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Mirtazapine is a very strong H 1 receptor antagonist and, as a result, it can cause powerful sedative and hypnotic effects. [11] A single 15 mg dose of mirtazapine to healthy volunteers has been found to result in over 80% occupancy of the H 1 receptor and to induce intense sleepiness. [92]
In addition, due to their blockade of certain serotonin receptors, serotonergic neurotransmission is not facilitated in unwanted areas, which prevents the incidence of many side effects often associated with selective serotonin reuptake inhibitor (SSRI) antidepressants; [1] [3] hence, in part, the "specific serotonergic" label of NaSSAs. [2]
Dosages of 50 mg to 75 mg daily are usually satisfactory as maintenance therapy for elderly patients who do not tolerate higher amounts. [ 21 ] [ 22 ] In any case, 225 m.g./d. is the absolute-maximum highest recommended dose for this drug, as any more can predispose more significantly to seizures. 150 m.g. is the average optimal daily dose for ...
0.25 mg dose Ramosetron: Benzimidazole derivative 5-HT 3 receptor antagonist 5.8 hours 300 μg/kg Tropisetron [30] Indole: 5-HT 3 receptor antagonist 5.6 hours CYP 3A3/4/5, CYP2D6: 200 μg/kg Vortioxetine: Phenylpiperazine: 5-HT 3 receptor antagonist Antidepressant 66h CYP 2D6/ 2A6/CYP2B6/CYP2C8/9, CYP2C19: 5 mg, 10 mg, 20 mg doses
Notably, esmirtazapine has a shorter half life of around 10 hours, compared to R-mirtazapine and racemic mixture, which has a half-life of 18–40 hours. [1] Merck has run several studies on low dose (3–4.5 mg) esmirtazapine for the treatment of insomnia.
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Besides mirtazapine, they also block the α 1-adrenergic receptor [citation needed]. Conversely, whereas TCAs have relatively low affinity for the α 2 -adrenergic receptor , mianserin and mirtazapine potently antagonize this receptor, and this action is thought to be involved in their antidepressant effects [ citation needed ] .
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