Non-selective MAO inhibitors. MAO inhibitors: pharmacological properties and trade names

MAO inhibitors are biologically active substances which enhance the transmission of nerve impulses. The drugs are aimed at treating certain nervous disorders, depression, and narcolepsy.

MAO inhibitors - what are they?

According to their pharmacological properties, these drugs are divided into several types:

  1. Non-selective irreversible - inhibitors that are very similar in composition to iproniazid. They reduce the number of angina attacks, and also take a person out of depression.
  2. Selective reversible ones are aimed at suppressing the deamination of norepinephrine and serotonin. These drugs have an antidepressant effect.
  3. Selective irreversibles are used to treat parkinsonism. They are directly involved in the metabolism of catecholamines and dopamine.

MAO inhibitors - a list of drugs

Non-selective irreversible drugs

  1. Ipronizad. A medicine that belongs to the group of antidepressants. It has a clear hepatotoxic effect - it harms the human liver.
  2. Nialamide. This is an antidepressant. Fine white powder with a slight yellow tint. It is poorly soluble in water, and in alcohol - even worse. The medicine is forbidden to be taken by people with problems of the liver, kidneys, heart. It is also undesirable for people with impaired cerebral circulation.
  3. Isocarboxazid. Often used to treat depression and narcolepsy. Like other drugs in the group, it can harm the liver, kidneys and heart.
  4. Phenelzine. It is taken to improve the condition in general. Mainly used as an antidepressant.
  5. Tranylcypromine. This medicine is also designed to fight depression. It is considered stimulating. In the active phase, the agent partially passes into amphetamine. Some patients may become dependent on the stimulant effect.

List of selective reversible MAO inhibitor drugs

  1. Befol. Considered an antidepressant. It has an anti-reserpine effect. The effect of potentiation of phenamine is provided.
  2. Maclobemide. A drug that belongs to antidepressants. In composition, it is similar to befol, but still has a difference in molecular structure. During the reception, dry mucous membranes, headaches, nausea, or vice versa, insomnia may appear. In some cases, constipation, stomach problems, muscle spasms and temporary visual impairment were observed. In patients with bipolar depression, a phase change to manic was often observed.
  3. Pyrazidol. Its action is similar to inkazan and tetrindol. It is an activating agent in people with apathetic depressions. Has a sedative effect. Improves cognitive functions. It stands out from the rest due to the possibility of regulating the effect on the nervous system.
  4. Inkazan. He is metrolindol. It is considered the original drug. It is used in the development of schizophrenia, manic psychosis or for the treatment vascular diseases brain. It is indicated for adynamic and apathetic depressions, lethargy, conditions with poor hypochondriacal symptoms. Often used to treat depression in alcoholics.

What drugs are selective irreversible MAO inhibitors?

  1. Selegilin. A medicine whose action is aimed at treating Parkinson's disease and derivative syndromes caused by a lack of dopamine.
  2. Razagilin. This medicine belongs to a new generation of drugs. It fights symptomatic parkinsonism, mainly with minor motor impairments. Often used with other drugs of the group.

Video: The Neon Channels feat. MAO Inhibitors Almost Life in the Ozerov House

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 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.

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, severe psychosis, prostatic hyperplasia, angle-closure, large-scale tremor, peptic ulcer of the gastrointestinal tract, tardive dyskinesia, diffuse toxic goiter, and also pheochromocytoma.

Side effects

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

Video: Header of the section "Spiritual Growth"

When using non-selective irreversible medicines 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.

MAO inhibitors are considered to be a group of antidepressants that increase the concentration of “good mood” hormones in the blood. The drugs are aimed at slowing down the breakdown of monoaminooxidase, thereby increasing the amount of serotonin, norepinephrine, dopamine, tryptamines, phenylethylamine. These substances provide high performance, concentration, high spirits, stable emotional background.

MAO inhibitors are available in synthetic tablet form and are also found in some natural substances. They are prescribed for the treatment of panic attacks, depression, narcolepsy.

