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lipids lowering drugs

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https://www.readbyqxmd.com/read/29338456/an-update-on-the-safety-of-nutraceuticals-and-effects-on-lipid-parameters
#1
Arrigo F G Cicero, Alessandro Colletti
Cardiovascular diseases (CVDs) are the leading cause of mortality and disability in developed countries, whereas a large portion of patients in primary prevention have uncontrolled level of CVD risk factors. Dietary supplementation with bioactive natural compounds with demonstrated lipid-lowering effects is currently supported by the international guidelines for CVD prevention and some international expert panels. Areas covered: This review provides insights on issues concerning the tolerability and safety of the most commonly used nutraceuticals with demonstrated lipid-lowering effect in humans...
January 16, 2018: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/29337265/99mtc-vinorelbine-tartrate-loaded-spherulites-lung-disposition-study-in-sprague-dawley-rats-by-gamma-scintigraphy
#2
Rahul Dhande, Amit Tyagi, Rakesh Kumar Sharma, Hetal Thakkar
Vinorelbine Tartrate (VLB) is the first line chemotherapeutic agent for treatment of Non-Small Cell Lung Cancer, whose non-specific distribution causes unwanted side effects. The aim of the present investigation was to formulate VLB loaded spherulites intended for targeting the lung. Spherulites were composed of Soyabean Phosphatidylcholine (SPC), Cholesterol (Chol), Potassium oleate and Mannitol. Lipid film prepared using SPC, Chol and Potassium oleate, was dispersed in aqueous phase comprising Mannitol and VLB, followed by controlled shearing and extrusion...
January 11, 2018: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29337216/in-vitro-lung-epithelial-cell-transport-and-anti-interleukin-8-releasing-activity-of-liposomal-ciprofloxacin
#3
Ruba S Darweesh, Masahiro Sakagami
As a promising long-acting inhaled formulation, liposomal ciprofloxacin (Lipo-CPFX) was characterized in the in vitro human lung epithelial Calu-3 cell monolayer system, compared to ciprofloxacin in solution (CPFX). Its modulated absorptive transport and uptake, and sustained inhibitory activity against induced pro-inflammatory interleukin-8 (IL-8) release were examined. The absorptive transport and uptake kinetics for Lipo-CPFX and CPFX were determined at 0.1-50 mg/ml in the Transwell system. The Lipo-CPFX transport was then challenged for mechanistic exploration via cell energy depletion, a reduced temperature, endocytosis and/or lipid fusion inhibition, and addition of excess non-loaded liposomes...
January 11, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29325370/-association-between-carotid-artery-plaques-and-all-cause-mortality-and-cardiovascular-events
#4
W Li, F Ma, Y M Jiang, J J Li, L Song, S H Chen, X M Liu, X Q Li, S L Wu
Objective: To observe the association of carotid artery plaque with all-cause mortality and cardiovascular events. Methods: A total of 7 017 participants who completed the carotid sonography examination between 2010 and 2011 were selected from the stroke and the elderly prospective cohort Kailuan study. The participants of stroke cohort received health examination between 2006 and 2007, and participants of elderly cohort received health examination between 2010 and 2011. All participants were divided into plaque group (3 285 cases) and without plaque group (3 732 cases) according to with or without carotid artery plaque...
December 24, 2017: Zhonghua Xin Xue Guan Bing za Zhi
https://www.readbyqxmd.com/read/29321031/deprescribing-preventive-cardiovascular-medication-in-patients-with-predicted-low-cardiovascular-disease-risk-in-general-practice-the-ecstatic-study-a-cluster-randomised-non-inferiority-trial
#5
Clare H Luymes, Rosalinde K E Poortvliet, Nan van Geloven, Margot W M de Waal, Yvonne M Drewes, Jeanet W Blom, Nynke Smidt, Willem J J Assendelft, Wilbert B van den Hout, Wouter de Ruijter, Mattijs E Numans
BACKGROUND: The use of cardiovascular medication for the primary prevention of cardiovascular disease (CVD) is potentially inappropriate when potential risks outweigh the potential benefits. It is unknown whether deprescribing preventive cardiovascular medication in patients without a strict indication for such medication is safe and cost-effective in general practice. METHODS: In this pragmatic cluster randomised controlled non-inferiority trial, we recruited 46 general practices in the Netherlands...
January 11, 2018: BMC Medicine
https://www.readbyqxmd.com/read/29320955/therapeutic-roles-of-statins-in-gynecology-and-obstetrics-the-current-evidence
#6
Burak Zeybek, Maged Costantine, Gokhan S Kilic, Mostafa A Borahay
INTRODUCTION: Statins are a class of drugs, which act by inhibiting the rate-limiting enzyme of cholesterol biosynthesis (3-hydroxy-3-methyl-glutaryl-CoA reductase). The inhibition of mevalonate synthesis leads to subsequent inhibition of downstream products of this pathway, which explains the pleiotropic effects of these agents in addition to their well-known lipid-lowering effects. Accumulating evidence suggests that statins might be beneficial in various obstetric and gynecologic conditions...
