ハロペリドール 化学特性,用途語,生産方法
外観
白色～わずかにうすい黄色, 結晶～粉末
溶解性
氷酢酸に易溶、クロロホルムに可溶、メタノール,エタノール,アセトンに微溶、エーテル,2-プロパノールに難溶、水に不溶。酢酸に溶けやすく、クロロホルムにやや溶けやすく、メタノール、エタノール及びアセトンにやや溶けにくく、水にほとんど溶けない。
解説
ハロペリドール,ブチロフェノン誘導体の抗精神病薬の一つである (→向精神薬 ) 。作用機序として，抗ドーパミン，抗ヒスタミン作用のほか，弱いが抗αアドレナリン，抗セロトニン作用が考えられている。臨床では，精神病治療のほかに強化麻酔，止痒，制吐などに用いられる。抗精神病薬の原型であるクロルプロマジンと作用も副作用も類似しており，強弱の差があるだけである。ハロペリドールのほうが，副作用としての鎮静作用は弱く，パーキンソン症状は強く，起立性低血圧は軽度である。
用途
神経化学研究用。
用途
抗精神病薬,精神安定剤
用途
ブチロフェノン系化合物です。 ドパミンD2 受容体遮断作用を示します。
用途
ブチロフェノン系化合物です。
ドーパミンD2 受容体遮断作用を示します。
効能
統合失調症治療薬, 抗ジスキネジア, 神経遮断薬, ドパミンD2受容体拮抗薬
商品名
セレネース (大日本住友製薬); セレネース (大日本住友製薬); セレネース (大日本住友製薬)
説明
Haloperidol is a butyrophenone with a long duration of action. It has lile α-
adrenoceptor blocking activity and minimal effect on the cardiovascular
system. It is an effective antiemetic but has a high incidence of
extrapyramidal adverse effects. Haloperidol may be used in the short-term
management of the acutely agitated patient (when sinister causes of
confusion such as hypoxaemia and sepsis have been excluded) and in the
management of delirium in ICU. The duration of action of
haloperidol is approximately 24–48h.
化学的特性
White Crystalline Powder
使用
Haloperidol is one of the most actively used modern neuroleptics. Its high antipsychotic
activity is combined with a moderate sedative effect. It effectively stops various types of
psychomotor excitement. It is used for schizophrenic psychoses, manic, paranoid, and
delirious conditions, depression, psychomotor excitement of various origins, and for delirium and hallucinations of different origin.
定義
ChEBI: A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.
一般的な説明
Haloperidol, 4-[4-(p-chlorophenyl)-4-hydroxypiperidino]-4-fluorobutyrophenone (Haldol), is anodorless white to yellow crystalline powder. Haloperidol iswell and rapidly absorbed and has a high bioavailability. It ismore than 90% bound to plasma proteins. Haloperidol is excretedslowly in the urine and feces. About 30% of a dose isexcreted in urine and about 20% of a dose in feces via biliaryelimination,and only 1% of a dose is excreted as unchangeddrug in the urine.Haloperidol is a minor substrate of CYP1A2 and a major substrate of CYP2D6 and CYP3A4.CYP2D6 inhibitors may increase the levels/effects ofhaloperidol.Haloperidol may increase the levels/effects ofCYP2D6 substrates and it may decrease the bioactivationof CYP2D6 prodrugs substrates. Haloperidol also is a moderateinhibitor of CYP2D6 and CYP3A4. CYP3A4 inducersmay decrease the levels/effects of haloperidol, whereasCYP3A4 inhibitors may increase the levels/effects ofhaloperidol. Centrally acting acetylcholinesterase inhibitorsmay increase the risk of antipsychotic-related EPS. The precisemechanism of antipsychotic action is unclear but isconsidered to be associated with the potent DA D
2receptor–blocking activity in the mesolimbic system and theresulting adaptive changes in the brain. Haloperidol is usedprimarily for the long-term treatment of psychosis and is especiallyuseful in patients who are noncompliant with theirdrug treatment.
応用例（製薬）
Haloperidol is an analogue of the dopamine D2 receptor antagonist and is an older antipsychotic drug. The drug is used in the treatment of schizophrenia, a neuropsychiatric disorder. In general, antipsychotic drugs work by blocking the dopamine D
2 receptors.
Haloperidol is such an antipsychotic drug, which was developed in the 1950s and entered the clinic soon after that. Its use is limited by the high incidence of extrapyramidal symptoms (movement disorders caused by drugs affecting the extrapyramidal system, a neural network which is part of the motor system). Nevertheless, haloperidol may be used for the rapid control of hyperactive psychotic states and is popular for treating restlessness in the elderly.
生物活性
Dopamine antagonist with selectivity for D 2 -like receptors (K i values are 1.2, ~ 7, 2.3, ~ 80 and ~ 100 nM for D 2 , D 3 , D 4 , D 1 and D 5 receptors respectively). Subtype-selective NMDA antagonist.
ハロペリドール 上流と下流の製品情報
原材料
準備製品