Mao blockers. MoA inhibitors: what it is, a list of drugs and their trade names

Monoaminoxidase inhibitors (IMAO, MAOI) - biologically active substances that can inhibit the monoaminoxidase enzyme contained in the nerve endings, preventing the destruction of various monoamines (serotonin, norepinerenaline, dopamine, phenylethylamine, triptamins, octopamine) and thereby contributing to the increase in their concentration in the synaptic slit.

Monoaminoxidase inhibitors include some antidepressants, as well as a number of natural substances.

IMAO classification

According to its pharmacological properties, monoaminoxidase inhibitors are divided into reversible and irreversible, selective and non-selective.

Selective imoo inhibit mainly any one of the types of MAO, non-selective - both types (mao-a and mao-b).

Unpaid IMAO interact with monoaminoxidase, forming chemical bonds with it. The enzyme after this turns out to be unable to perform its functions and is metabolized, and instead the organism is synthesized by a new one, which usually takes about two weeks.

Reversible Imao, binding to the active center of the enzyme, form a relatively stable complex with it. This complex is gradually dissociable, releaseing IMAO, which further enters the blood and is excreted from the body, leaving the enzyme intact.

Non-selective irreversible imoo

• IPRONIZID
• Niamid.
• Isocarboxazid
• Phenelzin
• Tralylsipromin

Strictly speaking, to attract the tralylsipromine to this group is not entirely correct, as it is a reversible inhibitor, however, on the dissociation of its complex with an enzyme and its full removal from the body may be needed to 30 days. In addition, it exhibits some selectivity towards Mao-A.

Currently, non-selective Mao inhibitors are rarely used. This is due to their high toxicity. Unlike most other non-selective IMAO, it is not at all used by the IProniazide, currently universally filmed from production due to high hepatotoxicity; In many countries, for the same reason also removed from the production of isocarboxazid.

Anonyazide is also clinically significant activity, historically the first IMAO: it is the euphorizing effect of isoniazide, observed in tuberculosis patients, led to the discovery of monoaminoxidase inhibitors. Due to its significant hepatotoxicity and ability to cause pyridoxidoxine polyneuropathy, itoniazid has ceased to be applied as an IMAO, with the exception of its use of off-label in high doses in combination with high doses of vitamin B6 in countries where other hydrazine IMAOs are not available.

Reversible selective inhibitors of Mao-A

• Moklobmeoid
• Porlindol (pyrazidol)
• Befol.
• Metraldol.
• Harmalin
• Derivatives of beta carbolins

Irreversible selective inhibitors of Mao-B

• SELEGINE
• Razgilin
• Pargilin

The division on Imao-A and Imao-B partly conditionally, since in high doses imoo-b loss the selectivity and begin to block Mao-A, and imoo-a in high doses (exceeding the maximum recommended doses recommended in the instructions) significantly block Mao-B . The division of irreversible and reversible MAO is also in some extent conditionally: completely irreversible IMAO are only hydrazine derivatives - niamid, phenelzine, isocarboxazide, and irony. Tralylsipromine and Selegylin are partly reversible: after the cessation of their reception of monoaminoxidase is restored not after 2 weeks, as after stopping the reception of hydrazine IMAO, and after 5-7 days.

SELEGINLIN and RAGILILLY are officially registered in Russia only for the treatment of Parkinson's disease. The antidepressive effect of selegyline during monotherapy is observed only in high doses when it loses the selective action. However, in the quality of potentiation means, selegylin and zealille can be used in selective mao-b dosages in which they act as dopaminergic agents.

Traniltsipromin and SELEGILIN in the body are substantially metabolized into amphetamine, with which their strong stimulating activity is associated with a partly.

Therapeutic action

IMAO, blocking the destruction of monoamines by monoaminoxidase, increase the content of one or more media monoamines (norenine, serotonin, dopamine, phenylethylamine, etc.) in the synaptic slit and enhance the monoaminergic (monoamine-mediated) transmission of nerve pulses (neurotransmission). For this reason, for medical purposes, these substances are used mainly as antidepressants. IMAO-B is also used in the treatment of Parkinsonism and Narcolepsy.

Side effects

Non-selective inhibitors

Basic undesirable effect is an ortostatic hypotension, which is observed in almost all patients taking these drugs, while a hypertensive reaction as a result of the interaction of Mao inhibitors with products or drugs capable of provoking hypertensive crisis, it is rare.

