Selective antidepressants. SSRI drugs - how they work, properties, list of drugs. What do SSIOs not work with?

Especially in outpatient practice, relatively new antidepressants are used - selective serotonin reuptake inhibitors (SSRIs), which have significantly fewer side effects than tricyclic antidepressants, due to a selective effect on serotonin metabolism (selective inhibition of 5-HT uptake).

SSRIs are represented by such drugs as: fluoxetine (Prozac), fluvoxamine (Fevarin), sertraline (Zoloft, Stimoton, Asentra), paroxetine (Paxil, Rexetin), cipramil (Citalopram, Cipralex).

Unlike TCAs, a feature of the action of serotonergic antidepressants is their selective effect on the serotonergic system, originally identified in laboratory studies (Wong D., et al., 1974; Fuller R., et al., 1977). The effectiveness of SSRI therapy for depression is at least 65% (Mulrow D., et al., 2000)

Due to the affinity of these drugs and their active metabolites for serotonin receptors, blockade of serotonin reuptake occurs at the level of presynaptic endings, thereby increasing the concentration of the mediator in the synaptic cleft, which in turn leads to a decrease in the synthesis and circulation of serotonin (Stark R., et al., 1985).

Selective, but non-specific for a certain subtype of receptors (Stahl S., 1993) action of SSRIs does not always increase the effectiveness of treatment, especially when it comes to treating patients suffering from severe depression (Anderson I., Tomenson B., 1994; Burce M., Prescorn S., 1995).

SSRI drugs have completely different chemical structures and differ from each other in terms of pharmacokinetic parameters, dosages, and side effect profiles. The selectivity of 5-HT reuptake suppression reduces the number of side effects, improves tolerability and reduces the frequency of refusals to take drugs in comparison with TCAs (Anderson I., Tomenson T., 1994).

Table Comparative characteristics of SSRIsaccording to the intensity of the effect of the antidepressant

Note: +++ - significant intensity, ++ - moderate intensity, + - weak intensity of the effect.

It is necessary to emphasize the relative safety of SSRIs (less number and severity of side effects) and greater comfort of treatment (the possibility of conducting therapy on an outpatient basis).

SSRIs are also distinguished by low toxicity (the risk of death in case of poisoning or overdose is practically zero), as well as the possibility of using drugs of this group in patients with contraindications to the use of TCAs (cardiac arrhythmia, difficulty urinating due to prostatic hypertrophy, angle-closure glaucoma) ( Mashkovsky M.D., 1997).

It should be noted that in the literature there are cases of central and peripheral side effects during the treatment of SSRIs (Baldessarini R., 1989).

These drugs are more expensive antidepressants than other drugs used to treat depression.

Most of the selective serotonin reuptake inhibitors (SSRIs) are long-acting and are used in fixed doses. The pharmacokinetics of various representatives of the SSRI group has its own characteristics depending on the age of patients and somatic burden. So the half-life of fluvoxamine slightly increases in elderly patients and patients with liver pathology (Raghoebar M., Roseboom H., 1988). The duration of the half-life of sertraline is also influenced by age (Warrington S. 1988), and the effect of fluoxetine significantly affects the functionality of the liver (Bergstrom M., Lemberg L, et al., 1988).

Clinical trials of SSRIs have demonstrated that they, like TCAs, are effective in most depressive conditions, including anxiety, sleep disturbances, psychomotor agitation, and lethargy. (Levine S. et al., 1987, Dunlop S. et al., 1990, Claghorn J., 1992, Kiev A., 1992).

Table Comparative assessment of the additional therapeutic effect of SSRIs

Indications for the use of SSRIs are severe and moderate depression (simple type) with mild anxiety and anxiety (Pujynski S., et al., 1994; Pujynski S, 1996). In addition, SSRIs can be used to treat personality disorders, including anger reactions and impulsiveness.

The medical literature emphasizes the sensitivity of vital disorders to the action of these antidepressants (Laakmann G. et al. 1988).

A number of studies have described that patients in whom melancholy prevailed in the structure of the syndrome demonstrated a good therapeutic response when using SSRIs (Reimherr F. et al., 1990, Tignol G. et al., 1992; Mosolov S.N., Kalinin V .V., 1994).

Given the good tolerability of these drugs, they are recommended for use in old age.

At the same time, most researchers note a fairly high anxiolytic activity of SSRIs (Amin M. et al., 1989; Kiev A., 1992, Bovin R.Ya., et al. 1995, Ivanov M.V. et al. 1995). At the initial stages of the appearance of SSRIs in the domestic literature, there were indications of low effectiveness, and sometimes even increased anxiety when using SSRIs in patients with anxious depression (Kalinin V.V., Kostyukova E.G., 1994, Lopukhov I.G. et al. , 1994, Mosolov S.N., et al., 1994).

In recent years, studies have been conducted that provide comparative assessments of SSRIs with TCAs. Most authors note that the activity of new compounds is comparable to traditional drugs (Guelli J.. et al., 1983; Shaw D., et al., 1986; Hale A. et al., 1991, Fontaine R. et al., 1991 ). When comparing SSRIs with TCAs, traditionally used in the treatment of anxiety and depressive conditions, it is usually indicated that differences in the effectiveness of the studied drugs in terms of the ability to relieve anxiety are not statistically significant (Feighner J., 1985, Laws D. et al., 1990 , Avrutsky G.Ya., Mosolov S.N., 1991, Doogan D., Gailard V., 1992).

According to many authors, SSRIs are effective in some cases when the use of TCAs has proven ineffective (Weilburg J.B. et al., 1989, Beasley C.M. et al.. 1990; Ivanov M.V. et al., 1991; Bovin R.Ya. s et al., 1992; Serebryakova T.V., 1994; Bovin R.Ya., et al. 1995). According to Beasley C., Sayler M. (1990), patients resistant to TCAs are sensitive to new drugs in 50-60% of cases.

It is necessary to emphasize the greater safety of SSRIs compared to TCAs (less number and severity of side effects), greater comfort of treatment (the possibility of conducting therapy on an outpatient basis) (Boyer W. Feighner J., 1996).

When taking TCAs, 30% of patients are forced to refuse treatment due to the severity of side effects, while in the case of prescribing new drugs, only 15% of patients have to interrupt medication (Cooper G., 1988).

S. Montgomery, S. Kasper (1995) showed that the frequency of drug discontinuation due to side effects was 14% of patients treated with SSRIs and 19% with TCAs. The advantage of second-generation antidepressants is especially important during long-term therapy (Medavar T. et al., 1987).

R.Ya. Bovin (1989) points to an increasing risk of suicide in the early stages of TCA therapy. While, in most studies on SSRIs, the authors pay attention to the high orientation of these drugs against suicide (Fava M. et al., 1991; Cohn D. et al., 1990; Sacchetti E. et al., 1991) .

In addition to the treatment of depression, attempts are increasingly being made to long-term use of antidepressants (fluoxetine, sertraline) to prevent its relapse.

Cohn G.N. et al., (1990), given the good tolerability of SA, recommend their use in geriatric psychiatry.

There is no consensus on the rate of onset of effect with SSRIs. According to foreign authors, the clinical effect of SSRIs is detected later than TCAs (Roose S, et al. 1994). At the same time, domestic scientists indicate that SSRIs tend to have a faster onset of therapeutic effect compared to other antidepressants (Avrutsky G.Ya., Mosolov S.N., 1991).

In the SSRI group, different drugs differ in the strength of the action on the receptors and the level of selectivity. Moreover, selectivity and strength of action do not coincide. Paroxetine was found to be a more potent inhibitor of serotonin return, while citalopram was more selective. Differences in selectivity and power of action on receptors determine not only the characteristics of the therapeutic effect of a particular drug, but also the presence of side effects (Thopas D., et al., 1987; Hyttel G., 1993).

Ceteris paribus, depression relapses are more common after fluoxetine than paroxetine and after citalopram than sertraline; with an almost equal number of relapses during treatment with sertraline and paroxetine.

Since fluvoxamine and paroxetine have a pronounced sedative and anti-anxiety effect, they are close in their spectrum of activity to drugs such as amitriptyline or doxepin. Most other drugs, especially fluoxetine, are more reminiscent of the profile of imipramine, as they have a disinhibitory effect and can increase the manifestations of anxiety and anxiety (Caley Ch., 1993; Pujynski S., et al., 1994; Montgomery S., Johnson F., 1995 ). In the domestic literature there are also indications of low efficiency, and sometimes even increased anxiety when using SSRIs in patients with anxiety depression (Kalinin V.V., Kostyukova E.G., 1994, Lopukhov I.G. et al., 1994, Mosolov S.N., et al., 1994).

Due to the disinhibitory effect, such drugs should not be used for anxiety, restlessness, motor disinhibition, insomnia, suicidal thoughts and tendencies. According to S. Pujynski (1996), psychotic forms of depression are a relative contraindication to the use of SSRIs. However, Feighner J., Bouer W (1988), on the contrary, note the positive effect of these drugs even in the psychotic version of depression.

The most common side effects when taking serotonin inhibitors are gastrointestinal disorders: nausea and vomiting, constipation and loose stools. Some patients experience weight loss.

Table Comparative characteristics of SSRIs in terms of severity of side effects

Note: +++ - significant severity of side effects, ++ - moderate severity of side effects, + - mild severity of side effects

The next most common side effects are restlessness, anxiety, insomnia, less often increased drowsiness.

Patients are especially concerned about sexual disorders that may occur when using these drugs. The most common of them: decreased libido, weak erection and difficulty achieving orgasm. With severe sexual disorders that have developed during SSRI therapy, drug doses are usually reduced or canceled for several days. In some cases, drugs that are antagonists of serotonin (cyproheptadine) or drugs that enhance sexual functions (yohimbine) are prescribed.