January 1, 2018: Reproductive Sciences
https://www.readbyqxmd.com/read/29313565/utilization-of-the-lipid-lowering-therapies-in-outpatient-settings-in-poland-epidemiological-survey-economedica-dyslipidemia-2015
#7
Filip M Szymański, Anna E Płatek, Anna Ryś, Karolina Semczuk-Kaczmarek, Bartosz Krzowski, Katarzyna Wróbel, Krzysztof J Filipiak
BACKGROUND: Dyslipidemia, especially elevated low-density lipoprotein (LDL) cholesterol is one of the most important cardiovascular risk factors. Treatment of dyslipidemia and prevention of cardiovascular disease with lipid-lowering drugs is one of the key issues in reducing cardiovascular mortality. Nevertheless, underutilization of statins and lipid-lowering drugs is still a problem globally. AIM: The present study aimed to describe the utilization of lipid-lowering drugs in groups of patients with indications for statin treatment and elevated LDL cholesterol...
January 9, 2018: Kardiologia Polska
https://www.readbyqxmd.com/read/29313218/thallium-induced-toxicity-in-rat-brain-crude-synaptosomal-mitochondrial-fractions-is-sensitive-to-anti-excitatory-and-antioxidant-agents
#8
Marisol Maya-López, María Verónica Mireles-García, Monserrat Ramírez-Toledo, Ana Laura Colín-González, Sonia Galván-Arzate, Isaac Túnez, Abel Santamaría
The mechanisms by which the heavy metal thallium (Tl+) produces toxicity in the brain remain unclear. Herein, isolated synaptosomal/mitochondrial P2 crude fractions from adult rat brains were exposed to Tl+ (5-250 μM) for 30 min. Three toxic endpoints were evaluated: mitochondrial dysfunction, lipid peroxidation, and Na+/K+-ATPase activity inhibition. Concentration-response curves for two of these endpoints revealed the optimum concentration of Tl+ to induce damage in this preparation, 5 μM. Toxic markers were also estimated in preconditioned synaptosomes incubated in the presence of the N-methyl-D-aspartate receptor antagonist kynurenic acid (KYNA, 50 μM), the cannabinoid receptor agonist WIN 55,212-2 (1 μM), or the antioxidant S-allyl-L-cysteine (SAC, 100 μM)...
January 8, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29310996/appropriateness-of-statin-prescription-in-the-elderly
#9
M Ruscica, C Macchi, C Pavanello, A Corsini, A Sahebkar, C R Sirtori
Statins, the most widely used drugs in the Western world, have become a pivotal component in the primary and secondary prevention of vascular diseases. Although benefits have been well documented in younger-than-75-year-old individuals, the value of statins in people aged >75years and over is controversial. The CTT meta-analysis calculated an absolute risk reduction of 0.6%/year per 38.7mg/dl reduction in LDL-C levels in patients aged >75years, that would translate into a number needed to treat of 167...
January 5, 2018: European Journal of Internal Medicine
https://www.readbyqxmd.com/read/29310481/nanostructured-lipid-carriers-for-intraocular-brimonidine-localization-development-in-vitro-and-in-vivo-evaluation
#10
Noha S El-Salamouni, Ragwa M Farid, Amal H El-Kamel, Safaa S El-Gamal
Brimonidine ocular hypotensive effect can be enhanced by increasing residence time and corneal penetration. The current work aimed to formulate, evaluate and compare nanostructured lipid carriers (NLCs) to solid lipid nanoparticles (SLNs) and commercial eye drops for controlled brimonidine delivery. NLCs prepared by modified high shear homogenization were spherical with a mean size of 151.97 ±1.98 nm, negative zeta potential (ZP) of -44.2± 7.81 mV, % entrapment efficiency (EE) of 83.631 ±0.495% and low crystallinity index (CI) (17...
January 9, 2018: Journal of Microencapsulation
https://www.readbyqxmd.com/read/29306457/cost-effectiveness-of-pcsk9-inhibition-in-addition-to-standard-lipid-lowering-therapy-in-patients-at-high-risk-for-vascular-disease
#11
Manon C Stam-Slob, Yolanda van der Graaf, Anthonius de Boer, Jacoba P Greving, Frank L J Visseren
BACKGROUND: As proprotein convertase subtilisin-kexin type 9 (PCSK9) monoclonal antibodies are entering the market, we assessed the cost-effectiveness of PCSK9 inhibition added to standard lipid-lowering therapy in patient groups at high risk for major adverse cardiovascular events (MACE). METHODS: A lifetime Markov Model was designed to estimate healthcare costs, quality-adjusted life years (QALYs) and incremental cost-effectiveness ratios (ICERs) for PCSK9 inhibition added to standard therapy in patients with Familial Hypercholesterolemia (FH), patients with vascular disease at high MACE recurrence risk, and patients with vascular disease with diabetes mellitus...
