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https://www.readbyqxmd.com/read/28933256/combined-effect-of-telmisartan-and-fluvastatin-on-arachidonic-acid-metabolism-in-human-liver-microsomes
#1
Yuka Kato, Yuji Mukai, Anders Rane, Nobuo Inotsume, Takaki Toda
Epoxyeicosatrienoic acids (EETs), metabolites of arachidonic acid (AA) via cytochrome P450s, have a protective effect on the cardiovascular system involving vasodilation. We have previously demonstrated that telmisartan (TEL) inhibits EETs production from AA in vitro. The objectives of the study were to examine the inhibitory effect of fluvastatin (FLU), an inhibitor of CYP2C9, and the combined effect of TEL and FLU on the production of EETs using human liver microsomes. The combined effect of TEL and FLU was evaluated using two methods, the fixed concentration method and the fixed ratio method...
September 21, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28919704/secondary-prevention-of-major-cerebrovascular-events-with-seven-different-statins-a-multi-treatment-meta-analysis
#2
Ping Zhong, Danhong Wu, Xiaofei Ye, Ying Wu, Tuming Li, Shuwen Tong, Xueyuan Liu
BACKGROUND: Statins have been recommended for the use in atherosclerotic cardiovascular diseases, but different statins have distinct pharmacological characteristics. This multi-treatment meta-analysis aimed to evaluate the efficacy of seven statins in the secondary prevention of major cerebrovascular events (CVEs). METHODS AND ANALYSES: The PubMed, Embase, Cochrane Database of Systematic Reviews and Cochrane Central Register of Controlled Trials were searched to identify studies published between January 1, 2011, and June 30, 2016...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28883515/factor-xa-mediates-calcium-flux-in-endothelial-cells-and-is-potentiated-by-igg-from-patients-with-lupus-and-or-antiphospholipid-syndrome
#3
Bahar Artim-Esen, Natalia Smoktunowicz, Thomas McDonnell, Vera M Ripoll, Charis Pericleous, Ian Mackie, Eifion Robinson, David Isenberg, Anisur Rahman, Yiannis Ioannou, Rachel C Chambers, Ian Giles
Factor (F) Xa reactive IgG isolated from patients with antiphospholipid syndrome (APS) display higher avidity binding to FXa with greater coagulant effects compared to systemic lupus erythematosus (SLE) non APS IgG. FXa signalling via activation of protease-activated receptors (PAR) leads to increased intracellular calcium (Ca(2+)). Therefore, we measured alterations in Ca(2+) levels in human umbilical vein endothelial cells (HUVEC) following FXa-mediated PAR activation and investigated whether FXa reactive IgG from patients with APS or SLE/APS- alter these responses...
September 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28840831/fluvastatin-use-and-risk-of-acute-pancreatitis-a-population-based-case-control-study-in-taiwan
#4
Kuan-Fu Liao, Po-Tsung Huang, Ching-Chun Lin, Cheng-Li Lin, Shih-Wei Lai
OBJECTIVES: This study aimed to examine the association between fluvastatin use and acute pancreatitis in Taiwan. METHODS: Using the database from the Taiwan National Health Insurance (NHI) Program, we designed a case-control study which consisted of 3501 individuals aged 20-84 with new at-the-time diagnoses acute pancreatitis as the case group and 8373 randomly selected individuals without acute pancreatitis as the control group during the period of 1998-2011. Both groups were matched for sex, age, and index year of being diagnosed with acute pancreatitis...
September 2017: BioMedicine
https://www.readbyqxmd.com/read/28782480/recent-progress-in-biological-activities-of-indole-and-indole-alkaloids
#5
O M Singh, Thokchom Prasanta Singh
The indole scaffold is a prominent and privileged structural motif found in numerous natural products and in a wide range of bioactive heterocycles. Starting from the simple structural framework of serotonin, the well known neurotransmitter to complex alkaloids which are used clinically as anticancer agent, mitomycin C, and the antihypertensive alkaloid reserpine, the indole moiety is considered as the active principle. Thus over the past decade, a large number of indole-containing compounds have revealed remarkable pharmacological activity and their utility as therapeutic agents have attracted considerable attention from chemists...
