Ezetimibe

It is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe does not inhibit cholesterol synthesis in the liver or increase bile acid excretion. Instead ezetimibe localized and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, 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, this distinct mechanism is complementary to that of HMG-CoA reductase inhibitors.

Indications

Primary Hypercholesterolemia Monotherapy, Combination therapy with HMG-CoA reductase inhibitors, Homozygous Familial hypercholesterolemia (HoFH), Homozygous Sitosterolemia.

Dosage

Adults and children (?10 years): 10 mg once daily, with or without food.

Contra-Indications

-Hypersensitivity to ezetimibe or any component of the formulation -Active liver disease or unexplained persistent elevations in hepatic transaminase levels when used in combination with a statin

Special Precautions

-Monitor liver enzyme levels before and during treatment when combined with statins. -Use caution in patients with moderate to severe hepatic impairment. -Not recommended for use in pregnant or breastfeeding women. -Consider secondary causes of hypercholesterolemia before initiating therapy. -Regularly monitor lipid levels to assess efficacy.

Side Effects

-Common: Headache, diarrhea, upper respiratory tract infection, myalgia, sinusitis. -Serious: Elevated liver enzymes, rhabdomyolysis (especially when combined with statins), hypersensitivity reactions, pancreatitis.

Drug Interactions

-Statins: Increased risk of myopathy and rhabdomyolysis. -Fibrates: Increased risk of cholelithiasis. -Cyclosporine: Increased levels of both ezetimibe and cyclosporine. -Warfarin: Monitor INR closely as there may be an increased risk of bleeding. -Bile acid sequestrants: Decrease the absorption of ezetimibe; administer ezetimibe at least 2 hours before or 4 hours after a bile acid sequestrant.