Mast cell membrane stabilizers are widely used to treat patients with mild or moderate bronchial asthma, as well as allergic rhinitis.
The group of mast cell membrane stabilizers includes ketotifen and cromone derivatives - cromoglycic acid and nedocromil.

Mechanism of action and pharmacological effects
The mechanism of action of mast cell membrane stabilizers is due to inhibition of the release from target cells, especially from mast cells, of allergy mediators - histamine and other biological active substances. The release of these substances from mast cell granules occurs when an antigen interacts with an antibody on the cell surface. It is assumed that ketotifen and cromones indirectly inhibit the entry into the cell of Ca2+ ions necessary for degranulation, blocking the conductivity of membrane channels for Cl- ions, and also inhibit phosphodiesterase and the process of oxidative phosphorylation.
Inhibiting the function of allergy target cells makes possible use these medications to prevent attacks of bronchial asthma induced by allergens, physical activity and cold air. With their regular use, there is a decrease in the frequency and severity of exacerbations of bronchial asthma, a decrease in the need for bronchospasmolytic drugs, and prevention of the onset of symptoms of the disease caused by physical activity.

Rice. 1. Mechanism of action of mast cell membrane stabilizers

Ketotifen has antianaphylactic and antihistamine effects, inhibits the release of inflammatory mediators (histamine, leukotrienes) by mast cells and basophils, is a calcium antagonist, and eliminates β-adrenergic receptor tachyphylaxis. It reduces airway hyperresponsiveness associated with platelet-activating factor or allergen exposure; suppresses accumulation in respiratory tract eosinophils. The drug also blocks H1-histamine receptors.

Cromoglycate sodium prevents the development of early and late phase allergen-induced bronchial obstruction, reduces bronchial hyperreactivity, prevents bronchospasm caused by physical activity, cold air and allergen inhalation. However, it does not have bronchodilator and antihistamine properties. The main mechanism of its action is the inhibition of the release of allergic mediators from target cells, preventing the early and late stages of the allergic reaction in response to immunological and other stimuli in the lungs. It is known that sodium cromoglycate acts on the bronchial receptor apparatus, increases the sensitivity and concentration of β-adrenergic receptors. The drug blocks reflex bronchoconstriction by inhibiting the activity of C-fibers of sensory endings vagus nerve in the bronchi, which leads to the release of substance P and other neurokinins. The latter are mediators of neurogenic inflammation and cause bronchoconstriction. Prophylactic use of sodium cromoglycate inhibits reflex bronchospasm caused by stimulation of sensitive nerve C-fibers.

Nedocromil sodium similar in chemical structure and mechanism of action to sodium cromoglycate, however, as experimental and clinical studies have shown, nedocromil sodium is 4-10 times more effective than sodium cromoglycate in preventing the development of bronchial obstruction and allergic reactions. Nedocromil sodium is able to suppress the activation and release of allergy mediators from more immunocompetent cells (eosinophils, mast cells, basophils, macrophages, platelets), which is associated with the effect of the drug on chloride channels cell membranes. It inhibits IgE-dependent secretion of histamine and prostaglandin D2 from fat lung cells human, prevents the migration of eosinophils from the vascular bed and inhibits their activity. The drug restores the functional activity of ciliated cells and blocks the release of eosinophilic cationic protein by eosinophils.

allergy immune disease hypersensitivity

Medicines that stabilize the membranes of mast cells and basophils, inhibit the release of histamine and other nutrients (bradykinin, MRSA, lymphokines, prostaglandins) involved in the development of allergic and other pathological reactions are used for the prevention of bronchial asthma, bronchospasm and the treatment of seasonal allergic reactions. Cromoglicic acid, nedocromil, ketotifen, oxatomide, and lodoxamide have these properties. The mechanism of action of these drugs is associated with the stabilization of cell membranes. By changing the hydration properties of these cells, the drugs inhibit the entry of calcium ions into the intracellular space, which in turn reduces the contraction of myofibrils and blocks the process of release of mediators from the granules that cause the main symptoms of allergy.

