Rosuvastatin

Rosuvastatin
ATC Code C10AA07
Formula C22H28FN3O6S
Molar Mass (g·mol−1) 481,538
Physical State solid
CAS Number 287714-41-4
PUB Number 446157
Drugbank ID DB01098
Solubility sparingly soluble in water

Basics

Rosuvastatin is an active ingredient from the group of statins. Due to its lipid-lowering properties, it is used to treat disorders of lipid metabolism and reduce the risk of cardiovascular disease.

It is considered the most effective statin drug because in clinical trials, the reduction in LDL cholesterol levels was about three times that of atorvastatin. However, despite this difference in efficacy, there are no differences in the effect on the progression of coronary atherosclerosis according to the results of the SATURN study.

Pharmacology

Pharmacodynamics

Elevated cholesterol and low-density lipoprotein (LDL) levels are significant risk factors for the development of cardiovascular disease. Rosuvastatin inhibits the enzyme HMG-CoA reductase, which plays a central role in endogenous cholesterol biosynthesis. The drug acts mainly in the liver, where the number of LDL receptors is increased, allowing more LDL to be taken up and broken down, and also inhibits the synthesis of VLDL (very low density lipoprotein). This leads to a decrease in LDL and VLDL in plasma. At the same time, HDL cholesterol (High Density Lipoprotein) is increased and triglycerides are decreased.

Pharmacokinetics

Rosuvastatin has an oral bioavailability of 20% and is 50% absorbed. Maximum plasma concentration is reached after approximately 5 hours. The drug binds 88% to plasma proteins and is absorbed primarily in the liver, where only about 10% is metabolized by the cytochrome P450 enzyme family. The half-life is approximately 19 hours but does not increase with increasing dose. Rovastatin is excreted unchanged 90% in the stool, the remainder in the urine.

It takes between two to four weeks for the effects of the statin to occur.

Drug Interactions

Because rosuvastatin is minimally metabolized via the cytochrome P450 system, fewer interactions occur (in contrast to atorvastatin, lovastatin, and simvastatin) with drugs metabolized by the same enzyme system.

Toxicity

Side effects

Adverse side effects such as myalgia (muscle pain), abdominal pain, nausea, and weakness may occur when taking rosuvastatin.

Toxicological Data

Overdose of rosuvastatin has mytoxic and hepatotoxic (damaging the muscle cells and liver) consequences.

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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