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Ezetimibe/atorvastatin (trade names Liptruzet, Atozet) is a cholesterol lowering combination drug. In the United States, it was approved in May 2013, by the Food and Drug Administration for the treatment of elevated low-density lipoprotein (LDL) in patients with primary or mixed hyperlipidemia as adjunctive therapy to diet. [ 1 ]
Atorvastatin, sold under the brand name Lipitor among others, is a statin medication used to prevent cardiovascular disease in those at high risk and to treat abnormal lipid levels. [6] For the prevention of cardiovascular disease, statins are a first-line treatment in reducing cholesterol. [ 6 ]
The exact mechanism responsible for the possible increased risk of diabetes mellitus associated with statin use is unclear. [106] However, recent findings have indicated the inhibition of HMGCoAR as a key mechanism. [110] Statins are thought to decrease cells' uptake of glucose from the bloodstream in response to the hormone insulin. [106]
Cholesterol absorption inhibitors are known to have a synergistic effect when combined a class of antihyperlipidemics called statins, to achieve an overall serum cholesterol target. For statin-resistant or statin-sensitive populations that are characterized by low one-year compliance rates, such a combination therapy is proving to be especially ...
Simvastatin is an effective serum lipid-lowering drug that can decrease low density lipoprotein (LDL) levels by up to 50%. [citation needed] Simvastatin had been shown to interact with lipid-lowering transcription factor PPAR-alpha [36] and that interaction might control the neurotrophic action of the drug.
With median follow-up of 6 years, simvastatin+ezetimibe was found to reduce the primary outcome of CV mortality, major CV event, or nonfatal stroke (34.7% vs. 32.7%; P=0.016; NNT 50 per 7 years or NNT 350 per 1 year ). There was no reduction in all-cause or CV mortality with simvastatin+ezetimibe, though there was a reduction in MI and stroke. [6]
Simvastatin and lovastatin are inactive lactones which must be metabolized to their active hydroxy-acid forms in order to inhibit HMGR. [7] Type 2 statins all exist in their active hydroxy-acid forms. Fluvastatin has indole ring structure, while atorvastatin and rosuvastatin have pyrrole and pyrimidine based ring structure
Ezetimibe, sold under the brand name Zetia among others, is a medication used to treat high blood cholesterol and certain other lipid abnormalities. [3] [4] Generally it is used together with dietary changes and a statin. [5]