Kintscher Ulrich
Charité - Universitätsmedizin, Institute of Pharmacology, Berlin, Germany.
Handb Exp Pharmacol. 2012(209):339-47. doi: 10.1007/978-3-642-24716-3_15.
Pharmacological inhibition of monoamine reuptake transporters has been known for many years as an effective therapy to reduce food intake and body weight in obese subjects. However, most of the marketed drugs failed after a distinct period in clinical use and had to be withdrawn because of serious adverse effects resulting in a negative benefit-risk profile. The most common side effects for this drug class included increases in systemic or pulmonary blood pressure and/or heart rate, cardiac valvulopathies, higher cardiovascular event rates, psychiatric disorders, or high abuse potential. The recent withdrawal of sibutramine as result of its adverse actions on the cardiovascular system highlighted again the problems with this drug class in antiobesity therapy. Recent developments to combine reuptake inhibitors with other drug classes, for example, opioid antagonists seem to be a promising approach to improve the benefit-risk profile of these compounds.This chapter will discuss the history of this drug class in appetite control, its mechanism of action, and the clinical effects of selected drugs from this class.
多年来，人们一直知道对单胺再摄取转运蛋白进行药理抑制是减少肥胖受试者食物摄入量和体重的有效疗法。然而，大多数已上市的药物在临床使用一段时间后失败，并因严重不良反应导致利弊比不佳而不得不撤回。这类药物最常见的副作用包括全身或肺血压和/或心率升高、心脏瓣膜病、较高的心血管事件发生率、精神障碍或高滥用潜力。西布曲明因对心血管系统的不良作用而最近被撤回，这再次凸显了这类药物在抗肥胖治疗中的问题。将再摄取抑制剂与其他药物类别（例如阿片类拮抗剂）联合使用的最新进展似乎是改善这些化合物利弊比的一种有前景的方法。本章将讨论这类药物在食欲控制方面的历史、其作用机制以及这类药物中某些选定药物的临床效果。
