Action of tricyclic antidepressants. What are tricyclic antidepressants? The power of "magic pills"

The term "antidepressants" speaks for itself. It stands for group medicines to fight depression. However, the scope of antidepressants is much wider than the name might suggest. In addition to depression, they know how to combat feelings of melancholy, anxiety and fears, relieve emotional stress, and normalize sleep and appetite. With the help of some of them they even fight smoking and nocturnal enuresis. And quite often, antidepressants are used as painkillers for chronic pain. Currently, there are a significant number of drugs that are classified as antidepressants, and their list is constantly growing. From this article you will learn about the most common and frequently used antidepressants.

How do antidepressants work?

Antidepressants affect the neurotransmitter systems of the brain through various mechanisms. Neurotransmitters are special substances through which various “information” is transmitted between nerve cells. Not only a person’s mood and emotional background, but also almost all nervous activity depends on the content and ratio of neurotransmitters.

The main neurotransmitters whose imbalance or deficiency is associated with depression are serotonin, norepinephrine, and dopamine. Antidepressants lead to normalization of the amount and ratio of neurotransmitters, thereby eliminating clinical manifestations depression. Thus, they have only a regulatory effect, and not a replacement, therefore they do not cause addiction (contrary to existing opinion).

There is not yet a single antidepressant whose effect would be visible from the first pill taken. Most drugs require quite long time to show off your capabilities. This often causes patients to stop taking the drug on their own. After all, I want it to unpleasant symptoms were eliminated as if by magic. Unfortunately, such a “golden” antidepressant has not yet been synthesized. The search for new drugs is driven not only by the desire to accelerate the development of the effect of taking antidepressants, but also by the need to get rid of unwanted side effects, reduce the number of contraindications for their use.

Choosing an antidepressant

Choosing an antidepressant among the abundance of drugs presented on the pharmaceutical market is a rather difficult task. An important point that every person should remember is that an antidepressant cannot be chosen independently by a patient with an already established diagnosis or a person who has “discovered” the symptoms of depression. Also, the drug cannot be prescribed by a pharmacist (which is often practiced in our pharmacies). The same applies to changing the drug.

Antidepressants are not harmless medications. They have a lot side effects, and also have a number of contraindications. In addition, sometimes symptoms of depression are the first signs of another, more serious illness(for example, brain tumors), and uncontrolled use of antidepressants can play a fatal role in this case for the patient. Therefore, such drugs should only be prescribed by the attending physician after an accurate diagnosis has been established.

Classification of antidepressants

All over the world, it is common practice to divide antidepressants into groups based on their chemical structure. For doctors, at the same time, this distinction also means the mechanism of action of the drugs.

From this position, several groups of drugs are distinguished.
Monoamine oxidase inhibitors:

• non-selective (non-selective) - Nialamid, Isocarboxazid (Marplan), Iproniazid. To date, they are not used as antidepressants due to the large number of side effects;
• selective (selective) - Moclobemide (Aurorix), Pirlindol (Pyrazidol), Befol. IN Lately The use of this subgroup of funds is very limited. Their use is associated with a number of difficulties and inconveniences. The difficulty of use is due to the incompatibility of the drugs with drugs from other groups (for example, painkillers and cold medications), as well as the need to follow a diet when taking them. Patients must avoid eating cheese, legumes, liver, bananas, herring, smoked meats, chocolate, sauerkraut and a number of other products due to the possibility of developing the so-called “cheese” syndrome (high blood pressure with a greater risk of myocardial infarction or stroke). Therefore, these drugs are already becoming a thing of the past, giving way to more “convenient” medications to use.

Non-selective neurotransmitter reuptake inhibitors(that is, drugs that block the uptake of all neurotransmitters by neurons without exception):

• tricyclic antidepressants - Amitriptyline, Imipramine (Imizin, Melipramine), Clomipramine (Anafranil);
• four-cyclic antidepressants (atypical antidepressants) – Maprotiline (Lyudiomil), Mianserin (Lerivon).

Selective neurotransmitter reuptake inhibitors:

• serotonin - Fluoxetine (Prozac, Prodel), Fluvoxamine (Fevarin), Sertraline (Zoloft). Paroxetine (Paxil), Cipralex, Cipramil (Cytahexal);
• serotonin and norepinephrine – Milnacipran (Ixel), Venlafaxine (Velaxin), Duloxetine (Cymbalta),
• norepinephrine and dopamine - Bupropion (Zyban).

Antidepressants with a different mechanism of action: Tianeptine (Coaxil), Sydnofen.
The subgroup of selective neurotransmitter reuptake inhibitors is currently the most commonly used worldwide. This is due to the relatively good tolerability of the drugs, a small number of contraindications and wide possibilities for use not only for depression.

From a clinical point of view, antidepressants are quite often divided into drugs with a predominantly sedative (calming), activating (stimulating) and harmonizing (balanced) effect. The latter classification is convenient for the attending physician and the patient, since it reflects the main effects of drugs, in addition to antidepressant. Although, in fairness, it is worth saying that it is not always possible to clearly distinguish between drugs according to this principle.

