© 2015 The Authors. Background: Simvastatin, 20. mg, plus ezetimibe, 10. mg, daily (simvastatin plus ezetimibe) reduced major atherosclerotic events in patients with moderate to severe chronic kidney disease (CKD) in the Study of Heart and Renal Protection (SHARP), but its cost-effectiveness is unknown. Study Design: Cost-effectiveness of simvastatin plus ezetimibe in SHARP, a randomized controlled trial. Setting & Population: 9,270 patients with CKD randomly assigned to simvastatin plus ezetimibe versus placebo; participants in categories by 5-year cardiovascular risk (low,|10%; medium, 10%-|20%; or high,≥20%) and CKD stage (3, 4, 5 not on dialysis, or on dialysis therapy). Model, Perspective, & Timeline: Assessment during SHARP follow-up from the UK perspective; long-term projections. Intervention: Simvastatin plus ezetimibe (2015 UK £1.19 per day) during 4.9 years median follow-up in SHARP; scenario analyses with high-intensity statin regimens (2015 UK £0.05-£1.06 per day). Outcomes:
Title: Synthesis and Bioactivities of 2-Azetidinone Derivatives as Cholesterol Absorption Inhibitors. VOLUME: 7 ISSUE: 6. Author(s):Yubin Wang, Hai Qian, Jinpei Zhou, Huibin Zhang, Jianfeng Ji and Wenlong Huang. Affiliation:Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.. Keywords:2-Azetidinones, cholesterol absorption inhibitor, synthesis, bioactivities, hamsters, cardiovascular research, coronary heart disease (CHD), exogenous pathways, 3-methylglutaryl, 3-hydroxy. Abstract: Twenty-four 2-azetidinone derivatives have been designed and synthesized as cholesterol absorption inhibitors. All new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed considerable effects in lowering the levels of total cholesterol in the serum, especially compound 2d, 4a, 4f, 4i and 4j. ...
Ezetimibe is a potent cholesterol absorption inhibitor that lowers LDL cholesterol and raises HDL cholesterol in hypercholesterolemic humans (4) and is now in phase III clinical trials. Preclinical studies have demonstrated that ezetimibe selectively inhibits the transport of radiolabeled cholesterol through the intestinal wall and ultimately into the plasma (1,3). The precise molecular mechanism by which cholesterol is absorbed in the intestine (and how ezetimibe inhibits this absorption) is currently unknown and under intensive investigation.. In the present studies, we demonstrated that feeding high-fat diets containing modest cholesterol to hamsters leads to obesity accompanied by hyperinsulinemia, hyperleptinemia, hypercholesterolemia, and hypertriglyceridemia, which are characteristic of the profile often observed in obese insulin-resistant and/or type 2 diabetic patients (9). In an initial report, we described the potent cholesterol absorption inhibitor ezetimibe, which inhibited the rise ...
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BACKGROUND: Lowering LDL cholesterol with statin regimens reduces the risk of myocardial infarction, ischaemic stroke, and the need for coronary revascularisation in people without kidney disease, but its effects in people with moderate-to-severe kidney disease are uncertain. The SHARP trial aimed to assess the efficacy and safety of the combination of simvastatin plus ezetimibe in such patients. METHODS: This randomised double-blind trial included 9270 patients with chronic kidney disease (3023 on dialysis and 6247 not) with no known history of myocardial infarction or coronary revascularisation. Patients were randomly assigned to simvastatin 20 mg plus ezetimibe 10 mg daily versus matching placebo. The key prespecified outcome was first major atherosclerotic event (non-fatal myocardial infarction or coronary death, non-haemorrhagic stroke, or any arterial revascularisation procedure). All analyses were by intention to treat. This trial is registered at ClinicalTrials.gov, NCT00125593, and
Cholesterol absorption inhibitors are a class of compounds that prevents the uptake of cholesterol from the small intestine into the circulatory system. Most of these molecules are monobactams but show no antibiotic activity. An example is ezetimibe (SCH 58235) Another example is Sch-48461. The Sch is for Schering-Plough, where these compounds were developed. Phytosterols are also cholesterol absorption inhibitors. There are two sources of cholesterol in the upper intestine: dietary (from food) and biliary (from bile). Dietary cholesterol, in the form of lipid emulsions, combines with bile salts, to form bile salt micelles from which cholesterol can then be absorbed by the intestinal enterocyte. Once absorbed by the enterocyte, cholesterol is reassembled into intestinal lipoproteins called chylomicrons. These chylomicrons are then secreted into the lymphatics and circulated to the liver. These cholesterol particles are then secreted by the liver into the blood as VLDL particles, precursors to ...