February 15, 2018: International Journal of Cardiology
https://www.readbyqxmd.com/read/29305864/fenofibrate-inhibits-mtor-p70s6k-signaling-and-simultaneously-induces-cell-death-in-human-prostate-cancer-cells
#12
Xin Lian, Junlian Gu, Baoshan Gao, Yan Li, Chendil Damodaran, Wei Wei, Yaowen Fu, Lu Cai
Fenofibrate is the most widely used lipid-lowering drug, but it seems to have anti-tumor effects in several tumor cell lines. However, there are only a few reports on its effects on human prostate cancer cells. Thus, we investigated the anti-proliferative effects of fenofibrate on human prostate cancer cells and potential mechanisms. The methods used include cell viability analysis with an MTT assay, as well as apoptosis and related signaling pathway analyses with flow cytometry and Western blotting. Fenofibrate inhibited PC-3 cell growth in dose- and time-dependent manners...
January 3, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29303009/dyslipidaemia-in-the-elderly-to-treat-or-not-to-treat
#13
Niki Katsiki, Genovefa Kolovou, Pablo Perez-Martinez, Dimitri P Mikhailidis
The elderly population (i.e. aged ≥ 65 years) is increasing worldwide. Ageing is associated with a higher incidence and prevalence of cardiovascular disease (CVD). Areas covered: The prevalence of CVD risk factors including type 2 diabetes mellitus, hypertension and dyslipidaemia also increases with advancing age, contributing to the higher absolute CVD risk observed in the elderly. The present narrative review comments on the associations of dyslipidaemia with CVD as well as the effects of lifestyle measures and lipid-lowering drugs on lipids and CVD risk with a special focus on the elderly population...
January 5, 2018: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/29301757/prior-medications-and-the-cardiovascular-benefits-from-combination-angiotensin-converting-enzyme-inhibition-plus-calcium-channel-blockade-among-high-risk-hypertensive-patients
#14
Robert D Brook, Niko Kaciroti, George Bakris, Björn Dahlöf, Bertram Pitt, Eric Velazquez, Michael Weber, Dion H Zappe, Tsushung Hau, Kenneth A Jamerson
BACKGROUND: The ACCOMPLISH (Avoiding Cardiovascular Events Through Combination Therapy in Patients Living with Systolic Hypertension) trial demonstrated that combination therapy using amlodipine, rather than hydrochlorothiazide, in conjunction with benazepril provided greater cardiovascular risk reduction among high-risk hypertensive patients. Few trials have evaluated the effect of prior antihypertensive therapy used among participants on the study outcomes. METHODS AND RESULTS: In a post hoc observational analysis, we examined the characteristics of the drug regimens taken before trial enrollment in the context of the primary composite outcome (death from cardiovascular causes, nonfatal myocardial infarction, nonfatal stroke, hospitalization for angina, resuscitation after sudden cardiac death, and coronary revascularization)...
January 4, 2018: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29301191/cytotoxic-apoptotic-and-genotoxic-effects-of-lipid-based-and-polymeric-nano-micelles-an-in-vitro-evaluation
#15
Fatemeh Bahadori, Abdurrahim Kocyigit, Hayat Onyuksel, Aydan Dag, Gulacti Topcu
Self-assembly systems (SAS) mainly consist of micelles, and liposomes are the classes of Nano Drug Delivery Systems with superior properties compared to traditional therapeutics in targeting cancer tumors. All commercially available nano-formulations of chemotherapeutics currently consist of SAS. According to our knowledge, a specific toxicity comparison based on material differences has not yet been performed. The purpose of this study was to evaluate and compare the toxicity of two SAS consisting of Sterically Stabilized Micelles (SSM) made of a lipid-based amphiphilic distearoyl-sn-glycero-phosphatidylethanolamine-polyethylene glycol (PEG)-2000 and a polymeric micelle (PM) consisting of Y-shape amphiphilic block copolymer, synthesized using poly ε-caprolactone and PEG...
