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https://www.readbyqxmd.com/read/29782986/antiglycation-study-of-hmg-r-inhibitors-and-tocotrienol-against-glycated-bsa-and-ldl-a-comparative-study
#1
Rabia Nabi, Sahir Sultan Alvi, Rizwan Khan, Shafeeque Ahmad, Saheem Ahmad, M Salman Khan
Non-enzymatic glycation mediated advanced glycation end products (AGEs) generation results in the pathogenesis of diabetic complications and atherosclerotic cardiovascular disease (ASCVD) which is greatly influenced by 3-hydroxy-3-methyl-glutaryl Co-A reductase (HMG-R) activity. HMG-R inhibitors, statins, are well known for reducing mortality and morbidity of ASCVD in patients with diabetes due to their pleiotropic effects independent of cholesterol lowering. Due to distinct chemical structures, various statins may play important role in the inhibition of AGEs mediated pathologies...
May 18, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29768081/unremarkable-impact-of-oatp-inhibition-on-the-liver-concentration-of-fluvastatin-lovastatin-and-pitavastatin-in-wild-type-and-oatp1a-1b-knockout-mouse
#2
Jae H Chang, Xiaolin Zhang, Kirsten Messick, Yi-Chen Chen, Eugene Chen, Jonathan Cheong, Justin Ly
1. OATP inhibitors have been shown to significantly increase the plasma exposure of statins. However, understanding alterations of liver concentration is also important. While modeling has simulated liver concentration changes, availability of experimental data is limited, especially when concerning drug-drug interactions (DDI). The objective of this work was to determine blood and liver concentrations of fluvastatin, lovastatin and pitavastatin, when blocking uptake transporters. 2. In wild-type mouse, rifampin pre-treatment decreased the unbound liver-to-plasma ratio (Kp,uu ) of fluvastatin by 4...
May 16, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29748935/comparative-study-of-the-dose-dependence-of-oatp1b-inhibition-by-rifampicin-using-probe-drugs-and-endogenous-substrates-in-healthy-volunteers
#3
Issey Takehara, Takashi Yoshikado, Keiko Ishigame, Daiki Mori, Ken-Ichi Furihata, Nobuaki Watanabe, Osamu Ando, Kazuya Maeda, Yuichi Sugiyama, Hiroyuki Kusuhara
PURPOSE: To evaluate association of the dose-dependent effect of rifampicin, an OATP1B inhibitor, on the plasma concentration-time profiles among OATP1B substrates drugs and endogenous substrates. METHODS: Eight healthy volunteers received atorvastatin (1 mg), pitavastatin (0.2 mg), rosuvastatin (0.5 mg), and fluvastatin (2 mg) alone or with rifampicin (300 or 600 mg) in a crossover fashion. The plasma concentrations of these OATP1B probe drugs, total and direct bilirubin, glycochenodeoxycholate-3-sulfate (GCDCA-S), and coproporphyrin I, were determined...
May 10, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29746136/relative-activity-factor-raf-based-scaling-of-uptake-clearance-mediated-by-organic-anion-transporting-polypeptide-oatp-1b1-and-oatp1b3-in-human-hepatocytes
#4
Saki Izumi, Yoshitane Nozaki, Hiroyuki Kusuhara, Koichiro Hotta, Toshiki Mochizuki, Takafumi Komori, Kazuya Maeda, Yuichi Sugiyama
In vitro-in vivo extrapolation based on uptake clearance determined in human hepatocytes has been used to predict in vivo hepatic clearance of organic anion transporting polypeptide (OATP) substrates. This study evaluated the relative activity factor (RAF) approach to extrapolate active uptake clearance in transporter-transfected cell systems (CLuptake ) to that in human hepatocyte suspensions (PSinf,act ). RAF values for OATP1B1 and OATP1B3 were determined in two batches of cryopreserved human hepatocytes using estrone-3-sulfate and cholecystokinin octapeptide as reference substrates, respectively...
May 10, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29723430/relationships-of-changes-in-pharmacokinetic-parameters-of-substrate-drugs-in-drug-drug-interactions-on-metabolizing-enzymes-and-transporters
#5
Shinji Yamazaki
A general objective of drug-drug interaction (DDI) studies is to determine whether potential interactions of new molecular entities with concomitantly administered other drugs exist and, if DDIs occur, whether dosage adjustments are required. A typical end point for DDI evaluations is the ratio of area under the plasma concentration-time curve (AUC) of substrate drugs (AUCR), whereas the ratios of maximal plasma concentration (Cmax ) and terminal half-life (t1/2 ) are also important to understand DDI mechanisms (Cmax R and t1/2 R, respectively)...