Background: Intestinal cholesterol absorption inhibitor ezetimibe (EZE) added to a statin therapy has demonstrated benefits in the IMPROVE-IT trial by further reducing LDL-cholesterol levels than statin therapy alone. We investigated the mechanisms by which EZE could contribute to cardiovascular events reduction in apolipoprotein E knock-out (apoE ko) mice.. Methods: ApoE ko mice were fed a Paigen diet without (control) or with EZE (7mg/kg/day) for 6 weeks. To evaluate the effects of EZE on LDL-cholesterol metabolism and excretion, a first set of mice was injected intravenously with 3H-cholesteryl oleate labeled human LDL. A second set of mice was used for in vivo SPECT/CT imaging of 99mTc-cAbVCAM1-5, a single domain antibody directed against the Vascular Cell Adhesion Molecule-1 (VCAM-1), which was used as a marker of inflamed atherosclerotic plaques. The same mice were sacrificed for autoradiography and histology of aortic atherosclerotic plaques.. Results: Compared with control, EZE treatment ...
Background: Dietary cholesterol oxidation products (oxysterols) are known to be absorbed and incorporate into lipoprotein in blood and atherosclerotic lesions and to accelerate the formation of atherosclerosis in animals. However, the mechanism of enhanced atherogenesis induced by dietary oxysterols has not been explored.. Aim: The aims of this study are to investigate molecular and cellular mechanisms of atherogenesis induced by dietary oxysterols and to examine therapeutic effects of a cholesterol absorption inhibitor ezetimibe.. Methods and Results: ApoE-deficient mice were fed either a control high-fat diet (control-HFD) or HFD containing oxysterols (oxysterol-HFD; 6.8 % of cholesterol was oxidized) for 8 weeks and infused with angiotensin II. Compared to control-HFD, dietary oxysterol-HFD enhanced the formation of aortic atherosclerosis, macrophage infiltration, lipid accumulation, immunoreactive MCP-1, and activated MMPs in atherosclerotic lesions without affecting plasma lipid levels ...
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Modulation of abdominal aortic aneurysm (AAA) expansion by HMG-CoA reductase inhibitors (statins) might be linked to reducing IL-6 and MMP-9, which may be consequent on reducing plasma cholesterol. Ezetimibe is a novel cholesterol absorption inhibitor used in combination with statins. This pilot study compared the biological effects of ezetimibe combination therapy with simvastatin alone on parameters relevant to aneurysm expansion including cytokines and proteolytic enzymes ...
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Therapeutic goals for lipid lowering treatment in the prevention of ischemic heart disease are often not reached in clinical practice. Even the highest doses of statins do not guarantee good control of hypercholesterolemia in all patients. Therefore, new lipid lowering drugs are being investigated. One of them is ezetimibe - intestinal cholesterol absorption inhibitor. Treatment with ezetimibe results in significant reduction of total cholesterol and LDL cholesterol levels. It is hoped that concomitant treatment with ezetimibe and other lipid lowering drugs (particularly statins) will be more effective. In large randomized clinical trials, co-administration of ezetimibe with atorvastatin and simvastatin proved to be more effective in lowering cholesterol levels and reaching target therapeutic levels than treatment with statin alone. In addition, combined treatment with ezetimibe and simvastatin was more effective compared to treatment with todays most effectively used statin (rosuvastatin) ...
PubMed journal article Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with ongoing simvastatin treatment: a multicenter, randomized, double-blind, placebo-controlled, 48-week extension stud were found in PRIME PubMed. Download Prime PubMed App to iPhone or iPad.
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Subjects must have documented coronary heart disease (CHD). For the purposes of this study, CHD will include one or more of the following features: documented stable angina (with evidence of ischemia on exercise testing); history of myocardial infarction; history of percutaneous coronary intervention (primarily PTCA with or without stent placement); symptomatic peripheral vascular disease (claudication); documented history of atherothrombotic cerebrovascular disease; and/or documented history of unstable angina or non-Q wave myocardial infarction ...
