Grzesiak Magdalena, Beszłej Jan Aleksander, Szewczuk-Bogusławska Monika
Katedry i Kliniki Psychiatrii AM we Wrocławiu.
Psychiatr Pol. 2003 Sep-Oct;37(5):825-37.
Therapeutic drug monitoring (TDM) is used to optimise therapy by an assessment of the drug's plasma concentration. The indications for TDM according to Preskorn are: 1. well defined relationships between plasma concentration of a drug and its therapeutic efficacy, and between plasma level and adverse events and/or toxicity, 2. narrow therapeutic index of a drug, 3. significant interindividual variability of the dose--plasma concentration relationship, 4. delayed onset of action, 5. difficulty in early diagnosis of toxic events. Tricyclic antidepressants (TCA's) fulfill many criteria for TDM. Interethnic and interindividual differences in pharmacokinetics of TCA's lead to pronounced differences of plasma level. Interindividual variability of plasma concentration of TCA's is connected with age, concomitant diseases, genetically determined polimorphism of cytochrome P-450 enzymes (e.g. CYP2D6) and co-medications (the drug may change pharmacokinetic properties of TCA's). There is no clear relationship between plasma concentration of TCA's and therapeutic efficacy of a drug. Contrary there is clear correlation between plasma level and adverse events (especially cardiotoxic and neurotoxic AE). Therapeutic ranges of plasma concentration for TCA's are well established. In the case of SSRI's or newer antidepressants the clear relationship between plasma level and their therapeutic effect, that is their efficacy and tolerability has not been determined yet. The relationships between plasma concentrations and efficacy and tolerability of TCA's, as well as therapeutic ranges of TCA's and other antidepressants are presented in this paper.
治疗药物监测(TDM)用于通过评估药物的血浆浓度来优化治疗。根据普雷斯科恩的观点,TDM的适应证为:1. 药物血浆浓度与其治疗效果之间以及血浆水平与不良事件和/或毒性之间存在明确的关系;2. 药物的治疗指数狭窄;3. 剂量-血浆浓度关系存在显著的个体间差异;4. 起效延迟;5. 毒性事件的早期诊断困难。三环类抗抑郁药(TCA)符合TDM的许多标准。TCA药代动力学的种族间和个体间差异导致血浆水平存在明显差异。TCA血浆浓度的个体间差异与年龄、伴随疾病、细胞色素P-450酶(如CYP2D6)的基因决定多态性以及联合用药(该药物可能改变TCA的药代动力学特性)有关。TCA的血浆浓度与药物的治疗效果之间没有明确的关系。相反,血浆水平与不良事件(尤其是心脏毒性和神经毒性不良事件)之间存在明显的相关性。TCA的血浆浓度治疗范围已经明确。对于选择性5-羟色胺再摄取抑制剂(SSRI)或新型抗抑郁药,血浆水平与其治疗效果(即疗效和耐受性)之间的明确关系尚未确定。本文介绍了TCA的血浆浓度与疗效和耐受性之间的关系,以及TCA和其他抗抑郁药的治疗范围。