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
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.