올란자핀

개요Zyprexa 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-HT2/D2 antagonist with anticholinergic activity. It has a greater antagonistic effect at 5-HT2a than at dopamine D2 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.

용도A serotonin (5-HT2) and dopamine (D1/D2) receptor antagonist with anticholinergic activity. Antipsychotic.

일반 설명Olanzapine, 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 D2, 5-HT2A,5-HT2C, 5-HT6,α1, and H1 histamine receptors. The effectsof olanzapine for the treatment of schizophrenia are presumablymediated through antagonism at D2 and 5-HT2Areceptors.The use of olanzapine in acute maniathat is associated with bipolar I disorder is thought to bemediated by antagonism at D2 and other monamine receptors.Additionally, olanzapine is postulated to produce itsmood stabilizing and antidepressant effects through 5-HT2Areceptor 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.