This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited. This article has been cited by other articles in PMC. Abstract The lowering of low-density lipoprotein cholesterol LDL-C is the primary target of therapy in the primary and secondary prevention of cardiovascular events. Although statin therapy is the mainstay for LDL-C lowering, a significant percentage of patients prescribed these agents either do not achieve targets with statin therapy alone or have partial or complete intolerance to them.
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This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited. This article has been cited by other articles in PMC. Abstract The lowering of low-density lipoprotein cholesterol LDL-C is the primary target of therapy in the primary and secondary prevention of cardiovascular events.
Although statin therapy is the mainstay for LDL-C lowering, a significant percentage of patients prescribed these agents either do not achieve targets with statin therapy alone or have partial or complete intolerance to them. For such patients, the use of adjuvant therapy capable of providing incremental LDL-C reduction is advised. One such agent is ezetimibe, a cholesterol absorption inhibitor that targets uptake at the jejunal enterocyte brush border. Its primary target of action is the cholesterol transport protein Nieman Pick C1 like 1 protein.
Ezetimibe is an effective LDL-C lowering agent and is safe and well tolerated. In response to significant controversy surrounding the use and therapeutic effectiveness of this drug, we provide an update on the biochemical mechanism of action for ezetimibe, its safety and efficacy, as well as the results of recent randomized studies that support its use in a variety of clinical scenarios. Keywords: bile, coronary artery disease, ezetimibe, low-density lipoprotein cholesterol, Nieman pick C1 like 1 protein, statin Introduction The association between elevated serum cholesterol levels and risk of cardiovascular disease has been well established through a number of epidemiologic studies, such as the Framingham Heart Study and the Seven Countries Study.
Ezetimibe inhibits intestinal and biliary cholesterol absorption and can significantly lower LDL-C and nonhigh-density lipoprotein cholesterol non-HDL-C, defined as total cholesterol minus high-density lipoprotein cholesterol when used alone or in combination with statin therapy.
This review aims to detail the biological mechanisms, lipid effects, and safety of ezetimibe treatment and discuss the vascular and clinical outcomes data that may impact the use of ezetimibe in clinical practice. Mechanism of action Circulating plasma levels of cholesterol are derived from two primary sources: cholesterol production from the liver and peripheral tissues, and the absorption of dietary and biliary cholesterol in the gastrointestinal tract Figure 1.
The transfer of cholesterol from the peripheral tissues to the liver is mediated by HDL. The cholesterol undergoes subsequent esterification by lecithin— cholesterol acetyltransferase. The esterified cholesterol moves into the hydrophobic core of the HDL particle, and as the particles become progressively more lipidated, they mature and become progressively larger and more spherical.
The cholesteryl esters in these mature HDL particles can be removed from the circulation by hepatic scavenger receptor BI or undergo transfer of cholesterol to apolipoprotein B-containing lipoproteins such as LDL and IDL via the activity of cholesteryl ester transfer protein.
Ezetimibe therapy: mechanism of action and clinical update
The Mechanism of Action of Ezetimibe Zetia on the Inhibition of Cholesterol Absorption Summary: Ezetimibe Zetia is useful in treating LDL-C as either monotherapy, in combination with statins, in combination with fenofibrate, in patients with homozygous familial hypercholesterolemia on either atorvastatin or simvastatin and in patients with homozygous sitosterolemia. Therefore, there is a reduction in the amount of Apo-B48 containing lipoproteins available to go into circulation. Editor-in-Chief: Anthony J. Nuzum, PharmD, BCACP, CDE Last Reviewed: October Explanation Ezetimibe Zetia is the first cholesterol absorption inhibitor that can primarily reduce low density lipoprotein cholesterol LDL-C , either as monotherapy, in combination with HMG CoA reductase inhibitor statin therapy, in combination with fenofibrate, or in patients with homozygous familial hypercholesterolemia on either atorvastatin or simvastatin and in patients with homozygous sitosterolemia.
EZETIMIBE MECANISMO DE ACCION PDF
Kazralrajas Interventions Patients were assigned ezetimine a hour infusion of levosimendan 0. Evangelizacion Indigena en Cuba Similarly, the microspheroids are spherical to sub-spherical, and occur as isolated elements or aggregates forming series of chains of parallel-packed light lamina mm thick. Pharmaco-economics of levosimendan in cardiology: Mechanistic and proof-of-concept studies are still required to clarify the ezetimibd mechanisms involved, while properly designed clinical trials are warranted to translate preclinical or early-phase clinical data into more robust clinical evidence. Scope of this study is to determine whether longer infusion patterns without the hypotension-inducing loading dose could justify an effective and safe alternative approach. All inodilators increased RV ejection fraction, preload recruitable stroke work, and ventricular-vascular coupling without jeopardizing perfusion pressure. Acute kidney injury AKI occurs frequently after cardiac surgery.