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In rabbits, liver cells sense the reduced levels of liver cholesterol and seek to compensate by synthesizing LDL receptors to draw cholesterol out of the circulation. [143] This is accomplished via proteases that cleave membrane-bound sterol regulatory element binding proteins, which then migrate to the nucleus and bind to the sterol response ...
All statins are metabolized by the liver, which causes their low systemic bioavailability. [13] Lovastatin and simvastatin are administered in their lactone forms, which is more lipophilic than their free acid forms, and therefore they have to be activated by hydrolysis to the active anionic carboxylate form.
In March 2012, the U.S. Food and Drug Administration (FDA) updated its guidance for statin users to address reports of memory loss, liver damage, increased blood sugar, development of type 2 diabetes, and muscle injury. [26] The new guidance indicates: FDA has found that liver injury associated with statin use is rare but can occur. [citation ...
A new analysis re-evaluates statins and who should use them. Statins are widely used to help lower cholesterol. Using a new analysis, researchers found that millions of people may be taking ...
In 1994, the findings of a Merck-funded study were published in The Lancet concluding the efficacy of statins in lowering cholesterol proving for the first time not only that a "statin reduced 'bad' LDL cholesterol but also that it led to a sharp drop in fatal heart attacks among people with heart disease." [110] [114]
Serious side effects may include rhabdomyolysis, liver problems, and diabetes. [5] Use during pregnancy may harm the fetus. [5] Like all statins, pravastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver that plays a role in producing cholesterol. [5] Pravastatin was patented in 1980 and approved for medical use in 1989. [6]