The most frequently mentioned contraindications to taking SSRIs include: hypersensitivity to the drug, pregnancy (cases of fluoxetine therapy for depression during this period are known) and breastfeeding (the effect of SSRIs on the fetus and child development is little studied), epilepsy, impaired kidney and liver function. Preparations of this group can not be used for poisoning with alcohol and psychotropic drugs. SSRIs should not be used earlier than 2 weeks after the end of therapy with non-selective MAO inhibitors, as well as together with other serotonergic drugs (Feihner J., Boyer W., 1996).

All registered SSRIs can provoke a phase change from depressive to manic in persons with a bipolar course of the disease, but such a phase change occurs less frequently than with the use of TCAs (Kharkevich M.Yu., 1996). In addition, in the treatment of dysthymia with antidepressants, a mild degree of mania occurs in 10% of patients.

In connection with the trend towards a wider use of serotonin reuptake inhibitors in the treatment of depression, it makes sense to dwell on the characteristics of individual representatives of this group of drugs.

In his practical work, the psychiatrist in some cases faces difficulties in distinguishing the clinical manifestations of depression from the side effects of SSRIs, SSRI withdrawal syndrome, and potentially life-threatening serotonin syndrome.

In the practice of a psychiatrist, differential diagnosis of the withdrawal syndrome of these drugs, their side effects and clinical serotonin syndrome is of particular importance in the process of SSRI therapy. The SSRI withdrawal syndrome, which occurs in the event of a rapid decrease in the dose of the drug or its abrupt withdrawal, is characterized by such signs as: dizziness, nausea, anxiety and headache. As noted above, the side effects of SSRIs usually appear in the first two weeks of therapy and are expressed in asthenia, diarrhea, nausea, anxiety, dizziness, sleep disturbance, nervousness and tremor. For serotonin syndrome that occurs with an overdose of SSRIs or its combination with TCAs, abdominal cramps, psychomotor agitation, diarrhea, convulsions, tachycardia, hypo or hypertension, sweating, hyperthermia are typical. In depression, the core of the depressive state is anhedonia.

fluoxetine

One of the first serotonin reuptake inhibitors was fluoxetine (Prozac), which since the early 80s has been actively used to treat various depressive spectrum disorders. In addition, its positive effect in the treatment of bulimia has been noted.

Fluoxetine is prescribed at a dose of 20 mg. once a day in the morning, if necessary, the dose is increased to 40-80 mg. (in addition to tablet forms, a special solution of fluosetin 4 mg / ml is used abroad).

The drug is well absorbed when administered orally, demethylated in the liver with the formation of inactive metabolites and pharmacologically active norfluoxetine. Due to the peculiarities of metabolism, the effect of fluoxetine significantly affects the functionality of the liver (Bergstrom M., Lemberg L, et al., 1988). It inhibits the activity of hepatic cytochromes P4502D6, and therefore slows down the metabolism of a number of psychotropic drugs, including TCA, with an increase in their plasma concentration, which determines the possibility of toxic effects (Creve N., et.al., 1992).

The maximum concentration in the blood when taking fluoxetine is reached after 6 hours. It has the longest half-life of all SSRIs, which in this case is two to three days, and the half-life of its active metabolite, norfluoxetine, reaches 7-9 days. This circumstance provides an advantage in the treatment of patients who occasionally forget about taking the next dose, but, on the other hand, complicates the replacement of the drug with other antidepressants (especially MAOIs). It takes several weeks to reach a stable concentration of the active substance. It was noted that, despite the anxiolytic effect, fluoxetine is able to increase the manifestations of anxiety and arousal at the initial stage of therapy.

In terms of its spectrum of action, fluoxetine is more reminiscent of the profile of imipramine, since it has a disinhibitory effect and, as noted above, can increase the manifestations of anxiety and anxiety (Caley Ch., 1993; Pujynski S., et al., 1994; Montgomery S., Johnson F., 1995). There is a point of view according to which, due to the disinhibitory effect of fluoxetine, it should not be used for anxiety, restlessness, motor disinhibition, insomnia, suicidal thoughts and tendencies, however, recent studies have shown that taking fluosetine does not increase the risk of suicide (Freemante N., et.al ., 2000).

Fluoxetine (Prozac), compared to other SSRIs, eliminates signs of depression much more slowly (over 2-3 weeks), however, its final effect turned out to be similar to that of other drugs of this class (Edwards J., Anderson I., 1999). There are observations according to which, in terms of its effectiveness in relieving symptoms of depression, fluoxetine is approximately equal to TCAs (Beasley C., et al., 1991).

At the same time, there is a point of view according to which fluoxetine is inferior to other SSRIs in terms of its ability to stop the general manifestations of depression (Williams J., et al., 2000).

In the first days of using fluoxetine, and possibly at later stages of treatment, nausea, akathisia, headaches, impaired visual acuity, and allergic skin reactions may occur. When taking fluosetine, sexual dysfunctions were noted (Guthrie S., 1991; De Vane C. 1994; Pujynski S., 1996).

fluvoxamine

Fluvoxamine (fevarin), as a selective serotonin reuptake inhibitor, has a distinctly activating, mood-enhancing effect, it calms, stabilizes the activity of the autonomic system and can be recommended when depression is combined with anxiety. In addition, fluvoxamine treatment has the advantage of being relatively fast onset and smooth onset, which generally promotes a good relationship between the patient and their physician.

Fluvoxamine is prescribed at a dose of 50 mg. per day once in the evening. The dose of the drug can be increased to 100 mg. (average dose of effectiveness) for 5-7 days. If necessary, the dosage of the drug can be further increased at intervals of 2-4 weeks (maximum daily dosage - 500 mg.), Starting with a dose of 150 mg. the drug is prescribed several times a day.

The active metabolites of fluvoxamine are unknown. The mean elimination half-life is 20 hours, plasma concentration is not proportional to the dose taken.

Symptoms of anxiety disorder in most cases are eliminated earlier than depressive. This was clinically manifested by an improvement in the general condition of patients, leading them to be more collected, confident and outwardly calm. The effectiveness of this drug in patients with obsessive-compulsive disorders and social phobia, in particular, in childhood, is noted.

The addition of fluvoxamine to atypical neuroleptics can reduce the severity of primary negative symptoms in patients with chronic schizophrenia. At the same time, comparative studies have shown that from the group of selective serotonin reuptake inhibitors, it has the most side effects (Freemante N., et al., 2000), the least - sertraline (Edwards J., Anderson I., 1999 ).

Citalopram

Citalopram has a significantly higher level of selectivity for serotonin transporters than norepinephrine and dopamine transporters.

The drug is prescribed in a dose of 20 mg. per day once a day in the morning. For most patients, this dose is the most effective, the maximum daily dose of the drug is 60 mg.

Citalopram practically does not enter into drug interactions, due to the fact that it has little effect on the activity of certain liver enzymes (cytochrome P450 enzyme system). Therefore, it is often used in the treatment of depressive conditions that develop as a result of chronic somatic diseases. Interdrug drug interactions are minimal. Under the influence of cytochrome P450, citalopram is converted into two main metabolites: demethylcitalopram and didemethylcitalopram. These metabolites have pharmacological activity, but much less than that of citalopram itself. The half-life of citalopram is 30 hours. It is characterized by a linear dependence of plasma concentration versus dose in the therapeutic range. For the treatment of severe depression, the dose of the drug should be increased.

When prescribing citalopram, the percentage of men with impaired sexual function turned out to be extremely insignificant - a side effect that is relatively common when prescribing this group of drugs. Headache and nausea were the most common side effects during the first two weeks of treatment with citalopram.

Sertraline

Sertraline (zoloft, stimuloton, asentra) is characterized by a thymoanaleptic (anxiolytic) effect of moderate severity. There are no vegetostabilizing, sedative, timerectic, adrenergic and anticholinergic (muscarinic) effects. The drug does not affect psychomotor functions, has a weak antiphobic and very weak hypotensive effect.

Indications for use are mild and moderate dreary depressions with secondary anxiety and somatoform disorders. After obtaining a satisfactory effect, continued treatment with sertraline helps to prevent the recurrence of depression or its occurrence in the future.

Sertraline is also used to treat obsessive-compulsive disorder (OCD).

As a rule, the antidepressant effect occurs after one week of therapy.

After reaching the initial effect, long-term treatment with sertraline for up to 2 years ensures its sufficient efficacy and good tolerability. Sertraline is used to treat panic disorders, post-traumatic stress disorder syndrome (PTSD). The initial therapeutic effect in this case may appear within 7 days, but the full effect is usually achieved later - after 2-4 weeks (possibly for a longer time, especially with OCD). There is a point of view according to which the drug usually reduces the secondary anxiety associated with melancholy depression.

Sertraline (zoloft, stimuloton) is a relatively low-toxic antidepressant from the SSRI group, it is used in child psychiatry, as well as in cases of depressive spectrum disorders that develop after an acute episode of schizophrenia.

Sertraline is prescribed at a dose of 50 mg. per day (usually once a day in the morning, regardless of the meal). The dose can be increased by 50 mg. in Week. Recommended daily doses: for inpatient treatment of depression - 50-100 mg, for outpatient use - 25-50 mg. If necessary, the dose is increased at intervals of 2-4 weeks (the maximum daily dose is 200 mg.).

At therapeutic doses, sertraline inhibits platelet uptake of serotonin. It is actively metabolized in the liver, approximately 98% of it is present in the body in a protein-bound form, and its main metabolite has a weak pharmacological activity. Unlike most antidepressants, it predominantly binds to a1-glycoprotein, while other drugs interact mainly with albumin.

The half-life of sertraline is influenced by age. In children, sertraline metabolism is more active (Warrington S. 1988). Given the latter circumstance, the drug is recommended for use in children at a lower dose in order to avoid excessive plasma levels. At the same time, according to other authors, the pharmacokinetic profile in adolescents and the elderly does not differ significantly from the profile of patients aged 18 to 65 years.

Sertraline is slowly absorbed within 4-6 hours, eliminated through the gastrointestinal tract and kidneys, the equilibrium concentration of the drug is reached within one week after the start of treatment.

The mean half-life of sertraline is 22-36 hours. Equilibrium concentrations of sertraline are established after 1 week of treatment.

