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What are antihistamines and which ones are better and more effective for children and adults? New generation antihistamines: high efficiency and affordability

Preparations of this group reduce the body's response to histamine, relieve spasm of smooth muscles, reduce capillary permeability, eliminate tissue edema, prevent the development and facilitate the course of allergic reactions. Some of them (diphenhydramine, diprazine) have a sedative effect.

Diphenhydramine(Dimedrolum) is one of the main representatives of the group of antihistamines that block Hi-receptors. Assign adults in tablets of 0.03-0.05 g 1-3 times a day, children - in smaller doses depending on age: up to 2 years old - 0.002-0.005 g each, up to 6 years old - 0.005-0.015 g each, from 7 to 12 years - 0.015-0.03 g per reception.

Rep.: Tab. Dimedroli 0.05 N. 20

D.S. 1 tablet 2-3 times a day (for allergic diseases). Course of treatment 10 days

Rp.: Sol. Dimedroli I % 1 ml D.t.d. N. 6 in amp. S. 1 ml intramuscularly

Zepfnaiv(Cetirizine). Synonyms: Zyrtec, Zirtec, Zyrtec.

It is a Hi-histamine receptor antagonist. Assign when allergic stomatitis, dermatitis, urticaria, angioedema. Adults and children aged 12 years and older are prescribed 0.01 g 1 time per day (in the evening) or 20 drops; children from 2 to 6 years - 5 mg (1/2 tablet) or 10 drops 1 time per day or 2.5 mg in the morning and evening. Patients with renal insufficiency are recommended to reduce the dose of the drug by 2 times. Available in tablets of 0.01 and 0.02 g and in drops in 10 ml vials.

Diprazine(Diprazinum). Synonyms: Pipolfen, A1-lergan, Antiallersin, Pipolphenum, Promethazine hydro-chloride, etc.

It has a high antihistamine and sedative activity, and also enhances the effect of narcotic, hypnotic, analgesic and local anesthetics. Assign inside adults at 0.025 and 0.05 g, intramuscularly - 1-2 ml of a 2.5% solution; children - depending on age: from 0.005 to 0.01 g 2-3 times a day.

Rep.: Tab. Diprazini 0.025 N. 10

D.S. 1 tablet 2-3 times daily (after meals) allergic diseases

Rp.: Sol. Diprazini 2.5% 1 ml D.t.d. N. 6 in amp. S. 1 ml intramuscularly

Suprastin(Suprastin) is an antihistamine drug with a sedative effect. Assign inside during meals, 0.025 g, 1 tablet 2-3 times a day. In severe cases, with allergies and anaphylactic shock, 1-2 ml of a 2% solution (0.02 g) is administered intramuscularly or intravenously.

Rep.: Tab. Suprastini 0.025 N. 20

D.S. 1 tablet 2-3 times a day with meals

Rp.: Sol. Suprastini 2% 1 ml D.t.d. N. 6 in amp. S. 1 ml intramuscularly

Diazolin(Diazolinum) is used to treat allergic diseases. Unlike diphenhydramine, sup-rastin and diprazine do not have a sedative and hypnotic effect. Assign inside after meals for adults 0.05-0.1-0.2 g 1-2 times a day, for children 0.02-0.05 g 1-2 times a day.

Rp.: Dragee Diazolini 0.05 N. 20

D.S. 1 tablet a day after meals

Fenkarol(Phencarolum) is an antihistamine drug that blocks hi-receptors and reduces the content of histamine in tissues. It has a high antihistamine activity in the treatment of allergic diseases. Unlike diphenhydramine and diprazine, it does not have a pronounced sedative and hypnotic effect. Assign inside after eating 0.025-0.05 g 3-4 times a day. The course of treatment is 10-20 days. Available in powder and tablet form.

Rep.: Tab. Phencaroli 0.025 N.50

D.S. 1 tablet 3 times a day

Tavegil(Tavegil). Synonyms: Clemastin, Fenistil, Alagyl, Anhistan, etc.

Antihistamine drug. Its properties are close to diphenhydramine, but more active and longer acting (8-12 hours). After a single dose, it has a moderate sedative effect: it enhances the effect of sleeping pills and alcohol. When taking tavegil, you should not take alcoholic beverages. Assign inside 1 tablet 2 times a day in the morning and evening. Children 6-12 years old are given 1/3 tablet 2 times a day.

Rep.: Tab. Tavegili 0.001 N. 20

D.S. 1 tablet 2 times a day after meals

Rp.: Tavegili 2 ml

D.t.d. N. 5 in amp. S. 2 ml intramuscularly

Terfenadine(Terfenadin). Synonyms: Bronal, Ter-fed, Terfena, Treksil, Histadin, Rapidal, etc.

It has an antihistamine effect, blocks Hi-histamine receptors. The chemical structure is similar to fencarol. Well absorbed in the gastrointestinal tract. The action of the drug develops 1-2 hours after administration, the maximum of its action occurs after 3-4 hours, the duration of action is 12 hours. Terfenadine, like phencarol, does not penetrate the blood-brain barrier and does not have a pronounced sedative effect.

Used in the treatment of allergic medicinal stomatitis, dermatitis; contact stomatitis, angioedema.

Adults and children over 12 years old are prescribed 0.06 g (60 mg) 2 times a day, children from 6 to 12 years old - 30 mg 2 times a day.

It is produced in the form of tablets of 0.06 g (60 mg) and 0.12 g (120 mg) and a suspension containing 0.03 g of the drug in 5 ml (1 teaspoon).

Loratadine(Loratadine). Synonyms: Claritin, C1a-ritin.

Antihistamine drug. Blocks Hi-histamine receptors. The onset of action of the drug is after 30 minutes, the duration of action is 24 hours. Due to the duration of the therapeutic effect, loratadine is referred to as antihistamines of the second or third generation. Loratadine is not addictive and does not affect the central nervous system. It has anti-allergic and anti-exudative action. Reduces capillary permeability, eliminates edema, relieves spasms of smooth muscles.

Loratadine is used to treat allergic rhinitis, conjunctivitis, urticaria, Quincke's edema, contact allergic stomatitis and dermatitis.

The drug is administered orally in tablets or as a syrup. Adults and children over 12 years old - 1 tablet or 2 teaspoons of syrup; children from 2 to 12 years old - 1/2 tablet or 1 teaspoon of syrup.

Available in tablets of 0.01 g (10 mg) in a package of 10 pieces or as a syrup in 120 ml vials.

Astemizol(Astemizole). Synonyms: Astelong, Histazol, Histalong, Mibiron, Hismanal, Histamanal, etc.

Antiallergic drug, Hi-histamine receptor blocker. It has some antiserotonin activity. Due to the long-term action, astemizole is considered a second-generation antihistamine. Taking the drug once a day is sufficient to suppress allergic reactions within 24 hours.

Used in the treatment of allergic rhinitis (hay fever), urticaria, Quincke's edema and other allergic conditions.

Adults and children over 12 years of age are prescribed 1 tablet - 0.01 g (10 mg) 1 time per day on an empty stomach. In severe cases, the dose is increased to 3 tablets per day. The maximum period of taking the drug is 7 days. Children aged 6 to 12 years are given 5 mg (1 / s tablet) per day, from 2 to 6 years - 2 mg per 10 kg of body weight.

It is produced in tablets of 0.01 g (10 mg) in a package of 10 pieces and as a suspension in 50 ml vials containing 0.005 g (5 mg) of the drug in 5 ml (1 teaspoon).

Cyproheptadine(Cyproheptadine). Synonyms: Peritol, Adekin, Ciprastin, Cyprodin, etc.

It has antihistamine activity (blocks Hj-histamine receptors); has a pronounced antiserotonin (reduces spasmodic and other symptoms caused by serotonin) and anticholinergic (blocks M-cholinergic receptors) action.

Cyproheptadine prevents the development and facilitates the course of allergic reactions. It has antiallergic, antiexudative and antipruritic effect. Effective in the treatment of itchy dermatoses. Cyproheptadine is used as an antiallergic agent for the treatment of urticaria, Quincke's edema, migraine, vasomotor rhinitis, hay fever, neurodermatitis, drug stomatitis, contact stomatitis and dermatitis.

The drug is administered orally: adults - 4 mg (1 tablet) 3-4 times a day, children from 6 months to 2 years - with caution in a daily dose of 0.4 mg / kg, from 2 to

6 years - up to 6 mg per day (1/3 tablet 3 times a day), from 6 to 14 years - up to 12 mg per day (1 tablet 3 times a day)

Produced in tablets of 4 mg in a package of 20 pieces and in the form of syrup in vials of 100 ml (in 1 ml 0.4 mg of the drug).


are substances that inhibit the action of free histamine. When an allergen enters the body, histamine is released from mast cells. connective tissue included in the body's immune system. It begins to interact with specific receptors and cause itching, swelling, rash and other allergic manifestations. Antihistamines are responsible for blocking these receptors. There are three generations of these drugs.


1st generation antihistamines

They appeared in 1936 and continue to be used. These drugs reversibly bind to H1 receptors, which explains the need for a large dosage and high frequency of administration.

Antihistamines of the 1st generation are characterized by the following pharmacological properties:

    reduce muscle tone;

    have a sedative, hypnotic and anticholinergic effect;

    potentiate the effects of alcohol;

    have a local anesthetic effect;

    give a quick and strong, but short-term (4-8 hours) therapeutic effect;

    long-term use reduces antihistamine activity, so every 2-3 weeks the funds are changed.

The bulk of 1st generation antihistamines are fat-soluble, can overcome the blood-brain barrier and bind to the H1 receptors of the brain, which explains the sedative effect of these drugs, which is enhanced after taking alcohol or psychotropic drugs. When taking medium therapeutic doses in children and high toxic doses in adults, psychomotor agitation may be observed. Due to the presence of a sedative effect, 1st generation antihistamines are not prescribed to persons whose activities require increased attention.

The anticholinergic properties of these drugs cause atropine-like reactions, such as dryness of the nasopharynx and mouth, urinary retention, visual impairment. These features can be beneficial when, but they can increase airway obstruction caused by bronchial (sputum viscosity increases), exacerbate prostate adenoma, glaucoma and other diseases. At the same time, these drugs have an antiemetic and anti-swaying effect, reduce the manifestation of parkinsonism.

A number of these antihistamines are included in the composition combined funds, which are used for colds, motion sickness or have a sedative or hypnotic effect.

An extensive list of side effects from taking these antihistamines makes them less likely to be used in the treatment of allergic diseases. Many developed countries have banned their implementation.

Diphenhydramine is prescribed for hay, urticaria, sea, air sickness, vasomotor, bronchial asthma, with allergic reactions caused by the introduction medicinal substances(e.g. antibiotics), in the treatment peptic ulcer, dermatoses, etc.

    Advantages: high antihistamine activity, reduced severity of allergic, pseudo-allergic reactions. Diphenhydramine has antiemetic and antitussive effects, has a local anesthetic effect, due to which it is an alternative to Novocaine and Lidocaine in case of their intolerance.

    Cons: unpredictability of the consequences of taking the drug, its effects on the central nervous system. It can cause urinary retention and dry mucous membranes. Side effects include sedative and hypnotic effects.

