Ezetimibe

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[edit] BRAND NAMES

[edit] STRUCTURE

Ezetimibe.jpg

[edit] MECHANISM OF ACTION

Ezetimibe is a hypolipidemic drug that selectively inhibits the intestinal absorption of cholesterol and related phytosterols leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood. Ezetimibe molecular target has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols.

This distinct mechanism of action is complementary to that of statins and of fenofibrate

[edit] INDICATIONS

  • To reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary hyperlipidemia, alone or in combination with a statin (e.g. Simvastatin/Ezetimibe)
  • To reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia in combination with fenofibrate
  • To reduce elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH), in combination with atorvastatin or simvastatin.
  • To reduce elevated sitosterol and campesterol in patients with homozygous sitosterolemia (phytosterolemia)

[edit] DOSAGE

The recommended dose is 10 mg once daily, with or without food

Dosing of Ezetimibe should occur either 2 hours before or 4 hours after administration of a bile acid sequestrant (e.g. Cholestyramine)

[edit] DOSAGE FORMS AND STRENGTHS

Tablets: 10 mg

[edit] CONTRAINDICATIONS

Known hypersensitivity to Ezetimibe

[edit] WARNINGS AND PRECAUTIONS

Ezetemibe is not recommended in patients with moderate or severe hepatic impairment.

[edit] INTERACTIONS

  • Fibrates: concomitant administration of Ezetimibe with Fibrates other than fenofibrate would lead to an increase in cholesterol in gallbladder (cholelithiasis) and therefore is not recommended. So avoid co-administration of Ezetimibe with gemfibrozil or bezafibrate.
  • Fenofibrate: If cholelithiasis is suspected in a patient receiving Ezetimibe and fenofibrate, gallbladder studies are indicated and alternative lipid-lowering therapy should be considered
  • Cholestyramine: Ezetimibe is decreased by 55% with concomitant Cholestyramine administration and would be resulted in lower than expected LDL-C reduction. Dosing of Ezetimibe should occur either 2 hours before or 4 hours after administration of Cholestyramine.
  • Cyclosporine: Concentration of Ezetimibe would be increased by 12 folds. Cyclosporine concentrations should be monitored in patients taking Ezetimibe concomitantly

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US) Ezetimibe Ezetimibe should be used during pregnancy only if the potential benefit justifies the risk to the fetus
  • Ezetimibe should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant.

[edit] SIDE EFFECTS

Common adverse reactions (incidence ≥2% and greater than placebo): upper respiratory tract infection, diarrhea, arthralgia, sinusitis, and pain in extremity

[edit] RELATED LINKS

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[edit] REFERENCES