Valdoxan (Agomelatine)

Agomelatine - agonist melatonin (MT1 and MT2 receptors)and the antagonist5HT2c.Represents an energizer, active on validate depression models (the test of the learnt feebleness, the despair test, chronic stress of moderate expressiveness), no less than at models with decinhronise a warm rhythm, and also in experimental situations of alarm and stress. It has been shown that Valdoxan does not influence capture monoamines and has no affinity to an alpha - beta-adrenergicheskim, gistaminergic, holinergic, dophaminergic and benzodiazepines to receptors; it explains absence at Valdoxan characteristic for other energizers of collateral actions on a gastroenteric path, sexual functions and cardiovascular system.

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Agomelatine, thanks to antagonistic action on 5 HT2c receptors, liberation dophamine and noradrenaline, in particular in area prefrontal strengthens brain barks. In experiments on animals with the simulated syndrome of the braked phase of a dream (Delayed Sleep Phase Syndrome) at blind and old animals it has been shown that Valdoxan restores synchronisation cirkad rhythms through stimulation melatonine receptors. At chronic stress Valdoxan interferes with occurrence "broken off" (fragmented) a dream. In experiences on healthy volunteers Agomelatine did not break normal structure of a dream and well influenced a dream at sick of depression. In therapeutic doses Valdoxan prevented development of a sleeplessness and infringements of memory from the moment of reception of a preparation and till the morning.

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Agomelatine does not cause accustoming that has been shown in research on healthy volunteers with use of a visual analogue scale or the Questionnaire of the Research Center on studying of fatal predilections (Addiction Research Center Inventory - ARCI 49 check-list). Valdoxan also investigated about occurrence of a syndrome of cancellation at sick of depression by means of a Questionnaire revealing signs of a syndrome of cancellation (Discontinuation Emergent Signs and Symptoms (DESS)). It was found out that the cancellation syndrome does not develop even at the sharp termination of treatment.
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Valdoxan does not influence weight of a body.
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During the program of clinical development Valdoxan its efficiency and safety against the big depressive frustration was investigated. In плацебо comparative controllable research 4500 patients from whom 2500 received a preparation from 6 weeks about one year are surveyed. Agomelatine it has appeared statistically significantly more effective in comparison with placebo, thus the antidepressive effect comes within two weeks (disorder of efficiency: from 49,1 % to 61 % against 34,3 % - 46,3 % in group receiving placebo).Also the authentic data about efficiency Valdoxan at patients with heavier forms of depressive frustration (indicators of a scale of Hamilton> 25), two thirds of population making more has been obtained. Researches with the active control have confirmed the received results.

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Valdoxan also it was effective at initially high levels of alarm, no less than at a combination of disturbing and depressive frustration. Influence Agomelatine on sexual function sick of depression with remmitic a clinical course was studied. The Scale of studying of influence on sexual sphere (Sex Effects Scale - SEXFX) was used. It has been shown that Agomelatine does not cause sexual infringements and does not influence occurrence of excitation and orgazm. At sick of depression, since second week of treatment, Valdoxan statistically signi/ficantly improved process sleep, without causing thus the subsequent day block.