Antidepressants

The first antidepressant introduced in the late 1950's. In 1957 were discovered by iproniazid and imipramine. The first group was the ancestor of antidepressants, MAO inhibitors, on the basis of the second were synthesized tricyclic antidepressants.

In accordance with modern ideas, with depression decreasing serotoninergicheskaya noradrenergicheskaya and synaptic transmission. It is therefore an important link in the mechanism of action of antidepressants is considered to be caused by the accumulation of brain norepinephrine and serotonin.

MAO inhibitors block monoaminoksidazu - the enzyme that causes oxidative desamidization and inactivation monoanines. There are currently two known forms of MAO - type A and type B, differing in the substrate, are subjected to their operation. MAO type A resulting in desamidization noradrenaline, adrenaline, dofamina, serotonin, tiramina and MAO type B - desamidization feniletilamina and some other amines. There are competitive and non-inhibition, reversible and irreversible. It can be observed substrate specificity of the drug, ie, predominant influence on the different desamidization monoanines. All this greatly affects the therapeutic and pharmacological properties of different MAO inhibitors. For example, iproniazid, nialamid, fenelzin, traniltsipromin irreversibly blocking MAO type A. At the same time pirlindol, tetrindol, metralindol, eprobemid, moklobemid, etc. (which belong to a new generation of antidepressants, MAO ignibitorov) - have on monoaminoksidazu reversible and selective influence .

Tricyclic antidepressants are known thanks to its characteristic trehtsiklicheskoy structure. The mechanism of action due to a seizure of oppression NEUROMEDIATOR monoanines presinapticheskimi the nerve endings, which leads to the accumulation of mediators in the synaptic gap and the activation of synaptic transmission. Most tricyclic antidepressants at the same time reduce the capture of different NEUROMEDIATOR monoanines (norepinephrine, serotonin, dofamina).

Recently created antidepressants that selectively block the reverse capture serotonin (fluvoksamin, fluoxetin, sertralin, etc.).

In addition, there are a number of so-called "atypical" antidepressants, distinct from "typical" how to structure and mechanism of action. There are bi-products and chetyrehtsiklicheskoy structure, which did not reveal any pronounced influence on the activity of either MAO or to capture neuromediators (mianserin, etc.).

Common property of all antidepressants - they timolepticheskoe (antidepressive) effects, ie a positive impact on the emotional (affective), the scope of the patient, with the overall mental state and, in particular, better mood.

Various antidepressants differ, however, the amount of pharmacological properties. So, for imipramine and MAO inhibitors, along with antidepressive, characterized by a catalytic effect, for amitriptyline, pipofezina, fluatsizina, clomipramine, and trimipramina doksepina - on the contrary, sedative. Maprotilin has trankviliziruyuschimi properties pirlindol - nootropnymi, etc.

Many antidepressants are used not only in the psychiatric practice but also in the treatment of a number of (psycho) somatic diseases, vegetative disorders, chronic pain syndromes, etc.

The therapeutic effect of antidepressants develops gradually and can be seen, usually through a 3-10 or more days after the treatment. This is because the development of antidepressive action due to the gradual accumulation of neuromediators in nerve endings and slowly emerging changes in the adaptation cycle neuromediators, and the sensitivity of receptors to the brain.