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calcium channel blocker

Chia-Wen Hsu, Jui-Hua Hsieh, Ruili Huang, Dirk Pijnenburg, Thai Khuc, Jon Hamm, Jinghua Zhao, Caitlin Lynch, Rinie van Beuningen, Xiaoqing Chang, Rene Houtman, Menghang Xia
Chemicals that alter normal function of farnesoid X receptor (FXR) have been shown to affect the homeostasis of bile acids, glucose, and lipids. Several structural classes of environmental chemicals and drugs that modulated FXR transactivation were previously identified by quantitative high-throughput screening (qHTS) of the Tox21 10K chemical collection. In the present study, we validated the FXR antagonist activity of selected structural classes, including avermectin anthelmintics, dihydropyridine calcium channel blockers, 1,3-indandione rodenticides, and pyrethroid pesticides, using in vitro assay and quantitative structural-activity relationship (QSAR) analysis approaches...
October 20, 2016: Toxicology and Applied Pharmacology
George L Bakris, John M Burkart, Eric D Weinhandl, Peter A McCullough, Michael A Kraus
Hypertension is a cardinal feature of end-stage renal disease (ESRD). Hypertensive nephropathy is the primary cause of ESRD for nearly 30% of patients, and the prevalence of hypertension is >85% in new patients with ESRD. In contemporary hemodialysis (HD) patients, mean predialysis systolic blood pressure (SBP) is nearly 150mmHg, and about 70%, 50%, and 40% use β-blockers, calcium channel blockers, and renin-angiotensin system inhibitors, respectively. Predialysis SBP generally exhibits a U-shaped association with mortality risk...
November 2016: American Journal of Kidney Diseases: the Official Journal of the National Kidney Foundation
Alessandro Rubini, Vincenzo Catena, Daniele Del Monte, Gerardo Bosco
CONTEXT: Calcium channel blockers may theoretically exhibit relaxing effects not only on vascular smooth muscle but also on airway smooth muscle. OBJECTIVE: To investigate possible effects of nifedipine on respiratory mechanics in the rat. METHODS: Respiratory system mechanical parameters were measured by the end-inflation occlusion method in the rat in vivo before and after the intraperitoneal administration of nifedipine. RESULTS: We found that nifedipine affects respiratory mechanics, inducing a reduction of airway resistance and of respiratory system elastance, probably because of a relaxing action on airway and parenchimal smooth muscle cells...
October 21, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Donal Melanaphy, Christpher D Johnson, Maxim Kustov, Connall Watson, Lyudmyla Borysova, Theodore Burdyga, Alexander V Zholos
Transient receptor potential melastatin 8 (TRPM8) is the principal cold and menthol receptor channel. Characterized primarily for its cold sensing role in sensory neurons, it is expressed and functional in several non-neuronal tissues, including vasculature. We previously demonstrated that menthol causes vasoconstriction and vasodilatation in isolated arteries, depending on vascular tone. Here we investigated calcium's role in responses mediated by TRPM8 ligands in rat tail artery myocytes using patch-clamp electrophysiology and ratiometric Ca(2+) recording...
October 7, 2016: American Journal of Physiology. Heart and Circulatory Physiology
Sheng-Jie Shiue, Chi-Hsu Wang, Tao-Yeuan Wang, Yi-Chun Chen, Jen-Kun Cheng
OBJECTIVE: T-type channel (TCC) CaV3.2 plays a pivotal role in pain transmission. In this study, we examined the effects of intrathecal TCC blockers on CaV3.2 expression in a L5/6 spinal nerve ligation (SNL) pain model. The neurotoxicity of TCC blockers were also evaluated. METHODS: Male Sprague-Dawley rats (200-250 g) were used for right L5/6 SNL to induce neuropathic pain. Intrathecal infusion of saline or TCC blockers [mibefradil (0.7 μg/h) or ethosuximide (60 μg/h)] was started after surgery for 7 days...
October 17, 2016: Acta Anaesthesiologica Taiwanica: Official Journal of the Taiwan Society of Anesthesiologists
A Muruganathan, Mangesh Tiwaskar
While the incidence and prevalence of stroke is gradually decreasing in the western world, a parallel increase is seen in the developing world. It is a matter of special concern to us as approximately 20-30% of stroke occur in people younger than 45 years in India. Indians are prone to higher stroke risk because of urbanization, diabetes, cigarette smoking and high incidence of hypertension. Unfortunately, there is an inadequate awareness about the risk of stroke with hypertension among general public. Hypertension is considered to be the most important risk factor for stroke, and all forms of hypertension are associated with an increased risk of both ischemic and haemorrhagic stroke...
