home » Immunology, allergology » What are corticosteroids and why they are used in the treatment of diseases of the nasopharynx and respiratory system. Glucocorticosteroid ointments for external use: what is GCS? Combined intranasal corticosteroids

What are corticosteroids and why they are used in the treatment of diseases of the nasopharynx and respiratory system. Glucocorticosteroid ointments for external use: what is GCS? Combined intranasal corticosteroids

Nasal glucocorticoids

Currently, beclomethasone dipropionate, flunisolide, budesonide, gluticasone propionate, mometasone furoate, triamcinolone acetonide are used in clinical practice for intranasal use. Flunisolide and triamsinalon in the form of initial aerosols are not currently used in Russia. Hydrocortisone, prednisolone and dexamethasone should not be used intranasally, as they have a very high bioavailability and may cause side effects characteristic of systemic glucocorticoid therapy. Based on safety data, mometasone furoate and fluticasone propionate are recommended for long-term use.

Pharmacodynamic effects
Nasal corticosteroids have a desensitizing and anti-inflammatory effect - they reduce the secretion of mucosal glands, plasma extravasation and tissue edema, reduce the sensitivity of nasal mucosal receptors to histamine and mechanical stimuli, that is, they also affect nonspecific nasal hyperreactivity. Regular use of topical corticosteroids has a pronounced effect on all the symptoms of AR: nasal congestion, rhinorrhea, sneezing, itching and tickling in the nose, to a lesser extent - on a decrease in smell. In AR, topical corticosteroids are more effective than decongestants, systemic and topical antihistamines, and mast cell membrane stabilizers (ketotifen and sodium cromoglycate).

Pharmacokinetics
After intranasal administration, part of the dose that settles in the pharynx is swallowed and absorbed in the intestine (> 50% of the administered dose), part is absorbed into the blood from the nasal mucosa. With a functioning mucociliary transport, only a small part of the drug remains in the nasal cavity already 20-30 minutes after spraying the powder or aerosol. Up to 96% of the drug is transported by the cilia of the nasal mucosa into the pharynx, swallowed, enters the stomach, and is absorbed into the blood. Therefore, oral and intranasal bioavailability are important pharmacokinetic characteristics of topical steroids (Table 6.6). These indicators largely determine the therapeutic index of glucocorticoids, i.e. the ratio of their local anti-inflammatory activity and possible systemic action.
The low bioavailability of modern topical corticosteroids is explained by their minimal (1-8%) absorption from gastrointestinal tract and almost complete (about 100%) biotransformation to inactive metabolites during the first passage through the liver. A small part of the drug, which is absorbed from the mucous membrane of the respiratory tract, is hydrolyzed by esterases to inactive substances. The bioavailability of many intranasal corticosteroids is relatively high. For example, in beclomethasone, it is approximately 10%. Modern drugs this group (fluticasone and mometasone) have a bioavailability of 1% and 0.1%, respectively. That is, among intranasal corticosteroids, mometasone has the lowest bioavailability.

Table 6. Bioavailability of nasal glucocorticoids

Glucocorticoids	Bioavailability after intranasal administration (%)	Oral bioavailability (%)
Beclomethasone dipropionate
Triamcinolone acetonide	No data
Flunisolide
Budesonide
fluticasone propionate
mometasone furoate

Corticoids are hormonal substances produced by the human adrenal cortex. There are several varieties of them - mineral and glucocorticoids. Preparations that contain only one type of the given hormonal substances are called corticosteroids. Intranasal corticosteroids are the most commonly used form of these drugs in otolaryngology.

Synthetic glucocorticoids have the same properties as natural ones. Nasal corticosteroids, like other forms of hormonal drugs, have a pronounced anti-inflammatory and anti-allergic effect. The basis of the anti-inflammatory effect is the inhibition of the production of active substances (leukotrienes, prostaglandins), which are involved in the protective function of the body. There is also a delay in the reproduction of new protective cells, which significantly affects local immunity. Antiallergic action hormonal preparations perform by inhibiting the release of allergy mediators, in particular, histamine. As a result, a long-term (during the day) anti-edematous effect is achieved.

Due to all the above properties, nasal hormonal preparations are indispensable for many inflammatory and allergic diseases of the nose.

Use of nasal corticosteroids

Currently, in the practice of an ENT doctor, the use of hormonal groups of drugs is widespread, based on their high efficiency. Most often they are prescribed for diseases that occur against the background of contact with an allergen:

allergic rhinitis.
Sinusitis.
Sinusitis.

Nasal corticosteroids effectively eliminate local allergic manifestations, namely sneezing, nasal congestion, rhinorrhea.

The drugs are also prescribed for vasomotor rhinitis in pregnant women. In this situation, they significantly improve nasal breathing, but do not contribute to a complete cure.

When polyps are detected in the nasal cavity, the use of nasal hormonal preparations, at the moment, has no alternative among other methods of drug treatment.

Before the direct use of a nasal hormonal agent, it is important to establish the cause of the disease.

It must be remembered that these drugs do not affect the pathogen itself (viruses, bacteria), but only eliminate the main local manifestations of the disease.

Contraindications

In most cases, the use of glucocorticoid drugs is well tolerated by patients. Despite this, there are a number of limitations to their appointment:

Hypersensitivity to the components of the drug.
Tendency to nosebleeds.
Younger children's age.

Taking hormonal drugs for pregnant women is prescribed with caution, and during breastfeeding it is not recommended for use at all.

Side effects

Most often, undesirable clinical manifestations on the part of the body occur with their prolonged and uncontrolled use.

May be observed:

Pain in the nasopharynx.
Dryness of the nasal mucosa.
Bleeding from the nasal passages.
Headaches, dizziness, drowsiness.

If high doses of corticosteroids are used for a long time, the risk of developing candidiasis in the nasopharyngeal region increases.

The possibility of such clinical manifestations remains quite low, since intranasal hormonal preparations, unlike tablets, act only locally and are not absorbed into the bloodstream.

Release form

Intranasal hormonal drugs are released in the form of drops and sprays. It is necessary to bury the medicine in the nose in a supine position, with the head thrown back and set aside for better penetration of the drug into the nasal cavity.

If the technique of instillation of the drug is not followed, a person may experience pain in the forehead, a taste of the drug in the mouth. Unlike drops, nasal sprays are much more convenient to use because they do not require any preparation before using them.

Their main advantage is that due to the presence of a dispenser, the drug is difficult to overdose.

Types of intranasal hormonal preparations

Currently, there are a large number of hormonal drugs on the pharmaceutical market that are similar in their action, but have varying degrees of pronounced effectiveness.

The table below shows the most commonly used nasal corticosteroids and their analogues.

It is worth dwelling in detail on the features of the main drugs in order to understand what the advantage of each of them is.

Flixonase

In addition to the main substance - fluticasone propionate, the drug contains a number of auxiliary components: dextrose, cellulose, phenylethyl alcohol and purified water.

Flixonase is produced in vials with a dispenser of 60 and 120 doses (in one dose - 50 μg of the active substance). The anti-inflammatory effect of the drug is moderately pronounced, but it has a fairly strong anti-allergic property.

The clinical effect of the drug develops 4 hours after administration, but a significant improvement occurs only on the 3rd day from the start of therapy. With a decrease in the symptoms of the disease, the dosage can be reduced.

The average duration of the course is 5-7 days. It is allowed to take the drug for prophylactic purposes during seasonal allergies. Unlike other hormonal drugs, Flixonase does not have a negative effect on the hypothalamic-pituitary system.

The medication is strictly forbidden to be taken with a herpes infection, and also, in addition to those common with other hormones adverse reactions, can provoke the development of glaucoma and cataracts. For children, the drug is allowed for use only from 4 years of age.

Alcedin

The drug is available in 8.5 g bottles with a dispenser and a mouthpiece in the form of a white, opaque suspension. Contains the active substance - beclomethasone (in a single dose - 50 mcg). In addition to anti-inflammatory, anti-allergic, it also has an immunosuppressive effect. When using standard doses, the drug does not have a systemic effect.

When injecting Alcedin into the nasal cavity, direct contact of the applicator with the mucosa should be avoided. Rinse your mouth after each dose. In addition to indications for use common with other hormonal agents, it can be used as part of complex therapy. bronchial asthma(not used during an attack).

Alcedin can increase blood glucose, so it should be taken with caution in people with diabetes. Also, special attention during its administration is given to people with hypertension, with dysfunction of the liver and thyroid gland.

For women in the first trimester of pregnancy and during breastfeeding, as well as for children under 6 years of age, the drug is contraindicated.

Nasonex

The main component of the drug is mometasone furoate, a synthetic glucocorticosteroid with pronounced anti-inflammatory and antihistamine effects. Produced in the form of a white suspension in plastic bottles of 60 and 120 doses.

In its action and method of application, Nasonex is similar to Flixonase, but, unlike it, has an effect on the hypothalamic-pituitary system. The first clinical effect after the administration of the drug is observed after 12 hours, which is significantly later than when taking Flixonase.

Very rarely, prolonged and uncontrolled use of the drug can lead to an increase in intraocular pressure and disruption of the integrity of the nasal septum (its perforation).

Nasonex is not prescribed for people with pulmonary tuberculosis, with acute infectious diseases, as well as people who have recently suffered injuries or surgical interventions in the region of the nasopharynx. There are no absolute contraindications to taking this drug in pregnant women.

However, after the birth of a child, it must be examined for the safety of adrenal function. He is appointed to children from the age of two.

Avamys

A hormonal drug in which, unlike others, a powerful anti-inflammatory effect prevails. It contains fluticasone furoate and Excipients. It is produced, like previous drugs, in vials of 30, 60 and 120 doses.

