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癸酸氟哌啶醇。其药效学、药代动力学特性及在精神病治疗中的应用的初步综述。

Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis.

作者信息

Beresford R, Ward A

出版信息

Drugs. 1987 Jan;33(1):31-49. doi: 10.2165/00003495-198733010-00002.

Abstract

Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate has no intrinsic activity: its pharmacodynamic actions are those of haloperidol--primarily that of central antidopamine activity. The monthly administered depot formulation has several clinical and practical advantages over oral haloperidol: better compliance and more predictable absorption; more controlled plasma concentrations; fewer extrapyramidal side effects; less frequent reminders of condition; and reduced medical workload. In open and controlled studies, haloperidol decanoate has produced adequate maintenance or improvement of the condition of patients with psychoses (mainly schizophrenia) when an abrupt change from orally administered haloperidol or other antipsychotic drugs has been instituted. Limited comparative studies indicate that the depot and oral forms of haloperidol are equally effective, and that haloperidol decanoate is at least as effective as depot forms of fluphenazine, pipothiazine, flupenthixol and perphenazine in controlling the symptoms of psychosis. Extrapyramidal side effects and the need for concomitant anti-Parkinsonian drugs may be a problem, but may be less frequent than with oral haloperidol or other depot antipsychotics. Thus, haloperidol decanoate offers a useful alternative in the treatment of psychoses to orally administered haloperidol or to other depot antipsychotic drugs.

摘要

癸酸氟哌啶醇是氟哌啶醇的长效制剂,氟哌啶醇是一种常用的具有抗精神病活性的丁酰苯衍生物。癸酸氟哌啶醇本身无活性:其药效学作用即为氟哌啶醇的作用,主要是中枢抗多巴胺活性。与口服氟哌啶醇相比,每月给药一次的长效制剂具有若干临床和实际优势:更好的依从性和更可预测的吸收;血浆浓度控制更佳;锥体外系副作用更少;对病情的提醒更少;以及减轻医疗工作量。在开放和对照研究中,当从口服氟哌啶醇或其他抗精神病药物突然转换为癸酸氟哌啶醇时,癸酸氟哌啶醇已使精神病患者(主要是精神分裂症)的病情得到充分维持或改善。有限的比较研究表明,氟哌啶醇的长效制剂和口服制剂同样有效,并且在控制精神病症状方面,癸酸氟哌啶醇至少与氟奋乃静、哌泊噻嗪、氟哌噻吨和奋乃静的长效制剂一样有效。锥体外系副作用以及是否需要同时使用抗帕金森病药物可能是个问题,但可能比口服氟哌啶醇或其他长效抗精神病药物的情况更少见。因此,癸酸氟哌啶醇为精神病治疗提供了一种有用的选择,可替代口服氟哌啶醇或其他长效抗精神病药物。

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