[Pharmacologic characteristics of rosuvastatin, a new HMG-CoA reductase inhibitor].
Rosuvastatin is a new synthetic statin that produces a more potent and prolonged inhibition of HMG-CoA reductase than any of the other statins currently available. It is also characterised by a very low lipophilicity, which is close to that of pravastatin, and by a high hepatic selectivity. Rosuvastatin is not extensively metabolised, with little or no transformation by the different isoenzymes of cytochrome P450. It is mainly eliminated in the faeces, with an elimination half-life in humans of between 13 and 21 hours. In patients with hypercholesterolaemia, rosuvastatin was associated with large dose-dependent reductions in low density lipoprotein (LDL)-cholesterol, by 50.5% at a dose of 10 mg/day and up to 64.8% at a dose of 80 mg. Each doubling of the dose of rosuvastatin results in an additional 4.5% decrease in blood LDL-cholesterol. In phase III studies, rosuvastatin decreased LDL-cholesterol significantly more than atorvastatin, pravastatin and simvastatin. Compared with the other statins, the decrease in triglyceride levels was similar and the increase in high density lipoprotein-cholesterol was more marked, with a significant difference in most cases. To date, there has not been an excess of adverse reactions, especially liver or muscle problems, compared with the reference statins. The safety of rosuvastatin can only be definitively established in post-marketing surveys.
Bousquet
Pascal
P
Département de Pharmacologie, Université de Strasbourg, Strasbourg, France.
Gayet
Jean-Louis
JL
D000818:Animals; D000924:Anticholesteremic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D002784:Cholesterol / Q000097:blood; D005464:Fluorobenzenes / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D011743:Pyrimidines; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides
D000924:Anticholesteremic Agents; D005464:Fluorobenzenes; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D011743:Pyrimidines; D013449:Sulfonamides; D000068718:Rosuvastatin Calcium; D002784:Cholesterol