Subjects must have documented coronary heart disease (CHD). For the purposes of this study, CHD will include one or more of the following features: documented stable angina (with evidence of ischemia on exercise testing); history of myocardial infarction; history of percutaneous coronary intervention (primarily PTCA with or without stent placement); symptomatic peripheral vascular disease (claudication); documented history of atherothrombotic cerebrovascular disease; and/or documented history of unstable angina or non-Q wave myocardial infarction ...
BACKGROUND: Five years of statin therapy lowers low-density lipoprotein (LDL) cholesterol substantially and, over a 5-year period, results in reductions in the incidence of cardiovascular events. The Simvastatin and Ezetimibe in Aortic Stenosis (SEAS) trial (ClinicalTrials.gov number, NCT00092677) has raised the hypothesis that adding ezetimibe to statin therapy for larger LDL cholesterol reductions might increase the incidence of cancer. METHODS: We compared the results of a hypothesis-generating analysis of the incidence of cancer in the SEAS trial of ezetimibe plus simvastatin in 1873 patients (mean follow-up after ezetimibe or matching placebo was begun, 4.1 years) with a hypothesis-testing analysis of cancer data from the two large ongoing trials of this regimen: the Study of Heart and Renal Protection (SHARP) (NCT00125593) with 9264 patients (mean follow-up, 2.7 years) and the Improved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVE-IT) (NCT00202878), currently with 11,353
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In this study, we have shown that after peritoneal injection of [3H]-cholesterol-labeled mouse primary peritoneal macrophages, L1-KO mice expressing hepatic NPC1L1 (L1LivOnly) accumulated more [3H]-tracer in blood and tissues and secreted significantly reduced amounts of [3H]-neutral sterols in gallbladder bile and feces, when compared with L1-KO mice expressing no hepatic NPC1L1. Ezetimibe treatment reversed the accumulation of [3H]-tracer in blood and tissues and restored biliary and fecal excretion of [3H]-neutral sterols in L1LivOnly mice. Our results demonstrate an essential role of biliary sterol secretion in mediating macrophage-to-feces RCT in mice deficient in intestinal cholesterol absorption. Given that human livers express NPC1L1,8,10,15 our findings suggest that ezetimibe may have a previously unappreciated action: promoting macrophage RCT via direct inhibition of hepatic NPC1L1 in humans.. Recent studies on mice genetically or surgically deficient in biliary cholesterol secretion ...
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The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.
The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.
The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.
2-Azetidinone is a chemical compound with the molecular formula C3H5NO. It is the simplest β-lactam and it forms the central core structure of the β-lactam antibiotics and certain cholesterol medications ...
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This trial will compare the efficacy and tolerability of atorvastatin, alone or in combination with ezetimibe, in patients with hypercholesterolaemia.
The heterocycle moieties form the site of reaction in many enzymes and co-enzymes and also act as an important pharmacophore in the pharmaceutical drug designs. 2-Azetidinones are the 2-carbonyl derivatives of azetidine, more commonly known as ?-lactams. These structural entities occupied a central role in the vigil against bacterial infections over the past few decades. A subclass of these heterocyclic systems, monobactams or monocyclic ?-lactam derivatives exhibits several biological activities including antibacterial, antifungal, antiprotozoal, anti-mycobacterial, anti-HIV, antiviral, antimalarial, antioxidant, apoptotic inhibitors, anti-inflammatory activity, anticancer activity, herbicidal activity, etc. Monobactams has resistant to the ?-lactamase enzyme and could be a reasonable starting point for developing new drugs or inhibitors. In the present review, pharmacological activities of monocyclic ?-lactam derivatives have been discussed with respect to current research in the ...
The article reports on a warning issued by the U.S. Food and Drug Administration (FDA) about the possible relationship between combination simvastatin plus ezetimibe and an increased incidence of cancer. According to preliminary data from the Simvastatin Ezetimibe Aortic Stenosis (SEAS) trial, the combination of simvastatin and ezetimibe lowered the low-density lipoprotein (LDL) levels of patients with mild to moderate aortic stenosis ...
