Side effects of irreversible MAO inhibitors. MAO inhibitors: pharmacological properties and trade names. Stress drives progress

Hi all! Today you will learn a terrible spell in medicine! It is so strong that it can kill a person, so this 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, it is dangerous and can only be used by the best specialists in the field of biology.

Agree, sometimes you want to read something unusual, in the style of “”, with the goal of “finding out” and, perhaps, telling your friends. You can check it out, after graduation there will be something to talk about, or at least think about. Even the title of the topic: “MAO inhibitors” sounds pretty good.

What do inhibitors mean?

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

To make it easier to understand, remember your feelings from the games. When you “win”, processes associated with , and serotonin are activated, but, for example, GABA is suppressed. Feeling of pleasure and happiness, and suppression of calm and prudence.

So, when we activate something, we suppress something and vice versa. It's a 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 transmitters into the synaptic cleft, into the space from where they are absorbed by the 2nd neuron. While the transmitters are in neither the first nor the second neuron, in the middle, the smart body selects their excess with the help of the enzyme monoamine oxidase.

This word just sounds scary, let's break it down into parts: “mono” means one, “amine” implies 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. And monoamines are neurotransmitters.

- monoamine oxidase, which destroys transmitters such as dopamine, norepinephrine and serotonin from the synaptic cleft and sends the excess back to the first neuron, for re-accumulation in vesicles and “shooting” into the 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, “extra 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 mitochondria in cells.

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

Monoamine oxidase inhibition refers to the process whereby the suppressors of monoamines are “inhibited.” As we remember from mathematics, minus by minus is a plus. Thus, similar processes occur in cells. By inhibiting monoamine oxidase, we destroy something that was meant to destroy something else.

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 drinking coffee, or, even worse, taking nootropics, will cause such rapid expression and the production of mediators that the effect of strong psychostimulant drugs will be obtained. Well, we understand how a person’s behavior changes under drugs.

Inhibitors are also divided into more or less “strong”; it is not a binary system where inhibition either occurs or not. It's more of a scale where 0 is no inhibition, and 100 is a 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 ones block both types.

Irreversible practically destroy MAO, forcing the body to launch 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 is becoming more or less clear to you. But non-selective ones are now almost never used.

Regarding application, then many antidepressants have selective reversible MAOIs. They act on serotonin and dopamine, temporarily increasing their levels in the synaptic cleft. Areas of application of irreversible are many diseases that are long-term or chronic, for example, chronic alcoholism, Parkinson's disease.

Relatively safe MAO inhibitors

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

Interesting facts

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

This syndrome was first noted in the 90s. 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 effect, 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 weak MAO activity are more prone to antisocial behavior in adulthood (Frazzetto G, Di Lorenzo G, Carola V).

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

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

Result:

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

— The body benefits from normal, average values ​​of MAO activity. If it is higher than the norm - a tendency to depression, lower - lower IQ and hot temper.

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

Well, I hope you liked the information! See you soon!

Content

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

What are MAO inhibitors

To understand which drugs are classified as MAO inhibitors, you need to know their pharmacological action. These medications have the ability to improve quality of life and combat anxiety. Another name for them is monoamine oxidase inhibitors (MAOIs). These are substances of plant and chemical origin, widely used in psychiatry.

The effect on the body is based on blocking the enzyme monoamine oxidase. As a result, the breakdown of various substances and neurotransmitters in the stomach is disrupted. Symptoms of depressive and mental disorders are mitigated. The entire list of drugs can be classified according to their pharmacological action.

Irreversible MAO inhibitors

Irreversible MAOIs include drugs whose principle of action is based on the formation of chemical bonds with monoamine oxidase. The result is suppression of enzyme functionality. These are first generation drugs with a lot of side effects. They have poor compatibility with other pharmacological agents. The patient must adhere to a diet during treatment. 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, and a diet is not necessary when taking them. The principle of operation of this group of medications 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 (Caroxazone, Incazan).

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. Concomitant use with medications that increase serotonin levels leads to the appearance of serotonin syndrome. This dangerous disease is a sign of intoxication of the body. To treat it, it is necessary to stop all antidepressants.

Non-selective MAO inhibitors

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

MAO inhibitors - list of medications

You can find out which drugs are classified as MAOIs and what can help in a particular case at a medical institution. The use of antidepressants must be agreed with your doctor. The doctor selects medications individually, based on the symptoms of the disease. The entire list of drugs is divided according to pharmacological classification. List of MAO inhibitors:

  1. Irreversible non-selective are: Phenelzine, Tranylcypromine, Isocarboxazid, Nialamid.
  2. The smallest is a list of representatives of irreversible selective ones: Selegiline, Rasagiline, Pargyline.
  3. Reversible selective ones are the most extensive group, these include the following drugs: Pirlindole (pyrazidol), Metralindole, Moclobemide, Befol, Tryptamine, beta-carboline derivatives (trade name Garmalin).