Diazolin

Diazolin has the same indications for use as other antihistamines, but differs from them in the features of the effect.

    Advantages: a mild sedative effect allows it to be used where it is undesirable to have a depressing effect on the central nervous system.

    Cons: irritates the mucous membranes of the gastrointestinal tract, causes dizziness, impaired urination, drowsiness, slows down mental and motor reactions. There is information about the toxic effect of the drug on nerve cells.

Suprastin

Suprastin is prescribed for the treatment of seasonal and chronic allergic conjunctivitis, urticaria, atopic, Quincke's edema, itching of various etiologies,. It is used in parenteral form for those requiring emergency care acute allergic conditions.

    Advantages: it does not accumulate in the blood serum, therefore, even with long-term use does not cause overdose. Due to the high antihistamine activity, a rapid therapeutic effect is observed.

    Cons: side effects - drowsiness, dizziness, inhibition of reactions, etc. - are present, although they are less pronounced. The therapeutic effect is short-term, in order to prolong it, Suprastin is combined with H1-blockers that do not have sedative properties.

in the form of injections used for angioedema, as well as anaphylactic shock, as a prophylactic and therapeutic agent for allergic and pseudo-allergic reactions.

    Advantages: It has a longer and stronger antihistamine effect than Diphenhydramine, and has a more moderate sedative effect.

    Cons: can itself cause an allergic reaction, has some inhibitory effect.

Fenkarol

Phencarol is prescribed when addiction to other antihistamines appears.

    Advantages: it has a weak sedative effect, does not have a pronounced inhibitory effect on the central nervous system, has low toxicity, blocks H1 receptors, and is able to reduce the content of histamine in tissues.

    Cons: less antihistamine activity in comparison with Diphenhydramine. Fenkarol is used with caution in the presence of diseases of the gastrointestinal tract, cardiovascular system and liver.

2nd generation antihistamines

They have advantages over first generation drugs:

    there is no sedative and anticholinergic effect, since these drugs do not cross the blood-brain barrier, only some individuals experience moderate drowsiness;

    mental activity, physical activity do not suffer;

    the effect of the drugs reaches 24 hours, so they are taken once a day;

    they are not addictive, which allows them to be prescribed for a long time (3-12 months);

    when you stop taking the drugs, the therapeutic effect lasts about a week;

    drugs are not adsorbed with food in the gastrointestinal tract.

But 2nd generation antihistamines have a cardiotoxic effect. varying degrees Therefore, when they are taken, cardiac activity is monitored. They are contraindicated in elderly patients and patients suffering from disorders of the cardiovascular system.

The Emergence of Cardio toxic action due to the ability of 2nd generation antihistamines to block potassium channels hearts. The risk is increased when these drugs are combined with antifungal drugs, macrolides, antidepressants, grapefruit juice, and if the patient has severe liver dysfunction.

Claridol and Clarisens

used to treat seasonal as well as cyclic allergic rhinitis, allergic, Quincke's edema and a number of other diseases of allergic origin. It copes with pseudo-allergic syndromes and allergies to insect bites. Included in the complex measures for the treatment of itchy dermatoses.

    Benefits: Claridol has antipruritic, antiallergic, antiexudative effects. The drug reduces capillary permeability, prevents the development of edema, relieves spasm of smooth muscles. It does not affect the central nervous system, has no anticholinergic and sedative effect.

    Cons: occasionally after taking Claridol, patients complain of dry mouth, nausea and vomiting.

Clarotadine

Clarotadine contains the active substance loratadine, which is a selective blocker of H1-histamine receptors, on which it has a direct effect, allowing you to avoid unwanted effects inherent in other antihistamines. Indications for use are allergic conjunctivitis, acute chronic and idiopathic urticaria, rhinitis, pseudo-allergic reactions associated with the release of histamine, allergic insect bites, itchy dermatoses.

    Advantages: the drug does not have a sedative effect, is not addictive, acts quickly and for a long time.

    Cons: undesirable consequences of taking Clarodin include disorders nervous system: asthenia, anxiety, drowsiness, depression, amnesia, tremor, agitation in a child. Dermatitis may appear on the skin. Frequent and painful urination, constipation and diarrhea. Weight gain due to dysfunction endocrine system. The defeat of the respiratory system can be manifested by cough, bronchospasm, sinusitis and similar manifestations.

shown at allergic rhinitis(rhinitis) of a seasonal and permanent nature, skin rashes of allergic origin, pseudo-allergies, reactions to insect bites, allergic inflammation mucous membrane of the eyeball.

    Benefits: Lomilan is able to relieve itching, reduce the tone of smooth muscles and the production of exudate (a special fluid that appears when inflammatory process), to prevent tissue edema already after half an hour from the moment of taking the drug. The greatest efficiency comes in 8-12 hours, then subsides. Lomilan is not addictive and does not negative impact on the activity of the nervous system.

    Cons: adverse reactions are rare, manifested by headache, fatigue and drowsiness, inflammation of the gastric mucosa, nausea.

LauraGeksal

    Advantages: the drug has neither anticholinergic nor central action, its intake does not affect the attention, psychomotor functions, working capacity and mental qualities of the patient.

    Cons: LoraGeksal is usually well tolerated, but occasionally it causes fatigue, dry mouth, headache, tachycardia, dizziness, allergic reactions, cough, vomiting, gastritis, liver dysfunction.

Claritin

Claritin contains an active ingredient - loratadine, which blocks H1-histamine receptors and prevents the release of histamine, bradycanin and serotonin. Antihistamine effectiveness lasts a day, and therapeutic comes after 8-12 hours. Claritin is prescribed for the treatment of allergic rhinitis, allergic skin reactions, food allergies and mild bronchial asthma.

    Advantages: high efficiency in the treatment of allergic diseases, the drug is not addictive, drowsiness.

    Cons: cases of side effects are rare, they are manifested by nausea, headache, gastritis, agitation, allergic reactions, drowsiness.

Rupafin

Rupafin has a unique active ingredient- rupatadine, which is distinguished by antihistamine activity and a selective effect on H1-histamine peripheral receptors. It is prescribed for chronic idiopathic urticaria and allergic rhinitis.

    Advantages: Rupafin effectively copes with the symptoms of the allergic diseases listed above and does not affect the functioning of the central nervous system.

    Cons: undesirable consequences of taking the drug - asthenia, dizziness, fatigue, headache, drowsiness, dry mouth. It can affect the respiratory, nervous, musculoskeletal, and digestive systems, as well as metabolism and skin.

Zyrtec

Zyrtec is a competitive antagonist of the hydroxyzine metabolite, histamine. The drug facilitates the course and sometimes prevents the development of allergic reactions. Zyrtec limits the release of mediators, reduces the migration of eosinophils, basophils, neutrophils. The drug is used for allergic rhinitis, bronchial asthma, urticaria, conjunctivitis, dermatitis, fever, skin, angioedema.

    Benefits: effectively prevents the occurrence of edema, reduces capillary permeability, relieves smooth muscle spasm. Zyrtec does not have anticholinergic and antiserotonin effects.

    Cons: improper use of the drug can lead to migraines, drowsiness, allergic reactions.

blocks histamine receptors that increase vascular permeability, causing muscle spasms leading to an allergic reaction. It is used to treat allergic conjunctivitis, rhinitis and chronic idiopathic urticaria.

    Advantages: the drug acts an hour after application, the therapeutic effect lasts for 2 days. A five-day intake of Kestin allows you to maintain an antihistamine effect for about 6 days. Sedative effects are practically non-existent.

    Cons: the use of Kestin can cause insomnia, abdominal pain, nausea, drowsiness, asthenia, headache, sinusitis, dry mouth.

New antihistamines, 3rd generation

These substances are prodrugs, which means that when they enter the body, they are converted from their original form into pharmacologically active metabolites.

All 3rd generation antihistamines do not have a cardiotoxic and sedative effect, so they can be used by people whose activities are related to high concentration attention.

These drugs block H1 receptors, and also have an additional effect on allergic manifestations. They have high selectivity, do not overcome the blood-brain barrier, so they are not peculiar to Negative consequences from the side of the central nervous system, absent side effect on .

The presence of additional effects contributes to the use of 3rd generation antihistamines in long-term treatment most allergic manifestations.

prescribed as a therapeutic and prophylactic agent for hay fever, allergic skin reactions, including urticaria, allergic rhinitis. The effect of the drug develops within 24 hours and reaches a maximum after 9-12 days. Its duration depends on the previous therapy.

    Advantages: the drug has practically no sedative effect, does not enhance the effect of taking sleeping pills or alcohol. It also does not affect the ability to drive a car or mental activity.

    Cons: Gismanal can cause increased appetite, dry mucous membranes, tachycardia, drowsiness, QT prolongation, palpitations, collapse.

is a fast-acting, selectively active H1 receptor antagonist derived from buterophenol, which differs chemical structure from analogues. It is used in allergic rhinitis to relieve its symptoms, allergic dermatological manifestations (dermographism, contact dermatitis, urticaria, atonic eczema,), asthma, atonic and provoked by exercise, as well as in connection with acute allergic reactions to various irritants.

    Benefits: no sedative and anticholinergic effect, no effect on psychomotor activity and well-being of a person. The drug is safe to use in patients with glaucoma and prostate disorders.

- a highly effective antihistamine drug, which is a metabolite of terfenadine, therefore, has a great similarity with histamine H1 receptors. Telfast binds to them and blocks them, preventing their biological manifestations as allergic symptoms. Mast cell membranes are stabilized and the release of histamine from them is reduced. Indications for use are angioedema, urticaria, hay fever.

    Advantages: does not show sedative properties, does not affect the speed of reactions and concentration of attention, heart function, is not addictive, highly effective against the symptoms and causes of allergic diseases.

    Cons: rare consequences of taking the drug are headache, nausea, dizziness, very rarely there is shortness of breath, anaphylactic reaction, skin flushing.

The drug is used to treat seasonal allergic rhinitis with the following manifestations of hay fever: pruritus, sneezing, rhinitis, redness of the mucous membrane of the eyes, as well as for the treatment of chronic idiopathic urticaria and its symptoms: skin itching, redness.

    Advantages- when taking the drug, side effects characteristic of antihistamines do not appear: visual impairment, constipation, dryness of the oral mucosa, weight gain, negative action for the work of the heart muscle. The drug can be purchased at a pharmacy without a prescription, no dose adjustment is required for the elderly, patients and renal and hepatic insufficiency. The drug acts quickly, maintaining its effect during the day. The price of the drug is not too high, it is available to many people suffering from.

    Flaws- after some time, addiction to the action of the drug is possible, it has side effects: dyspepsia, dysmenorrhea, tachycardia, headache and dizziness, anaphylactic reactions, taste perversion. Dependence on the drug may form.

The drug is prescribed for the appearance of seasonal allergic rhinitis, as well as for chronic.

    Advantages- the drug is rapidly absorbed, reaching the desired one within an hour after ingestion, this action continues for a day. Its reception does not require restrictions for people operating complex mechanisms, driving vehicles, and does not cause a sedative effect. Fexofast is available without a prescription, has an affordable price, and is highly effective.

