Drug Detail:Crestor (Rosuvastatin [ roe-soo-va-sta-tin ])
Drug Class: Statins
1. How it works
- Crestor is a brand (trade) name for rosuvastatin which may be used to treat high cholesterol.
- Crestor (rosuvastatin) works by blocking an enzyme, called HMG-CoA reductase, in the liver that makes different types of lipids (this is the collective term for fats and cholesterol). Rosuvastatin also boosts the breakdown of lipids.
- Crestor belongs to the class of medicines known as statins. Crestor is also known as an HMG-CoA reductase inhibitor.
2. Upsides
- Crestor, 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, primary dysbetalipoproteinemia, hypertriglyceridemia, and some other lipid disorders.
- Also indicated in adults and 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.
- Crestor is also used to slow the progression of atherosclerosis in adult patients.
- Reduces Total-C, LDL-C, ApoB, nonHDL-C, and triglycerides and increases HDL-C.
- Crestor may also be used to lower the risk of coronary events (including heart attack, stroke, and angina) in patients at high risk of these events - such as 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, family history of heart disease).
- Can be taken at any time of the day. Administered as a single dose.
- May be administered with or without food.
- Available in four strengths: 5mg, 10mg, 20mg, and 40mg.
- Grapefruit products or juice have little effect on blood levels of Crestor.
- Crestor is available as a generic under the name rosuvastatin.
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:
- Muscle pain, tenderness, or weakness - initially 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, gemfibrozil, HIV antivirals), who drink more than two alcoholic drinks per day, or with kidney disease, appear more at risk of serious side effects.
- Rarely, has been associated with memory loss, forgetfulness, amnesia, memory impairment, and confusion. These symptoms typically resolve with discontinuation.
- Abdominal pain, nausea, headache, lack of energy, dizziness, and constipation are also common.
- Hypersensitivity reactions have also been reported, including rash, pruritus, urticaria, and angioedema. Has been associated with immune-mediated necrotizing myopathy (IMNM) which is characterized by muscle weakness and elevated serum creatine kinase. Treatment with immunosuppressive agents may be needed.
- May interact with other drugs including cyclosporine, gemfibrozil, warfarin, and protease inhibitors.
- Crestor, 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. Liver function tests are recommended before starting therapy and at periodic intervals throughout therapy.
- May not be suitable for those with liver or kidney disease. Has not been studied in Fredrickson Type I and V dyslipidemia.
- Asian people may be particularly sensitive to Crestor and require lower dosages. For people with kidney disease initiate with 5 mg/day and do not exceed 10 mg/day.
- The dosage of Crestor 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.
- Only use the maximum dose of 40mg for those who have not achieved their LDL-C goal using the 20mg dose.
- The dosage may also need to be reduced for people taking interacting medications (see interactions).
- Requires monitoring of cholesterol levels at least initially, to determine effective dose.
- Proteinuria and hematuria have ben reported particularly with the 40mg dose. May also increase HbA1c and fasting glucose levels.
- Do not use Crestor during pregnancy. Women should not breastfeed while taking Crestor.
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. Tips
- May be taken as a single dose daily, any time of the day, either with or without food. It is best to be consistent with the time you take your tablets. Grapefruit juice or products do not appear to affect Crestor.
- Do not take 2 doses of Crestor within 12 hours of each other.
- Separate administration of Crestor from antacids (give two hours apart).
- Consider temporarily withholding Crestor 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.
- Eat healthily and stick to a heart-friendly diet, such as the TLC diet, designed by the National Cholesterol Education Program (NCEP), while taking Crestor. Plan to exercise regularly and stop smoking if you smoke. Try to avoid second-hand smoke.
- Report any unexplained fatigue, shortness of breath, unexplained cough, weight loss, abdominal pain, dark urine, or yellowing of the skin. Your doctor may wish to monitor your liver function regularly.
- Crestor should not be taken during pregnancy or while breastfeeding. Ensure you use effective contraception while taking Crestor if you are a woman of childbearing age and talk to your doctor if you intend to become pregnant before you become pregnant.
5. Response and effectiveness
- Peak levels 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 Crestor are apparent.
- Crestor appears as effective as atorvastatin and reduces LDL cholesterol levels by around 60%.
- Crestor and atorvastatin are more effective at lowering triglycerides than simvastatin or pravastatin. Crestor is more effective in raising HDL cholesterol (“good cholesterol”) than atorvastatin, simvastatin, or pravastatin.
6. Interactions
Medicines that interact with Crestor may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with Crestor. 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 Crestor include:
- amiodarone
- antacids containing magnesium or aluminum
- antifungals, such as itraconazole, ketoconazole, posaconazole, or voriconazole
- carbamazepine
- cimetidine
- clopidogrel
- colchicine (may enhance adverse muscle effects)
- cyclosporine or darolutamide: do not exceed 5mg daily
- fusidic acid
- HIV medications, such as combinations containing atazanavir, ritonavir, simeprevir, grazoprevir, sofosbuvir, and glecaprevir (initiate with 5 mg/day; do not exceed 10 mg/day)
- niacin
- other lipid-lowering drugs such as gemfibrozil (initiate with 5 mg/day; do not exceed 10 mg/day) and fenofibrate
- other strong CYP3A4 inhibitors, such as clarithromycin
- regorafenib (do not exceed 10 mg/day)
- warfarin and other coumarin anticoagulants (may cause prolongation of the prothrombin time/INR).
Note that this list is not all-inclusive and includes only common medications that may interact with Crestor. You should refer to the prescribing information for Crestor for a complete list of interactions.