Trade Names:Livalo- Tablets 1 mg- Tablets 2 mg- Tablets 4 mg
Increases rate at which body removes cholesterol from blood and reduces production of cholesterol by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis.
Rapidly absorbed; T max is 1 h. Absolute bioavailability of oral solution is 51%. Food decreases C max by 43% but does not significantly reduce AUC.
Vd is approximately 148 L. More than 99% protein bound.
Major metabolite is the lactone, formed by glucuronidation. Marginally metabolized by CYP2C9 and 2C8.
Urine (15%), feces (79%); half-life of approximately 12 h
AUC and C max were 79% and 60% higher in patients with CrCl 30 to 60 mL/min and 86% and 40% higher in patients with ESRD on hemodialysis, respectively. The effect of mild and severe renal impairment on exposure is not known. Do not use in patients with severe renal impairment not yet on hemodialysis.Hepatic Function Impairment
Half-life was 15, 10, and 8 h for patients with moderate hepatic impairment, mild hepatic impairment, and healthy hepatic function, respectively.Elderly
C max and AUC were 10% and 30% higher, respectively, in elderly patients compared with younger patients.Gender
C max and AUC were 60% and 54% higher, respectively, in women compared with men.Race
C max and AUC were 21% and 5% lower, respectively, in black patients compared with white patients.
Adjunct to diet to reduce elevated total cholesterol, LDL-C, apolipoprotein B, and triglycerides, and to increase HDL-C in adults with primary hyperlipidemia or mixed dyslipidemia.
Active liver disease; women who are pregnant or may become pregnant; breast-feeding mothers; coadministration with cyclosporine; hypersensitivity to any component.
PO Start with 2 mg once daily (max, 4 mg/day; range, 1 to 4 mg/day).Coadministration with erythromycin
PO Do not exceed 1 mg/day.Coadministration with rifampin
PO Do not exceed 2 mg/day.Renal Function Impairment
PO Mild renal impairment (CrCl 30 to less than 60 mL/min) or ESRD on hemodialysis, start with 1 mg once daily (max, 2 mg/day). Severe renal impairment (CrCl less than 30 mL/min and not on hemodialysis), use is not recommended.
Store at 59° to 86°F. Protect from light.
Pitavastatin C max and AUC may be increased more than 6- and 4-fold, respectively. Coadministration is contraindicated.Digoxin
Digoxin and pitavastatin exposure may be decreased slightly. These changes are not likely to be clinically important.Enalapril
Pitavastatin plasma concentrations may be decreased slightly and enalapril exposure may be decreased slightly. These changes are not likely to be clinically important.Erythromycin
Pitavastatin C max and AUC may be increased more than 3- and 2-fold, respectively. The pitavastatin dosage should not exceed 1 mg once daily.Ezetimibe
Ezetimibe and pitavastatin exposure may be increased slightly. These changes are not likely to be clinically important.Fibric acids (eg, fenofibrate, gemfibrozil)
Pitavastatin exposure may be increased. The risk of myopathy may be increased. Use with caution, monitoring serum creatine kinase.Grapefruit juice
Concomitant use of grapefruit juice and pitavastatin decreased the pitavastatin C max slightly and increased the AUC slightly. The changes are not likely to be clinically important.Itraconazole
Pitavastatin exposure may be reduced about 20%. A clinically important interaction is unlikely. However, monitor the clinical response of the patient and adjust the pitavastatin dose as needed.Niacin
The risk of myopathy may be increased. Use with caution. Consider reducing the pitavastatin dose.Protease inhibitors (eg, atazanavir, ritonavir/lopinavir)
Protease inhibitor exposure may be increased. Avoid coadministration of pitavastatin and ritonavir/lopinavir. Monitor the clinical response of the patient when starting or stopping atazanavir. Adjust the pitavastatin dose as needed.Rifampin
Pitavastatin C max may be reduced approximately 2-fold and the AUC approximately 29%, while rifampin exposure may be decreased approximately 15%. The pitavastatin dosage should not exceed 2 mg once daily.Warfarin
Monitoring PT and INR is recommended when starting pitavastatin in patients receiving warfarin.
None well documented.
Constipation (4%); diarrhea (3%).
Elevated alkaline phosphatase, bilirubin, creatine phosphokinase, glucose, and transaminases.
Back pain (4%); myalgia (3%); arthralgia, pain in extremity (2%).
Headache, hypersensitivity reactions (eg, rash, pruritis, urticaria), influenza, nasopharyngitis.
Analyze lipid levels 4 weeks after initiation of therapy or dosage titration. Monitor liver enzymes before and 12 wk after initiation of therapy or dosage titration, and periodically (eg, semiannually) thereafter. Monitor patients who develop increased transaminases until the abnormalities resolve.
Category X .
Safety and effectiveness not established.
Greater sensitivity of some older individuals cannot be ruled out.
Patients with moderate renal impairment (CrCl 30 to less than 60 mL/min) and ESRD on hemodialysis should receive decreased initial and maintenance dosages.
Contraindicated in patients with active liver disease.
Increases in transaminases have been reported. Use with caution in patients who consume substantial quantities of alcohol and/or have a history of chronic liver disease.
Rhabdomyolysis with renal dysfunction secondary to myoglobinuria has been reported. The risk of myopathy may be increased if coadministered with fibrates or lipid-modifying doses of niacin. Temporarily withhold therapy in any patient experiencing an acute or serious condition predisposing to the development of renal failure secondary to rhabdomyolysis (eg, hypotension, sepsis). Discontinue therapy if markedly elevated creatine kinase levels occur or if myopathy is diagnosed or suspected.
Copyright © 2009 Wolters Kluwer Health.