Effects of selective serotonin reuptake inhibitors on mood. Antidepressants without a prescription: what they are, how they differ from tranquilizers Other treatment strategies

Serotonin is one of the neurotransmitters of the nervous system. It is also considered the hormone of happiness, as it has a very positive effect on human emotions. This biologically active substance is formed from the amino acid tryptophan, which comes from outside with food.

Serotonin synthesis occurs in the pineal gland. As a transmitter, serotonin takes part in the transmission of impulses between neurons, thus carrying information to different parts of the brain. Due to serotonin receptors, serotonin has the ability to regulate and control most processes occurring in organs and systems. This is possible because serotonin receptors are present not only in neurons, but also in vascular walls, in the gastrointestinal tract, and in the muscles of the bronchial walls. Impulse transmission occurs electrically, during the transition of ions between neurons.

First of all, for the work of neurons. In the CNS he is responsible for:

• good mood;
• memory;
• cognitive functions;
• regulates appetite;
• nutritional and sexual;
• social behavior of an individual.

One of its major functions is that melatonin, the sleep hormone, is produced from serotonin. Thus, serotonin is directly involved in circadian rhythms - sleep and wakefulness.

With melatonin deficiency, insomnia develops. Serotonin is also involved in thermoregulation and the functioning of the thyroid gland, increasing the production of TSH in the pituitary gland. Serotonin also increases the production of insulin, which, in turn, increases tryptophan. Therefore, after eating chocolate, your mood will improve: blood glucose rises, insulin rises, tryptophan rises, serotonin rises.

Serotonin increases the synthesis of prolactin and milk secretion, and is responsible for the proper course of pregnancy, childbirth and uterine contractions during them.

Participates in normal intestinal motility, stimulates respiratory rate, increases blood clotting, reduces pain sensitivity, and increases stress resistance. But excess serotonin exaggerates the positive, which is not very good.

What happens when there is a lack of serotonin

With its deficiency, a person develops anxiety and irritability. A person becomes sensitive to pain, his biorhythms are disrupted, and the functioning of the central nervous system is disrupted. The main manifestation of this is the development of migraine pain and depression, obsessive-compulsive disorder syndromes, which can cause visual illusions.

Antidepressants

To bring a person out of a state of depression, it is necessary to resort to the prescription of various psychotropic drugs; Among them are new generation antidepressants – SSRIs. Meaning: selective serotonin reuptake inhibitors.

What can they give? How do they show themselves? They can improve mood, relieving a person of such negative aspects as anxiety and apathy, melancholy and emotional stress.

They make a person resistant to stress, restore biorhythms, stabilize sleep and improve appetite.

Mechanism of action of SSRIs

To understand the mechanism of their action, it is worth remembering a little the physiology of the central nervous system. At the sites where impulses are transmitted between neurons, there is a synaptic cleft, where serotonin, which carries information, is released.

What happens next: the mediator transmitted the signal, his role is over. Now he should be eliminated as unnecessary, on the principle that the Moor has done his job - the Moor can leave. The fact is that if the transmitter is not removed and remains on the postsynaptic membrane, it will interfere with the receipt of new information from new signals.

Removal of unnecessary neurotransmitter molecules occurs in several ways: diffusion, enzymatic breakdown and reuse by reuptake - serotonin reuptake. These reactions are very complex and there is no need to bother your head with them. You just need to know that SSRIs block the inhibition of these molecules and prolong the effect of serotonin, accumulating and sending it into the bloodstream.

The selectivity of inhibitors is manifested in the fact that they selectively act on only serotonin receptors. Thus, serotonin can no longer return to its cell; its signal goes to other cells that are in a state of inhibition and depression.

They are activated and depression gradually softens and decreases. Serotonin itself increases in the synaptic cleft and goes into the bloodstream, reaching other receptors too.

The half-life of the drugs takes about a day and is excreted by the kidneys. This group of antidepressants varies in terms of effectiveness.

List of SSRIs and their effects

The drugs are considered 3rd generation antidepressants. They have certain advantages and disadvantages. The pharmacological effect is manifested in the correction of a depressive background, reducing anxiety and melancholy, some phobias, improving appetite, and a slight analgesic effect.

The advantage of inhibitors is that they are easier to tolerate by patients, do not produce a cardiotoxic effect, do not aggravate glaucoma, and do not lead to severe sedation and hypotension, which is typical, for example, of TCAs (tricyclic antidepressants such as amitriptyline). SSRIs can be prescribed on an outpatient basis. They can also be prescribed if there are contraindications to the use of TCAs.

The most popular in use are: Fluoxetine, Prozac, Paroxetine, Citalopram, Indalpin, Sertraline, Fluvoxamine, Femoxetine, etc. The result of treatment does not appear immediately, only after 4-5 weeks.

Stimulation of serotonin receptors by stimulating them during the entire period of taking SSRIs necessarily produces side effects, like a double-edged sword: due to the fact that the receptors are represented very widely in various organs, with long-term use of SSRIs dyspeptic symptoms occur: abdominal pain, nausea and vomiting, stool disorders, even gastrointestinal bleeding; sexual disorders such as anorgasmia, delayed ejaculation. Insomnia (every 4-5 patients) and anxiety may occur. Disorders from the gastrointestinal tract are noted in 1-2 weeks of use, then they disappear. Violations on the part of the central nervous system are much more persistent.

Indications

In addition to depression, SSRIs are prescribed for social phobias, anxiety neurosis, panic attacks, obsessions, anorexia, stress after injury, and chronic algia. In general practice, they are prescribed for uncontrolled appetite, obesity, PMS, borderline disorders, and alcoholism.

Opinions differ about the effectiveness of SSRIs: psychiatrists in Russia believe that selective inhibitors help better with moderate forms of depression - mild and moderate; in severe cases the effect is less. But in the West, they are doing their best to prove the effectiveness of these drugs for any form of depressive disorders.

