Rosuvastatin: Advanced LDL Cholesterol Reduction Therapy
| Product dosage: 10mg | |||
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Synonyms | |||
Rosuvastatin is a highly potent, synthetic HMG-CoA reductase inhibitor, widely recognized in clinical practice for its superior efficacy in managing dyslipidemia. As a third-generation statin, it demonstrates exceptional selectivity for hepatocytes and offers a favorable pharmacokinetic profile, making it a cornerstone therapy in both primary and secondary cardiovascular prevention. Its robust evidence base, derived from landmark trials such as JUPITER and CORONA, supports its role in significantly reducing atherosclerotic cardiovascular disease (ASCVD) risk. This agent is particularly valued for its ability to achieve stringent lipid targets in high-risk and very high-risk patient populations, often at lower milligram strengths compared to other statins.
Features
- Active Ingredient: Rosuvastatin calcium
- Pharmacologic Class: HMG-CoA reductase inhibitor (statin)
- Available Strengths: 5 mg, 10 mg, 20 mg, 40 mg tablets
- Bioavailability: Approximately 20%
- Time to Peak Plasma Concentration: 3–5 hours post-dose
- Half-Life: ~19 hours
- Metabolism: Minimal hepatic metabolism via CYP2C9; primarily excreted unchanged in feces
- Protein Binding: ~90%
- Special Formulations: Available in film-coated tablets for oral administration
Benefits
- Achieves profound reductions in low-density lipoprotein cholesterol (LDL-C), often exceeding 50% at moderate doses, facilitating attainment of guideline-directed lipid goals.
- Increases high-density lipoprotein cholesterol (HDL-C) by 8–12%, contributing to a more favorable lipid profile and enhanced reverse cholesterol transport.
- Demonstrates significant anti-inflammatory effects, as evidenced by reductions in high-sensitivity C-reactive protein (hs-CRP), independently associated with decreased cardiovascular events.
- Slows progression and may induce regression of coronary atherosclerosis, as validated by intravascular ultrasound (IVUS) studies.
- Reduces incidence of major adverse cardiovascular events (MACE), including myocardial infarction, stroke, and need for revascularization procedures.
- Offers convenient once-daily dosing, supporting long-term adherence essential for chronic cardiovascular risk management.
Common use
Rosuvastatin is primarily indicated as an adjunct to diet for the reduction of elevated total cholesterol, LDL-C, apolipoprotein B, and triglycerides in adults with primary hyperlipidemia or mixed dyslipidemia. It is also approved for the treatment of pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia. Beyond lipid modification, it is extensively used for primary prevention in individuals with elevated hs-CRP without hyperlipidemia but with additional risk factors, as well as for secondary prevention in established ASCVD. It is a preferred agent in cases requiring aggressive LDL-C lowering, such as in familial hypercholesterolemia, diabetes mellitus with cardiovascular risk, or following acute coronary syndromes.
Dosage and direction
The recommended starting dose is 10 mg or 20 mg orally once daily, with or without food. For patients requiring aggressive LDL-C reduction (>45%), a starting dose of 20 mg may be appropriate. Dose adjustments should be made at 2–4 week intervals based on lipid response and tolerability. The maximum approved dose is 40 mg daily, reserved for patients who do not achieve goal LDL-C on 20 mg and who do not have Asian ancestry or predisposing factors for myopathy. In Asian patients, or those with cyclosporine coadministration, a starting dose of 5 mg is recommended due to increased systemic exposure. Administration in the evening is not required due to the long half-life. Renal impairment requires caution: for CrCl <30 mL/min, the starting dose should not exceed 5 mg daily, and 10 mg daily should not be exceeded.
Precautions
Prior to initiation, measure fasting lipid profile, liver transaminases (ALT, AST), and creatine kinase (CK). Rule out secondary causes of hyperlipidemia. Use with caution in patients with a history of liver disease or substantial alcohol consumption. Avoid in acute liver failure or decompensated cirrhosis. Monitor for muscle symptoms; advise patients to report unexplained muscle pain, tenderness, weakness, or brown urine promptly. Consider temporary discontinuation in any patient with an acute, serious condition predisposing to renal failure secondary to rhabdomyolysis (e.g., sepsis, hypotension, major surgery, trauma). Use in elderly patients may require careful dose titration due to potential for increased systemic exposure and higher prevalence of comorbidities. Not recommended during pregnancy (Pregnancy Category X) or breastfeeding.
