MAO inhibitor drugs. Pharmacological action of MAO inhibitors. irreversible MAO inhibitors

Hi all! Today you will learn a terrible spell in medicine! It is so strong that it can kill a person, so such information is more of an educational nature. She is interesting and beautiful, like some kind of bizarre poisonous snake. We will not describe how to apply this knowledge in real life, they are dangerous and can only be used by the most the best specialists in the field of biology.

Agree, it happens that you want to read something unusual, in the style of "", with the aim of "learning" and, possibly, telling your friends. You can check, after the release, there will be something to talk about, or at least think about. Even the title of the topic: "MAO Inhibitors" sounds pretty good.

What does inhibitors mean?

Activators and inhibitors are the 2 main directions in the regulation biological processes. Activators and inhibitors are often compounds, and, in biology, there are no 100% activating or inhibitory substances. Gaining a big plus in one thing, we lose in another.

To make it easier to understand, remember your feelings from the games. When you "win", the processes associated with, and serotonin are activated, but GABA, for example, is suppressed. Feelings of pleasure and happiness, and suppression of calmness and reason.

So, when we activate something, we suppress something and vice versa. This is balance.

Inhibitors are suppressors/destroyers.

What is MAO?

Before clarifying this term, it is important to recall the basics of synaptic transmission of neurotransmitters, when one neuron releases mediators into the synaptic cleft, into the space from which they are absorbed by the 2nd neuron. As long as mediators are neither in the first nor in the second neuron, in the middle, the smart organism selects their excess with the help of the monoamine oxidase enzyme.

This word only sounds scary, let's break it into parts: "mono" means one, "amine" means an amine group, 1 nitrogen atom, 2 hydrogen. Oxidase comes from the word "oxide" - oxygen, redox reactions.

So it turns out that monoamine oxidase, that is, MAO, is a substance that oxidizes and destroys monoamines. Monoamines are neurotransmitters.

- monoamine oxidase, which destroys such mediators as dopamine, norepinephrine and serotonin from the synaptic cleft and directs the excess back to the first neuron, for re-accumulation in vesicles and "shooting" into space to the second neuron. Creates a circuit so that our lazy body does not have to re-create neurotransmitters from amino acids.

Imagine how you fill a mug with water, and the water begins to overflow and flow down the walls. In our body, excess water"does not spread, but returns back to the container from where you poured the water into the mug. In this context, "water" refers to neurotransmitters.

MAO-A is found in the outer membrane of the mitochondria in cells.

MAO-B- monoamine oxidase, also located in mitochondria and destroys dopamine and other less significant, weighty mediators. For reference, more than a hundred different neurotransmitters are already known.

Inhibition of monoamine oxidase refers to the process by which "suppressors" of monoamines are "suppressed". As we remember from mathematics, minus times minus is plus. Thus, similar processes occur in cells. By inhibiting monoamine oxidase, we destroy what should have destroyed another.

Monoamine oxidase inhibitors- These are strong substances that can change a person beyond recognition, in particular, his behavior. The stronger these inhibitors, these substances, the stronger the changes. A situation may arise when taking coffee or, even worse, taking nootropics will cause such a violent expression, the production of mediators, that the effect of strong psychostimulant drugs will turn out. Well, we understand how the behavior of a person under drugs changes.

Inhibitors are also divided into more or less "strong", this is not a binary system, when inhibition either occurs or not. It is rather a scale, where 0 is the absence of inhibition, and 100 is conditional 100%. A fatal outcome is possible for a person when taking "strong" substances that act on neurotransmitters, and "strong" MAO inhibitors.

In science, they are usually classified into reversible and irreversible, selective and non-selective.

selective act on a specific monoamine oxidase A or B. By blocking the destruction of certain substances in our brain. Non-selective blocks both types.

irreversible practically destroy MAO, forcing the body to start a new creation of the enzyme, which takes about 2 weeks. Reversible can be said to bind MAO for a certain time.

Now such a terrible term as an irreversible non-selective monoamine oxidase inhibitor becomes more or less clear to you. But non-selective ones are almost never used now.

