Rosuvastatin is a highly potent, synthetic HMG-CoA reductase inhibitor (statin) belonging to the latest generation of lipid-lowering agents. It is specifically engineered to provide superior efficacy in reducing low-density lipoprotein cholesterol (LDL-C) and apolipoprotein B, while also offering significant benefits in raising high-density lipoprotein cholesterol (HDL-C). Clinically, it is a cornerstone therapy for the management of dyslipidemia and the primary and secondary prevention of atherosclerotic cardiovascular disease (ASCVD). Its robust pharmacokinetic profile allows for effective dosing flexibility and reliable long-term lipid control.

Features

• Active Pharmaceutical Ingredient: Rosuvastatin calcium
• Standard 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%
• Time to Peak Plasma Concentration (Tmax): 3–5 hours post oral administration
• Half-life: ~19 hours, supporting once-daily dosing
• Protein Binding: ~90%, primarily to albumin
• Metabolism: Minimal hepatic metabolism via CYP2C9 (≈10%); primarily excreted unchanged in feces
• Special Formulation Options: Some brands offer film-coated tablets for ease of swallowing

Benefits

• Achieves profound reductions in LDL-C levels, often exceeding 50% at higher doses, which is associated with significant reductions in major adverse cardiac events
• Demonstrates favorable effects on other lipid parameters, including increases in HDL-C and reductions in triglycerides
• Provides well-established anti-inflammatory effects, as measured by reductions in high-sensitivity C-reactive protein (hs-CRP)
• Supports regression of coronary atheroma volume, as evidenced in intravascular ultrasound studies
• Offers a convenient once-daily dosing regimen, enhancing long-term patient adherence
• Possesses a generally favorable safety and tolerability profile in appropriately selected patients

Common use

Rosuvastatin is indicated as an adjunct to diet and lifestyle modifications for:

• Primary hyperlipidemia and mixed dyslipidemia (Fredrickson Type IIa and IIb)
• Primary prevention of cardiovascular events in adults without clinically evident coronary heart disease but with increased risk factors (e.g., age, smoking, hypertension, low HDL-C, family history)
• Secondary prevention in adults with established cardiovascular disease to reduce the risk of nonfatal myocardial infarction, nonfatal stroke, and the need for arterial revascularization procedures
• Homozygous familial hypercholesterolemia to reduce LDL-C, total cholesterol, and apolipoprotein B
• Slowing the progression of atherosclerosis in adult patients as part of a comprehensive risk-reduction strategy

Dosage and direction

• The recommended starting dose is 5–10 mg orally once daily, with or without food. Dose selection should be individualized based on patient characteristics, lipid goals, and anticipated response.
• For patients requiring aggressive LDL-C reduction (e.g., >45%), a starting dose of 20 mg may be appropriate after assessing cardiovascular risk and ruling out contraindications.
• The 40 mg dose is reserved for patients with severe hypercholesterolemia (e.g., homozygous FH) who do not achieve goal on lower doses and is not recommended as an initial dose.
• Dosage adjustments should be made at 2–4 week intervals, based on fasting lipid panel results.
• In patients with severe renal impairment (CrCl <30 mL/min) not on hemodialysis, the recommended starting dose is 5 mg; the 40 mg dose is contraindicated in these patients.
• Asian patients may exhibit increased systemic exposure; consider a starting dose of 5 mg.

Precautions

• Hepatic Effects: Obtain liver enzyme tests (e.g., ALT, AST) before initiating therapy and as clinically indicated thereafter. Discontinue if persistent elevations >3x ULN occur.
• Skeletal Muscle Effects: Inform patients to promptly report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. Monitor CPK levels in symptomatic patients.
• Renal Impairment: Use with caution in patients with moderate to severe renal impairment; dose adjustment is necessary.
• Diabetes: Statins may increase HbA1c and fasting serum glucose levels. The cardiovascular benefits generally outweigh the small absolute increase in diabetes risk.
• Concomitant Therapy: Exercise caution with drugs that inhibit transporters or enzymes involved in rosuvastatin clearance (e.g., cyclosporine, gemfibrozil).
• Pregnancy and Lactation: Contraindicated in pregnancy and breastfeeding due to potential fetal harm and excretion in breast milk.