Classification of drugs

Pharmacists divide MAO preparations according to their effects into 4 types:

  1. Reversible.
  2. Irreversible.
  3. Selective.
  4. Non-selective.

Reversible MAO combine with the enzyme, forming a single whole with it. This duet releases the necessary substances into the body over time, the capture and accumulation of monoamines occurs, and is excreted without damaging the enzyme.

Irreversible attaches to monoamine oxidase. After that, the natural organic enzyme is not produced, a new substance is synthesized. These drugs begin to act only after 2 weeks.

Selective drugs capture only one type of MAO, non-selective - both types.

All types of drugs are aimed at reducing anxiety disorders, improving mood, relieving symptoms of depression.

MAO preparations

Pharmacological preparations of MAO are divided into only three types:

  1. Non-selective irreversible. This is a group of drugs of the first generation with a large list of contraindications and side effects. Their high toxicity destroys the function of the liver, heart, causes nausea. When taking it, you must additionally adhere to a diet. The admission period is strictly limited.
  2. Reversible selective. Second generation drugs. They are prescribed for depression, social phobia, apathy. Inhibitors are mainly aimed at the capture of serotonin. Widely used by psychiatrists for nervous disorders. They have a withdrawal syndrome.
  3. Irreversible selective. Designed for the treatment of more severe diseases of the central nervous system, such as Parkinson's disease. Substances of drugs are involved in the metabolism of dopamine. Does not affect the work of the heart, can reduce blood pressure in hypertensive patients.

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

Widely known reversible selective drugs: Inkazan, Befol, Pyrazidol, Moclobemide.

Irreversible selective: Selegiline, Rasagiline, Pargiline.

Each drug from the MAO group must be prescribed by a doctor, dispensed in pharmacies with a prescription.

Who are shown

MAO drugs are prescribed for clinical depression, anxiety disorders, catalepsy, Parkinson's disease, Alzheimer's, withdrawal (alcohol) syndrome, panic attacks, VVD, schizophrenia. In recent years, they have been widely used to reduce social phobia, increase efficiency by regulating sleep, and in all forms of depression. Some people use antidepressants for weight loss.

The similarity of MAO with the action of amphetamines put them in the category of narcotic dangerous substances. Some drugs are addictive. Clinical studies have shown that MAO removes shyness, tightness; a person becomes more liberated, sociable, self-confident. People suffering from narcolepsy (pathological drowsiness) during the reception note an increase in periods of vigor, a decrease in fatigue.

However, these drugs can only be used as directed by a neurologist or psychiatrist. Only a specialist will be able to determine exactly which medicine will be most effective and how long it will take.

Improper intake of tablets can lead to chronic insomnia, anxiety, tachycardia, hand tremors, anorexia, hypertensive crisis, hypotension.

The non-selective group is particularly distinguished by the size of the list of side effects. Simultaneously with their intake, supportive therapy for the liver should be prescribed, a diet with a restriction of a number of products should be followed.

How to use

The method of taking drugs, the dosage is prescribed by the doctor, taking into account the symptoms, diagnosis, age, and diseases of the patient. Most often, tablets of the desired dosage of the substance are prescribed, one per day. At first, doctors recommend smoothly entering therapy, taking half the dosage in order to reduce side effects, and prepare the body for a change in the chemical composition.

Taking pills is not associated with eating, you can drink them with any liquid. The recommendation is to take it in the morning to avoid evening overexcitation, insomnia.

Do not take with other antidepressants, be careful to drink sedative herbal tinctures.

Simultaneous reception of other psychotropic drugs is possible only as prescribed by the attending physician.

  • a ban on alcohol;
  • restriction of caffeine and cola for those who have a stimulating effect;
  • reduce the amount of chocolate consumed;
  • morning reception;
  • dosage compliance.

Some experts believe that when taking antidepressants, it is imperative to follow a diet, limiting yourself in certain foods or completely eliminating them from the diet. Here is a list of "forbidden" foods:

  1. Wine, beer, liquor.
  2. Sausages, smoked meats, salami, pates.
  3. Ice cream, especially with sweet syrups.
  4. Cheese, milk, sour cream, cream.
  5. Herring, dried, pickled, smoked fish.
  6. Meat broths, sauces, marinades.
  7. Brewer's and baker's yeast.
  8. Legumes: beans, peas, soybeans, lentils.
  9. Spices, cookies, chocolate.

