Simbex™

[Simvastatin + Ezitimibe]

Active Ingredients

  • Simbex™ 10/10: Ezetimibe 10mg + Simvastatin 10mg
  • Simbex™ 10/20: Ezetimibe 10mg + Simvastatin 20mg
  • Simbex™ 10/40: Ezetimibe 10mg + Simvastatin 40mg

    Description / Properties

    Simbex Simbex™ contains ezetimibe, a selective inhibitor of intestinal cholesterol and related phytosterol absorption, and simvastatin, a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor. The chemical name of ezetimibe is 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]- 4(S)-(4-hydroxyphenyl)-2-azetidinone. The empirical formula is C24H21F2NO3 and its molecular weight is 409.4. Simvastatin, an inactive lactone, is hydrolyzed to the corresponding ß-hydroxyacid form, which is an inhibitor of HMG-CoA reductase. The empirical formula of Simvastatin is C25H38O5 and its molecular weight is 418.57. Simvastatin is a white to off-white, nonhygroscopic, crystalline powder that is practically insoluble in water, and freely soluble in chloroform, methanol and ethanol. Simbex™ is available for oral use as tablets containing 10 mg of ezetimibe, and 10 mg of simvastatin (Simbex™ 10/10), 20 mg of simvastatin (Simbex™ 10/20) or 40 mg of simvastatin (Simbex™ 10/40). Each tablet contains the following inactive ingredients: butylated hydroxyanisole NF, citric acid monohydrate USP, croscarmellose sodium NF, hydroxypropyl methylcellulose USP, lactose monohydrate NF, magnesium stearate NF, microcrystalline cellulose NF, and propyl gallate NF.

    Warning and Precautions

    The concurrent administration of potassium supplements, a diet rich in potassium or other potassium sparing diuretics is not recommended. Periodic estimation of serum electrolytes is desirable due to the possibility of hyperkalemia, hyponatremia, hypochloremic alkalosis and possible transient BUN elevation especially in patients with preexisting impaired renal function.

    Dosage & Administration

    The patient should be placed on a standard cholesterol-lowering diet before receiving Simbex™ and should continue on this diet during treatment with Simbex™. The dosage should be individualized according to the baseline LDL-C level, the recommended goal of therapy, and the patient’s response. (See NCEP Adult Treatment Panel (ATP) III Guidelines, summarized in Table 4.) Simbex™ should be taken as a single daily dose in the evening, with or without food.

    The dosage range is 10/10 mg/day through 10/80 mg/day. The recommended usual starting dose is 10/20 mg/day. Initiation of therapy with 10/10 mg/day may be considered for patients requiring less aggressive LDL-C reductions. Patients who require a larger reduction in LDL-C (greater than 55%) may be started at 10/40 mg/day. After initiation or titration of Simbex™, lipid levels may be analyzed after 2 or more weeks and dosage adjusted, if needed. See below for dosage recommendations for patients receiving certain concomitant therapies and for those with renal insufficiency.

    Patients with Homozygous Familial Hypercholesterolemia
    The recommended dosage for patients with homozygous familial hypercholesterolemia is Simbex™ 10/40 mg/day or 10/80 mg/day in the evening. Simbex™ should be used as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) in these patients or if such treatments are unavailable.

    Patients with Hepatic Insufficiency
    No dosage adjustment is necessary in patients with mild hepatic insufficiency.

    Patients with Renal Insufficiency
    No dosage adjustment is necessary in patients with mild or moderate renal insufficiency. However, for patients with severe renal insufficiency, Simbex™ should not be started unless the patient has already tolerated treatment with simvastatin at a dose of 5 mg or higher. Caution should be exercised when Simbex™ is administered to these patients and they should be closely monitored.

    Geriatric Patients
    No dosage adjustment is necessary in geriatric patients.

    Coadministration with Bile Acid Sequestrants
    Dosing of Simbex™ should occur either 2 hours before or 4 hours after administration of a bile acid sequestrant.

    Patients taking Cyclosporine or Danazol
    Caution should be exercised when initiating Simbex™ in the setting of cyclosporine. In patients taking cyclosporine or danazol, Simbex™ should not be started unless the patient has already tolerated treatment with simvastatin at a dose of 5 mg or higher. The dose of Simbex™ should not exceed 10/10 mg/day.

    Patients taking Amiodarone or Verapamil
    In patients taking amiodarone or verapamil concomitantly with Simbex™, the dose should not exceed 10/20 mg/day (see WARNINGS, Myopathy/Rhabdomyolysis and PRECAUTIONS, Drug Interactions, Other drug interactions).

    Presentations Available

    All strengths of Simbex&trade are available in white to off-white, coverd & scored blister pack tablets.

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