Rosuvastatin
Brand names: Crestor
Class: 🧪 Statins
On board day, rosuvastatin is the statin of choice when CYP3A4 interactions complicate other options. It is the most potent statin per milligram — high-intensity at 20–40 mg, dropping LDL by ~50% — and is metabolized primarily through CYP2C9 with minimal CYP3A4 involvement, so amiodarone, clarithromycin, and protease inhibitors are less worrisome than with simvastatin or atorvastatin. Indications cover the ACC/AHA benefit groups for primary and secondary ASCVD prevention. Dose-adjust in CKD and in Asian patients (slower metabolism). Side effects are the statin class set: myalgias, rare rhabdomyolysis, mild transaminase elevations. Contraindicated in pregnancy and active liver disease. Counsel on muscle-pain reporting, not routine baseline CK.
✅ Indications
Primary + secondary ASCVD prevention; particularly for high LDL, intolerance to other statins.
⚙️ Mechanism of Action
HMG-CoA reductase inhibitor.
📏 Dosing
5–40 mg PO daily. Start 5 mg in Asian patients (↑ levels).
🚫 Contraindications
Active liver disease, pregnancy, lactation.
⚠️ Adverse Effects
Myalgia, ↑ LFTs, rhabdomyolysis, proteinuria (dose-dependent), ↑ BG.
🔬 Monitoring
LFTs at baseline, lipid panel at 4–12 weeks.
💎 Board Pearls
- 🏆 HIGHEST intensity per mg — 20 mg ≈ atorvastatin 40 mg LDL-lowering.
- 🌏 Asian patients have ↑ plasma levels → start at 5 mg.
- 💧 Most hydrophilic statin → less muscle penetration → theoretically less myalgia.
Practice Questions
A 45-year-old Japanese man with LDL of 168 mg/dL and an ASCVD 10-year risk of 9% is being started on rosuvastatin (Crestor). Which starting dose is most appropriate based on current FDA labeling and pharmacokinetic data?
Related Drugs in This Class
- Atorvastatin — Lipitor
- Simvastatin — Zocor
Sources
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