Rosuvastatin is a potent, synthetic HMG-CoA reductase inhibitor belonging to the statin class of pharmaceuticals, specifically engineered for superior lipid-modifying efficacy. It functions by competitively inhibiting the rate-limiting enzyme in hepatic cholesterol biosynthesis, resulting in upregulation of LDL receptors and enhanced clearance of atherogenic lipoproteins from the bloodstream. Clinically, it is indicated for the management of dyslipidemias, primary prevention of cardiovascular events in high-risk patients, and secondary prevention in established atherosclerotic cardiovascular disease. Its distinct pharmacokinetic profile, including minimal metabolism via CYP450 isoenzymes, contributes to a predictable efficacy and safety spectrum, making it a cornerstone in modern lipid-lowering therapy.

Features

• Active pharmaceutical ingredient: Rosuvastatin calcium
• Available strengths: 5 mg, 10 mg, 20 mg, 40 mg film-coated tablets
• High hepatic selectivity with low extrahepatic exposure
• Minimal cytochrome P450 metabolism (primarily CYP2C9)
• Plasma half-life of approximately 19 hours
• Excretion primarily via feces (90%) with renal elimination accounting for approximately 10%
• Demonstrated LDL-C reduction efficacy of 45-63% across dosage range
• Significant HDL-C elevation and triglyceride reduction capabilities

Benefits

• Achieves rapid and substantial reduction in low-density lipoprotein cholesterol (LDL-C) levels
• Demonstrates significant regression of coronary atheroma volume in intravascular ultrasound studies
• Reduces incidence of major adverse cardiovascular events (myocardial infarction, stroke, revascularization procedures)
• Provides comprehensive lipid management through triglyceride reduction and HDL-C elevation
• Offers flexible dosing options tailored to individual patient lipid goals and tolerance
• Maintains consistent 24-hour lipid-lowering effect with once-daily dosing convenience

Common use

Rosuvastatin is primarily prescribed for patients requiring significant reduction in LDL-C levels, particularly those with heterozygous familial hypercholesterolemia, homozygous familial hypercholesterolemia (as an adjunct to other lipid-lowering treatments), or mixed dyslipidemia. It is extensively utilized in both primary and secondary prevention of cardiovascular disease, especially in patients who have not achieved target LDL-C levels with other statins. The medication is commonly employed in metabolic syndrome management and is increasingly used in patients with diabetes mellitus who require aggressive lipid control. Clinical guidelines position rosuvastatin as a first-line option for high and very high-risk patients according to ASCVD risk stratification.

Dosage and direction

Initiate treatment with 5-10 mg once daily, with dosage adjustment based on lipid response and tolerability after 4 weeks of therapy. The recommended dosing range is 5-40 mg daily, with the 40 mg dose reserved for patients who do not achieve LDL-C goals with 20 mg and who are not of Asian ancestry. Administer orally with or without food, preferably at the same time each day. For Asian patients or those with predisposing factors for myopathy, initiate with 5 mg daily. Dose adjustment is required in patients with severe renal impairment (CrCl <30 mL/min): start with 5 mg daily, not to exceed 10 mg daily. No dosage adjustment is necessary for mild to moderate hepatic impairment; contraindicated in active liver disease.

Precautions

Monitor liver function tests prior to initiation and periodically thereafter (e.g., at 12 weeks following initiation or dose elevation, and periodically thereafter). Assess creatine kinase levels in patients presenting with unexplained muscle pain, tenderness, or weakness. Exercise caution in patients consuming substantial quantities of alcohol or with history of liver disease. Monitor glycemic control in patients with diabetes, as statins may increase HbA1c and fasting serum glucose levels. Consider the potential for cognitive impairment (memory loss, confusion) though generally not serious and reversible upon discontinuation. Use with caution in patients with risk factors for myopathy/rhabdomyolysis including advanced age, hypothyroidism, renal impairment, and concomitant use of certain medications.

