Gancher S
Department of Neurology, Oregon Health Sciences University, Portland, USA.
J Neural Transm Suppl. 1995;45:137-41.
The pharmacokinetic properties of apomorphine in patients with Parkinson's disease are described. Apomorphine is lipophilic; it has a large volume of distribution and is rapidly cleared from plasma, with an elimination half life of 33 minutes. It is rapidly absorbed following subcutaneous injection, with peak levels achieved within 5-10 minutes in most patients. There is a large variation in absorption between patients but is more constant within patients following repeated dosing. Apomorphine rapidly equilibrates between plasma and brain. Like levodopa, the response tends to be largely "all or none"; larger doses produce a longer duration of effect within a 30-90 minute range. Apomorphine may be administered intranasally and sublingually; of these routes, the former is more quickly and completely absorbed. Other routes of administration, including rectally, are not as well absorbed but may also be used effectively.
描述了阿扑吗啡在帕金森病患者中的药代动力学特性。阿扑吗啡具有亲脂性；其分布容积大，能迅速从血浆中清除，消除半衰期为33分钟。皮下注射后吸收迅速，大多数患者在5 - 10分钟内达到峰值水平。患者之间的吸收差异很大，但重复给药后患者体内的吸收更稳定。阿扑吗啡在血浆和脑之间迅速达到平衡。与左旋多巴一样，反应往往在很大程度上是“全或无”的；较大剂量在30 - 90分钟范围内产生更长的作用持续时间。阿扑吗啡可经鼻内和舌下给药；在这些给药途径中，前者吸收更快、更完全。其他给药途径，包括直肠给药，吸收不太好，但也可有效使用。
