HMG CoA Reductase Inhibitor
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.
Remarkable drug interactions of Rosuvastatin are-
Cyclosporine: Combination increases Rosuvastatin exposure. Rolip 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.
Hypersensitivity to Rosuvastatin or any of it’s components, active liver disease or with unexplained persistent elevations of serum transaminases.
Generally well tolerated. Myalgia, constipation, asthenia, abdominal pain, & nausea.
Not recommended. Should be administered to women of childbearing age only when such patients are highly unlikely to conceive.
There is no specific treatment in the event of overdose. In the event of overdose, the patient should be treated symptomatically and supportive measures instituted as required. Hemodialysis does not significantly enhance clearance of Rosuvastatin.
Keep below 30oC temperature, protected from light & moisture. Keep out of the reach of children.
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