Rosuvastatin
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alejandro Lemor, M.D. [2]
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Overview
Rosuvastatin is a HMG-CoA reductase inhibitor that is FDA approved for the {{{indicationType}}} of hyperlipidemia and mixed dyslipidemia, hypertriglyceridemia, primary dysbetalipoproteinemia (Type III hyperlipoproteinemia), homozygous familial hypercholesterolemia, slowing of the progression of atherosclerosis, primary prevention of cardiovascular disease. Common adverse reactions include headache, myalgia, abdominal pain, asthenia, and nausea.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
General Dosing Information
- Dosing Information
- 5 to 40 mg orally once daily.
Homozygous Familial Hypercholesterolemia
- Dosing Information
- 20 mg once daily
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Rosuvastatin in adult patients.
Non–Guideline-Supported Use
Acute Coronary Syndrome
Prophylaxis for Atrial Fibrillation
Prophylaxis for Cardiovascular Event in Percutaneous Coronary Intervention (PCI)
- Dosing Information
- 40 mg preprocedure
Prophylaxis for Venous Thromboembolism
- Dosing Information
- 20 mg/day
Metabolic Syndrome
- Dosing Information
- 10 mg/day
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Heterozygous Familial Hypercholesterolemia in Pediatric Patients (10 to 17 years of age)
- Dosing Information
- 5‑20 mg/day; the maximum recommended dose is 20 mg/day
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Rosuvastatin in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Rosuvastatin in pediatric patients.
Contraindications
- Patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions including rash, pruritus, urticaria, and angioedema have been reported with rosuvastatin.
- Patients with active liver disease, which may include unexplained persistent elevations of hepatic transaminase levels.
- Women who are pregnant or may become pregnant. Because HMG‑CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, rosuvastatin may cause fetal harm when administered to regnant women. Additionally, there is no apparent benefit to therapy during pregnancy, and safety in pregnant women has not been established. If the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus and the lack of known clinical benefit with continued use during pregnancy.
- Nursing mothers. Because another drug in this class passes into breast milk, and because HMG‑CoA reductase inhibitors have the potential to cause serious adverse reactions in nursing infants, women who require rosuvastatin treatment should be advised not to nurse their infants.
Warnings
Skeletal Muscle Effects
Cases of myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with HMG-CoA reductase inhibitors, including Rosuvastatin. These risks can occur at any dose level, but are increased at the highest dose (40 mg).
Rosuvastatin should be prescribed with caution in patients with predisposing factors for myopathy (e.g., age ≥ 65 years, inadequately treated hypothyroidism, renal impairment).
The risk of myopathy during treatment with Rosuvastatin may be increased with concurrent administration of some other lipid-lowering therapies (fibrates or niacin), gemfibrozil, cyclosporine, lopinavir/ritonavir, or atazanavir/ritonavir. Cases of myopathy, including rhabdomyolysis, have been reported with HMG-CoA reductase inhibitors, including rosuvastatin, coadministered with colchicine, and caution should be exercised when prescribing Rosuvastatin with colchicine.
Rosuvastatin therapy should be discontinued if markedly elevated creatine kinase levels occur or myopathy is diagnosed or suspected. Rosuvastatin therapy should also be temporarily withheld in any patient with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (e.g., sepsis, hypotension, dehydration, major surgery, trauma, severe metabolic, endocrine, and electrolyte disorders, or uncontrolled seizures).
There have been rare reports of immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, associated with statin use. IMNM is characterized by: proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuation of statin treatment; muscle biopsy showing necrotizing myopathy without significant inflammation; improvement with immunosuppressive agents.
All patients should be advised to promptly report to their physician unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever or if muscle signs and symptoms persist after discontinuing Rosuvastatin.
Liver Enzyme Abnormalities
It is recommended that liver enzyme tests be performed before the initiation of Rosuvastatin, and if signs or symptoms of liver injury occur.
Increases in serum transaminases AST (SGOT) or ALT (SGPT)] have been reported with HMG‑CoA reductase inhibitors, including Rosuvastatin. In most cases, the elevations were transient and resolved or improved on continued therapy or after a brief interruption in therapy. There were two cases of jaundice, for which a relationship to Rosuvastatin therapy could not be determined, which resolved after discontinuation of therapy. There were no cases of liver failure or irreversible liver disease in these trials.
