Rosuvastatin
A statin with strong uptake into the liver, used to lower LDL cholesterol and triglycerides and to prevent heart attack and stroke.
Drug card
- Class
- Statin
- How it works
- Blocking HMG-CoA reductase, so the liver makes less cholesterol
- Used for
- High LDL cholesterol, including familial forms
- Lowering heart attack and stroke risk in at-risk adults
- High triglycerides (with diet)
- Known for
- Muscle aches (myalgia)
- Myopathy and rhabdomyolysis
- Its name
- -vastatin means a statin (HMG-CoA reductase inhibitor)
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does rosuvastatin work?
A selective, competitive HMG-CoA reductase inhibitor that is taken up readily by the liver, its target organ. It adds hepatic LDL receptors and cuts the liver's VLDL output, so fewer VLDL and LDL particles circulate. Only about 10% is metabolized, mostly by CYP2C9; its half-life is about 19 hours.
Like other statins: Statins competitively inhibit HMG-CoA reductase, the enzyme that sets the pace of cholesterol synthesis by turning HMG-CoA into mevalonate. Short of cholesterol, liver cells put more LDL receptors on their surface and take up more LDL from the blood, and the liver releases less VLDL. Plasma LDL cholesterol falls, and with it the risk of heart attack and stroke.
Uses
What is rosuvastatin used for?
- High LDL cholesterol, including familial forms
- Lowering heart attack and stroke risk in at-risk adults
- High triglycerides (with diet)
Side effects
Side effects of rosuvastatin
- Muscle aches (myalgia)Known for
- Myopathy and rhabdomyolysisKnown forSerious
- Immune-mediated necrotizing myopathy (rare)Serious
- Raised liver enzymes, rarely liver failureSerious
- Protein and blood in the urine
- Higher blood sugar and HbA1c
- Headache
- Nausea
- Constipation
- Weakness and tiredness (asthenia)
- Abdominal pain
- Rash, itching, hives or angioedema
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Asian patients reach about twice the blood levels and may have more myopathy, so treatment starts at the lowest dose.
- Cyclosporine, darolutamide, regorafenib, gemfibrozil and several HIV and hepatitis C antivirals raise its levels: limit the dose or avoid.
- With warfarin it can raise the INR: check the INR before starting and until it is stable.
- Contraindicated in acute liver failure or decompensated cirrhosis; stop it in pregnancy and avoid breastfeeding.
Good to know: Barely metabolized and long-acting; people of Asian descent, including South Asians, reach about double the exposure, so lower starting doses are used.
Remember it
A way to remember it
Statins shut the cholesterol factory, and the liver goes shopping for LDL.
With HMG-CoA reductase blocked, liver cells make less cholesterol and add LDL receptors to pull LDL out of the blood. The harms to watch for are in the muscles (myalgia, rhabdomyolysis) and the liver.
Written for biofideX
Its name
-vastatin means statin (HMG-CoA reductase inhibitor)
Atorvastatin, simvastatin, rosuvastatin and pravastatin block HMG-CoA reductase. WHO files the stem under -stat (enzyme inhibitors); nystatin, an antifungal, is not a statin.
- Every drug name stem
Its class
Statins
Other statins with a card:
Easily mixed up with fibrates and cholesterol absorption inhibitors.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
- Rosuvastatin calcium tablets: label (DailyMed)
- Rosuvastatin tablets: label (DailyMed)
- Rosuvastatin (NCI Thesaurus)
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Blood clots and cholesterol
Rosuvastatin is one of 19 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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