Indications

Primary hyperlipidemia and mixed dyslipidemia as an adjunct to diet to reduce elevated Total-C, LDL-C, ApoB, non-HDL-C, and triglycerides, and to increase HDL-C.
Hypertriglyceridemia as an adjunct to diet.
Primary dysbetalipoproteinemia (Type III hyperlipoproteinemia) as an adjunct to diet.
Heterozygous familial hypercholesterolemia (HeFH) to reduce LDL-C, Total-C, and ApoB.
Slowing progression of atherosclerosis as part of a treatment strategy to lower Total-C and LDL-C.
Pediatric patients (10–17 years) with HeFH to reduce elevated Total-C, LDL-C, and ApoB after adequate dietary therapy.
Risk reduction of myocardial infarction (MI), stroke, and arterial revascularization procedures in patients without clinically evident coronary heart disease (CHD) but with multiple risk factors.

Pharmacology Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis. It lowers cholesterol by:

Increasing hepatic LDL receptors to enhance LDL uptake and catabolism.
Inhibiting hepatic synthesis of VLDL and LDL particles, reducing total circulating LDL.

Dosage & Administration

Adults:
- High cholesterol / high risk of MI or stroke: 40 mg once daily.
- Homozygous familial hypercholesterolemia: Start with 20 mg once daily.
Pediatric (10–17 years, HeFH): 5–20 mg/day; maximum 20 mg/day. Adjust every ≥4 weeks.
Asian patients: Initiate with 5 mg once daily.
With cyclosporine: Limit to 5 mg once daily.
With lopinavir/ritonavir or atazanavir/ritonavir: Limit to 10 mg once daily.
With fibrates or niacin: Use lower doses; avoid combination with gemfibrozil.
Severe renal impairment (CrCl <30 mL/min): Start at 5 mg once daily; do not exceed 10 mg/day.

Interactions

Cyclosporine: Increases exposure; limit dose to 5 mg/day.
Gemfibrozil: Avoid; if used, limit dose to 10 mg/day.
Lopinavir/Ritonavir or Atazanavir/Ritonavir: Limit dose to 10 mg/day.
Coumarin anticoagulants: May prolong INR; monitor closely.
Other lipid-lowering agents (fibrates, niacin): Increase risk of muscle toxicity.

Contraindications

Hypersensitivity to components.
Active liver disease or unexplained persistent elevation of transaminases.
Pregnancy and lactation.
Women of childbearing potential not using effective contraception.

Side Effects Generally well tolerated. Common adverse effects include headache, myalgia, constipation, asthenia, abdominal pain, and nausea.

Pregnancy & Lactation Contraindicated. Discontinue immediately if pregnancy occurs. Unknown if excreted in breast milk; avoid use during lactation.

Precautions & Warnings

Use cautiously in patients predisposed to myopathy (e.g., age >65, hypothyroidism, renal impairment).
Risk increases with concurrent fibrates, niacin, cyclosporine, or protease inhibitors.
Discontinue if markedly elevated creatine kinase or myopathy occurs.
Temporarily withhold in acute conditions predisposing to renal failure (e.g., sepsis, dehydration, trauma, major surgery).
Perform liver enzyme tests before initiation, at 12 weeks, and periodically thereafter.