    Flaws- for some patients, the drug brings only temporary relief, without bringing a complete recovery from the manifestations of allergies. It has side effects: swelling, increased drowsiness, nervousness, insomnia, weakness, increased allergy symptoms in the form of itching, skin rash.

The drug is prescribed for symptomatic treatment hay fever (pollinosis), urticaria, allergic and allergic conjunctivitis with itching, lacrimation, conjunctival hyperemia, dermatosis with rash and rashes, angioedema.

    Advantages– Levocitirizine-Teva quickly shows its effectiveness (after 12-60 minutes) and during the day it prevents the appearance and weakens the course of allergic reactions. The drug is rapidly absorbed, showing 100% bioavailability. Can be used for long-term treatment and for emergency assistance with seasonal exacerbations of allergies. Available for the treatment of children from 6 years.

    Flaws- has such side effects as drowsiness, irritability, nausea, headache, weight gain, tachycardia, abdominal pain, migraine. The price of the medicine is quite high.

The drug is used for the symptomatic treatment of such manifestations of pollinosis and urticaria as skin itching, sneezing, inflammation of the conjunctiva, rhinorrhea, Quincke's edema, allergic dermatoses.

    Advantages– Ksizal has a pronounced anti-allergic orientation, being a very effective remedy. It prevents the onset of allergy symptoms, facilitates their course, and has no sedative effect. The drug acts very quickly, maintaining its effect for a day from the moment of administration. Xyzal can be used to treat children from 2 years of age, it is available in two dosage forms(tablets, drops), acceptable for use in pediatrics. It eliminates nasal congestion, the symptoms of chronic allergies are quickly stopped, it does not have a toxic effect on the heart and central nervous system.

    Flaws- the remedy may exhibit the following side effects: dry mouth, fatigue, abdominal pain, pruritus, hallucinations, shortness of breath, convulsions, muscle pain.

The drug is indicated for the treatment seasonal hay fever, allergic rhinitis, chronic idiopathic urticaria with symptoms such as lacrimation, cough, itching, swelling of the nasopharyngeal mucosa.

    Advantages- Erius acts exceptionally quickly on allergy symptoms, can be used to treat children from one year old, as it has a high degree security. Well tolerated by both adults and children, it is available in several dosage forms (tablets, syrup), which is very convenient for use in pediatrics. It can be taken for a long time period (up to a year) without causing addiction (resistance to it). Reliably stops the manifestations of the initial phase of the allergic response. After a course of treatment, the effect of it persists for 10-14 days. Overdose symptoms were not observed even with a fivefold increase in the dose of Erius.

    Flaws- side effects may occur (nausea and headache, tachycardia, local allergic symptoms, diarrhea, hyperthermia). Children usually have insomnia, headache, fever.

The drug is intended for the treatment of allergic manifestations such as allergic rhinitis, and urticaria, marked by itching and skin rashes. The drug stops such symptoms of allergic rhinitis as sneezing, itching in the nose and in the sky, watery eyes.

    Advantages– Desal prevents the appearance of edema, muscle spasm, reduces capillary permeability. The effect of taking the drug can be seen after 20 minutes, it lasts for a day. A single dose of the medicine is very convenient, two forms of its release are syrup and tablets, the intake of which does not depend on food. Since Desal is taken to treat children from 12 months of age, the syrup form of the drug is in demand. The drug is so safe that even a 9-fold excess of the dose does not lead to negative symptoms.

    Flaws- occasionally, symptoms of side effects such as increased fatigue, headache, dryness of the oral mucosa may occur. Additionally, side effects such as insomnia, tachycardia, the appearance of hallucinations, diarrhea, and hyperactivity are manifested. Allergic manifestations of side effects are possible: itching, urticaria, angioedema.

4th generation antihistamines - do they exist?

All statements of advertisers positioning trade marks drugs like "fourth-generation antihistamines" are nothing more than a publicity stunt. This pharmacological group does not exist, although marketers refer to it not only newly created drugs, but also second-generation drugs.

The official classification indicates only two groups of antihistamines - these are first and second generation drugs. The third group of pharmacologically active metabolites is positioned in pharmaceuticals as "H 1 histamine blockers of the third generation."


For the treatment of allergic manifestations in children, antihistamines of all three generations are used.

Antihistamines of the 1st generation are distinguished by the fact that they quickly show their healing properties and are excreted from the body. They are in demand for treatment. acute manifestations allergic reactions. They are appointed short courses. The most effective of this group is Tavegil, Suprastin, Diazolin, Fenkarol.

A significant percentage of side effects leads to a reduction in the use of these drugs for childhood allergies.

Antihistamines of the 2nd generation do not cause sedation, act for a longer time and are usually used once a day. Few side effects. Among the drugs in this group, Ketotifen, Fenistil, Cetrin are used to treat manifestations of childhood allergies.

3rd generation antihistamines for children include Gismanal, Terfen and others. They are used in chronic allergic processes, because they are able to for a long time be in the body. There are no side effects.

Erius can be attributed to newer drugs.

Negative consequences:

    1st generation: headache, constipation, tachycardia, drowsiness, dry mouth, blurred vision, urinary retention and lack of appetite;

    2 generation: Negative influence on the heart and;

For children, antihistamines are produced in the form of ointments (allergic reactions on the skin), drops, syrups and tablets for oral administration.

Antihistamines during pregnancy

In the first trimester of pregnancy, it is forbidden to take antihistamines. In the second they are appointed only in extreme cases because none of these remedies are completely safe.

Natural antihistamines, which include vitamins C, B12, pantothenic, oleic and nicotinic acid, zinc, fish oil.

The safest antihistamines are Claritin, Zirtek, Telfast, Avil, but their use must be agreed with the doctor without fail.


About the doctor: From 2010 to 2016 practicing physician of the therapeutic hospital of the central medical unit No. 21, the city of Elektrostal. Since 2016 he has been working in diagnostic center №3.

Allergic reactions are often a phenomenon, especially in babies, antihistamines for children help to deal with this nuisance. Timely intake of these medicines will help eliminate allergy symptoms and avoid serious illnesses(bronchial asthma, angioedema, atypical dermatitis, etc.). In some cases, preventive medication is indicated. For example, to avoid seasonal allergic rhinitis, you need to start taking the medicine about a week before the flowering of trees and plants. Then the allergy will not manifest itself.

How does an allergy occur?

To understand how antihistamines work, you need to know exactly how an allergic reaction occurs. The human immune system produces histamine, a special substance that does not manifest itself in the normal state. Under the influence of certain factors, histamine is activated, and its amount increases markedly. This substance acts on special receptors that cause various reactions - tearfulness, runny nose, swelling of mucous membranes, shortness of breath, skin reactions. In this case, the causative agent of allergies is not dangerous for the body, but the immune system tries to fight it. In addition to the usual manifestations of allergies, histamine can cause the following conditions in babies:

  • gastrointestinal disorders - vomiting, nausea, indigestion, colic;
  • pathological changes in the internal organs with smooth muscles;
  • violations of the heart and changes in vascular tone - lowering blood pressure, arrhythmia, tachycardia, etc.;
  • non-standard skin reaction, manifested in the form of blisters, swelling of the skin, itching, peeling, etc.

It is important to know that antihistamines do not treat allergies or stop exposure to the allergen, they only combat the symptoms. Allergy cannot be cured at all, since this disease is caused by human immunity.


Features of antihistamines for children, and when to take them

Due to unstable immunity, children are more likely to suffer from allergic reactions than adults, but their body can react very sharply and unpredictably to the medicine. For this reason, children can be given drugs with a minimum number of side effects, mild action and fairly high efficiency. Many companies produce allergy medicines in children's doses in drops, syrup or suspension. This makes it easier to take the drug and does not cause aversion in the child to treatment. Also, in most cases, you can use antihistamines in the form of a gel. They are used externally from birth if there is an allergic skin reaction (for example, to an insect bite).

Antihistamines of the 4th generation are distinguished by their effectiveness and prolonged action, but they should not be given to children under 6 years of age, as intoxication and disruption of the internal organs are possible.

Many of the best new generation drugs fight not only with allergies, but have additional pharmacological properties, so their use is different. Most of the old and time-tested drugs have a sedative effect, which is relevant if the sick baby is anxious and cannot sleep for a long time. Also, many antiallergic drugs enhance the effect of concomitant medications, so they are often taken together with antipyretic drugs for colds, runny nose, and chickenpox in children. Also, antihistamines are often used before vaccination to reduce stress on the body and avoid an allergic reaction to the vaccine.

Important: you need to choose a drug for your baby together with the doctor. If this is not possible, and the child needs to be treated for allergies as soon as possible, then it is important to take into account the symptoms, the cause of the allergy and the age of the child, as Dr. Komarovsky advises.


First generation antihistamines

These remedies, despite their "advanced" age, are considered the best in cases where an allergy is accompanied by a cold, the child gets sick chickenpox. Experiencing great anxiety and overexcitation due to illness. The best drugs in this category include:

  • Dimedrol. In the form of an injection, it is allowed for children from 7 months (0.5 ml per day), from 1 year to 3 years - 1 ml per day. Dimedrol tablets are safe for children up to 12 months at a dosage of 2 mg per day, up to 5 years - 5 mg per day, up to 12 years - 20 mg per day. This medicine has a strong sedative and analgesic effect, it fights well with skin manifestations of allergies, but it is better not to use it for swelling of the mucous membranes of the nasopharynx and bronchospasm.
  • Psilo balm. Ointment for external use based on Dimedrol, which can be used for allergies in babies up to a year old. A small amount of ointment is applied to the affected area and rubbed thoroughly.
  • Diazolin. A drug with analgesic and sedative effects that can be given to children from two years of age. Effective in laryngospasms and severe swelling. The daily dose for children 2 years old is 50-100 mg, for children from 5 to 10 years old - 100-200 mg.
  • Tavegil (Clemastin). Effective for allergies that have skin manifestations. In the form of tablets, it is allowed for children from 6 years of age. From 6 to 12 years old daily dose should be 0.5 - 1 tablet, which is taken either at bedtime or during breakfast. From 1 year old, you can also use Tavegil syrup, which is taken 2 times a day - in the morning and at bedtime at the dosage indicated in the instructions.
  • Fenkarol. The drug is used for laryngospasm, allergic rhinitis, for all skin manifestations allergies. The tool is powerful, but toxic, so it should not be given to children under 3 years old. The exception is Fenkarol in powder 5 mg, which can be taken 2-3 times a day.

First generation antihistamines long-term use need to be replaced every 2 weeks, as they are addictive, as a result of which their effectiveness is reduced. The price of such drugs is usually very low.


Second generation antihistamines

Means of this generation do not cause drowsiness in adults, but a pronounced sedative effect may occur in children. Therefore, if the allergy is not too strong, it is best to give the drug to the baby at bedtime. A list of the best drugs suitable for children is given below.

