Generic Name and Formulations:
Rosuvastatin (as calcium) 5mg, 10mg, 20mg, 40mg; tabs.
Indications for CRESTOR:
As an adjunct to diet in primary hyperlipidemia and mixed dyslipidemia to reduce elevated total-C, LDL-C, ApoB, non-HDL-C, and TG, and to increase HDL-C. Adjunct to diet in hypertriglyceridemia. Adjunct to diet in primary dysbetalipoproteinemia (Type III hyperlipoproteinemia). Adjunct to other lipid-lowering treatments (or if these treatments are unavailable), in homozygous familial hypercholesterolemia (HoFH) to reduce LDL-C, total-C, and ApoB. Adjunct to diet to slow the progression of atherosclerosis as part of a treatment strategy to lower total-C and LDL-C to target levels. To reduce risk of MI, stroke, or arterial revascularization procedures in patients without clinically evident CHD but with an increased risk of CVD based on age (men ≥50yrs, women ≥60yrs), hs-CRP ≥2mg/L, and at least one additional risk factor. Pediatric patients 8–17yrs of age with heterozygous familial hypercholesterolemia (HeFH) to reduce elevated total-C, LDL-C and ApoB after failing an adequate trial of diet therapy. Pediatric patients 7–17yrs of age with HoFH to reduce LDL-C, total-C, non-HDL-C, and ApoB as adjunct to diet, either alone or with other lipid-lowering therapies.
Limitations Of use:
Not studied in Fredrickson Type I and V dyslipidemias.
Swallow whole. Take once daily. Dose range 5–40mg. HoFH: initially 20mg. All others: usual starting dose 10–20mg. Use max 40mg dose only if 20mg is insufficient. Asian patients: consider 5mg initially (see full labeling). Concomitant cyclosporine: max 5mg. Concomitant simeprevir, lopinavir/ritonavir or atazanavir/ritonavir: max 10mg. Concomitant gemfibrozil: avoid; if needed, max 10mg. Severe renal impairment (CrCl <30mL/min) not on hemodialysis: initially 5mg; max 10mg.
HeFH: <8yrs: not established. 8–<10yrs: usual range 5–10mg/day; 10–17yrs: 5–20mg/day. HoFH: <7yrs: not studied. 7–17yrs: 20mg once daily.
Active liver disease. Unexplained persistent elevated serum transaminases. Pregnancy. Nursing mothers.
Discontinue if myopathy or elevated CK levels occur; suspend if a predisposition to development of renal failure secondary to rhabdomyolysis develops. Monitor liver function before starting therapy and as clinically indicated. Interrupt therapy if serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs; do not restart if alternate etiology not found. History of liver disease or heavy alcohol ingestion. Severe renal impairment. Hypothyroidism (if inadequately treated). Asian patients. Elderly. Females of reproductive potential must use effective contraception during treatment.
HMG-CoA reductase inhibitor.
See Adult. Avoid gemfibrozil. Increased risk of myopathy with niacin (≥1g/day), fibrates, inhibitors of certain transporter proteins including OATP1B1 and BCRP (eg, cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, simeprevir), colchicine; use caution. Monitor with anticoagulants. Caution with drugs that decrease levels or activity of steroid hormones (eg, ketoconazole, spironolactone, cimetidine). Separate dosing of antacids (give ≥2hrs after rosuvastatin).
Headache, myalgia, abdominal pain, asthenia, nausea; myopathy, rhabdomyolysis with renal dysfunction, elevated liver enzymes, proteinuria and hematuria (consider dose reduction if persistent), increased HbA1c and fasting serum glucose, rare: cognitive impairment, hepatic failure, immune-mediated necrotizing myopathy.
Tabs 5mg, 10mg, 20mg—90; 40mg—30