Lapierre Y D
Prog Neuropsychopharmacol Biol Psychiatry. 1983;7(4-6):641-6. doi: 10.1016/0278-5846(83)90038-6.
Clinical observations are not always consistent with laboratory findings where half-life or pharmacokinetics do not always correlate with pharmacodynamics, ie. clinically effective duration of action. The parent compound, chlordiazepoxide, was observed to have anticonvulsant, anxiolytic, muscle relaxant properties to varying degrees. Subsequently, diazepam seemed to exert a greater potency in these three areas. The final metabolite, oxazepam, has been observed to have a different therapeutic profile. The advent of the triazolo compounds brought a new dimension to benzodiazepine treatment both in primary and side effects. The relationship between blood levels and clinical efficacy is considered in the light of clinical observations as well as in the perspective of clinical management. Problems of tolerance and escalation of dosage must be addressed in the administration of these drugs where the confluence of pharmacokinetic and pharmacodynamic findings may serve as a guide in the management of anxious patients.
临床观察结果并不总是与实验室结果一致,因为半衰期或药代动力学并不总是与药效学相关,即临床有效作用持续时间。母体化合物氯氮卓被观察到具有不同程度的抗惊厥、抗焦虑和肌肉松弛特性。随后,地西泮在这三个方面似乎具有更强的效力。最终代谢产物奥沙西泮具有不同的治疗特性。三唑类化合物的出现为苯二氮䓬类药物的治疗带来了新的维度,无论是在主要作用还是副作用方面。血液水平与临床疗效之间的关系从临床观察以及临床管理的角度进行了考量。在使用这些药物时,必须解决耐受性和剂量增加的问题,药代动力学和药效学结果的融合可为焦虑症患者的管理提供指导。