What SSRIs are not compatible with

The simultaneous use of inhibitors and other drugs carries a great risk. SSRIs cannot be combined with MAOIs; this causes serotonin syndrome, one of the most serious complications in the patient. When combining TCAs and SSRIs, the dosage of TCAs is reduced, otherwise their amount may increase and a toxic effect may occur.

Lithium salts increase the serotonergic effects of SSRIs, and the unpleasant effects of lithium itself are more pronounced. SSRIs, when used simultaneously with antipsychotics, increase extrapyramidal disorders because they increase the level of antipsychotics in the blood serum.

The same applies to antipsychotics such as Rispolept (atypical). SSRIs cannot be combined with aspirin and NSAIDs, antiplatelet agents; the risk of gastrointestinal bleeding increases. In addition, NSAIDs significantly reduce the effect of SSRIs. The combination of the group with ethanol, sedatives, and barbiturates enhances the effect of the latter on the central nervous system.

Serotonin syndrome

This dangerous, potentially fatal condition is perhaps the most serious side effect of SSRI use. It develops when they are combined with serotonergic antidepressants - for example, MAOIs.

The clinical picture has symptoms of 3 groups:

1. From the central nervous system, autonomic nervous system and neuromuscular system.
2. On the part of the central nervous system, any manifestations of excitement: dysphoria, agitation, hypomania and anxiety, dyssomnia and hallucinations, confusion and delirium.
3. On the part of the ANS – symptoms of dyspepsia – rumbling in the abdomen, vomiting and nausea, loose stools, abdominal pain; fever, chills, hyperhidrosis, cephalgia, salivation and lacrimation, mydriasis, tachycardia, apnea, blood pressure surges.

Neuromuscular disorders: convulsions, increased reflexes - these 2 symptoms are the most common; disturbance of gait, coordination, paresthesia, muscle tension to the point of rigidity, spasm of the masticatory muscles, tremor of the whole body.

Against this background, CVS disorders occur, severe myopathy with the destruction of muscle tissue (rhabdomyolysis), the appearance of myoglobin in the urine - appears during the breakdown of protein, acute renal failure, liver failure, increased potassium content in the blood, a dangerous form of violation of the blood glucose level towards oxidation (acidosis), aspiration pneumonia, NK, strokes, drop in white blood cells and platelets, seizures. To prevent such a complication, you need to take some precautions: at least 2 weeks should pass between taking drugs of different groups.

The same principle must be observed when prescribing drugs from the same group. An interval of 5 weeks should be after discontinuation of Fluoxetine and the appointment of an irreversible MAOI, for the elderly - 8 weeks. For return transfer – 4 weeks.

At the first sign of complications, all medications taken are immediately discontinued. Then self-elimination of manifestations may occur within 24 hours. Symptomatic treatment of the condition is also carried out. In severe cases, serotonin antagonists are prescribed; infusion therapy; measures to reduce temperature, mechanical ventilation, lowering blood pressure, muscle relaxants.

Contraindications to the use of SSRIs

Individual intolerance, mania, MAOI use, gestation and breastfeeding, epilepsy. There are also no prescriptions for those with a history of antidepressant-induced mania. Contraindications are acute renal failure, liver failure; attacks of glaucoma; the presence of ulcerative lesions of the gastrointestinal tract; alcohol and other intoxications.

Withdrawal syndrome

Withdrawal syndrome is characteristic not only of SSRIs, but also of all antidepressants. In this case, somatic and mental symptoms are noted. They occur with abrupt, immediate withdrawal of the drug and are difficult to tolerate by patients.

They go away in only 5-6 weeks. Moreover, the shorter the half-life of the drug taken, the more severe the withdrawal syndrome. This syndrome especially occurs when taking Paroxetine, followed by Fluvoxamine.

What symptoms might there be? Weakness and cephalgia, dizziness, nausea and vomiting, diarrhea, muscle pain, paresthesia, tremors, insomnia, unsteady gait, unreasonable anxiety and irritability, agitation, mood swings, panic attacks and arrhythmias.

Anxiety and depression produce similar withdrawal symptoms. In such cases, the drug is resumed and gradually withdrawn. To prevent this syndrome, medications should be gradually discontinued, over a period of at least a month.

Criticism

Many foreign critics argue that there is no evidence that the root of depression is a lack of serotonin. The serotonin hypothesis is therefore incorrect. The same mistrust is caused by the effects of SSRIs. But manufacturers and advertisers widely use this thesis. A number of American and English famous psychiatrists also question the serotonin theory.

There is a lot of evidence for this opinion. Some clinical studies have shown a connection between taking Fluoxetine, Sertraline and Paroxetine and the appearance of hostility, a tendency to self-destruction, and aggression in patients. Many pharmaceutical companies that make SSRIs hide these facts and greatly downplay them.

This was discovered by independent researchers and FDA experts. They give such side effects a very vague name - emotional lability. It has been noted that the number of suicides in America has increased since the late 50s, when the first antidepressants began to appear on the market.

There were many sensational cases on this issue in 2000. the amount of compensation in court regarding, for example, the side effects of Prozac, reached $50 million. WHO data also notes that patients taking Paroxetine experience very severe withdrawal symptoms when compared with other antidepressants. The company GlaxoSmithKline, which produces paroxetine, has long and persistently denied the possibility of addiction to the drug.

The same applies to other SSRI manufacturers Eli Lilly and Company and Pfizer. In 2002, the FDA issued a warning, and the International Federation of Pharmaceutical Manufacturers Associations announced similar fraud by pharmaceutical companies on TV in the United States. Hundreds of lawsuits have been brought forward, although companies have assured that such manifestations are the result of depression itself or caused by an overdose of an antidepressant.

A BBC report in 2002 also stated that paroxetine causes aggression, self-harm, and suicide. The plaintiffs' lawyers studied the companies' internal documentation and discovered the fact that GlaxoSmithKline, back in 1989, had information about an 8-fold increase in the risk of suicide when taking its products.

The fact is that serotonin reuptake is not as simple and good as it seems at first glance. Presynaptic neurons turn out to be unclaimed and actually release less serotonin, while postsynaptic neurons are no longer sensitive to it.

