Dosing & Uses
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
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

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
Warnings
Contraindications
Hypersensitivity to drug or excipients
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
- 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
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.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)
Images
Patient Handout
Formulary
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