The clinical effect after the first dose becomes noticeable after 8 hours. If accidentally swallowed during instillation, Avamys is not absorbed into the bloodstream and does not have a systemic effect.

The drug has a number of advantages in comparison with other nasal hormones and, first of all, this is due to good tolerance. medicinal substance and with the absence of serious contraindications to its appointment.

Caution requires only the appointment of Avamys to people with severe impairment of the functional ability of the liver. It is not recommended to use the drug for pregnant and lactating women due to the insufficient number of ongoing studies on its action.

Avaris children are prescribed from the age of two. Cases of overdose with this drug have also not been recorded.

Polydex

The drug is significantly different from all previous ones. This is a combination drug that includes drugs from three groups, namely antibiotics (neomycin and polymyxin sulfate), vasoconstrictors (phenylephrine hydrochloride) and hormones (dexamethasone 0.25 mg).

Due to the presence of an antibiotic, Polydex is active against bacterial infections (the only exception is representatives of the coccus group). Therefore, its appointment is justified for people with diseases of the nasopharynx of an allergic nature, in the presence of an infectious agent.

Polydex is made in the form of drops and spray. Drops, as a rule, are used only in the treatment of inflammatory ear diseases, however, their use for the treatment inflammatory processes in the nose is also acceptable. Drops are released in bottles of yellow-brown color, with a capacity of 10.5 ml. Spray, unlike ear drops, includes phenylephrine in its composition and is available in a blue bottle (15 ml), protected from daylight.

The duration of drug therapy averages 5-10 days, with prolonged use of the drug, the risk of developing candidiasis and nasopharyngeal dysbiosis is high.

The use of Polydex is absolutely contraindicated in viral diseases nasopharynx, angle-closure glaucoma, severe renal impairment, and during pregnancy and breastfeeding.

Children under two years of age are not prescribed the drug. It is forbidden to use Polidex simultaneously with antibacterial aminoglycoside drugs.

Comparative characteristics of nasal corticosteroids

Given the variety of nasal hormonal preparations, it is often difficult for a person to distinguish them by their action and give preference to any of them. The following table is presented, the main purpose of which is to simplify the understanding of the main differences between nasal corticosteroids.

Despite the fact that hormonal preparations in the form of nasal sprays do not enter the general circulation, the risk of adverse reactions remains high. Given this, the choice of corticosteroids should be approached with all seriousness.

Only the attending physician can prescribe these medicines. The patient should take only the prescribed dosage and observe the duration of the drug.

For the stability of the dosage form, purified water, cellulose and other auxiliary compounds are added to them.

Fast positive effect hormonal agents due to their powerful anti-inflammatory action. Synthetic corticosteroid fluticasone, contained in the drugs Flixonase or Nazarel, affects the formation in the body of mediators that cause the inflammatory process. It inhibits the formation of biologically active substances (leukotrienes, histamine, prostaglandins), which are involved in the protective reaction of the body.

In addition, fluticasone delays cell proliferation, that is, the formation of new macrophages, neutrophils, lymphocytes, eosinophils. This property affects the local immunity of the nasal mucosa.

A positive effect from the use of hormones occurs within 2-4 hours and is expressed in a decrease in swelling of the mucous membrane, cessation of sneezing and itching in the nose, restoration of nasal breathing, and a decrease in the formation of secretions.

Fluticasone, like other corticosteroids, has no effect on the formation of its own hormones in the body. It does not inhibit the adrenal glands, pituitary gland, hypothalamus. With intranasal use (drops in the nose), it is 90% bound by blood plasma and is quickly excreted from the body through the kidneys and liver.

Decongestant, anti-inflammatory, anti-allergic effect after topical application of hormonal drugs lasts about a day. Therefore, they are prescribed no more than 1 time per day. But there is also a negative property of drugs with synthetic corticosteroids. They suppress local immunity - with prolonged and uncontrolled use of them, it can be significantly weakened.

Self-administration of hormonal drugs is not recommended. It is necessary to consult a doctor who will determine the indications for their appointment, prescribe the dose, frequency of use, duration of the course and monitor the effectiveness of therapy.

The use of hormonal drugs for allergic rhinitis and sinusitis

Runny nose, caused by exposure to various allergens, is in second place in frequency of occurrence after infectious rhinitis. Allergic sinusitis is also diagnosed, more often sinusitis. The time of their occurrence, the brightness of the clinical picture and the duration pathological process largely dependent on the properties of the allergen. Seasonal allergic rhinitis, or hay fever, can be autumn or spring and is caused by pollen from flowering plants.

Episodic runny nose occurs under the short-term influence of a certain allergen (for example, contact with animal hair). With constant exposure to allergens (house or book dust), the phenomena of allergic rhinitis are also constant.

Regardless of the characteristics of the allergen, a runny nose or sinusitis occurs with a similar clinical picture. Because of the release huge amount mediators of inflammation (histamine, prostaglandins), the inflammatory process begins. The capillaries of the mucous membrane of the nose and sinuses expand, the permeability of their walls increases. Through them, blood plasma seeps into the intercellular space of the membrane, mixes with the secret that is produced by epithelial cells.

As a result, the mucous membrane thickens, partially or completely blocking the nasal passages and making it difficult to breathe through the nose. Congestion is accompanied by abundant clear discharge, frequent sneezing and constant itching or burning in the nose.

With allergic sinusitis in the sinuses, the formation of a secret increases, which can accumulate due to swelling of the drainage ducts. Symptoms of intoxication (fever, headache, weakness) are absent, since the inflammation is not of infectious origin.

Nose drops containing corticosteroids have been used successfully for allergic rhinitis or sinusitis. They are necessarily included in the complex treatment regimen along with antihistamine, vasoconstrictor, immunomodulatory and barrier agents. With the right selection of drugs from all these groups, their positive qualities are enhanced, and the negative effects are smoothed out.

For example, the suppression of local immunity when using hormonal agents is successfully compensated by the appointment of immunomodulatory drugs. Corticosteroid preparations can be used not only for the treatment of allergic rhinitis, but also for its prevention, before the expected onset of the allergen (before the flowering of a certain plant).

Flixonase nose drops in the form of a spray are prescribed by a doctor strictly individually. With a bright clinical picture of allergy, with a combination of a runny nose and conjunctivitis, in the first two days it is possible to take 2 injections in each nostril 1 time per day. With the weakening of symptoms, the dose is reduced to 1 injection 1 time per day. The course should be no more than 5-7 days, at the discretion of the attending physician.

As a prophylactic, Flixonase is used 1 dose 1 time per day in the first 5-6 days of flowering of the allergen plant. The drug is approved for use in pediatrics in children from 4 years old, 1 injection in each nostril 1 time per day according to strict indications.

Avamis or Nazarel nasal drops containing the synthetic corticosteroid fluticasone are used for the same indications and in the same doses as Flixonase. Depending on the effect obtained and the severity of the clinical picture, the dosage of hormonal drugs in adults and children may vary under the strict supervision of a doctor.

Polydex nose drops are a combination remedy that includes drugs from three groups. These are antibiotics (polymyxin, neomycin), a vasoconstrictor (phenylephrine) and a hormonal agent (dexmetasone).

The appointment of Polydex is justified in cases where a person with an allergic rhinitis or sinusitis has a layering of infectious inflammation caused by bacterial microflora. Appearance in the background allergic rhinitis symptoms of intoxication, a change in the mucous nature of nasal discharge to purulent clearly indicates this.

Polydex nasal drops are prescribed for children from 2 to 15 years old, 1-2 drops 3 times a day, adults - 2 drops up to 5 times a day. The course of treatment is determined by the doctor and is 5-7 days.

The use of hormonal nasal drops for vasomotor rhinitis

A runny nose caused by a violation of the neuro-reflex regulation of capillary tone is called vasomotor. It can be caused by a sudden change in temperature when going from warm to cold, when lighting changes from dark to bright light, or when strong odors are inhaled.

One form of vasomotor rhinitis is the so-called rhinitis of pregnancy, which occurs with a sharp increase in the amount of female sex hormones and with an increase in the volume of circulating blood. Very often, vasomotor rhinitis is combined with allergic.

The effectiveness of the use of hormonal agents in vasomotor rhinitis has been proven by many studies. They are an important part of complex therapy, not having a systemic effect on the body and not causing addiction. For treatment, Nazarel, Nazocort, Aldecin can be used. In each case, especially during pregnancy, the dosage and duration of the course is determined by the attending physician strictly individually.

Side effects and contraindications for hormonal treatment

The effectiveness of the use of hormonal nasal drops leaves no doubt, but it must be remembered that various side effects are possible. They occur most often with unreasonable or uncontrolled intake of hormonal drugs.

Perhaps the appearance of dryness and irritation of the mucous membrane, nosebleeds, an unpleasant taste and smell, a rash on the skin and mucous membranes. With long courses, osteoporosis, adrenal suppression, and bronchospasm may develop.

The use of hormonal nasal drops is contraindicated in case of intolerance to the components of the drug, in children under 4 years of age, in nursing mothers. During pregnancy, their appointment should be very careful, only when absolutely necessary and under constant medical supervision.

The use of drugs with synthetic corticosteroids, including hormonal nasal drops, is justified and very effective in certain forms of the common cold and sinusitis. But they should be used only as directed by a doctor, with strict adherence to all recommendations.

Sinusitis (32)
Nasal congestion (18)
Medicines (32)
Treatment (9)
Folk remedies (13)
Runny nose (41)
Other (18)
Rhinosinusitis (2)
Sinusitis (11)
Snot (26)
Frontit (4)

Corticosteroid nasal sprays (aerosols)

Examples of steroid nasal sprays: aldecine, nasobek, rhinoclenil (active ingredient beclomethasone), flixonase, nazarel (fluticasone), nasonex (mometasone).

