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https://www.readbyqxmd.com/read/29127904/pharmacokinetics-and-brain-uptake-study-of-novel-ampa-receptor-antagonist-perampanel-in-sd-rats-using-a-validated-uhplc-qtof-ms-method
#1
David Paul, Lingesh Allakonda, Amit Sahu, Shruti Surendran, Nanjappan Satheeshkumar
Perampanel (PER) is a novel AMPA receptor antagonist for antiepileptic therapy and is prospective for the treatment of other neurological disorders. A highly sensitive and rapid UHPLC-QTOF-MS method was developed for the quantification of PER in plasma/brain homogenate of SD rat with alogliptin as an internal standard (IS). Chromatographic separation was carried out on an Acquity UPLC HSS Cyano column (100mm×2.1mm, 1.8μm) using gradient mobile phase consisting of 0.1% formic acid and acetonitrile at a flow rate of 0...
November 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29091894/zinc-alogliptin-combination-attenuates-testicular-toxicity-induced-by-doxorubicin-in-rats-role-of-oxidative-stress-apoptosis-and-tgf-%C3%AE-1-nf-%C3%AE%C2%BAb-signaling
#2
Ahmed M Kabel
The aim of this study was to assess the effect of alogliptin and/or zinc on doxorubicin (DOX)-induced testicular toxicity in rats. Sixty male Wistar rats were divided into 6 equal groups: Control; DOX; DOX+Zinc; DOX+Alogliptin; DOX+Carboxymethyl cellulose and DOX+Zinc+Alogliptin. Testis weight, testicular functions, serum testosterone, luteinizing hormone, follicle stimulating hormone and zinc were measured. Also, testicular tissue zinc, 3 β-hydroxysteroid dehydrogenase, 17 β- hydroxysteroid dehydrogenase, antioxidant enzymes, pro-inflammatory cytokines, transforming growth factor beta 1 (TGF-β1), nuclear factor (erythroid-derived 2)-like 2 (Nrf2) and sperm characteristics were assessed...
October 27, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29064626/high-sensitivity-c-reactive-protein-low-density-lipoprotein-cholesterol-and-cardiovascular-outcomes-in-patients-with-type-2-diabetes-in-the-examine-examination-of-cardiovascular-outcomes-with-alogliptin-versus-standard-of-care-trial
#3
You-Cheol Hwang, David A Morrow, Christopher P Cannon, Yuyin Liu, Richard Bergenstal, Simon Heller, Cyrus Mehta, William Cushman, George L Bakris, Faiez Zannad, William B White
OBJECTIVE: We sought to assess the risk of major adverse cardiovascular events (MACE) by utilizing high-sensitivity C-reactive protein (hsCRP) level and low-density lipoprotein cholesterol (LDL-C) in patients with type 2 diabetes and recent acute coronary syndrome. RESEARCH DESIGN AND METHODS: Study participants enrolled in the EXAMINE trial, were stratified by baseline hsCRP levels (<1, 1-3, and >3 mg/l) and were also sub-divided into 4 groups according to baseline hsCRP (≤3 or >3 mg/l) and achieved LDL-C (<70 or ≥70 mg/dl) levels...
October 24, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28932239/computational-analysis-of-gynura-bicolor-bioactive-compounds-as-dipeptidyl-peptidase-iv-inhibitor
#4
Lina Rozano, Muhammad Redha Abdullah Zawawi, Muhamad Aizuddin Ahmad, Indu Bala Jaganath
The inhibition of dipeptidyl peptidase-IV (DPPIV) is a popular route for the treatment of type-2 diabetes. Commercially available gliptin-based drugs such as sitagliptin, anagliptin, linagliptin, saxagliptin, and alogliptin were specifically developed as DPPIV inhibitors for diabetic patients. The use of Gynura bicolor in treating diabetes had been reported in various in vitro experiments. However, an understanding of the inhibitory actions of G. bicolor bioactive compounds on DPPIV is still lacking and this may provide crucial information for the development of more potent and natural sources of DPPIV inhibitors...
