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https://www.readbyqxmd.com/read/28532144/physically-targeted-intravenous-polyurethane-nanoparticles-for-controlled-release-of-atorvastatin-calcium
#1
Behnaz Sadat Eftekhari, Akbar Karkhaneh, Ali Alizadeh
Background: Intravenous drug delivery is an advantageous choice for rapid administration, immediate drug effect, and avoidance of first-pass metabolism in oral drug delivery. In this study, the synthesis, formulation, and characterization of atorvastatin-loaded polyurethane (PU) nanoparticles were investigated for intravenous route of administration. Methods: First, PU was synthesized and characterized. Second, nanoparticles were prepared in four different ratios of drug to polymer through two different techniques including emulsion-diffusion and single-emulsion...
May 23, 2017: Iranian Biomedical Journal
https://www.readbyqxmd.com/read/28529649/sak-hv-triggered-a-short-period-lipid-lowering-biotherapy-based-on-the-energy-model-of-liver-proliferation-via-a-novel-pathway
#2
Chao Zhang, Zhiguang Huang, Haoran Jing, Wenliang Fu, Min Yuan, Wenrong Xia, Ling Cai, Xiangdong Gan, Yao Chen, Minji Zou, Minhui Long, Jiaxi Wang, Min Wang, Donggang Xu
The accumulations of excess lipids within liver and serum are defined as non-alcoholic fatty liver disease (NAFLD) and hyperlipemia respectively. Both of them are components of metabolic syndrome that greatly threaten human health. Here, a recombinant fusion protein (SAK-HV) effectively treated NAFLD and hyperlipemia in high-fat-fed ApoE(-/-) mice, quails and rats within just 14 days. Its triglyceride and cholesterol-lowering effects were significantly better than that of atorvastatin during the observation period...
2017: Theranostics
https://www.readbyqxmd.com/read/28527109/erratum-to-clinical-pharmacokinetics-of-sacubitril-valsartan-lcz696-a-novel-angiotensin-receptor-neprilysin-inhibitor
#3
Surya Ayalasomayajula, Thomas Langenickel, Parasar Pal, Sreedevi Boggarapu, Gangadhar Sunkara
Sacubitril/valsartan (LCZ696) is indicated for the treatment of heart failure with reduced ejection fraction. Absorption of sacubitril/valsartan and conversion of sacubitril (prodrug) to sacubitrilat (neprilysin inhibitor) was rapid with maximum plasma concentrations of sacubitril, sacubitrilat, and valsartan (angiotensin receptor blocker) reaching within 0.5, 1.5-2.0, and 2.0-3.0 h, respectively. With a twofold increase in dose, an increase in the area under the plasma concentration-time curve was proportional for sacubitril, ~1...
May 19, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28526884/combined-use-of-metformin-and-atorvastatin-attenuates-atherosclerosis-in-rabbits-fed-a-high-cholesterol-diet
#4
Fei Luo, Yuan Guo, Gui-Yun Ruan, Jun-Ke Long, Xi-Long Zheng, Qin Xia, Shui-Ping Zhao, Dao-Quan Peng, Zhen-Fei Fang, Xiang-Ping Li
Statins are widely used to reduce cardiovascular risk. Unfortunately, some patients still experience cardiovascular events though prescribed with high-intensity statins. Metformin, an anti-diabetic drug, was reported to possess anti-atherosclerotic effects. Therefore, the experiments were designed to evaluate whether combined use of metformin and atorvastatin can achieve additional benefits. In rabbits fed a high-cholesterol diet, we evaluated the effects of the combination therapy on atherosclerotic plaques, lipid profiles, blood glucose levels, liver and kidney functions...
May 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28515189/10-year-trends-in-statin-utilization-in-taiwan-a-retrospective-study-using-taiwan-s-national-health-insurance-research-database
#5
Hsing-Chun Hsieh, Jason C Hsu, Christine Y Lu
OBJECTIVE: Statins have been commonly used to treat patients with hypercholesterolaemia and to prevent cardiovascular disease (CVD) worldwide. This study examined trends in use of statins in Taiwan from 2002 to 2011. DESIGN: This is a retrospective observational study focusing on the utilisation of statins. SETTING: The monthly claims data for statins between 2002 and 2011 were retrieved from Taiwan's National Health Insurance Research Database...
