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https://www.readbyqxmd.com/read/28513286/azelnidipine-is-a-useful-medication-for-the-treatment-of-heart-failure-preserved-ejection-fraction
#1
Shunsuke Kiuchi, Shinji Hisatake, Takayuki Kabuki, Takashi Oka, Shintaro Dobashi, Takahiro Fujii, Takanori Ikeda
BACKGROUND: The optimal therapy in patients with heart failure preserved ejection fraction (HFpEF) and hypertension (HT) has not been revealed. The beta blocker (BB) and the renin angiotensin aldosterone system inhibitor (RAAS-I) are recommend as class IIa in patients with HFpEF. The calcium channel blocker (CCB), a major anti-hypertensive drugs in Japan, is also recommend as class IIa in patients with HFpEF. However, the difference between azelnidipine, an L type CCB, and cilnidipine, an N type CCB, is unclear...
May 17, 2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28498149/inhibition-of-glutamate-release-by-cilnidipine-in-rat-cerebrocortical-nerve-terminals-synaptosomes
#2
Cheng Wei Lu, Tzu Yu Lin, Shu Kuei Huang, Su Jane Wang
Cilnidipine is an antihypertensive drug that was reported to have a neuroprotective profile. The present study aimed to investigate the effect of cilnidipine on the 4-aminopyridine (4-AP)-induced glutamate release in the rat cerebral cortex using isolated nerve terminals (synaptosomes). Cilnidipine reduced the release of glutamate release induced by 4-AP in a concentration-dependent manner. This inhibitory effect was associated with a reduction in the 4-AP-induced intrasynaptosomal Ca concentration elevation and was not because of an alteration of the synaptosomal membrane potential...
June 14, 2017: Neuroreport
https://www.readbyqxmd.com/read/28448181/blood-pressure-control-with-cilnidipine-treatment-in-japanese-post-stroke-hypertensive-patients-the-ca-attend-study
#3
Shiro Aoki, Naohisa Hosomi, Tomohisa Nezu, Tsukasa Teshima, Hitoshi Sugii, Shinobu Nagahama, Yoshiki Kurose, Hirofumi Maruyama, Masayasu Matsumoto
Blood pressure control is important in post-stroke hypertensive patients and antihypertensive treatment is recommended for such patients. Ca-channel blockers are recommended as the medications of choice for the treatment of post-stroke patients. Here, we report the results of a large-scale prospective post-marketing surveillance study of post-stroke hypertensive patients (n = 2667, male 60.4%, 69.0 ± 10.9 years) treated with cilnidipine, with regard to blood pressure control and adverse reactions. Cilnidipine treatment caused a decrease in both clinic and home blood pressures 2 months after the beginning of treatment, and the decreased blood pressure was maintained until the end of 12 months' observation...
2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28197288/serum-triglyceride-lowering-effect-of-cilnidipine-in-patients-with-essential-hypertension
#4
Prakash Kumar, Arijit Das, Satish Chandra, Manju Gari, U S P Keshri, Kusum Kumari
BACKGROUND: Many epidemiological studies have established the relationship between hypertension and dyslipidemia. Calcium channel blockers (CCBs) are one of the first-line drugs for newly diagnosed patients with essential hypertension. Cilnidipine as a newer CCB acting by blocking both L- and N-type calcium channels possesses additional beneficial effects apart from lowering blood pressure (BP). The aim of this study was to evaluate the effectiveness of cilnidipine in patients with essential hypertension with borderline dyslipidemia and its effects on lipid profile...
October 2016: Cardiology Research
https://www.readbyqxmd.com/read/28197287/effects-of-cilnidipine-on-heart-rate-and-uric-acid-metabolism-in-patients-with-essential-hypertension
#5
Arijit Das, Prakash Kumar, Abha Kumari, Satish Chandra, Manju Gari, Nidhi Singh, Debleena Dey
BACKGROUND: The relation between hypertension and hyperuricemia has been established by epidemiological studies. Calcium channel blockers are one of the first-line drugs for newly diagnosed patients with essential hypertension. Cilnidipine is a new calcium channel blocker acting by blocking both L- and N-type calcium channels. The aim of this study was to compare the effectiveness of amlodipine and cilnidipine in patients with essential hypertension and their effects on heart rate and serum uric acid levels...