Non-selective Mao inhibitors possess large number side effects. These include dizziness, headache, urination delay, constipation, fatigue, dry mouth, fuzzy vision, skin rashes, anorexia, paresthesia, feet, convulsive epileptiform seizures, hepatitis. In addition, due to a pronounced psychostimulating effect, these drugs can cause Euphoria, insomnia, tremor, hypomanic assessment; Due to the accumulation of dopamine - nonsense, hallucinations and others mental violations. The development of Korsakovsky syndrome is possible. The reception of non-selective inhibitors of Mao often leads to sexual side effects, such as a decrease in libido, erectile dysfunction, orgasm delay or its absence, delayed ejaculation or its absence.

Like other antidepressants, IMAO can provoke a manic episode in patients who have the appropriate predisposition. IMAO more often cause manic episodes than some other antidepressants, and for this reason they are not the preparations of choice in the treatment of depressive episodes with the presence of preceding manic.

The ironymide has a pronounced hepatotoxic effect, which predetermines its unsuitability for widespread use in psychiatry. Phenlaylzine is less toxic for the liver compared to the ironiazide, but its frequent side effects are hypotension and sleep disorders, and the isocarboxeside can be used in cases where patients are well treatable with phenylsine, but suffer from these side effects.

Tranyltsipromin differs from other imao combination of ability to inhibit Mao and amphetami-like stimulating action; This drug is partially metabolized into amphetamine. Some patients become dependent on the stimulating effect of trahnibromine. Compared to Phenlaylzin, it can more often provoke hypertensive crises, but less affects the liver. According to the reasons, Traniltsipromin should be prescribed with great care.

Selective inhibitors

Used wider, as they give much smaller side effects. Possible side effects include non-terrible dry dryness, urine delay, tachycardia, dyspeptic phenomena; In rare cases, dizziness are possible, headache, anxiety, anxiety, tremor hands. Skin allergic reactions may also occur.

Interaction

The combination of monoaminoxidase inhibitors with substances affecting monoamines can lead to an unpredictable strengthening of their action and be life-threatening.

Food incompatible with imao

Significant danger when using IMAO, especially non-selective irreversible imooRepresents the use of food containing various monoamines and their metabolic precursors. First of all, it is Tiramine and its metabolic predecessor of the amino acid Tyrosine, as well as tryptophan. Tiramine, similar to amphetamine psychostimulants, causes the release of catecholamines from nerve endings. Its joint with IMAO is welcome with a hypertensive crisis (see Tiramine Syndrome).

Triptophan is used by the organism to produce serotonin, and the use of products containing a large amount of its amount may entail a serotonin syndrome.

Foods that should be avoided:

• All cheeses other than fresh home cheese (cottage cheese), especially sharp and weathered; milk, cream, sour cream, kefir
• Ice cream with syrup
• Red wine, beer containing yeast (crude), El, liqueles, whiskey
• Smoked, salami, chicken and beef liver, chicken pate, meat broths, marinades, any products made of stubble meat, roasted poultry and roasted game
• Caviar, smoked fish, herring (dried or salty), dried fish, pate of shrimp, pickled fish (fresh fish relatively safe)
• Extracts of yeast and beer yeast (ordinary bakery yeast safe)
• Protein additives
• Beans (beans, lentils, beans, soy), soy juice
• Sauerkraut
• Overripe fruit, canned figs, bananas, avocado, raisins
• Spicy
• All kinds of cookies

Products to which should be treated with caution:

• White Wine, Portwine
• Strong alcoholic beverages (danger of oppression of the respiratory center)
• Some fruits, such as figs, prunes, raspberries, pineapple, coconut
• Equality products (Prostokvasha, Yogurt, etc.)
• Chocolate
• Soy sauce
• Peanut
• Caffeine, Theobromin, Teophylline (Coffee, Tea, Mate, Coca-Cola)
• Spinach

Irreversible non-selective IMAOs require the refusal of these products and the drugs mentioned below narcotic drugs During their reception and within two weeks after the end of the reception. In the case of reversible IMAO, the diet restrictions are usually less strict and distributed for a while until the substance is maintained in the body (no more than a day). From use together with reversible IMAO drugs and the surfactants listed in the list, should also be refracted to fully eliminate them.