Cromoglycic acid is available under different names trade names and in different dosage forms it is Cromolyn sodium, a 2% solution of the drug in aerosol packaging (spray) in 15 ml cans (1 mg - 200 single doses); Cromohexal solution for inhalation, 10 mg/ml/2 ml, nasal spray 2% - 15 (30) ml; Cromogen inhaler, Cromogen easy breath, Bicromat - aerosol 15 g, (20 mg/2 ml) and ampoules for inhalation 2% - 10 ml, Intal - powder for inhalation in capsules 20 mg and aerosol for inhalation dosed 5 mg dose, 112 doses; Optikrom, Lekrolin - eye drops, 20 mg/ml, tube cap 0.25 or fl cap 10 ml; Ifiral capsules with powder for inhalation 20 mg; Cromoglin - eye drops 20 mg/ml, 10 ml bottles and spray 300 mg/15 ml spray bottles; Sodium cromoglicate - dosed nasal spray; Lomuzol is a spray for intranasal use, one dose contains 2.6 mg of sodium cromoglycate, available in bottles of 26 ml of 2% solution; Nalkrom - capsules, soluble in the intestines; Kropoz is an aerosol for inhalation, 1 dose contains 5 mg of cromoglycic acid, 150 doses in a 15 ml can; combination drug Ditek. One inhalation dose of Ditek contains 1 mg of sodium cromoglycate and 0.05 mg of fenoterol and exhibits bronchodilator, protective and anti-inflammatory effects. The presence of two drugs makes it possible to block not only the early phase, but also to influence the later manifestations of bronchospasm.

Cromoglicic acid inhibits the entry of calcium ions into the cell and blocks the process of release of biologically active substances from granules. It is believed that the drug inhibits the chemotaxis of eosinophils, neutrophils, and monocytes (directed movement of cells towards the object of phagocytosis). It is effective for the treatment of patients with allergic bronchial asthma and has a preventive effect when used before an asthma attack. The drug is not used to relieve acute asthma attacks. Assign dosage forms the drug as the main or auxiliary agent, depending on the course of the disease, because its action develops slowly. The maximum effect usually occurs after a week. During your appointment inhalation forms The drug sometimes causes a cough or short-term bronchospasm, laryngeal edema. In case of severe adverse events, discontinuation of the drug is required. When taking oral forms, nausea, unpleasant taste in the mouth, burning sensation, swelling, skin rash. Upon admission eye drops lacrimation, dryness around the eyes occurs, short-term disturbance vision.

In terms of antihistamine and antiallergic effects, Ketotifen (Zaditen, Astaphen) is close to cromoglycic acid, but unlike it, it has a weak sedative effect and non-competitively blocks H1-histamine receptors. The BBB passes through and depresses the central nervous system. Stabilizes mast cells and basophils, inhibits phosphodiesterase, increases cAMP levels in cells, suppresses eosinophil sensitization and prevents the development of symptoms of airway hyperresponsiveness. Penetrates breast milk. A pronounced therapeutic effect develops after 6-8 weeks. Available in 1 mg tablets and syrup in bottles. When using it, dizziness, drowsiness, lethargy, dry mouth, increased appetite, and weight gain are observed.

Oxatomide (Tinset, Phensedyl) pharmacological action close to cromoglycic acid, available in 30 mg tablets, take 1-2 tablets 2 times a day.

Nedocromil (Tailed, Tilarin, Tilavist), in addition to its antiallergic effect, has anti-inflammatory activity. Reduces the yield of cationic protein and mobilizes intracellular calcium ions to a lesser extent. Nedocromil is available as an aerosol in cans containing 56 or 112 single doses of the drug, each dose containing 2 mg. The drug improves night symptoms in patients with bronchospastic reactions and reduces the need for bronchodilators. Not applicable for cupping acute attack bronchospasm. Adults and children over 12 years of age are prescribed 2 doses 4 times a day, maintenance therapy - 2 inhalations 2 times a day.

Lodoxamide (Alomid) is mainly used for allergic eye diseases: vernal keratoconjunctivitis, vernal keratitis and others, as well as for allergic reactions caused by wearing contact lenses. Doesn't show up when applied locally systemic action, no mutagenic or carcinogenic effects. Prescribed to adults and children over 2 years of age, 1-2 drops 4 times a day for no more than 3 months. It is not recommended to wear contact lenses during treatment.

Drugs in this group include cromoglicic acid, nedocromil, ketotifen.

Cromoglicic acid stabilizes mast cell membranes, preventing calcium ions from entering them. In this regard, degranulation of sensitized mast cells decreases (the release of leukotrienes, platelet activating factor, histamine and other mediators of inflammation and allergy stops). Due to this mechanism of action, cromoglycic acid preparations are extremely effective as a means of prevention(but not docking) bronchospasm. At systematic application the effect increases gradually, reaching a maximum after 2-4 weeks.

