Ezetimibe is a new drug of its own kind that acts by inhibiting intestinal absorption of cholesterol and phytosterols. It interferes with a specific CH transport protein NPC1C1 in the intestinal mucosa and reduces absorption of both dietary and biliary CH. There is compensatory increase in hepatic CH synthesis, but LDL-CH level is lowered by 15—20%. The enhanced CH synthesis can be blocked by statins, and the two drugs have synergistic LDL-CH lowering effect.
Due to very poor aqueous solubiity, Ezetimibe is not absorbed as such. It is absorbed partly after getting conjugated with glucuronic acid in the intestinal mucosa — secreted in bile — undergoes enterohepatic circulation and is mainly excreted in faeces. A plasma t 1/2 of 22 hours has been calculated.
Used alone, ezetimibe is a weak hypocholesterolaemic drug; LDL-CH lowering beyond 15—20% is not obtained by increasing the dose. Though it may be used alone in mild hypercholesterolaemia when a statin is contraindicated/ not tolerated, its main value is to supplement statins without increasing their dose. The combination of ezetimibe + low dose of a statin is as effective in lowering LDL-CH as high dose of statiri alone. Upto 60% decrease in LDL-CH level has been obtained with a combination of simvastatin + ezetimibe . No specific adverse effect, except reversible hepatic dysfunction and rarely myositis has been noted with ezetimibe .
Dose: 10 mg OD; ZETICA, EZEDOC 10 mg tab.