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

The quick positive effect of hormonal drugs is due to their powerful anti-inflammatory effect. The synthetic corticosteroid fluticasone, contained in the preparations Flixonase or Nazarel, affects the formation of mediators in the body that cause the inflammatory process. It inhibits the formation of biologically active substances (leukotrienes, histamine, prostaglandins), which are involved in the body's defense reaction.

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.

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

Fluticasone, like other corticosteroids, does not have any effect on the formation of its own hormones in the body. It does not inhibit the adrenal glands, pituitary gland, hypothalamus. When administered intranasally (nasal drops), it is 90% bound by blood plasma and rapidly excreted from the body through the kidneys and liver.

Decongestant, anti-inflammatory, anti-allergic effect after topical application hormonal drugs last 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, a significant weakening of it can occur.

Apply on your own hormonal drugs 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.

Use of hormonal agents for allergic rhinitis and sinusitis

A runny nose caused by exposure to various allergens is in second place in terms of frequency after infectious rhinitis. Allergic sinusitis is also diagnosed, more often sinusitis. Time of their occurrence, brightness clinical picture and the duration of the pathological process largely depends 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.

An 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 proceeds with a similar clinical picture. Due to the release of a huge amount of inflammatory mediators (histamine, prostaglandins), the inflammatory process begins. The capillaries of the mucous membrane of the nose and sinuses expand, and the permeability of their walls increases. Through them, blood plasma seeps into the intercellular space of the membrane, mixes with the secretion 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. The congestion is accompanied by abundant transparent discharge, frequent sneezing and constant itching or burning in the nose.

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

Nasal drops containing corticosteroids are used with success for allergic rhinitis or sinusitis. They are necessarily included in the scheme complex treatment along with antihistamines, vasoconstrictor, immunomodulatory and barrier agents. With the correct selection of drugs from all these groups, their positive qualities are enhanced, and the negative effects are smoothed out.

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

Fliksonase nasal drops in the form of a spray are prescribed by a doctor strictly individually. With a vivid 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 into each nostril once a day. When symptoms subside, 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 agent, Fliksonase is used 1 dose once a day in the first 5-6 days of flowering of the allergen plant. The agent is approved for use in pediatrics in children from 4 years of age, 1 injection into each nostril 1 time per day for strict indications.

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

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

The appointment of Polydexa is justified in cases when a person with an allergic rhinitis or sinusitis has a layer of infectious inflammation caused by bacterial microflora. The appearance of symptoms of intoxication against the background of allergic rhinitis, 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, for adults - 2 drops up to 5 times a day. The course of treatment is determined by the doctor and is 5-7 days.

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 heat to cold, when lighting changes from dark to bright light, when inhaling strong odors.

One of the forms of vasomotor rhinitis is the so-called rhinitis of pregnant women, which occurs with a sharp increase in the number of female sex hormones and with an increase in the volume of circulating blood. Very often, a vasomotor rhinitis is combined with an allergic one.

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, without systemic effects on the body and without 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 using 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.

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

The use of hormonal nasal drops is contraindicated in case of intolerance to the components medicinal product, 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 rhinitis and sinusitis. But they should only be used as directed by a doctor, with strict adherence to all recommendations.

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Corticosteroid nasal sprays (aerosols)

Examples of steroid nasal sprays: aldecin, nasobek, rhinoclenil (the active ingredient is beclomethasone), flixonase, nazarel (fluticasone), nazonex (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 any discharge from your nose. Close (pinch) 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. In the same way, inject the prescribed dose of medication into the other nostril.
• Side effects. These aerosols can cause nosebleeds or sore throat.

Intranasal corticosteroids: drug characteristics

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

Properties of corticosteroids

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

Due to all of 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 arise against the background of contact with an allergen:

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

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 drugs, on this moment, has no alternative among other methods of drug treatment.

Before using the nasal hormonal agent directly, 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, taking glucocorticoid drugs is well tolerated by patients. Despite this, there are a number of restrictions on their purpose:

• Hypersensitivity to drug components.
• Tendency to nosebleeds.
• Younger childhood.

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

Side effects

The most often undesirable clinical manifestations on the part of the body occur during their prolonged and uncontrolled use.

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

If corticosteroid drugs are used for a long time in high doses, the risk of developing candidiasis in the nasopharynx area increases.

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

Forms of issue

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

If the technique of instilling the medicine is not followed, a person may experience painful sensations in the forehead, a sensation of 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 applying them.

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

Types of intranasal hormonal drugs

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

The table below shows the most common nasal corticosteroid medications 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.

Fliksonase

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

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

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

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

The medication is strictly prohibited for taking with herpes infection, as well as, in addition to common with other hormones adverse reactions, can provoke the development of glaucoma and cataracts. For children, the drug is approved for use only from the age of 4.

Alcedeen

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

When injecting Alsedin into the nasal cavity, avoid direct contact of the applicator with the mucous membrane. After each dose, you need to rinse your mouth. 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).

Alcedine can increase blood glucose levels, so it must be taken with caution by people with diabetes mellitus... Also, special attention during its reception is paid to people with hypertension, with impaired function 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.

Nazonex

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

In its action and method of application, Nasonex is similar to Fliksonase, 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 much later than when taking Fliksonase.

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

Nasonex is not prescribed to persons with pulmonary tuberculosis, in acute infectious diseases, as well as people who have recently undergone trauma or surgery in the area 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. It is assigned to children from the age of two.

Avamis

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

The clinical effect after the first dose becomes noticeable after 8 hours. If accidentally swallowed during instillation, Avamis 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.

Only the appointment of Avamis to people with severe violations of the functional ability of the liver requires caution. The use of the drug for pregnant and lactating women is not recommended due to the insufficient number of studies on its effect.

Children are prescribed Avaris from the age of two. Cases of overdose with this drug were also not recorded.

Polydexa

The drug is significantly different from all previous ones. This combination drug, which includes preparations of 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 exceptions are representatives of the cocci group). Therefore, its appointment is justified for persons with diseases of the nasopharynx of an allergic nature, in the presence of an infectious pathogen.

Polydexa is made in the form of drops and spray. Drops, as a rule, are used only in the treatment of diseases of the ear of an inflammatory nature, however, their use for the treatment of inflammatory processes in the nose is also permissible. Drops are produced in yellow-brown bottles with a capacity of 10.5 ml. The 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 is on average 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 dysfunction, as well as during pregnancy and breastfeeding.

The drug is not prescribed for children under two years of age. It is forbidden to simultaneously use Polydex with antibacterial aminoglycoside drugs.

Comparative characteristics of nasal corticosteroids

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

Despite the fact that hormonal drugs in the form of nasal sprays do not enter the general circulation, the risk of adverse reactions remains high. With this in mind, the choice of corticosteroids should be taken seriously.

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

Corticosteroid drugs

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

What drugs are corticosteroids?