As regards the application, then many antidepressants have selective reversible MAOIs. They act on serotonin and dopamine, temporarily increasing their levels in the synaptic cleft. The areas of application of irreversible are many diseases that have a long or chronic eg chronic alcoholism, Parkinson's disease.

Relatively safe MAO inhibitors

Dangerous, they are strong, google "list of MAO inhibitors" and get a bunch of drug names. We will consider those MAOIs whose action is not so pronounced: Rhodiola Rosea, Yohimbine, Green tea, Nutmeg, Tobacco, Tyramine.

Interesting Facts

Crime can be genetically based. There are statistically significant correlations between crime rates and MAO activity (http://www.ncbi.nlm.nih.gov/pubmed/7792602). special case this correlation is Brunner's syndrome.

This syndrome was first noted in the 1990s. in one American family where 14 men had the MAO-A mutation. This mutation caused their bodies to produce more dopamine, norepinephrine and serotonin. In fact, this meant partial inhibition of monoamine oxidase throughout life. These people had below average IQs and were prone to aggressive and impulsive behavior. Moreover, it has been proven that children with low MAO activity are more prone to antisocial behavior in adulthood (Frazzetto G, Di Lorenzo G, Carola V).

Hence the suggestion that genetics, MAO mutations, are involved in low IQ and aggressive, criminal behavior.

Has a connection with increased activity MAO. It has been found that in depression, MAO activity is increased by 34% on average (PMID 17088501).

When taking antidepressants based on MAOIs, and, in general, when taking MAOIs, special attention is paid to the selection proper nutrition. If in ordinary life it is considered useful to eat fish, meat, dairy products, then on the MAOI course all this can cause side effects. These products are rich in useful amino acids, from which neurotransmitters are synthesized, and so, if you eat a lot of fish, you will get a lot of tryptophan. And serotonin will be produced from it, there will be a lot of serotonin (after all, it is not destroyed by MAO). The person will get serotonin syndrome: nausea, dizziness, etc. That is why it is said that consuming medicinal MAOIs and nootropics that pump, for example, dopamine, will result in hyperstimulation with all the consequences.

MAOIs interact mainly with catecholamines and serotonin, they do not inhibit, say,. It has its own "MAO" called acetylcholine transferase.

Outcome:

- Monoamine oxidase is a substance that can determine not only our behavior and lifestyle, but also the type of character.

- Normal, average values ​​of MAO activity are more beneficial for the body. It will be above the norm - a tendency to depression, below - lower IQ and irascibility.

- MAO inhibitors increase the levels of norepinephrine, dopamine and serotonin. Examples: yohimbine, rhodiola, green tea.

Well, I hope you enjoyed the information! See you later!

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).

AT medical purposes MAOIs are used as antidepressants and sometimes to treat Parkinson's disease and narcolepsy attacks - 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.

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 for treatment chronic alcoholism and depressions (neurotic, involutional and cyclothymic), reversible selective - in depressions 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 of the 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);
• Increased 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, provided for informational purposes and does not replace the 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 may occur, appear skin rash, bronchospasm.

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 their pharmacological action. These medicines have the ability to improve the quality of life and fight against anxiety states. 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, digestion is impaired in the stomach. various substances and neurotransmitters. Alleviate symptoms of depression and mental disorders. 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 large quantity side effects. Have poor compatibility with others pharmacological agents. 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, diet when taking them is not required. 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 a 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, disorders coronary circulation. 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 and 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 are very diverse. 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. Active substance- 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. Renders positive influence on the emotional and mental background in a depressed state, lethargy, lethargy, obsessive disorder. 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. Psychostimulant with the same name 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. Considered enough safe drug, is actively used in psychiatry;
• Azilect. Produced in Israel, contains rasagiline. Enough new inhibitor. recommended for therapy true disease Parkinson's 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. It is indicated for depression of various origins (including in the case of organic brain damage), as well as for chronic alcoholism;
• Aurorix (Switzerland). Contains moclobemide. Psychoanaleptic. Relieves symptoms of depression nervous exhaustion, low concentration of attention, dysphoria, helps 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 enzyme monoamine oxidase 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 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 cream cheeses and pressed cottage cheese are allowed);
• 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 for 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, dietary nutrition is not necessary.