August 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28744693/vegfa-involves-in-the-use-of-fluvastatin-and-zoledronate-against-breast-cancer
#6
Haihong Pu, Qingyuan Zhang, Chunbo Zhao, Lei Shi, Yan Wang, Jingxuan Wang, Minghui Zhang
Our study aimed to identify key genes involved in the use of fluvastatin and zoledronate against breast cancer, as well as to investigate the roles of vascular endothelial growth factor A (VEGFA) in the malignant behaviors of breast cancer cells. The expression data GSE33552 was downloaded from Gene Expression Omnibus database, including mocked-, fluvastatin- and zoledronate-treated MDA-MB-231 cells. Differentially expressed genes (DEGs) were identified in fluvastatin- and zoledronate-treated cells using limma package, respectively...
July 25, 2017: Pathology Oncology Research: POR
https://www.readbyqxmd.com/read/28741244/efficacy-and-safety-of-alternate-day-versus-daily-dosing-of-statins-a-systematic-review-and-meta-analysis
#7
REVIEW
Kamal Awad, Dimitri P Mikhailidis, Peter P Toth, Steven R Jones, Patrick Moriarty, Gregory Y H Lip, Paul Muntner, Alberico L Catapano, Michael J Pencina, Robert S Rosenson, Jacek Rysz, Maciej Banach
PURPOSE: We conducted a meta-analysis of randomized controlled trials (RCTs) and quasi-RCTs to synthesize evidence about the efficacy and safety of alternate-day vs daily dosing of statins. METHODS: We searched selected databases through January 2, 2017 to identify relevant RCTs and quasi-RCTs. The primary outcome was change in low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), and triglycerides (TG), while secondary outcomes included adverse events and adherence...
July 24, 2017: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/28722780/add-on-effects-of-fluvastatin-in-simeprevir-pegylated-interferon-ribavirin-combination-therapy-for-patients-with-genotype-1-hepatitis-c-virus-infection-a-randomized-controlled-study
#8
Goki Suda, Jun Ito, Atsushi Nagasaka, Yoshiya Yamamoto, Ken Furuya, Munenori Okamoto, Katsumi Terashita, Tomoe Kobayashi, Izumi Tsunematsu, Junichi Yoshida, Takashi Meguro, Masatsugu Ohara, Naoki Kawagishi, Megumi Kimura, Machiko Umemura, Takaaki Izumi, Yoko Tsukuda, Masato Nakai, Takuya Sho, Mitsuteru Natsuizaka, Kenichi Morikawa, Koji Ogawa, Naoya Sakamoto
BACKGROUND: The Japan Society of Hepatology guidelines indicate that HCV protease inhibitor combination therapy with simeprevir (SMV), pegylated-interferon (Peg-IFN), and ribavirin (RBV) is a therapeutic option for patients who fail to respond to a direct direct-acting antiviral (DAA) containing regimen. However, treatment outcomes have room for improvement. Fluvastatin (FLV) add-on treatment in Peg-IFN and RBV combination therapy for hepatitis C-infected patients significantly improved the sustained virological response (SVR), but the add-on effect of FLV on SMV combination therapy is not well understood...
July 19, 2017: Hepatology Research: the Official Journal of the Japan Society of Hepatology
https://www.readbyqxmd.com/read/28717145/acetylsalicylic-acid-differentially-limits-the-activation-and-expression-of-cell-death-markers-in-human-platelets-exposed-to-staphylococcus-aureus-strains
#9
Adrien Chabert, Pauline Damien, Paul O Verhoeven, Florence Grattard, Philippe Berthelot, Fabrice Zeni, Laurence Panicot-Dubois, Stéphane Robert, Françoise Dignat-George, Marie-Ange Eyraud, Bruno Pozzetto, Bernard Payrastre, Fabrice Cognasse, Olivier Garraud, Hind Hamzeh-Cognasse
Beyond their hemostatic functions, platelets alter their inflammatory response according to the bacterial stimulus. Staphylococcus aureus is associated with exacerbated inflammation and thrombocytopenia, which is associated with poor prognosis during sepsis. Acetylsalicylic acid and statins prevent platelet aggregation and decrease the mortality rate during sepsis. Therefore, we assessed whether these two molecules could reduce in vitro platelet activation and the inflammatory response to S. aureus. Platelets were exposed to clinical strains of S...
