pitavastatin (Rx)

Brand and Other Names:Livalo, Zypitamag
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

Livalo is the calcium salt of pitavastatin

Zypitamag is the magnesium salt of pitavastatin

tablet

  • 1mg
  • 2mg
  • 4mg

Primary Hyperlipidemia and Mixed Dyslipidemia Adjunct 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

Zypitamag is the magnesium 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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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (6)

            • atazanavir

              atazanavir increases levels of pitavastatin by unknown mechanism. Contraindicated. Potential for increased toxicity. .

            • cyclosporine

              cyclosporine increases toxicity of pitavastatin by Other (see comment). Contraindicated. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • gemfibrozil

              gemfibrozil increases toxicity of pitavastatin by Other (see comment). Contraindicated. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • letermovir

              letermovir increases levels of pitavastatin by Other (see comment). Contraindicated. Comment: Coadministration of letermovir and pitavastatin is not recommended. When letermovir is coadministered with cyclosporine, use of either pitavastatin is contraindicated due to significantly increased pitavastatin concentrations and risk of myopathy or rhabdomyolysis. .

            • lopinavir

              lopinavir increases levels of pitavastatin by decreasing metabolism. Contraindicated.

            • red yeast rice

              pitavastatin, red yeast rice. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. May increase creatine kinase levels and increase risk of myopathy or rhabdomyolysis; red yeast rice contains monocolin K (reportedly identical to lovastatin).

            Serious - Use Alternative (14)

            • colchicine

              colchicine, pitavastatin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Increased risk of rhabdomyolysis (incl a fatality).

            • darolutamide

              darolutamide will increase the level or effect of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Darolutamide is a BCRP inhibitor. Avoid coadministration with BCRP inhibitors. If use is unavoidable, closely monitor for adverse reactions and consider dose reduction of BCRP substrate drug (refer BCRP substrate prescribing information).

            • eltrombopag

              eltrombopag increases toxicity of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • erythromycin base

              erythromycin base increases levels of pitavastatin by decreasing metabolism. Avoid or Use Alternate Drug. Do not exceed 1 mg/d pitavastatin.

              erythromycin base increases toxicity of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate increases levels of pitavastatin by decreasing metabolism. Avoid or Use Alternate Drug. Do not exceed 1 mg/d pitavastatin.

              erythromycin ethylsuccinate increases toxicity of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • erythromycin lactobionate

              erythromycin lactobionate increases levels of pitavastatin by decreasing metabolism. Avoid or Use Alternate Drug. Do not exceed 1 mg/d pitavastatin.

              erythromycin lactobionate increases toxicity of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • erythromycin stearate

              erythromycin stearate increases levels of pitavastatin by decreasing metabolism. Avoid or Use Alternate Drug. Do not exceed 1 mg/d pitavastatin.

              erythromycin stearate increases toxicity of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • fenofibrate

              fenofibrate, pitavastatin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Fenofibrate may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs.

            • fenofibrate micronized

              fenofibrate micronized, pitavastatin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Fenofibrate may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs.

            • fenofibric acid

              fenofibric acid, pitavastatin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Fenofibrate may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs.

            • gemfibrozil

              gemfibrozil, pitavastatin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Gemfibrozil may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs.

            • lasmiditan

              lasmiditan increases levels of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: Lasmiditan inhibits BCRP in vitro. Avoid coadministration of lasmiditan with BCRP substrates.

            • niacin

              niacin, pitavastatin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Increased risk of rhabdomyolysis (>1 g/day niacin).

            • rifampin

              rifampin increases toxicity of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            Monitor Closely (44)

            • acalabrutinib

              acalabrutinib increases levels of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: Acalabrutinib may increase exposure to coadministered BCRP substrates by inhibition of intestinal BCRP.

            • apalutamide

              apalutamide will decrease the level or effect of pitavastatin by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces BCRP and OATP1B1 and may decrease systemic exposure of drugs that are substrates of both BCRP and OATP1B1.