How do steroid nasal sprays work? These drugs reduce inflammation in the nasal passages, thereby making nasal breathing easier.
Who should not use these medicines? People who are allergic to any of the ingredients in these sprays should not use them.
Application. Shake container lightly. Blow your nose to clear secretions from your nose. Close (clamp) one nostril and insert the nasal applicator into the other nostril. Breathe in through your nose while pressing down on the applicator to inject the medication. Inject the prescribed dose of medicine into the other nostril in the same way.
Side effects. These aerosols can cause nosebleeds or sore throats.

Intranasal corticosteroids: drug characteristics

Properties of corticosteroids

Synthetic glucocorticoids have the same properties as natural ones. Nasal corticosteroids, like other forms of hormonal drugs, have a pronounced anti-inflammatory and anti-allergic effect. The basis of the anti-inflammatory effect is the inhibition of the production of active substances (leukotrienes, prostaglandins), which are involved in the protective function of the body. There is also a delay in the reproduction of new protective cells, which significantly affects local immunity. Anti-allergic action of hormonal drugs is performed by inhibiting the release of allergy mediators, in particular, histamine. As a result, a long-term (during the day) anti-edematous effect is achieved.

Due to all the above properties, nasal hormonal preparations are indispensable for many inflammatory and allergic diseases of the nose.

Use of nasal corticosteroids

Nasal corticosteroids effectively eliminate local allergic manifestations, namely sneezing, nasal congestion, rhinorrhea.

The drugs are also prescribed for vasomotor rhinitis in pregnant women. In this situation, they significantly improve nasal breathing, but do not contribute to a complete cure.

When polyps are detected in the nasal cavity, the use of nasal hormonal preparations, at the moment, has no alternative among other methods of drug treatment.

Before the direct use of a nasal hormonal agent, it is important to establish the cause of the disease.

It must be remembered that these drugs do not affect the pathogen itself (viruses, bacteria), but only eliminate the main local manifestations of the disease.

Contraindications

In most cases, the use of glucocorticoid drugs is well tolerated by patients. Despite this, there are a number of limitations to their appointment:

Hypersensitivity to the components of the drug.
Tendency to nosebleeds.
Younger children's age.

Taking hormonal drugs for pregnant women is prescribed with caution, and during breastfeeding it is not recommended for use at all.

Side effects

Most often, undesirable clinical manifestations on the part of the body occur with their prolonged and uncontrolled use.

Pain in the nasopharynx.
Dryness of the nasal mucosa.
Bleeding from the nasal passages.
Headaches, dizziness, drowsiness.

If high doses of corticosteroids are used for a long time, the risk of developing candidiasis in the nasopharyngeal region increases.

The possibility of such clinical manifestations remains quite low, since intranasal hormonal preparations, unlike tablets, act only locally and are not absorbed into the bloodstream.

Release form

If the technique of instillation of the drug is not followed, a person may experience pain in the forehead, a sensation of the taste of the drug in the mouth. Unlike drops, nasal sprays are much more convenient to use because they do not require any preparation before using them.

Their main advantage is that due to the presence of a dispenser, the drug is difficult to overdose.

Types of intranasal hormonal preparations

Currently, there are a large number of hormonal drugs on the pharmaceutical market that are similar in their action, but have varying degrees of pronounced effectiveness.

The table below shows the most commonly used nasal corticosteroids and their analogues.

It is worth dwelling in detail on the features of the main drugs in order to understand what the advantage of each of them is.

Flixonase

In addition to the main substance - fluticasone propionate, the drug contains a number of auxiliary components: dextrose, cellulose, phenylethyl alcohol and purified water.

The medication is strictly forbidden to be taken with a herpes infection, and also, in addition to the side reactions common with other hormones, it can provoke the development of glaucoma and cataracts. For children, the drug is allowed for use only from 4 years of age.

Alcedin

When injecting Alcedin into the nasal cavity, direct contact of the applicator with the mucosa should be avoided. Rinse your mouth after each dose. In addition to indications for use common with other hormonal agents, it can be used as part of the complex therapy of bronchial asthma (not used during an attack).

For women in the first trimester of pregnancy and during breastfeeding, as well as for children under 6 years of age, the drug is contraindicated.

Nasonex

Very rarely, prolonged and uncontrolled use of the drug can lead to an increase in intraocular pressure and disruption of the integrity of the nasal septum (its perforation).

Nasonex is not prescribed for people with pulmonary tuberculosis, for acute infectious diseases, as well as for people who have recently undergone trauma or surgery in the nasopharynx. There are no absolute contraindications to taking this drug in pregnant women.

However, after the birth of a child, it must be examined for the safety of adrenal function. He is appointed to children from the age of two.

Avamys

A hormonal drug in which, unlike others, a powerful anti-inflammatory effect prevails. It contains fluticasone furoate and excipients. It is produced, like previous drugs, in vials of 30, 60 and 120 doses.

The drug has a number of advantages in comparison with other nasal hormones and, first of all, this is due to the good tolerance of the drug substance and the absence of serious contraindications to its administration.

Avaris children are prescribed from the age of two. Cases of overdose with this drug have also not been recorded.

Polydex

Polydex is made in the form of drops and spray. Drops, as a rule, are used only in the treatment of inflammatory ear diseases, however, their use for the treatment of inflammatory processes in the nose is also acceptable. Drops are released in bottles of yellow-brown color, with a capacity of 10.5 ml. Spray, unlike ear drops, includes phenylephrine in its composition and is available in a blue bottle (15 ml), protected from daylight.

The duration of drug therapy averages 5-10 days, with prolonged use of the drug, the risk of developing candidiasis and nasopharyngeal dysbiosis is high.

The use of Polydex is absolutely contraindicated in viral diseases of the nasopharynx, angle-closure glaucoma, severe renal impairment, as well as during pregnancy and lactation.

Children under two years of age are not prescribed the drug. It is forbidden to use Polidex simultaneously with antibacterial aminoglycoside drugs.

Comparative characteristics of nasal corticosteroids

Only the attending physician can prescribe these medicines. The patient should take only the prescribed dosage and observe the duration of the drug.

Corticosteroid preparations

The adrenal cortex produces corticosteroid hormones, which are natural substances in the body. They participate in most biochemical processes and regulate the basic mechanisms of life, control the immune system, blood glucose levels, as well as carbohydrate, protein, water-salt exchange.

What drugs are corticosteroids?

There are two types of substances under consideration - glucocorticoids and mineralocorticoids. Medicines that contain one of the types of hormones are corticosteroids. They allow you to effectively remove any inflammatory processes, eliminate pathological swelling, and are effective in relation to allergic reactions.

Synthetic drugs containing corticosteroids are available in the form of capsules, tablets, solutions for intravenous administration, powders, ointments, gels, sprays, drops.

Corticosteroid drugs - list of pills

List of tablets and capsules with hormones:

The above funds are effective in the treatment of most infectious and fungal diseases, disorders of the gastrointestinal tract, circulatory pathologies, including cerebral, autoimmune diseases, neuritis.

Treatment of dermatological ailments necessarily requires the application of external medicines in combination with a systemic scheme.

Corticosteroid preparations - ointments, creams, gels:

These drugs, in addition to corticosteroid hormones, may contain antiseptic components, anti-inflammatory agents and antibiotics.

For the most part, such medicines are used to treat allergic rhinitis and chronic purulent processes V maxillary sinuses. They allow you to quickly achieve relief from nasal breathing and stop reproduction. pathogenic microorganisms on mucous membranes.

Corticosteroid preparations for nasal use:

It should be noted that in the form of release under consideration, corticosteroid hormones have fewer side effects and negative effects on the body than in the form of tablets or injections.

During the treatment of bronchial asthma and prolonged spastic conditions of the bronchi, the described group medicines irreplaceable. The most convenient is their use in the form of inhalation.

Budesonide;
Triamsinalon;
fluticasone propionate;
Flunisolide;
beclomethasone dipropionate;
Beclazone Eco;
Klenil;
Beclospir;
Benacort;
Pulmicort Turbuhaler;
Budenitis Steri-Sky;
Depot medrol;
Tafen Novolizer;
Diprospan;
Bekodisk.

Medicines from this list can be in the form of a ready-made solution, emulsion or powder for dilution and preparation of an inhaler filler.

Like nasal corticosteroids, these drugs are almost not absorbed into the blood and mucous membranes, which avoids resistance to the active substance and serious consequences of the use of drugs.

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Allergy medications

Allergy is one of those diseases that a person has to deal with most often. At the same time, there are many special preparations that can relieve symptoms allergic diseases, with a high degree of effectiveness, if it was not possible to prevent contact with the allergen.

Allergy preparations are currently used exclusively as a means for symptomatic treatment. They are not able to act on the cause of allergic reactions - incorrect operation. immune system. There are quite a few varieties of allergy drugs: antihistamines, corticosteroids, membrane stabilizers, vasoconstrictors. These drugs can be used in a wide variety of forms: tablets, injections, ointments, drops, sprays.

Antihistamines

As the name suggests, this group medicines directed against the action of a hormone such as histamine. Why is it so important to neutralize the effect of this substance in order to cope with allergy symptoms? The fact is that histamine is a special hormone with a wide functional spectrum. One of its actions is the development of symptoms of allergic reactions. It is able to affect the cells of the mucous membranes, skin, as well as blood vessels.

