イミプラミン塩酸塩 化学特性,用途語,生産方法
外観
白色〜うすい黄色, 結晶性粉末〜粉末
溶解性
エタノール、アセトン及び水に溶ける。
用途
三環系抗うつ作用化合物です。 モノアミン神経伝達物質再取り込み阻害作用 を示します。
用途
三環系抗うつ作用化合物です。
モノアミン神経伝達物質再取り込み阻害作用
を示します。
効能
抗うつ薬, セロトニン・ノルアドレナリン再取り込み阻害薬
商品名
イミドール (田辺三菱製薬); トフラニール (アルフレッサファーマ)
使用上の注意
アルゴン封入
化学的特性
White Solid
使用
Imipramine hydrochloride is used as a serotonin uptake inhibitor. It mainly used in the treatment of major depression and enuresis (inability to control urination). It has also been evaluated for use in panic disorder.
一般的な説明
Imipramine hydrochloride, 5-[3-(dimethylamino)propyl]-10,11-dihydro-5H-dibenz[b,f]azepine monohydrochloride(Tofranil), is the lead compound of the TCAs. It is also a closerelative of the antipsychotic phenothiazines (replace the10–11 bridge with sulfur, and the compound is the antipsychoticagent promazine). It has weaker D
2 postsynaptic blockingactivity than promazine and mainly affects amines (5-HT,NE, and DA) via the transporters. As is typical of dimethylaminocompounds, anticholinergic and sedative (central H
1block) effects tend to be marked. The compound per se has a tendency toward a high 5-HT-to-NE uptake block ratio andprobably can be called a serotonin transport inhibitor(SERTI). Metabolic inactivation proceeds mainly by oxidativehydroxylation in the 2-position, followed by conjugationwith glucuronic acid of the conjugate. Urinary excretion predominates(about 75%), but some biliary excretion (up to25%) can occur, probably because of the large nonpolargrouping. Oxidative hydroxylation is not as rapid or completeas that of the more nucleophilic ring phenothiazine antipsychotics;consequently, appreciable N-demethylation occurs,with a buildup of norimipramine (or desimipramine).
臨床応用
The demethylated metabolite is less anticholinergic, lesssedative, and more stimulatory and is a SNERI.Consequently, a patient treated with imipramine has twocompounds that contribute to activity. Overall, the effect isnonselective 5-HT versus NE reuptake.
安全性プロファイル
Human poison by
ingestion. An experimental poison by
ingestion, intravenous, subcutaneous, and
intraperitoneal routes. An experimental
teratogen. Human systemic effects by
ingestion: sleep, somnolence, convulsions,
muscle contraction or spasticity, coma, blood pressure decrease, dyspnea (difficulty
in breathing), paresthesia (abnormal
sensations), and kidney changes.
Experimental reproductive effects. Mutation
data reported. Used in the treatment of
depression. When heated to decomposition
it emits very toxic fumes of NO, and HCl.
See also DIAZEPAM.
イミプラミン塩酸塩 上流と下流の製品情報
原材料
準備製品