Rosuvastatin
CRESTOR
What it isHMG-CoA reductase inhibitor; high-intensity LDL lowering for hyperlipidemia and ASCVD prevention.
Why this oneVery potent with little CYP3A4 metabolism, making it useful when atorvastatin interactions are problematic.
What limits itRenal impairment and Asian ancestry increase exposure; cyclosporine and gemfibrozil greatly raise myopathy risk.
FDA-approved for
- hyperlipidemia (2003)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Hyperlipidemia / mixed dyslipidemia / CV risk reduction | Adults | 5–10 mg QD (per LDL-C and CV risk) | per LDL-C goal | 40 mg QD |
| Heterozygous familial hypercholesterolemia (HeFH) | Pediatric 8–<10 yr | 5 mg QD | — | 10 mg QD |
| Heterozygous familial hypercholesterolemia (HeFH) | Pediatric >=10 yr | 5 mg QD | — | 20 mg QD |
| Homozygous familial hypercholesterolemia (HoFH) | Pediatric >=7 yr | 20 mg QD | 20 mg QD | 20 mg QD |
| Asian patients | Adults | 5 mg QD | — | consider risk/benefit above 20 mg QD |
Titration Assess LDL-C and adjust dose as early as 4 weeks after initiation.
Renal No adjustment in mild-moderate impairment. Severe (CrCl <30, not on hemodialysis): initiate 5 mg, do not exceed 10 mg QD.
Hepatic Contraindicated in acute liver failure or decompensated cirrhosis.
Instructions
- Take orally once daily at any time of day, with or without food
- Swallow tablets whole
- Take at least 2 hours before an aluminum/magnesium hydroxide antacid
Contraindications
- Acute liver failure or decompensated cirrhosis
Cautions
- Myopathy and rhabdomyolysis (higher risk: age >=65, hypothyroidism, renal impairment, drug interactions, higher dose, Asian patients)
- Immune-mediated necrotizing myopathy
- Hepatic dysfunction
- Proteinuria and hematuria
- Increases in HbA1c / fasting serum glucose
Adverse reactions
- Headache
- Nausea
- Myalgia
- Asthenia
- Constipation
Pregnancy Discontinue when pregnancy is recognized; decreases cholesterol synthesis.
Lactation Undefined
NO BOXED WARNINGS
Principal riskMyopathy, rarely rhabdomyolysis
Cost, est. cash$4–$80/month
Generic entry2016
Classes and tags
Clinical profile
Legacy pregnancy categoryX
Defining liabilityMyopathy/rhabdomyolysis and hepatotoxicity; interaction burden varies by agent.
Mechanism of action: Rosuvastatin ballicule
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