Kidney pathology has almost no effect on the clearance of sertraline. At the same time, in case of liver pathology, the "half-life" of sertraline in serum, as well as its concentration in plasma, increase by almost 50%.

Side effects: tremor, nausea, dry mouth, diarrhea. Usually, side effects resolve spontaneously by the end of 4 weeks of therapy. Early unwanted side effects are especially common in the treatment of panic disorders.

Contraindications to the appointment of the drug are diseases of the liver, kidneys with a violation of their function. After discontinuation of the drug, MAOIs are prescribed no earlier than 5 weeks later.

With chronic use of sertraline, addiction develops to it, since its prolonged use leads to a decrease in the number of its receptors (Anthony P., et al., 2002).

Paroxetine

Paroxetine (paxil, rexetine) has the highest affinity for serotonin receptors of all SSRIs. This drug inhibits the reuptake of serotonin much more actively than sertraline or fluoxetine.

Begin treatment with paroxetine with a daily dose of 20 mg. (once a day). In some cases, the initial dose is 10 mg. Most studies show that this dose becomes effective for most patients treated with this drug. If necessary, it is increased by 10 mg. per day with an interval of 2-4 weeks (the maximum daily dose of paroxetine is 50 mg.).

The half-life of paroxetine is 21-24 hours. Therefore, one week after the start of treatment is sufficient to achieve a stable concentration.

During the metabolism of this drug, active substances are not formed. Up to 60% of poroxetine present in serum is filtered in the kidneys. With mild or moderate impairment of their function, the maximum concentration of a substance in serum can double.

This enzyme is easily saturated, and with an increase in the dose of paroxetine, the relationship between its dose and plasma concentration becomes non-linear. With long-term use of paroxetine, its stable plasma concentration is several times higher than that which would be expected, based on the results of its single dose.

Paroxetine may cause slight weight gain.

Recently, the number of people suffering from depression has increased significantly. This is largely facilitated by the frantic rhythm of modern life, the 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 are reflected in 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 one should not be afraid of this diagnosis. The disease does not indicate that the person suffering from it is mentally or mentally handicapped. 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 roll over 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 its 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 not actually the result of a person's weak will, his insufficient efforts to correct the situation. In most cases, it is a biochemical disease caused by a metabolic disorder 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 is not always possible to cure non-drug means. It is well known that a change of scenery, relaxation techniques and auto-training, etc., can help a person with a depressed mood. but all these methods require considerable effort on the part of the patient, his will, desire and energy. And with depression, they just don’t exist. It turns out a vicious circle. And it is often impossible to break it without the help of drugs that change the 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 what kind of clinical effect the drugs have on the nervous system. In total, three types of such actions are distinguished:

  • Sedative
  • Balanced
  • Activating

Sedative antidepressants have a calming effect on the psyche, relieving anxiety and at the same time increasing the activity of nervous processes. Activating drugs fight well with 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 the intake.

Classification of antidepressants according to 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 of the group allows us to consider them a benchmark for antidepressants.

Tricyclic drugs are able to 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

Amitriptyline

Tricyclic antidepressant. It has both antidepressant and mild analgesic effects

Composition: 10 or 25 mg amitriptyline hydrochloride

Dosage form: dragee or tablets

Indications: depression, sleep disorders, behavioral disorders, mixed emotional disorders, chronic pain syndrome, migraine, enuresis.

Side effects: agitation, hallucinations, visual disturbances, tachycardia, pressure fluctuations, tachycardia, indigestion

Contraindications: heart attack, individual intolerance, lactation, intoxication with alcohol and psychotropic drugs, conduction disorders of the heart muscle.

Application: immediately after meals. The initial dose is 25-50 mg at night. Gradually, the daily dose increases to 200 mg in three divided 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 number 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 they have a large number of side effects. These include:

  • hypotension
  • hallucinations
  • Insomnia
  • Agitation
  • constipation
  • Headache
  • Dizziness
  • sexual dysfunction
  • visual impairment

When taking certain drugs, you should also follow a special diet to avoid the ingestion of potentially dangerous enzymes that are metabolized with the help of MAO.

The most modern antidepressants of this class have the ability to inhibit only one of two types of the 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.

The main selective MAO inhibitors:

  • Moclobemide
  • Pirlindol (pyrazidol)
  • befol
  • Metralindol
  • Garmalin
  • Selegiline
  • 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 so 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 that transmits the nerve impulse, but is transferred to another cell. Thus, antidepressants such as SSRIs increase the activity of serotonin in the neural circuit, which has a beneficial effect on brain cells affected by depression.

As a rule, drugs of this group are especially effective in severe depression. In depressive disorders of minor and moderate severity, the effect of drugs is not so noticeable. However, a number of doctors have a different opinion, which is that in 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

fluoxetine

Antidepressant, selective serotonin reuptake inhibitor. Has an antidepressant effect, relieves feelings of depression

Release form: 10 mg tablets

Indications: depression of various origins, obsessive-compulsive disorder, bulimia nervosa

Contraindications: epilepsy, convulsive tendencies, severe renal or hepatic insufficiency, glaucoma, adenoma, suicidal tendencies, taking MAO inhibitors

Side effects: hyperhidrosis, chills, serotonin intoxication, indigestion

Application: regardless of the meal. The usual scheme is once a day, in the morning, 20 mg. 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 these 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. 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 disorders.

Contraindications: allergy to components, age up to 18 years, simultaneous use with MAO inhibitors, anorexia nervosa, convulsive disorders.

Side effects: an overdose of the drug is extremely dangerous, which can cause epileptic seizures (2% of patients at a dose of 600 mg). Urticaria, anorexia or lack of appetite, tremor, tachycardia are also observed.

Application: the medicine should be taken once a day, in the morning. The typical dose is 150 mg, with a maximum daily dose of 300 mg.

Next generation antidepressants

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

  • Sertraline
  • fluoxetine
  • fluvoxamine
  • Mirtazalin
  • Escitalopram

The difference between antidepressants and tranquilizers

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

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

Tranquilizers, as a rule, are fast-acting drugs. They can be used to fight depression, but mostly as ancillary drugs. The essence of their impact on the human psyche is not in the correction of his emotional background in the long term, as in drugs for depression, but in the suppression of manifestations of negative emotions. They can be used as a means to reduce fear, anxiety, agitation, panic attacks, etc. Thus, they are more of an anti-anxiety and sedative than an antidepressant. In addition, during the course of treatment, most tranquilizers, especially diazepine drugs, are addictive and addictive.

Can you buy antidepressants without a prescription?

According to the current rules for dispensing 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 bought without prescriptions. In practice, of course, pharmacists can sometimes turn a blind eye to the rules in 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 situation will be the same in another.

You can buy without a doctor's prescription only drugs for the treatment of mild depressive disorders such as Afobazol, "daytime" tranquilizers and herbal preparations. But in most cases, it is difficult to attribute them to real antidepressants. It would be more correct to classify them as sedative drugs.

Afobazole

Russian-made anti-anxiety, anxiolytic and mild antidepressant without side effects. OTC drug.

Release form: 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 can be allergic reactions, disorders of the gastrointestinal tract, headaches.

Application: It is advisable to take the drug after meals. A single dose is 10 mg, daily - 30 mg. The course of treatment is 2-4 weeks.

Contraindications: hypersensitivity to the components of the tablets, age up to 18 years, pregnancy and lactation

Why is self-treatment of depression dangerous?

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

Almost all depression medications, even the mildest and safest, can cause side effects. And strong drugs without side effects simply do not exist. Especially dangerous is prolonged uncontrolled use of drugs or excess dosage. In this case, intoxication of the body with serotonin (serotonin syndrome) can occur, which can lead to death.

How to get a prescription for the drug?

If you think that you have depression, it is recommended to consult a psychotherapist or neurologist. Only he can carefully examine your symptoms and prescribe the appropriate remedy for your case.

Herbal remedies for depression

The most popular herbal preparations for raising the mood today contain extracts of mint, chamomile, valerian, motherwort. But preparations containing St. John's wort showed the greatest effectiveness in depression.

The mechanism of the therapeutic action of St. John's wort has not yet been clearly elucidated, but scientists believe that the enzyme hypericin contained in it is able to accelerate 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.

Hypericum preparations are mild antidepressants. They will not help with any depression, especially with its severe forms. However, the effectiveness of St. John's wort in mild to moderate depression has been proven by serious clinical studies, in which it proved to be no worse, and in some respects even better than the 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 the age of 12. Among the negative effects of taking St.

St. John's wort-based medicines are sold without a prescription. So if you're looking for over-the-counter depression remedies, this class of drugs may be your best bet.

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 administration, poured into 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, urticaria, increased allergic reactions, gastrointestinal disorders, headaches, iron deficiency anemia.