The drug is contraindicated in epilepsy, diabetes mellitus, chronic diseases liver and kidneys, under the age of 18 and after 60 years.

By and large, there is no ideal antidepressant. Each drug has its own disadvantages and advantages. And individual sensitivity is also one of the main factors in the effectiveness of a particular antidepressant. And although it is not always possible to hit depression in the very heart on the first try, there will definitely be a drug that will become a salvation for the patient. The patient will definitely come out of depression, you just need to be patient.

Reading time: 9 minutes. Published 08/16/2019

Tricyclic antidepressants (TCAs) were developed in the 1950s as a chemical treatment for depression. These drugs are known for their specific chemical structure, consisting of three rings of atoms, which is why they are called tricyclics. Tricyclics were developed after researchers began studying derivatives of the first typical antipsychotic drug Thorazine (Aminazine). Experiments led to the development of the first tricyclic antidepressant - Imipramine.

Imipramine was not originally intended to treat depressive symptoms, but caused mania. This led researchers to believe that it may have some antidepressant effects. In testing, Imipramine was found to produce a strong antidepressant response among people with depression. This led to the production of a new class of antidepressant drugs—tricyclic antidepressants (TCAs).

TCAs became widely used to treat depression and were considered very effective. At the time TCAs were approved, they were considered a first-line treatment option. These days they are still used to treat depression, but are considered second-line drugs. After and.

They are still considered highly effective by many, but doctors and patients prefer the new drugs because they have fewer side effects and are considered safer. TCAs are usually prescribed as a treatment alternative before use.

Tricyclic antidepressants list

Below are several lists of TCAs, grouped by how they function. Although some TCAs affect both and , others have a greater effect on one of them. In addition, there are others that do not affect any of the neurotransmitters. They are listed as "atypical" TCAs.

Balanced TCAs: Serotonin and Norepinephrine

Below is a list of tricyclic antidepressants that affect serotonin and norepinephrine to the same extent.

Amitriptyline (Amizol, Elivel). It is the most commonly used TCA. Created by Merck in 1961. In addition to affecting , it also affects Alpha-1 receptors and acetylcholine receptors.

Amitriptyloxide (Amioxide, Ambivalon, Equilibrin). Amitriptyl oxide appeared in Europe in the 1970s. It acts similarly to Amitriptyline because it is a metabolite. However, it works faster and with fewer side effects.

Butriptyline (Evadin). Butriptyline appeared in Europe in 1974. It is very similar to Amitriptyline, but has significantly fewer side effects and contraindications. It acts as a potent antihistamine and anticholinergic and is also a moderate agonist of the Alpha-1 receptor and the 5-HT2 receptor. It affects serotonin to a very small extent.

Dosulepin (Protiaden). Used mainly in Australia, New Zealand and South Africa. In addition to its effects on serotonin and norepinephrine, it also has anticholinergic and antihistamine properties and blocks the Alpha-1 receptor.

Doxepin (Sinequan, Spectra). Used worldwide to treat major depression, anxiety disorders and insomnia. It is also considered a drug that can be used to treat hives and severe itching.

Melitracene (Adaptol). Used throughout Europe and Japan to treat depressive and anxiety disorders. The method of action is similar to the drugs Imipramine and Amitriptyline. Works faster and has fewer side effects.

Nitroxazepine (Syntamil). Marketed in India for the treatment of depression in 1982. Like many other TCAs, it can also be used to treat bedwetting in children. Similar to the drug Imipramine, but has fewer side effects (in particular, anticholinergic).

Noxiptyline (Agedal, Elronon). Combines Noxiptyline and Dibenzoxin. It was originally released in the 1970s in Europe and was considered one of the most effective TCAs.

Propizepine (Vagran). Released in France in the 1970s. Not many documents have been published on the pharmacology of this drug.

Tricyclic antidepressants that act on serotonin

Below is a list of TCAs that increase serotonin significantly relative to norepinephrine.

Clomipramine (Anafranil, Clofranil). Developed in the 1960s and is a derivative of the first TCA, Imipramine. It inhibits the reuptake of serotonin 200 times more than norepinephrine. In addition to this, it also acts as an antagonist at the histamine H1 receptor, alpha-1 adrenergic receptor and various acetylcholine receptors.

Dimethacrine (Istonil). Used to treat major depression throughout Europe. It was previously used in Japan. It is less effective compared to Imipramine. Rarely used due to effects on the liver.

Imipramine (Deprinol, Tofranil, Imizin). It is the first TCA discovered and has been used since the 1950s. Used to treat depression, but in some cases prescribed for bedwetting due to its ability to reduce delta brain waves during sleep. Although this drug has very potent serotonin reuptake inhibitory properties, it has effects on a number of other neurotransmitters including: norepinephrine, (to a very small extent at the D1 and D2 receptors), acetylcholine (anticholinergic), epinephrine (antagonist), and histamine (antagonist) .

