COMPARISON OF PROPERTIES OF 4 INHIBITORS OF 3-HYDROXY-3-METHYLGLUTARYL-COENZYME-A REDUCTASE

被引:181
作者
BLUM, CB [1 ]
机构
[1] COLUMBIA UNIV,COLL PHYS & SURG,DEPT MED,NEW YORK,NY
关键词
D O I
10.1016/0002-9149(94)90626-2
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Four inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase have been approved for treatment of hypercholesterolemia. Three of these are fungal metabolites or derivatives thereof: lovastatin, simvastatin, and pravastatin. The fourth, fluvastatin, Is totally synthetic. Its structure, containing a fluorophenyl-substituted indole ring, is distinct from that of the fungal metabolites. Lovastatin and simvastatin are administered as prodrugs, which undergo in vivo transformation to active inhibitory forms; fluvastatin acid pravastatin are administered as active agents. The HMG-CoA reductase inhibitors are all effective in reducing plasma concentrations of low density lipoprotein. They have differing pharmacokinetic properties, which may be of importance in some patients. All of these drugs are very well tolerated, and there do not appear to be major differences In toxicity or adverse effects. When LDL reductions >30% are needed, simvastatin is the most cost-effective HMG-CoA reductase inhibitor. However, these drugs are most commonly used in dosages that reduce LDL-C by 20-30%. For this degree of LDL reduction, fluvastatin is the most cost-effective HMG-CoA reductase inhibitor.
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页码:D3 / D11
页数:9
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