Indication
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
Pharmacology
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.
Dosage
Dose range: 5-40 mg once daily. Use 40 mg dose only for patients not reaching LDL-C goal with 20 mgHoFH: 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.
Interaction
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.
Contradiction
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
Side Effect
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.
Pregnancy
The safety in pregnant women has not been established. It is not known whether Rosuvastatin is excreted in human milk or not.
Precaution
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
Overdose
Storage
Keep below 30oC temperature, protected from light & moisture. Keep out of the reach of children.