There are two types of substances considered - glucocorticoids and mineralocorticoids. Medicines that contain one of the types of hormones are corticosteroid. They make it possible to achieve effective removal of any inflammatory processes, eliminate pathological edema, and are effective in relation to allergic reactions.

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

Corticosteroid drugs - pill list

List of hormone tablets and capsules:

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

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

Corticosteroid preparations - ointments, creams, gels:

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

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

Nasal corticosteroids:

It should be noted that in the considered form of release, 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 long-term spastic conditions of the bronchi, the described group of drugs is indispensable. The most convenient is their use in the form of inhalation.

• Budesonide;
• Triamsinalon;
• Fluticasone propionate;
• Flunisolide;
• Beclomethasone dipropionate;
• Beklazon Eco;
• Maple;
• Beclospir;
• Benacort;
• Pulmicort Turbuhaler;
• Budenite Steri-Neb;
• Depo-medrol;
• Tafen Novolizer;
• Diprospan;
• Bekodisk.

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

Like nasal corticosteroids, these agents are almost not absorbed into the blood and mucous membranes, which avoids resistance to the active substance and the 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, to combat it, there are many special drugs, thanks to which it is possible to eliminate the symptoms of allergic diseases, with a high degree of effectiveness, if it was not possible to prevent contact with the allergen.

Otallergy drugs, today are used exclusively as a means for symptomatic treatment... They are not able to act on the cause of allergic reactions - the malfunctioning of the immune system. There are quite a few varieties of drugs for allergies: 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 implies, this group drugs 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 the symptoms of allergies? 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 on the blood vessels.

This is achieved due to the fact that these cells have special receptors (H1). Released, under the action of antibodies, which are produced in response to the ingress of an allergen, histamine enters the general bloodstream, with the help of which it reaches sensitive cells and triggers a cascade of allergic reactions. Antihistamines work in such a way that they prevent histamine from coming into contact with its receptors. As a result, the allergic reaction is interrupted. Most effective method, according to which the use of antihistamines is carried out - application several days before the intended contact with the allergen.

On the modern pharmacological market, a large number of antihistamines are available. Since 1936, when the first antihistamine drug demidrol was released, a lot of time has passed, during which new formulas have been sought. As a result, three generations of these drugs are available today. Often, the younger the antihistamine is, the more effective and safe it is. However, in some cases, the use of the first antihistamines may be necessary, due to which they are still used today.

1st generation drugs

These drugs are the first in their class. Their active substances very quickly lose contact with receptors, 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 funds require constant replacement, every 2-3 weeks.

In addition, there is one significant nuance that forces people to abandon the use of these drugs more and more often. This feature is due to the ability of antihistamines to influence the receptors of the central nervous system. This leads to the fact that inhibitory processes are intensively developing 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. He has the most powerful depressing influence on the central nervous system, which is manifested by severe drowsiness and fatigue, a decrease in reaction. This group of side effects, in practice, is very difficult to tolerate, which makes you either refuse to use diphenhydramine, or forces you to change your lifestyle during treatment.

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

Suprastin is one of the safest first generation drugs. The depressing effect on the central nervous system is present, but less pronounced. In general, most people tolerate it very well.

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

2nd generation drugs

Unlike their predecessors, second-generation drugs do not affect the central nervous system. They are extremely convenient in the aspect of everyday use, since 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 over a wider time range, from 12 to 24 hours. Also, addiction does not develop to them, which makes them suitable means for long-term therapy.

Loratidine is an effective medication for counteracting the symptoms of allergic rhinitis and conjunctivitis, most often used for respiratory allergies. It also well suppresses itching and vasodilation that accompany an allergic reaction. Unfortunately, some patients experience dizziness and nausea.

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 reception 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 the relief of acute allergic reactions.

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

Allergy corticosteroid medications

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 vasodilatation, 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 current medical arsenal to combat allergies, corticosteroids are the most potent drugs. They are used as a means to relieve acute manifestations of allergic reactions. The course of therapy, while often not more than 5 days.

Side effects:

• Violation of sodium excretion, accompanied by the development of edema of the extremities and face;
• Decreased bone density;
• Increased blood glucose concentration;
• Breakdown 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 rate of regeneration processes (slow down recovery, after trauma);
• Increase in body weight due to body fat;
• Decreased functional capacity of the adrenal cortex

Mast Cell Membrane Stabilizers

Mast cell membrane stabilizers are drugs that make the mast cell membrane chemically neutral, preventing it from opening. As a result, the histamine they contain does not enter the general bloodstream 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 unable to cope with allergy symptoms on their own if applied after exposure. These drugs are most effective when used as a means of prevention. Their use is very effective for carrying out preventive measures aimed at eliminating the symptoms of pollen allergy. In this case, it is possible to calculate the flowering time 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.

Allergy nose drops

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

Nazarel is a safe form local drug(fluticasone). An effective and safe drug that 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 for the treatment of allergic rhinitis in pregnant and lactating mothers, since the active substance has a toxic effect on the fetus.

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 the case of acute manifestations of allergic rhinitis, which negatively affect the health of the mother and child, with the ineffectiveness of other means.

Fenistil - antihistamine nasal drops that can be used in children over 1 year old.

Corticosteroid drops and nasal sprays

Intranasal corticosteroids are most effective. Corticosteroid drops relieve all symptoms of allergic conjunctivitis: eliminate allergic rhinitis, relieve swelling, prevent vasodilation, eliminate sneezing. Corticosteroid drops can cause dry and irritated nose, nosebleeds, and thinning of the nasal septum. In order 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, nazonex, alcedin, flunisolid, beclomethasone, etc.

Vasoconstrictor nasal drops

Vasoconstrictor drops can quickly reduce the swelling of the sinuses, which is one of the most unpleasant symptoms of 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 in the composition of these drops there are active substances that affect the narrowing processes in the vessels, due to which the excessive blood flow that causes this congestion is removed.

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

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

Allergy eye drops

An allergic reaction often affects our eyes, since this organ, having increased sensitivity, is the first to be susceptible to allergic reactions. Such an unfavorable picture can often be observed with a respiratory type of allergy (to pollen, cat hair, dust, household chemicals, etc.). In view of this, the use of local agents intended to be applied 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, thereby preventing 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 hands and face before instillation;
• Maintain the dosage indicated by the manufacturer or prescribed by your doctor;
• Instillation is carried out into the conjunctival sac;
• After instillation, hold your head thrown back for 30 minutes so that the active ingredients spread as evenly as possible;
• If you use several eye drops at once, observe the required intervals between their application;
  • Be sure to tell your doctor if you have diseases or disorders of the organs of vision;

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

• 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, already 20-30 minutes after spraying a powder or aerosol, only a small part of the drug remains in the nasal cavity. 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 bloodstream. Therefore, the important pharmacokinetic characteristics of topical steroids are oral and intranasal bioavailability. 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 GCS is explained by their minimal (1-8%) absorption from the 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 beclamethasone, it is approximately 10%. Modern drugs of this group (fluticasone and mometasone) have a bioavailability of 1% and 0.1%, respectively. That is, among intranasal corticosteroids, mometasone has the lowest bioavailability.
  Bioavailability of nasal glucocorticoids
  

  Glucocorticoids	Intranasal bioavailability (%)	Oral Bioavailability
  Beclomethasone dipropionate	44	20-25
  Triamcinolone acetonide	There is no data	10,6-23
  Flunisolide	40-50	21
  Budesonide	34	11
  Fluticasone propionate	0,5-2
  Mometasone furoate

  
  Nasal glucocorticoid delivery systems
  The efficacy and safety of topical steroids is largely determined by their delivery systems to the nasal cavity. The characteristics of existing systems for inhalation administration are given in the table.

