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右旋芬氟拉明。其在体重控制中的地位。

Dexfenfluramine. Its place in weight control.

作者信息

Turner P

机构信息

Department of Clinical Pharmacology, St Bartholomew's Hospital, London, United Kingdom.

出版信息

Drugs. 1990;39 Suppl 3:53-62. doi: 10.2165/00003495-199000393-00007.

Abstract

Dexfenfluramine, the dextrostereoisomer of fenfluramine, is a pure serotonin (5-hydroxytryptamine) agonist, apparently devoid of any additional antidopaminergic or sympathomimetic effects. The drug is approximately twice as effective as its racemic predecessor in reducing food intake in animals, and at a dose of 30 mg/day dexfenfluramine substantially modifies eating behaviour in man. Thus, a reduction in the motivation to eat and fewer snacking episodes were seen in volunteers treated with the drug, while total caloric and carbohydrate (but not protein) intakes were reduced in obese carbohydrate cravers. In clinical studies in obesity, dexfenfluramine combined with dietary support has produced mean weight reductions superior to those achieved with placebo over 3-month treatment periods. Importantly, the drug appears to maintain its weight-reducing effects for at least 12 months, without serious adverse effects. Dexfenfluramine appears to possess many of the properties of an 'ideal' pharmacotherapeutic agent for obesity. However, further long term clinical studies are required to confirm the promising efficacy and safety data obtained to date, and to further define the most appropriate indications for its use. Ideally, the drug should be used as adjunctive treatment in the clinical management of more severe cases of obesity, which are refractory to simpler supportive measures such as dietary or psychological counseling.

摘要

右芬氟拉明是芬氟拉明的右旋异构体,是一种纯的血清素(5-羟色胺)激动剂,显然没有任何额外的抗多巴胺能或拟交感神经作用。该药物在减少动物食物摄入量方面的效果约为其消旋前体的两倍,并且在每天30毫克的剂量下,右芬氟拉明能显著改变人的饮食行为。因此,在用该药物治疗的志愿者中,观察到进食动机降低且吃零食的次数减少,而在肥胖的碳水化合物渴望者中,总热量和碳水化合物(但不包括蛋白质)摄入量减少。在肥胖症的临床研究中,右芬氟拉明与饮食支持相结合,在3个月的治疗期内产生的平均体重减轻优于安慰剂。重要的是,该药物似乎至少能维持12个月的减肥效果,且没有严重的不良反应。右芬氟拉明似乎具备许多“理想”的肥胖症药物治疗剂的特性。然而,需要进一步的长期临床研究来证实迄今为止获得的有前景的疗效和安全性数据,并进一步确定其最适合的使用适应症。理想情况下,该药物应用于肥胖症更严重病例的临床管理中的辅助治疗,这些病例对饮食或心理咨询等更简单的支持措施无效。

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