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nifedipine

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https://www.readbyqxmd.com/read/29158664/impact-of-baseline-blood-pressure-on-the-magnitude-of-blood-pressure-lowering-by-nifedipine-gastrointestinal-therapeutic-system-refreshing-the-wilder-s-principle
#1
Haijuan Hu, Jidong Zhang, Yan Wang, Zejun Tian, Demin Liu, Guangming Zhang, Guoqiang Gu, Hongmei Zheng, Ruiqin Xie, Wei Cui
Background: The objective of the study was to investigate the relationship between baseline blood pressure (BP) and the magnitude of BP reduction in patients with essential hypertension treated with nifedipine gastrointestinal therapeutic system (NGTS). Methods and patients: One hundred and thirty-eight patients with essential hypertension were enrolled in this prospective, single-arm, open-label study. NGTS was administered for 24 weeks to achieve target BP of 140/90 mmHg...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29155306/reverse-t3-interacts-with-%C3%AE-v%C3%AE-3-integrin-receptor-and-restores-enzyme-activities-in-the-hippocampus-of-hypothyroid-developing-rats-insight-on-signaling-mechanisms
#2
Juliana Tonietto Domingues, Daiane Cattani, Patricia Acordi Cesconetto, Bianka Alzira Nascimento de Almeida, Paula Peirozan, Guilherme Razzera, Fátima Regina Mena Barreto Silva, Regina Pessoa-Pureur, Ariane Zamoner
In the present study we provide evidence that 3,3',5'-triiodothyronine (reverse T3, rT3) restores neurochemical parameters induced by congenital hypothyroidism in rat hippocampus. Congenital hypothyroidism was induced by adding 0.05% propylthiouracil in the drinking water from gestation day 8 and continually up to lactation day 15. In the in vivo rT3 exposure, hypothyroid 12-day old pups were daily injected with rT3 (50 ng/kg body weight) or saline until day 14. In the ex vivo rT3 treatment, hippocampal slices from 15-day-old hypothyroid pups were incubated for 30 min with or without rT3 (1 nM)...
November 16, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/29147891/long-term-presence-of-angiotensin-ii-type-1-receptor-autoantibody-reduces-aldosterone-production-by-triggering-ca-2-overload-in-h295r-cells
#3
Jinghui Lei, Suli Zhang, Pengli Wang, Yang Liao, Jingwei Bian, Xiaochen Yin, Ye Wu, Lina Bai, Feng Wang, Xiaoli Yang, Huirong Liu
Preeclamptic women are reported to have inadequate plasma volume expansion coupled with a suppressed secretion of aldosterone; however, the specific mechanism of preeclampsia remains unclear. We demonstrated that the presence of long-term angiotensin II type 1 receptor autoantibody (AT1-AA) reduces aldosterone production by triggering a Ca(2+) overload in H295R cells. AT1-AA was discovered in preeclamptic women and reported to activate AT1R, and consequently elevate intracellular Ca(2+). We found that AT1-AA significantly prolonged the time of intracellular Ca(2+) elevation...
November 16, 2017: Immunologic Research
https://www.readbyqxmd.com/read/29146539/hyaluronan-decorated-liposomes-as-drug-delivery-systems-for-cutaneous-administration
#4
Silvia Franzé, Alessandro Marengo, Barbara Stella, Paola Minghetti, Silvia Arpicco, Francesco Cilurzo
The work aimed to evaluate the feasibility to design hyaluronic acid (HA) decorated flexible liposomes to enhance the skin penetration of nifedipine. Egg phosphatidylcholine (e-PC) based transfersomes (Tween 80) and transethosomes (ethanol) were prepared. HA was reacted with 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (HA-DPPE) and two molar ratios (0.5 and 3%) of conjugate with respect to e-PC were tested. The presence of HA significantly increased the packing order of the bilayer (as verified by differential scanning calorimetry), reducing both the encapsulation efficiency and the flexibility of the decorated liposomes in a dose-dependent manner...
