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Rosuvastatin

    DEA Class; Rx

    Common Brand Names; Crestor, Ezallor Sprinkle

    • Lipid-Lowering Agents, Statins; 
    • HMG-CoA Reductase Inhibitors

    Most potent, oral HMG-CoA reductase inhibitor
    Approved for primary hypercholesterolemia, hyperlipoproteinemia and/or hypertriglyceridemia, heterozygous familial hypercholesterolemia (for patients 8 to 17 years), homozygous familial hypercholesterolemia (for patients 7 years and older), and primary prevention of cardiovascular disease
    Limited metabolism; less potential for CYP3A4 drug interactions compared to simvastatin or lovastatin

    Indicated for the treatment of hypercholesterolemia, including hyperlipidemia, hyperlipoproteinemia, or hypertriglyceridemia, as an adjunct to dietary control.

    For primary prevention of cardiovascular disease including myocardial infarction prophylaxis and stroke prophylaxis, and to reduce the risk of arterial revascularization procedures in patients without evidence of coronary heart disease but who have risk factors for cardiovascular disease.

    Hypersensitivity

    Active liver disease (including unexplained persistent elevations of LFTs)

    • Myalgia (3-13%)
    • Arthralgia (10%)
    • Pharyngitis (9%)
    • Headache (3.1-8.5%)
    • Myalgia (7.6%)
    • Nausea (2.4-6.3%)
    • Asthenia (0.9-6.3%)
    • Constipation (2.1-4.7%)
    • Dizziness (4%)
    • Arthralgia (3.8%)
    • CPK increased (3%)
    • Diabetes mellitus (2.8%)
    • Abdominal pain (2%)
    • ALT increased (2%)
    • Flulike illness (2%)
    • UTI (2%)
    • <1%
    • Jaundice
    • Myopathy
    • Rhabdomyolysis
    • Arthralgia
    • Peripheral neuropathy
    • Depression and sleep disorders (including insomnia and nightmares)
    • Fatal and nonfatal hepatic failure, hepatitis, jaundice
    • Thrombocytopenia
    • Gynecomastia
    • Interstitial lung disease
    • Immune-mediated necrotizing myopathy
    • Cognitive impairment (eg, memory loss, forgetfulness, amnesia, memory impairment, confusion)

    Nonserious and reversible cognitive adverse effects may occur

    Increased blood glucose and glycosylated hemoglobin (HbA1c) levels reported with statin intake; in some instances, these increases may exceed the threshold for the diagnosis of diabetes mellitus

    Use caution in patients who consume large amounts of ethanol or have a history of liver disease

    Interrupt therapy if serious hepatotoxicity with clinical symptoms and/or hyperbilirubinemia or jaundice occurs during treatment

    Increases in AST or ALT reported with HMG-CoA reductase inhibitors; monitor liver enzymes before initiating and if signs or symptoms of liver injury occur

    Cases of myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria reported with HMG-CoA reductase inhibitors; may occur at any dose level, but are increased at the highest dose (40 mg); caution in patients with predisposing factors for myopathy (eg, age ≥65 years, inadequately treated hypothyroidism, renal impairment)

    Discontinue treatment if markedly elevated creatine kinase levels occur or myopathy is diagnosed or suspected; temporarily withhold in any patient with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis; hypotension; dehydration; major surgery; trauma; severe metabolic, endocrine, or electrolyte disorders; uncontrolled seizures)

    Pharmacokinetic studies demonstrated an ~2-fold elevation in median exposure (AUC and peak plasma concentrations) in Asian subjects when compared with a white control group

    Hematuria and proteinuria reported without decrease in renal function; consider dosage reduction if unexplained hematuria and proteinuria persists

    Rule out secondary causes of hyperlipidemia prior to initiating therapy

    Owing to HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, fetal harm may occur when administered to pregnant females

    There is no available information on effects of drug on breastfed infant or on milk production

    Unknown whether is present in human milk; it has been shown that drugs in this class pass into human milk and atorvastatin is present in rat milk

    Not recommended during treatment

    Adults

    40 mg/day PO.

    Geriatric

    40 mg/day PO.

    Adolescents

    20 mg/day PO (rosuvastatin tablets). Safety and efficacy of rosuvastatin capsules have not been established.

    Children

    7 to 12 years: 20 mg/day PO (rosuvastatin tablets). Safety and efficacy of rosuvastatin capsules have not been established.
    1 to 6 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    Rosuvastatin calcium

    tablet (Crestor)

    • 5mg
    • 10mg
    • 20mg
    • 40mg

    capsule (Ezallor Sprinkle)

    • 5mg
    • 10mg
    • 20mg
    • 40mg