Medicines of the MAO group are taken 1 time per day, one or 0.5 tablets. The first 2 weeks of treatment begins with ½ of the full dosage. Exit from therapy should also be at reduced doses for two weeks to a month.

The first tangible effect of the drug can be felt only after 7-14 days, when the concentration of the drug in the brain is the maximum value.

After treatment, which usually lasts from 3 to 9 months, maintenance therapy may be prescribed by the doctor to avoid withdrawal symptoms. It can last up to six months. Methods of application vary: it can be half or a quarter of a tablet; or taking a whole tablet 1 time in 2-3 days.

With extreme caution, MAO is prescribed to adolescent children, the elderly, patients with heart, liver, and kidney diseases.

Contraindications for use

MAO active substances should not be taken by people suffering from kidney, heart, liver failure, diabetes, atherosclerosis; suffered from severe hepatitis, heart attacks, strokes.

Reception is prohibited for children under 14 years of age, during pregnancy and lactation.

Reception of MAO is not possible with:

  • severe liver disease;
  • renal failure;
  • heart diseases with rhythm disturbance, changes in the vessels;
  • after hemorrhagic stroke;
  • severe alcoholism;
  • taking other antidepressants;
  • manic states;
  • suicidal tendencies.

It is prescribed with caution:

  • with nodular goiter;
  • tachycardia;
  • psychoses accompanied by hysteria, overexcitation;
  • multiple sclerosis, age-related dementia;
  • obstruction of the bile ducts.

In addition to diseases and special conditions, contraindications are concomitant use with certain medicines, such as:

  1. Amphetamines.
  2. A number of cold medicines: ephedrine, coldrex, teraflu, rinza, naphthyzinum.
  3. All drugs for weight loss.
  4. St. John's wort, eleutherococcus, ginseng, Rhodiola rosea.
  5. Adrenalin.
  6. Diuretics.
  7. Barbiturates, sleeping pills.
  8. Antihistamines.

Row clinical research proved the ineffectiveness of MAO in the treatment of all types of manic disorders. Substances only increase manic states, anxiety, fear, psychopathy.

Side effects

Record holders in quantity side effects are considered non-selective MAOs. Their intake is accompanied by: constipation, migraine, dry mouth, decreased vision, edema, hepatitis, insomnia, tremor, delirium, hallucinations, changes in intracranial pressure.

Selective inhibitors have fewer side effects, including urinary retention, dry mouth, tachycardia, and stomach discomfort. Less often - headaches, insomnia, dizziness, anxiety, restlessness, lack of appetite. Many patients note a decrease in sexual desire (libido) during the reception, the inability to achieve orgasm, a decrease in their brightness. Men may not ejaculate. After the end of the reception, everything is restored.

In elderly patients, MAO inhibitors can cause hypertensive crisis, stroke. A serious reason for discontinuation of drugs is confusion, delirium, psychosis, hysteria, suicidal thoughts.

Currently, due to the increase in the level of stress factors, many are interested in how medication can reduce anxiety, strengthen disturbed sleep and stabilize their condition.

Among pharmaceutical products over-the-counter medications, there are often drugs recommended as antidepressants, but they are mostly homeopathic preparations that do not provide full assistance in some cases.

Paintings of depression

Before getting carried away with MAO inhibitors, drugs should be thoroughly studied or consult a doctor. Drugs of the "antidepressants" group can affect many functions of the body: the above-mentioned MAO (monoamine oxidase) inhibitors have a wide range of side effects, which will be discussed below. But even earlier, you should realize whether the body requires such intervention, or is it just a whim caused by a desire to make certain moments of your life easier. Most people on Earth have experienced depressive states, and their presence is due to the need for stress.

Many authoritative works of our contemporaries and predecessors have been written about the benefits of moderate stress. In most cases, the negative perception of stress is due to advertising of antidepressants, which suggests that consumers get rid of it as an unnecessary thing that spoils our lives, as “slags and toxins”, so to speak ...

