Pharmacology and mechanism of action of the new HMG-CoA reductase inhibitors.

摘要: Summary The new inhibitors of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase are synthetic compounds, fungal origin, inhibiting a key and unidirectional enzyme in the sterol biosynthetic pathway. Lovastatin, simvastatin pravastatin, currently available, differ, to some extent: lovastatin inactive pro-drugs, undergoing conversion by liver, most their metabolites active. Pravastatin is instead active per se with mostly metabolites. Distribution drugs different tissues, also depending upon relative inhibitory activity, may result cholesterol lowering potency as well in, eventually, tissue selectivity. Otherwise, plasma kinetics three agents rather short, usually progressive decay activity within 24 h from administration. Enzyme inhibition results upregulation high affinity receptors for low density lipoproteins (LDL), whose clearance markedly raised after treatment. HMG-CoA do not affect significant extent levels and/or composition other major lipoprotein fractions.