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The groupPharmaceuticals, specifically eliminate depression emerged in the late 1950s. In 1957, he opened iproniazid that is the genesis of the antidepressants, MAO inhibitors, and imipramin, on the basis of which received Tricyclic antidepressants.
In today's depressed in the state has decreased serotoninergicescoy noradrainergicescoy and synaptic transmission. Therefore, an important link in the mechanism of action of antidepressants is caused by the accumulation in the brain serotonin and norarenalina. MAO inhibitors block monoaminoxydazu enzyme, which causes oxidative dezaminirovanie and inachtiwatia monoaminov. At present, there are now two forms of MAO-type A and type B, which differ in Substrates subject their action. MAO type A is mainly dezaminirovanie norarenalina, adrenaline, dopamine, serotonin, tiramina, and the type of MAO-B dezaminirovanie fenilatilamina and some other amines. Has inhibition competitive and uncompetitive, forming and irreversible. Can occur substrate specificity : predominant influence on dezaminirovanie monoaminov different. All of this plays an important role in the clinical and therapeutic properties of MAO inhibitors. Thus, iproniazid, nialamid, fenelzin, tranilcipromin irreversibly blocking MAO type A and pirlindol, tetrindol, metralindol, eprobemid, moklobemid and others (new generation drugs), had a selective and forming influence.
Tricyclic antidepressants have been dubbed because of the presence of characteristic trehziklicescoy structure. The mechanism of action is related to the oppression of reverse takeover neiromediatornah monoaminov presinapticakimi nerve endings, resulting in the accumulation of mediators in the synaptic junctions and activating cholinergic transmission. Tricyclic antidepressants, as a rule, at the same time reduce the seizure of neiromediatornah amines (norarenalina, serotonin, dopamine). Recently, a antidepressants, mainly blocker (selectively) reverse takeover serotonin (fluoxetin, sertralin, fluvoksamin etc.).
There are so-called "atypical" drugs, as distinct from "typical" both on the structure and mechanism of action. New drugs and stomach cetarehziklicescoy structures, which have been expressed influence either on neiromediatorov seizure, or MAO activity (mianserin, etc.).
Total property all antidepressants -- they timolepticescoe effect, ie a positive impact on the affeguuyu patient accompanied by improvements in mood and overall mental state. Different drugs vary, but the amount of pharmacological properties. Thus, the imipramina and some other antidepressants timolepticeski effect combined with a stimulating, and the amitriptilina, pipofezina, fluazizina, claumipramina, trimipramina, doksepina more pronounced sedative component. The maprotilina antidepressant effect combined with anksioliticski and sedative. MAO inhibitors (nialamid, eprobemid) have incentives properties. Pirlindol, reducing symptoms of depression, is nootroponuu activity improves "fu" ( "" Hotel ") as agent.
24.2.1 been applied not only in a psychiatric practice, but also for the treatment of a number of neirovegetativeh and somatic diseases for chronic pain syndromes, etc.
Therapeutic effect of antidepressants such as oral, and in the application of Injecting develops gradually and is typically 10 days or more after the start of treatment. This is because the development of antidepressive effects associated with the accumulation neiromediatorov of nerve endings and the slowly emerging adaptive changes in the rotation neiromediatorov and sensitivity to the brain receptors.