pitavastatin (Rx)

Brand and Other Names:Livalo, Zypitamag, more...Nikita
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

Livalo is the calcium salt of pitavastatin

Zypitamag is the magnesium salt of pitavastatin

Nikita is the sodium salt of pitavastatin

tablet

  • 1mg
  • 2mg
  • 4mg

Hypercholesterolemia

Indicated for primary hyperlipidemia or mixed dyslipidemia as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C)

Recommended starting dose: 2 mg PO qDay

May increase to 4 mg PO qDay if necessary

Dosage Modifications

Interactions

  • Coadministration with erythromycin: Not to exceed pitavastatin 1 mg/day
  • Coadministration with rifampin: Not to exceed pitavastatin 2 mg/day

Renal impairment

  • Moderate-to-severe (CrCl 15-60 mL/min/1.73 m²) or ESRD: 1 mg PO qDay initially; not to exceed 2 mg/day

Hepatic impairment

  • Contraindicated in active liver disease or unexplained transaminase elevations

Dosage Forms & Strengths

Livalo is the calcium salt of pitavastatin

tablet

  • 1mg
  • 2mg
  • 4mg

Heterozygous Familial Hypercholesterolemia

Livalo only

Indicated for heterozygous familial hypercholesterolemia (HeFH) to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), and apolipoprotein B (Apo B) in children aged ≥8 years

<8 years: Safety and efficacy not established

≥8 years

  • Recommended starting dose: 2 mg PO qDay
  • May increase to 4 mg PO qDay if necessary

Dosage Modifications

Interactions

  • Coadministration with erythromycin: Not to exceed pitavastatin 1 mg/day
  • Coadministration with rifampin: Not to exceed pitavastatin 2 mg/day

Renal impairment

  • Moderate-to-severe (CrCl 15-60 mL/min/1.73 m²) or ESRD: 1 mg PO qDay initially; not to exceed 2 mg/day

Hepatic impairment

  • Contraindicated in active liver disease or unexplained transaminase elevations

Dosing Considerations

Individualize dose according to patient characteristics, goal of therapy, and response

After initiation or upon titration, analyze lipid levels after 4 weeks and adjust the dosage accordingly

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Interactions

Interaction Checker

and pitavastatin

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            Adverse Effects

            1-10%

            Back pain (1.4-3.9%)

            Constipation (1.5-3.6%)

            Diarrhea (1.5-2.6%)

            Myalgia (1.9-3.1%)

            Pain in extremity (0.6-2.3%)

            Postmarketing Reports

            Gastrointestinal disorders: Abdominal discomfort, abdominal pain, dyspepsia, nausea

            General disorders: Asthenia, fatigue, malaise, dizziness

            Hepatobiliary disorders: Hepatitis, jaundice, fatal and nonfatal hepatic failure

            Immune system disorders: Immune-mediated necrotizing myopathy-associated with statin use

            Metabolism and nutrition disorders: Increases in HbA1c, fasting serum glucose levels

            Musculoskeletal and connective tissue disorders: Muscle spasms, myopathy, rhabdomyolysis

            Nervous system disorders: Hypoesthesia, peripheral neuropathy

            Psychiatric disorders: Insomnia, depression; rare reports of cognitive impairment (eg, memory loss, forgetfulness, amnesia, memory impairment, confusion) associated with statin use; cognitive impairment was generally nonserious, and reversible upon discontinuation, with variable times to symptom onset (1 day to years) and symptom resolution (median of 3 weeks)

            Reproductive system and breast disorders: Erectile dysfunction

            Respiratory, thoracic and mediastinal disorders: Interstitial lung disease

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            Warnings

            Contraindications

            Hypersensitivity

            Active liver disease or persistent unexplained elevations of hepatic transaminases

            Pregnancy

            Breastfeeding

            Concurrent use with cyclosporine

            Cautions

            Increased HbA1c and fasting serum glucose levels reported with statins; optimize lifestyle measures, including regular exercise, maintaining healthy body weight, and making healthy food choices

