monoamine oxidase inhibitors. MAO inhibitors list of medicines trade names MAO drugs

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MAO inhibitors are antidepressants that are prescribed for the treatment of parkinsonism, as well as epilepsy.

pharmachologic effect

Preparations of MAO inhibitors are divided into the following groups: non-selective reversible, selective irreversible and reversible selective. The latter have antidepressant and psycho-energizing properties. They serve to suppress the deamination of serotonin and norepinephrine.

Non-selective irreversible drugs are designed to reduce seizures, as well as improve the condition of patients in the deep. These drugs are similar in structure to iproniazids.

Irreversible selective MAO inhibitors have antiparkinsonian properties and are involved in the metabolism of dopamine and catecholamines.

Video: Brain Biochemistry

List of drugs

Non-selective irreversible drugs include: Nialamide, Iproniazid, Phenelzine, Isocarboxazid, Tranylcypromine.

Selective irreversible drugs include the drug Selegiline.

The list of MAO inhibitors (reversible selective) includes the following medicines: Befol, Metralindol, Moclobemide, Pirlindol, beta-carboline derivatives.

Indications for use

Preparations of MAO inhibitors (reversible selective) should be taken for depression of a different nature, with melancholic syndrome, depressive syndrome, astheno-dynamic disorders. Non-selective irreversible drugs should be prescribed to patients with neurotic, cyclothymic, involutional depressions. Taking pharmaceuticals is also indicated in the treatment of chronic.

Irreversible selective drugs should be prescribed in the treatment of Parkinson's disease.

Contraindications

Reception of MAO inhibitors (reversible selective) is contraindicated in patients who have:

• Hypersensitivity to the drug;
• Acute inflammatory diseases of the liver or kidneys have been identified.

Drugs are not prescribed for alcohol withdrawal syndrome. It is strictly forbidden to take medicines during pregnancy and lactation.

You should not take drugs (non-selective irreversible) in the following cases:

• If the patient has hypersensitivity;
• Revealed liver failure;
• There is a violation of cerebral circulation;
• A diagnosis of chronic heart failure was made.

The intake of MAO inhibitors (irreversible selective) is strictly contraindicated in patients who are taking other antidepressants. Also, drugs in this category are not prescribed during pregnancy and during lactation, with Huntington's Chorea, essential tremor.

With caution, drugs (irreversible selective) should be taken by patients who have: severe angina, progressive, severe psychosis, prostatic hyperplasia, angle-closure, large-scale tremor, peptic ulcer of the gastrointestinal tract, tardive dyskinesia, diffuse toxic goiter, and pheochromocytoma.

Side effects

When using reversible selective drugs, the patient may experience the following body reactions: insomnia, headache (of a periodic nature), dry mouth, anxiety.

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When using non-selective irreversible drugs, a person may experience: lower blood pressure, anxiety, insomnia, headache,.

When using irreversible selective MAO inhibitors, the following body reactions may occur:

• Raise blood pressure, arrhythmia, hypotension;
• In some cases, the patient's appetite decreases, the mucous membrane of the eye becomes dry, and transaminase activity increases;
• In addition, constipation, nausea may occur;
• A small percentage of people experience urinary retention, painful urge to urinate;
• When taking drugs, shortness of breath, skin rash, bronchospasm may appear.

When taking drugs (irreversible selective), a person may begin the process of hair loss, hypoglycemia may form.

Most cells, including those in nerve endings. It participates to a small extent in the elimination of blood catecholamines, but performs an important function in regulating the content of catecholamines in sympathetic endings.

Monoamine oxidase (MAO) is an oxidoreductase that deaminates monoamines. It is found in many tissues, but in the highest concentrations - in the liver, stomach, kidneys.

At least two MAO isoenzymes have been described: MAO-A of the nervous tissue, which deaminates serotonin, adrenaline and norepinephrine, and MAO-B of other (non-nervous) tissues, which is most active in relation to 2-phenylethylamine and benzylamine. Dopamine and tyramine are metabolized by both forms. The question of the relationship between affective disorders and an increase or decrease in the activity of these isoenzymes is being intensively studied. MAO inhibitors have found use in the treatment of hypertension and depression, but the ability of these compounds to enter into dangerous reactions with sympathomimetic amines contained in food and drugs reduces their value.

O-Methoxylated derivatives undergo further modification by forming conjugates with glucuronic or sulfuric acid.

Monoamine oxidase plays a central role in regulating the metabolism of biogenic amines, many of which perform neurotransmitter functions in living organisms. The study of the properties of monoamine oxidase for more than 60 years has led to the creation of antidepressant drugs - "monoamine oxidase inhibitors", the third generation of which is widely used in medicine.

The first information about the existence in the liver tissue of a cyanide-resistant enzyme catalyzing the oxidation of tyramine was obtained by M. Hare in 1928. The classical experiments of M. Hare were independently confirmed and further developed "in addition to" tyramine oxidase "," adrenaline oxidase "was discovered" , "histaminase", "deaminase of aliphatic amines". In 1938, E. Zeller summarized the experience of studying amine oxidases and formulated the concept of "monoamine oxidase" (catalyses the oxidative deamination of tyramine, adrenaline, aliphatic monoamines) and "diaminoxidase" (catalyses oxidative deamination of histamine and aliphatic diamines).

In the early 50s, E. Zeller discovered specific monoamine oxidase inhibitors, and in the early 60s, V.Z. Gorkin and independently I. Knoll drew attention to the fact that some monoamine oxidase inhibitors have the ability to selectively block oxidative telny deamination of certain monoamines. In 1968, T. Johnston formulated the concept of two types of monoamine oxidases, differing in their sensitivity to the action of low (on the order of 0.1 µM) concentrations of chlorhyline. Type A includes monoamine oxidases blocked by low concentrations of chlorhyline. Monoamine oxidases that are resistant to the inhibitory action of low concentrations of chlorhyline are classified as type B. A few years later, I. Knoll synthesized a selective inhibitor of type B monoamine oxidase, deprenyl. At the same time, differences in the substrate specificity of both types of monoamine oxidases were described.

The pharmacological classification of monoamine oxidases into types A and B has given rise to many ideas and hypotheses about the nature of enzymes. Whether monoamine oxidases A and B, which are often present in the same organ, represent two different proteins, or whether differences in substrate specificity and inhibitory selectivity are due to the presence of two active centers on one protein molecule and/or different components of the (phospho)lipid environment of one enzyme?

In the mid-70s, V.Z. Gorkin and his colleagues discovered that partial oxidation of sulfhydryl groups of monoamine oxidase type A (but not B) is accompanied by a change in substrate specificity (“transformation” of catalytic properties) and the appearance of qualitatively new reactions of deamination of nitrogen-containing compounds, which usually are substrates of diamine oxidases, and even nitrogen-containing compounds that do not belong to the number of substrates of amine oxidases at all (glucosamine, gamma-aminobutyric acid, etc.).

In the 1980s, monoclonal antibodies were obtained for monoamine oxidases of types A and B, highly specific for each type of enzyme. Peptide maps obtained from proteinase cleavage products of purified type A and B monoamine oxidases indicated different amino acid sequences of the enzymes.

