Zetia (ezetimibe)

ZETIA (ezetimibe) – an inhibitor of intestinal cholesterol (and related phytosterol) absorption commonly used to certain types of hyperlipidemias. Specifically, Ezetimibe works to reduce blood cholesterol by inhibiting the absorption of cholesterol by the small intestine.

FDA approved uses: Zetia is as an adjunct to diet to:

  • Reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary hyperlipidemia, alone or in combination with an HMG-CoA reductase inhibitor (statin).
  • Reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia in combination with fenofibrate.
  • Reduce elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH), in combination with atorvastatin or simvastatin.
  • Reduce elevated sitosterol and campesterol in patients with homozygous sitosterolemia (phytosterolemia).
  • Available dosage forms: Tablets – 10 mg.

    Usual dosage: One 10-mg tablet once daily, with or without food. Dosing of ZETIA should occur either ≥2 hours before or ≥4 hours after administration of a bile acid sequestrant.

    Contraindications: Zetia (ezetimibe hydrochloride) is contraindicated in patients with known hypersensitivity to ezetimibe hydrochloride or to any excipients used in the formulation. If used with a statin, the following statin contraindications apply – Active liver disease, which may include unexplained persistent elevations in hepatic transaminase levels; Women who are pregnant or may become pregnant; Nursing mothers.

    Special warnings: Zetia is not recommended for patients with moderate or severe liver disease. Cases of myopathy and rhabdomyolysis have been reported in patients treated with ZETIA co-administered with a statin and with ZETIA administered alone. Risk for skeletal muscle toxicity increases with higher doses of statin, advanced age (>65), hypothyroidism, renal impairment, and depending on the statin used, concomitant use of other drugs.

    Adverse reactions (side effects) of these medications: The most common side effects of include upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremity. The most common side effects seen when Zetia was co-administered with a statin were nasopharyngitis, myalgia, upper respiratory tract infection, arthralgia, and diarrhea.

    Common drug interactions: The following agents have been implicated in interactions with ezetimibe and thus warrant extra monitoring and caution during co-administration – cyclosporin, fibrates, enofibrate, cholestyramine, and coumarin anticoagulants.

    Special instructions for patients: Take this medication exactly as directed by physician. Read the official medication guide before you start taking Zetia and each time you refill Zetia. Tell physician prior to starting Zetia if you have ever had liver problems. Notify physician if you have muscle pains, tenderness or weakness while taking Zetia.

    Full prescribing information may be found at the manufacturer‘s official website Zetia.com or at the U.S. Food and Drug Administration’s website at Zetia Info at Drugs@FDA

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