Gram L F, Kragh-Sørensen P, Kristensen C B, Møller M, Pedersen O L, Thayssen P
Adv Biochem Psychopharmacol. 1984;39:399-411.
For TCAs there is a strong rationale for drug level monitoring in clinical therapy. Therapeutic drug concentration ranges have been established in controlled studies with NT, imipramine, and AT. It has been shown that by appropriate choice of antidepressant and close monitoring of drug levels, treatment with antidepressants in elderly and other risk patients can be carried out effectively and safely, reducing the use of electroconvulsive therapy. Finally, the practical clinical use of antidepressant concentration measurements is now feasible and not expensive, and the analytical procedures can be established in most hospital settings. On the basis of these premises the following can be concluded: Plasma level monitoring should be used as a routine for imipramine, NT, and AT. Further plasma level studies on other antidepressants and in overdose cases should be initiated. Plasma level monitoring is indispensable in clinical research on antidepressants (trials, new drugs, toxicology). Pharmacokinetic considerations may be useful to determine which receptor effects are clinically relevant in therapy and toxicology.
对于三环类抗抑郁药(TCAs),在临床治疗中进行血药浓度监测有充分的理论依据。在对去甲替林(NT)、丙咪嗪和阿米替林(AT)的对照研究中已确定了治疗药物浓度范围。研究表明,通过合理选择抗抑郁药并密切监测血药浓度,可有效且安全地对老年人及其他高危患者进行抗抑郁药治疗,减少电休克治疗的使用。最后,目前抗抑郁药浓度测定在实际临床中的应用可行且成本不高,大多数医院都能建立分析程序。基于这些前提,可以得出以下结论:应将血药浓度监测作为丙咪嗪、NT和AT的常规操作。应启动对其他抗抑郁药及过量用药情况的进一步血药浓度研究。血药浓度监测在抗抑郁药的临床研究(试验、新药、毒理学)中不可或缺。药代动力学考量可能有助于确定在治疗和毒理学中哪些受体效应具有临床相关性。