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Verapamil

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https://www.readbyqxmd.com/read/28938338/mortality-implications-of-lower-dbp-with-lower-achieved-systolic-pressures-in-coronary-artery-disease-long-term-mortality-results-from-the-international-verapamil-trandolapril-study-us-cohort
#1
Anita Wokhlu, Steven M Smith, Yan Gong, Eileen M Handberg, Islam Y Elgendy, Anthony A Bavry, Rhonda M Cooper-DeHoff, Carl J Pepine
OBJECTIVES: A goal SBP 120 mmHg or less reduced mortality in high-risk Systolic Blood Pressure Intervention Trial patients; however, mortality implications of concomitant DBP lowering in coronary artery disease (CAD) are uncertain. We examined the relationship between DBP lowering and all-cause mortality with lower achieved SBPs in a large cohort. METHODS: We categorized 17 131 hypertensive patients from the INternational VErapamil-trandolapril STudy US cohort, aged at least 50 years with CAD, by mean achieved SBP (<120, 120 to <130, 130 to <140, and ≥140 mmHg) and DBP tertiles (low, middle, and high per SBP category) during active follow-up...
September 21, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28935591/evidence-that-p-glycoprotein-inhibitor-elacridar-loaded-nanocarriers-improve-epidermal-targeting-of-an-anticancer-drug-via-absorptive-cutaneous-transporters-inhibition
#2
Daniela V Giacone, Vanessa F M Carvalho, Soraia K P Costa, Luciana B Lopes
Because P-glycoprotein (P-gp) plays an absorptive role in the skin, its pharmacological inhibition represents a strategy to promote cutaneous localization of anticancer agents that serve as its substrates, improving local efficacy while reducing systemic exposure. Here, we evaluated the ability of a nanoemulsion (NE) co-encapsulating a P-gp inhibitor (elacridar) with the antitumor drug paclitaxel to promote epidermal targeting. Loaded NE displayed a nanometric size (45.2±4.0 nm) and negative zeta potential (-4...
September 18, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28929535/extracellular-acidosis-selectively-inhibits-pharmacomechanical-coupling-induced-by-carbachol-in-strips-of-rat-gastric-fundus
#3
Daniel Maia Nogueira de Oliveira, Francisco José Batista-Lima, Emanuella Carvalho Feitosa, Alexandre Havt, Moisés Tolentino Bento da Silva, Armênio Aguiar Dos Santos, Pedro Jorge Caldas Magalhães
Acute acidosis that results from short-term exercise delays gastric emptying in rats and decreases the responsiveness to carbachol in gastric fundus strips. The regulation of cytosolic Ca(2+) levels appears to be a mechanism of action of acidosis. The present study investigated the way in which acidosis interferes with gastric smooth muscle contractions. Rat gastric fundus isolated strips at pH 6.0 presented a lower magnitude of carbachol-induced contractions compared with preparations at pH 7.4. This lower magnitude was absent in carbachol-stimulated duodenum and KCl-stimulated gastric fundus strips...
September 19, 2017: Experimental Physiology
https://www.readbyqxmd.com/read/28928566/effect-of-verapamil-as-an-adjuvant-to-levobupivacaine-in-supraclavicular-brachial-plexus-block
#4
Sidharth Sraban Routray, Debasis Mishra, Daityari Routray, Kasturi Nanda
BACKGROUND: Many adjuvants have been used with local anesthetics to reduce the time of onset and prolong the duration of analgesia in brachial plexus blocks. However, few studies are there using verapamil as an adjuvant with levobupivacaine. AIMS: This study aims to study the effects of verapamil as adjuvant to levobupivacaine in supraclavicular block for upper extremity surgery. METHODS: In this double-blinded clinical trial, 60 American Society of Anesthesiologist Class I and II patients posted to undergo upper extremity surgery were divided into 2 different groups randomly...
July 2017: Anesthesia, Essays and Researches
https://www.readbyqxmd.com/read/28927342/expert-opinion-biomimetic-functionalized-surfaces-and-the-induction-of-bone-formation
#5
Ugo Ripamonti
Tissue engineering still needs to assign the molecular basis of pattern formation, tissue induction and morphogenesis: What next to morphogens and stem cells? Macroporous biomimetic matrices per se, without the addition of the soluble osteogenic molecular signals of the transforming growth factor-β (TGF-β) supergene family, initiate the induction of bone formation. Carving geometries within different calcium phosphate-based macroporous bioreactors we show that geometric cues imprinted within the macroporous spaces initiate the spontaneous induction of bone...
