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Efthymia D Tsakiridou, Evangelos Liberopoulos, Zoe Giotaki, Stelios Tigas
We report the case of a patient with probable heterozygous familial hypercholesterolemia and mitotane-induced resistant hypercholesterolemia, despite combination therapy with rosuvastatin and ezetimibe. The patient was managed with the addition of evolocumab. Use of a proprotein convertase subtilisin-kexin type 9 inhibitor, should be considered in patients who develop mitotane-related hypercholesterolemia that cannot be managed with conventional lipid-lowering treatment.
March 13, 2018: Journal of Clinical Lipidology
Polina German, Anita Mathias, Diana M Brainard, Brian P Kearney
Ledipasvir/sofosbuvir (Harvoni® ), a fixed-dose combination tablet of an NS5A inhibitor ledipasvir and an NS5B polymerase inhibitor sofosbuvir, is approved for the treatment of chronic hepatitis C virus infection. Ledipasvir/sofosbuvir exhibits a favorable drug-drug interaction profile and can be administered with various medications that may be used by hepatitis C virus-infected patients, including patients with comorbidities, such as co-infection with human immunodeficiency virus or immunosuppression following liver transplantation...
April 11, 2018: Clinical Pharmacokinetics
Ayse Ufuk, Rachel E Kosa, Hongying Gao, Yi-An Bi, Sweta Modi, Dana Gates, A David Rodrigues, Larry M Tremaine, Manthena V S Varma, J Brian Houston, Aleksandra Galetin
Hepatic organic anion transporting polypeptides (OATP) 1B1 and 1B3 are clinically relevant transporters associated with significant drug-drug interactions (DDIs) and safety concerns. Given that OATP1Bs in cynomolgus monkey share >90% degree of gene and amino acid sequence identity with human orthologs, we evaluated the in vitro-in vivo translation of OATP1B-mediated DDI risk using this preclinical model. In vitro studies using cynomolgus monkey hepatocytes showed active uptake Km values of 2.0 and 3.9 µM for OATP1B probe substrates, pitavastatin and rosuvastatin, respectively...
April 11, 2018: Journal of Pharmacology and Experimental Therapeutics
Z-W Zeng, Y-N Zhang, W-X Lin, W-Q Zhang, R Luo
OBJECTIVE: Non-cardiac surgery is associated with perioperative cerebral complications (delirium, postoperative cognition dysfunction, stroke). While rare, these complications can lead to disabilities and deaths. Information is ambiguous as to whether pharmacological preoperative treatment exerts neuroprotection. We wished to systematically assess potential modulation by statins, lidocaine, ketamine or magnesium sulfate of the relative risk of cerebral complications in noncardiac surgery...
March 2018: European Review for Medical and Pharmacological Sciences
Stefan Chiorescu, Nicolae Ovidiu Grad, Ion Aurel Mironiuc, Octavian Aurel Andercou
OBJECTIVES: The purpose of the present experimental research was to assess the efficacy of intraperitoneal administration of rosuvastatin in preventing the formation of postoperative peritoneal adhesions. MATERIAL AND METHOD: Peritoneal adhesions were induced in 120 male rats of the Wistar-Bratislava breed, divided into 4 groups (n=30), using a parietal and visceral abrasion model. Group I was designated as the control group; in the case of group II, a saline solution was administered intraperitoneally, while in the case of groups III and IV, rosuvastatin solution with a concentration of 10 mg/kg and 5 mg/kg, respectively, was administered in a single dose, during laparotomy...
2018: Annali Italiani di Chirurgia
Takayuki Katsube, Shiro Miyazaki, Yukitoshi Narukawa, Martha Hernandez-Illas, Toshihiro Wajima
PURPOSE: Cefiderocol, a siderophore cephalosporin, will be used concomitantly with other medications for treatment of bacterial infections. In vitro studies demonstrated inhibition potential of cefiderocol on organic anion transporter (OAT) 1, OAT3, organic cation transporter (OCT) 1, OCT2, multidrug and toxin extrusion (MATE) 2-K, and organic anion transporting polypeptide (OATP) 1B3. The aim of this study was to assess in vivo drug-drug interaction (DDI) potential of cefiderocol using probe substrates for these transporters...
April 7, 2018: European Journal of Clinical Pharmacology
Ryan Hyde, Julian Chung, Jason Chertoff, Hassan Alnuaimat, Ali Ataya
A 77-year-old woman presented to the hospital with symptoms of progressive shortness of breath with associated right-sided pleuritic pain. The patient had begun noting dyspnea on exertion, limiting her ability to go on hikes over the few days prior to admission. Her medical history is significant for carcinoid tumor status postresection in 2012 without recurrence. She has no history of thromboembolism or clotting disorders, and she has no history of smoking or drug abuse. Current medications include amlodipine, celecoxib, hydrochlorothiazide, and rosuvastatin...