This is achieved due to the fact that these cells have special receptors (H1). Released under the action of antibodies that are produced in response to the allergen, histamine enters the general circulation, through which it reaches sensitive cells and triggers a cascade of allergic reactions. Antihistamines work by preventing histamine from reaching its receptors. As a result, the allergic reaction is interrupted. Most effective method, according to which the use of antihistamines passes - use a few days before the alleged contact with the allergen.

In the modern pharmacological market, a large number of antihistamines are available. Since 1936 - the moment of release of the first antihistamine drug Demidrol, a lot of time has passed, during which there was a search for new formulas. As a result, three generations of these drugs are currently available. Often, the younger the antihistamine is, the more effective and safe it is. However, in some cases, the use of the first antihistamines may have been necessary, which is why they are still used today.

1st generation drugs

These drugs are the first in their class. Their active substances lose contact with receptors very quickly, which leads to a short duration of the therapeutic effect (4-8 hours). Also, another disadvantage of these drugs is the extremely rapid addiction, as a result of which the use of these medications loses their therapeutic effect. Because of this feature, it is impossible to choose one, the most favorably tolerated drug, these drugs require permanent replacement, every 2-3 weeks.

In addition, there is one significant nuance that forces you to abandon the use of these drugs more and more often. This feature is due to the ability of the influence of antihistamines to act also on the receptors of the central nervous system. This leads to the fact that inhibitory processes intensively develop in the body, which are manifested by a feeling of lethargy, daytime sleepiness, constant fatigue and lethargy.

Diphenhydramine is an effective drug for relieving symptoms of allergic reactions. It has the strongest inhibitory effect on the central nervous system, which is manifested by severe drowsiness and fatigue, a decrease in reaction. This group side effects, in practice, it is very difficult to tolerate, which forces either to refuse the use of diphenhydramine, or forces you to change your lifestyle, for the duration of treatment.

Diazolin is a drug that practically does not cause a depressant effect on the central nervous system. The negative side of taking it is an increased risk of peptic ulcer or gastritis of the stomach. This is due to the fact that the active substance also acts on the receptors of the stomach, causing increased secretion of hydrochloric acid.

Suprastin is one of the safest first-generation drugs. The inhibitory effect on the central nervous system is present, but less pronounced. In general, it is well tolerated by most people.

Tavegil is a fast-acting remedy for relieving the symptoms of allergic diseases. Just like diphenhydramine, it has a strong inhibitory effect on the central nervous system. It is often used to treat conditions such as anaphylactic shock or Quincke's edema, due to its rapid action in relieving allergy symptoms.

2nd generation drugs

Unlike their predecessors, second-generation drugs do not affect the central nervous system. They are extremely convenient in terms of everyday use, because they do not cause drowsiness, and also do not provoke lethargy. The disadvantage of these drugs is that most of them cause disorders of the cardiovascular system, therefore, they are very rarely used in patients with impaired functioning of this organ.

Another significant plus on the side of these drugs is that they do not need to be used often at all. Their action occurs in a wider time range, from 12 to 24 hours. They also do not develop addiction, which makes them suitable for long-term therapy.

Loratidine is an effective drug to counter the symptoms of allergic rhinitis and conjunctivitis, most commonly used for respiratory allergies. It also suppresses itching and vasodilation that accompany an allergic reaction. Unfortunately, it causes dizziness and nausea in some patients.

Clarisens - the effectiveness of this drug is due to the fact that in addition to its antihistamine effect, it also has the ability to suppress the release of leukotreins, which are also involved in allergic reactions. The therapeutic effect occurs within half an hour. In some cases, subject to intolerance, its administration may be accompanied by migraine attacks and dyspeptic symptoms.

Claritin is an effective substance that not only blocks histamine receptors, but also prevents the release of serotonin, which is also responsible for some allergic reactions. Most patients, the drug is well tolerated and causes side effects, only in rare cases. The therapeutic effect develops after 10 hours and lasts a day, which makes it a drug that is convenient to use, but not suitable for stopping acute allergic reactions.

Cestin - effectively copes with various symptoms allergic diseases. The effect of its use lasts for several days, which makes it extremely effective drug from allergies long-term use.

Corticosteroid drugs for allergies

Corticosteroids are a group of drugs based on the effects of synthetic corticosteroids, as well as their derivatives. They have a pronounced anti-inflammatory effect, relieve vasodilation, prevent allergic rhinitis, relieve skin manifestations of allergies. They have a universal effect on allergy symptoms, as they neutralize all phases of the immune response. In the modern medical arsenal aimed at combating allergies, corticosteroids are the most powerful means. They are used as a means of removing acute manifestations allergic reactions. The course of therapy, while often does not exceed more than 5 days.

Side effects:

Violation of sodium excretion, accompanied by the development of edema of the limbs and face;
Density reduction bone tissue;
Increasing the concentration of glucose in the blood;
Destruction of muscle protein;
Dystrophy of the heart muscle (with long-term use);
Weakening of the strength of joints and ligaments;
Disruptions in the menstrual cycle;
Violation of immunity;
Decrease in the speed of regeneration processes (slow down recovery after traumatization);
Increase in body weight due to body fat;
Decreased functional ability of the adrenal cortex

Mast cell membrane stabilizers

Mast cell membrane stabilizers are drugs that make the wall of mast cells chemically neutral, preventing it from opening. As a result, the histamine they contain does not enter the general circulation and does not cause allergy symptoms. This is achieved by the ability of certain substances to block the calcium-dependent membrane transport channel.

Mast cell membrane stabilizers are not able to cope with allergy symptoms on their own if applied after ingestion. These drugs are most effective when used as a preventive measure. Their use is very effective, for preventive measures aimed at eliminating the symptoms of pollen allergy. In this case, it is possible to calculate the time of flowering of the allergen and start using these drugs in advance.

These drugs include: ketotifen, sodium cromoglycate, cromohexal, tranilast, alomid, allergic chest of drawers, stafen, cromosol, positan, lecrolin, etc.

nose drops for allergies

To treat the symptoms of allergic conjunctivitis, local antiallergic drugs are used, in the form of nasal drops and sprays. Nasal antihistamines begin to develop their activity within 10 minutes after application. The high speed with which the therapeutic effect occurs is the secret of their effectiveness. Also, being a means for local use, nasal drops do not carry such a pronounced side effect as allergy drugs in the form of tablets and injections.

Nazarel - safe form local drug(fluticasone). An effective and safe drug, which is also used to treat pregnant and lactating mothers.

Allergodil is a drug for the elimination of symptoms of allergic rhinitis based on azelastine, for topical use. It is not used to treat allergic rhinitis in pregnant and lactating mothers, since the active substance has toxic effects to the fruit.

Histimet is an antihistamine spray that suppresses the symptoms of an allergic rhinitis, nasal congestion, swelling and other symptoms caused by an allergic reaction. It is prescribed for the treatment of allergies in pregnant women, only in case of acute manifestations of allergic rhinitis, which adversely affect the health of the mother and child, with the ineffectiveness of other means.

Fenistil - antihistamine nasal drops that can be used in children older than 1 year.

Corticosteroid nasal drops and sprays

Corticosteroid agents for intranasal use are the most effective. Corticosteroid drops relieve all symptoms of allergic conjunctivitis: eliminate allergic rhinitis, relieve swelling, prevent vasodilation, eliminate sneezing. Corticosteroid drops can cause dryness and irritation in the nose, nosebleeds, and thinning of the nasal septum. To avoid the development of negative side effects, corticosteroid drops are used in short courses, only in the presence of acute manifestations of symptoms of allergic rhinitis.

These drugs include: fluticasone, nasonex, alcedin, flunisolide, beclomethasone, etc.

Vasoconstrictor nasal drops

Vasoconstrictor drops allow you to quickly reduce the swelling of the sinuses, which is one of the most unpleasant symptoms allergic manifestations. The use of vasoconstrictor drops allows you to quickly restore breathing, which occurs as a result of the expansion of the vessels of the nasal sinuses. A similar effect is achieved due to the fact that these drops contain active substances that affect the narrowing processes in the vessels, thereby removing the excessive blood flow that causes this congestion.

It should be remembered that these drugs are not independent means for the treatment of allergies, since they only temporarily relieve the manifestations of swelling in the sinuses without affecting the cause of its occurrence. For this reason, vasoconstrictor drops for the nose are not used, as an independent remedy for the treatment of allergies.

These drugs include: naphthyzine, adrianol, tizin, okumetil, betadrin, sanorin, etc.

Allergy eye drops

An allergic reaction often affects our eyes because this body, having increased sensitivity, the first is prone to allergic reactions. Such an unfavorable picture can often be observed with a respiratory variety of allergy (to pollen, cat hair, dust, household chemicals etc.). In view of this, the use of local agents intended for application directly to the conjunctiva is of great importance for the treatment of allergic conjunctivitis.

Antihistamine eye drops - effective remedy for the prevention and elimination of allergy symptoms. As in the case of drugs for topical use, their use allows you to block the contact of histamine with receptors, which prevents the development of allergic reactions.

These substances include: azelastine, olapatidine, ketotifen, lecrolin, opatanol.

How to apply eye drops:

Always keep the pipette clean and avoid contamination of the solution;
Wash your hands and face before instillation;
Maintain the dosage indicated by the manufacturer or prescribed by a doctor;
Instillation is carried out in the conjunctival sac;
After instillation, keep your head thrown back for about 30 minutes so that the active ingredients spread most evenly;
If you use several eye drops at once, observe the required intervals between their use;
- Be sure to inform your doctor if you have any diseases or disorders of the organs of vision;

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Glucocorticoids are steroid hormones synthesized by the adrenal cortex. Natural glucocorticoids and their synthetic analogues are used in medicine for adrenal insufficiency. In addition, in some diseases, anti-inflammatory, immunosuppressive, anti-allergic, anti-shock and other properties of these drugs are used.

