Rosuvastatin !

A potent, long-acting statin that relies little on CYP3A4. It lowers LDL cholesterol strongly and reduces heart attacks and strokes.

Updated 2026-11-01

Class: Statins
Enzyme: HMG-CoA reductase
ATC code: C10AA07

HMG-CoA reductaseRosuvastatin

The figure shows rosuvastatin in the HMG-CoA pocket of the catalytic portion of human HMG-CoA reductase.

Target in 3D: HMG-CoA reductase. PDB structure 1HWL (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Rosuvastatin competitively inhibits HMG-CoA reductase, the rate-limiting enzyme of cholesterol synthesis. Its dihydroxy acid chain mimics the HMG part of the substrate, and its polar sulfonamide group adds extra contacts in the pocket. Less cholesterol in the hepatocyte activates SREBP-2, which increases LDL receptors, so the liver clears more LDL from the blood.

Occupies the HMG-CoA pocket of HMG-CoA reductase
Liver cholesterol synthesis falls
SREBP-2 adds LDL receptors to liver cells
Blood LDL falls: fewer heart attacks and strokes

Pharmacokinetics

Absorption: Oral, with or without food, at any time of day.
Metabolism: Not extensively metabolized; about 10% appears as metabolite, formed mainly by CYP2C9. Taken up into the liver by OATP1B1.
Elimination: Mostly in feces.
Half-life: About 19 hours.

Indications

High LDL cholesterol and mixed dyslipidemia, and prevention in people at high cardiovascular risk Atherosclerosis and dyslipidaemia →
Familial hypercholesterolemia Familial hypercholesterolemia →
Secondary prevention after myocardial infarction (high-intensity statin) Myocardial Infarction (Heart Attack) →

Adverse effects

Common

Muscle aches (myalgia)
Headache, nausea, abdominal pain
Raised liver transaminases
Rises in HbA1c and fasting glucose

Contraindications

Acute liver failure or decompensated cirrhosis
Hypersensitivity to rosuvastatin or an excipient

Key interactions

Cyclosporine: Raises rosuvastatin levels markedly; the dose is restricted.
Gemfibrozil: Raises rosuvastatin levels and myopathy risk; the combination is avoided.
Aluminium and magnesium hydroxide antacids: Lower absorption; rosuvastatin is given at least 2 hours before the antacid.
Warfarin: Can raise the INR; it is checked when rosuvastatin is started or changed.

What is monitored

Lipid panel before starting and some weeks after
Liver enzymes at baseline and if symptoms appear
Creatine kinase if there are muscle symptoms
Urine and kidney function if proteinuria or hematuria is suspected

Administration and safety

Oral tablet once daily, at any time of day, with or without food; swallowed whole.
Separated from aluminium–magnesium antacids by at least 2 hours.
Lower starting doses are used in patients of Asian ancestry and in severe kidney impairment.

Nursing care

Before: lipid panel, liver enzymes, kidney function, list of interacting drugs.
Ask about muscle pain, weakness or dark urine, and report it promptly.
Teach that the benefit depends on taking it every day, alongside diet and exercise.
Ask about pregnancy plans.

Pregnancy and breastfeeding

Stopped when pregnancy is recognized; the label allows weighing continuation in a patient with very high cardiovascular risk. Not used while breastfeeding.

Test yourself

Think of the answer, then tap the question to see it.

Why is rosuvastatin less affected than simvastatin by CYP3A4 inhibitors such as clarithromycin?

Rosuvastatin is barely metabolized and not a CYP3A4 substrate; its interactions come mainly from transporters such as OATP1B1 (e.g., cyclosporine, gemfibrozil).

Which ancestry is associated with higher rosuvastatin exposure?

Asian ancestry: exposure is about twice that of White subjects, so lower starting doses are used.

Which kidney finding is listed in rosuvastatin's warnings?

Proteinuria and hematuria, mostly at the highest dose; the dose is reviewed if they persist.

Why can rosuvastatin be taken in the morning while simvastatin is usually taken at night?

Its half-life is long (about 19 hours), so the effect does not depend on the night-time peak of cholesterol synthesis.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Rosuvastatin: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); DailyMed - ROSUVASTATIN CALCIUM tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); COMPLEX OF THE CATALYTIC PORTION OF HUMAN HMG-COA REDUCTASE WITH ROSUVASTATIN (FORMALLY KNOWN AS ZD4522) (RCSB Protein Data Bank, 2001); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.