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gemfibrozil

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https://www.readbyqxmd.com/read/29100124/effects-of-gemfibrozil-on-the-growth-reproduction-and-energy-stores-of-daphnia-magna-in-the-presence-of-varying-food-concentrations
#1
Dylan Steinkey, Ebrahim Lari, Samuel G Woodman, Kim H Luong, Charles S Wong, Greg G Pyle
Gemfibrozil, a common lipid regulator, enters aquatic environments through treated municipal wastewater effluent that fails to remove it completely from effluent streams. When exposed to gemfibrozil concentrations of 50, 500, 5,000, and 50,000 ng L(-1), Daphnia magna showed increased lipid reserves by 14-21% (significant at 500 ng L(-1)), increased length by 9-13% (significant at 50 ng L(-1)), increased mass by 6-13% (significant at 50 ng L(-1)) and increased neonate production by 57-74% (significant at 50 ng L(-1))...
October 31, 2017: Chemosphere
https://www.readbyqxmd.com/read/29079777/pharmacological-preconditioning-with-gemfibrozil-preserves-cardiac-function-after-heart-transplantation
#2
Kálmán Benke, Csaba Mátyás, Alex Ali Sayour, Attila Oláh, Balázs Tamás Németh, Mihály Ruppert, Gábor Szabó, Gábor Kökény, Eszter Mária Horváth, István Hartyánszky, Zoltán Szabolcs, Béla Merkely, Tamás Radovits
While heart transplantation (HTX) is the definitive therapy of heart failure, donor shortage is emerging. Pharmacological activation of soluble guanylate cyclase (sGC) and increased cGMP-signalling have been reported to have cardioprotective properties. Gemfibrozil has recently been shown to exert sGC activating effects in vitro. We aimed to investigate whether pharmacological preconditioning of donor hearts with gemfibrozil could protect against ischemia/reperfusion injury and preserve myocardial function in a heterotopic rat HTX model...
October 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29069966/seasonal-occurrence-removal-and-risk-assessment-of-10-pharmaceuticals-in-two-sewage-treatment-plants-of-guangdong-china
#3
Ying Tang, Lu-Lu Guo, Cheng-Yang Hong, Yong-Xin Bing, Zhen-Cheng Xu
A long term investigation, which covered 10 sampling campaigns over three years, was performed to evaluate the occurrence, removal and risk of ten pharmaceuticals in two full-scale sewage treatment plants (STPs) in Guangdong, South China. Target pharmaceuticals except for clofibrate and ibuprofen were detected in every sample, with mean concentrations of 12.5-685.6 ng/L and 7.9-130.3 ng/L in the influent and effluent, respectively. Salicylic acid was the most abundant compound in both the influents and effluents in the two STPs...
October 25, 2017: Environmental Technology
https://www.readbyqxmd.com/read/28990588/triglycerides-cross-the-blood-brain-barrier-and-induce-central-leptin-and-insulin-receptor-resistance
#4
W A Banks, S A Farr, T S Salameh, M L Niehoff, E M Rhea, J E Morley, A J Hanson, K M Hansen, S Craft
OBJECTIVE: Resistance at the brain receptors for leptin and insulin has been associated with increased feeding, obesity and cognitive impairments. The causal agent for central resistance is unknown but could be derived from the blood. Here we postulate whether hypertriglyceridemia, the major dyslipidemia of the metabolic syndrome, could underlie central leptin and insulin resistance. DESIGN: We used radioactively labeled triglycerides to measure blood-brain barrier (BBB) penetration, western blots to measure receptor activation, and feeding and cognitive tests to assess behavioral endpoints...
October 9, 2017: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/28951665/prevalence-of-potential-drug-interactions-in-thai-patients-receiving-simvastatin-the-causality-assessment-of-musculoskeletal-adverse-events-induced-by-statin-interaction
#5
Methira Siriangkhawut, Patthana Tansakul, Verawan Uchaipichat
Drug-drug interactions are one of the major risk factors associated with statin-induced myopathy. Although simvastatin is widely used in Thailand, studies investigating the prevalence of potential simvastatin-drug interactions (SDIs) and its clinical relevance in Thai population are still limited. We aimed to investigate the prevalence of potential SDIs (phase 1 study) and musculoskeletal adverse effects (AEs) associated with those interactions (phase 2 study). A phase 1 study was retrospectively conducted with outpatients at a 60-bed hospital who received simvastatin between July 1, 2012 and June 30, 2013...
