Stephens P
Harvard Department of Psychiatry, McLean Hospital, Belmont, MA 02178.
Compr Psychiatry. 1990 Jul-Aug;31(4):315-26. doi: 10.1016/0010-440x(90)90038-t.
This report reviews over 25 years of literature of the development, pharmacology, proposed mechanism of action, efficacy, adverse effects, and recommendations for use of clozapine. Clozapine, synthesized in 1960, is an efficacious antipsychotic that rarely causes extrapyramidal side effects. However, in the mid-1970s, it was associated with an increased incidence of agranulocytosis resulting in restrictions of use. Recent trials with treatment-resistant schizophrenic patients found clozapine to be superior to chlorpromazine and haloperidol, fortifying the potential contribution of this drug. This has generated optimism that clozapine will obtain Food and Drug Administration approval. Generally well tolerated, the 1% to 2% risk of agranulocytosis can be minimized with careful patient selection, white blood cell (WBC) count monitoring, and weighing of risks versus benefits for use beyond the relatively safe initial 4-week period.
本报告回顾了25年多来有关氯氮平的研发、药理学、作用机制、疗效、不良反应及使用建议的文献。氯氮平于1960年合成,是一种有效的抗精神病药物,很少引起锥体外系副作用。然而,在20世纪70年代中期,它与粒细胞缺乏症发病率的增加有关,导致其使用受到限制。最近针对难治性精神分裂症患者的试验发现,氯氮平优于氯丙嗪和氟哌啶醇,这增强了这种药物的潜在作用。这使人们乐观地认为氯氮平将获得美国食品药品监督管理局的批准。氯氮平一般耐受性良好,通过仔细选择患者、监测白细胞计数以及权衡相对安全的初始4周后使用的风险与益处,可将1%至2%的粒细胞缺乏症风险降至最低。