Rosutin

Indications

Rosuvastatin is indicated for patients with primary hyperlipidemia and mixed dyslipidemia as an adjunct to diet to reduce elevated total-C, LDL-C, ApoB, non HDL-C and TG levels and to increase HDL-C; patients with hypertriglyceridemia as an adjunct to diet; and patients with primary dysbetalipoproteinemia (Type III hyperlipoproteinemia) as an adjunct to diet.

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. It increases the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL and inhibits hepatic synthesis of VLDL, reducing the total number of VLDL and LDL particles.

Dosage & Administration

• Children 10 to 17 years with heterozygous familial hypercholesterolemia: 5-20 mg/day; maximum recommended dose 20 mg/day. Doses should be individualized according to the treatment goal, with adjustments at intervals of 4 weeks or more.
• Very high cholesterol and high risk of MI or stroke: 40 mg once daily.
• Homozygous familial hypercholesterolemia: Starting dose 20 mg once daily. Response should be estimated from preapheresis LDL-C levels.
• Asian patients: Initiation with 5 mg once daily should be considered.
• With Cyclosporine: Limit the dose to 5 mg once daily.
• With Lopinavir/Ritonavir or Atazanavir/Ritonavir: Limit the dose to 10 mg once daily.
• With Niacin or Fenofibrate: A reduction in Rosuvastatin dosage should be considered because of increased risk of skeletal muscle effects.
• With Gemfibrozil: Combination should be avoided; if used, limit Rosuvastatin to 10 mg once daily.
• Severe renal impairment: For patients with ClCr<30 mL/min/1.73 m² who are not on hemodialysis, start at 5 mg once daily and do not exceed 10 mg once daily.

Interaction

• Cyclosporine: Increases Rosutin exposure; limit the dose to 5 mg once daily.
• Gemfibrozil: Avoid the combination; if used together, limit the dose to 10 mg once daily.
• Lopinavir/Ritonavir or Atazanavir/Ritonavir: Increases Rosutin exposure; limit the dose to 10 mg once daily.
• Coumarin anticoagulants: May prolong INR. Stable INR should be achieved before starting Rosutin, with frequent monitoring until stable after initiation or dose alteration.
• Fibrates and niacin: May increase the risk of skeletal muscle effects.

Contraindications

• 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 Effects

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

Pregnancy & Lactation

Rosuvastatin should be administered to women of childbearing age only when they are highly unlikely to conceive and have been informed of the potential hazards. If pregnancy occurs while taking this drug, therapy should be discontinued immediately. It is not known whether Rosuvastatin is excreted in human milk, but a small amount of another drug in this class does pass into breast milk.

Precautions & Warnings

Rosutin should be prescribed with caution in patients with factors predisposing to myopathy, such as age over 65 years, inadequately treated hypothyroidism and renal impairment. The risk of myopathy may increase with Fibrates, Niacin, Gemfibrozil, Cyclosporine, Lopinavir/Ritonavir or Atazanavir/Ritonavir. Discontinue Rosutin if markedly elevated creatinine kinase levels occur or myopathy is diagnosed or suspected. Temporarily withhold therapy in acute, serious conditions suggestive of myopathy or predisposing to renal failure secondary to rhabdomyolysis. Liver enzyme tests are recommended before treatment, at 12 weeks after initiation and after dose increases, and periodically thereafter.

Overdose Effects

There is no specific treatment for overdose. Treatment should be symptomatic with supportive measures as required. Hemodialysis does not significantly enhance clearance of Rosutin.

Storage Conditions

Keep below 30°C, protected from light and moisture. Keep out of the reach of children.