September 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28946176/species-related-exposure-of-phase-ii-metabolite-gemfibrozil-1-o-%C3%AE-glucuronide-between-human-and-mice-a-net-induction-of-mouse-p450-activity-was-revealed
#6
Min Luo, Manyun Dai, Hante Lin, Minzhu Xie, Jiao Lin, Aiming Liu, Julin Yang
Gemfibrozil is a fibrate drug widely used for dyslipidemia associated with atherosclerosis. Clinically, both gemfibrozil and its phase II metabolite gemfibrozil1-O-β-glucuronide (gem-glu) are involved in drug-drug interaction (DDI). But the DDI risk caused by gem-glu between human and mice has not been compared. In this study, 6 volunteers were recruited and took therapeutic dose of gemfibrozil for 3 days for examination of the gemfibrozil and gem-glu level in human. Male mice were fed a gemfibrozil diet (0...
September 25, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28941579/-fibrates-and-risk-of-venous-thromboembolism-case-no-case-study-in-french-pharmacovigilance-database
#7
Xavier Humbert, Charles Dolladille, Marion Sassier, Marie-Blanche Valnet-Rabier, Thierry Vial, Emmanuelle Guitton, Annabelle Page, Elodie Sole, Pascal Auriche, Antoine Coquerel, Joachim Alexandre, Sophie Fedrizzi
INTRODUCTION: Several studies have investigated the occurrence of venous thromboembolic events (phlebitis and pulmonary embolism) [VTE] and fibrates. Fibrates could be associated with VTE although published data are contradictory. The objective of this study is to confirm the link between VTE and fibrates. MATERIALS AND METHODS: Retrospective disproportionality analysis (case/non-case method) from observations recorded consecutively in the French pharmacovigilance database between 1985 and 2016...
August 1, 2017: Thérapie
https://www.readbyqxmd.com/read/28866393/occurrence-distribution-and-environmental-risk-of-pharmaceutically-active-compounds-phacs-in-coastal-and-ocean-waters-from-the-gulf-of-cadiz-sw-spain
#8
Miriam Biel-Maeso, Rosa María Baena-Nogueras, Carmen Corada-Fernández, Pablo A Lara-Martín
In this study, we have evaluated the occurrence and distribution of 78 pharmaceuticals in different aquatic marine environments from the Gulf of Cadiz (SW Spain) for the first time. The obtained results revealed that pharmaceuticals were present in seawater at total concentrations ranging 61-2133 and 16-189ngL(-1) in coastal and oceanic transects, respectively. Potential marine pollution hotspots were observed in enclosed or semi-enclosed water bodies (Cadiz Bay), showing concentrations that were one or two orders of magnitude higher than in the open ocean...
January 15, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/28865372/impact-of-inoculum-sources-on-biotransformation-of-pharmaceuticals-and-personal-care-products
#9
Sunah Kim, Karen Rossmassler, Corey D Broeckling, Sarah Galloway, Jessica Prenni, Susan K De Long
Limited knowledge of optimal microbial community composition for PPCP biotreatment, and of the microbial phylotypes that drive biotransformation within mixed microbial communities, has hindered the rational design and operation of effective and reliable biological PPCP treatment technologies. Herein, bacterial community composition was investigated as an isolated variable within batch biofilm reactors via comparison of PPCP removals for three distinct inocula. Inocula pre-acclimated to model PPCPs were derived from activated sludge (AS), ditch sediment historically-impacted by wastewater treatment plant effluent (Sd), and material from laboratory-scale soil aquifer treatment (SAT) columns...
November 15, 2017: Water Research
https://www.readbyqxmd.com/read/28809556/radical-chemistry-and-structural-relationships-of-ppcp-degradation-by-uv-chlorine-treatment-in-simulated-drinking-water
#10
Kaiheng Guo, Zihao Wu, Chii Shang, Bo Yao, Shaodong Hou, Xin Yang, Weihua Song, Jingyun Fang
The UV/chlorine process is an emerging advanced oxidation process (AOP) used for the degradation of micropollutants. However, the radical chemistry of this AOP is largely unknown for the degradation of numerous structurally diverse micropollutants in water matrices of varying quality. These issues were addressed by grouping 34 pharmaceuticals and personal care products (PPCPs) according to the radical chemistry of their degradation in the UV/chlorine process at practical PPCP concentrations (1 μg L(-1)) and in different water matrices...