September 2016: Journal of the Association of Physicians of India
M Nagai, K Dote, M Kato, S Sasaki, N Oda, E Kagawa, Y Nakano, A Yamane, Y Kubo, T Higashihara, S Miyauchi, W Harada, H Masuda
In a cross-sectional study, visit-to-visit blood pressure (BP) variability was shown to be associated with artery remodelling. Here, we investigated the impact of visit-to-visit BP variability and average BP on the carotid artery remodelling progression in high-risk elderly according to different classes of antihypertension medication use/non-use. BP measurements and carotid ultrasound were performed in the common carotid artery in 164 subjects (mean age 79.7 years at baseline, 74.7% females) with one or more cardiovascular risk factors...
October 20, 2016: Journal of Human Hypertension
Ricardo Rodrigues Figueiredo, Andréia Aparecida Azevedo, Norma De Oliveira Penido
INTRODUCTION: Tinnitus is the perception of noise in the absence of an external source and is considered by most authors as a multifactorial symptom. A systematic review concerning the association of tinnitus and systemic arterial hypertension retrieved suggestions of a positive association, but the articles included failed to perform a detailed analysis on the theme. PURPOSE: To analyze the presence of arterial hypertension in tinnitus and non-tinnitus patients, to analyze differences between tinnitus impact and psychoacoustic measurements in hypertensive and normotensive patients, and to evaluate the association between the presence of tinnitus and the diverse antihypertensive drugs employed...
2016: Frontiers in Neurology
Almotasembellah Aljaafareh, Jose Ruben Valle, Yu-Li Lin, Yong-Fang Kuo, Gulshan Sharma
OBJECTIVES: Long-acting bronchodilators are mainstay treatment for moderate to severe chronic obstructive pulmonary disease. A growing body of evidence indicates an increased risk of cardiovascular events upon initiation of these medications. We hypothesize that this risk is higher in patients with chronic obstructive pulmonary disease who had a preexisting cardiovascular disease regardless of receipt of any cardiovascular medication. METHODS: A retrospective cohort of patients with a diagnosis of chronic obstructive pulmonary disease based on two outpatient visits or one inpatient visit for chronic obstructive pulmonary disease (International Classification of Diseases, 9th Edition, Clinical Modification codes 491...
2016: SAGE Open Medicine
Emmanuel Bourinet, Gerald W Zamponi
Venoms from various predatory species, such as fish hunting mollusks scorpions, snakes and arachnids contain a large spectrum of toxins that include blockers of voltage-gated calcium channels. These peptide blockers act by two principal manners - physical occlusion of the pore and prevention of activation gating. Many of the calcium channel-blocking peptides have evolved to tightly occupy their binding pocket on the principal pore forming subunit of the channel, often rendering block poorly reversible. Moreover, several of the best characterized blocking peptides have developed a high degree of channel subtype selectivity...
October 15, 2016: Neuropharmacology
Eun Joo Cho, Hae Young Lee, Ki Chul Sung, Sungha Park, Chang Gyu Park, Dong-Ju Choi, Jong Won Ha, Young Keun Ahn, Jinho Shin, Soon-Jun Hong, Soon Kil Kim, Wook-Jin Chung, Byung Su Yoo, Taek Jong Hong, Ho Joong Youn, Myeong-Chan Cho, Shung Chull Chae, Young Jo Kim, Chong-Jin Kim
BACKGROUND: The aim of this study was to compare 24-hour central blood pressure (24 hr c-BP) reduction efficacy between angiotensin II receptor blocker (ARB) combined with calcium channel blocker and with diuretics. METHODS: We conducted a prospective, randomized, double-blind trial in 220 hypertensive patients [mean age = 59.6 ± 12.3 years, men = 154(70%)]. Patients received losartan 50 mg monotherapy for 4 weeks, followed by additional use of amlodipine 5 mg (L/A group) or hydrochlorothiazide 12...
September 2016: Journal of Hypertension
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
Rha Seung-Woon, Choi Byoung Geol, Li Hu, Na Jin Oh, Choi Cheol Ung, Park Chang Gyu, Seo Hong Seog, Oh Dong Joo, Kim Yong Hoon, Her Ae-Young, Park Sang-Ho
OBJECTIVE: Recently several studies reported that anti-hypertensive drugs were associated with development of new-onset diabetes mellitus (NODM). However, data on the relationship between detailed prescription types and long-term incidence of NODM are still limited in Asian patients (pts). DESIGN AND METHOD: A total of 3,208 consecutive hypertension pts prescribed with calcium channel blockers (CCB) were enrolled with the exclusion of diabetic pts. Pts were divided into two groups according to the additional prescription of renin angiotensin system (RAS) blockers; 1) the CCB group (n = 1,987) and 2) CCB + RAS group (n = 1,221)...
