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Verapamil

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https://www.readbyqxmd.com/read/29132176/verapamil-ver-enhances-the-cytotoxic-effects-of-docetaxel-and-vinblastine-combined-therapy-against-non-small-cell-lung-cancer-cell-lines
#1
Soleiman Jaferian, Maryam Soleymaninejad, Hadis Daraee
Lung cancer is one of the foremost tumor-associated cause of death in the world. Most of the patients with NSCLC possesses an advanced disease at diagnosis, and are thus probable subject for systemic therapy. This study aims to evaluate the cytotoxicity of vinblastine and docetaxel combined therapy for the treatment of NSCLC, as well as verapamil (VER) enhancement of the combined therapy. We conducted P-glycoprotein (P-gp) gene expression, protein expression with RT-PCR and western blot respectively, apoptotic response of the combined therapy with VER is also determined using DAPI staining (%)...
November 13, 2017: Drug Research
https://www.readbyqxmd.com/read/29132172/can-screening-and-confirmatory-testing-in-the-management-of-patients-with-primary-aldosteronism-be-improved
#2
Michael Stowasser, Ashraf Ahmed, Zeng Guo, Martin Wolley, Jacobus Ungerer, Brett McWhinney, Marko Poglitsch, Richard Gordon
Widespread application of the plasma aldosterone/renin ratio (ARR) as a screening test has led to the recognition that primary aldosteronism (PA) is the most common specifically treatable and potentially curable form of hypertension, accounting for 5-10% of patients. Maximal detection requires accurate diagnostic approaches and awareness and control of factors that confound results, including most antihypertensives, posture, time of day, dietary salt, and plasma potassium. Recent studies have revealed potential for false positives in patients on beta-adrenoceptor blockers, and, when direct renin concentration (but not plasma renin activity) is used to measure renin, in women during the luteal phase of the menstrual cycle or receiving estrogen-containing contraceptives or hormonal replacement therapy...
November 13, 2017: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://www.readbyqxmd.com/read/29131061/kinetic-aspects-of-verapamil-binding-on-rate-on-wild-type-and-six-hkv1-3-mutant-channels
#3
Ann-Kathrin Diesch, Stephan Grissmer
BACKGROUND/AIMS: The human-voltage gated Kv1.3 channel (hKv1.3) is expressed in T- and B lymphocytes. Verapamil is able to block hKv1.3 channels. We characterized the effect of verapamil on currents through hKv1.3 channels paying special attention to the on-rate (kon) of verapamil. By comparing on-rates obtained in wild-type (wt) and mutant channels a binding pocket for verapamil and impacts of different amino acid residues should be investigated. METHODS: Using the whole-cell patch clamp technique the action of verapamil on currents through wild-type and six hKv1...
November 6, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29128272/cytoprotection-of-lipoic-acid-against-toxicity-induced-by-saxitoxin-in-hippocampal-cell-line-ht-22-through-in-silico-modeling-and-in-vitro-assays
#4
Patrícia Ramos, Marcos Schmitz, Sibele Gama, Aline Portantiolo, Michael Gonzalez Durruthy, Ana Paula de Souza Votto, Luisa Rodrigues Cornetet, Karina Dos Santos Machado, Adriano Wehrli, Mariana Zancan Tonel, Solange Binotto Fagan, João Sarkis Yunes, José Maria Monserrat
Saxitoxins (STXs) are potent neurotoxins that block voltage-gated channels in neurons and induce cytotoxicity. These toxins not only can generate reactive oxygen species but also can alter antioxidant levels, promoting oxidative stress. Under this pro-oxidant situation, the use of the antioxidant lipoic acid (LA) can represent a chemoprotective alternative to minimize the deleterious effects induced by neurotoxins as STXs. P-glycoprotein (P-gp) is a well-known ATP-binding cassette (ABC) transporter that plays a crucial role in the extrusion of toxic substances, decreasing their accumulation and potential intracellular effects in virtue of its broad substrate specificity, its expression in many excretory tissues and its large efflux capacity...
November 8, 2017: Toxicology
https://www.readbyqxmd.com/read/29127703/comparison-of-two-highly-automated-ecg-algorithms-for-detection-of-drug-induced-cardiac-ion-channel-block
#5
M Brockway, A A Fossa, J W Mason
FDA investigators recently demonstrated in a crossover study that early (J-Tpeak c) and late (Tpeak -Tend ) repolarization duration can differentiate selective potassium block with a high arrhythmia risk from multichannel block with lower risk in subjects receiving dofetilide, verapamil, quinidine or ranolazine. The purpose of this study was to determine if findings by FDA using their published software algorithm could be corroborated using an alternative software algorithm for the same metrics and to determine if methodological differences resulted in clinically meaningful differences in interpretation...