By the beginning of the 1990s, it was possible to obtain cDNAs corresponding to monoamine oxidases types A and B from human liver, on the basis of which the primary structure of these various proteins was established. It was shown that the biosynthesis of types A and B monoamine oxidases is encoded by similar but not identical genes with different promoter organization. In humans, these genes are located on the X chromosome.

Monoamine oxidase, an integral protein of the outer membrane of mitochondria, catalyzes the reaction of oxidative deamination.

R-CH -NH + O + H O L R-CHO + NH + HO where R are aromatic or aliphatic radicals. Secondary and tertiary amines containing methyl groups as substituents are also substrates for monoamine oxidase. Optimum pH 7.0-7.4. The kinetic mechanism can be described by two half-reactions. Initially, the oxidation of the amine leads to the formation of aldehyde, NH, and the reduced form of the enzyme"

E + R-CH -NH + H O L EH + R-CHO + NH In this partial reaction, an imine is formed as an intermediate, which then reacts with water to form ammonia and an aldehyde"

R-CH -NH L R-CH=NH + (2H)

R-CH=NH + H O L RCHO + NH The reduced enzyme is then oxidized to form hydrogen peroxide"

EH + O L E + HO This half-reaction is rate-limiting.

Kinetic studies, carried out mainly on type B monoamine oxidases, showed that in experiments with phenylethylamine as a substrate, the reaction proceeds according to the "ping-pong" mechanism, with oxygen reacting with the free reduced form of the enzyme. If the substrate is benzylamine, then a ternary complex is formed: reduced enzyme - reaction product (ammonia) - oxygen.

Molecules of both type A and type B monoamine oxidases are dimers built from two identical subunits, the number of amino acid residues and molecules. the mass of which have minor species differences. The monoamine oxidase type A subunit from human and rat liver consists of 527 amino acid residues and has a mole. mass 59.7 kDa. The sub'unit of the human or rat liver monoamine oxidase type B molecule consists of 520 amino acid residues and has a molecule. mass 58.8 kDa. Molek. the mass of a subunit of monoamine oxidase type A from human placenta is 65 kDa, and that of monoamine oxidase type B from bovine liver is 57 kDa.

Each of the subunits of type A or B monoamine oxidase, according to T. Singer, contains a covalently bound FAD (8-alpha-cysteinyl-FAD), and the amino acid sequence of the flavin-binding sites is identical for both enzymes and includes the pentapeptide Ser-Gly -GlyCys-Tyr (Fig. 1.25). The domain containing the cysteine ​​residue with which the covalent bond is carried out is located in the region of the C-terminus. In monoamine oxidases of type A, the cysteine ​​residue involved in the formation of a thioether bond occupies position 406, and in monoamine oxidases of type B, it occupies position 397. This region, which is directly involved in the interaction of apoenzyme with flavin, is present in the molecules of all studied so far (regardless of organ from which the purified enzyme preparations were isolated, and their specific features) monoamine oxidases. In this region, the homology of amino acid residues reaches 90%, while the homology of the sequence of amino acid residues not only of the specified domain, but of the entire polypeptide chain for monoamine oxidases of types A and B of one species is 70%.

There are 3 domains in the monoamine oxidase molecule, within which the sequence homology of amino acid residues reaches 90%, one domain is involved in the interaction with the flavin component, the other is localized in the region of the N-terminus of the polypeptide chain and includes the ADP region. This domain was also found in the molecules of other studied flavin enzymes. The study of type A monoamine oxidases shows that this region is located between amino acid residues from 15 to 45. Finally, the third domain occupies the region from 187 to 230 amino acid residues.

The biosynthesis of monoamine oxidases is carried out in the fraction of free (non-membrane-bound) polysomes of cells, such as the liver. The molecules synthesized in the fraction of cytoplasmic polysomes are not subjected to processing associated with the action of proteinases, but are transported in an energy-dependent way to the outer membranes of mitochondria. According to R. McCauley (Fig. 1.26), incorporation of types A and B monoamine oxidases into the membrane requires the presence of a ubiquitin (UB) polypeptide consisting of 76 amino acid residues, as well as ATP. For monoamine oxidase type B, it was shown that the 29 C-terminal amino acid residues act as a signal peptide when incorporated into the membrane. The catalytically complete conformation of the membrane-bound form of monoamine oxidases is formed during membrane binding, and this process precedes ATP and UB-dependent incorporation of the enzyme into the membrane (see Fig. 1.26). It should be noted that the synthesis of wu thmg monoamine oxidases of types A and B, as assessed by quantitative autoradiography, occurs faster in peripheral organs and tissues than in the brain; their half-life is 4.5 and 13 days, respectively.

The functioning of monoamine oxidases in mitochondria is significantly affected by the features of the membrane microenvironment. At the same time, the content of sialic acid residues in membrane glycolipids, as well as the state and composition of phospholipids, are of great importance. Treatment of mitochondria with neuraminidase or phospholipases reduces the activity of membrane-bound monoamine oxidases. Incubation of liver mitochondria with lipoxygenase leads to rapid inactivation of type B monoamine oxidases and, in particular, type A, with the simultaneous appearance of diamine oxidase activity, which was absent in the control. Interpreting this phenomenon as a consequence of modifying the properties of mitochondrial monoamine oxidases, it was suggested that it may be due to changes in the phospholipid environment of monoamine oxidases in membranes.

Post-translational modifications of the catalytic properties of their molecules are of great biological importance for the functioning of monoamine oxidases in the cell. Thus, contact (20 hours, 5) of a purified preparation of monoamine oxidase type B from human blood platelets with purified preparations of monoamine oxidase type A from the human placenta is sufficient to induce changes in the conformation of catalytic centers in the molecules of monoamine oxidases, as a result of which the sub - stratum specificity and sensitivity to the inhibitory action of chlorhyline and deprenyl in the direction of approaching their values ​​to the characteristics characteristic of type A monoamine oxidases. At the same time, the immunochemical characteristic of the enzyme from platelets did not change.

Monoamine oxidases are widely distributed in nature. They are found in almost all organs of humans and animals. For preparations of type A monoamine oxidases, the human placenta is usually used; Type B monoamine oxidase preparations are often sourced from human platelets. It is generally accepted that human placenta and platelets contain only one type of enzyme (A or B). Using 3H-pargyline, which specifically blocks the catalytic centers of monoamine oxidases, it has been shown that the content of type A monoamine oxidases in the human placenta is 3.9 pmol/mg, and that of type B in human platelet membranes is 5.7 pmol/mg protein, the total content of monoamine oxidases of both types in the cortex and caudate nucleus of the human brain does not exceed 1.6–2 pmol/mg of protein. Immunochemical methods have shown that circulating blood platelets contain 0.33 µg of type B monoamine oxidase per 10 platelets, which corresponds to 16,500 enzyme molecules per 1 platelet.

The problem of the physiological regulation of monoamine oxidases attracts the attention of researchers, mainly in connection with the involvement of these enzymes in maintaining the normal functional state of the central nervous system. The delta-sleep-inducing peptide, when administered parenterally, stimulates the activity of rat brain monoamine oxidases. The rat brain peptide neurocatin selectively inhibits the activity of type A monoamine oxidases. An important regulator of the activity of monoamine oxidases is tribulin (the name of the fraction of endogenous enzyme inhibitors, a significant increase in which in tissues and biological fluids of humans and animals is found when various types stress); The quantitatively predominant component of this fraction isatin (2,3-dioxoindole) selectively inhibits the activity of type B monoamine oxidase.

