Hyperlipoproteinemias:
Indications for: CRESTOR
To reduce risk of MI, stroke, or arterial revascularization procedures in adults without established CHD who are at increased risk of CVD based on age, hsCRP ≥2mg/L, and at least one additional CV risk factor. As an adjunct to diet to reduce LDL-C and slow the progression of atherosclerosis in adults. As an adjunct to diet to reduce LDL-C: in adults with primary hyperlipidemia; or in adults and children aged ≥8yrs with heterozygous familial hypercholesterolemia (HeFH). As an adjunct to other LDL-C-lowering treatments (or alone if such treatments are unavailable), to reduce LDL-C in adults and children aged ≥7yrs with homozygous familial hypercholesterolemia (HoFH). As an adjunct to diet for adults with primary dysbetalipoproteinemia or hypertriglyceridemia.
Adult Dosage:
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, darolutamide: max 5mg. Concomitant regorafenib, teriflunomide, capmatinib: max 10mg. Concomitant fostamatinib, febuxostat: max 20mg. Concomitant gemfibrozil (if unavoidable), tafamidis (if unavoidable), atazanavir/ritonavir, lopinavir/ritonavir, simeprevir, dasabuvir/ombitasvir/paritaprevir/ritonavir, elbasvir/grazoprevir, sofosbuvir/velpatasvir, glecaprevir/pibrentasvir: initiate at 5mg; max 10mg. Severe renal impairment (CrCl <30mL/min) not on hemodialysis: initially 5mg; max 10mg.
Children Dosage:
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.
CRESTOR Contraindications:
Active liver disease or decompensated cirrhosis.
CRESTOR Warnings/Precautions:
Risk for myopathy and rhabdomyolysis (esp. aged ≥65yrs, uncontrolled hypothyroidism, renal impairment, concomitant use with certain drugs, higher Crestor dosage). Discontinue if elevated CK levels or myopathy occur or if myopathy is suspected; suspend if a predisposition to development of renal failure secondary to rhabdomyolysis develops. Discontinue if immune-mediated necrotizing myopathy is suspected. Monitor liver function before starting therapy and as clinically indicated. Discontinue promptly if serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs. History of liver disease or heavy alcohol ingestion. Severe renal impairment. Hypothyroidism (if inadequately treated). Asian patients (See Adult dose). Elderly. Pregnancy: discontinue when recognized. Nursing mothers: not recommended.
CRESTOR Classification:
HMG-CoA reductase inhibitor.
CRESTOR Interactions:
See Adult dose. Avoid gemfibrozil, sofosbuvir/velpatasvir/voxilaprevir, ledipasvir/sofosbuvir. Increased risk of myopathy with niacin (≥1g/day), other fibrates, inhibitors of certain transporter proteins (eg, cyclosporine, darolutamide, regorafenib, atazanavir/ritonavir, lopinavir/ritonavir, simeprevir, dasabuvir/ombitasvir/paritaprevir/ritonavir, elbasvir/grazoprevir, sofosbuvir/velpatasvir, glecaprevir/pibrentasvir), colchicine; use caution. Monitor INR with warfarin. Caution with drugs that decrease levels or activity of steroid hormones (eg, ketoconazole, spironolactone, cimetidine). Separate dosing of aluminum/magnesium hydroxide combination antacids (give ≥2hrs after rosuvastatin).
Adverse Reactions:
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.
Drug Elimination:
Following oral administration, rosuvastatin and its metabolites are primarily excreted in the feces (90%). After an intravenous dose, ~28% of total body clearance was via the renal route, and 72% by the hepatic route. The elimination half-life of rosuvastatin is ~19 hours.
Generic Drug Availability:
YES
How Supplied:
Tabs 5mg, 10mg, 20mg—90; 40mg—30