The beginning of the use of glucocorticoids as drugs (drugs) refers to the 40s. XX century. Back in the late 30s. of the last century, it was shown that hormonal compounds of a steroid nature are formed in the adrenal cortex. In 1937, the mineralocorticoid deoxycorticosterone was isolated from the adrenal cortex, in the 40s. - glucocorticoids cortisone and hydrocortisone. Wide spectrum pharmacological effects hydrocortisone and cortisone predetermined the possibility of their use as drugs. Their synthesis was soon carried out.

The main and most active glucocorticoid formed in the human body is hydrocortisone (cortisol), others, less active, are cortisone, corticosterone, 11-deoxycortisol, 11-dehydrocorticosterone.

The production of adrenal hormones is under the control of the central nervous system and is closely related to the function of the pituitary gland. Pituitary adrenocorticotropic hormone (ACTH, corticotropin) is a physiological stimulant of the adrenal cortex. Corticotropin enhances the formation and release of glucocorticoids. The latter, in turn, affect the pituitary gland, inhibiting the production of corticotropin and thus reducing further stimulation of the adrenal glands (by the principle of negative feedback). Prolonged administration of glucocorticoids (cortisone and its analogs) into the body can lead to inhibition and atrophy of the adrenal cortex, as well as to inhibition of the formation of not only ACTH, but also gonadotropic and thyroid-stimulating hormones of the pituitary gland.

Cortisone and hydrocortisone have found practical use as drugs from natural glucocorticoids. Cortisone, however, is more likely than other glucocorticoids to cause side effects and, due to the advent of more effective and safer drugs, is currently of limited use. In medical practice, natural hydrocortisone or its esters (hydrocortisone acetate and hydrocortisone hemisuccinate) are used.

A number of synthetic glucocorticoids have been synthesized, among which are non-fluorinated (prednisone, prednisolone, methylprednisolone) and fluorinated (dexamethasone, betamethasone, triamcinolone, flumethasone, etc.) glucocorticoids. These compounds tend to be more active than natural glucocorticoids and act at lower doses. The action of synthetic steroids is similar to the action of natural corticosteroids, but they have a different ratio of glucocorticoid and mineralocorticoid activity. Fluorinated derivatives have a more favorable ratio between glucocorticoid/anti-inflammatory and mineralocorticoid activity. Thus, the anti-inflammatory activity of dexamethasone (compared to that of hydrocortisone) is 30 times higher, betamethasone - 25-40 times, triamcinolone - 5 times, while the effect on water-salt metabolism is minimal. Fluorinated derivatives are distinguished not only by high efficiency, but also by low absorption when applied topically, i.e. less likely to develop systemic side effects.

The mechanism of action of glucocorticoids at the molecular level is not fully understood. It is believed that the effect of glucocorticoids on target cells is carried out mainly at the level of regulation of gene transcription. It is mediated by the interaction of glucocorticoids with specific intracellular glucocorticoid receptors (alpha isoform). These nuclear receptors are capable of binding to DNA and belong to the family of ligand-sensitive transcriptional regulators. Glucocorticoid receptors are found in almost all cells. In different cells, however, the number of receptors varies, they can also differ in molecular weight, hormone affinity, and other physicochemical characteristics. In the absence of the hormone, intracellular receptors, which are cytosolic proteins, are inactive and are part of heterocomplexes, which also include heat shock proteins (heat shock protein, Hsp90 and Hsp70), immunophilin with a molecular weight of 56,000, etc. Heat shock proteins help maintain the optimal conformation of the hormone-binding receptor domain and provide a high affinity of the receptor for the hormone.

After penetration through the membrane into the cell, glucocorticoids bind to receptors, which leads to the activation of the complex. In this case, the oligomeric protein complex dissociates - heat shock proteins (Hsp90 and Hsp70) and immunophilin are detached. As a result, the receptor protein included in the complex as a monomer acquires the ability to dimerize. Following this, the resulting “glucocorticoid + receptor” complexes are transported to the nucleus, where they interact with DNA regions located in the promoter fragment of the steroid-responding gene - the so-called. glucocorticoid response elements (GRE) and regulate (activate or suppress) the process of transcription of certain genes (genomic effect). This leads to stimulation or suppression of mRNA formation and changes in the synthesis of various regulatory proteins and enzymes that mediate cellular effects.

Recent studies show that GC receptors interact, in addition to GRE, with various transcription factors, such as transcription activator protein (AP-1), nuclear factor kappa B (NF-kB), etc. It has been shown that nuclear factors AP-1 and NF-kB are regulators of several genes involved in the immune response and inflammation, including genes for cytokines, adhesion molecules, proteinases, and others.

In addition, another mechanism of action of glucocorticoids has recently been discovered, associated with the effect on transcriptional activation of the cytoplasmic inhibitor of NF-kB, IkBa.

However, a number of effects of glucocorticoids (for example, the rapid inhibition of ACTH secretion by glucocorticoids) develop very quickly and cannot be explained by gene expression (the so-called extragenomic effects of glucocorticoids). Such properties may be mediated by non-transcriptor mechanisms, or by interaction with glucocorticoid receptors on the plasma membrane found in some cells. It is also believed that the effects of glucocorticoids can be realized at different levels depending on the dose. For example, at low concentrations of glucocorticoids (>10 -12 mol/l), genomic effects are manifested (their development requires more than 30 minutes), at high concentrations, they are extragenomic.

Glucorticoids cause many effects, tk. affect most cells in the body.

They have anti-inflammatory, desensitizing, anti-allergic and immunosuppressive effects, anti-shock and anti-toxic properties.

The anti-inflammatory effect of glucocorticoids is due to many factors, the leading of which is the suppression of the activity of phospholipase A 2 . At the same time, glucocorticoids act indirectly: they increase the expression of genes encoding the synthesis of lipocortins (annexins), induce the production of these proteins, one of which, lipomodulin, inhibits the activity of phospholipase A 2 . The inhibition of this enzyme leads to the suppression of the liberation of arachidonic acid and inhibition of the formation of a number of inflammatory mediators - prostaglandins, leukotrienes, thromboxane, platelet activating factor, etc. In addition, glucocorticoids reduce the expression of the gene encoding the synthesis of COX-2, further blocking the formation of pro-inflammatory prostaglandins.

In addition, glucocorticoids improve microcirculation in the focus of inflammation, cause capillary vasoconstriction, and reduce fluid exudation. Glucocorticoids stabilize cell membranes, incl. membranes of lysosomes, preventing the release of lysosomal enzymes and thereby reducing their concentration at the site of inflammation.

Thus, glucocorticoids affect the alterative and exudative phases of inflammation and prevent the spread of the inflammatory process.

Limiting the migration of monocytes to the focus of inflammation and inhibition of fibroblast proliferation determine the antiproliferative effect. Glucocorticoids inhibit the formation of mucopolysaccharides, thereby limiting the binding of water and plasma proteins in the focus of rheumatic inflammation. They inhibit the activity of collagenase, preventing the destruction of cartilage and bones in rheumatoid arthritis.

The antiallergic effect develops as a result of a decrease in the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the proliferation of lymphoid and connective tissues, a decrease in the number of T- and B-lymphocytes, mast cells , reducing the sensitivity of effector cells to allergy mediators, inhibition of antibody formation, changes in the body's immune response.

A characteristic feature of glucocorticoids is their immunosuppressive activity. Unlike cytostatics, the immunosuppressive properties of glucocorticoids are not associated with a mitostatic effect, but are the result of suppression of various stages of the immune response: inhibition of stem cell migration bone marrow and B-lymphocytes, suppression of the activity of T- and B-lymphocytes, as well as inhibition of the release of cytokines (IL-1, IL-2, interferon-gamma) from leukocytes and macrophages. In addition, glucocorticoids reduce the formation and increase the breakdown of the components of the complement system, block the Fc receptors of immunoglobulins, and suppress the functions of leukocytes and macrophages.

The anti-shock and antitoxic effect of glucocorticoids is associated with an increase in blood pressure (due to an increase in the amount of circulating catecholamines, restoration of the sensitivity of adrenoreceptors to catecholamines and vasoconstriction), activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

Glucocorticoids have a pronounced effect on all types of metabolism: carbohydrate, protein, fat and mineral. On the part of carbohydrate metabolism, this is manifested by the fact that they stimulate gluconeogenesis in the liver, increase the content of glucose in the blood (glucosuria is possible), and contribute to the accumulation of glycogen in the liver. The effect on protein metabolism is expressed in the inhibition of protein synthesis and the acceleration of protein catabolism, especially in the skin, in muscle and bone tissue. This is manifested by muscle weakness, atrophy of the skin and muscles, and slower wound healing. These drugs cause a redistribution of fat: increase lipolysis in the tissues of the extremities, contribute to the accumulation of fat mainly in the face (moon face), shoulder girdle, belly.

Glucocorticoids have mineralocorticoid activity: they retain sodium and water in the body by increasing reabsorption in the renal tubules, and stimulate the excretion of potassium. These effects are more typical for natural glucocorticoids (cortisone, hydrocortisone), to a lesser extent - for semi-synthetic ones (prednisone, prednisolone, methylprednisolone). The mineralocorticoid activity of fludrocortisone predominates. Fluorinated glucocorticoids (triamcinolone, dexamethasone, betamethasone) have practically no mineralocorticoid activity.

Glucocorticoids reduce the absorption of calcium in the intestine, promote its release from the bones and increase the excretion of calcium by the kidneys, resulting in the development of hypocalcemia, hypercalciuria, glucocorticoid osteoporosis.