The biological function of monoamine oxidases has traditionally been reduced to protecting the body from the toxic effects of exogenous or biogenic amines formed in organs and tissues by their inactivation. Monoamine oxidases are involved in the regulation of the intraneuronal concentration of biogenic amines and, indirectly, in the regulation of melatonin biosynthesis and adenylate cyclase activity. However, along with the performance of these functions, monoamine oxidases also catalyze the formation of substances with their own biological activity. Thus, monoamine oxidase type B carries out oxidative bioactivation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine to 1-methyl-4-phenylpyridinium neurotoxin, which selectively affects dopaminergic neurons and causes parkinsonism in primates and human. The dealkylation of 2-n-pentylacetamide (milacetamide) catalyzed by brain monoamine oxidases leads to the formation of pentoic acid, hydrogen peroxide and glycinamide; the latter breaks down into ammonia and the inhibitory neurotransmitter glycine. Monoamine oxidase is one of the main intracellular generators of hydrogen peroxide and is involved in the regulation of the latter-dependent release of Ca2+ ions from brain mitochondria. It is believed that monoamine oxidase thyroid gland provide the formation of hydrogen peroxide, necessary for the iodination of tyrosine molecules and, ultimately, for the biosynthesis of iodothyronines.

Under pathological conditions, the following main changes in the properties of monoamine oxidases are possible: 1) partial or (much less often) complete inhibition of catalytic activity; 2) stimulation of catalytic activity; 3) partial solubilization of membrane-bound and/or impaired incorporation of soluble monoamine oxidases; 4) a qualitative change in the substrate specificity ("transformation" of the catalytic properties) of type A monoamine oxidases; 5) a combination of these phenomena.

Selective inhibitors of monoamine oxidases are used to treat a number of neuropsychiatric diseases. Type A monoamine oxidase inhibitors - antidepressants - are used to treat depressive conditions, and type B monoamine oxidase inhibitors (mainly deprenyl) are used in the treatment of parkinsonism.

Monoamine oxidase inhibitors (MAO) are biological substances that, by reducing the rate of chemical reactions of the monoamine oxidase enzyme, prevent the destruction of various monoamines (this group includes serotonin, norepinephrine, dopamine, phenylethylamine, tryptamine and octamine). This enhances the concentration of the active element between two neurons or between a neuron and an effector molecule (a particle that binds to proteins to increase biological activity).

For medical purposes, MAOIs are used as antidepressants, and sometimes to treat Parkinson's disease and narcolepsy attacks - a pathological condition. nervous system, which causes drowsiness and a sudden "attack" of sleep.

According to their pharmacological properties, MAOIs are divided into:

• non-selective irreversible;
• reversible selective;
• irreversible selective.

So, let's take a brief look at each group and learn about the active ingredients, properties and trade names.

Non-selective irreversible MAOIs - inhibit MAO-A and MAO-B

Table 1

Reversible selective MAO-A inhibitors

table 2

Irreversible selective MAO-B

Table 3

Surely each of us has been exposed. Due to abrupt life changes, the human body, as it were, develops "mental immunity", thereby increasing its regenerative abilities. Thus, before using psychotropic drugs (monoamine oxidase inhibitors), you should find out whether they are really essential to survive depression or stress.

This group of short-acting drugs is divided into two groups:

1. selective, blocking MAO type A;
2. non-selective, blocking MAO type A and type B.

Group 2 - non-selective

Indopan (alphamethyltryptamine). A domestic drug that, in terms of pharmacological actions, is similar to tryptamine and phenamine.
In addition to short-term reversible inhibition of MAO, it has a stimulating effect on the central and peripheral adrenoreactive systems. Therefore, it is sometimes referred to as psychostimulants.

It has a less stimulating effect than others (such as nu-redal), also has a thymoanaleptic effect. Target Syndromes:

1. astheno-depressive;
2. astheno-hypochondriac;
3. astheno-anergic;
4. apato-abulic;
5. different in genesis of depression with lethargy.

Assign in the first half of the day from 5-10 mg / day to 60 mg / day. Duration - several months.
Well tolerated. In case of overdose - agitation, hypomania, insomnia, exacerbation of productive symptoms, hypertensive phenomena and allergic reactions.
The rest is compliance with the rules for prescribing all MAO inhibitors.

Inkazan (Metralindol). Original domestic drug. Tetracycline derivative of carboline.
The effect is associated with pyrazidol: it inhibits the reuptake of serotonin and norepinephrine, reversibly undifferentiated blocks MAO, does not have an anticholinergic effect.
It has a thymoanaleptic and stimulating effect. Inferior to pyrazidol, but has a vegetative-stabilizing effect.
"Small antidepressant".
Indications:

1. asthenic anergic depression on an outpatient basis;
2. asthenodepressive conditions in patients with alcoholism in remission. First, there is a stimulating effect.

Dosage from 25-30 mg / day to 400 mg / day.
Well tolerated. Sometimes causes dyspepsia, fluctuations in blood pressure, bradycardia. Contraindications:

1. acute alcohol withdrawal;
2. together with other MAO inhibitors.

Caroxazone (thymostenil, surodil). Bicyclic derivative of benzoxaline.
"Small antidepressant" balanced action.
Indications:

1. cyclothymia with asthenovegetative symptoms;
2. chronic neuroleptic parkinsonism;
3. prolonged neuroleptic depression. TU2 = 24 hours, dosage 400-1200 mg / day. Well tolerated.

In case of overdose - dyspepsia, fluctuations in blood pressure, sleep disturbances.

Group 1 - electoral

pyrazidol. It blocks the reuptake of norepinephrine and serotonin and reversibly blocks MAO type A. It does not have an anticholinergic effect, but enhances the effects of sympathomimetic amines.

It has a thymoanaleptic effect (weaker than melipramine and amitriptyline), but is a balanced antidepressant, that is, with inhibited depression it has a stimulating effect, and with anxiety it has a sedative effect.
Indications:

1. depression of various origins, including alcoholic depression;
2. somatized depression, as it has a pronounced vegetative-stabilizing effect.

It goes well with neuroleptics in the treatment of apatoabulic syndrome, combined with tranquilizers.
Dosage: 50-100 mg/day - 400-500 mg/day.
Therapeutic improvement - by the 7-14th day. Well tolerated, can be used in debilitated patients, children, the elderly.
Side effects: dry mouth, hand tremor, tachycardia, dizziness.
Contraindications:

1. acute diseases of the liver, kidneys;
2. blood diseases;
3. other MAO inhibitors;
4. sympathomimetic amines (adrenaline, mezaton);
5. acute alcohol withdrawal.

Tetrindol. New original drug.
Tetracyclic blood pressure, close in all respects to pyrazidol. Does not give side effects of MAO, has no anticholinergic properties. Exceeds pyrazidol by the strength of the stimulating effect. Indications:

1. mild depression with lethargy, apatoaboulia, asthenia;
2. dysthymia;
3. cyclothymia;
4. hypochondriacal and obsessive-phobic phenomena;
5. somatized depression;
6. asthenodepressive syndrome in alcoholism. Dosage: 25-50 mg/day - 400 mg/day.

