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https://www.readbyqxmd.com/read/28230659/sulfonylurea-blockade-of-k-atp-channels-unmasks-a-distinct-type-of-glucose-induced-ca-2-decrease-in-pancreatic-%C3%AE-cells
#1
Bo Hellman, Heléne Dansk, Eva Grapengiesser
OBJECTIVES: This study aimed to explore how sulfonylurea blockade of KATP channels affects the early Ca signals for glucose generation of insulin release. METHODS: Cytoplasmic Ca was measured with ratiometric microfluorometry in isolated mouse islets loaded with Fura-PE3. RESULTS: After sulfonylurea blockade of the KATP channels (50 μM-1 mM tolbutamide or 1 μM-1 mM gliclazide), increase of glucose from 3 to 20 mM resulted in suppression of elevated Ca during a 3- to 5-minute period...
February 23, 2017: Pancreas
https://www.readbyqxmd.com/read/28213290/zd0947-a-sulphonylurea-receptor-modulator-detects-functional-sulphonylurea-receptor-subunits-in-murine-vascular-smooth-muscle-atp-sensitive-k-channels
#2
Tadashi Yamamoto, Kohei Takahara, Keiichiro Uchida, Noriyoshi Teramoto
In order to identify functional sulphonylurea receptor (SUR.x) subunits of native ATP-sensitive K(+) channels (KATP channels) in mouse portal vein, the effects of ZD0947, a SUR.x modulator, were investigated on spontaneous portal vein contractions, macroscopic membrane currents and unitary currents recorded (using patch-clamp techniques) in freshly dispersed mouse portal vein myocytes. Spontaneous contractions in mouse portal vein were reversibly reduced by ZD0947 in a concentration-dependent manner (Ki = 293nM)...
February 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28192663/surfactant-free-solid-dispersions-of-hydrophobic-drugs-in-an-amorphous-sugar-matrix-dried-from-an-organic-solvent
#3
Koji Takeda, Yuto Gotoda, Daichi Hirota, Fumihiro Hidaka, Tomo Sato, Tsutashi Matsuura, Hiroyuki Imanaka, Naoyuki Ishida, Koreyoshi Imamura
The technique for homogeneously dispersing hydrophobic drugs in a water-soluble solid matrix (solid dispersion) is a subject that has been extensively investigated in the pharmaceutical industry. Herein, a novel technique for dispersing a solid, without the need to use a surfactant, is reported. A freeze-dried amorphous sugar sample was dissolved in an organic solvent, that contained a soluble model hydrophobic component. The suspension of the sugar and the model hydrophobic component was vacuum foam dried to give a solid powder...
February 13, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28162170/-effects-of-different-sulfonylureas-on-the-warm-up-phenomenon-in-diabetes-patients-with-coronary-artery-disease
#4
M Zheng, L Z Li, Z A Jiang, L H Li, Y G Feng, X H Fu
Objective: To explore the different effects of chronic treatment with glibenclamide and gliclazide on the warm-up phenomenon in diabetes patients with coronary artery disease. Methods: A total of seventy-one patients with chronic stable angina and diabetes who were positive for exercise test and was proven that the stenosis degree was 70%-90% in at least one major branch through coronary angiogram were included into the study.They were divided into three groups, diet control group (DMD), glibenclamide group (DMG1) and gliclazide group (DMG2), according to the treatment of diabetes...
January 17, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/28105986/canagliflozin-dapagliflozin-and-empagliflozin-monotherapy-for-treating-type-2-diabetes-systematic-review-and-economic-evaluation
#5
Rhona Johnston, Olalekan Uthman, Ewen Cummins, Christine Clar, Pamela Royle, Jill Colquitt, Bee Kang Tan, Andrew Clegg, Saran Shantikumar, Rachel Court, J Paul O'Hare, David McGrane, Tim Holt, Norman Waugh
BACKGROUND: Most people with type 2 diabetes are overweight, so initial treatment is aimed at reducing weight and increasing physical activity. Even modest weight loss can improve control of blood glucose. If drug treatment is necessary, the drug of first choice is metformin. However, some people cannot tolerate metformin, which causes diarrhoea in about 10%, and it cannot be used in people with renal impairment. This review appraises three of the newest class of drugs for monotherapy when metformin cannot be used, the sodium-glucose co-transporter 2 (SGLT2) inhibitors...