May 3, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29701749/simultaneous-determination-of-rosuvastatin-naringin-and-naringenin-in-rat-plasma-by-rrlc-ms-ms-and-its-application-to-a-pharmacokinetic-drug-interaction-study
#6
Xuan Zeng, Weiwei Su, Hong Liu, Yuying Zheng, Taobin Chen, Weijian Zhang, Zenghao Yan, Yang Bai, Hongliang Yao
A rapid resolution liquid chromatography tandem mass spectrometry method was developed and validated for simultaneous determination of rosuvastatin, naringin and naringenin in rat plasma. Chromatographic separation of analytes and internal standard (fluvastatin for rosuvastatin, while isoquercitrin for naringin and naringenin) was performed on Agilent Poroshell 120 EC-C18 column (3.0 × 50 mm, 2.7 μm) using gradient elution with a mobile phase of methanol and water, both with 0.1% formic acid (v/v). The detection was operated in multiple reaction monitoring mode to monitor the precursor-to-product ion transitions of m/z 579...
April 26, 2018: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/29693013/effect-of-stains-on-ldl-reduction-and-liver-safety-a-systematic-review-and-meta-analysis
#7
REVIEW
Xiao Liang, Qin He, Qinghua Zhao
Background and Aim: Statin is a class of medications used to decrease low-density lipoprotein cholesterol level to prevent cardiovascular disease. However, the risk of hepatic damage caused by statin therapy is still controversial. We conducted a systematic review and meta-analysis summarizing the existing evidence of the effect of statin therapy on incidence of liver injury to clarify whether statin therapy could lead to liver function test abnormalities. Methods: We searched the Cochrane Library, PubMed, and Embase database for the relevant studies update till Jan...
2018: BioMed Research International
https://www.readbyqxmd.com/read/29670468/analysis-of-drug-effects-on-primary-human-coronary-artery-endothelial-cells-activated-by-serum-amyloid-a
#8
K Lakota, D Hrušovar, M Ogrič, K Mrak-Poljšak, S Čučnik, M Tomšič, B Božič, P Žigon, S Sodin-Semrl
Background: RA patients have a higher incidence of cardiovascular diseases compared to the general population. Serum amyloid A (SAA) is an acute-phase protein, upregulated in sera of RA patients. Aim: To determine the effects of medications on SAA-stimulated human coronary artery endothelial cells (HCAEC). Methods: HCAEC were preincubated for 2 h with medications from sterile ampules (dexamethasone, methotrexate, certolizumab pegol, and etanercept), dissolved in medium (captopril) or DMSO (etoricoxib, rosiglitazone, meloxicam, fluvastatin, and diclofenac)...
2018: Mediators of Inflammation
https://www.readbyqxmd.com/read/29665899/-statins-regulate-the-proliferation-and-apoptosis-of-t-all-cells-through-the-inhibition-of-akt-pathway
#9
Jun-Jie Wang, Yu Tian, Kai-Lin Xu, Rui-Xue Fu, Ming-Shan Niu, Kai Zhao
OBJECTIVE: To investigate the effect of Statins on proliferation and apoptosis in human acute T lymphocytic leukemia (T-ALL) cells and its possible mechanism. METHODS: Jurkat and CCRF-CEM cells were cultured in different concentrations of Fluvastatin and Simvastatin for 24 h respectively. Then, the cell growth inhibition level was defected by CCK-8; the DNA replication was analyzed by EdU; the cell apoptosis was analyzed by Annexin V/7-AAD double labeling; the cell cycle changes were analyzed by flow cytometry; the expressions of Cyclin D1, p21, p27, BAX, BCL-2 and p-Akt were determined by Western blot...