MAO inhibitors - instructions for use

Use of MAO inhibitors:

  1. Irreversible non-selective are used for treatment of:
  • involutional depressions;
  • neurotic depression;
  • cyclothymic depression;
  • in the treatment of chronic alcoholism.
  1. Irreversible selective ones are used only in the treatment of Parkinson's disease.
  1. Reversible selective use:
  • with melancholic syndrome;
  • for asthenoadynamic disorders;
  • with depressive syndrome.

Contraindications depend on the type of medicine. Irreversible, non-selective should not be used in the presence of cardiac, renal, liver failure, or coronary circulatory disorders. Irreversible selective ones are prohibited for use during pregnancy and breastfeeding and Huntington's chorea. They are not prescribed in combination with antipsychotic drugs. Contraindications to taking reversible selective drugs will be: infancy, acute liver failure.

Side effects when using a medicine that has a reversible selective effect will be expressed by the following symptoms: insomnia, periodic headaches, constipation, dry mouth, increased anxiety. If the recommended dosage is increased or patients do not comply with the treatment regimen, this drug increases the occurrence of side effects.

Taking non-selective irreversible MAOIs can cause the following side effects: dyspepsia, disruption of the gastrointestinal tract. Hypotension (low blood pressure) and headaches in the frontal part of the head are often observed. When taking reversible MAOIs, the list of negative effects increases: hypertension, decreased appetite, urinary retention, rash,.

Video: what applies to MAO inhibitors

Attention! The information presented in the article is for informational purposes only. The materials in the article do not encourage self-treatment. Only a qualified doctor can make a diagnosis and give treatment recommendations based on the individual characteristics of a particular patient.

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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, and phenylethylamine. These substances provide high performance, concentration, high spirits, and a stable emotional background.

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

Classification of drugs

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

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

Reversible MAOs combine with the enzyme, forming a single whole with it. Over time, this duet releases the necessary substances into the body, monoamines are captured and accumulated, and are excreted without damaging the enzyme.

Irreversible binds to monoamine oxidase. After this, 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 drugs capture both types.

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

MAO drugs

Pharmacological preparations of MAO are divided into only three types:

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

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

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

Irreversible selective: Selegiline, Rasagiline, Pargyline.

Each drug from the MAO group must be prescribed by a doctor and is available in pharmacies with a prescription.

To whom are they shown?

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

The similarity of MAOs to the effects of amphetamines puts them in the category of dangerous narcotic substances. Some drugs are addictive. Clinical studies have shown that MAO remove shyness and tightness; a person becomes more relaxed, sociable, and self-confident. People suffering from narcolepsy (pathological drowsiness) during use note an increase in periods of vigor and a decrease in fatigue.

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

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

The non-selective group is particularly different in the size of the list of side effects. At the same time as taking them, supportive therapy for the liver should be prescribed, and a diet should be followed with a limited number of foods.

How to take

The method of taking medications and the dosage are prescribed by the doctor, taking into account the symptoms, diagnosis, age, and illness of the patient. Most often, tablets of the required dosage of the substance are prescribed, one per day. At first, doctors recommend gradually entering therapy, taking half the dosage at a time to reduce side effects and prepare the body for changes in chemical composition.

Taking pills is not associated with eating food; you can wash them down with any liquid. The recommendation is to take it in the morning to avoid evening overexcitation and insomnia.

Do not take with other antidepressants; use sedative herbal tinctures with caution.

Simultaneous use of other psychotropic medications is possible only as prescribed by the attending physician.

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

Some experts believe that when taking antidepressants, it is necessary 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. Cheeses, 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 once a day, one or 0.5 tablets. For the first 2 weeks, 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 noticeable effect of the drug can be felt only after 7-14 days, when the concentration of the drug in the brain is at its maximum.

After treatment, which usually lasts from 3 to 9 months, your doctor may prescribe maintenance therapy to avoid withdrawal symptoms. It can last up to six months. Directions for use vary: it can be half or a quarter of a tablet; or take a whole tablet once every 2-3 days.

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

Contraindications for use

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

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

Taking MAO is not possible if:

  • severe liver diseases;
  • renal failure;
  • heart diseases with rhythm disturbances, changes in blood 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 biliary tract.

In addition to diseases and special conditions, simultaneous use with certain medications, such as:

  1. Amphetamines.
  2. A number of cold medicines: ephedrine, Coldrex, Theraflu, Rinza, Naphthyzin.
  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.