Imipramine oxide (Elepsin). Created in the 1960s and used in Europe. In addition to affecting serotonin, it also acts on adrenaline, histamine and acetylcholine receptors as an antagonist. It acts similarly to Imipramine due to the fact that it is a metabolite and has a similar structure. However, Imipramine Oxide works faster and with fewer side effects.

Pipofezin (Azafen). Approved for the treatment of depression in the 1960s and used in Russia. This drug also has antihistamine properties due to the fact that many experience sedation as a side effect. In addition, it has anticholinergic and adrenergic effects.

Tricyclic antidepressants that act on norepinephrine

These are TCAs that affect norepinephrine more than serotonin. Many are more stimulating, which can also increase anxiety. They are suitable for people with more low level emotional excitement.

Demexiptyline (Deparon, Tinoran). Used in France. It works similarly to the more widely documented drug Desipramine.

Desipramine (Norpramin, Petilil). Used to treat major depression, but has been found useful in the treatment of neuropathic pain and some ADHD symptoms. Desipramine is associated with increased risk development of breast cancer in women and is considered genotoxic. It contains the active metabolite of the drug Imipramine.

Dibenzepine (Noveril). Only available in European countries. Acts primarily as a norepinephrine reuptake inhibitor, but also has significant antihistamine properties. It is considered to be similar to Imipramine, but with fewer side effects and a similar degree of effectiveness.

Lofepramine (Gamanil). Introduced in 1983. It is a relatively weak acetylcholine receptor antagonist. It is considered to be less sedating and safer than other TCAs.

Metapramine (Prodasten). Appeared in France in the mid-1980s. Has little effect as an NMDA receptor antagonist. This drug also acts as an analgesic, so some doctors may prescribe it for pain relief. It does not have anticholinergic properties like other TCAs.

Nortriptyline (Pamelor). This is a second generation TCA used for depression and sometimes for childhood bedwetting. Due to its stimulant properties it is sometimes used for treatment chronic fatigue, neuropathic pain and ADHD.

Protriptyline (Vivaktil). Used to treat depression as well as ADHD. This drug is known for its stimulant effects and generally promotes alertness, so it is used in some cases for narcolepsy.

Atypical tricyclic antidepressants

Atypical TCAs work differently than most and have unique properties. Unlike other TCAs, which focus primarily on norepinephrine, serotonin, or a combination of both, these drugs may act on 5-HT2 receptors, dopamine, Sigma-1 receptors, or glutamate receptors.

Amineptine (Survector). Developed in the 1960s and approved in 1978 in France. Due to its euphoric stimulant effects, people began to use it recreationally and abuse it. In 1999, after reports of liver damage, the drug was withdrawn from sale.

Iprindol (Prondol, Galatur, Tertran). Used in Europe since 1967. Acts primarily as a 5-HT2 receptor antagonist with minimal effects on serotonin and norepinephrine.

Opipramol (Pramolone, Insidon). Used in various European countries to treat anxiety disorders as well as depression due to its strong anxiolytic and tranquilizing effects. Opipramol acts primarily as an agonist at the Sigma-1 receptor and to a lesser extent as an agonist at the Sigma-2 receptor. Compared to SSRIs and SNRIs, this drug has fewer side effects.

Quinupramine (Quinupril, Adeprim). Used in Europe. Acts primarily as an acetylcholine receptor antagonist and also as a histamine antagonist at the H1 receptor. Affects the 5-HT2 receptor as a moderate antagonist.

Tianeptine (Coaxil, Stablon). Developed in the 1960s and used to treat depression, but is sometimes prescribed to treat irritable bowel syndrome. Tianeptine affects both the activity of glutamate receptors AMPA and NMDA, and. The researchers also noted that it functions as an agonist at the mu and delta opioid receptor.

Trimipramine (Gerfonal, Surmontil). Used to treat depression as a 5-HT2 receptor antagonist and an H1 receptor antagonist. It is known for its very calming effects and in some cases this drug is good for treating insomnia and anxiety. It is considered unique in that it is the only medicine that does not affect sleep stages.

Conclusion

There is current debate as to whether tricyclic antidepressants deserve classification as second-line treatments for depression. SSRIs, SNRIs, and the newer atypical antidepressants are considered to be the safest, have the fewest side effects, and are more effective than TCAs. However, many people do not respond to these classes of drugs, and for them the tricyclic class may be an ideal option.

There is some evidence that tricyclics may be better for treating people who have significant melancholic features associated with depression. The tricyclic antidepressant class is often tested only when a patient has not experienced any improvement in depressive symptoms from newer classes of medications. Assuming a person can tolerate the initial side effects, TCAs can be very effective as antidepressants.

It should be noted that these drugs are sometimes also used for conditions other than depression, such as ADHD, chronic pain, insomnia, and nocturnal enuresis.

