Rosuvastatin

• High Cholesterol
• Cardiovascular Disease Prevention
• Familial Hypercholesterolemia
• Atherosclerosis

Rosuvastatin is a potent HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and reduce cardiovascular risk. It is among the most effective statins for LDL reduction and is used in both primary and secondary prevention of atherosclerotic cardiovascular disease.

Mechanism of Action

Rosuvastatin inhibits cholesterol biosynthesis:

• HMG-CoA reductase inhibition: Competitively blocks the rate-limiting enzyme in cholesterol synthesis
• Reduces hepatic cholesterol: Leads to upregulation of LDL receptors
• Increases LDL clearance: More LDL receptors remove more LDL from circulation
• Pleiotropic effects: May improve endothelial function, reduce inflammation, and stabilize atherosclerotic plaques

Rosuvastatin is one of the most potent statins, achieving up to 55% LDL reduction at maximum dose.

Available Formulations

Rosuvastatin is available as tablets:

• 5 mg, 10 mg, 20 mg, 40 mg tablets

Also available as oral suspension and in combination products.

Medical Uses

FDA-Approved Indications:

• Primary hyperlipidemia and mixed dyslipidemia
• Hypertriglyceridemia
• Primary dysbetalipoproteinemia (Type III hyperlipoproteinemia)
• Homozygous familial hypercholesterolemia
• Pediatric patients 8-17 years with heterozygous familial hypercholesterolemia
• Primary prevention of cardiovascular disease in adults without clinical evidence of CHD but with elevated hsCRP and at least one additional CV risk factor
• Slowing progression of atherosclerosis

Dosing Guidelines

Adults (Hyperlipidemia):

• Initial: 10-20 mg once daily (5 mg for Asian patients or those with predisposing factors for myopathy)
• Range: 5-40 mg daily
• Maximum: 40 mg daily (requires careful patient selection)

Primary Prevention:

• 10-20 mg once daily

Pediatric (Heterozygous FH, 8-17 years):

• Initial: 5-10 mg once daily
• Maximum: 20 mg daily

Administration:

• May be taken with or without food, any time of day

Important Safety Information

Contraindications:

• Active liver disease or unexplained persistent transaminase elevations
• Pregnancy and breastfeeding
• Known hypersensitivity to rosuvastatin

Warnings and Precautions:

• Myopathy/Rhabdomyolysis: Risk increases with higher doses, renal impairment, hypothyroidism, and drug interactions
• Liver enzyme elevations: Monitor ALT before starting and as clinically indicated
• Proteinuria and hematuria: Observed at 40 mg dose
• Immune-mediated necrotizing myopathy: Rare autoimmune myopathy

Drug Interactions

• Cyclosporine: Contraindicated with rosuvastatin
• Gemfibrozil: Limit rosuvastatin to 10 mg/day
• Atazanavir/ritonavir, lopinavir/ritonavir: Limit to 10 mg/day
• Regorafenib, clopidogrel: May increase rosuvastatin exposure
• Warfarin: Monitor INR closely when initiating or adjusting dose
• Antacids: Take rosuvastatin 2 hours after aluminum/magnesium-containing antacids

Special Populations

• Asian Patients: Start with 5 mg due to increased exposure
• Renal Impairment:
  • eGFR ≥30: No adjustment (start 5 mg if severe impairment)
  • eGFR <30: Start 5 mg; max 10 mg; 40 mg contraindicated
• Hepatic Impairment: Contraindicated in active liver disease
• Pregnancy: Contraindicated (Category X)
• Lactation: Contraindicated