原發性性膽固醇醇症及混合型型脂異常與10歲以上兒童家族性性膽固醇

Antilipemic Agent, HMG-CoA Reductase Inhibitor

Distribution: ~148 L.
Protein binding: >99%, primarily to albumin and alpha 1-acid glycoprotein.
Metabolism: Hepatic, via UGT1A3 and UGT2B7; minimal metabolism via CYP2C9 and CYP2C8.
Bioavailability: 51%.
Half-life elimination: ~12 hours.
Time to peak, plasma: ~1 hour.
Excretion: Feces (79%); urine (15%).

Hypersensitivity to pitavastatin or any component of the formulation; active liver disease or decompensated cirrhosis; coadministration with cyclosporine.

Concerns related to adverse effects:
1. Diabetes mellitus: increases in HbA1c and fasting blood glucose.
2. Hepatotoxicity: elevations in serum transaminases.
3. Hypersensitivity: angioedema, rash, pruritus, and urticarial.
4. Myopathy/Rhabdomyolysis: myopathy with CPK >10 times the ULN and rhabdomyolysis (sometimes fatal) with or without acute renal failure secondary to myoglobinuria.

1. Heterozygous familial hypercholesterolemia: moderate-intensity therapy: 1 to 4 mg once daily.
2. Prevention of atherosclerotic cardiovascular disease (off-label use) : 1 to 4 mg once daily.

Familial hypercholesterolemia (FH): Children ≥10 years and Adolescents: Initial: 1mg once daily; maximum daily dose: 2 mg/day. Lipid levels should be evaluated 4 weeks after any dose adjustment.

GFR 15 to 59 mL/minute/1.73 m2 (not receiving hemodialysis): Initial: 1 mg once daily; maximum: 2 mg/day.
ESRD receiving hemodialysis: Initial: 1 mg once daily; maximum: 2 mg/day

Contraindicated in active liver disease or decompensated cirrhosis.