[Pharmacology of HMG CoA reductase inhibitors (statins)].
Statins without doubt belong to the most potent cholesterol and LDL-C lowering drugs. The mode of action is the stimulation of the LDL receptor activity in addition to a reduction of the assembly and biosynthesis of cholesterol-rich lipoproteins in the liver. The statins differ in their pharmakocinetic and pharmakodynamic properties in a qualitative and quantitative manner. Most of the pleiotropic effects of the statins are beneficial but not evenly distributed. The statins with the highest efficacy for reduction of cholesterol and triglycerides are atorvastatin and simvastatin. Statins are poor on side-effects, at maximal doses, however, it is important to consider drug interaction with other medication which are degraded by cytochrome-P450 oxidoreductase 3A4. Statins belong to the class of drugs which proved to reduce the total mortality in primary and secondary prevention of CHD. This is caused not only by the action on plasma lipids but also by their protective effect on endothelial cells, smooth muscle cells and platelets. In this way, they were found to stabilize atherosclerotic plaques. Because of these proven effects statins are nowadays applied also in patients with coronary heart diseases whose lipid values are relatively low and were considered as "normal" 5 to 10 years ago.
Institut für Medizinische Biochemie, Universität Graz. gerhard.kostner@kfunigraz.ac.at
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Kostner
D000924:Anticholesteremic Agents / Q000494:pharmacology*; D000069059:Atorvastatin; D002784:Cholesterol / Q000097:blood*; D008078:Cholesterol, LDL / Q000097:blood*; D004305:Dose-Response Relationship, Drug; D006538:Heptanoic Acids / Q000494:pharmacology; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000494:pharmacology*; D011758:Pyrroles / Q000494:pharmacology; D019821:Simvastatin / Q000494:pharmacology
D000924:Anticholesteremic Agents; D008078:Cholesterol, LDL; D006538:Heptanoic Acids; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D011758:Pyrroles; D002784:Cholesterol; D000069059:Atorvastatin; D019821:Simvastatin
Die Pharmakologie der HMG-CoA-Reduktasehemmer (Statine).