April 2018: Chest
Yinhui Liu, Xiaobo Song, Huimin Zhou, Xue Zhou, Yunlong Xia, Xin Dong, Wei Zhong, Shaoying Tang, Lili Wang, Shu Wen, Jing Xiao, Li Tang
Background: Statin has been widely used to treat hyperlipidemia because of its high potency in decreasing cholesterol levels. The present study aimed to examine the lipid-lowering effect of rosuvastatin and the composition, diversity and species abundance of gut microbiome in association with rosuvastatin efficacy. TRIAL REGISTRATION: ChiCTR-ORC-17013212 at the First Affiliated Hospital of Dalian Medical University, November 2, 2017. Results: Totally 64 patients with hyperlipidemia were treated with 10 mg/day of rosuvastatin for 4-8 weeks...
2018: Frontiers in Microbiology
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
Junya Ako, Kiyoshi Hibi, Ken Kozuma, Katsumi Miyauchi, Yoshihiro Morino, Toshiro Shinke, Kenichi Tsujita, Kiyoko Uno, Yumiko Kawabata, Takafumi Hiro
BACKGROUND: Serial intravascular ultrasound (IVUS) imaging can be used to evaluate the effect of cholesterol-lowering on coronary atheroma progression and plaque volume, with evidence of potential incremental effects with more aggressive lipid-lowering treatments. Alirocumab is a highly specific, fully human monoclonal antibody to proprotein convertase subtilisin/kexin type 9 (PCSK9). This study will investigate the effect of alirocumab on coronary artery plaque volume in Japanese patients with a recent acute coronary syndrome (ACS) and hypercholesterolemia while on stable statin therapy...
March 29, 2018: Journal of Cardiology
Yasin Ahmadi, Amir Ghorbani Haghjoo, Siavoush Dastmalchi, Mahboob Nemati, Nasrin Bargahi
BACKGROUND: Statins mostly target the liver; therefore, increase in the synthesis of cholesterol by extra-hepatic tissues and then transferring this cholesterol to the liver can be regarded as adaptive responses by these tissues. In addition to cholesterol, these adaptive responses can increase isoprenoid units as byproducts of the cholesterol biosynthesis pathway; isoprenoids play a key role in regulating cell signaling pathways and cancer development. Thus, there is a primary need for in vivo investigation of the effects of statins on the cholesterol metabolism in the extra-hepatic tissues...
March 29, 2018: Gene
Amirhossein Sahebkar, Luis E Simental-Mendía, Dimitri P Mikhailidis, Matteo Pirro, Maciej Banach, Cesare R Sirtori, Massimiliano Ruscica, Željko Reiner
BACKGROUND: Statins are well-established low-density lipoprotein cholesterol-lowering drugs. Elevated apolipoprotein CIII (Apo CIII) levels are associated with elevated triglyceride-rich particles, which are also considered to be a possible risk factor for cardiovascular disease. OBJECTIVE: The aim of this meta-analysis of randomized placebo-controlled clinical trials was to assess the effect of statins on Apo CIII concentrations. METHODS: Randomized placebo-controlled trials investigating the impact of statin treatment on cholesterol lowering that include lipoprotein measurement were searched in PubMed, MEDLINE, Scopus, Web of Science, and Google Scholar databases (up to July 31, 2017)...
February 1, 2018: Journal of Clinical Lipidology
S Ades, D Douce, C E Holmes, S Cory, S Prior, S Butenas, P Callas, M Cushman
BACKGROUND: Statin therapy is associated with lower risk of venous thromboembolism (VTE), but has not been prospectively evaluated in patients with advanced cancer. OBJECTIVES: We determined if statin administration in this high-risk population reduces VTE risk, based on established and emerging biomarkers. PATIENTS/METHODS: This double-blind crossover randomized controlled trial among patients with advanced cancer receiving systemic therapy allocated participants to rosuvastatin 20mg daily, or placebo for 3-4 weeks prior to crossover to the alternative therapy with a 3-5 week washout...
March 25, 2018: Journal of Thrombosis and Haemostasis: JTH
Jörn F Dopheide, Lucija Papac, Marc Schindewolf, Iris Baumgartner, Heinz Drexel
BACKGROUND: Patients with peripheral artery disease (PAD) are at very high risk of future cardiovascular (CV) events. Strict lipid-lowering therapy is recommended. However, data on target level attainment are scarce. OBJECTIVE: The objective of the study was to investigate guideline equitable lipid lowering in a large observational study of symptomatic PAD patients. METHODS: Single-center observational study including 1109 patients with symptomatic PAD planned for revascularization at a tertiary university center...