Contraindications and side effects

The use of MAO inhibitors from the list of reversible selective drugs is contraindicated in hypersensitivity, alcohol withdrawal syndrome, acute inflammatory diseases of the liver and kidneys, 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 may occur. 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 a hypertensive crisis and an increased effect 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, depressive states there is a decrease in serotonergic and noradrenergic synaptic transmission. 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 different MAO inhibitors. So, iproniazid, nialamide, phenelzine, tranylcypromine irreversibly block MAO type A, and pirlindol, tetrindole, metralindol, 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). AT recent times 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 associated both with the accumulation of neurotransmitters in the region of 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. That's what they call psychotropic drugs. 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. AT modern medicine Siberian rue seeds are used. It contains harmine and harmaline. When admitted to in large numbers these alkaloids can cause vomiting, nausea, hallucinations, convulsions.

Classification of MAO inhibitors by pharmacological properties

All existing inhibitors are divided into 3 categories.

1. Non-selective irreversible inhibitors. Them distinctive feature we can say 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 harm to 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 high rate due to exposure 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 your doctor. 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 medicine. But your patience will be rewarded with improved well-being. And that means you have conquered the disease.

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 is similar in pharmacological actions 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) asthenodepressive;
2) asthenohypochondriac;
3) asthenoanergic;
4) apatoabolic;
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:

2) acute alcohol withdrawal;
3) 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 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 disorders;
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.

Monoamine oxidase inhibitors (MAOIs) are chemical substances, which inhibit the activity of monoamine oxidase enzymes. They have long been used as drugs to treat depression. These substances are particularly effective in the treatment of atypical depression. These drugs are also used to treat Parkinson's disease and some other conditions. Due to potentially dangerous dietary and drug interactions, monoamine oxidase inhibitors have historically been used as a last resort, and were used only when other antidepressants (eg, selective serotonin reuptake inhibitors and tricyclic antidepressants) have failed. A new MAO study shows that most of concern about dangerous dietary side effects is due to misconceptions and misinformation, and that despite the proven efficacy of drugs in this class, they are underused in medicine. The new study also casts doubt on the validity of the perceived severity of food reactions, based on data from outdated studies.

Indications

In the past, MAO inhibitors were prescribed to patients resistant to the effects of tricyclic antidepressants. Newer MAO inhibitors such as selegiline (typically used to treat Parkinson's disease) and the reversible MAO inhibitor moclobemide are safer alternatives to these drugs and are now sometimes used as first-line treatment. However, these substances do not always act as effectively as their predecessors. IMAO have been recognized effective means for the treatment of panic disorder with agoraphobia, social phobia, atypical depression or mixed anxiety and depression, bulimia and post-traumatic stress disorder, and borderline disorder personality. There is evidence of the effectiveness of MAOIs in the treatment of obsessive-compulsive disorder (OCD), trichotillomania, body dysmorphic disorder, and avoidant personality disorder, however, these data are obtained from uncontrolled clinical sources. MAOIs can also be used in the treatment of Parkinson's disease, acting in particular on MAO-B (thus acting on dopaminergic neurons) and also providing an alternative for migraine prevention. Inhibition of MAO-A and MAO-B is used to treat depression and anxiety. MAO inhibitors are especially commonly prescribed for outpatients with "neurotic depression" complicated by panic disorder or hysteroid dysphoria, which includes repeated episodes of depressed mood in response to feelings of rejection.

Mechanism of action

MAOIs act by inhibiting monoamine oxidase activity, preventing the breakdown of monoamine neurotransmitters, thereby increasing their availability. There are two isoforms of monoamine oxidase, MAO-A and MAO-B. MAO-A predominantly deaminates serotonin, melatonin, epinephrine and norepinephrine. MAO-B preferentially deaminates phenylethylamine and residual amines. Dopamine is equally deaminated by both types of isoforms.

reversibility

First-generation MAOIs irreversibly inhibit monoamine oxidase. In reaction with monoamine oxidase, they permanently deactivate it, and the enzyme cannot function until it is replaced in the body with a new one, which can take about two weeks. Some of the newer MAOIs, most notably moclobemide, are reversible, meaning they can be separated from the enzyme to facilitate normal substrate catabolism. The level of inhibition is thus regulated by the concentration of the substrate and the MAOI. Harmaline, found in the plants harmala vulgaris, ayahuasca, spirit vine, and meat red stratoflower, is a reversible MAO-A inhibitor (RIMA).

