Crestor Generic Name & Formulations
Mechanism of Action
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.
Crestor Dosage and Administration
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.
Active liver disease or decompensated cirrhosis.
Crestor Boxed Warnings
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.
In clinical pharmacology studies in man, peak plasma concentrations of rosuvastatin were reached 3–5 hours following oral dosing. The absolute bioavailability of rosuvastatin is ~20%.
Mean volume of distribution at steady-state of rosuvastatin is ~134 liters. Rosuvastatin is 88% bound to plasma proteins, mostly albumin.
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.
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).
Crestor Adverse Reactions
Crestor Clinical Trials
Crestor Patient Counseling