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Emilie Catry, Barbara D Pachikian, Nuria Salazar, Audrey M Neyrinck, Patrice D Cani, Nathalie M Delzenne
AIMS: Hypolipidemic drugs are prescribed in the most of cases for the treatment of cardiovascular diseases. Several studies have showed that the gut microbiota is able to regulate the host cholesterol metabolism. This study aimed to investigate the potential impact of hypolipidemic drugs on the gut microbiota in mice, and to correlate it to the regulation of cholesterol metabolism. MAIN METHODS: Male C57Bl/6J mice were divided into four groups fed either a control diet alone (CT), or supplemented with simvastatin (0...
July 1, 2015: Life Sciences
Hannes Hentze, Kristian K Jensen, Ser Mien Chia, Douglas G Johns, Rachel J Shaw, Harry R Davis, Shian-Jiun Shih, Kenny K Wong
OBJECTIVES: To assess the lipid-lowering efficacy of ezetimibe in dyslipidemic cynomolgus monkeys comparing two dosing methods, and to evaluate PCSK9 plasma levels during dyslipidemia induction by feeding a high-fat/high-cholesterol diet (HFD), ezetimibe (Zetia(®), Ezetrol(®)) treatment, ezetimibe washout, and HFD washout. METHODS AND RESULTS: Twenty dyslipidemic cynomolgus monkeys on HFD for seven months (LDL cholesterol 100-400 mg/dL) were randomized into two groups and treated with ezetimibe for two weeks, either by oral gavage or by using food treats...
November 2013: Atherosclerosis
Filip Kiekens, Siemon Eelen, Loes Verheyden, Tinne Daems, Johan Martens, Guy Van Den Mooter
The aim of this study was to investigate the bioavailability enhancement of the biopharmaceutics classification system class II compound ezetimibe loaded in ordered mesoporous silica (OMS) in dogs. The OMS was characterized as highly ordered mesoporous material with a narrow pore size distribution. Ezetimibe was loaded in OMS via incipient wetness impregnation to obtain a 20% (w/w) drug load, characterized by nitrogen adsorption and differential scanning calorimetry, and formulated in one capsule and two tablet formulations...
March 2012: Journal of Pharmaceutical Sciences
A V Susekov, N B Gorniakova, M Iu Zubareva
The review describes the history of hypolipidemic therapy with statins. It gives the results of studies of the primary prevention of atherosclerosis and the treatment of hyperlipidemias with lovastatin, pravastatin, and fluvastatin. Emphasis is laid on trial data on the efficacy, tolerability, and safety of simvastatin (zocor). The results of studies, including regression ones, of this drug in different doses, controlled by biochemical, clinical, magnet resonance imaging, and ultrasonic data are summarized...
2010: Terapevticheskiĭ Arkhiv
Harry R Davis, Robert S Lowe, David R Neff
Ezetimibe (Zetia(®), Ezetrol(®), Merck, Whitehouse Station, NJ) is a potent inhibitor of sterol absorption, which selectively blocks the uptake of biliary and dietary cholesterol in the small intestine. Clinical trials have demonstrated the beneficial effects of ezetimibe on the reduction of atherogenic lipoproteins and the attainment of guideline-recommended lipid levels. Direct evidence that these improvements translate to a reduction in atherosclerosis or cardiovascular events is limited, although reductions in major atherosclerotic events that are consistent with the LDL-C lowering achieved have recently been presented for patients with chronic kidney disease treated with ezetimibe/simvastatin 10/20mg in the SHARP trial...
April 2011: Atherosclerosis
A J Scheen, R P Radermecker
Ezetimibe (Ezetrol) selectively inhibits the intestinal absorption of cholesterol and phytosterols. Its mechanism of action results in a synergistic cholesterol-lowering effect together with a statin that inhibits cholesterol synthesis by the liver, which leads to the development of a fixed ezetimibe-simvastatin combination (Inegy). Ezetimibe has been more particularly studied in patients with type 2 diabetes whose high cardiovascular risk is well known. The present article aims at describing recent advances and specificities concerning the use of ezetimibe in the diabetic population...
December 2009: Revue Médicale de Liège
(no author information available yet)
Ezetimibe (Ezetrol - MSD-Schering Plough) is a lipid-lowering drug that reduces plasma concentrations of low-density lipoprotein (LDL) cholesterol and total cholesterol when used alone or in combination with a statin. In 2004, we could find no evidence on the effects of ezetimibe on cardiovascular morbidity and mortality and concluded that it should not replace a statin in the routine management of patients at increased risk of developing complications of atherosclerotic disease.1 Since then, a fixed-dose combination product, containing simvastatin and ezetimibe ( Inegy - MSD-Schering Plough), has been launched in the UK, and new evidence on the safety and efficacy of ezetimibe has been published...
August 2009: Drug and Therapeutics Bulletin
John S Sampalis, Stéphane Bissonnette, Rafik Habib, Stella Boukas
BACKGROUND: The aim of lipid-lowering treatment is to reduce the risk for cardiovascular events. Patients not at target lipid levels while on hydroxymethylglutaryl coenzyme A reductase inhibitors (statin) monotherapy are at increased cardiovascular risk. OBJECTIVE: To describe the impact of coadministration of ezetimibe with a statin on the estimated 10 year risk for coronary artery disease (E-R(CAD)) in patients with hypercholesterolemia and above-target low-density lipoprotein cholesterol (LDL-C) levels after statin monotherapy...