Stress drives progress

However, stressful conditions serve as a kind of motor that helps a person to experience and feel the “black stripes” of his life, so that he can see the “white ones”. If there were no darkness, we would not know what light is (F. Aquinas). If there was no stress, no one would feel calm. But, in addition to the theosophical, stress has a completely scientifically based physiological background. Stress improves immunity, stimulates the regenerative abilities of the body, improves memory and increases endurance. These facts are scientifically proven. Therefore, before using antidepressants, drugs - MAO inhibitors, it is necessary to determine how necessary they are in a given situation.

Drugs and MAOIs)

The favorite among over-the-counter drugs that are weak MAOIs is St. John's wort. This plant has been studied for centuries, unlike new drugs, more studied. It is the main component of such popular drugs as Negrustin, Deprim.

More cheap analogue- alcohol, which is the least convenient in everyday use, but excludes the presence of additives, which in some cases may manifest the effects of individual intolerance.

Valerian. It is also the basis for the preparation of many dosage forms. Does not belong to the group "MAO inhibitors". The list of drugs from the group of selective and non-selective monoamine oxidase inhibitors, contrary to popular belief, does not include valerian as an auxiliary drug - due to incompatibility. Like St. John's wort, valerian is a drug with a balanced natural biochemical composition and is sold in pharmacies without a prescription.

Motherwort. Certain types of this plant are used not only in neurology, but also in general therapy and cardiology. Motherwort-based tinctures have a calming and tonic effect when used regularly. Medicinal collections based on motherwort serve as the basis for herbal teas, and its extract in combination with eucalyptus is effective tool for inhalation.

Synthetic drugs

Non-herbal preparations have a shorter history, and the treatment experience of the "pioneers from the 50s" was very questionable. However, due to the spasmodic development of the pharmaceutical industry, the drug market currently offers a fairly wide range of drugs that are more effective than herbal drugs.

MAO inhibitors have become a big leap in the treatment of mental disorders and borderline depressive states. The list of drugs in this group includes 145 trade names.

How MAOIs work

The principle of action of drugs in this group is based on slowing down the destruction of one or more groups of monoamines and increasing the concentration of certain mediators between two synapses. These mediators include norepinephrine, others. In the future, by increasing the concentration of a certain mediator, the desired therapeutic effect is achieved. The question of what belongs to selective MAO inhibitors and what to non-selective ones is solved by a simple formulation. If the drug stimulates an increase in the concentration of one mediator, then it is considered selective. If several - then indiscriminate, respectively.

What are MAO inhibitors: a list of requirements and precautions for the use of drugs in this group due to the possibility of side effects

1. Obligatory intervention of a doctor. Preparations of this group, with the exception of drugs of plant origin, for the most part belong to the group of drugs dispensed only by prescription. And for good reason (see next paragraph).

2. Accurate dosage. Taking drugs of this group should be carried out regularly and in certain doses, taking into account the physiological characteristics of the body. You can not take these drugs, based on the principle "I'm more nervous - I drink more pills." The effect of an overdose can be diametrically opposed to what is expected. Recently, unconscious poisoning with MAO inhibitors is often observed.

Drugs are taken in large doses in a domestic environment in order to "calm down". And, sadly, it is not uncommon for people to calm down forever.

3. Differentiation with the type of human activity. In all instructions for drugs of this group, the column “with caution” is indicated and a group of people is named for which taking drugs in connection with the performance of a certain work is incompatible or incompatible. Antidepressants of this group can affect the reaction rate, which can have a deplorable effect on the work of drivers, pilots, and law enforcement officers. The presence in the blood and urine of residual enzymes of drugs of this group can show positive results in athletes (like doping).

4. The principle of calculating the side effect common to the MAOI group. Drugs of this group can cause mental and somatic disorders. On the part of the psyche - lethargy, fatigue, withdrawal syndrome. In difficult cases - exacerbation of schizophrenia, suicidal tendencies. From the side of somatics: violation of blood pressure, a negative effect on parenchymal organs (liver, kidneys).

