オランザピン 化学特性,用途語,生産方法
外観
うすい黄色〜褐色, 結晶〜粉末
溶解性
アセトニトリルに可溶
用途
ドーパミン、セロトニン受容
体をはじめ、多数の神経物質受容体に対する
拮抗作用を示します。
用途
ドパミン、セロトニン受容体 をはじめ、多数の神経物質受容体に対する拮 抗作用を示します。
効能
統合失調症治療薬
商品名
オランザピン (ニプロ); ジプレキサ (日本イーライリリー); ジプレキサ (日本イーライリリー); ジプレキサ (日本イーライリリー); ジプレキサ (日本イーライリリー)
説明
Zyprexa was launched in Canada, Germany, the UK and US as an
antipsychotic agent. Prepared in three steps via the intermediate diazepinone, it is an
atypical antipsychotic with a high affinity for dopaminergic and serotonergic
receptors. Specifically, olazapine is a potent 5-HT
2/D
2 antagonist with anticholinergic
activity. It has a greater antagonistic effect at 5-HT
2a than at dopamine D
2 receptors
and in vivo is clozapine-like. Thus it is less likely to produce extrapyramidal side
effects and does not produce any granulocytopenia. Its 10 metabolic products are all
inactive.
化学的特性
Yellow Crystalline Powder
使用
A serotonin (5-HT2) and dopamine (D1/D2) receptor antagonist with anticholinergic activity. Antipsychotic.
定義
ChEBI: A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.
一般的な説明
Olanzapine, 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine (Zyprexa), isa yellow crystalline solid that is essentially insoluble in water.Olanzapine orally disintegrating tablets (Zyprexa Zydis) is asolid dosage form that immediately disintegrates when exposedto saliva. This product is useful for elderly patients whohave difficulty in swallowing. An injectable form, olanzapinefor injection (Zyprexa IM), is indicated for agitation associatedwith schizophrenia or bipolar I mania. Olanzapine iscombined with fluoxetine (Symbyax) for use in depressionthat is associated with bipolar I disorder. Peak concentrationsof oral olanzapine are reached at 6 hours after oral administration,and absorption of the compound is not affected byfood.
Olanzapine binds with high affinity at DA D
2, 5-HT
2A,5-HT
2C, 5-HT
6,α1, and H
1 histamine receptors. The effectsof olanzapine for the treatment of schizophrenia are presumablymediated through antagonism at D
2 and 5-HT
2Areceptors.The use of olanzapine in acute maniathat is associated with bipolar I disorder is thought to bemediated by antagonism at D
2 and other monamine receptors.Additionally, olanzapine is postulated to produce itsmood stabilizing and antidepressant effects through 5-HT
2Areceptor blockade and increased cortical DA and NE concentrations.Several studies have investigated the effectof olanzapine-induced weight gain and new-onset type 2diabetes.In a comparison study with risperidone,olanzapine was shown to have a greater risk of producingdyslipidemia and type 2 diabetes.
臨床応用
The thienobenzodiazepine olanzapine is an effective atypical antipsychotic agent that is close in structure to
clozapine but has a somewhat different neuropharmacological profile, in that it is a more potent antagonist at
dopamine D2 and, especially, serotonin 5-HT2A receptors. Olanzapine is well absorbed after oral administration
and is metabolized mainly by CYP1A2 to inactive metabolites, with a variable half-life of approximately 20 to 50
hours.
オランザピン 上流と下流の製品情報
原材料
準備製品