Antihypertensive effect of NZ-105, a novel dihydropyridine derivative

Masuda, Yuichi; Sakai, Toshinori; Sakashita, Mitsuaki; Takeguchi, Midori; Takahashi, Tamayo; Arakawa, Chizuru; Hibi, Morihide; Tanaka, Sakura; Shigenobu, Koki; Kasuya, Yutaka

doi:10.1016/s0021-5198(19)57638-7

Cited by 4 publications

(5 citation statements)

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“… 18) In experiments with spontaneously hypertensive rats, the hypotensive action of NZ-105 (efonidipine; 5 mg/kg) peaked at 3 hours and lasted for more than 9 hours, while that of nicardipine (5 mg/kg) peaked at 0.5 hours and lasted for 3 hours. 11) A pharmacodynamic study showed that the binding affinity of 3 H-efonidipine for DHP receptors in rabbit aortic microsomes was 5.7-fold less potent than that of 3 H-nitrendipine, and the dissociation constant (K d ) of 3 H-efonidipine (4.48 nM) was approximately 6 times larger than that of 3 H-nitrendipine (0.79 nM). 19) On the basis of these experimental results, efonidipine has been considered to belong to the group of slow-onset and long-lasting CCB.…”

Section: Discussionmentioning

confidence: 99%

“…Ltd., Tokyo, Japan), which was administered once daily immediately after waking. 11) This drug has been known as an L- and T-type CCB that exerts long-lasting antihypertensive action. 11) 12) If the attending physician determined that the voluntary blood pressure levels had normalized during the follow-up period after treatment, a second 24-hour ABPM was performed.…”

Section: Methodsmentioning

confidence: 99%

“… 11) This drug has been known as an L- and T-type CCB that exerts long-lasting antihypertensive action. 11) 12) If the attending physician determined that the voluntary blood pressure levels had normalized during the follow-up period after treatment, a second 24-hour ABPM was performed. If either the voluntary blood pressure or second 24-hour ABPM had not normalized for 3 months, efonidipine was replaced with another antihypertensive agent.…”

Section: Methodsmentioning

confidence: 99%

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Effect of an L- and T-Type Calcium Channel Blocker on 24-Hour Systolic Blood Pressure and Heart Rate in Hypertensive Patients

et al. 2012

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Background and ObjectivesThe aim of this study was to evaluate the effects of an L- and T-type calcium channel blocker (CCB) on 24-hour systolic blood pressure (24-hour SBP) and heart rate (24-hour HR) profiles in essential hypertensive patients.Subjects and MethodsThirty-seven consecutive patients were enrolled in this study. The 24-hour SBP and HR were recorded before and after treatment with efonidipine (L- and T-type CCB, 40 mg), after waking. Changes in 24-hour SBP and HR and the diurnal to nocturnal SBP ratio were measured. The best-fit curves of changes in SBP and HR were depicted using a periodic function.ResultsThe mean 24-hour SBP and HR decreased significantly after treatment. The diurnal to nocturnal SBP ratio in dipper-type hypertension cases decreased from 16.7±6.1% to 8.3±9.8% (p<0.05), whereas in non-dipper hypertension cases, it increased from 2.3±2.9% to 7.7±5.1% (p<0.01). The antihypertensive effect was minimal at 5.0 hours after drug administration and it slowly recovered at a constant rate (2.1 mm Hg/h) over 12 hours in dipper cases. The median 24-hour changes in HR in the dipper and non-dipper cases were -2.3/min and -5.4/min, respectively. A continuous reduction in the change in HR was seen from 3.5 to 23 hours after drug administration.ConclusionThe antihypertensive action of efonidipine was characterized by a slow recovery of the SBP decrease at a constant rate (2.1 mm Hg/h) and a non-administration time dependent reduction in 24-hour HR.

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Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Effect of an L- and T-Type Calcium Channel Blocker on 24-Hour Systolic Blood Pressure and Heart Rate in Hypertensive Patients

et al. 2012

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“…The presence of a phosphate moiety at position 5 of the DHP ring confers distinctive pharmacological properties to efonidipine and distinguishes it from other DHP derivatives. It protects the kidneys from hypertension-induced damage by reducing intra-glomerular pressure [17][18][19]. Efonidipine also has a potent vasodilatory effect on cardiac smooth muscle and a prolonged hypotensive effect with a slow onset [20][21].…”

Section: Introductionmentioning

confidence: 99%

Development of ZnO-adorned glassy carbon electrode for voltammetric sensing and electro-kinetic investigations of antihypertensive drug efonidipine

Agarwal,

Jhankal,

Yadav

et al. 2023

Monatsh Chem

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The fast, accurate, and affordable determination of efonidipine (EFO) is the need of the time for human mental health. In this work, we proposed a ZnO-adorned glassy carbon electrode (ZnO/GCE) for the voltammetric sensing and electro-kinetic investigations of efonidipine in pharmaceutical samples. ZnOdecorated glassy carbon electrode exhibit enhanced electro-catalytic activity, higher surface area, rapid electron transfer rate, and enhanced electrical conductivity, these properties result in an ampli ed peak current response for the electro-reduction of EFO. The ZnO nanoparticles are synthesized by a simple and economical sol-gel method and characterized by XRD, SEM, and EDS techniques. The electro-kinetic studies of efonidipine on the ZnO fabricated glassy carbon electrode was investigated using CV, EIS, LSV, DPSV, and Chronocoulometry techniques. The diffusion-controlled electro-reduction of EFO produced three well-de ned peaks in the cyclic voltammograms. The various electro-kinetics parameters like diffusion coe cient (D o ), heterogeneous rate constant (K h ), electron transfer coe cient (α), and surface coverage (Γ) were evaluated and the mechanism of electro-reduction was proposed. The peak current in LSV and DPSV techniques shows a linear relationship with the concentration of EFO in the range of 0.14-0.98 µmolL − 1 with detection limits of 0.21 and 0.07 µmolL − 1 , respectively. The proposed ZnO/GCE sensor demonstrates a cost-effective and environmentally compatible approach for the detection of efonidipine in pharmaceutical samples.

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“…1 and Table 1), is a dihydropyridine derivative and Ca antagonist with a phosphonate skeleton, and was discovered by Nissan Chemical Industries. [16][17][18] The compound is already distributed in Japan by ZERIA Pharmaceutical Co., Ltd. and Shionogi & Co., Ltd. as a film-coated tablet called "Landel®," which is characteristically released gradually in comparison to existing Ca antagonists and exhibits a longer period of activity.…”

Section: Introductionmentioning

confidence: 99%

Developmental considerations for ethanolates with regard to stability and physicochemical characterization of efonidipine hydrochloride ethanolate

et al. 2015

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Antihypertensive effect of NZ-105, a novel dihydropyridine derivative

Cited by 4 publications

References 0 publications

Effect of an L- and T-Type Calcium Channel Blocker on 24-Hour Systolic Blood Pressure and Heart Rate in Hypertensive Patients

Effect of an L- and T-Type Calcium Channel Blocker on 24-Hour Systolic Blood Pressure and Heart Rate in Hypertensive Patients

Development of ZnO-adorned glassy carbon electrode for voltammetric sensing and electro-kinetic investigations of antihypertensive drug efonidipine

Developmental considerations for ethanolates with regard to stability and physicochemical characterization of efonidipine hydrochloride ethanolate

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