December 30, 2017: Toxics
https://www.readbyqxmd.com/read/29300349/enhanced-and-selective-antiproliferative-activity-of-methotrexate-functionalized-nanocapsules-to-human-breast-cancer-cells-mcf-7
#16
Catiúscia P de Oliveira, Sabrina L Büttenbender, Willian A Prado, Aline Beckenkamp, Ana C Asbahr, Andréia Buffon, Silvia S Guterres, Adriana R Pohlmann
Methotrexate is a folic acid antagonist and its incorporation into nanoformulations is a promising strategy to increase the drug antiproliferative effect on human breast cancer cells by overexpressing folate receptors. To evaluate the efficiency and selectivity of nanoformulations containing methotrexate and its diethyl ester derivative, using two mechanisms of drug incorporation (encapsulation and surface functionalization) in the in vitro cellular uptake and antiproliferative activity in non-tumoral immortalized human keratinocytes (HaCaT) and in human breast carcinoma cells (MCF-7)...
January 4, 2018: Nanomaterials
https://www.readbyqxmd.com/read/29299890/comparison-of-the-effects-of-clofibrate-and-silafibrate-on-sperm-parameters-quality-and-sex-hormones-in-male-rats
#17
Masoud Delashoub, Mojtaba Ziaee, Arash Khorrami, Seyed Mahdi Banan-Khojasteh
PURPOSE: Fibrates are drugs widely used for the treatment of hyperlipidemic disorders. Previous studies on a novel analogue of clofibrate, called silafibrate, have shown good lipid lowering effects. This study was designed to assess the role of silafibrate as a peroxisome proliferator-activated receptors (PPARs) agonist on sperm health and spermatogenesis in adult male rats. MATERIAL AND METHODS: Seventy male Wistar rats were randomly allocated into 7 groups: Cl-10, Cl-20, and Cl-40 mg/kg/day (clofibrate); Si-10, Si-20, and Si-40 mg/kg/day (silafibrate); and C, control...
January 3, 2018: Urology Journal
https://www.readbyqxmd.com/read/29297106/idalopirdine-a-selective-5-ht6-receptor-antagonist-reduces-food-intake-and-body-weight-in-a-model-of-excessive-eating
#18
Magdalena Kotańska, Klaudia Lustyk, Adam Bucki, Monika Marcinkowska, Joanna Śniecikowska, Marcin Kołaczkowski
Obesity, from early childhood onwards, is a common societal problem. The overconsumption of sweet, salty and high-fat products are the main factors that cause excessive weight gain. It is therefore necessary to search for new drugs that affect satiety centers and reduce the sense of hunger and caloric intake. It has been suggested that the blockade of 5-HT6 receptors may reduce food intake, and since idalopirdine is a clinically tested, selective 5HT6 receptor antagonist, it was chosen to be examined in animal models of obesity...
January 3, 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29296233/srebp-2-driven-transcriptional-activation-of-human-snd1-oncogene
#19
Sandra Armengol, Enara Arretxe, Leire Enzunza, Irati Llorente, Unai Mendibil, Hiart Navarro-Imaz, Begoña Ochoa, Yolanda Chico, María José Martínez
Upregulation of Staphylococcal nuclease and tudor domain containing 1 (SND1) is linked to cancer progression and metastatic spread. Increasing evidence indicates that SND1 plays a role in lipid homeostasis. Recently, it has been shown that SND1-overexpressing hepatocellular carcinoma cells present an increased de novo cholesterol synthesis and cholesteryl ester accumulation. Here we reveal that SND1 oncogene is a novel target for SREBPs. Exposure of HepG2 cells to the cholesterol-lowering drug simvastatin or to a lipoprotein-deficient medium triggers SREBP-2 activation and increases SND1 promoter activity and transcript levels...
December 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/29295555/relationship-between-lipid-phenotypes-overweight-lipid-lowering-drug-response-and-kif6-and-hmg-coa-genotypes-in-a-subset-of-the-brisighella-heart-study-population
#20
Sabrina Angelini, Martina Rosticci, Gianmichele Massimo, Muriel Musti, Gloria Ravegnini, Nicola Consolini, Giulia Sammarini, Sergio D'Addato, Elisabetta Rizzoli, Dauren Botbayev, Claudio Borghi, Giorgio Cantelli-Forti, Arrigo F Cicero, Patrizia Hrelia
The existence of genetic traits might explain the susceptibility to develop hypercholesterolemia and the inter-individual differences in statin response. This study was performed to evaluate whether individuals' polymorphisms in HMG-CoA and KIF6 genes are independently associated with hypercholesterolemia, other lipid-associated traits, and statin response in unselected individuals enrolled in the Brisighella heart study (Survey 2012). A total of 1622 individuals, of which 183 under statin medication, were genotyped for a total of five polymorphisms (KIF6 rs20455, rs9471077, rs9462535; HMG-CoA rs3761740, rs3846662)...
December 24, 2017: International Journal of Molecular Sciences
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