Interaction with medicinal and narcotic drugs

To prevent Tiramin syndrome and serotonin syndrome, it is necessary to avoid applications during the IMAO therapy of the following tools:

• The amphetamine group psychostimulants and related to them are the increase in the levels of catecholamines in the synaptic slit (amphetamine, methamphetamine, sedokarb, etc.)
• Any empathogens (enticctogens)
• Tools from colds containing sympathomimetics (ephedrine, pseudoephedrine, phenylpropanolamine, phenylephrine, chlorophenyramine, oxymethazoline, etc.): Koldrex, teraflu, rhines, etc., sprays and drops for nasal (naphtizin, etc.)
• Means for weight loss
• Oral hypoglycemic products
• Inhibitors of the reverse neural capture of monoamines:
  • Cocaine
  • Cyclic antidepressants, including clomipramine, imipramine
  • Selective inhibitors reverse grip Serotonin (SSIRS), for example, paroxetine, cytalopram, fluoxetine
  • Venlafaxin
  • Trazodon, nefazodon
• Vegetable antidepressant agents containing St.
• 5-hydroxytriptophan, tryptophan
• Lithium preparations
• Dextromethorphan (DCM)
• Metabolic precursors monoamines: levodopa, methyldop, 5-hydroxytriptophan
• Hypotensive drugs (Guanethidine, reserpine, pargalin)
• Adrenaline and local anesthetics containing adrenaline (Lidocaine and Novocain harmless)
• Antioapmatic drugs
• Diuretics
• Beta blockers
• Antihistamines
• Barbiturates
• Anticholinergic drugs
• Narcotic analgesics.
• Alcohol.

After the abolition of fluoxetine before appointing an irreversible IMAO, it is necessary to withstand a gap of at least five weeks to prevent serotonin syndrome. In the elderly patients, this gap should be at least eight weeks. After the abolition of SOSIs short action Before appointment, IMAO should have a break for at least two weeks.

When translated from irreversible IMAO, the SIRES should be withstanding for four weeks; When transferring from Moklobemide to SSIRS enough 24 hours.

The probability of the development of serotonin syndrome in the interaction of SEELS with selenium or moklobemide is significantly lower compared to the risk of its occurrence, with a combination of SSIRS with non-selective irreversible IMAO, but still the interaction of this kind is not excluded. Serotonin syndrome was also observed with Moklobemide monotherapy.

Unpaid IMAO is undesirable to combine with hypotensive drugs due to the risk of severe orthostatic hypotension, or should be reduced by the dose of the hypotensive preparation.

Imao enhances the effect of alcohol, sedative and anxiolytic agents, as well as painkillers, sometimes deriving the effect of these drugs.

IMAO can complicate procedures related to anesthesia or analgesia, as they interact with narcotic substances, causing syndrome, manifested by a fitting, fever, headaches, convulsions, a coma with the possibility of a deadly outcome. They may be the reason for the oppression of breathing. Female outcomes were observed when using meperidine. Patients who have to have an operation should be reduced in advance to the dose of Mao inhibitors in order to exclude unwanted reactions to medicines.

In patients with diabetes, taking insulin, a sharper decrease in sugar levels may occur. In this case, the insulin dose can be reduced.

Restrictions on application

The presence of an irreversible IMAO of the hypotensive effect and the ability to provoke an orthostatic hypotension makes their use in patients with initial hypotension and a tendency to faint, in elderly patients with severe cerebral atherosclerosis, with pronounced cerebral atherosclerosis arterial hypertensionWhen dangerously a sharp decrease in blood pressure.

Precautions

In case of sudden change, the position of the body may arise a sense of instability. This can be avoided if you rise from the horizontal position slowly. If the pills are accepted while eating, this one and others sideflines expressed much weaker.

Care should be taken when servicing mechanisms and when managing the machine, since many patients in the initial period of treatment of IMAO are prone to high drowsiness.

Non-medical use

There are a number of messages about the abuse of Mao inhibitors. The abuse mechanism may be due to the similarity of the chemical structure of the IMAO with the chemical structure of amphetamine; However, the mechanism of action of the IMAO and amphetamine differ significantly. Persons who abuse IMAO can be particularly inclined to develop hypertensive crises, as they use high doses of IMAO and / or may not be aware of the recommended diet.