2017: Advances in Bioinformatics
https://www.readbyqxmd.com/read/28895030/type-2-diabetes-and-cardiovascular-prevention-the-dogmas-disputed
#5
Dario Giugliano, Maria Ida Maiorino, Giuseppe Bellastella, Katherine Esposito
In randomized controlled trials (RCTs), more intensive glucose control in patients with type 2 diabetes leads to a modest (9%) reduction in major cardiovascular events (MACE), associated with a 20% reduction of kidney events and 13% reduction of eye events. The FDA issued guidance in 2008 led to the conduct of numerous cardiovascular outcomes (CVOT) trials to assess cardiovascular safety of new antihyperglycemic therapies in patients with type 2 diabetes. The results of these trials show that insulin glargine, three different dipeptidyl peptidase-4 (DPP-4) inhibitors (saxagliptin, alogliptin, and sitagliptin) and lixisenatide (a glucagon like peptide-1 receptor agonist) produce no significant difference in CVOT when compared with usual care or placebo...
September 11, 2017: Endocrine
https://www.readbyqxmd.com/read/28853228/comparison-of-effects-of-anagliptin-and-alogliptin-on-serum-lipid-profile-in-type-2-diabetes-mellitus-patients
#6
Akira Kurozumi, Yosuke Okada, Tadashi Arao, Takuya Kobayashi, Daisaku Masuda, Shizuya Yamashita, Yoshiya Tanaka
INTRODUCTION: Anagliptin (ANA) improves dyslipidemia in addition to blood glucose levels. However, there are no comparative studies on the effects of ANA and other dipeptidyl peptidase-4 inhibitors on serum lipid profile. We compared the effects of ANA on serum lipid profile with those of alogliptin (ALO) in type 2 diabetes mellitus outpatients. MATERIALS AND METHODS: The study participants were 87 type 2 diabetes mellitus patients who had been treated with dipeptidyl peptidase-4 inhibitors for ≥8 weeks and had a low-density lipoprotein cholesterol (LDL-C) level of ≥120 mg/dL...
August 29, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/28844525/oral-antidiabetic-agents-and-cardiovascular-outcomes
#7
Manan Pareek, Deepak L Bhatt
Cardiovascular disease is the leading cause of morbidity and mortality among patients with type 2 diabetes; however, a direct protective effect of tight glycemic control remains unproven. In fact, until 2008, when concerns related to rosiglitazone prompted regulatory agencies to mandate assessment of cardiovascular safety of new antidiabetic agents, little was known about how these medications affected cardiovascular outcomes. Since then, there has been a considerable increase in the number of cardiovascular trials, which employ a noninferiority design and focus on high-risk populations to establish safety in the shortest time possible...
July 29, 2017: Current Problems in Cardiology
https://www.readbyqxmd.com/read/28827024/gastrointestinal-adverse-events-of-dipeptidyl-peptidase-4-inhibitors-in-type-2-diabetes-a-systematic-review-and-network-meta-analysis
#8
Shanshan Wu, Sanbao Chai, Jun Yang, Ting Cai, Yang Xu, Zhirong Yang, Yuan Zhang, Linong Ji, Feng Sun, Siyan Zhan
PURPOSE: The purpose of this study was to systematically evaluate the effect of dipeptidyl peptidase 4 inhibitors on gastrointestinal adverse events in patients with type 2 diabetes. METHODS: MEDLINE, Embase, the Cochrane Library, and ClinicalTrials.gov were searched from inception through April 28, 2016. Randomized controlled trials that compared dipeptidyl peptidase 4 inhibitor-based therapies with placebo and other hypoglycemic agents in type 2 diabetes were included...
September 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28817485/anti-diabetic-drug-alogliptin-protects-the-heart-against-ischemia-reperfusion-injury-via-glp-1-receptor-dependent-and-independent-pathways-involving-no-production-in-rabbits
#9
Shinya Baba, Masamitsu Iwasa, Kenshi Higashi, Shingo Minatoguchi, Yoshihisa Yamada, Hiromitsu Kanamori, Masanori Kawasaki, Kazuhiko Nishigaki, Shinya Minatoguchi
GLP-1 has been reported to be cardioprotective against ischemia-reperfusion injury. We aimed to examine the effect of alogliptin, which may produce GLP-1, on ischemia-reperfusion injury and its mechanisms. Rabbits were fed a normal chow (control group) and a chow containing alogliptin (2 mg/kg/day: alogliptin-L group, and 20 mg/kg/day: alogliptin-H group) for 7 days. The rabbits underwent 30 min of coronary occlusion and 48 h of reperfusion. Exendin (9-39) (5 or 50μg/kg, i.v., alogliptin-H+exendin (9-39)-L group and alogliptin-H+exendin (9-39)-H group) or L-NAME(10 mg/kg, i...