Application: three times a day is taken in a capsule of Negrustin or 1 ml of solution. 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 alphabetically

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, OTC
befol
Bupropion atypical antidepressant used in the treatment of nicotine addiction
Valdoxan Agomelatine
Wellbutrin Bupropion
Venflaxin
Herbion Hypericum hypericin
Heptor Ademetionine
Hypericin atypical antidepressant herbal preparation, non-prescription
Deprex fluoxetine
Default sertraline
Deprim hypericin
Doxepin TCA
Zyban Bupropion
Zoloft sertraline
Ixel Milnacipran
Imipramine TCA
Calixta Mirtazapine
Clomipramine TCA
Coaxil Tianeptine
Lenuxin Escitalopram
Lerivon Mianserin
Maprotiline tetracyclic antidepressant, selective norepinephrine reuptake inhibitor
Melipramine Imipramine
Metralindol reversible selective MAO inhibitor 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 inhibitor type A
Negrustin hypericin
Neuroplant hypericin
Newwelong Venflaxin
Paroxetine SSRIs
Paxil paroxetine
Pipofezin TCA
pyrazidol Pirlindol
Pirlindol reversible selective MAO inhibitor type A
Plizil paroxetine
Prodep fluoxetine
Prozac fluoxetine
Rasagiline
Reboxetine selective norepinephrine reuptake inhibitor
Rexetin Paroxetine
Remeron Mirtazapine
Selegiline selective MAO inhibitor type B
selectra Escitalopram
Serenata Sertraline
Sirlift Sertraline
Sertraline SSRIs new generation drug
Siozam Citalopram
Stimuloton Sertraline
Tianeptine atypical TCA
Trazadone serotonin reuptake antagonist/inhibitor
Trittico Trazadone
Thorin Sertraline
Fevarin fluvoxamine
fluvoxamine SSRIs new generation drug
fluoxetine SSRIs
Cipralex Escitalopram
Cipramil Citalopram
Citalon Citalopram
Citalopram SSRIs
acepi Escitalopram
Elycea Escitalopram
Escitalopram SSRIs

List of antidepressants produced in Russia and Ukraine:

Azafen MAKIZ Pharma
Adepress Veropharm
Amitriptyline ALSI Pharma, Moscow Endocrin Plant, Alvivls, Veropharm
Afobazole Pharmstandard
Heptor Veropharm
Clomipramine Vector Pharm
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 CSC Ltd
fluoxetine Vector Medica, Medisorb, Production of Medicines, Valeant, Ozone, Biocom, Russian Cardiology Research and Production Complex, Vector Pharm
Citalopram ALSI Pharma
acepi 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.
Lenuxin 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.
Rexetin 789 rub.
Remeron 1364 rub.
selectra 953 rub.
Serenata 1127 rub.
Sirlift 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.
acepi 439 rub.
Elycea 597 rub.
Escitalopram 307 rub.

Used as antidepressants until the mid-1950s. They disappeared from use due to a large number of side effects. However, some alkaloids have been used for longer - for example, preparations of St. John's wort extract have been used for a long time as an adjuvant therapy.

The first synthetic antidepressants were introduced into medical practice in the mid-1950s. Until the 1990s, psychiatrists had only two groups of drugs: MAO inhibitors and tricyclic antidepressants. In the 1990s, selective drugs were synthesized that had fewer side effects and a stronger antidepressant effect.

Further development

The new drugs, which were named antidepressants in 1952, became prescription-only drugs by the mid-1950s. At the time, it was thought that only 50-100 people out of a million people were affected by depression, so pharmaceutical companies showed little interest in antidepressants. Sales of these drugs in the 1960s were incomparable in volume to sales of antipsychotics and benzodiazepines.

Later, imipramine came into wide use, and its analogues were synthesized. In the 1960s, selective monoamine oxidase inhibitors appeared, as well as selective serotonin reuptake inhibitors. In the future, the main direction in the creation of new antidepressants was the reduction of side effects, as well as the strengthening of the main ones. This is achieved by increasing the selectivity of the action of drugs on the "necessary" receptors.

Scheme of action

The main effect of antidepressants is that they block the breakdown of monoamines (serotonin, norepinephrine, dopamine, phenylethylamine, etc.) under the action of monoamine oxidases (MAOs) or block the reverse neuronal uptake of monoamines. According to modern concepts, one of the leading mechanisms for the development of depression is the lack of monoamines in the synaptic cleft - especially serotonin and dopamine. With the help of antidepressants, the concentration of these mediators in the synaptic cleft increases, because of this, their effects are enhanced.

It should be noted that there is a so-called "antidepressive threshold", which is individual for each patient. Below this threshold, there is no antidepressant effect and only non-specific effects appear: in particular, side effects, sedative and stimulant properties. Current data indicate that drugs that reduce monoamine reuptake require a 5- to 10-fold reduction in reuptake for antidepressant effects to occur. For the manifestation of the antidepressant effect of drugs that reduce the activity of MAO, it is necessary to reduce it by about 2 times.

However, current research shows that antidepressants also work through other mechanisms. For example, antidepressants are thought to reduce stress hyperreactivity of the hypothalamic-pituitary-adrenal system. Some antidepressants can also act as NMDA receptor antagonists, reducing the toxic effects of glutamate, which are undesirable in depression. Modern studies have shown that some antidepressants reduce the concentration of substance P in the central nervous system. However, to date, insufficient activity of monoamines is considered the most important mechanism for the development of depression, which is affected by all antidepressants.

Classification

The most convenient for practical use is the following classification of antidepressants:

  1. Drugs that block neuronal uptake of monoamines
    • Non-selective action, blocking the neuronal uptake of serotonin and norepinephrine (imizin, amitriptyline)
    • electoral action
      • Blocking neuronal uptake of serotonin (fluoxetine)
      • Blocking the neuronal reuptake of norepinephrine (maprotiline)
  2. Monoamine oxidase (MAO) inhibitors
    • Non-selective action, inhibit MAO-A and MAO-B (nialamide, transamine)
    • Selective action, inhibit MAO-A (moclobemide).
    • Noradrenergic and specific serotonergic antidepressants
    • Specific serotonergic antidepressants

However, there are other classifications of antidepressants. For example, it is proposed to classify antidepressants according to their clinical effect:

  1. Sedative antidepressants: trimipramine, doxepin, amitriptyline, mianserin, mirtazapine, trazodone, fluvoxamine
  2. Balanced antidepressants: maprotiline, tianeptine, milnacipran, sertalin, paroxetine, pyrazidol, clomipramine
  3. Stimulant antidepressants: imipramine, desipramine, citalopram, fluoxetine, moclobemide, ademethionine

Classes of antidepressants

Monoamine oxidase inhibitors

Non-selective inhibitors

Non-selective and irreversible monoamine oxidase inhibitors are first-generation antidepressants. These drugs irreversibly block both types of monoamine oxidase. These include derivatives of isonicotinic acid hydrazide (GINK), or the so-called "hydrazine" MAOIs - iproniazid (iprazide), isocarboxazid, nialamide, as well as amphetamine derivatives - tranylcypromine, pargyline. Most of the drugs from this group are not combined with a number of other drugs due to the inactivation of a number of liver enzymes and require a special diet to prevent the development of tyramine (“cheese”) syndrome.

Currently, non-selective MAO inhibitors are used quite rarely. This is due to their high toxicity.

Selective Inhibitors

Newer drugs in this class - selective MAO-A inhibitors (moclobemide, pirlindol, metralindol, befol) or MAO-B (selegiline) are used more widely, as they give significantly fewer side effects, are better tolerated and do not require a special diet. They are compatible with many drugs that non-selective MAOIs are not compatible with. However, selective MAOI-A and selective MAOI-B have significantly weaker antidepressant activity compared to non-selective MAOIs. Their antidepressant effect is somewhat weaker than that of tricyclic antidepressants.

Nonselective neuronal reuptake blockers of monoamines

Tricyclic antidepressants

Tricyclic antidepressants (TCAs), or tricyclics, are a group of highly effective antidepressants with much fewer side effects compared to MAOIs, do not require a special diet and do not impose great restrictions on the drugs used simultaneously. The reason these drugs are grouped together is that they have three rings linked together in the molecule, although the structure of these rings and the radicals attached to them can be very different.

Within the class of tricyclics, two subclasses are distinguished, differing in the features of the chemical structure - tricyclics, which are tertiary amines ( tertiary amine tricyclics), and tricyclics, which are secondary amines ( secondary amine tricyclics). Many of the tricyclics in the secondary amine subgroup are active metabolites of tertiary amines that are formed from them in the body. For example, desipramine is one of the active metabolites of imipramine, nortriptyline is one of the active metabolites of amitriptyline.

Tertiary amines

Tertiary amines, as a rule, are distinguished by stronger sedative and anti-anxiety activity than secondary amines, more pronounced side effects (M-anticholinergic, antihistamine, α-adrenergic blocking), stronger antidepressant activity and a more balanced effect on the reuptake of both norepinephrine and serotonin. Typical representatives of tertiary amines are amitriptyline, clomipramine (anafranil), imipramine (melipramine, tofranil), trimipramine (gerfonal), doxepin, dothiepin (dosulepin).

Doxepin is a representative of tertiary amines. Produced in the form of coated tablets.

Secondary amines

Selective norepinephrine reuptake inhibitors

Selective norepinephrine reuptake inhibitors (SNRIs) are a modern group of antidepressants with minimal side effects and good tolerability. A characteristic property of this group is a pronounced stimulating effect in the absence or low severity of a sedative effect. Famous representatives of this group are reboxetine (edronax), atomoxetine (straterra). According to some studies, these drugs are superior to selective serotonin reuptake inhibitors, at least in the treatment of severe depression.

Selective serotonin and norepinephrine reuptake inhibitors

Selective serotonin and norepinephrine reuptake inhibitors (SNRIs), or "dual acting" antidepressants ( double-action antidepressants) is a modern group of antidepressants with few or minimal side effects and good tolerability. The drugs of this group are powerful antidepressants, superior in antidepressant activity to selective serotonin reuptake inhibitors, and are close in strength to tricyclic antidepressants. These drugs are especially effective in treating severe depression. Well-known representatives of this group are venlafaxine (Velaxin, Efevelon), duloxetine (Cymbalta), Milnacipran (Ixel).

Selective norepinephrine and dopamine reuptake inhibitors

Selective norepinephrine and dopamine reuptake inhibitors (SNRIs) are a modern group of antidepressants with minimal side effects and good tolerability. The only representative of this class of antidepressants known today is bupropion (wellbutrin, zyban). Distinctive features of bupropion are the low probability of phase reversal into mania or hypomania and the low probability of provoking a "fast cycle" - less than that of SSRIs, and much less than that of TCAs or MAOIs and other powerful antidepressants. In this regard, bupropion is especially recommended for patients with bipolar depression who are prone to phase inversion or the development of a "fast cycle" in the treatment of various antidepressants. Important features of bupropion are also a pronounced general stimulating and psycho-energizing effect (so pronounced that a number of experts previously classified it not as an antidepressant, but as a psychostimulant, despite the absence of narcotic properties), as well as a disinhibitory effect on libido. Because of this, bupropion is often used to correct the sexual side effects of other antidepressants.