September 19, 2017: Tissue Engineering. Part A
https://www.readbyqxmd.com/read/28926677/ca-2-influxes-and-transmembrane-transport-are-essential-for-phytic-acid-degradation-in-mung-bean-sprouts
#6
Ting Zhou, Pei Wang, Runqiang Yang, Xinyue Wang, Zhenxin Gu
BACKGROUND: Phytic acid is considered as an antinutrient. Ca(2+) addition during germination has been proved to be an effective method for reducing phytic acid content in seeds. In this study, mung bean sprouts were treated with LaCl3 (La), verapamil (VP), ruthenium red (RR) and CaCl2 to explore the effect of Ca(2+) influxes on phytic acid degradation. RESULTS: 6 mM CaCl2 significantly improved extracellular and intracellular calcium precipitates and calcium content, elevated phytase and acid phosphatase activity and further enhanced phytic acid degradation...
September 19, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/28916530/elucidation-of-the-impact-of-p-glycoprotein-and-breast-cancer-resistance-protein-on-the-brain-distribution-of-catechol-o-methyltransferase-inhibitors
#7
Joana Bicker, Ana Fortuna, Gilberto Alves, Patricio Soares-da-Silva, Amilcar Falcao
P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) are clinically important efflux transporters that act cooperatively at the blood-brain barrier, limiting the entry of several drugs into the CNS and affecting their pharmacokinetics, therapeutic efficacy and safety. In the present study, the interactions of catechol-O-methyltransferase (COMT) inhibitors (BIA 9-1059, BIA 9-1079, entacapone, nebicapone, opicapone and tolcapone) with P-gp and BCRP were investigated in order to determine the contribution of these transporters in their access to the brain...
September 15, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28910660/toxic-effects-of-pb-2-entering-sperm-through-ca-2-channels-in-the-freshwater-crab-sinopotamon-henanense
#8
Na Li, Peng Xu, Wei-Xin Jing, Jiang-Shiou Hwang, Lan Wang
Lead (Pb) is a heavy metal that can damage animal sperm. To study the effects of Pb on calcium homeostasis and calcium channel in the sperm of freshwater crab Sinopotamon henanense, the induction of acrosome reaction (AR) and acrosin activity were investigated when crabs were exposed to different Pb concentrations (0, 3.675, 7.35, 14.7, 29.4 and 58.8mg/L) for 3, 5 and 7 d separately. Fluorescent probe Fluo-3/AM was loaded into the sperm, and [Ca(2+)] in the sperm was measured by fluorescence microscopy and using microplate reader...
September 4, 2017: Aquatic Toxicology
https://www.readbyqxmd.com/read/28905315/preliminary-studies-of-acute-cadmium-administration-effects-on-the-calcium-activated-potassium-skca-and-bkca-channels-and-na-k-atpase-activity-in-isolated-aortic-rings-of-rats
#9
Dalton V Vassallo, Camila C P Almenara, Gilson Brás Broseghini-Filho, Ariane Calazans Teixeira, David Chaves F da Silva, Jhuli K Angeli, Alessandra S Padilha
Cadmium is an environmental pollutant closely linked with cardiovascular diseases that seems to involve endothelium dysfunction and reduced nitric oxide (NO) bioavailability. Knowing that NO causes dilatation through the activation of potassium channels and Na(+)/K(+)-ATPase, we aimed to determine whether acute cadmium administration (10 μM) alters the participation of K(+) channels, voltage-activated calcium channel, and Na(+)/K(+)-ATPase activity in vascular function of isolated aortic rings of rats. Cadmium did not modify the acetylcholine-induced relaxation...
September 13, 2017: Biological Trace Element Research
https://www.readbyqxmd.com/read/28901803/in-vitro-activity-of-calcium-channel-blockers-in-combination-with-conventional-antifungal-agents-against-clinically-important-filamentous-fungi
#10
Mónika Homa, Kinga Hegedűs, Ádám Fülöp, Vanessza Wolfárt, Shine Kadaikunnan, Jamal M Khaled, Naiyf S Alharbi, Csaba Vágvölgyi, László Galgóczy
Despite the current therapeutic options, filamentous fungal infections are associated with high mortality rate especially in immunocompromised patients. In order to find a new potential therapeutic approach, the in vitro inhibitory effect of two antiarrhythmic agents, diltiazem and verapamil hydrochloride were tested against different clinical isolates of ascomycetous and mucoralean filamentous fungi. The in vitro combinations of these non-antifungal drugs with azole and polyene antifungal agents were also examined...