May 17, 2017: BMJ Open
https://www.readbyqxmd.com/read/28514518/a-retrosynthesis-approach-for-biocatalysis-in-organic-synthesis
#6
Uwe Bornscheuer, Rodrigo O M A de Souza, Leandro S M Miranda
Lead-In: For the planning of an organic synthesis route, the disconnection approach guided by retrosynthetic analysis of possible intermediates and the chemical reactions involved, back to ready available starting materials, is well established. In contrast, such concepts just get developed for biocatalytic routes. In this review we highlight functional group interconversions catalyzed by enzymes. The article is organized rather by chemical bonds formed - exemplified for C-N, C-O- and C-C-bonds - and not by enzyme classes, covering a broad range of reactions to incorporate the desired functionality in the target molecule...
May 17, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28513969/effect-of-steady-state-faldaprevir-on-pharmacokinetics-of-atorvastatin-or-rosuvastatin-in-healthy-volunteers-a-prospective-open-label-fixed-sequence-crossover-study
#7
Fenglei Huang, Kristell Marzin, Rüdiger Koenen, Klaus Peter Kammerer, Natalja Strelkowa, Mabrouk Elgadi, Anne-Marie Quinson, Sebastian Haertter
Faldaprevir (FDV) is a potent, orally administered inhibitor of hepatitis C virus protease. It inhibits multiple cytochrome P-450 enzymes and multiple membrane transporters. The objective of this study was to evaluate the effect of steady-state faldaprevir on the pharmacokinetics (PK) of a single dose of atorvastatin or rosuvastatin. In this single-center, open-label, fixed-sequence crossover study, 33 healthy adult male and female volunteers were given either atorvastatin 10 mg (n = 16) or rosuvastatin 10 mg (n = 17) on day 1...
May 17, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28513233/effect-of-statins-on-blood-pressure-analysis-on-adverse-events-released-by-fda
#8
Tao You, Xing-Guang Liu, Xiao-Dong Hou, Xin-Kuan Wang, Han-Hui Xie, Fan Ding, Kang Yi, Peng Zhang, Xiao-Dong Xie
OBJECTIVE: As a class of cholesterol-lowering drugs, statins have been reported to cause unexpected decrease in blood pressure (BP). However, most studies in this issue were subject to inadequate study design or very small sample size. The present study was designed to examine the BP-lowering effect of various statins. METHODS: Here we retrieved 5.9 million clinical reports submitted to FDA Adverse Event Reporting System (FAERS) from 2004 to 2015. Meta-analysis was performed to estimate the overall reporting odds ratio (ROR) of hypotension adverse events concurrent with various statins (i...
May 17, 2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28511404/statin-induced-rhabdomyolysis-with-non-oliguric-renal-failure-a-rare-presentation
#9
Hashir Kareem, Devavrata Sahu, Mugula Sudhakar Rao, Tom Devasia
Statins are safe, well tolerated, efficient and time tested drugs for the management of hypercholesterolemia, and thus play a cardinal role in the management of patients with heart disease. Although safe in clinical practice, they are associated with adverse effects, clinically the most important and most severe being muscle related complications/myotoxicity. Rhabdomyolysis, though rare, is the most severe form of myotoxicity. The US Food and Drug Administration (USFDA) adverse event reporting system reports rate of statin induced rhabdomyolysis at 0...
March 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28509674/evidence-for-more-intensive-cholesterol-lowering
#10
Handrean Soran, See Kwok, Safwaan Adam, Jan Hoong Ho, Paul N Durrington
PURPOSE OF REVIEW: In randomized clinical trials, reduction in cardiovascular disease (CVD) risk with cholesterol-lowering drugs correlates with the LDL cholesterol decrease. However, because the majority have investigated a fixed statin dose, current guidelines disagree about the use of statin dose titration or non-statin adjunctive cholesterol-lowering drugs. RECENT FINDINGS: We conducted a meta-analysis of all randomized controlled trials with CVD end-points, comparing two intensities of lipid-lowering regimens within the same population, using varying statins doses and/or potency, ezetimibe or PCSK9 inhibitors and compared the observed number of patients needed to be treated for 10 years to prevent one CVD event (NNT) with NNT predicted from trials of predominantly single-dose statin...
