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Rosuvastatin/Ezetimibe

    Brands

    DEA Class; Rx

    Common Brand Names; Roszet

    • Lipid-Lowering Agents, 2-Azetidinones; 
    • Lipid-Lowering Agents, Statins

    Rosuvastatin

    • HMG-CoA reductase inhibitor; inhibits the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase

    Ezetimibe

    • Blocks GI cholesterol absorption via NPC1L1 (Niemann-Pick C1-Like 1) inhibition, reducing cholesterol deliver to the liver

    • This action reduces hepatic cholesterol stores and increases LDL receptors, resulting in clearance of cholesterol from the blood

    • NPC1L1 is a sterol transporter that mediates intestinal cholesterol absorption

    Indicated as an adjunct to diet for primary nonfamilial hyperlipidemia to reduce LDL-C

    Indicated alone or with other LDL-C lowering therapies in adults with homozygous familial hypercholesterolemia (HoFH) to recue LDL-C

    Acute liver failure or decompensated cirrhosis.

    Hypersensitivity to rosuvastatin, ezetimibe, or any excipients in drug product(s)

    Rosuvastatin 

    • Myalgia (2.8-12.7%)

    • Arthralgia (10.1%)

    • Headache (5.5-6.4%)

    • Dizziness (4%)

    • Nausea (3.4%)

    • Asthenia (2.7%)

    • Increased CPK (2.6%)

    • Constipation (2.4%)

    • Abdominal (2.4%)

    • ALT >3x ULN (2.2%)

    Ezetimibe

    • Diarrhea (4.1%)

    • Arthralgia (3%)

    • Sinusitis (2.8%)

    • Pain in extremity (2.7%)

    • Fatigue (2.4%)

    • Influenza (2%)

    • Nasopharyngitis (3.7%)

    • Myalgia (3.2%)

    • Upper respiratory tract infection (2.9%)

    • Arthralgia (2.6%)

    • Diarrhea (2.5%)

    • Back pain (2.4%)

    • Influenza (2.2%)

    • Pain in extremity (2.1%)

    • Fatigue (2%)

    Increased fasting 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; optimize lifestyle measures, including regular exercise, maintaining a healthy body weight, and making healthy food choices

    Hematuria and proteinuria reported in clinical trials; findings were more frequent with rosuvastatin 40 mg compared to lower doses of rosuvastatin or other statins; effects are generally transient and was not associated with worsening renal function; consider dosage reduction if unexplained hematuria and proteinuria persists

    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

    Dosage range: Rosuvastatin/ezetimibe 10mg/10mg to 40mg/10mg PO qDay

    Pediatric

    Safety and efficacy not established

    Rosuvastatin/ezetimibe

    tablet

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