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新型食欲抑制剂氟替雷司在人体中的初步评估。

Preliminary assessment of flutiorex, a new anorectic drug, in man.

作者信息

Giudicelli J F, Richer C, Berdeaux A

出版信息

Br J Clin Pharmacol. 1976 Feb;3(1):113-21. doi: 10.1111/j.1365-2125.1976.tb00578.x.

Abstract

1 The effects of +/--flutiorex, a new anorectic agent, on food intake, the sympathetic nervous system and the central nervous system were compared to those of fenfluramine and a placebo in a double-blind trial involving six healthy volunteers. 2. Flutiorex exerts a singificant anorectic effect and was shown to be approximately twice as potent as fenfluramine in this regard. 3 Flutiorex induces a definite alpha-adrenergic sympathomimetic stimulation as was shown by a rise in systolic blood pressure and the development of marked mydriasis. 4 Flutiorex is a central nervous system stimulant producing an increase in critical flicker frequency. It does not, however, influence psychomotor coordination as reflected in the pursuit rotor test. 5 Serial determinations of blood and urine levels of flutiorex and its deethylated metabolite, norflutiorex, showed that flutiorex is rapidly absorbed and deethylated, accumulates in large quantities in the tissues and, like its metabolite, is excreted in the urine in very small quantities. Blood levels of norflutiorex appear to remain elevated longer than those fo flutiorex.

摘要
  1. 在一项涉及六名健康志愿者的双盲试验中,将新型食欲抑制剂±氟替雷司与芬氟拉明和安慰剂相比较,观察其对食物摄取、交感神经系统及中枢神经系统的影响。2. 氟替雷司具有显著的食欲抑制作用,在这方面其效力约为芬氟拉明的两倍。3. 氟替雷司可引起明确的α-肾上腺素能拟交感神经刺激作用,表现为收缩压升高及明显的瞳孔散大。4. 氟替雷司是一种中枢神经系统兴奋剂,可使临界闪烁频率增加。然而,在跟踪旋转试验中,它并不影响精神运动协调能力。5. 对氟替雷司及其脱乙基代谢产物去甲氟替雷司的血药浓度和尿药浓度进行系列测定,结果表明,氟替雷司吸收迅速且能脱乙基,在组织中大量蓄积,与其代谢产物一样,经尿液排泄的量极少。去甲氟替雷司的血药浓度似乎比氟替雷司维持升高的时间更长。

相似文献

6
Anorectic effectiveness of differing dosage forms of fenfluramine.
Curr Ther Res Clin Exp. 1976 Jun;19(6):589-94.

本文引用的文献

5
Fenfluramine and critical flicker frequency.
J Pharm Pharmacol. 1967 May;19(5):337-8. doi: 10.1111/j.2042-7158.1967.tb08098.x.

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