Salawu Fatai Kunle
Division of Neurology, Department of Medicine, Federal Medical Centre Yola, Adamawa State, Nigeria.
Patient Prefer Adherence. 2012;6:49-54. doi: 10.2147/PPA.S11841. Epub 2012 Jan 16.
This article reviews the role of an extended-release formulation of pramipexole in the treatment of Parkinson's disease at an early stage. Pramipexole is a nonergot D(2)/D(3) synthetic aminobenzothiazole derivative that is effective as monotherapy in early disease and as an adjunct to levodopa in patients with motor fluctuations. Although levodopa is the current "gold standard" for treatment of Parkinson's disease, its effectiveness fades rapidly and its use results in serious motor fluctuations (on-off, wearing-off, freezing, involuntary movements) for most patients with the disease. Pramipexole has selective actions at dopamine receptors belonging to the D(2) subfamily, where it possesses full activity similar to dopamine itself. Its preferential affinity for the D(3) receptor subtype could contribute to its efficacy in the treatment of both the motor and psychiatric symptoms of Parkinson's disease. The best approach to medical management of early Parkinson's disease remains controversial. While enormous progress has been made in the treatment of the disease, challenges still remain. A variety of treatment-related and patient-related factors must be taken into account when making these decisions. The current approach to treatment of early Parkinson's disease depends in part on individual patient factors, including age, severity and nature of symptoms and their impact, presence of cognitive dysfunction, possible underlying behavioral factors predisposing to impulse control disorders, and other comorbidities. Today, the once-daily extended-release formulation of pramipexole offers the advantages of easy continuous delivery of drug and convenience to patients, particularly early in the disease when monotherapy is the rule. Thus, a new "levodopa-sparing" paradigm for treating Parkinson's disease may now be possible, whereby patients are initially treated with pramipexole and levodopa is added only as necessary.
本文综述了普拉克索缓释制剂在帕金森病早期治疗中的作用。普拉克索是一种非麦角类D(2)/D(3)合成氨基苯并噻唑衍生物，在疾病早期作为单一疗法有效，在有运动波动的患者中作为左旋多巴的辅助药物。虽然左旋多巴是目前治疗帕金森病的“金标准”，但其疗效迅速消退，对大多数患者而言，使用它会导致严重的运动波动（开关现象、剂末现象、冻结现象、不自主运动）。普拉克索对属于D(2)亚家族的多巴胺受体具有选择性作用，在该受体上它具有与多巴胺本身相似的完全活性。其对D(3)受体亚型的优先亲和力可能有助于其治疗帕金森病的运动和精神症状。早期帕金森病的最佳药物治疗方法仍存在争议。虽然在该疾病的治疗方面已取得巨大进展，但挑战依然存在。在做出这些决定时，必须考虑各种与治疗相关和与患者相关的因素。目前早期帕金森病的治疗方法部分取决于个体患者因素，包括年龄、症状的严重程度和性质及其影响、认知功能障碍的存在、可能导致冲动控制障碍的潜在行为因素以及其他合并症。如今，普拉克索每日一次的缓释制剂具有药物易于持续给药以及方便患者的优点，尤其是在疾病早期以单一疗法为主时。因此，现在可能出现一种治疗帕金森病的新的“左旋多巴节省”模式，即患者最初用普拉克索治疗，仅在必要时添加左旋多巴。