October 2016: Cardiology Research
https://www.readbyqxmd.com/read/27823932/n-and-l-type-calcium-channels-blocker-cilnidipine-ameliorates-neuropathic-pain
#6
Shohei Yamamoto, Yuma Suzuki, Hideki Ono, Kazuhiko Kume, Masahiro Ohsawa
Cilnidipine is a dihydropyridine derivative that inhibits N-type and L-type voltage-gated Ca(2+) channels (VDCCs). We recently reported that a selective N-type VDCC blocker attenuated the spinal long-term potentiation (LTP) of C-fiber-evoked field potentials recorded in the spinal dorsal horn of rats, which served as a model for examining synaptic function during central pain sensitization. In this study, we investigated the effects of cilnidipine on the changes related to neuropathic pain induced by nerve injury...
December 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27754221/os-32-06-mouse-glomerular-injury-reduced-by-blocking-n-type-calcium-channel
#7
Yu Guan, Daisuke Nakano, Zhang Yifan, Akira Nishiyama
OBJECTIVE: Previous studies have indicated the beneficial effects of N-type calcium channel blocker, cilnidipine, on protecting renal podocyte injury in metabolic syndrome model rats. In the present study, we examined the effects of cilnidipine (L/N-type calcium channel blocker) and nifedipine (L-type calcium channel blocker) on the glomerular filtration barrier damage in the doxorubicin-induced nephropathy mice model. DESIGN AND METHOD: Balb/c mice (male, 5 week-old) were treated with vehicle (n = 5), doxorubicin (20 mg/kg, i...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27734656/cilnidipine-next-generation-calcium-channel-blocker
#8
Mukesh Madhukar Shete
Hypertension is one of the most common conditions seen in primary care and a major public health problem in India. It can lead to various complications if not detected early and treated appropriately. As per the latest Eighth Joint National Committee (JNC 8) the goal BP in most hypertensive patients age <60 years should be <140/90 mmHg and treatment can be started by selecting drugs from among 4 specific medication classes i.e. angiotensin converting enzyme inhibitor (ACEI) or angiotensin receptor blocker (ARB), calcium channel blocker (CCB) or diuretics...
April 2016: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/27696904/investigational-calcium-channel-blockers-for-the-treatment-of-hypertension
#9
REVIEW
J Tamargo, Luis Miguel Ruilope
Voltage-gated Ca(2+) channels are the primary route of Ca(2+) entry in vascular smooth muscle cells, playing a key role in the regulation of arterial tone and blood pressure. Since the 60´s, L-type Ca(2+) channel blockers (CCBs) have been widely used for the treatment of hypertension. Areas covered: T-type Ca(2+) channels regulate vascular tone in small-resistance vessels and aldosterone secretion, and N-type channels expressed in sympathetic nerve terminals regulate the release of neurotransmitters. We performed a literature search in MEDLINE, PubMed and ClinicalTrials...
November 2016: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27643181/os-32-06-mouse-glomerular-injury-reduced-by-blocking-n-type-calcium-channel
#10
Yu Guan, Daisuke Nakano, Zhang Yifan, Akira Nishiyama
OBJECTIVE: Previous studies have indicated the beneficial effects of N-type calcium channel blocker, cilnidipine, on protecting renal podocyte injury in metabolic syndrome model rats. In the present study, we examined the effects of cilnidipine (L/N-type calcium channel blocker) and nifedipine (L-type calcium channel blocker) on the glomerular filtration barrier damage in the doxorubicin-induced nephropathy mice model. DESIGN AND METHOD: Balb/c mice (male, 5 week-old) were treated with vehicle (n = 5), doxorubicin (20 mg/kg, i...
September 2016: Journal of Hypertension
https://www.readbyqxmd.com/read/27515419/on-the-top-of-arb-n-l-type%C3%A2-ca-channel-blocker-leads-to-less-elevation-of-aldosterone
#11
Tadashi Konoshita, Saori Kaeriyama, Machi Urabe, Takahiro Nakaya, Mika Yamada, Mai Ichikawa, Katsushi Yamamoto, Satsuki Sato, Michiko Imagawa, Miki Fujii, Yasukazu Makino, Yasuo Zenimaru, Shigeyuki Wakahara, Jinya Suzuki, Tamotsu Ishizuka, Hiroyuki Nakamura
The activation of the renin-angiotensin system (RAS) is one of the unfavourable characteristics of calcium channel blocker (CCB). N type calcium channel is thought to be involved in renin gene transcription and adrenal aldosterone release. Accordingly, N/L type CCB has a possibility of less elevation of plasma aldosterone concentrations (PAC) among CCBs. In a monotherapy study, we had already demonstrated that N/L type CCB leads to less activation of the RAS compared with L type CCB. The objective of this study is to substantiate the hypothesis that at the condition of additive administration on the top of an angiotensin receptor blocker (ARB), still N/L type CCB leads to less elevation of PAC compared with L type one...