August 4, 2017: Journal of Cardiovascular Pharmacology
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
#10
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/28804210/efficacy-and-safety-of-alogliptin-in-a-pediatric-patient-with-maturity-onset-diabetes-of-the-young-type-1
#11
Ryosuke Tonouchi, Yusuke Mine, Masako Aoki, Misako Okuno, Junichi Suzuki, Tatsuhiko Urakami
The first-line pharmacological treatment for patients with maturity-onset diabetes of the young type 1 (MODY1) and maturity-onset diabetes of the young type 3 (MODY3) are sulfonylureas (SUs) or insulin. However, several reports have suggested the possibility of using incretin-associated drugs, including dipeptidyl-peptidase-4 (DPP-4) inhibitors, for the treatment of patients with these types of MODY. Here we report a case of a pediatric patient with MODY1 who was successfully treated with a DPP-4 inhibitor, alogliptin...
2017: Clinical Pediatric Endocrinology: Case Reports and Clinical Investigations: Official Journal of the Japanese Society for Pediatric Endocrinology
https://www.readbyqxmd.com/read/28725321/effect-of-switching-from-an-anti-diabetic-loose-dose-combination-to-a-fixed-dose-combination-regimen-at-equivalent-dosage-for-6-months-on-glycemic-control-in-japanese-patients-with-type-2-diabetes-a-pilot-study
#12
Kazutaka Aoki, Mieko Nagakura, Masataka Taguri, Hiroshi Kamiyama, Makoto Masumura, Tadashi Furuie, Masanao Oka, Kazunari Kamiko, Shigeru Nakajima, Noriko Akema, Yasuo Terauchi
BACKGROUND: Patients with type 2 diabetes mellitus often take multiple anti-diabetic drugs for a long period. Fixed dose combination (FDC) therapy is expected to improve drug adherence for patients with diabetes. The effect of switching from a loose dose combination (LDC) regimen to an FDC regimen at equivalent dosage on glycemic control has not been evaluated fully. Therefore, we investigated the effect of switching from LDC to FDC at equivalent dosage for 6 months on glycemic control in Japanese patients with type 2 diabetes...
August 2017: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/28635331/network-meta-analysis-of-liraglutide-versus-dipeptidyl-peptidase-4-inhibitors-for-the-treatment-of-type-2-diabetes-in-japanese-patients
#13
Dieter Ayers, Steve Kanters, Rachel Goldgrub, Monica Hughes, Ryo Kato, Nana Kragh
AIMS: To determine the comparative efficacy and safety of liraglutide and dipeptidyl peptidase-4 (DPP-4) inhibitors as antidiabetics for Japanese patients with uncontrolled type 2 diabetes (T2DM). METHODS AND MATERIALS: We searched for randomized controlled trials (RCTs) evaluating outcomes among Japanese adults with uncontrolled T2DM and including liraglutide or DPP-4 inhibitors up to August 2016. We extracted data on trial and patient characteristics, and the following outcomes: HbA1c, weight, patients meeting HbA1c <7%, patients experiencing hypoglycemic events, microalbuminuria, estimated glomerular filtration rate (eGFR) and creatinine...
September 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28622738/assessment-of-the-risk-of-hospitalization-for-heart-failure-with-dipeptidyl-peptidase-4-inhibitors-saxagliptin-alogliptin-and-sitagliptin-in-patients-with-type-2-diabetes-using-an-alternative-measure-to-the-hazard-ratio
#14
Masayuki Kaneko, Mamoru Narukawa
BACKGROUND: Saxagliptin statistically significantly increased the risk of hospitalization for heart failure compared with placebo in the clinical trial of SAVOR-TIMI 53. Neither the reason why only saxagliptin among several dipeptidyl peptidase-4 (DPP-4) inhibitors increased the risk, nor the clinical implication of the result has been explained. OBJECTIVE: To evaluate the risk of hospitalization for heart failure associated with DPP-4 inhibitors by using an alternative measure to the hazard ratio...
July 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28611856/a-randomized-controlled-trial-of-vildagliptin-versus-alogliptin-effective-switch-from-sitagliptin-in-patients-with-type-2-diabetes
#15
Erina Shigematsu, Tadashi Yamakawa, Mari S Oba, Jun Suzuki, Jo Nagakura, Kazuaki Kadonosono, Yasuo Terauchi
BACKGROUND: We investigated the effects of vildagliptin or alogliptin on blood glucose and hemoglobin A1c (HbA1c) in patients with type 2 diabetes inadequately controlled by sitagliptin. METHODS: In a single-center open-label trial, 35 patients with inadequate glycemic control on sitagliptin therapy (50 mg once daily) were randomly switched to treatment with vildagliptin (50 mg twice daily) or alogliptin (25 mg once daily). After 12 weeks, patients who failed to achieve the target HbA1c level of < 7...
