Rosuvastatin, or Crestor, is a medication that lowers cholesterol. Rosuvastatin belongs to a class of drugs called HMG-CoA reductase inhibitors (statins).[20] Other medicines in this class include atorvastatin, pravastatin, and simvastatin. These drugs are used to treat high cholesterol and prevent heart disease, strokes, and heart attacks.[20]
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How Rosuvastatin Works
Rosuvastatin and other medications in the statin class work at the liver's level to decrease cholesterol production.
Mechanism of Action
Statins selectively inhibit hydroxymethylglutaryl-CoA (HMG-CoA) reductase, which converts HMG-CoA to mevalonate during the synthesis of cholesterol.[24] They also inhibit the synthesis of other compounds in the cellular signaling proteins. They also have anti-inflammatory, antioxidant, antiproliferative, and immune system effects. They can stabilize cholesterol plaques that can form in arteries and keep platelets from sticking together and blocking arteries.[24]
By decreasing cholesterol synthesis, rosuvastatin can decrease LDL cholesterol levels. In addition, it also increases HDL cholesterol levels.[17] Rosuvastatin also lowers triglyceride levels by improving other cholesterol markers such as VLDL and apoC-III.[13]
Studies have shown that rosuvastatin can delay the progression of atherosclerosis and may also help prevent cardiovascular disease, even in people with low LDL levels.[5,6] A 2010 study published in the European Heart Journal showed a 54% reduction in heart attacks and a 48% reduction in stroke.[6]
Dosage and Administration
Rosuvastatin is a tablet that is taken orally (by mouth). Dosing ranges from 5mg to 40mg daily.
- In most people, dosing is usually started at 10 or 20 mg daily.[19] People with homozygous familial hypercholesterolemia are generally started on 20mg daily. People with very high cholesterol or a high risk for cardiovascular disease may be started on 40mg daily.[9]
- Rosuvastatin is approved by the Food and Drug Administration (FDA) to treat children aged 7 to 17 with homozygous familial hypercholesterolemia and children aged 8 to 17 with heterozygous familial hypercholesterolemia.[21] The maximum dose in children is 20mg daily.[9]
- People who have active liver disease should not use statin medications. People who have metabolic dysfunction associated with steatotic liver disease (MASLD) can be treated with statins, as can people with chronic liver disease who also have atherosclerotic cardiovascular disease.[24]
- People with severe kidney impairment who are not on dialysis should be started on 5mg and should not be put on more than 10mg. It is reasonable to consider a lower starting dose (5mg) in the Asian population.[19]
Effectiveness and Benefits
Multiple studies have confirmed the benefits of statin medications in both primary and secondary prevention of cardiovascular disease in people with high LDL or low HDL levels. Rosuvastatin appears to have the best results for lowering total cholesterol, LDL cholesterol, non-HDL cholesterol, and increasing HDL cholesterol.[11,12]
Studies have also shown that, in high doses, statin medications can slow or even stop the progression of atherosclerosis.
- The JUPITER study also demonstrated a decreased risk of developing deep venous thrombosis or pulmonary embolism by 43%.[13] The JUPITER study was also the first study of statin medications that showed benefits in several subgroups, including women, Blacks, Hispanics, and the elderly.[13]
Rosuvastatin Side Effects and Safety
Some of the common (occurring in at least 1% of people) side effects of rosuvastatin include [9, 14,16,17]:
- Nausea (2%)
- Headaches (4%)
- Abdominal pain (3%)
- Fatigue (2%)
- Dizziness (1-2%)
- Constipation
- Proteinuria (3%)
- Muscle aches (3-6%)
Muscle aches can be benign but may also be a sign of more severe side effects. One of the mechanisms believed to cause muscle pain is calcium leaking from within cells. The calcium leak may damage muscle cells. The leaking is spontaneous and irregular, and researchers believe that most people’s muscle cells can tolerate it without damage.[7]
Serious Side Effects
Rosuvastatin can also cause potentially serious side effects. While these side effects are rare, they can be severe and even life-threatening.
These include [27]:
- Rhabdomyolysis
- Liver damage
- Kidney damage
- Pancreatitis
- Erythema multiforme
- Myasthenia gravis
Serious side effects may be more common in people who are over age 65 or who have underlying kidney or liver disease.[18]
Managing and Minimizing Side Effects
Monitoring for and managing potential side effects often involves laboratory (blood) testing. For example:
- Liver function tests (LFT) help assess for liver damage. LFT elevation occurs in 1-3% of patients using rosuvastatin.[12] Usually, the elevation is mild and doesn’t require any treatment or dose adjustment.
- Liver function should be tested before rosuvastatin therapy is started and should be repeated as clinically indicated.[12] If ALT levels rise above 10-fold in someone without symptoms or 5-fold in someone with symptoms, the medication should be stopped. Symptoms usually resolve in 1-2 months.[12]
You can minimize side effects of rosuvastin by:
- Eating meals that aren’t rich or spicy may help with nausea.
