Aisen M L, Dietz M A, Rossi P, Cedarbaum J M, Kutt H
Burke Rehabilitation Center, White Plains, New York 10605.
J Am Paraplegia Soc. 1992 Oct;15(4):211-6. doi: 10.1080/01952307.1992.11761520.
Baclofen is a centrally acting muscle relaxant used for treatment of spasticity. Some patients, to experience adequate symptomatic relief, require dosages of baclofen that significantly exceed the conventional 80 mg daily maximum advocated by the 1992 Physicians' Desk Reference. In this pilot study of baclofen kinetics and dynamics in eleven patients, the safety and efficacy of high dose baclofen was confirmed. The data suggest that the pharmacokinetics of high dose baclofen may vary from those described previously. Time-to-peak plasma levels and plasma half-lives were noted to be substantially longer than prior reports indicate. Baclofen blood levels were observed to rise gradually over time in some patients on a stable dosing regimen, probably a result of impaired renal clearance. These findings may indicate that a change in pattern of prescription is warranted and that a reliable and practical measurement of systemic baclofen levels has a useful role in clinical practice, particularly for the patient with neurogenic bladder and potential renal insufficiency.
巴氯芬是一种用于治疗痉挛的中枢性肌肉松弛剂。一些患者为了获得足够的症状缓解，所需的巴氯芬剂量显著超过1992年《医师案头参考》所倡导的常规每日最大剂量80毫克。在这项针对11名患者的巴氯芬动力学和动态学的初步研究中，高剂量巴氯芬的安全性和有效性得到了证实。数据表明，高剂量巴氯芬的药代动力学可能与先前描述的有所不同。血浆达峰时间和血浆半衰期明显长于先前报告所示。在一些采用稳定给药方案的患者中，观察到巴氯芬血药浓度随时间逐渐升高，这可能是肾清除率受损的结果。这些发现可能表明有必要改变处方模式，并且可靠实用的全身性巴氯芬水平测量在临床实践中具有重要作用，特别是对于患有神经源性膀胱和潜在肾功能不全的患者。
