Department of Neurological Sciences, Sapienza University of Rome, Rome, Italy.
J Neurol. 2010 Nov;257(Suppl 2):S292-7. doi: 10.1007/s00415-010-5734-x.
The controlled-release preparations of levodopa or newer soluble preparations of levodopa may improve levodopa bioavailability and tolerability and help managing (or even preventing) motor complications. Whether the controlled-release preparations or soluble preparations can really take the place of standard levodopa remains highly controversial, especially in patients receiving chronic levodopa therapy. Controlled-release formulations have a longer half-life and provide more stable plasma levels than standard levodopa. In de novo parkinsonian patients, controlled-release levodopa and standard levodopa are equally efficacious, and carry similar motor complication rates. In patients with advanced disease, whether motor fluctuations respond better to controlled release than to standard oral levodopa remains unclear. In selected parkinsonian patients, single bedtime doses of controlled-release levodopa may improve sleep and nocturnal disability. The poor solubility of levodopa may be overcome by soluble formulations that achieve maximal absorption. A levodopa formulation that guarantees faster and more reliable absorption would be especially useful in the clinical treatment of Parkinson's disease patients experiencing "no-on" or "delayed-on" phenomena. However, further studies with these new formulations are needed to understand if they offer better benefit to parkinsonian patients. New dual formulations incorporating both a faster absorption and an increased half-life than standard levodopa are currently under study.
左旋多巴的控释制剂或新型左旋多巴可溶性制剂可能会提高左旋多巴的生物利用度和耐受性，并有助于控制（甚至预防）运动并发症。控释制剂或可溶性制剂是否真的能代替标准左旋多巴，这仍然存在很大争议，尤其是在接受慢性左旋多巴治疗的患者中。控释制剂具有更长的半衰期，提供更稳定的血浆水平，优于标准左旋多巴。在新诊断的帕金森病患者中，控释左旋多巴和标准左旋多巴同样有效，运动并发症发生率相似。在晚期疾病患者中，运动波动对控释制剂的反应是否优于标准口服左旋多巴尚不清楚。在选定的帕金森病患者中，控释左旋多巴单剂量睡前给药可能会改善睡眠和夜间残疾。左旋多巴的溶解度差可以通过达到最大吸收的可溶性制剂来克服。对于经历“无动”或“延迟动”现象的帕金森病患者，一种能保证更快、更可靠吸收的左旋多巴制剂将特别有用。然而，需要进一步研究这些新制剂，以了解它们是否能为帕金森病患者带来更好的益处。目前正在研究新的双制剂，其吸收速度比标准左旋多巴更快，半衰期也更长。
