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Repaglinide

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https://www.readbyqxmd.com/read/28495568/quantitative-analyses-of-the-influence-of-parameters-governing-rate-determining-process-of-hepatic-elimination-of-drugs-on-the-magnitudes-of-drug-drug-interactions-via-hepatic-oatps-and-cyp3a-using-physiologically-based-pharmacokinetic-models
#1
Takashi Yoshikado, Maeda Kazuya, Hiroyuki Kusuhara, Ken-Ichi Furihata, Yuichi Sugiyama
Physiologically-based pharmacokinetic (PBPK) models were constructed for hepatic organic anion transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) substrates (bosentan, repaglinide, clarithromycin, and simeprevir), a CYP3A probe substrate (midazolam), and selective inhibitors for OATPs (rifampicin) and CYP3A (itraconazole), though the role of OATPs in the hepatic uptake of clarithromycin is unclear. The pharmacokinetic data were obtained from our previous clinical drug-drug interaction (DDI) study...
May 8, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28484975/a-clinical-cassette-dosing-study-for-evaluating-the-contribution-of-hepatic-oatps-and-cyp3a-to-drug-drug-interactions
#2
Takashi Yoshikado, Kazuya Maeda, Sawako Furihata, Hanano Terashima, Takeshi Nakayama, Keiko Ishigame, Kazunobu Tsunemoto, Hiroyuki Kusuhara, Ken-Ichi Furihata, Yuichi Sugiyama
PURPOSE: To demonstrate the relative importance of organic anion-transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) in the hepatic elimination of substrate drugs. METHODS: A cocktail of subtherapeutic doses of bosentan, repaglinide, clarithromycin, darunavir, simeprevir, and midazolam (CYP3A probe) was administered orally to eight healthy volunteers. Rifampicin (OATP inhibitor; 600 mg, p.o.) and itraconazole (CYP3A inhibitor; 200 mg, i.v.) were coadministered with the cocktail in the second and third phases, respectively...
May 8, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28483598/the-mechano-sensitivity-of-cardiac-atp-sensitive-potassium-channels-is-mediated-by-intrinsic-mgatpase-activity
#3
Mohammad Fatehi, Christian J Carter, Nermeen Youssef, Alexander S Clanachan, Peter E Light
Cardiac ATP-sensitive K(+) (KATP) channel activity plays an important cardio-protective role in regulating excitability in response to metabolic stress. Evidence suggests that these channels are also mechano-sensitive and therefore may couple KATP channel activity to increased cardiac workloads. However, the molecular mechanism that couples membrane stretch to channel activity is not currently known. We hypothesized that membrane stretch may alter the intrinsic MgATPase activity of the cardiac KATP channel resulting in increased channel activation...
May 5, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/28479356/quantitative-analysis-of-complex-drug-drug-interactions-between-repaglinide-and-cyclosporin-a-gemfibrozil-using-physiologically-based-pharmacokinetic-models-with-in-vitro-transporter-enzyme-inhibition-data
#4
Soo-Jin Kim, Kota Toshimoto, Yoshiaki Yao, Takashi Yoshikado, Yuichi Sugiyama
Quantitative analysis of transporter- and enzyme-mediated complex drug-drug interactions (DDIs) is challenging. Repaglinide (RPG) is transported into the liver by OATP1B1 and then is metabolized by CYP2C8 and CYP3A4. The purpose of this study is to describe the complex DDIs of RPG quantitatively based on unified physiologically-based pharmacokinetic (PBPK) models using in vitro Ki values for OATP1B1, CYP3A4, and/or CYP2C8. Cyclosporin A (CsA) or gemfibrozil (GEM) increased the blood concentrations of RPG. The time profiles of RPG and the inhibitors were analyzed by PBPK models, considering the inhibition of OATP1B1 and CYP3A4 by CsA, or OATP1B1 inhibition by GEM and its glucuronide and the mechanism-based inhibition of CYP2C8 by GEM glucuronide...
May 4, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28476618/identification-of-repaglinide-as-a-therapeutic-drug-for-glioblastoma-multiforme
#5
Zui Xuan Xiao, Ruo Qiao Chen, Dian Xing Hu, Xiao Qiang Xie, Shang Bin Yu, Xiao Qian Chen
Glioblastoma multiforme (GBM) is a highly aggressive brain tumor with a median survival time of only 14 months after treatment. It is urgent to find new therapeutic drugs that increase survival time of GBM patients. To achieve this goal, we screened differentially expressed genes between long-term and short-term survived GBM patients from Gene Expression Omnibus database and found gene expression signature for the long-term survived GBM patients. The signaling networks of all those differentially expressed genes converged to protein binding, extracellular matrix and tissue development as revealed in BiNGO and Cytoscape...