            • carbamazepine

              carbamazepine increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • caspofungin

              caspofungin increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • cholestyramine

              cholestyramine decreases levels of pitavastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • cholic acid

              pitavastatin increases toxicity of cholic acid by decreasing elimination. Modify Therapy/Monitor Closely. Avoid concomitant use of inhibitors of the bile salt efflux pump (BSEP). May exacerbate accumulation of conjugated bile salts in the liver and result in clinical symptoms. If concomitant use is necessary, monitor serum transaminases and bilirubin.

            • clarithromycin

              clarithromycin increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • clotrimazole

              clotrimazole increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • cobicistat

              cobicistat will increase the level or effect of pitavastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. For HMG-CoA reductase inhibitors that are not contraindicated with cobicistat, start with the lowest recommended dose and titrate while monitoring for safety.

            • crofelemer

              crofelemer increases levels of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: Crofelemer has the potential to inhibit transporters MRP2 and OATP1A2 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • daptomycin

              pitavastatin, daptomycin. Either increases toxicity of the other by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration of daptomycin with HMG-CoA reductase inhibitors may increase CPK levels and risk for myopathy; consider temporary suspension of HMG-CoA reductase inhibitors during daptomycin therapy.

            • darunavir

              darunavir will increase the level or effect of pitavastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. For HMG-CoA reductase inhibitors that are not contraindicated with darunavir, start with the lowest recommended dose and titrate while monitoring for safety.

            • eluxadoline

              eluxadoline increases levels of pitavastatin by decreasing metabolism. Use Caution/Monitor. Eluxadoline may increase the systemic exposure of coadministered OATP1B1 substrates.

            • fostemsavir

              fostemsavir will increase the level or effect of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits OATP1B1/3 and BCRP transporters. If possible, avoid coadministration or modify dose of OATP1B1/3 or BCRP substrates coadministered with fostemsavir. Use lowest possible starting dose for statins and monitor for associated adverse events.

            • glecaprevir/pibrentasvir

              glecaprevir/pibrentasvir increases levels of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. Use lowest approved dose of pitavastatin. If a higher dose is needed, use the lowest necessary statin dose based on a risk/benefit assessment.

            • glyburide

              glyburide increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • indinavir

              indinavir increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • ketoconazole

              ketoconazole increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • lanthanum carbonate

              lanthanum carbonate decreases levels of pitavastatin by cation binding in GI tract. Use Caution/Monitor. Administer statin at least 2 hr before or 2 hr after lanthanum. Monitor serum concentrations.

            • metyrapone

              metyrapone increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • mifepristone

              mifepristone increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • mipomersen

              mipomersen increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs; OATP1B1 inhibitors may increase risk of myopathy.

            • nelfinavir

              nelfinavir increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • ombitasvir/paritaprevir/ritonavir & dasabuvir

              ombitasvir/paritaprevir/ritonavir & dasabuvir increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • paclitaxel

              paclitaxel increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • pazopanib

              pazopanib increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • pioglitazone

              pioglitazone increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • ponatinib

              ponatinib increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • ranolazine

              ranolazine increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • regorafenib

              regorafenib will increase the level or effect of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Regorafenib likely inhibits BCRP (ABCG2) transport. Coadministration with a BCRP substrate may increase systemic exposure to the substrate and related toxicity.

            • rifampin

              rifampin increases levels of pitavastatin by decreasing metabolism. Use Caution/Monitor. Do not exceed 2 mg/d pitavastatin.

            • ritonavir

              ritonavir increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • rosiglitazone

              rosiglitazone increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • sacubitril/valsartan

              sacubitril/valsartan increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • safinamide

              safinamide will increase the level or effect of pitavastatin by Other (see comment). Use Caution/Monitor. Safinamide and its major metabolite may inhibit intestinal BCRP. Monitor BCRP substrates for increased pharmacologic or adverse effects.

            • saquinavir

              saquinavir increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • sofosbuvir/velpatasvir

              sofosbuvir/velpatasvir increases levels of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Comment: Velpatasvir is an inhibitor of OATP1B1, OATP1B3, and OATP2B1 transporters. Coadministration may increase systemic exposure of drugs that are substrates of these transporters. Coadministration may significantly increase pitavastatin serum concentration, which is associated with increased risk of myopathy, including rhabdomyolysis.