MAO inhibitors. List of drugs commonly used in the practice of neurologists and psychiatrists

Table-list of drugs with notes
A drugViewIndicationsNote
Aurorixreversible MAOIdepression various etiologies, social phobiaUndemanding to diet. Trade name of the active substance maclobenide
pyrazidolElectoral MAOIDepression of various origins, b. Alzheimer'sDomestic drug at an affordable price
befolMinor depression, hypochondriaDomestic drug
InkazanSelective reversible MAOIDepression of various origins. Schizophrenia, manic-depressive psychosesAlso known as metrailindol
SelegelinElectoral MAOIParkinson's disease, polyetiological parkinsonian syndromes (excluding drug)Synergy with Levodopa

These drugs are the most commonly used in practice due to their high efficiency and predictable therapeutic effect. These are the most profitable drugs in terms of price / effectiveness among the group of "MAO inhibitors". The list of drugs with similar and similar effects and other commercial names is more extensive, since the domestic market is supplied with products from 43 pharmaceutical manufacturers, and many drugs are generics.

conclusions

However, the price / quality duet should include the third element, which many consider "third wheel". Fully determine which antidepressant drug is suitable certain person only a doctor can. And to decide what place depression takes in a person's life, whether he will be happy or not, only he himself can.

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 - 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 quick look at each group and learn about active substances, properties and trade names.

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

Table 1

Active substance Short description Tradename
1. Iproniazid It has a pronounced hepatotoxic effect. In this regard, it is used and appointed very rarely. Apply no more than 2 weeks. "Iprazid"
2. Nialamide The chemical structure is similar to iproniazid, but has a more gentle toxic effect. Improves general condition and helps to recover from depression. The appearance of a therapeutic effect is observed after 1-2 weeks. "Nialamid"
3. Isocarboxazid Activates some natural components in the brain to maintain mental balance. "Marplan"
4. Phenelzine It is prescribed to reduce depression. Reduces anxiety and anxiety. "Nardil"
5. Tranylcypromine Recommended during treatment mental illness that develop against the background of depression. Has a stimulating effect. May be metabolized to amphetamine. "Parnat"

Reversible selective MAO-A inhibitors

table 2

Active substance Short description Tradename
1. Moclobemide It is prescribed for depression, as well as social phobia. Blocks the destruction of norepinephrine and serotonin. "Aurorix"
2. pyrazidol It has a therapeutic effect in patients with apathetic attacks and depressive disorders. It is also prescribed for agitation - strong emotional arousal, which is manifested by a feeling of anxiety and fear. The drug is widely used in psychiatric practice. "Pirlindol"
3. befol Indications: depressive syndrome, anxiety and delusional disorders, hallucinations. With alcoholism: asthenosubdepressive syndrome. "Befol"
4. Inkazan Pharmacological properties are similar to pyrazidol. Activates norepinephrine and serotonin in the central nervous system. Widely used in mental disorders: schizophrenia, manic-depressive psychosis, mood swings, as well as to improve blood circulation in the brain. In the treatment of alcoholism, the drug is recommended to be taken in the period of remission. "Metralindol"
5. Derivatives of beta-carbolines The β-carboline backbone is the main structure for many alkaloids that are isolated from plant components. Medicines containing this substance can be used in the fight against alcoholism and depression. Derivatives are also used in antiviral, antibacterial and antitumor therapy. In addition, active compounds help in the fight against rheumatoid arthritis, osteoarthritis, bronchial asthma. Garman, Garmin

Irreversible selective MAO-B

Table 3

Active substance Short description Tradename
1. Selegiline Pharmacological group: antiparkinsonian agent. Selegin is involved in the metabolism of dopamine (inhibits). Thus, there is an increase in the neurotransmitter in various parts of the brain. The time for which the enzyme is restored is 2 weeks. Umeks, Stillin
2. Rasagiline Antiparkinsonian drug. It is recommended for the treatment of true Parkinson's disease, as well as in the presence of symptoms that indicate this pathology. The tool has an effect due to the accumulation of special natural compounds in the brain. The drug is taken according to the scheme; sudden withdrawal or a sharp increase in dose can lead to serious consequences. "Azilect"
3. Pargylin Antidepressant, recommended for mental and nervous disorders. In combination with the drug Meticlothiazide may lower blood pressure. "Pargilin"

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.