  • Zodak. An effective medicine that has proven itself in the treatment seasonal allergies, urticaria, rhinitis, allergic conjunctivitis. Available in tablets, drops and syrup. Babies from 1 year old are given 5 drops twice a day, and children over 6 years old - 0.5 tablets each. The syrup can be taken by children from 2 years old, 1 spoon once a day. This dose can be halved and taken in the morning and at bedtime.
  • Tsetrin. This drug is similar in its action to the Zodak, you need to take it in exactly the same way.
  • Fenistil. The remedy, which is suitable for infants from 1 month old, is available in drops. Effective in the fight against seasonal allergies, hives, it can be given to a child before vaccination. Also, Fenistil can be taken by mothers of infants during lactation. The drug practically does not cause drowsiness and addiction. Fenistil, produced in the form of a gel, can also be used externally for children from 1 month old.

Important! Allergy treatment for newborns should be selected together with a doctor, since even the most harmless drugs can be dangerous for a child of this age.


Third generation antihistamines

These are metabolite drugs that are devoid of a sedative effect. They are not addictive and act much longer than their predecessors (up to 3 days).

Telfast (Fexofast). This is one of the few 3rd generation antihistamines that does not cause side effects in children. It can be taken by children from 5 years old (up to 60 mg). Children from 12 years old can take 120-180 mg. Telfast is usually taken as a single dose skin allergies and very quickly eliminates allergy symptoms. This strong drug, which Dr. Komarovsky advises to use only in extreme cases. In some cases, it is prescribed before vaccination.

Fourth generation antihistamines

The latest generation of drugs are characterized by almost instantaneous action and versatility. In addition, they can be taken every few days for a long time. The list of the best of them, judging by the reviews, is given below:

  • Erius. In the form of a syrup, you can give children from one year of age 2.5 ml per day, from 6 to 12 years old - 5 ml per day. Erius tablets can be taken from the age of 12, preferably only 1 time.
  • Xizal (Glenset). basis this drug is levocetrizine. It can be prescribed to children from 6 years of age, 5 mg once.

Flaw the latest drugs lies in the fact that they all release in adult dosage, so it is likely that the child will have side effects.


What antihistamines are suitable for children of different ages?

No absolutely safe drugs for newborns and while breastfeeding, but in critical cases it is recommended to take the following drugs:

  • Fenkarol;
  • Fenistil;
  • Tavegil;
  • Donormil;
  • clemastine;
  • Diphenhydramine;
  • Bravegil.

Nursing mothers can take Zyrtec as a single dose, as it is very effective and has a long-lasting effect.

For children from three to five years old, such drugs are not bad:

  • Erus;
  • Claritin;
  • Cetrin;
  • Diazolin;

All these drugs can be taken 1 tablet per day. Their price is quite high, so it makes sense to pay attention to cheaper analogues:

  • Zodal;
  • Litesin;
  • Zetrinal;
  • Cetrinax.

After 6 years, children are often prescribed new drugs:

  • clemastine;
  • Zyrtec;
  • Terfenadine.

If the child's condition worsens, or new symptoms appear after taking the drug, you should immediately stop taking the drug. In case of severe swelling, you should immediately call an ambulance.

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Types of drugs

Allocate antihistamines of the 1st, 2nd and 3rd generations.

First generation drugs are enough effective pills, powders and ointments, which quickly remove all allergic manifestations, but are practically not prescribed for long-term systemic treatment, as they have a number of side effects, even with exact dosage.

One of the main disadvantages of these drugs is a strong effect on the central nervous system, heart and blood vessels.

They are contraindicated for the elderly, pregnant women and children, which is why this group is called sedative.

They are used only in emergency cases when quick help is needed:

  • with Quincke's edema;
  • with seasonal hay fever;
  • with extensive skin rashes;
  • with acute food or drug allergies.

As soon as acute stage passed, these funds are replaced by others, more gentle.

Allergy remedies related specifically to the first generation:

  1. Suprastin;
  2. Diazolin;
  3. Dimedrol.

Second-generation allergy drugs belong to the non-sedative group, they are more a wide range actions in comparison with the drugs of the first.

They are prescribed for:

  1. various hay fever;
  2. atopic dermatitis;
  3. bronchial asthma.

They act softer, but also have their drawbacks.

A striking example similar drugs- means "Ketatifen" in any form, the exact effect of which on the body has not yet been established, despite numerous studies.

Third-generation antihistamines are considered the best of what has been created to date, they are classified as active metabolites with non-sedative effects.

Their main feature is that they act directly on the peripheral receptors of cells without affecting the central nervous system.

This means that there are practically no side effects.

Such drugs can be used for a long time even for children, they have a prolonged effect up to 48 hours - that is, 1-2 doses are enough per day.

When are antihistamines prescribed?

Antihistamines, depending on the generation, are prescribed for chronic or acute allergies of any nature:

  • bronchial asthma;
  • angioedema;
  • urticaria;
  • various dermatitis;
  • hay fever;
  • conjunctivitis;
  • allergic rhinitis;
  • hay fever and other diseases.

Medicines of the third generation are good because they do not cause drowsiness, which means that they can be prescribed to people whose occupation requires increased concentration of attention - drivers, machine tool adjusters and other serious mechanisms, etc.

They don't reinforce alcohol intoxication, they are allowed to be prescribed to children from the age of two, since they do not affect the central nervous system, kidneys and liver.

This is an ideal remedy for the treatment of chronic allergies, when the drug must be taken daily for a long time.

Mechanism of action

Allergic irritation of the mucous membranes of the eyes, nasopharynx and skin causes a special substance histamine. It begins to be produced in the body upon contact with the allergen.

All antihistamines of the third generation are aimed at suppressing the histamine receptors of the H1 and H2 groups, they not only stop the manifestations of allergies, but also prevent them.

Medicines provide:

  • decongestant;
  • antipruritic;
  • anesthetic effect, but only locally.

Therefore, for maximum effectiveness, the same drug can be produced in different forms, which will have different mechanism actions.

Mechanism of action:

  • Tablets. Tablets are taken orally, and no matter how fast the medicine is, they will not work instantly. First, the tablet must dissolve, after which the active substance is absorbed through the gastric mucosa into the blood, and then it begins to act. Agents in gelatin capsules, inside of which there is a powder, begin to work faster.
  • Ointments and creams. This form is mainly used in the treatment of dermatitis, urticaria and other skin manifestations of allergies, although it is also used in ophthalmology. The drugs act locally, because itching and pain decrease almost immediately after application. After a while, as the active ingredient acts, swelling and redness go away.
  • Capel. Drops are used for rhinitis and conjunctivitis - where local action and precise dosage are necessary. The advantage of this form is that the drug does not enter the bloodstream, but acts only locally, where it is needed. And this significantly reduces the likelihood of side effects.
  • Sprays. A very effective form of antihistamines that allows you to quickly distribute the substance over a large area. Also, sprays are very convenient for asthmatics, as they act almost instantly, the bottle fits easily in a pocket or purse, taking medication does not require any conditions and additional devices - just press the button and that's it. Disadvantage: the effect is short, the spray should not be the main remedy.

Indications

Drugs in this group are prescribed for:

  1. allergic rhinitis seasonal or year-round;
  2. different forms of conjunctivitis;
  3. urticaria;
  4. allergic contact and atopic dermatitis.

Contraindications

This generation has a significant drawback: some of them can cause serious malfunctions in the cardiovascular system.

They are prescribed with caution to patients suffering from hyperkalemia and impaired liver function.

In the absence of individual intolerance to the active substance or any other of the components of the medicinal product, there are no contraindications.

Side effect

Behind recent decades Allergology is far ahead when it comes to antihistamines. different generations.

Preparations from the third generation have absorbed all the best that has been achieved over the years of research and experience. But, nevertheless, it was not possible to completely get rid of side effects.

A person may experience drowsiness, or vice versa, insomnia, irritability, nervousness, anxiety.

Also, at the very beginning of the intake, allergy symptoms - coughing, sneezing, redness of the mucosa, swelling - may increase.

This is usually a temporary phenomenon that does not require separate therapy.

But if the symptoms do not go away, but intensify (which is extremely rare), it is advisable to stop taking it and seek help from a specialist as soon as possible.

Sometimes there are symptoms such as:

  • fatigue and drowsiness;
  • dry mouth;
  • headache;
  • convulsions, tachycardia, shortness of breath;
  • nausea, vomiting, abdominal pain;
  • hallucinations.

Video: What to do with a seasonal runny nose

List of popular third generation allergy remedies

How and when to apply

Since almost every 3rd generation allergy drug lasts an average of 24 hours, it doesn't really matter when you take it.

The main thing is to remember at least an approximate time so as not to miss a dose - after all, an allergy attack is easier to prevent than to stop later.

At the same time, antihistamines should not be abused, taking them more often than necessary.

The medicine in tablets can be taken regardless of the meal, washed down with plain water.

Spray for asthmatics can be used several times a day according to the instructions.

Drops are also instilled, depending on the doctor's prescription.

Although broad-spectrum antihistamines usually work well with other drugs, some of them are not prescribed in combination with antifungals, antidepressants, and antiarrhythmics.

Do I need a doctor's consultation

In no case should you start treatment with antihistamines on your own, since no one is immune from individual intolerance and side effects.

When to take medicines of any group, and for how long, only the attending physician, who knows the patient's medical history, his general condition and the results of recent tests, can decide.

Price policy

If you are prescribed 3rd generation allergy medications, the price will be higher than the 1st and 2nd generation drugs, you need to be prepared for this.

The form also affects the cost - tablets will always be cheaper than analogues in syrup or suspension for children. Of course, the manufacturer also plays a role.

In any case, saving is not worth it, especially when it comes to children - remember that this is very effective medicines, which are enough to take once or twice a day, that is, one package will last you for a long time.

Depending on the active substance, release form and packaging volume prices vary from 120 to 799 rubles.

Use in children

Unfortunately, children often suffer from allergies, even babies under the age of 1.5 years.

children's cosmetics, washing powders, new foods in the diet, taking serious medications - these are the factors that can cause severe allergies in a baby.

Previously, parents were wary of any antihistamines, considering them extremely harmful to the health of the child.

Indeed, this was the case with the 1st generation drugs.

Suprastin alone could cause:

  • vomiting;
  • migraine;
  • dizziness in a child;
  • prolonged sleep (more than 12 hours) or, conversely, insomnia.

Medicines of the 3rd generation do not have any special side effects - if the dosage is observed.

For children, they are available in the form of syrups with fruit flavors.

What are allergy nose drops for children? The answer is here.

Is it possible to do calcium gluconate with allergies intramuscularly? Details in the article.

allergycentr.ru

Diazolin

Diazolin has the same indications for use as other antihistamines, but differs from them in the features of the effect.

Advantages: a mild sedative effect allows it to be used where it is undesirable to have a depressing effect on the central nervous system.

Minuses: irritates the mucous membranes of the gastrointestinal tract, causes dizziness, impaired urination, drowsiness, slows down mental and motor reactions. There is information about the toxic effect of the drug on nerve cells.

Suprastin

Suprastin is prescribed for the treatment of seasonal and chronic allergic conjunctivitis, urticaria, atopic dermatitis, angioedema, itching of various etiologies, eczema. It is used in parenteral form for acute allergic conditions requiring emergency care.

