コレスチラミン 化学特性,用途語,生産方法
定義
本品は、スチレンとスチレンメチレントリモニウムクロリドの共重合体をジビニルベンゼンで架橋したものである。
化粧品の成分用途
吸着剤
効能
脂質異常症治療薬, 胆汁酸吸収阻害薬, 除去剤 (レフルノミド活性代謝物)
商品名
クエストラン (サノフィ)
化学的特性
White or almost white, fine powder, hygroscopic.
使用
Antihyperlipidemic;
ion-exchange resin (bile salts).
適応症
Cholestyramine
is a powder that is mixed with water or another fluid before ingesting.
Colestipol (Colestid) is another ion exchange resin that may be substituted
in patients who find cholestyramine too constipating. Like charcoal, ion
exchange resins may bind other orally administered drugs.
定義
A synthetic, strongly basic anion exchange resin that
contains functional quaternary ammonium groups
linked to a styrene-divinylbenzene copolymer.
一般的な説明
Cholestyramine (Cuemid,Questran) is the chloride form of a strongly basic anionexchangeresin. It is a styrene copolymer with divinylbenzenewith quaternary ammonium functional groups. After oral ingestion,cholestyramine resin remains in the gastrointestinaltract, where it readily exchanges chloride ions for bile acids inthe small intestine, to be excreted as bile salts in the feces.Cholestyramine resin is also useful in lowering plasma lipids.The reduction in the amounts of reabsorbed bile acids resultsin increased catabolism of cholesterol in bile acids in the liver.The decreased concentration of bile acids returning to theliver lowers the feedback inhibition by bile acids of 7- -hydroxylase, the rate-limiting enzyme in the conversion ofcholesterol to bile acids, increasing the breakdown of hepaticcholesterol. Although biosynthesis of cholesterol is increased,it appears that the rate of catabolism is greater, resulting in anet decrease in plasma cholesterol levels by affecting LDLclearance. The increase of LDL receptors in the liver that occurswhen its content of cholesterol is lowered augments thisbiochemical event.
空気と水の反応
Hygroscopic [Merck.] Insoluble in water.
反応プロフィール
An amine. Amines are chemical bases. They neutralize acids to form salts plus water. These acid-base reactions are exothermic. The amount of heat that is evolved per mole of amine in a neutralization is largely independent of the strength of the amine as a base. Amines may be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen is generated by amines in combination with strong reducing agents, such as hydrides.
危険性
Low toxicity; tumorigen; questionable carcinogen; teratogen.
健康ハザード
SYMPTOMS: Symptoms of exposure to CHOLESTYRAMINE RESIN may include nausea, abdominal discomfort indigestion and constipation. It also causes vitamin K deficiency, rash, mucous membrane irritation, osteoporosis and eosinophilia. Other symptoms include flatulence, vomiting, diarrhea, heartburn, anorexia, steatorrhea, vitamin A and D deficiencies and hyperchloremic acidosis in children.
火災危険
Flash point data for CHOLESTYRAMINE RESIN are not available. CHOLESTYRAMINE RESIN is probably combustible.
薬理学
Cholestyramine, an anion exchange resin,
is frequently effective, although, as mentioned earlier, its antipruritic effect
seems separate from its ability to normalize bile salt levels.
臨床応用
Cholestyramine resin is the drug of choice for type IIa hyperlipoproteinemia.When used in conjunction with a controlleddiet, it reduces -lipoproteins. The drug is an insolublepolymer and, thus, probably one of the safest because itis not absorbed from the gastrointestinal tract to cause systemictoxic effects.
安全性プロファイル
Low toxicity by
ingestion. Questionable human carcinogenproducing colon tumors. An experimental
teratogen. Other experimental reproductive
effects. Toxic effects by ingestion: acidosis
and nosebleeds. When heated to
decomposition it emits acrid smoke and
irritating fumes.
コレスチラミン 上流と下流の製品情報
原材料
準備製品