            • stiripentol

              stiripentol will increase the level or effect of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Stiripentol is a CYP2C8 and BCRP transport inhibitor. Consider dosage reduction for BCRP substrates if adverse effects are experienced when coadministered.

            • tacrolimus

              tacrolimus increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • tafamidis

              tafamidis will increase the level or effect of pitavastatin by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.

            • tafamidis meglumine

              tafamidis meglumine will increase the level or effect of pitavastatin by Other (see comment). Use Caution/Monitor. Tafamidis inhibits breast cancer resistant protein (BCRP) in vitro and may increase exposure of BCRP substrates following tafamidis or tafamidis meglumine administration. Dosage adjustment of these BCRP substrates may be necessary.

            • telmisartan

              telmisartan increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            • teriflunomide

              teriflunomide increases levels of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.

            • valsartan

              valsartan increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.

            Minor (6)

            • coenzyme Q10

              pitavastatin decreases levels of coenzyme Q10 by unspecified interaction mechanism. Minor/Significance Unknown.

            • colestipol

              colestipol decreases levels of pitavastatin by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • isradipine

              isradipine decreases levels of pitavastatin by unknown mechanism. Minor/Significance Unknown.

            • orlistat

              orlistat increases effects of pitavastatin by pharmacodynamic synergism. Minor/Significance Unknown.

            • trazodone

              trazodone increases levels of pitavastatin by unspecified interaction mechanism. Minor/Significance Unknown.

            • voclosporin

              voclosporin will increase the level or effect of pitavastatin by Other (see comment). Minor/Significance Unknown. Information suggests voclosporin (an OATP1B1 inhibitor) may increase in the concentration of OATP1B1 substrates is possible. Monitor for adverse reactions of OATP1B1 substrates when coadministered with voclosporin.

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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; angioedema

            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 to drug or excipients

            Active liver disease or persistent unexplained elevations of hepatic transaminases

            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
              • Immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, reported with statin use
              • IMNM is characterized by muscle biopsy showing necrotizing myopathy without significant inflammation improvement with immunosuppressive agents, proximal muscle weakness, and elevated serum creatine kinase, which persist despite discontinuation of statin treatment
              • Treatment with immunosuppressive agents may be required
              • Advice all patients starting therapy or whose dose is being increased, about the risk of myopathy, including rhabdomyolysis
              • Patients should report promptly any unexplained muscle pain, tenderness, or weakness particularly if accompanied by malaise or fever or if muscle signs and symptoms persist after discontinuing therapy; additional neuromuscular and serologic testing may be necessary
              • Therapy should be discontinued immediately if myopathy is diagnosed or suspected
              • Discontinue therapy if markedly elevated creatine kinase (CK) levels occur or if myopathy diagnosed or suspected
              • Therapy should be temporarily withheld in any patient experiencing an acute or serious condition predisposing to development of renal failure secondary to rhabdomyolysis, eg, sepsis; hypotension; dehydration; major surgery; trauma; severe metabolic, endocrine, and electrolyte disorders; or uncontrolled epilepsy
              • Consider risk of IMNM carefully prior to initiation of a different statin
              • If therapy is initiated with a different statin, monitor for signs and symptoms of IMNM
              • Additional neuromuscular and serologic testing may be necessary
              • Treatment with immunosuppressive agents may be required
              • Consider risk of IMNM carefully prior to initiation of a different statin
              • If therapy is initiated with a different statin, monitor for signs and symptoms of IMNM

            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

            Owing to HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, fetal harm may occur when administered to pregnant females; 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

            FDA MedWatch

            • On July 20, 2021, the FDA request to remove the contraindication against HMG-CoA reductase inhibitors in pregnant females
            • Despite the changes, most females found to be pregnant should stop therapy

            Lactation

            There is no available information on effects of drug on breastfed infant or on milk production

            Unknown whether is present in human milk; it has been shown that drugs in this class pass into human milk and atorvastatin is present in rat milk

