Olanzapine Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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.
Chemische Eigenschaften
Yellow Crystalline Powder
Verwenden
A serotonin (5-HT2) and dopamine (D1/D2) receptor antagonist with anticholinergic activity. Antipsychotic.
Definition
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.
Allgemeine Beschreibung
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.
Clinical Use
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.
Olanzapine Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
