Ezetimibe Disease Interactions

Ezetimibe is partially metabolized in the liver. After a single 10 mg dose, the mean area under the plasma concentration-time curve (AUC) for total ezetimibe was increased approximately 1.7-fold, 3- to 4-fold, and 5- to 6-fold, in patients with mild (Child-Pugh score 5 to 6), moderate (Child-Pugh score 7 to 9), and severe hepatic impairment (Child-Pugh score 10 to 15), respectively, compared to healthy subjects. Due to the unknown effects of increased exposure to ezetimibe in patients with moderate or severe hepatic impairment, therapy with ezetimibe is not recommended in these patients. The combination of ezetimibe with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations in hepatic transaminase levels.

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Myopathy and rhabdomyolysis are known adverse reactions to statins and other lipid-lowering drugs. In post-marketing experience with ezetimibe, cases of myopathy and rhabdomyolysis have been reported. Most patients who developed rhabdomyolysis were taking a statin prior to initiating ezetimibe. However, rhabdomyolysis has been reported with ezetimibe monotherapy and with the addition of ezetimibe to agents known to be associated with increased risk of rhabdomyolysis, such as fibrates. In the presence of muscle symptoms and a CPK level >10 × the ULN indicative of myopathy, ezetimibe and any statin or fibrate that the patient is taking concomitantly should be immediately discontinued if myopathy is diagnosed or suspected.

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No dosage adjustment of ezetimibe is necessary in patients with renal impairment. However, when ezetimibe therapy is given in combination with simvastatin in patients with moderate to severe renal impairment (estimated glomerular filtration rate <60 mL/min/1.73 m2), doses of simvastatin exceeding 20 mg should be used with caution and close monitoring is recommended.

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