After 4-5 weeks of taking selective inhibitors, the brain’s efforts to compensate and level out the biochemical situation are not effective, and side effects appear. For example, excess serotonin leads to mania. To relieve side effects, new drugs are prescribed all the time and long-term negative changes appear in the functioning of neurons.

When the drug is discontinued, serotonin rapidly decreases, and there is nothing to compensate for it. Presynaptic synapses no longer release enough of it, and postsynapses do not have the required number of receptors. Suicidality and mania often occur in adolescents and children after using SSRIs. Suicidal behavior in adults is still under study. All this suggests that when prescribing SSRIs, the doctor must approach each patient individually and constantly monitor his condition. Today, SSRIs remain quite popular antidepressants and are widely prescribed in Russia.

There are many groups of medications that are aimed at psychotropic correction in the treatment of anxiety and depressive conditions.

All of them have a common mechanism of action, the essence of which is to control the influence of certain neurotransmitters on the state of the central nervous system, depending on the genesis of the disease. According to research, a central deficiency of serotonin in synoptic transmission has a special effect on the pathogenesis of depression, by controlling which one can regulate mental activity.

Selective serotonin reuptake inhibitors (SSRIs) are third generation drugs that are relatively easily tolerated by patients. They are used for the treatment of depressive disorders and disorders in mono and poly therapy.

This group of medications works by maintaining the continued activity of central serotonergic processes by preventing the uptake of serotonin by brain tissue, as a result of which the mediator, accumulating in the receptor area, exerts its influence on them longer.

The main advantage of SSRIs over other groups is the selective inhibition of only one type of biogenic amines, which helps prevent unwanted side effects on the body. This has a positive effect on the body’s tolerance of this group of drugs, due to which their popularity among patients and specialists is growing every year.

Mechanism of action and pharmacological properties

When serotonin is released from the fibers of the nerve endings in the area of ​​the reticular formation, which is responsible for wakefulness, as well as the limbic system, which is responsible for controlling the emotional state, it enters a space called the synoptic cleft, where it attaches to special serotonin receptors.

During this interaction, the neurotransmitter excites the cell membranes of these structures, thereby increasing their activity. As a result, this substance breaks down under the action of special enzymes, after which its elements are recaptured by the structures through which its initial release was made.

Reuptake inhibitors exert their influence at the stage of enzymatic breakdown of serotonin, preventing its destruction, promoting the subsequent accumulation and prolongation of its stimulating effects.

As a result, the increase in neurotransmitter activity eliminates the pathological processes of depressive and phobic disorders, and compensates for the deficit in emotional behavior and regulation of mental states.

Scope of application

The main purpose of using this group of antidepressants is to suppress various types of depression by providing a stimulating effect on brain structures.

SSRIs are also used in the following cases:

This group of drugs is also effective in the treatment of alcoholism and withdrawal symptoms.

Restrictions and contraindications

Taking SSRI antidepressants is prohibited if there are psychostimulant drugs in the blood or while under the influence of alcohol or drugs.

The combination of several drugs with serotonergic effects is contraindicated. The use of serotonin reuptake inhibitors is also incompatible if there is a history of serotonin reuptake inhibitors.

Hepatic and renal failure, as well as cardiovascular diseases in the decompensation stage are a contraindication to the use of selective inhibitors.

1. Nausea, vomiting, congestion in the intestines and, as a result, constipation.
2. Restless states may occur and develop to the point of insomnia or reversion to increased sleepiness.
3. Increased nervous agitation, appearance, loss of visual acuity, appearance of skin rash are possible, a change in the phase of the disease is possible with a transition from depressive to manic.
4. There may be an appearance, decreased libido, development in the form of, or acute. There is an increase in prolactin production.
5. With long-term use, a phenomenon such as loss of motivation with emotional dulling, which is also known as SSRI-induced apathy syndrome, is possible.
6. Bradycardia may develop, and a decrease in sodium levels in the blood may occur, leading to edema.
7. When taking drugs during pregnancy, spontaneous abortions are possible as a result of a teratogenic effect on the fetus, as well as developmental abnormalities in late pregnancy.
8. In rare cases, it is possible with corresponding mental, autonomic and neuromuscular disorders.

Food for thought

According to recent studies, the treatment of endogenous depression in adolescence is effective and safe when used as therapy with SSRI antidepressants, due to the absence of such side effects as when taking tricyclic drugs.

The predictability of the treatment effect allows us to provide the correct treatment to this group of patients, despite the atypical symptoms of depression at this age associated with neurobiological changes in adolescence.

SSRIs make it possible, already at the initial stages of treatment, to prevent exacerbation of the condition and reduce the relevance of suicidal behavior, which is typical for people suffering from juvenile depression.

Also, serotonin reuptake inhibitors have proven effective in the treatment of postpartum depression and have a positive effect in menopausal syndrome in the form of depression and depressive states, which allows the use of antidepressants as a replacement for hormonal therapy.

TOP 10 popular SSRI drugs

Ten selective serotonin reuptake inhibitors that are deservedly popular among patients and doctors:

Full list of drugs available for 2017

An exhaustive list of SSRIs, which consists of all the active substances of the group, as well as drugs based on them (trade names).

Structural formulas of popular SSRIs (clickable)

Preparations based on;

• Prozac;
• Deprex;
• Flunisan;
• Fluval;
• Profluzak;
• APO-fluoxetine;
• Prodep;
• Flunate;
• Fluxonil;
• Fludak.

This group of drugs has a stimulating and thymoanaleptic effect. Medicines are used for different types of depression.

• Avoxin.

The drugs specifically inhibit serotonin reuptake and have an anxiolytic effect. Used for the prevention and treatment of obsessive-compulsive disorders. They also have an effect on adrenergic, histamine and dopamine receptors.

• Paroxetine;
• Rexitin;
• Serestill;
• Plizil;
• Actaparoxetine;
• Apo-paroxetine.

