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Repaglinide

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https://www.readbyqxmd.com/read/29663513/a-variant-of-grk5-is-associated-with-the-therapeutic-efficacy-of-repaglinide-in-chinese-han-patients-with-type-2-diabetes-mellitus
#1
Zhenhai Shang, Feifei Han, Xueyan Zhou, Zejun Bao, Jing Zhu, Tao Wang, Qian Lu, Lei Du, Wei Li, Dongmei Lv, Xiaoxing Yin
Post-Market Research We aimed to investigate the impact of G protein-coupled receptor kinase 5 (GRK5) rs10886471 polymorphism on repaglinide efficacy in Chinese patients with type 2 diabetes mellitus (T2DM). A total of 300 T2DM patients and 210 healthy controls were genotyped for GRK5 rs10886471 on a three-dimensional polyacrylamide gel-based DNA microarray. Eighty-five patients with the same genotypes of cytochrome P450 (CYP) 2C8*3 139Arg and organic anion-transporting polypeptide 1B1 (OATP1B1) 521TT were randomly selected to orally take repaglinide for eight consecutive weeks...
April 16, 2018: Drug Development Research
https://www.readbyqxmd.com/read/29648532/bioequivalence-of-a-fixed-dose-repaglinide-metformin-combination-tablet-and-equivalent-doses-of-repaglinide-and-metformin-tablets
#2
Hea-Young Cho, Lien Ngo, Sang-Ki Kim, Yoonho Choi, Yong-Bok Lee
OBJECTIVE: This study was conducted to determine whether a fixed-dose combination (FDC) tablet of repaglinide/metformin (2/500 mg) is equivalent to coadministration of equivalent doses of individual (EDI) tablets of repaglinide (2 mg) and metformin (500 mg) in healthy Korean male subjects. MATERIALS AND METHODS: This study was conducted as an open-label, randomized, single-dose, two-period, two-sequence crossover design in 50 healthy Korean male subjects who received an FDC tablet or EDI tablets...
April 12, 2018: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29555503/characteristics-of-repaglinide-effects-on-insulin-secretion
#3
Harumi Takahashi, Shihomi Hidaka, Chihiro Seki, Norihide Yokoi, Susumu Seino
The dynamics of insulin secretion stimulated by repaglinide, a glinide, and the combinatorial effects of repaglinide and incretin were investigated. At 4.4mM glucose, repaglinide induced insulin secretion with a gradually increasing first phase, showing different dynamics from that induced by glimepiride, a sulfonylurea. In the presence of glucagon-like peptide-1 (GLP-1), insulin secretion by repaglinide was augmented significantly but to lesser extent and showed different dynamics from that by glimepiride...
March 16, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29523177/inhibition-of-dream-atf6-interaction-delays-onset-of-cognition-deficit-in-a-mouse-model-of-huntington-s-disease
#4
Alejandro López-Hurtado, Daniel F Burgos, Paz González, Xose M Dopazo, Valentina González, Alberto Rábano, Britt Mellström, Jose R Naranjo
The transcriptional repressor DREAM (downstream regulatory element antagonist modulator) is a multifunctional neuronal calcium sensor (NCS) that controls Ca2+ and protein homeostasis through gene regulation and protein-protein interactions. Downregulation of DREAM is part of an endogenous neuroprotective mechanism that improves ATF6 (activating transcription factor 6) processing, neuronal survival in the striatum, and motor coordination in R6/2 mice, a model of Huntington's disease (HD). Whether modulation of DREAM activity can also ameliorate cognition deficits in HD mice has not been studied...
March 9, 2018: Molecular Brain
https://www.readbyqxmd.com/read/29512235/glycaemic-control-and-treatment-of-type-2-diabetes-in-adults-aged-75-years-or-older
#5
Antonio Rodriguez-Poncelas, Joan Barrot-de la-Puente, Gabriel Coll de Tuero, Carles López-Arpí, Bogdan Vlacho, Flora Lopéz-Simarro, Xavier Mundet Tudurí, Josep Franch-Nadal
AIM: The aim of this study was to assess glycaemic control and prescribing practices of antihyperglycaemic treatment in patients with diabetes mellitus type 2 aged 75 years or older. METHODS: We analysed data from health electronic records from 4,581 persons attended at primary healthcare centres of the Institut Català de la Salut (ICS), in the Girona Sud area of Catalonia, Spain, during 2013 and 2016. Variables such as age, gender, body mass index (BMI), diabetes duration, age at diabetes diagnosis, glycated haemoglobin (HbA1c), creatinine, glomerular filtrate rate and the albumin/creatinine ratio in urine were collected...