May 2, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28432599/the-beneficial-effect-of-repaglinide-on-in-vitro-maturation-and-development-ability-of-immature-mouse-oocytes
#6
Eshrat Kalehoei, Mehri Azadbakht
Repaglinide is a hypoglycemic drug, causing depolarization of the cell membrane, opening the voltage-gated calcium channels, and then increasing intracellular calcium in the pancreatic B cells by inhibition of the K-ATP-sensitive channels. Oocyte in vitro maturation (IVM) is influenced by different factors such as calcium signaling. In this study, we examined the effects of repaglinide on in vitro maturation and fertilization ability of mouse oocyte. Immature oocytes were isolated from female Naval Medical Research Institute mice which are 6-8 wk old mechanically and then cultured in 30 μl droplets of T6 medium with different concentrations of repaglinide...
April 21, 2017: In Vitro Cellular & Developmental Biology. Animal
https://www.readbyqxmd.com/read/28421713/identification-isolation-and-synthesis-of-seven-novel-impurities-of-anti-diabetic-drug-repaglinide
#7
Prasad Kancherla, Srinivas Keesari, Pallavi Alegete, Mukkanti Khagga, Parthasarathi Das
Seven unknown impurities in Repaglinide bulk drug batches at below 0.1% (ranging from 0.05-0.10%) were detected by an ultra-performance liquid chromatographic (UPLC) method. These impurities were isolated from the crude sample of Repaglinide using preparative high performance liquid chromatography (prep-HPLC). Based on LC-ESI/MS study, the chemical structures of seven new impurities (8, 9, 10, 11, 13, 14 and 16) were presumed and characterized as 4-(cyanomethyl)-2-ethoxybenzoic acid (8), 4-(cyanomethyl)-2-ethoxy-N-(3-methyl-1-(2-(piperidin-1-yl)phenyl)butyl)benzamide (9), 4-(2-amino-2-oxoethyl)-2-ethoxy-N-(3-methyl-1-(2-(piperidin-1-yl)phenyl)butyl) benzamide (10) and 2-(3-ethoxy-4-((3-methyl-1-(2-(piperidin-1-yl)phenyl)butyl) carbamoyl) phenyl) acetic acid (11) and 4-(cyanomethyl)-N-cyclohexyl-2-ethoxybenzamide (13), 2-(4-(cyclohexylcarbamoyl)-3-ethoxyphenyl) acetic acid (14) and N-cyclohexyl-4-(2-(cyclohexylamino)-2-oxoethyl)-2-ethoxybenzamide (16)...
April 19, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28420700/diabetes-associated-clinical-spectrum-long-term-prognosis-and-genotype-phenotype-correlations-in-201-adult-patients-with-hepatocyte-nuclear-factor-1-b-hnf1b-molecular-defects
#8
Danièle Dubois-Laforgue, Erika Cornu, Cécile Saint-Martin, Joël Coste, Christine Bellanné-Chantelot, José Timsit
OBJECTIVE: Molecular defects of hepatocyte nuclear factor 1B (HNF1B) are associated with a multiorgan disease, including diabetes (maturity-onset diabetes of the young 5) and kidney abnormalities. The HNF1B-syndrome is related to HNF1B mutations or to a 17q12 deletion spanning 15 genes, including HNF1B. Here, we described HNF1B-related diabetes and associated phenotypes and assessed genotype/phenotype correlations at diagnosis and in the long-term. RESEARCH DESIGN AND METHODS: This multicenter retrospective cohort study included 201 patients, aged 18 or older at follow-up, with HNF1B mutations (n = 101) or deletion (n = 100)...
April 18, 2017: Diabetes Care
https://www.readbyqxmd.com/read/28411400/physiologically-based-pharmacokinetic-modeling-suggests-limited-drug-drug-interaction-between-clopidogrel-and-dasabuvir
#9
Mohamad Shebley, Wentao Fu, Prajakta Badri, Daniel A J Bow, Volker Fischer
Dasabuvir, a non-nucleoside NS5B polymerase inhibitor, is a sensitive substrate of cytochrome P450 (CYP) 2C8 with a potential for drug-drug interaction (DDI) with clopidogrel. A physiologically-based pharmacokinetic (PBPK) model was developed for dasabuvir to evaluate the DDI potential with clopidogrel, the acyl-β-D glucuronide metabolite of which has been reported as a strong mechanism-based inhibitor of CYP2C8 based on an interaction with repaglinide. In addition the PBPK model for clopidogrel and its metabolite were updated with additional in vitro data...
