Rosuvastatin is a highly potent, synthetic HMG-CoA reductase inhibitor belonging to the statin class of pharmaceuticals. It is specifically engineered to manage dyslipidemia by significantly reducing low-density lipoprotein cholesterol (LDL-C) and triglyceride levels while elevating high-density lipoprotein cholesterol (HDL-C). Clinically, it serves as a cornerstone therapy for primary and secondary prevention of atherosclerotic cardiovascular disease (ASCVD), demonstrating robust efficacy in slowing plaque progression and reducing major adverse cardiac events. Its advanced hydrophilicity contributes to selective hepatic uptake and a favorable pharmacokinetic profile, minimizing extrahepatic exposure. Approved by regulatory bodies including the FDA and EMA, rosuvastatin represents a first-line intervention in modern lipid management protocols.

Features

• Active pharmaceutical ingredient: Rosuvastatin calcium
• Available in tablet strengths: 5 mg, 10 mg, 20 mg, 40 mg
• High hepatic selectivity due to hydrophilic properties
• Long half-life (~19 hours), enabling once-daily dosing
• Significant LDL-C reduction (up to 63% at maximum dose)
• Modest HDL-C elevation (up to 14%)
• Triglyceride reduction (up to 28%)
• Renal excretion primarily unchanged (≈10%)
• CYP2C9-mediated metabolism (minimal CYP3A4 involvement)
• Bioavailability: ~20%
• Time to peak plasma concentration: 3–5 hours

Benefits

• Substantially lowers risk of myocardial infarction, stroke, and cardiovascular mortality
• Promotes regression of coronary atheroma volume
• Reduces need for revascularization procedures
• Improves endothelial function and vascular inflammation markers
• Provides predictable, dose-dependent lipid modulation
• Supports long-term adherence through once-daily dosing convenience

Common use

Rosuvastatin is indicated for the treatment of hypercholesterolemia, including heterozygous and homozygous familial hypercholesterolemia, as an adjunct to diet. It is prescribed for primary prevention in patients with elevated CRP levels without clinically evident CAD but with multiple risk factors. For secondary prevention, it is used in patients with established cardiovascular disease to reduce the risk of nonfatal MI, nonfatal stroke, and hospitalization for unstable angina. It may also be used in combination with other lipid-lowering therapies in complex dyslipidemias under specialist supervision.

Dosage and direction

Initiate treatment with 5–10 mg orally once daily, with or without food. Dosage should be individualized based on baseline LDL-C levels, goal targets, and patient comorbidities. Asian patients or those with predisposing factors for myopathy should start at 5 mg. The maximum recommended dose is 40 mg, reserved for patients not achieving LDL-C goals with 20 mg and without evidence of myopathy. Dosage adjustments are necessary in patients with severe renal impairment (CrCl <30 mL/min): initiation not to exceed 5 mg, with 10 mg as maximum. Reassess lipid levels within 2–4 weeks after initiation or titration.

Precautions

Monitor liver enzymes before initiation, at 12 weeks, after dose elevation, and periodically thereafter. Discontinue if ALT/AST persistently exceed 3× ULN. Assess creatine kinase (CK) levels in patients reporting unexplained muscle pain, tenderness, or weakness. Use caution in patients with history of liver disease, excessive alcohol consumption, or renal impairment. Consider potential risks in elderly patients (>65 years) due to increased exposure. Glycemic parameters should be monitored, as statins may increase HbA1c. Not recommended during pregnancy (Category X) or lactation.

Contraindications

Hypersensitivity to rosuvastatin or any product component. Active liver disease or unexplained persistent elevations of serum transaminases. Concomitant use with cyclosporine. Pregnancy, women of childbearing potential not using contraception, and breastfeeding. Severe renal impairment (CrCl <30 mL/min) at doses above 10 mg.

Possible side effect

Common (≥1/100 to <1/10): headache, myalgia, constipation, nausea, asthenia. Uncommon (≥1/1,000 to <1/100): dizziness, pruritus, rash, abdominal pain. Rare (≥1/10,000 to <1/1,000): myopathy, rhabdomyolysis, hepatitis, pancreatitis, memory loss. Very rare (<1/10,000): lupus-like syndrome, gynecomastia, tendon disorders. Laboratory abnormalities: elevated transaminases, CK, glucose, HbA1c; proteinuria (dose-related).

Drug interaction

Cyclosporine: contraindicated (increases rosuvastatin AUC ~7-fold). Gemfibrozil: avoid combination (increases rosuvastatin exposure 2x). Other fibrates: use with caution. Warfarin: monitor INR closely (may enhance anticoagulant effect). Oral contraceptives: increases ethinyl estradiol and norgestrel levels. Antacids: administer at least 2 hours apart. Protease inhibitors: use with caution (particularly with lopinavir/ritonavir).

Missed dose

Take the missed dose 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. Maintain regular dosing schedule to ensure consistent lipid-lowering effect.

Overdose

No specific antidote exists. Supportive measures should be employed, with attention to symptomatic treatment. Hemodialysis is unlikely to be beneficial due to high protein binding. Monitor for signs of myopathy or rhabdomyolysis; consider CK monitoring and hydration. Liver function tests should be performed.

Storage

Store at room temperature (15–30°C/59–86°F) in original container. Protect from light and moisture. Keep out of reach of children. Do not use after expiration date printed on packaging.

Disclaimer

This information is for educational purposes and does not replace professional medical advice. Dosage and treatment decisions must be made by a qualified healthcare provider based on individual patient characteristics. Always consult prescribing information and clinical guidelines before initiation.

Reviews

“Rosuvastatin has demonstrated superior LDL-lowering efficacy compared to other statins in our clinical practice, particularly in high-risk patients requiring >50% reduction. Its once-daily dosing and minimal drug interactions make it a preferred choice.” – Cardiologist, 12 years experience

“Consistent results in primary prevention trials, especially JUPITER, confirm its role in reducing cardiovascular events in patients with elevated hs-CRP. Tolerability profile is generally favorable, though Asian populations require careful dosing.” – Lipidologist, 8 years experience

“Notable for its potent effect on atherogenic lipoproteins. However, requires vigilance for diabetic predisposition and muscle symptoms, particularly in elderly patients and those on concomitant interacting medications.” – Internal Medicine Specialist, 15 years experience