Tricyclic antidepressants are drugs consisting of 3 rings in the molecule and radicals attached to them. Radicals can be different substances. In the classification of antidepressants, this group is classified as non-selective monoamine reuptake blockers.

Mechanism of action

The main mechanism is to block the reuptake of the active neurotransmitter; they act on the presynaptic membrane. This leads to their accumulation in the synaptic cleft and activation of synaptic transmission.

Neurotransmitters blocked by TCAs include:

• serotonin;
• norepinephrine;
• dopamine;
• phenylethylamine.

Antidepressants block the breakdown of monoamines (neurotransmitters) and act on monoamine oxidase, preventing reverse synthesis. They act as activators of the occurrence of depressive and affective states, which manifests itself when there is insufficient supply of monoamines into the synaptic cleft.

Within the class they are divided into:

1. Tertiary amines. TCAs of this group are distinguished by a balanced effect on the reuptake of monoamines (norepinephrine, serotonin). They are characterized by sedative and anti-anxiety, antidepressant activity and, in accordance with this, many side effects.
2. Secondary amines. TCAs have a lesser effect compared to tertiary amines, but a greater stimulating effect. They are distinguished by an imbalance in the uptake of monamines, mainly norepinephrine. Side effects are expressed to a lesser extent.
3. Atypical tricyclic antidepressants. The structure of their molecules corresponds to TCAs, but the mechanism of action is different or similar to classical TCAs. This large group medicines intended for use in clinical practice.
4. Heterocyclic antidepressants. Chemical structure, four-cyclic formula, mechanism of action corresponds to tricyclics.

The main characteristics of this group are:

1. Thymoleptic effect, which is expressed in reducing the severity of disturbances in the patient’s affective sphere. Taking it improves your mood psychological condition patient.
2. Psychomotor and somatic effects.
3. Analgesic effect.
4. Anticonvulsant action.
5. They have a nootropic effect on the cognitive sphere.
6. Stimulating effect.
7. Antihistamine effect.

Adaptive changes when taking medications occur after the accumulation of neurotransmitters. Therapeutic effect occurs regardless of the method of taking the drugs (orally or parenterally), 3-10 days are enough for the effect to occur.

Indications for use

Disorders of the human psychosomatic sphere and the occurrence of conditions that contribute to the development of diseases as complications of these conditions. The most common diseases are:

1. Depressive states of various etiologies. Sometimes they occur as a result of treatment with antipsychotics or other psychotropic drugs.
2. Neuroses and neurotic conditions reactive in nature.
3. Organic disorders in the functioning of the central nervous system. These include disorders such as Alzheimer's disease, which develops as a result of deposits amyloid plaques in the vessels of the central nervous system. Tricyclics reduce the rate of their formation and have a nootropic effect.
4. Anxiety states for schizophrenia and severe depression.

The use of antidepressants requires a careful history taking concomitant diseases. This pharmacological group has wide range side effects.

List of tricyclic antidepressants

The group of antidepressants includes 2466 drugs, of which only 16 are tricyclics. They are classified according to active substance.

The most common new generation antidepressants are:

• Trazadone;
• Fluoxetine;
• Fluxonil;
• Sertalin.

Medicines and over-the-counter products that can be purchased:

• Deprim;
• Novo-passit;
• Persen et al.

Prices in pharmacies for drugs of this pharmaceutical group depend on the manufacturer, the quality of the drug, its properties and the characteristics of dispensing from the pharmacy. Some drugs contain narcotic substances and are sold with a prescription.

Side effects

The use of medications as a result of long-term use can lead to the following disorders:

• cardiotoxic effect - disturbance of rhythm, conduction, etc.;
• teratogenic effect;
• autonomic disorders (dry mouth, dizziness, impaired accommodation, etc.);
• changes in blood count (eosinophilia, leukocytosis);
• violation of ejaculation, urination, etc.

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

People feel changes in the psyche when they affect their performance and social relations. 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 Bad mood or sadness, which can roll over from time to time and healthy people. 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 efforts 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 activity nervous processes. Activating drugs fight well against such manifestations of depression as apathy and lethargy. Balanced drugs have universal action. 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.

TCA – 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

Amitriptyline Tricyclic antidepressant. Has both antidepressant and mild analgesic effects Composition: 10 or 25 mg amitriptyline hydrochloride Dosage form: dragees or tablets Indications: depression, sleep disorders, behavioral disorders, mixed emotional disorders, chronic pain syndrome, migraine, enuresis. Side effects: agitation, hallucinations, visual disturbances, tachycardia, blood pressure fluctuations, tachycardia, stomach upset Contraindications: heart attack, individual intolerance, lactation, intoxication with alcohol and psychotropic drugs, cardiac muscle conduction disorders. Application: immediately after meals. The initial dose is 25-50 mg at night. Gradually the daily dose is increased to 200 mg in three doses.

