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丁螺环酮。作为一种抗焦虑药的药理特性及治疗效果的初步综述。

Buspirone. A preliminary review of its pharmacological properties and therapeutic efficacy as an anxiolytic.

作者信息

Goa K L, Ward A

出版信息

Drugs. 1986 Aug;32(2):114-29. doi: 10.2165/00003495-198632020-00002.

DOI:10.2165/00003495-198632020-00002
PMID:2874976
Abstract

Buspirone hydrochloride (HCl)1 is a new anxiolytic with a unique chemical structure. Its mechanism of action remains to be elucidated. Unlike the benzodiazepines, buspirone lacks hypnotic, anticonvulsant and muscle relaxant properties, and hence has been termed 'anxioselective'. As evidenced by a few double-blind clinical trials, buspirone 15 to 30 mg/day improves symptoms of anxiety assessed by standard rating scales similarly to diazepam, clorazepate, alprazolam and lorazepam. Like diazepam, buspirone is effective in patients with mixed anxiety/depression, although the number of patients studied to date is small. In several studies, a 'lagtime' of 1 to 2 weeks to the onset of anxiolytic effect has been noted; hence motivation of patient compliance may be necessary. Sedation occurs much less often after buspirone than after the benzodiazepines; other side effects are minor and infrequent. In healthy volunteers, buspirone does not impair psychomotor or cognitive function, and appears to have no additive effect with alcohol. Early evidence suggests that buspirone has limited potential for abuse and dependence. Thus, although only wider clinical use for longer periods of time will more clearly define some elements of its pharmacological profile, with its low incidence of sedation buspirone is a useful addition to the treatments available for generalised anxiety. It may well become the preferred therapy in patients in whom daytime alertness is particularly important.

摘要

盐酸丁螺环酮是一种具有独特化学结构的新型抗焦虑药。其作用机制尚待阐明。与苯二氮䓬类药物不同,丁螺环酮缺乏催眠、抗惊厥和肌肉松弛特性,因此被称为“抗焦虑选择性药物”。一些双盲临床试验表明,丁螺环酮每日15至30毫克改善焦虑症状的效果与地西泮、氯氮䓬、阿普唑仑和劳拉西泮相似,这可通过标准评定量表评估得出。与地西泮一样,丁螺环酮对混合性焦虑/抑郁患者有效,尽管迄今为止研究的患者数量较少。在几项研究中,已注意到丁螺环酮产生抗焦虑作用的起效时间为1至2周的“延迟期”;因此可能需要患者配合治疗。丁螺环酮引起镇静的情况比苯二氮䓬类药物少得多;其他副作用轻微且不常见。在健康志愿者中,丁螺环酮不会损害精神运动或认知功能,而且似乎与酒精没有相加作用。早期证据表明,丁螺环酮的滥用和成瘾可能性有限。因此,尽管只有更长时间的更广泛临床应用才能更清楚地确定其药理学特征的某些方面,但由于其镇静发生率低,丁螺环酮是可用于治疗广泛性焦虑的一种有用药物。对于白天警觉性特别重要的患者,它很可能会成为首选治疗药物。

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Buspirone. A preliminary review of its pharmacological properties and therapeutic efficacy as an anxiolytic.丁螺环酮。作为一种抗焦虑药的药理特性及治疗效果的初步综述。
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本文引用的文献

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Identification and quantitation of 1-(2-pyrimidinyl)piperazine, an active metabolite of the anxiolytic agent buspirone, in rat plasma and brain.抗焦虑药丁螺环酮的活性代谢物1-(2-嘧啶基)哌嗪在大鼠血浆和脑中的鉴定与定量分析。
J Chromatogr. 1982 Dec 3;252:310-4. doi: 10.1016/s0021-9673(01)88424-7.
2
Dopaminergic effects of buspirone, a novel anxiolytic agent.新型抗焦虑药丁螺环酮的多巴胺能效应。
Biochem Pharmacol. 1983 Mar 15;32(6):1069-74. doi: 10.1016/0006-2952(83)90627-5.
3
Comparison of buspirone in two separate studies.在两项独立研究中对丁螺环酮进行的比较。
丁螺环酮治疗大麻依赖:一项随机、安慰剂对照试验。
Drug Alcohol Depend. 2015 Nov 1;156:29-37. doi: 10.1016/j.drugalcdep.2015.08.013. Epub 2015 Aug 25.
4
Buspirone for management of dyspnea in cancer patients receiving chemotherapy: a randomized placebo-controlled URCC CCOP study.丁螺环酮用于接受化疗的癌症患者呼吸困难的管理:一项随机安慰剂对照的URCC CCOP研究。
Support Care Cancer. 2016 Mar;24(3):1339-47. doi: 10.1007/s00520-015-2903-6. Epub 2015 Sep 2.
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Psychopharmacological characterisation of the successive negative contrast effect in rats.大鼠相继负性对比效应的精神药理学特征
Psychopharmacology (Berl). 2015 Aug;232(15):2697-709. doi: 10.1007/s00213-015-3905-2. Epub 2015 Mar 21.
6
Pharmacotherapy of alcohol use disorders: seventy-five years of progress.酒精使用障碍的药物治疗:75年的进展
J Stud Alcohol Drugs Suppl. 2014;75(17):79-88. doi: 10.15288/jsads.2014.s17.79.
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Evaluation of buspirone on streptozotocin induced type 1 diabetes and its associated complications.评价丁螺环酮对链脲佐菌素诱导的 1 型糖尿病及其相关并发症的作用。
Biomed Res Int. 2014;2014:948427. doi: 10.1155/2014/948427. Epub 2014 Jan 20.
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Role of Hypothalamic-pituitary-adrenal-axis in Affective Disorders: Anti-depressant and Anxiolytic Activity of Partial 5-HT1A Agonist in Adrenalectomised Rats.下丘脑-垂体-肾上腺轴在情感障碍中的作用:部分5-羟色胺1A受体激动剂对肾上腺切除大鼠的抗抑郁和抗焦虑活性
Indian J Psychol Med. 2013 Jul;35(3):290-8. doi: 10.4103/0253-7176.119501.
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Phasic and sustained fear are pharmacologically dissociable in rats.在大鼠中,阶段性和持续性恐惧在药理学上是可分离的。
Neuropsychopharmacology. 2011 Jul;36(8):1563-74. doi: 10.1038/npp.2011.29. Epub 2011 Apr 6.
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Management of generalized anxiety disorder in primary care: identifying the challenges and unmet needs.基层医疗中广泛性焦虑障碍的管理:识别挑战与未满足的需求。
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4
Disposition and metabolism of buspirone and its metabolite 1-(2-pyrimidinyl)-piperazine in the rat.丁螺环酮及其代谢产物1-(2-嘧啶基)-哌嗪在大鼠体内的处置与代谢
Xenobiotica. 1983 Mar;13(3):147-53. doi: 10.3109/00498258309052248.
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J Neural Transm. 1983;57(4):255-65. doi: 10.1007/BF01248997.