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rosuvastatin (Rx)Brand and Other Names:Crestor

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 5mg
  • 10mg
  • 20mg
  • 40mg
more...

Hypercholesterolemia

Hypertriglyceridemia, hyperlipidemia, mixed dyslipidemia, slowing progression of atherosclerosis, primary dysbetalipoproteinemia

10-20 mg PO qDay initially; may titrate; not to exceed 40 mg/day

Dosage range: 5-40 mg/day

Homozygous familial hypercholesterolemia: Initiate with 20 mg PO qDay; may titrate; not to exceed 40 mg/day

Primary Prevention

Primary prevention of cardiovascular disease in individuals with no clinically evident heart disease but who are at risk because of combined effect of risk factors listed below

Approval based on JUPITER trial (Justification for the Use of statins in Prevention: an Intervention Trial Evaluation Rosuvastatin)

Initial: 10-20 mg PO qDay

Dosage range 5-40 mg/day

Cardiovascular disease

  • Shown to reduce risk of stroke, MI, and arterial revascularization procedures (including CABG, bypass grafting of peripheral artery or carotid artery, and angioplasty or stent placement)

Risk factors

  • Age (>50 yr in men; >60 yr in women), AND
  • Elevated high-sensitivity C-reactive protein level (>2 mg/L), AND
  • Presence of at least 1 additional cardiovascular risk factor (eg, high blood pressure, low HDL-C, smoking, family history of premature heart disease)

Dosing Considerations

Patients of Asian descent: Initiate with 5 mg/day

Coadministration with other lipid-lowering therapy: Consider dose reduction if combined with niacin or fenofibrate, because of increased risk for skeletal muscle effects

Coadministration with cyclosporine: Not to exceed 5 mg/day

Coadministration with gemfibrozil: Avoid if possible; if used together, do not exceed 10 mg/day

Coadministration with ritonavir, lopinavir/ritonavir, or atazanavir/ritonavir: Not to exceed 10 mg/day

Overdose management

  • Adverse drug reactions from overdose may include peripheral neuropathy, diarrhea, increased K+, myopathy, rhabdomyolysis, acute renal failure, elevated LFTs, eye lens opacities
  • Treatment is supportive

Dosing Modifications

Renal impairment

  • Severe (CrCl <30 mL/min/1.73m²) and not on hemodialysis: Decrease starting dose to 5 mg PO qDay; not to exceed 10 mg PO qDay
  • CrCl>30mL/min/1.73m²: Dose adjustment not necessary
  • Active liver disease: Use is contraindicated
  • Chronic alcoholic liver disease is known to increase rosuvastatin exposure; caution advised

Dosage Forms & Strengths

tablet

  • 5mg
  • 10mg
  • 20mg
  • 40mg
more...

Heterozygous Familial Hypercholesterolemia (HeFH)

Indicated to reduce total-C, LDL-C, and ApoB levels in children and adolescents aged 8-17 yr if after an adequate trial of diet therapy the following findings are present: LDL-C >190 mg/dL, or >160 mg/dL along with a positive family history of premature cardiovascular disease (CVD) or ≥2 CVD risk factors

<8 years: Safety and efficacy not established

8 to <10 years: 5-10 mg PO qDay

10-17 years: 5-20 mg PO qDay; may adjust dose at intervals of at least 4 wk; not to exceed 20 mg/day

Homozygous Familial Hypercholesterolemia (HoFH)

Indicated to reduce LDL-C, Total-C, nonHDL-C and ApoB in children and adolescents aged 7 to 17 yr with homozygous familial hypercholesterolemia, either alone or with other lipid-lowering treatments (eg, LDL apheresis)

<7 years: Safety and efficacy not established

7-17 years: 20 mg PO qDay

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Interactions

Interaction Checker

rosuvastatin and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Myalgia (3-13%)

            1-10%

            Arthralgia (10%)

            Diabetes mellitus, new onset (3%)

            Pharyngitis (9%)

            Headache (6%)

            Asthenia (up to 5%)

            Dizziness (4%)

            CPK increased (3%)

            Nausea (3%)

            Abdominal pain (2%)

            ALT increased (2%)

            Constipation (2%)

            Flulike illness (2%)

            UTI (2%)

            <1%

            Jaundice

            Myopathy

            Rhabdomyolysis

            Postmarketing Reports

            Arthralgia

            Peripheral neuropathy

            Depression and sleep disorders (including insomnia and nightmares)

            Fatal and nonfatal hepatic failure, hepatitis, jaundice

            Thrombocytopenia

            Gynecomastia

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            Warnings

            Contraindications

            Hypersensitivity

            Active liver disease, elevated LFTs

            Pregnancy, lactation

            Cautions

            Nonserious and reversible cognitive side effects may occur

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

            Chronic liver disease

            Measure liver enzymes before initiating and if signs or symptoms of liver injury occur

            Consider lower initial dose (5 mg qDay) in patients with risk of myopathy

            Increased risk of rhabdomyolysis, especially at highest approved dose of 40 mg/day; reserve highest dose only for patients who fail to achieve desired cholesterol level at 20 mg/day

            Use 5 mg/day starting dose in people of Asian ancestry, who may build up higher drug levels and be at higher risk of myopathy

            Rare reports of immune-mediated necrotizing myopathy (IMNM), characterized by increased serum creatine kinase that persists despite discontinuing statin

            Discontinue if CK levels are markedly elevated

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            Pregnancy & Lactation

            Pregnancy

            Contraindicated

            Because HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol (eg, cell membranes), rosuvastatin may cause fetal harm when administered to pregnant women

            Lactation

            Contraindicated

            Limited data indicate that rosuvastatin is present in human milk; because statins have the potential for serious adverse reactions in nursing infants, women who require rosuvastatin treatment should not breastfeed their infants

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

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

            Absorption

            Bioavailability: 20%

            Peak plasma time: 3-5 hr

            Distribution

            Vd: 134 L

            Protein bound: 88%

            Metabolism

            Metabolism: ~10% by hepatic CYP2C9

            Metabolites: N-desmethyl, lactone

            Elimination

            Half-Life, Elimination: 19 hr

            Excretion: Feces (90%)

            Pharmacogenomics

            Hepatic influx and efflux transporters (single-nucleotide polymorphisms [SNPs] within the solute carrier organic anion transporter 1B1 (SLCO1B1) gene, encoding the organic anion transporter polypeptide 1B1 (OATP1B1) influx transporter)

            SLCO1B1 (OATP1B1) CC genotype significantly increases AUCs of parent drug and metabolites compared with the CT or TT genotypes

            This polymorphism is proposed to reduced transport into the liver, the main site of statin metabolism and elimination, resulting in elevated plasma concentrations

            SLCO1B1 polymorphism is thought to have a lesser effect on the more hydrophilic statins (eg, rosuvastatin, fluvastatin) compared with those that are more lipophilic (eg, atorvastatin, pravastatin, simvastatin)

            Other genetic polymorphisms of elimination (eg, CYP450, P-glycoprotein) for each individual drug must also be considered, to explain variability for statin clearance among patients that exhibit SCLO1B1 polymorphism

            SLCO1B1 CC genotype is most common in Caucasians and Asians (15%); decrease dose by 50% in people of Asian descent

            Risk of myopathy is 2.6- to 4.3-fold higher if the C allele is present and 16.9-fold higher in CC homozygotes than in TT homozygotes

            Genetic testing laboratories

            • Optivia Biotechnology, Inc (http://optiviabio.com)
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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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