Rosuvastatin
Rosuvastatin is a high-intensity statin used in adults for primary and secondary prevention of cardiovascular disease. It inhibits HMG-CoA reductase, reduces LDL cholesterol substantially and lowers the risk of cardiovascular events.
- Chemical formula
- C22H28FN3O6S
- CAS number
- 287714-41-4
- ATC code
- C10AA07
- Molecular weight
- 481.54 g/mol
- Drug class
- HMG-CoA reductase inhibitor (statin)
- Also known as
- ZD-4522, Rosuvastatina
What is it?
Rosuvastatin is a synthetic HMG-CoA reductase inhibitor approved in 2003. It is supplied as oral tablets at multiple strengths and is dispensed only on prescription. Compared with other statins, rosuvastatin is one of the most potent on a per-milligram basis, with consistent reduction of LDL cholesterol and a long elimination half-life. The molecule is part of routine cardiovascular prevention strategies in adults at increased risk.
Mechanism of action
Rosuvastatin competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol synthesis. The reduction in intracellular cholesterol upregulates LDL receptors and increases clearance of circulating LDL. Pleiotropic effects on endothelial function, inflammation and plaque stability contribute to cardiovascular protection. The compound is more hydrophilic than many other statins, which may influence tissue distribution and the side-effect profile in some patients.
Pharmacokinetics
Rosuvastatin is absorbed orally with peak plasma concentrations reached after three to five hours. Absolute bioavailability is approximately 20%. Plasma protein binding is about 88%. The drug is excreted predominantly unchanged in faeces, with limited cytochrome P450 metabolism, mainly by CYP2C9. The terminal half-life is approximately 19 hours. Asian ethnicity is associated with higher exposure at the same dose, requiring lower starting doses according to the prescribing information.
Indications
Rosuvastatin is approved in adults for the treatment of primary hypercholesterolaemia and mixed dyslipidaemia, for the prevention of cardiovascular events in patients at elevated risk and for the secondary prevention of cardiovascular events. It is also approved in paediatric populations from age 6 with familial hypercholesterolaemia in some markets, under specialist supervision. According to international guidelines, dose selection depends on baseline risk and target LDL.
Safety profile
Common adverse effects include myalgia, gastrointestinal symptoms, headache and mild elevations of liver enzymes. As with other statins, severe muscle injury including rhabdomyolysis is rare but possible, particularly at high doses or with predisposing factors. Asymptomatic dipstick proteinuria has been reported, mostly transient and benign. New-onset diabetes has been reported with statin therapy. According to the prescribing information, baseline liver function should be checked, and unexplained muscle symptoms should be reported promptly.
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Frequently asked questions
How is rosuvastatin different from atorvastatin? ▾
Both are high-intensity statins, but rosuvastatin is more hydrophilic, has a longer half-life of about 19 hours and is excreted mostly unchanged in faeces, while atorvastatin is more lipophilic and metabolised mainly by CYP3A4. Rosuvastatin is approximately three to four times more potent on a per-milligram basis. According to international guidelines, both are first-line in high-risk patients; the choice is made by the prescriber.
Why are starting doses lower in Asian patients? ▾
Pharmacokinetic studies have shown that systemic exposure to rosuvastatin is approximately twice as high in patients of Asian descent at the same dose, due to genetic differences in transporter activity. The prescribing information therefore recommends a lower starting dose in patients of Asian ancestry, with cautious titration. According to the prescribing information, the medical history including ethnicity should be reviewed by the prescriber.
Is rosuvastatin safe in kidney disease? ▾
Mild to moderate renal impairment does not require routine dose adjustment, but rosuvastatin clearance decreases in severe renal impairment, where the dose is limited and starting from the lower strengths is recommended in the prescribing information. Asymptomatic transient proteinuria is more common at high doses. Patients with severe renal impairment require periodic monitoring of renal function and creatine kinase under medical supervision.
Should rosuvastatin be taken at a specific time? ▾
Rosuvastatin can be taken at any time of day, with or without food, because its long half-life provides sustained inhibition of cholesterol synthesis throughout the 24-hour cycle. According to the prescribing information, consistency is the most important factor — taking the dose at the same time each day improves adherence and supports stable lipid control.
What are the main contraindications for rosuvastatin? ▾
Rosuvastatin is contraindicated in known hypersensitivity to the molecule, in active liver disease or unexplained persistent elevation of serum transaminases, in severe renal impairment for the higher doses defined in the prescribing information, in concomitant ciclosporin therapy at full doses, and during pregnancy and breastfeeding. According to the prescribing information, the medical history must be reviewed by a clinician before any prescription.
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