Advantages: does not accumulate in the blood serum, therefore, even with prolonged use does not cause an overdose. Due to the high antihistamine activity, a rapid therapeutic effect is observed.

Minuses: side effects - drowsiness, dizziness, inhibition of reactions, etc. - are present, although they are less pronounced. The therapeutic effect is short-term, in order to prolong it, Suprastin is combined with H1-blockers that do not have sedative properties.

Tavegil

Tavegil in the form of injections is used for angioedema, as well as anaphylactic shock, as a prophylactic and therapeutic agent for allergic and pseudo-allergic reactions.

Advantages: has a longer and stronger antihistamine effect than Diphenhydramine, and has a more moderate sedative effect.

Minuses: may itself cause an allergic reaction, has some inhibitory effect.

Fenkarol

Fenkarol is prescribed when addiction to other antihistamines appears.

Advantages: has a weak severity of sedative properties, does not have a pronounced inhibitory effect on the central nervous system, low toxicity, blocks H1 receptors, is able to reduce the content of histamine in tissues.

Minuses: less antihistamine activity in comparison with Diphenhydramine. Fenkarol is used with caution in the presence of diseases of the gastrointestinal tract, cardiovascular system and liver.

2nd generation antihistamines

They have advantages over first generation drugs:

there is no sedative and anticholinergic effect, since these drugs do not cross the blood-brain barrier, only some individuals experience moderate drowsiness;
mental activity, physical activity do not suffer;
the effect of the drugs reaches 24 hours, so they are taken once a day;
they are not addictive, which allows them to be prescribed for a long time (3-12 months);
when you stop taking the drugs, the therapeutic effect lasts about a week;
drugs are not adsorbed with food in the gastrointestinal tract.

But antihistamines of the 2nd generation have a cardiotoxic effect of varying degrees, therefore, when they are taken, cardiac activity is monitored. They are contraindicated in elderly patients and patients suffering from disorders of the cardiovascular system.

The occurrence of cardiotoxic action is explained by the ability of 2nd generation antihistamines to block the potassium channels of the heart. The risk is increased when these drugs are combined with antifungal drugs, macrolides, antidepressants, grapefruit juice, and if the patient has severe liver dysfunction.

Claridol

Claridol is used to treat seasonal as well as cyclic allergic rhinitis, urticaria, allergic conjunctivitis, Quincke's edema and a number of other diseases of allergic origin. It copes with pseudo-allergic syndromes and allergies to insect bites. Included in the complex measures for the treatment of itchy dermatoses.

Advantages: Claridol has antipruritic, antiallergic, antiexudative effect. The drug reduces capillary permeability, prevents the development of edema, relieves spasm of smooth muscles. It does not affect the central nervous system, has no anticholinergic and sedative effect.

Minuses: occasionally after taking Claridol, patients complain of dry mouth, nausea and vomiting.

Claricens

Clarisens is able to suppress the release of histamine and leukotriene C4 from mast cells. It is used to treat and prevent such manifestations of allergies as rhinitis, conjunctivitis, dermatosis. The drug is included in complex treatment angioedema and various allergic insect bites. In the presence of pseudo-allergic reactions, Clarisens is able to quickly alleviate the patient's condition.

Advantages: the drug is not addictive, does not affect the work of the central nervous system, has an anti-exudative effect, relieves swelling and spasms of smooth muscles. The therapeutic effect occurs within half an hour after taking the medicine and lasts a day.

Minuses: a side effect occurs when the patient has an individual intolerance to the drug and is expressed by dyspepsia, severe headache, fatigue, allergic reactions.

Clarotadine

Clarotadine contains the active substance loratadine, which is a selective blocker of H1-histamine receptors, on which it has a direct effect, avoiding the undesirable effects inherent in other antihistamines. Indications for use are allergic conjunctivitis, acute chronic and idiopathic urticaria, rhinitis, pseudo-allergic reactions associated with the release of histamine, allergic insect bites, itchy dermatoses.

Advantages: the drug does not have a sedative effect, is not addictive, acts quickly and for a long time.

Minuses: undesirable consequences of taking Clarodin include disorders of the nervous system: asthenia, anxiety, drowsiness, depression, amnesia, tremor, agitation in a child. Dermatitis may appear on the skin. Frequent and painful urination, constipation and diarrhea. Weight gain due to disruption of the endocrine system. The defeat of the respiratory system can be manifested by cough, bronchospasm, sinusitis and similar manifestations.

Lomilan

Lomilan is indicated for allergic rhinitis (rhinitis) of a seasonal and permanent nature, skin rashes of allergic origin, pseudo-allergies, reactions to insect bites, allergic inflammation of the mucous membrane of the eyeball.

Advantages: Lomilan is able to relieve itching, reduce the tone of smooth muscles and the production of exudate (a special fluid that appears during the inflammatory process), prevent tissue edema already half an hour after taking the drug. The greatest efficiency comes in 8-12 hours, then subsides. Lomilan is not addictive and does not adversely affect the activity of the nervous system.

Minuses: adverse reactions are rare, manifested by headache, fatigue and drowsiness, inflammation of the gastric mucosa, nausea.

LauraGeksal

Advantages: the drug has neither anticholinergic nor central action, its administration does not affect the attention, psychomotor functions, working capacity and mental qualities of the patient.

Minis: LoraGeksal is usually well tolerated, but occasionally it causes fatigue, dry mouth, headache, tachycardia, dizziness, allergic reactions, cough, vomiting, gastritis, liver dysfunction.

Claritin

Claritin contains an active ingredient - loratadine, which blocks H1-histamine receptors and prevents the release of histamine, bradycanin and serotonin. Antihistamine effectiveness lasts a day, and therapeutic comes after 8-12 hours. Claritin is indicated for the treatment of allergic rhinitis, allergic skin reactions, food allergies, and mild asthma.

Advantages: high efficiency in the treatment of allergic diseases, the drug does not cause addiction, drowsiness.

Minuses: cases of side effects are rare, they are manifested by nausea, headache, gastritis, agitation, allergic reactions, drowsiness.

Rupafin

Rupafin has a unique active ingredient - rupatadine, which is distinguished by antihistamine activity and a selective effect on H1-histamine peripheral receptors. It is prescribed for chronic idiopathic urticaria and allergic rhinitis.

Advantages: Rupafin effectively copes with the symptoms of the above allergic diseases and does not affect the central nervous system.

Minuses: undesirable consequences of taking the drug - asthenia, dizziness, fatigue, headache, drowsiness, dry mouth. It can affect the respiratory, nervous, musculoskeletal, and digestive systems, as well as metabolism and skin.

Kestin

Kestin blocks histamine receptors that increase vascular permeability, causing muscle spasms, leading to an allergic reaction. It is used to treat allergic conjunctivitis, rhinitis and chronic idiopathic urticaria.

Advantages
: the drug acts an hour after application, the therapeutic effect lasts 2 days. A five-day intake of Kestin allows you to maintain an antihistamine effect for about 6 days. Sedative effects are practically non-existent.

Minuses: the use of Kestin can cause insomnia, abdominal pain, nausea, drowsiness, asthenia, headache, sinusitis, dry mouth.

New antihistamines, 3rd generation

These substances are prodrugs, which means that when they enter the body, they are converted from their original form into pharmacologically active metabolites.

All 3rd generation antihistamines do not have a cardiotoxic and sedative effect, so they can be used by people whose activities are associated with a high concentration of attention.

These drugs block H1 receptors, and also have an additional effect on allergic manifestations. They have high selectivity, do not overcome the blood-brain barrier, so they are not characterized by negative consequences from the central nervous system, there is no side effect on the heart.

The presence of additional effects contributes to the use of 3rd generation antihistamines in the long-term treatment of most allergic manifestations.

Gismanal is prescribed as a therapeutic and prophylactic agent for hay fever, allergic skin reactions, including urticaria, and allergic rhinitis. The effect of the drug develops within 24 hours and reaches a maximum after 9-12 days. Its duration depends on the previous therapy.

Advantages: the drug has practically no sedative effect, does not enhance the effect of taking sleeping pills or alcohol. It also does not affect the ability to drive a car or mental activity.

Minuses: Hismanal can cause increased appetite, dry mucous membranes, tachycardia, drowsiness, arrhythmia, QT prolongation, palpitations, collapse.

Trexil

Trexil is a fast-acting, selectively active H1 receptor antagonist derived from buterophenol, which differs in chemical structure from analogues. It is used in allergic rhinitis to relieve its symptoms, allergic dermatological manifestations (dermographism, contact dermatitis, urticaria, atonic eczema,), asthma, atonic and provoked by exercise, as well as in connection with acute allergic reactions to various irritants.

Advantages: lack of sedative and anticholinergic effect, influence on psychomotor activity and well-being of a person. The drug is safe to use in patients with glaucoma and prostate disorders.

Telfast

Telfast is a highly effective antihistamine drug, which is a metabolite of terfenadine, therefore, it has a great similarity with histamine H1 receptors. Telfast binds to them and blocks them, preventing their biological manifestations as allergic symptoms. Mast cell membranes are stabilized and the release of histamine from them is reduced. Indications for use are angioedema, urticaria, hay fever.

Advantages: does not show sedative properties, does not affect the speed of reactions and concentration of attention, the work of the heart, is not addictive, highly effective against the symptoms and causes of allergic diseases.

Minuses: rare consequences of taking the drug are headache, nausea, dizziness, there are isolated reports of shortness of breath, anaphylactic reaction, skin flushing.

Zyrtec

Zyrtec is a competitive antagonist of the hydroxyzine metabolite, histamine. The drug facilitates the course and sometimes prevents the development of allergic reactions. Zyrtec limits the release of mediators, reduces the migration of eosinophils, basophils, neutrophils. The drug is used for allergic rhinitis, bronchial asthma, urticaria, conjunctivitis, dermatitis, fever, skin itching, anti-neurotic edema.

Advantages: effectively prevents the occurrence of edema, reduces capillary permeability, relieves spasm of smooth muscles. Zyrtec does not have anticholinergic and antiserotonin effects.

Minuses: improper use of the drug can lead to dizziness, migraine, drowsiness, allergic reactions.

Antihistamines for children

For the treatment of allergic manifestations in children, antihistamines of all three generations are used.

Antihistamines of the 1st generation are distinguished by the fact that they quickly show their healing properties and are excreted from the body. They are in demand for the treatment of acute manifestations of allergic reactions. They are prescribed in short courses. The most effective of this group is Tavegil, Suprastin, Diazolin, Fenkarol.

A significant percentage of side effects leads to a reduction in the use of these drugs for childhood allergies.

Antihistamines of the 2nd generation do not cause sedation, act for a longer time and are usually used once a day. Few side effects. Among the drugs in this group, Ketitofen, Fenistil, Cetrin, Erius are used to treat manifestations of childhood allergies.

3rd generation antihistamines for children include Gismanal, Terfen and others. They are used in chronic allergic processes, since they are able to stay in the body for a long time. There are no side effects.

Negative consequences:

1st generation: headache, constipation, tachycardia, drowsiness, dry mouth, blurred vision, urinary retention and lack of appetite;
2nd generation: negative effect on the heart and liver;
3rd generation: do not have, recommended for use from 3 years.

