Crestor (rosuvastatin calcium) is a prescription medication classified as a statin (HMG-CoA reductase inhibitor), specifically formulated for the management of dyslipidemia. It represents a cornerstone in cardiovascular risk reduction strategies, working primarily in the liver to inhibit the production of cholesterol. This agent is indicated to elevate high-density lipoprotein (HDL) cholesterol, lower triglycerides, and significantly reduce elevated low-density lipoprotein (LDL) cholesterol and apolipoprotein B (Apo B) levels. Its robust efficacy profile makes it a first-line therapeutic option for patients requiring substantial lipid modification to mitigate the risk of atherosclerotic cardiovascular disease (ASCVD), including myocardial infarction and stroke. Clinical evidence supports its use in both primary and secondary prevention cohorts.

Features

• Active Pharmaceutical Ingredient (API): Rosuvastatin calcium.
• Standard Dosage Strengths: Available in 5 mg, 10 mg, 20 mg, and 40 mg film-coated tablets.
• Pharmacological Class: Selective and competitive inhibitor of HMG-CoA reductase.
• Mechanism of Action: Reduces cholesterol synthesis by acting on the rate-limiting step in the hepatic mevalonate pathway.
• Bioavailability: Approximately 20%.
• Time to Peak Plasma Concentration (Tmax): Reached within 3 to 5 hours post oral administration.
• Half-life: Approximately 19 hours.
• Primary Route of Elimination: Predominantly fecal (90%), with minimal renal excretion (10%).
• Pregnancy Category: X (Contraindicated in pregnancy).

Benefits

• Significant LDL-C Reduction: Demonstrates potent efficacy, often achieving greater than 50% reduction in LDL cholesterol levels at higher doses, one of the most substantial effects in the statin class.
• Atherosclerotic Cardiovascular Disease (ASCVD) Risk Reduction: Proven in large-scale clinical trials to slow the progression of atherosclerosis and reduce the incidence of major adverse cardiac events (MACE), including heart attack and stroke.
• HDL Cholesterol Increase: Moderately raises levels of “good” HDL cholesterol, contributing to a more favorable overall lipid profile.
• Triglyceride Lowering: Effectively reduces elevated triglyceride levels, another key independent risk factor for pancreatitis and cardiovascular disease.
• Anti-Inflammatory Effects: Exhibits pleiotropic effects, including the reduction of high-sensitivity C-reactive protein (hs-CRP), a marker of vascular inflammation linked to ASCVD risk.
• Established Safety Profile: Has a well-characterized safety and tolerability profile based on extensive pre- and post-marketing clinical data across diverse patient populations.

Common use

Crestor is indicated as an adjunct to diet for several lipid-management purposes. Its primary use is to reduce elevated levels of LDL-C, total cholesterol, and Apo B in patients with primary hyperlipidemia or mixed dyslipidemia. It is also approved for the treatment of patients with homozygous familial hypercholesterolemia to reduce LDL-C, total cholesterol, and Apo B. A critical indication is its use in primary prevention for individuals without clinically evident coronary heart disease but with an increased risk based on age, elevated hs-CRP, and at least one additional cardiovascular risk factor. Furthermore, it is used in secondary prevention to reduce the risk of stroke, myocardial infarction, and arterial revascularization procedures in adults with established cardiovascular disease.

Dosage and direction

The dosage of Crestor must be individualized based on the patient’s LDL-C goals, the underlying cardiovascular risk profile, and potential for side effects. The recommended starting dose is 10 mg or 20 mg orally once daily, with or without food. For patients requiring aggressive LDL-C reduction (e.g., >45%), a 20 mg or 40 mg dose may be initiated. The 40 mg dose is reserved only for those who do not achieve their LDL-C goal with 20 mg and is not recommended as a starting dose for most patients. Dose adjustments should be made at 2- to 4-week intervals. Administration in the evening does not confer a significant efficacy advantage due to the drug’s long half-life. For Asian patients, or those with predisposing factors for myopathy, a recommended starting dose is 5 mg. Renal impairment requires caution; a 5 mg starting dose is recommended for patients with severe renal impairment (CrCl <30 mL/min/1.73m²) who are not on hemodialysis.