Monoamine receptor agonists

Noradrenergic and specific serotonergic antidepressants

Noradrenergic and specific serotonergic antidepressants (NaSSA) are a modern group of antidepressants with minimal side effects and good tolerability. They are called specific serotonergic drugs because, by blocking "inhibitory" presynaptic α 2 -adrenergic receptors and increasing the content of norepinephrine and serotonin in synapses, drugs of this group simultaneously strongly block postsynaptic serotonin 5-HT2 and 5-HT3 receptors responsible for the manifestation of a number of "serotonergic » side effects of SSRIs. These side effects include, in particular, a decrease in libido, anorgasmia, frigidity in women and inhibition of ejaculation in men, as well as insomnia, anxiety, nervousness, nausea, vomiting, decreased appetite and anorexia.

Well-known representatives of the HaCCA group are drugs similar in structure to mianserin (lerivon, bonserin) and mirtazapine (remeron, mirtazonal).

Specific serotonergic antidepressants

Specific serotonergic antidepressants (SSAs) are a group of antidepressants with relatively few side effects and good tolerability. Along with blocking serotonin reuptake and increasing serotonergic neurotransmission, drugs in this group strongly block 5-HT2 subtype serotonin receptors, which are “bad” in the context of the treatment of depression, which explains the low likelihood of sexual side effects, as well as the low likelihood of exacerbating anxiety, insomnia and nervousness compared to SSRIs. Often, on the contrary, there is an increase in libido and sexual disinhibition, an improvement in the quality and brightness of orgasm, in connection with which SSA are sometimes used as correctors for the sexual side effects of other antidepressants.

The drugs in this group include trazodone (tritico) and its newer derivative, nefazodone (serzon).

The antidepressant activity of these drugs is estimated as moderate. In severe depression, SSA is ineffective or insufficiently effective.

A specific feature of SSA, especially trazodone, is a strong normalizing effect on the phase structure of sleep and the ability to suppress nightmares by reducing the proportion of REM sleep, which is increased in depression and anxiety. This effect is realized even in small doses that do not have a noticeable antidepressant effect. Therefore, trazodone has become widely used and especially loved by psychiatrists in Western countries as a hypnotic and sedative for insomnia (not only depressive origin), as well as a corrector for insomnia and nightmares in the treatment of SSRIs or TCAs.

A specific feature of trazodone is also the ability to improve erectile function in men, up to causing priapism (painful spontaneous erections), which is not associated with antidepressant activity and is realized in any type of functional (non-organic) erectile dysfunction. Due to this property, trazodone is widely used for the treatment of impotence, erectile dysfunction, including those not associated with depression or anxiety.

Unfortunately, shortly after the start of its clinical use, nefazodone showed a rather significant (1%) hepatotoxicity (toxicity to the liver), in some cases leading to death, which forced the US FDA to first require mention of this in large letters in a black box at the beginning of the tab - annotations to the drug and informed consent of the patient for treatment with nefazodone, and then generally prohibit the production and distribution of nefazodone in the United States.

After that, the manufacturer of nefazodone announced the withdrawal of the drug from the pharmacy network in all countries and the termination of its production. Meanwhile, nefazodone, if it were not for liver toxicity, would be a very good expansion of the arsenal of antidepressants - unlike trazodone, it does not cause involuntary painful erections, has a significantly less sedative effect and better tolerability, almost does not lower blood pressure, and at the same time same time has a strong antidepressant activity.

Indications for the use of antidepressants

Antidepressants are a group of drugs used to treat depression. However, antidepressants are also used in clinical practice to correct other disorders. Among them are panic states, obsessive-compulsive disorders (SSRIs are used), enuresis (TCAs are used as an additional therapy), chronic pain syndromes (TCAs are used).

Action Features

Antidepressants are serious drugs that always require individual selection of a specific drug and dose, and therefore their self-administration without a doctor's prescription is not recommended.

Antidepressants are virtually incapable of improving mood in a healthy person, so their recreational use is unlikely or nearly impossible. The exceptions are MAOI, as well as coaxil, which was often used for recreational purposes, which led to its inclusion in the lists of PKU (subject-quantitative accounting).

Antidepressants don't work right away - it usually takes two to four weeks before they start working. Nevertheless, there is often an immediate effect, which can be explained by a sedative or, conversely, a stimulating effect.

Studies have shown that many antidepressants, in particular fluoxetine, can increase the likelihood of suicide in the first months of therapy, especially in children and adolescents. This is due to the rapidly onset stimulating, energizing effect that occurs before the onset of a true antidepressant effect. Therefore, a patient who is still at risk of suicide can thus receive enough energy and strength to realize suicidal thoughts against the background of still remaining bad mood and melancholy. In addition, many antidepressants can cause or exacerbate anxiety, insomnia or irritability, impulsivity at the beginning of therapy, which can also lead to an increased risk of suicide.

Taking antidepressants (not only SSRIs, but also SNRIs) can induce hypomania, mania, psychosis in both patients with bipolar affective disorder and in patients without it. For example, in one study, forty-three of 533 patients who took antidepressants developed mania.

Notes

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  9. Healy D. The three faces of the antidepressants: a critical commentary on the clinical-economic context of diagnosis // J. Nerv. Ment. Dis.. - 1999. - T. 187. - No. 3. - S. 174-80.
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  14. Krylov V.I. Antidepressants in general medical practice. Efficacy and safety of therapy. // Boytsov S.A., Okovity S.V., Kazantsev V.A. and etc. PHARMindex-Practician. - St. Petersburg: 2003. - V. 5. - S. 22-32. - ISBN 5-94403-011-9.
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  17. Vega, JA., Mortimer, A.M., Tyson, PJ. Conventional antipsychotic prescription in unipolar depression, I: An audit and recommendations for practice // Physicians Postgraduate Press, Memphis, TN, ETATS-UNIS (1978) (Revue) The Journal of clinical psychiatry. - 2003. - T. 64. - No. 5. - S. 568-574. - ISBN 0160-6689.
  18. Smulevich A.B., Dubnitskaya E.B., Tkhostov A.Sh. and etc. Depression and comorbid disorders. . - M.: 1997.
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There are many groups of drugs 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 effect of certain neurotransmitters on the state of the central nervous system, depending on the genesis of the disease. According to studies, a central deficiency of serotonin in synoptic transmission has a special effect on the pathogenesis of depression, by controlling which it is possible to regulate mental activity.

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

This group of medicines works by maintaining the prolonged activity of central serotonergic processes by preventing the capture of serotonin by brain tissues, as a result of which the mediator, accumulating in the receptor area, exerts its effect on them for a longer time.

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 tolerance of this group of drugs by the body, 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 nerve endings in the region of the reticular formation responsible for wakefulness, as well as the limbic system 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 those structures through which its initial release was made.

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

As a result of an increase in the activity of the neurotransmitter, the pathological processes of depressive and phobic disorders are leveled, the deficit of emotional behavior and the regulation of mental states are compensated.

Scope of application

The main purpose of the use of 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:

Also, this group of drugs is effective in the treatment of alcoholism and withdrawal symptoms.

Restrictions and contraindications

Taking SSRI antidepressants is prohibited in the presence of psychostimulant drugs in the blood, in a state of alcoholic or drug intoxication.

The combination of several drugs with a serotonergic effect is contraindicated. Also incompatible is the use of serotonin reuptake inhibitors in the presence of a history.

Hepatic and renal insufficiency, as well as cardiovascular diseases in the stage of decompensation, 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 be noted, develop up to insomnia or reversion to increased drowsiness.
  3. Increased nervous agitation, appearance, loss of visual acuity, the appearance of a skin rash are possible, a change in the phase of the disease is possible with the transition from depressive to manic.
  4. There may be an appearance, a decrease in libido, development in the form of, or acute. There is an increase in the production of prolactin.
  5. With prolonged use, a phenomenon such as loss of motivation with emotional dulling, which is also known as SSRI-induced apathetic syndrome, is possible.
  6. Bradycardia may develop, a decrease in the sodium content in the blood can be observed, 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 anomalies in late pregnancy.
  8. In rare cases, it is possible with the corresponding mental, autonomic and neuromuscular disorders.

Information 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 therapeutic effect makes it possible to provide the correct treatment to this group of patients, despite the atypical symptoms of depression of this age associated with neurobiological changes in adolescence.

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

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

TOP-10 popular drugs of the SSRI group

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;
  • Flunat;
  • Fluxonil;
  • Fludak.

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

  • Avoxin.

The drugs specifically inhibit the reuptake of serotonin and have an anxiolytic effect. They are used to prevent and treat obsessive-compulsive disorders. They also have an effect on adrenergic, histamine and dopamine receptors.

  • paroxetine;
  • Rexitin;
  • Serestill;
  • Pleased;
  • 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 apply to endogenous, neurotic and reactive depressions.

Preparations based on Sertraline:

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

The group minimally has 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 the start of taking 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 hallmark of these derivatives.

General treatment regimen

Preparations from the group of selective serotonin reuptake inhibitors are used once a day. It can be 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 a regression of the symptoms of depressive states, after the 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 organism, manifested in the absence of a positive result within 6-8 months, the group of antidepressants is replaced with another one. The dosage of the drug at one time depends on the derivative of the substance, as a rule, it ranges from 20 to 100 mg per day.

Once again about the warnings!

Antidepressants are contraindicated in renal and hepatic insufficiency, due to a violation of the elimination of drug metabolites from the body, resulting in its toxic poisoning.

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

In diseases that cause tremors, such as antidepressants, they can increase the negative clinic, which can negatively respond to the patient's condition.

Given the fact that inhibitors are teratogenic, they are not recommended for use during pregnancy and lactation.

It should be remembered that with severe physical exhaustion of the body, drugs of this group cannot be used because of the risk of even greater suppression of appetite.

