Rosuvastatin

Rosuvastatin is a highly potent HMG-CoA reductase inhibitor, widely recognized in clinical practice for its efficacy in managing dyslipidemia and reducing atherosclerotic cardiovascular disease (ASCVD) risk. As a third-generation statin, it demonstrates superior LDL-cholesterol lowering capabilities compared to earlier agents, alongside beneficial effects on other lipid parameters. Its well-established safety profile and evidence-based outcomes make it a cornerstone therapy in both primary and secondary prevention strategies. This comprehensive overview details its pharmacological characteristics, clinical applications, and practical prescribing considerations for healthcare professionals.

Features

• Active Ingredient: Rosuvastatin calcium
• Pharmacological Class: HMG-CoA reductase inhibitor (statin)
• Available Strengths: 5 mg, 10 mg, 20 mg, 40 mg tablets
• Bioavailability: Approximately 20%
• Half-life: ~19 hours
• Time to Peak Plasma Concentration: 3–5 hours post-administration
• Metabolism: Minimal cytochrome P450 metabolism (primarily CYP2C9); mostly excreted unchanged in feces
• Protein Binding: ~90%
• Therapeutic Onset: LDL-C reduction observed within 1 week; maximal effect achieved by 4 weeks

Benefits

• Significant LDL-C Reduction: Achieves up to 63% reduction in low-density lipoprotein cholesterol at maximum dose, aiding in rapid attainment of lipid targets.
• Cardiovascular Event Risk Reduction: Demonstrated reduction in major adverse cardiovascular events (MACE), including myocardial infarction and stroke, in high-risk populations.
• Plaque Stabilization: Contributes to regression and stabilization of coronary atherosclerotic plaques through potent lipid-lowering and anti-inflammatory effects.
• HDL-C Increase: Modest increase in high-density lipoprotein cholesterol, further supporting cardiovascular protection.
• Triglyceride Lowering: Effective reduction of triglyceride levels by 10–25%, addressing mixed dyslipidemia.
• Renal Safety Profile: Suitable for use in mild-to-moderate chronic kidney disease without dose adjustment in many cases.

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 to slow the progression of atherosclerosis and for primary prevention of cardiovascular disease in individuals without clinically evident coronary heart disease but with increased risk factors (e.g., age, hypertension, low HDL-C, family history). Additionally, it is used in pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia. Its use is supported by major guidelines including ACC/AHA and ESC/EAS for ASCVD risk reduction.

Dosage and direction

The recommended starting dose is 5–10 mg once daily, with dosage individualized based on LDL-C goals, patient characteristics, and cardiovascular risk. For aggressive LDL-C lowering (>50% reduction), 20–40 mg may be used. Dosage should be taken orally, with or without food, at any time of day—though consistency is advised. Renal impairment (CrCl <30 mL/min): initial dose should not exceed 10 mg daily. Asian patients may have increased systemic exposure; consider 5 mg as starting dose. Dose adjustments should be made at 2–4 week intervals based on lipid response and tolerability.

Precautions

• Liver Function Monitoring: Obtain liver enzymes before initiation and as clinically indicated; discontinue if AST/ALT persistently exceed 3× ULN.
• Muscle Symptoms: Advise patients to report unexplained muscle pain, tenderness, or weakness; monitor CPK in symptomatic patients.
• Renal Effects: Proteinuria may occur, typically tubular in origin and not indicative of renal injury; monitor urinalysis periodically.
• Diabetes Risk: May increase HbA1c and fasting glucose; weigh benefits against potential small increased risk in predisposed individuals.
• Avoid Grapefruit Juice: May increase rosuvastatin exposure; consumption should be limited.
• Pregnancy/Lactation: Contraindicated in pregnancy and breastfeeding due to potential fetal harm and excretion in milk.

Contraindications

• Active liver disease or unexplained persistent elevations of serum transaminases
• Pregnancy, women who are or may become pregnant, and breastfeeding
• Hypersensitivity to rosuvastatin or any component of the formulation
• Concomitant use with cyclosporine

Possible side effect

Common (≥2%):

• Headache
• Myalgia
• Constipation
• Nausea
• Abdominal pain
• Asthenia

Less common:

• Increased ALT/AST
• Proteinuria
• Dizziness
• Insomnia
• Rash

Rare but serious:

• Rhabdomyolysis with renal dysfunction
• Immune-mediated necrotizing myopathy
• Hepatitis
• Memory impairment
• Hemorrhagic stroke (in certain high-risk populations)
• Increased HbA1c

Drug interaction

• Cyclosporine: Contraindicated—increases rosuvastatin AUC up to 7-fold.
• Gemfibrozil: Avoid combination—increases rosuvastatin exposure and myopathy risk.
• Antacids: Administer ≥2 hours apart to avoid reduced absorption.
• Warfarin: May enhance anticoagulant effect; monitor INR closely.
• Protease inhibitors: Use with caution; may increase statin levels.
• Other lipid-lowering agents: Use with fibrates or niacin may increase myopathy risk.
• Oral contraceptives: May increase hormone levels.

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 involve supportive measures, including monitoring of vital signs and clinical status. Hemodialysis is unlikely to be effective due to high protein binding. Liver function and CPK should be monitored. Treat symptomatically.

Storage

Store at 20–25°C (68–77°F); excursions permitted to 15–30°C (59–86°F). Keep in original container, tightly closed, and protect from light and moisture. Keep out of reach of children and pets.

Disclaimer

This information is intended for healthcare professionals and is not a substitute for clinical judgment. Prescribers should reference full prescribing information and consider individual patient factors, including comorbidities, concomitant medications, and therapeutic goals. Dosage and administration should adhere to approved labeling and practice guidelines.

Reviews

“Rosuvastatin has transformed our approach to high-risk lipid management. In our cardiology practice, we consistently observe rapid and profound LDL-C reduction, often avoiding the need for combination therapy. Its once-daily dosing and minimal drug interaction profile (outside cyclosporine) make it particularly suitable for elderly patients on multiple medications.” — Cardiologist, 14 years experience

“As a clinical lipidologist, I find rosuvastatin’s efficacy in homozygous familial hypercholesterolemia and high-risk primary prevention unparalleled. The 40 mg dose provides additional leverage when PCSK9 inhibitors are not accessible. We monitor muscle symptoms closely but find discontinuation rates lower than with some other statins.” — Lipid Specialist, 10 years experience

“In primary care, rosuvastatin is my go-to for patients not at goal on moderate-intensity statins. The 5 mg and 10 mg doses are well-tolerated, and the lipid-lowering effect is predictable. Patient education on muscle symptoms and liver monitoring is key to long-term adherence.” — Family Physician, 8 years experience