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
- Active liver failure or decompensated cirrhosis: Contraindicated
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
- Active liver failure or decompensated cirrhosis: Contraindicated
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
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 (17)
- 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.
- leniolisib
leniolisib will increase the level or effect of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Leniolisib, a BCRP, OATP1B1, and OATP1B3 inhibitor, may increase systemic exposure of these 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).
- oteseconazole
oteseconazole will increase the level or effect of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Otesezonale, a BCRP inhibitor, may increase the effects and risk of toxicities of BCRP substrates. Use lowest starting dose of BCRP substrate, or consider reducing BCRP substrate dose.
- rifampin
rifampin increases toxicity of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- trofinetide
trofinetide will increase the level or effect of pitavastatin by Other (see comment). Avoid or Use Alternate Drug. Trofinetide (an OATP131 and OATP13B inhibitor) may increase plasma levels of OATP131 or OATP13B substrates. Avoid coadministration with sensitive substrates.
Monitor Closely (48)
- 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.
- encorafenib
encorafenib will increase the level or effect of pitavastatin by Other (see comment). Modify Therapy/Monitor Closely. Encorafenib (a OATP1B1, OATP1B3, and BCRP inhibitor) may increase the concentration and toxicities of OATP1B1, OATP1B3, and BCRP substrates. Closely monitor for signs and symptoms of increased exposure and consider adjusting the dose of these substrates. Screen reader support enabled.
- 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.
- levoketoconazole
levoketoconazole increases toxicity of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: OATP1B1 inhibitors may increase risk of myopathy.
- 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.
- momelotinib
momelotinib increases toxicity of pitavastatin by plasma protein binding competition. Modify Therapy/Monitor Closely. Momelotinib (BCRP inhibitor) may increase exposure of BCRP substrates, which may increase the risk of BCRP substrate adverse reactions. Dose adjustment of other BCRP substrates may necessary.
- 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 (DSC)
ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) 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.
- pretomanid
pretomanid will increase the level or effect of pitavastatin by Other (see comment). Use Caution/Monitor. Increase monitoring for drug-related adverse effects if pretomanid is coadministered with sensitive OATP1B3 substrates.
- 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.
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
Skin and subcutaneous tissue disorders: Lichen planus
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
- Monitor all patients with renal impairment for development of myopathy; due to risk of myopathy, dosage modification is recommended for patients with moderate and severe renal impairment
- 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
Owing to 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 pregnant patients based on mechanism of action; in addition, treatment of hyperlipidemia is not generally necessary during pregnancy;
Discontinue therapy as soon as pregnancy is recognized; atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on outcome of long-term therapy of primary hyperlipidemia for most patients
Available data from case series and prospective and retrospective observational cohort studies over decades of use with statins in pregnant women have not identified a drug-associated risk of major congenital malformations
Published data from prospective and retrospective observational cohort studies with statin use in pregnant women are insufficient to determine if there is a drug-associated risk of miscarriage
Animal data
- In animal reproduction studies, no embryo-fetal toxicity or congenital malformations were observed in pregnant rats and rabbits orally administered this drug during period of organogenesis at doses which were 22 and 4 times, respectively, the human exposure at the maximum recommended human dosage (MRHD) of 4 mg, based on AUC
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 about prescence of pitavastatin in human or animal milk, effects of drug on breastfed infant, or on milk production
It has been shown that another drug in this class passes into human milk; therapy decreases cholesterol synthesis and possibly synthesis of other biologically active substances derived from cholesterol and may cause harm to breastfed infant
Because of potential for serious adverse reactions in a breastfed infant, based upon mechanism of action, advise patients that breastfeeding is not recommended during therapy
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.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
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Livalo oral - | 1 mg tablet |  | |
| Livalo oral - | 2 mg tablet |  | |
| Livalo oral - | 4 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
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.The 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 last 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. Tell your doctor right away if you develop symptoms of liver problems, including: nausea/vomiting that doesn't stop, stomach/abdominal pain, 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.During pregnancy, this medication should be used only when clearly needed. It may harm an unborn baby. Discuss the risks and benefits with your doctor.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, 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.Lab and/or medical tests (such as blood cholesterol/triglyceride levels, liver function) should be done while you are taking this medication. Keep all medical and lab appointments. 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 January 2023. Copyright(c) 2023 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.
Formulary
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