Goa K L, Ward A
Drugs. 1986 Aug;32(2):114-29. doi: 10.2165/00003495-198632020-00002.
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.
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。