August 31, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28808332/magnetic-microsphere-based-portable-solid-phase-extraction-device-for-on-site-pre-concentration-of-organics-from-large-volume-water-samples
#11
Zhijian Yao, Qingqing Zhao, Yan Ma, Wei Wang, Qing Zhou, Aimin Li
In this research a new magnetic material called M88 was fully synthetized and characterized for the extraction of pharmaceutical and personal care products in water samples. In addition, a portable prototype of magnetic solidphase extraction (MSPE) device was developed for the onsite preconcentration. The MSPE coupling with high performance liquid chromatography-Diode array detector (HPLC-DAD) method was developed and validated for simultaneous analysis of 11 PPCPs (mefenamic acid, chloroamphenicol, ketoprofen, clofibric acid, indometacin, acetylsalicylic acid, bisphenol A, phenylphenol, gemfibrozil, triclosan, and ibuprofen) in environmental water samples...
August 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28798859/amelioration-of-abnormalities-associated-with-the-metabolic-syndrome-by-spinacia-oleracea-spinach-consumption-and-aerobic-exercise-in-rats
#12
Vandana Panda, Kinjal Mistry, S Sudhamani, Mukesh Nandave, Shreesh Kumar Ojha
The present study evaluates the protective effects of an antioxidant-rich extract of Spinacea oleracea (NAOE) in abnormalities associated with the metabolic syndrome (MetS) in rats. HPTLC of NAOE revealed the presence of 13 total antioxidants, 14 flavonoids, and 10 phenolic acids. Rats administered with fructose (20% w/v) in drinking water for 45 days to induce abnormalities of MetS received NAOE (200 and 400 mg/kg, po), the standard drug gemfibrozil (60 mg/kg, po), aerobic exercise (AE), and a combination of NAOE 400 mg/kg and AE (NAOEAE) daily for 45 days...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28752027/the-potential-of-natural-products-for-targeting-ppar%C3%AE
#13
REVIEW
Daniela Rigano, Carmina Sirignano, Orazio Taglialatela-Scafati
Peroxisome proliferator activated receptors (PPARs) α, -γ and -β/δ are ligand-activated transcription factors and members of the superfamily of nuclear hormone receptor. These receptors play key roles in maintaining glucose and lipid homeostasis by modulating gene expression. PPARs constitute a recognized druggable target and indeed several classes of drugs used in the treatment of metabolic disease symptoms, such as dyslipidemia (fibrates, e.g. fenofibrate and gemfibrozil) and diabetes (thiazolidinediones, e...
July 2017: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/28735742/genotoxicity-of-gemfibrozil-in-the-gilthead-seabream-sparus-aurata
#14
A Barreto, L G Luis, A M V M Soares, P Paíga, L H M L M Santos, C Delerue-Matos, K Hylland, S Loureiro, M Oliveira
Widespread use of pharmaceuticals and suboptimal wastewater treatment have led to increased levels of these substances in aquatic ecosystems. Lipid-lowering drugs such as gemfibrozil, which are among the most abundant human pharmaceuticals in the environment, may have deleterious effects on aquatic organisms. We examined the genotoxicity of gemfibrozil in a fish species, the gilthead seabream (Sparus aurata), which is commercially important in southern Europe. Following 96-h waterborne exposure, molecular (erythrocyte DNA strand breaks) and cytogenetic (micronuclei and other nuclear abnormalities in cells) endpoints were measured...
September 2017: Mutation Research
https://www.readbyqxmd.com/read/28715853/effect-of-gemfibrozil-and-rifampicin-on-the-pharmacokinetics-of-selexipag-and-its-active-metabolite-in-healthy-subjects
#15
Shirin Bruderer, Marc Petersen-Sylla, Margaux Boehler, Tatiana Remeňová, Atef Halabi, Jasper Dingemanse
AIMS: Based on in vitro data, there is evidence to suggest that cytochrome P450 (CYP) 2C8 is involved in the metabolism of selexipag and its active metabolite, ACT-333679. The present study evaluated the possible pharmacokinetic interactions of selexipag with gemfibrozil, a strong CYP2C8 inhibitor, and rifampicin, an inducer of CYP2C8. METHODS: The study consisted of two independent parts, each conducted according to an open-label, randomized, crossover design. The pharmacokinetics and safety of selexipag and ACT-333679 were studied following single-dose administration either alone or in the presence of multiple-dose gemfibrozil (part I) or rifampicin (part II) in healthy male subjects...