Stimulating effect - by the end of the 1st week, thymoanaleptic - at the 2-4th week. Well tolerated.
In case of overdose - dyspeptic disorders, insomnia, agitation. Contraindications are the same as for pyrazidol.

Moclobemide (Aurorix, Monerix). Monocyclic benzamide.
Selective reversible MAO blocker, has no anticholinergic, hypotensive and cardiotoxic properties.
Pharmacokinetics: rapidly absorbed in the gastrointestinal tract, bioavailability up to 85%. 50% binds to blood proteins. V/ = 1-2 hours, safe.
"Small antidepressant".
Indications:

1. "atypical" depression with obsessive-phobic, hypochondriacal symptoms;
2. somatized depression;
3. panic disorder;
4. hyperactive syndrome in children. Dosage up to 300-600 mg / day.

Side effects are rare, contraindications - like all ADs.

befol. Original domestic drug. Benzamide derivative.
A reversible type A MAO blocker with a selective effect on serotonin deamination, that is, serotonergic blood pressure.
It does not have anticholinergic, antihistamine properties.
Pharmacokinetics: rapidly absorbed in the gastrointestinal tract, T1 / 2 = 3-5 hours. Peak concentration 1 hour after ingestion.
"Small antidepressant". Indications:

1. somatogenic depression;
2. cyclothymia;
3. adynamic depression;
4. somatovegetative depression;
5. anergic depression.

The therapeutic effect - on the 5-6th day. Dosage - 100-500 mg / day. Rarely and few side effects, therefore, it is indicated for children, the elderly. In case of overdose - dyspeptic disorders, tremor, palpitations.

Brofaromin. Bicyclic derivative of piperidine.
Selective reversible MAO inhibitor, serotonin reuptake blocker.
Efficiency approaches classical MAO inhibitors.
Indications:

1. endogenous depression resistant to treatment with tricyclic AD;
2. panic reaction;
3. phobias.

Therapeutic dose - 75-250 mg / day. Well tolerated. Side effects:

1. sleep disorders;
2. hypotension;
3. enhances the action of sympathomimetics.

Toloxatone (humor, humor, renum). Monocyclic derivative of oxazolidinone. Similar in effects to moclobemide. Indications: shallow depression with lethargy. Therapeutic doses - 600-1000 mg / day. T "/2 = 0.5-2.5 hours, safe. It is prescribed 4-6 times a day.
In case of overdose - dyspeptic symptoms, hyperstimulation, exacerbation of productive symptoms, inversion of sleep phases, hypotension, hepatitis.
Contraindications:

1. diseases of the liver and kidneys;
2. the use of irreversible MAO.

The latter have antidepressant and psycho-energizing properties. They serve to suppress the deamination of serotonin and norepinephrine.

List of drugs

Indications for use

Contraindications

• Hypersensitivity to the drug;
• Acute inflammatory diseases of the liver or kidneys have been identified.

Side effects

MAO inhibitors: pharmacological properties and trade names

Monoamine oxidase inhibitors (MAO) are biological substances that, by reducing the rate of chemical reactions of the monoamine oxidase enzyme, prevent the destruction of various monoamines (this group includes serotonin, norepinephrine, dopamine, phenylethylamine, tryptamine and octamine). This enhances the concentration of the active element between two neurons or between a neuron and an effector molecule (a particle that binds to proteins to increase biological activity).

For medical purposes, MAOIs are used as antidepressants and sometimes to treat Parkinson's disease and narcolepsy attacks, a pathological condition of the nervous system that causes drowsiness and a sudden "attack" of sleep.

According to their pharmacological properties, MAOIs are divided into:

• non-selective irreversible;
• reversible selective;
• irreversible selective.

So, let's take a brief look at each group and learn about the active ingredients, properties and trade names.

MAO inhibitors - drugs, list, intake

MAO is classified according to pharmacological properties into non-selective irreversible, reversible selective and irreversible selective.

• Phenelzine;
• Iproniazid;
• Isocarboxazid;
• Nialamide;
• Tranylcypromine.

• Metralindol;
• Pirlindol;
• Befol;
• Moclobemide;
• Derivatives of beta-carbolines.

Contraindications

• hypersensitivity;

• hypersensitivity;
• liver failure;

• Taking other antidepressants;
• hypersensitivity;
• Essential tremor;
• Chorea of ​​Huntington.

irreversible selective MAO inhibitors are prescribed for:

• progressive dementia;
• tardive dyskinesia;
• severe psychosis;
• severe angina;
• Angle-closure glaucoma;
• large-scale tremor;
• tachycardia;
• Pheochromocytoma;
• Diffuse toxic goiter.

Side effects

• Anxiety;
• dry mouth;
• Headache;
• Insomnia.

• Dyspepsia;
• Decreased blood pressure;
• Anxiety;
• insomnia;
• Headache;
• dry mouth;
• Constipation.

MAO inhibitors

Instructions for use:

MAO inhibitors are antidepressants used in the treatment of parkinsonism and narcolepsy.

Pharmacological action of MAO inhibitors

MAO inhibitors are classified according to their pharmacological properties into non-selective irreversible, reversible selective and irreversible selective.

Non-selective irreversible MAO inhibitors are similar in chemical structure to iproniazids, improve general state patients with depression and reduce angina attacks.

Reversible selective MAO inhibitors have antidepressant and psychoenergizing effects, actively suppress the deamination of serotonin and norepinephrine.

Irreversible selective MAO inhibitors have an antiparkinsonian effect, are involved in the metabolism of dopamine and catecholamines.

List of MAO inhibitor drugs

The list of non-selective irreversible MAO inhibitors includes:

Selegiline is an irreversible selective MAO inhibitor.

The list of reversible selective MAO inhibitors includes:

Indications for the use of MAO inhibitors

Non-selective irreversible MAO inhibitors are prescribed in the treatment of chronic alcoholism and depression (neurotic, involutional and cyclothymic), reversible selective - in depression of various origins, depressive syndrome, melancholic syndrome and astheno-dynamic disorders, and irreversible selective - in the treatment of Parkinson's disease.

Contraindications

The intake of reversible selective MAO inhibitors is contraindicated in:

• hypersensitivity;
• Acute inflammatory diseases kidneys and liver;
• Withdrawal alcohol syndrome;
• Pregnancy and lactation.

Also, reversible selective MAO inhibitors are not prescribed in infancy.

Reception of non-selective irreversible MAO inhibitors is not prescribed for:

• hypersensitivity;
• liver failure;
• Violation of cerebral circulation;
• Chronic renal failure;
• Chronic heart failure.

Reception of irreversible selective MAO inhibitors is contraindicated in:

• Pregnancy and lactation;
• Taking other antidepressants;
• hypersensitivity;
• Essential tremor;
• Chorea of ​​Huntington.

With caution, irreversible selective MAO inhibitors are prescribed for:

• progressive dementia;
• tardive dyskinesia;
• severe psychosis;
• Peptic ulcer of the gastrointestinal tract;
• Hyperplasia of the prostate;
• severe angina;
• Angle-closure glaucoma;
• large-scale tremor;
• tachycardia;
• Pheochromocytoma;
• Diffuse toxic goiter.