Small intestinal and colonic epithelial cells. SI: Small intestine; C: Colon. (PDF)Author ContributionsObtained funding and supervised the study: RAB SR.
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This trial will investigate the effect of ezetimibe on glucose metabolism in patients with type 2 diabetes mellitus and hypercholesterolaemia. The primary
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The long-delayed and much-speculated-about data from Merck and Schering-Ploughs Enhance study comparing whether a combination of Zetia and Zocor works better than Zocor alone were finally released today. Bottom line: Zetia, or ezetimibe generically, didnt bring anything important to the cholesterol party. Thats bound to be a bummer for sales of Zetia and Vytorin, the drug that combines Zocor, now sold generically as simvastatin, and ezetimibe.. The telling detail: there was no statistically significant difference in the primary endpoint of the study, a marker of atherosclerotic changes in the arteries called intima-media thickness, according to a Schering-Plough press release. Important secondary endpoints, the fallbacks for worried study designers, also showed no statistical difference between treatment groups.. The results of this two-year-long trial of 720 people with heterozygous familial hypercholesterolemia (HeFH), a rare, inherited form of high cholesterol that affects about 0.2% of ...
Ezetimibe interferes with the gastrointestinal absorption not only of cholesterol, but also of other molecular entities that could conceivably affect the growth of cancer cells. The fact that the combined data from all three trials showed an increase in cancer mortality with ezetimibe should not be assumed to be a chance finding until further data are in. It is appropriate that SHARP and IMPROVE-IT continue. Careful follow-up of the patients in these trials will be essential, and other existing data sets on ezetimibe-treated patients should be analyzed for cancer end points. The Food and Drug Administration has already announced that during the next few months it will conduct its own analysis of the potential cancer hazard of ezetimibe ...
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In March 2008, I had the honor of participating on a panel with Drs Joseph Messer, Rick Nishimura, and Patrick OGara, all exemplary clinicians and teachers, to discuss the results of the Ezetimibe and Simvastatin in Hypercholesterolemia Enhances Atherosclerosis Regression (ENHANCE) trial at the American College of Cardiology annual Scientific Session. The meeting was full of expectation for this trial, which compared the effect of simvastatin plus ezetimibe with simvastatin alone on the progression of carotid artery intima-media thickness. Anticipation was intensified because of the controversy that accompanied delays in the publication of the trial results.1 Our panel had early access to the results and discussed the findings. When our discussions led to a consensus of opinion, we decided to present a single statement rather than 4 distinct views. I was asked to draft the statement, which was discussed and approved by the panel, and present it at the Scientific Session.. ENHANCE, presented at ...
Where To Purchase Cheap Zetia without prescription. Zetia (ezetimibe) is used either alone or with other drugs, along with a low cholesterol/low fat diet, to help lower cholesterol in the blood. Reducing cholesterol helps prevent strokes and heart attacks. Ezetimibe works by reducing the amount of cholesterol your body absorbs from your diet. Generic Zetia may also be marketed as: Ezedoc, Ezetrol, Ezetimibe ...
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Use of a controversial new cholesterol-lowering drug, ezetimibe (trade names: Zetia, Ezetrol, Vytorin), has increased in the United States, far beyond that seen in Canada, where direct-to-consumer advertising (DTCA) is prohibited and there is more government regulation of drug reimbursement in publicly-funded drug formularies. Worldwide sales for ezetimibe is estimated at $5 billion in 2007.. A new study from Western University of Health Sciences in Pomona, Calif., in partnership with Ontario, Canadas Institute for Clinical Evaluative Sciences (ICES) and Yale University in Connecticut, found that over a recent four-year period, yearly prescriptions for ezetimibe in the U.S. grew to more than 33 million, while in Canada, with one-tenth of the U.S. population, ezetimibe only grew to 824,000 prescriptions. In 2006, ezetimibe accounted for 15 percent of all cholesterol-lowering prescriptions in the United States, while in Canada, it only represented 3.4 percent.. The study Use of Ezetimibe in the ...
