Statins represent a class of cholesterol-lowering agents used for the treatment of dyslipidemia (abnormal amount of lipids) and the reduction of atherosclerotic cardiovascular disease risk. Their broad and potent effects on the lipid profile and cholesterol-independent pleiotropic cardioprotective effects positioned them among the most prescribed medications worldwide.
Statins were introduced in the late 1980s and early 1990s as a novel group of cholesterol-lowering drugs in attempt to offer patients with hypercholesterolemia a safe and effective means of reducing their plasma cholesterol. Research has shown that they not only have an important effect in reducing blood lipid levels, but also an individual’s risk of vascular disease in general.
Chemical structure and pharmacokinetics
The chemical structure of statins is constituted by two …show more content…
HMG-CoA reductase catalyzes the conversion of HMG-CoA to L-mevalonate and coenzyme A through four-electron reductive deacetylation. The pharmacophore of all statins bears resemblance to the endogenous HMG-CoA moiety, thus it competitively binds to the catalytic domain of HMG-CoA reductase, causing steric hindrance and halting HMG-CoA from accessing the active site.
Their antiatherosclerotic effects positively correlate with the percent decrease in LDL cholesterol, but such effects can be exerted independently of their hypolipidemic action. Such non-lipid effects at least partly reflect statins’ ability to block the synthesis of significant isoprenoid intermediates, which act as lipid attachments for a plethora of intracellular signaling
Statins were introduced in the late 1980s and early 1990s as a novel group of cholesterol-lowering drugs in attempt to offer patients with hypercholesterolemia a safe and effective means of reducing their plasma cholesterol. Research has shown that they not only have an important effect in reducing blood lipid levels, but also an individual’s risk of vascular disease in general.
Chemical structure and pharmacokinetics
The chemical structure of statins is constituted by two …show more content…
HMG-CoA reductase catalyzes the conversion of HMG-CoA to L-mevalonate and coenzyme A through four-electron reductive deacetylation. The pharmacophore of all statins bears resemblance to the endogenous HMG-CoA moiety, thus it competitively binds to the catalytic domain of HMG-CoA reductase, causing steric hindrance and halting HMG-CoA from accessing the active site.
Their antiatherosclerotic effects positively correlate with the percent decrease in LDL cholesterol, but such effects can be exerted independently of their hypolipidemic action. Such non-lipid effects at least partly reflect statins’ ability to block the synthesis of significant isoprenoid intermediates, which act as lipid attachments for a plethora of intracellular signaling