Escitalopram

Escitalopram （Lexapro，Cipralex）is a selective inihibitor of serotonin(5-HT) reuptake (SSRI) with a Ki value of 6.6nM for [3H]-5-HT uptake [1].

Escitalopram is the S-(+)-enantiomer of citalopram and has the inhibition of [3H]-5-HT uptake and [125I]-RTI-55 binding in COS-1 cells expressing the human serotonin transporter (5-HTT) with Ki values of 6.6±1.4nM and 3.9±2.2nM, respectively. In addition, Escitalopram has been reported to inhibit the accumulation of 3H-labelled monoamines into rat brain synaptosomes in vitro with IC50 values of 2.1±0.75nM, 2500±202nM and 40000±15500nM for [3H]-5-HT, [3H]-I-NA and [3H]-DA, respectively. Apart from these, Escitalopram has shown the in vitro affinity for rat histamine H1 receptors and the rat sigma σ1 site with Ki values of 1500±780nM and 100±71nM, respectively [1].

References:
[1] Sánchez C1, Bergqvist PB, Brennum LT, Gupta S, Hogg S, Larsen A, Wiborg O. Escitalopram, the S-(+)-enantiomer of citalopram, is a selective serotonin reuptake inhibitor with potent effects in animal models predictive of antidepressant and anxiolytic activities. Psychopharmacology (Berl). 2003 Jun;167(4):353-62. Epub 2003 Apr 26.

Efficacy and tolerability of escitalopram in treatment of major depressive disorder with anxiety symptoms: a 24-week, open-label, prospective study in Chinese population.[Pubmed:28255239]

Neuropsychiatr Dis Treat. 2017 Feb 17;13:515-526.

BACKGROUND: Significant anxiety symptoms are associated with poor clinical course and outcome in major depressive disorder (MDD). This single-arm, open-label study aimed to evaluate the efficacy and tolerability of Escitalopram treatment in patients with MDD and anxiety symptoms. METHODS: Adult patients with MDD and anxiety symptoms (Montgomery-Asberg Depression Rating Scale [MADRS] >/=22 and Hamilton Anxiety Rating Scale [HAM-A] >/=14) were enrolled and received Escitalopram (10-20 mg/day) treatment for 24 weeks. Symptom status was assessed by MADRS, 17-item-Hamilton Depression Rating Scale, HAM-A, and Clinical Global Impression Scale at baseline and the following visits. Quality of life was assessed by Short Form-12, and safety was evaluated by adverse events, laboratory investigations, vital signs, and physical findings. RESULTS: Overall, 200 of 318 (66.2%) enrolled patients completed the 24-week treatment. The remission (MADRS 2%) were headache (4.0%), nasopharyngitis (3.6%), nausea (3.0%), and dizziness (2.6%). Serious TEAEs were reported by 1.3% patients; no deaths were reported. CONCLUSION: Escitalopram 10-20 mg/day was effective and well-tolerated in the long-term treatment of MDD with anxiety symptoms in adult Chinese population.

The impact of childhood maltreatment on the differential efficacy of CBASP versus escitalopram in patients with chronic depression: A secondary analysis.[Pubmed:28326653]

Clin Psychol Psychother. 2017 Sep;24(5):1155-1162.

Childhood maltreatment (CM) has been indicated as a predictor of a differential response to antidepressant treatment with psychotherapy compared to medication. In this secondary analysis, we investigated whether the presence of CM results in a differential indication for the Cognitive Behavioral Analysis System of Psychotherapy (CBASP) or Escitalopram plus clinical management (ESC). Sixty patients with chronic depression were randomized to either 22 sessions of CBASP or ESC over the course of 8 weeks of acute and 20 weeks of extended treatment at 2 German treatment sites. CM was assessed using the Childhood Trauma Questionnaire and the clinician rated Early Trauma Inventory. Intention-to-treat analyses were used to examine the impact of CM on depression, global functioning, and quality of life. The presence of CM did not result in significant differences in treatment response to CBASP or ESC on any outcome measure after 28 weeks of treatment independent of the type of CM assessment. After 8 weeks, a significant CM x treatment interaction was found for scores on the Montgomery-Asberg Depression Rating Scale. Patients with a history of CM receiving CBASP had a significantly lower response rate compared to patients without CM and to those receiving ESC after 8 weeks. Conclusively, CBASP and ESC are equally effective treatment options for the difficult to treat subgroup of patients with chronic depression and a history of CM. CM may be a predictor of a longer latency of treatment response in the case of psychotherapy. KEY PRACTITIONER MESSAGE: CBASP and Escitalopram are equally effective treatment options for chronic depression. Both treatments are also equally effective for the difficult to treat subgroup of patients with chronic depression and a history of childhood maltreatment. Childhood maltreatment may result in a longer latency of treatment response in the case of psychotherapy.

Efficacy and safety of escitalopram in treatment of severe depression in Chinese population.[Pubmed:28299626]

Metab Brain Dis. 2017 Jun;32(3):891-901.

Severe depression accounts for one-third of depressed patients. Increasing severity of depression usually hinders patients from achieving remission. This study evaluated the efficacy and safety of Escitalopram in acute-phase treatment of severe major depressive disorder (MDD). A total of 225 participants with severe MDD (Diagnostic and Statistical Manual of Mental Disorders, 4th Edition criteria), with a current depressive episode and Montgomery-Asberg Depression Rating Scale (MADRS) score of >/=30 were enrolled. Participants received flexible dose Escitalopram (10-20 mg/d) treatment for 8 weeks. Symptoms status was assessed by MADRS, Hamilton Depression Rating Scale (HAM-D-17), and Hamilton Anxiety Rating Scale (HAM-A). Quality of life was assessed by Short Form-12 (SF-12) and safety by adverse events, laboratory investigations, vital signs and physical findings. The remission (MADRS total score 4%) were somnolence (9.0%), nausea (7.7%), hyperhidrosis (4.5%), dry mouth and dizziness (4.1% each). No serious TEAEs were reported. Escitalopram was effective and well-tolerated for acute-phase treatment of severe depression in Chinese population.