            Not recommended during treatment

            FDA MedWatch

            • On July 20, 2021, the FDA request to remove the contraindication against HMG-CoA reductase inhibitors in pregnant females
            • Breastfeeding is still not recommended if taking statins; drug may still pass through milk and pose a risk breastfed children
            • For patients with lower risk, temporarily stop statin therapy until breastfeeding ends
            • Patients who are at high risk of heart attack or stroke who require statins after delivery should not breastfeed and should use alternatives such as infant formula

            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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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Livalo oral
            -
            4 mg tablet
            Livalo oral
            -
            2 mg tablet
            Livalo oral
            -
            1 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            pitavastatin calcium oral

            PITAVASTATIN - ORAL

            (pit-A-va-STAT-in)

            COMMON BRAND NAME(S): Livalo, Zypitamag

            USES: Pitavastatin is used along with a proper diet to help lower "bad" cholesterol and fats (such as LDL, triglycerides) and raise "good" cholesterol (HDL) in the blood. It belongs to a group of drugs known as "statins." It works by reducing the amount of cholesterol made by the liver. Lowering "bad" cholesterol and triglycerides and raising "good" cholesterol decreases the risk of heart disease and helps prevent strokes and heart attacks.In addition to eating a proper diet (such as a low-cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking. Consult your doctor for more details.

            HOW TO USE: Take this medication by mouth with or without food as directed by your doctor, usually once daily.Dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).If you also take certain other drugs to lower your cholesterol (bile acid-binding resins such as cholestyramine or colestipol), take pitavastatin at least 1 hour before or at least 4 hours after taking these medications. These products can react with pitavastatin, preventing its full absorption.Take this medication regularly in order to get the most benefit from it. Remember to take it at the same time each day. Keep taking this medication even if you feel well. Most people with high cholesterol or triglycerides do not feel sick.It is very important to continue to follow your doctor's advice about diet and exercise. It may take up to 4 weeks before you get the full benefit of this drug.

            SIDE EFFECTS: Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.A very small number of people taking pitavastatin may have mild memory problems or confusion. If these rare effects occur, talk to your doctor.Rarely, statins may cause or worsen diabetes. Talk to your doctor about the benefits and risks.This drug may rarely cause muscle problems (which can rarely lead to very serious conditions called rhabdomyolysis and autoimmune myopathy). Tell your doctor right away if you develop any of these symptoms during treatment and if these symptoms persist after your doctor stops this drug: muscle pain/tenderness/weakness (especially with fever or unusual tiredness), signs of kidney problems (such as change in the amount of urine).This medication may rarely cause liver problems. If you notice any of the following serious side effects, tell your doctor right away: stomach/abdominal pain, persistent nausea/vomiting, yellowing eyes/skin, dark urine.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking pitavastatin, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, alcohol use.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Limit alcoholic beverages. Daily use of alcohol may increase your risk for liver problems, especially when combined with pitavastatin. Ask your doctor or pharmacist for more information.Older adults may be more sensitive to the side effects of this drug, especially muscle problems.This medication must not be used during pregnancy. Pitavastatin may harm an unborn baby. It is important to prevent pregnancy while taking this medication. Consult your doctor for more details and to discuss the use of reliable forms of birth control (such as condoms, birth control pills) while taking this medication. If you become pregnant or think you may be pregnant, tell your doctor right away. Discuss with your doctor when you should stop pitavastatin if you are trying to become pregnant.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: colchicine, daptomycin, gemfibrozil.Other medications can affect the removal of pitavastatin from your body, which may affect how pitavastatin works. Examples include cyclosporine, letermovir, macrolide antibiotics (such as erythromycin), rifamycins (such as rifampin), sofosbuvir/velpatasvir/voxilaprevir, among others.Do not take any red yeast rice products while you are taking pitavastatin because some red yeast rice products may also contain a statin called lovastatin. Taking pitavastatin and red yeast rice products together can increase your risk of serious muscle and liver problems.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Laboratory and/or medical tests (such as blood cholesterol/triglyceride levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
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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.