March 7, 2018: International Journal of Clinical Practice
https://www.readbyqxmd.com/read/29448869/development-and-validation-of-probe-drug-cocktails-for-the-characterization-of-cyp450-mediated-metabolism-by-human-heart-microsomes
#6
Jade Huguet, Fleur Gaudette, Véronique Michaud, Jacques Turgeon
The objective of our study was to develop and validate a cocktail approach to allow the simultaneous characterization of various CYP450-mediated oxydations by human heart microsomes for nine probe drug substrates namely. ethoxyresorufin. bupropion. repaglinide. tolbutamide. bufuralol. chlorzoxazone. ebastine. midazolam and dodecanoic acid. The first validation step was conducted using recombinant human CYP450 isoenzymes by comparing activity measured for each probe drug as a function of 1) buffer used. 2) selectivity towards specific isoenzymes...
February 16, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29439129/simultaneous-assessment-in-vitro-of-transporter-and-metabolic-processes-in-hepatic-drug-clearance-use-of-a-media-loss-approach
#7
James Harrison, Tom De Bruyn, Adam S Darwich, J Brian Houston
Hepatocyte drug depletion-time assays are well established for the determination of metabolic clearance in vitro. The present study focuses on the refinement and evaluation of a "media loss" assay, an adaptation of the conventional depletion assay involving centrifugation of hepatocytes prior to sampling, allowing estimation of uptake in addition to metabolism. Using experimental procedures consistent with a high throughput, a selection of 12 compounds with a range of uptake and metabolism characteristics (atorvastatin, cerivastatin, clarithromycin, erythromycin, indinavir, pitavastatin, repaglinide, rosuvastatin, saquinavir and valsartan, together with two control compounds - midazolam and tolbutamide) were investigated in the presence and absence of the cytochrome P450 inhibitor 1-aminobenzotriazole and organic anion transporter protein inhibitor rifamycin SV...
February 8, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29381228/implications-of-inter-correlation-between-hepatic-cyp3a4-cyp2c8-enzymes-for-the-evaluation-of-drug-drug-interactions-a-case-study-with-repaglinide
#8
Kosuke Doki, Adam S Darwich, Brahim Achour, Aleksi Tornio, Janne T Backman, Amin Rostami-Hodjegan
AIMS: Statistically significant positive correlations are reported for the abundance of hepatic drug-metabolising enzymes. We investigate, as an example, the impact of CYP3A4-CYP2C8 inter-correlation on the predicted inter-individual variabilities of clearance and drug-drug interactions (DDIs) for repaglinide using physiologically-based pharmacokinetic (PBPK) modelling. METHODS: PBPK modelling and simulation was employed using Simcyp Simulator (v15.1). Virtual populations were generated assuming inter-correlations between hepatic CYP3A4-CYP2C8 abundances derived from observed values in 24 human livers...
January 30, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29325745/chitosan-nanoparticles-cellulose-nanocrystals-nanocomposites-as-a-carrier-system-for-the-controlled-release-of-repaglinide
#9
Wafaa S Abo-Elseoud, Mohammad L Hassan, Magdy W Sabaa, Mona Basha, Enas A Hassan, Shaimaa M Fadel
The aim of the present work was to study the use of cellulose nanocrystals (CNC) and chitosan nanoparticles (CHNP) for developing controlled-release drug delivery system of the anti-hyperglycemic drug Repaglinide (RPG). CNC was isolated from palm fruit stalks by sulfuric acid hydrolysis; the dimensions of the isolated nanocrystals were 86-237 nm in length and 5-7 nm in width. Simple and economic method was used for the fabrication of controlled release drug delivery system from CNC and CHNP loaded with RPG drug via ionic gelation of chitosan in the presence of CNC and RPG...
May 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29199116/repaglinide-versus-insulin-for-newly-diagnosed-diabetes-in-patients-with-cystic-fibrosis-a-multicentre-open-label-randomised-trial
#10
Manfred Ballmann, Dominique Hubert, Baroukh M Assael, Doris Staab, Alexandra Hebestreit, Lutz Naehrlich, Tanja Nickolay, Nicole Prinz, Reinhard W Holl
BACKGROUND: As survival among patients with cystic fibrosis has improved in recent decades, complications have become increasingly relevant. The most frequent complication is cystic-fibrosis-related diabetes. The recommended treatment is injected insulin, but some patients are treated with oral antidiabetic drugs to ease the treatment burden. We assessed the efficacy and safety of oral antidiabetic drugs. METHODS: We did a multicentre, open-label, comparative, randomised trial in 49 centres in Austria, France, Germany, and Italy...
