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https://www.readbyqxmd.com/read/29891589/transport-kinetics-selective-inhibition-and-successful-prediction-of-in-vivo-inhibition-of-rat-hepatic-oatps
#1
Kazuya Ishida, Mohammed Ullah, Beata Toth, Viktoria Juhasz, Jashvant D Unadkat
For successful in vitro -to- in vivo extrapolation (IVIVE) of hepatic drug uptake and DDI, it is important to characterize the kinetic properties of the individual transporters involved, their fraction (ft) contribution to hepatic uptake, and their selective inhibitors. Here, we characterized the in vitro transport kinetics of two model drugs, rosuvastatin (RSV) and olmesartan acid (OLM), by rat hepatic organic anion transporting polypeptides (Oatp1a1, 1a4 and 1b2) and identified selective inhibitors of these transporters...
June 11, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29885251/serious-hypoglycemia-and-use-of-warfarin-in-combination-with-sulfonylureas-or-metformin
#2
Young Hee Nam, Colleen M Brensinger, Warren B Bilker, Charles E Leonard, Xu Han, Sean Hennessy
Prior research suggests that warfarin, when given concomitantly with some sulfonylureas, may increase the risk of serious hypoglycemia. However, the clinical significance remains unclear. We examined rate ratios (RRs) for the association between serious hypoglycemia and concomitant use of warfarin with either sulfonylureas or metformin using a self-controlled case series design and US Medicaid claims (supplemented with Medicare claims) from 1999-2011. Across all risk windows combined, warfarin was associated with an elevated rate of serious hypoglycemia when given concomitantly with glimepiride (RR:1...
June 9, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29884910/nlrp3-asc-mediated-alveolar-macrophage-pyroptosis-enhances-hmgb1-secretion-in-acute-lung-injury-induced-by-cardiopulmonary-bypass
#3
Lei Hou, Zhongwei Yang, Zhankui Wang, Xiao Zhang, Yanhua Zhao, Hao Yang, Beijie Zheng, Weitian Tian, Shaocheng Wang, Zhengyu He, Xiangrui Wang
Our previous study showed that high levels of HMGB1 existed in rats following cardiopulmonary bypass (CPB)-induced acute lung injury (ALI) and neutralization of high-mobility group box 1(HMGB1) reduced CPB-induced ALI. However, the mechanism by which CPB increases HMGB1 secretion is unclear. Recent studies have shown that inflammasome-mediated cell pyroptosis promotes HMGB1 secretion. This study aimed to investigate the relationship between inflammasome-mediated pyroptosis and HMGB1 in CPB-related ALI. We employed oxygen-glucose deprivation (OGD)-induced alveolar macrophage (AM) NR8383 pyroptosis to measure HMGB1 secretion...
June 8, 2018: Laboratory Investigation; a Journal of Technical Methods and Pathology
https://www.readbyqxmd.com/read/29805453/factitious-hypoglycemia-caused-by-a-unique-pattern-of-drug-use-a-case-report
#4
Mojtaba Akbari, Akbar Soltani, Mohammad Reza Mohajeri-Tehrani, Hamidreza Aghaei Meybodi, Imaneh Sadat Mousavi Fakhr, Sayed Mahmoud Sajjadi-Jazi
Introduction: Factitious hypoglycemia, caused by the surreptitious use of insulin and sulfonylureas, is one of the most challenging differential diagnoses of hypoglycemia. Diagnosis is usually established via exclusion with respect to the special patterns of plasma insulin and C-peptide during hypoglycemic episodes. Case Presentation: We report a case of recurrent hypoglycemic episodes and confusing patterns of insulin and C-peptide levels. In the primary evaluations, insulinoma was suspected considering the high plasma concentrations of insulin and C-peptide, besides negative urine and plasma sulfonylureas during hypoglycemic episodes...
January 2018: International Journal of Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29802529/nlrp3-inflammasome-is-involved-in-q-vd-oph-induced-necroptosis-following-cerebral-ischemia-reperfusion-injury
#5
Xue Teng, Weiwei Chen, Zhihan Liu, Tao Feng, Hui Li, Sheng Ding, Yonggang Chen, Ying Zhang, Xianping Tang, Deqin Geng
Necroptosis is a manner of caspase-independent cell death,which accounts for delayed ischemic cerebral injury, and can be used as a novel tool to expand the treatment time window in ischemic cerebral injury. Q-VD-OPH, a novel pan caspase inhibitor, has been identified as an inducer of necroptosis. In this study, we determined the optimal dose of Q-VD-OPH, which induces necroptosis in rats by the middle cerebral artery occlusion, followed by reperfusion. Furthermore, we report that the NLRP3 inflammasome is involved in necroptosis, with levels of NLRP3 inflammasome proteins as well as inflammatory cytokines, such as IL-1β, being elevated...