November 11, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29126726/exploration-of-1-2-3-triazole-pyrimidine-hybrids-as-potent-reversal-agents-against-abcb1-mediated-multidrug-resistance
#6
Bo Wang, Bing Zhao, Zhe-Sheng Chen, Lu-Ping Pang, Yuan-Di Zhao, Qian Guo, Xin-Hui Zhang, Ying Liu, Guang-Yao Liu, Hao-Zhang, Xin-Yuan Zhang, Li-Ying Ma, Hong-Min Liu
ABCB1-mediated multidrug resistance (MDR) is a principal obstacle for successful cancer chemotherapy. A series of pyrimidine-based hybrid molecules containing 1,2,3-triazole moiety were evaluated for their reversal activities against MDR. The majority of target compounds displayed moderate to great reversal potency. Among these compounds, compound 25 displayed the most potent reversal activity, about 7-fold more potent than Verapamil (VRP). Further mechanism studies revealed that compound 25 could obviously reverse paclitaxel (PTX) resistance in SW620/AD300 cells by increasing accumulation and extending maintenance of PTX...
October 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29125571/the-blood-brain-barrier-permeability-of-six-indole-alkaloids-from-uncariae-ramulus-cum-uncis-in-the-mdck-phamdr-cell-monolayer-model
#7
Yi-Nan Zhang, Yan-Fang Yang, Wei Xu, Xiu-Wei Yang
Uncariae Ramulus Cum Uncis (URCU) is a widely used traditional Chinese medicine, and is reported to have various central nervous system effects. Alkaloids have been demonstrated to be the predominant pharmacological active components of URCU. In order to evaluate the blood-brain barrier (BBB) permeability and transport mechanism of six typical indole alkaloids from URCU, the MDCK-pHaMDR cell monolayer model was used as an in vitro surrogate model for BBB. The samples were analyzed by high-performance liquid chromatography, and the apparent permeability coefficients (Papp) were calculated...
November 10, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29122673/involvement-of-dual-mechanisms-of-anti-muscarinic-and-ca-antagonistic-activities-to-validate-the-folkloric-uses-of-cyperus-niveus-retz-in-multiple-gastrointestinal-ailments
#8
Ambreen Aleem, Khalid Hussain Janbaz
ETHNOPHARMACOLOGICAL RELEVANCE: Cyperus species are famous for their traditional uses and very commonly used for their anti-spasmodic and anti-diarrheal activities. Cyperus niveus Retz. is used in local traditional system of medicine in Pakistan to treat various gastrointestinal ailments. AIM OF THE STUDY: The aim of the study was to validate the traditional uses and to provide the possible mechanisms for the medicinal use of Cyperus niveus Retz. in gastrointestinal ailments...
November 6, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29121796/absorption-properties-of-luteolin-and-apigenin-in-genkwa-flos-using-in-situ-single-pass-intestinal-perfusion-system-in-the-rat
#9
Xin He, Zi-Jing Song, Cui-Ping Jiang, Chun-Feng Zhang
The flower bud of Daphne genkwa (Genkwa Flos) is a commonly used herbal medicine in Asian countries. Luteolin and apigenin are two recognized active flavonoids in Genkwa Flos. The aim of this study was to investigate the intestinal absorption mechanisms of Genkwa Flos flavonoids using in situ single-pass intestinal perfusion rat model. Using HPLC, we determined its major effective flavonoids luteolin, apigenin, as well as, hydroxygenkwanin and genkwanin in biological samples. The intestinal absorption mechanisms of the total flavonoids in Genkwa Flos (TFG) were investigated using in situ single-pass intestinal perfusion rat model...
November 9, 2017: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29121121/emodin-reverses-leukemia-multidrug-resistance-by-competitive-inhibition-and-downregulation-of-p-glycoprotein
#10
Hongping Min, Miaomiao Niu, Weilin Zhang, Jia Yan, Jiachang Li, Xiying Tan, Bo Li, Mengxiang Su, Bin Di, Fang Yan
Development of multidrug resistance (MDR) is a continuous clinical challenge partially due to the overexpression of P-glycoprotein (P-gp) for chronic myelogenous leukemia (CML) patients. Herein, we evaluated the inhibitory potency of emodin, a natural anthraquinone derivative isolated from Rheum palmatum L, on P-gp in P-gp positive K562/ADM cells. Competition experiments combined with molecular docking analysis were utilized to investigate the binding modes between emodin and binding sites of P-gp. Emodin reversed adriamycin resistance in K562/ADM cells accompanied with the decrease of P-gp protein expression, further increasing the uptake of rhodamine123 in both K562/ADM and Caco-2 cells, indicating the inhibition of P-gp efflux function...