  Efficiency of drug delivery into the nasal cavity using various dosing devices
  

  Dosing device	The amount of the drug delivered to the patient (% of a single dose)	The amount of the drug remaining in the nasal cavity (% of the delivered dose)
  Dosing aerosol	64	20
  Nasal spray	100	50
  Turbuhaler	70	90

  
  In our country, dosage forms are currently registered in the form of a metered aerosol and a nasal spray. The latter has a greater efficiency of drug delivery and fewer local side effects that occur in patients with the use of glucocorticoids (nosebleeds, dry and burning in the nose, itching and sneezing). It is believed that they are caused by the irritating effect of freon and the high rate of drug entry into the nasal cavity, observed when using metered aerosols.
  

Catad_tema Clinical pharmacology - articles

Comparative analysis efficacy and safety of fluorinated and chlorinated topical glucocorticosteroids

Published in the magazine:
« Contemporary problems dermatovenerology, immunology and medical cosmetology ", 3, 2010 Svirshchevskaya E.V. 1 , Matushevskaya E.V. 2
1 Institute for Advanced Studies FMBA, Moscow
2 Institute of Bioorganic Chemistry RAS
Svirshchevskaya Elena Viktorovna 117997, Moscow, st. Miklukho-Maclay, 16/10

Topical glucocorticosteroids and their mechanism of action

Topical glucocorticosteroids (GCS) are the main and virtually uncontested drugs for the external treatment of many dermatoses. Recently, dermatologists have identified a number of skin diseases, the main treatment of which is GCS. This group is called steroid-sensitive dermatoses. It includes diseases that differ in pathogenesis and clinical manifestations, but they are united by the need for a suppressive effect on the cells of the immune system associated with the skin. These are atopic dermatitis (AD), allergic dermatitis, eczema, seborrheic inflammation of the skin, psoriasis and many others. In accordance with the European classification of local GCS activity, 4 classes of topical drugs have been identified, divided by the degree of vasoconstrictor effect ( tab. one).

When using topical corticosteroids, there is a local increase in the concentration of GCS in the area of ​​the inflammatory process, due to which GCS drugs do not have a suppressive effect on both the central immune system and other body systems, which avoids severe side effects. Topical corticosteroids have pronounced anti-inflammatory, anti-allergic, anti-exudative and antipruritic effects. They inhibit the accumulation of leukocytes, the release of lysosomal enzymes and pro-inflammatory mediators in the focus of inflammation, inhibit phagocytosis, reduce vascular tissue permeability, and prevent the formation of inflammatory edema. Thus, it becomes clear that the use of topical corticosteroids is advisable due to their local action on activated cells in the skin. Modern synthetic corticosteroids have a greater affinity for the glucocorticosteroid receptor (GCR), and therefore the effect develops much faster and lasts longer.

Topical analogues of glucocorticosteroids

Currently, a number of highly effective GCS drugs have been synthesized, used in the form of ointments, creams, lotions, aerosols and, less often, in the form of solutions and suspensions. The structure of the main derivatives is shown in the figure. The most effective at the moment are considered fluorinated and chlorinated derivatives of cortisol ( tab. 2). Among the fluorinated drugs, betamethasone dipropionate (BDP), containing one fluorine atom, and fluticasone propionate (FP), containing three fluorine atoms, are most active. Among the chlorinated derivatives, the most effective are mometasone furoate (MF), which contains 2 chlorine atoms, and beclomethasone dipropionate (BKDP), which contains one chlorine atom.

Comparison of fluorinated and chlorinated derivatives of cortisol was carried out for many indicators. The most important parameters of action, such as the binding of steroids to GCR, suppression of protein transcription, a decrease in the resulting synthesis of various cytokines and vasoactive factors, etc., are given in Table. 3 for the most studied chlorinated derivative of MF and fluorinated FP preparation in comparison with dexamethasone (DM). In in vitro tests, the activities of MF and EP practically do not differ and significantly exceeds DM.

Rice. 1. The structure of cortisol and synthetic GCS derivatives. Ring D is the basis of all derivatives of GCS (based on the article by S. P. Umland)

Fluorinated corticosteroids are highly effective inhibitors of cell activation not only in vitro, but also when used in vivo... However, with prolonged use, they can cause skin atrophy and an increase in the level of cortisone in the blood in patients, aggravate the course of osteoporosis. Currently available data indicate a greater safety of the use of chlorinated derivatives in long-term therapy, for example, seasonal rhinitis and atopic dermatitis. Thus, the use of MF in 68 patients with AD for 6 months led to the maintenance of remission in 61 patients; however, minor complications were observed in only one patient. Efficiency and safety of MF (cream Uniderm) were also confirmed in domestic studies of children and adults with atopic dermatitis and psoriasis.

Table 1. Classification of topical corticosteroids

Table 2. Classification of chlorinated and fluorinated GCS

Table 3. Comparative activity of fluorinated and chlorinated derivatives of GCS in various tests,% of the activity of mometasone fuorate (according to Umland, 2002)

Action	MF	FP	DM
Binding to the GCS receptor	100	65-79	5-10
Suppression of transcription activation	100	25	5
Suppression of the synthesis of IL-4 and IL-5	100	90-100	20
Suppression of constitutive expression of adhesion molecules	100	90-100	15
Suppression of expression of adhesion molecules VCAM-1 and ICAM-1 induced by TNF-α	0	0	0
Suppression of rhinovirus-induced expression of adhesion molecules VCAM-1 and ICAM-1	100	100	18
Suppression of eosinophil function	100	90-100	20
Suppression of leukotriene production	100	90-100	15
Suppression of migration of leukocytes into tissue	100	100

Notes:
MF - mometasone furoate
FP - fluticasone propionate
DM - dexamethasone
IL - interleukin
TNF-α - tumor necrosis factor alpha

A comparative study of BDP and MF showed that the use of mometasone furoate by patients with AD once a day gave a faster resolution of the disease symptoms with fewer side effects than the use of BDP twice a day. However, with short-term use (2 to 4 weeks) of fluoridated drugs side effects practically not observed.