October 2016: Bioscience Reports
https://www.readbyqxmd.com/read/27426453/study-of-the-structures-of-photodegradation-impurities-and-pathways-of-photodegradation-of-cilnidipine-by-liquid-chromatography-q-orbitrap-mass-spectrometry
#12
Hongxia Zeng, Fan Wang, Bingqi Zhu, Weihui Zhong, Weiguang Shan, Jian Wang
RATIONALE: The structures of photodegradation impurities in cilnidipine were studied by liquid chromatography/Q-Orbitrap mass spectrometry (LC/Q-Orbitrap MS) for the further improvement of the official monographs in Pharmacopoeias. The complete fragmentation patterns of impurities were investigated to obtain their structural information. Two pathways of photodegradation of cilnidipine were also explored to clarify the source of impurities in cilnidipine. METHODS: Chromatographic separation was performed on a Boston Group C18 column (250 mm × 4...
August 15, 2016: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/27325120/l-n-type-ca-2-channels-blocker-cilnidipine-ameliorated-the-repolarization-abnormality-in-a-chronic-hemodialysis-patient
#13
Xin Cao, Yuji Nakamura, Takeshi Wada, Hiroko Izumi-Nakaseko, Kentaro Ando, Atsushi Sugiyama
A 53-year-old woman with end-stage renal disease and hypertension, who had received regular artificial hemodialysis for 10 years, has been treated with candesartan in a dose of 8 mg/day against her hypertension, but premature ventricular contractions were often observed during the hemodialysis. QT interval was 445 ms before hemodialysis, which was prolonged to 515 ms immediately after it, possibly reflecting the presence of reduced repolarization reserve in her heart. Since the blood pressure was often elevated to >160 mmHg before the hemodialysis, a daily dose of an L/N-type Ca(2+) channels blocker cilnidipine of 5 mg/day was added...
January 2017: Heart and Vessels
https://www.readbyqxmd.com/read/27273361/ablation-of-the-n-type-calcium-channel-ameliorates-diabetic-nephropathy-with-improved-glycemic-control-and-reduced-blood-pressure
#14
Shoko Ohno, Hideki Yokoi, Kiyoshi Mori, Masato Kasahara, Koichiro Kuwahara, Junji Fujikura, Masaki Naito, Takashige Kuwabara, Hirotaka Imamaki, Akira Ishii, Moin A Saleem, Tomohiro Numata, Yasuo Mori, Kazuwa Nakao, Motoko Yanagita, Masashi Mukoyama
Pharmacological blockade of the N- and L-type calcium channel lessens renal injury in kidney disease patients. The significance of specific blockade of α1 subunit of N-type calcium channel, Cav2.2, in diabetic nephropathy, however, remains to be clarified. To examine functional roles, we mated Cav2.2(-/-) mice with db/db (diabetic) mice on the C57BLKS background. Cav2.2 was localized in glomeruli including podocytes and in distal tubular cells. Diabetic Cav2.2(-/-) mice significantly reduced urinary albumin excretion, glomerular hyperfiltration, blood glucose levels, histological deterioration and systolic blood pressure (SBP) with decreased urinary catecholamine compared to diabetic Cav2...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27194426/comparison-of-anti-anginal-effect-of-cilnidipine-with-those-of-nicardipine-and-nifedipine-in-the-vasopressin-induced-angina-model-of-rats
#15
Xin Cao, Yuji Nakamura, Takeshi Wada, Hiroko Izumi-Nakaseko, Kentaro Ando, Bingmei Zhu, Bin Xu, Akira Takahara, Masaki Saitoh, Atsushi Sugiyama
We assessed the anti-anginal effects of cilnidipine in comparison with those of nicardipine and nifedipine (1 and 10 µg/kg, n = 6 for each drug) or vehicle (n = 6) by using the vasopressin-induced angina model of rats. The administration of vasopressin (0.5 IU/kg, i.v.) to the rats depressed the S-wave level of the electrocardiogram reflecting the presence of subendocardial ischemia, whereas it significantly increased the mean blood pressure, resulting in the decrease of the heart rate and the prolongation of the PR interval possibly through a reflex-mediated increase in vagal tone...
