氯丙咪嗪
舍曲林
药效学
血清素转运体
医学
强迫症
CYP2D6型
药理学
氟西汀
药代动力学
精神科
血清素
内科学
抗抑郁药
细胞色素P450
焦虑
受体
新陈代谢
作者
Sheldon Preskorn,Ryan Rode
标识
DOI:10.1097/pra.0000000000000750
摘要
Clomipramine (CIMI) is an effective treatment for obsessive-compulsive disorder in patients who have failed to respond to trials of selective serotonin transport inhibitors (eg, sertraline). The case presented here illustrates how knowledge of the pharmacodynamics and pharmacokinetics of CIMI in a specific patient can be used to personalize treatment to optimize the likelihood of efficacy (ie, maximum benefit to risk ratio). The approach described in this column considered: (1) the patient’s diminished ability to clear CIMI and its major metabolite, desmethlyclomipramine due to a genetic deficiency in cytochrome P450 2D6 enzyme activity, and (2) the patient’s ability to extensively convert CIMI to desmethlyclomipramine. That conversion impairs the ability to inhibit the serotonin transporter, the mechanism that is most likely responsible for the efficacy of CIMI in obsessive-compulsive disorder.
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