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[胆碱酯酶抑制剂治疗重症肌无力——原则与药理监测]

[Therapy of myasthenia gravis with cholinesterase inhibitors--principles and pharmacologic monitoring].

作者信息

Henze T

机构信息

Abt. Akut-Neurologie, Neurologisches Fach- und Rehabilitationskrankenhaus, Kliniken Schmieder, Allensbach.

出版信息

Fortschr Neurol Psychiatr. 1996 Mar;64(3):110-21. doi: 10.1055/s-2007-996377.

DOI:10.1055/s-2007-996377
PMID:8900891
Abstract

Cholinesterase inhibitors are still important in the treatment of myasthenic patients. Therapeutic principles, indications and adverse effects are discussed in detail. Methods of pharmacological monitoring had been searched over many years. Besides determination of pyridostigmine plasma concentration, erythrocyte-bound acetylcholinesterase (AChE) activity could provide a possibility to monitor therapy with cholinesterase inhibitors. 88 patients with myasthenia gravis were investigated. The results demonstrated that after pyridostigmine erythrocyte-bound as well as synaptic AChE is inhibited. Moreover, erythrocyte-bound AChE has proven to be a parameter of cholinesterase inhibitor effect. After injection of edrophonium-chloride (Tensilon) inhibition of AChE activity can be demonstrated as well. During steady pyridostigmine doses stable plasma concentrations and AChE inhibition depend on the respective dosage. Higher daily doses result in greater stability of pharmacologic parameters, whereas low daily doses lead to great interindividual differences of AChE inhibition even after equal pyridostigmine doses. Intraindividually there is no strong correlation, too. Therefore estimation of erythrocyte-bound AChE activity is not useful for routine pharmacological monitoring of cholinesterase inhibitor therapy, but may be helpful in some clinical conditions. The method provides some advantages over pyridostigmine plasma concentration, since it is applicable for other cholinesterase inhibitors, too, and since it requires less technical equipment and time.

摘要

胆碱酯酶抑制剂在重症肌无力患者的治疗中仍然很重要。本文详细讨论了其治疗原则、适应证及不良反应。多年来一直在探寻药理监测方法。除了测定吡啶斯的明血浆浓度外,红细胞结合型乙酰胆碱酯酶(AChE)活性可为监测胆碱酯酶抑制剂治疗提供一种可能。对88例重症肌无力患者进行了研究。结果表明,服用吡啶斯的明后,红细胞结合型以及突触型AChE均受到抑制。此外,红细胞结合型AChE已被证明是胆碱酯酶抑制剂效果的一个参数。注射氯化依酚氯铵(腾喜龙)后,也可证明AChE活性受到抑制。在吡啶斯的明剂量稳定期间,稳定的血浆浓度和AChE抑制作用取决于各自的剂量。每日剂量较高会导致药理参数更稳定,而每日剂量较低即使在吡啶斯的明剂量相同的情况下也会导致个体间AChE抑制作用存在很大差异。个体内部也没有很强的相关性。因此,估计红细胞结合型AChE活性对胆碱酯酶抑制剂治疗的常规药理监测并无用处,但在某些临床情况下可能会有所帮助。该方法比吡啶斯的明血浆浓度具有一些优势,因为它也适用于其他胆碱酯酶抑制剂,并且所需的技术设备和时间较少。

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