Description

inhibitors of HMG-CoA reductase
presence of high levels of cholesterol in the blood
one of first statins to be isolated, not available to human treatment (Compactin)
second derivative of statin discovered (Altocor)
lovastatin and simvastatin are prodrugs containing this closed-ring functional group
more lipophilic and potent statin derived from lovastatin (Zocor)
derivative of Compactin, not needing activation when absorbed (Pravachol)
key compound in cholesterol production that is reduced by statins
refers to the hydrophilic and lipophilic nature of statins
major area of absorption of statins
statins are metabolized by this organ before entering circulation, decreasing bioavailability to 5-30%
major family of enzymes that metabolize statins
statins are typically substrates for this CYP enzyme
statins are observed to help preserve endothelial nitric oxide synthase which leads to:
buildup of cholesterol in blood vessels which can result in heart disease
statins are known to increase resistance to this hormone, which can lead to diabetes
common adverse effect of statin use
blood in urine – rare side effect associated with statins
statin with low rate of renal excretion allowing for use in patient with impaired renal function (Lipitor)
hypercholesterolemia is a main risk factor for this condition
an adverse effect of statin use can result in an increase of this enzyme
breakdown of damaged skeletal muscle – most severe adverse effect of statin use
drug often paired with statins to increase antilipidemic effect
statins first studies for this use, to reduce cholesterol synthesis in bacteria
precursor to mevalonate, substrate for HMG-CoA reductase
major course of HMG-CoA reductase
any combination of fats/lipids with proteins in the blood plasma
lipoprotein associated with increased cholesterol, excess can lead to heart disease
1 of 2 isoprenoid intermediates decreased by statins – decrease inflammatory response
1 of 2 isoprenoid intermediates decreased by statins – decrease inflammatory response (bound to pyrophosphate)
contains about 25% of body’s cholesterol, which may be affected by statins
source of first isolated cholesterol crystals extracted in 1784
patients on statin therapy may show lower erosion of this part of the chromosome
possible adverse tumor formation in very high doses of lovastatin
common electron carrier serving as a cofactor for the reduction of HMG-CoA to mevalonate
halide added in newer generation statins in increase substrate binding
about 100x more potent that lovastatin, withdrawn from market increased toxicity
Use of statins are shown to _________ levels of HMG-CoA reductase in the liver
vital mitochondrial electron transporter molecule that can be potentially reduced with statins
compound required for glycoprotein synthesis that can be reduced with stain use
other class of lipids that can be reduced with statins

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