The group has anxiolytic and sedative properties. The active substance has a bicyclic structure, which distinguishes it from other drugs.

With a long course, the pharmacokinetic properties do not change. The main indications cover endogenous, neurotic and reactive depression.

Preparations based on Sertraline:

• Oprah;
• Pram;
• Sedopram;
• Siozam;
• Moral;
• Citalift;
• Citalorin;
• Cytol;
• Citalopram.

The group has minimal third-party effects on dopamine and adrenergic receptors. The main therapeutic effect is aimed at correcting emotional behavior, leveling feelings of fear and. The therapeutic effect of other groups of antidepressants may be enhanced by simultaneous interaction with Citalopram derivatives.

Medicines based on Escitalopram:

Medicines are used for. The maximum therapeutic effect develops 3 months after starting to take this group of SSRI drugs. Medicines practically do not interact with other types of receptors. Most of the metabolites are excreted by the kidneys, which is a distinctive feature of these derivatives.

General treatment regimen

Drugs from the group of selective serotonin reuptake inhibitors are used once a day. This may be for a different time period, but most often it is taken in the morning before meals.

The medicinal effect occurs after 3-6 weeks of continuous treatment. The result of the body's response to therapy is regression of symptoms of depressive states, after complete suppression of which the therapeutic course is continued for 4 to 5 months.

It is also worth considering that in the presence of individual intolerance or resistance of the body, manifested in the absence of a positive result within 6-8 months, the group of antidepressants is replaced with another. The dosage of the drug per dose depends on the derivative substance; as a rule, it ranges from 20 to 100 mg per day.

Once again about warnings!

Antidepressants are contraindicated for use in cases of renal and liver failure, due to a violation of the elimination of drug metabolites from the body, resulting in toxic poisoning.

Serotonin reuptake inhibitors should be used with caution in people whose work requires high concentration and attention.

In diseases that cause tremor, such as, antidepressants can increase the negative clinical picture, which can negatively affect the patient’s condition.

Taking into account the fact that inhibitors have a teratogenic effect, they are not recommended for use during pregnancy and lactation.

It should be remembered that if the body is severely physically exhausted, drugs in this group cannot be used due to the risk of even greater suppression of appetite.

It is also always worth remembering about withdrawal syndrome, which is a complex of negative symptoms that develop when the course of treatment is abruptly stopped:

However, these drugs have their own disadvantages, which are manifested in incomplete knowledge of all their properties and the presence of certain side effects characteristic only of SSRIs.

Pharmacotherapy of depressive conditions

S. Puzhinsky. The work briefly outlines the main stages in the development of pharmacotherapy for depression, provides a classification of antidepressant drugs according to the criteria of their chemical structure and mechanism of action (tricyclic antidepressants, serotonin reuptake inhibitors - selective and non-selective, dopamine inhibitors; MAO inhibitors - selective and non-selective, reversible and irreversible; others ). The main pharmacokinetic parameters and profiles of psychotropic activity of drugs from the main groups of thymoleptics, indications for clinical use and side effects are presented. Combinations of antidepressant drugs and their interactions with other drugs and chemicals are also considered. Factors that can lead to distortion of data from clinical trials of psychotropic drugs are separately analyzed and the role of clinical practice as the main criterion for the effectiveness of new antidepressants is emphasized. This paper presents a review of the history of pharmacotherapy of depressions together with classification of anti-depressants according to their chemical structure and and neurochemical mechanisms (tricyclic antidepressants, selective and non-selective inhibitors of serotonin re-uptake, MAO inhibitors and others). The basic pharmacokinetic principals as well as psychotropic profiles, indications and side-effects of these antidepressants are also described. Possible variants of combination of anti-depressants and their interactions with other drugs and chemicals are considered in this paper. Special attention is paid to the analysis of the factors that can lead to misinterpretation of the controlled study data concerning the effectiveness of psychtropic drugs and the role of every-day clinical practice in evaluation of this effectiveness is emphasized. Introduction Psychopharmacology and psychopharmacotherapy of depressive states are dynamically developing research areas that, on the one hand, stimulate the development of ideas about the pathogenesis of affective disorders, and on the other, the synthesis of new antidepressant drugs. The introduction of tricyclic antidepressants (TCAs) into psychiatric practice at the border of the 50-60s, and the discovery shortly thereafter of the preventive properties of lithium carbonate, carbamazepine (Tegretol, Finlepsin), as well as sodium valproate derivatives, significantly changed the prognosis of many depressed patients (this applies to duration, severity and frequency of phases). At the same time, the number of patients whose treatment is possible on an outpatient basis has expanded significantly. In the history of pharmacotherapy for depression, several stages and important dates can be distinguished. However, the history of the development of pharmacotherapy for depression is still far from complete; It is possible that we are still at the beginning of the journey. The main criterion for classifying a drug into the group of antidepressants is its therapeutic effect on symptom complexes of endogenous depression (at least of moderate severity). The effect of the drug should concern all the main components of the depressive syndrome. A medicine that acts selectively on one of the manifestations of depression, such as sleep disturbance or psychomotor inhibition (amphetamine), or has an anxiolytic effect (benzodiazepines), is not an antidepressant. The number of drugs classified as antidepressants reaches 50 and is represented by several hundred drugs produced by various pharmaceutical companies. Classification of antidepressants. Antidepressants are a heterogeneous group in terms of both chemical structure and mechanism of action. If we take the chemical structure of an antidepressant as a starting point, they can be divided into the following groups: 1. Tricyclic antidepressants (TCAs) cover most of the drugs used to treat depression over the past 30 years - imipramine (melipramine, tofranil), clomipramine (anafranil), amitriptyline, etc. This group can be considered as the most well-researched and reliable in the treatment of depression. 2. Medicines that differ in structure from tricyclics (two-, four-cyclic, etc.). These are the majority of new drugs defined as “second generation antidepressants”—maprotiline (Ludiomil), mianserin (Miansan), fluoxetine (Prozac, Prodep), fluvoxamine, moclobemide (Aurorix). Based on the hypothetical mechanism of action, among antidepressants we can distinguish: 1. Drugs whose action is mainly due to inhibition of the reuptake of certain monoamines, which play the role of neurotransmitters in the central nervous system. This applies to norepinephrine (NA) and/or serotonin (5-hydroxytryptamine, 5HT). In this group we can distinguish: Non-selective inhibitors of norepinephrine and 5HT uptake, increasing transmission (transmission) in both noradrenergic and serotonergic neurons. This:

• drugs that, along with inhibition of NA and 5HT uptake, affect other types of transmission (anticholinergic, antihistamine and other effects) (this subgroup includes tricyclic antidepressants)
• drugs that selectively inhibit the uptake of norepinephrine and 5HT without affecting other types of transmission are represented by venlafaxine (Effexor).
• Selective monoamine uptake inhibitors include:
• serotonin uptake inhibitors - fluoxetine, fluvoxamine, sertraline, paroxetine (Aropax),
• dopamine uptake inhibitors such as bupropion (amphebutamon).

• Non-selective MAO inhibitors that simultaneously inhibit the activity of MAO A and B. These are old, currently rarely used MAO inhibitors - phenelzine (Nardil), isocarboxazid (Marplan), tranylcypromine (parnate).
• Selective MAO inhibitors that inhibit the activity of isolated isoenzyme A or B. These include: selective MAO-A inhibitors (moclobemide), selective MAO-B inhibitors (selegiline) (used in the early stages of Parkinson's disease).

• antidepressants with a pronounced anti-anxiety and sedative effect without a noticeable effect on psychomotor agitation - doxepin (Sinequan), trimipramine - (Surmontil), and among new drugs - fluvoxamine and paroxetine;
• antidepressants with a weak anti-anxiety effect and a moderate effect on psychomotor agitation - amitriptyline, imipramine, clomipramine, moclobemide;
• antidepressants without a pronounced sedative and anti-anxiety effect, but with a disinhibiting effect on reduced psychomotor activity - desipramine (Pertofran), nortriptyline (Pamelor), protriptyline.

1. These studies are conducted on selective groups of patients in whom “major depression” is recognized to be of moderate severity, as evidenced by the ability to conduct most studies in outpatient studies
2. Severe criteria, for obvious reasons, exclude from the study a group of so-called problematic patients with somatic diseases, the need to take other medications (including psychotropic ones), elderly age, dependence on various types of drugs, organic changes in the central nervous system, atypical clinical picture, high risk of suicide and etc. Thus, the study was conducted within the framework of the 3rd and 4th phases in a group of patients that is not representative of everyday clinical practice.
3. The widespread use of a 50% reduction in the Hamilton score in assessing the results should not mean an improvement that is quite satisfactory from a clinical point of view, which does not mean that some of the treated patients did not achieve such an improvement
4. Studies conducted under controlled conditions usually use a medium dose of drug, usually standardized (eg, 150 mg melipramine or amitriptyline), which may not be optimal for some patients and therefore may not provide improvement, while the drug being studied (eg, fluoxetine) optimal doses provide a therapeutic effect. In this regard, the comparative assessment of the effectiveness of the new drug may be overestimated.

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Recently, the number of people suffering from depression has increased significantly. This is largely due to the frantic pace of modern life and the increased level of stress. Added to this are also economic and social problems. All this cannot affect the mental and emotional health of people.

People feel changes in their psyche when they affect their performance and social relationships. They turn to a doctor for advice, and often he diagnoses them with depression.

First of all, it should be noted that you should not be afraid of this diagnosis. The disease does not indicate that the sufferer is mentally or mentally disabled. It does not affect the cognitive functions of the brain, and in most cases it can be cured.

However, depression is not just a bad mood or sadness that can affect healthy people from time to time. With depression, a person loses all interest in life, feels overwhelmed and tired all the time, and cannot make a single decision.

Depression is dangerous because it can affect the entire body, causing irreversible changes in individual organs. In addition, with depression, relationships with others deteriorate, work becomes impossible, thoughts of suicide appear, which can sometimes be carried out.

Depression is actually not a consequence of a person’s weak will, or his insufficient efforts to correct the situation. In most cases, it is a biochemical disease caused by metabolic disorders and a decrease in the amount of certain hormones in the brain, primarily serotonin, norepinephrine and endorphin, which act as neurotransmitters.

Therefore, as a rule, depression cannot always be cured with non-drug measures. It is well known that when a person is in a depressed mood, a change of environment, relaxation methods and auto-training, etc. can help. but all these methods require significant effort on the part of the patient, his will, desire and energy. But with depression, they just don’t exist. It turns out to be a vicious circle. And it is often impossible to break it without the help of drugs that change biochemical processes in the brain.

Classification of antidepressants according to the principle of action on the body

There are several options for classifying antidepressants. One of them is based on exactly what clinical effect the drugs have on the nervous system. There are three types of such actions:

• Sedative
• Balanced
• Activating

Sedative antidepressants have a calming effect on the psyche, relieving anxiety and increasing the activity of nervous processes. Activating drugs fight well against such manifestations of depression as apathy and lethargy. Balanced drugs have a universal effect. As a rule, the sedative or stimulating effect of drugs begins to be felt from the very beginning of administration.

Classification of antidepressants based on the principle of biochemical action

This classification is considered traditional. It is based on what chemicals are included in the drug and how they affect the biochemical processes in the nervous system.

Tricyclic antidepressants (TCAs)

A large and diverse group of drugs. TCAs have long been used in the treatment of depression and have a solid evidence base. The effectiveness of some drugs in the group allows them to be considered a standard for antidepressants.

Tricyclic drugs can increase the activity of neurotransmitters - norepinephrine and serotonin, thereby reducing the causes of depression. The name of the group was given by biochemists. It is associated with the appearance of the molecules of substances of this group, consisting of three carbon rings connected together.

TCAs are effective drugs, but have many side effects. They are observed in approximately 30% of patients.