April 2018: Zhongguo Shi Yan Xue Ye Xue za Zhi
https://www.readbyqxmd.com/read/29607441/in-hospital-mortality-following-traumatic-brain-injury-among-older-medicare-beneficiaries-comparing-statin-users-with-nonusers
#10
Bilal Khokhar, Linda Simoni-Wastila, Julia F Slejko, Eleanor Perfetto, Min Zhan, Gordon S Smith
Background: Traumatic brain injury (TBI) is a significant public health concern for older adults. Small-scale human studies have suggested pre-TBI statin use is associated with decreased in-hospital mortality following TBI, highlighting the need for large-scale translational research. Objective: To investigate the relationship between pre-TBI statin use and in-hospital mortality following TBI. Methods: A retrospective study of Medicare beneficiaries 65 and older hospitalized with a TBI during 2006 to 2010 was conducted to assess the impact of pre-TBI statin use on in-hospital mortality following TBI...
December 2017: Journal of Pharmacy Technology: JPT: Official Publication of the Association of Pharmacy Technicians
https://www.readbyqxmd.com/read/29522792/differences-in-statin-associated-neuroprotection-corresponds-with-either-decreased-production-of-il-1%C3%AE-or-tnf-%C3%AE-in-an-in-vitro-model-of-neuroinflammation-induced-neurodegeneration
#11
A J McFarland, A K Davey, C M McDermott, G D Grant, J Lewohl, S Anoopkumar-Dukie
3-Hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors (statins) have been associated with conflicting effects within the central nervous system (CNS), with underlying mechanisms remaining unclear. Although differences between individual statins' CNS effects have been reported clinically, few studies to date have compared multiple statins' neuroprotective effects. This study aimed to compare six statins (atorvastatin, fluvastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin; 0-100 μM) using an in vitro model of lipopolysaccharide (LPS)-induced neuroinflammation and subsequent neurodegeneration...
April 1, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29521223/effects-of-a-series-of-acidic-drugs-on-l-lactic-acid-transport-by-the-monocarboxylate-transporters-mct1-and-mct4
#12
Yat H Leung, Francois Belanger, Jennifer Lu, Jacques Turgeon, Veronique Michaud
BACKGROUND: Drug-induced myopathy is a serious side effect that often requires removal of a medication from a drug regimen. For most drugs, the underlying mechanism of drug-induced myopathy remains unclear. Monocarboxylate transporters (MCTs) mediate L-lactic acid transport, and inhibition of MCTs may potentially lead to perturbation of L-lactic acid accumulation and muscular disorders. Therefore, we hypothesized that L-lactic acid transport may be involved in the development of drug-induced myopathy...
2017: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/29520172/fluvastatin-inhibits-advanced-glycation-end-products-induced-proliferation-migration-and-extracellular-matrix-accumulation-in-vascular-smooth-muscle-cells-by-targeting-connective-tissue-growth-factor
#13
Ae-Rang Hwang, Ju-Ock Nam, Young Jin Kang
Connective tissue growth factor (CTGF) is a novel fibrotic mediator, which is considered to mediate fibrosis through extracellular matrix (ECM) synthesis in diabetic cardiovascular complications. Statins have significant immunomodulatory effects and reduce vascular injury. We therefore examined whether fluvastatin has anti-fibrotic effects in vascular smooth muscle cells (VSMCs) and elucidated its putative transduction signals. We show that advanced glycation end products (AGEs) stimulated CTGF mRNA and protein expression in a time-dependent manner...
March 2018: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29508377/fluvastatin-for-lowering-lipids
#14
REVIEW
Stephen P Adams, Sarpreet S Sekhon, Michael Tsang, James M Wright
BACKGROUND: Fluvastatin is thought to be the least potent statin on the market, however, the dose-related magnitude of effect of fluvastatin on blood lipids is not known. OBJECTIVES: Primary objectiveTo quantify the effects of various doses of fluvastatin on blood total cholesterol, low-density lipoprotein (LDL cholesterol), high-density lipoprotein (HDL cholesterol), and triglycerides in participants with and without evidence of cardiovascular disease.Secondary objectivesTo quantify the variability of the effect of various doses of fluvastatin...
March 6, 2018: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29482467/the-role-of-oral-fluvastatin-on-postoperative-peritoneal-adhesion-formation-in-an-experimental-rat-model
#15
Yinzi Yue, Shuai Yan, Huan Li, Yang Zong, Jin Yue, Li Zeng
BACKGROUND: Postoperative peritoneal adhesions are a momentousness complication after abdominal surgery. Although varied means have been used to prevent and treat adhesions, the effects have not been satisfactory. Fluvastatin, a HMG-CoA reductase inhibitors, exhibits a variety of pharmacological effects. Aim of this study was to evaluate the effect of fluvastatin on postoperative peritoneal adhesion formation. METHODS: Seventy-five male Wistar rats weighting 220-250g were randomly assigned equally to three groups...