BACKGROUND: Despite the established efficacy of statins, many patients do not achieve recommended LDL cholesterol (LDL-C) goals. Contributing factors may be inadequate dosing, increased risk for adverse effects with high-dose monotherapy, and increased potential for intolerance and adverse effects with combinations of available agents.. METHODS AND RESULTS: In a double-blind study, 628 patients with baseline LDL-C 145 to 250 mg/dL and triglycerides , or =350 mg/dL were randomly assigned to receive 1 of the following for 12 weeks: ezetimibe (10 mg/d); atorvastatin (10, 20, 40, or 80 mg/d); ezetimibe (10 mg) plus atorvastatin (10, 20, 40, or 80 mg/d); or placebo. The primary efficacy end point was percentage reduction in LDL-C for pooled ezetimibe plus atorvastatin versus pooled atorvastatin treatment groups. Ezetimibe plus atorvastatin significantly improved LDL-C, HDL cholesterol (HDL-C), triglycerides, total cholesterol:HDL-C, and high-sensitivity C-reactive protein (hs-CRP) compared with ...
Consumer Medicine Information (CMI) about APO-Ezetimibe/Simvastatin (Ezetimibe/Simvastatin) intended for persons living in Australia.
TY - JOUR. T1 - NPC1L1 inhibitor ezetimibe is a reliable therapeutic agent for non-obese patients with nonalcoholic fatty liver disease. AU - Enjoji, Munechika. AU - MacHida, Kazuyuki. AU - Kohjima, Motoyuki. AU - Kato, Masaki. AU - Kotoh, Kazuhiro. AU - Matsunaga, Kazuhisa. AU - Nakashima, Manabu. AU - Nakamuta, Makoto. PY - 2010/12/1. Y1 - 2010/12/1. N2 - Background: We recently examined the distribution of abdominal fat, dietary intake and biochemical data in patients with nonalcoholic fatty liver disease (NAFLD) and found that non-obese NAFLD patients did not necessarily exhibit insulin resistance and/or dysregulated secretion of adipocytokines. However, dietary cholesterol intake was superabundant in non-obese patients compared with obese patients, although total energy and carbohydrate intake was not excessive. Therefore, excess cholesterol intake appears to be one of the main factors associated with NAFLD development and liver injury. Methods. We reviewed a year of follow-up data of ...
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Dear Sir:. When platelets are activated, they increase in size and change from a quiescent disc to a swollen sphere. Large platelets are more reactive and likely aggregate more than small ones [1]. Mean platelet volume (MPV), an indicator of platelet size and activation, has been shown to predict ischemic stroke, myocardial infarction, and overall vascular mortality [2,3]. The IMProved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVEIT) study showed that ezetimibe added to statin therapy further decreases low density lipoprotein cholesterol (LDL-C) levels and prevented acute coronary syndromes [4]. In this study, we investigated the lowering effect of LDL-C and MPV changes in patients who are on statin-ezetimibe combination therapy and those who receive statin monotherapy.. Patients with acute ischemic cerebral infarctions (n=120) were divided into those who were on statin therapy (n=60) and those on statin plus ezetimibe (n=60). The statin group received either atorvastatin ...
Very few vytorin is indicated to reduce the risk of major. ;Annual spending on statins exceeded $19 million in 2005, ezetimibe (in the form of vytorin and; vytorin 10mg/20mg tablets manufactured by merck sharp ; dohme product of new zealand. ;S ($mrk) cholesterol franchise, an fda advisory panel shot down its bid to tout vytorin and zetia as preventives; 17 nov 2014 the long-awaited results of a trial of the cholesterol-lowering drug vytorin showed modest benefit and indicated that adding a non-statin drug to; vytorin is available for oral use as tablets containing 10 mg of ezetimibe, and 10 mg of (vytorin 10/10), 20 mg of simvastatin (vytorin 10/20), 40 mg of; compare prices and print coupons for vytorin and other high cholesterol drugs at cvs, walgreens, and other pharmacies ...
Ezetimibe And Simvastatin with NDC 43598-745 is a a human prescription drug product labeled by Dr.reddys Laboratories Inc. The generic name of Ezetimibe And Simvastatin is ezetimibe and simvastatin.