Side effects

The use of reversible selective MAO inhibitors can cause:

The use of non-selective irreversible MAO inhibitors can cause:

The use of irreversible selective MAO inhibitors can cause complications from various systems organism, namely:

• Decreased appetite, dryness of the oral mucosa, increased activity of transaminases, nausea, diarrhea, constipation and dysphagia (digestive system);
• Fatigue, insomnia, dizziness, hallucinations, headache, anxiety, dyskinesia, motor and mental agitation, confusion and psychosis (nervous system);
• Increased blood pressure, orthostatic hypotension and arrhythmia (cardiovascular system);
• Diplopia and impaired visual acuity (sense organs);
• Nocturia, urinary retention and painful urge to urinate (urinary system);
• Shortness of breath, photosensitivity, skin rash and bronchospasm (allergic reactions).

Also, taking irreversible selective MAO inhibitors can cause perspiration, hypoglycemia, and hair loss.

Information about the drug is generalized, is provided for informational purposes and does not replace official instructions. Self-medication is dangerous to health!

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MAO inhibitors

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MAO inhibitors are antidepressants that are prescribed for the treatment of parkinsonism, as well as epilepsy.

pharmachologic effect

Preparations of MAO inhibitors are divided into the following groups: non-selective reversible, selective irreversible and reversible selective. The latter have antidepressant and psycho-energizing properties. They serve to suppress the deamination of serotonin and norepinephrine.

Non-selective irreversible drugs are designed to reduce angina attacks, as well as improve the condition of patients who are in deep depression. These drugs are similar in structure to iproniazids.

Irreversible selective MAO inhibitors have antiparkinsonian properties and are involved in the metabolism of dopamine and catecholamines.

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List of drugs

Non-selective irreversible drugs include: Nialamide, Iproniazid, Phenelzine, Isocarboxazid, Tranylcypromine.

Selective irreversible drugs include the drug Selegiline.

The list of MAO inhibitors (reversible selective) includes the following drugs: Befol, Metralindol, Moclobemide, Pirlindol, beta-carboline derivatives.

Indications for use

Preparations of MAO inhibitors (reversible selective) should be taken for depression of a different nature, with melancholic syndrome, depressive syndrome, astheno-dynamic disorders. Non-selective irreversible drugs should be prescribed to patients with neurotic, cyclothymic, involutional depressions. Taking pharmaceuticals is also indicated in the treatment of chronic alcoholism.

Irreversible selective drugs should be prescribed in the treatment of Parkinson's disease.

Contraindications

Reception of MAO inhibitors (reversible selective) is contraindicated in patients who have:

Drugs are not prescribed for alcohol withdrawal syndrome. It is strictly forbidden to take medicines during pregnancy and lactation.

You should not take drugs (non-selective irreversible) in the following cases:

• If the patient has hypersensitivity;
• Revealed liver failure;
• There is a violation of cerebral circulation;
• A diagnosis of chronic heart failure was made.

The intake of MAO inhibitors (irreversible selective) is strictly contraindicated in patients who are taking other antidepressants. Also, drugs in this category are not prescribed during pregnancy and during lactation, with Huntington's Chorea, essential tremor.

With caution, drugs (irreversible selective) should be taken by patients who have: severe angina pectoris, progressive dementia, severe psychosis, prostatic hyperplasia, angle-closure glaucoma, large-scale tremor, peptic ulcer of the gastrointestinal tract, tardive dyskinesia, tachycardia, diffuse toxic goiter, as well as pheochromocytoma.

Side effects

When using reversible selective drugs, the patient may experience the following body reactions: insomnia, headache (of a periodic nature), dry mouth, anxiety.

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When using non-selective irreversible drugs, a person may experience: dyspepsia, lower blood pressure, anxiety, insomnia, headache, constipation.

When using irreversible selective MAO inhibitors, the following body reactions may occur:

• Increased blood pressure, arrhythmia, hypotension;
• In some cases, the patient's appetite decreases, the mucous membrane of the eye becomes dry, and transaminase activity increases;
• In addition, diarrhea, constipation, dysphagia, nausea may occur;
• A small percentage of people experience urinary retention, painful urge to urinate;
• When taking drugs, shortness of breath, skin rash, bronchospasm may appear.

When taking drugs (irreversible selective), a person may begin the process of hair loss, hypoglycemia may form.

MAO inhibitors - what is it and a list of drugs. Mechanism of action and use of monoamine oxidase inhibitors

MAO inhibitors - that only people who are interested in medical news know this. The decoding is simple - this is a group of medicines that belongs to antidepressants that block the breakdown of MonoAmin Oxidase. They are used as medicines for depression, to restore normal emotional background and mental health.

What are MAO Inhibitors

To understand which drugs are MAO inhibitors, you need to know them pharmachologic effect. These medicines have the ability to improve the quality of life and fight anxiety. Another name for them is monoamine oxidase inhibitors (MAOIs). These are substances of plant and chemical origin, widely used in psychiatry.

The impact on the body is based on blocking the enzyme monoamine oxidase. As a result, the breakdown of various substances and neurotransmitters is disrupted in the stomach. The symptoms of depressive and mental disorders are alleviated. It is possible to classify the entire list of drugs according to their pharmacological action.

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irreversible MAO inhibitors

Irreversible MAOIs include drugs whose principle of action is based on the formation of chemical bonds with monoamine oxidase. As a result, the enzyme functionality is suppressed. These are first generation drugs with a lot of side effects. Have poor compatibility with others pharmacological means. The patient during treatment must adhere to a diet. They can also be divided into hydrazine (Nialamide, Iproniazid) and non-hydrazine (Tranylcypromine, Isocarboxazid).

Reversible MAO inhibitors

Reversible MAOIs are prescribed for many diseases. They are representatives of the second generation. They do not have serious negative effects, a diet is not required when taking them. The principle of functioning of this group of medicines is based on the capture of the enzyme and the creation of a stable complex with it. They are divided into: selective (Moclobemide, Tetrindol) and non-selective (Caroxazon, Inkazan).

Selective MAO inhibitors

Selective MAOIs are able to inactivate only one type of monoamine oxidase. As a result, the breakdown of serotonin, norepinephrine and dopamine decreases. Simultaneous use with drugs that increase the level of serotonin leads to the appearance of serotonin syndrome. This dangerous disease is a sign of intoxication of the body. For its treatment it is necessary to cancel all antidepressants.

Non-selective MAO inhibitors

Non-selective MAOIs block the enzyme monoamine oxidase in A and B varieties. They are rarely prescribed because they have a pronounced toxic effect on the liver. The effect of the use of these drugs persists for a long time (up to 20 days) after the end of therapy. They tend to reduce the frequency of attacks in angina pectoris, which allows them to be prescribed to patients with cardiovascular diseases.

MAO inhibitors - list of drugs

What drugs belong to MAOI, and what can help in a particular case, you can find out in medical institution. The use of antidepressants must be agreed with the attending physician. The doctor selects drugs individually, based on the symptoms of the disease. The entire list of drugs is divided according to the pharmacological classification. List of MAO inhibitors:

1. Irreversible non-selective are: Phenelzine, Tranylcypromine, Isocarboxazid, Nialamide.
2. The smallest is the list of irreversible selective representatives: Selegilin, Razagilin, Pargilin.
3. Reversible selective drugs are the largest group, they include the following drugs: Pirlindol (pyrazidol), Metralindol, Moclobemide, Befol, Tryptamine, beta-carboline derivatives (trade name Garmalin).

