Escitalopram
Escitalopram
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DOI：
10.1517/13543784.11.10.1477
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发表时间：
2002-10-01
影响因子：
6.1
通讯作者：
Burke, WJ
中科院分区：
文献类型：
--
作者：
Burke, WJ
艾司西普兰草酸盐(5-西酞普兰，来克沙普罗(TM))是一种选择性5-羟色胺再摄取抑制剂抗抑郁药，是西酞普兰的S对映体，目前正在世界各地用于治疗抑郁症和焦虑症的临床开发。临床前研究表明，西酞普兰的治疗活性存在于S-异构体中，而西酞普兰与人5-羟色胺转运体具有很高的亲和力。相反，在这种转运体中，R-西酞普兰的效力类似于埃司西普兰的30倍。艾司西普兰具有线性药代动力学，因此血浆浓度随着剂量的增加而成比例和可预测地增加，其27-32小时的半衰期与每天一次给药一致。此外，艾司匹兰在体外对细胞色素P450药物代谢酶的影响可以忽略不计，这表明药物-药物相互作用的可能性很低。艾司西普兰对严重抑郁障碍患者的疗效已在多项短期安慰剂对照临床试验中得到证明，其中三项试验包括西酞普兰作为积极对照，以及一项为期36周的研究，该研究评估了预防抑郁症复发的有效性。在这些研究中，与安慰剂相比，艾司西妥兰被证明在治疗抑郁症和相关的焦虑症状方面有很强的疗效。在治疗广泛性焦虑症、恐慌症和社交焦虑症方面也显示出疗效。结果还表明，在可比剂量下，艾司西普兰在临床上表现出比西酞普兰更早的安慰剂治疗在统计学上的显著优势。对安全性数据库的分析表明，由于不良事件而停止治疗的比率很低，埃司替普兰10毫克/天和安慰剂在因不良事件而提前停止治疗的患者比例方面没有统计上的显著差异。与埃西妥普兰相关的最常见的不良事件发生的比率高于安慰剂，包括恶心、失眠、射精障碍、腹泻、口干和嗜睡。接受依西他普兰治疗的患者中只有10%出现恶心。
Escitalopram oxalate (5-citalopram, Lexapro((TM))), a selective serotonin re-uptake inhibitor antidepressant which is the S-enantiomer of citalopram, is in clinical development worldwide for the treatment of depression and anxiety disorders. Preclinical studies demonstrate that the therapeutic activity of citalopram resides in the S-isomer and that escitalopram binds with high affinity to the human serotonin transporter. Conversely R-citalopram is similar to 30-fold less potent than escitalopram at this transporter. Escitalopram has linear pharmacokinetics, so that plasma levels increase proportionately and predictably with increased doses and its half-life of 27 - 32 h is consistent with once-daily dosing. In addition, escitalopram has negligible effects on cytochrome P450 drugmetabolising enzymes in vitro, suggesting a low potential for drug-drug interactions. The efficacy of escitalopram in patients with major depressive disorder has been demonstrated in multiple short-term, placebo-controlled clinical trials, three of which included citalopram as an active control, as well as in a 36-week study evaluating efficacy in the prevention of depression relapse. In these studies, escitalopram was shown to have robust efficacy in the treatment of depression and associated symptoms of anxiety relative to placebo. Efficacy has also been shown in treating generalised anxiety disorder, panic disorder and social anxiety disorder. Results also suggest that, at comparable doses, escitalopram demonstrates clinically relevant and statistically significant superiority to placebo treatment earlier than citalopram. Analysis of the safety database shows a low rate of discontinuation due to adverse events, and there was no statistically significant difference between escitalopram 10 mg/day and placebo in the proportion of patients who discontinued treatment early because of adverse events. The most common adverse events associated with escitalopram which occurred at a rate greater than placebo include nausea, insomnia, ejaculation disorder, diarrhoea, dry mouth and somnolence. Only nausea occurred in > 10% of escitalopram-treated patients.