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Rosuvastatin

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https://www.readbyqxmd.com/read/29468841/development-verification-and-prediction-of-osimertinib-drug-drug-interactions-using-pbpk-modelling-approach-to-inform-drug-label
#1
Venkatesh Pilla Reddy, Michael Walker, Pradeep Sharma, Peter Ballard, Karthick Vishwanathan
Osimertinib is a potent, highly selective, irreversible inhibitor of Epidermal Growth Factor Receptor and T790M resistance mutation receptor. In vitro metabolism data suggested osimertinib is a substrate of CYP3A4/5, a weak inducer of CYP3A and an inhibitor of BCRP. A combination of in vitro data, clinical pharmacokinetic data and drug-drug interaction (DDI) data of osimertinib in oncology patients were used to develop the physiologically based pharmacokinetic (PBPK) model and verify the DDI data of osimertinib...
February 22, 2018: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/29460396/lower-sperm-quality-and-testicular-and-epididymal-structural-impairment-in-adult-rats-exposed-to-rosuvastatin-during-prepuberty
#2
Gabriel Adan Araújo Leite, Marciana Sanabria, Marilia Martins Cavariani, Janete Aparecida Anselmo-Franci, Patrícia Fernanda Felipe Pinheiro, Raquel Fantin Domeniconi, Wilma De Grava Kempinas
The increase of obesity, bad eating habits and the lack of physical exercises are highly related to dyslipidemias. Rosuvastatin is a lipid-lowering drug and has been indicated to prevent cardiovascular diseases and to treat dyslipidemias due to its higher efficiency to reduce serum cholesterol concentrations. This study aimed to evaluate the reproductive adverse effects on sexual maturity due to rosuvastatin exposure in juvenile male rats during prepuberty. Three groups were randomly formed with newly weaned rats: control, whose rats received saline solution 0...
February 19, 2018: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29449331/lipid-lowering-therapy-with-ezetimibe-decreases-spontaneous-atherothrombotic-occlusions-in-a-rabbit-model-of-plaque-erosion-a-role-of-serum-oxysterols
#3
Katsuya Honda, Tetsuya Matoba, Yoshibumi Antoku, Jun-Ichiro Koga, Ikuyo Ichi, Kaku Nakano, Hiroyuki Tsutsui, Kensuke Egashira
OBJECTIVE: Plaque erosion is increasing its importance as one of the mechanisms of acute coronary syndromes in this statin era. However, the clinical efficacy of currently used lipid-lowering agents in the prevention of thrombotic complications associated with plaque erosion has not been clarified. Therefore, we examined the therapeutic effects of ezetimibe or rosuvastatin monotherapy on spontaneous atherothrombotic occlusion. APPROACH AND RESULTS: Femoral arteries of Japanese white rabbits, fed a high-cholesterol diet, were injured by balloon catheter, and then angiotensin II was continuously administrated...
February 15, 2018: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/29440955/intraperitoneal-administration-of-rosuvastatin-prevents-postoperative-peritoneal-adhesions-by-decreasing-the-release-of-tumor-necrosis-factor
#4
Stefan Chiorescu, Octavian Aurel Andercou, Nicolae Ovidiu Grad, Ion Aurel Mironiuc
Objectives: The purpose of this experimental study was to demonstrate the reduction of peritoneal adhesions formation in rats after intraperitoneal administration of rosuvastatin, due to its anti-inflammatory effect. Method: Peritoneal adhesions were induced in 120 Wistar-Bratislava rats divided into 4 groups (n=30), using a parietal and visceral (cecal) abrasion model. Group I was designated as control group; in group II, a saline solution was administered intraperitoneally; in groups III and IV, a single dose of rosuvastatin solution, 10 mg/kg and 5 mg/kg respectively, was injected intraperitoneally...
2018: Clujul Medical (1957)
https://www.readbyqxmd.com/read/29440178/evaluation-of-alteration-in-hepatic-and-intestinal-bcrp-function-in-vivo-due-to-abcg2-c-421c-a-polymorphism-based-on-pbpk-analysis-of-rosuvastatin
#5
Azusa Futatsugi, Kota Toshimoto, Takashi Yoshikado, Yuichi Sugiyama, Yukio Kato
Polymorphism c.421C>A in ABCG2 gene is thought to reduce the activity of breast cancer resistance protein (BCRP), a xenobiotic transporter, although it is not clear which organ(s) contributes to the polymorphism-associated pharmacokinetic change. The aim of the present study was to quantitatively estimate the influence of c.421C>A on intestinal and hepatic BCRP activity, using a physiologically based pharmacokinetic (PBPK) model of rosuvastatin developed from clinical data and several in vitro studies...