Selectivity

In addition to reversibility, MAO inhibitors differ in their MAO receptor selectivity. Some MAO inhibitors can equally inhibit MAO-A and MAO-B, while other MAO inhibitors have been developed for specific purposes. Inhibition of MAO-A reduces the breakdown primarily of serotonin, norepinephrine and dopamine; selective inhibition of MAO-A allows it to be metabolized through MAO-B. Taking drugs that act on serotonin when taken with another drug that increases serotonin levels can lead to a potentially fatal interaction called serotonin syndrome. When taking MAOIs with irreversible and non-selective inhibitors(for example, older generation MAOI), as a result of interaction with tyramine in the diet, it is possible to provoke the development of a hypertensive crisis. Tyramine is degraded by MAO-A and MAO-B, therefore inhibition of this action can lead to its excessive accumulation, so the patient should carefully monitor the intake of tyramine. Inhibition of MAO-B reduces the breakdown of mainly dopamine and phenylethylamine, so there are no associated dietary restrictions. MAO-B will also metabolize since the only differences between dopamine, phenylethylamine and tyramine are the two phenylhydroxyl groups on carbons 3 and 4. 4-OH does not sterically hinder MAO-B on tyramine. Two MAO-B drugs, selegiline and rasagiline, have been approved by the FDA without dietary restrictions except for high dose treatment, in which case they lose their selectivity.

dangers

At oral administration MAO inhibitors inhibit the catabolism of dietary amines. When eating foods containing tyramine (the so-called "cheese effect"), a person may experience a hypertensive crisis. When consuming foods containing tryptophan, hyperserotonemia may develop. The amount of substance required to develop a reaction varies greatly from person to person and depends on the degree of inhibition, which in turn depends on dose and selectivity. The exact mechanism by which tyramine induces a hypertensive response is not well understood, but it is hypothesized that tyramine displaces norepinephrine from the vesicles in which it is stored. This can cause a cascade of effects in which excessive amounts of norepinephrine can lead to the development of a hypertensive crisis. Another theory suggests that a hypertensive crisis causes the distribution and accumulation of catecholamines. It is tyrosine, not tyramine, that is the precursor of catecholamines. Tyramine is a breakdown product. In the intestines and during fermentation, the amino acid tyrosine is decarboxylated to tyramine. Under normal circumstances, tyramine is deaminated in the liver to inactive metabolites, but when hepatic MAO (predominantly MAO-A) is suppressed, the first pass of tyramine is blocked, which can lead to an increase in circulating levels of tyramine. Tyramine competes in increased amounts for transport across the blood-brain barrier (via aromatic amino acids), where it can enter adrenergic nerve endings. After entering the cytoplasmic space, tyramine is transported by the vesicular monoamine transporter to synaptic vesicles, thereby displacing norepinephrine. The massive movement of norepinephrine from its vesicular storage into the intercellular space can accelerate the development of a hypertensive crisis. Hypertensive crises, if left untreated, can cause stroke or cardiac arrhythmias. Both types of intestinal MAO inhibition can lead to the development of hyperthermia, nausea and psychosis, with the consumption of substances with high content. Foods and drinks with potentially high levels of tyramine include: liver and fermented substances such as alcoholic beverages and aged cheeses. found in foods such as beans. These dietary restrictions are not necessary for individuals taking selective MAO-B inhibitors at normal or low doses. Special mention deserves the fact that some meat extracts and yeast extracts (Bovril, Marmite, Vegemite) contain extremely high level, and they should also not be consumed while taking such medications.