AIM: Patients with a recent myocardial infarction have an increased risk of recurrent ischaemic events. In the ESTEEM trial, the oral direct thrombin inhibitor ximelagatran reduced the risk of new ischaemic events when compared with placebo in aspirin treated post myocardial infarction patients. Ximelagatran persistently reduced markers of coagulation activity, i.e. prothrombin fragment 1 + 2 (F1 + 2) and D-dimer levels. The aim of this substudy was to evaluate the levels of these markers and activated thromboplastin time (APTT) in relation to new ischaemic events or bleeding. METHODS AND RESULTS: In the substudy, 518 out of 1883 patients were included and within 14 days after a myocardial infarction randomized to ximelagatran or placebo for 6 months. The clinical endpoints death, myocardial infarction, severe recurrent ischaemia, ischaemic stroke, and bleeding were evaluated. The levels of F1 + 2, D-dimer, and APTT were analysed at randomization and in serial samples during the study. ...
While the latest guidelines have recommended only statin-based treatments, ezetimibe, a drug that inhibits cholesterol absorption from the small intestine, has been introduced to the market. Ezetimibe lowers cholesterol in the blood by blocking Niemann-Pick C1-like 1 proteins, which are responsible for absorbing cholesterol in the pericytes of the small intestine wall and in hepatocytes, thereby enabling cholesterol to be excreted in the stool [12]. The IMProved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVE-IT), which examined the effect of ezetimibe in 18,144 patients with acute coronary syndrome, compared the incidence of cardiovascular diseases between a simvastatin 40 mg/ezetimibe 10 mg group and a simvastatin 40 mg group [13]. After 6 years of follow-up, the mean LDL-C concentration at the end of the study was 53.7 mg/dL in the simvastatin/ezetimibe group and 69.5 mg/dL in the simvastatin group. This result demonstrated that the additional administration of ezetimibe ...
study: a patient treated with atorvastatin, 20 mg/d, died of Ezetimibe/simvastatin reduced LDL-C levels by more than chronic obstructive pulmonary disease (not considered 50% from baseline at these doses, fulfilling the ADA rec- ommendation of a 30% to 40% reduction from baseline.2 Laboratory adverse events occurred in 8 patients (1.6%) This study also confirmed the superior attainment of LDL- in the ezetimibe/simvastatin group and 10 patients (1.4%) C levels of less than 70 mg/dL in high-risk patients with in the atorvastatin group. Drug-related LAEs occurred in 3 ezetimibe/simvastatin vs atorvastatin and did so across a patients in both treatment assignments. No serious LAEs wider range of dosages than previously reported.20 Thus, occurred, and no patients discontinued study participation these results add to the clinical experience with ezetimibe/ simvastatin, affirming its effectiveness in the management No patient had a creatine kinase elevation 10 or more of high LDL-C levels11-13,20,21 ...
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Ezetimibe/simvastatin is commonly prescribed to treat high cholesterol and triglycerides. This eMedTV resource describes how the medication works, explains when and how to take it, lists some of its potential side effects, and more.
BACKGROUND: Combining lipid-lowering agents with complementary mechanisms of action can provide greater cholesterol reductions than using either agent alone, improving achievement of target low-density lipoprotein cholesterol (LDL-C) levels.. OBJECTIVES: The aim of this study was to assess the effects of fluvastatin extended-release (XL) 80 mg/d administered alone or combined with ezetimibe 10 mg/d on plasma lipid levels and inflammatory parameters in patients with primary hypercholesterolemia. The tolerability of both regimens was also evaluated.. METHODS: In this multicenter, randomized, open-label, parallel-group study, patients with hypercholesterolemia were randomized in a 1:1 ratio to receive fluvastatin XL 80 mg/d alone or in combination with ezetimibe 10 mg/d for 12 weeks. The primary end point was the percentage change from baseline to week 12 in LDL-C level with fluvastatin XL + ezetimibe combination therapy compared with fluvastatin XL alone. Plasma concentrations of inflammatory ...
Lipitor (atorvastatin) and Vytorin (simvastatin and ezetimibe) are used to lower cholesterol levels in the blood. Lipitor and Vytorin contain HMG-CoA reductase inhibitors (
The results of the multicenter, randomized ENHANCE trial seem to suggest that in patients with very high baseline LDL levels, such as those with HeFH, the combination of ezetimibe/simvastatin 10/80 mg does not result in significant changes in the mean carotid IMT at 2 years when compared with high-dose simvastatin 80 mg alone. There was also no difference in the incidence of cardiovascular mortality, nonfatal myocardial infarction, nonfatal stroke, and need for revascularization, although this study was not powered to study clinical outcomes. The incidence of adverse events was similar. The LDL-lowering effect of ezetimibe/simvastatin was greater than that achieved with high-dose simvastatin alone ...
