HMG-CoA reductase is the rate-limiting enzyme that transforms 3-hydroxy-3-methyl glutaryl coenzyme A to mevalonate, a precursor of cholesterol. Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase. Rosuvastatin has two mechanisms for altering lipid levels. To begin, it boosts the amount of hepatic LDL receptors on the cell surface, which improves LDL absorption and degradation. Second, Rosuvastatin lowers the overall amount of VLDL and LDL particles by inhibiting VLDL production in the liver.
Dosage & Administration
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.
Rosuvastatin can be taken with or without food, at any time of day.
Remarkable drug interactions of Rosuvastatin are-
Cyclosporine: Combination increases Rosuvastatin exposure. Rosuvastatin dose should be limited to 5 mg once daily.
Gemfibrosil: Combination should be avoided. If used together, Rosuvastatin dose should be limited to 10 mg once daily.
Lopinavir/Ritonavir or atazanavir/ritonavir: Combination increases Rosuvastatin exposure. Rosuvastatin dose should be to 10 mg once daily.
Coumarin anticoagulants: Combination prolongs international normalized ratio (INR). Stable INR should be achieved prior to starting Rosuvastatin. INR should be monitored frequently until stable upon initiation or alteration of Rosuvastatin therapy.
Concomitant lipid-lowering therapies: Use with fibrates and niacin products may increase the risk of skeletal muscle effects.
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
Rosuvastatin is well tolerated by most people. Headache, myalgia, constipation, asthenia, stomach discomfort, and nausea were the most common side effects linked to Rosuvastatin.
Pregnancy & Lactation
The safety of the drug in pregnant women has yet to be determined. Rosuvastatin is not known whether or whether it is excreted in human milk.
Precautions & Warnings
Effects on skeletal muscle (e.g., myopathy and rhabdomyolysis): Usage of the 40 mg dosage, advanced age (>65 years), hypothyroidism, renal impairment, and use of cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, or some other lipid-lowering medications all enhance the risks. Patients should be encouraged to report any unexplained muscular discomfort, soreness, or weakness as soon as possible. If indications or symptoms occur, rosuvastatin can be stopped.
Abnormalities in liver enzymes and monitoring: Hepatic transaminases might be persistently elevated.
Before and throughout therapy, liver enzymes should be checked.
Other Anti-anginal & Anti-ischaemic drugs, Statins
Keep below 30oC temperature, protected from light & moisture. Keep out of the reach of children.