Interaction with phenylethylamine and triptamine psychedelic

Most tryptamins are good substrates for Mao-A. DMT and 5-meo-dmt with oral reception It is metabolized by it already in the gastrointestinal tract and liver, not to get into the blood, so they are inactive for oral administration. 4-hydroxy-DMT (psilocin) is less susceptible to degradation by Mao, since its hydroxyl group in the 4th position makes it difficult to bind to the active center of the enzyme, as a result of which it turns out to be orally active. Alkyl substituents on the amino group, more voluminous than methyl (ethyl, propyl, cyclopropyl, isopropyl, allyl, etc.), also make it difficult to the metabolism of tryptamins with such substituents through Mao, therefore all such tripartamins are active in oral use. Alpha-methyl in triptamine molecules like AMT and 5-Meo-AMT significantly makes it difficult to make their metabolism through Mao and turns them de facto from substrates into weak inhibitors of this enzyme.

Inhibition of peripheral mao-A in the gastrointestinal tract and liver strong IMAO allows you to make such tripartamins as DMT and 5-mero-DMT, orally active, and in addition, to strengthen and extend the effect of other tripartamins, such as psilotsin and Det. On the other hand, the long-lasting intake of the IMAO as antidepressants weakens the effect of psychedelics. This happens, obviously, due to changes in monoaminergic brain systems caused by increased level monoamines. The nature of this phenomenon is currently unclear and does not explain the simple loss of sensitivity of serotonin receptors, with which psychedelics interact.

Thus, the reception of IMAO together with tryptamins or immediately before use of tryptamins is prolonged and in some cases enhances the effect of the latter, and in addition, it makes it possible to use orally such tripartamans as DMT. This is based on the principle of action of Ayaua and similar mixtures, including the so-called pharmacist, in which instead of plant components use pure DMT, and traditional Banisteriopsis Caapi, and PEGANUM HARMALA seeds, or extracts, or even, can be used as IMAO. Moklobemoid (Aurorix). However, the reception of irreversible IMAOs a few days before the psychedelic reception will weaken its action. The same thing happens during long-term use and irreversible, and reversible IMAO before psychedelic adopted.

The use of 5-meo-DMT together with imoo is unsafe. Many note the strong and unpleasant side effects of such a combination, up to serotonin syndrome. In addition, this experience for many people is psychologically extremely difficult and may be associated with a serious danger to mental health.

Triptamins, significantly improving monoamin levels in the synaptic slit (AMT, 5-MEO-AT, AET, etc.), can be deadly in combination with IMAO. Certain suspicions cause the safety of IMAO with such a tryptamon as DPT.

The LSD metabolism is currently not well understood, but Mao, apparently, does not take any participation in it. Nevertheless, according to some authors, when used together with harmala, its effects are enhanced and extended. The same applies to other ergolines.

Mao plays a minor role or even practically does not participate in the metabolism of phenylethylamine psychedelic. Therefore, the reception of IMAO together with them is devoid of practical meaning. Although, according to some users, and the harmala, and Moklobmeid enhance the effect of some FEAs, such as 2c-b.

In most cases, the reception of IMAO with phenylethylamine psychedelices does not carry serious health hazards. However, it should be refrained from the use of IMAO together with phenylethylamines containing sulfur, such as 2C-T-7 and ALEPH-7, as a result of their ambiguous and low-examined action on monoamin levels in the brain and high toxicity. IMAO combinations can also be unsafe with TMA-6 and TMA-2.

Overdose

IMAO antidepressants are extremely toxic in overdose, and the symptoms of intoxication are not necessarily manifested immediately. For acute poisoning Large doses of IMAO are observed total weakness, dizziness, ataxia, lubricated speech, clonic twirl muscles; Following this develop comatous states or convulsive seizures (such as generalized epileptiform seizures) with a subsequent coma. After leaving the coma, some time can persist a state of stunning. In some cases, coma does not occur, while primary symptoms Overdose is replaced by delirious syndrome. Violations of consciousness in the overdose of IMAO not always marked; In cases where they are absent, depression, which caused the assignment of the IMAO, is very quickly, the euphoria is accurately replaced.