For children, antihistamines are produced in the form of ointments (allergic reactions on the skin), drops, syrups and tablets for oral administration.

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General concept of antihistamines

To everyone who wants to understand in depth the question of what it is - antihistamines, doctors explain that these drugs are designed to counter histamine - an allergic mediator.

When human body comes into contact with an irritant, specific substances are produced, among which histamine exhibits increased activity. At healthy person it resides in mast cells and remains inactive. Under the influence of an allergen, histamine enters the active phase and provokes allergy symptoms.

To stop negative reactions at different times, medicines were invented that could lower the amount of histamine and neutralize its harmful effects on humans. Thus, antihistamines are general definition all drugs that have the specified effectiveness. To date, their classification has 4 generations.

The advantages of the drugs under consideration are a gentle effect on the body, in particular, on the cardiovascular system, rapid relief of symptoms and a prolonged effect.

Review of new generation antihistamines

Antihistamines are also called H1 receptor blockers. They are quite safe for the body, but still have some contraindications. For example, during pregnancy and in childhood, the doctor has the right not to prescribe allergy pills if these conditions are listed among the contraindications in their instructions.

All new generation antihistamines - list of new drugs:

  • Erius.
  • Ksizal.
  • Bamipin.
  • Cetirizine.
  • Ebastine.
  • Fenspiride.
  • Levocetirizine.
  • Fexofenadine.
  • Desloratadine.

It is difficult to single out the most effective 4th generation antihistamines from this list, because some of them have appeared relatively recently and have not yet managed to prove themselves 100%. Fenoxofenadine is a popular allergy treatment option. Taking tablets containing this substance does not have a hypnotic and cardiotoxic effect on the patient.

Medications with cetirizine well remove skin manifestations of allergies. One tablet brings significant relief after 2 hours from the moment of use. The result is stored for a long time.

The drug Erius is an improved analogue of Loratadine. But its efficiency is about 2.5 times higher. Erius is suitable for children over the age of 1 who are prone to allergies. They are given the drug in liquid form with a dosage of 2.5 ml 1 time per day. From the age of 5, the dosage of Erius is increased to 5 ml. From the age of 12, the child is given 10 ml of medication per day.

The drug Ksizal is also in high demand today. It prevents the release of inflammatory mediators. Effectiveness is determined by the reliable elimination of allergic reactions.

Feksadin (Allegra, Telfast)

The drug with fexofenadine reduces the production of histamine and completely blocks histamine receptors. Suitable for the treatment of seasonal allergies and chronic urticaria. The tool is not addictive. The body is affected for 24 hours.

Feksadin should not be taken during pregnancy, breastfeeding and children under 12 years of age.

Zodak (Cetrin, Zyrtec, Cetirizine)

Efficiency taken pill felt after 20 minutes, and after discontinuation of the drug persists for another 72 hours. Zodak and its synonyms are used for the treatment and prevention of allergies. Long-term use is allowed. The release form is not only tablets, but also syrup and drops.

In pediatrics, Zodak drops have been used since 6 months. After 1 year, syrup is prescribed. Children can take tablets from the age of 6. Dosages for each type of medication are selected individually.

Cetirizine should not be taken by pregnant women. If there is a need to treat allergies during lactation, the baby is temporarily weaned.

Xyzal (Suprastinex, Levocetirizine)

Drops and tablets Ksizal work 40 minutes after ingestion.

The drug is indicated for the treatment of urticaria, allergies, pruritus. For children, fourth-generation antihistamines for allergies called Ksizal are prescribed from the age of 2 and 6 (drops and tablets, respectively). The pediatrician calculates the dosage according to the age and weight of the child.

Xyzal is prohibited during pregnancy. But it can be taken while breastfeeding.

Suprastinex helps well with seasonal allergies, when the body reacts to the pollen of flowering plants. As the main drug, it is used in the treatment of conjunctivitis and allergic rhinitis. Take Suprastinex with food.

Desloratadine (Erius, Lordestin, Desal)

Desloratadine and its synonyms have antihistamine and anti-inflammatory properties.

They quickly treat seasonal allergies and recurrent hives, but occasionally cause side effects such as headaches and dry mouth. Desloratadine is sold in the form of tablets and syrup.

For children 2 to 6 years old, doctors prescribe syrup. Tablets are allowed to be used only from 6 years. Pregnant and lactating women Desloratadine is completely contraindicated. But with Quincke's edema and bronchospasm, a specialist can choose a gentle option for using this medication.

Antihistamines for toddlers

Newborns are not recommended to take antihistamines. But sometimes there are situations when it is impossible to do without drugs, for example, if the baby was stung by an insect. From 1 month of life, a child can be given Fenistil in drops.

Diphenhydramine, which was previously given to children in different occasions, pediatricians today prescribe only from the 7th month of life.

The most gentle option for the smallest is Suprastin. He quickly shows medicinal properties without causing the slightest harm to the body. Also, children are prescribed Fenkarol and Tavegil. With urticaria, drug dermatosis and food allergies, it is better for a child to give Tavegil. Tablets relieve puffiness, restore skin color and work as an antipruritic agent.

Analogues of Tavegil are Donormil, Dimedrol, Bravegil and Clemastin. Their child takes in the presence of contraindications to the use of Tavegil.

From 2 to 5 years children's body gradually strengthens and can normally tolerate more strong medicines. When the skin is itchy, the names of antihistamines for this age group The patient specialist will consider the following:

  1. Erius (4th generation).
  2. Tsetrin.
  3. Claritin.
  4. Diazolin.

Erius was mentioned above, now we will focus on Tsetrin. These tablets can be used to prevent allergies in children prone to negative reactions. With individual intolerance constituent components Cetrin is replaced by analogues - Letizen, Cetirinax, Zodak, Zetrinal. After 2 years, the child can take Astemizol.

From the age of 6, the list of antihistamines is being expanded, since drugs of different generations are suitable for such children - from 1 to 4. Younger students can drink Zirtek, Terfenadine, Clemastine, Glenset, Suprastinex, Cezera tablets.

What Komarovsky says

The famous pediatrician E.O. Komarovsky does not advise parents to give antihistamines to young children without emergency and medical prescriptions. If a pediatrician or an allergist has deemed it necessary to prescribe an antiallergic agent to a child, it can be taken for no more than 7 days.

Evgeny Olegovich also forbids combining antihistamines with antibiotics and says that it is not at all necessary to give a child antihistamine pill before vaccination or after vaccination.

Some parents, based on their own considerations, try to give their child Suprastin to drink before DTP, but Komarovsky does not see any point in this. The children's doctor explains that the reaction of the body to the vaccine has nothing to do with the manifestations of allergies.

Allergic women planning to have offspring are always interested in what antihistamines can be taken during pregnancy and preferably during lactation, or is it worth enduring the inconvenience associated with hay fever, rash and swelling. Doctors say that during the gestation period, it is better for women not to take any medications, because they are potentially dangerous for the mother and fetus.

In the 1st trimester, it is strictly forbidden to treat allergies with pills, except in cases where the disease threatens the life of the expectant mother. In the 2nd - 3rd trimesters, treatment with antihistamines is allowed with a number of restrictions, because no pills are 100% harmless.

Women who experience allergies every season should plan pregnancy in advance so that irritating substances are inactive during the bearing of the baby. If conception did occur, and you have to carry a pregnancy in the summer, expectant mothers can reduce the severity of allergic reactions by taking natural antihistamines:

  • Zinc.
  • Fish fat.
  • Vitamin B12.
  • Ascorbic acid.
  • Organic acids - oleic, pantothenic, nicotinic.
  • Loratadine instructions for use tablets for what

Historically, the term "antihistamines" means drugs that block H1-histamine receptors, and drugs that act on H2-histamine receptors (cimetidine, ranitidine, famotidine, etc.) are called H2-histamine blockers. The former are used to treat allergic diseases, the latter are used as antisecretory agents.

Histamine, this the most important mediator various physiological and pathological processes in the body, was chemically synthesized in 1907. Subsequently, it was isolated from animal and human tissues (Windaus A., Vogt W.). Even later, its functions were determined: gastric secretion, neurotransmitter function in the central nervous system, allergic reactions, inflammation, etc. Almost 20 years later, in 1936, the first substances with antihistamine activity were created (Bovet D., Staub A.). And already in the 60s, the heterogeneity of histamine receptors in the body was proven and three of their subtypes were identified: H1, H2 and H3, differing in structure, localization and physiological effects that occur during their activation and blockade. Since that time, an active period of synthesis and clinical testing of various antihistamines begins.

Numerous studies have shown that histamine, acting on receptors respiratory system, eyes and skin, causes characteristic symptoms allergies, and antihistamines that selectively block the H1-type receptors are able to prevent and stop them.

Most of the antihistamines used have a number of specific pharmacological properties characterizing them as separate group. These include the following effects: antipruritic, decongestant, antispastic, anticholinergic, antiserotonin, sedative and local anesthetic, as well as the prevention of histamine-induced bronchospasm. Some of them are not due to histamine blockade, but to structural features.

Antihistamines block the action of histamine on H1 receptors by the mechanism of competitive inhibition, and their affinity for these receptors is much lower than that of histamine. Therefore, these drugs are not able to displace histamine bound to the receptor, they only block unoccupied or released receptors. Accordingly, H1-blockers are most effective in preventing immediate allergic reactions, and in the case of a developed reaction, they prevent the release of new portions of histamine.

In my own way chemical structure most of them are fat-soluble amines, which have a similar structure. The core (R1) is represented by an aromatic and/or heterocyclic group and is linked via a nitrogen, oxygen or carbon (X) molecule to the amino group. The core determines the severity of antihistamine activity and some of the properties of the substance. Knowing its composition, one can predict the strength of the drug and its effects, such as the ability to penetrate the blood-brain barrier.

There are several classifications of antihistamines, although none of them is generally accepted. According to one of the most popular classifications, antihistamines are divided into first and second generation drugs according to the time of creation. First-generation drugs are also called sedatives (according to the dominant side effect), in contrast to non-sedative second-generation drugs. At present, it is customary to single out the third generation: it includes fundamentally new drugs - active metabolites that, in addition to the highest antihistamine activity, exhibit the absence of a sedative effect and the cardiotoxic effect characteristic of second-generation drugs (see).

In addition, according to the chemical structure (depending on the X-bond), antihistamines are divided into several groups (ethanolamines, ethylenediamines, alkylamines, derivatives of alphacarboline, quinuclidine, phenothiazine, piperazine and piperidine).

First generation antihistamines (sedatives). All of them are well soluble in fats and, in addition to H1-histamine, also block cholinergic, muscarinic and serotonin receptors. Being competitive blockers, they reversibly bind to H1 receptors, which leads to the use of quite high doses. The following pharmacological properties are most characteristic of them.