April 15, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28383856/-dapagliflozin-forxiga%C3%A2-sglt-2-cotransporter-inhibitor-as-glucose-lowering-agent-in-type-2-diabetes
#10
REVIEW
A J Scheen
Dapagliflozin, a specific inhibitor of sodium-glu¬cose cotransporters type 2 (SGLT2, inhibits glucose reabsorp¬tion in renal tubules and thus promotes glucosuria. This effect results in a reduction in fasting and postprandial glycaemia and a decrease of glycated haemoglobin (HbA1c), with a minor risk of hypoglycaemia, a weight reduction and a reduction in arterial blood pressure. The efficacy of empagliflozin on HbA1c reduction increases according to the level of hyper¬glycaemia but decreases in patients with renal insufficiency...
October 2016: Revue Médicale de Liège
https://www.readbyqxmd.com/read/28349868/ultimate-biodegradability-and-ecotoxicity-of-orally-administered-antidiabetic-drugs
#11
Marta Markiewicz, Christian Jungnickel, Stefan Stolte, Anna Białk-Bielińska, Jolanta Kumirska, Wojciech Mrozik
Hypoglycaemic pharmaceuticals are recently more and more frequently detected in the environment. In our previous study, we have shown that even though many of them undergo significant primary degradation some are transformed to stable products or undergo such transformation that a large part of the structure is still preserved. One of the main routes of elimination from wastewaters or surface waters is biodegradation and a lack thereof leads to accumulation in the environment. Within this work we tested the ultimate biodegradability of six oral antidiabetics: metformin and its main metabolite guanylurea, acarbose, glibenclamide, gliclazide, glimepiride and repaglinide...
March 16, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28342563/type-2-diabetes-mellitus-treatment-patterns-across-europe-a-population-based-multi-database-study
#12
Jetty A Overbeek, Edith M Heintjes, Daniel Prieto-Alhambra, Patrick Blin, Régis Lassalle, Gillian C Hall, Francesco Lapi, Elisa Bianchini, Niklas Hammar, Irene D Bezemer, Ron M C Herings
PURPOSE: The aim of this study was to determine the similarities and differences of type 2 diabetes mellitus (T2DM) treatment patterns in daily practice in 5 European countries and whether these reflect differences in guidelines. METHODS: Prescriptions for drugs used in diabetes treatment during a 5-year study period were obtained from electronic databases. Patients initiating T2DM treatment during the study period were included. An SAS analysis tool was developed to create episodes of use of drug classes, which resulted in treatment patterns...
March 22, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28276787/granulated-colloidal-silicon-dioxide-based-self-microemulsifying-tablets-as-a-versatile-approach-in-enhancement-of-solubility-and-therapeutic-potential-of-anti-diabetic-agent-formulation-design-and-in-vitro-in-vivo-evaluation
#13
Vikas Pandey, Ritu M Gilhotra, Seema Kohli
The current research work was executed with an aim to explore and promote the potential of self-microemusifying drug delivery systems (SMEDDS) in the form of tablets, in order to enhance solubility and oral bioavailability of poorly aqueous soluble drug Repaglinide (RPG). RPG-loaded liquid SMEDDS were developed consisting Labrafil M 1944CS, Kolliphor EL and Propylene glycol, which were then characterized on various parameters. After characterization and optimization, liquid SMEDDS were converted into solid form by adsorbing on Aeroperl® 300 pharma and polyplasdone(TM) XL...
June 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28271251/efficacy-and-safety-of-metformin-and-sitagliptin-based-triple-antihyperglycemic-therapy-strategy-a-multicenter-randomized-controlled-non-inferiority-clinical-trial
#14
RANDOMIZED CONTROLLED TRIAL
Wen Xu, Yiming Mu, Jiajun Zhao, Dalong Zhu, Qiuhe Ji, Zhiguang Zhou, Bin Yao, Anhua Mao, Samuel S Engel, Bin Zhao, Yan Bi, Longyi Zeng, Xingwu Ran, Juming Lu, Linong Ji, Wenying Yang, Weiping Jia, Jianping Weng
Despite the current guideline's recommendation of a timely stepwise intensification therapy, the "clinical inertia", termed as the delayed treatment intensification, commonly exists in the real world, which may be partly due to the relatively little substantial evidence and no clear consensus regarding the efficacy and safety of triple oral agents in patients inadequately controlled with dual therapy. In this clinical trial performed in 237 centers in China, 5,535 type 2 diabetic patients inadequately controlled by previous therapies were treated with a stable metformin/sitagliptin dual therapy for 20 weeks...
