原發性高膽固醇血症

Antilipemic Agent, 2-Azetidinone; Antilipemic Agent, HMG-CoA Reductase Inhibitor

Ezetimibe:
Onset of action: Within 1 week; Maximum effect: 2 to 4 weeks.
Protein binding: >90% to plasma proteins.
Half-life elimination: 22 hours.
Time to peak, plasma: 4-12 hours (ezetimibe); 1-2 hours (active metabolite); Effects: ~2 weeks.
Excretion: Feces (78%, 69% as ezetimibe); urine (11%, 9% as metabolite).
Rosuvastatin:
Onset of action: Within 1 week; maximal at 4 weeks.
Distribution: 134 L.
Protein binding: 88%.
Metabolism: Hepatic (10%), via CYP2C9.
Bioavailability: 20% (high first-pass extraction by liver).
Half-life elimination: 19 hours.
Time to peak, plasma: 3 to 5 hours.
Excretion: Feces (90%).

Hypersensitivity to rosuvastatin, ezetimibe, or any component of the formulation; acute liver failure or decompensated cirrhosis.

X

Ezetimibe:
1% to 10%: increased serum transaminases, arthralgia (3%), sinusitis (3%), upper respiratory tract infection (4%).
Rosuvastatin:
>10%:myalgia (2% to 13%).
1% to 10%:diabetes mellitus, constipation (3% to 5%), nausea (4% to 6%), increased serum transaminases, asthenia (5%), dizziness (4%), headache (6% to 9%), arthralgia (4% to 10%), increased creatine phosphokinase in blood specimen (3%).

Take once daily ranging from 10/10 mg to 10/20 mg. Maximum: ezetimibe/rosuvastatin 10 mg /20 mg once daily.
When combined with bile acid-binding resin, it should have been administered 2 hours before or 4 hours after the administration of bile acid-binding resin.

CrCl <30 mL/minute/1.73 m2: maximum: 1 tab a day.

systemic exposure of rosuvastatin may be increased in patients with liver disease (increased AUC and Cmax); use is contraindicated in active liver disease or decompensated cirrhosis.