MAO inhibitors - instructions for use

The use of MAO inhibitors:

1. Irreversible non-selective are used to treat:

• involutional depressions;
• neurotic depressions;
• cyclothymic depressions;
• in the treatment of chronic alcoholism.

1. Irreversible selective drugs are used only in the treatment of Parkinson's disease.

1. Reversible selective use:

• with melancholic syndrome;
• with asthenodynamic disorders;
• with depressive syndrome.

Contraindications depend on the type of medication. Irreversible non-selective should not be used in the presence of cardiac, renal, hepatic insufficiency, coronary circulation disorders. Irreversible selective drugs are prohibited during pregnancy and breastfeeding and Huntington's chorea. Do not prescribe them in combination with antipsychotic drugs. Contraindications to taking reversible selective will be: infancy, acute liver failure.

Side effects when using a drug that has a reversible selective effect will be expressed by the following symptoms: insomnia, recurrent headache, constipation, dry mouth, increased anxiety. With an increase in the recommended dosage or non-compliance with the treatment regimen in patients, this drug increases the manifestation of side effects.

When taking non-selective irreversible MAOIs, the following side effects are possible: dyspepsia, disruption of the gastrointestinal tract. Often there is the appearance of hypotension (lowering blood pressure), headaches in the frontal part of the head. When taking reversible MAOIs, the list of negative effects is replenished: hypertension, decreased appetite, urinary retention, rash, shortness of breath.

MOA inhibitors: what is it, a list of drugs and their trade names

Depression is not just "I'm in a bad mood today." This is a dangerous and serious condition that is associated with an imbalance of certain chemical compounds in the brain. To normalize this imbalance, as well as to treat Parkinson's disease, MAO inhibitors are used. We offer a list of such drugs and their brief characteristics.

These drugs are intended for the treatment of severe depression, in which other drugs do not work properly. They provide a long-term pharmacological effect, which lasts from 1 to 2 weeks after the end of therapy, but they have many contraindications, they can provoke quite serious adverse reactions. Therefore, their reception can be considered a last resort. Such medications are prescribed by a psychiatrist or neurologist.

The first generation of MAO inhibitors: dangerous irreversible non-selective

Such drugs are used extremely rarely today, since they do not combine well with other drugs, are toxic (very harmful to the liver), and have a wide variety of side effects. In addition, their intake requires the patient to follow a certain diet: you have to exclude cheese, coffee, wine, beer, cream, smoked meats from the diet. They are prescribed for the elimination of neurotic, involutional, cyclomatic depression and the treatment of chronic alcohol dependence.

The list of irreversible MAO inhibitors with non-selective action is quite wide. Here is what applies to them:

• Nardil (Belgium). A drug based on phenelzine, a powerful MAO inhibitor. Eliminates the feeling of anxiety, fear, sadness, restores peace of mind. Not the most modern antidepressant, however, it is often used to treat social phobias. The effect is found after a 2-week intake;
• Marplan. The active substance is isocarboxazid. Relieves some symptoms of depression: longing, feeling of worthlessness, low self-esteem, chronic sadness, phobias. In many countries, it has ceased to be produced, as it leads to the destruction of the liver and provokes serious side effects;
• Parnat (Japan). Its action is due to the presence of the active component of tranylcypromine. It has a positive effect on the emotional and mental background in a depressed state, lethargy, lethargy, obsessive disorders. It shows relatively little side activity, but produces a very short effect on MAO - about 12 hours;
• Iprazid (Russia). The active substance is iproniazid. It was used in psychiatry and in cardiology (in the treatment of angina pectoris to reduce pain and improve the ECG). Causes persistent inhibition of MAO. It is now universally discontinued due to high hepatotoxicity. It is forbidden to drink it for more than 2 weeks;
• Nialamide. A psychostimulant with the same active ingredient, produced in Russia. It has a more gentle effect, improves the general condition of people suffering from depression. It is indicated for asthenia, oligophrenia, trigeminal neuralgia, angina pectoris. The result of therapy is noticeable after 1-2 weeks of admission. The course is from 1 to 6 months.

Important! Although these drugs are sold without a prescription, they are not the first choice in the treatment of depression. Such drugs can cause clinical deterioration, fatal side effects, and increase the risk of suicide. Thus, they should only be taken with the permission of a doctor.

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Irreversible selective: narrow spectrum agents

With the help of drugs included in this group, only one pathology is treated - Parkinson's disease. Since they are highly specialized, the list of these MAO inhibitors is not too long. Here are the trade names of such drugs, under which they are sold in the pharmacy chain:

• Yumeks (Hungary), Stillin (Israel). The registration period of the second drug has expired, so it is not sold in pharmacies in our country. The active active ingredient of drugs is selegin. It inhibits the metabolism of dopamine, thereby increasing its concentration in the nuclei of cells of certain parts of the brain. The main purpose of these drugs is the treatment of Parkinson's disease and the symptoms of parkinsonism (as monotherapy or together with Levodopa), but there are attempts to use them as antidepressants and anti-smoking agents. Some experts are of the opinion that Yumex is a drug for prolonging life, as it has neuroprotective properties;
• Pargylin (India). It is an antidepressant, recommended for neuropsychiatric disorders. The active substance is parligin. It is considered a fairly safe drug, is actively used in psychiatry;
• Azilect. Produced in Israel, contains rasagiline. Fairly new inhibitor. Recommended for the treatment of true Parkinson's disease and essential tremor. Restores motor activity, coordination, gait in such patients. Additionally, it stops age-related memory decline, improves mood and learning outcomes. The produced effect is associated with the accumulation of special natural compounds in the brain.

Important! All of these drugs should not be combined with serotonin drugs, including fluoxetine.

Reversible selective: gentle but effective

Such drugs belong to the second generation of MAO inhibitors. They help to alleviate the condition of those who suffer from asthenic, melancholic syndrome and asthenodynamic disorders. They revealed several advantages over their predecessors at once: their intake is not accompanied by dangerous side effects, the patient does not have to adhere to dietary restrictions.

This group of MAO inhibitors is the most extensive. The list of medicines includes, in particular:

• Tetrindol (Russia). Fast-acting remedy: the result of its administration is manifested in just 2-3 days from the start of treatment. Indicated for depression of various origins (including in the case of organic damage brain), as well as in chronic alcoholism;
• Aurorix (Switzerland). Contains moclobemide. Psychoanaleptic. Relieves symptoms of depression - nervous exhaustion, low concentration of attention, dysphoria, helps to eliminate social phobia, increases psychomotor activity. Not prescribed for agitation;
• Metralindol (Russia). The active element is inkazan. Often prescribed for manic-depressive syndrome, schizophrenia, unmotivated mood swings, as well as to activate blood circulation in the brain;
• Caroxazon. Refers to the "small" antidepressants. Produces a moderate stimulating effect. Out of production;
• Befol (Russia). It is prescribed for delusional disorders, hallucinations, dependence on alcohol;
• Pirlindol (created on the basis of pyrazidol). It is indicated for attacks of apathy, depressive disorders, emotional overexcitation, accompanied by fear and anxiety.

Important! All MAO inhibitors are prohibited for pregnant and lactating women.