2017: PloS One
https://www.readbyqxmd.com/read/29105666/-low-or-reduced-semantics-of-the-doses-of-new-oral-anticoagulants
#11
Andrea Rubboli
The four new oral anticoagulants (NOACs) dabigatran, rivaroxaban, apixaban and edoxaban are marketed in two doses each for the prevention of stroke and/or systemic thromboembolism in non-valvular atrial fibrillation (NVAF). The meaning and indications for use of the lower dose compared with the higher dose are, however, different between the thrombin-inhibitor dabigatran on the one hand and the activated factor X (Xa) inhibitors on the other. These differences stem from the different design of the registration studies where NOACs were compared with warfarin for the prevention of stroke and/or systemic thromboembolism in patients with NVAF...
September 2017: Giornale Italiano di Cardiologia
https://www.readbyqxmd.com/read/29104273/study-of-absorption-characteristics-of-the-total-saponins-from-radix-ilicis-pubescentis-in-an-in-situ-single-pass-intestinal-perfusion-spip-rat-model-by-using-ultra-performance-liquid-chromatography-uplc
#12
Guojun Kuang, Huan Yi, Mingjuan Zhu, Jie Zhou, Xueying Shang, Zhongxiang Zhao, Chenchen Zhu, Qiongfeng Liao, Shixia Guan, Lei Zhang
In contrast to the extensively reported therapeutic activities, far less attention has been paid to the intestinal absorption of the total saponins from Radix Ilicis Pubescentis (in Chinese Mao-Dong-Qing, MDQ). This study aimed to investigate the intestinal absorption characteristics of ilexgenin A (C1), ilexsaponin A1 (C2), ilexsaponin B1 (C3), ilexsaponin B2 (C4), ilexsaponin B3 (DC1), and ilexoside O (DC2) when administrated with the total saponins from MDQ (MDQ-TS). An UPLC method for simultaneous determination of C1, C2, C3, C4, DC1, and DC2 in intestinal outflow perfusate was developed and validated...
November 1, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29098993/effect-of-efflux-pump-inhibitors-on-the-susceptibility-of-mycobacterium-tuberculosis-to-isoniazid
#13
Indu Jaiswal, Amita Jain, Sanjeev Kumar Verma, Pooja Singh, Surya Kant, Mastan Singh
BACKGROUND: Mycobacterium can develop drug resistance (DR) by mutation of its existing gene. However, the existence of DR without mutation shows the need to look for an alternative mechanism such as the role of efflux pumps. In this study, we examined the effect of efflux pump inhibitors on isoniazid (INH) susceptibility in clinical isolates of Mycobacterium tuberculosis (Mtb). MATERIALS AND METHODS: Resazurin microtiter assay was used to examine the effect of efflux pump inhibitors on minimum inhibitory concentration (MIC) levels of INH in eighteen Mtb clinical isolates...
November 2017: Lung India: Official Organ of Indian Chest Society
https://www.readbyqxmd.com/read/29097388/genetic-variants-associated-with-uncontrolled-blood-pressure-on%C3%A2-thiazide-diuretic-%C3%AE-blocker-combination-therapy-in-the-pear-pharmacogenomic-evaluation-of-antihypertensive-responses-%C3%A2-and-invest-international-verapamil-sr-trandolapril-study-trials
#14
Oyunbileg Magvanjav, Yan Gong, Caitrin W McDonough, Arlene B Chapman, Stephen T Turner, John G Gums, Kent R Bailey, Eric Boerwinkle, Amber L Beitelshees, Toshihiro Tanaka, Michiaki Kubo, Carl J Pepine, Rhonda M Cooper-DeHoff, Julie A Johnson
BACKGROUND: The majority of hypertensive individuals require combination antihypertensive therapy to achieve adequate blood pressure (BP) control. This study aimed to identify genetic variants associated with uncontrolled BP on combination therapy with a thiazide diuretic and a β-blocker. METHODS AND RESULTS: A genome-wide association study of uncontrolled BP on combination therapy was conducted among 314 white participants of the PEAR (Pharmacogenomic Evaluation of Antihypertensive Responses) trial...
November 2, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29092973/landiolol-is-effective-for-the-treatment-of-tachycardia-induced-cardiogenic-shock-in-patients-during-septic-shock-therapy
#15
Yoh Arita, Takatsugu Segawa, Shohei Yamamoto, Shinji Hasegawa
Septic shock is a life-threatening condition that occurs when the blood pressure drops to a low level after an infection. Atrial fibrillation (AF) is the most common arrhythmia to complicate its course. Beta (β)-blockers are often administrated to manage supraventricular tachyarrhythmias observed in patients presenting with sepsis. A 74-year-old woman presenting with sepsis demonstrated AF tachycardia characterised by severe hypotension. She was refractory to conventional therapy including verapamil and digoxin; therefore, treatment using landiolol (an ultrashort-acting β-blocker) was initiated...
