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The discovery of HMG-CoA (3-hydroxy-3-methylglutaryl-CoA) reductase inhibitors, called statins, was a breakthrough in the prevention of hypercholesterolemia and related diseases. Hypercholesterolemia is considered to be one of the major risk factors for atherosclerosis which often leads to cardiovascular, cerebrovascular and peripheral vascular ...
The risk of statin-induced rhabdomyolysis increases with older age, use of interacting medications such as fibrates, and hypothyroidism. [94] [95] Coenzyme Q10 (ubiquinone) levels are decreased in statin use; [96] CoQ10 supplements are sometimes used to treat statin-associated myopathy, though evidence of their efficacy is lacking as of 2017. [97]
The water-soluble MβCD is known to form soluble inclusion complexes with cholesterol, thereby enhancing its solubility in aqueous solution. MβCD is employed for the preparation of cholesterol-free products: the bulky and hydrophobic cholesterol molecule is easily lodged inside cyclodextrin rings.
Lovastatin is a prodrug, an inactive lactone in its native form, the gamma-lactone closed ring form in which it is administered, is hydrolysed in vivo to the β-hydroxy acid open ring form; which is the active form. Lovastatin and other statins have been studied for their chemopreventive and chemotherapeutic effects.
Atorvastatin is a statin medication used to prevent cardiovascular disease in those at high risk and to treat abnormal lipid levels. [4] For the prevention of cardiovascular disease, statins are a first-line treatment. [4] It is taken by mouth.
Coadministration of statins with phytosterol-enriched foods increases the cholesterol-lowering effect of phytosterols, again without any proof of clinical benefit and with anecdotal evidence of potential adverse effects. [23] Statins work by reducing cholesterol synthesis via inhibition of the rate-limiting HMG-CoA reductase enzyme.
Pitavastatin is a lipophillic statin. [8] [9] Reports indicate that this statin may lead to fewer muscle side effects than other statins. [10] One study found that coenzyme Q 10 was not reduced as much as with certain other statins (though this is unlikely given the inherent chemistry of the HMG-CoA reductase pathway that all statin drugs inhibit).
Cerivastatin is a pure synthetic drug, produced to create a more potent inhibitor of HMG-CoA reductase. Cerivastatin was the most potent inhibitor with an inhibitory constant of 0.5 μg/L, which made it already effective at a low dose. It is taken up orally as tablets, where it is combined with sodium salt.