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 also have a different opinion, which is that when severe forms 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

Fluoxetine Antidepressant, selective serotonin reuptake inhibitor. Has an antidepressant effect, relieves feelings of depression Release form: Tablets 10 mg Indications: depression of various origins, obsessive-compulsive disorder, bulimia nervosa Contraindications: epilepsy, tendency to seizures, severe renal or liver failure, glaucoma, adenoma, suicidal tendencies, taking MAO inhibitors Side effects: hyperhidrosis, chills, serotonin intoxication, stomach upset Application: regardless of food intake. The usual regimen is 20 mg once a day, in the morning. After three weeks, the dose can be doubled. Fluoxetine analogues: Deprex, Prodep, Prozac

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.

Bupropion (Zyban) Antidepressant, selective norepinephrine and dopamine reuptake inhibitor. An antagonist of nicotinic receptors, due to which it is widely used in the treatment of nicotine addiction. Release form: Tablets 150 and 300 mg. Indications: depression, social phobia, nicotine addiction, seasonal affective disorder. Contraindications: allergy to components, age under 18 years, simultaneous use with MAO inhibitors, anorexia nervosa, seizure disorders. Side effects: an overdose of the drug is extremely dangerous, which can cause epileptic seizures(2% of patients at 600 mg dose). Urticaria, anorexia or lack of appetite, tremor, and tachycardia are also observed. Application: the medicine should be taken once a day, in the morning. The typical dose is 150 mg, the maximum daily dose is 300 mg.

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 good remedy tranquilizers are used 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 means fast acting. 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 buy without a doctor’s prescription only drugs for the treatment of mild depressive disorders such as Afobazole, “daytime” tranquilizers and drugs for plant based. But in most cases it is difficult to classify them as real antidepressants. It would be more correct to classify them as sedatives.

Afobazole Anti-anxiety, anxiolytic and mild antidepressant Russian production no side effects. Over-the-counter drug. Release forms: Tablets 5 and 10 mg Indications: anxiety disorders and conditions of various origins, sleep disorders, neurocirculatory dystonia, alcohol withdrawal. Side effects: Side effects while taking the drug are extremely rare. These may be allergic reactions, work disorders gastrointestinal tract, headache. Application: it is advisable to take the drug after meals. Single dose is 10 mg, daily – 30 mg. The course of treatment is 2-4 weeks. Contraindications: increased sensitivity to tablet components, age under 18 years, pregnancy and lactation

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 say which better antidepressants use for a specific patient. After all, the same medicine used different people, will lead in one case to complete cure, in another - it will not have any effect, in the third - it may even worsen the situation.

Almost all medications for depression, even the mildest and safest ones, can cause side effects. A strong drugs There is simply no such thing as without side effects. 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 today herbal preparations To lift your mood, they contain extracts of mint, chamomile, valerian, and motherwort. But preparations containing St. John's wort have demonstrated the greatest effectiveness in treating depression.

Mechanism therapeutic action 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

Negrustin Antidepressant and anti-anxiety agent based on St. John's wort extract Release form: there are two release forms - capsules containing 425 mg of St. John's wort extract and a solution for internal use, bottled in 50 and 100 ml bottles. Indications: mild and moderate depression, hypochondriacal depression, anxiety, manic-depressive states, chronic fatigue syndrome. Contraindications: photodermatitis, endogenous depression, pregnancy and lactation, simultaneous use of MAO inhibitors, cyclosporine, digoxin and some other drugs. Side effects: eczema, hives, increased allergic reactions, gastrointestinal disorders, headaches, iron deficiency anemia. Application: take Negrustin capsule or 1 ml of solution three times a day. Children under 16 are prescribed 1-2 capsules per day. The maximum daily dose is 6 capsules or 6 ml of solution.

