pitavastatin
Brand: Livalo, Zypitamag
Prototype: atorvastatin
Drug Class: HMG-CoA reductase inhibitor (statin)
Drug Family: antilipemic
Subclass: synthetic statin
Organ Systems: cardiovascular
Mechanism of Action
Competitively inhibits HMG-CoA reductase, reducing hepatic cholesterol synthesis and upregulating LDL receptors; notable for minimal CYP450 metabolism, conferring a favorable drug interaction profile.
HMG-CoA reductase
Indications
- primary hyperlipidemia
- mixed dyslipidemia
- cardiovascular risk reduction
Contraindications
- active liver disease
- pregnancy
- breastfeeding
- concomitant cyclosporine
Adverse Effects
Common
- myalgia
- back pain
- constipation
- elevated transaminases
Serious
- rhabdomyolysis
- myopathy
- hepatotoxicity
Pharmacokinetics (ADME)
| Absorption | approximately 51% oral bioavailability; peak at 1 hour |
| Distribution | extensive protein binding; Vd approximately 148 L |
| Metabolism | minimal CYP2C9 involvement; primary pathway via glucuronidation (UGT1A3, UGT2B7); largely CYP-independent |
| Excretion | fecal (>90%) via biliary excretion |
| Half-life | approximately 12 hours |
| Onset | days to weeks |
| Peak | 1 hour |
| Duration | 24 hours |
| Protein Binding | >99% |
| Vd | approximately 148 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| cyclosporine | inhibits OATP1B1; markedly increases pitavastatin exposure — contraindicated | major |
| erythromycin | OATP1B1 inhibition increases pitavastatin AUC approximately 2-fold | moderate |
| rifampin | OATP1B1 induction and UGT induction reduce pitavastatin levels | moderate |
Nursing Considerations
- Administer at any time of day without regard to meals; the consistent schedule improves adherence.
- Monitor liver function tests at baseline and if symptoms of hepatic injury develop; routine periodic monitoring is not required by current labeling.
- Counsel patients to report unexplained muscle pain, weakness, or dark urine; obtain creatine kinase if myopathy is suspected.
- Confirm absence of pregnancy before initiating; advise women of childbearing potential to use effective contraception throughout therapy.
Clinical Pearls
- Pitavastatin's minimal CYP450 metabolism makes it an attractive option in HIV-positive patients on antiretroviral therapy, where CYP3A4 drug interactions are common.
- Unlike most statins, pitavastatin does not significantly affect insulin sensitivity; some evidence suggests it may be less diabetogenic than other statins at equivalent doses.
Safety Profile
Pregnancy contraindicated
Lactation contraindicated
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
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