  • The sedative effect is determined by the fact that most of the first-generation antihistamines, being easily dissolved in lipids, penetrate well through the blood-brain barrier and bind to the H1 receptors of the brain. Perhaps their sedative effect consists of blocking the central serotonin and acetylcholine receptors. The degree of manifestation of the sedative effect of the first generation varies in different drugs and in different patients from moderate to severe and increases when combined with alcohol and psychotropic drugs. Some of them are used as sleeping pills (doxylamine). Rarely, instead of sedation, psychomotor agitation occurs (more often in medium therapeutic doses in children and in high toxic doses in adults). Due to the sedative effect, most drugs should not be used during tasks that require attention. All first generation drugs potentiate the action of sedatives and sleeping pills, narcotic and non-narcotic analgesics, monoamine oxidase inhibitors and alcohol.
  • The anxiolytic effect characteristic of hydroxyzine may be due to the suppression of activity in certain areas of the subcortical region of the central nervous system.
  • Atropine-like reactions associated with the anticholinergic properties of drugs are most characteristic of ethanolamines and ethylenediamines. Manifested by dry mouth and nasopharynx, urinary retention, constipation, tachycardia and visual impairment. These properties ensure the effectiveness of the discussed remedies in non-allergic rhinitis. At the same time, they can increase obstruction in bronchial asthma (due to an increase in sputum viscosity), exacerbate glaucoma and lead to infravesical obstruction in prostate adenoma, etc.
  • The antiemetic and antiswaying effects are also probably associated with the central anticholinergic effect of the drugs. Some antihistamines (diphenhydramine, promethazine, cyclizine, meclizine) reduce the stimulation of vestibular receptors and inhibit the function of the labyrinth, and therefore can be used for motion sickness.
  • A number of H1-histamine blockers reduce the symptoms of parkinsonism, which is due to central inhibition of the effects of acetylcholine.
  • Antitussive action is most characteristic of diphenhydramine, it is realized through a direct action on the cough center in the medulla oblongata.
  • The antiserotonin effect, which is primarily characteristic of cyproheptadine, determines its use in migraine.
  • The α1-blocking effect with peripheral vasodilation, especially seen in phenothiazine antihistamines, can lead to a transient decrease in blood pressure in sensitive individuals.
  • Local anesthetic (cocaine-like) action is characteristic of most antihistamines (occurs due to a decrease in membrane permeability to sodium ions). Diphenhydramine and promethazine are stronger local anesthetics than novocaine. However, they have systemic quinidine-like effects, manifested by prolongation of the refractory phase and the development of ventricular tachycardia.
  • Tachyphylaxis: decrease in antihistamine activity with long-term use, confirming the need for alternating drugs every 2-3 weeks.
  • It should be noted that the first generation antihistamines differ from the second generation in the short duration of exposure with a relatively rapid onset of the clinical effect. Many of them are available in parenteral forms. All of the above, as well as low cost, determine the widespread use of antihistamines today.

Moreover, many of the qualities that were discussed allowed the “old” antihistamines to occupy their niche in the treatment of certain pathologies (migraine, sleep disorders, extrapyramidal disorders, anxiety, motion sickness, etc.) that are not associated with allergies. Many first-generation antihistamines are included in combined drugs used for colds, as sedatives, sleeping pills and other components.

The most commonly used are chloropyramine, diphenhydramine, clemastine, cyproheptadine, promethazine, phencarol, and hydroxyzine.

Chloropyramine(Suprastin) is one of the most widely used sedative antihistamines. It has significant antihistamine activity, peripheral anticholinergic and moderate antispasmodic action. Effective in most cases for the treatment of seasonal and year-round allergic rhinoconjunctivitis, angioedema, urticaria, atopic dermatitis, eczema, itching various etiologies; in parenteral form - for the treatment of acute allergic conditions requiring urgent care. Provides a wide range of usable therapeutic doses. It does not accumulate in the blood serum, so it does not cause an overdose with prolonged use. Suprastin is characterized by a rapid onset of effect and short duration (including side effects). At the same time, chloropyramine can be combined with non-sedating H1-blockers in order to increase the duration of the antiallergic effect. Suprastin is currently one of the best-selling antihistamines in Russia. This is objectively related to the proven high efficiency, controllability of its clinical effect, the availability of various dosage forms, including injections, and low cost.

Diphenhydramine, best known in our country under the name diphenhydramine, is one of the first synthesized H1-blockers. It has a fairly high antihistamine activity and reduces the severity of allergic and pseudo-allergic reactions. Due to the significant anticholinergic effect, it has an antitussive, antiemetic effect and at the same time causes dry mucous membranes, urinary retention. Due to lipophilicity, diphenhydramine gives pronounced sedation and can be used as a hypnotic. It has a significant local anesthetic effect, as a result of which it is sometimes used as an alternative for intolerance to novocaine and lidocaine. Diphenhydramine is presented in various dosage forms, including for parenteral use, which determined its widespread use in emergency care. However, a significant range of side effects, unpredictability of consequences and effects on the central nervous system require increased attention in its application and, if possible, the use of alternative means.

clemastine(tavegil) is a highly effective antihistamine drug similar in action to diphenhydramine. It has a high anticholinergic activity, but to a lesser extent penetrates the blood-brain barrier. It also exists in an injectable form that can be used as additional remedy with anaphylactic shock and angioedema, for the prevention and treatment of allergic and pseudo-allergic reactions. However, hypersensitivity to clemastine and other antihistamines with a similar chemical structure is known.

Cyproheptadine(peritol), along with antihistamine, has a significant antiserotonin effect. In this regard, it is mainly used in some forms of migraine, dumping syndrome, as an appetite enhancer, in anorexia. various genesis. It is the drug of choice for cold urticaria.

Promethazine(pipolphen) - pronounced impact on the central nervous system determined its use in Meniere's syndrome, chorea, encephalitis, sea and air sickness, as antiemetic. In anesthesiology, promethazine is used as a component lytic mixtures to potentiate anesthesia.

Quifenadine(fenkarol) - has less antihistamine activity than diphenhydramine, but is also characterized by less penetration through the blood-brain barrier, which determines the lower severity of its sedative properties. In addition, fenkarol not only blocks histamine H1 receptors, but also reduces the content of histamine in tissues. May be used in the development of tolerance to other sedative antihistamines.

Hydroxyzine(atarax) - despite the existing antihistamine activity, it is not used as an antiallergic agent. It is used as an anxiolytic, sedative, muscle relaxant and antipruritic agent.

Thus, first-generation antihistamines that affect both H1- and other receptors (serotonin, central and peripheral cholinergic receptors, a-adrenergic receptors) have various effects, which determined their application in a variety of conditions. But the severity of side effects does not allow us to consider them as drugs of first choice in the treatment of allergic diseases. The experience gained with their use has allowed the development of unidirectional drugs - the second generation of antihistamines.

Second generation antihistamines (non-sedating). Unlike the previous generation, they have almost no sedative and anticholinergic effects, but differ in their selective action on H1 receptors. However, for them, a cardiotoxic effect was noted to varying degrees.

The following properties are the most common for them.

  • High specificity and high affinity for H1 receptors with no effect on choline and serotonin receptors.
  • Rapid onset of clinical effect and duration of action. Prolongation can be achieved due to high protein binding, accumulation of the drug and its metabolites in the body, and delayed elimination.
  • Minimal sedative effect when using drugs in therapeutic doses. It is explained by the weak passage of the blood-brain barrier due to the peculiarities of the structure of these funds. Some particularly sensitive individuals may experience moderate drowsiness, which is rarely the reason for discontinuing the drug.
  • Absence of tachyphylaxis with prolonged use.
  • The ability to block the potassium channels of the heart muscle, which is associated with prolongation of the QT interval and cardiac arrhythmia. The risk of this side effect increases when antihistamines are combined with antifungals (ketoconazole and itraconazole), macrolides (erythromycin and clarithromycin), antidepressants (fluoxetine, sertraline and paroxetine), grapefruit juice, and in patients with severe liver dysfunction.
  • Absence of parenteral formulations, however, some of them (azelastine, levocabastine, bamipine) are available as topical formulations.

Below are second-generation antihistamines with their most characteristic properties.

Terfenadine- the first antihistamine drug, devoid of a depressant effect on the central nervous system. Its creation in 1977 was the result of a study of both the types of histamine receptors and the features of the structure and action of existing H1-blockers, and laid the foundation for the development of a new generation of antihistamines. Currently, terfenadine is used less and less, which is associated with its increased ability to cause fatal arrhythmias associated with prolongation of the QT interval (torsade de pointes).

Astemizol- one of the longest active drugs group (half-life of its active metabolite up to 20 days). It is characterized by irreversible binding to H1 receptors. Virtually no sedative effect, does not interact with alcohol. Since astemizole has a delayed effect on the course of the disease, it is not advisable to use it in an acute process, but it may be justified in chronic allergic diseases. Since the drug has the ability to accumulate in the body, the risk of developing serious disorders increases. heart rate sometimes fatal. Due to these dangerous side effects the sale of astemizole in the United States and some other countries has been suspended.

Akrivastine(semprex) is a drug with high antihistamine activity with a minimally pronounced sedative and anticholinergic effect. A feature of its pharmacokinetics is a low level of metabolism and the absence of cumulation. Acrivastine is preferred in cases where there is no need for permanent antiallergic treatment due to the rapid onset of effect and short-term effect, which allows for a flexible dosing regimen.

Dimethenden(Fenistil) - is closest to the first generation antihistamines, but differs from them in a much less pronounced sedative and muscarinic effect, higher antiallergic activity and duration of action.

Loratadine(claritin) is one of the most purchased drugs of the second generation, which is quite understandable and logical. Its antihistamine activity is higher than that of astemizole and terfenadine, due to the greater strength of binding to peripheral H1 receptors. The drug is devoid of a sedative effect and does not potentiate the effect of alcohol. In addition, loratadine practically does not interact with other drugs and does not have a cardiotoxic effect.

The following antihistamines are topical preparations and are intended to relieve local manifestations of allergies.

Levocabastin(Histimet) is used as an eye drop for the treatment of histamine-dependent allergic conjunctivitis or as a spray for allergic rhinitis. At topical application enters the systemic circulation in small quantities and does not have undesirable effects on the central nervous and cardiovascular systems.

Azelastine(allergodil) - highly effective agent for the treatment of allergic rhinitis and conjunctivitis. Used as a nasal spray and eye drops, azelastine has little to no systemic effects.

Other topical antihistamine- bamipin (soventol) in the form of a gel is intended for use in allergic skin lesions accompanied by itching, insect bites, jellyfish burns, frostbite, sunburn, as well as thermal burns mild degree.

Antihistamines of the third generation (metabolites). Their fundamental difference in that they are active metabolites of previous generation antihistamines. Their main feature is the inability to influence the QT interval. Currently, there are two drugs - cetirizine and fexofenadine.

cetirizine(Zyrtec) is a highly selective peripheral H1 receptor antagonist. It is an active metabolite of hydroxyzine, which has a much less pronounced sedative effect. Cetirizine is almost not metabolized in the body, and the rate of its excretion depends on the function of the kidneys. Its characteristic feature is its high ability to penetrate the skin and, accordingly, its effectiveness in skin manifestations of allergies. Cetirizine neither experimentally nor in the clinic showed any arrhythmogenic effect on the heart, which predetermined the area of ​​practical use of metabolite drugs and determined the creation of a new drug, fexofenadine.