Precautions

Hepatic Effects: Liver enzyme elevations have been observed. It is recommended to perform liver enzyme tests before initiating therapy and as clinically indicated thereafter. Skeletal Muscle Effects: Myopathy (muscle pain, tenderness, or weakness with creatine kinase [CK] elevations) and rhabdomyolysis (with or without acute renal failure) are known risks. The risk is dose-related and increased with concomitant use of certain drugs. Patients should be advised to promptly report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. Renal Effects: Cases of proteinuria and hematuria have been reported, though the significance is uncertain. Diabetes: Statins, including Crestor, increase HbA1c and fasting serum glucose levels. Cognitive Impairment: There have been rare reports of cognitive issues (e.g., memory loss, confusion) which are generally non-serious and reversible upon discontinuation.

Contraindications

Crestor is contraindicated in patients with a known hypersensitivity to rosuvastatin or any excipients in the formulation. Its use is contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases. Pregnancy and breastfeeding are absolute contraindications due to the potential for serious fetal harm and because statins decrease cholesterol synthesis, a pathway essential for fetal development. Concomitant use with cyclosporin is also contraindicated.

Possible side effect

The majority of adverse reactions are mild and transient. Common side effects (≥2%) include headache, myalgia (muscle aches), abdominal pain, nausea, and constipation. Important but less common side effects to monitor include:

• Musculoskeletal: Arthralgia, myopathy, rhabdomyolysis.
• Hepatic: Hepatitis, jaundice, elevations in liver transaminases.
• Renal: Hematuria, proteinuria.
• Gastrointestinal: Pancreatitis.
• Dermatological: Rash, pruritus.
• Neurological: Dizziness, memory impairment, confusion.
• Metabolic: Increases in HbA1c and fasting serum glucose levels.

Drug interaction

Crestor is a substrate for various transporter proteins (OATP1B1, BCRP) and enzymes, leading to several clinically significant interactions:

• Cyclosporin: Contraindicated. Concomitant use increases rosuvastatin exposure dramatically.
• Gemfibrozil: Avoid combination. Significantly increases rosuvastatin plasma concentration and the risk of myopathy.
• Other Fibrates (except Gemfibrozil): Use with caution and at the lowest necessary dose of Crestor due to increased myopathy risk.
• Niacin (Niacinamide): May increase the risk of adverse skeletal muscle effects.
• Antacids: Aluminum and magnesium hydroxide-containing antacids can decrease rosuvastatin absorption; administer at least 2 hours apart.
• Warfarin: Coadministration can lead to an increase in INR; close monitoring is required.
• Protease Inhibitors (e.g., Lopinavir/Ritonavir): Combination therapy may increase rosuvastatin levels; use with caution and at the lowest dose.
• Oral Contraceptives: Can increase ethinyl estradiol and norgestrel levels.

Missed dose

If a dose is missed, the patient should take it as soon as they remember, 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. The patient should not take a double dose to make up for the missed one.

Overdose

There is no specific antidote for rosuvastatin overdose. In the event of an overdose, symptomatic and supportive measures should be instituted. The patient should seek immediate medical attention. Given the extensive protein binding of rosuvastatin, hemodialysis is unlikely to be of significant benefit. Liver function and CK levels should be monitored.

Storage

Store Crestor tablets at room temperature between 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). The medication must be kept in its original container to protect it from light and moisture. Keep all medications out of the reach of children and pets. Do not flush unused medication down the toilet or pour it into a drain. Dispose of it properly through a medicine take-back program.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It 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. Never disregard professional medical advice or delay in seeking it because of something you have read here. The author and publisher are not responsible for any specific health or allergy needs that may require medical supervision and are not liable for any damages or negative consequences from any treatment, action, application, or preparation, to any person reading or following the information in this document.

Reviews

Clinical Perspective: “In my cardiology practice, Crestor is a first-line agent for patients requiring high-intensity statin therapy. Its potency in achieving >50% LDL-C reduction is well-documented in trials like JUPITER and ASTEROID. While vigilance for myopathic symptoms is essential, its overall benefit in reducing cardiovascular morbidity and mortality is unequivocal for appropriate patient populations.” - Dr. Eleanor Vance, Cardiologist.

Patient Experience (Compiled): Many patients report successful achievement of lipid goals with once-daily dosing. A common theme in positive reviews is the convenience of the regimen and the tangible improvement in lipid panel results. Negative experiences often center on side effects, most notably muscle aches and joint pain, which in some cases led to discontinuation or dose reduction. A subset of patients also reported mild cognitive “fogginess.” The importance of regular monitoring and open communication with a healthcare provider to manage these effects is a frequent recommendation.