It is also always worth remembering about the withdrawal syndrome, which is a complex of negative symptoms that develop with a sharp cessation of the course of treatment:

However, these drugs have their own drawbacks, manifested in the incomplete study of all their properties and the presence of individual, characteristic only for SSRIs, side effects.

The use of such drugs stimulates the human psyche. But what strong antidepressants to choose, below we will offer a list of drugs that you can drink without fear of side effects.

Antidepressants available to everyone

Without a doctor's prescription, you can only buy light pills that can also have a positive effect on mood. Here are the names of the medicine, the tablets of which can be bought on the free market. What are these products, and why you do not need a prescription to buy them.

When choosing the best antidepressant, pay attention to this tetracyclic drug. With its help, you can cheer up, eliminate apathy, anxiety, stabilize psychomotor retardation. Speaking about side effects, such a drug should not be taken during pregnancy, liver dysfunction, kidney disease.

Prozac (fluval, prodep, profluzac, fluoxetine)

These over-the-counter antidepressants belong to the group of selective serotonin inhibitors (SSRIs). Such names of the remedy are often used by a neurologist and therapist. The maximum effect of drugs is achieved in the treatment of menstrual disorders, elimination of anxiety and panic conditions, improves mood, can be used to get rid of obsessive thoughts. If you take such medicines regularly, you can find a balanced psyche and cheer up.

Paxil (sirestill, rexetin, plizil, adepress)

Taking antidepressants of the tricyclic group brings good effects, such drugs are often prescribed to drink in the doctor's office. You can take such drugs as an antidepressant and anti-anxiety agent. If we talk about side effects and consequences, then it does not affect the functioning of the heart and psychomotor functions. Can be taken to correct the work of the heart. It is recommended to drink in stressful situations, depression, various types of phobias.

Taking antidepressants of this type improves mood and performance. Such drugs contain St. John's wort, which has a good effect.

Choosing treatment with antidepressants, you can opt for Persen. The drug provides a high effect, contains natural ingredients (peppermint, valerian, lemon balm). Uplifts mood and fights stress.

The action of antidepressants of this type has a pronounced sedative effect. Such drugs contain passionflower, hops, guaifenesin, lemon balm, elderberry, St. John's wort and hawthorn. You can take medications when you need to relieve feelings of anxiety, tension, pain in the head, alleviate premenstrual and climatic syndromes.

herbal antidepressants

They may contain drugs, they have a good effect and almost no side effects. It is recommended to drink such funds when you need to cope with a depressive and anxious state that has appeared against the background of experiences and stress. We recommend taking the following natural preparations:

  • Infusions of immortelle, Rhodiola rosea, maral root, lemongrass - these remedies eliminate the feeling of overwork. Preparations should be drunk before meals, 150 grams each;
  • Alcoholic extract of leuzea - ​​such drugs stimulate the psychometric functions of a person, improve mood, increase efficiency;
  • Ginseng tincture is able to show an effect in the form of stimulation of the immune system. It treats manifestations of depression, increases the body's resistance to stress. As a side effect, increased sensitivity to the sun should be noted. It is not recommended to go to the solarium if you decide to drink ginseng tincture;
  • Zamaniha - can be used to increase efficiency, improves mood, normalizes sleep;
  • Motherwort, oregano, blue honeysuckle, meadow clover. Such remedies allow you to get rid of a depressive state;
  • Hawthorn produces a calming effect;
  • Hops, peppermint, valerian are excellent herbal antidepressants with no particular side effects;
  • Medicinal angelica copes well with insomnia;
  • You can drink calendula to relieve overwork and stress.

All these herbal medicines can be used exclusively for moderate and mild illness. They have an effect on sleep disorders, anxiety, anxiety.

Another indication for treatment with herbal remedies is various psycho-vegetative disorders. This is a number of conditions in which the pathology of internal organs is not detected during examinations, and the manifestations themselves are formed as a consequence of disruptions in the work of the nervous autonomic system. They include:

  • A recurring feeling of lack of air;
  • Pain in the head and dizziness;
  • Pain in the abdomen and heart;
  • Cardiopalmus;
  • Disorders of emptying and urination of the intestine.

St. John's wort-based antidepressants have practically no side effects, they can be used without a doctor's prescription. But in the case of more severe depressive conditions, such remedies will not bring an effective result. In such conditions, the help of the attending physician and the appointment of antidepressants of a different category are necessary.

Security measures

Many people have various mental disorders. Unfortunately, for people who are constantly in stressful situations, at work, at home and even on vacation, problems of sleep disturbance and irritability are familiar. Women usually at the first manifestations of depression try to drink medications without thinking about the consequences, men “kill their nerves”.

Do not shy away from the help of a psychiatrist. Such over-the-counter drugs may not help if there are factors that cause pathology. Only after its determination can you start taking medications. In other cases, the disease will develop into a chronic form with intervals of remissions and exacerbations.

Before you try to get a new generation of antidepressants in the public domain, think about the side effects. Can you tell a neurosis from a depressive state? It may be better to visit a professional doctor who can rule out the negative effects of drugs on your body. Even herbal preparations have a number of side effects if used incorrectly.

Medical statistics say that most modern people who buy a variety of sedatives do not suffer from mental problems. Such patients create within themselves a setting for depression and try to recover from a fictional state.

Selective serotonin reuptake inhibitors: TOP 10 best and complete list

There are many groups of drugs 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 effect of certain neurotransmitters on the state of the central nervous system, depending on the genesis of the disease. According to studies, a central deficiency of serotonin in synoptic transmission has a special effect on the pathogenesis of depression, by controlling which it is possible to regulate mental activity.

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

This group of medicines works by maintaining the prolonged activity of central serotonergic processes by preventing the capture of serotonin by brain tissues, as a result of which the mediator, accumulating in the receptor area, exerts its effect on them for a longer time.

The main advantage of SSRIs over other groups of antidepressants 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 tolerance of this group of drugs by the body, 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 nerve endings in the region of the reticular formation responsible for wakefulness, as well as the limbic system 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 those structures through which its initial release was made.

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

As a result of an increase in the activity of the neurotransmitter, the pathological processes of depressive, anxiety, anxiety-depressive and phobic disorders are leveled, the deficit of emotional behavior and the regulation of mental states are compensated.

Scope of application

The main purpose of the use of 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:

  • psychasthenic conditions, which are anxiety disorders of the personality;
  • psychopathy and neuroses, manifesting themselves in hysterical behavior and a decrease in mental and physical performance;
  • chronic pain syndromes associated with psychosomatic aspects;
  • panic disorder;
  • obsessive-compulsive disorders associated with episodic obsessive thoughts, ideas, actions, movements;
  • mental disorders of food consumption - anorexia nervosa, bulimia and psychogenic overeating;
  • social phobic experiences associated with the behavioral perception of oneself in society;
  • post-traumatic stress disorder;
  • disorders of depersonalization and derealization associated with a violation of self-perception and the inability to control one's behavior and accept the surrounding reality;
  • syndrome of premenstrual experiences, as a result of psycho-emotional instability.

Also, this group of drugs is effective in the treatment of alcoholism and withdrawal symptoms.

Restrictions and contraindications

Taking SSRI antidepressants is prohibited in the presence of psychostimulant drugs in the blood, in a state of alcoholic or drug intoxication.

The combination of several drugs with a serotonergic effect is contraindicated. Also incompatible is the use of serotonin reuptake inhibitors in the presence of a history of epilepsy.

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

The presence of foci of ischemic lesions or malignant tumor formations in the midbrain.

It is not practiced to use SSRIs earlier than two weeks after the end of the course of treatment with non-selective monoamine oxidase inhibitors.

It is forbidden to take drugs of the group in the presence of glaucoma in the active phase. Diabetes mellitus is also a contraindication to the use of SSRIs.

Selective serotonin reuptake inhibitors are incompatible with anticholinesterase agents, sympatholytics, heparin, indirect anticoagulants, narcotic analgesics, salicylates, cholinomimetics and phenylbutazone.

Side effects

When taking selective serotonin reuptake inhibitors, the following adverse reactions may occur (although much less frequently than, for example, when using tricyclic antidepressants):

  1. Nausea, vomiting, congestion in the intestines and, as a result, constipation.
  2. Restless states may be noted, mania, anxiety, sleep disturbance up to insomnia or reversion to increased drowsiness may develop.
  3. Possible increased nervous agitation, the appearance of a migraine-like headache, loss of visual acuity, the appearance of a skin rash, it is possible to change the phase of the disease in bipolar personality disorder with the transition from depressive to manic.
  4. There may be a tremor, a decrease in libido, the development of extrapyramidal disorders in the form of akathisia, parkinsonism, or acute dystonia. There is an increase in the production of prolactin.
  5. With prolonged use, a phenomenon such as loss of motivation with emotional dulling, which is also known as SSRI-induced apathetic syndrome, is possible.
  6. Bradycardia may develop, a decrease in the sodium content in the blood can be observed, 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 anomalies in late pregnancy.
  8. In rare cases, serotonin syndrome is possible with associated mental, autonomic and neuromuscular disorders.

Information 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 therapeutic effect makes it possible to provide the correct treatment to this group of patients, despite the atypical symptoms of depression of this age associated with neurobiological changes in adolescence.

