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Differential pharmacology and benefit/risk of azilsartan compared to other sartans.

Kurtz TW, Kajiya T - Vasc Health Risk Manag (2012)

Bottom Line: Greater antihypertensive effects of azilsartan might be due in part to its unusually potent and persistent ability to inhibit binding of angiotensin II to AT(1) receptors.Preclinical studies have indicated that azilsartan may also have potentially beneficial effects on cellular mechanisms of cardiometabolic disease and insulin sensitizing activity that could involve more than just blockade of AT(1) receptors and/or reduction in BP.Given that the general ability of antihypertensive drugs to protect against target organ damage is largely mediated by their ability to decrease BP, the enhanced antihypertensive effects of azilsartan should serve to justify clinical interest in this ARB relative to other molecules in the class that have a lower capacity to reduce BP.

View Article: PubMed Central - PubMed

Affiliation: Department of Laboratory Medicine, University of California, San Francisco, CA 94107, USA. kurtzt@labmed2.ucsf.edu

ABSTRACT
Azilsartan, an angiotensin II type 1 (AT(1)) receptor blocker (ARB), was recently approved by regulatory authorities for treatment of hypertension and is the 8th ARB to join the clinical market. This article discusses the medical reasons for introducing a new AT(1) receptor blocker and reviews the experimental and clinical studies that have compared the functional properties of azilsartan to those of other ARBs. The main question addressed is: Does azilsartan have distinguishing features that should motivate choosing it over any of the other sartans for use in clinical practice? Based on studies conducted to date in hypertensive patients without serious comorbidities, azilsartan appears to be characterized by a superior ability to control 24-hour systolic blood pressure (BP) relative to other widely used ARBs including valsartan, olmesartan, and candesartan, and presumably others as well (eg, losartan). Compared to these other ARBs, azilsartan may increase the BP target control and response rate by an absolute value of 8%-10%. Greater antihypertensive effects of azilsartan might be due in part to its unusually potent and persistent ability to inhibit binding of angiotensin II to AT(1) receptors. Preclinical studies have indicated that azilsartan may also have potentially beneficial effects on cellular mechanisms of cardiometabolic disease and insulin sensitizing activity that could involve more than just blockade of AT(1) receptors and/or reduction in BP. However, the clinical relevance of these additional actions is unknown. Given that the general ability of antihypertensive drugs to protect against target organ damage is largely mediated by their ability to decrease BP, the enhanced antihypertensive effects of azilsartan should serve to justify clinical interest in this ARB relative to other molecules in the class that have a lower capacity to reduce BP.

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Related in: MedlinePlus

Mean changes in 24-hour systolic BP from baseline (difference from placebo) in patients with stages 1 and 2 hypertension without serious comorbidities treated for 6 weeks with maximum approved doses of azilsartan medoxomil (80 mg/day), olmesartan medoxomil (40 mg/day), or valsartan (320 mg/day) as reported by White et al.25 Error bars denote limits of the 95% confidence intervals for the means.Abbreviation: BP, blood pressure.
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f2-vhrm-8-133: Mean changes in 24-hour systolic BP from baseline (difference from placebo) in patients with stages 1 and 2 hypertension without serious comorbidities treated for 6 weeks with maximum approved doses of azilsartan medoxomil (80 mg/day), olmesartan medoxomil (40 mg/day), or valsartan (320 mg/day) as reported by White et al.25 Error bars denote limits of the 95% confidence intervals for the means.Abbreviation: BP, blood pressure.

Mentions: Azilsartan, in clinically approved doses as azilsartan medoxomil, has been shown to lower 24-hour BP in hypertensive patients significantly more than the maximum approved dose of olmesartan medoxomil, the latter being considered by some to be one of the most potent ARBs for lowering BP.23,25,26 Azilsartan medoxomil has also been shown to lower 24-hour BP significantly more than the maximum approved dose of valsartan, the most widely prescribed drug in the ARB class.25,27,44 Specifically, in head-to-head studies using ambulatory BP monitoring in hypertensive patients without serious comorbidities, treatment for 6 weeks with 80 mg azilsartan medoxomil lowered 24-hour systolic BP by 2–4 mmHg (P < 0.01 to P < 0.001) more than 40 mg olmesartan medoxomil or 320 mg valsartan, respectively (Figure 2).25,26 Azilsartan medoxomil also lowered 24-hour diastolic BP more than olmesartan medoxomil and valsartan, and was just as well tolerated and as safe as the comparator agents.