February 12, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29439129/simultaneous-assessment-in-vitro-of-transporter-and-metabolic-processes-in-hepatic-drug-clearance-use-of-a-media-loss-approach
#6
James Harrison, Tom De Bruyn, Adam S Darwich, J Brian Houston
Hepatocyte drug depletion-time assays are well established for the determination of metabolic clearance in vitro. The present study focuses on the refinement and evaluation of a "media loss" assay, an adaptation of the conventional depletion assay involving centrifugation of hepatocytes prior to sampling, allowing estimation of uptake in addition to metabolism. Using experimental procedures consistent with a high throughput, a selection of 12 compounds with a range of uptake and metabolism characteristics (atorvastatin, cerivastatin, clarithromycin, erythromycin, indinavir, pitavastatin, repaglinide, rosuvastatin, saquinavir and valsartan, together with two control compounds - midazolam and tolbutamide) were investigated in the presence and absence of the cytochrome P450 inhibitor 1-aminobenzotriazole and organic anion transporter protein inhibitor rifamycin SV...
February 8, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29434381/ismp-adverse-drug-reactions-influenza-vaccine-induced-stevens-johnson-syndrome-vilazodone-induced-nightmares-dabigatran-induced-pustular-eruptions-neurotoxic-and-cardiotoxic-symptoms-after-cannabis-concentrate-exposure-rosuvastatin-induced-skin-eruption
#7
Michael A Mancano
The purpose of this feature is to heighten awareness of specific adverse drug reactions (ADRs), discuss methods of prevention, and promote reporting of ADRs to the US Food and Drug Administration's (FDA) MedWatch program (800-FDA-1088). If you have reported an interesting, preventable ADR to MedWatch, please consider sharing the account with our readers. Write to Dr. Mancano at ISMP, 200 Lakeside Drive, Suite 200, Horsham, PA 19044 (phone: 215-707-4936; e-mail: mmancano@temple.edu). Your report will be published anonymously unless otherwise requested...
February 2018: Hospital Pharmacy
https://www.readbyqxmd.com/read/29432839/protective-effects-of-rosuvastatin-and-vitamin-e-against-fipronil-mediated-oxidative-damage-and-apoptosis-in-rat-liver-and-kidney
#8
Mohamed M Abdel-Daim, Ahmed Abdeen
Fipronil (FPN) is a phenylpyrazole insecticide that is extensively used in agriculture and veterinary applications. However, FPN is also a potent environmental toxicant to animals and humans. Therefore, the current study aimed to investigate the protective role of rosuvastatin (ROSU) and vitamin E (Vit E) against FPN-induced hepatorenal toxicity in albino rats. Seven groups with eight rats each were used for this purpose; these groups included the control vehicle group that received corn oil, the Vit E group (1000 mg/kg, orally), the ROSU group (10 mg/kg, orally), the FPN group (20 mg/kg, orally), the FPN-ROSU group, the FPN-Vit E group, and the FPN-Vit E-ROSU group...
February 9, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29427912/adjunctive-therapy-with-statins-in-schizophrenia-patients-a-meta-analysis-and-implications
#9
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)...
February 5, 2018: Psychiatry Research
https://www.readbyqxmd.com/read/29427042/amyotrophic-lateral-sclerosis-associated-with-statin-use-a-disproportionality-analysis-of-the-fda-s-adverse-event-reporting-system
#10
Beatrice A Golomb, Abril Verden, Alexis K Messner, Hayley J Koslik, Keith B Hoffman
INTRODUCTION: Apparent elevations in reporting of amyotrophic lateral sclerosis (ALS)-like conditions associated with statin use have been previously described from data obtained via US and European databases. OBJECTIVE: The aim of this study was to examine US FDA Adverse Event Reporting System (FAERS) data to compare reporting odds ratios (RORs) of ALS and ALS-like conditions between statins and other drugs, for each statin agent. METHODS: We assessed for disproportional rates of reported ALS and ALS-related conditions for each statin agent separately by using the ROR formula...
