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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
HMG-CoA Reductase Inhibitor [EPC]
Rosuvastatin is a high-potency HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and triglycerides while increasing HDL cholesterol to reduce cardiovascular risk.
Name
Rosuvastatin
Raw Name
ROSUVASTATIN CALCIUM
Category
HMG-CoA Reductase Inhibitor [EPC]
Salt Form
Calcium
Drug Count
5
Variant Count
267
Last Verified
February 17, 2026
RxCUI
859751, 859419, 859424, 859747, 859421, 859426, 859749, 859753, 2167557, 2167563, 2167565, 2167567, 2167569, 2167571, 2167573, 2167575
UNII
83MVU38M7Q, 413KH5ZJ73
About Rosuvastatin
Rosuvastatin is a high-potency HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and triglycerides while increasing HDL cholesterol to reduce cardiovascular risk.
Detailed information about Rosuvastatin
This page is for informational purposes only and does not replace medical advice. Consult a qualified healthcare professional before using any medication containing Rosuvastatin.
Clinically, Rosuvastatin is used to manage primary hyperlipidemia and mixed dyslipidemia, as well as to treat patients with hypertriglyceridemia (high triglycerides). It is also one of the few statins specifically indicated for the treatment of homozygous familial hypercholesterolemia (HoFH), a rare genetic condition characterized by extremely high cholesterol levels from birth. Beyond lipid management, Rosuvastatin plays a critical role in slowing the progression of atherosclerosis (the buildup of plaque in the arteries), which is a major contributor to heart attacks and strokes. Your healthcare provider may prescribe this medication if lifestyle modifications, such as diet and exercise, have not sufficiently lowered your cholesterol levels to target ranges.
To understand how Rosuvastatin works, one must look at the internal machinery of the liver, where the majority of the body's cholesterol is produced. Rosuvastatin works by competitively inhibiting an enzyme called 3-hydroxy-3-methylcholesteryl coenzyme A (HMG-CoA) reductase. This enzyme is the 'rate-limiting' step in the mevalonate pathway, which is the chemical sequence the body uses to synthesize cholesterol. By blocking this enzyme, Rosuvastatin significantly reduces the amount of cholesterol produced within the liver cells (hepatocytes).
However, the reduction in production is only half of the story. When the liver senses that its internal cholesterol levels are low, it responds by increasing the number of LDL receptors on the surface of the liver cells. These receptors act like 'magnets' that pull LDL cholesterol out of the bloodstream and into the liver for processing and elimination. This dual action—decreasing production and increasing clearance from the blood—results in a dramatic drop in circulating LDL-C levels. Furthermore, Rosuvastatin inhibits the hepatic synthesis of Very-Low-Density Lipoprotein (VLDL), which leads to a subsequent reduction in triglycerides. Clinical studies, such as the JUPITER trial (Justification for the Use of Statins in Prevention: an Intervention Trial Evaluating Rosuvastatin, 2008), have demonstrated that Rosuvastatin not only lowers lipids but also reduces markers of systemic inflammation, such as C-reactive protein (CRP), which is independently linked to cardiovascular risk.
Understanding how the body processes Rosuvastatin is essential for optimizing its therapeutic effect and minimizing risks. Unlike some other statins (like simvastatin or lovastatin), Rosuvastatin is relatively hydrophilic (water-soluble), which influences how it moves through the body.
Rosuvastatin is FDA-approved for several specific clinical indications, all aimed at improving lipid profiles and reducing cardiovascular morbidity and mortality:
Rosuvastatin is primarily available in oral solid dosage forms to ensure consistent delivery and patient compliance. The most common forms include:
> Important: Only your healthcare provider can determine if Rosuvastatin is right for your specific condition. They will evaluate your lipid panel, overall cardiovascular risk, and medical history to decide the appropriate starting dose and monitoring schedule.
The dosage of Rosuvastatin must be individualized based on the patient's specific goals for cholesterol reduction and their overall risk for cardiovascular events. According to standard clinical guidelines (AHA/ACC), the typical adult dosage range is 5 mg to 40 mg once daily.
Rosuvastatin is approved for use in pediatric patients with heterozygous familial hypercholesterolemia (HeFH).
For patients with mild to moderate kidney disease, no dose adjustment is usually necessary. However, for patients with severe renal impairment (Creatinine Clearance < 30 mL/min) who are not on dialysis, the starting dose should be 5 mg once daily, and the total dose should not exceed 10 mg once daily. This is because the kidneys play a role in the elimination of the drug, and accumulation can increase the risk of toxicity.
