Statins · Cardiovascular
Rosuvastatin
Crestor®(brand names vary by market)
The most potent statin per milligram, and the one that mostly stays out of CYP3A4.
Mechanism
HMG-CoA reductase inhibitor: less hepatic cholesterol synthesis, upregulated LDL receptors, lower circulating LDL.
Indications
- Primary and secondary prevention of atherosclerotic cardiovascular disease
- Hypercholesterolemia
Formulations
Dosing concepts
Intensity
Statin choice is by intensity band rather than by milligrams: what matters is the expected percentage LDL reduction, and a lower dose of a potent statin can outperform a high dose of a weak one.
Ancestry
Exposure is higher in patients of East Asian ancestry, and starting doses are conventionally lower for that reason.
Concepts, not prescribing instructions. Practice numbers live in current references and local protocols.
Pharmacokinetics
- Bioavailability
- ~20%
- Half-life
- ~19 h
- Elimination
- hepatic: Largely unchanged in bile; minimal CYP3A4 involvement, unlike simvastatin and atorvastatin
- Protein binding
- ~90%
Its long half-life means it does not need to be taken at night, unlike the short-acting statins.
Play with these concepts in the PK LabAdverse effects
- MyalgiacommonCommon as a complaint, much rarer as a genuine drug effect in blinded trials; rechallenge often succeeds.
- RhabdomyolysisseriousRare; risk rises with interacting drugs, hypothyroidism and renal impairment.
- Transaminase elevationcommon
- New-onset diabetescommonSmall absolute risk, outweighed by cardiovascular benefit in those who need it.
Contraindications & precautions
Contraindications
- Active liver disease with unexplained persistent transaminase elevation
- Pregnancy and breastfeeding
Precautions
- Renal impairment at higher doses
- Hypothyroidism
- Concurrent fibrates or ciclosporin
Interactions
Monitoring
Lipid panel
Response, judged as percentage reduction · 6 to 12 weeks after starting or changing
Liver enzymes at baseline
Routine repeat testing is no longer recommended without symptoms
Muscle symptoms and CK if symptomatic
CK is not checked routinely in the well
Counselling points
- Any time of day, with or without food.
- Muscle aches are worth reporting; most turn out not to be the statin, and there are ways to test that.
- Not to be taken in pregnancy.
- Antacids reduce absorption if taken at the same time; separate them by two hours.
Clinical pearls
- Because it barely uses CYP3A4, it is the statin that survives a course of clarithromycin or a diltiazem prescription, where simvastatin would have to be held.
- The 'statin intolerance' conversation is worth having properly: blinded n-of-1 rechallenge studies find most muscle symptoms recur on placebo.
References & review
- Rosuvastatin product monograph (consult the current version for your market) (monograph)
- Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed. (reference-work)
Last reviewed 2026-08-16 · jurisdiction: global · drug information changes; verify against current references before practice use.