The greatest effectiveness was observed in children with atopic syndrome, which made it the drug of first choice in pediatric practice.

In adults, the effectiveness of using cromolyn sodium to prevent attacks is about 50%, which may be due to the late start of basic therapy.

Cromoglicic acid is practically insoluble in lipids and is poorly absorbed when taken orally, so it is used by inhalation (powder and liquid metered-dose aerosols) - 4 times a day

At bronchial asthma The following cromoglycic acid preparations are used: Cromolyn, Intal, Kropoz, Thaleum, etc. Due to the low ability of cromoglycic acid to be absorbed into the systemic circulation, the drugs have virtually no systemic side effects. Local side effects manifest themselves in the form of irritation of the mucous membrane of the respiratory tract: burning and sore throat, cough, short-term bronchospasm is possible.

In addition, cromoglycic acid preparations can be used for allergic rhinitis in the form of nasal drops or intranasal spray (Vividrin, Cromoglin, Cromosol) and allergic conjunctivitis in the form of eye drops (Vividrin, Cromohexal, Hi-Krom, Lecrolin).

Nedocromil(Tyled, Tyled mint) is available in the form of calcium and disodium salts (nedocromil sodium). Similar in action and use to cromoglycic acid, but more active . Used by inhalation, 8-17% of the substance is absorbed into the systemic circulation. Used as means of prevention(but not docking) bronchospasm. The effect increases gradually, reaching a maximum by the end of the 1st week of regular use. Prescribe 4 mg 2 - 4 times a day.

Ketotifen(Zaditen, Zetifen) has the properties of a stabilizer of mast cell membranes and a blocker of histamine H1 receptors. Almost completely absorbed from the intestines. Not very high bioavailability (about 50%) is explained by the effect of the first passage through the liver. Taken orally 1 mg 2 times a day (with meals).

The therapeutic effect is fully manifested after 1.5-2 months from the start of therapy.

For a long time the drug was used for anti-relapse treatment of asthma. However, in the 90s, a number of studies were carried out in accordance with GCP requirements, in which it was shown that ketotifen is significantly inferior in clinical effectiveness to sodium cromoglycate, and its advantages over placebo are not obvious. In this regard, the attitude towards the drug has been revised - today it is believed that it has no independent significance in the treatment of asthma. More often it is prescribed to prevent allergic skin reactions, hay fever, allergic rhinitis, conjunctivitis, and in the treatment of food allergies.

Side effects: sedative effect, slowed psychomotor reactions, drowsiness, dry mouth, weight gain, thrombocytopenia.

The drug is contraindicated during pregnancy.

According to modern concepts, bronchial asthma in children is a disease that develops on the basis of chronic allergic inflammation of the bronchi, causing repeated episodes of bronchial obstruction and hyperreactivity of the respiratory tract.

Characteristic features of allergic inflammation are an increased number of activated mast cells, eosinophils and Th2 lymphocytes in the mucosa bronchial tree and its lumen, an increase in microvascular permeability, desquamation of the epithelium, as well as an increase in the thickness of the reticular layer of the basement membrane.

The main provisions and approaches to the management of children with bronchial asthma are set out in the National Program “Bronchial Asthma in Children. Treatment strategy and prevention” (1997). The modern concept of the pathogenesis of the disease, based on allergic inflammation of the airways, predetermined the strategy for the treatment of bronchial asthma, namely, basic anti-inflammatory therapy. Drugs that can affect the main link in the pathogenesis of bronchial asthma—allergic inflammation of the airways—are an important and necessary component of the treatment of bronchial asthma in children. The choice of drug for treatment is determined by the severity of bronchial asthma, the age of sick children, considerations of effectiveness and risk side effects from the use of the drug.

Children with mild to moderate bronchial asthma are treated with drugs related to pharmacological group, indicated in the reference book “Register of Medicines of Russia. Encyclopedia of drugs. 2001” as stabilizers of mast cell membranes. The group of these drugs includes cromoglycic acid, nedocromil, ketotifen (Table 17-1).

Cromoglicic acid, synonym - sodium cromoglycate. (Drugs - Intal, Cromohexal, Chromogen, Chromogen easy breathing, Chromoglin, Chropoz).

