Crestor: Advanced LDL Cholesterol Management for Cardiovascular Risk Reduction
Crestor
| Product dosage: 10mg | |||
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| Product dosage: 20mg | |||
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| Product dosage: 5mg | |||
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Synonyms | |||
Similar products
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 reducing low-density lipoprotein (LDL) and triglycerides while increasing high-density lipoprotein (HDL). Clinical evidence supports its efficacy in slowing atherosclerosis progression and reducing incidence of major cardiovascular events in appropriately indicated patients. This agent is indicated for use as an adjunct to diet and lifestyle modifications in adults and pediatric patients with heterozygous familial hypercholesterolemia.
Features
- Contains rosuvastatin calcium as active pharmaceutical ingredient
- Available in 5mg, 10mg, 20mg, and 40mg film-coated tablets
- Once-daily oral administration regimen
- Bioavailability of approximately 20%
- Maximum plasma concentration achieved within 3-5 hours post-administration
- Extensive hepatic metabolism primarily via CYP2C9 isoenzyme
- Elimination half-life of approximately 19 hours
Benefits
- Significantly reduces LDL cholesterol levels by 45-63% depending on dosage
- Lowers triglyceride levels by 10-28%
- Increases HDL cholesterol by 3-12%
- Reduces risk of myocardial infarction and stroke in high-risk populations
- Slows progression of coronary atherosclerosis
- May reduce need for revascularization procedures
Common use
Crestor is primarily prescribed for the treatment of dyslipidemia, including primary hypercholesterolemia and mixed dyslipidemia. It is indicated for adult patients who have not achieved target cholesterol levels through diet and exercise alone. Additionally, it is used as part of comprehensive risk reduction strategies in patients without clinically evident coronary heart disease but with multiple risk factors, including hypertension, low HDL-C, smoking, or family history of early coronary heart disease. Pediatric use (ages 8-17) is approved for heterozygous familial hypercholesterolemia after failure of adequate trial of diet therapy.
Dosage and direction
The recommended starting dose is 10-20 mg once daily, with dosage adjustments based on LDL-C goals and patient tolerance. For patients requiring aggressive LDL-C reduction (>45%), initial dose of 20-40 mg may be appropriate. Dosage should be individualized according to baseline LDL-C levels, goal of therapy, and patient response. Maximum recommended dose is 40 mg daily. Administration may occur at any time of day, with or without food. Regular monitoring of lipid levels should occur within 2-4 weeks after initiation or dosage adjustment.
Precautions
Liver function tests should be performed before initiation and periodically during therapy. Patients should report unexplained muscle pain, tenderness, or weakness promptly. Use with caution in patients consuming substantial quantities of alcohol or with history of liver disease. Blood glucose levels should be monitored as statins may increase HbA1c and fasting serum glucose levels. Not recommended during pregnancy or breastfeeding. Elderly patients may require dose adjustment due to decreased hepatic function.
Contraindications
Hypersensitivity to rosuvastatin or any component of formulation. Active liver disease or unexplained persistent elevations of serum transaminases. Pregnancy and lactation. Concomitant use with cyclosporine. Patients of Asian ancestry may require lower starting doses due to increased systemic exposure.
Possible side effect
Common adverse reactions (>2% incidence) include headache, myalgia, abdominal pain, nausea, and constipation. Less frequent effects include dizziness, insomnia, and rash. Serious but rare side effects include rhabdomyolysis with renal dysfunction, hepatic failure, and immune-mediated necrotizing myopathy. Increased incidence of diabetes mellitus has been observed in statin-treated patients. Cognitive impairment such as memory loss and confusion has been reported.
Drug interaction
Strong inhibitors of CYP2C9 (e.g., fluconazole) may increase rosuvastatin exposure. Concomitant use with gemfibrozil increases rosuvastatin exposure and risk of myopathy. Cyclosporine significantly increases rosuvastatin concentration. Antacids containing aluminum and magnesium hydroxide decrease rosuvastatin absorption. Warfarin coadministration may potentiate anticoagulant effect requiring INR monitoring. Oral contraceptives containing ethinyl estradiol and norgestrel may have increased AUC when coadministered.
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, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not take double or extra doses to make up for a missed dose. Consistency in daily administration is important for maintaining stable lipid control.
Overdose
There is no specific antidote for rosuvastatin overdose. Symptomatic and supportive measures should be implemented. Liver function and CPK levels should be monitored. Hemodialysis is unlikely to enhance elimination since rosuvastatin is extensively protein bound. Cases of overdose have reported symptoms including gastrointestinal disturbance, elevated transaminases, and myalgia.
Storage
Store at room temperature (20-25°C/68-77°F) with excursions permitted between 15-30°C (59-86°F). Keep container tightly closed and protect from moisture. Keep out of reach of children. Do not use after expiration date printed on packaging. Tablets should be kept in original blister packaging until administration.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Crestor is available by prescription only and should be used under appropriate medical supervision. Individual results may vary based on patient factors and adherence to treatment. Patients should consult their healthcare provider for personalized medical advice and before making any changes to their treatment regimen.
Reviews
Clinical trials demonstrate consistent efficacy in lipid parameter improvement across diverse patient populations. The JUPITER trial showed 44% reduction in major cardiovascular events in patients with elevated high-sensitivity C-reactive protein. Real-world evidence supports maintained efficacy in long-term use with generally favorable tolerability profile. Some patients report gastrointestinal discomfort during initial treatment phase, which typically resolves with continued use. Muscle-related symptoms remain the most commonly reported reason for discontinuation.