July 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28692940/betulinic-acid-and-fluvastatin-exhibits-synergistic-effect-on-toll-like-receptor-4-mediated-anti-atherogenic-mechanism-in-type-ii-collagen-induced-arthritis
#10
Limi Elizabeth Mathew, Vrinda Rajagopal, Helen A
Cardiovascular disease (CVD) is a major problem during rheumatoid arthritis which leads to morbidity and mortality in arthritic patients. So the present study emphasizes combinatorial effect of Betulinic acid, a triterpenoid and fluvastatin, an HMG CoA reductase inhibitor on atherogenesis during arthritis. Arthritis was induced by bovine type II collagen dissolved in 0.01M acetic acid at a concentration of 4mg/mL and emulsified in equal volume of incomplete Freund's adjuvant. Betulinic acid (2mg/kg) and fluvastatin (5mg/kg) alone and in combination was administered orally from day 14 to 60...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28674251/co-administration-of-fluvastatin-and-cyp3a4-and-cyp2c8-inhibitors-may-increase-the-exposure-to-fluvastatin-in-carriers-of-cyp2c9-genetic-variants
#11
Yuji Mukai, Masayuki Narita, Erika Akiyama, Kanami Ohashi, Yasutaka Horiuchi, Yuka Kato, Takaki Toda, Anders Rane, Nobuo Inotsume
Fluvastatin, which is one of the hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitors (statins), is primarily metabolized by CYP2C9 and to a lesser extent by CYP3A4 and CYP2C8. Predictions of drug-drug interactions (DDI) are important for the safety of combination therapies with statins, in particular drugs that are metabolized by CYP3A4. Little information is available regarding drug interactions with fluvastatin. Since CYP2C9 is a polymorphic enzyme, we investigated the effect of DDI via CYP2C9, CYP3A4, and CYP2C8 on fluvastatin pharmacokinetics by using a validated prediction method in relation to CYP2C9 variants...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28650504/experimental-and-theoretical-studies-on-fluvastatin-primary-photoproduct-formation
#12
Dorota Jarmużek, Tomasz Pedzinski, Marcin Hoffmann, Tomasz Siodła, Kinga Salus, Donata Pluskota-Karwatka
Fluvastatin (FLV) belongs to the group of compounds referred to as statins, also known as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Statins act as cholesterol-lowering agents and are among the most frequently prescribed drugs. They upregulate low-density lipoprotein receptors in the liver by binding to the active site of HMG-CoA reductase, which is the key enzyme in cholesterol biosynthesis. Statins have been detected as contaminants in natural waters and are susceptible to degradation upon exposure to light...
August 23, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28636885/differential-changes-in-the-pharmacokinetics-of-statins-in-collagen-induced-arthritis-rats
#13
Chun-Han Lin, Ke-Wei Hsu, Chia-Hao Chen, Yow-Shieng Uang, Chun-Jung Lin
The elevated systemic levels of cytokines in rheumatoid arthritis (RA) can change the expression of metabolic enzymes and transporters. Given that statins are lipid-lowering agents frequently used in RA patients with concurrent cardiovascular diseases, the objective of the present study was to investigate the impacts of RA on the pharmacokinetics of statins of different disposition properties in rats with collagen-induced arthritis (CIA). The expression of metabolic enzymes and transporters in tissues of CIA rats were analyzed by RT-qPCR...
June 19, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28620871/lipophilic-statins-and-the-risk-of-intracranial-hemorrhage-following-ischemic-stroke-a-population-based-study
#14
Kieran L Quinn, Erin M Macdonald, Muhammad M Mamdani, Christina Diong, David N Juurlink
BACKGROUND: Statins are commonly prescribed for the secondary prevention of ischemic stroke, but there is conflicting evidence as to whether they increase the risk of intracranial hemorrhage. Lipophilic statins cross the blood-brain barrier more freely than hydrophilic statins and may therefore increase the risk of intracranial hemorrhage. OBJECTIVE: To determine whether, in older patients following ischemic stroke, receipt of lipophilic statins was associated with differences in the risk of intracranial hemorrhage...