An analysis of the cost of drugs in England showed that MF is about 2.5 - 3 times more expensive than BDP. At the same time, the use of MF once a day can reduce the cost of treatment. If long-term use of topical steroids is necessary, especially on large surfaces of the skin, when applied to the face, neck, folds, it makes sense to use MF, and if a short course is necessary, the use of cheaper and equally effective fluorinated drugs is quite adequate (Table 4).

Table 4. Comparative characteristics of the effectiveness of action and features of the use of fluorinated and chlorinated topical GCS class III

Betamethasone dipropionate	Mometasone furoate
Contains 1 atom of fluorine	Contains 2 chlorine atoms
The speed of the onset of the therapeutic effect (in the first 4 - 5 days)	The speed of the onset of the therapeutic effect (in the first 2 - 3 days)
Apply to face, neck, folds for no more than 5 days	Apply to face, neck, folds for up to 14 days
Mainly on small surfaces	Mainly on large surfaces
Dosage form- ointment, cream	Dosage form - cream
High local security	High local security
Apply 2 times a day	Apply once a day
"Line" with combinations active ingredients (Akriderm)	Monopreparation ( Uniderm)
OTC drug	Prescription drug
Allowed for use in children from 1 year old	Approved for use in children from 6 months

Taking into account the long-term nature of the course of many skin diseases, the intermittent scheme for the use of topical corticosteroids - two days a week or every other day for several months - is now becoming more and more relevant. The effectiveness and safety of this scheme has been proven by foreign and Russian studies.

One of the possible options for topical corticosteroid therapy is a combination with antimycotic or antibacterial drugs... So, in the presence of concomitant infections, it is effective to use drugs such as Akriderm SK, Akriderm GK and Akriderm Genta, which include betamethasone dipropionate as an active corticosteroid, as well as salicylic acid (SA), the antibiotic gentamicin (Genta) or gentamicin and an antifungal agent clotrimazole (HA), respectively. However, it should be noted that randomized studies have shown that the use of steroids alone for the treatment of bacterial and mycotic infections was as effective as the use of combined topical drugs.

Currently, "strong" topical GCS (betamethasone dipropionate and mometasone furoate) are recommended by leading experts in Russia and abroad as drugs of choice in the treatment of many dermatoses.

List of used literature

1. Weston W. L. The use and abuse of topical steroids // Contemp. Pediatr. - 1988. - Vol. 5. - P. 57 - 66.
2. Medansky R. S., Brody N. I., Kanof N. B. Clinical investigations of momethasone furoate - a novel, non-fluorinated, topical corticosteroid // Semin. Dermatol. - 1987. - Vol. 6. - P. 94 - 100.
3. Viglioglia P., Jones M. L., Peers E. A. Once daily 0.1% momethasone furoate cream versus twice daily 0.1% betamethasone valerate cream in the treatment of a variety of dermatoses // J. Int. Med. Res. - 1990. - Vol. 18. - P. 460 - 467.
4. Roumestan C., Henriquet C., Bousquet J. et al. Fluticasone propionate and mometasone furoate have equivalent transcriptional potencies // Clin. Exp. Allergy. - 2003. - Vol. 33. - P. 895 - 901.
5. Umland S.P., Schleimer R.P., Johnston S.L. Review of the molecular and cellular mechanisms of action of glucocorticoids for use in asthma // Pulmonary Pharmacol. & Therapeutics. - 2002. - Vol. 15. - P. 35 - 50.
6. Stoppoloni G., Prisco F., Santinelli R. Potential hazards of topical steroid therapy // Am. J. Dis. Child. - 1983. - Vol. 137. - P. 1130 - 1331.
7. Faergemann J., Christensen O., Sjovall P. et al... An open study of efficacy and safety of long-term treatment with mometasone furoate fatty cream in the treatment of adult patients with atopic dermatitis // J. Eur. Acad. Dermatol. Venereol. -2000. - Vol. 14, No. 5. - P. 393 - 396.
8. Potekaev N.N., Zhukova O.V., Lekasheva N.N. and others. Non-invasive diagnostic methods in assessing the effectiveness of external therapy for chronic inflammatory dermatoses // Klin. dermatol. and venerol. - 2010. - No. 2. - P. 32 - 37.
9. Korotkiy N.G., Gamayunov B.N., Tikhomirov A.A... The practice of using new external agents in the treatment of atopic dermatitis in children // Klin. dermatol. and venerol. - 2010. - No. 1. - P. 2 - 6.
10. Green C., Colquitt J. L., Kirby J. et al. Clinical and cost-effectiveness of once-daily versus more frequent use of same potency topical corticosteroids for atopic eczema: a systematic review and economic evaluation // Health Technol. Assessment. - 2004. - Vol. 8. - P. 47.
11. Tayab Z R., Fardon T. C., Lee D. K. C. et al. Pharmacokinetic / pharmacodynamic evaluation of urinary cortisol suppression after inhalation of fluticasone propionate and mometasone furoate // Br. J. Clin. Pharmacol. - 2007. - Vol. 64, No. 5. - P. 698 - 705
12. Bruni F. M., De Luca G., Venturoli V. et al... Intranasal corticosteroids and adrenal suppression // Neuroimmunomodulation. - 2009. - Vol. 16, No. 5. - P. 353 - 362.
13. Lebrun-Vignes B., Legrain V., Amoric J. et al... Comparative study of efficacy and effect on plasma cortisol levels of micronised desonide cream 0.1 p. 100 versus betamethasone dipropionate cream 0.05 p. 100 In the treatment of childhood atopic dermatitis // Ann. Dermatol. Venereol. - 2000. - Vol. 127, No. 6 - 7. - P. 590 - 595.
14. Delescluse J., van der Endt J. D. A comparison of the safety, tolerability, and efficacy of fluticasone propionate ointment, 0.005%, and betamethasone-17,21-dipropionate ointment, 0.05%, in the treatment of eczema // Cutis. - 1996. - Vol. 57, No. 2, Suppl. - P. 32 - 38.
15. Hanifin J., Gupta A. K., Rajagopalan R. Intermittent dosing of fluticasone propionate cream for reducing the risk of relapse in atopic dermatitis patients // J. Dermatol. - 2002. - Vol. 147, No. 3. - P. 528 - 537.
16. Veien N. K., Olholm Larsen P., Thestrup-Pedersen K. et al. Long-term, intermittent treatment of chronic hand eczema with mometasone furoate // Br. J. Dermatol. - 1999. - Vol. 140, No. 5. - P. 882 - 886.
17. Sokolovsky E.V., Monakhov K.N., Kholodilova N.A. and others. Intermittent therapy with betamethasone of atopic dermatitis and eczema of the hands // Ros. zhurn. skin. and venus. diseases. - 2009. - No. 3. - P. 16 - 21.
18. Larsen F. S., Simonsen L., Melgaard A. et al... An efficient new formulation of fusidic acid and betamethasone 17-valerate (fucicort lipid cream) for treatment of clinically infected atopic dermatitis // Acta Derm. Venereol. - 2007. - Vol. 87, No. 1. - P. 62 - 68.
19. Khobragade K.J. Efficacy and safety of combination ointment "fluticasone propionate 0.005% plus mupirocin 2.0%" for the treatment of atopic dermatitis with clinical suspicion of secondary bacterial infection: an open label uncontrolled study // Indian J. Dermatol. Venereol. Leprol. - 2005. - Vol. 71, No. 2. - P. 91 - 95.
20. Hjorth N., Schmidt H., Thomsen K... Fusidic acid plus betamethasone in infected or potentially infected eczema // Pharmatherapeutica. - 1985. - Vol. 4, no. 2. - P. 126 - 131.
21. Matushevskaya E.V., Shakurov I.G., Khismatulina Z.R... Efficiency and tolerability of Akriderm® line preparations in the practice of a dermatovenerologist // Klin. dermatol. and venerol. - 2008. - No. 2. - P. 2 - 4.
22. Mosges R., Domrose C. M., Loffler J. Topical treatment of acute otitis externa: clinical comparison of an antibiotics ointment alone or in combination with hydrocortisone acetate // Eur. Arch. Otorhinolaryngol. - 2007. - Vol. 264, No. 9. - P. 1087-1094.
23. Gong J. Q., Lin L., Lin T. et al. Skin colonization by Staphylococcus aureus in patients with eczema and atopic dermatitis and relevant combined topical therapy: a double-blind multicenter randomized controlled trial // Br. J. Dermatol. - 2006. - Vol. 155, No. 4. - P. 680 - 687.
24. Birnie A. J., Bath-Hextall F. J., Ravenscroft J. C. et al. Interventions to reduce Staphylococcus aureus in the management of atopic eczema // Cochrane Database Syst. Rev. - 2008. - Vol. 16, no. 3. - CD003871.

