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Pramipexole: new use for an old drug – the potential use of pramipexole in the treatment of restless legs syndrome

机译:普拉克索:旧药物的新用途–普拉克索在治疗腿不安综合征中的潜在用途

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摘要

Restless legs syndrome (RLS) is characterized by paraesthesias–dysesthesias and motor restlessness worsening at rest–in the evening, with at least temporary relief by activity. Its etiology is unknown, though it could be secondary to various conditions. It is well known, however, that dopamine plays a crucial role in the pathophysiology of RLS, as dopaminergic agonists achieve marked improvement. Pramipexole is a nonergoline compound with selectivity for D3 dopamine receptors. This drug is very effective in the treatment of idiopathic and secondary RLS and in treatment-resistant patients, as shown by double-blind, placebo-controlled studies in adults. In children, studies are much more limited, and RLS is often misdiagnosed as “growing pain” or attention deficit hyperactivity disorder. Pramipexole has been successful in open studies, eliminating clinical symptoms. This medication has the advantage of being free of the frequently encountered problems seen with ergot derivatives. The side-effects are limited, particularly at the dosages usually prescribed for RLS treatment: They are much lower than in Parkinson’s disease, and inappropriate sleepiness and sleep attacks, particularly while driving, or compulsive behavior have not been seen. Compared with the adverse reactions of levodopa, including tolerance, rebound, and augmentation phenomena in RLS, which led to usage of dopamine agonists as first line of treatment for RLS, pramipexole has had one of the best profiles. Augmentation can still be noted with the drug, but after longer usage time compared with many other dopamine agonists. Although excessive daytime sleepiness has been noted, sleep attacks have not been encountered in RLS patients treated with pramipexole.
机译:不安腿综合症(RLS)的特征是感觉异常–感觉异常,休息时运动不安加重–晚上,至少通过活动可暂时缓解。尽管其病因可能是继发于各种情况的,但其病因仍未知。然而,众所周知,多巴胺在RLS的病理生理中起着至关重要的作用,因为多巴胺能激动剂取得了显着改善。普拉克索是一种非麦角灵化合物,对D3多巴胺受体具有选择性。如成人双盲,安慰剂对照研究所示,该药物在治疗特发性和继发性RLS以及对治疗有抵抗力的患者中非常有效。在儿童中,研究更为有限,RLS经常被误诊为“成长性疼痛”或注意力缺陷多动障碍。普拉克索已在开放研究中成功消除了临床症状。这种药物的优点是没有麦角衍生物经常遇到的问题。副作用是有限的,尤其是在通常用于RLS治疗的剂量下:副作用远低于帕金森氏病,并且还没有出现不适的嗜睡和睡眠发作,尤其是在驾驶或强迫行为时。与左旋多巴的不良反应(包括RLS的耐受性,反弹和增强现象)相比,导致多巴胺激动剂被用作RLS的首选治疗方法,普拉克索具有最好的特征之一。仍然可以注意到该药物具有增强作用,但是与许多其他多巴胺激动剂相比,使用时间更长。尽管已经注意到白天过度嗜睡,但在接受普拉克索治疗的RLS患者中未遇到睡眠发作。

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