May 15, 2017: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/28506387/effects-of-atorvastatin-treatment-on-left-ventricular-diastolic-function-in-peritoneal-dialysis-patients-the-alevent-clinical-trial
#11
Cho-Kai Wu, Chih-Fan Yeh, Jiun-Yang Chiang, Ting-Tse Lin, Yi-Fan Wu, Chih-Kang Chiang, Tze-Wah Kao, Kuan-Yu Hung, Jenq-Wen Huang
BACKGROUND: Left ventricular diastolic dysfunction (LVDD) is common among patients undergoing peritoneal dialysis (PD). Increased levels of inflammatory biomarkers, such as high-sensitivity C-reactive protein, predict the development of LVDD. OBJECTIVES: We hypothesized that PD patients with elevated high-sensitivity C-reactive protein levels might benefit from statin treatment for LVDD and designed a randomized clinical trial to prove the hypothesis. METHODS: We screened 213 PD patients and randomly assigned 32 men and women with low-density lipoprotein cholesterol levels <130 mg/dL, high-sensitivity C-reactive protein levels of ≥1...
May 2017: Journal of Clinical Lipidology
https://www.readbyqxmd.com/read/28504565/early-intensive-statin-treatment-reduces-hard-cardiovascular-outcomes-after-acute-coronary-syndrome
#12
Gregory G Schwartz, Rana Fayyad, Michael Szarek, David DeMicco, Anders G Olsson
Background Early, intensive statin treatment is the standard of care after acute coronary syndrome (ACS). However, the benefit of this approach to prevent major adverse cardiovascular events has been demonstrated in only one randomised, placebo controlled trial. The Myocardial Ischemia Reduction with Aggressive Cholesterol Lowering (MIRACL) trial demonstrated that atorvastatin 80 mg daily, compared with placebo, reduced time to first occurrence of death, non-fatal myocardial infarction, resuscitated cardiac arrest, or hospitalisation for unstable angina (stroke not included) during the 16 week period following ACS...
January 1, 2017: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/28503146/statin-therapy-is-associated-with-reduced-risk-of-peptic-ulcer-disease-in-the-taiwanese-population
#13
Chun-Jung Lin, Wei-Chih Liao, Yu-An Chen, Hwai-Jeng Lin, Chun-Lung Feng, Cheng-Li Lin, Ying-Ju Lin, Min-Chuan Kao, Mei-Zi Huang, Chih-Ho Lai, Chia-Hung Kao
Although statin use may affect the severity of chronic gastritis and gastric cancer, no data exists about the relationship between statin therapy and risk of peptic ulcer disease (PUD) in patients. We investigated the effect of statin use and the incidence of PUD from the Taiwan National Health Insurance Research Database (NHIRD). A total of 35,194 patients records for medical claims were enrolled. We performed a population-based case-control analysis to compare the incidence of PUD in patients who were prescribed statins and that in patients who were not...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28500776/analysis-of-national-pharmacovigilance-data-associated-with-statin-use-in-korea-adverse-drug-reactions-with-statins
#14
Hyunah Kim, Namhyo Kim, Da Hee Lee, Hun-Sung Kim
The aim of this study was to evaluate clinical manifestations, age distribution and risk factors of adverse drug reactions (ADRs) of statins. Korean Adverse Event Reporting System (KAERS) database records (July 2009 - June 2014) on statin-treated adults were used. ADRs classified as "certain," "probable" and "possible" based on the WHO-Uppsala Monitoring Centre criteria were analysed. The frequency of ADRs was compared between adults (18-64 years) and older people (age ≥ 65 years) groups. In total, 2161 ADRs from 1690 patients (579, 34...
May 13, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28500253/linc00341-exerts-an-anti-inflammatory-effect-on-endothelial-cells-by-repressing-vcam1
#15
Tse-Shun Huang, Kuei-Chun Wang, Sara Quon, Phu Nguyen, Ting-Yu Chang, Zhen Chen, Yi-Shuan Li, Shankar Subramaniam, John Y-J Shyy, Shu Chien
The long non-coding RNAs (lncRNAs), which constitute a large portion of the transcriptome, have gained intense research interest because of their roles in regulating physiological and pathophysiological functions in the cell. We identified from RNA-seq profiling a set of lncRNAs in cultured human umbilical vein endothelial cells (HUVECs) that are differentially regulated by atheroprotective vs. atheroprone shear flows. Among the comprehensively annotated lncRNAs, including both known and novel transcripts, LINC00341 is one of the most abundant lncRNAs in endothelial cells...