Excipients: dispersed cellulose (microcrystalline cellulose treated with sodium carmellose) - 20 mg, glycerol - 21 mg, citric acid monohydrate - 2 mg, sodium citrate dihydrate - 2.8 mg, polysorbate 80 - 0.1 mg, (in the form of a 50% solution) - 0.2 mg, purified water - 950 mg.

60 doses (10 g) - polyethylene bottles (1) complete with a dosing device - cardboard packs.
120 doses (18 g) - polyethylene bottles (1) complete with a dosing device - cardboard packs.
120 doses (18 g) - polyethylene bottles (2) complete with a dosing device - cardboard packs.
120 doses (18 g) - polyethylene bottles (3) complete with a dosing device - cardboard packs.

pharmachologic effect

GCS for local use. Has anti-inflammatory and effect when used in doses that do not cause systemic effects.

Inhibits the release of inflammatory mediators. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, which causes a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of metabolic products of arachidonic acid - cyclic endoperoxides, prostaglandins. Prevents marginal accumulation of neutrophils, which reduces inflammatory exudate and the production of lymphokines, inhibits the migration of macrophages, and leads to a decrease in the processes of infiltration and granulation. Reduces inflammation by reducing the formation of chemotaxis substance (effect on late allergy reactions), inhibits the development of an immediate type of allergic reaction (due to inhibition of the production of metabolites of arachidonic acid and a decrease in the release of inflammatory mediators from mast cells).

In studies with provocative tests with the application of antigens to the nasal mucosa, a high anti-inflammatory activity of mometasone was demonstrated, both in the early and late stages of an allergic reaction.

This was confirmed by a decrease (compared to placebo) in the concentration of histamine and eosinophil activity, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils and epithelial cell adhesion proteins.

Pharmacokinetics

Suction

With intranasal administration, the systemic bioavailability of mometasone furoate is<1% (при чувствительности метода определения 0.25 пг/мл).

Mometasone is very poorly absorbed from the gastrointestinal tract.

Metabolism and excretion

A small amount of an active substance that can enter the gastrointestinal tract after intranasal administration is actively metabolized during the "first pass" through the liver. It is excreted in urine and bile.

Indications

- seasonal and year-round allergic rhinitis in adults, adolescents and children from 2 years of age;

- acute sinusitis or exacerbation of chronic sinusitis in adults (including the elderly) and adolescents from 12 years old - as an auxiliary therapeutic agent in antibiotic treatment;

- acute rhinosinusitis with mild to moderate symptoms without signs of severe bacterial infection in patients aged 12 years and older;

- prevention of moderate and severe seasonal allergic rhinitis in adults and adolescents from the age of 12 (it is recommended to carry out 2-4 weeks before the expected start of the dusting season);

- nasal polyposis, accompanied by impaired nasal breathing and smell in adults (over 18 years old).

Contraindications

- hypersensitivity to the components of the drug;

- recent surgery or nasal trauma with damage to the mucous membrane of the nasal cavity - until the wound heals (due to the inhibitory effect of GCS on the healing process);

- children and adolescents (with seasonal and year-round allergic rhinitis - up to 2 years, with acute sinusitis or exacerbation of chronic sinusitis - up to 12 years, with polyposis - up to 18 years) - due to the lack of relevant data;

WITH caution the drug should be used for tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, systemic viral infection or infection caused by Herpes simplex with eye damage (as an exception, it is possible to prescribe the drug for these infections as directed by a doctor), the presence of untreated local infection with the involvement of the nasal mucosa in the process.

Dosage

The drug is administered intranasally.

Treating seasonal or perennial allergic rhinitis

The recommended prophylactic and therapeutic dose of the drug is 2 inhalations (50 mcg each) in each nostril 1 time / day (total daily dose - 200 mcg). Upon reaching the therapeutic effect for maintenance therapy, it is possible to reduce the dose to 1 inhalation in each nostril 1 time / day (total daily dose - 100 mcg).

If a decrease in the symptoms of the disease cannot be achieved by using the drug in the recommended therapeutic dose, the daily dose can be increased to 4 inhalations in each nostril 1 time / day (total daily dose - 400 mcg). After symptom relief, dose reduction is recommended.

The onset of action of the drug is usually noted clinically within 12 hours after the first use of the drug.

Children aged 2-11

For the use of the drug in young children, adult assistance is required.

Adjunctive treatment of acute sinusitis or exacerbation of chronic sinusitis

Adults (including elderly patients) and adolescents from 12 years old

If a decrease in the symptoms of the disease cannot be achieved by using the drug in the recommended therapeutic dose, the daily dose can be increased to 4 inhalations in each nostril 2 times / day (total daily dose - 800 mcg). After symptom relief, dose reduction is recommended.