February 2018: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/29108130/comparative-risk-of-serious-hypoglycemia-with-oral-antidiabetic-monotherapy-a-retrospective-cohort-study
#11
Charles E Leonard, Xu Han, Colleen M Brensinger, Warren B Bilker, Serena Cardillo, James H Flory, Sean Hennessy
PURPOSE: To examine and compare risks of serious hypoglycemia among antidiabetic monotherapy-treated adults receiving metformin, a sulfonylurea, a meglitinide, or a thiazolidinedione. METHODS: We performed a retrospective cohort study of apparently new users of monotherapy with metformin, glimepiride, glipizide, glyburide, pioglitazone, rosiglitazone, nateglinide, or repaglinide within a dataset of Medicaid beneficiaries from California, Florida, New York, Ohio, and Pennsylvania...
January 2018: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/29069819/comparison-of-twelve-single-drug-regimens-for-the-treatment-of-type-2-diabetes-mellitus
#12
Shao-Lian Wang, Wen-Bin Dong, Xiao-Lin Dong, Wen-Min Zhu, Fang-Fang Wang, Fang Han, Xin Yan
We performed a network meta-analysis to compare the efficacy of 12 single-drug regimens (Glibenclamide, Glimepiride, Pioglitazone, Rosiglitazone, Repaglinide, Metformin, Sitaglitin, Exenatide, Liraglutide, Acarbose, Benfluorex, and Glipizide) in the treatment of type 2 diabetes mellitus (T2DM). Fifteen relevant randomized controlled trials (RCTs) were included; direct and indirect evidence from these studies was combined, and weighted mean difference (WMD) and surface under the cumulative ranking curves (SUCRAs) were examined to evaluate the monotherapies...
September 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/29058840/-use-of-oral-glucose-lowering-agents-in-patients-with-renal-impairment
#13
A J Scheen, N Paquot
Patients with type 2 diabetes (T2D) and chronic kidney disease (CKD) are increasingly numerous, especially in the elderly population. Surprisingly, this situation is often under-recognized or even neglected in clinical practice. Yet, most oral antidiabetic (OAD) agents have limitations in case of renal impairment, either because they require a dose reduction, or are contra-indicated mainly for safety reasons. This clinical case gives the opportunity to discuss the modalities of prescription and cautions to be taken when using most commonly prescribed OAD, metformin, insulin secretagogues (sulfonylureas, repaglinide), DPP-4 inhibitors (gliptins) and SGLT2 inhibitors, in a patient with T2D and CKD...
October 2017: Revue Médicale de Liège
https://www.readbyqxmd.com/read/29038231/evaluation-of-clinical-drug-interaction-potential-of-clofazimine-using-static-and-dynamic-modeling-approaches
#14
Ramachandra Sangana, Helen Gu, Dung Yu Chun, Heidi J Einolf
The 2016 World Health Organization treatment recommendations for drug-resistant tuberculosis (DR-TB) positioned clofazimine as a core second-line drug. Being identified as a cytochrome P450 (P450) inhibitor in vitro, a P450-mediated drug interaction may be likely when clofazimine is coadministered with substrates of these enzymes. The P450-mediated drug interaction potential of clofazimine was evaluated using both static [estimation of the R 1 and area under the plasma concentration-time curve ratio (AUCR) values] and dynamic [physiologically based pharmacokinetics (PBPK)] modeling approaches...
January 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29021480/the-effects-of-mitiglinide-and-repaglinide-on-postprandial-hyperglycemia-in-patients-undergoing-methylprednisolone-pulse-therapy
#15
Kenichi Tanaka, Yosuke Okada, Hiroko Mori, Keiichi Torimoto, Tadashi Arao, Yoshiya Tanaka
One adverse effect of methylprednisolone (MP) pulse therapy is an acute dose-dependent increase in the blood glucose level. Five patients with thyroid ophthalmopathy but normal glucose tolerance received MP pulse therapy (3 cycles, 3 days/week) and were assessed by continuous glucose monitoring. Steroid therapy increased the mean sensor glucose level, and all patients developed steroid-induced diabetes. The patients were treated alternately with mitiglinide (30 mg/day) and repaglinide (1.5 mg/day) during the second or third MP pulse therapy...
