Department of Neurology, Innsbruck Medical University, Anichstraße 35, 6020, Innsbruck, Austria.
CNS Drugs. 2019 Sep;33(9):905-918. doi: 10.1007/s40263-019-00661-z.
Satisfactory management of Parkinson's disease is a challenge that requires a tailored approach for each individual. In the advanced phase of the disease, patients may experience motor complications despite optimized pharmacological therapy. Apomorphine, a short-acting D- and D-like receptor agonist, is the only drug proven to have an efficacy equal to that of levodopa, albeit with a shorter time to onset and effect duration. Clinical trials have shown that intermittent apomorphine injections provide rapid and effective relief from unpredictable "off" periods. Continuous apomorphine infusion reduced around 50% of the daily "off" time in several studies. Dopaminergic side effects such as nausea, somnolence and hypotonia, as well as administration site reactions, are often mild or treatable, but somnolence and skin reactions in particular can sometimes be reasons for premature discontinuation. We provide an overview of the pharmacological mechanism of action of the drug in light of its effects on Parkinson's disease symptoms. We then summarize the evidence regarding the efficacy and tolerability of apomorphine, both in its established formulations (subcutaneous intermittent injection and continuous infusion) and in the new preparations currently under investigation.
帕金森病的满意管理是一项挑战,需要为每个个体制定个性化的治疗方案。在疾病的晚期,尽管经过优化的药物治疗,患者仍可能出现运动并发症。阿扑吗啡是一种短效的 D 型和 D 样受体激动剂,是唯一被证明疗效与左旋多巴相当的药物,尽管起效时间和作用持续时间较短。临床试验表明,间歇性阿扑吗啡注射可迅速有效地缓解不可预测的“关期”。几项研究表明,连续阿扑吗啡输注可减少约 50%的日常“关期”时间。多巴胺能副作用,如恶心、嗜睡和低张力,以及给药部位反应,通常较轻或可治疗,但嗜睡和皮肤反应有时可能是提前停药的原因。我们根据阿扑吗啡对帕金森病症状的影响,概述了其药物作用的药理学机制。然后,我们总结了阿扑吗啡在已确立的制剂(皮下间歇性注射和连续输注)和目前正在研究的新制剂中的疗效和耐受性的证据。