Dosing and uses of Livalo (pitavastatin)
Adult dosage forms and strengths
tablet
- 1mg
- 2mg
- 4mg
Hypercholesterolemia
2 mg PO qDay
May increase to 4 mg PO qDay if necessary
Renal Impairment
Moderate-to-severe (CrCl 15-60 mL/min/1.73 m²): 1 mg PO qDay initially; not to exceed 2 mg PO qDay
End stage renal disease: 1 mg PO qDay initially; not to exceed 2 mg PO qDay
Hepatic Impairment
Contraindicated in active liver disease or unexplained transaminase elevations
Pediatric dosage forms and strengths
Safety and efficacy not established
Livalo (pitavastatin) adverse (side) effects
Frequency not defined
Constipation
Diarrhea
Back pain
Joint pain
Myalgias
Myopathy
Rhabdomyolysis
Increased alkaline phosphatase
Increased bilirubin
Increased CPK
Increased blood glucose
Reversible amnesia
Memory impairment
Hyperglycemia
Confusion
Pruritus
Urticaria
Rash
Nasopharyngitis
Warnings
Contraindications
Hypersensitivity
Active liver disease or persistent unexplained elevations of hepatic transaminases
Pregnancy
Breastfeeding
Concurrent use wit cyclosporine
Cautions
Non-serious and reversible cognitive side effects may occur
Increased blood sugar and glycosylated hemoglobin (HbA1c) levels reported with statin intake
Caution in history of liver or renal impairment
If symptoms of hepatotoxicity (hyperbilirubinemia or jaundice) occurs, discontinue therapy; if no alternate etiology explains the symptoms do not restart therapy
Heavy alcohol use
Risk of rhabdomyolysis
Myopathy, risk of myopathy increases when coadministered with fibrates, niacin, cyclosporine, colchicine, and CYP2C9 inhibitors (eg, fluconazole, gemfibrozil, nevirapine, sulfisoxazole)
Withhold or discontinue if myopathy develops, renal failure, or transaminase levels >3x ULn
Rare reports of immune-mediated necrotizing myopathy (IMNM), characterized by increased serum creatine kinase that persist despite discontinuing statin
Pregnancy and lactation
Pregnancy category: X
Lactation: Contraindicated
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 of Livalo (pitavastatin)
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: 2-4wks
Distribution
Protein Binding: >99%
Metabolism
Metabolism: Hepatic via UGT1A3 and UGT2B7; minimally through CYP2C9 and OATP1B1
Elimination
Half-Life: 12 hr
Excretion: Feces (79%); urine (15%)
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 (https://optiviabio.com/index.html)