When MAOIs are first introduced to the market, these risks

nothing was known, and over the next four decades, less than 100 people died from a hypertensive crisis. Presumably due to the sudden onset and violent onset of the reaction, MAOIs have gained a reputation for being hazardous substances that for some time they were completely discontinued in America. However, it is now believed that when using MAOIs under the supervision of a qualified psychiatrist, this class of drugs is a viable alternative, even for long-term use. The most significant risk associated with the use of MAO inhibitors is associated with the possibility of interaction with medicines, both over-the-counter and prescription-only drugs, illegal drugs or medicines, and some supplements (such as St. John's wort). It is very important that the doctor supervise such combinations in order to avoid possible adverse reactions. For this reason, many users have an MAOI card that gives all the information about the ambulance. medical care about drugs that the patient should avoid (for example, the dose of adrenaline in this case should be reduced by 75%, and the duration of exposure should be increased). The risk of interactions of MAOI drugs with other drugs or certain products is especially dangerous because often patients taking such drugs are in the position that they "do not care if they live or not." MAO inhibitors should not be combined with other psychoactive substances (antidepressants, painkillers, stimulants and illegal substances), except in cases of expert assistance. Certain combinations can cause fatal outcome, including combination with SSRIs, TCAs, MDMA, meperidine, tramadol and dextromethorphan. Drugs that act on epinephrine, norepinephrine, or dopamine should be administered at much lower doses due to the potentiation and long-term effect. Nicotine, a substance that often causes tobacco addiction, has a "relatively weak" potential to be addictive when used alone. With the simultaneous administration of MAOIs, the potential for addiction increases dramatically, which leads to an allergenic musculoskeletal response in rats, which is a measure of the potential of a substance to develop addiction. This can be expressed in the difficulty of quitting smoking, since in addition to nicotine, tobacco contains natural compounds.

Conclusion

Antidepressants, including MAOIs, have addictive properties, the most notable result of which is withdrawal symptoms, which can be severe, especially when MAOIs are stopped suddenly or too quickly. However, the dependence potential of MAO inhibitors or antidepressants in general is not as significant as that of benzodiazepines. To minimize or prevent withdrawal symptoms, you can gradually reduce the dose over several weeks, months or years. MAO inhibitors, like any other antidepressants, cannot change the course of the disease, so it is possible that if the patient stops taking it, he can return to the state that he had before starting treatment. This circumstance significantly complicates the patient's switch from MAOIs to SSRIs, since after taking one drug and before starting to take another, a complete cleansing of the body system is necessary. By gradually tapering the dose, the patient will find himself struggling with depression for several weeks without pharmacological support during the drug-free interval. This may be preferable to the risk of developing interaction effects between the two drugs, but often such a test is not given to the patient so easily.