March 1, 2018: Journal of Clinical Lipidology
Justin D Lutz, Brian J Kirby, Lu Wang, Qinghua Song, John Ling, Benedetta Massetto, Angela Worth, Brian P Kearney, Anita Mathias
Drug transporter and cytochrome P450 expression is regulated by shared nuclear receptors and hence, an inducer should induce both, though magnitude may differ. The objective of this study was to establish relative induction relationships between CYP3A and drug transporters (P-gp, OATP and BCRP) or other P450s (CYP2C9 and CYP1A2) using ascending doses of the prototypical PXR agonist, rifampin, to elicit weak, moderate and strong PXR agonism. Healthy subjects received dabigatran etexilate, pravastatin, rosuvastatin and a midazolam/tolbutamide/caffeine cocktail before and after rifampin 2, 10, 75, or 600 mg qd...
March 23, 2018: Clinical Pharmacology and Therapeutics
Ying Yu, Lin Jin, Yamin Zhuang, Yan Hu, Jing Cang, Kefang Guo
Rosuvastatin, a member of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors, exerts various pharmacological activities. This study evaluated the cardioprotective effect of rosuvastatin on isoproterenol-induced myocardial infarction injury in rats. A rat model of myocardial infarction injury was induced by isoproterenol (ISO) for 2 consecutive days, rosuvastatin was administered for 8 weeks. The levels of myocardial infarct size, aspartate transaminase (AST), alanine transaminase (ALT), creatine kinase-MB (CK-MB), lactate dehydrogenase (LDH) activities, as well as malondialdehyde (MDA) levels, superoxide dismutase (SOD), glutathione peroxidase (GPX), catalase (CAT) activities and reduced glutathione (GSH) concentrations were determined...
March 15, 2018: International Journal of Molecular Medicine
Nasr M El-Abasawi, Khalid A M Attia, Ahmad A M Abo-Serie, Samir Morshedy, Ashraf Abdel-Fattah
Simultaneous determination of rosuvastatin calcium and propranolol hydrochloride using the first derivative synchronous spectrofluorimetry was described. This method involves measuring the synchronous fluorescence of both drugs in ethanol using, ∆ λ = 60 nm then the first derivative was recorded and the peak amplitudes were measured at 350 and 374 nm for rosuvastatin calcium and propranolol hydrochloride, respectively. Under the optimum conditions, the linear ranges of rosuvastatin calcium and propranolol hydrochloride were 0...
March 13, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
George Machairas, Irene Panderi, Ariadni Geballa-Koukoula, Stavroula Rozou, Nikolaos Antonopoulos, Christos Charitos, Ariadni Vonaparti
A hydrophilic interaction liquid chromatography method with diode array detection (HILIC-DAD) was developed and validated for the simultaneous determination of impurities in extended-release fixed-dose combination tablets containing rosuvastatin and metformin in a ratio 1:100. The analytes were separated by hydrophilic interaction liquid chromatography using an XBridge®-HILIC analytical column under isocratic elution. The mobile phase was composed of ammonium formate at 150 mM containing 0.05% diethylamine (pH 8...
June 1, 2018: Talanta
László Márk, Mária Nagy, Győző Dani, Csaba Baranyai, Marianna Borbély, András Katona, Zoltán Jambrik
INTRODUCTION: The actual guidelines of cardiovascular prevention lay special emphasis on the lipid-lowering therapy of patients suffering from acute coronary syndrome (ACS). AIM: To evaluate the occurrence of high-intensity statin therapy, recommended by guidelines, at discharge in a Hungarian county hospital with hemodynamic laboratory in patients who underwent percutaneous intervention, furthermore the LDL-cholesterol (LDL-C) levels and goal attainment rate in the first year...
March 2018: Orvosi Hetilap
Song-Jian He, Qiang Liu, Hua-Qiu Li, Fang Tian, Shi-Yu Chen, Jian-Xin Weng
Background: The prevention of cardiac surgery-associated acute kidney injury (CSA-AKI) by statins remains controversial. Therefore, the present meta-analysis including randomized controlled trials (RCTs) was performed to assess the effect of perioperative statin on CSA-AKI. Methods: Two reviewers independently searched for RCTs about perioperative statin for prevention of CSA-AKI. The primary endpoint was CSA-AKI. Relative risk was calculated between statin and placebo for preventing CSA-AKI using the random-effect model or fixed-effect model according to different heterogeneity...
2018: Therapeutics and Clinical Risk Management
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