November 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29129665/intravasation-of-sw620-colon-cancer-cell-spheroids-through-the-blood-endothelial-barrier-is-inhibited-by-clinical-drugs-and-flavonoids-in-vitro
#5
Silvio Holzner, Stefan Brenner, Atanas Georgiev Atanasov, Daniel Senfter, Serena Stadler, Chi Huu Nguyen, Adryan Fristiohady, Daniela Milovanovic, Nicole Huttary, Sigurd Krieger, Zsuzsanna Bago-Horvath, Oliver de Wever, Ioannis Tentes, Ali Özmen, Walter Jäger, Helmut Dolznig, Verena Maria Dirsch, Robert Michael Mader, Liselotte Krenn, Georg Krupitza
Mechanisms how colorectal cancer (CRC) cells penetrate blood micro-vessel endothelia and metastasise is poorly understood. To study blood endothelial cell (BEC) barrier breaching by CRC emboli, an in vitro assay measuring BEC-free areas underneath SW620 cell spheroids, so called "circular chemorepellent induced defects" (CCIDs, appearing in consequence of endothelial retraction), was adapted and supported by Western blotting, EIA-, EROD- and luciferase reporter assays. Inhibition of ALOX12 or NF-κB in SW620 cells or BECs, respectively, caused attenuation of CCIDs...
November 10, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29105520/preparation-and-characterization-of-textile-based-carrier-systems-for-anal-fissure-treatment
#6
A M Sarıışık, S Y Karavana, G C Türkoğlu, S Rençber, T Önder
Anal fissure is common and painful disease of anorectum. In this study, microparticles containing nifedipine and lidocaine HCl were prepared by spray drying and applied to bio-degradable and bio-stable tampons. Characterization of microparticles was determined by visual analyses, mass yield, particle size measurement, encapsulation efficiency, drug loading and in vitro drug release. Mass yield was between 5.5 and 45.9%. The particle size was between 15.1 and 26.8 µm. Encapsulation efficiency were 96.142 ± 5...
November 5, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/29098644/melts-of-octaacetyl-sucrose-as-oral-modified-release-dosage-forms-for-delivery-of-poorly-soluble-compound-in-stable-amorphous-form
#7
Dorota Haznar-Garbacz, Ewa Kaminska, Daniel Zakowiecki, Marek Lachmann, Kamil Kaminski, Grzegorz Garbacz, Przemysław Dorożyński, Piotr Kulinowski
The presented work describes the formulation and characterization of modified release glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model BCS (Biopharmaceutical Classification System) class II drug. The GSDFs were prepared by melting nifedipine together with octaacetyl sucrose. Dissolution profiles, measured under standard and biorelevant conditions, were compared to those obtained from commercially available formulations containing nifedipine such as modified release (MR) tablets and osmotic release oral system (OROS)...
November 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29097142/exploring-the-feasibility-of-the-use-of-biopolymers-as-a-carrier-in-the-formulation-of-amorphous-solid-dispersions-part-i-gelatin
#8
Timothy Pas, Bjorn Vergauwen, Guy Van den Mooter
Biopolymers have rarely been used so far as carriers in the formulation of amorphous solid dispersions (ASD) to overcome poor solubility of active pharmaceutical ingredients (APIs). In an attempt to enlarge our knowledge on this topic, gelatin, type 50PS was selected. A screening study was initiated in which twelve structurally different poorly soluble biopharmaceutical classification system (BCS) Class II drugs (carbamazepine, cinnarizine, diazepam, itraconazole, nifedipine, indomethacin, darunavir (ethanolate), ritonavir, fenofibrate, griseofulvin, ketoconazole and naproxen) were selected for evaluation...
October 31, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29089544/a-network-meta-analysis-on-the-beneficial-effect-of-medical-expulsive-therapy-after-extracorporeal-shock-wave-lithotripsy
#9
Tong-Xin Yang, Bang-Hua Liao, Yun-Tian Chen, Hong Li, Qing He, Qin-Yu Liu, Kun-Jie Wang
We applied a newly introduced method, network meta-analysis, to re-evaluate the expulsion effect of drugs including tamsulosin, doxazosin, nifedipine, terazosin and rowatinex after extracorporeal shock wave lithotripsy (ESWL) as described in the literature. A systematic search was performed in Medline, Embase and Cochrane Library for articles published before March 2016. Twenty-six studies with 2775 patients were included. The primary outcome was the number of patients with successful stone expulsion. The data were subdivided into three groups according to duration of follow-up...