- Staying well hydrated can help reduce kidney side effects and headaches.
- Eating and drinking slowly and resting if you feel tired or dizzy may help offset some side effects.
- Increasing fiber and minimizing alcohol use is also recommended.[27]
Seek urgent medical evaluation for any of the following: [27]
- Severe muscle pain, tenderness, or weakness
- Yellowing of skin or eyes
- Severe abdominal pain
- Double vision, drooping eyelids, weakness after activity
- Pink-red rash on palms of hands or soles of feet
- Cough with shortness of breath and weight loss
- Difficulty swallowing
Special Considerations and Contraindications
Patients with certain conditions should avoid rosuvastatin. For example:
- Liver disease: Rosuvastatin is not recommended in people with active liver disease. It may be used in people with chronic liver disease with regular monitoring. Statin therapy, including rosuvastatin, shouldn’t be used in people with a severe allergy to the medications.[24]
- Pregnancy: All statin medications are currently contraindicated during pregnancy and while breastfeeding. In scarce circumstances, the healthcare team may recommend continuing statin medications during pregnancy, but generally, treatment of hyperlipidemia is not necessary during pregnancy. [14, 16]
Interactions with Other Medications
Rosuvastatin should be used cautiously and under the care of a healthcare provider by patients who are taking medications such as: [7,10]
- Anti-viral medications such as sofosbuvir/velpatasvir/voxilaprevir
- Ledipasvir/sofosbuvir
- Cyclosporine
- Darolutamide
- Gemfibrozil
- Regorafenib
- Warfarin (coumadin)
- Other lipid-lowering agents
Monitoring and Follow-Up
Routine monitoring of liver function and lipid profiles can help ensure that treatment is effective and not causing harm to organs such as the liver. Current guidelines recommend checking:
- LFTs about 12 weeks after starting therapy and then at least annually after.
- Lipids at 6-8 weeks after starting therapy and then every 4-6 months.
- Creatinine kinase (CK) at baseline and if there are any symptoms of muscle pain.[8]
Rosuvastatin in Special Populations
Some populations require additional consideration for the initiation and monitoring of rosuvastatin.
Older Adults
The ACC/AHA 2018 guidelines recommend considering initiating statin therapy in adults over 75 years if they have diabetes for primary prevention of atherosclerotic cardiovascular disease. They also recommend continuing previously initiated statins in people over 75 because they are at the greatest risk for cardiovascular disease. Generally, the recommendation is to start with a lower dosage, less aggressive treatment.[16]
Patients with Chronic Conditions
- People with advanced kidney disease should be started on a lower dose of rosuvastatin and titrating with caution.
- Statins should be avoided in people with active liver disease. People with chronic liver disease can use statins, but they need to be monitored more closely.[25]
Pregnancy and Lactation
Rosuvastatin and other members of the statin class are contraindicated in pregnancy due to a concern about the medications interfering with the developing embryo.[10]
- In 2021, the FDA removed the pregnancy category X label from the statin medications due to growing data that statins may be safe during pregnancy and may have some benefit for certain people with high-risk conditions. However, there is still a recommendation to discontinue statin treatment for most pregnant patients.[10]
Patient Education and Support
There is a lot of potentially confusing information out there on statin medications. Compliance with medications is vital to getting the best outcomes. Patient education and support play a vital role in ensuring compliance with medication.
Understanding the Risks and Benefits
One way to help patients understand the impact of statin medications on their health is to use a risk calculator to better demonstrate risks specific to their health status.
- The ASCVD risk calculator is one such tool. This tool estimates risk based on age, sex, race, blood pressure, cholesterol levels, medications, and risk factors such as history of diabetes and smoking status.[27]
Addressing Patient Concerns
Statins are used as long-term therapies. Patients may often have concerns about any medication that is used long-term. Multiple studies have shown that the benefits of statin medications outweigh the risks in most patients.
Preparing patients for the possible side effects of medications and discussing strategies for managing the side effects, as well as the warning signs for serious complications, can help patients feel empowered if they encounter any issues or side effects.
Lifestyle and Medication Adherence
Cholesterol medications work best in combination with diet and exercise. A heart-healthy diet limits your saturated and trans fats while using healthier oils. The American Heart Association also recommends at least 150 minutes of moderate-intensity aerobic exercise to lower blood pressure and cholesterol.[15]
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Key Takeaways
Rosuvastatin is an effective medication for lowering cholesterol and decreasing the risk of cardiovascular disease.
- Doses start at 5mg but may be higher if high-risk.
- Regular monitoring of liver function and cholesterol helps to catch side effects early and to ensure effectiveness.
- Statins are contraindicated in pregnancy and breastfeeding, but the data is changing.
- Statins are long-term therapy that works best with diet and exercise
- Statins work best with lifestyle modifications
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On December 11th, join Dr. Terry Wahls in a 
