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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...
March 6, 2018: Toxicology and Applied Pharmacology
Yat Hei 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...
March 7, 2018: Current Pharmaceutical Biotechnology
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
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
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
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
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
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
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
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
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
Bilal Khokhar, Linda Simoni-Wastila, Julia F Slejko, Eleanor Perfetto, Min Zhan, Gordon S Smith
OBJECTIVE: To assess the relationship between posttraumatic brain injury statin use and (1) mortality and (2) the incidence of associated morbidities, including stroke, depression, and Alzheimer's disease and related dementias following injury. SETTING AND PARTICIPANTS: Nested cohort of all Medicare beneficiaries 65 years of age and older who survived a traumatic brain injury (TBI) hospitalization during 2006 through 2010. The final sample comprised 100 515 beneficiaries...
January 30, 2018: Journal of Head Trauma Rehabilitation
He Li, Chunmei Wang, Jinghui Sun, Cong Liu, Ning Li, Jianguang Chen
Our previous study showed that pravastatin prevents ischemia and reperfusion-induced lethal ventricular fibrillation in rats. This study explored whether pravastatin decreases myocardial infarct size and this effect is associated with endothelial nitric oxide synthase (eNOS) expression in myocardium. Rats were treated with ischemia (30 minutes) and reperfusion (60 minutes) after chronic oral administration of pravastatin, fluvastatin, or vehicle once daily for 22 days. Electrocardiograms and blood pressure were continuously recorded, myocardial infarct size was measured by TTC-staining, and eNOS expression was measured by western blot...
2018: International Heart Journal
Yang Cheng, Hang Zheng, Biao Wang, WanFu Xu, Jiajia Xu, Yun Zhu
BACKGROUND: Effective strategies for the treatment of hepatic fibrosis are urgently in need. AIMS: To investigate the effect of the co-treatment of sorafenib and fluvastatin on hepatic fibrosis and the underlying mechanisms. METHODS: A diethylnitrosamine-induced hepatic fibrosis rat model was used to evaluate the anti-fibrosis effect. Epithelial mesenchymal transition (EMT) of hepatocytes and hepatic stellate cells (HSCs) in response to sorafenib and fluvastatin was explored...
December 28, 2017: Digestive and Liver Disease
Shingen Misaka, Osamu Abe, Hideyuki Sato, Tomoyuki Ono, Yayoi Shikama, Satomi Onoue, Hirooki Yabe, Junko Kimura
PURPOSE: The objective of this study is to assess the effects of green tea and its major catechin component, (-)-epigallocatechin gallate (EGCG), on CYP2C9-mediated substrate metabolism in vitro, and the pharmacokinetics of fluvastatin in healthy volunteers. METHODS: The metabolism of diclofenac and fluvastatin in human recombinant CYP2C9 was investigated in the presence of EGCG. In a randomized three-phase crossover study, 11 healthy volunteers ingested a single 20-mg dose of fluvastatin with green tea extract (GTE), containing 150 mg of EGCG, along with water (300 mL), brewed green tea (300 mL), or water (300 mL) after overnight fasting...
January 24, 2018: European Journal of Clinical Pharmacology
V Moraschini, D C F Almeida, J A Calasans-Maia, M Diuana Calasans-Maia
The purpose of this systematic review was to evaluate the quantitative histomorphometric outcomes of animal studies investigating statins as a pro-osteogenic agent to enhance the osseointegration of dental implants. Some animal studies have suggested a beneficial action of statins on bone tissue. Electronic and manual literature searches, without date or language restriction, ​​were performed by two independent review authors up to February 2017. Eligibility criteria included animal trials quantitatively analysing the pro-osteogenic effect of statins on dental implants...
January 15, 2018: International Journal of Oral and Maxillofacial Surgery
Mariusz Stolarczyk, Anna Apola, Anna Maślanka, Anna Kwiecień, Włodzimierz Opoka
Applicability of derivative spectrophotometry for the determination of valsartan in the presence of a substance from the group of statins was checked. The obtained results indicate that the proposed method may be effective by using appropriate derivatives: for valsartan and fluvastatin - D1, D2 and D3, for valsartan and pravastatin - D1 and D3, for valsartan and atorvastatin - D2 and D3. The method was characterized by high sensitivity and accuracy. Linearity was maintained in the following ranges: 9.28-32...
December 20, 2017: Acta Pharmaceutica
Katja Vogt, Shailaja Mahajan-Thakur, Robert Wolf, Susanne Bröderdorf, Conny Vogel, Andreas Böhm, Christoph A Ritter, Markus Gräler, Stefan Oswald, Andreas Greinacher, Heyo K Kroemer, Gabriele Jedlitschky, Bernhard H Rauch
Sphingosine-1-phosphate (S1P) is a potent lipid mediator released from activated platelets by an adenosine triphosphate (ATP)-dependent export mechanism. A candidate transport protein is the multidrug resistance protein 4 (MRP4/ABCC4), an ATP-dependent transporter highly expressed in platelets. Furthermore, several statins are known to affect platelet functions and exhibit antithrombotic properties. This study determines the involvement of MRP4 in the transport of S1P and a possible interference by statins...
January 2018: Thrombosis and Haemostasis
Shaoping Zhu, Junyu Wang, Xianguo Wang, Jinping Zhao
Statins are Hydroxymethylglutaryl-coenzyme A reductase inhibitors, which are typically used to lower blood cholesterol. Additional beneficial effects, including improvement to pulmonary arterial hypertension (PAH), have also been confirmed. However, the mechanisms underlying this improvement have not yet been clarified. The present study was conducted to determine if fluvastatin was protective against experimental PAH development and to investigate the potential effects of fluvastatin on caveolin‑1 (cav‑1) expression...
December 22, 2017: Molecular Medicine Reports
Rosemary Yu, Joseph Longo, Jenna E van Leeuwen, Peter J Mullen, Wail Ba-Alawi, Benjamin Haibe-Kains, Linda Z Penn
The statin family of drugs preferentially trigger tumor cell apoptosis by depleting mevalonate pathway metabolites farnesyl pyrophosphate (FPP) and geranylgeranyl pyrophosphate (GGPP), which are used for protein prenylation, including the oncoproteins of the RAS superfamily. However, accumulating data indicate that activation of the RAS superfamily are poor biomarkers of statin sensitivity, and the mechanism of statin-induced tumor-specific apoptosis remains unclear. Here we demonstrate that cancer cell death triggered by statins can be uncoupled from prenylation of the RAS superfamily of oncoproteins...
December 11, 2017: Cancer Research
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