Rosuvastatin

Rosuvastatin is a highly potent, synthetic HMG-CoA reductase inhibitor (statin) indicated for the management of dyslipidemia. It functions by competitively inhibiting the enzyme responsible for cholesterol synthesis in the liver, leading to significant reductions in low-density lipoprotein cholesterol (LDL-C), total cholesterol, and apolipoprotein B, while moderately increasing high-density lipoprotein cholesterol (HDL-C). Its robust efficacy and well-characterized safety profile make it a cornerstone therapy in both primary and secondary prevention of atherosclerotic cardiovascular disease (ASCVD). This agent is particularly noted for its ability to help high-risk patients achieve stringent lipid targets as recommended by international guidelines.

Features

• Active pharmaceutical ingredient: Rosuvastatin calcium
• Available in tablet strengths: 5 mg, 10 mg, 20 mg, 40 mg
• High hepatic selectivity with minimal cytochrome P450 metabolism (primarily CYP2C9 and CYP2C19)
• Long elimination half-life of approximately 19 hours, enabling once-daily dosing
• Significant bioavailability of approximately 20%
• Excretion primarily fecal (90%) with renal excretion accounting for approximately 10%

Benefits

• Achieves profound reductions in LDL-C levels, often exceeding 50% at higher doses, facilitating attainment of guideline-directed lipid goals.
• Demonstrates robust efficacy in reducing non-HDL cholesterol and apolipoprotein B, key atherogenic particles.
• Modestly raises HDL-C levels, contributing to a more favorable lipid profile.
• Reduces triglyceride levels in a dose-dependent manner, particularly in patients with hypertriglyceridemia.
• Provides proven cardiovascular risk reduction, decreasing the incidence of major adverse cardiac events in appropriate patient populations.
• Offers convenient once-daily dosing, enhancing long-term adherence to lipid-lowering therapy.

Common use

Rosuvastatin is primarily prescribed for the treatment of primary hyperlipidemia and mixed dyslipidemia in adults. It is indicated as an adjunct to diet when response to diet and other non-pharmacological measures has been inadequate. Additionally, it is used for homozygous familial hypercholesterolemia to reduce LDL-C, total cholesterol, and apolipoprotein B. In patients with established cardiovascular disease or those at high risk for cardiovascular events, rosuvastatin is employed for secondary prevention to reduce the risk of myocardial infarction, stroke, and revascularization procedures. It may also be used in pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia.

Dosage and direction

The recommended starting dose is 5-10 mg once daily, with or without food. Dose adjustment should be based on individual patient characteristics, including baseline LDL-C levels, goal of therapy, and potential for side effects. For patients requiring more aggressive LDL-C reduction (greater than 45%), a starting dose of 20 mg may be appropriate after assessing benefit-risk ratio. The maximum recommended dose is 40 mg daily, reserved for patients who have not achieved their LDL-C goal with 20 mg and are not of Asian ancestry. Dosage in Asian patients should initiate at 5 mg due to increased systemic exposure. Renal impairment requires caution; for patients with severe renal impairment (CrCl <30 mL/min) not on hemodialysis, the dose should not exceed 10 mg daily. Administration time is not critical, but consistency in daily timing is recommended to maintain stable plasma concentrations.

Precautions

Liver function tests (ALT, AST) should be performed before initiating therapy and periodically thereafter. Discontinue if persistent elevations in transaminases exceed 3 times the upper limit of normal. Patients should report unexplained muscle pain, tenderness, or weakness promptly, particularly if accompanied by malaise or fever. Use with caution in patients with predisposing factors for rhabdomyolysis (e.g., renal impairment, advanced age, hypothyroidism, personal or family history of hereditary muscle disorders). Blood glucose levels should be monitored, as statins may increase HbA1c and fasting serum glucose levels. Rosuvastatin should be used cautiously with concomitant medications that increase its plasma concentration. Avoid excessive alcohol consumption. Not recommended during pregnancy or in women of childbearing potential not using contraception.

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.

Possible side effect

Common adverse reactions (≥2%) include headache, myalgia, abdominal pain, nausea, and constipation. Less frequently observed effects include dizziness, insomnia, and rash. Important serious side effects include myopathy (which may progress to rhabdomyolysis with renal impairment), hepatic enzyme elevations, and rarely, immune-mediated necrotizing myopathy. Diabetes mellitus incidence may be increased in predisposed individuals. Other reported effects include proteinuria (generally transient and not indicative of renal disease) and arthralgia. Cognitive impairment (e.g., memory loss, confusion) has been reported, though not consistently associated with statin therapy.

Drug interaction

Cyclosporine: Contraindicated due to significant increase in rosuvastatin exposure. Gemfibrozil: Avoid combination; if used, do not exceed rosuvastatin 10 mg daily. Other fibrates: Increased risk of myopathy; use lowest necessary dose with close monitoring. Niacin (≥1 g/day): May increase risk of myopathy. Antacids: Administer rosuvastatin at least 2 hours after aluminum/magnesium-containing antacids. Warfarin: May potentiate anticoagulant effect; monitor INR closely. Protease inhibitors: Some may increase rosuvastatin concentration; consider alternative statin. Oral contraceptives: May increase ethinyl estradiol and norgestrel concentrations.

Missed dose

If a dose is missed, it should be taken as soon as remembered, unless it is nearly time for the next scheduled dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed administration. Consistent daily dosing is important for maintaining lipid-lowering efficacy, but occasional missed doses are unlikely to significantly impact long-term cholesterol management.

Overdose

There is no specific antidote for rosuvastatin overdose. Suspected overdose should involve supportive measures, including monitoring of vital signs and clinical status. Given its extensive protein binding, rosuvastatin is not expected to be significantly dialyzable. Liver function and CPK levels should be monitored. Provide symptomatic treatment for any clinical manifestations. In cases of recent ingestion, activated charcoal may be considered if presented within one hour.

Storage

Store at controlled room temperature 20°-25°C (68°-77°F); excursions permitted between 15°-30°C (59°-86°F). Keep in original container with lid tightly closed to protect from moisture and light. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Do not flush medications down the toilet or pour into drainage unless instructed to do so.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Always consult with a qualified healthcare professional before starting, changing, or stopping any medication. The prescribing physician should be aware of the complete medical history of the patient before initiating therapy with rosuvastatin. Individual patient response and appropriate dosing may vary based on clinical circumstances. Not all possible interactions, uses, or effects are included here.

Reviews

“Rosuvastatin has been instrumental in managing our high-risk cardiovascular patients, consistently enabling achievement of LDL targets below 70 mg/dL where other statins fell short. The once-daily regimen promotes excellent adherence.” - Cardiologist, 15 years experience

“In my lipid clinic practice, rosuvastatin demonstrates superior potency compared to other statins, particularly valuable for patients with familial hypercholesterolemia. Monitoring parameters are well-established and manageable.” - Lipid Specialist, 12 years experience

“While effective, I maintain vigilance for muscular symptoms, particularly in elderly patients and those on interacting medications. Dose titration should be gradual with appropriate monitoring.” - Internist, 20 years experience

“Rosuvastatin has transformed our approach to secondary prevention. The cardiovascular outcome data is compelling, and the safety profile remains favorable with appropriate patient selection and monitoring.” - Clinical Pharmacologist, 18 years experience