Rosuvastatin

DEA Class; Rx

Common Brand Names; Crestor, Ezallor Sprinkle

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

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