エゼチミブ

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H410：長期的影響により水生生物に非常に強い毒性

• 注意書き

  P273：環境への放出を避けること。

  P391：漏出物を回収すること。

  P501：内容物/容器を．．．に廃棄すること。

エゼチミブ 価格

エゼチミブ 化学特性,用途語,生産方法

• 用途

  エゼチミブ（Ezetimibe）は、小腸からのコレステロール吸収を抑制し、血中コレステロール値を低下させる医薬品である。他のコレステロール低下薬に不忍容の場合に単剤で用いられるほか、スタチン単剤でのコントロールが悪い場合に併用される。

• 効能

  脂質異常症治療薬, コレステロール吸収阻害薬

• 商品名

  ゼチーア (MSD); ゼチーア (MSD)

• 化学的特性

  White Solid

• 来歴

  Ezetimibe (brand name Zetia) was approved by the FDA in October 2002 for lowering levels of total cholesterol and LDL (bad) cholesterol in the blood. Zetia is used to treat high cholesterol in people whose cholesterol levels cannot be controlled by diet and exercise alone. It is sometimes given in combination with other cholesterol-lowering drugs, including fenofibrate, or statins, such as atorvastatin, lovastatin, simvastatin, pravastatin, or fluvastatin.

• 使用

  Ezetimibe (9) was approved as the first hypolipidemic drug to act by blocking the absorption of dietary cholesterol. This drug was discovered by Schering-Plough and is codeveloped and co-marketed by Merck and Schering-Plough for the treatment of hypercholesterolemia and also two less common forms of hyperlipidemia: homozygous familial hypercholesterolemia and homozygous sitosterolemia.

• 定義

  ChEBI: Ezetimibe is a beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer). It has a role as an anticholesteremic drug, an antilipemic drug and an antimetabolite. It is a member of azetidines, an organofluorine compound and a beta-lactam.

• 生物学の機能

  Ezetimibe lowers plasma cholesterol levels by inhibiting the absorption of cholesterol at the brush border of the small intestine. Specifically, it has been proposed to bind to a specific transport protein located in the wall of the small intestine, resulting in a reduction of cholesterol transport and absorption. Ezetimibe appears to be selective in its actions in that it does not interfere with the absorption of triglycerides, lipid-soluble vitamins or other nutrients. The decreased absorption of cholesterol eventually leads to enhanced receptor-mediated LDL uptake similar to that seen with bile acid sequestrants and HMGRIs. When used as monotherapy, the decreased absorption of cholesterol causes a compensatory increase in cholesterol biosynthesis. This is similar to that described for bile acid sequestrants and is insufficient to override the overall LDL lowering effects of ezetimibe.

• 一般的な説明

  Ezetimibe, (3R,4S)-1-(4-fluorophenyl)-3-((3S)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)-2-azetidinone (Zetia), is an antihyperlipidemicagent that has usefulness in lowering cholesterol levels. Itacts by decreasing cholesterol absorption in the intestine byblocking the absorption of the sterol at the Brush boarder.Specifically, the -lactam binds to the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract that isresponsible for cholesterol absorption. Although it may beused alone, it is marketed as a combination product withsimvastatin under the trade name Vytorin.

• 薬物動態学

  Ezetimibe is administered orally; however, its absolute bioavailability cannot be determined because of its aqueous insolubility and the lack of an injectable formulation. Based on area under the curve values, the oral absorption ranges from 35 to 60%. Mean peak concentrations of the active glucuronidated metabolite are reached within 1 to 2 hours. Both ezetimibe and its glucuronide conjugate are extensively bound (>90%) to plasma proteins. The relative plasma concentrations of ezetimibe and its glucuronide conjugate range from 10 to 20% and from 80 to 90%, respectively. Both compounds have a long half-life of approximately 22 hours. The coadministration of food with ezetimibe has no effect on the extent of absorption.

• 臨床応用

  Ezetimibe is indicated as monotherapy or in combination with an HMGRI for the reduction of elevated total cholesterol, LDL cholesterol, and apoB in patients with primary (heterozygous familial and nonfamilial) hypercholesterolemia. When used as monotherapy, ezetimibe reduces LDL cholesterol by approximately 18%. When used in combination therapy with an HMGRI, LDL levels are reduced by 25 to 65% depending on the dose of the HMGRI inhibitor. Ezetimibe also is indicated for homozygous familial hypercholesterolemia in combination with either atorvastatin or simvastatin and for homozygous familial sitosterolemia. All indications are for patients who have not responded to diet, exercise, and other nonpharmacological methods.

• 副作用

  Ezetimibe generally is well tolerated. The most common adverse effects are listed above. Whenever ezetimibe is used in combination with an HMGRI, the incidence of myopathy or rhabdomyolysis does not increase above that seen with HMGRI monotherapy.

• 代謝

  Following oral administration, ezetimibe is rapidly and extensively metabolized in the intestinal wall and the liver to its active metabolite, a corresponding phenol glucuronide. This glucuronide is reexcreted in the bile back to its active site. A small amount (<5%) of ezetimibe undergoes oxidation to covert the benzylic hydroxyl group to a ketone; however, ezetimibe does not appear to exert any significant effect on the activity of CYP450 enzymes.

エゼチミブ 上流と下流の製品情報

エゼチミブ 生産企業

Global(770)Suppliers

エゼチミブ スペクトルデータ(¹HNMR)

163222-33-1, エゼチミブ キーワード