November 1, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/29084166/determination-of-verapamil-hcl-in-pharmaceutical-preparations-by-a-fluorescent-nano-probe-based-on-cdte-cds-zns-quantum-dots
#16
Sohail Muhammad, Guanhong Xu, Fangdi Wei, Yujie Ma, Yunsu Ma, Yueyue Song, Menglan Shi, Xiaoman Xu, Yao Cen, Qin Hu
An analytical technique based on fluorescence quenching of CdTe/CdS/ZnS quantum dots (QDs) was developed to quantify verapamil in commercially available preparations. Various reaction parameters were optimized and the method developed was validated. One way analysis of variance (ANOVA) and post hoc tests at a 5% significance level were performed to justify the significance of the variation in observations. The linear range of the verapamil concentration was 0.25-5 µg/mL while the limit of detection was 20 µg/mL...
October 30, 2017: Nanomaterials
https://www.readbyqxmd.com/read/29083341/a-case-of-refractary-epilepsy-and-related-pain-due-to-dysmenorrhea-solved-with-loading-dose-of-lacosamide-clinical-and-neurophysiological-correlates
#17
Nicolino Marchitto, Umberto Ceratti, Serenella Dalmaso, Gianfranco Raimondi
 In most cases, the etiology of epilepsy is unknown, although some individuals may develop epilepsy as a result of certain brain injuries, following a stroke, a brain tumor or because of drugs and alcohol. Even some rare genetic mutations may be related to the onset of the condition. Seizures are the result of excessive and abnormal activity of neurons in the cerebral cortex. In this case report we show a clinical case of refractory epilepsy due to pain related to uncontrolled dysmenorrhea. The patient, 43 yrs old, had a history of epilepsy of 20 years and ovarian cancer...
October 23, 2017: Acta Bio-medica: Atenei Parmensis
https://www.readbyqxmd.com/read/29078953/the-application-of-a-novel-high-resolution-mass-spectrometry-based-analytical-strategy-to-rapid-metabolite-profiling-of-a-dual-drug-combination-in-humans
#18
Jie Xing, Meitong Zang, Huixiang Liu
Metabolite profiling of combination drugs in complex matrix is a big challenge. Development of an effective data mining technique for simultaneously extracting metabolites of one parent drug from both background matrix and combined drug-related signals could be a solution. This study presented a novel high resolution mass spectrometry (HRMS)-based data-mining strategy to fast and comprehensive metabolite identification of combination drugs in human. The model drug combination was verapamil-irbesartan (VER-IRB), which is widely used in clinic to treat hypertension...
November 15, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/29073626/diosgenin-an-activator-of-1-25d3-marrs-receptor-erp57-attenuates-the-effects-of-tnf-%C3%AE-by-causing-adam10-dependent-ectodomain-shedding-of-tnf-receptor-1
#19
Won Seok Yang, Soo Young Moon, Mee Jeong Lee, Eun Kyoung Lee, Su-Kil Park
BACKGROUND/AIMS: We investigated how diosgenin, a steroidal sapogenin, has anti-tumor necrosis factor-α (TNF-α) effects in human aortic endothelial cells (HAECs). METHODS: Tumor necrosis factor receptor 1 (TNFR1) was assessed by Western blot analysis. Intracellular Ca2+ was measured using Fluo-4 AM. Immunofluorescence staining was performed for a disintegrin and metalloprotease 10 (ADAM10). RESULTS: Diosgenin (1 ∼ 100 nM) induced ectodomain shedding of TNFR1 within 30 min and attenuated TNF-α-induced intercellular adhesion molecule-1 (ICAM-1) expression...
October 27, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29071859/-validation-of-in-situ-single-pass-perfusion-model-based-on-p-gp
#20
Yue-Liu Dong, Yang Liu, Xiu-Wen Yin, Meng Pan, Xue-Lian Li, Zi-Yu Wang, Ling Dong
To validate in situ rats intestinal single pass perfusion model based on P-glycoprotein (P-gp). Firstly, phenol red perfusion was carried out to verify the close connection structure of intestinal epithelial cells, and the integrity of the intestinal epithelium, with a gravimetric method for correcting water flux. The level of phenol red was determined by high performance liquid chromatography (HPLC) both before and after perfusion. Secondly, the positive drug digoxin specified by FDA was used to validate the model...
April 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
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