Overview
Rosuvastatin is a statin medication used to lower LDL cholesterol and reduce cardiovascular risk. It works by inhibiting HMG-CoA reductase in the liver, which decreases cholesterol production and increases LDL receptor expression. It is indicated for primary hyperlipidemia, heterozygous and homozygous familial hypercholesterolemia, and cardiovascular risk reduction in appropriate patients.
Mechanism of Action
Rosuvastatin competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis in the liver. This inhibition reduces hepatic cholesterol production, leading to upregulation of LDL receptors on hepatocytes and increased clearance of LDL cholesterol from the bloodstream.
Indications
- To reduce the risk of major adverse cardiovascular events in adults without established coronary heart disease who are at increased risk based on age, hsCRP ≥2 mg/L, and at least one additional CV risk factor
- As an adjunct to diet to reduce LDL-C in adults with primary hyperlipidemia
- As an adjunct to diet to reduce LDL-C and slow progression of atherosclerosis in adults
- As an adjunct to diet to reduce LDL-C in adults and pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia (HeFH)
- As an adjunct to other LDL-C-lowering therapies to reduce LDL-C in adults and pediatric patients aged 7 years and older with homozygous familial hypercholesterolemia (HoFH)
- As an adjunct to diet for treatment of adults with primary dysbetalipoproteinemia
- As an adjunct to diet for treatment of adults with hypertriglyceridemia
Common Doses
- 5 mg
- 10 mg
- 20 mg
- 40 mg
Dosage
Typical starting dose is 5-20 mg once daily, with maximum dose of 40 mg daily. Dose should be individualized based on indication, LDL-C goals, and patient factors. Asian patients may require lower starting doses.
Contraindications
- Acute liver failure or decompensated cirrhosis
- Hypersensitivity to rosuvastatin or any excipients in the formulation
- Concomitant use with cyclosporine
Side Effects
- Headache
- Myalgia
- Abdominal pain
- Nausea
- Asthenia
- Constipation
- Increased hepatic transaminases
- Muscle spasms
- Arthralgia
- Rhabdomyolysis (rare but serious)
- Immune-mediated necrotizing myopathy
- Hypersensitivity reactions including rash, pruritus, urticaria, and angioedema
Interactions
- Cyclosporine - concomitant use contraindicated
- Gemfibrozil - avoid combination due to increased risk of myopathy
- Other fibrates - increased risk of myopathy
- Warfarin - may potentiate anticoagulant effect
- Protease inhibitors - may increase rosuvastatin exposure
- Antacids - separate administration by at least 2 hours
Counseling Points
- Take once daily with or without food, preferably in the evening
- Report unexplained muscle pain, tenderness, or weakness immediately
- Avoid excessive alcohol consumption
- Maintain a heart-healthy diet while taking this medication
- Inform healthcare provider of all medications, including over-the-counter products and supplements
- Regular monitoring of cholesterol levels and liver function tests is required
- Do not take during pregnancy or breastfeeding