Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methyl glutaryl coenzyme A to mevalonate, a precursor of cholesterol. Rosuvastatin produces its lipid-modifying effects in two ways. First, it increases the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL. Second, Rosuvastatin inhibits hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles.

Rosuvastatin is indicated in-

• Heterozygous Hypercholesterolemia (Familial and Non familial)
• Homozygous Hypercholesterolemia (Familial)
• Mixed Dyslipidemia (Fredrickson Type IIa and IIb)
• Primary prevention of cardiovascular disease

Dose range: 5-40 mg once daily. Use 40 mg dose only for patients not reaching LDL-C goal with 20 mg

HoFH: Starting dose 20 mg/day.

Pediatric patients with HeFH: 5-10 mg/day for patients 8 to less than 10 years age, and 5-20 mg/day for patients 10 to 17 years of age.

Pediatric patients with HoFH: 20 mg/day for patients 7 to 17 years of age.

Administration

Rosuvastatin can be taken with or without food, at any time of day.

Rosuvastatin is contraindicated if-

• Known hypersensitivity to product components
• Liver disease, which may include unexplained persistent elevations in hepatic transaminase levels
• Pregnant women and women who may become pregnant
• Nursing mothers

Rosuvastatin is generally well tolerated. The most frequent adverse events thought to be related to Rosuvastatin were headache, myalgia, constipation, asthenia, abdominal pain and nausea.

Skeletal muscle effects (e.g., myopathy and rhabdomyolysis): Risks increase with use of 40 mg dose, advanced age (>65 year), hypothyroidism, renal impairment and combination use with cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir or certain other lipid-lowering drugs. Patients should be advised to promptly report unexplained muscle pain, tenderness or weakness. Rosuvastatin can be discontinued if signs or symptoms appear.

Liver enzyme abnormalities and monitoring: Persistent elevations in hepatic transaminases can occur.

Liver enzymes should be monitored before and during treatment

Use in Special Populations

Use in children: The safety and effectiveness in pediatric patients have not been established.

Pregnancy & Lactation

The safety in pregnant women has not been established. It is not known whether Rosuvastatin is excreted in human milk or not.