Thase Michael E
University of Pittsburgh Medical Centre, Western Psychiatric Institute and Clinic, Pittsburgh, PA 15213-2593, USA.
Expert Opin Pharmacother. 2006 Mar;7(4):429-40. doi: 10.1517/14656566.7.4.429.
This article reviews escitalopram, the S-stereoisomer of the racemic compound citalopram, and a highly selective and potent member of the selective serotonin re-uptake inhibitor class of antidepressants. Escitalopram has a straightforward pharmacokinetic profile, little effect on hepatic metabolism, and is relatively safe in overdose. Similar to other members of the selective serotonin re-uptake inhibitor class, escitalopram (10-20 mg/day) is a well-tolerated and effective treatment of major depressive disorder. Although relatively few head-to-head comparative studies with other antidepressants have been published, pooled analyses of studies using citalopram as the active comparator suggest a modest advantage for the stereoisomer. This advantage, which is more apparent among patients with greater symptom levels, may be attributable to a greater than predicted potency compared with citalopram, presumably as a result of the greater effect of escitalopram at the allosteric binding site of the serotonin transporter. Results of two published studies versus venlafaxine also suggest better tolerability in the context of comparable efficacy. Escitalopram is also approved for the treatment of generalised anxiety disorder (in the US) and social anxiety disorder and panic disorder (in the EU). Pharmacoeconomic models suggest that the greater drug acquisition cost of this patent-protected compound may be offset by greater efficacy (relative to generic citalopram) and tolerability (compared with extended release venlafaxine).
本文综述了艾司西酞普兰,它是消旋化合物西酞普兰的S-立体异构体,属于选择性5-羟色胺再摄取抑制剂类抗抑郁药中高选择性且强效的一员。艾司西酞普兰具有简单的药代动力学特征,对肝脏代谢影响小,过量服用时相对安全。与选择性5-羟色胺再摄取抑制剂类的其他成员相似,艾司西酞普兰(每日10 - 20毫克)对重度抑郁症是一种耐受性良好且有效的治疗药物。尽管与其他抗抑郁药的直接对比研究发表得相对较少,但以西酞普兰作为活性对照药的研究汇总分析表明,这种立体异构体具有一定优势。这种优势在症状较严重的患者中更为明显,可能是由于与西酞普兰相比,其效力超出预期,推测这是艾司西酞普兰在5-羟色胺转运体变构结合位点作用更强的结果。两项与文拉法辛对比的已发表研究结果也表明,在疗效相当的情况下,艾司西酞普兰耐受性更好。艾司西酞普兰还被批准用于治疗广泛性焦虑症(在美国)以及社交焦虑症和惊恐障碍(在欧盟)。药物经济学模型表明,这种受专利保护的化合物较高的购药成本可能会被更高的疗效(相对于普通西酞普兰)和耐受性(与缓释文拉法辛相比)所抵消。