The main drugs of the group include:

• Amitriptyline
• Imipramine
• Maprotiline
• Clomipramine
• Mianserin

Monoamine oxidase inhibitors (MAO inhibitors)

These are first generation antidepressants.

Monoamine oxidase is an enzyme that destroys various hormones, including neurotransmitters. MAO inhibitors interfere with this process, due to which the amount of neurotransmitters in the nervous system increases, which in turn leads to the activation of mental processes.

MAO inhibitors are quite effective and cheap antidepressants, but have a large number of side effects. These include:

• Hypotension
• Hallucinations
• Insomnia
• Agitation
• Constipation
• Headache
• Dizziness
• Sexual dysfunction
• Visual impairment

When taking certain medications, you must also follow a special diet to avoid introducing potentially dangerous enzymes into your body that are metabolized by MAO.

The most modern antidepressants of this class have the ability to inhibit only one of two types of enzyme - MAO-A or MAO-B. These antidepressants have fewer side effects and are called selective inhibitors. Non-selective inhibitors are currently rarely used. Their main advantage is their low price.

Main selective MAO inhibitors:

• Moclobemide
• Pirlindol (pyrazidol)
• Bethol
• Metrolindole
• Garmaline
• Selegilin
• Rasagiline

Selective serotonin reuptake inhibitors (SSRIs)

These drugs belong to the third generation of antidepressants. They are relatively easily tolerated by patients and have fewer contraindications and side effects compared to TCAs and MAO inhibitors. Their overdose is not as dangerous as compared to other groups of drugs. The main indication for drug treatment is major depressive disorder.

The principle of operation of the drugs is based on the fact that the neurotransmitter serotonin, which is used to transmit impulses between neuron contacts, when exposed to SSRIs, does not return back to the cell transmitting the nerve impulse, but is transferred to another cell. Thus, antidepressants such as SSRIs increase the activity of serotonin in the nerve circuit, which has a beneficial effect on brain cells affected by depression.

As a rule, drugs in this group are especially effective for severe depression. For depressive disorders of minor and moderate severity, the effect of the drugs is not so noticeable. However, a number of doctors have a different opinion, which is that for severe forms of depression it is preferable to use proven TCAs.

The therapeutic effect of SSRIs does not appear immediately, usually after 2-5 weeks of use.

The class includes substances such as:

• Fluoxetine
• Paroxetine
• Citalopram
• Sertraline
• Fluvoxamine
• Escitalopram

Other types of drugs

There are also other groups of drugs, for example, norepinephrine reuptake inhibitors, selective norepinephrine reuptake inhibitors, noradrenergic and specific serotonergic drugs, melatonergic antidepressants. Among such drugs are Bupropion (Zyban), Maprotiline, Reboxetine, Mirtazapine, Trazadone, Agomelatine. All of these are good antidepressants, proven in practice.

New generation antidepressants

These are new drugs, which mainly include antidepressants of the SSRI class. Among the drugs synthesized relatively recently, the following drugs have performed well:

• Sertraline
• Fluoxetine
• Fluvoxamine
• Mirtazaline
• Escitalopram

Difference between antidepressants and tranquilizers

Many people believe that tranquilizers are a good way to combat depression. But in fact, this is not the case, although tranquilizers are often used to treat depression.

What is the difference between these classes of drugs? Antidepressants are drugs that, as a rule, have a stimulating effect, normalize mood and relieve mental problems associated with a lack of certain neurotransmitters. This class of drugs acts for a long time and does not affect people with a healthy nervous system.

Tranquilizers, as a rule, are quick-acting drugs. They can be used to combat depression, but mainly as adjuvant drugs. The essence of their effect on the human psyche is not to correct his emotional background in the long term, like drugs for depression, but to suppress the manifestations of negative emotions. They can be used as a means to reduce fear, anxiety, agitation, panic attacks, etc. Thus, they are anti-anxiety and anti-anxiety drugs rather than antidepressants. In addition, during a course of treatment, most tranquilizers, especially diazepine drugs, are addictive and dependent.

Can you buy antidepressants without a prescription?

According to the rules for the dispensing of medicines in Russia, in order to obtain psychotropic drugs in pharmacies, a doctor’s prescription is required, that is, a prescription. And antidepressants are no exception. Therefore, theoretically, strong antidepressants cannot be purchased without prescriptions. In practice, of course, pharmacists may sometimes turn a blind eye to the rules in the pursuit of profit, but this phenomenon cannot be taken for granted. And if you are given a medicine without a prescription in one pharmacy, this does not mean that the same situation will happen in another.

You can only buy drugs for the treatment of mild depressive disorders such as Afobazole, “daytime” tranquilizers and herbal-based drugs without a doctor’s prescription. But in most cases it is difficult to classify them as real antidepressants. It would be more correct to classify them as sedatives.

The dangers of self-treatment for depression

There are many factors to consider when treating depression. This is the patient’s health status, the physiological parameters of his body, the type of disease, and other medications he is taking. Not every patient will be able to independently analyze all the factors and choose a medicine and its dosage in such a way that it would be useful and would not cause harm. Only specialists - psychotherapists and neurologists with extensive practical experience - will be able to solve this problem and tell which antidepressants are best to use for a particular patient. After all, the same medicine, used by different people, will lead to a complete cure in one case, will not have any effect in another, and may even worsen the situation in a third.

Almost all medications for depression, even the mildest and safest ones, can cause side effects. But strong drugs without side effects simply do not exist. Particularly dangerous is long-term uncontrolled use of drugs or excess dosage. In this case, the body may become intoxicated with serotonin (serotonin syndrome), which can be fatal.

How to get a prescription for the drug?

If you believe that you are depressed, it is recommended that you consult a psychotherapist or neurologist. Only he can carefully examine your symptoms and prescribe the drug that is appropriate for your case.

Herbal remedies for depression

The most popular herbal preparations today to lift your mood contain extracts of mint, chamomile, valerian, and motherwort. But preparations containing St. John's wort have demonstrated the greatest effectiveness in treating depression.