February 26, 2018: Acta Chirurgica Belgica
https://www.readbyqxmd.com/read/29445111/fluvastatin-protects-cochleae-from-damage-by-high-level-noise
#16
Claus-Peter Richter, Hunter Young, Sonja V Richter, Virginia Smith-Bronstein, Stuart R Stock, Xianghui Xiao, Carmen Soriano, Donna S Whitlon
Exposure to noise and ototoxic drugs are responsible for much of the debilitating hearing loss experienced by about 350 million people worldwide. Beyond hearing aids and cochlear implants, there have been no other FDA approved drug interventions established in the clinic that would either protect or reverse the effects of hearing loss. Using Auditory Brainstem Responses (ABR) in a guinea pig model, we demonstrate that fluvastatin, an inhibitor of HMG-CoA reductase, the rate-limiting enzyme of the mevalonate pathway, protects against loss of cochlear function initiated by high intensity noise...
February 14, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29442055/incidence-of-statin-drug-interactions-in-croatian-community-pharmacy
#17
I Samardzic, I Benkovic, V Bacic Vrca
Statins are among the most frequently issued drugs that patients usually need to take for a lifetime. They are often an integral part of a polytherapeutic approach in preventing and treating cardiovascular diseases. As such, they might often interact with drugs prescribed for treating acute and chronic conditions. A pharmacist is the final professional control before a drug reaches the patient and his role in preventing drug-drug interactions is crucial. The objective of this research was to analyse the incidence and relevance of potential drug interactions with statins in community pharmacy...
March 1, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29427912/adjunctive-therapy-with-statins-in-schizophrenia-patients-a-meta-analysis-and-implications
#18
Hong Shen, Rui Li, Rong Yan, Xia Zhou, Xia Feng, Mengjie Zhao, Hong Xiao
There are some conflicting results regarding the benefit of adjunctive therapy with statins for severity of negative symptoms in schizophrenia. This study aimed to verify whether statins use for adjunctive therapy was indeed beneficial to improve psychiatric symptoms in schizophrenia. The data were from CENTRAL, PubMed, Embase and MEDLINE. The Boolean search term used for the electronic database search was (statin OR simvastatin OR atorvastatin OR fluvastatin OR lovastatin OR mevastatin OR pitavastatin OR pravastatin OR rosuvastatin OR cerivastatin) and (schizophrenia OR schizoaffective disorder OR psychosis)...
April 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29409499/mechanisms-of-multiple-neurotransmitters-in-the-effects-of-lycopene-on-brain-injury-induced-by-hyperlipidemia
#19
Weichun Yang, Ziyi Shen, Sixian Wen, Wei Wang, Minyu Hu
BACKGROUND: Lycopene is a kind of carotenoid, with a strong capacity of antioxidation and regulating the bloodlipid. There has been some evidence that lycopene has protective effects on the central nervous system, but few studies have rigorously explored the role of neurotransmitters in it. Therefore, the present study was designed to investigate the effects of several neurotransmitters as lycopene exerts anti-injury effects induced by hyperlipidemia. METHODS: Eighty adult SD rats, half male and half female, were randomly divided into eight groups on the basis of serum total cholesterol (TC) levels and body weight...
February 7, 2018: Lipids in Health and Disease
https://www.readbyqxmd.com/read/29405807/interaction-of-deoxyschizandrin-and-schizandrin-b-with-liver-uptake-transporters-oatp1b1-and-oatp1b3
#20
Yanli Lu, Qingqing Hu, Lin Chen, Hong Zhang, Shibo Huang, Yuqing Xiong, Chunhua Xia
1. Deoxyschizandrin and schizandrin B have diverse pharmacological effects, including hepatoprotective activity. We aim to study their hepatic uptake and their effects on the hepatic uptake of other clinical drugs mediated by OATP1B1 and OATP1B3. 2. Deoxyschizandrin exhibited a high affinity for OATP1B1 with Km of 17.61 ± 0.43 μM but a low affinity for OATP1B3. Similarly, schizandrin B also showed a strong affinity for OATP1B1 with Km of 18.45 ± 1.23 μM but a weak affinity for OATP1B3. 3. Atorvastatin and rifampicin could inhibit the uptake of deoxyschizandrin and schizandrin B mediated by OATP1B1...
February 18, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
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