In a pooled analysis of placebo-controlled trials, increases in serumtransaminases to >3 times the upper limit of normal occurred in 1.1% of patients taking Rosuvastatin versus 0.5% of patients treated with placebo.
There have been rare postmarketing reports of fatal and non-fatal hepatic failure in patients taking statins, including rosuvastatin. If serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs during treatment with Rosuvastatin, promptly interrupt therapy. If an alternate etiology is not found, do not restart Rosuvastatin.
Rosuvastatin should be used with caution in patients who consume substantial quantities of alcohol and/or have a history of chronic liver disease. Active liver disease, which may include unexplained persistent transaminase elevations, is a contraindication to the use of Rosuvastatin.
Concomitant Coumarin Anticoagulants
Caution should be exercised when anticoagulants are given in conjunction with Rosuvastatin because of its potentiation of the effect of coumarin-type anticoagulants in prolonging the prothrombin time/INR. In patients taking coumarin anticoagulants and Rosuvastatin concomitantly, INR should be determined before starting Rosuvastatin and frequently enough during early therapy to ensure that no significant alteration of INR occurs.
Proteinuria and Hematuria
In the Rosuvastatin clinical trial program, dipstick-positive proteinuria and microscopic hematuria were observed among Rosuvastatin treated patients. These findings were more frequent in patients taking Rosuvastatin 40 mg, when compared to lower doses of Rosuvastatin or comparator HMG‑CoA reductase inhibitors, though it was generally transient and was not associated with worsening renal function. Although the clinical significance of this finding is unknown, a dose reduction should be considered for patients on Rosuvastatin therapy with unexplained persistent proteinuria and/or hematuria during routine urinalysis testing.
Endocrine Effects
Increases in HbA1c and fasting serum glucose levels have been reported with HMG‑CoA reductase inhibitors, including Rosuvastatin. Based on clinical trial data with Rosuvastatin, in some instances these increases may exceed the threshold for the diagnosis of diabetes mellitus.
Although clinical studies have shown that Rosuvastatin alone does not reduce basal plasma cortisol concentration or impair adrenal reserve, caution should be exercised if Rosuvastatin is administered concomitantly with drugs that may decrease the levels or activity of endogenous steroid hormones such as ketoconazole, spironolactone, and cimetidine.
Adverse Reactions
Clinical Trials Experience
There is limited information regarding Rosuvastatin Clinical Trials Experience in the drug label.
Postmarketing Experience
The following adverse reactions have been identified during postapproval use of rosuvastatin : arthralgia, fatal and non-fatal hepatic failure, hepatitis, jaundice, thrombocytopenia, depression, sleep disorders (including insomnia and nightmares) and gynecomastia. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
There have been rare reports of immune-mediated necrotizing myopathy associated with statin use.
There have been rare postmarketing reports of cognitive impairment (e.g., memory loss, forgetfulness, amnesia, memory impairment, confusion) associated with statin use. These cognitive issues have been reported for all statins. The reports are generally nonserious, and reversible upon statin discontinuation, with variable times to symptom onset (1 day to years) and symptom resolution (median of 3 weeks).
Drug Interactions
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Use in Specific Populations
Pregnancy
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Labor and Delivery
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Nursing Mothers
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Pediatric Use
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Geriatic Use
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Race
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Renal Impairment
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Hepatic Impairment
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Females of Reproductive Potential and Males
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Immunocompromised Patients
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Others
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Administration and Monitoring
Administration
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Monitoring
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IV Compatibility
Solution
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Y-Site
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Admixture
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Syringe
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TPN/TNA
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Overdosage
Acute Overdose
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Management
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Chronic Overdose
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Pharmacology
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Rosuvastatin
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Clinical Studies
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Storage
There is limited information regarding Rosuvastatin Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
(Patient Counseling Information)
Precautions with Alcohol
Alcohol-Rosuvastatin interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Rosuvastatin Brand Names in the drug label.
Look-Alike Drug Names
- (Paired Confused Name 1a) — (Paired Confused Name 1b)
- (Paired Confused Name 2a) — (Paired Confused Name 2b)
- (Paired Confused Name 3a) — (Paired Confused Name 3b)
Drug Shortage Status
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References
The contents of this FDA label are provided by the National Library of Medicine.