July 17, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28693900/biodegradation-of-pharmaceuticals-and-endocrine-disruptors-with-oxygen-nitrate-manganese-iv-iron-iii-and-sulfate-as-electron-acceptors
#16
Natalie Schmidt, Declan Page, Andreas Tiehm
Biodegradation of pharmaceuticals and endocrine disrupting compounds was examined in long term batch experiments for a period of two and a half years to obtain more insight into the effects of redox conditions. A mix including lipid lowering agents (e.g. clofibric acid, gemfibrozil), analgesics (e.g. diclofenac, naproxen), beta blockers (e.g. atenolol, propranolol), X-ray contrast media (e.g. diatrizoic acid, iomeprol) as well as the antiepileptic carbamazepine and endocrine disruptors (e.g. bisphenol A, 17α-ethinylestradiol) was analyzed in batch tests in the presence of oxygen, nitrate, manganese (IV), iron (III), and sulfate...
August 2017: Journal of Contaminant Hydrology
https://www.readbyqxmd.com/read/28689959/removal-of-nutrients-and-pharmaceuticals-and-personal-care-products-from-wastewater-using-periphyton-photobioreactors
#17
Du Kang, Qichao Zhao, Yonghong Wu, Chenxi Wu, Wu Xiang
In this work, periphyton photobioreactors were built and were used for the treatment of synthetic wastewater spiked with PPCPs under different operational conditions. The removal rates of total nitrogen were relatively stable and varied from 39% to 77% overtime in different treatments. However, the removal rates of soluble reactive phosphorus decreased overtime from 42% to 68% on day 2 to 15.8% to 44% on day 22. For the selected PPCPs, only bisphenol A was effectively removed (72%-86.4%), hydrochlorothiazide and ibuprofen were moderately removed (26...
June 29, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/28653847/glucuronides-as-potential-anionic-substrates-of-human-cytochrome-p450-2c8-cyp2c8
#18
Yong Ma, Yue Fu, S Cyrus Khojasteh, Deepak Dalvie, Donglu Zhang
Glucuronidation is in general considered as a terminal metabolic step that leads to direct elimination of drugs and generally abolishes their biological activity. However, there is growing evidence to suggest that glucuronides can be ligands of human CYP2C8, making CYP2C8 distinct from the other CYP isoforms. Several classes of glucuronide conjugates, which include acyl glucuronides, ether glucuronides, N-glucuronides, and carbamoyl glucuronides, have been shown to be substrates or time-dependent inhibitors of CYP2C8...
June 27, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28623936/safety-and-potential-efficacy-of-gemfibrozil-as-a-supportive-treatment-for-children-with-late-infantile-neuronal-ceroid-lipofuscinosis-and-other-lipid-storage-disorders
#19
REVIEW
Kyeongsoon Kim, Hynda K Kleinman, Hahn-Jun Lee, Kalipada Pahan
Neuronal Ceroid Lipofuscinosis (NCL), also known as Batten disease, is a group of genetically distinct lysosomal disorders that mainly affect the central nervous system, resulting in progressive motor and cognitive decline primarily in children. Multiple distinct genes involved in the metabolism of lipids have been identified to date with various mutations in this family of diseases. There is no cure for these diseases but some new therapeutic approaches have been tested that offer more hope than the standard palliative care...
June 17, 2017: Orphanet Journal of Rare Diseases
https://www.readbyqxmd.com/read/28547184/combination-of-magnetic-dispersive-micro-solid-phase-extraction-and-supramolecular-solvent-based-microextraction-followed-by-high-performance-liquid-chromatography-for-determination-of-trace-amounts-of-cholesterol-lowering-drugs-in-complicated-matrices
#20
Somayeh Arghavani-Beydokhti, Maryam Rajabi, Alireza Asghari
A novel, efficient, rapid, simple, sensitive, selective, and environmentally friendly method termed magnetic dispersive micro solid-phase extraction combined with supramolecular solvent-based microextraction (Mdμ-SPE-SSME) followed by high-performance liquid chromatography (HPLC) with UV detection is introduced for the simultaneous microextraction of cholesterol-lowering drugs in complicated matrices. In the first microextraction procedure, using layered double hydroxide (LDH)-coated Fe3O4 magnetic nanoparticles, an efficient sample cleanup is simply and rapidly provided without the need for time-consuming centrifugation and elution steps...
May 26, 2017: Analytical and Bioanalytical Chemistry
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