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 number of hepatic LDL receptors on the cell surface, which improves LDL absorption and degradation. Second, Rosuvastatin decreases the total quantity of VLDL and LDL particles by inhibiting VLDL formation 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.
The following are notable Rosuvastatin medication interactions: Cyclosporine: When used together, Rosuvastatin exposure is increased. The daily dose of rosuvastatin should be kept to 5 mg.
The combination should be avoided with gemfibrozil. If taken concurrently, the dose of rosuvastatin should be kept at 10 mg once a day.
The combination of coumarin anticoagulants increases the international normalized ratio (INR). Prior to commencing Rosuvastatin, make sure your INR is stable. When starting or stopping Rosuvastatin medication, the INR should be checked often until it is stable.
Concurrent lipid-lowering therapies: Using fibrates and niacin products at the same time may raise the risk of skeletal muscle side effects.
Rosuvastatin is contraindicated in the following situations: Known hypersensitivity to product ingredients Liver disease, including unexplained persistent increases in hepatic transaminase levels Pregnant women and women who may become pregnant Nursing mothers.
Rosuvastatin is well tolerated by most people. Headache, myalgia, constipation, asthenia, stomach pain, 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
Skeletal muscle effects (e.g., myopathy and rhabdomyolysis): The risk of myopathy and rhabdomyolysis increases with the use of the 40 mg dose, advanced age (>65 years), hypothyroidism, renal impairment, and combination use with cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, or certain other lipid-lowering drugs. Patients should be encouraged to report any unexplained muscle discomfort, soreness, or weakness as soon as possible. If indications or symptoms arise, rosuvastatin can be stopped.
Abnormalities in liver enzymes and monitoring: Hepatic transaminases might be persistently elevated.
Before and during treatment, liver enzymes should be checked.
Statins and other anti-anginal and anti-ischemic medications.
Keep the temperature below 30°C and keep it away from light and moisture. Keep out of children's reach.