Treating acute rhinosinusitis without evidence of severe bacterial infection

Recommended dose for adults and adolescents is 2 inhalations of 50 mcg in each nasal passage 2 times / day (total daily dose of 400 mcg). If symptoms worsen during treatment, consultation with a specialist is necessary.

Treatment of nasal polyposis

For adults (including elderly patients) from 18 years the recommended therapeutic dose is 2 inhalations (50 mcg each) in each nostril 2 times / day (total daily dose - 400 mcg).

Rules for using the drug Nasonex

Inhalation of the suspension contained in the spray bottle is carried out using a special dispensing nozzle on the bottle.

Before the first use of Nasonex nasal spray, it is necessary to calibrate by pressing the dosing device 10 times, until splashes appear, which indicates that the drug is ready for use.

You should tilt your head and inject the medicine into each nostril as recommended by your doctor.

If the nasal spray has not been used for 14 days or longer, you must press the dispensing nozzle 2 times until a splash appears.

Shake the bottle vigorously before each use.

Cleaning the dispensing tip

It is important to clean the dispensing tip regularly to avoid malfunctioning. Remove the dust cap on the nozzle, then carefully remove the spray tip. Thoroughly rinse spray tip and dust cap in warm water and rinse under tap.

Do not try to open the nasal applicator with a needle or other sharp object, as this will damage the applicator and may result in an incorrect dose of the drug.

Dry the cap and tip in a warm place. After that, you need to attach the spray tip to the bottle and screw the cap back to the bottle to protect it from dust. When using the nasal spray for the first time after cleaning, recalibrate by pressing the dispensing tip 2 times.

Side effects

Adults and adolescents

Adverse events associated with the use of the drug (> 1%) identified during clinical research in patients with allergic rhinitis or nasal polyposis, and during the period of post-registration use of the drug, regardless of the indication for use, are presented in Table 1. Adverse reactions are listed in accordance with the classification of system-organ classes MedDRA. Within each system-organ class, adverse reactions are classified by frequency of occurrence.

Nasal bleeding, as a rule, was moderate and stopped on its own, the frequency of their occurrence was slightly higher than with placebo (5%), but equal or less than with the appointment of other intranasal corticosteroids, which were used as active control (in some of the the incidence of nosebleeds was up to 15%). The incidence of all other adverse events was comparable to that with placebo.

* revealed with a frequency of "rare" when using the drug 2 times / day with nasal polyposis

** detected when using the drug 2 times / day with nasal polyposis

Children

Violations from the outside respiratory system, bodies chest and mediastinum: nosebleeds (6%), irritation of the nasal mucosa (2%), sneezing (2%).

Nervous system disorders: headache (3%).

The incidence of these adverse events in children was comparable to the incidence with placebo.

With the use of intranasal corticosteroids, systemic side effects may develop, especially with prolonged use of intranasal corticosteroids in high doses (see section "Special instructions").

Overdose

With prolonged use of GCS in high doses or with the simultaneous use of several GCS, it is possible to suppress the hypothalamic-pituitary-adrenal system.

The drug has a low systemic bioavailability (<1%, при чувствительности метода определения 0.25 пг/мл), поэтому маловероятно, что при случайной или намеренной передозировке потребуется принятие каких-либо специальных мер, кроме наблюдения с возможным последующим возобновлением приема препарата в рекомендованной дозе.

Drug interactions

The combination therapy was well tolerated by patients. At the same time, no effect of the drug on the concentration of loratadine or its main metabolite in blood plasma was noted. In these studies, mometasone furoate was not detected in the blood (with a sensitivity of the method of determination of 50 pg / ml).

special instructions

As with any long-term treatment, patients who have been using Nasonex nasal spray for several months or longer should periodically see a doctor for possible changes in the nasal mucosa. It is necessary to monitor patients receiving intranasal corticosteroids for a long time. Development of growth retardation in children is possible. In case of detection of growth retardation in children, it is necessary to reduce the dose of intranasal corticosteroids to the lowest that allows effective control of symptoms. In addition, the patient should be referred to a pediatrician for consultation.

If a local fungal infection of the nose or throat develops, it may be necessary to discontinue therapy with Nasonex nasal spray and conduct special treatment. Persistent irritation of the nasal mucosa and pharynx for a long time may also serve as a reason for discontinuing treatment with Nasonex nasal spray.

When conducting placebo-controlled clinical studies in children, when Nasonex nasal spray was used in a daily dose of 100 mcg for a year, growth retardation was not observed in children.

With prolonged treatment with Nasonex nasal spray, signs of suppression of the function of the hypothalamic-pituitary-adrenal system were not observed. Patients who switch to treatment with Nasonex nasal spray after prolonged therapy with systemic corticosteroids require special attention. Cancellation of systemic corticosteroids in such patients can lead to insufficiency of adrenal function, the subsequent recovery of which can take up to several months. If signs of adrenal insufficiency appear, you should resume taking systemic corticosteroids and take other necessary measures.

With the use of intranasal corticosteroids, systemic side effects may develop, especially with prolonged use in high doses. The likelihood of developing these effects is much less than with the use of oral corticosteroids. Systemic side effects may differ both in individual patients and depending on the GCS used. Potential systemic effects include Cushing's syndrome, characteristic features of Cushingoid, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and, less commonly, a range of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggression (especially in children).

During the transition from treatment with systemic corticosteroids to treatment with Nasonex nasal spray, some patients may experience initial symptoms of cancellation of systemic corticosteroids (for example, pain in joints and / or muscles, fatigue and depression), despite a decrease in the severity of symptoms associated with mucosal damage shell of the nose. Such patients need to be specially convinced of the advisability of continuing treatment with Nasonex nasal spray. The transition from systemic to local corticosteroids can also reveal allergic diseases, such as allergic conjunctivitis and eczema, which already existed, but were masked by systemic corticosteroids therapy.

Patients undergoing treatment with GCS have a potentially reduced immune reactivity and should be warned about the increased risk of infection for them in case of contact with patients with certain infectious diseases (for example, chickenpox, measles), as well as the need for medical advice if such contact occurs ... If signs of severe bacterial infection appear (for example, fever, persistent and sharp pain on one side of the face or toothache, swelling in the orbital or periorbital region), immediate medical advice is required.

When using the nasal spray Nasonex for 12 months, there were no signs of atrophy of the nasal mucosa. In addition, mometasone furoate tended to contribute to the normalization of the histological picture in the study of biopsies of the nasal mucosa.

The efficacy and safety of mometasone has not been studied in the treatment of unilateral polyps, polyps associated with cystic fibrosis, and polyps that completely obstruct the nasal cavity.

If unilateral polyps of an unusual or irregular shape are detected, especially ulcerated or bleeding polyps, additional medical examination is necessary.

Influence on the ability to drive vehicles and work with mechanisms

There is no data on the effect of Nasonex on the ability to drive or move machinery.