Intal has been used in the treatment of bronchial asthma for about 30 years. In 1967, it was shown that cromoglycic acid can prevent the development of bronchospasm caused by inhalation of an allergen. The drug is a derivative of kellin, an active substance obtained from the extract of the seeds of the Mediterranean plant Ammi visnaga.

Cell membrane stabilizers

A drug	Release form	Recommended Doses
Cromoglycic acid/cromoglicate Intal	Powder for inhalation in capsules 20 mg	1 capsule 4 times a day via Spinhaler
	Metered aerosol for inhalation (200 doses) 1 inhalation dose -1 mg cromoglycic acid
	Metered aerosol for inhalation (112 doses) 1 inhalation dose -2 mg cromoglycic acid	2 inhalations 4 times a day
	Metered aerosol for inhalation (112 doses) 1 inhalation dose -5 mg cromoglycic acid	2 inhalations 4 times a day
	Solution for inhalation in ampoules of 2 ml 1 ml - 10 mg of cromoglycic acid	1 ampoule 4 times a day in inhalation using a compressor, ultrasonic inhaler through a face mask or mouthpiece
Intal plus	Metered aerosol for inhalation (200 doses) 1 inhalation dose - 1 mg cromoglycic acid and 100 mcg salbutamol
Ditek	Metered aerosol for inhalation (200 doses) 1 inhalation dose - 1 mg cromoglycic acid and 50 mcg fenoterol	1-2 inhalations 4 times a day
Nedocromil/nedocromil sodium Tailed Tiled mint	Metered aerosol for inhalation (112 doses) 1 inhalation dose - 2 mg nedocromil	2 inhalations 2-4 times a day
Ketotifen	Tablets 1 mg Syrup in a 100 ml bottle, 5 ml of syrup contains - 1 mg of ketotifen	1-2 tablets per day or 0.05 mg/kg/day

Cromoglycic acid prevents the development of the early and late phases of allergen-provoked bronchial obstruction, reduces bronchial hyperreactivity, prevents bronchospasm caused by physical activity, cold air and sulfur dioxide, and can prevent the occurrence of bronchospasm in response to antigen inhalation. However, cromoglycic acid does not have a bronchodilator or antihistamine effect [Belousov Yu.B. et al., 1996; Konig R, 2000; Krawiec M.E., 1999].

It is known that the main direction of its action is the ability to inhibit the process of degranulation of mast cells, eosinophils, neutrophils, and thereby prevent the release of inflammatory mediators and prevent the development of bronchospasm, the formation of inflammatory changes in the bronchi [KauA.V., 1987; Leung K.V., 1988].

It is believed that this mechanism of action of cromoglycic acid is due to its ability to inhibit calcium-dependent mechanisms of mediator release and prevent the entry of Ca 2+ ions into cells. An explanation for this is found in the ability of cromogicate to block membrane channels for the transport of chlorine ions. It is known that activation of low-conductivity chloride channels ensures the entry of CI ions into the cell and hyperpolarization of the cell membrane, which is necessary to maintain the entry of Ca 2+ ions into the cell and, accordingly, to ensure the process of degranulation of cells involved in allergic inflammatory reactions [Gushchin I.S., 1998; Janssen L.J., 1998; Zegara-Moran O., 1998]. Cromoglicic acid blocks the release of histamine, bradykinin, leukotrienes and other biologically active substances that contribute to the development of allergic reactions, inflammation and bronchospasm. There is evidence that cromoglycic acid acts on the bronchial receptor apparatus, increasing the sensitivity and concentration of beta-adrenergic receptors [Fedoseev G.B., 1998].

IN last years Another mechanism of action of cromoglycic acid has become known. The drug blocks reflex bronchoconstriction, which significantly expands its therapeutic effect. Evidence has been obtained that intal derivatives are capable of inhibiting the activation of C-fibers of the sensory endings of the vagus nerve in the bronchi, which release substance P and other neurokinins, which are mediators of neurogenic inflammation and lead to bronchoconstriction. Prophylactic use of cromoglycate inhibits reflex bronchospasm caused by stimulation of sensitive nerve C-fibers.