List of popular drugs in alphabetical order

Name	Active substance	Type	Special properties
Amitriptyline		TCA
Agomelatine		melatonergic antidepressant
Ademetionine		mild atypical antidepressant	hepatoprotector
Adepress	Paroxetine
Azafen	Pipofezin
Azilect	Rasagiline
Aleval	Sertraline
Amizol	Amitriptyline
Anafranil	Clomipramine
Asentra	Sertraline
Aurorix	Moclobemide
Afobazole		anxiolytic and anti-anxiety drug	can be used for mild depression, over-the-counter
Bethol
Bupropion		atypical antidepressant	used in the treatment of nicotine addiction
Valdoxan	Agomelatine
Wellbutrin	Bupropion
Venflaxin
Herbion Hypericum	hypericin
Heptor	Ademetionine
Hypericin		atypical antidepressant	a drug plant origin, over-the-counter
Deprex	Fluoxetine
Deprefault	sertraline
Deprim	hypericin
Doxepin		TCA
Zyban	Bupropion
Zoloft	sertraline
Ixel	Milnacipran
Imipramine		TCA
Calixta	Mirtazapine
Clomipramine		TCA
Coaxil	Tianeptine
Lenuksin	Escitalopram
Lerivon	Mianserin
Maprotiline		tetracyclic antidepressant, selective norepinephrine reuptake inhibitor
Melipramine	Imipramine
Metrolindole		reversible selective inhibitor of MAO type A
Miansan		Mianserin
Mianserin		TCA
Miaser		Mianserin
Milnacipran		selective serotonin and norepinephrine reuptake inhibitor
Miracitol	Escitalopram
Mirtazapine		noradrenergic and specific serotonergic antidepressant	new generation drug
Moclobemide		selective MAO type A inhibitor
Negrustin	hypericin
Neuroplant	hypericin
Newwelong	Venflaxin
Paroxetine		SSRIs
Paxil	paroxetine
Pipofezin		TCA
Pyrazidol	Pearlindol
Pearlindol		reversible selective inhibitor of MAO type A
Plizil	paroxetine
Prodep	fluoxetine
Prozac	fluoxetine
Rasagiline
Reboxetine		selective norepinephrine reuptake inhibitor
Rexetine	Paroxetine
Remeron	Mirtazapine
Selegilin		selective MAO type B inhibitor
Selectra	Escitalopram
Serenata	Sertraline
Surlift	Sertraline
Sertraline		SSRIs	new generation drug
Siozam	Citalopram
Stimuloton	Sertraline
Tianeptine		atypical TCA
Trazadone		serotonin antagonist/reuptake inhibitor
Trittico	Trazadone
Thorin	Sertraline
Fevarin	Fluvoxamine
Fluvoxamine		SSRIs	new generation drug
Fluoxetine		SSRIs
Cipralex	Escitalopram
Cipramil	Citalopram
Citalon	Citalopram
Citalopram		SSRIs
Asipi	Escitalopram
Elycea	Escitalopram
Escitalopram		SSRIs

List of antidepressants produced in Russia and Ukraine:

Azafen	MAKIZ Pharma
Adepress	Veropharm
Amitriptyline	ALSI Pharma, Moscow Endocrine Plant, Alvivls, Veropharm
Afobazole	Pharmstandard
Heptor	Veropharm
Clomipramine	Vector Farm
Melipramine	Egis Rus
Miaser	Pharma Start
Ixel	Sotex
Paroxetine	Berezovsky Pharmaceutical Plant, Alvils
Pyrazidol	Pharmstandard, Lugansk Chemical Plant
Siozam	VeroPharm
Stimuloton	Egis Rus
Thorin	Veropharm
Trittico	C.S.C. Ltd.
Fluoxetine	Vector Medica, Medisorb, Medicine Production, Valeant, Ozone, Biocom, Russian Cardiology Research and Production Complex, Vector Pharm
Citalopram	ALSI Pharma
Asipi	VeroPharm
Escitalopram	Berezovsky Pharmaceutical Plant

Approximate price of drugs

Name	Price from
Adepress	595 rub.
Azafen	25 rub.
Amitriptyline	25 rub.
Anafranil	331 rub.
Asentra	732 rub.
Afobazole	358 rub.
Valdoxan	925 rub.
Heptor	979 rub.
Deprim	226 rub.
Zoloft	489 rub.
Ixel	1623 rub.
Calixta	1102 rub.
Clomipramine	224 rub.
Lenuksin	613 rub.
Lerivon	1060 rub.
Melipramine	380 rub.
Miratazapine	619 rub.
Paxil	728 rub.
Paroxetine	347 rub.
Pyrazidol	171 rub.
Plizil	397 rub.
Rasagiline	5793 rub.
Rexetine	789 rub.
Remeron	1364 rub.
Selectra	953 rub.
Serenata	1127 rub.
Surlift	572 rub.
Siozam	364 rub.
Stimuloton	422 rub.
Thorin	597 rub.
Trittico	666 rub.
Fevarin	761 rub.
Fluoxetine	31 rub.
Cipramil	1910 rub.
Cipralex	1048 rub.
Citalopram	386 rub.
Asipi	439 rub.
Elycea	597 rub.
Escitalopram	307 rub.

Antidepressants are medications that are active against depressive conditions. Depression is a mental disorder characterized by decreased mood, weakened motor activity, intellectual poverty, erroneous assessment of one’s “I” in the surrounding reality, and somatovegetative disorders.

The most likely cause of depression is biochemical theory, according to which there is a decrease in the level of neurotransmitters - nutrients in the brain, as well as a decreased sensitivity of receptors to these substances.

All drugs in this group are divided into several classes, but now let’s talk about history.

History of the discovery of antidepressants

Since ancient times, humanity has approached the issue of treating depression with different theories and hypotheses. Ancient Rome was famous for its ancient Greek physician named Soranus of Ephesus, who offered for treatment mental disorders, and depression including, lithium salts.

As scientific and medical progress progressed, some scientists resorted to a variety of substances that were used against the war against depression - from cannabis, opium and barbiturates to amphetamine. The last of them, however, was used in the treatment of apathetic and lethargic depression, which was accompanied by stupor and refusal to eat.

