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Appendix C – Drug Companion Document – Selective Cholesterol Absorption Inhibitors

Ezetimibe

Efficacy

    Long-term effects on cardiovascular morbidity and mortality are unknown.
 
    LDL-cholesterol lowered about 18%.
 
    Additive LDL-cholesterol reduction when used in combination with statins.

    FDA approved Ezetimibe with fenofibrate.

Safety

    Short-term tolerability is similar to placebo. Long-term safety is unknown.
 
    Not recommended for use in patients with moderate to severe hepatic impairment based on Child-Pugh score. The AUC of ezetimibe
     increased fourfold in patients with moderate hepatic impairment (Child-Pugh score 7 to 9).
 
    Co-administration with cyclosporine increased ezetimibe blood level 12-fold in one renal transplant patient. Patients on cyclosporine and
      ezetimibe should be monitored carefully.
 
    Cholestyramine co-administration decreased the mean AUC of total ezetimibe by 55%. Ezetimibe should be given two hours before or
     four hours after bile-acid sequestrants.
 

Dosing

    10 mg daily without regard to meals or time of day.

    When combined with a statin, ezetimibe may be taken at the same time.
 

Exetimibe/Statin Combination Product

    Ezetimibe plus simvastatin.
 
    Ezetimibe 10 mg/simvastatin 10 mg.

    Ezetimibe 10 mg/simvastatin 20 mg.
 
    Ezetimibe 10 mg/simvastatin 40 mg.
 
    Ezetimibe 10 mg/simvastatin 80 mg.

Efficacy

    Additive effects on LDL-cholesterol reduction.

Safety

    Please refer to information in the ezetimibe and statin sections of this appendix.

Dosing

    Please refer to dosing for simvastatin.

Please consult manufacturer's product labeling insert, or PDF for full prescribing information.

(Dujovne, 2002 [C]; Gagne, 2002 [C]; McKenney, 2002 [R])