Pharmacokinetics. The cromoglycic acid molecule is highly polar and has lipophobic and acidic properties. At physiological pH values, cromoglycic acid is in an ionized state. Due to this, it is poorly absorbed into gastrointestinal tract. The slow absorption of the highly ionized compound ensures its relatively long-term presence on the bronchial mucosa. After inhalation, about 90% of the drug settles in the trachea and large bronchi, and only 10% reaches the small bronchi. With direct injection of cromoglycate (1 mg) into the 2nd order bronchus initial period the half-life is about 2 minutes, the terminal half-life is about 65 minutes, and the time to reach maximum concentration (about 9 ng/ml) in the blood is 15 minutes. The high degree of ionization of the molecule is also associated with the fact that cromoglycate does not penetrate cells, is not metabolized and is excreted from the body unchanged in urine and bile [Gushchin I.S., 1998].

Clinical application. Long-term use of the drug reduces and alleviates attacks of bronchial asthma in children, reduces the need for bronchodilators, and prevents the development of exacerbations. In children with severe frequent attacks of suffocation, the therapeutic effectiveness of Intal is inferior to inhaled corticosteroids, however, in some patients with severe disease, Intal has a pronounced positive effect, which in some cases makes it possible to avoid the prescription of corticosteroids or reduce the need for them.

Cromoglicic acid is a topical drug. Currently, the drug exists in the form of several inhalation forms: in powders, in the form of a dosed aerosol, in the form of a solution for inhalation. Until recently, the most common form of cromoglycic acid was powder capsules for inhalation. Each capsule contains 20 mg of cromoglycic acid with the addition of a small amount (0.1 mg) of isadrin. In this form, spraying the powder and inhaling it should be done with active inhalations using a special Spinhalera turbo inhaler, into which a capsule with the drug is placed. The need for the patient's active participation in the act of inhaling intal limits the prescription of the drug due to the age of the child. As a rule, Intal inhalation powders can be used by children over 5 years of age.

In the mid-80s, dosage forms of cromoglicic acid appeared in the form of a metered aerosol, which made it possible to treat children and younger children with the drug using a spacer and a face mask. Cromoglycic acid is available as a spray solution. Using a nebulizer operating with an air compressor (nebulizer) is most convenient for children under 2 years of age.

The frequency of inhalation of the drug is 4 times a day. The duration of action of the drug is 5 hours; if the patient has bronchial obstruction, to increase the bioavailability of the drug 5-10 minutes before taking it, 1-2 inhalations of a short-acting sympathomimetic (salbutamol, Berotec, terbutaline) are recommended. The therapeutic effect develops gradually. The effectiveness of the drug can be assessed after 2-4 weeks from the start of treatment. When remission is achieved, the dose of the drug is reduced and then discontinued, although Lately Long-term, and in some cases constant, use of cromones for bronchial asthma in children is considered appropriate as a “basic” therapy.

For mild asthma with rare attacks and for long periods remission courses of cromoglycic acid are prescribed to prevent seasonal exacerbations. Taking the drug for prophylactic purposes is also indicated for asthma due to physical exertion or contact with an allergen. In children with severe bronchial asthma, upon achieving clinical and functional remission, a decrease daily dose inhaled corticosteroids should be accompanied by the inclusion of cromone-type drugs in therapy.

Side effects of the drug are mainly due to local reactions. Some children experience irritation of the oral cavity, upper respiratory tract, cough, and sometimes bronchospasm due to the mechanical effects of the drug [Balabolkin I.I., 1985]. Although in the literature there are indications of isolated cases of the appearance of urticaria, eosinophilic pneumonia and allergic granulomatosis while taking sodium cromoglycate, nevertheless, in general, the drug is characterized by good tolerability and rare side effects [Belousov Yu.B. et al., 1996].

Since the second half of the 80s, in addition to cromoglycic acid, an inhaled drug with antiallergic and anti-inflammatory activity, nedocromil, a synonym for nedocromil sodium, has become widely used for “basic therapy” of bronchial asthma. The drug is produced in the form of a dosed aerosol for inhalation under the names Tilade and Tilade mint.

This drug is similar in both its chemical structure and mechanisms of action to cromoglycic acid, however, as experimental and clinical studies have demonstrated, it is 4-10 times more effective than Intal in preventing the formation of allergic reactions and the development of bronchospasm.

It has been shown that Tailed is able to suppress the activation and release of mediators from a large number of inflammatory cells: eosinophils, neutrophils, mast cells, monocytes, macrophages and platelets, which is associated with the drug’s effect on chloride channels of cell membranes.