The first antidepressant was synthesized in the laboratories of the Geigy company in 1948. This drug became. After this we carried out clinical researches, but they did not begin to release it until 1954, when it was received. Since then, many antidepressants have been discovered, the classification of which we will talk about later.

Magic pills - their groups

All antidepressants are divided into 2 large groups:

1. Thymiretics- drugs with a stimulating effect that are used to treat depressive states with signs of depression and oppression.
2. Thymoleptics– drugs with sedative properties. Treatment of depression with predominantly excitatory processes.

Indiscriminate action:

Selective action:

• block serotonin uptake– Flunisan, Sertraline, ;
• block norepinephrine uptake— Maproteline, Reboxetine.

Monoamine oxidase inhibitors:

• indiscriminate(inhibit monoamine oxidase A and B) – Transamine;
• electoral(inhibit monoamine oxidase A) – Autorix.

Antidepressants of others pharmacological groups– Coaxil, Mirtazapine.

Mechanism of action of antidepressants

In short, antidepressants can correct some processes occurring in the brain. Human brain consists of a colossal number nerve cells called neurons. A neuron consists of a body (soma) and processes - axons and dendrites. The neurons communicate with each other through these processes.

It should be clarified that they communicate with each other by a synapse (synaptic cleft), which is located between them. Information from one neuron to another is transmitted using a biochemical substance - a transmitter. On this moment About 30 different mediators are known, but the following triad is associated with depression: serotonin, norepinephrine, dopamine. By regulating their concentration, antidepressants correct impaired brain function due to depression.

The mechanism of action differs depending on the group of antidepressants:

1. Neuronal uptake inhibitors(non-selective action) block the reuptake of mediators - serotonin and norepinephrine.
2. Neuronal serotonin uptake inhibitors: Inhibit the process of serotonin uptake, increasing its concentration in the synaptic cleft. Distinctive feature this group is the absence of m-anticholinergic activity. There is only a slight effect on α-adrenergic receptors. For this reason, such antidepressants have virtually no side effects.
3. Neuronal norepinephrine uptake inhibitors: prevent the reuptake of norepinephrine.
4. Monoamine oxidase inhibitors: monoamine oxidase is an enzyme that destroys the structure of neurotransmitters, resulting in their inactivation. Monoamine oxidase exists in two forms: MAO-A and MAO-B. MAO-A acts on serotonin and norepinephrine, MAO-B acts on dopamine. MAO inhibitors block the action of this enzyme, thereby increasing the concentration of mediators. The drugs of choice for treating depression are often MAO-A inhibitors.

Modern classification of antidepressants

Tricyclic antidepressants

Information is known about effective reception antidepressants as an auxiliary pharmacotherapy for early ejaculation and smoking.

Side effects

Since these antidepressants have a diverse chemical structure and mechanism of action, side effects may vary. But all antidepressants have the following characteristics: general signs when taking them: hallucinations, agitation, insomnia, development of manic syndrome.

Thymoleptics cause psychomotor retardation, drowsiness and lethargy, decreased concentration. Thymiretics can lead to psychoproductive symptoms (psychosis) and increased.

The most common side effects include:

• constipation;
• mydriasis;
• urinary retention;
• intestinal atony;
• violation of the act of swallowing;
• tachycardia;
• impairment of cognitive functions (impaired memory and learning processes).

Elderly patients may experience: disorientation, anxiety, visual hallucinations. In addition, the risk of weight gain increases, the development orthostatic hypotension, neurological disorders ( , ).

With long-term use - cardiotoxic effects (cardiac conduction disturbances, arrhythmias, ischemic disorders), decreased libido.

When taking selective inhibitors of neuronal serotonin uptake, the following reactions are possible: gastroenterological - dyspeptic syndrome: abdominal pain, dyspepsia, constipation, vomiting and nausea. Increased anxiety levels, insomnia, increased fatigue, tremors, impaired libido, loss of motivation and emotional dulling.

Selective norepinephrine reuptake inhibitors cause side effects such as: insomnia, dry mouth, dizziness, constipation, atony Bladder, irritability and aggressiveness.

Tranquilizers and antidepressants: what's the difference?

From this we can conclude that tranquilizers and antidepressants have different mechanisms of action and differ significantly from each other. Tranquilizers are unable to treat depressive disorders, therefore their appointment and reception is irrational.

The power of "magic pills"

Depending on the severity of the disease and the effect of use, several groups of drugs can be distinguished.

Strong antidepressants - effectively used in the treatment of severe depression:

1. – has pronounced antidepressant and sedative properties. The onset of the therapeutic effect is observed after 2-3 weeks. Side effect: tachycardia, constipation, difficulty urinating and dry mouth.
2. Maprotiline,– similar to Imipramine.
3. Paroxetine– high antidepressant activity and anxiolytic effect. Taken once a day. Therapeutic effect develops within 1-4 weeks after starting treatment.

