[Statins in hypercholesterolemia treatment].
Statins are microorganism derived drugs that greatly impair the cell synthesis of cholesterol by competitively inhibiting the activity of the enzyme HMG-CoA reductase. Statins, however lower the blood level of cholesterol chiefly by increasing the number of high affinity receptors that recognize plasma LDL and by diminishing the VLDL synthesis rate in the liver. The latter explains the mild triglyceride reducing effect of these drugs. Statins efficiency in lowering the plasma cholesterol concentration is comparable to that of the bile acid binding polymers, but is better than that of the fibrates and nicotinic acid. Statins are better tolerated than the latter two drugs but are less efficient in lowering plasma triglycerides and in increasing the HDL-cholesterol concentrations. Tissue selectivity varies for the different statins but this is a secondary issue when the rarity of side effects is taken into account. Statins should be prescribed considering solely their pharmacologic efficiency and cost. Coronary angiography studies in coronary heart disease patients treated with placebo as compared to statins alone, or combined to other lipid lowering drugs, indicate that coronary artery disease regression can be achieved by pharmacological means.
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Laboratório de Lípides do Hospital das Clínicas, Faculdade de Medicina, Universidade de São Paulo.
D006801:Humans; D006903:Hydroxymethylglutaryl CoA Reductases / Q000187:drug effects / Q000378:metabolism; D006937:Hypercholesterolemia / Q000378:metabolism*; D008074:Lipoproteins / Q000187:drug effects / Q000378:metabolism; D008148:Lovastatin / Q000031:analogs & derivatives / Q000494:pharmacology*; D017035:Pravastatin / Q000494:pharmacology*
D008074:Lipoproteins; D008148:Lovastatin; D006903:Hydroxymethylglutaryl CoA Reductases; D017035:Pravastatin
Estatinas no tratamento da hipercolesterolemia.