Nyholm Dag, Lennernäs Hans
Department of Neuroscience, Neurology, Uppsala University Hospital, Uppsala, Sweden.
Expert Opin Drug Metab Toxicol. 2008 Feb;4(2):193-203. doi: 10.1517/17425255.4.2.193.
Symptomatic treatment of Parkinson's disease (PD) is based on the dopamine precursor levodopa. Levodopa is only absorbed in the small intestine, where transit time is approximately 3 h and the plasma elimination half-life is short. Therefore, gastric emptying is a major determining factor for onset of symptom relief.
Gastric emptying is delayed in PD, thereby causing motor fluctuations such as 'delayed on'. Factors that further slow gastric emptying should be recognised and eliminated if possible.
A literature search was performed with the aim to cover the area of irregular gastrointestinal drug absorption in PD.
RESULTS/CONCLUSION: Methods for facilitation of pyloric passage or increase of bioavailability are discussed. Development of new drug formulations and alternative routes of administration is ongoing. Transdermal patches and pumps for subcutaneous or intraduodenal infusions are available for patients with severe fluctuations due to erratic gastric emptying.
帕金森病(PD)的症状性治疗基于多巴胺前体左旋多巴。左旋多巴仅在小肠吸收,小肠转运时间约为3小时,且血浆消除半衰期较短。因此,胃排空是症状缓解起效的主要决定因素。
PD患者存在胃排空延迟,从而导致运动波动,如“起效延迟”。应识别并尽可能消除进一步减慢胃排空的因素。
进行文献检索,旨在涵盖PD患者胃肠道药物吸收不规则的领域。
结果/结论:讨论了促进幽门通过或提高生物利用度的方法。新型药物制剂和替代给药途径的研发正在进行中。对于因胃排空不稳定而出现严重波动的患者,可使用透皮贴剂以及用于皮下或十二指肠内输注的泵。