The mechanism of the therapeutic effect of St. John's wort has not yet been precisely clarified, but scientists believe that the enzyme hypericin contained in it is capable of accelerating the synthesis of norepinephrine from dopamine. St. John's wort also contains other substances that have a beneficial effect on the nervous system and other body systems - flavonoids, tannins, essential oils.

St. John's wort preparations are mild antidepressants. They will not help with all depression, especially with its severe forms. However, the effectiveness of St. John's wort for mild and moderate depression has been proven by serious clinical studies, in which it has shown to be no worse, and in some respects even better, than popular tricyclic drugs for depression and SSRIs. In addition, St. John's wort preparations have a relatively small number of side effects. They can be taken by children from 12 years of age. Among the negative effects of taking St. John's wort, the phenomenon of photosensitivity should be noted, which means that when the skin is exposed to sunlight during the course of treatment with the drug, rashes and burns may appear on it.

Medicines based on St. John's wort are sold without a prescription. So if you're looking for depression medications that you can take without a prescription, this class of drugs may be your best choice.

Some preparations based on St. John's wort:

• Negrustin
• Deprim
• Gelarium Hypericum
• Neuroplant

List of popular drugs in alphabetical order

List of antidepressants produced in Russia and Ukraine:

Approximate price of drugs

Depression is a very common phenomenon that is difficult to ignore. The chronic form of this condition can become a threat not only to health, but also to human life. People perceive the world around them differently and find themselves in different life situations. If a person’s potential is not realized, he faces an insoluble problem - they develop depression.

They can be caused by hormonal age-related changes, frequent stressful situations, chronic (or incurable) illness, or disability. These factors lead to a general biochemical failure. The level of pleasure hormones (endorphins, in particular) in the body sharply decreases serotonin). This is expressed in dissatisfaction with oneself, a depressed state, lack of will and desire to change anything.

SSRI - C Selective Serotonin Reuptake Inhibitors

It is very difficult to get out of this state. Support from loved ones, specialist help, and medication are often necessary. Medicines, developed to treat depression, are called antidepressants. They have a different mechanism of action, but the dynamics of the patient’s condition when using them is definitely positive.

Such facilities have virtually no effect on a healthy person. In people who suffer from depression after treatment antidepressants, mood improves, anxiety, melancholy, and apathy go away. Their psychological stability returns, sleep and biological rhythms normalize, and their appetite improves.

Third-generation drugs for effectively combating depression are selective serotonin reuptake inhibitors.

Classification of antidepressants

Depression has been known to mankind since time immemorial, as have ways to overcome it. In ancient Rome, the famous physician Soranus of Ephesus used lithium salts to treat them, for example. Cannabis, opium, barbiturates, amphetamines are all numerous attempts to chemically manipulate the body to help people cope with emotional exhaustion.

The first drug to combat depression was Imipramine, which was synthesized in 1948. To date, many have been developed antidepressants, which are currently classified. Depending on the general picture of the manifestation of the mental processes of patients:

• Thymiretics are used for depressed and depressed states;
• thymoleptics have a calming effect, so they are used when there is increased mental arousal.

According to biochemical effects on the body antidepressants there are :

• non-selective action (for example, Melipramine, Amizol),
• selective action: blocking serotonin uptake (for example, Sertraline), blocking norepinephrine uptake (for example, Reboxetine),
• inhibition monoamine oxidases: non-selective action (for example, Transamine), selective action (for example, Autorix).

There are other pharmacological groups of drugs against depression.

How do antidepressants work?

Antidepressants are able to control some processes that occur in brain cells. This organ consists of a huge number of nerve cells. The body and processes are the components of neurons. They transmit impulses between themselves using processes and through the synapse (the space that is located between two neurons).

Antidepressants were discovered by accident while testing drugs against tuberculosis

This space is filled with a special substance (mediator), through which information is transmitted from one neuron to another. About 30 mediators are currently known in biochemistry. But depressive states are associated, as a rule, with only three hormones that function as neurotransmitters: dopamine, norepinephrine.
The mechanism of action of antidepressants is aimed at regulating the concentration of these hormones in the brain and correcting its functioning, impaired as a result of depression.

What are SSRIs

In modern medical practice, the most popular are third generation drugs - selective serotonin reuptake inhibitors. These drugs differ from traditional tricyclic drugs for depression by having fewer side effects and being more effective.

With an overdose of these drugs, virtually no cardiotoxic effect is observed. SSRIs are recommended for patients who have contraindications to the use of conventional antidepressants (for example, closed glaucoma, cardiac arrhythmias).

How the drugs work

One of the causes of depression is decreased concentration of serotonin in the brain. This important neurotransmitter, hormone is called the hormone of happiness, joy, pleasure. Moreover, its normal concentration provides a long-lasting, stable feeling of quiet happiness and harmony.

Serotonin reuptake inhibitor works to increase the concentration of the hormone serotonin in the brain. The active ingredients of this antidepressant selectively block (inhibit) serotonin in the brain. This process occurs directly at the synapse. That is, the reuptake of the hormone by the adhesive does not occur; this process is prevented by the drug.

Serotonin remains in place, so the circulation of nerve impulses continues. They activate cells who are depressed, softening its manifestation. The advantage of drugs in this group is that the dosage is immediately determined by the attending physician; there is no need to increase it, since the additional therapeutic effect does not depend on it.

When using a group of inhibitors, there is no point in monitoring the concentration of serotonin in the blood. An exception may be some diseases of patients, due to which the elimination of drugs from the body slows down.

When are SSRIs prescribed?

Drugs in this group are prescribed for:

• deep depressive disorders;
• stress, panic attacks, neurotic anxiety;
• manias, phobias;
• obsessive-compulsive neuroses;
• bulimia;
• alcoholism;
• chronic pain syndrome;
• emotionally unstable personality disorder.