Rosuvastatin is contraindicated in patients with active liver disease or unexplained, persistent elevations in liver enzymes (transaminases). In patients with chronic liver disease (Child-Pugh scores 8 or 9), increased systemic exposure has been observed, requiring cautious dosing and frequent monitoring.
Patients aged 65 and older may be more susceptible to muscle-related side effects. While no specific starting dose adjustment is mandated by age alone, healthcare providers often start at the lower end of the dosing spectrum (5-10 mg) and monitor these patients closely.
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose (within 12 hours), skip the missed dose and resume your regular schedule. Never take two doses at once to make up for a missed one, as this increases the risk of side effects.
There is no specific antidote for Rosuvastatin overdose. In the event of an accidental overdose, contact your local poison control center or seek emergency medical attention immediately. Treatment is generally supportive, focusing on maintaining vital functions and monitoring liver and muscle enzyme levels (Creatine Phosphokinase or CPK).
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking the medication without medical guidance, as your cholesterol levels may rise quickly once the drug is discontinued.
Most patients tolerate Rosuvastatin well, but like all medications, it can cause side effects. Common side effects are generally mild and often diminish as the body adjusts to the medication. These may include:
> Warning: Stop taking Rosuvastatin and call your doctor immediately if you experience any of the following serious symptoms:
With prolonged use over years, the primary concern remains the management of blood glucose levels and the monitoring of liver health. Long-term studies, such as those following the JUPITER cohort, suggest that the benefits of preventing major adverse cardiovascular events (MACE) like heart attacks far outweigh the risks of long-term side effects for the majority of patients. Some patients may develop chronic, mild muscle aches that require a dose adjustment or a switch to an alternative statin.
No FDA black box warnings currently exist for Rosuvastatin. However, the FDA does require prominent warnings regarding the risk of myopathy and rhabdomyolysis, particularly at the highest dose (40 mg) and in specific populations like the elderly or those with renal impairment.
Report any unusual symptoms to your healthcare provider. They may perform blood tests to check your liver enzymes or muscle enzymes (CPK) to ensure the medication is safe for you to continue.
Rosuvastatin is a powerful medication that requires careful medical supervision. It is not suitable for everyone, particularly those with active liver disease or those who are pregnant. Patients must be aware that while Rosuvastatin significantly reduces the risk of heart disease, it must be used in conjunction with a heart-healthy diet and regular physical activity for maximum benefit.
As of the 2026 clinical updates, there are no FDA black box warnings for Rosuvastatin. It is considered to have a well-established safety profile when used according to the prescribing information.
To ensure the safe use of Rosuvastatin, your healthcare provider will likely order the following tests:
Rosuvastatin generally does not interfere with the ability to drive or operate heavy machinery. However, some patients experience dizziness or fatigue. If you feel dizzy or unwell, avoid these activities until you know how the medication affects you.
Excessive alcohol consumption can increase the risk of liver damage and may also raise triglyceride levels, counteracting the benefits of the medication. While a moderate drink is usually acceptable, patients who drink heavily or have a history of alcohol abuse should discuss this with their doctor, as they are at a higher risk for statin-induced liver injury.
Do not stop taking Rosuvastatin abruptly unless directed by a doctor. Stopping the medication will cause your cholesterol levels to return to their previous high levels within a few weeks. There is no 'withdrawal syndrome' associated with statins, but the cardiovascular protection the drug provides will cease once it is discontinued.
> Important: Discuss all your medical conditions, including any history of liver or kidney disease, thyroid problems, or alcohol use, with your healthcare provider before starting Rosuvastatin.
Certain medications significantly increase the concentration of Rosuvastatin in the blood, drastically raising the risk of rhabdomyolysis. These should not be used together:
Rosuvastatin may cause a false-positive result on certain urine protein tests (dipstick testing). It does not typically interfere with other standard laboratory tests, but always inform your lab technician that you are taking a statin.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. A comprehensive review of your 'medication list' is the best way to prevent dangerous interactions.
There are several scenarios where Rosuvastatin must never be used because the risks clearly outweigh any potential benefits:
These are conditions that require a careful risk-benefit analysis by a healthcare provider:
Patients who have had an allergic reaction to other statins (like atorvastatin, simvastatin, or pravastatin) may have a higher risk of reacting to Rosuvastatin. While they are chemically different, they share similar structural components. Always inform your doctor of any previous adverse reactions to lipid-lowering drugs.
> Important: Your healthcare provider will evaluate your complete medical history, including liver health and pregnancy status, before prescribing Rosuvastatin.
