Ezetimibe Dosage

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Usual Adult Dose for:

Additional dosage information:

Usual Adult Dose for Hyperlipidemia

10 mg once a day with or without food.

Usual Adult Dose for Sitosterolemia

10 mg once a day with or without food.

Renal Dose Adjustments

No adjustment necessary

Liver Dose Adjustments

If a patient has a Child-Pugh score of 7 or greater, then use of this drug is not recommended.

Dose Adjustments

Ezetimibe is usually dosed daily, but its 22-hour elimination half life permits significant cholesterol reduction with less frequent dosing. A study examined lipid changes in 33 patients treated with three times weekly ezetimibe for greater than or equal to one month, who had pre- and post-ezetimibe lipid levels and no other concurrent changes in their lipid treatment. Ninety-four percent of the patients in the study were treated with ezetimibe because they experienced myalgias, elevated transaminase levels, or gastrointestinal intolerance with higher doses of other lipid-lowering agents. Total cholesterol decreased by 15% and low-density lipoprotein cholesterol by 20% during 58 plus or minus 50 days of treatment. Most patients (85%) tolerated the treatment, and many (48%) achieved their low-density lipoprotein cholesterol goals. The study concluded that ezetimibe given three times weekly decreases total and low-density lipoprotein cholesterol and is well tolerated. It is a viable treatment for patients intolerant of other lipid-lowering medications.

Precautions

Because of the unknown effects of the increased exposure to ezetimibe in patients with moderate to severe hepatic insufficiency, use of ezetimibe is not recommend in these patients. The combination of ezetimibe with an HMG-CoA reductase inhibitor is contraindicated in patients with active liver disease or unexplained persistent elevations in serum transaminases.

The incidence of consecutive elevations (greater than or equal to 3 × the upper limit of normal [ULN]) in serum transaminases have not been reported in ezetimibe studies. In studies of ezetimibe initiated concurrently with an HMG-CoA reductase inhibitor, the incidence of consecutive elevations (greater than or equal to 3 × ULN) in serum transaminases was reported. These elevations in transaminases were generally asymptomatic, not associated with cholestasis, and returned to baseline after discontinuation of treatment or with continued therapy. When ezetimibe is coadministered with an HMG-CoA reductase inhibitor, liver function tests should be performed at initiation of treatment and according to the recommendations of the HMG-CoA reductase inhibitor.

In clinical trials, there was no excess of myopathy or rhabdomyolysis associated with ezetimibe compared with the relevant control arm (placebo or HMG-CoA reductase inhibitor alone). However, myopathy and rhabdomyolysis are known adverse reactions to HMG-CoA reductase inhibitors and other lipid-lowering drugs. In postmarketing experience with ezetimibe, cases of myopathy and rhabdomyolysis have been reported regardless of causality. Most patients who developed rhabdomyolysis were taking an HMG-CoA reductase inhibitor prior to initiating ezetimibe. However, rhabdomyolysis has been reported very rarely with ezetimibe monotherapy and very rarely with the addition of ezetimibe to agents known to be associated with increased risk of rhabdomyolysis, such as fibrates. All patients starting therapy with ezetimibe should be advised of the risk of myopathy and told to report promptly any unexplained muscle pain, tenderness or weakness. Ezetimibe and any HMG-CoA reductase inhibitor or fibrate that the patient is taking concomitantly should be immediately discontinued if myopathy is diagnosed or suspected. The presence of these symptoms and a creatine phosphokinase (CPK) level greater than 10 times the ULN indicates myopathy.

The safety and efficacy of ezetimibe in pediatric patients less than 10 years of age have not been determined.

Dialysis

Data not available

Other Comments

Ezetimibe should be dosed 2 or more hours before or 4 or more hours after administration of a bile acid sequestrant.

The patient should be placed on a standard cholesterol-lowering diet before receiving ezetimibe and should continue on this diet during treatment with ezetimibe.

Ezetimibe may be administered with an HMG-CoA reductase inhibitor (in patients with primary hypercholesterolemia) or fenofibrate (in patients with mixed hyperlipidemia) for incremental effect. Ezetimibe may be administered at the same time as the HMG-CoA reductase inhibitor or fenofibrate, depending on the dosing recommendations for the HMG-CoA reductase inhibitor.

The package labeling reports that treatment experience in the pediatric population is limited to four patients (9 to 17 years) in the sitosterolemia study and five patients (11 to 17 years) in the HoFH study.

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