Azelnidipine and Amlodipine: a Comparison of Their Pharmacokinetics and Effects on Ambulatory Blood Pressure.

Kuramoto, Kizuku; Ichikawa, Shûichi; Hirai, Aizan; Kanada, Shigeto; Nakachi, Tetsu; Ogihara, Toshio

doi:10.1291/hypres.26.201

Cited by 106 publications

(103 citation statements)

References 28 publications

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“…OLM and AZL are new ARB and CCB with more potent vasodilator effects compared to other drugs in the same class (Kuramoto et al 2003;Mire et al 2005;Kojima et al 2011). Furthermore, we have previously demonstrated that their combination ameliorate endothelial function to a greater extent than each monotherapy in ApoE −/− mice (Hosoya et al 2010); however, it remains to be examined whether this combination therapy also suppresses atherosclerosis and parenchymal tissue damage such in the kidney and the liver.…”

Section: Anti-atherogenic Effects Of Olm Plus Azlmentioning

confidence: 99%

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Anti-Atherogenic Effects of the Combination Therapy with Olmesartan and Azelnidipine in Diabetic Apolipoprotein E-Deficient Mice

Noda

Hosoya

Nakajima

et al. 2012

Tohoku J. Exp. Med.

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Many studies have aimed to identify anti-atherogenic agents in cardiovascular medicine. We have recently demonstrated that the combination therapy with olmesartan (OLM), an angiotensin II receptor blocker, and azelnidipine (AZL), a dihydroprydine calcium-channel blocker, improves endothelial function in diabetic Apolipoprotein-deficient (ApoE −/− ) mice. In the present study, we examined whether this combination therapy also inhibits atherosclerosis in mice. We used male control and streptozocin-induced diabetic ApoE −/− mice. Diabetic ApoE −/− mice were orally treated for 5 weeks with vehicle (Untreated), OLM (30 mg/ kg/day), AZL (10 mg/kg/day), their combination (OLM+AZL), or hydralazine (HYD, 5 mg/kg/day) as an antihypertensive control. At 5 weeks, systolic blood pressure was significantly elevated in Untreated but was normalized in OLM+AZL and HYD. The atherosclerosis area in the thoracic aorta, perivascular fibrosis and medial thickness of the coronary arteries were increased in Untreated and were ameliorated in OLM+AZL but not in HYD. Staining with a fluorescent probe dihydroethidium showed that production of reactive oxygen species was increased in Untreated, and ameliorated in OLM+AZL. Consistent with these findings, macrophage infiltration in the kidney and the expression of receptor for advanced glycation end-products in the heart, kidney and liver were increased in Untreated and were all ameliorated in OLM+AZL, associated with up-regulation of endothelial NO syntheses (eNOS). In conclusion, the combination therapy with OLM and AZL exerts anti-atherogenic effect in diabetic ApoE −/− mice through suppression of oxidative stress and activation of eNOS, independent of its blood pressure-lowering effects. Clinically, this combination therapy may be useful for patients with hypertension, hyperlipidemia and diabetes.

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Section: Anti-atherogenic Effects Of Olm Plus Azlmentioning

confidence: 99%

“…AZL is a dihydropyridine calcium channel blocker with potent and long-acting blood pressure lowering effects without changing heart rate (Kuramoto et al 2003). HYD is a vasodilator agent with only a few pleiotropic effects besides blood pressure lowering effects (Kandler et al 2011).…”

Section: Pharmacological Characteristic Of Olm Azl and Hydmentioning

confidence: 99%

Anti-Atherogenic Effects of the Combination Therapy with Olmesartan and Azelnidipine in Diabetic Apolipoprotein E-Deficient Mice

Noda

Hosoya

Nakajima

et al. 2012

Tohoku J. Exp. Med.