We show that, consistent with studies of ezetimibe coadministration with simvastatin in adults, significant incremental decreases of approximately 15% in LDL-C levels compared with administration of simvastatin alone were achieved within 6 weeks of treatment. These decreases were sustained throughout the subsequent 26-week, double-blind phase of the study in adolescent subjects with HeFH. Prolonged reductions were maintained through 53 weeks in the overall study population. Significantly greater reductions from baseline in total cholesterol, non-HDL-C, and apo B levels were also documented after 6 weeks and again at 33 weeks in subjects who received coadministration of ezetimibe with simvastatin compared with simvastatin monotherapy. These parameters also remained at reduced levels throughout the final 20-week phase of the study.. Mean incremental LDL-C reductions associated with coadministration of ezetimibe were consistent across the 10-, 20-, and 40-mg simvastatin dosing groups after 6 weeks ...
Diabetes mellitus (DM) is metabolic diseases characterized by chronic hyperglycemia due to reducing in insulin secretion, insulin function, or both. Ezetimibe is a drug that lowers plasma cholesterol levels. A total of 18 male adult albino rats were used in this study. The animals randomized into 3 groups (of 6 rats each). Rats in first group were injected with citrate buffer only and used as healthy control group. While the rats in other two groups were injected with streptozotocin (STZ) at a dose of 60 mg/kg I.P. and treated as following (for 12 weeks), diabetic control group rats received no treatment. Ezetimibe treated group rats received Ezetimibe 6 mg/kg orally once daily. Every 2 weeks, blood glucose level is measured. At the end of 12th weeks, blood samples were collected to measure the blood glucose level and superoxide dismutase activity, and then the animals were sacrificed. The pancreas was removed for histopathology assessment for the degree of islets damage. In result, Ezetimibe was
For patients with primary hypercholesterolemia, fixed-dose combination of ezetimibe plus rosuvastatin is more effective than rosuvastatin alone
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Ran-Ezetimibe: Ezetimibe belongs to the group of medications known as cholesterol absorption inhibitors. It lowers cholesterol levels by decreasing the bodys ability to absorb cholesterol from the digestive system. It is used in addition to exercise and a healthy diet to lower cholesterol levels for people with high cholesterol. It may also be used with additional cholesterol-lowering medications known as statins or fenofibrate when either therapy alone is not sufficient to reduce cholesterol to desired levels.
Simvastatin + Ezetimibe-ன் பயன்பாடுகள், மருந்தளவு, பக்க விளைவுகள், நன்மைகள், தொடர்புகள் மற்றும் எச்சரிக்கைகள் ஆகியவற்றை கண்டுபிடியுங்கள்.
Pyrrole and 2-azetidinone are two essential heterocyclic scaffolds, which are being broadly used in medicinal chemistry and drug discovery field. A green and practical method to synthesize novel N-(2-azetidinonyl) 2,5-disubstituted pyrroles, which are comprised of both pyrrole and 2-azetidinone moieties, has
TY - JOUR. T1 - 2-[18F]F-A-85380. T2 - A PET radioligand for α4β2 nicotinic acetylcholine receptors. AU - Chefer, Svetlana I.. AU - Horti, Andrew G.. AU - Koren, Andrei O.. AU - Gündisch, Daniela. AU - Links, Jonathan M.. AU - Kurian, Varughese. AU - Dannals, Robert F.. AU - Mukhin, Alexey G.. AU - London, Edythe D.. PY - 1999/9/9. Y1 - 1999/9/9. N2 - 2-[18F]FLUORO-3-(2(S)-AZETIDINYLMETHOXY)PYRIDINE (2[18F]F-A-85380), a ligand for nicotinic acetylcholine receptors (nAChRs) was evaluated in an in vitro binding assay with membranes of rat brain and in vivo by PET in Rhesus monkey brain. The ligand has high affinity for α4β2 nAChRs (K(D) = 50 pM), crosses the blood-brain barrier, and distributes in the monkey brain in a pattern consistent with that of α4β2 nAChRs. The specific/non- specific binding ratio increased steadily, reaching a value of 3.3 in the thalamus at 4 h. The specific binding of 2-[18F]F-A-85380 was reversed by cytisine. These results, in combination with the data ...