Fexofenadine(Telfast) is the active metabolite of terfenadine. Fexofenadine does not undergo transformations in the body and its kinetics does not change with impaired liver and kidney function. It does not enter into any drug interactions, does not have a sedative effect and does not affect psychomotor activity. In this regard, the drug is approved for use by persons whose activities require increased attention. A study of the effect of fexofenadine on the QT value showed, both in the experiment and in the clinic, the complete absence of a cardiotropic effect when using high doses and with long-term use. Along with maximum security this remedy demonstrates the ability to relieve symptoms in the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria. Thus, the pharmacokinetics, safety profile and high clinical efficacy make fexofenadine the most promising of the antihistamines at present.

So, in the doctor's arsenal there is a sufficient amount of antihistamines with various properties. It must be remembered that they provide only symptomatic relief from allergies. In addition, depending on the specific situation, you can use both different drugs and their diverse forms. It is also important for the physician to be aware of the safety of antihistamines.

Three generations of antihistamines (trade names in brackets)
1st generation II generation III generation
  • Diphenhydramine (diphenhydramine, benadryl, allergin)
  • Clemastine (tavegil)
  • Doxylamine (Decaprine, Donormil)
  • Diphenylpyralin
  • Bromodifenhydramine
  • Dimenhydrinate (Dedalone, Dramamine)
  • Chloropyramine (suprastin)
  • pyrilamine
  • Antazolin
  • Mepyramine
  • Brompheniramine
  • Chloropheniramine
  • Dexchlorpheniramine
  • Pheniramine (avil)
  • Mebhydrolin (diazolin)
  • Quifenadine (Phencarol)
  • Sequifenadine (bicarfen)
  • Promethazine (phenergan, diprazine, pipolfen)
  • trimeprazine (teralen)
  • Oxomemazine
  • Alimemazine
  • Cyclizine
  • Hydroxyzine (atarax)
  • Meclizine (bonin)
  • Cyproheptadine (peritol)
  • Acrivastine (semprex)
  • Astemizol (gismanal)
  • Dimetinden (Fenistil)
  • Oksatomide (tinset)
  • Terfenadine (bronal, histadine)
  • Azelastine (allergodil)
  • Levocabastin (Histimet)
  • Mizolastin
  • Loratadine (Claritin)
  • Epinastin (alesion)
  • Ebastin (Kestin)
  • Bamipin (soventol)
  • Cetirizine (Zyrtec)
  • Fexofenadine (Telfast)

The third generation includes drugs whose active metabolites belong to the previous group of drugs.

The low level of transformations, the lack of interaction with isoenzymes of the cytochrome 450 system allows them to be used by people with pathology of the hepatobiliary zone.

At the same time, it is not necessary to resort to significant changes in the dosage of the drug and to prescribe it with metabolic derivatives of other groups.

Modern drugs - a new milestone in medicine

The list of third-generation antihistamines belongs to the new class of drugs. They are devoid of the side effects inherent in their predecessors. They do not affect the level of performance, they are conveniently dosed. An important advantage is the absence of cardiotoxicity in most of these drugs: there is no prolongation of the repolarization period on the electrocardiogram, an increase in heart rate.

The mechanism of action is through the release into the blood of active metabolites that have high bioavailability, are rapidly absorbed, which reduces allergic manifestations shortly after application. Do not depend on food intake, are excreted unchanged.

The main impetus for the creation of next-generation allergy drugs is the need to develop drugs that do not pass through the blood-brain barrier, which minimizes the suppression of the central nervous system. Therefore, taking histamine preparations is not accompanied by sedation, is not addictive, does not require the abolition of activities that require concentration and attention.

For whom they are intended, when they are not assigned

Antiallergic drugs modern generation used for:

  • urticaria;
  • hay fever;
  • food allergies;
  • insect allergy;
  • itchy dermatosis;
  • atonic eczema;
  • bronchial asthma;
  • vasomotor rhinitis;
  • contact dermatitis;
  • atopic dermatitis;
  • angioedema;
  • anaphylactic shock (parenteral);
  • seasonal and chronic conjunctivitis;
  • seasonal and cyclic allergic rhinitis;
  • an allergic reaction as a result of taking antibiotics;
  • chronic and acute skin allergies (urticaria, dermatitis).

General contraindications:

  • pregnancy;
  • lactation period;
  • severe renal failure;
  • severe liver failure;
  • intolerance to the components of the drug.

Contraindications for taking liquid forms (syrups): intolerance, impaired absorption and binding of carbohydrates, children's age when taking solid forms for desloratadine.

Possible side effects:

  • rash;
  • fatigue;
  • skin itching;
  • redness;
  • CNS disorders;
  • sore throat;
  • cardiac arrhythmias, decreased total peripheral resistance, increased cardiac output;
  • V biochemical analysis blood: increased creatiphosphokinase, lactate dehydrogenase, aspartate aminotransferase, bilirubin.

Children 2-4 years old may experience drowsiness, dyspeptic symptoms (nausea, vomiting, diarrhea, pain and bloating). In children over 12 years of age, headaches, severe drowsiness, apathy. But most of the third new generation allergy medications do not cause drowsiness.

Dosage Forms for Healthy Reform

The newest allergy remedies come in many forms: there are allergy shots, pills, etc., a list with prices of some is given in the table.

International generic names Trade names Release form Prices in rubles
Levocetirizine Levocetirizine-Teva Tablets of 0.005 g, 7 pcs. per pack or 0.005 g, 10 pcs. 200- 270
Suprastinex 230-400
or drops inside of 0.005 g (bottle) 340
Xizal Tablet forms of 0.005 g 350-670
or drops for internal use 0.005 g each (10 ml bottle) 380
Desloratadine Erius 0.005 g 450-650
or 0.005 g each (bottle 0.06 l, 012 l with a spoon / measuring syringe) 550-750
Lordestin Tablets 0.005 g 300-700
or syrup 0.005 g (bottle 0.06 l with a measuring cap). 160
Desloratadine-teva Tablets 0.005 g, 10 pcs. packaged. 100
Eliza Tablets 0.005 150-360
Desal Tablets weighing 5 mg 200-400
Apply 5 mg solution inside (bottle 0.1 l with a spoon / measuring syringe). 300
Rupatadine fumarate Rupafin Tablets of 0.01 380-600
Cetirizine-Teva Tablets of 0.01 80-200

Medications for skin symptoms

Skin allergy is accompanied by rashes, itching, burning, as a result of sleep disturbance, restriction habitual life. Treatment is aimed at eliminating the allergen from the body and preventing re-contact with it. To fight, they resort to means that reduce the manifestations of itching. Third generation antihistamines for skin symptoms:

  1. cetirizine at a dose of 20-40 mg. This dosage is associated with the development of a pronounced sedative effect, therefore, modern forms are used: Zirtek (480 rubles - the price for a package of 10 tablets), inside 5 mg once a day. In severe cases, the amount of the agent used is gradually increased by 2 times from the original.
  2. Loratadine(Claridol 90 rubles - price for 7 tablets) 10 mg once a day.
  3. Fexofenadine(Allegra 480 rubles - price for 10 tablets) 120 mg 1 time per day.

The presence of a pronounced sleep disorder makes it necessary to refuse the appointment of certain medications. Local forms of the third class have not been studied in large studies, so their use does not guarantee the development best effect compared with systemic drugs. The appointment of this group of drugs is justified when combined with allergies to the respiratory departments.

Options for children

We present a list of good antihistamines for children.

Trade names Age Diseases Peculiarities
Suprastinex After 6 years Seasonal rhinitis, urticaria, angioedema, dermatoses, hay fever Inside, half a tablet every 24 hours - up to 6 years. Older children - a tablet a day. Taken before meals or during meals
Xizal From 6 years old Seasonal allergic rhinitis, urticaria, hay fever, itching Inside, half a tablet in 24 hours - up to 6 years. Children over six years of age one tablet
Erius Syrup from one year old, tablets from 12 years old Seasonal rhinitis, urticaria, itching The daily dose is 1 teaspoon with a small amount of liquid. From 1 to 5 years liquid forms - syrup 0.0025 g
Allegra From 12 years old Rhinitis, chronic urticaria 0.12 g per day or 0.18 g per day. When taking antacids, the interval should be more than 150 minutes

Remedies for seasonal allergies

The treatment of the seasonal reaction is to relieve the symptoms of the disease, such as rhinorrhea (abundant discharge from the nose), allergic conjunctivitis, tearing, burning and itching.

If nasal breathing is very difficult, it is advisable to prepare the nasal passages before conducting antiallergic therapy.

For this purpose, medicines for seasonal allergies are used in the form of nasal drops with a vasoconstrictive effect (Xylometazoline, Oxymetazoline, Naphazoline), 2 instillations in both halves of the nose with an interval of 7-11 hours. The course of therapy should not exceed ten days in order to avoid undesirable effects: atrophy of the nasal mucosa, swelling and enlargement of the turbinates, dysfunction of the heart muscle.

With abundant nasal discharge, inhibitors of acetylcholine receptors (a mediator parasympathetic system), in topical form every 7 hours, by performing two sprays in each nostril (ipratropium bromide). With rhinitis moderate cromones (preparations of cromoglycic acid) are used at 0.025 g with an interval of 4-6 hours in the form of a nasal spray.

Derivatives of levocetirizine () are effective. Rupatadine fumarate (Rupafine) 10 mg per day is also prescribed.

Effective drugs

Among the antihistamines of the last class, there are especially effective ones. Erius is among them. The mechanism of action is due to the blockade of histamine receptors due to the release of active metabolites of loratadine after the penetration of the drug into the blood. The agent blocks the release of allergy mediators (interleukins, histamine, serotonin), which explains the antipruritic and antiexudative effect.

Erius from allergies does not pass through the blood-brain barrier, does not cause a cardiotoxic effect. For persons employed in areas requiring increased attention and concentration, the drug is indicated. The action is not accompanied by a sedative effect, due to the lack of influence on the work of the inhibitory centers of the nervous system.

Erius - universal remedy, which combines the elimination of allergies, antihistamine action (blocks histamine receptors), prevention of inflammation (reduces the production of chemokines, selectin, interleukins, migration of eosinophils, chemotaxis to inflammation foci).

New antiallergic drugs in 2016 and 2017 include:

  • Eliza;
  • Allerway;
  • Alestamine;
  • Levocetirizine.

The presented tablets of the new generation for allergies for 2016 and 2017 are prolonged, they are used once during the day. The use of these latest 3rd generation allergy drugs in pregnant women is not carried out, since there are no relevant studies. Appointment is acceptable from adolescence.

Adverse disorders include cerebral disorders, heart failure, increased liver enzymes, dyspepsia. Perhaps the development of myalgia, increased photosensitivity (however, there is no clinical evidence).

The specified list of 3rd generation antihistamines is derivatives of levocetirizine and desloratadine, characterized by high bioavailability, rapid development of the pharmacological effect.

Before starting treatment, you should consult a doctor. He will tell you what to buy for allergies, which medicines for symptoms are best suited for a particular patient.