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Lin-Hu Ye, Ling-Ti Kong, Ming-Zhu Yan, Fang-Rui Cao, Li-Sha Wang, Yong-Hong Liao, Rui-Le Pan, Qi Chang
ETHNOPHARMACOLOGICAL RELEVANCE: The Chinese herbal medicine He-Ye, the leaves of the lotus (Nelumbo nucifera) plant, is traditionally used in China for the treatment of sunstroke, thirst, diarrhea, and fever. Currently, the leaf is used not only as an herbal tea to reduce lipid level and control body weight, but also as a major ingredient in some lipid-lowering Chinese patented medicines. Our previous study demonstrated that the alkaloid fraction (AF) of the herb has a strong inhibitory effect on CYP2D6 isoenzyme activity in vitro...
October 19, 2016: Journal of Ethnopharmacology
Jing Chen, Bao Qiong Li, Min Li Xu, Xue Wang, Yu Hong Jing, Hong Lin Zhai
The interference signals and overlapped peaks are common phenomena in fluorescence determination, which seriously influence the accuracy and reliability of analytical results. In this paper, Krawtchouk image moment method was introduced to the analysis of fluorescence three-dimensional (3D) spectra and applied to the quantitative analysis of three drugs including nicotinic acid, metoprolol and amlodipine in human plasma. Without any pretreatment to the obtained spectra, Krawtchouk moments were directly calculated on the grayscale images of 3D spectra, and the quantitative linear models for the three drugs were established by stepwise regression, respectively...
December 1, 2016: Talanta
Laureen A Lammers, Roos Achterbergh, Marcel C M Pistorius, Yuma Bijleveld, Emmely M de Vries, Anita Boelen, Heinz-Josef Klümpen, Johannes A Romijn, RonA A Mathôt
BACKGROUND: The metabolic activity of P450 enzymes in vivo can be determined by using selective probe drugs. The simultaneous administration of multiple CYP-specific probe drugs is commonly referred to as the "cocktail approach." Disadvantages of a cocktail are large volumes of samples required for analysis and time-consuming analyses. The aim of this study was to develop and validate a simplified but sensitive method for the simultaneous quantification of five probe drugs (caffeine (CYP1A2), metoprolol (CYP2D6), midazolam (CYP3A4), omeprazole (CYP2C19), and S-warfarin (CYP2C9)) in a previously validated cocktail using an LC-MS/MS method...
October 19, 2016: Therapeutic Drug Monitoring
Jeffrey B Doyon, Kristina J Liu, Rebecca A Berman
No abstract text is available yet for this article.
October 19, 2016: Journal of General Internal Medicine
Tomomichi Ishizaka, Yu Yoshimatsu, Yu Maeda, Wataru Takasaki, Katsuyoshi Chiba, Kazuhiko Mori
INTRODUCTION: Load-independent cardiac parameters obtained from the ventricular pressure-volume relationship are recognized as gold standard indexes for evaluating cardiac inotropy.In this study, for better analyses of cardiac risks, load-independent pressure-volume loop parameters were assessed in addition to load-dependent inotropic, hemodynamic and electrocardiographic changes in isoflurane-anesthetized monkeys. METHODS: The animals were given milrinone (a PDE 3 inhibitor), metoprolol (a β-blocker), or dl-sotalol (a β+IKr blocker) intravenously over 10min at two dose levels including clinically relevant doses (n=5/drug)...
October 15, 2016: Journal of Pharmacological and Toxicological Methods
Zengwu Wang, Zuo Chen, Xin Wang, Guang Hao, Liyuan Ma, Xin Zhao, Yang Li, Manlu Zhu
OBJECTIVE: To compared blood pressure (BP) lowing effects of nitrendipine and hydrochlorothiazide (NH) and nitrendipine plus metoprolol (NM), and estimated the economic effect of these therapies on hypertension. DESIGN AND METHOD: This is a randomized, open-label, prospective clinical trial, outpatients (N = 793) 18-70 years-of-age with stage 2 or severe hypertension (systolic BP ≥ 160 mmHg and/or diastolic BP ≥ 100 mmHg) were recruited from 4 rural community health centers in Beijing and Jilin...
September 2016: Journal of Hypertension
Meghan MacKenzie, Richard Hall
PURPOSE: Knowledge of how alterations in pharmacogenomics and pharmacogenetics may affect drug therapy in the intensive care unit (ICU) has received little study. We review the clinically relevant application of pharmacogenetics and pharmacogenomics to drugs and conditions encountered in the ICU. SOURCE: We selected relevant literature to illustrate the important concepts contained within. PRINCIPAL FINDINGS: Two main approaches have been used to identify genetic abnormalities - the candidate gene approach and the genome-wide approach...
