atorvastatin (Rx)

Brand and Other Names:Lipitor
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 10mg
  • 20mg
  • 40mg
  • 80mg
more...

Hyperlipidemia

Primary hypercholesterolemia and mixed dyslipidemia

  • Indicated as an adjunct to diet for treatment of elevated total-C, Apo B, and TG levels and to increase HDL-C in patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (Fredrickson type IIa and IIb)
  • 10-20 mg PO qDay initially
  • Starting dose in patients requiring larger LDL-C reduction (ie, >45%): 40 mg PO qDay
  • Maintenance: 10-80 mg PO qDay
  • After initiation and/or upon dose titration, check lipid levels after 2-4 weeks and adjust dose accordingly

Hypertriglyceridemia

  • Adjunct to diet for elevated TG levels (Fredrickson type IV)
  • 10 mg PO qDay initially
  • Maintenance: 10-80 mg PO qDay maintenance
  • After initiation and/or upon dose titration, check lipid levels after 2-4 weeks and adjust dose accordingly

Primary dysbetalipoproteinemia

  • Dysbetalipoproteinemia (Fredrickson type III) in patient with inadequate response to diet
  • Maintenance: 10-80 mg PO qDay
  • After initiation and/or upon dose titration, check lipid levels after 2-4 weeks and adjust dose accordingly

Homozygous familial hypercholesterolemia

  • Reduction of total-C and LDL-C in HoFH as an adjunct to other lip-lowering treatments (eg, LDL apheresis) or if such treatments are unavailable
  • 10-80 mg PO qDay

Cardiovascular Disease Prevention

10-80 mg PO qDay

Indications

  • Reduction of risk of stroke and heart attack in type 2 diabetes patients without evidence of heart disease but with other CV risk factors
  • Reduction of risk of stroke, heart attack, and revascularization procedures in patients without evidence of coronary heart disease (CHD) but with multiple risk factors other than diabetes (eg, smoking, HTN, low HDL-C, family history of early CHD)
  • Patients with CHD, to reduce risks of MI, stroke, revascularization procedures, hospitalization for CHF, and angina

Dosage Modifications

Coadministration with other drugs

  • Bile acid sequestrant: Administer atorvastatin/ezetimibe ≥2 hr before or ≥4 hr after administering bile acid sequestrant
  • Cyclosporine, tipranavir plus ritonavir, gemfibrozil: Avoid coadministration with atorvastatin (increased risk of rhabdomyolysis)
  • Lopinavir plus ritonavir: Use lowest dose of atorvastatin necessary
  • Clarithromycin, itraconazole, saquinavir plus ritonavir, darunavir plus ritonavir, fosamprenavir: Do not exceed atorvastatin dose of 20 mg/day
  • Nelfinavir: Do not exceed atorvastatin dose of 40 mg/day

Dosing Considerations

Overdose management

  • Generally considered safe in acute overdose, although not formally studied
  • 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

Dosage Forms & Strengths

tablet

  • 10mg
  • 20mg
  • 40mg
  • 80mg
more...

Heterozygous Familial Hypercholesterolemia

Indicated as an adjunct to diet to reduce total-C, LDL-C, and apo B levels in boys and postmenarchal girls aged 10-17 years with HeFH who have an inadequate response to diet alone (ie, LDL-C remains ≥190 mg/dL or LDL-C remains ≥160 mg/dL and there is positive family history or early CV disease or 2 or more other CVD risk factors present)

<10 years: Safety and efficacy not established

≥10 years: Initially, 10 mg PO qDay; titrate at 4-week intervals; not to exceed 20 mg PO qDay

Homozygous Familial Hypercholesterolemia (Off-label)

<10 years: Safety and efficacy not established

≥10 years: 10-40 mg PO qDay

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Interactions

Interaction Checker

and atorvastatin

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     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Diarrhea (5-14%)

            Nasopharyngitis (4-13%)

            Arthralgia (4-12%)

            1-10%

            Insomnia (1-5%)

            Urinary tract infection (4-8%)

            Nausea (4-7%)

            Dyspepsia (3-6%)

            Increased transaminases (2-3%)

            Muscle spasms (2-5%)

            Musculoskeletal pain (2-5%)

            Myalgia (3-8%)

            Limb pain (3-8%)

            Pharyngolaryngeal pain (1-4%)

            Frequency Not Defined

            Angina

            Syncope

            Dyspnea

            Myopathy

            Anaphylaxis

            Stevens-Johnson syndrome

            Myositis

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            Warnings

            Contraindications

            Hypersensitivity to atorvastatin

            Active liver disease or unexplained transaminase elevation

            Pregnancy, lactation

            Cautions

            Nonserious and reversible cognitive side effects may occur

            Increased blood sugar and glycosylated hemoglobin (HbA1c) levels reported with statin intake

            Use with caution in the elderly; risk of myopathy

            Heavy alcohol use, renal failure, history of liver disease

            Fatal and nonfatal hepatic failure reported (rare)

            Risk of rhabdomyolysis

            Risk of myopathy: Increased by coadministration with fibrates, niacin, cyclosporine, macrolides, telaprevir, boceprevir, combinations of HIV protease inhibitors (eg, saquinavir plus ritonavir, lopinavir plus ritonavir, tipranavir plus ritonavir, darunavir plus ritonavir, fosamprenavir, and fosamprenavir plus ritonavir), or azole antifungals

            Withhold or discontinue treatment in any patient developing myopathy, renal failure, or transaminase levels >3x ULN

            Temporary therapy discontinuation recommended for patients with acute surgical or medical conditions, elective major surgery, or serious condition suggestive of a myopathy or risk factor predisposing to development of renal failure secondary to rhabdomyolysis

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

            Use caution in hepatic impairment, recent stroke

            CYP3A4 substrate; avoid grapefruit products and caution with other CYP3A4 inhibitors

            Secondary causes of hyperlipidemia should be ruled out before initiating therapy

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            Pregnancy & Lactation

            Pregnancy

            Contraindicated for use in pregnant women since safety in pregnant women has not been established and there is no apparent benefit of lipid lowering drugs during pregnancy; because HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, therapy may cause fetal harm when administered to a pregnant woman; discontinue therapy as soon as pregnancy is recognized; limited published data are insufficient to determine a drug-associated risk of major congenital malformations or miscarriage

            Contraception

            • Advise females of reproductive potential to use effective contraception during treatment

            Lactation

            Use is contraindicated during breastfeeding; there is no available information on effects of drug on breastfed infant or on milk production.; not known whether atorvastatin is present in human milk; it has been shown that another drug in this class passes into human milk and atorvastatin is present in rat milk; because of potential for serious adverse reactions in breastfed infant, advise women that breastfeeding is not recommended during treatment

            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 rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase

            Absorption

            Bioavailability: 14% (parent drug)

            Onset: 3-5 days

            Duration: 48-72 hr

            Peak serum time: 1-2 hr

            Maximum effect: 2 weeks

            Distribution

            Protein bound: 98%

            Vd: 381 L

            Metabolism

            Via hepatic P450 enzyme CYP3A4

            Metabolites: Ortho- and parahydroxylated derivatives and beta-oxidation product (inactive)

            Elimination

            Half-life: 14 hr

            Dialyzable: No (HD)

            Excretion: Mainly via bile; urine (2%)

            Pharmacogenomics

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

            This polymorphism is proposed to reduce transport into the liver, the main site of statin metabolism and elimination

            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, 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%)

            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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            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.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the 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.