October 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29079070/pharmacologic-interventions-for-intractable-and-persistent-hiccups-a-systematic-review
#10
Nick B Polito, Shawn E Fellows
BACKGROUND: Chlorpromazine is the only drug approved by the US Food and Drug Administration for the treatment of hiccups; however, many other pharmacologic treatments have been proposed for intractable and persistent hiccups. Currently, there is little evidence to support the use of one agent over another. OBJECTIVE: This review aims to identify literature concerning the use of pharmacologic treatments for intractable and persistent hiccups with the goal of evaluating therapies in terms of their level of evidence, mechanism of action, efficacy, dosing, onset of action, and adverse effects...
October 2017: Journal of Emergency Medicine
https://www.readbyqxmd.com/read/29061745/mechanism-of-action-of-miltefosine-on-leishmania-donovani-involves-the-impairment-of-acidocalcisomes-function-and-the-activation-of-the-sphingosine-dependent-plasma-membrane-ca-2-channel
#11
Andrea K Pinto-Martinez, Jessica Rodriguez-Durán, Xenon Serrano-Martin, Vanessa Hernandez-Rodriguez, Gustavo Benaim
Leishmania donovani is the causing agent of visceral leishmaniasis, a common infection that affects millions of people from the most underdeveloped countries. Miltefosine is the only oral drug to treat infections caused by L. donovani. Nevertheless, its mechanism of action is not well understood. While miltefosine inhibits the synthesis of phosphatidylcholine, and also affects the parasite mitochondrion inhibiting the cytochrome C oxidase, it is to be expected that this potent drug also produces its effect through other targets...
October 23, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29058012/taming-photo-induced-oxidation-degradation-of-dihydropyridine-drugs-through-cocrystallization
#12
Qihui Yu, Zhicheng Yan, Junjie Bao, Jian-Rong Wang, Xuefeng Mei
Cocrystallization of nifedipine (NFD) and isonicotinamide (INA) resulted in two monotropic cocrystal polymorphs. The thermodynamically more stable polymorph presents superior photostability compared to the other. Cocrystallization can be an efficient approach to address the stability deficit of dihydropyridine drugs.
October 23, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29050967/role-of-k-channels-in-regulating-spontaneous-activity-in-the-muscularis-mucosae-of-guinea-pig-bladder
#13
Ken Lee, Ayu Isogai, Minori Antoh, Shunichi Kajioka, Masatoshi Eto, Hikaru Hashitani
To explore the roles of various K(+) channels in regulating the spontaneous activity of bladder muscularis mucosae (MM) that is considered to play an important role in maintaining mucosal function. Effects of K(+) channel modulators on electrical and contractile activity in the guinea-pig bladder MM were examined using intracellular microelectrode and isometric tension recording. The MM predominately generated bursting spontaneous action potentials (SAPs) and phasic contractions (SPCs) that were blocked by nifedipine (1µM)...
October 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29048755/nifedipine-prevents-apoptosis-of-alcohol-exposed-first-trimester-trophoblast-cells
#14
Alan D Bolnick, Jay M Bolnick, Hamid-Reza Kohan-Ghadr, Brian A Kilburn, Michael Hertz, Jing Dai, Sascha Drewlo, D Randall Armant
BACKGROUND: Maternal alcohol abuse leading to fetal alcohol spectrum disorder (FASD) includes fetal growth restriction (FGR). Ethanol induces apoptosis of human placental trophoblast cells, possibly disrupting placentation and contributing to FGR in FASD. Ethanol facilitates apoptosis in several embryonic tissues, including human trophoblasts, by raising intracellular Ca(2+) . We previously found that acute ethanol exposure increases trophoblast apoptosis due to signaling from both intracellular and extracellular Ca(2+) ...
October 19, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29036433/left-ventricular-hypertrophy-predicts-cardiovascular-events-in-hypertensive-patients-with-coronary-artery-calcifications
#15
Chagai Grossman, Michael Levin, Nira Koren-Morag, Gill Bornstein, Avshalom Leibowitz, Ilan Ben-Zvi, Joseph Shemesh, Ehud Grossman
Background: Coronary artery calcification (CAC) is associated with increased cardiovascular (CV) risk. Left ventricular hypertrophy (LVH) is an independent risk factor for CV events. Our aim was to estimate the relative CV risk of LVH in the presence of CAC. Methods: We included asymptomatic hypertensive patients who were enrolled in the calcification arm of the INSIGHT (International Nifedipine Study Intervention as Goal for Hypertension Therapy). Patients had baseline echocardiography and computed tomography (CT) to assess CAC...