Pregnancy and lactation

Special, well-controlled studies of the safety of the drug Nasonex during pregnancy have not been conducted.

Like other corticosteroids for intranasal use, Nasonex should be prescribed during pregnancy and during breastfeeding only if the expected benefit from its use justifies the potential risk to the fetus or infant.

Infants whose mothers received GCS during pregnancy should be carefully examined to identify possible adrenal hypofunction.

Childhood use

Contraindicated in seasonal and year-round allergic rhinitis - in children under 2 years of age, with acute sinusitis or exacerbation of chronic sinusitis - up to 12 years, with polyposis - up to 18 years (due to the lack of relevant data).

When conducting placebo-controlled clinical studies in children, when Nasonex was used at a dose of 100 μg / day for a year, no growth retardation was observed.

For violations of liver function

A small amount of the active substance, which can enter the gastrointestinal tract during intranasal administration, is absorbed to an insignificant extent and is actively biotransformed during the "first pass" through the liver.

Conditions of dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug should be stored out of the reach of children at a temperature of 2 ° to 25 ° C. Do not freeze. Shelf life is 2 years.

Hydrocortisone (Hydrocortisone, Cortef, Laticort, Oxycort).

Dexamethasone (Ambene, Dexa-Gentamicin, Maxidex, Maxitrol, Polydex, Tobradex).

Methylprednisolone (Advantan, Metipred, Solu-Medrol).

Mometasone furoate (Momat, Nazonex, Elokom).

Prednisolone (Aurobin, Dermozolone, Prednisolone).

Triamcinolone acetonide (Kenalog, Polcortolone, Ftorocort).

Fluticasone propionate (Fliksonase, Flixotide).

Flucortolone (Ultraproct).

• Mechanism of action

  Glucocorticosteroids by diffusion penetrate into the cytoplasm of the cell and interact with intracellular steroid receptors.

  Inactive glucocorticosteroid receptors are hetero-oligomeric complexes, which, in addition to the receptor itself, include heat shock proteins, various types of RNA, and other structures.

  The C-terminus of steroid receptors is associated with a large protein complex that includes two subunits of the hsp90 protein. After the interaction of the glucocorticosteroid with the receptor, hsp90 is cleaved off, and the resulting hormone-receptor complex moves into the nucleus, where it acts on certain sections of DNA.

  Hormone-receptor complexes also interact with various transcription factors or nuclear factors. Nuclear factors (for example, an activated transcription factor protein) are natural regulators of several genes involved in the immune response and inflammation, including genes for cytokines, their receptors, adhesion molecules, and proteins.

  By stimulating steroid receptors, glucocorticosteroids induce the synthesis of a special class of proteins - lipocortins, including lipomodulin, which inhibits the activity of phospholipase A 2.

  The main effects of glucocorticosteroids.
  

  Glucocorticosteroids, due to their multifaceted effect on metabolism, mediate the adaptation of the body to stressful influences from the external environment.

  Glucocorticosteroids have anti-inflammatory, desensitizing, immunosuppressive, anti-shock and antitoxic effects.

  The anti-inflammatory effect of glucocorticosteroids is due to the stabilization of cell membranes, suppression of the activity of phospholipase A 2 and hyaluronidase, inhibition of the release of arachidonic acid from phospholipids of cell membranes (with a decrease in the levels of its metabolic products - prostaglandins, thromboxane, leukotrienes), as well as inhibition of processes (degranulation of mast cells) , serotonin, bradykinin), platelet activating factor synthesis and connective tissue proliferation.

  The immunosuppressive activity of glucocorticosteroids is the total result of the suppression of various stages of immunogenesis: the migration of stem cells and B-lymphocytes, the interaction of T- and B-lymphocytes.

  The anti-shock and antitoxic effect of glucocorticosteroids is mainly explained by an increase in blood pressure (due to an increase in the concentration of catecholamines circulating in the blood, restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in vascular permeability and activation of liver enzymes involved in the biotransformation of endo- and xenobiotics.

  Glucocorticosteroids activate hepatic gluconeogenesis and enhance protein catabolism, thereby stimulating the release of amino acids - gluconeogenesis substrates from peripheral tissues. These processes lead to the development of hyperglycemia.

  Glucocorticosteroids enhance the lipolytic effect of catecholamines and growth hormone, and also reduce the consumption and utilization of glucose by adipose tissue. An excessive amount of glucocorticosteroids leads to stimulation of lipolysis in some parts of the body (limbs) and lipogenesis in others (on the face and trunk), as well as to an increase in the level of free fatty acids in plasma.

  Glucocorticosteroids have an anabolic effect on the metabolism of proteins in the liver and catabolic - on the metabolism of proteins in muscles, adipose and lymphoid tissues, skin, bones. They inhibit the growth and division of fibroblasts, the formation of collagen.

  In the hypothalamus-pituitary-adrenal system, glucocorticosteroids suppress the formation of corticotropin-releasing hormone and adrenocorticotropic hormone.

  The biological effects of glucocorticosteroids persist for a long time.

  
  By duration of action allocate:
  • Short-acting glucocorticosteroids (hydrocortisone).
  • Medium-acting glucocorticosteroids (methylprednisolone, prednisolone).
  • Long-acting glucocorticosteroids (betamethasone, dexamethasone, triamcinolone acetonide).

• Pharmacokinetics By method of administration distinguish between:
  • Oral glucocorticosteroids.
  • Inhaled glucocorticosteroids.
  • Intranasal glucocorticosteroids.
  Oral glucocorticosteroids.
  

  When taken orally, glucocorticosteroids are well absorbed in the gastrointestinal tract and actively bind to plasma proteins (albumin, transcortin).

  The maximum concentration of drugs in the blood is reached after about 1.5 hours. Glucocorticosteroids undergo biotransformation in the liver, partly in the kidneys and in other tissues, mainly by conjugation with glucuronide or sulfate.

  About 70% of conjugated glucocorticosteroids are excreted in the urine, 20% in the feces, the remainder through the skin and other biological fluids.

  The half-life of oral glucocorticosteroids is on average 2-4 hours.

  
  Some pharmacokinetic parameters of glucocorticosteroids

  A drug	Plasma half-life, h	Tissue half-life, h
  Hydrocortisone	0,5-1,5	8-12
  Cortisone	0,7-2	8-12
  Prednisone	2-4	18-36
  Methylprednisolone	2-4	18-36
  Fludrocortisone	3,5	18-36
  Dexamethasone	5	36-54

  
  Inhaled glucocorticosteroids.
  

  Currently, beclomethasone dipropionate, budesonide, mometasone furoate, flunisolide, fluticasone propionate and triamcinolone acetonide are used in clinical practice.

