ドロペリドール 化学特性,用途語,生産方法
解説
C22H22FN3O2(379.43)．4-クロロ-1-(4-フルオロフェニル)-ブタン-1-オンを1-(1,2,3,6-テトラヒドロ-4-ピリジル)-2-ベンズイミダゾリノンと縮合させると得られる．ドロペリドール, 融点145 ℃．λmax 245，280 nm．pKa 7.64．水に不溶，クロロホルム，アセトンに可溶．光や熱に不安定である．鎮痛，鎮静効果をもち，全身麻酔や局所麻酔にほかの合成剤として併用される．また，制吐薬としても使用される．LD50 22.1 mg/kg(マウス，静注)．森北出版「化学辞典（第2版）
効能
静脈麻酔薬, 統合失調症治療薬
商品名
ドロレプタン (アルフレッサファーマ)
説明
D roperidol is a butyrophenone that has potent antidopaminergic (D2)
activity and mild α2-blocking actions. It produces sedation and anxiolysis and
is an effective antiemetic. A dverse effects include
vasodilatation and hypotension, and at higher doses, dystonic reactions can
occur. D roperidol was used for premedication and in neuroleptanaesthesia
until reports of death from long QT syndrome led to its withdrawal in 2001. It
has recently been reintroduced and licenced at lower doses for prevention of
postoperative nausea and vomiting. D roperidol has an onset of 3–10 min
after i.v. injection and duration of action of 6–12h. It undergoes hepatic
metabolism, but approximately 10% of the drug is excreted unchanged in the
urine.
化学的特性
Pale Yellow Solid
使用
The neuroleptic droperidol possesses antipsychotic, sedative, and antishock action. It potentiates the action of drugs for narcosis. In psychiatric practice, droperidol is used for psychomotor excitement and hallucinations. The principal use of this drug lies in anesthesiology
for neuroleptanalgesia in combination with fentanyl. It is used in premedication as well as in
surgical operations and post-operational circumstances.
定義
ChEBI: An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the
management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeo
.
一般的な説明
Droperidol, 1-{1-[3-(p-fluorobenzoyl)propyl]-1,2, 3,6-tetrahydro-4-pyridyl}-2-benzimidazolinone(Inapsine), may be used alone as a preanestheticneuroleptic or as an antiemetic. Because of its very shortactingand highly sedating properties, its most frequent useis in combination (Innovar) with the narcotic agent fentanyl(Sublimaze) preanesthetically.
ドロペリドール 上流と下流の製品情報
原材料
準備製品