September 2016: Journal of Hypertension
Chan Joo Lee, Jaewon Oh, Sang-Hak Lee, Seok-Min Kang, Donghoon Choi, Hyeon-Chang Kim, Sungha Park
OBJECTIVE: In most cases, the 5 first line drugs are recommended for management of hypertension without preference for one or the other. However, it is unclear whether different classes of anti-hypertensive agents have different effect on survival in low risk, uncomplicated hypertension. The aim of this study was to evaluate effects of 4 classes of first line anti-hypertensive agents on improving survival in patients with low risk, uncomplicated hypertension. DESIGN AND METHOD: Adult hypertensive patients without chronic kidney disease, end stage renal disease, diabetes mellitus, acute coronary syndrome, and heart failure in 2002 were selected from Korean National Health Insurance sample cohort consisting of one million subjects...
September 2016: Journal of Hypertension
Naoki Nakagawa, Keisuke Maruyama, Motoki Matsuki, Nobuyuki Sato, Kenjiro Kikuchi, Naoyuki Hasebe
OBJECTIVE: Uric acid is a risk factor for cardiovascular disease. We investigated the relationship between the change of urinary albumin excretion (UAE) and the changes of serum uric acid (SUA) during antihypertensive treatment in hypertensive patients with microalbuminuria as a subanalysis of the results of the NICE Combi (Nifedipine and Candesartan Combination) Study. DESIGN AND METHOD: A total of 86 subjects with essential hypertension with microalbuminuria (UAE < 300 mg•g-1 creatinine) were randomly assigned in a double-blind manner to a combination therapy group (standard-dose candesartan at 8 mg/day plus controlled-release (CR) nifedipine 20 mg/day) (n = 42) or an up-titrated monotherapy group (candesartan 12 mg/day) (n = 44) for 8 weeks of continuous treatment after initially receiving standard-dose candesartan (8 mg/day) monotherapy for 8 weeks (initial treatment)...
September 2016: Journal of Hypertension
Michal Behuliak, Michal Bencze, Anna Vavrinova, Ivana Vaneckova, Josef Zicha
OBJECTIVE: Voltage-dependent calcium channels (VDCCs) play an important role in two major abnormalities observed in spontaneously hypertensive rats (SHR) - hyperactivity of sympathetic nervous system (SNS) and enhanced Ca influx to vascular smooth muscle cells (VSMC). α2δ subunit of VDCC, which promotes surface trafficking and modulates the biophysical properties of VDCC, was identified as a critical component of increased L-type VDCC calcium currents in arterial myocytes of SHR. On the other hand, N-type VDCCs control a neurotransmitter release in the peripheral sympathetic nervous system and play an important role in sympathetic hyperactivity in SHR...
September 2016: Journal of Hypertension
David John Webb
Treatment-resistant hypertension (TRH) is defined as the failure to achieve an office BP target of <140/90 mmHg (<130/80 mmHg in patients with chronic kidney disease (CKD) or diabetes) in patients with hypertension (HT), despite adherence to at least 3 antihypertensive medications at optimal tolerated doses, ideally including a diuretic (Calhoun et al., Circulation 2008). TRH identifies patients with hard-to-treat HT, who might benefit from specialist investigation and treatment. Although some studies put the prevalence of TRH as >10%, these levels may be inflated by white-coat hypertension and poor adherence...
September 2016: Journal of Hypertension
William C Cushman
Beginning with the Veterans Administration (VA) Cooperative Hypertension Study of the 1960 s, blood pressure (BP) lowering with antihypertensive medications has been shown to reduce major cardiovascular (CV) outcomes, including coronary heart disease, stroke, heart failure (HF) and CV and all-cause mortality in randomized controlled CV outcome trials. Multiple drugs were usually required in these trials to lower BP in treated participants. Medication regimens in the early trials, including the VA trial, included a thiazide-type diuretic (TTD) as initial therapy...
September 2016: Journal of Hypertension
Kazuyuki Shimada
Stroke is known to frequently recur in patients with a history of cerebrovascular disease, and the control of hypertension is extremely important for the treatment of those patients. The robust relationship between the recurrent cerebrovascular disease and blood pressure control has been demonstrated in large-scale clinical studies. The antihypertensive drug therapy significantly reduces the recurrence rate of all types of cerebrovascular disease, incidences of myocardial infarction and all vascular events...
September 2016: Journal of Hypertension
Michael Weber
: Age is the most powerful cardiovascular risk factor. Based on a meta-analysis of a million control patients in hypertension trials, the Clinical Trialists Collaboration has estimated that doubling of major cardiac and stroke events occurs with age increments of < 10 years (1). Data from the ACCOMPLISH trial, which will be presented at this ISH meeting for the first time, show that patients aged > 70 (mean: 75.2), compared with those < 70 (mean: 63.7), had a 2.82-fold greater event rate for cardiovascular death and a 2...
September 2016: Journal of Hypertension
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