September 2017: Acta Biologica Hungarica
https://www.readbyqxmd.com/read/28899749/cyp4a-cyp2c-modulation-of-the-interaction-of-calcium-channel-blockers-with-cyclosporine-on-edhf-mediated-renal-vasodilations-in-rats
#11
Safaa H Hammoud, Amal G Omar, Assaad A Eid, Mahmoud M El-Mas
The endothelium-derived hyperpolarizing factor (EDHF) serves as a back-up mechanism that compensates for reduced nitric oxide (NO)/prostanoids bioavailability. Here we investigated whether (i) under conditions of vascular endothelium dysfunction, the immunosuppressant drug cyclosporine (CSA) upregulates EDHF-dependent renal vasodilations through altering CYP4A/CYP2C signaling, and (ii) calcium channel blockers modulate the CSA/EDHF/CYP interaction. Rats were treated with CSA, verapamil, nifedipine, or their combinations for 7days...
September 9, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28895074/in-vitro-comparison-of-the-role-of-p-glycoprotein-and-breast-cancer-resistance-protein-on-direct-oral-anticoagulants-disposition
#12
Sophie Hodin, Thierry Basset, Elodie Jacqueroux, Olivier Delezay, Anthony Clotagatide, Nathalie Perek, Patrick Mismetti, Xavier Delavenne
BACKGROUND: Pharmacokinetics of direct oral anticoagulants (DOACs) are influenced by ATP-binding cassette (ABC) transporters such as P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). OBJECTIVES: To better understand the role of transporters in DOAC disposition, we evaluated and compared the permeabilities and transport properties of these drugs. METHODS: Bidirectional permeabilities of DOACs were investigated across Caco-2 cells monolayer...
September 11, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28889243/a-high-throughput-qcm-chip-configuration-for-the-study-of-living-cells-and-cell-drug-interactions
#13
Haibo Shen, Tiean Zhou, Jiajin Hu
In this study, we present a novel design of interference-free, negligible installation-induced stress, suitable for the fabrication of high-throughput quartz crystal microbalance (HQCM) chips. This novel HQCM chip configuration was fabricated using eight independent yet same-batch quartz crystal resonators within a common glass substrate with eight through-holes of diameter slightly larger than that of the quartz resonator. Each quartz resonator's rim was adhered to the inner part of the through-hole via silicone glue to form the rigid (quartz)-soft (silicone)-rigid (glass) structure (RSRS) which effectively eliminates the acoustic couplings among different resonators and largely alleviates the installation-induced stresses...
September 9, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28884083/hydro-alcoholic-extract-of-matricaria-recutita-exhibited-dual-anti-spasmodic-effect-via-modulation-of-ca-2-channels-no-and-pka2-kinase-pathway-in-rabbit-jejunum
#14
Hamidreza Yazdi, Akhtar Seifi, Shima Changizi, Vahid Khori, Fatemeh Hossini, Ali Davarian, Yahya Jand, Ayesheh Enayati, Masumeh Mazandarani, Fateme Nanvabashi
OBJECTIVE: Several studies have shown the antispasmodic activity of Matricariarecutita without detailing the underlying mechanism(s). The present study was designed to determine whether the antispasmodic mechanisms of M. recutita extract mediated via histaminergic/cholinergic receptors, Ca(2+)channels, activation of PKA2 and NO release in isolated rabbit jejunum. MATERIALS AND METHODS: The concentration- dependent (3 × 10(-3)-1.3 × 10(-2) mg/ml) antispasmodic effect of the hydro-alcoholic extract of M...