May 25, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29789393/long-term-outcomes-in-patients-aged-%C3%A2-70-years-with-intravenous-glyburide-from-the-phase-ii-games-rp-study-of-large-hemispheric-infarction-an-exploratory-analysis
#6
Kevin N Sheth, Nils H Petersen, Ken Cheung, Jordan J Elm, Holly E Hinson, Bradley J Molyneaux, Lauren A Beslow, Gordon K Sze, J Marc Simard, W Taylor Kimberly
BACKGROUND AND PURPOSE: We aimed to determine whether subjects aged ≤70 years who were treated with intravenous glyburide (RP-1127; BIIB093; glibenclamide) would have better long-term outcomes than those who received placebo. METHODS: GAMES-RP (Glyburide Advantage in Malignant Edema and Stroke-Remedy Pharmaceuticals) was a prospective, double-blind, randomized, placebo-controlled phase 2 clinical trial. Eighty-six participants, aged 18 to 80 years, who presented to 18 centers with large hemispheric infarction (baseline diffusion-weighted imaging volumes, 82-300 cm3 ) randomized within 10 hours of symptom onset were enrolled...
June 2018: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/29749110/metformin-for-the-prevention-of-hypertensive-disorders-of-pregnancy-in-women-with-gestational-diabetes-and-obesity-a-systematic-review-and-meta-analysis
#7
REVIEW
Erkan Kalafat, Yavuz Emre Sukur, Abdulkadir, Basky Thilaganathan, Asma Khalil
OBJECTIVES: Metformin has been reported to reduce the risk of preeclampsia. It is also known to influence soluble fms-like tyrosine kinase-1 (sFlt-1) levels, which correlate significantly with the gestation of onset and severity of preeclampsia. The main aim of this systematic review and meta-analysis was to determine whether metformin use is associated with the incidence of hypertensive disorders of pregnancy (HDP). METHODS: MEDLINE (1947 - September 2017), Scopus (1970 - September 2017) and the Cochrane Library (since inception - September 2017) were searched for relevant citations in English language...
May 10, 2018: Ultrasound in Obstetrics & Gynecology
https://www.readbyqxmd.com/read/29715355/effect-of-glyburide-vs-subcutaneous-insulin-on-perinatal-complications-among-women-with-gestational-diabetes-a-randomized-clinical-trial
#8
RANDOMIZED CONTROLLED TRIAL
Marie-Victoire Sénat, Helene Affres, Alexandra Letourneau, Magali Coustols-Valat, Marie Cazaubiel, Helene Legardeur, Julie Fort Jacquier, Nathalie Bourcigaux, Emmanuel Simon, Anne Rod, Isabelle Héron, Virginie Castera, Loic Sentilhes, Florence Bretelle, Catherine Rolland, Mathieu Morin, Philippe Deruelle, Celine De Carne, François Maillot, Gael Beucher, Eric Verspyck, Raoul Desbriere, Sandrine Laboureau, Delphine Mitanchez, Jean Bouyer
Importance: Randomized trials have not focused on neonatal complications of glyburide for women with gestational diabetes. Objective: To compare oral glyburide vs subcutaneous insulin in prevention of perinatal complications in newborns of women with gestational diabetes. Design, Settings, and Participants: The Insulin Daonil trial (INDAO), a multicenter noninferiority randomized trial conducted between May 2012 and November 2016 (end of participant follow-up) in 13 tertiary care university hospitals in France including 914 women with singleton pregnancies and gestational diabetes diagnosed between 24 and 34 weeks of gestation...
May 1, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29715338/insulin-vs-glyburide-for-gestational-diabetes
#9
EDITORIAL
Donald R Coustan, Linda Barbour
No abstract text is available yet for this article.
May 1, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29679622/pharmacotherapy-for-hyperglycemia-in-pregnancy-do-oral-agents-have-a-place
#10
REVIEW
Rosa Corcoy, Montserrat Balsells, Apolonia García-Patterson, Anat Shmueli, Eran Hadar
Diabetes is a frequent condition in pregnancy and achieving adequate glycemic control is of paramount importance. Insulin treatment is the gold standard, oral agents are more attractive, but their safety and efficiency should be a prerequisite for their use. We have more information regarding treatment of women with gestational diabetes mellitus where glyburide can induce a picture of fetal hyperinsulinism (higher birthweight and more neonatal hypoglycemia) whereas metformin requires supplemental insulin in a larger proportion of women but achieves satisfactory perinatal outcomes with the exception of preterm birth...