Contraindications

• Hypersensitivity to rosuvastatin or any component of the formulation
• Active liver disease or unexplained persistent elevations of serum transaminases
• Pregnancy, women who are trying to conceive, and lactation
• Concomitant use with cyclosporine
• Severe renal impairment (CrCl <30 mL/min) for the 40 mg dose

Possible side effect

Common (≥1/100 to <1/10):

• Headache
• Myalgia (muscle pain)
• Constipation
• Nausea
• Abdominal pain
• Asthenia (weakness)

Uncommon (≥1/1,000 to <1/100):

• Dizziness
• Pruritus (itching)
• Rash
• Increased ALT/AST

Rare (≥1/10,000 to <1/1,000):

• Myopathy
• Rhabdomyolysis (with renal impairment secondary to myoglobinuria)
• Pancreatitis
• Hepatitis
• Jaundice
• Peripheral neuropathy
• Memory impairment
• Arthralgia
• Hypersensitivity reactions (including angioedema)

Drug interaction

• Cyclosporine: Contraindicated. Concomitant use increases rosuvastatin exposure (AUC) by approximately 7-fold.
• Gemfibrozil: Avoid combination if possible. Increases rosuvastatin exposure ~2-fold and increases risk of myopathy.
• Other Fibrates (e.g., fenofibrate): May increase risk of myopathy; use the lowest necessary dose and monitor closely.
• Warfarin: Rosuvastatin may potentiate anticoagulant effect; monitor INR closely upon initiation or dose adjustment.
• Oral Contraceptives: May increase ethinyl estradiol and norgestrel levels; clinical significance is uncertain.
• Protease Inhibitors (e.g., atazanavir, lopinavir/ritonavir): May increase rosuvastatin concentration; consider alternative statin or use lowest dose.
• Vitamin K Antagonists: Monitor INR as statins may enhance anticoagulant effect.

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 scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. Do not double the dose to make up for a missed one.

Overdose

There is no specific antidote for rosuvastatin overdose. Suspected overdose should be managed with supportive measures, focusing on symptomatic treatment. Given its extensive protein binding, rosuvastatin is not expected to be significantly dialyzable. Liver function and CPK levels should be monitored. Provide general supportive care for any presenting symptoms.

Storage

Store at controlled room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 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 for educational and professional reference purposes only and does not constitute medical advice. The prescribing physician is responsible for determining the appropriateness of therapy based on the individual patient’s clinical status, contraindications, and therapeutic goals. Always consult official prescribing information and clinical guidelines before initiation or modification of therapy. The patient should be fully informed of the benefits and risks and should adhere to the prescribed dosage and monitoring schedule.

Reviews

“Rosuvastatin has been a game-changer in our lipid clinic. Its potency allows us to achieve aggressive LDL targets even in resistant cases, and the once-daily dosing supports excellent long-term adherence. We monitor liver and muscle enzymes routinely, but significant issues have been rare in our practice.” – Cardiologist, 12 years of use

“In my experience with high-risk primary prevention patients, rosuvastatin consistently delivers robust LDL reductions and hs-CRP decreases. The cardiovascular outcome data is compelling. I start with 10 mg in most patients and titrate based on response and tolerance.” – Internal Medicine Specialist

“While effective, I am always cautious with Asian patients and those with renal impairment due to the increased exposure. Starting with a 5 mg dose and monitoring closely has helped mitigate risks. The efficacy at low doses is still appreciable.” – Nephrologist

“Patient tolerance is generally good. The most common complaint is mild myalgia, which often resolves with dose adjustment or switching to alternate-day dosing. The benefits in slowing atherosclerosis progression are well worth the management of minor side effects.” – Clinical Lipidologist

“As a primary care physician, I value the predictable efficacy and straightforward dosing. It simplifies patient education and follow-up. The drug interaction profile requires attention, especially with fibrates, but it’s manageable with careful patient selection.” – General Practitioner