December 2016: Heart and Vessels
https://www.readbyqxmd.com/read/26845200/a-chiral-lc-ms-ms-method-for-the-stereospecific-determination-of-efonidipine-in-human-plasma
#16
Man Liu, Ming Deng, Dan Zhang, Xiaolin Wang, Jingyi Ma, Hongna Zhao, Lina Zhang, Yang Tong, Huichen Liu
Efonidipine hydrochloride is a new generation dihydropyridine Ca(2+) channel blocker designed to inhibit both T-type and L-type Ca(2+) channels. Efonidipine possesses a chiral carbon and is clinically administered as a racemate. In the present study, an enantioselective and sensitive LC-MS/MS method of determining efonidipine enantiomers in human plasma was developed and validated to characterize the stereoselective pharmacokinetics. Plasma samples were processed by liquid-liquid extraction (LLE). Chiral separation was optimized on a CHIRALPAK(®) ID column using an isocratic mobile phase of acetonitrile/water (60:40, v/v)...
April 15, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/26820407/comparison-of-direct-effects-of-clinically-available-vasodilators-nitroglycerin-nifedipine-cilnidipine-and-diltiazem-on-human-skeletonized-internal-mammary-harvested-with-ultrasonic-scalpel
#17
COMPARATIVE STUDY
Shoji Fukuda, Yuji Nakamura, Koso Egi, Shunichiro Fujioka, Satoshi Nagasaka, Pham Ngoc Minh, Koji Toguchi, Takeshi Wada, Hiroko Izumi-Nakaseko, Kentaro Ando, Tetsuya Mizoue, Kenji Takazawa, Shigeru Hosaka, Atsushi Sugiyama
Direct vasodilator effects of nitroglycerin, nifedipine, cilnidipine and diltiazem on human skeletonized internal mammary artery graft harvested with ultrasonic scalpel were assessed in the presence of 0.1 or 0.2 µM of noradrenaline. Ring preparations were made of distal end section of the bypass grafts, and those dilated by acetylcholine were used for assessment. Each drug dilated the artery in a concentration-related manner (0.01-10 µM, n = 6 for each drug) with a potency of nitroglycerin > nifedipine = cilnidipine > diltiazem...
October 2016: Heart and Vessels
https://www.readbyqxmd.com/read/26676157/an-open-label-parallel-group-study-to-assess-the-effects-of-amlodipine-and-cilnidipine-on-pulse-wave-velocity-and-augmentation-pressures-in-mild-to-moderate-essential-hypertensive-patients
#18
Rama Mohan Pathapati, Sujith Tumkur Rajashekar, Madhavulu Buchineni, Rajesh Kumar Meriga, Chirra Bhakthavasthala Reddy, Kolla Praveen Kumar
INTRODUCTION: Hypertension is a major cardiovascular risk factor, which affects both large and small arteries. Because of the associated morbidity and mortality and the cost to society, it is an important public health challenge. Population based studies have reported that large artery stiffness is an important determinant of cardiovascular events and mortality in general population and in patients with hypertension. This study was designed to compare the effects of 8 weeks blood pressure control using Amlodepine and cilnidipine on haemodynamic parameters and vascular indices in mild to moderate hypertensive patients...
November 2015: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/26664207/reduction-of-microalbuminuria-in-type-2-diabetes-mellitus-with-angiotensin-converting-enzyme-inhibitor-alone-and-with-cilnidipine
#19
V K Singh, A Mishra, K K Gupta, R Misra, M L Patel, Shilpa
The aim of our study was to find out the antiproteinuric effect of enalapril angiotensin-converting enzyme (ACE inhibitor) alone or in combination with cilnidipine in patients with type-2 diabetes mellitus. The study was conducted on 71 patients with type-2 diabetes mellitus patients with hypertension and microalbuminuria. They were divided into two groups randomly as follows: Group I (enalaprilalone, n = 36) and Group II (enalapril with cilnidipine, n = 35). In both the groups, baseline 24 h urinary albumin was estimated and was repeated every 3 months upto 1-year...
November 2015: Indian Journal of Nephrology
https://www.readbyqxmd.com/read/26245661/calcium-channel-blockers-benefits-upon-vascular-biology-in-hypertensive-patients
#20
Daniel Duda-Seiman, Corina Duda-Seiman, Florin Borcan, Livia-Cristina Borcan, Silvia Mancas, Speranta Avram
Calcium channel blockers (CCB) are widely used in cardiovascular medicine expressing high hopes upon decreasing cardiovascular risk, morbidity and mortality. Here, the potency of CCBs on 58 Romanian asymptomatic hypertensive patients, with no atherothrombotic cardiovascular disease, was studied by clinical and in silico methods. In our study, arterial elasticity/stiffness was assessed; anthropometric, metabolic (lipidic) parameters were quantified. We concluded that lercanidipine 10 mg once daily, during three weeks, is able to dramatically improve central aortic systolic blood pressure, aortic pulse wave velocity...
2015: Cardiovascular & Hematological Agents in Medicinal Chemistry
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