Manifestations of overdose may also be anxiety, confusion, hypertensive crisis, heart rate disorders, rhabomiolysis, coagulopathy.

Due to the high toxicity of IMAO, patients with suicidal inclinations should be written out in quantities sufficient only for several days of reception.

Inhibitors of MAO, it is customary to consider a group of antidepressants that increase the concentration in the blood of hormones " have a good mood" Preparations are aimed at slowing the splitting of monoamicaxidase, thereby increasing the number of serotonin, norepinephrine, dopamine, tryptamins, phenylethylamine. These substances provide high performance, concentration, elevated mood, stable emotional background.

Mao inhibitors are a synthetic form of release in tablets, and are also found in some natural substances. Appointed for the treatment of panic attacks, depressions, narcolepsy.

Classification of drugs

Pharmacists are separated by Mao drugs by exposure to 4 types:

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

Reversible MAOs are connected to the enzyme, forming a single whole. This duet over time releases the necessary substances into the body, and the accumulation of monoamines occurs, excluded without damage to the enzyme.

Irreversible joins monoaminoxidase. A natural organic enzyme after that is not produced, a new substance is synthesized. These drugs begin to act only in 2 weeks.

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

All types of drugs are aimed at reducing the alarming disorders, improving the mood, removing the symptoms of depression.

Preparations of Mao.

Pharmacological preparations of Mao are divided into just three types:

1. Non-selective irreversible. This is a group of first generation preparations with a large list of contraindications and side effects. Their high toxicity destroys the function of the liver, heart, causes nausea. When receiving, you must additionally stick to the diet. The reception period is strictly limited.
2. Reversible selective. Second-generation preparations. Appointed with depression, sociophobia, apathy. Inhibitors are directed mainly to seeding serotonin. Widely used psychiatrists with nervous disorders. Have cancel syndrome.
3. Irreversible selective. Designed for the treatment of heavier diseases of the Central nervous system, such as Parkinson's disease. The substances of drugs are involved in dopamine metabolism. Does not affect the work of the heart, can reduce arterial pressure In hypertensive.

The non-selective irreversible drugs Mao include: IProniazide, Niamid, Fenelzine, Tranyltsipromine, isocarboxes.

Excellent reversible selective preparations: Inazan, Befol, Pyrazidol, Moklobemide.

Irreversible selective: Selegylin, Razgilin, pargilin.

Each drug from the MAO group should be appointed by a doctor, they are released in pharmacies with a recipe.

Who are shown

Mao preparations are prescribed under clinical depressions, disturbing disorders, catalepsy, Parkinson's disease, Alzheimer, an abstineent (alcoholic) syndrome, panic attacks, ICC, schizophrenia. IN last years They are widely used to reduce sociophobia, increasing performance by regulating sleep, with all forms of depression. Some use antidepressants to reduce weight.

The similarity of Mao with the action of amphetamines put them in the category of narcotically hazardous substances. Some drugs cause addiction. Clinical studies have shown that Mao is removed shower, pressure; A person becomes more liberated, sociable, confident. People suffering from narcolepsy (pathological drowsiness) during the reception noted the increase in periods of vigor, decrease in fatigue.

However, these drugs can be used only by appointing a neuropathologist or psychiatrist. Only a specialist will be able to accurately determine which medicine will be the most effective and what is the duration of reception.

The wrong taking tablets can lead to chronic insomnia, anxiety, tachycardia, tremor of hands, anorexia, hypertensive crisis, hypotension.

The non-reliable group is particularly different in the size of the side effects list. At the same time, supporting therapy for the liver should be assigned to their reception, it is necessary to observe a diet with a limitation of a number of products.

How to use

The method of receiving drugs, the dosage appoints a doctor, given the symptoms, diagnosis, age, patient disease. Most often prescribed tablets of the desired dosage of the substance one per day. At first, doctors recommend smoothly into therapy, take half dosage to reduce side effects, prepare an organism to change the chemical composition.

Receiving tablets is not associated with eating, it is possible to drink them any liquid. The recommendation is the reception in the morning hours to avoid evening overexcitation, insomnia.

It is impossible to take with other antidepressants, with caution to drink sedative tincture of herbs.

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

• ban on alcohol;
• the restriction of caffeine and cola for those who are expressed by the exciting effect;
• reduce the amount of chocolate consumed;
• morning reception;
• compliance with dosage.