February 9, 2018: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/29423787/human-immunodeficiency-virus-infection-antiretroviral-therapy-and-statin-a-clinical-update
#11
REVIEW
Hugo Ribeiro Zanetti, Leonardo Roever, Alexandre Gonçalves, Elmiro Santos Resende
PURPOSE OF REVIEW: This clinical update is intended to focus in relationship between HIV infection and use of antiretroviral therapy (ART) and statin. RECENT FINDINGS: Though ART significantly changed the course of HIV infection, it is related to numerous side effects principally to the lipid profile. In this way, statins became one of the most used lipid-lowering therapies in this population. In our clinical update, we evaluated studies that demonstrate the relationship and molecular mechanisms that HIV infection and ART use trigger dyslipidemia and also the use of statin to reduce this condition...
February 8, 2018: Current Atherosclerosis Reports
https://www.readbyqxmd.com/read/29406237/a-68-year-old-man-with-chronic-myelogenous-leukemia-and-a-large-unilateral-pleural-effusion
#12
Adam Alter, Neal Chaisson, Sudipto Mukherjee, Thomas Gildea
A 68-year-old man with chronic myelogenous leukemia presents for evaluation of 2 months of dyspnea with exertion. He denies cough, fever, chest pain, weight gain, orthopnea, and edema. Since diagnosis of chronic myelogenous leukemia 5 years ago, he has been treated with dasatinib, with recent BCR-ABL1 assay showing no detectable disease in the peripheral blood. Medical history also includes hyperlipidemia, prostate enlargement, and hypothyroidism, but no prior heart or lung disease. Born in the Middle East, he immigrated to the United States 30 years ago and is working as a physician...
February 2018: Chest
https://www.readbyqxmd.com/read/29405807/interaction-of-deoxyschizandrin-and-schizandrin-b-with-liver-uptake-transporters-oatp1b1-and-oatp1b3
#13
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 6, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29404156/influence-of-statin-therapy-on-exacerbation-frequency-in-patients-with-chronic-obstructive-pulmonary-disease
#14
Şehnaz Olgun Yıldızeli, Baran Balcan, Emel Eryüksel, Berrin Bağcı Ceyhan, Sait Karakurt, Turgay Çelikel
OBJECTIVES: Chronic obstructive pulmonary disease (COPD) is an inflammatory disease, in which chronic and systemic inflammation plays an important role. By decreasing neutrophil infiltration and cytokine production, statins have anti-inflammatory mechanisms. MATERIALS AND METHODS: Fifty-seven patients who had diagnosis of chronic obstructive pulmonary disease according to GOLD guideline were included in the study; 20 of them were statin users. Statin users group were patients being under medication with regular simvastatin, atorvastatin or rosuvastatin 20 mg per day for at least the past 1 year...
April 2017: Turkish Thoracic Journal
https://www.readbyqxmd.com/read/29403315/high-potency-statins-but-not-all-statins-decrease-the-risk-of-new-onset-osteoporotic-fractures-a-nationwide-population-based-longitudinal-cohort-study
#15
Tsung-Kun Lin, Yi-Sheng Liou, Ching-Heng Lin, Pesus Chou, Gwo-Ping Jong
Background: Statins have been linked to new-onset osteoporotic fractures (NOFs), and different statins may alter the risk for the development of NOFs. Aim: In this study, we investigated the association between different statins and the development of NOFs. Patients and methods: This was a longitudinal cohort study performed using data from claim forms submitted to the Taiwan Bureau of National Health Insurance, including case patients with NOFs from January 2004 to December 2013 and non-NOF subjects...
2018: Clinical Epidemiology
https://www.readbyqxmd.com/read/29402848/do-statins-affect-thyroid-volume-and-nodule-size-in-patients-with-hyperlipidemia-in-a-mildly-to-moderately-iodine-deficient-region-a-prospective-study
#16
Canan Demir, Cuneyd Anil, Yusuf Bozkus, Umut Mousa, Altug Kut, Asli Nar, Neslihan B Tutuncu
OBJECTIVE: The objective of this study was to assess the anti-proliferative pleiotropic effects of statins on thyroid function, volume and nodularity. SUBJECTS AND METHODS: One hundred and six hyperlipidemic patients were included in this prospective study. Sixty nine patients in the statin groups received atorvastatin (16 patients received 10 mg, 18 received 20 mg) or rosuvastatin (20 patients received 10 mg, 15 received 20 mg); 37 patients in the control group assessed as not requiring drugs only made lifestyle changes...
