Sertraline is a naphthalenamine derivative with the predominant pharmacological action of inhibiting presynaptic reuptake of serotonin from the synaptic cleft. It was initially marketed for the treatment of major depressive disorder and is now approved for the management of panic disorder, obsessive-compulsive disorder and post-traumatic stress disorder. Sertraline is slowly absorbed following oral administration and undergoes extensive first-pass oxidation to form N-desmethyl-sertraline, a weakly active metabolite that accumulates to a greater concentration in plasma than the parent drug at steady state. Sertraline is eliminated from the body by other metabolic pathways to form a ketone and an alcohol, which are largely excreted renally as conjugates. The elimination half-life of sertraline ranges from 22-36 hours, and once-daily administration is therapeutically effective. Steady-state plasma concentrations vary widely, up to 15-fold, in patients receiving usual antidepressant dosages between 50 and 150 mg/day. However, only sparse data have been published that support useful correlations between sertraline plasma concentrations and therapeutic or adverse effects to justify therapeutic drug monitoring. Sertraline has minimal inhibitory effects on the major cytochrome P450 enzymes, and few drug-drug interactions of clinical significance have been documented. Like other selective serotonin reuptake inhibitors, sertraline is well tolerated in therapeutic dosages and relatively safe in overdosage.

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舍曲林的临床药代动力学。

舍曲林是萘胺衍生物，具有主要的药理作用，可抑制突触前裂隙中5-羟色胺突触前再摄取。它最初用于治疗重度抑郁症，现在被批准用于应对恐慌症，强迫症和创伤后应激障碍。舍曲林在口服给药后被缓慢吸收，并经历大量的首过氧化反应以形成N-去甲基-舍曲林，这是一种弱活性代谢产物，在稳态时其血浆中的积累浓度高于母体药物。舍曲林通过其他新陈代谢途径从体内清除，形成酮和酒精，这些酮和酒精在肾脏中作为结合物大量排泄。舍曲林的消除半衰期为22-36小时，并且每天一次给药是治疗有效的。接受50至150毫克/天的常规抗抑郁剂治疗的患者的稳态血浆浓度变化很大，最高可达15倍。但是，仅公开了稀疏的数据来支持舍曲林血浆浓度与治疗或不良反应之间的有用相关性，以证明对治疗药物进行监测是合理的。舍曲林对主要的细胞色素P450酶具有最小的抑制作用，很少有临床意义的药物相互作用。像其他选择性5-羟色胺再摄取抑制剂一样，舍曲林的治疗剂量耐受性良好，并且在用药过量时相对安全。接受50至150毫克/天的常规抗抑郁药剂量的患者。但是，仅公开了稀疏的数据来支持舍曲林血浆浓度与治疗或不良反应之间的有用相关性，以证明对治疗药物进行监测是合理的。舍曲林对主要的细胞色素P450酶具有最小的抑制作用，很少有临床意义的药物相互作用。像其他选择性5-羟色胺再摄取抑制剂一样，舍曲林的治疗剂量耐受性良好，并且在用药过量时相对安全。接受50至150毫克/天的常规抗抑郁药剂量的患者。但是，仅公开了稀疏的数据来支持舍曲林血浆浓度与治疗或不良反应之间的有用相关性，以证明对治疗药物进行监测是合理的。舍曲林对主要的细胞色素P450酶具有最小的抑制作用，很少有临床意义的药物相互作用。像其他选择性5-羟色胺再摄取抑制剂一样，舍曲林的治疗剂量耐受性良好，并且在用药过量时相对安全。很少有临床意义的药物相互作用。像其他选择性5-羟色胺再摄取抑制剂一样，舍曲林的治疗剂量耐受性良好，并且在用药过量时相对安全。很少有临床意义的药物相互作用。像其他选择性5-羟色胺再摄取抑制剂一样，舍曲林的治疗剂量耐受性良好，并且在用药过量时相对安全。