Rosuvastatin
Regulatory sources consulted
- AEMPS CIMA Ficha Técnica: https://cima.aemps.es/cima/dochtml/ft/82061/FT_82061.html
- AEMPS CIMA · nº registro 82061 ↗
- RxNorm rxcui 301542 ↗
Approved indications
- Treatment of primary hypercholesterolemia (type IIa, including heterozygous familial hypercholesterolemia) or mixed dyslipidemia (type IIb) as an adjunct to diet when response to diet and other non-pharmacological treatments (e.g., exercise, weight loss) is inadequate.
- Treatment of homozygous familial hypercholesterolemia as an adjunct to diet and other lipid-lowering treatments (e.g., LDL apheresis) or if such treatments are not appropriate.
- Prevention of major cardiovascular events in patients estimated to be at high risk for a first cardiovascular event, as an adjunct to correction of other risk factors.
Contraindications
Absolute
- Hypersensitivity to rosuvastatin or to any of the excipients.
- Active liver disease.
- Myopathy.
- Concomitant treatment with cyclosporine.
- Pregnancy and lactation.
Clinical warnings
- Major warning · Muscle effects: Cases of myalgia, myopathy, and rarely, rhabdomyolysis have been reported. The risk increases with higher doses, age >65 years, hypothyroidism, renal impairment, and drug interactions. — AEMPS CIMA
- Major warning · Hepatic effects: Liver function tests are recommended before initiating treatment and periodically thereafter. Contraindicated in active liver disease. — AEMPS CIMA
- Diabetes Mellitus: Statins may increase HbA1c and fasting serum glucose, and in some high-risk patients, may precipitate hyperglycemia requiring diabetes management. — AEMPS CIMA
Drug interactions
- HighCyclosporineL04AD01
Mechanism: Inhibition of OATP1B1 and BCRP transporters, resulting in a 7-fold increase in rosuvastatin AUC.
Recommendation: Contraindicated. Concomitant use is forbidden.
AEMPS CIMA
- HighGemfibrozilC10AB04
Mechanism: Inhibition of OATP1B1 transporter and possible inhibition of rosuvastatin metabolism, resulting in a 2-fold increase in rosuvastatin AUC.
Recommendation: Avoid concomitant use. If necessary, start rosuvastatin at 5 mg and do not exceed a dose of 10 mg/day.
AEMPS CIMA
Adverse events
Common (≥1%)
myalgia · asthenia · headache · nausea · constipation · diabetes mellitus
Rare but serious
rhabdomyolysis · hepatotoxicity · pancreatitis · immune-mediated necrotizing myopathy · angioedema
Pregnancy and lactation
FDA category: X
Rosuvastatin is contraindicated during pregnancy and lactation. Women of childbearing potential should use appropriate contraceptive measures.