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

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

TOP-10 popular drugs of the SSRI group

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

  1. fluoxetine. Along with an increase in serotonergic influence on the principle of negative feedback, it almost does not affect the accumulation of norepinephrine and dopamine. Slightly has an effect on cholinergic and histamine H1 receptors. When applied, it is well absorbed, the maximum dose in the blood from the moment of administration is noted after 6-8 hours. May cause drowsiness, loss of appetite, decreased libido, nausea and vomiting.
  2. fluvoxamine. It is an antidepressant with an anxiolytic effect. It is also characterized by a weak anticholinergic effect. The bioavailability of the drug is 50%. Already four hours after taking the medicine, the maximum therapeutic dose in the blood can be noted. In the liver, it is metabolized with the subsequent formation of the active substance norfluoxetine. Possible manic states, xerostomia, tachycardia, arthralgia.
  3. Sertraline. It is used in severe depressive states and is considered the most balanced drug of the group. The onset of action is noted 2-4 weeks after the start of therapy. When taken, hyperkinesis, edema, and also such a phenomenon as bronchospasm can be observed.
  4. Paroxetine. Anxiolytic and sedative effects prevail. Completely absorbed through the gastrointestinal tract, the maximum dose of the active substance is determined after 5 hours. The main application was found in panic and obsessive-compulsive states. Incompatible with MAO inhibitors. When taken with indirect coagulants, it increases bleeding.
  5. Citalopram. Together with serotonin, it blocks adrenoreceptors, histamine and m-cholinergic receptors. Within 2 hours after ingestion, the maximum concentration can be observed. Tremor, migraine, urinary disorders, and orthostatic hypotension are possible.
  6. Trazodone. Combines anxiolytic, sedative and thymonaleptic effects. An hour after administration, the maximum content in the blood is noted. It is used to suppress anxiety and neurotic endogenous depressions.
  7. Escitalopram. It is used in the pathology of behavior of mild and moderate severity. A feature of the drug is the lack of effect on liver cells, which allows you to combine Escitalopram with other drugs. Possible thrombocytopenia, anaphylactic shock, impaired production of vasopressin.
  8. Nefazodon. Used for sleep disorders, anxiety and depression of varying severity. Does not have a depressing effect on sexual function. May cause increased sweating, dry mouth, drowsiness.
  9. Paxil. Does not have a sedative effect. Used for mild depression. When applied, sinusitis, swelling of the face, aggravation of depressive conditions, changes in the quality of seminal fluid, and aggression are possible.
  10. Serenata. Providing an antidepressant effect, does not violate psychomotor functions. It is used as a prophylaxis of depressive episodes. May cause chest pain, tinnitus, headache, dyspepsia and shortness of breath.

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)

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

The drugs specifically inhibit the reuptake of serotonin and have an anxiolytic effect. They are used to prevent and treat obsessive-compulsive disorders. They also have an effect on adrenergic, histamine and dopamine receptors.

Medications based on 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 apply to endogenous, neurotic and reactive depressions.

Preparations based on Sertraline:

  • Aleval;
  • Asentra;
  • Zoloft;
  • Serlift;
  • Serenata;
  • Stimuloton;
  • Thorin.

This subgroup of drugs is used for obsessive-compulsive disorders. It does not have a sedative effect and does not affect other receptors besides serotonergic ones. It is used as a prevention of recurrence of depressive conditions.

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

Medicines based on Escitalopram:

Medicines are used in panic conditions. The maximum therapeutic effect develops 3 months after the start of taking 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 hallmark of these derivatives.

General treatment regimen

Preparations from the group of selective serotonin reuptake inhibitors are used once a day. It can be 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 a regression of the symptoms of depressive states, after the 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 organism, manifested in the absence of a positive result within 6-8 months, the group of antidepressants is replaced with another one. The dosage of the drug at one time depends on the derivative of the substance, as a rule, it ranges from 20 to 100 mg per day.

Once again about the warnings!

Antidepressants are contraindicated in renal and hepatic insufficiency, due to a violation of the elimination of drug metabolites from the body, resulting in its toxic poisoning.

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

In diseases that cause tremors, such as Parkinson's disease, antidepressants can increase the negative clinic, which can negatively respond to the patient's condition.

Given the fact that inhibitors are teratogenic, they are not recommended for use during pregnancy and lactation.

It is also always worth remembering about the withdrawal syndrome, which is a complex of negative symptoms that develop with a sharp cessation of the course of treatment:

These phenomena can occur in response to abrupt discontinuation of the drug. To prevent such situations, the dosage of drugs should be gradually reduced over a period of one month.

Selective serotonin inhibitors have found their wide application due to the absence of many adverse reactions associated with the use of other groups of antidepressants.

SSRI drugs are prescribed for varying degrees of severity of depressive disorders, with virtually no restrictions in the field of psychiatric practice.

However, these drugs have their own drawbacks, manifested in the incomplete study of all their properties and the presence of individual, characteristic only for SSRIs, side effects.

Tricyclic antidepressants: a list of drugs

At one time, the pharmaceutical market was filled with first-generation antidepressants - these are the so-called "Tricyclic antidepressants". These drugs are non-selective monoamine reuptake inhibitors (Norepinephrine, Dopamine, Serotonin - brain substances that elevate mood and cause emotions of joy, see brain biochemistry), which, due to numerous side effects, have given way to more modern drugs selective serotonin reuptake inhibitor (SSRI).

So, the list of drugs tricyclic antidepressants

The list of tricyclic antidepressant drugs includes several similar non-selective (non-selective) monoamine reuptake inhibitors (process delayers) (neurotransmitters: Norepinephrine, Dopamine, Serotonin - chemicals responsible for the transmission of impulses between neurons and maintaining a good mood ... in everyday life - “Hormones happiness").

The latter, with depression, anxiety, fears, are not developed to the proper extent, leading a person to a bad mood, severe depression, emotional and psychological suffering and mental disorders.

Tricyclic antidepressants - list of drugs:

Remember! tricyclic antidepressants, in addition to numerous side effects, do not cure the disease itself, do not remove the source - they only relieve the symptoms of the disease. This means that even if after taking tricyclic antidepressants your symptoms disappeared and remission occurred, then probably soon, if not immediately after stopping the drug , you will have the same condition, if not worse.

If you really want to get rid of depression, anxiety and fears forever, and learn how to independently resist these ailments in the future, without tricyclic antidepressants, then go through a full-fledged and really healing (removing the source of the disease) course of psychotherapy online

The use of antidepressants: a list of drugs

Antidepressants are used in the treatment of depression, a list of which can be seen below. Antidepressants are drugs that selectively affect a person's depressive state. These drugs and antipsychotics for depression can be used in the case of relief of affective-delusional syndromes in children and adults.

The most common mild antidepressants are:

This is only some of the antidepressants used to combat nervous disorders and depression. All of them are divided into several classifications.

soothing

Calming antidepressants - a classification of the most common drugs to combat depression.

Amitriptyline belongs to the classical type of mild tricyclic antidepressants. It is distinguished from Imipramine by a rather strong sedative effect. It is used to get rid of depressions of anxious and agitated types, which can manifest themselves with "vitality". This drug is available in the form of tablets and injections.

Another domestic antidepressant is Azafen, or Hypophysin. It is used to combat the symptoms of "minor" depressive disorders of the cyclothymic register. The drug has moderate sedative and thymoanaleptic effects.

Mianserin, or Lerivon, is a drug that, when used in small doses, has a strong sedative effect. Due to this effect, it can be used to treat cyclothymia in combination with insomnia. It is able to cure depression with large episodes.

Stimulants

Moclobemide, or Aurorix, is a selective MAO inhibitor. The drug has a powerful stimulating effect on people suffering from inhibited types of depression. It is prescribed for somatized types of depression. But the drug is strictly prohibited for use in anxiety depression.

Imipramine, or Melipramine, is the first fully studied tricyclic antidepressant. It is used in the treatment of severe depression with a high predominance of sadness and lethargy, with suicidal thoughts. The drug is produced both in the form of tablets and in the form of intramuscular injections.

Fluoxetine is a thymoanaleptic drug. Its second name is Prozac. The drug is effective in the treatment of depression with obsessive-phobic symptoms.

This type of drug belongs to the so-called selective serotonin reuptake inhibitors (SSRIs). The drug is devoid of some of the effects of clinical tricyclic antidepressants:

  • antihistamine;
  • adrenolytic;
  • anticholinergic.

Pertofran is a more powerful version of Imipramine (desmethylated). It has a brighter activating effect. The drug is used to combat depression, combined with depersonalization.

Preparations of a balanced effect

The second name of Pyrazidol is Pirlindol. The drug is produced in Russia. It is a reversible MAO type A inhibitor, like Moclobemide. This drug is used to prevent and treat depression of the inhibited type, as well as depressive disorders with pronounced anxiety manifestations. The advantages of the drug in the possibility of taking it for glaucoma, prostatitis and cardiac pathologies.

Another powerful drug created as a result of the synthesis and introduction of a chlorine atom into the imipramine molecule is Anafranil. It is used for the treatment of resistant-type depression and for the relief of the affective phases of severe depression.

Maprotiline, or Lyudiomil, is a tetracyclic antidepressant. It has a fairly powerful thymoanaleptic effect when interacting with anxiolytic and sedative components. It can be used in circular depression in combination with ideas of self-blame. The drug is used for involutional melancholia. Maprotiline is produced in the form of oral preparations and injections.

Reversible monoamine oxidase inhibitors and selective reuptake inhibitors

Befol refers to domestic drugs that are prescribed for depressive disorders of asthenic and anergic types. It is used to treat the depressive phase of cyclothymia.

Fevarin and Fluoxetine belong to the classification of thymoanaleptic drugs. The preparations have a vegetative-stabilizing effect.

Citalopram and Cipramil are other names for thymoanaleptic antidepressants that can be used to treat depression. They belong to the group of sedative serotonin reuptake inhibitors (SSRIs).

Afobazole is an over-the-counter antidepressant. It is used to combat somatic diseases with adjustment disorders, anxiety, neurasthenia, and oncological and dermatological diseases.

The drug has a good effect in the treatment of sleep disorders and the removal of symptoms of PMS. But it should be borne in mind that taking it to children and women during pregnancy and lactation is contraindicated.

Tricyclic

Trimipramine, or Gerfonal, is used in the treatment of depression with increased anxiety. This is one of the most powerful drugs of its kind. Its psychotropic activity is similar to Amitriptyline. When conducting treatment, it is worth considering the list of contraindications for this antidepressant:

  • dry mouth;
  • orthostatic hypotension;
  • problems with urination.

Next generation antidepressants

Sertraline and Zoloft are the names of antidepressants with a strong thymoanaleptic effect with a weak stimulating effect. At the same time, the drugs do not have anticholinergic and cardiotoxic properties.

