Rosuvastatin: Advanced Lipid Management for Cardiovascular Risk Reduction
| Product dosage: 10mg | |||
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Synonyms | |||
Rosuvastatin is a potent, synthetic HMG-CoA reductase inhibitor, widely prescribed for the management of dyslipidemia. As a third-generation statin, it demonstrates superior efficacy in reducing low-density lipoprotein cholesterol (LDL-C) and elevating high-density lipoprotein cholesterol (HDL-C), thereby addressing a critical component of atherosclerotic cardiovascular disease (ASCVD) risk. Its well-characterized pharmacokinetic profile and extensive evidence base support its use in both primary and secondary prevention settings, making it a cornerstone therapy in modern cardiology and lipidology practice.
Features
- Active Ingredient: Rosuvastatin calcium
- Available Strengths: 5 mg, 10 mg, 20 mg, 40 mg tablets
- Mechanism of Action: Competitive inhibition of HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol synthesis
- Bioavailability: Approximately 20%
- Half-life: ~19 hours
- Protein Binding: 90%, primarily to albumin
- Metabolism: Minimal hepatic metabolism via CYP2C9 and CYP2C19; primarily excreted unchanged in feces
- Special Formulations: Some markets offer authorized generic versions
Benefits
- Significant LDL-C Reduction: Demonstrates dose-dependent LDL-C reduction of 45–63%, among the highest in the statin class
- HDL-C Elevation: Increases HDL-C by 8–14%, contributing to reverse cholesterol transport
- Atherosclerotic Plaque Stabilization: Reduces plaque inflammation and may promote regression of coronary atheroma volume
- Cardiovascular Event Reduction: Proven to significantly reduce major adverse cardiac events (MACE) in appropriate patient populations
- Versatile Dosing Options: Wide dosing range allows for tailored therapy across diverse patient phenotypes and risk categories
- Once-Daily Dosing: Enhances adherence through convenient 24-hour pharmacokinetic coverage
Common use
Rosuvastatin is indicated as an adjunct to diet for the reduction of elevated total cholesterol, LDL-C, apolipoprotein B, non-HDL-C, 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 parameters, it is utilized in the slowing of atherosclerosis progression and for primary prevention of cardiovascular events in individuals with elevated hs-CRP without clinically evident coronary disease but with additional risk factors. Its use extends to patients with homozygous familial hypercholesterolemia as part of a comprehensive lipid-lowering regimen.
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 20 mg starting dose may be appropriate. The 40 mg dose is reserved for patients who do not achieve LDL-C goal with 20 mg and should only be used in patients without predisposing factors for myopathy. Asian patients may require initiation at 5 mg due to increased systemic exposure. Dosage adjustments are necessary in patients with severe renal impairment (CrCl <30 mL/min), with recommended initiation at 5 mg not to exceed 10 mg daily. Administration timing is flexible but should be consistent daily; evening dosing may provide marginally better LDL-C reduction in some patients due to circadian cholesterol synthesis patterns.
Precautions
Liver function tests (ALT, AST) should be performed before initiation and as clinically indicated thereafter. Patients should report unexplained muscle pain, tenderness, or weakness promptly, particularly if accompanied by malaise or fever. Use with caution in patients consuming substantial quantities of alcohol or with a history of liver disease. Rosuvastatin may increase HbA1c and fasting serum glucose levels; monitor diabetic parameters appropriately. Consider discontinuation if serum transaminases persist at >3× ULN. In elderly patients (≥65 years), increased systemic exposure warrants careful dose titration. The 40 mg dose carries increased risk of myopathy and proteinuria and should be avoided in patients of Asian ancestry, those with predisposing factors for myopathy, or with 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 (Category X – may cause fetal harm). Concomitant use with cyclosporine. The 40 mg dose is contraindicated in patients with predisposing factors for rhabdomyolysis, including renal impairment, hypothyroidism, personal or family history of hereditary muscular disorders, previous statin intolerance, or excessive alcohol intake.
Possible side effect
Common (≥2%): headache, myalgia, constipation, nausea, abdominal pain, asthenia. Less common: dizziness, insomnia, rash, pruritus. Important but rare: myopathy (≥10× ULN CK elevation), rhabdomyolysis with acute renal failure, hepatitis, jaundice, peripheral neuropathy, memory impairment, confusion, pancreatic dysfunction, gynecomastia, proteinuria (usually transient and not indicative of renal disease), arthralgia. Laboratory abnormalities: elevated transaminases, CK, glucose, HbA1c; decreased thyroid function tests interference in some assays.
Drug interaction
Contraindicated combinations: Cyclosporine (increases rosuvastatin AUC up to 7-fold). Significant interactions: Gemfibrozil and other fibrates (increase rosuvastatin exposure and myopathy risk – avoid combination with gemfibrozil; fenofibrate preferred if necessary). Moderate interactions: Niacin (>1 g/day), colchicine, azole antifungals, HIV protease inhibitors, macrolide antibiotics, warfarin (monitor INR closely). Mild interactions: Oral contraceptives (increases ethinyl estradiol and norgestrel levels), antacids (administer至少 2 hours apart). Note: Rosuvastatin has lower CYP450 interaction potential than other statins but remains subject to transporter-mediated interactions (OATP1B1, BCRP).
Missed dose
If a dose is missed, take it as soon as remembered on the same day. If remembered the next day, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed dose. Consistent daily administration is important for maintaining stable lipid-lowering effects; consider setting reminders or using pill organizers if missed doses occur frequently.
Overdose
No specific antidote exists. Management should be supportive and symptomatic. Consider activated charcoal if ingestion recent. Monitor for signs of myopathy (muscle pain, weakness, dark urine) and renal function. Hemodialysis is unlikely to be effective due to high protein binding. In cases of significant overdose, hospitalization for monitoring of CK, renal function, and liver enzymes is recommended. Provide symptomatic treatment for gastrointestinal distress if present.
Storage
Store at 20–25°C (68–77°F); excursions permitted to 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 expiration date printed on packaging. Do not transfer to other containers as moisture protection may be compromised.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Rosuvastatin is a prescription medication that should only be used under the supervision of a qualified healthcare provider. Individual response to therapy may vary. Patients should not initiate, discontinue, or change dosage without consulting their physician. The full prescribing information should be consulted before use.
Reviews
“Rosuvastatin has been transformative in our high-risk CVD clinic. The LDL-C reduction is consistently robust, and we’ve successfully titrated many patients to goal who previously failed other statins. The once-daily dosing improves adherence significantly.” – Cardiologist, 15 years experience
“In my pediatric lipid clinic, rosuvastatin has enabled us to achieve target LDL levels in heterozygous FH patients where other agents fell short. The safety profile in adolescents has been excellent with appropriate monitoring.” – Pediatric Endocrinologist
“While the efficacy is unquestionable, I maintain vigilance for myopathic symptoms, particularly in patients on higher doses or with concomitant interacting medications. The dose-dependent risk requires careful patient selection and education.” – Clinical Pharmacist
“The 5 mg dose has been particularly valuable in our Asian patient population, providing effective lipid control without excessive exposure. The ethnic sensitivity in dosing is a crucial consideration in prescribing.” – Internal Medicine Specialist