July 2017: Journal of Clinical Medicine Research
https://www.readbyqxmd.com/read/28601548/comparative-study-between-different-simple-methods-manipulating-ratio-spectra-for-the-analysis-of-alogliptin-and-metformin-co-formulated-with-highly-different-concentrations
#16
Wafaa A Zaghary, Shereen Mowaka, Mostafa A Hassan, Bassam M Ayoub
Different simple spectrophotometric methods were developed for simultaneous determination of alogliptin and metformin manipulating their ratio spectra with successful application on recently approved combination, Kazano® tablets. Spiking was implemented to detect alogliptin in spite of its low contribution in the pharmaceutical formulation as low quantity in comparison to metformin. Linearity was acceptable over the concentration range of 2.5-25.0μg/mL and 2.5-15.0μg/mL for alogliptin and metformin, respectively using derivative ratio, ratio subtraction coupled with extended ratio subtraction and spectrum subtraction coupled with constant multiplication...
June 6, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28554326/update-of-cardiovascular-effects-of-older-and-newer-anti-diabetic-medications
#17
Ioanna Eleftheriadou, Pinelopi Grigoropoulou, Evangelos Liberopoulos, Stavros Liatis, Alexandros Kokkinos, Nikolaos Tentolouris
It is known that cardiovascular (CV) disease is the leading cause of morbidity and mortality in individuals with type 2 diabetes. Over the last years one of the most discussed topics is the CV safety of anti-diabetic medications. Regarding CV safety of older anti-diabetic agents the data are less clear and conclusions about their CV safety is based mostly on randomized controlled trials designed to assess their glucose lowering efficacy. In this review we summarize current knowledge about the CV safety of older and newer anti-diabetic medications...
May 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28528664/enhanced-lc-ms-ms-analysis-of-alogliptin-and-pioglitazone-in-human-plasma-applied-to-a-preliminary-pharmacokinetic-study
#18
Maha F Abdel-Ghany, Miriam F Ayad, Mariam M Tadros
A new fast LC-MS/MS method was developed for determination of alogliptin and pioglitazone in human plasma. Linearity ranges of 10-400ngmL(-1) for alogliptin and 25-2000ngmL(-1) for pioglitazone, were found to be suitable for their bioanalysis covering the Cmin and Cmax values of the drugs. Direct precipitation technique was used for simultaneous extraction of the drugs successfully from human plasma samples. Chromatographic separation was achieved on a BEH C18 column (50mm×2.1mm, 1.7μm) with 0.1% aqueous formic acid: acetonitrile (40:60, v/v) at a flow rate of 0...
July 15, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28514822/-cardiovascular-effects-of-antidiabetic-therapies
#19
Katharina Laubner, Jochen Seufert
Type 2- diabetes mellitus (T2DM) represents a major risk factor for cardiovascular complications and mortality. Strict glucose control in the early course of the disease prevents cardiovascular complications only in the long run. Non-medical therapies (diet, exercise, body weight reduction) bear little evidence for positive cardiovascular effects.Bariatric surgery is not number one choice in therapy of T2DM. Metformin seems to provide positive cardiovascular effects. Insulin seems to be cardiovascular neutral, as well as the DPP4-inhibitors Saxagliptin, Sitagliptin and Alogliptin...
May 2017: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/28507060/alogliptin-a-dipeptidyl-peptidase-4-inhibitor-alleviates-atrial-remodeling-and-improves-mitochondrial-function-and-biogenesis-in-diabetic-rabbits
#20
Xiaowei Zhang, Zhiwei Zhang, Yungang Zhao, Ning Jiang, Jiuchun Qiu, Yajuan Yang, Jian Li, Xue Liang, Xinghua Wang, Gary Tse, Guangping Li, Tong Liu
BACKGROUND: There is increasing evidence implicating atrial mitochondrial dysfunction in the pathogenesis of atrial fibrillation. In this study, we explored whether alogliptin, a dipeptidyl peptidase-4 inhibitor, can prevent mitochondrial dysfunction and atrial remodeling in a diabetic rabbit model. METHODS AND RESULTS: A total of 90 rabbits were randomized into 3 groups as follows: control group (n=30), alloxan-induced diabetes mellitus group (n=30), and alogliptin-treated (12...
May 15, 2017: Journal of the American Heart Association
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