The anti-inflammatory therapeutic effects of nedocromil sodium are also due to the ability to prevent the migration of eosinophils from the vascular bed and inhibit their activity. Nedocromil sodium is able to restore the functional activity of ciliated cells, namely, influence the beating of cilia, impaired in the presence of activated eosinophils, and also block the release of eosinophilic cationic protein by eosinophils.

Nedocromil sodium, like Intal, is able to inhibit bronchospasm caused by allergen inhalation, prevent the development of late allergic reactions and the formation of bronchial hyperreactivity, and influence neurogenic inflammation in the bronchi.

Clinical observations have shown that the use of nedocromil sodium in the treatment of bronchial asthma has fast action on the symptoms of the disease, improves functional indicators of the lungs, reduces nonspecific bronchial hyperreactivity.

In clinical studies, nedocromil has been shown to control asthma symptoms more effectively than cromoglycic acid, in some cases having similar effectiveness to inhaled corticosteroids. At the same time, the need for sympathomimetics during treatment with nedocromil is less than against the background of sodium cromoglycate [Belousov Yu.B. et al., 1996].

In adult patients, the drug is used as maintenance anti-inflammatory therapy at an early stage of the disease. Clinical studies of nedocromil sodium in children showed effectiveness therapeutic action drug, similar to adult patients.

Pharmacokinetics. After inhalation of nedocromil sodium, about 90% of the drug settles in the oral cavity, trachea and large bronchi, and only no more than 10% of the drug enters the small bronchi and lung tissue, where it affects the cells responsible for the formation of inflammation. Nedocromil sodium does not accumulate in the body, it is eliminated in urine and feces [Belousov Yu.B. et al., 1996].

The drug is available in the form of a metered aerosol for inhalation. In adults and children over 12 years of age, the drug is used to prevent exacerbation of asthma, starting from 2 mg (1 inhalation dose of the drug) twice a day to 4-8 mg 4 times a day. The effect of the drug should be assessed no earlier than a month from the start of treatment.

When treated with nedocromil sodium, in extremely rare cases, cough, bronchospasm, headache, mild dyspeptic disorders, nausea, rarely - vomiting and abdominal pain. In addition to cromoglycic acid and nedocromil, ketotifen is also a preventive anti-asthmatic membrane-stabilizing drug. Drugs - Zaditen, Zetifen, Ketotifen, Ketof.

Ketotifen does not have a bronchodilator effect and has antianaphylactic and antihistamine properties. Ketotifen blocks the response of the bronchial tree to inhalation of histamine, allergens, as well as allergic rhino-conjunctival and skin reactions in people sensitive to it.

Possible mechanisms of action of the drug are based on the ability of ketotifen to suppress the release of inflammatory mediators (histamine, leukotrienes) by mast cells, basophils and neutrophils, prevention of acute bronchospasm caused by leukotrienes (LTC4) and platelet activating factor (PAF), inhibition of the accumulation of eosinophils in the respiratory tract. Ketotifen eliminates tachyphylaxis of beta-adrenergic receptors and has a blocking effect on H1-histamine receptors [Belousov Yu.B. et al., 1996].

Controlled studies evaluating the therapeutic efficacy of ketotifen in asthma have had mixed results. A number of authors have testified that although ketotifen has a pronounced antiasthmatic effect in vitro, but in clinical practice it does not have the expected therapeutic effect in children suffering from bronchial asthma. However, most clinicians have concluded that long-term use of ketotifen in children leads to a slow but significant reduction in asthma symptoms and the need for other asthma medications.

An important point The therapeutic effect of ketotifen is its ability to influence allergy manifestations accompanying bronchial asthma. However, it is most effective when allergic dermatitis with a pronounced exudative component (eczema, recurrent angioedema, urticaria) [Balabolkin I.I., 1985].

The use of ketotifen is indicated for children with mild bronchial asthma, especially in cases where early age makes it difficult for a child to use inhaled sodium cromoglycate preparations, as well as in cases of combined manifestations of bronchial asthma and atopic dermatitis. Children under 4 years of age are recommended to take the drug twice a day, 0.5 mg (1/2 tablet or 2.5 syrup), children over 4 years of age - 1 mg in the morning and evening. Therapeutic effect when using ketotifen, it usually manifests itself within 10-14 days from the start of treatment, reaching a maximum after 1-2 months of therapy.

