Crestor: Advanced LDL Cholesterol Reduction Therapy
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| Product dosage: 20mg | |||
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| Product dosage: 5mg | |||
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Synonyms | |||
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Crestor (rosuvastatin calcium) is a prescription medication classified as a statin, specifically designed to manage elevated cholesterol levels and associated cardiovascular risks. It functions by inhibiting HMG-CoA reductase, a key enzyme in the hepatic synthesis of cholesterol, thereby effectively reducing low-density lipoprotein (LDL) and triglycerides while increasing high-density lipoprotein (HDL). Clinically proven in extensive trials, Crestor is indicated for primary hyperlipidemia, mixed dyslipidemia, and as an adjunct to diet and lifestyle modifications. It is also approved for slowing the progression of atherosclerosis and reducing the risk of major cardiovascular events in appropriately selected patients. This agent represents a cornerstone in preventive cardiology, offering robust lipid-lowering efficacy with a well-characterized safety profile.
Features
- Active ingredient: Rosuvastatin calcium
- Available in tablet strengths: 5 mg, 10 mg, 20 mg, 40 mg
- Mechanism: Selective and competitive inhibition of HMG-CoA reductase
- Administration: Oral, once daily, with or without food
- Bioavailability: Approximately 20%
- Half-life: ~19 hours
- Excretion: Primarily fecal (90%), with minor renal elimination
- Special formulations: None; standard film-coated tablets
Benefits
- Significantly reduces LDL cholesterol levels, often by 45–55% at higher doses
- Lowers triglyceride concentrations and increases HDL cholesterol, improving overall lipid profile
- Demonstrates proven reduction in the risk of myocardial infarction, stroke, and arterial revascularization procedures
- Slows the progression of atherosclerosis, as evidenced by intravascular ultrasound studies
- Offers flexible dosing to accommodate individual patient response and tolerance
- Supported by a substantial body of clinical evidence including the JUPITER trial, highlighting cardiovascular event reduction in specific populations
Common use
Crestor is primarily prescribed for the management of dyslipidemias. It is used in adult patients with primary hyperlipidemia or mixed dyslipidemia to lower elevated total cholesterol, LDL cholesterol, apolipoprotein B, non-HDL cholesterol, and triglycerides. Additionally, it is indicated to increase HDL cholesterol. In patients without clinically evident coronary heart disease but with increased risk factors based on elevated high-sensitivity C-reactive protein and LDL levels, Crestor is employed to reduce the likelihood of myocardial infarction, stroke, and arterial revascularization. It is also used in pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia, as an adjunct to diet.
Dosage and direction
The recommended starting dose for most patients is 10 mg or 20 mg orally once daily. For patients requiring aggressive LDL cholesterol reduction (e.g., >45%), a 20 mg or 40 mg dose may be initiated. The 40 mg dose is reserved for patients who do not achieve goal LDL cholesterol with 20 mg and should be used with caution due to increased risk of adverse effects. Dosage should be individualized based on baseline LDL cholesterol levels, goal of therapy, and patient response. Administration can occur with or without food, at any time of day, though consistency is advised. Renal impairment necessitates caution: in patients with severe renal impairment (CrCl <30 mL/min/1.73m²) not on hemodialysis, the recommended starting dose is 5 mg, not to exceed 10 mg daily. For Asian patients, consider a 5 mg starting dose due to increased systemic exposure.
Precautions
Before initiating Crestor, perform a lipid panel and liver enzyme tests. Use with caution in patients who consume substantial quantities of alcohol or have a history of liver disease. Monitor liver enzymes before treatment initiation and as clinically indicated thereafter; discontinue if serum transaminase levels persist at >3 times the upper limit of normal. Assess renal function before and during treatment, especially in patients with predisposing factors for myopathy. Patients should be advised to report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. Crestor may increase HbA1c and fasting serum glucose levels. Pregnancy and breastfeeding are contraindicated due to potential fetal harm and excretion in breast milk.
Contraindications
Crestor is contraindicated in patients with hypersensitivity to rosuvastatin or any component of the formulation. It must not be used in patients with active liver disease or unexplained persistent elevations of serum transaminases. Use is contraindicated during pregnancy and in nursing mothers. Concomitant use with cyclosporine is prohibited.
Possible side effect
Common adverse reactions (incidence ≥2%) include headache, myalgia, abdominal pain, nausea, and constipation. Less frequently, dizziness, asthenia, and insomnia may occur. Important serious side effects include myopathy and rhabdomyolysis with acute renal failure, particularly at higher doses and in susceptible patients. Elevated liver enzymes occur in a small percentage of patients. Rare events include immune-mediated necrotizing myopathy, hepatitis, jaundice, and hypersensitivity reactions. Some patients may experience memory impairment or confusion, though typically reversible upon discontinuation.
Drug interaction
Crestor interacts with several medications that may increase the risk of myopathy or rhabdomyolysis. Avoid concomitant use with cyclosporine. Gemfibrozil significantly increases rosuvastatin exposure; combination should be avoided. Other fibrates and niacin (≥1 g/day) may increase risk of myopathy; use with caution and monitor closely. Antacids containing aluminum and magnesium hydroxide decrease rosuvastatin absorption; administer at least 2 hours apart. Protease inhibitors, particularly combinations used in HIV treatment, may increase statin concentration. Warfarin: Crestor may enhance anticoagulant effect; monitor INR closely. Use with caution alongside other drugs known to affect myopathy risk, such as colchicine.
Missed dose
If a dose is missed, it should be taken as soon as remembered, unless it is nearly time for the next scheduled dose. In that case, skip the missed dose and resume the usual dosing schedule. Do not double the dose to make up for a missed one.
Overdose
There is no specific antidote for rosuvastatin overdose. In the event of overdose, provide supportive treatment aimed at maintaining vital functions. Hemodialysis is unlikely to be beneficial due to high protein binding. Monitor for signs and symptoms of adverse reactions, particularly muscle pain or weakness, and manage symptomatically.
Storage
Store Crestor tablets at room temperature, between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C to 30°C (59°F to 86°F). Keep in the original container, tightly closed, and protect from moisture and light. Keep out of reach of children and pets.
Disclaimer
This information is for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider for personalized recommendations and before starting or changing any medication regimen. Do not disregard or delay seeking professional medical advice based on content herein.
Reviews
Clinical studies and post-marketing surveillance indicate that Crestor is generally well-tolerated and effective in reducing LDL cholesterol and cardiovascular risk. Many healthcare providers report satisfactory patient outcomes with appropriate dosing and monitoring. Some patients note mild gastrointestinal discomfort or muscle aches, which often resolve with time or dose adjustment. Overall, it is regarded as a potent and reliable option within the statin class, particularly for patients requiring significant LDL reduction. Long-term user experiences emphasize the importance of regular monitoring and adherence to lifestyle modifications for optimal results.