They achieve the maximum effect in the fight against somatized atypical depressions with some manifestations of bulimia.

Paroxetine is a derivative of piperidine. It has a fairly complex bicyclic structure. The main properties of Paroxetine are thymoanaleptic and anxiolytic. They appear in the presence of stimulation.

The drug shows itself well in the fight against endogenous and neurotic depressions, their dreary or inhibited variants.

Venlafaxine is an antidepressant used for depression associated with severe mental disorders such as schizophrenia, etc.

Opipramol is used to treat somatic and alcoholic depression. It is able to prevent vomiting, convulsions and generally stabilize the autonomic nervous system.

Toloxatone, or Humoril, is similar in how it affects the human body with Moclobemide. The drug has no anticholinergic and cardiotoxic properties. But he copes well with the treatment of depression with pronounced lethargy.

Cymbalta or Duloxetine are used to fight depression with panic attacks.

Side effects

Most antidepressants have their fair share of side effects. Their list is quite large:

  • hypotension;
  • arrhythmia;
  • sinus tachycardia;
  • violation of intracardiac conduction;
  • oppression of bone marrow functions;
  • agranulocytosis;
  • thrombocytopenia;
  • hemolytic anemia;
  • dry mucous membranes;
  • disturbance of accommodation;
  • intestinal hypotension;
  • problems with urination;
  • increased appetite;
  • weight gain.

Such side effects due to the use of the tricyclic type of antidepressants occur quite often. In contrast, serotonin reuptake inhibitor antidepressants have less side effects. But these may be:

  • frequent headaches;
  • insomnia;
  • anxiety states;
  • depotent effects.

If combination therapy is used for treatment, that is, drugs of both types are used simultaneously, then serotonin syndrome may occur, characterized by fever, signs of intoxication of the body and disorders in the work of the heart and blood vessels.

Any antidepressants for depression should be taken only after a complete medical examination and an accurate and complete diagnosis.

And for children, they are prescribed with extreme caution. Be sure to do this under the supervision of a doctor so as not to harm the body.

Antidepressants without a doctor's prescription: names, prices, list

Recently, the number of people suffering from depression has increased significantly. This is largely facilitated by the frantic rhythm of modern life, the 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 are reflected in their performance and social relationships. They turn to a doctor for advice, and often he diagnoses them with depression.

What is depression and why is it dangerous?

First of all, it should be noted that one should not be afraid of this diagnosis. The disease does not indicate that the person suffering from it is mentally or mentally handicapped. 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 roll over 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 its 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 not actually the result of a person's weak will, his insufficient efforts to correct the situation. In most cases, it is a biochemical disease caused by a metabolic disorder 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 is not always possible to cure non-drug means. It is well known that a change of scenery, relaxation techniques and auto-training, etc., can help a person with a depressed mood. but all these methods require considerable effort on the part of the patient, his will, desire and energy. And with depression, they just don’t exist. It turns out a vicious circle. And it is often impossible to break it without the help of drugs that change the 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 what kind of clinical effect the drugs have on the nervous system. In total, three types of such actions are distinguished:

  • Sedative
  • Balanced
  • Activating

Sedative antidepressants have a calming effect on the psyche, relieving anxiety and at the same time increasing the activity of nervous processes. Activating drugs fight well with 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 the intake.

Classification of antidepressants according to 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 of the group allows us to consider them a benchmark for antidepressants.

Tricyclic drugs are able to 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

Amitriptyline

Tricyclic antidepressant. It has both antidepressant and mild analgesic effects

Composition: 10 or 25 mg amitriptyline hydrochloride

Dosage form: dragee or tablets

Indications: depression, sleep disorders, behavioral disorders, mixed emotional disorders, chronic pain syndrome, migraine, enuresis.

Side effects: agitation, hallucinations, visual disturbances, tachycardia, pressure fluctuations, tachycardia, indigestion

Contraindications: heart attack, individual intolerance, lactation, intoxication with alcohol and psychotropic drugs, conduction disorders of the heart muscle.

Application: immediately after meals. The initial dose is mg at night. Gradually, the daily dose increases to 200 mg in three divided 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 number 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 they have a large number of side effects. These include:

  • hypotension
  • hallucinations
  • Insomnia
  • Agitation
  • constipation
  • Headache
  • Dizziness
  • sexual dysfunction
  • visual impairment

When taking certain drugs, you should also follow a special diet to avoid the ingestion of potentially dangerous enzymes that are metabolized with the help of MAO.

The most modern antidepressants of this class have the ability to inhibit only one of two types of the 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.

The main selective MAO inhibitors:

  • Moclobemide
  • Pirlindol (pyrazidol)
  • befol
  • Metralindol
  • Garmalin
  • Selegiline
  • Rasagiline

Moclobemide

Antidepressant, selective MAO inhibitor. It acts mainly on MAO type A, has an antidepressant and immunostimulating effect.

Indications: schizophrenia, social phobia, manic-depressive psychosis, alcoholism, reactive, senile, neurotic depression

Contraindications: exacerbation of mental illness, agitation, confusion, agitation, pregnancy and lactation.

Side effects: headaches, dizziness, upset stomach and intestines

Application: after meals. The daily dosage is mg, three doses per day. The dosage is gradually increased.

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 so dangerous as compared to other groups of drugs. The main indication for drug treatment is major depressive disorder.

Photo: Sherry Yates Young/Shutterstock.com

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 that transmits the nerve impulse, but is transferred to another cell. Thus, antidepressants such as SSRIs increase the activity of serotonin in the neural circuit, which has a beneficial effect on brain cells affected by depression.

As a rule, drugs of this group are especially effective in severe depression. In depressive disorders of minor and moderate severity, the effect of drugs is not so noticeable. However, a number of doctors have a different opinion, which is that in 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

fluoxetine

Antidepressant, selective serotonin reuptake inhibitor. Has an antidepressant effect, relieves feelings of depression

Release form: 10 mg tablets

Indications: depression of various origins, obsessive-compulsive disorder, bulimia nervosa

Contraindications: epilepsy, convulsive tendencies, severe renal or hepatic insufficiency, glaucoma, adenoma, suicidal tendencies, taking MAO inhibitors

Side effects: hyperhidrosis, chills, serotonin intoxication, indigestion

Application: regardless of the meal. The usual scheme is once a day, in the morning, 20 mg. 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 these 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. 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 disorders.

Contraindications: allergy to components, age up to 18 years, simultaneous use with MAO inhibitors, anorexia nervosa, convulsive disorders.

Side effects: an overdose of the drug is extremely dangerous, which can cause epileptic seizures (2% of patients at a dose of 600 mg). Urticaria, anorexia or lack of appetite, tremor, tachycardia are also observed.

Application: the medicine should be taken once a day, in the morning. The typical dose is 150 mg, with a maximum daily dose of 300 mg.

Next generation antidepressants

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

  • Sertraline
  • fluoxetine
  • fluvoxamine
  • Mirtazalin
  • Escitalopram

The difference between antidepressants and tranquilizers

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

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

Tranquilizers, as a rule, are fast-acting drugs. They can be used to fight depression, but mostly as ancillary drugs. The essence of their impact on the human psyche is not in the correction of his emotional background in the long term, as in drugs for depression, but in the suppression of manifestations of negative emotions. They can be used as a means to reduce fear, anxiety, agitation, panic attacks, etc. Thus, they are more of an anti-anxiety and sedative than an antidepressant. In addition, during the course of treatment, most tranquilizers, especially diazepine drugs, are addictive and addictive.

Can you buy antidepressants without a prescription?

According to the current rules for dispensing 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 bought without prescriptions. In practice, of course, pharmacists can sometimes turn a blind eye to the rules in 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 situation will be the same in another.

You can buy without a doctor's prescription only drugs for the treatment of mild depressive disorders such as Afobazol, "daytime" tranquilizers and herbal preparations. But in most cases, it is difficult to attribute them to real antidepressants. It would be more correct to classify them as sedative drugs.

Afobazole

Russian-made anti-anxiety, anxiolytic and mild antidepressant without side effects. OTC drug.

Release form: 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 can be allergic reactions, disorders of the gastrointestinal tract, headaches.

Application: It is advisable to take the drug after meals. A single dose is 10 mg, daily - 30 mg. The course of treatment is 2-4 weeks.

Contraindications: hypersensitivity to the components of the tablets, age up to 18 years, pregnancy and lactation

Why is self-treatment of depression dangerous?

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

Almost all depression medications, even the mildest and safest, can cause side effects. And strong drugs without side effects simply do not exist. Especially dangerous is prolonged uncontrolled use of drugs or excess dosage. In this case, intoxication of the body with serotonin (serotonin syndrome) can occur, which can lead to death.

How to get a prescription for the drug?

If you think that you have depression, it is recommended to consult a psychotherapist or neurologist. Only he can carefully examine your symptoms and prescribe the appropriate remedy for your case.

Herbal remedies for depression

The most popular herbal preparations for raising the mood today contain extracts of mint, chamomile, valerian, motherwort. But preparations containing St. John's wort showed the greatest effectiveness in depression.

The mechanism of the therapeutic action of St. John's wort has not yet been clearly elucidated, but scientists believe that the enzyme hypericin contained in it is able to accelerate 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.

Photo: Ron Rowan Photography/Shutterstock.com

Hypericum preparations are mild antidepressants. They will not help with any depression, especially with its severe forms. However, the effectiveness of St. John's wort in mild to moderate depression has been proven by serious clinical studies, in which it proved to be no worse, and in some respects even better than the 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 the age of 12. Among the negative effects of taking St.

St. John's wort-based medicines are sold without a prescription. So if you're looking for over-the-counter depression remedies, this class of drugs may be your best bet.

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 administration, poured into 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, urticaria, increased allergic reactions, gastrointestinal disorders, headaches, iron deficiency anemia.

Application: three times a day is taken in a capsule of Negrustin or 1 ml of solution. Children under 16 are prescribed 1-2 capsules per day. The maximum daily dose is 6 capsules or 6 ml of solution.