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“…[17][18][19][20] AZL is also reported to have the following effects: antioxidative effect, antiatherosclerotic effect, maintaining cerebral blood flow, prevention of proteinuria and PR reduction which is not observed with amlodipine. [21][22][23][24][25] Furthermore, combined use of ARB and AZL is reported to prevent microalbuminuria in diabetic nephropathy patients. 26 A nonclinical study demonstrated that OLM plus CCB combination showed the various preventive effects on vascular injury depending on which CCB was used; AZL was the most effective CCB tested.…”

Section: Safetymentioning

confidence: 99%

A randomized, double-blind, four-arm parallel-group study of the efficacy and safety of azelnidipine and olmesartan medoxomil combination therapy compared with each monotherapy in Japanese patients with essential hypertension: the REZALT study

et al. 2009

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A 12-week randomized, double-blind, four-arm parallel-group, comparative study was conducted in patients with essential hypertension to evaluate the antihypertensive effect and safety of combination therapy with olmesartan medoxomil (OLM, an angiotensin-receptor blocker) 20 mg plus azelnidipine (AZL, a long-acting dihydropyridine calcium channel blocker (20) and AZL (16) monotherapy groups (À12.1/À6.9 and À12.0/À6.9 mm Hg). The proportion of patients achieving the SeBP goal (o130/85 mm Hg for normal BP or o140/90 mm Hg for high-normal BP) was significantly higher in the O/A (20/16) combination group than in the monotherapy groups. The incidence of adverse events was similar in the O/A combination groups and the monotherapy groups. These results showed that combination therapy with O/A was well tolerated and exerted a stronger antihypertensive effect compared with monotherapy with OLM or AZL in patients with essential hypertension.

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“…Therefore, administration of amlodipine, a long acting calcium antagonist, is recommended in patients with hypertension and angina (8). However, Kuramoto et al (9) have reported that the heart rate (HR) increases after short-term treatment with amlodipine but not azelnidipine. Azelnidipine, a third-generation dihydropyridine calcium antagonist, has a higher vascular selectivity with few adverse reactions (10).…”

Section: Introductionmentioning

confidence: 99%

Comparative Effects of Azelnidipine and Amlodipine on Myocardial Function and Mortality After Ischemia/Reperfusion in Dogs

et al. 2011

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Abstract. Effects of azelnidipine were examined and compared with those of amlodipine on stunned myocardium in dogs. The left anterior descending (LAD) coronary artery was ligated for 20 min and subsequently released for 60 min. A vehicle, azelnidipine (0.3 mg/kg), or amlodipine (0.3 or 1 mg/kg) was injected intravenously 20 min before LAD ligation. The heart rate increased after a depressor response in the presence of amlodipine, while it decreased despite a decrease in arterial pressures in the presence of azelnidipine. After reperfusion, the coronary flow (CF) significantly increased in the presence of azelnidipine, but did not change with amlodipine after reperfusion. A positive inotropic effect was observed after treatment with both calcium antagonists. Ischemia significantly decreased the percentage of segment shortening (%SS) in all groups. Treatment with both calcium antagonists significantly increased %SS after reperfusion, although highenergy phosphate levels did not improve in the presence of calcium antagonists 60 min after reperfusion. Mortality with azelnidipine was significantly lower than that with 0.3 mg/kg amlodipine immediately after reperfusion. In conclusion, improvement in myocardial stunning after pretreatment with azelnidipine is associated with an increase in CF after reperfusion. The negative chronotropic action may have contributed to decreased mortality due to reperfusion arrhythmias. Azelnidipine is more beneficial than amlodipine and may provide an additional advantage to patients with angina and hypertension.

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Azelnidipine and Amlodipine: a Comparison of Their Pharmacokinetics and Effects on Ambulatory Blood Pressure.

Cited by 106 publications

References 28 publications

Anti-Atherogenic Effects of the Combination Therapy with Olmesartan and Azelnidipine in Diabetic Apolipoprotein E-Deficient Mice

Anti-Atherogenic Effects of the Combination Therapy with Olmesartan and Azelnidipine in Diabetic Apolipoprotein E-Deficient Mice

A randomized, double-blind, four-arm parallel-group study of the efficacy and safety of azelnidipine and olmesartan medoxomil combination therapy compared with each monotherapy in Japanese patients with essential hypertension: the REZALT study

Comparative Effects of Azelnidipine and Amlodipine on Myocardial Function and Mortality After Ischemia/Reperfusion in Dogs

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