rosuvastatin (Rx)

Brand and Other Names:Crestor, Ezallor Sprinkle
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet (Crestor)

  • 5mg
  • 10mg
  • 20mg
  • 40mg

capsule (Ezallor Sprinkle)

  • 5mg
  • 10mg
  • 20mg
  • 40mg

Hypercholesterolemia

Indicated as adjunctive therapy to diet in adults with hypertriglyceridemia, hyperlipidemia, mixed dyslipidemia, or primary dysbetalipoproteinemia

Tablets and capsules: 10-20 mg PO qDay; not to exceed 40 mg/day

After initiation or upon titration, analyze lipid levels within 2-4 weeks and adjust dosage accordingly

Homozygous Familial Hypercholesterolemia

Indicated as adjunctive therapy in adults with homozygous familial hypercholesterolemia

Tablets and capsules: 20 mg PO qDay; not to exceed 40 mg/day

After initiation or upon titration, analyze lipid levels within 2-4 weeks and adjust dosage accordingly

Slowing Progression of Atherosclerosis

Indicated as adjunctive therapy to diet to slow the progression of atherosclerosis in adult patients as part of a treatment strategy to lower total cholesterol and LDL cholesterol to target levels

Tablets and capsules: 10-20 mg PO qDay; not to exceed 40 mg/day

After initiation or upon titration, analyze lipid levels within 2-4 weeks and adjust dosage accordingly

Primary Prevention

Indicated to reduce the risk of stroke, myocardial infarction, and arterial revascularization procedures in individuals without clinically evident coronary heart disease with risk factors

Risk factors

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

Tablets: 10-20 mg PO qDay; not to exceed 40 mg/day

Dosage range 5-40 mg/day

Dosage Modifications

Dosing in Asian patients

  • Consider starting at 5 mg PO qDay, owing to increased rosuvastatin plasma concentrations
  • May increase up to 20 mg/day if patients are not adequately controlled

Dosage adjustment for rosuvastatin with concomitant therapy

  • Coadministered with cyclosporine: Do not exceed rosuvastatin 5 mg qDay
  • Coadministered with gemfibrozil: Avoid use; if use cannot be avoided, initiate rosuvastatin at 5 mg qDay; not to exceed 10mg/day
  • Coadministered with atazanavir and ritonavir, lopinavir and ritonavir, or simeprevir: Initiate rosuvastatin at 5 mg qDay; not to exceed 10mg/day

Renal impairment

  • Mild or moderate (CrCl ≥30 mL/min/1.73m²): No dosage adjustment necessary
  • Severe (CrCl <30 mL/min/1.73m²) and not on hemodialysis: Decrease starting dose to 5 mg PO qDay; not to exceed 10 mg/day

Hepatic impairment

  • Active liver disease: Contraindicated
  • Chronic alcoholic liver disease: Use with caution; known to increase rosuvastatin exposure

Dosing Considerations

Initiating therapy or switching from another HMG-CoA reductase inhibitor: Start on appropriate dose and then titrate based on patient’s response and individualized goal of therapy

Limitation of use: Not studied in Fredrickson type I and V dyslipidemias

Dosage Forms & Strengths

tablet (Crestor)

  • 5mg
  • 10mg
  • 20mg
  • 40mg

Familial Hypercholesterolemia

Heterozygous

  • Adjunctive therapy to diet to reduce total cholesterol, LDL cholesterol, and ApoB levels in children and adolescents (8-17 years) with heterozygous familial hypercholesterolemia after an inadequate response to diet therapy
  • Inadequate response defined as when the following findings are present: LDL cholesterol >190 mg/dL OR >160 mg/dL 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

  • Adjunctive therapy to diet to reduce LDL cholesterol, total cholesterol, non-HDL cholesterol, and ApoB in children and adolescents (7-17 year) 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

Dosage Modifications

Dosing in Asian patients

  • Consider starting at 5 mg PO qDay, owing to increased rosuvastatin plasma concentrations
  • May increase up to 20 mg/day if patients are not adequately controlled

Dosage adjustment for rosuvastatin with concomitant therapy

  • Coadministered with cyclosporine: Do not exceed rosuvastatin 5 mg qDay
  • Coadministered with gemfibrozil: Avoid use; if use cannot be avoided, initiate rosuvastatin at 5 mg qDay; not to exceed 10mg/day
  • Coadministered with atazanavir and ritonavir, lopinavir and ritonavir, or simeprevir: Initiate rosuvastatin at 5 mg qDay; not to exceed 10mg/day

Renal impairment

  • Mild or moderate (CrCl ≥30 mL/min/1.73m²): No dosage adjustment necessary
  • Severe (CrCl <30 mL/min/1.73m²) and not on hemodialysis: Decrease starting dose to 5 mg PO qDay; not to exceed 10 mg/day

Hepatic impairment

  • Active liver disease: Contraindicated
  • Chronic alcoholic liver disease: Use with caution; known to increase rosuvastatin exposure

Dosing Considerations

Initiating therapy or switching from another HMG-CoA reductase inhibitor: Start on appropriate dose and then titrate based on patient’s response and individualized goal of therapy

Limitation of use: Not studied in Fredrickson type I and V dyslipidemias

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Interactions

Interaction Checker

and rosuvastatin

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    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%)

            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

            Postmarketing Reports

            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)

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            Warnings

            Contraindications

            Hypersensitivity

            Active liver disease (including unexplained persistent elevations of LFTs)

            Pregnancy, lactation

            Cautions

            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

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

            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

            Drug interactions overview

            • Exercise caution when anticoagulants coadministered with rosuvastatin because of its potentiation of effect of coumarin-type anticoagulants in prolonging the prothrombin time/INR; monitor INR at baseline and frequently during concomitant therapy
            • Cyclosporine and gemfibrozil increased rosuvastatin exposure and may result in increased risk of myopathy
            • Coadministration of rosuvastatin with certain protease inhibitors has differing effects on rosuvastatin exposure and may increase risk of myopathy
            • Risk of skeletal muscle effects may be enhanced when used in combination with lipid-modifying doses (≥1 g/day) of niacin; use with caution when administered with rosuvastatin
            • Because the risk of myopathy during treatment with HMG-CoA reductase inhibitors is increased with concomitant use of fenofibrates, use with caution
            • Cases of myopathy, including rhabdomyolysis, reported with HMG-CoA reductase inhibitors when coadministered with colchicine
            • Also see Dosage Modifications
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            Pregnancy & Lactation

            Pregnancy

            Contraindicated

            Because HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly 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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            Administration

            Oral Administration

            Take with or without food

            Tablets: Swallow whole

            Capsules

            • Swallow whole; do not crush or chew
            • For patients who have difficulty swallowing capsules
              • May open capsule and carefully empty granules onto 1 tsp of applesauce; swallow immediately, without chewing
              • Do not store mixture for future use
              • If not used in its entirety, discard remaining contents immediately

            Nasogastric Tube Administration

            Open capsule and empty granules into a 60-mL catheter-tipped syringe and add 40 mL of water

            Shake syringe vigorously for 15 seconds; granules may start dissolving which is acceptable

            Attach syringe to a nasogastric tube (≥16-French) and deliver contents of syringe through nasogastric tube

            After administering granules, flush nasogastric tube with 20 mL of additional water

            Use immediately after preparation and do not store for future use

            If not used in its entirety, discard remaining contents immediately

            Use with any other liquids is not recommended

            Storage

            Capsules and tablets: Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F)

            Protect from moisture

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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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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.