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.

Author

Markus Falkenstätter, BSc

Pharmacy student

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Reviewer

Mag. pharm. Stefanie Brandauer

Pharmacist

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

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