Some experts believe that when taking antidepressants, it is necessary to comply with the diet, limiting themselves in some products or exclude them to completely from the diet. Here is the list of "forbidden" food:

1. Wine, beer, liquor.
2. Sausage products, smoked, salami, pies.
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. Beer and bakery yeast.
8. Bean: beans, peas, soy, lentils.
9. Spices, cookies, chocolate.

MAO Groups are accepted 1 time per day on one or 0.5 tablet. The first 2 weeks the treatment begins with ½ from the total dosage. The exit from therapy should also be on reduced doses over 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 preparation in the brain is the maximum value.

After treatment, which usually lasts from 3 to 9 months, the doctor can be spelled out by supporting therapy to avoid cancellation syndrome. It can last until six months. Methods of application differ: it can be half or a quarter of a pill; Or the reception of a whole tablet 1 time in 2-3 days.

Mao's special care is prescribed to teenage children, elderly people, patients with heart, hepatic, renal diseases.

Contraindications for use

Mao's active substances can not be taken to people suffering from kidney, cardiac, liver failure, sugar diabetes, atherosclerosis; We have suffered heavy hepatitis, heart attacks, strokes.

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

Reception of MAO is impossible at:

• severe liver diseases;
• renal failure;
• heart diseases with rhythm impairment, changes in vessels;
• after hemorrhagic stroke;
• severe alcoholism;
• reception of other antidepressants;
• manic states;
• suicide addiction.

With caution, it is prescribed:

• under nodal zob;
• tachycardia;
• psychosis, accompanied by hysteria, excitation;
• sclerosis, age dementia;
• obstruction of biliary tract.

In addition to diseases and special conditions, the contraindications are considered simultaneous reception with some medicinal preparations, such as:

1. Amphetamines.
2. A number of cold medicines: ephedrine, koldrex, teraflu, rhines, naphtizin.
3. All preparations for weight loss.
4. St. John's wort, Eleutherococcus, a ladies, Rhodiola pink.
5. Adrenalin.
6. Diuretics.
7. Barbiturates, sleeping pills.
8. Antihistamines.

Row clinical studies Proved the inefficiency of MAO in the treatment of all types of manic disorders. Substances only enhance manic states, anxiety, fear, psychopathy.

Side effects

Recordsmen in the number of side effects are considered non-selective Mao. Their reception is accompanied by: constipation, migraine, dry mouth, reducing vision, swelling, hepatitis, insomnia, tremor, nonsense, hallucinations, intracranial pressure drops.

Selective inhibitors have fewer side effects, their number includes: urine delay, dry mouth, tachycardia, discomfort in the stomach. Less often headaches, insomnia, dizziness, anxiety, anxiety, lack of appetite. Many patients note a decrease in sexual attraction (libido) during the reception, the impossibility of reaching orgasm, a decrease in their brightness. Men may have ejaculation. After the end of the reception, everything is restored.

In elderly patients, Mao inhibitors can cause hypertensive crisis, stroke. A serious reason for the cancellation of drugs is the confusion, nonsense, psychosis, hysteria, suicidal thoughts.

IMAO classification

According to its pharmacological properties, monoaminoxidase inhibitors are divided into reversible and irreversible, selective and non-selective.

Selective imoo inhibit mainly any one of the types of MAO, non-selective - both types.

Unpaid IMAO interact with monoaminoxidase, forming chemical bonds with it. The enzyme after this turns out to be unable to perform its functions and is metabolized, and instead the organism is synthesized by a new one, which usually takes about two weeks.

Reversible Imao, binding to the active center of the enzyme, form a relatively stable complex with it. This complex will gradually dissociate, releaseing the IMAO, which further enters the blood and is excreted from the body, leaving the enzyme intact.

Non-selective irreversible imoo

Strictly speaking, to attract the trahniberamine to this group is not entirely correct, since it is a reversible inhibitor, but on the dissociation of its complex with the enzyme and its full removal from the body may be needed to 30 days. In addition, it exhibits some selectivity towards Mao-A.

Reversible selective inhibitors of Mao A

• Derivatives of beta carbolins

When receiving reversible IMAO, it is not necessary to observe the diet.