Interactions

MAO inhibitors are known by numerous drug interactions, including with the following types of substances: 1. Substances that are metabolized by monoamine oxidase, as they can increase their exposure several times. 2. Substances that increase the activity of serotonin, norepinephrine, or dopamine, since an excess of any of these neurochemicals can lead to serious acute consequences, including the development of serotonin syndrome, hypertensive crisis and psychosis, respectively. Such substances include: - Phenethylamines: 2C-B, mescaline, phenethylamines, etc. - Amphetamines: amphetamine, MDMA, dextroamphetamine, methamphetamine, DOM, etc. - Tryptamines: DMT, psilocin/psilocybin ("magic mushrooms"), etc. - Lysergamides: ergolines/LSA, LSD ("acid"), etc. - Serotonin, norepinephrine and/or dopamine reuptake inhibitors: - Serotonin reuptake inhibitors (SSRIs): citalopram, dapoxetine, escitalopram, fluvoxamine, paroxetine,. - Serotonin-norepinephrine reuptake inhibitors: dezvenlafaxine, duloxetine, milnacipran,. - Norepinephrine-dopamine reuptake inhibitors: amineptine, bupropion, methylphenidate, nomifensine. - Norepinephrine reuptake inhibitors: atomoxetine, mazindol, reboxetine. - Tricyclic antidepressants (TCAs): butriptyline, clomipramine, dosulepin, doxepin, imipramine, lofepramine, nortriptyline, protriptyline, trimipramine. - Tetracyclic antidepressants: amoxapine, maprotiline. - Phenylpiperidine opioid derivatives: meperidine/pethidine, tramadol, methadone, dextropropoxyphene, propoxyphene. - Others: brompheniramine, chlorpheniramine, cocaine, cyclobenzaprine, dextromethorphan (DXM), ketamine, MDPV, nefazodone, phencyclidine (PCP), pheniramine, sibutramine, trazodone. - Substances that release serotonin, norepinephrine and / or dopamine: 4-methitaminorex (4-MAR), amphetamine, benzphetamine, cathin, cathinone, diethylcathinone, levmethamphetamine, lisdexamphetamine, MDMA ("ecstasy"), methamphetamine, pemoline, phendimetrazine, phenethylamine ( PEA), phentermine, propylhexedrine, pseudoephedrine, phenylephrine, . - Serotonin, norepinephrine and/or dopamine precursors: 5-HTP, L-phenylalanine, L-tyrosine. - Anesthetics used in surgery and dentistry of local and general action, in particular, containing adrenaline. There is no universal practice in dentistry regarding the use of MAO inhibitors such as phenelzine, which is why it is important to inform all physicians, especially dentists, of the potential effect of MAO inhibitors in local anesthesia. In preparation for dental procedures it is desirable to stop taking phenelzine, however, given that it takes two weeks to stop, this option is not always desirable or practical. Dentists using local anesthesia, a non-epinephrine based anesthetic such as 3% carbocaine is recommended. Particular attention during the procedure should be paid to blood pressure. The anesthetic level must be replenished regularly and correctly, as non-adrenaline-based anesthetics take longer to act and wear off more quickly. Patients taking phenelzine should notify their psychiatrists before starting any dental treatment. - Some other supplements: Hypericum perforatum (St. John's wort), inositol, Rhodiola rosea, S-adenosyl-L-methionine (SAME), . - Other monoamine oxidase inhibitors.

Story

The heyday of the popularity of the IMAO falls for the most part during the period from 1957 to 1970. The initial popularity of "classic" non-selective irreversible MAO inhibitors has waned due to the presence of dangerous interactions of these drugs with sympathomimetic drugs and products containing tyramine, which can lead to the development of a hypertensive crisis. As a result, physician use of the previous generation of MAOIs has declined. When scientists discovered that there were two different MAO enzymes (MAO-A and MAO-B), they developed selective compounds for MAO-B, such as selegiline, which is used to treat Parkinson's disease, to reduce side effects and serious drug interactions. . Further improvement has come with the development of compounds (moclobemide and toloxatone) that are not only selective but also cause reversible MAO-A inhibition and have a reduced rate of dietary and drug interactions. Irreversible MAO inhibitors are the first antidepressants discovered, but their popularity has declined with the emergence of safe antidepressants; this new class antidepressants have fewer side effects, especially the dangerous irreversible interaction of MAOIs with food containing tyramine, sometimes called "cheese syndrome", leading to the development of severe hypertension. However, reversible MAO inhibitors do not have these adverse hypertensive effects. Moclobemide was the first reversible MAO-A inhibitor introduced to the public. clinical practice. Its features as a reversible inhibitor give it a number of advantages over the previous generation of irreversible MAOIs. On February 28, 2006, the US FDA approved a transdermal MAOI formulation of selegiline called Emsam for the treatment of depression.

List of MAOIs

Mentions in culture

In the episode "The Late Shaft" of the detective TV drama The Castle, Bobby Mann was taking MAO inhibitors. His killer used this fact to call negative interaction with the drug, which led to Bobby's death, which looked like a normal heart attack. In the Law & Order episode "Cut", a surgeon puts a patient on painkillers that interact with the MAO inhibitors she is taking, resulting in her death. The pilot episode "Law & Order" was based on a true story. Journalist Sidney Sione questioned the sudden death of his daughter Libby Sione in a Manhattan emergency room on October 4, 1984. The cause of death was listed as a "mysterious infection". The father persuaded the authorities to open a criminal case. This was done after it was discovered that his daughter had taken certain medications before her death, including Demerol, which reacted with Nardil, which the victim was taking. The district attorney brought a murder charge against a doctor who approved the use of special equipment and drugs on Libby. This case has led to many reforms in medical education and restrictions on the number of working hours for medical staff. As a result, it turned out that the main cause of death was drug abuse.