Mild antidepressants – prescribed in cases of moderate and mild depression:

1. Doxepin– improves mood, eliminates apathy and depression. A positive effect of therapy is observed after 2-3 weeks of taking the drug.
2. - has antidepressant, sedative and hypnotic properties.
3. Tianeptine– stops motor retardation, improves mood, increases the overall tone of the body. Leads to the disappearance of somatic complaints caused by anxiety. Due to availability balanced action, indicated for anxious and inhibited depression.

Herbal natural antidepressants:

1. St. John's wort– contains hepericin, which has antidepressant properties.
2. Novo-Passit– it contains valerian, hops, St. John's wort, hawthorn, lemon balm. Contributes to the disappearance, and.
3. Persen– also contains a collection of herbs: peppermint, lemon balm, and valerian. Has a sedative effect.
   Hawthorn, rose hips - have sedative properties.

Our TOP 30: the best antidepressants

We analyzed almost all antidepressants that were available for sale at the end of 2016, studied reviews and compiled a list of 30 the best drugs, which have virtually no side effects, but at the same time are very effective and perform their tasks well (each to their own):

1. Agomelatine– used for episodes of major depression of various origins. The effect occurs after 2 weeks.
2. – provokes inhibition of serotonin uptake, used for depressive episodes, the effect occurs after 7-14 days.
3. Azafen– used for depressive episodes. The treatment course is at least 1.5 months.
4. Azona– increases the content of serotonin, is part of the group of strong antidepressants.
5. Aleval– prevention and treatment of depressive conditions of various etiologies.
6. Amizol– prescribed for agitation, behavioral disorders, and depressive episodes.
7. – stimulation of catecholaminergic transmission. It has adrenergic blocking and anticholinergic effects. Scope of application: depressive episodes.
8. Asentra– a specific serotonin uptake inhibitor. Indicated for the treatment of depression.
9. Aurorix– MAO-A inhibitor. Used for depression and phobias.
10. Brintellix– antagonist of serotonin receptors 3, 7, 1d, agonist of serotonin receptors 1a, correction of depressive states.
11. Valdoxan– a stimulator of melatonin receptors, to a small extent a blocker of a subgroup of serotonin receptors. Therapy.
12. Velaxin– an antidepressant of another chemical group, enhances neurotransmitter activity.
13. – used for mild depression.
14. Venlaxor– a powerful serotonin reuptake inhibitor. Weak β-blocker. Treatment of depression and anxiety disorders.
15. Heptor– in addition to antidepressant activity, it has antioxidant and hepatoprotective effects. Well tolerated.
16. Herbion Hypericum– a herbal-based drug, part of the group of natural antidepressants. Prescribed for mild depression and.
17. Deprex– an antidepressant has an antihistamine effect, used in the treatment.
18. Deprefault– a serotonin uptake inhibitor, has a weak effect on dopamine and norepinephrine. There is no stimulating or sedative effect. The effect develops 2 weeks after administration.
19. – antidepressant and sedative effects occur due to the presence of St. John's wort herb extract. Approved for use in the treatment of children.
20. Doxepin– blocker of H1 serotonin receptors. The action develops 10-14 days after the start of administration. Indications -
21. Miansan– stimulator of adrenergic transmission in the brain. Prescribed for depression of various origins.
22. Miracitol– enhances the effect of serotonin, increases its content in the synapse. In combination with monoamine oxidase inhibitors, it causes severe side effects.
23. Negrustin– an antidepressant of plant origin. Effective for mild depressive disorders.
24. Newwelong– serotonin and norepinephrine reuptake inhibitor.
25. Prodep– selectively blocks the uptake of serotonin, increasing its concentration. Does not cause a decrease in the activity of β-adrenergic receptors. Effective for depression.
26. Citalon– a high-precision serotonin uptake blocker with minimal effect on the concentration of dopamine and norepinephrine.

There's something for everyone

Antidepressants are most often not cheap, we have compiled a list of the most inexpensive of them in ascending order of price, with the cheapest drugs at the beginning and the more expensive ones at the end:

The truth is always beyond theory

To understand the whole point about modern, even the most best antidepressants, to understand what their benefits and harms are, it is also necessary to study the reviews of people who had to take them. As you can see, there is nothing good in taking them.

I tried to fight depression with antidepressants. I quit because the result was depressing. I looked for a lot of information about them, read many sites. There is contradictory information everywhere, but everywhere I read it, they write that there is nothing good about them. I myself experienced shaking, pain, and dilated pupils. I got scared and decided that I didn’t need them.

Three years ago, depression began, while I was running to clinics to see doctors, it was getting worse. There was no appetite, she lost interest in life, there was no sleep, her memory deteriorated. I visited a psychiatrist, he prescribed Stimulaton for me. I felt the effect after 3 months of taking it, I stopped thinking about the disease. I drank for about 10 months. Helped me.

Karina, 27

It is important to remember that antidepressants are not harmless drugs and you should consult your doctor before using them. He will be able to pick up the right drug and its dosage.

You should monitor your mental health and contact specialized institutions in a timely manner so as not to aggravate the situation, but to get rid of the disease in time.