Depression is a condition that many describe as "I don't want to live." Even specialists cannot always help in such a situation, so it is impossible to cure this disorder on your own. Even knowing what MAO inhibitors are and what names are included in the list of these drugs, you should not buy them at a pharmacy and start taking them: they are far from safe! And even more so, you should not try to select drugs for the treatment of Parkinson's disease without doctors. So you will not help, but only harm a loved one.

MAO inhibitors

Instructions for use:

MAO (monoamine oxidase) inhibitors are a group of drugs used in psychiatric practice for the treatment of depressive conditions of various origins. As a rule, MAO inhibitor drugs are used in cases of advanced depression, in which any other treatment methods are ineffective.

Pharmacological effect and classification of drugs-MAO inhibitors

MAO inhibitors are biologically active substances capable of inhibiting the enzyme monoamine oxidase. These drugs block the process of destruction of mediator monoamines (serotonin, norepinephrine, dopamine, phenylethylamine and others) and increase their concentration, thereby enhancing the transmission of nerve impulses.

A distinctive feature of this group of antidepressants is a long pharmacological effect: the therapeutic effect of MAO inhibitors continues for one to two weeks after the end of the course of treatment.

Depending on their pharmacological properties MAO inhibitors are divided into selective and non-selective, as well as reversible and irreversible.

The action of selective monoamine oxidase inhibitors is directed mainly to the inhibition of one of the types of monoamine oxidase. Non-selective drugs inhibit both types of the enzyme.

Reversible MAO inhibitors bind to the enzyme and form a stable complex with it, which gradually releases the active components of the drug. They enter the bloodstream and then are excreted from the body naturally. Thus, the monoamine oxidase enzyme remains intact.

Irreversible MAO inhibitors form chemical bonds with monoamine oxidase, causing the enzyme to become non-functional and metabolized. Instead, the body synthesizes a new monoamine oxidase. On average, the enzyme production process takes about two weeks.

Non-selective irreversible MAO inhibitors include drugs such as Isocarboxazid, Iproniazid, Tranylcypromine, Nialamide, Phenelzine. The list of reversible MAO inhibitors includes Befol, Moclobemide, Metralindol, Pyrazidol and beta-carboline derivatives. Selegiline is an irreversible selective MAO inhibitor.

Indications for use

Irreversible MAO inhibitors are used in the treatment of depressive conditions accompanied by lethargy and lethargy. Reversible drugs are prescribed in the treatment of shallow depressions with not pronounced hypochondriacal and neurosis-like symptoms, as well as atypical depressive conditions. Selective MAO inhibitors of irreversible action are used in the treatment of narcolepsy and parkinsonism.

Reception features

The scheme of therapy and the dosage of drugs are determined strictly individually and depend on the indications, as well as the nature of the course of the disease.

Patients who are prescribed to take MAO inhibitors, in some cases, should follow a special diet. For the duration of treatment and for at least two weeks after its completion, the following foods and drinks should be excluded from the diet:

• meat, chicken and beef liver;
• smoked and pickled fish;
• dry sausages;
• chocolate and caffeine;
• dairy products (only allowed cream cheeses and pressed cottage cheese);
• soy sauce;
• canned dates;
• bean pods;
• bananas, avocados;
• yeast extract, including brewer's yeast;
• any alcoholic drinks;
• stale recycled meat, fish and dairy products.

In addition, during the period of taking MAO inhibitors, patients should not use the following drugs:

• cold remedies;
• drugs from colds(tablets, medicines);
• stimulants;
• inhalants and asthma medications;
• drugs for weight loss and appetite suppression;
• any drugs with a narcotic effect, including those containing caffeine.

When using reversible MAO inhibitors, compliance with diet food not necessary.

Contraindications and side effects

The use of MAO inhibitors from the list of reversible selective drugs is contraindicated in case of hypersensitivity, alcohol withdrawal syndrome, inflammatory diseases of the liver and kidneys in acute form as well as during pregnancy and breastfeeding.

MAO inhibitors of irreversible non-selective action are not prescribed for hypersensitivity, chronic renal or heart failure, liver failure and cerebrovascular accidents.

Irreversible selective MAO inhibitors are contraindicated in case of hypersensitivity, during pregnancy and breastfeeding, as well as in Huntington's chorea and essential tremor. In addition, MAO inhibitors from the list of drugs of irreversible selective action are not prescribed in combination with other antidepressants.

Side effects caused by reversible selective MAO inhibitors are most often manifested as insomnia, anxiety, headache and dry mouth. When taking MAO inhibitors of irreversible non-selective action, the same side effects. In addition, drugs in this group can cause dyspepsia, constipation and lowering blood pressure.

Irreversible selective monoamine oxidase inhibitors have the following side effects:

• dizziness, headache, insomnia, anxiety, fatigue, dyskinesia, increased mental and motor excitability, psychosis, confusion;
• nausea, loss of appetite, dry mouth, constipation, diarrhea;
• arrhythmia, orthostatic hypotension, increased blood pressure;
• visual impairment, diplopia;
• violations of the functions of the urinary system (urinary retention, nocturia);

It is also necessary to know that the use of MAO inhibitors in combination with alcohol can provoke hypertensive crisis and enhanced effects on the central nervous system.

The description posted on this page is a simplified version of the official version of the annotation for the drug. The information is provided for informational purposes only and is not a guide for self-treatment. Before using the drug, you should consult with a specialist and read the instructions approved by the manufacturer.

Pharmacological group - Antidepressants

Subgroup drugs are excluded. Turn on

Description

Drugs that specifically treat depression appeared in the late 1950s. In 1957, iproniazid was discovered, which became the ancestor of the group of antidepressants - MAO inhibitors, and imipramine, on the basis of which tricyclic antidepressants were obtained.

According to modern concepts, a decrease in serotonergic and noradrenergic synaptic transmission is observed in depressive states. Therefore, the accumulation of serotonin and norepinephrine in the brain caused by them is considered an important link in the mechanism of action of antidepressants. MAO inhibitors block monoamine oxidase, an enzyme that causes oxidative deamination and inactivation of monoamines. Currently, two forms of MAO are known - type A and type B, which differ in the substrates exposed to them. Type A MAO causes mainly the deamination of norepinephrine, adrenaline, dopamine, serotonin, tyramine, and type B MAO causes the deamination of phenylethylamine and some other amines. Allocate inhibition competitive and non-competitive, reversible and irreversible. Substrate specificity can be observed: a predominant effect on the deamination of various monoamines. All this significantly affects the pharmacological and therapeutic properties of various MAO inhibitors. Thus, iproniazid, nialamide, phenelzine, tranylcypromine irreversibly block MAO type A, and pirlindol, tetrindol, metrolindole, eprobemide, moclobemide, etc. have a selective and reversible effect on it.

Tricyclic antidepressants are named because of their characteristic tricyclic structure. The mechanism of their action is associated with inhibition of the reuptake of neurotransmitter monoamines by presynaptic nerve endings, resulting in the accumulation of mediators in the synaptic cleft and activation of synaptic transmission. Tricyclic antidepressants, as a rule, simultaneously reduce the capture of various neurotransmitter amines (norepinephrine, serotonin, dopamine). Recently, antidepressants have been created that block predominantly (selectively) the reuptake of serotonin (fluoxetine, sertraline, paroxetine, citalopram, escitalopram, etc.).