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Colantonio L, Cermignani E, Ciapponi A, Calcagno JI. Ezetimibe for primary hypercholesterolemia. Cochrane Database of Systematic Reviews 2015, Issue 6. Art. No.: CD006298. DOI: 10.1002/14651858.CD006298. ...
There are several alternatives to Advicor, including other statins or cholesterol medicines. As this eMedTV page explains, besides statins, other cholesterol medicines include fibrates, cholesterol absorption inhibitors, and bile acid sequestrants.
Subscribe: Apple Podcasts , Google Podcasts , Stitcher , RSS , More. On this episode, I discuss ezetimibe pharmacology. Ezetimibe works by inhibiting Niemann-Pick C1-Like1 (NPC1L1) transporter. This transporter aids in cholesterol absorption so by blocking it, we can reduce cholesterol levels (and LDL) in the bloodstream.. Ezetimibe is usually very well tolerated. Diarrhea, myopathy, and elevations in LFTs are adverse effects that have been reported but do not occur at high rates.. Ezetimibe is dosed at 10 mg once daily. This is a nice advantage because this is a starting dose and the usual treatment dose.. With the most recent cholesterol guideline updates, I do expect ezetimibe to be utilized a little more than it used to be. They place more emphasis on a target LDL and getting patients to goal.. Statins are going to be used first line for cholesterol and ezetimibe will be an add on therapy to consider. They dont, unfortunately, lower cholesterol as much as high-intensity statins do.. Be ...
Zetia has been reported to safely result in a modest further reduction of triglyceride levels in HIV+ patients in your situation. The ACTG has a Zetia study that is fully enrolled with results...
CDC is supporting blood centers by providing recommendations that will keep donors what is zetia used for and monitor recipients for human immunodeficiency virus (HIV), hepatitis B virus, and hepatitis C virus infections. CDC works to help people live longer, healthier and more productive lives. A US federal agency, CDC helps make the healthy choice the easy choice by putting science and prevention into action.. Findings from a Centers for Disease Control what is zetia used for and Prevention (CDC) and the American people by requiring air passengers entering the United Kingdom (U. Findings from a Centers for Disease Control and Prevention (CDC) will provide an update to media on the COVID-19 response. CDC has updated and expanded the U. Public Health Service (USPHS) published an updated solid organ transplant guideline to assess donors and monitor recipients for human immunodeficiency virus (HIV), hepatitis B virus, and hepatitis C virus infections.. The Centers for Disease Control and ...
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Vytorin (Ezetimibe/Simvastatin) is used for reducing total cholesterol, LDL cholesterol, and triglycerides and for increasing HDL cholesterol. buy cheap vytorin
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Before taking ezetimibe/simvastatin, tell your doctor or pharmacist if you think you are allergic to it; or to other drugs called statins; or if you have any other allergies. This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: active liver disease. Before using this medication, tell your doctor or pharmacist your medical history, especially of: heart disease, history of liver disease, kidney disease, underactive thyroid (hypothyroidism), poorly controlled diabetes, alcohol use. Developing severe muscle damage, which is rare, can sometimes lead to serious kidney problems (see the Side Effects section in this handout). This medication is usually temporarily stopped if you have any condition which can increase your risk of developing kidney problems. Before you stop taking your medication, notify your doctor immediately if you have any of the following conditions: major surgery, trauma, serious ...
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Vytorin 10/20 ( 10mg ezetimibe and 20mg simvastatin) is a combination drug which is used to reduce the total amounts of cholesterol, LDL (bad) cholesterol, triglycerides (another type of fat), and apolipoprotein B (a protein needed to make cholesterol) in the blood. Ezetimibe and simvastatin is also used to increase the level of HDL (good) cholesterol in the blood. Recent studies have found that it may possibly increase the risk of cancer in patients who are taking it. - Stock Image C003/0166
Results reported here Sunday may not put the nail in the coffin for a once wildly popular cholesterol-lowering drug, but they do put Zetia at the bottom of the list of medications that doctors will be using.
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