After taking even one dose of glucocorticoids, changes in the blood are noted: a decrease in the number of lymphocytes, monocytes, eosinophils, basophils in the peripheral blood with the simultaneous development of neutrophilic leukocytosis, an increase in the content of erythrocytes.

At long-term use glucocorticoids inhibit the function of the hypothalamus-pituitary-adrenals system.

Glucocorticoids differ in activity, pharmacokinetic parameters (degree of absorption, T 1/2, etc.), methods of application.

Systemic glucocorticoids can be divided into several groups.

According to their origin, they are divided into:

Natural (hydrocortisone, cortisone);

Synthetic (prednisolone, methylprednisolone, prednisone, triamcinolone, dexamethasone, betamethasone).

According to the duration of action, glucocorticoids for systemic use can be divided into three groups (in brackets - biological (from tissues) half-life (T 1/2 biol.):

Short-acting glucocorticoids (T 1/2 biol. - 8-12 hours): hydrocortisone, cortisone;

Glucocorticoids of medium duration of action (T 1/2 biol. - 18-36 hours): prednisolone, prednisone, methylprednisolone;

Long-acting glucocorticoids (T 1/2 biol. - 36-54 h): triamcinolone, dexamethasone, betamethasone.

The duration of action of glucocorticoids depends on the route / site of administration, the solubility of the dosage form (mazipredone is a water-soluble form of prednisolone), and the dose administered. After oral or intravenous administration, the duration of action depends on T 1/2 biol., With intramuscular injection - on the solubility of the dosage form and T 1/2 biol., After local injections - on the solubility of the dosage form and the specific route / site introductions.

When taken orally, glucocorticoids are rapidly and almost completely absorbed from the gastrointestinal tract. C max in the blood is noted after 0.5-1.5 hours. Glucocorticoids bind in the blood to transcortin (corticosteroid-binding alpha 1-globulin) and albumin, and natural glucocorticoids bind to proteins by 90-97%, synthetic ones by 40-60% . Glucocorticoids penetrate well through histohematic barriers, incl. through the BBB, pass through the placenta. Fluorinated derivatives (including dexamethasone, betamethasone, triamcinolone) pass through the histohematic barriers worse. Glucocorticoids undergo biotransformation in the liver with the formation of inactive metabolites (glucuronides or sulfates), which are excreted mainly by the kidneys. Natural drugs are metabolized faster than synthetic drugs and have a shorter half-life.

Modern glucocorticoids are a group of drugs widely used in clinical practice, incl. in rheumatology, pulmonology, endocrinology, dermatology, ophthalmology, otorhinolaryngology.

The main indications for the use of glucocorticoids are collagenoses, rheumatism, rheumatoid arthritis, bronchial asthma, acute lymphoblastic and myeloid leukemia, Infectious mononucleosis, eczema and other skin diseases, various allergic diseases. For the treatment of atopic autoimmune diseases glucocorticoids are the basic pathogenic agents. Glucocorticoids are also used for hemolytic anemia, glomerulonephritis, acute pancreatitis, viral hepatitis and respiratory diseases (COPD in the acute phase, acute respiratory distress syndrome, etc.). In connection with the anti-shock effect, glucocorticoids are prescribed for the prevention and treatment of shock (post-traumatic, surgical, toxic, anaphylactic, burn, cardiogenic, etc.).

The immunosuppressive effect of glucocorticoids makes it possible to use them in organ and tissue transplantation to suppress the rejection reaction, as well as in various autoimmune diseases.

The main principle of glucocorticoid therapy is to achieve the maximum therapeutic effect with minimal doses. The dosage regimen is selected strictly individually, to a greater extent depending on the nature of the disease, the patient's condition and the response to the treatment, than on age or body weight.

When prescribing glucocorticoids, it is necessary to take into account their equivalent doses: according to the anti-inflammatory effect, 5 mg of prednisolone correspond to 25 mg of cortisone, 20 mg of hydrocortisone, 4 mg of methylprednisolone, 4 mg of triamcinolone, 0.75 mg of dexamethasone, 0.75 mg of betamethasone.

There are 3 types of glucocorticoid therapy: substitution, suppressive, pharmacodynamic.

Replacement therapy glucocorticoids is necessary for adrenal insufficiency. In this type of therapy, physiological doses of glucocorticoids are used, in stressful situations (for example, surgery, trauma, acute illness) doses are increased by 2-5 times. When prescribing, the daily circadian rhythm of endogenous secretion of glucocorticoids should be taken into account: at 6-8 o'clock in the morning, most (or all) of the dose is prescribed. At chronic insufficiency adrenal cortex (Addison's disease) glucocorticoids can be used throughout life.

Suppressive therapy glucocorticoids is used for adrenogenital syndrome - congenital dysfunction of the adrenal cortex in children. At the same time, glucocorticoids are used in pharmacological (supraphysiological) doses, which leads to suppression of ACTH secretion by the pituitary gland and a subsequent decrease in the increased secretion of androgens by the adrenal glands. Most (2/3) of the dose is administered at night in order to prevent the peak of ACTH release, according to the principle of negative feedback.

Pharmacodynamic therapy used most often, incl. in the treatment of inflammatory and allergic diseases.

There are several types of pharmacodynamic therapy: intensive, limiting, long-term.

Intensive pharmacodynamic therapy: used in acute, life-threatening conditions, glucocorticoids are administered intravenously, starting with large doses (5 mg / kg - day); after the patient exits the acute state (1-2 days), glucocorticoids are canceled immediately, simultaneously.

Limiting pharmacodynamic therapy: prescribed for subacute and chronic processes, incl. inflammatory (systemic lupus erythematosus, systemic scleroderma, polymyalgia rheumatica, severe bronchial asthma, hemolytic anemia, acute leukemia, etc.). The duration of therapy is usually several months, glucocorticoids are used in doses exceeding physiological (2-5 mg / kg / day), taking into account the circadian rhythm.

To reduce the inhibitory effect of glucocorticoids on the hypothalamic-pituitary-adrenal system, various schemes for the intermittent administration of glucocorticoids have been proposed:

- alternative therapy- use glucocorticoids of short / medium duration of action (prednisolone, methylprednisolone), once, in the morning (about 8 hours), every 48 hours;

- intermittent circuit- glucocorticoids are prescribed in short courses (3-4 days) with 4-day breaks between courses;

-pulse therapy- rapid intravenous administration of a large dose of the drug (at least 1 g) - for emergency therapy. The drug of choice for pulse therapy is methylprednisolone (it enters inflamed tissues better than others and causes less side effects).

Long-term pharmacodynamic therapy: used in the treatment of chronic diseases. Glucocorticoids are prescribed orally, the doses exceed the physiological ones (2.5-10 mg / day), the therapy is prescribed for several years, the abolition of glucocorticoids with this type of therapy is carried out very slowly.

Dexamethasone and betamethasone are not used for long-term therapy, since with the strongest and longest anti-inflammatory action compared to other glucocorticoids, they also cause the most pronounced side effects, incl. inhibitory effect on lymphoid tissue and corticotropic function of the pituitary gland.

During treatment, it is possible to switch from one type of therapy to another.

Glucocorticoids are used orally, parenterally, intra- and periarticularly, inhalation, intranasally, retro- and parabulbarno, in the form of eye and ear drops, externally in the form of ointments, creams, lotions, etc.

For example, in rheumatic diseases, glucocorticoids are used for systemic, local or local (intraarticular, periarticular, external) therapy. In bronchial obstructive diseases, inhaled glucocorticoids are of particular importance.

Glucocorticoids are effective therapeutic agents in many cases. However, it must be taken into account that they can cause a number of side effects, including Itsenko-Cushing's symptom complex (sodium and water retention in the body with possible appearance edema, loss of potassium, increased blood pressure), hyperglycemia up to diabetes(steroid diabetes), slowing down the processes of tissue regeneration, exacerbation peptic ulcer stomach and duodenum, ulceration digestive tract, perforation of an unrecognized ulcer, hemorrhagic pancreatitis, a decrease in the body's resistance to infections, hypercoagulability with a risk of thrombosis, the appearance of acne, a moon-shaped face, obesity, menstrual irregularities, etc. When taking glucocorticoids, there is an increased excretion of calcium and osteoporosis (with prolonged use of glucocorticoids in doses of more 7.5 mg / day - in the equivalent of prednisolone - the development of osteoporosis of long tubular bones). Prevention of steroid osteoporosis is carried out with calcium and vitamin D preparations from the moment you start taking glucocorticoids. The most pronounced changes in the musculoskeletal system are observed in the first 6 months of treatment. One of dangerous complications is aseptic bone necrosis, so it is necessary to warn patients about the possibility of its development and with the appearance of "new" pain, especially in the shoulder, hip and knee joints, it is necessary to exclude aseptic bone necrosis. Glucocorticoids cause changes in the blood: lymphopenia, monocytopenia, eosinopenia, a decrease in the number of basophils in the peripheral blood, the development of neutrophilic leukocytosis, an increase in the content of red blood cells. Nervous and mental disorders are also possible: insomnia, agitation (with the development of psychosis in some cases), epileptiform convulsions, euphoria.

With prolonged use of glucocorticoids, one should take into account the probable inhibition of the function of the adrenal cortex (atrophy is not excluded) with the suppression of hormone biosynthesis. The introduction of corticotropin simultaneously with glucocorticoids prevents atrophy of the adrenal glands.