There are also so-called "atypical" antidepressants, which differ from the "typical" ones both in structure and in the mechanism of action. Preparations of a bi- and four-cyclic structure appeared, in which no pronounced effect was found either on the capture of neurotransmitters or on the activity of MAO (mianserin, etc.).

A common feature of all antidepressants is their thymoleptic effect, that is, a positive effect on the affective sphere of the patient, accompanied by an improvement in mood and general mental state. Different antidepressants differ, however, in the amount of pharmacological properties. So, in imipramine and some other antidepressants, the thymoleptic effect is combined with a stimulating one, and in amitriptyline, pipofezin, fluacizine, clomipramine, trimipramine, doxepin, a sedative component is more pronounced. In maprotiline, the antidepressant effect is combined with anxiolytic and sedative. MAO inhibitors (nialamide, eprobemide) have stimulating properties. Pirlindol, removing the symptoms of depression, exhibits nootropic activity, improves "cognitive" ("cognitive") functions of the central nervous system.

Antidepressants have found application not only in psychiatric practice, but also for the treatment of a number of neurovegetative and somatic diseases, in chronic pain syndromes and etc.

The therapeutic effect of antidepressants, both oral and parenteral, develops gradually and usually manifests itself after 3-10 days or more after the start of treatment. This is explained by the fact that the development of the antidepressant effect is also associated with the accumulation of neurotransmitters in the area nerve endings, and with slowly appearing adaptive changes in the circulation of neurotransmitters and in the sensitivity of brain receptors to them.

How antidepressants can help us: MAO inhibitors

Medical educational program

Anyone who monitors their health, is interested in medical news, is well aware of such an expression as MAO inhibitors. What it is, not everyone can explain. And meanwhile, everything is not so difficult. This is what psychotropic drugs are called. In other words, antidepressants. These remedies are able to eliminate negative emotions, feelings of longing or hopelessness. Particularly valuable is the fact that some representatives of the antidepressant group can cause not only a psychostimulant, but also a sedative (calming) effect. This distinguishes them from stimulants. Therefore, MAO inhibitors are often used in psychiatry.

What is an MAO inhibitor?

Let's figure out what this phrase means, let's define the words that make it up. An inhibitor is a substance that slows down or prevents the course of any chemical reaction. MAO (full name - monoamine oxidase) is an enzyme produced by gastrointestinal tract. It helps to break down literally all the substances that enter the human body with food. Thus, MAO inhibitors are biologically active substances that block the enzyme monoamine oxidase. Once in the body, they inhibit the reactions associated with the decomposition of certain substances. For example, serotonin (the so-called joy hormone), melatonin, dopamine. This alleviates the symptoms of depression.

Herbal MAO inhibitors

I must say that this group includes not only medications, but also some plants. For example, Indian tribes used the vine Banisteriopsis caapi as an MAO inhibitor. IN modern medicine Siberian rue seeds are used. It contains harmine and harmaline. When taken in large quantities, these alkaloids can cause vomiting, nausea, hallucinations, and convulsions.

Classification of MAO inhibitors by pharmacological properties

All existing inhibitors are divided into 3 categories.

1. Non-selective irreversible inhibitors. Their distinctive feature can be called the fact that they not only fight depression, but are also able to reduce angina attacks. These include "Nialamid", "Fenelzin" and other drugs.
2. Selective reversible inhibitors. They have a psycho-energizing effect. Excellent antidepressants, as they increase serotonin and norepinephrine. For example, "Befol" or "Pirlindol".
3. Selective irreversible inhibitors. Indispensable in the treatment of Parkinson's disease. A typical representative of this group is Selegiline.

Application in medicine

To date, MAO inhibitors are prescribed quite rarely. This is due to the large number of side effects they can cause. Their use is justified only in cases where other, more gentle means have been tried. Most often, synthetic inhibitors are used for treatment. This is due to the fact that they have a longer duration of action compared to herbal counterparts. So, for example, the same harmaline can act within 1-3 days after ingestion, while the effect of a synthetic inhibitor can last up to two weeks.

Contraindications

These psychotropic drugs should be taken with extreme caution, as they have many contraindications:

• Non-selective irreversible inhibitors are not prescribed for heart or kidney failure, as well as in cases where the patient has a cerebrovascular accident.
• Selective reversibles are contraindicated in acute inflammatory diseases, during pregnancy or lactation, in infancy, and in alcohol withdrawal.
• Selective irreversible MAO inhibitors should never be combined with other antidepressants. In addition, they are not used for tremor and Huntington's chorea (a disease characterized by mental and movement disorders). It is necessary to prescribe them with caution in psychosis, angina pectoris, tachycardia.

Precautionary measures

Taking inhibitors is associated with many side effects, so you must follow all the necessary rules for taking. Be sure to tell your doctor about your chronic diseases, pregnancy or intention to become pregnant, allergies to any drugs. It is better to consult a doctor if you are going to take other medicines. And, of course, you must strictly follow the diet.

Features of nutrition while taking MAO inhibitors

Taking inhibitors can be extremely hazardous to your health if you eat certain foods. This is due to this: blocking the MAO enzyme contributes to the accumulation of such an amino acid as tyramine. In the normal state, its level is successfully regulated by the body itself. But by taking MAO inhibitors, you increase this substance in the blood. Therefore, it is necessary to exclude from the diet all foods containing tyramine. These include:

1. Mature cheeses. For example, cheddar cheese contains 40 mg of tyramine per 30 g piece. Most likely, such a high content of this amino acid is due to fermentation processes. There is little tyramine in cottage cheese and processed cheeses, they can be eaten without compromising health.
2. Alcohol. In ale, chianti, live beer - 11 mg of this substance per 100 g of product. Therefore, they cannot be used. Red wine and bottled beer are allowed, but the measure must be observed.
3. Processed meat and fish products. It is forbidden to use smoked meats, dry sausages, pickled fish. The content of tyramine in them can reach up to 86 mg per serving. Such a high rate is due to aging and the presence of preservatives.
4. Seasonings. It is very difficult to single out one thing here, since tyramine is often found in mixed products. For example, Asian cuisine cannot be imagined without soy sauce. And it contains a huge amount of dangerous amino acids. Therefore, it is better to give preference to simple-to-cook dishes.

Prohibited drugs

As already mentioned, it is necessary to carefully combine inhibitors with other medications and always inform the attending physician. In no case should inhibitors be used with drugs such as:

• Remedies for colds or sinusitis.
• Inhalers for asthma.
• Drugs that are used to reduce appetite or weight loss.
• Stimulants.

Side effects

In many patients, taking inhibitors does not cause side effects. However, failure to follow the recommendations of a doctor can lead to sad consequences:

• The use of non-selective irreversible inhibitors can cause headache, constipation, dry mouth, and low blood pressure.
• Selective reversible inhibitors have side effects such as: insomnia, anxiety, headache.
• Selective irreversible inhibitors can cause impaired visual acuity, arrhythmia and urinary retention, dizziness and hallucinations.

I would like to say one more thing: taking inhibitors should not be abandoned in the middle of a course of treatment. Often, these funds do not work immediately. In some cases, the effect appears only 4 weeks after taking the medication. But your patience will be rewarded with improved well-being. And that means you have conquered the disease.