Burke R E, Fahn S
Ann Neurol. 1985 Jul;18(1):35-40. doi: 10.1002/ana.410180107.
Although trihexyphenidyl has been used effectively for many years in the treatment of Parkinson's disease, little is known about its pharmacokinetics. Using a sensitive radioreceptor assay for anticholinergic drugs, we assayed trihexyphenidyl in human serum and studied its pharmacokinetics following short-term and long-term administration to patients with dystonia. Previously untreated patients had a biphasic semilogarithmic plot of serum concentration-time consisting of an initial rapid distribution phase and a later slower elimination phase. Patients on long-term treatment showed only the slower elimination phase. Elimination followed first-order kinetics and was rapid, with a half-life of 3.7 +/- 0.4 (SEM) hours. There was no relationship between half-life and peak serum level, age, duration of therapy, or etiology or severity of dystonia. Although acute anticholinergic side effects paralleled the rise and fall of serum anticholinergic levels, the response of dystonia did not.
尽管苯海索多年来一直有效地用于治疗帕金森病，但其药代动力学却鲜为人知。我们使用一种针对抗胆碱能药物的灵敏放射受体分析法，测定了人血清中的苯海索，并研究了对肌张力障碍患者短期和长期给药后的药代动力学。未经治疗的患者血清浓度 - 时间呈双相半对数图，包括初始快速分布相和随后较慢的消除相。长期治疗的患者仅表现出较慢的消除相。消除遵循一级动力学且迅速，半衰期为3.7 +/- 0.4（标准误）小时。半衰期与血清峰值水平、年龄、治疗持续时间或肌张力障碍的病因或严重程度之间没有关系。尽管急性抗胆碱能副作用与血清抗胆碱能水平的升降平行，但肌张力障碍的反应并非如此。