June 15, 2017: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/28583899/statins-do-not-inhibit-the-fgfr-signaling-in-chondrocytes
#15
B Fafilek, M Hampl, N Ricankova, I Vesela, L Balek, M Kunova Bosakova, I Gudernova, M Varecha, M Buchtova, P Krejci
OBJECTIVE: Statins are widely used drugs for cholesterol lowering, which were recently found to counteract the effects of aberrant fibroblast growth factor receptor (FGFR3) signaling in cell and animal models of FGFR3-related chondrodysplasia. This opened an intriguing therapeutic possibility for human dwarfing conditions caused by gain-of-function mutations in FGFR3, although the mechanism of statin action on FGFR3 remains unclear. Here, we determine the effect of statins on FGFR signaling in chondrocytes...
September 2017: Osteoarthritis and Cartilage
https://www.readbyqxmd.com/read/28550055/potential-drug-interactions-mediated-by-renal-organic-anion-transporter-oatp4c1
#16
Toshihiro Sato, Eikan Mishima, Nariyasu Mano, Takaaki Abe, Hiroaki Yamaguchi
Organic anion-transporting polypeptide 4C1 (OATP4C1) is an organic anion transporter expressed in the basolateral membrane of the renal proximal tubules. It plays a major role in the urinary excretion of both exogenous drugs and endogenous compounds. Our previous studies have indicated the importance of OATP4C1 in pathologic and physiologic conditions; however, the majority of its pharmacologic characteristics remained unclear. Therefore, to provide essential information for clinical drug therapy decisions and drug development, we clarified drug interactions mediated by OATP4C1...
August 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28548867/statins-determination-a-review-of-electrochemical-techniques
#17
I Antal, M Koneracka, V Zavisova, M Kubovcikova, Zh Kormosh, P Kopcansky
The use of electroanalytical techniques for the determination of statins (Atorvastatin, Fluvastatin, Lovastatin, Pitavastatin, Pravastatin, Rosuvastatin and Simvastatin) is reviewed covering the period from 1997 to 2016. Among all of the published electrochemical methods, voltammetry and polarography are the most popular techniques for determination of statins and both are used for the analysis of pharmaceutical dosage forms and biological samples. Determination of statins by potentiometric method using ion-selective electrodes is reported in only few papers...
May 26, 2017: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/28546815/role-of-statin-drugs-for-polycystic-ovary-syndrome
#18
REVIEW
Lisa Cassidy-Vu, Edwina Joe, Julienne K Kirk
Objective: To review the potential role and specific impact of statin drugs in women with PCOS. The evidence for this use of statins in PCOS is limited and still under further investigation. Materials and methods: A search was conducted using PubMed, DynaMed and PubMedHealth databases through October 16, 2016 using the terms polycystic ovary syndrome, PCOS, hydroxymethylglutaryl-CoA reductase inhibitors, hydroxymethylglutaryl-CoA, statin, atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin and simvastatin...
December 2016: Journal of Family & Reproductive Health
https://www.readbyqxmd.com/read/28546657/statins-reduce-lipopolysaccharide-induced-cytokine-and-inflammatory-mediator-release-in-an-in-vitro-model-of-microglial-like-cells
#19
A J McFarland, A K Davey, S Anoopkumar-Dukie
The anti-inflammatory effects of statins (HMG-CoA reductase inhibitors) within the cardiovascular system are well-established; however, their neuroinflammatory potential is unclear. It is currently unknown whether statins' neurological effects are lipid-dependent or due to pleiotropic mechanisms. Therefore, the assumption that all statin compounds will have the same effect within the central nervous system is potentially inappropriate, with no studies to date having compared all statins in a single model. Thus, the aim of this study was to compare the effects of the six statins (atorvastatin, fluvastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin) within a single in vitro model of neuroinflammation...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28542559/fluvastatin-inhibits-age-induced-cell-proliferation-and-migration-via-an-erk5-dependent-nrf2-pathway-in-vascular-smooth-muscle-cells
#20
Ae-Rang Hwang, Jung-Hwa Han, Jae Hyang Lim, Young Jin Kang, Chang-Hoon Woo
Advanced glycation endproduct (AGE)-induced vascular smooth muscle cell (VSMC) proliferation and reactive oxygen species (ROS) production are emerging as important mechanisms of diabetic vasculopathy, but little is known about the molecular mechanism responsible for the antioxidative effects of statins on AGEs. It has been reported that statins exert pleiotropic effects on the cardiovascular system due to decreases in AGE-induced cell proliferation, migration, and vascular inflammation. Thus, in the present study, the authors investigated the molecular mechanism by which statins decrease AGE-induced cell proliferation and VSMC migration...
2017: PloS One
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