Irreversible selective inhibitors of Mao B

Pharmacology IMAO

General

IMAO, blocking the destruction of monoamines by monoaminoxidase, increase the content of one or more media monoamines (norenine, serotonin, dopamine, phenylethylamine, etc.) in the synaptic slit and enhance the monoaminergic (monoamine-mediated) transmission of nerve pulses (neurotransmission). For this reason, for medical purposes, these substances are used mainly as antidepressants. IMAO-B is also used in the treatment of Parkinsonism and Narcolepsy.

Interaction with medicines and some surfactants

The combination of monoaminoxidase inhibitors with substances affecting monoamines can lead to an unpredictable strengthening of their action and be life-threatening.

List of drugs to avoid:

Food incompatible with imao

Significant danger when using IMAO is the use of food products containing various monoamines and their metabolic predecessors. First of all, it is Tiramine and its metabolic predecessor of the amino acid Tyrosine, as well as tryptophan. Tiramine, similar to amphetamine psychostimulants, causes the release of catecholamines from nerve endings. His joint with imao reception is fraught with a hypertensive crisis. Triptophan is used by the organism to generate serotonin, and the use of products containing a large amount of its quantity may entail a serotonin syndrome.

Foods that should be avoided:

• Cheese, especially weathered
• Red wine, beer, especially dark (including and non-alcoholic), El, liqueurs, whiskey.
• Smoked smoked meat sausages and any food
• Marinated, smoked and dried fish (fresh fish relatively safe)
• Extracts of yeast and beer yeast (ordinary bakery yeast safe)
• Protein additives
• Bean (beans, lentils, beans, soy)

Products to which should be treated with caution:

• Strong alcoholic beverages (danger of the oppression of the respiratory center)
• Some fruits, such as bananas, avocado, figs, raisins, prunes, raspberries, pineapple, coconut
• Equal milk products (Prostokvasha, kefir, yogurt, sour cream)
• Caffeine, Theobromin, Teophylline (coffee, tea, Mate, Coca-Cola)

Unjuvenable non-selective IMAOs require refusal of the aforementioned substances and products during their use and within two weeks after the end of use. In the case of reversible IMAO, the diet restrictions are usually less strict and distributed for a while until the substance is maintained in the body (no more than a day). From use together with reversible IMAO drugs and surfactants listed in the list, should also be abstained until they are fully eliminated.

Interaction with phenylethylamine and triptamine psychedelic

Most tryptamins are good substrates for Mao-A. DMT and 5-meo-DMT, with oral administration, they are metabolized already in the gastrointestinal tract and liver, not to get into the blood, so they are inactive for oral administration. 4-hydroxy-DMT (Psilocin) is less susceptible to degradation by Mao, since its hydroxyl group in the 4th position makes it difficult to bind to the active center of the enzyme, as a result of which it turns out to be orally active. Alkyl substituents on the amino group, more voluminous than methyl (ethyl, propyl, cyclopropyl, isopropyl, allyl, etc.) also make it difficult for tryptamins metabolism with such substituents through Mao, therefore all such tripartamins are active during oral use. Alpha-methyl in the molecules of such tripartamins, as AMT and 5-Meo-AMT significantly complicates their metabolism through Mao, and turns them, de facto, from substrates into weak inhibitors of this enzyme.

Inhibition of peripheral mao-A - In the gastrointestinal tract and liver, strong IMAO allows you to make such tripartamans as DMT and 5-mero-DMT orally active, as well as strengthen and extend the effect of other triptamins, such as psilotsin and Det. On the other hand, the long-lasting intake of the IMAO as antidepressants weakens the effect of psychedelics. This happens, obviously, due to changes in monoaminergic brain systems caused by an elevated level of monoamines. The nature of this phenomenon is currently remaining unclear, and is not explained by the simple loss of sensitivity of serotonin receptors, which are interacting with psychic.

Thus, the reception of IMAO together with tryptamins or immediately before use of tryptamins, and, in some cases, enhances the effect of the latter, and also makes it possible to use orally such tripartamines as DMT. This is based on the principle of action of ayaua, and the mixtures similar to it, including the so-called pharmacist, in which instead of plant components use pure DMT, and as an imao can be used both traditional Banisteriopsis Caapi and PEGANUM HARMALA seeds, or their extracts, or even Moklobemid (Aurorix). At the same time, the reception of irreversible IMAOs a few days before the reception of the psychederain will weaken his action. The same happens during long-term use of both irreversible and reversible IMAO before the psychedelica will be accepted.