January 1, 2018: Internal Medicine
https://www.readbyqxmd.com/read/28977924/antihyperglycemic-treatment-in-patients-with-type-2-diabetes-in-italy-the-impact-of-age-and-kidney-function
#16
Sandro Gentile, Pamela Piscitelli, Francesca Viazzi, Giuseppina Russo, Antonio Ceriello, Carlo Giorda, Piero Guida, Paola Fioretto, Roberto Pontremoli, Felice Strollo, Salvatore De Cosmo
We describe AHA utilization pattern according to age and renal function in type 2 diabetes mellitus (T2DM), in real-life conditions. The analysis was performed using the data set of electronic medical records collected between 1 January and 31 December, 2011 in 207 Italian diabetes centers. The study population consisted of 157,595 individuals with T2DM. The AHA treatment regimens was evaluated. Kidney function was assessed by eGFR, estimated using the CKD-EPI formula. Other determinations: HbA1c, blood pressure (BP), low- density lipoprotein (LDL-c), total and high density lipoprotein cholesterol (TC and HDL-c), triglycerides (TG) and serum uric acid (SUA)...
September 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28891561/online-monitoring-of-hepatic-rat-metabolism-by-coupling-a-liver-biochip-and-a-mass-spectrometer
#17
Franck Merlier, Rachid Jellali, Eric Leclerc
A microfluidic liver biochip was coupled with a mass spectrometer to detect in real time the drug metabolism of hepatocytes. The hepatocytes were cultivated in the biochip for 35 h. The biochip was placed in a small-scale incubator in which the temperature and CO2 concentration were controlled. The biochip was connected serially to a mass spectrometer, a peristaltic pump and a culture medium reservoir. The injection in the mass spectrometer was performed every 10 min for 11 h. The metabolism of midazolam, phenacetin, omeprazole, dextromethorphan, repaglinide, rosuvastatin, tolbutamide and caffeine was investigated...
September 25, 2017: Analyst
https://www.readbyqxmd.com/read/28811859/long-term-effect-of-alogliptin-on-glycemic-control-in-japanese-patients-with-type-2-diabetes-a-3-5-year-observational-study
#18
Kohzo Takebayashi, Tatsuhiko Suzuki, Rika Naruse, Kenji Hara, Mariko Suetsugu, Takafumi Tsuchiya, Toshihiko Inukai
BACKGROUND: The goal of the current study was to investigate the long-term effects (after 3 years or more) of alogliptin on glycemic control in Japanese patients with type 2 diabetes. METHODS: We retrospectively studied the effect of alogliptin on glycemic control in the patients with type 2 diabetes who had participated in our previous 3-month study and who continued to take alogliptin for at least 36 months. RESULTS: The mean duration of alogliptin treatment was 42...
September 2017: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/28717973/design-and-development-of-repaglinide-microemulsion-gel-for-transdermal-delivery
#19
Ujwala A Shinde, Sheela H Modani, Kavita H Singh
Microemulsion formulation of repaglinide, a BCS class II hypoglycemic agent with limited oral bioavailability, was developed considering its solubility in various oils, surfactants, and cosurfactants. The pseudo-ternary phase diagrams for microemulsion regions were constructed by water titration method at Km 1:1 and characterized for optical birefringence, percentage transmittance, pH, refractive index, globule size, zeta potential, viscosity, drug content, and thermodynamic stability. To enhance the drug permeation and residence time, the optimized microemulsions having mean globule size of 36...
January 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28700358/antihyperglycemic-treatment-in-patients-with-type-2-diabetes-in-italy-the-impact-of-age-and-kidney-function
#20
Sandro Gentile, Pamela Piscitelli, Francesca Viazzi, Giuseppina Russo, Antonio Ceriello, Carlo Giorda, Piero Guida, Paola Fioretto, Roberto Pontremoli, Felice Strollo, Salvatore De Cosmo, The Amd-Annals Study Group
We describe AHA utilization pattern according to age and renal function in type 2 diabetes mellitus (T2DM), in real-life conditions.The analysis was performed using the data set of electronic medical records collected between 1 January and 31 December, 2011 in 207 Italian diabetes centers. The study population consisted of 157,595 individuals with T2DM. The AHA treatment regimens was evaluated. Kidney function was assessed by eGFR, estimated using the CKD-EPI formula. Other determinations: HbA1c, blood pressure (BP), low- density lipoprotein (LDL-c), total and high density lipoprotein cholesterol (TC and HDL-c), triglycerides (TG) and serum uric acid (SUA)...
June 28, 2017: Oncotarget
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