ATORVASTATIN - A REVIEW OF ITS PHARMACOLOGY AND THERAPEUTIC POTENTIALIN THE MANAGEMENT OF HYPERLIPIDEMIAS

Authors
Citation
Ap. Lea et D. Mctavish, ATORVASTATIN - A REVIEW OF ITS PHARMACOLOGY AND THERAPEUTIC POTENTIALIN THE MANAGEMENT OF HYPERLIPIDEMIAS, Drugs, 53(5), 1997, pp. 828-847
Citations number
129
Categorie Soggetti
Pharmacology & Pharmacy",Toxicology
Journal title
DrugsACNP
ISSN journal
00126667
Volume
53
Issue
5
Year of publication
1997
Pages
828 - 847
Database
ISI
SICI code
0012-6667(1997)53:5<828:A-AROI>2.0.ZU;2-Q
Abstract
Atorvastatin is a synthetic HMG-CoA reductase inhibitor which lowers p lasma cholesterol levels by inhibiting endogenous cholesterol synthesi s. it also reduces triglyceride levels through an as yet unproven mech anism. Dose-dependent reductions in total cholesterol, low density lip oprotein(LDL)-cholesterol and triglyceride levels have been observed w ith atorvastatin in patients with hypercholesterolaemia and in patient s with hypertriglyceridaemia. In large trials involving patients with hypercholesterolaemia, atorvastatin produced greater reductions in tot al cholesterol, LDL-cholesterol, apolipoprotein B and triglyceride lev els than lovastatin, pravastatin and simvastatin. In patients with pri mary hypercholesterolaemia, the combination of atorvastatin and colest ipol tended to produce larger reductions in LDL-cholesterol levels and smaller reductions in triglyceride levels than atorvastatin monothera py. Although atorvastatin induced smaller reductions in triglyceride l evels and more modest increases in high density lipoprotein (HDL)-chol esterol levels than either fenofibrate or nicotinic acid in patients w ith combined hyperlipidaemia, it produced larger reductions in total c holesterol and LDL-cholesterol. As with other HMG-CoA reductase inhibi tors, the most frequently reported adverse events associated with ator vastatin are gastrointestinal effects. In comparative trials, atorvast atin had a similar adverse event profile to that of other HMG-CoA redu ctase inhibitors. Clinical data with atorvastatin are limited at prese nt. However with its ability to markedly reduce LDL-cholesterol levels , atorvastatin is likely to join other members of its class as a first -line agent for the treatment of patients with hypercholesterolaemia, if changes in lipid levels with atorvastatin convert to reductions in CHD mortality and morbidity. Atorvastatin may be particularly suitable for patients with heterozygous or homozygous familial hypercholestero laemia because of the marked reductions in LDL-cholesterol experienced with the drug. Additionally, because of its triglyceride-lowering pro perties, atorvastatin appears to have the potential to become an appro priate treatment for patients with combined hyperlipidaemia or hypertr iglyceridaemia.