            Hepatic dysfunction

            • Increased serum transaminases reported; typically, elevations are transient and either resolved or improved on continued therapy or after briefly interrupting therapy
            • There have been rare postmarketing reports of fatal and nonfatal hepatic failure in patients taking statins
            • Consuming substantial quantities of alcohol and/or a history of liver disease may increase risk
            • Assess liver transaminases before initiating and thereafter, when clinically indicated
            • Contraindicated with active liver disease including unexplained persistent elevations in hepatic transaminase levels
            • Promptly discontinue if serious hepatic injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs

            Myopathy

            • Myopathy (muscle pain, tenderness, or weakness with creatine kinase [CK] >10 x ULN) and rhabdomyolysis (with or without acute renal failure secondary to myoglobinuria) reported with statins; rare fatalities have occurred as a result of rhabdomyolysis
            • Myopathy risk factors include: age ≥65 yr, uncontrolled hypothyroidism, renal impairment, coadministration of drugs that decrease statin clearance or add to myopathy risk
            • Pitavastatin doses >4 mg/day were associated with increased risk for severe myopathy in clinical trials
            • Steps to prevent or reduce myopathy/rhabdomyolysis risk
              • See Drug Interaction Overview or Drug Interaction Checker for drugs that are contraindicated (eg, cyclosporine), not recommended (eg, gemfibrozil), require pitavastatin dosage modification (eg, erythromycin, rifampin), and other drugs that may increase myopathy or rhabdomyolysis risk
              • Discontinue if markedly elevated CK levels occur or myopathy is diagnosed or suspected; muscle symptoms and CK increases may resolve following discontinuation
              • Temporarily discontinue in patients experiencing an acute or serious condition at high risk of developing renal failure secondary to rhabdomyolysis (eg, sepsis; shock; severe hypovolemia; major surgery; trauma; severe metabolic, endocrine, or electrolyte disorders; uncontrolled epilepsy)
              • Inform patients of risk when starting or increasing dose
              • Instruct patients to promptly report any unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever
            • Immune-mediated necrotizing myopathy
              • Rare reports of immune-mediated necrotizing myopathy (IMNM) associated with statin use IMNM characterized by proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuing statins
              • Muscle biopsy shows necrotizing myopathy without significant inflammation, which improves with immunosuppressive agents
              • Additional neuromuscular and serologic testing may be necessary
              • Treatment with immunosuppressive agents may be required

            Drug interaction overview

            • Contraindicated: Coadministration with cyclosporine
            • Not recommended: Coadministration with gemfibrozil
            • Dosage modifications for pitavastatin: Coadministration with erythromycin or rifampin
            • The following drugs may also increase myopathy and/or rhabdomyolysis risk if coadministered: Lipid-modifying dosages of niacin (>1 g/day), fibrates, and colchicine
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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 to therapy during pregnancy; therapy should be discontinued as soon as pregnancy is recognized

            May cause fetal harm when administered to a pregnant woman; advise females of reproductive potential to use effective contraception during therapy

            Lactation

            Contraindicated during breastfeeding; there is no available information on effects of drug on breastfed infant or effects of drug on milk production; however, another drug in this class passes into human milk; because of potential for serious adverse reactions in a breastfed infant, advise patients 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: 51%

            Peak plasma time: 1 hr

            Onset: 2-4 weeks

            Distribution

            Protein binding: >99%

            Metabolism

            Metabolism: Hepatic via UGT1A3 and UGT2B7; minimally through CYP2C9 and OATP1B1

            Elimination

            Half-life: 12 hr

            Excretion: 79% feces; 15% urine

            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 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 more 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%)

            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 compared with TT homozygotes

            Genetic testing laboratories

            • Optivia Biotechnology, Inc (http://optiviabio.com/index.html)
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            Formulary

            FormularyPatient Discounts

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            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.
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            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.
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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.