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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.
The exact mechanism responsible for the possible increased risk of diabetes mellitus associated with statin use is unclear. [105] However, recent findings have indicated the inhibition of HMGCoAR as a key mechanism. [109] Statins are thought to decrease cells' uptake of glucose from the bloodstream in response to the hormone insulin. [105]
Atorvastatin synthesis in commercial production (process) chemistry. The key step of establishing this medication's stereocenters, through initial use of an inexpensive natural product (chiral pool approach). Atorvastatin synthesis during discovery chemistry. The key step of establishing stereocenters, using of a chiral ester auxiliary approach.
Moreover, statins are not recommended in pregnancy as they may cause foetal harm because of their mechanism of action. [19] Metabolised by the Cytochrome P450 (CYP450) enzyme, a major metabolic enzyme, simvastatin and lovastatin may accumulate in blood when administered with CYP450 inhibitors.
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 ]
In studies using standard doses, statins have been found to lower LDL-C by 18% to 55%, depending on the specific statin being used. A risk exists of muscle damage (myopathy and rhabdomyolysis) with statins. Hypercholesterolemia is not a risk factor for mortality in persons older than 70 years and risks from statin drugs are more increased after ...
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]
Ezetimibe inhibits the intestinal absorption of cholesterol and can be used alone or with statins. [24] Regarding cardiovascular events, patients with chronic kidney disease saw a reduction in vascular and major atherosclerotic events when on simvastatin and ezetimibe compared to placebo. [25]
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