March 2017: Science China. Life Sciences
https://www.readbyqxmd.com/read/28238899/estimation-of-the-contribution-of-cyp2c8-and-cyp3a4-in-repaglinide-metabolism-by-human-liver-microsomes-under-various-buffer-conditions
#15
Toshiyuki Kudo, Hitomi Goda, Yuki Yokosuka, Ryo Tanaka, Seina Komatsu, Kiyomi Ito
We have previously reported that the microsomal activities of CYP2C8 and CYP3A4 largely depend on the buffer condition used in in vitro metabolic studies, with different patterns observed between the 2 isozymes. In the present study, therefore, the possibility of buffer condition dependence of the fraction metabolized by CYP2C8 (fm2C8) for repaglinide, a dual substrate of CYP2C8 and CYP3A4, was estimated using human liver microsomes under various buffer conditions. Montelukast and ketoconazole showed a potent and concentration-dependent inhibition of CYP2C8-mediated paclitaxel 6α-hydroxylation and CYP3A4-mediated triazolam α-hydroxylation, respectively, without dependence on the buffer condition...
February 24, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28169935/biomedical-informatics-approaches-to-identifying-drug-drug-interactions-application-to-insulin-secretagogues
#16
Xu Han, ChienWei Chiang, Charles E Leonard, Warren B Bilker, Colleen M Brensinger, Lang Li, Sean Hennessy
BACKGROUND: Drug-drug interactions with insulin secretagogues are associated with increased risk of serious hypoglycemia in patients with type 2 diabetes. We aimed to systematically screen for drugs that interact with the five most commonly used secretagogues-glipizide, glyburide, glimepiride, repaglinide, and nateglinide-to cause serious hypoglycemia. METHODS: We screened 400 drugs frequently coprescribed with the secretagogues as candidate interacting precipitants...
May 2017: Epidemiology
https://www.readbyqxmd.com/read/28115226/dual-crosslinked-pectin-alginate-network-as-sustained-release-hydrophilic-matrix-for-repaglinide
#17
Rajendra Awasthi, Giriraj T Kulkarni, Malipeddi Venkata Ramana, Terezinha de Jesus Andreoli Pinto, Irene Satiko Kikuchi, Daniela Dal Molim Ghisleni, Marina de Souza Braga, Paul De Bank, Kamal Dua
Repaglinide, an oral antidiabetic agent, has a rapid onset of action and short half-life of approximately 1h. Developing a controlled and prolonged release delivery system is required to maintain its therapeutic plasma concentration and to eliminate its adverse effects particularly hypoglycemia. The present study aimed to develop controlled release repaglinide loaded beads using sodium alginate and pectin with dual cross-linking for effective control of drug release. The prepared beads were characterized for size, percentage drug entrapment efficiency, in vitro drug release and the morphological examination using scanning electron microscope...
April 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28092161/estimation-of-ellagic-acid-and-or-repaglinide-effects-on-insulin-signaling-oxidative-stress-and-inflammatory-mediators-of-liver-pancreas-adipose-tissue-and-brain-in-insulin-resistant-type-2-diabetic-rats
#18
COMPARATIVE STUDY
Mohamed M Amin, Mahmoud S Arbid
Even though ellagic acid has previously been valued in many models of cancer, so far its full mechanistic effect as a natural antiapoptotic agent in the prevention of type 2 diabetes complications has not been completely elucidated, which was the goal of this study. We fed albino rats a high-fat fructose diet (HFFD) for 2 months to induce insulin resistance/type 2 diabetes and then treated the rats with ellagic acid (10 mg/kg body weight, orally) and/or repaglinide (0.5 mg/kg body weight, orally) for 2 weeks...
February 2017: Applied Physiology, Nutrition, and Metabolism, Physiologie Appliquée, Nutrition et Métabolisme
https://www.readbyqxmd.com/read/28067999/evaluation-of-pharmacokinetic-interactions-between-lesinurad-a-new-selective-urate-reabsorption-inhibitor-and-cyp-enzyme-substrates-sildenafil-amlodipine-tolbutamide-and-repaglinide
#19
Michael Gillen, Chun Yang, David Wilson, Shakti Valdez, Caroline Lee, Bradley Kerr, Zancong Shen
Lesinurad is a selective uric acid reabsorption inhibitor approved for the treatment of hyperuricemia associated with gout in combination with xanthine oxidase inhibitors. In vitro assays indicate that lesinurad is an inducer of CYPs in the order CYP3A > CYP2C8 > CYP2C9 > CYP2C19 > CYP2B6 and an inhibitor of CYP2C8 and CYP2C9. To investigate the drug interaction potential of lesinurad, clinical drug interaction studies were conducted. Open-label studies in volunteers investigated the effects of single-/multiple-dose lesinurad on the pharmacokinetics of sildenafil and amlodipine (CYP3A4 induction), tolbutamide (CYP2C9 inhibition/induction), and repaglinide (CYP2C8 inhibition/induction)...
January 9, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28000562/synchronized-fast-spe-and-uflc-methods-for-the-analyses-of-eight-antidiabetic-drugs-in-human-plasma
#20
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
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