January 2017: Health Technology Assessment: HTA
https://www.readbyqxmd.com/read/28105082/genetic-diagnosis-and-treatment-of-a-chinese-ketosis-prone-mody-3-family-with-depression
#6
Jun Tang, Chen-Yi Tang, Fang Wang, Yue Guo, Hao-Neng Tang, Ci-La Zhou, Shu-Wen Tan, Shi-Ping Liu, Zhi-Guang Zhou, Hou-De Zhou
BACKGROUND: To analyze the gene mutation and mental disorder of a Chinese ketosis-prone diabetes (KPD) family, and to make a precise diagnosis and give a treatment for them. METHODS: We studied a Chinese family with a clinical diagnosis of maturity-onset diabetes of the young (MODY). The clinical data and the blood samples were collected. The promotor and coding regions inclusive intron exon boundaries of the HNF1A, HNF4A were detected by polymerase chain reaction (PCR) and direct sequencing...
2017: Diabetology & Metabolic Syndrome
https://www.readbyqxmd.com/read/28079268/renoprotective-effect-of-hypericum-perforatum-against-diabetic-nephropathy-in-rats-insights-in-the-underlying-mechanisms
#7
Dalia M Abd El Motteleb, Dalia I Abd El Aleem
Oxidative stress and inflammation play a key role in the initiation and progression of diabetic nephropathy (DN). The present study aimed to investigate the possible protective effect of hypericum perforatum (HP) against DN. Rats were allocated into six groups; control: received normal saline, diabetic untreated (DM): received single dose of streptozotocin (STZ) after injection of nicotinamide (NA), gliclazide: received STZ,NA+ gliclazide (10mg/kg), DM+HP50, DM+HP100, DM+HP200:received STZ,NA and HP 50, 100, 200 mg/kg respectively...
January 12, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28035627/supramolecular-cocrystals-of-gliclazide-synthesis-characterization-and-evaluation
#8
Renu Chadha, Dimpy Rani, Parnika Goyal
PURPOSE: To prepare the supramolecular cocrystals of gliclazide (GL, a BCS class II drug molecule) via mechanochemical route, with the goal of improving physicochemical and biopharmaceutical properties. METHODS: Two cocrystals of GL with GRAS status coformers, sebacic acid (GL-SB; 1:1) and α-hydroxyacetic acid (GL-HA; 1:1) were screened out using liquid assisted grinding. The prepared cocrystals were characterized using thermal and analytical techniques followed by evaluation of antidiabetic activity and pharmacokinetic parameters...
December 29, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/28017142/gliclazide-induced-insulin-autoimmune-syndrome-a-rare-case-report-and-review-on-literature
#9
Xiu Feng, Lu Yuan, Hu Yun, Yunqing Zhu, Fan Yang, Lanlan Jiang, Rengna Yan, Yong Luo, Enhui Zhao, Chenxiao Liu, Ying Wang, Qi Li, Xin Cao, Qian Li, Jianhua Ma
Insulin Autoimmune Syndrome (IAS) is a rare condition characterized by the combination of recurrent severely spontaneous hypoglycemia without evidence of exogenous insulin administration, high concentration of total serum insulin, and the presence of a high titer of insulin autoantibody (IAA)[ ]. But now we describe a case with IAS caused by gliclazide and hardly occuring hypoglycemia. A 70-year-old man with type 2 diabetes presented to our department with poor glycemic control without evidence of hypoglycemia, but the levels of serum insulin and IAA were very high...
