Rosuvastatin: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on July 25, 2023.

1. How it works

• Rosuvastatin may be used to treat high cholesterol.
• Rosuvastatin works by blocking an enzyme in the liver known as HMG-CoA reductase that is responsible for the conversion of HMG-CoA to mevalonate, an important substance necessary for the synthesis of cholesterol and coenzyme Q10. Rosuvastatin also boosts the breakdown of lipids (this is the collective term for fats and cholesterol).
• Rosuvastatin belongs to the class of medicines known as statins. Rosuvastatin is also known as an HMG-CoA reductase inhibitor.

2. Upsides

• Rosuvastatin, in conjunction with dietary measures, is used to treat high lipid levels in people at increased risk of cardiovascular disease, if initial dietary measures fail to lower cholesterol.
• Used to treat primary hyperlipidemia or mixed dyslipidemia, hypertriglyceridemia, and some other lipid disorders.
• Also indicated in children aged 8 and older (heterozygous), or 7 or older (homozygous) with familial hypercholesterolemia (a genetic disorder resulting in high cholesterol) in addition to dietary measures and sometimes other lipid-lowering agents. Rosuvastatin is also used to slow the progression of atherosclerosis in adult patients.
• Rosuvastatin may be used for primary prevention of cardiovascular disease, to lower the risk of coronary events (such as heart attack, stroke, and angina) in patients at high risk of these events (for example those people with pre-existing coronary heart disease; diabetes; peripheral vessel disease; a previous history of stroke and stroke-like events or heart attack; or with multiple risk factors such as older age, smoking, high blood pressure, low HDL-C, or a family history of heart disease).
• Does not interact with grapefruit juice or products to the same extent as atorvastatin.
• Generic rosuvastatin is available.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• A headache, abdominal pain, weakness, a lack of energy, constipation, or nausea.
• Muscle aches and pain, tenderness, or weakness. Initially, this needs further investigation to rule out more serious muscle effects (such as rhabdomyolysis - the destruction of muscle cells). People aged older than 65, taking certain medications (for example cyclosporine, itraconazole, HIV antivirals), who drink more than two alcoholic drinks per day, or with kidney disease appear more at risk of serious side effects.
• Cognitive effects (memory loss, forgetfulness, confusion) may occur with long-term use; however, these effects are usually reversible on discontinuation.
• Rosuvastatin, like other statins, may affect liver function, manifesting as changes in liver function tests or jaundice (yellowing of the skin) requiring dosage reduction or discontinuation.
• May also affect some diabetes markers (such as HbA1c or fasting glucose), may increase the risk of developing diabetes, and may not be suitable in those with liver or kidney disease. Transient dipstick-positive proteinuria and microscopic hematuria may also occur in rosuvastatin-treated patients.
• The dosage of rosuvastatin needs to be reduced in severe renal impairment (CL_CR < 30 mL/minute). Consider initiating treatment at lower dosages (5mg once daily) in Asian patients.
• May interact with other drugs including cyclosporine, gemfibrozil, warfarin, and protease inhibitors.
• May not be suitable for some people including those with active liver disease (including persistent, unexplained elevations of aminotransferases), in people who drink excessively, during pregnancy, lactation, or with a known hypersensitivity to rosuvastatin or statins.
• The safety of rosuvastatin has not been established in children less than eight years of age.
• Do not use rosuvastatin during pregnancy. Suppression of cholesterol biosynthesis may cause harm to a developing fetus. Discontinue immediately if pregnancy occurs and women of childbearing age should use adequate contraception. Women should not breastfeed while taking rosuvastatin.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Rosuvastatin is effective at lowering cholesterol; however, its use may be limited by side effects such as muscle pain. People of Asian descent may be more sensitive to the effects of rosuvastatin. Rosuvastatin does not interact with grapefruit juice or products to the same extent as atorvastatin.

5. Tips

• May be taken as a single dose daily, any time of the day, either with or without food.
• Do not take 2 doses of rosuvastatin within 12 hours of each other.
• Separate administration of rosuvastatin from antacids (give two hours apart).
• Consider temporarily withholding rosuvastatin and seeking urgent medical advice if you have any acute muscle pain or another condition that may increase your risk of serious muscle injury or kidney failure such as a severe infection, major surgery, trauma, uncontrolled seizures, severe electrolyte or metabolic disorders.
• Asian people may be particularly sensitive to rosuvastatin and require lower dosages.
• The dosage needs to be individualized but initially should start at 10-20 mg/day (Asian/pediatric patients: 5 mg/day) and be guided by the results of cholesterol tests taken 2 to 4 weeks later.
• Limit your alcohol intake and avoid drinking more than two glasses of alcohol per day while you are taking rosuvastatin.
• Seek urgent medical advice and consider temporarily withholding rosuvastatin if you develop any acute muscle pain or have another condition that may increase your risk of serious muscle injury or kidney failure such as a severe infection, major surgery, trauma, uncontrolled seizures, severe electrolyte or metabolic disorders.
• See your doctor straight away if you notice any yellowing of your skin or shortness of breath, unexplained cough, or general tiredness.
• Adhere to the TLC diet, designed by the National Cholesterol Education Program (NCEP), or a similar diet, while taking rosuvastatin.
• Rosuvastatin should not be taken during pregnancy or while breastfeeding. Ensure you use effective contraception while taking rosuvastatin if you are a woman of childbearing age and talk to your doctor if you intend to become pregnant before you become pregnant. Rosuvastatin should be stopped immediately if you become pregnant. Do not breastfeed while taking rosuvastatin.

6. Response and effectiveness

• Peak levels of rosuvastatin are seen within three to five hours of oral administration. However, it may take one to two weeks of regular dosing before improvements in your cholesterol level are seen, and up to four weeks before the maximal cholesterol-lowering effects of rosuvastatin are apparent.

7. Interactions

Medicines that interact with rosuvastatin may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with rosuvastatin. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with rosuvastatin include:

• amiodarone
• antacids containing magnesium or aluminum
• antifungals, such as itraconazole, ketoconazole, posaconazole, or voriconazole
• carbamazepine
• cimetidine
• clopidogrel
• colchicine (may enhance adverse muscle effects)
• digoxin
• dronedarone
• eltrombopag
• erythromycin
• ezetimibe
• fibric acid derivatives
• fusidic acid
• HCV protease inhibitors such as simeprevir
• HIV protease inhibitors such as ritonavir-boosted atazanavir or lopinavir/ritonavir
• niacin
• oral contraceptives
• other lipid-lowering drugs such as gemfibrozil and fenofibrate
• other strong CYP3A4 inhibitors, such as clarithromycin, cyclosporine, atazanavir, or ritonavir
• red yeast rice
• rifampin
• warfarin.

Note that this list is not all-inclusive and includes only common medications that may interact with rosuvastatin. You should refer to the prescribing information for rosuvastatin for a complete list of interactions.

References

• Rosuvastatin. Revised 07/2022. EMC PHARMA, LLC https://www.drugs.com/pro/rosuvastatin-tablets.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use rosuvastatin only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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