Tablets: 5 mg, 10 mg, 20 mg, 40 mg
As adjunctive therapy to diet to reduce elevated total-C, LDL-C, Apo B, non-HDL-C, and TG levels (Fredrickson Type IV), primary dysbetalipoproteinemia (Fredrickson Type III hyperlipoproteinemia), and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and nonfamilial), and mixed dyslipidemia (Fredrickson Type IIa and IIb): Initiate therapy with 10 mg once daily. Patients with less aggressive LDL-C reductions or who have predisposing factors for myopathy may be started on 5 mg. Patients with marked hypercholesterolemia (LDL-C >190 mg/dL) may be started on 20 mg. The maintenance dose range is from 5-40 mg once daily. The 40 mg dose is reserved for those patients who have not achieved their LDL-C goal using the 20 mg dose.
To reduce LDL-C, total-C, and Apo B in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments: The recommended starting dose is 20 mg once daily. The maximum daily dose is 40 mg.
As an adjunct to diet to slow the progression of atherosclerosis by lowering total-C and LDL-C: 10-20 mg daily.
Monitor: LFT, Lipid panel
Pharmacology/Pharmacokinetics:
Rosuvastatin is a selective, competitive inhibitor of HMG-CoA reductase. This enzyme is responsible for the conversion of HMG-CoA to mevalonate, an early rate-limiting step in the synthesis of cholesterol. It increases the number of LDL receptors on the surface cell, thereby increasing uptake and catabolism of LDL (low-density lipoprotein) and inhibits the hepatic synthesis of VLDL (very low-density lipoprotein). Rosuvastatin reduces total cholesterol, LDL-C, apo B (apolipoprotein), VLDL-C, and triglycerides and produces variable increases in HDL and apolipoprotein, A-1. Rosuvastatin is not extensively metabolized and is excreted in the feces. The elimination half-life of rosuvastatin is 19 hours.
Drug Interactions:
CYCLOSPORIN coadministration increase rosuvastatin plasma levels by 7-11-fold. Use with warfarin produces clinically significant rises in INR. Use with gemfibrozil increases rosuvastatin plasma levels two-fold. Use with fenofibrate does not produce significant changes in the plasma levels of either drug. Coadministration (within 2 hours) of ANTACIDS significantly decreases rosuvastatin plasma levels.
Contraindications/Precautions:
Contraindicated in patients with active liver disease or with unexplained persistent elevations of serum transaminases and during pregnancy and lactation. Use in women of childbearing age only when such patients are highly unlikely to conceive and have been informed of the potential hazards. Use with caution in patients who consume substantial quantities of alcohol and/or have a history of liver disease. It is recommended that liver function be performed before and at 12 weeks following any increase in doses. May cause rare cases of severe myopathy and rhabdomyolysis, therefore use with caution in patients with renal impairment, advanced age (>65 years), and hypothyroidism. Patients should report any signs of unexplained muscle pain or weakness to their physician. Pregnancy Category X.
Adverse Effects:
Most frequent adverse effects include myalgia, constipation, asthenia, abdominal pain, and nausea. Patients should report any signs of muscle pain or weakness, especially if accompanied by malaise or fever, to their physician.
Contact a physician if symptoms of myopathy occur (e.g., muscle pain or tenderness, especially if accompanied by malaise or fever).
Closely follow prescribed diet.
Do not become pregnant during therapy. If pregnancy occurs or is suspected, discontinue medication and consult physician.
Limit alcohol intake during therapy.
Store in a cool, dry place away from sunlight and children.
If a dose is missed, take it as soon as possible. If more than 8 hours has lapsed between the time the dose was to be taken, skip it and return to normal dosing schedule.