Differential pharmacology and benefit/risk of azilsartan compared to other sartans.

Kurtz TW, Kajiya T - Vasc Health Risk Manag (2012)

Mean changes in 24-hour systolic BP from baseline (difference from placebo) in patients with stages 1 and 2 hypertension without serious comorbidities treated for 6 weeks with maximum approved doses of azilsartan medoxomil (80 mg/day), olmesartan medoxomil (40 mg/day), or valsartan (320 mg/day) as reported by White et al.25 Error bars denote limits of the 95% confidence intervals for the means.Abbreviation: BP, blood pressure.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3295635&req=5

f2-vhrm-8-133: Mean changes in 24-hour systolic BP from baseline (difference from placebo) in patients with stages 1 and 2 hypertension without serious comorbidities treated for 6 weeks with maximum approved doses of azilsartan medoxomil (80 mg/day), olmesartan medoxomil (40 mg/day), or valsartan (320 mg/day) as reported by White et al.25 Error bars denote limits of the 95% confidence intervals for the means.Abbreviation: BP, blood pressure.
Mentions: Azilsartan, in clinically approved doses as azilsartan medoxomil, has been shown to lower 24-hour BP in hypertensive patients significantly more than the maximum approved dose of olmesartan medoxomil, the latter being considered by some to be one of the most potent ARBs for lowering BP.23,25,26 Azilsartan medoxomil has also been shown to lower 24-hour BP significantly more than the maximum approved dose of valsartan, the most widely prescribed drug in the ARB class.25,27,44 Specifically, in head-to-head studies using ambulatory BP monitoring in hypertensive patients without serious comorbidities, treatment for 6 weeks with 80 mg azilsartan medoxomil lowered 24-hour systolic BP by 2–4 mmHg (P < 0.01 to P < 0.001) more than 40 mg olmesartan medoxomil or 320 mg valsartan, respectively (Figure 2).25,26 Azilsartan medoxomil also lowered 24-hour diastolic BP more than olmesartan medoxomil and valsartan, and was just as well tolerated and as safe as the comparator agents.

Bottom Line: Greater antihypertensive effects of azilsartan might be due in part to its unusually potent and persistent ability to inhibit binding of angiotensin II to AT(1) receptors.Preclinical studies have indicated that azilsartan may also have potentially beneficial effects on cellular mechanisms of cardiometabolic disease and insulin sensitizing activity that could involve more than just blockade of AT(1) receptors and/or reduction in BP.Given that the general ability of antihypertensive drugs to protect against target organ damage is largely mediated by their ability to decrease BP, the enhanced antihypertensive effects of azilsartan should serve to justify clinical interest in this ARB relative to other molecules in the class that have a lower capacity to reduce BP.

View Article: PubMed Central - PubMed

Affiliation: Department of Laboratory Medicine, University of California, San Francisco, CA 94107, USA. kurtzt@labmed2.ucsf.edu

ABSTRACT
Azilsartan, an angiotensin II type 1 (AT(1)) receptor blocker (ARB), was recently approved by regulatory authorities for treatment of hypertension and is the 8th ARB to join the clinical market. This article discusses the medical reasons for introducing a new AT(1) receptor blocker and reviews the experimental and clinical studies that have compared the functional properties of azilsartan to those of other ARBs. The main question addressed is: Does azilsartan have distinguishing features that should motivate choosing it over any of the other sartans for use in clinical practice? Based on studies conducted to date in hypertensive patients without serious comorbidities, azilsartan appears to be characterized by a superior ability to control 24-hour systolic blood pressure (BP) relative to other widely used ARBs including valsartan, olmesartan, and candesartan, and presumably others as well (eg, losartan). Compared to these other ARBs, azilsartan may increase the BP target control and response rate by an absolute value of 8%-10%. Greater antihypertensive effects of azilsartan might be due in part to its unusually potent and persistent ability to inhibit binding of angiotensin II to AT(1) receptors. Preclinical studies have indicated that azilsartan may also have potentially beneficial effects on cellular mechanisms of cardiometabolic disease and insulin sensitizing activity that could involve more than just blockade of AT(1) receptors and/or reduction in BP. However, the clinical relevance of these additional actions is unknown. Given that the general ability of antihypertensive drugs to protect against target organ damage is largely mediated by their ability to decrease BP, the enhanced antihypertensive effects of azilsartan should serve to justify clinical interest in this ARB relative to other molecules in the class that have a lower capacity to reduce BP.

Show MeSH
Related in: MedlinePlus