Rosuvastatin is generally avoided during pregnancy. Historically, the FDA classified statins as Category X. While the FDA has recently updated its labeling to allow for individualized risk-benefit assessments (especially for extremely high-risk patients with HoFH), the standard clinical practice is to discontinue Rosuvastatin as soon as pregnancy is recognized. Cholesterol and other products of the cholesterol biosynthesis pathway are essential for fetal development, including the formation of cell membranes and hormones. Animal studies have shown that exposure to statins can lead to structural abnormalities in the fetus.
Due to the potential for serious adverse reactions in a nursing infant, such as interference with the infant's lipid metabolism, breastfeeding is not recommended while taking Rosuvastatin. If the medication is essential for the mother's health, an alternative method of infant feeding should be used.
Rosuvastatin is approved for children aged 7 to 17 years with heterozygous familial hypercholesterolemia. Clinical trials have shown that it is effective in lowering LDL-C in this population and does not appear to adversely affect growth, weight, or sexual maturation. However, it is not approved for children under 7, and its use in pediatric patients must be managed by a specialist in pediatric lipidology.
Patients aged 65 and older represent a significant portion of Rosuvastatin users. While the drug is effective in the elderly, this population is at an increased risk for myopathy and rhabdomyolysis. This risk is often compounded by the presence of other conditions (comorbidities) like kidney disease or the use of multiple other medications (polypharmacy). Healthcare providers often use a 'start low, go slow' approach with dosing in geriatric patients.
In patients with mild to moderate renal impairment, no dose adjustment is necessary. However, in patients with severe renal impairment (CrCl < 30 mL/min), the plasma concentration of Rosuvastatin can be three times higher than in those with normal kidney function. For these patients, the starting dose is 5 mg, and the maximum dose is 10 mg. Rosuvastatin is not significantly removed by hemodialysis.
Rosuvastatin should not be used in patients with active liver disease. In patients with chronic liver disease, particularly those with Child-Pugh scores of 8 or 9, systemic drug exposure is increased. These patients require very careful monitoring of liver enzymes and muscle symptoms.
> Important: Special populations require individualized medical assessment to ensure the benefits of Rosuvastatin therapy outweigh any potential risks.
Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol. The primary site of action for Rosuvastatin is the liver, the target organ for cholesterol lowering. By inhibiting this enzyme, Rosuvastatin reduces the hepatic synthesis of cholesterol. This intracellular depletion of cholesterol triggers an up-regulation of high-affinity LDL receptors on the surface of hepatocytes, which increases the uptake and catabolism of circulating LDL cholesterol. Additionally, Rosuvastatin inhibits the hepatic synthesis of VLDL, thereby reducing the total number of VLDL and LDL particles in the blood.
Rosuvastatin produces a dose-related reduction in LDL-C, Total-C, and triglycerides. A therapeutic response is typically evident within 1 week of starting therapy, and the maximum response is usually achieved within 4 weeks. The effect is maintained during long-term administration. There is no evidence of 'tachyphylaxis' (tolerance) developing over time. Beyond its lipid effects, Rosuvastatin has 'pleiotropic' effects, which include improving endothelial function, stabilizing atherosclerotic plaques, and reducing oxidative stress and inflammation.
| Parameter | Value |
|---|---|
| Bioavailability | ~20% |
| Protein Binding | ~88% (primarily albumin) |
| Half-life | ~19 hours |
| Tmax | 3 to 5 hours |
| Metabolism | Minimal (~10%), primarily CYP2C9 |
| Excretion | Fecal 90%, Renal 10% |
Rosuvastatin belongs to the HMG-CoA Reductase Inhibitor [EPC] class. It is categorized as a 'statin.' Other medications in this class include atorvastatin (Lipitor), simvastatin (Zocor), and pravastatin (Pravachol). Rosuvastatin and Atorvastatin are the only two statins currently classified as 'high-intensity' at their upper dosage ranges.
Medications containing this ingredient
Common questions about Rosuvastatin
Rosuvastatin is primarily used to lower high levels of 'bad' cholesterol (LDL) and triglycerides in the blood, while simultaneously increasing 'good' cholesterol (HDL). It belongs to the statin class of drugs and is often prescribed to patients with hyperlipidemia or mixed dyslipidemia when diet and exercise alone are not enough. Additionally, it is used to slow the progression of atherosclerosis, which is the buildup of fatty plaques in the arteries. Healthcare providers also prescribe it for the primary prevention of heart attacks and strokes in individuals who have high risk factors but no current heart disease. It is considered a high-potency statin, meaning it can achieve significant results at lower doses than many other medications.