December 23, 2016: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/28000562/synchronized-fast-spe-and-uflc-methods-for-the-analyses-of-eight-antidiabetic-drugs-in-human-plasma
#10
Imran Ali, Kamlesh Dutta, A K Jain
The number of the diabetic patients is increasing rapidly globally. The treatment of these patients is a complex phenomenon due to the use of the different drugs. The present article reports a synchronized fast SPE-UFLC separation of eight antidiabetic drugs in human plasma. The separated drugs include metformin HCl, vildagliptin, gliclazide, linagliptin, sitagliptin, pioglitazone, glimepiride and repaglinide. The column used was Sunshell C18 (150 x 4.6 mm, 2.6 µm) with mobile phase of acetate buffer (0.05% TEA in 0...
December 20, 2016: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/27972218/patient-compliance-to-treatment-with-gliclazide-for-type-2-diabetes-mellitus
#11
V Petkova, N I Marchokova, M Dimitrov
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27930700/simultaneous-quantification-of-antidiabetic-agents-in-human-plasma-by-a-uplc-qtof-ms-method
#12
Mariana Millan Fachi, Letícia Bonancio Cerqueira, Letícia Paula Leonart, Thais Martins Guimarães de Francisco, Roberto Pontarolo
An ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry method for the simultaneous quantification of chlorpropamide, glibenclamide, gliclazide, glimepiride, metformin, nateglinide, pioglitazone, rosiglitazone, and vildagliptin in human plasma was developed and validated, using isoniazid and sulfaquinoxaline as internal standards. Following plasma protein precipitation using acetonitrile with 1% formic acid, chromatographic separation was performed on a cyano column using gradient elution with water and acetonitrile, both containing 0...
2016: PloS One
https://www.readbyqxmd.com/read/27904436/effects-of-metformin-on-blood-and-urine-pro-inflammatory-mediators-in-patients-with-type-2-diabetes
#13
Wei Chen, Xiaojie Liu, Shandong Ye
BACKGROUND: Metformin has been used for the treatment of type 2 diabetes by suppressing hepatic gluconeogenesis. It has been shown that the subclinical inflammatory responses play important roles in the pathogenesis of type 2 diabetes. In the present study, we determined the effects of metformin on the levels of pro-inflammatory cytokines (i.e., IL-6, TNF-α, and MCP-1) and anti-inflammatory mediator IL-10 in blood and urine of patients with type 2 diabetes. There were 210 patients with type 2 diabetes, which were randomized into metformin (n = 112) and non-metformin (gliclazide, acarbose, and repaglinide, n = 98) groups...
2016: Journal of Inflammation
https://www.readbyqxmd.com/read/27895517/influence-of-curcumin-on-the-pharmacodynamics-and-pharmacokinetics-of-gliclazide-in-animal-models
#14
Leela Krishna Vatsavai, Eswar Kumar Kilari
PURPOSE: Patients suffering from obesity-related diseases use multiple prescription drugs to control their condition, and it is therefore essential to determine the safety and efficacy of any combination. Gliclazide is one of the most commonly used drug of choice for treatment of type 2 diabetes, and curcumin is a widely used herbal supplement to counter obesity condition. The objective of this study was to investigate the effect of oral administration of curcumin on pharmacodynamics and pharmacokinetics of gliclazide in rats and rabbits to further evaluate the safety and effectiveness of this combination...
2016: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/27829515/primary-degradation-of-antidiabetic-drugs
#15
Marta Markiewicz, Christian Jungnickel, Stefan Stolte, Anna Białk-Bielińska, Jolanta Kumirska, Wojciech Mrozik
Type 2 diabetes is a chronic disease affecting a large portion of the world population and is treated by orally administered drugs. Since these drugs are often taken in high doses and are excreted unchanged or partially metabolised many of them are nowadays detected in surface waters or wastewater treatment plants effluents. Unmetabolised antidiabetics or some of their transformation products retain their pharmacological activity, therefore their presence in the environment is highly undesired. One of the main routes of elimination from wastewaters or surface waters is biodegradation...