October 5, 2017: American Journal of Hypertension
https://www.readbyqxmd.com/read/29029261/selective-enhancement-of-domoic-acid-toxicity-in-primary-cultures-of-cerebellar-granule-cells-by-lowering-extracellular-na-concentration
#16
Anabel Pérez-Gómez, David Cabrera-García, Davide Warm, Ann M Marini, Javier Salas Puig, Maria Teresa Fernández-Sánchez, Antonello Novelli
Domoic acid (DOM) is an excitatory amino acid analog of kainic acid (KA) that acts through glutamic acid (GLU) receptors, inducing a fast and potent neurotoxic response. Here we present evidence for an enhancement of excitotoxicity following exposure of cultured cerebellar granule cells to DOM in the presence of lower than physiological Na+ concentrations. The concentration of DOM that reduced by 50% neuronal survival was ̴ 3 µM in Na+-free conditions and 16 µM in presence of a physiological concentration of extracellular Na+...
September 25, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28993436/efficacy-of-resveratrol-to-supplement-oral-nifedipine-treatment-in-pregnancy-induced-preeclampsia
#17
Jian Ding, Yan Kang, Yuqin Fan, Qi Chen
OBJECTIVE: Preeclampsia (PE) is a complication affecting pregnant women worldwide, which usually manifests as severe maternal hypertension. Resveratrol (RESV), a naturally existing polyphenol, is known to exhibit beneficial effects in cardiovascular disease including hypertension. We evaluated the outcome of treatment combining oral nifedipine (NIFE) and RESV against PE. DESIGN AND METHODS: Using a randomized group assignment, 400 PE patients were enrolled and received oral treatments of either NIFE + RESV or NIFE + placebo...
November 2017: Endocrine Connections
https://www.readbyqxmd.com/read/28979318/effect-of-crude-venom-of-odonthobuthus-doriae-scorpion-in-cell-culture-using-ion-channel-modulators
#18
Sainaz Ghasemi, Amir Ahmad Salarian, Abbas Zare Mirakabadi, Somayeh Jafarinejad, Mahmoud Ghazi-Khansari
Scorpion venom toxicity is one of the major medical concerns from old years, due to its influence on human activities and health. From many years ago a lot of researches established to examine different aspects of venom toxicity and its effects on different organs. During these years researchers are doing more specific studies on the cytotoxicity of scorpion venom. In Iran, Odonthobuthus doriae, the yellow scorpion is one of the major threats based on its neuro toxicity and severe pathophysiologic effects and researchers tried to find the mechanism of these neuro toxic effects...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28975698/dopamine-d4-receptor-activation-restores-ca1-ltp-in-hippocampal-slices-from-aged-mice
#19
Fangli Guo, Jianhua Zhao, Dandan Zhao, Jiangang Wang, Xiaofang Wang, Zhiwei Feng, Martin Vreugdenhil, Chengbiao Lu
Normal aging is characterized with a decline in hippocampal memory functions that is associated with changes in long-term potentiation (LTP) of the CA3-to-CA1 synapse. Age-related deficit of the dopaminergic system may contribute to impairment of CA1 LTP. Here we assessed how the modulation of CA1 LTP by dopamine is affected by aging and how it is dependent on the Ca(2+) source. In slices from adult mice, the initial slope of the field potential showed strong LTP, but in slices from aged mice LTP was impaired...
December 2017: Aging Cell
https://www.readbyqxmd.com/read/28974495/prenatal-hypoxia-induced-dysfunction-in-cerebral-arteries-of-offspring-rats
#20
Jiaqi Tang, Na Li, Xueyi Chen, Qinqin Gao, Xiuwen Zhou, Yingying Zhang, Bailin Liu, Miao Sun, Zhice Xu
BACKGROUND: Hypoxia during pregnancy could cause abnormal development and lead to increased risks of vascular diseases in adults. This study determined angiotensin II (AII)-mediated vascular dysfunction in offspring middle cerebral arteries (MCA). METHODS AND RESULTS: Pregnant rats were subjected to hypoxia. Vascular tension in offspring MCA by AII with or without inhibitors, calcium channel activities, and endoplasmic reticulum calcium stores were tested. Whole-cell patch clamping was used to investigate voltage-dependent calcium channel currents...
October 3, 2017: Journal of the American Heart Association
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