The most common side effects of Rosuvastatin include muscle aches (myalgia), headaches, nausea, and a general feeling of weakness or tiredness (asthenia). Some patients may also experience stomach pain or constipation as their body adjusts to the medication. While these symptoms are usually mild, it is important to report any persistent or worsening muscle pain to your doctor, as it can occasionally signal a more serious issue. In some cases, a slight increase in blood sugar levels may occur, which your doctor will monitor through regular blood tests. Most side effects are manageable and do not require stopping the medication, but always consult your healthcare provider before making changes.
Moderate alcohol consumption is generally considered safe for most people taking Rosuvastatin, but heavy or chronic drinking should be avoided. Because both Rosuvastatin and alcohol are processed by the liver, excessive alcohol use can increase the risk of liver damage or inflammation. Furthermore, alcohol can raise triglyceride levels, which may counteract the cholesterol-lowering benefits of the medication. If you have a history of liver disease or heavy alcohol use, your doctor may choose a different medication or monitor your liver enzymes more frequently. It is best to discuss your specific alcohol consumption habits with your healthcare provider to ensure your safety.
Rosuvastatin is generally not recommended during pregnancy and is often contraindicated because cholesterol is essential for the healthy development of a fetus. If you are planning to become pregnant or find out that you are pregnant, you should stop taking the medication and contact your healthcare provider immediately. Research suggests that inhibiting cholesterol production during pregnancy could lead to birth defects or other developmental issues. While the FDA has recently allowed for some flexibility in high-risk cases, the standard clinical protocol is to avoid statins during pregnancy and breastfeeding. Your doctor will help you manage your cholesterol through diet or other safer methods during this time.
Rosuvastatin begins to lower your cholesterol levels fairly quickly, with initial changes typically seen within one to two weeks of starting the medication. However, it usually takes about four weeks of consistent daily use to reach the full therapeutic effect and see the maximum reduction in your LDL cholesterol. Your doctor will likely schedule a follow-up blood test (lipid panel) four to twelve weeks after you start the drug to check your progress. It is important to continue taking the medication even if you feel fine, as high cholesterol does not usually have noticeable symptoms. Consistency is key to maintaining the protective cardiovascular benefits of the drug.
You should not stop taking Rosuvastatin suddenly without first consulting your healthcare provider. While stopping the medication does not cause physical withdrawal symptoms, your cholesterol levels will likely return to their previous high levels within a few weeks, increasing your risk of heart attack or stroke. If you are concerned about side effects, your doctor can often adjust your dose or switch you to a different type of statin that you might tolerate better. Statins are typically intended for long-term use to provide ongoing protection for your arteries. Always have a discussion with your medical team before discontinuing any chronic medication.
If you miss a dose of Rosuvastatin, take it as soon as you remember. However, if your next scheduled dose is less than 12 hours away, you should skip the missed dose and simply take your next one at the usual time. Do not take two doses at once to make up for the one you missed, as this can increase the risk of side effects like muscle pain or liver irritation. Because Rosuvastatin has a long half-life, missing a single dose occasionally will not significantly impact your long-term cholesterol management. To help you remember, try taking your medication at the same time every day, such as with breakfast or before bed.
Weight gain is not a commonly reported side effect of Rosuvastatin in clinical trials. However, some studies have shown that statins can slightly increase the risk of developing Type 2 diabetes, which can be associated with changes in metabolism or weight in some individuals. If you notice a significant or unexplained increase in weight while taking this medication, it is important to discuss it with your doctor to rule out other causes. Maintaining a healthy diet and regular exercise routine is essential while on Rosuvastatin, both for weight management and for maximizing the drug's heart-health benefits. Your healthcare provider can help you monitor your weight and blood sugar levels during treatment.
Rosuvastatin can interact with several other medications, so it is vital to provide your doctor with a full list of everything you take, including supplements and over-the-counter drugs. Specific medications like cyclosporine, gemfibrozil, and certain HIV or Hepatitis C antivirals can significantly increase the levels of Rosuvastatin in your blood, raising the risk of muscle damage. Antacids containing aluminum or magnesium can also interfere with its absorption and should be taken at least two hours after your Rosuvastatin dose. While Rosuvastatin has fewer interactions than some other statins because it avoids the CYP3A4 pathway, careful monitoring is still required. Your pharmacist is an excellent resource for checking for potential drug interactions.
Yes, Rosuvastatin is widely available as a generic medication, which is typically much more affordable than the brand-name version, Crestor. Generic Rosuvastatin contains the same active ingredient and meets the same FDA standards for safety, strength, and quality as the brand-name drug. Most insurance plans cover the generic version, making it an accessible option for long-term cholesterol management. Whether you take the brand or the generic, the clinical effects and potential side effects remain the same. If you have questions about the cost or availability of the generic form, your pharmacist can provide the most current information for your area.