The use of 5-meo-DMT together with imoo is unsafe. Many note the strong and unpleasant side effects of such a combination, up to serotonin syndrome. In addition, such an experience for many people is psychologically extremely difficult, and may carry a serious danger to mental health.

Triptamins, significantly improving monoamin levels in the synaptic slit, such as AMT, 5-MEO-AT and AET can be fatally dangerous in combination with IMAO. Certain suspicions cause the safety of IMAO with such a tryptamon as DPT.

The LSD metabolism is currently not well understood, but Mao, apparently, does not take any participation in it. Nevertheless, according to some participants, when using together with harmala, its effects are enhanced and extended. The same applies to other ergolines.

Mao plays a secondary role, or even practically does not participate in the metabolism of phenylethylamine psychodeliki. Therefore, the reception of IMAO together with them is deprived of a practical meaning. Although reports of some users, both harmal and mocklobmeids, enhance the effect of some FEAs, such as 2c-b. In most cases, the reception of IMAO with phenylethylamine psychedelices does not carry serious health hazards. However, it is necessary to refrain from the use of IMAO in conjunction with phenylethylamines containing sulfur, such as 2C-T-7 and ALEPH-7, as a result of their ambiguous and low-investigated action on monoamin levels in the brain and high toxicity. IMAO combinations can also be unsafe with TMA-6 and TMA-2.

Other IMAO

Amphetamines and alpha methyltriptamins

Nicotiana Rustica.

Notes

Links

see also

How can Mao inhibitors help you win in the fight against chronic alcoholism and depression?

The synaptic slit is called an operation, where 1 neuron absorbs neuromediators, which highlights the second neuron. In turn, monoaminoxidase inhibitors help with an increase in the concentration of different monoamines in the synaptic slit.

When neurotransmitters are in the middle of 1 and 2 neuron, our organism with you chooses surrounding neurotransmitters. Why? Just he knows how much the amount should be in the synaptisco gap. And so that you have no excessive peace of mind or excrectedness - the enzyme monoaminoxidase is observed.

IMAO forms

Today there are two forms of Mao:

• Type A. implies the process of removing such substances as: noranedrenaline, adrenaline, dopamine, serotonin, thiramine and then directs their excess from the synoptic slot again in that neuron, from where they stand out.
• Type B. Removes phenylethylamine and some other amines.

More Mao inhibitors are divided into:

• selective;
• non-selective;
• reversible;
• irreversible imoo - as an antidepressant.

Pharmacological properties

Some difference is reflected on therapeutic and pharmacological propertiesah different inhibitors of Mao. Non-selective medicinal products MAO type A Mao is blocked, and reversible selective inhibitors of Mao have a selective and reversible effect on it.

In aggregate with typos, Mao inhibitors can cause so strong expressiveness of neurotransmitters, which is fully comparable to the most strong psychostimulating drugs.

Selective reversible MAO inhibitor will be applied at depression. The irreversible selective inhibitors of Mao, like SELEGILIN and RAGILIN, are used to treat Parkinson's disease.

Contraindications before using antidepressant data

As mentioned earlier, Mao inhibitors are used to treat depression and some other disturbing disorders. And, like when taking many drugs, Imao has its incompatible foods that can cause an unpredictable strengthening of the drug, flesh to the threat of a person's life.

During the use of this psychotropic agent A special threat is the use of food containing tiramine, tyrosine and tryptophan.

Here is a list of specific products that are used to refrain during the IMAO reception:

• dairy / fermented milk products;
• alcohol;
• fried meat dishes, foods from stupid meat;
• fish (all but fresh);
• brewer's yeast;
• legumes;
• sauerkraut;
• protein additives;
• overripe fruit;
• spices;
• cookies (all kinds);
• soy sauce;
• chocolate and caffeine.

It was proved that children who have a low-effective enzyme Mao in the future are more often criminals or behave asocial life. And if the activity of the Mao enzyme is increased, this means that in the future a person threatens the frequent stay in a depressive state, since the depression of the Mao enzyme activity increases.

Thus, it is possible to conclude that monoaminoxidase inhibitors are a substance that determines our type of character and even lifestyle.