The frequency and strength of side effects caused by glucocorticoids can be expressed to varying degrees. Side effects, as a rule, are a manifestation of the actual glucocorticoid action of these drugs, but to a degree exceeding physiological norm. With the correct selection of the dose, the observance of the necessary precautions, constant monitoring of the course of treatment, the incidence of side effects can be significantly reduced.

To prevent undesirable effects associated with the use of glucocorticoids, it is necessary, especially with long-term treatment, to carefully monitor the dynamics of growth and development in children, periodically conduct an ophthalmological examination (to detect glaucoma, cataracts, etc.), regularly monitor the function of the hypothalamic-pituitary-adrenal systems, glucose content in blood and urine (especially in patients with diabetes mellitus), control blood pressure, ECG, electrolyte composition of the blood, control the state of the gastrointestinal tract, the musculoskeletal system, control the development of infectious complications, etc.

Most complications in the treatment of glucocorticoids are treatable and disappear after drug withdrawal. Irreversible side effects of glucocorticoids include growth retardation in children (occurs when treated with glucocorticoids for more than 1.5 years), subcapsular cataract (develops in the presence of a family predisposition), steroid diabetes.

Abrupt withdrawal of glucocorticoids can cause an exacerbation of the process - a withdrawal syndrome, especially when long-term therapy is stopped. In this regard, treatment should end with a gradual decrease in dose. The severity of the withdrawal syndrome depends on the degree of preservation of the function of the adrenal cortex. In mild cases, the withdrawal syndrome is manifested by fever, myalgia, arthralgia, and malaise. In severe cases, especially with severe stress, an Addisonian crisis (accompanied by vomiting, collapse, convulsions) may develop.

In connection with side effects, glucocorticoids are used only if there are clear indications and under close medical supervision. Contraindications for the appointment of glucocorticoids are relative. In emergency situations, the only contraindication for short-term systemic use of glucocorticoids is hypersensitivity. In other cases, when planning long-term therapy, contraindications should be taken into account.

The therapeutic and toxic effects of glucocorticoids are reduced by inducers of microsomal liver enzymes, enhanced by estrogens and oral contraceptives. Digitalis glycosides, diuretics (causing potassium deficiency), amphotericin B, carbonic anhydrase inhibitors increase the likelihood of arrhythmias and hypokalemia. Alcohol and NSAIDs increase the risk of erosive and ulcerative lesions or bleeding in the gastrointestinal tract. Immunosuppressants increase the chance of developing infections. Glucocorticoids weaken the hypoglycemic activity of antidiabetic drugs and insulin, natriuretic and diuretic - diuretics, anticoagulant and fibrinolytic - derivatives of coumarin and indandione, heparin, streptokinase and urokinase, the activity of vaccines (due to a decrease in antibody production), reduce the concentration of salicylates, mexiletine in the blood. When using prednisolone and paracetamol, the risk of hepatotoxicity increases.

There are five known drugs that suppress the secretion of corticosteroids by the adrenal cortex. (inhibitors of synthesis and action of corticosteroids): mitotane, metyrapone, aminoglutethimide, ketoconazole, trilostane. Aminoglutethimide, metyrapone and ketoconazole inhibit the synthesis of steroid hormones due to the inhibition of hydroxylases (cytochrome P450 isoenzymes) involved in biosynthesis. All three drugs have specificity, tk. act on different hydroxylases. These drugs can cause acute adrenal insufficiency, so they should be used in strictly defined doses and with careful monitoring of the state of the patient's hypothalamic-pituitary-adrenal system.

Aminoglutethimide inhibits 20,22-desmolase, which catalyzes the initial (limiting) stage of steroidogenesis - the conversion of cholesterol to pregnenolone. As a result, the production of all steroid hormones is disrupted. In addition, aminoglutethimide inhibits 11-beta-hydroxylase as well as aromatase. Aminoglutethimide is used to treat Cushing's syndrome caused by unregulated excess cortisol secretion by adrenal cortical tumors or ectopic ACTH production. The ability of aminoglutethimide to inhibit aromatase is used in the treatment of hormone-dependent tumors such as prostate cancer, breast cancer.

Ketoconazole is mainly used as an antifungal agent. However, at higher doses, it inhibits several cytochrome P450 enzymes involved in steroidogenesis, incl. 17-alpha-hydroxylase, as well as 20,22-desmolase, and thus blocks steroidogenesis in all tissues. According to some data, ketoconazole is the most effective inhibitor of steroidogenesis in Cushing's disease. However, the feasibility of using ketoconazole in case of excessive production of steroid hormones requires further study.

Aminoglutethimide, ketoconazole, and metyrapone are used to diagnose and treat adrenal hyperplasia.

TO glucocorticoid receptor antagonists refers to mifepristone. Mifepristone is a progesterone receptor antagonist, in large doses it blocks glucocorticoid receptors, prevents inhibition of the hypothalamic-pituitary-adrenal system (by the negative feedback mechanism) and leads to a secondary increase in the secretion of ACTH and cortisol.

One of the most important areas of clinical application of glucocorticoids is the pathology of various parts of the respiratory tract.

Indications for appointment systemic glucocorticoids in respiratory diseases are bronchial asthma, COPD in the acute phase, severe pneumonia, interstitial lung disease, acute respiratory distress syndrome.

After systemic glucocorticoids (oral and injectable forms) were synthesized in the late 1940s, they immediately began to be used to treat severe bronchial asthma. Despite a good therapeutic effect, the use of glucocorticoids in bronchial asthma was limited by the development of complications - steroid vasculitis, systemic osteoporosis, and diabetes mellitus (steroid mellitus). Local forms of glucocorticoids began to be used in clinical practice only some time later - in the 70s. XX century. The publication of the successful use of the first topical glucocorticoid, beclomethasone (beclomethasone dipropionate), for the treatment of allergic rhinitis dates back to 1971. In 1972, a report appeared on the use of a topical form of beclomethasone for the treatment of bronchial asthma.

Inhaled glucocorticoids are basic drugs in the treatment of all pathogenetic variants of persistent bronchial asthma, are used in moderate and severe COPD (with a spirographically confirmed response to treatment).

Inhaled glucocorticoids include beclomethasone, budesonide, fluticasone, mometasone, triamcinolone. Inhaled glucocorticoids differ from systemic glucocorticoids in pharmacological properties: high affinity for GK receptors (act in minimal doses), strong local anti-inflammatory effect, low systemic bioavailability (oral, pulmonary), rapid inactivation, short T 1/2 from the blood. Inhaled glucocorticoids inhibit all phases of inflammation in the bronchi and reduce their increased reactivity. Very important is their ability to lower bronchial secretion (reduce the volume of tracheobronchial secretion) and potentiate the action of beta 2-adrenergic agonists. Application inhalation forms glucocorticoids can reduce the need for tableted glucocorticoids. An important characteristic of inhaled glucocorticoids is the therapeutic index - the ratio of local anti-inflammatory activity and systemic action. Of the inhaled glucocorticoids, budesonide has the most favorable therapeutic index.

One of the factors that determine the efficacy and safety of inhaled glucocorticoids are systems for their delivery to the respiratory tract. Currently, metered-dose and powder inhalers (turbuhaler, etc.), nebulizers are used for this purpose.

At right choice systems and techniques of inhalation systemic side effects of inhaled glucocorticoids are insignificant due to the low bioavailability and rapid metabolic activation of these drugs in the liver. It should be borne in mind that all existing inhaled glucocorticoids are absorbed to some extent in the lungs. Local side effects of inhaled glucocorticoids, especially with prolonged use, are the occurrence of oropharyngeal candidiasis (in 5-25% of patients), less often - esophageal candidiasis, dysphonia (in 30-58% of patients), cough.

It has been shown that inhaled glucocorticoids and long-acting beta-agonists (salmeterol, formoterol) have a synergistic effect. This is due to stimulation of the biosynthesis of beta 2 -adrenergic receptors and an increase in their sensitivity to agonists under the influence of glucocorticoids. In this regard, combination drugs intended for long-term therapy, but not for relief of attacks, are effective in the treatment of bronchial asthma, for example, a fixed combination of salmeterol / fluticasone or formoterol / budesonide.

Inhalations with glucocorticoids are contraindicated in fungal infections respiratory tract, tuberculosis, pregnancy.

Currently for intranasal applications in clinical practice use beclomethasone dipropionate, budesonide, fluticasone, mometasone furoate. In addition, dosage forms in the form of nasal aerosols exist for flunisolide and triamcinolone, but they are not currently used in Russia.

Nasal forms of glucocorticoids are effective in the treatment of non-infectious inflammatory processes in the nasal cavity, rhinitis, incl. medical, professional, seasonal (intermittent) and year-round (persistent) allergic rhinitis, to prevent the recurrence of polyps in the nasal cavity after their removal. Topical glucocorticoids are characterized by a relatively late onset of action (12-24 hours), a slow development of the effect - it manifests itself by the 3rd day, reaches a maximum on the 5-7th day, sometimes after a few weeks. Mometasone begins to act most quickly (12 hours).

Modern intranasal glucocorticoids are well tolerated; when used at recommended systemic doses (part of the dose is absorbed from the nasal mucosa and enters the systemic circulation), the effects are minimal. Among the local side effects in 2-10% of patients at the beginning of treatment, nosebleeds, dryness and burning in the nose, sneezing and itching are noted. Perhaps these side effects are due to the irritant effect of the propellant. Isolated cases of perforation of the nasal septum have been described with the use of intranasal glucocorticoids.

Intranasal use of glucocorticoids is contraindicated in hemorrhagic diathesis, as well as in repeated nosebleeds in history.

