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Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Esmirtazapine is an antidepressant having antagonist action on 5-HT2A and H1 receptors. It showed good hypnotic effects in patients of insomnia. Esmirtazapine was found to improve the time to fall asleep, maintenance and total duration of sleep with course of 6 weeks. The drug is well tolerated, no rebound insomnia seen except for residual daytime effect as one of its side effects. A double-blind trial of 2 weeks was conducted in non-elderly adult patients with primary insomnia which showed improved sleep parameters as compared with placebo and the dose used was well tolerated and safe (Ivgy-May et al., 2015).
Managing vasomotor symptoms effectively without hormones
Published in Climacteric, 2020
C. A. McCormick, A. Brennan, M. Hickey
Esmirtazapine is an enantiomer of the sleep-promoting antidepressant mirtazapine that acts antagonistically at histamine, serotonin, and adrenergic receptors. Esmirtazapine has a stronger and more selective affinity for the histamine receptor 5-HT2A. Two double-blind phase 3 RCTs have demonstrated a modest reduction in moderate to severe VMS with a reduction in frequency of 1.4–2.4 per day with doses over 4.5 mg56. Individual change in baseline severity scores only remained significant for doses of esmirtazapine over 18 mg compared with placebo at 12 weeks. Adverse events included somnolence, fatigue, and weight gain. Discontinuation due to adverse events was over 19% at high doses (18 mg), suggesting that esmirtazapine may not be well tolerated at therapeutic doses for VMS56.
Esmirtazapine treatment of postmenopausal vasomotor symptoms: two randomized controlled trials
Published in Climacteric, 2019
M. Birkhaeuser, J. Bitzer, S. Braat, Y. Ramos
Weight gain associated with mirtazapine has been linked to its affinity for H1 receptors25 and 5-HT2C receptors26. In our studies, increasing body weight was generally observed with greater increases from baseline corresponding with higher esmirtazapine doses. These findings are consistent with two randomized, double-blind, placebo-controlled studies of esmirtazapine for insomnia treatment8,21. In a 6-week study, the proportion of participants with ≥7% weight gain, defined by the Food and Drug Administration as clinically significant, was 0.7% for esmirtazapine 3.0 mg and placebo, and 4.9% for esmirtazapine 4.5 mg21.