Contraindications

Hypersensitivity to rosuvastatin or any component of the formulation; active liver disease or unexplained persistent elevations of serum transaminases; pregnancy and breastfeeding; concomitant use with cyclosporine. The 40 mg dose is contraindicated in patients with predisposing factors for myopathy/rhabdomyolysis, including Asian patients, severe renal impairment (CrCl <30 mL/min), and concomitant therapy with gemfibrozil.

Possible side effect

Common adverse reactions (≥2%) include headache, myalgia, abdominal pain, nausea, and constipation. Musculoskeletal events range from mild myalgia (5-10%) to rare rhabdomyolysis (<0.1%). Elevated liver enzymes (AST/ALT >3x ULN) occur in 0.1-2.3% of patients, typically dose-dependent. Other reported effects include diabetes mellitus (increased incidence in predisposed patients), proteinuria (generally transient and not indicative of renal disease), and rarely, immune-mediated necrotizing myopathy. Dermatological reactions including rash and pruritus may occur in approximately 1-3% of patients.

Drug interaction

Potent inhibitors of OATP1B1 and BCRP transporters (e.g., cyclosporine) significantly increase rosuvastatin exposure—avoid concomitant use. Gemfibrozil increases rosuvastatin AUC approximately 2-fold—avoid combination. Other fibrates may increase myopathy risk—use with caution. Warfarin: monitor INR closely as rosuvastatin may enhance anticoagulant effect. Oral contraceptives: increased ethinyl estradiol and norgestrel concentrations. Antacids: administer at least 2 hours apart to avoid reduced absorption. Lopinavir/ritonavir combination increases rosuvastatin exposure—limit rosuvastatin to 10 mg daily.

Missed dose

If a dose is missed, take it as soon as remembered on the same day. If remembered on the following day, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed administration. Maintain consistent daily dosing to ensure continuous inhibition of cholesterol synthesis. The extended half-life of rosuvastatin provides some buffer against temporary fluctuations in plasma concentrations, though adherence to prescribed regimen is crucial for optimal therapeutic outcomes.

Overdose

No specific antidote exists for rosuvastatin overdose. Suspected overdose requires symptomatic and supportive measures. Gastric lavage may be considered if performed shortly after ingestion. Monitor for signs and symptoms of myopathy/rhabdomyolysis (myalgia, muscle weakness, dark urine) and provide appropriate hydration to prevent renal compromise. Liver function tests and creatine kinase levels should be monitored serially. Hemodialysis is unlikely to be beneficial due to high protein binding and extensive hepatic extraction. Contact poison control center for latest management recommendations.

Storage

Store at controlled room temperature 20-25°C (68-77°F) with excursions permitted between 15-30°C (59-86°F). Protect from light and moisture. Keep in original container with tight closure. Do not remove desiccant from bottle. Keep out of reach of children and pets. Do not use after expiration date printed on packaging. Properly dispose of unused medication through medication take-back programs or according to local regulations.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Prescription and use of rosuvastatin must be under the supervision of a qualified healthcare professional who can assess individual patient factors, contraindications, and monitoring requirements. Dosage and administration should be strictly according to prescribing information. The manufacturer and distributor are not liable for any consequences arising from inappropriate use or interpretation of this information. Always consult with a healthcare provider for personalized medical advice.

Reviews

Clinical trials consistently demonstrate rosuvastatin’s efficacy in achieving LDL-C reduction targets across diverse patient populations. The JUPITER trial showed 44% reduction in primary endpoint (myocardial infarction, stroke, arterial revascularization, hospitalization for unstable angina, or death from cardiovascular causes) in patients with elevated hs-CRP but normal LDL-C. Meta-analyses confirm its position among the most potent statins for LDL-C reduction per mg dose. Real-world evidence supports maintained efficacy in clinical practice with generally favorable tolerability profile. Specialist consensus guidelines consistently rank rosuvastatin as a preferred agent for patients requiring >50% LDL-C reduction.