October 17, 2016: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
S Gibiino, A Trappoli, B Balzarro, A R Atti, D De Ronchi
A 71-year-old man developed coma with severe respiratory failure, hypotension, and tachycardia induced by the intentional ingestion of quetiapine fumarate extended release (XR) 20 g. At the time, he had been treated for bipolar depression with venlafaxine 75 mg/day, lamotrigine 100 mg/day, pregabalin 75 mg/day, and quetiapine XR 400 mg/day for approximately 1 year. Comorbidities were hypertension treated with metoprolol, diabetes mellitus type 2 treated with metformin, and benign prostatic hyperplasia treated with silodosin...
December 2015: Drug Saf Case Rep
Marta O Barbosa, Ana R Ribeiro, Manuel F R Pereira, Adrián M T Silva
Organic micropollutants present in drinking water (DW) may cause adverse effects for public health, and so reliable analytical methods are required to detect these pollutants at trace levels in DW. This work describes the first green analytical methodology for multi-class determination of 21 pollutants in DW: seven pesticides, an industrial compound, 12 pharmaceuticals, and a metabolite (some included in Directive 2013/39/EU or Decision 2015/495/EU). A solid-phase extraction procedure followed by ultra-high-performance liquid chromatography coupled to tandem mass spectrometry (offline SPE-UHPLC-MS/MS) method was optimized using eco-friendly solvents, achieving detection limits below 0...
October 12, 2016: Analytical and Bioanalytical Chemistry
Maryam Hemmati, Alireza Asghari, Mohammad Bazregar, Maryam Rajabi
In this research work, an efficient tandem dispersive liquid-liquid microextraction (TDLLME) procedure coupled with high performance liquid chromatography-ultraviolet detection (HPLC-UV) was successfully applied for the determination of beta-blockers in human plasma and pharmaceutical wastewater samples. High clean-up and preconcentration factor are easily and rapidly feasible via this novel, cheap, and safe microextraction method, leading to high quality experimental data. It consists of two sequential dispersive liquid-liquid microextraction methods, accomplished via air/ultrasonic agitation and air agitation, respectively...
November 2016: Analytical and Bioanalytical Chemistry
Catherine Girouard, Jean-Pierre Grégoire, Paul Poirier, Jocelyne Moisan
PURPOSE: β-Blockers (bisoprolol, carvedilol, and metoprolol) are the cornerstone of heart failure (HF) management. The incidence rate of β-blocker initiation and discontinuation and their associated factors among seniors with a first HF diagnosis were assessed. METHODS: A population-based inception cohort study that included all individuals aged ≥65 years with a first HF diagnosis in Quebec was conducted. β-Blockers initiation among 91,131 patients who were not using β-blockers at the time of HF diagnosis and discontinuation among those who initiated a β-blocker after HF diagnosis were assessed...
2016: Patient Preference and Adherence
Jee Sun Min, Doyun Kim, Jung Bae Park, Hyunjin Heo, Soo Hyeon Bae, Jae Hong Seo, Euichaul Oh, Soo Kyung Bae
BACKGROUND: Evaluating the potential risk of metabolic drug-drug interactions (DDIs) is clinically important. OBJECTIVE: To develop a physiologically based pharmacokinetic (PBPK) model for sarpogrelate hydrochloride and its active metabolite, (R,S)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol (M-1), in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP) 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine...
2016: Drug Design, Development and Therapy
Venkata Ramana Malipeddi, Rajendra Awasthi, Daniela Dal Molim Ghisleni, Marina de Souza Braga, Irene Satiko Kikuchi, Terezinha de Jesus Andreoli Pinto, Kamal Dua
The present study aimed to develop matrix-type transdermal drug delivery system (TDDS) of metoprolol tartrate using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA). The transdermal films were evaluated for physical parameters, Fourier transform infrared spectroscopy analysis (FTIR), differential scanning calorimetry (DSC), in vitro drug release, in vitro skin permeability, skin irritation test and stability studies. The films were found to be tough, non-sticky, easily moldable and possess good tensile strength...