January 23, 2018: Medical Principles and Practice: International Journal of the Kuwait University, Health Science Centre
https://www.readbyqxmd.com/read/29402522/a-phase-iii-multicenter-randomized-double-blind-active-comparator-clinical-trial-to-compare-the-efficacy-and-safety-of-combination-therapy-with-ezetimibe-and-rosuvastatin-versus-rosuvastatin-monotherapy-in-patients-with-hypercholesterolemia-i-rosette-ildong
#17
Soon Jun Hong, Han Saem Jeong, Jeong Cheon Ahn, Dong-Hun Cha, Kyung Heon Won, Weon Kim, Sang Kyoon Cho, Seok-Yeon Kim, Byung-Su Yoo, Ki Chul Sung, Seung-Woon Rha, Joon-Han Shin, Kyoo Rok Han, Wook Sung Chung, Min Su Hyon, Han Cheol Lee, Jang-Ho Bae, Moo-Yong Rhee, Jun Kwan, Dong Woon Jeon, Ki Dong Yoo, Hyo-Soo Kim
PURPOSE: Combination therapy with ezetimibe and statins is recommended in cases of statin intolerance or insufficiency. The objective of this study was to compare the efficacy and safety of combination therapy with ezetimibe and rosuvastatin versus those of rosuvastatin monotherapy in patients with hypercholesterolemia. METHODS: I-ROSETTE (Ildong ROSuvastatin & ezETimibe for hypercholesTElolemia) was an 8-week, double-blind, multicenter, Phase III randomized controlled trial conducted at 20 hospitals in the Republic of Korea...
February 2, 2018: Clinical Therapeutics
https://www.readbyqxmd.com/read/29402296/sex-disparity-in-the-management-and-outcomes-of-dyslipidemia-of-diabetic-patients-in-the-arabian-gulf-findings-from-the-cepheus-study
#18
Ibrahim Al-Zakwani, Fatma Al-Mahruqi, Khalid Al-Rasadi, Abdullah Shehab, Wael Al Mahmeed, Mohammed Arafah, Ali T Al-Hinai, Omer Al Tamimi, Mahmoud Al Awadhi, Raul D Santos
BACKGROUND: Little is known about sex gap in the management and outcomes of dyslipidemia among diabetics in the Arabian Gulf. The aim if this study was to determine sex differences in the management and outcomes of dyslipidemia in diabetic patients in the Arabian Gulf. METHODS: This study was derived from the Centralized Pan-Middle-East Survey on the management of hypercholesterolemia. Patients recruited were aged ≥18 years on lipid lowering drugs for ≥3 months (stable medication for ≥6 weeks)...
February 5, 2018: Lipids in Health and Disease
https://www.readbyqxmd.com/read/29400079/drug-eruption-to-rosuvastatin-with-recurrence-on-simvastatin-a-case-report
#19
Ian T Y Wong, Yuanshen Huang, Youwen Zhou
No abstract text is available yet for this article.
February 1, 2018: Journal of Cutaneous Medicine and Surgery
https://www.readbyqxmd.com/read/29399524/statins-as-a-preventative-therapy-for-venous-thromboembolism
#20
REVIEW
Alex Wallace, Hassan Albadawi, Peter Hoang, Andrew Fleck, Sailendra Naidu, Grace Knuttinen, Rahmi Oklu
The anti-inflammatory effects of statins have likely not been used to their fullest extent, particularly in reducing venous thromboembolic events. Current therapy for thrombotic events hinges on anticoagulation via heparin, warfarin or new oral anticoagulants. Interventional procedures with thrombectomy may also play a critical role. Unfortunately, thrombotic events can occur and recur despite meticulous anticoagulation therapy. Venous thromboembolism (VTE) includes both deep vein thrombosis (DVT) and pulmonary embolism (PE), two complicated and prevalent diseases that can cause chronic disease states such as post-thrombotic syndrome (PTS)...
December 2017: Cardiovascular Diagnosis and Therapy
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