  
  Pharmacokinetic parameters of inhaled glucocorticosteroids

  Drugs	Bioavailability,%	First pass effect through the liver,%	Plasma half-life, h	Distribution volume, l / kg	Local anti-inflammatory activity, units
  Beclomethasone dipropionate	25	70	0,5	-	0,64
  Budesonide	26-38	90	1,7-3,4 (2,8)	4,3	1
  Triamcinolone acetonide	22	80-90	1,4-2 (1,5)	1,2	0,27
  Fluticasone propionate	16-30	99	3,1	3,7	1
  Flunisolide	30-40		1,6	1,8	0,34

  
  Intranasal glucocorticosteroids.
  

  Currently, beclomethasone dipropionate, budesonide, mometasone furoate, triamcinolone acetonide, flunisolide, fluticasone propionate are used in clinical practice for intranasal use.

  After intranasal administration of glucocorticosteroids, part of the dose that settles in the pharynx is swallowed and absorbed in the intestine, part enters the bloodstream from the mucous membrane of the respiratory tract.

  Glucocorticosteroids entering the gastrointestinal tract after intranasal administration are absorbed by 1-8% and are almost completely biotransformed to inactive metabolites during the first passage through the liver.

  That part of glucocorticosteroids that is absorbed from the mucous membrane of the respiratory tract is hydrolyzed to inactive substances.

  Intranasal bioavailability of glucocorticosteroids

  A drug	Bioavailability for absorption from the gastrointestinal tract,%	Bioavailability when absorbed from the mucous membrane of the respiratory tract,%
  Beclomethasone dipropionate	20-25	44
  Budesonide	11	34
  Triamcinolone acetonide	10,6-23	There is no data
  Mometasone furoate
  Flunisolide	21	40-50
  Fluticasone propionate		0,5-2

• Place in therapy Indications for the use of oral glucocorticosteroids.
  • Replacement therapy for primary adrenal insufficiency.
  • Replacement therapy for secondary chronic adrenal insufficiency.
  • Acute adrenal insufficiency.
  • Congenital dysfunction of the adrenal cortex.
  • Subacute thyroiditis.
  • Bronchial asthma.
  • Chronic obstructive pulmonary disease (in the acute phase).
  • Severe pneumonia.
  • Acute Respiratory Distress Syndrome.
  • Interstitial lung disease.
  • Nonspecific ulcerative colitis.
  • Crohn's disease.
  Indications for the use of intranasal glucocorticoids.
  • Seasonal (intermittent) allergic rhinitis.
  • Year-round (persistent) allergic rhinitis.
  • Polyposis of the nose.
  • Non-allergic rhinitis with eosinophilia.
  • Idiopathic (vasomotor) rhinitis.

  Inhaled glucocorticosteroids are used to treat bronchial asthma, chronic obstructive pulmonary disease.

• Contraindications Glucocorticosteroids are prescribed with caution in the following clinical situations:
  • Itsenko-Cushing's disease.
  • Diabetes.
  • Peptic ulcer of the stomach or duodenum.
  • Thromboembolism.
  • Arterial hypertension.
  • Severe renal failure.
  • Mental illness with productive symptoms.
  • Systemic mycoses.
  • Herpetic infection.
  • Tuberculosis (active form).
  • Syphilis.
  • Vaccination period.
  • Purulent infections.
  • Viral or fungal eye diseases.
  • Corneal diseases associated with epithelial defects.
  • Glaucoma.
  • Lactation period.
  Intranasal administration of glucocorticoids is contraindicated in the following cases:
  • Hypersensitivity.
  • Hemorrhagic diathesis.
  • History of repeated nosebleeds.

• Side effects Systemic side effects of glucocorticosteroids:
  • From the side of the central nervous system:
    • Increased nervous irritability.
    • Insomnia.
    • Euphoria.
    • Depression.
    • Psychoses.
  • On the part of the cardiovascular system:
    • Myocardial dystrophy.
    • Increased blood pressure.
    • Deep vein thrombosis.
    • Thromboembolism.
  • From the digestive system:
    • Steroid ulcers of the stomach and intestines.
    • Bleeding from the gastrointestinal tract.
    • Pancreatitis
    • Fatty degeneration of the liver.
  • From the senses:
    • Posterior subcapsular cataract.
    • Glaucoma.
  • From the endocrine system:
    • Suppression of function and atrophy of the adrenal cortex.
    • Diabetes.
    • Obesity.
    • Cushing's Syndrome.
  • From the side of the skin:
    • Thinning of the skin.
    • Striae.
    • Alopecia.
  • From the musculoskeletal system:
    • Osteoporosis.
    • Fractures and aseptic necrosis of bones.
    • Growth retardation in children.
    • Myopathy.
    • Muscle hypotrophy.
  • On the part of the reproductive system:
    • Menstrual irregularities.
    • Sexual dysfunctions.
    • Delayed sexual development.
    • Hirsutism.
  • On the part of laboratory parameters:
    • Hypokalemia.
    • Hyperglycemia.
    • Hyperlipidemia.
    • Hypercholesterolemia.
    • Neutrophilic leukocytosis.
  • Others:
    • Retention of sodium and water.
    • Swelling.
    • Exacerbation of chronic infectious and inflammatory processes.
  Local side effects.
  Inhaled glucocorticosteroids:
  • Oral cavity and pharyngeal candidiasis.
  • Dysphonia.
  • Cough.
  Intranasal glucocorticosteroids:
  • Itching in the nose.
  • Sneezing.
  • Dryness and burning of the mucous membrane of the nose and throat.
  • Nosebleeds.
  • Perforation of the nasal septum.

• Precautionary measures

  In patients with hypothyroidism, liver cirrhosis, hypoalbuminemia, as well as in elderly and senile patients, the effect of glucocorticosteroids may increase.

  When prescribing glucocorticosteroids during pregnancy, the expected therapeutic effect for the mother and the risk of negative effects on the fetus should be taken into account, since the use of these drugs can lead to impaired fetal growth, some developmental defects (cleft palate), atrophy of the adrenal cortex in the fetus (in the III trimester pregnancy).

  In children and adults taking glucocorticosteroids, infectious diseases such as measles, chickenpox can be difficult.

  The administration of live vaccines is contraindicated in patients taking immunosuppressive doses of glucocorticosteroids.

  Osteoporosis develops in 30-50% of patients who take long-term systemic glucocorticosteroids (oral or injectable dosage forms). As a rule, the spine, pelvic bones, ribs, hands, feet are affected.

  Steroid ulcers during treatment with glucocorticosteroids can be asymptomatic or asymptomatic, manifesting bleeding and perforation. Therefore, patients who receive oral glucocorticosteroids for a long time should periodically carry out fibroesophagogastroduodenoscopy and fecal occult blood analysis.

  In a variety of inflammatory or autoimmune diseases (rheumatoid arthritis, systemic lupus erythematosus and bowel disease), cases of steroid resistance can occur.