Chen P C
Nihon Yakurigaku Zasshi. 1978 Oct;74(7):871-83. doi: 10.1254/fpj.74.871.
A long-term study was performed on the effects of fluphenazine decanoate and the results were compared with those of fluphenazine-2HCl and fluphenazine enanthate. These agents given orally were equipotent in inhibiting the motility of mice. With subcutaneous administration, decanoate and enanthate showed a clearly prolonged action, whereas fluphenazine-2HCl was effective for only 3 days. Decanoate and enanthate did not produce marked hypothermia in rats. Like enanthate, decanoate inhibited, for a long duration, apomorphine-induced stereotyped behavior and methamphetamine group toxicity in mice, as well as induced catalepsy in rats. It was found that fluphenazine-2HCl markedly inhibited certain agonists-induced contraction of isolated preparations while enanthate and decanoate inhibited these contractions almost equally. In rats, enanthate induced a persistent hypotension and marked changes in ECG while decanoate showed a transient hypotension and slight changes in ECG. In the study of rat brain catecholamine turnover, these three drugs significantly increased dopamine turnover, and decanoate and enanthate were found to have prolonged effects. No significant change in noradrenaline turnover was observed. These results indicate that fluphenazine decanoate has the same spectrum of activity as enanthate except for its slower onset, weaker potency and longer duration of action. A prolonged tranquilizing effect was most evident.
对癸酸氟奋乃静的作用进行了一项长期研究,并将结果与盐酸氟奋乃静和庚酸氟奋乃静的结果进行了比较。口服这些药物在抑制小鼠活动方面效力相当。皮下给药时,癸酸盐和庚酸盐显示出明显延长的作用,而盐酸氟奋乃静仅有效3天。癸酸盐和庚酸盐在大鼠中未产生明显的体温过低。与庚酸盐一样,癸酸盐长时间抑制阿扑吗啡诱导的小鼠刻板行为和甲基苯丙胺组毒性,以及诱导大鼠僵住症。发现盐酸氟奋乃静显著抑制某些激动剂诱导的离体标本收缩,而庚酸盐和癸酸盐几乎同等程度地抑制这些收缩。在大鼠中,庚酸盐诱导持续低血压和心电图明显变化,而癸酸盐显示短暂低血压和心电图轻微变化。在大鼠脑儿茶酚胺周转率的研究中,这三种药物显著增加多巴胺周转率,并且发现癸酸盐和庚酸盐有延长作用。未观察到去甲肾上腺素周转率有显著变化。这些结果表明,癸酸氟奋乃静除起效较慢、效力较弱和作用持续时间较长外,具有与庚酸氟奋乃静相同的活性谱。延长的镇静作用最为明显。