May 12, 2017: Physiological Genomics
https://www.readbyqxmd.com/read/28499669/atorvastatin-reduces-cardiac-and-adipose-tissue-inflammation-in-rats-with-metabolic-syndrome
#16
Yuichiro Yamada, Shino Takeuchi, Mamoru Yoneda, Shogo Ito, Yusuke Sano, Kai Nagasawa, Natsumi Matsuura, Ayako Uchinaka, Toyoaki Murohara, Kohzo Nagata
BACKGROUND: Statins are strong inhibitors of cholesterol biosynthesis and help to prevent cardiovascular disease. They also exert additional pleiotropic effects that include an anti-inflammatory action and are independent of cholesterol, but the molecular mechanisms underlying these additional effects have remained unclear. We have now examined the effects of atorvastatin on cardiac and adipose tissue inflammation in DahlS.Z-Lepr(fa)/Lepr(fa) (DS/obese) rats, which we previously established as a model of metabolic syndrome (MetS)...
May 4, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28498386/atorvastatin-inhibits-cholesterol-induced-caspase-3-cleavage-through-down-regulation-of-p38-and-up-regulation-of-bcl-2-in-the-rat-carotid-artery
#17
Roshanak Bayatmakoo, Nadereh Rashtchizadeh, Parichehreh Yaghmaei, Mehdi Farhoudi, Pouran Karimi
AIM: Atherosclerotic lesions in the carotid arteries lead to a broad range of cerebrovascular disorders such as vascular dementia and ischaemic stroke. Recent studies have verified the beneficial role of atorvastatin (AV) in atherosclerosis. Despite a large body of studies, the mechanisms underlying this effect have not been completely explained. In this study, several experiments were performed on atherosclerotic rat models to investigate the anti-inflammatory and anti-apoptotic effect of AV in the carotid artery...
May 5, 2017: Cardiovascular Journal of Africa
https://www.readbyqxmd.com/read/28496308/atorvastatin-a-double-weapon-in-osteoporosis-treatment-an-experimental-and-clinical-study
#18
Naglaa El-Nabarawi, Mohamed El-Wakd, Mostafa Salem
OBJECTIVE: The aim of this study was to evaluate the effect of atorvastatin on the bone formation and resorption markers in ovariectomized rats (experimental study), and to study its effect on the bone mineral density (BMD) in postmenopausal osteoporotic women (clinical study). MATERIALS AND METHODS: The study involved experimental and clinical aspects. In the experimental aspect, 42 female Wistar rats were divided into five groups: Group I (n=6; sham-operated), Group II (n=6; 1 mL of carboxymethyl cellulose [CMC] was administered orally), Group III (n=6; 20 mg/kg orally of atorvastatin was administered), Group IV (n=12; untreated ovariectomized [OVX] rats and served as a model of osteoporosis [OP]) and Group V (n=12; 20 mg/kg orally of atorvastatin was administered to ovariectomized rats)...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28487744/atorvastatin-diltiazem-combination-induced-rhabdomyolysis-leading-to-diagnosis-of-hypothyroidism
#19
N D B Ehelepola, S M B Y Sathkumara, H M P A G S Bandara, K L R Kalupahana
Statins and hypothyroidism, independently, can rarely cause rhabdomyolysis. The combination of them especially with concurrent intake of drugs such as diltiazem increases the risk of rhabdomyolysis. Hashimoto's encephalopathy is a rare condition associated with Hashimoto's thyroiditis and some patients with that can present with a stroke like picture. An elderly male who has been on atorvastatin for three years and on diltiazem for a week presented with sudden onset inability to walk and confusion. On examination muscle tenderness was noticed and creatine kinase levels indicated rhabdomyolysis which we attributed to atorvastatin...
2017: Case Reports in Medicine
https://www.readbyqxmd.com/read/28481663/development-and-optimization-of-atorvastatin-calcium-loaded-self-nanoemulsifying-drug-delivery-system-snedds-for-enhancing-oral-bioavailability-in-vitro-and-in-vivo-evaluation
#20
Abdulsalam M Kassem, Hany M Ibrahim, Ahmed M Samy
The objective of this study was to develop and optimize self-nanoemulsifying drug delivery system (SNEDDS) of atorvastatin calcium (ATC) for improving dissolution rate and eventually oral bioavailability. Ternary phase diagrams were constructed on basis of solubility and emulsification studies. The composition of ATC-SNEDDS was optimized using Box-Behnken optimization design. Optimized ATC-SNEDDS was characterized for various physicochemical properties. Pharmacokinetic, pharmacodynamic and histological finding were performed in rats...
May 8, 2017: Journal of Microencapsulation
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