July 2017: Avicenna Journal of Phytomedicine
https://www.readbyqxmd.com/read/28878678/verapamil-blocks-scopolamine-enhancement-effect-on-memory-consolidation-in-passive-avoidance-task-in-rats
#15
Verónica Giménez De Béjar, María Caballero Bleda, Natalija Popović, Miroljub Popović
Our recent data have indicated that scopolamine, a non-selective muscarinic receptor antagonist, improves memory consolidation, in a passive avoidance task, tested in rats. It has been found that verapamil, a phenylalkylamine class of the L-type voltage-dependent calcium channel antagonist, inhibits [3H] N-methyl scopolamine binding to M1 muscarinic receptors. However, there are no data about the effect of verapamil on memory consolidation in the passive avoidance task, in rats. The purpose of the present study was to examine the effects of verapamil (0...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28868071/verapamil-and-vasospastic-angina-underuse-in-the-elderly-population
#16
Xavier Humbert, Vincent Roule, Paul Milliez, Joachim Alexandre
No abstract text is available yet for this article.
July 2017: Journal of Geriatric Cardiology: JGC
https://www.readbyqxmd.com/read/28868038/quantitative-comparison-of-effects-of-dofetilide-sotalol-quinidine-and-verapamil-between-human-ex-vivo-trabeculae-and-in-silico-ventricular-models-incorporating-inter-individual-action-potential-variability
#17
Oliver J Britton, Najah Abi-Gerges, Guy Page, Andre Ghetti, Paul E Miller, Blanca Rodriguez
Background:In silico modeling could soon become a mainstream method of pro-arrhythmic risk assessment in drug development. However, a lack of human-specific data and appropriate modeling techniques has previously prevented quantitative comparison of drug effects between in silico models and recordings from human cardiac preparations. Here, we directly compare changes in repolarization biomarkers caused by dofetilide, dl-sotalol, quinidine, and verapamil, between in silico populations of human ventricular cell models and ex vivo human ventricular trabeculae...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28866469/l-type-vdccs-participate-in-behavioral-ltp-and-memory-retention
#18
Yuan-Yuan Han, Xiao-Dong Wang, Li Liu, Hong-Mei Guo, Wei Cong, Wen-Wen Yan, Jun-Ni Huang, Peng Xiao, Chu-Hua Li
Although L-type voltage-dependent calcium channels (VDCCs) have been reported to display different even contrary actions on cognitive functions and long-term potentiation (LTP) formation, there is little information regarding the role of L-type VDCCs in behavioral LTP, a learning-induced LTP model, in the intact brain of freely behaving animals. Here we investigated the effects of verapamil, a non-selective blocker of L-type VDCCs, on behavioral LTP and cognitive functions. Population spikes (PS) were recorded by using electrophysiological methods to examine the role of verapamil in behavioral LTP in the hippocampal dentate gyrus (DG) region...
September 1, 2017: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28827974/ex-vivo-antispasmodic-activity-of-aqueous-extract-of-flowers-of-muntingia-calabura-linn-on-excised-rabbit-s-jejunum
#19
Kannan Vadivel, Gollapudi Sandeep Kumar, Sitty Manohar Babu
OBJECTIVE: The present study has been undertaken with the main objective of evaluating the aqueous extract of flowers of Muntingia calabura for antispasmodic activity on isolated rabbit's jejunum. MATERIALS AND METHODS: The study was carried out on isolated rabbit's jejunum preparations. The aqueous extract of flowers of M. calabura was applied in different doses by cumulative manner without washing the tissue. Spontaneous contractions abolished by the extract were recorded...
July 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28821850/comparative-metabonomics-of-wenxin-keli-and-verapamil-reveals-differential-roles-of-gluconeogenesis-and-fatty-acid-%C3%AE-oxidation-in-myocardial-injury-protection
#20
Miaomiao Jiang, Qiuying Wang, Jingrui Chen, Yanan Wang, Guanwei Fan, Yan Zhu
Metabonomics/metabolomics is a rapid technology for comprehensive profiling of small molecule metabolites in cells, tissues, or whole organisms, the application of which has led to understanding pathophysiologic mechanisms of cardiometabolic diseases, defining predictive biomarkers for those diseases, and also assessing the efficacious effects of incident drugs. In this study, proton nuclear magnetic resonance (NMR)-based metabonomics was employed to identify the metabolic changes in rat plasma caused by myocardial ischemia-reperfusion injury (MIRI), and to compare the metabolic regulatory differences between traditional Chinese medicine Wenxin Keli (WXKL) and Western medicine verapamil...
August 18, 2017: Scientific Reports
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