February 15, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/27800567/investigation-of-the-dissolution-profile-of-gliclazide-modified-release-tablets-using-different-apparatuses-and-dissolution-conditions
#16
K K S Skripnik, M K Riekes, B R Pezzini, S G Cardoso, H K Stulzer
In the absence of an official dissolution method for modified-release tablets of gliclazide, dissolution parameters, such as apparatuses (1, 2, and 3), rotation speeds, pH, and composition of the dissolution medium were investigated. The results show that although the drug presents a pH-mediated solubility (pH 7.0 > 6.8 > 6.4 > 6.0 > 5.5 > 4.5), the in vitro release of the studied tablets was not dependent on this parameter, despite of the apparatus tested. On the other hand, the rotation speed demonstrated a greater influence (100 rpm >50 rpm)...
October 31, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27714702/amorphous-based-controlled-release-gliclazide-matrix-system
#17
Zheng Lu, Yonglai Yang, Rae-Ann Covington, Yunxia Vivian Bi, Thomas Dürig, Reza Fassihi
The aim of this study was to develop a hydrophilic oral controlled release system (CRS) using the amorphous form of gliclazide, a BCS class II compound, listed on the WHO list of essential medicines. For this purpose, spray-dried dispersions (SDDs) of gliclazide were produced using various grades of hydroxypropyl methylcellulose acetate succinate (HPMCAS) or copovidone as carrier under fully automated conditions. The solid-state properties of prepared SDDs were characterized using X-ray powder diffraction (XRPD), scanning electron microscopy (SEM), modulated differential scanning calorimetry (MDSC), and Fourier transform infrared spectroscopy (FTIR)...
October 6, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27694910/polymorphisms-of-the-kcnq1-gene-are-associated-with-the-therapeutic-responses-of-sulfonylureas-in-chinese-patients-with-type-2-diabetes
#18
Qing Li, Ting-Ting Tang, Feng Jiang, Rong Zhang, Miao Chen, Jun Yin, Yu-Qian Bao, Xiang Cheng, Cheng Hu, Wei-Ping Jia
KCNQ1 channel is a member of the voltage-gated potassium channel KQT-like subfamily. The KCNQ1 gene has recently been identified as a susceptibility locus for type 2 diabetes mellitus (T2DM). In the present study, we examined the effects of KCNQ1 variants on the therapeutic response to modified-release gliclazide (gliclazide MR) treatment in Chinese patients newly diagnosed with T2DM. A total of 100 newly diagnosed T2DM patients without a history of any anti-diabetic medications were treated with gliclazide MR for 16 weeks, but 91 patients completed the entire study...
January 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27666900/treatment-of-type-2-diabetes-with-a-breakable-extended-release-gliclazide-formulation-in-primary-care-the-xrise-study
#19
V Mohan, V Chopra, D Sanyal, S Jain, J Jayaprakashsai
OBJECTIVE: This study examines whether a new, scored and breakable once daily gliclazide tablet formulation, gliclazide XR 60 mg, that enables a simple 2-steps titration, can improve glycemic control rates in the community. METHODS: In a prospective multicenter study of 4 months duration, organised in the primary care setting of urban India, type 2 diabetes patients, uncontrolled with diet alone or metformin monotherapy, received 1 (60 mg), 1½ (90 mg), or 2 (120 mg) tablets of gliclazide XR 60 mg to achieve a target fasting plasma glucose of 126 mg/dl, or HbA1c of 7%...
December 2015: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/27664925/swelling-behavior-of-cross-linked-dextran-hydrogels-and-preliminary-gliclazide-release-behavior
#20
S K Bajpai, Navin Chand, Seema Tiwari, Shweta Soni
In this study, dextran (Dex) has been cross-linked with epichlorohydrin (Ech) to yield cross-linked hydrogels. These gels were characterized by Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD) analysis, Thermogravimetric analysis (TGA), and Scanning electron microscopy (SEM). The water absorption behavior of gels was studied in simulating gastric fluid (SGF) and simulating intestinal fluid (SIF) at 37°C. The data was interpreted by various kinetic models. The swelling was found to be totally diffusion controlled...
December 2016: International Journal of Biological Macromolecules
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