药品详情：
【依地普仑escitalopram 简述】
依地普仑又名依他普仑，商品名Lexapro，本品是选择性5-羟色胺（5-HT）抑制剂，是抗抑郁药西酞普兰的衍生物（S-西酞普兰消旋体），通过对5-HT再摄取的抑制而起到增强中枢神经系统5-羟色胺能的活性。
【依地普仑escitalopram 适应症】
依地普仑escitalopram用于严重的抑郁性障碍和一般焦虑症。
【依地普仑escitalopram 规格】
本品为片剂，每片含有效成份5mg/10mg/20mg，每瓶100片装。
【依地普仑escitalopram 服用方法】
口服，推荐剂量为每日10mg，如有必要，1周后可增至每日20mg。
【依地普仑escitalopram 注意事项】
1.依地普仑与其他中枢神经药物同时使用时需谨慎。
2.依地普仑与乙醇同时使用时需谨慎。
3.室温保存（15～30℃）。
【依地普仑escitalopram 不良反应】
1.常见心悸、高血压；罕见心动过缓、心动过速、心电图异常、面色潮红、静脉曲张。
2.中枢和外周神经系统：常见偏头痛；罕见震颤、多动、眩晕、肌紧张亢进、不随意运动。
3.胃肠道：常见食欲增加、胃灼热、胃肠炎、腹部绞痛；罕见食管反流、胃胀气、腹泻、嗳气、吞咽困难、恶心、胃息肉、痔疮等。
4.全身性：常见过敏、面潮红、发热、肢痛、胸痛；罕见四肢浮肿、腿痛、寒战、晕厥。
5.血液和淋巴系统紊乱：罕见贫血、鼻出血、淋巴结病、血肿。
6.骨骼肌系统紊乱：常见关节痛、肌痛；罕见肌肉痛性痉挛、关节僵直、背不适。
7.代谢性紊乱：常见体重增加；罕见高血糖、体重减轻、口渴、胆红素增加、痛风、血胆红素增加。
8.精神系统紊乱：常见嗜睡；罕见精神过敏、恐惧、激动、健忘、神经质、抑郁、有自杀倾向、幻听。
9.生殖系统紊乱（女性）：常见经期痉挛、经期紊乱；罕见月经过多、白带增加、乳房肿大、盆腔炎、经前期综合征。
10.呼吸系统：常见咳嗽、鼻窦充血、支气管炎；罕见哮喘、喉炎、气管炎、肺炎、气短。
11.皮肤：常见皮疹；罕见毛囊炎、斑秃、湿疹、瘙痒症、脂肪瘤。
12.感觉异常：常见视力模糊、耳鸣；罕见眼干、眼涩、味觉异常、结膜炎、视觉障碍、瞳孔放大。
13.泌尿系统：常见尿频、泌尿系统感染；罕见尿急、排尿困难、血尿、肾结石。
escitalopram
Escitalopram, sold under the brand names Cipralex and Lexapro among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.[2] Escitalopram is mainly used to treat major depressive disorder or generalized anxiety disorder.[2] It is taken by mouth.[2]
Common side effects include trouble sleeping, nausea, sexual problems, and feeling tired.[2]More serious side effects may include suicide in people under the age of 25.[2] It is unclear if use during pregnancy or breastfeeding is safe.[3] Escitalopram is the (S)-stereoisomer of the earlier medication citalopram, hence the name escitalopram.[2]
Escitalopram was approved for medical use in the United States in 2002.[2] In the United States the wholesale cost is about $2.04 per month as of 2017.[4] In the United Kingdom, as of 2018, non-proprietary escitalopram is around 1 / 20th as costly as the proprietary version.[5] Escitalopram is sometimes replaced by twice the dose of citalopram.[6] In 2016 it was the 26th most prescribed medication in the United States with more than 25 million prescriptions.[7]
Medical uses
Escitalopram has FDA approval for the treatment of major depressive disorder in adolescents and adults, and generalized anxiety disorder in adults.[2] In European countries and Australia, it is approved for depression (MDD) and anxiety disorders, these include: general anxiety disorder (GAD), social anxiety disorder (SAD), obsessive-compulsive disorder (OCD), and panic disorder with or without agoraphobia.
Depression
Escitalopram was approved by regulatory authorities for the treatment of major depressive disorder on the basis of four placebo controlled, double-blind trials, three of which demonstrated a statistical superiority over placebo.[8]
Controversy existed regarding the effectiveness of escitalopram compared to its predecessor citalopram. The importance of this issue followed from the greater cost of escitalopram relative to the generic mixture of isomers of citalopram, prior to the expiration of the escitalopram patent in 2012, which led to charges of evergreening. Accordingly, this issue has been examined in at least 10 different systematic reviews and meta analyses. As of 2012, reviews had concluded (with caveats in some cases) that escitalopram is modestly superior to citalopram in efficacy and tolerability.[9][10][11][12]
A 2011 review concluded that second-generation antidepressants appear equally effective, although they may differ in onset and side effects.[13] Treatment guidelines issued by the National Institute of Health and Clinical Excellence and by the American Psychiatric Association generally reflect this viewpoint.[14][15]
In 2018, a systematic review and network meta-analysis comparing the efficacy and acceptability of 21 antidepressant drugs showed escitalopram to be one of the most effective.[16]
Anxiety disorder
Escitalopram appears to be effective in treating general anxiety disorder, with relapse on escitalopram (20%) less than placebo (50%).[17]
Escitalopram appears effective in treating social anxiety disorder.[18]
Other
Escitalopram, as well as other SSRIs, are effective in reducing the symptoms of premenstrual syndrome, whether taken in the luteal phase only or continuously.[19] There are no good data available for escitalopram as treatment for seasonal affective disorder as of 2011.[20] SSRIs do not appear to be useful for preventing tension headaches or migraines.[21][22]
Overdose
Excessive doses of escitalopram usually cause relatively minor untoward effects, such as agitation and tachycardia. However, dyskinesia, hypertonia, and clonus may occur in some cases. Therapeutic blood levels of escitalopram are usually in the range of 20–80 μg/L but may reach 80–200 μg/L in the elderly, patients with hepatic dysfunction, those who are poor CYP2C19 metabolizers or following acute overdose. Monitoring of the drug in plasma or serum is generally accomplished using chromatographic methods. Chiral techniques are available to distinguish escitalopram from its racemate, citalopram.[41][42][43] Escitalopram seems to be less dangerous than citalopram in overdose and comparable to other SSRIs.[44]
Mechanism of action
Binding profile[45]
Site Ki (nM)
SERT 0.8-1.1
NET 7,800
DAT 27,400
5-HT1A >1,000
5-HT2A >1,000
5-HT2C 2,500
α1 3,900
α2 >1,000
D2 >1,000
H1 2,000
mACh 1,240
Escitalopram increases intrasynaptic levels of the neurotransmitter serotonin by blocking the reuptake of the neurotransmitter into the presynaptic neuron. Of the SSRIs currently on the market, escitalopram has the highest selectivity for the serotonin transporter (SERT) compared to the norepinephrine transporter (NET), making the side-effect profile relatively mild in comparison to less-selective SSRIs.[46]
Escitalopram is a substrate of P-glycoprotein and hence P-glycoprotein inhibitors such as verapamil and quinidine may improve its blood brain barrier penetrability.[47] In a preclinical study in rats combining escitalopram with a P-glycoprotein inhibitor, its antidepressant-like effects were enhanced.[47]
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