April 19, 2018: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/29627447/gestational-diabetes-mellitus-multi-disciplinary-treatment-approaches
#11
Evangelia Kintiraki, Dimitrios G Goulis
Gestational diabetes mellitus (GDM) is the most common metabolic disease of pregnancy, associated with several perinatal complications. Adequate glycemic control has been proved to decrease risk of GDM-related complications. Several studies have shown the beneficial effect of exercise and medical nutrition treatment on glycemic and weight control in GDM-affected women. Moreover, pharmacological agents, such as insulin and specific oral anti-diabetic agents can be prescribed safely during pregnancy, decreasing maternal blood glucose and, thus, perinatal adverse outcomes...
April 6, 2018: Metabolism: Clinical and Experimental
https://www.readbyqxmd.com/read/29618446/effects-of-qibaipingfei-capsules-on-pulmonary-vascular-relaxation-through-katp-channel-activation-by-the-no-cgmp-signaling-pathway
#12
Jie Zhu, Baoqin Wang, Mei Lu, Jiabing Tong, Cheng Yang, Zegeng Li
This research explores the effects of Qibaipingfei (QBPF) capsules on pulmonary vascular relaxation in vitro and the relationship of the ATP-sensitive K+ (KATP) channel and nitric oxide (NO) pathway. Vasodilator effects of QBPF (0.125-2 g/kg) on rat pulmonary artery rings were observed using a multi-wire myograph system. The maximum relaxation (Emax ) of QBPF was detected following treatment involving endothelial denudation, Nω-nitro-L-arginine methyl ester (L-NAME), 1H-[1,2,4] oxadiazolo[4,3-α]quinoxalin-1-one (ODQ), or glyburide (GLYB)...
March 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29617486/-structure-of-primary-healthcare-units-for-treating-persons-with-diabetes-cycles-i-and-ii-of-the-brazilian-national-program-to-improve-access-and-quality
#13
Rosália Garcia Neves, Suele Manjourany Silva Duro, Javier Muñiz, Teresa Rosalia Pérez Castro, Luiz Augusto Facchini, Elaine Tomasi
The objective was to describe the necessary structure for treating diabetes patients in the primary healthcare system, as evaluated in Cycles I and II of the Brazilian National Program for the Improvement of Access and Quality (PMAQ) in 2012 and 2014, according to the municipalities' characteristics. A descriptive study was used to assess primary care units whose teams participated in Cycles I and II of the PMAQ in 2012 and 2014. The study used variables from Module I of the external evaluation of the PMAQ that addresses the primary care units' structure...
March 29, 2018: Cadernos de Saúde Pública
https://www.readbyqxmd.com/read/29563527/mfsd2b-is-a-sphingosine-1-phosphate-transporter-in-erythroid-cells
#14
Naoki Kobayashi, Shoko Kawasaki-Nishi, Masato Otsuka, Yu Hisano, Akihito Yamaguchi, Tsuyoshi Nishi
Sphingosine 1-phosphate (S1P) is an intercellular signaling molecule present in blood. Erythrocytes have a central role in maintaining the S1P concentration in the blood stream. We previously demonstrated that S1P is exported from erythrocytes by a glyburide-sensitive S1P transporter. However, the gene encoding the S1P transporter in erythrocytes is unknown. In this study, we found that the mouse erythroid cell line, MEDEP-E14, has S1P export activity and exhibits properties that are consistent with those of erythrocytes...
March 21, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29529172/prescription-of-high-risk-medications-among-patients-with-chronic-kidney-disease-a-cross-sectional-study-from-the-washington-wyoming-alaska-montana-and-idaho-region-practice-and-research-network
#15
Janelle Guirguis-Blake, Gina A Keppel, John Holmes, Rex W Force, William Kriegsman, Laura-Mae Baldwin
Background: Patients with chronic kidney disease (CKD) are at high risk for adverse drug events related to medication dosing errors and prescriptions for relatively contraindicated medications, such as non-steroidal anti-inflammatory drugs (NSAIDs). Objectives: To examine the scope of and variation in prescribing relatively contraindicated medications and medications above the recommended dose levels among patients with stage III/IV CKD in primary care practice...
