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, resulting in significant reductions in low-density lipoprotein (LDL) and triglycerides, alongside increases in high-density lipoprotein (HDL). Clinically validated through 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. Its efficacy and safety profile make it a cornerstone in modern lipid-management protocols.

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: None; standard film-coated tablets

Benefits

• Significantly lowers LDL cholesterol levels, with reductions observed within one week of initiation
• Increases HDL cholesterol, contributing to improved lipid ratios and cardiovascular risk profiles
• Reduces triglyceride levels, addressing a key component of atherogenic dyslipidemia
• Proven to slow the progression of atherosclerosis and stabilize plaque, lowering the risk of acute coronary events
• Demonstrates efficacy in diverse patient populations, including those with diabetes or metabolic syndrome
• Once-daily dosing supports adherence and long-term therapeutic consistency

Common use

Crestor is commonly prescribed for the treatment of primary hyperlipidemia and mixed dyslipidemia in adults. It is also used to reduce the risk of stroke, myocardial infarction, and arterial revascularization procedures in patients without clinically evident coronary heart disease but with increased risk factors such as age, hypertension, low HDL-C, or a family history of early heart disease. Additionally, it is indicated to slow the progression of atherosclerosis in adult patients as part of a comprehensive treatment strategy aimed at modifying lipid levels.

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-C levels, goal of therapy, and patient response. For patients with severe hypercholesterolemia or aggressive LDL-lowering targets, a 40 mg dose may be used. Dose adjustments are recommended for patients taking concomitant cyclosporine or for those with predisposing factors for myopathy. Asian patients may require a lower starting dose (5 mg) due to increased systemic exposure. Administration timing is flexible but should be consistent daily to maintain stable plasma concentrations.

Precautions

Patients should be advised to report unexplained muscle pain, tenderness, or weakness promptly, as these may be signs of myopathy or rhabdomyolysis. Liver enzyme tests should be performed before initiation and periodically thereafter. Use with caution in patients with a history of liver disease or heavy alcohol consumption. Blood glucose levels should be monitored, as statins may increase HbA1c and fasting serum glucose. Caution is advised in patients with renal impairment, particularly those with creatinine clearance <30 mL/min. Patients should be informed that Crestor is not a substitute for lifestyle changes, including diet and exercise.

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 due to potential risk to the fetus and infant. Concomitant use with cyclosporine is contraindicated.

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 and fasting serum glucose levels. Pancreatitis and arthralgia have also been reported in post-marketing experience. Patients should seek medical attention for symptoms such as dark urine, severe stomach pain, or yellowing of the skin or eyes.

Drug interaction

Crestor may interact with cyclosporine, gemfibrozil, and other fibrates, increasing the risk of myopathy. Concurrent use with niacin or other lipid-lowering agents may also elevate this risk. Antacids containing aluminum and magnesium hydroxide can decrease rosuvastatin absorption; administration should be separated by at least 2 hours. Warfarin may require monitoring for increased INR. Protease inhibitors and certain immunosuppressants may increase rosuvastatin exposure. Clinicians should review all concomitant medications before prescribing.

Missed dose

If a dose is missed, it should be taken as soon as remembered, unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped, and the regular dosing schedule resumed. Doubling the dose to make up for a missed one is not recommended.

Overdose

There is no specific antidote for rosuvastatin overdose. Treatment should be supportive and symptomatic. Hemodialysis is unlikely to be effective due to high protein binding. Liver function and CK levels should be monitored, and general measures to prevent dehydration and renal impairment should be instituted if rhabdomyolysis is suspected.

Storage

Store at room temperature (20–25°C or 68–77°F), in a dry place, away from light and moisture. Keep the container tightly closed and out of reach of children. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Do not disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

Clinical studies and patient reports consistently affirm the efficacy of Crestor in achieving significant LDL-C reductions. In the JUPITER trial, rosuvastatin demonstrated a 44% reduction in major cardiovascular events among patients with elevated high-sensitivity C-reactive protein. Many patients note improved lipid profiles within weeks, though some report mild myalgia. Adherence is generally high due to once-daily dosing. Physician reviews often highlight its potency and reliability in high-risk and primary prevention settings.