September 27, 2016: Drug Delivery and Translational Research
Miyuki Tashiro, Yasuhide Watanabe, Tomomi Yamakawa, Kanna Yamashita, Satomi Kita, Takahiro Iwamoto, Junko Kimura
BACKGROUND AND AIMS: Carvedilol ((+/-)-1-(carbazol-4-yloxy)-3-[[2-(o-methoxyphenoxy)ethyl]amino]-2-propanol), a β-adrenoceptor-blocker, has multi-channel blocking and vasodilator properties. This agent dose-dependently improves left ventricular function and reduces mortality in patients with arrhythmia and chronic heart failure. However, the effect of carvedilol on the cardiac Na+/Ca2+ exchanger (NCX1) has not been investigated. METHODS AND RESULTS: We examined the effects of carvedilol and metoprolol, 2 β-blockers, on Na+/Ca2+ exchange current (INCX) in guinea-pig cardiac ventricular cells and fibroblasts expressing dog cardiac NCX1...
September 28, 2016: Pharmacology
Peter R Pellegrino, Alicia M Schiller, Karla K V Haack, Irving H Zucker
Elevated sympathetic tone and activation of the renin-angiotensin system are pathophysiologic hallmarks of hypertension, and the interactions between these systems are particularly deleterious. The importance of Rho kinase as a mediator of the effects of angiotensin-II (AngII) in the periphery is clear, but the role of Rho kinase in sympathoexcitation caused by central AngII is not well established. We hypothesized that AngII mediates its effects in the brain by the activation of the RhoA/Rho kinase pathway...
November 2016: Hypertension
Yan-Rong Ma, A-Xi Shi, Hong-Yan Qin, Tiffany Zhang, Yan-Fang Wu, Guo-Qiang Zhang, Xin-An Wu
Drug interactions are one of the commonest causes of side effects, particularly in long-term therapy. The aim of the current study was to investigate the possible effects of metoprolol on the pharmacokinetics of metformin in rats and to clarify the mechanism of drug interaction. In this study, rats were treated with metformin alone or in combination with metoprolol. Plasma, urine and tissue concentrations of metformin were determinated by HPLC. Western blotting and real-time qPCR were used to evaluate the expression of rOCTs and rMATE1...
September 23, 2016: Biopharmaceutics & Drug Disposition
Katie A McCrink, Ava Brill, Malika Jafferjee, Thairy Reyes Valero, Christine Marrero, Martha M Rodriguez, Genevieve M Hale, Anastasios Lymperopoulos
AIM: The β1-adrenergic receptor (AR) Arg389Gly polymorphism affects efficacy of its procontractile signaling in cardiomyocytes and carriers' responses to β-blockers. To identify molecular mechanisms underlying functional differences between Arg389 and Gly389 β1ARs, we examined their binding to β-arrestins (βarr-1 and -2), which mediate β1AR signaling, in neonatal rat ventricular myocytes. METHODS: We tested the β1AR-βarr interaction via β1AR immunoprecipitation followed by βarr immunoblotting...
October 2016: Pharmacogenomics
Zengwu Wang, Zuo Chen, Xin Wang, Guang Hao, Liyuan Ma, Xin Zhao, Yang Li, Manlu Zhu
OBJECTIVE: To compared blood pressure (BP) lowing effects of nitrendipine and hydrochlorothiazide (NH) and nitrendipine plus metoprolol (NM), and estimated the economic effect of these therapies on hypertension. DESIGN AND METHOD: This is a randomized, open-label, prospective clinical trial, outpatients (N = 793) 18-70 years-of-age with stage 2 or severe hypertension (systolic BP ≥ 160 mmHg and/or diastolic BP ≥ 100 mmHg) were recruited from 4 rural community health centers in Beijing and Jilin...
September 2016: Journal of Hypertension
Espen Skarstein Kolberg, Monica Sue-Chu, Astrid Rydning
No abstract text is available yet for this article.
September 14, 2016: Scandinavian Journal of Gastroenterology
Nurullah Sanli, Ibrahim Bulduk, Hatice Ozkurt, Senem Şanli, Sibel A Ozkan
Galanthamine is a second-generation cholinesterase inhibitor that has begun to be used in the treatment of Alzheimer's disease. In the presented research, a simple, accurate, precise and cost-effective capillary zone electrophoretic (CZE) method was used for the qualitative and quantitative estimation of Galanthamine from bulbs, leaves and fringes of Leucojum aestivum L. (summer snowflake) grown in Turkish habitats (Black Sea Region) and pharmaceutical dosage forms by capillary zone electrophoresis with direct UV detection form...
November 30, 2016: Journal of Pharmaceutical and Biomedical Analysis
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