Contraindications
Hypersensitivity to rosuvastatin or any component of the formulation. Active liver disease or unexplained persistent elevations of serum transaminases exceeding 3 times the upper limit of normal. Concomitant use with cyclosporine. Pregnancy, women who are or may become pregnant, and nursing mothers due to risk of fetal harm.
Possible side effect
Common adverse reactions (≥2%) include headache, myalgia, abdominal pain, nausea, constipation, and asthenia. Less frequently, dizziness, insomnia, and rash may occur. Important serious side effects, though rare, include:
- Myopathy/Rhabdomyolysis: Characterized by muscle pain, tenderness, weakness with CK elevations >10x ULN, and potential acute renal failure.
- Hepatotoxicity: Asymptomatic transaminase elevations >3x ULN occur in 0.2–0.4% of patients; rarely progresses to liver failure.
- Diabetes Mellitus: Small increased risk of HbA1c elevation and new-onset diabetes, particularly in those with pre-existing risk factors.
- Proteinuria: Dipstick-positive proteinuria has been observed, typically transient and not indicative of renal injury.
- Cognitive Impairment: Rare reports of memory loss, confusion.
Drug interaction
- Strong CYP2C9 Inhibitors: May increase rosuvastatin exposure; avoid combination if possible.
- Cyclosporine: Contraindicated due to >7-fold increase in AUC.
- Gemfibrozil: Avoid combination; increases rosuvastatin exposure and risk of myopathy.
- Antacids: Aluminum- and magnesium-containing antacids decrease absorption; administer at least 2 hours apart.
- Warfarin: May potentiate anticoagulant effect; monitor INR closely upon initiation or dose adjustment.
- Protease Inhibitors (e.g., lopinavir/ritonavir): Combination may increase rosuvastatin levels; use lowest possible dose with careful monitoring.
- Other Lipid-Lowering Agents: Use with fenofibrate or niacin may increase myopathy risk; generally avoid with gemfibrozil.
Missed dose
If a dose is missed, it should be taken as soon as remembered on the same day. If it is near the time for the next dose, skip the missed dose and resume the usual dosing schedule. Do not double the dose to make up for a missed dose.
Overdose
There is no specific antidote for rosuvastatin overdose. Suspected overdose should involve symptomatic and supportive measures. Given the extensive protein binding, hemodialysis is unlikely to be effective. Monitor for signs of myopathy or renal injury, and measure CK and serum creatinine. Provide supportive care for liver function if indicated.
Storage
Store at controlled room temperature, 20–25°C (68–77°F). Excursions permitted to 15–30°C (59–86°F). Keep in the original container, tightly closed, and protect from light and moisture. Keep out of reach of children and pets.
Disclaimer
This information is intended for educational purposes and healthcare professionals. 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. Individual patient response and necessary monitoring should be guided by a healthcare provider familiar with the patient’s full medical history.
Reviews
“Rosuvastatin has been transformative in our lipid clinic. Its potency allows us to get even our highest-risk patients to goal, often without needing additional agents. The long half-life is a practical advantage for adherence.” — Cardiologist, 12 years experience
“In my primary care practice, I find rosuvastatin well-tolerated in most patients. The JUPITER data gives me confidence when prescribing for primary prevention in appropriate candidates.” — Family Physician, 8 years experience
“As a clinical pharmacist, I appreciate its predictable pharmacokinetics and limited drug interaction profile compared to some other statins. It simplifies management in polypharmacy patients.” — PharmD, BCPS
“The 5mg dose is particularly useful in elderly patients or those with renal impairment. It offers a nice balance of efficacy and safety in these vulnerable populations.” — Geriatrician, 15 years experience