 (60-76) years and among 5217 controls, the median (IQR) age was 67 (60-76) years, and 1.9% of veterans in both groups were female. ARBs were received by 20.2% of controls and 19.6% of cases; ACEIs were received by 79.8% of controls and 80.4% of cases. The crude suicide odds ratio for ARBs vs ACEIs was 0.966 (95% CI, 0.828-1.127). Controlling for covariates, the adjusted odds ratio for ARBs was 0.985 (95% CI, 0.834-1.164). Sensitivity analyses using only those covariates that differed significantly between groups, restricting to veterans ages 65 and older, dropping matching criteria, and adjusting for the quantity and temporal proximity of ACEI and ARB exposure in the 100 days prior to the index date, had consistent findings. CONCLUSIONS AND RELEVANCE This case-control study did not identify differences in suicide risk by receipt of ARBs vs ACEIs in analyses specific to veterans receiving VHA care in contrast with findings from the referent study.

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A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

Cited by 249 publications

References 426 publications

Association Between Blood Pressure Lowering and Quality of Life by Treatment of Azilsartan

Association Between Blood Pressure Lowering and Quality of Life by Treatment of Azilsartan

Intestinal Absorption of Eprosartan Mesylate From Self Emulsifying System and Cyclodextrin Complex

Hypertension Treatment Modality and Suicide Risk Among Veterans in Veterans Health Administration Care From 2015 to 2017

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