Ketotifen is well tolerated by patients. Possible side effects of the drug include sedation, especially at the beginning of taking the drug, dry mouth, dizziness, weight gain, and possible thrombocytopenia.

Thus, cromoglycic acid, nedocromil sodium, ketotifen are among the main “basic” drugs used in modern medicine for the prevention and treatment of bronchial asthma in children. They are especially effective for mild to moderate cases of the disease. Long-term, regular treatment with membrane-stabilizing drugs suppresses allergic inflammation in the bronchi, which is the pathogenetic basis of bronchial asthma.

Literature

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Directory of essential medicines Elena Yurievna Khramova

Mast cell membrane stabilizers

Mast cell membrane stabilizers are medicines, which counteract the entry of calcium into mast cells and thus lead to a decrease in histamine production. They have an antiallergic effect on the body, eliminate swelling of the bronchial mucosa. Some drugs in this group also have an antihistamine effect. They bind to histamine-sensitive receptors in various tissues and organs and act similarly to H1-histamine blockers.

Ketotifen

Active substance: ketotifen fumarate.

Pharmachologic effect: stabilizer of mast cell membranes, unexpressed H1-hist blocker. Inhibits the asthmatic reaction to allergic irritants. Used to prevent bronchospasm.

Indications: prevention and treatment allergic diseases, including bronchial asthma, allergic bronchitis, urticaria, skin rashes.

Contraindications: hypersensitivity to the drug, pregnancy, breastfeeding.

Side effects: drowsiness, lethargy, dizziness, slow reaction, increased fatigue, nervousness, sleep disturbance. Dryness in oral cavity, nausea, vomiting, stool retention.

Mode of application: orally during meals for adults and children over 3 years old - 1 mg 2 times a day; children from 6 months to 3 years – 0.5 mg 2 times a day; children under 6 months - in the form of syrup, 0.05 mg/kg body weight 2 times a day.

Release form: 1 mg tablets, 15 pieces in a blister. Capsules 1 mg, 60 pieces per package. Syrup - bottles of 60 or 100 ml (5 ml - 1 mg).

Special instructions: During treatment with the drug, you should not drive a car or engage in potentially dangerous species activities that require high concentration and quick reactions. Prescribe with extreme caution for epilepsy and liver disorders.

Intal

Active substance: cromoglycic acid.

Pharmachologic effect: anti-allergy agent, mast cell membrane stabilizer, prevents bronchospasm. Long-term therapy helps reduce the frequency of bronchial asthma attacks.

Indications: prevention and treatment of bronchial asthma, chronic obstructive pulmonary disease.

Contraindications: hypersensitivity to the drug, pregnancy early stages, breastfeeding period, childhood(up to 5 years – for aerosol; up to 2 years – for powder inhalations).

Mode of application: inhalation. Powder for inhalation for adults and children - 1 capsule 4 times a day (1 inhalation is required before bedtime). Aerosol for inhalation for adults and children over 5 years old - 2 doses (2-10 mg) 4 times a day. Solution for inhalation for adults and children – 20 mg 4 times a day. After achieving the desired effect, it is not recommended to abruptly stop therapy or discontinue the drug within a week.

Release form: aerosol for inhalation, in cylinders – 112 doses (5 mg/dose), 200 doses (1 mg/dose). Capsules with powder for inhalation, 20 mg, 10 pieces in a blister. Solution for inhalation in ampoules of 2 ml (1 ml – 10 mg).

Special instructions: The container must not be pierced or brought near fire, as the contents are under pressure.

Tailed mint

Active substance: nedocromil sodium.

Pharmachologic effect: anti-allergy agent, stabilizer of mast cell membranes, blocks the release of histamine. Long-term therapy with the drug improves the functioning of the bronchi, external respiratory function, reduces the frequency of attacks of choking and coughing.

Indications: bronchial asthma of various origins.

Contraindications: hypersensitivity to the components of the drug, childhood (up to 2 years), pregnancy in the early stages.

Side effects: cough, bronchospasm, nausea, gastrointestinal disorders, headache, unpleasant taste in the mouth.

Mode of application: inhalation for adults and children over 12 years of age – 2 doses (4 mg) 2–4 times a day; children under 12 years of age – no more than 10 mg per day (2–4 inhalations).

Release form: aerosol for inhalation, in bottles - 56 or 112 doses (2 mg/dose).

Special instructions: Therapy with the drug should not be interrupted; the drug is not used to block an acute asthmatic attack.

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