February 26, 2018: Family Practice
https://www.readbyqxmd.com/read/29518757/prevalence-pathogenesis-and-management-of-prediabetes-and-type-2-diabetes-mellitus-in-patients-with-polycystic-ovary-syndrome
#16
REVIEW
Sofia Lazaridou, Konstantinos Dinas, Konstantinos Tziomalos
Polycystic ovary syndrome (PCOS) is the most common endocrinopathy in women of reproductive age. PCOS is not only the leading cause of anovulatory infertility but is also associated with an array of metabolic disorders, among which impaired glucose metabolism has been a topic of intense research. The aim of the present narrative review is to summarize the findings of the studies that have evaluated the prevalence and incidence of prediabetes and type 2 diabetes mellitus (T2DM) in patients with PCOS, to analyze the factors underpinning the association between T2DM and PCOS and to discuss the current strategies for screening and management of impaired glucose metabolism in this population...
October 2017: Hormones: International Journal of Endocrinology and Metabolism
https://www.readbyqxmd.com/read/29503767/pharmacokinetics-and-safety-of-oral-glyburide-in-dogs-with-acute-spinal-cord-injury
#17
Nick Jeffery, C Elizabeth Boudreau, Megan Konarik, Travis Mays, Virginia Fajt
Background: Glyburide (also known as glibenclamide) is effective in reducing the severity of tissue destruction and improving functional outcome after experimental spinal cord injury in rodents and so has promise as a therapy in humans. There are many important differences between spinal cord injury in experimental animals and in human clinical cases, making it difficult to introduce new therapies into clinical practice. Spinal cord injury is also common in pet dogs and requires new effective therapies, meaning that they can act as a translational model for the human condition while also deriving direct benefits from such research...
2018: PeerJ
https://www.readbyqxmd.com/read/29499921/pharmacological-treatment-of-gestational-diabetes-mellitus-point-counterpoint
#18
Oded Langer
Controversies persist over the most efficacious pharmacologic treatment for gestational diabetes mellitus. For purposes of accuracy in this article, the individual American College of Obstetricians and Gynecologists Practice Bulletin and American Diabetes Association Standards of Medical Care positions on each issue are quoted and then deliberated with evidence of counter claims presented in point/counterpoint. This is a review of all the relevant evidence for the most holistic picture possible. The main issues are (1) which diabetic drugs cross the placenta, (2) the quality of evidence and data source validity, (3) the rationale for the designation of glucose control as the primary outcome in gestational diabetes mellitus, and (4) which drugs (metformin, glyburide, or insulin) are most effective in improving secondary outcomes...
May 2018: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/29495011/potentially-inappropriate-prescribing-in-older-adults-with-hypertension-or-diabetes-mellitus-and-hypertension-at-primary-care-setting-in-bahrain
#19
Khalid Al Khaja, Husain Ahmed Isa, Sindhan Veeramuthu, Reginald P Sequeira
OBJECTIVES: The aims of the study were to evaluate: a) the prevalence and types of potentially inappropriate prescribing in older adults with hypertension or diabetes mellitus and hypertension; and b) whether or not the differences in training of primary care physicians was associated with the PIP. MATERIALS AND METHODS: Primary care prescriptions issued by family physicians and general practitioners were audited using Screening Tools of Older Person's Prescriptions criteria (version 1) with 18 out of 65 applicable criteria...
March 1, 2018: Medical Principles and Practice: International Journal of the Kuwait University, Health Science Centre
https://www.readbyqxmd.com/read/29485035/impact-of-oral-hypoglycemic-agents-on-mortality-among-diabetic-patients-with-non-muscle-invasive-bladder-cancer-a-population-based-analysis
#20
Patrick O Richard, Ardalan E Ahmad, Shaheena Bashir, Alexandre Zlotta, Bimal Bhindi, Ricardo Leao, Madhur Nayan, Aza Mohammed, Neil E Fleshner, Girish S Kulkarni
INTRODUCTION: Non-muscle invasive bladder cancer (NMIBC) accounts for 75-85% of all bladder cancers (UBC). Many UBC patients are also afflicted by diabetes mellitus (DM). It has been postulated that several oral hypoglycemic agents could impact disease-specific survival (DSS), but the data are sparse among NMIBC patients. Our primary objective was to evaluate the impact of metformin on DSS and overall survival (OS) in NMIBC patients. METHODS: This is a retrospective, population-based study that used linked administrative databases to identify diabetic patients ≥66 years who were subsequently diagnosed with NMIBC in Ontario, between 1992 and 2012...
February 23, 2018: Canadian Urological Association Journal, Journal de L'Association des Urologues du Canada
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