The effectiveness of treatment largely determines the timeliness of therapeutic measures. For minor manifestations of depressive conditions, there is no significant difference between the effectiveness of treatment with tricyclic antidepressants and SSRIs. But the effectiveness of the latter in the treatment of advanced nervous disorders has been proven by medical practice.

SSRI drugs do not have a therapeutic effect immediately. Depending on the severity of the disease and the individual characteristics of the body, positive dynamics are observed in the second, fifth, and sometimes only the eighth week from the start of taking the medicine.

The daily dosage depends on the rate of elimination of drugs from the body. Most often, the drug is prescribed to be taken once a day, since the half-life of most SSRIs is more than a day.

Side effects

Side effects include some disorders of the digestive system - nausea, vomiting. When using selective serotonin reuptake inhibitors, the following may occur:

• anxiety;
• anxiety;
• dizziness;
• fast fatiguability;
• sleep disturbance;
• sexual disorders.

Reactions to reception blockers depend on the individual characteristics of the organism.

If the patient has problems with the liver, kidneys selective serotonin reuptake inhibitors should be used with caution. Serotonin receptors are located in the human body not only in the brain, but also in the spinal cord. There are many of them in the gastrointestinal tract, respiratory system, and on the walls of blood vessels. When using inhibitors, the above conditions develop, which usually disappear after a month. That is side effects are observed only in the first stages of taking inhibitors.

Side effects of drugs are associated with an increase in the amount of neurotransmitter serotonin in the brain, this affects mental activity. Medical practice describes cases appearance of suicidal thoughts, mania during treatment with inhibitors in adolescents. This manifestation has not been proven in adult patients.

This reaction is individual in nature; among SSRIs, you can choose drugs that do not affect the activation of the psychomotor sphere and have a sedative effect.

If SSRI regimen involves a large dosage, it can develop, which causes convulsions, fever, and heart rhythm disturbances. In this case, the drug is discontinued. Third generation antidepressants easily replace each other, so if treatment is not effective, you can choose another drug. If any of the family members used inhibitors and achieved positive results, it makes sense to opt for this drug.

For treatment complex mental disorders, conditions of chronic depression, SSRIs are prescribed together with other drugs, for example, tranquilizers, tricyclic antidepressants. Complex therapy requires strict adherence to the doctor’s recommendations regarding the regimen and dosage of medications. There are known cases of death due to overdose.

SSRI drugs

List of drugs SSRIs are extensive. Today they are in great demand for treating depression, improving mood, and normalizing sleep. These medicines are available and sold in the pharmacy network without prescriptions. The most common are:

• Paroxetine;
• Fluvoxamine;
• Sertraline;
• Cipramil;
• Fluoxetine.

When choosing a drug, it is worth analyzing the effect of the drug:

Paroxetine

Of all the serotonin reuptake inhibitors Paroxetine is the most effective drug. It is prescribed in an initial concentration of 10 mg or 20 mg. In some cases, the dosage is gradually increased to 50 mg per day. Take the medicine once a day. The half-life of Paroxetine occurs in almost a day. Within a week of taking the drug, a stable concentration is achieved. The drug may cause slight weight gain.

Fluvoxamine

For manifestations of depression in combination with increased anxiety, Fluvoxamine is prescribed. The effectiveness of this drug appears almost immediately after starting treatment and subsequently has a smooth effect on the patient. The drug has proven itself positively in the manifestation of obsessive-compulsive disorder neuroses, social phobias (including in children), and in combination with other drugs has proven itself well in the treatment of schizophrenia.

The initial concentration of the drug is 50 mg once a day; it is recommended to take the drug in the evening. The initial dosage can be increased to 100 mg, the maximum amount is 500 mg (in this case, the regimen includes several doses of the drug). Within 5-7 days, the effective concentration of the active substance is achieved. Fluvoxamine has the largest number of side effects.

Sertraline

Indications for the use of Sertraline are mild depressive states. It does not affect psychomotor functions and has a weak antiphobic effect. The drug is prescribed for the treatment of obsessive-compulsive disorder. It gives a good therapeutic effect and can prevent relapse and the development of depression in the future.

The initial dose of Sertraline is 50 mg per day. The dosage can be gradually increased to 200 mg (50 mg per week). Half-life of active substances affected by the patient's age. With prolonged use of the drug, addiction develops.

Cipramil

Tsipramil is most often prescribed for the treatment of depressive conditions that arise as a result of chronic somatic diseases. In addition, it is indicated for elderly patients who have suffered a cerebral stroke.

The initial dose of Tsipramil is 20 mg per day. The drug is taken once a day in the morning. In most cases, this dose of the drug has a good therapeutic effect. The daily concentration can be increased to 60 mg, depending depending on the severity of the patient's condition.

In the practice of using Tsipramil, its interaction with other drugs is not described. The half-life of the inhibitor is 30 hours. Among the most common side effects are nausea and headache, but they are observed only in the initial stages of taking the drug.

Fluoxetine

Fluoxetine is known as one of the first serotonin reuptake inhibitors. It has been used in medical practice since the early 80s. Prescribed for the treatment of depressive symptoms of varying degrees. Known as an effective drug in the treatment of bulimia.

The medicine is taken in the morning, once a day at a dosage of 20 mg. It can be increased to 40-80 mg. The maximum concentration is observed after 6 hours. This drug has longest half-life- about 3 days, and the half-life of its active metabolite is up to 9 days. This circumstance provides benefits to patients who may miss doses of the drug.

The inhibitor has an effect on the body disinhibitory effect, in the first weeks of use, states of anxiety and restlessness may be observed. This drug slowly relieves signs of depression. The effect is observed only after 2-3 weeks of treatment. At the initial stages and with further use, side effects are noted in the form nausea, headaches, decreased vision, skin allergic manifestations, sexual dysfunction.

Selective serotonin reuptake inhibitors are third generation antidepressants. They allow you to stabilize a person’s emotional state at the biochemical level. SSRIs are effective in treating depression, neuroses, phobias, and obsessive disorders. At maximum efficiency they have minimal side effects.