September 2007: Annals of Pharmacotherapy
Laszlo Mark, Gyozo Dani, Ozseb Fazekas, Olga Szüle, Hajnalka Kovacs, Andras Katona
BACKGROUND: The epsilon4 allele of the gene encoding apolipoprotein E (apoE) is associated with elevated serum levels of total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C), as well as an increased risk of coronary heart disease (CHD), greater disease severity, and higher CHD mortality. ApoE epsilon4 allele carriers have also shown reduced lipid and lipoprotein responses to lipid-modifying pharmacotherapy and lifestyle modifications. OBJECTIVE: To provide preliminary descriptive data on the effects of apoE genotype on lipid and lipoprotein responses to the cholesterol absorption inhibitor ezetimibe (Ezetrol/Zetia) in Hungarian subjects not at cholesterol goals at baseline...
July 2007: Current Medical Research and Opinion
Ph Thibaut, J Sternon
No abstract text is available yet for this article.
November 2006: Revue Médicale de Bruxelles
Stéphane Bissonnette, Rafik Habib, Fotini Sampalis, Stella Boukas, John S Sampalis
BACKGROUND: For patients who have above-target low-density lipoprotein cholesterol (LDL-C) levels while on statin monotherapy, coadministration of a cholesterol absorption inhibitor with the statin may decrease serum LDL-C levels and improve overall lipid profiles. OBJECTIVES: To assess the effectiveness and safety of ezetimibe 10 mg/day coadministered with a statin in patients with primary hypercholesterolemia who have higher than recommended LDL-C levels while on statin monotherapy...
October 2006: Canadian Journal of Cardiology
Stefan Oswald, Eberhard Scheuch, Ingolf Cascorbi, Werner Siegmund
Ezetimibe (Ezetrol) is a novel cholesterol lowering drug which disposition is not fully understood in man. We developed a selective and high-sensitive assay to measure serum concentration-time profiles, renal and fecal elimination of ezetimibe in pharmacokinetic studies. Ezetimibe glucuronide, the major metabolite of ezetimibe was determined by enzymatic degradation to the parent compound. Ezetimibe was measured after extraction with methyl tert-butyl ether using 4-hydroxychalcone as internal standard and liquid chromatography coupled via an APCI interface with tandem mass spectrometry (LC-MS/MS) for detection...
January 2, 2006: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
J Ducobu
In the field of dyslipidemia and metabolic syndrome, four innovative therapies are reviewed: Ezetimibe (Ezétrol) is a selective cholesterol absorption inhibitor. Co-administration of ezetimibe with low dose of statins shows LDL lowering comparable to that of the highest dose of the respective statin alone. Combination therapy helps more patients in achieving target LDL-cholesterol. Nicotinic acid (Niacin) favourably modifies all lipoprotein level (including Lp(a)). Extended release niacin (Niaspanâ) is a new galenic form, with less side effects (flushing and hepatotoxicity) than the native nicotinic acid...
September 2005: Revue Médicale de Bruxelles
J Ducobu, J Sternon
Ezetimibe is a new cholesterol absorption inhibitor that selectively inhibits dietary and biliary cholesterol absorption from the intestine. This drug inhibits cholesterol absorption without affecting the absorption of triglycerides, biliary salts and fat-soluble vitamins. Inhibition of cholesterol absorption using ezetimibe 10 mg/day alone resulted in substantial reductions of plasma LDL-C concentrations (approximately 18%). Coadministration of ezetimibe 10 mg/day with statins 10 mg/day showed LDL lowering comparable to or greater than that of the highest dose of the respective statin alone...
October 2004: Revue Médicale de Bruxelles
J Vervaeren
No abstract text is available yet for this article.
2004: Journal de Pharmacie de Belgique
(no author information available yet)
Use of statin therapy is a key first-line approach in preventing coronary heart disease events and stroke in people at increased risk of developing such complications. Ezetimibe (Ezetrol - MSD-Schering-Plough), the first licensed azetidinone drug, is being promoted as an adjunct to statin therapy to achieve greater reductions in blood cholesterol concentrations than occur with a statin alone. Here we review ezetimibe and consider its place in clinical practice.
September 2004: Drug and Therapeutics Bulletin
A J Scheen
Ezetimibe (Ezetrol), recently launched in Belgium by Merck Sharp& Dohme and Schering Plough, is presented as 10 mg tablets. It belongs to a new class of lipid-lowering agents that selectively inhibit the intestinal absorption of cholesterol and phytosterols. Its mechanism of action results in a synergistic cholesterol-lowering effect together with a statin that inhibits cholesterol synthesis by the liver. Ezetimibe, at a daily dose of 10 mg, is indicated, in combination with a statin, as adjuvant treatment to diet in patients with primary hypercholesterolaemia (homozygote or heterozygote familial form and non-familial polygenic form) not well controlled with a statin alone...
April 2004: Revue Médicale de Liège
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