A number of clinical studies have proven the ineffectiveness of MAO in the treatment of all types of manic disorders. Substances only intensify manic states, anxiety, fear, and psychopathy.

Side effects

Non-selective MAOIs are considered to be the record holders for the number of side effects. Their use is accompanied by: constipation, migraine, dry mouth, decreased vision, edema, hepatitis, insomnia, tremors, delirium, hallucinations, changes in intracranial pressure.

Selective inhibitors have fewer side effects, including: urinary retention, dry mouth, tachycardia, and stomach discomfort. Less commonly – headaches, insomnia, dizziness, anxiety, restlessness, lack of appetite. Many patients note a decrease in sexual desire (libido) during use, the inability to achieve orgasm, and 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 and stroke. A serious reason for discontinuing medications is confusion, delirium, psychosis, hysteria, and suicidal thoughts.

Video: The Neon Channels feat. MAO inhibitors Almost Life in the Ozerova House

MAO inhibitors are antidepressants that are prescribed for the treatment of parkinsonism and epilepsy.

Pharmacological action

MAO inhibitor drugs are divided into the following groups: non-selective reversible, selective irreversible and selective reversible. 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 attacks, as well as improve the condition of patients in deep depression. These drugs are structurally similar to iproniazides.

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, Metralindole, Moclobemide, Pirlindol, beta-carboline derivatives.

Indications for use

MAO inhibitor drugs (reversible selective) should be taken for depression of various types, for melancholic syndrome, depressive syndrome, and asthenoadynamic disorders. Non-selective irreversible drugs should be prescribed to patients with neurotic, cyclothymic, involutional depression. The use of pharmaceuticals is also indicated for the treatment of chronic.

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

Contraindications

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

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

The drugs are not prescribed for alcohol withdrawal syndrome. It is strictly forbidden to take medications during pregnancy and lactation.

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

  • If the patient has increased sensitivity;
  • Liver failure was detected;
  • Cerebral circulation disorders are observed;
  • A diagnosis of chronic heart failure was made.

Taking MAO inhibitors (irreversible selective) is strictly contraindicated in patients taking other antidepressants. Also, medications in this category are not prescribed during pregnancy and breastfeeding, with Huntington's chorea, and essential tremor.

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

Video: Section title "Spiritual growth"

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

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, constipation and nausea may occur;
  • A small percentage of people experience urinary retention and painful urge to urinate;
  • When taking medications, shortness of breath, skin rash, and bronchospasm may occur.

When taking medications (irreversible selective), a person may experience hair loss and hypoglycemia.

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

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 iproniazides. They reduce the number of angina attacks and also lift a person out of depression.
  2. Selective reversible ones are aimed at suppressing the deamination of norepinephrine and serotonin. These medications have an antidepressant effect.
  3. Selective irreversible are used to treat parkinsonism. They are directly involved in the metabolism of catecholamines and dopamine.

MAO inhibitors - 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. Nialamid. This is an antidepressant. Fine white powder with a slight yellow tint. It dissolves poorly in water, and even worse in alcohol. The medicine is prohibited for people with liver, kidney, or heart problems. It is also undesirable for use by 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 overall condition. Mainly used as an antidepressant.
  5. Tranylcypromine. This medicine is also designed to combat depression. It is considered stimulating. In the active phase, the drug partially transforms into amphetamine. Some patients may become dependent on the stimulant effect.

List of selective reversible MAO inhibitor drugs

  1. Bethol. Considered an antidepressant. Has antireserpine effect. The potentiation effect of phenamine is provided.
  2. Maclobemid. A drug that is classified as an antidepressant. It is similar in composition to befol, but still has a difference in molecular structure. During use, dry mucous membranes, headaches, nausea, or, conversely, insomnia may appear. In some cases, constipation, stomach problems, muscle spasms and temporary blurred vision were observed. Patients with bipolar depression often experienced a phase change to manic.
  3. Pyrazidol. Its action is similar to incasan and tetrindole. It is an activating agent in people with apathetic depression. Has a sedative effect. Improves cognitive functions. It stands out among the rest due to the ability to regulate its effect on the nervous system.
  4. Incazan. Aka metralindol. It is considered an original drug. It is used for the development of schizophrenia, manic psychosis or for the treatment of vascular diseases of the brain. Indicated for adynamic and apathetic depression, lethargy, and conditions with poor hypochondriacal symptoms. Often used to treat depression in patients with alcoholism.

What drugs are classified as selective irreversible MAO inhibitors?

  1. Selegiline. A medicine whose action is aimed at treating Parkinson's disease and derivative syndromes caused by dopamine deficiency.
  2. Rasagiline. This medicine belongs to a new generation of drugs. It combats symptomatic parkinsonism, mainly minor motor impairment. Often used with other drugs in the group.