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). 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
• Administration: Oral, once daily
• Mechanism: Selective and competitive inhibition of HMG-CoA reductase
• Bioavailability: Approximately 20%
• Half-life: ~19 hours
• Excretion: Primarily fecal (90%), with minimal renal excretion
• Special formulations: Not available as chewable or liquid; tablets must be swallowed whole

Benefits

• Significantly reduces LDL cholesterol levels by up to 52–63% at maximum doses
• Lowers triglyceride levels and increases HDL cholesterol, improving overall lipid profile
• Reduces 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 tolerability
• Supported by a substantial body of clinical evidence, including the JUPITER trial, demonstrating cardiovascular risk reduction in selected populations

Common use

Crestor is commonly prescribed for the treatment of primary hyperlipidemia and mixed dyslipidemia in adults who have not achieved target lipid levels through diet and exercise alone. It is also used to reduce the risk of cardiovascular events—such as heart attack and stroke—in adults without clinically evident coronary heart disease but with increased risk factors, including elevated CRP levels. Additionally, it is indicated to slow the progression of atherosclerosis in adult patients. Pediatric use is approved for children aged 8 years and older with heterozygous familial hypercholesterolemia, following appropriate diagnostic confirmation.

Dosage and direction

The recommended starting dose for most patients is 10 mg or 20 mg taken orally once daily, with or without food. Dosage should be individualized based on LDL cholesterol levels, goal of therapy, and patient response. For patients requiring aggressive LDL reduction, a 40 mg dose may be used, but caution is advised due to increased risk of side effects. For Asian patients or those with predisposing factors for myopathy, a 5 mg starting dose is recommended. Administration time is flexible but should be consistent each day. Tablets must be swallowed whole and not crushed or split. Regular lipid level monitoring is necessary to assess efficacy and guide dosage adjustments.

Precautions

Before initiating Crestor, assess liver function tests, as unexplained persistent elevations may necessitate discontinuation. Patients should be advised to report unexplained muscle pain, tenderness, or weakness promptly, as these may be signs of myopathy or rhabdomyolysis. Use with caution in patients with renal impairment, particularly those with severe disease (CrCl <30 mL/min), for whom the 10 mg dose should not be exceeded. Crestor may cause elevated HbA1c and fasting serum glucose levels. Avoid excessive alcohol consumption. Patients should be informed that Crestor is not a substitute for a controlled diet or exercise regimen.

Contraindications

Crestor is contraindicated in patients with a known hypersensitivity to rosuvastatin or any component of the formulation. It is also contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases. Pregnancy and breastfeeding are absolute contraindications, as statins may cause fetal harm and are excreted in human milk. Concomitant use with cyclosporine is prohibited.

Possible side effect

Common side effects include headache, myalgia, abdominal pain, nausea, and constipation. Less frequently, patients may experience dizziness, insomnia, or rash. Serious side effects, though rare, include rhabdomyolysis with renal dysfunction, hepatotoxicity, immune-mediated necrotizing myopathy, and increased HbA1c levels. Pancreatitis and arthralgia have also been reported. Patients should seek immediate medical attention for symptoms of myopathy (unexplained muscle pain or weakness, especially with fever or malaise) or signs of liver injury (fatigue, anorexia, right upper quadrant discomfort, dark urine, jaundice).

Drug interaction

Crestor interacts with several medications. Concomitant use with cyclosporine is contraindicated. Gemfibrozil and other fibrates significantly increase rosuvastatin exposure and myopathy risk—avoid combination if possible. Caution is advised with niacin, azole antifungals, macrolide antibiotics, and HIV protease inhibitors. Warfarin coadministration may prolong INR; monitor closely. Antacids containing aluminum and magnesium hydroxide decrease rosuvastatin absorption; administer at least 2 hours apart. Oral contraceptives may increase hormone levels.

Missed dose

If a dose is missed, take it as soon as remembered, unless it is nearly time for the next scheduled dose. Do not double the dose to make up for a missed one. Resume the regular dosing schedule the following day. Consistent daily administration is important for maintaining stable lipid-lowering effects.

Overdose

There is no specific antidote for rosuvastatin overdose. Suspected overdose should be managed with supportive measures, including monitoring of vital signs and clinical status. Consider activated charcoal if ingestion was recent. Hemodialysis is unlikely to be effective due to high protein binding. Monitor for signs of myopathy or renal failure, and provide symptomatic treatment as necessary.

Storage

Store Crestor tablets at room temperature (20–25°C or 68–77°F), in a dry place, protected from light and moisture. Keep the bottle tightly closed and out of reach of children and pets. Do not use after the expiration date printed on the packaging. Dispose of unused medication via a drug take-back program or according to local regulations.

Disclaimer

This information is intended for educational purposes and does not replace professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting or changing any medication regimen. Individual patient needs and responses may vary. Full prescribing information should be reviewed for comprehensive details, including boxed warnings.

Reviews

Clinical studies and meta-analyses consistently demonstrate Crestor’s efficacy in significantly reducing LDL cholesterol and cardiovascular events. The JUPITER trial showed a 44% reduction in major cardiovascular events among patients with elevated high-sensitivity C-reactive protein. Real-world evidence supports its tolerability and effectiveness, though adherence to monitoring recommendations is essential. Some patients report mild gastrointestinal discomfort or muscle aches, which often resolve with dose adjustment. Overall, it is regarded as a potent and reliable option in statin therapy.