BLACK BOX WARNING
- myopathy and rhabdomyolysis
rosuvastatin
Brand: Crestor
⚠ BBW Prototype: atorvastatin
Drug Class: statin
Drug Family: antilipemic
Subclass: HMG-CoA reductase inhibitor (synthetic)
Organ Systems: cardiovascular
Mechanism of Action
Potent synthetic statin; less CYP3A4 metabolism than atorvastatin; most hydrophilic statin; high LDL reduction efficacy (up to 63% at maximum dose).
HMG-CoA reductase
Indications
- hyperlipidemia
- ASCVD prevention
- familial hypercholesterolemia
- mixed dyslipidemia
Contraindications
- active liver disease
- pregnancy
- unexplained transaminase elevation
- renal impairment (reduce dose)
Adverse Effects
Common
- myalgia
- headache
- nausea
- hyperglycemia
Serious
- rhabdomyolysis
- myopathy
- new-onset diabetes
Pharmacokinetics (ADME)
| Absorption | 20% oral bioavailability |
| Distribution | moderate |
| Metabolism | CYP2C9 minor; largely unchanged |
| Excretion | fecal 90% |
| Half-life | 19 hours |
| Onset | 2-4 hours |
| Peak | 3-5 hours |
| Duration | 24 hours |
| Protein Binding | 88% |
| Vd | 134 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| cyclosporine | markedly increases rosuvastatin — cap at 5 mg | major |
| gemfibrozil | OATP1B1 inhibition; cap at 10 mg | major |
| anticoagulants (warfarin) | may increase INR | moderate |
Nursing Considerations
- Most potent LDL-lowering statin per mg
- JUPITER trial: reduced CV events in patients with normal LDL but elevated hsCRP
- Dose cap with cyclosporine (5 mg) and gemfibrozil (10 mg)
- Asian patients may have higher plasma levels — start at lower doses (5 mg)
Clinical Pearls
- JUPITER trial: rosuvastatin 20 mg reduced CV events in primary prevention with elevated hsCRP
- Most hydrophilic statin — theoretically reduced risk of muscle/CNS side effects vs lipophilic agents (not proven)
Safety Profile
Pregnancy contraindicated
Lactation contraindicated
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Guideline Update pending
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.