Thus, glucocorticoids (systemic, inhaled, nasal) are widely used in pulmonology and otorhinolaryngology. This is due to the ability of glucocorticoids to stop the main symptoms of diseases of the ENT and respiratory organs, and in the case of a persistent course of the process, to significantly prolong the interictal period. The obvious advantage of using topical dosage forms of glucocorticoids is the ability to minimize systemic side effects, thus increasing the effectiveness and safety of therapy.

In 1952, Sulzberger and Witten first reported the successful use of 2.5% hydrocortisone ointment for the topical treatment of dermatosis. Natural hydrocortisone is historically the first glucocorticoid used in dermatological practice, subsequently it became the standard for comparing the strength of different glucocorticoids. Hydrocortisone, however, is not effective enough, especially in severe dermatoses, due to relatively weak binding to skin cell steroid receptors and slow penetration through the epidermis.

Later, glucocorticoids were widely used in dermatology for treatment various diseases skin of non-infectious nature: atopic dermatitis, psoriasis, eczema, lichen planus and other dermatoses. They have a local anti-inflammatory, anti-allergic effect, eliminate itching (use for itching is justified only if it is caused by an inflammatory process).

Topical glucocorticoids differ from each other in chemical structure, as well as the strength of the local anti-inflammatory action.

The creation of halogenated compounds (the inclusion of halogens - fluorine or chlorine in the molecule) made it possible to increase the anti-inflammatory effect and reduce systemic side effect when applied topically due to less absorption of drugs. Compounds containing two fluorine atoms in their structure are characterized by the lowest absorption when applied to the skin - flumethasone, fluocinolone acetonide, etc.

According to the European classification (Niedner, Schopf, 1993), there are 4 classes according to the potential activity of local steroids:

Weak (class I) - hydrocortisone 0.1-1%, prednisolone 0.5%, fluocinolone acetonide 0.0025%;

Medium strength (class II) - alklomethasone 0.05%, betamethasone valerate 0.025%, triamcinolone acetonide 0.02%, 0.05%, fluocinolone acetonide 0.00625%, etc.;

Strong (class III) - betamethasone valerate 0.1%, betamethasone dipropionate 0.025%, 0.05%, hydrocortisone butyrate 0.1%, methylprednisolone aceponate 0.1%, mometasone furoate 0.1%, triamcinolone acetonide 0.025%, 0 .1%, fluticasone 0.05%, fluocinolone acetonide 0.025%, etc.

Very strong (class III) - clobetasol propionate 0.05%, etc.

Along with the increase in therapeutic effect when using fluorinated glucocorticoids, the incidence of side effects also increases. The most common local side effects when using strong glucocorticoids are skin atrophy, telangiectasia, steroid acne, striae, and skin infections. The likelihood of developing both local and systemic side effects increases when applied to large surfaces and long-term use of glucocorticoids. Due to the development of side effects, the use of fluorine-containing glucocorticoids is limited if long-term use is necessary, as well as in pediatric practice.

IN last years by modifying the steroid molecule, local glucocorticoids of a new generation were obtained, which do not contain fluorine atoms, but are characterized by high efficiency and a good safety profile (for example, mometasone in the form of furoate is a synthetic steroid that began to be produced in 1987 in the USA, methylprednisolone aceponate, which has been used in practice since 1994).

The therapeutic effect of topical glucocorticoids also depends on the dosage form used. Glucocorticoids for topical use in dermatology are available in the form of ointments, creams, gels, emulsions, lotions, etc. The ability to penetrate the skin (depth of penetration) decreases in the following order: fatty ointment> ointment> cream> lotion (emulsion). With chronic dry skin, the penetration of glucocorticoids into the epidermis and dermis is difficult; moisturizing the stratum corneum of the epidermis with an ointment base increases the penetration of drugs into the skin several times. In acute processes with pronounced weeping, it is more expedient to prescribe lotions, emulsions.

Since topical glucocorticoids reduce the resistance of the skin and mucous membranes, which can lead to the development of superinfection, in case of secondary infection, it is advisable to combine in one dosage form glucocorticoid with an antibiotic, for example, Diprogent cream and ointment (betamethasone + gentamicin), oxycort aerosols (hydrocortisone + oxytetracycline) and Polcortolone TS (triamcinolone + tetracycline), etc., or with an antibacterial and antifungal agent, for example Akriderm GK (betamethasone + clotrimazole + gentamicin ).

Topical glucocorticoids are used in the treatment of such complications of chronic venous insufficiency(CVI) as trophic skin disorders, varicose eczema, hemosiderosis, contact dermatitis and others. Their use is due to the suppression of inflammatory and toxic-allergic reactions in soft tissues that occur in severe forms of CVI. In some cases, local glucocorticoids are used to suppress vascular reactions that occur during phlebosclerosing treatment. Most often, ointments and gels containing hydrocortisone, prednisolone, betamethasone, triamcinolone, fluocinolone acetonide, mometasone furoate, etc. are used for this.

The use of glucocorticoids in ophthalmology based on their local anti-inflammatory, antiallergic, antipruritic action. Indications for the administration of glucocorticoids are inflammatory diseases eyes of non-infectious etiology, incl. after injuries and operations - iritis, iridocyclitis, scleritis, keratitis, uveitis, etc. For this purpose, hydrocortisone, betamethasone, desonide, triamcinolone, etc. are used. The use of local forms is most preferable ( eye drops or suspension, ointments), in severe cases - subconjunctival injections. With systemic (parenteral, oral) use of glucocorticoids in ophthalmology, one should be aware of the high probability (75%) of developing steroid cataracts with daily use for several months of prednisolone at a dose of more than 15 mg (as well as equivalent doses of other drugs), while the risk increases with increasing the duration of treatment.

Glucocorticoids are contraindicated in acute infectious eye diseases. If necessary, for example, in case of bacterial infections, combined preparations containing antibiotics are used, such as Garazon eye / ear drops (betamethasone + gentamicin) or Sofradex (dexamethasone + framycetin + gramicidin), etc. Combined preparations, which include HA and antibiotics are widely used in ophthalmic and otorhinolaryngological practice. In ophthalmology - for the treatment of inflammatory and allergic eye diseases in the presence of concomitant or suspected bacterial infection, for example, with some types of conjunctivitis, in the postoperative period. In otorhinolaryngology - with otitis externa; rhinitis complicated by a secondary infection, etc. It should be borne in mind that the same bottle of the drug is not recommended for the treatment of otitis media, rhinitis and eye diseases in order to avoid the spread of infection.

Preparations

Preparations - 2564 ; Trade names - 209 ; Active ingredients - 27

Active substance	Trade names
Information is absent

The main intranasal corticosteroids (glucocorticosteroids) are beclomethasone, fluticasone, mometasone, budesonide, dexamethasone.

Beclomethasone dipropionate (Alcecin, Baconase, Nasobek, Rinoclenil)

Historically, the first commercially available intranasal corticosteroid preparation appeared in 1973. The effectiveness of this intranasal corticosteroid in seasonal, year-round and non-allergic rhinitis in adults and children has been confirmed by a number of controlled studies. With rhinitis, the recommended dose is 200 mcg, in children - 100 mcg per day. The drug Aldecin is available in cans equipped with two nozzles for intranasal and oral use. Unlike Aldecin, Nasobek is an aqueous suspension produced in 30 ml plastic bottles containing 200 doses. The maximum daily dose is 400 mcg (8 doses).

Budesonide (Tafen Nasal)

Appeared on the pharmaceutical market in 1980. It is available as an aerosol, aqueous nasal spray and powder for spraying into the nasal cavity. The effectiveness of the drug in terms of impact on all symptoms of allergic rhinitis has been proven in many studies.

Fluticasone propionate (Flixonase, Nazarel)

Produced as an aqueous suspension in vials containing 120 doses. One dose contains 50 micrograms of the drug. In allergic rhinitis, 2 doses are prescribed in each half of the nose (200 mcg) once a day, preferably in the morning. The maximum daily dose in the treatment of severe forms of rhinitis is 400 mcg. The bioavailability of the drug is low, no more than 1%, which makes it completely safe even with prolonged use. The effectiveness of fluticasone in seasonal, allergic rhinitis in adults and children over 5 years of age has been proven in a large number of controlled studies.

Mometasone furoate (Nasonex)

Aqueous nasal spray of intranasal GCS is available in vials containing 120 doses (50 mcg each). For the treatment of rhinitis, adults usually give 2 doses in each half of the nose (200 mcg) once a day. The daily dose for children from 3 to 12 years old is 100 mcg (one dose in each nostril). It is proved that these doses do not affect the production of endogenous cortisol and do not slow growth. At the moment, among the existing intranasal corticosteroids, mometasone has the lowest bioavailability, which is 0.1% and a rapid effect, which is recorded as early as 5-7 hours after the start of administration.

Fluticasone furoate (Avamys)

The latest in a generation of modern intranasal glucocorticosteroids, designed exclusively for the treatment of seasonal, allergic rhinitis. As with mometasone, high clinical efficacy is associated with the presence of a furoate ester group in the molecule, which provides a higher affinity for glucocorticosteroid receptors and selectivity of action. The effectiveness of intranasal corticosteroids in the treatment of various forms of allergic rhinitis has been proven by a number of large-scale multicenter studies. Produced in a highly ergonomic container with a shortened tip, which provide higher patient adherence during the course of therapy. One dose of the drug contains 27.5 mcg, adults are prescribed a daily dose of 110 mcg (2 doses in each half of the nose once). In children aged 2-11 years, the recommended starting dose is 55 mcg (dose in each nostril once a day), which, however, can be increased to 110 mcg / day if necessary.

Combined intranasal corticosteroids

There are several other intranasal corticosteroid drugs used. Dexamethasone is part of the combined nasal drops, aerosols, in combination with