The best antihistamine. Antihistamines - generations, principles of action, overview of drugs

People who experience allergies regularly buy antihistamines and know what it is.

Timely taken pills save from a debilitating cough, swelling, rash, itching and redness of the skin. The pharmaceutical industry has been releasing similar drugs for many years, and each new batch is formulated as a separate generation.

Today we will talk about the latest generation of antihistamines and consider the most effective of them.

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 the human body comes into contact with an irritant, specific substances are produced, among which histamine exhibits increased activity. In a healthy person, it is located 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 is a general definition of all drugs that have the indicated 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)

The effectiveness of the taken pill is felt after 20 minutes, and after the drug is discontinued, it remains 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 various cases, is now prescribed by pediatricians only from the 7th month of life.

The most gentle option for the smallest is Suprastin. It quickly exhibits healing 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 of age, the child's body gradually strengthens and can normally tolerate stronger drugs. When itching skin, the names of antihistamines for this age group of patients, the specialist will consider the following:

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 to the 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 an antihistamine tablet on the eve of 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.

Today we will talk about:

Antihistamines are substances that inhibit the action of free histamine. When an allergen enters the body, histamine is released from the mast cells of the connective tissue that are part of the body's immune system. It begins to interact with specific receptors and cause itching, swelling, rashes 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 tachycardia, dryness of the nasopharynx and mouth, urinary retention, constipation, visual impairment. These features can be beneficial in rhinitis, but they can increase airway obstruction caused by bronchial asthma (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 combination products that are used for migraines, 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

Diphenhydramine is prescribed for hay fever, urticaria, sea sickness, air sickness, vasomotor rhinitis, bronchial asthma, allergic reactions caused by the administration of medicinal substances (for example, antibiotics), in the treatment of 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.

Minuses: 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.

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, Quincke's edema, 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 the complex treatment of Quincke's edema 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

LoraGeksal is recommended for year-round and seasonal allergic rhinitis, conjunctivitis, itchy dermatoses, urticaria, Quincke's edema, allergic insect bites and various pseudo-allergic reactions.

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.

Hismanal

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.

Antihistamines during pregnancy

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

Natural antihistamines, which include vitamins C, B12, pantothenic, oleic and nicotinic acids, zinc, fish oil, can help get rid of some allergic symptoms.

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

There are several groups of drugs used in allergic diseases. This:

• antihistamines;
• membrane stabilizing drugs - preparations of cromoglycic acid () and ketotifen;
• topical and systemic glucocorticosteroids;
• intranasal decongestants.

In this article, we will only talk about the first group - antihistamines. These are drugs that block H1-histamine receptors and, as a result, reduce the severity of allergic reactions. To date, there are more than 60 antihistamines for systemic use. Depending on the chemical structure and the effects on the human body, these drugs are combined into groups, which we will discuss below.

What is histamine and histamine receptors, the principle of action of antihistamines

There are several types of histamine receptors in the human body.

Histamine is a biogenic compound formed as a result of a number of biochemical processes, and is one of the mediators involved in the regulation of vital body functions and playing a leading role in the development of many diseases.

Under normal conditions, this substance is in the body in an inactive, bound state, however, with various pathological processes (hay fever, and so on), the amount of free histamine increases many times, which is manifested by a number of specific and nonspecific symptoms.

Free histamine has the following effects on the human body:

• causes spasm of smooth muscles (including the muscles of the bronchi);
• dilates capillaries and lowers blood pressure;
• causes stagnation of blood in the capillaries and an increase in the permeability of their walls, which entails thickening of the blood and swelling of the tissues surrounding the affected vessel;
• reflexively excites the cells of the adrenal medulla - as a result, adrenaline is released, which contributes to the narrowing of arterioles and an increase in heart rate;
• enhances the secretion of gastric juice;
• plays the role of a neurotransmitter in the central nervous system.

Outwardly, these effects appear in the following way:

• bronchospasm occurs;
• the nasal mucosa swells - nasal congestion appears and mucus is released from it;
• itching, redness of the skin appears, all kinds of elements of a rash form on it - from spots to blisters;
• the digestive tract responds to an increase in the level of histamine in the blood with a spasm of the smooth muscles of the organs - there are pronounced cramping pains throughout the abdomen, as well as an increase in the secretion of digestive enzymes;
• from the side of the cardiovascular system, and can be noted.

In the body, there are special receptors for which histamine has an affinity - H1, H2 and H3-histamine receptors. In the development of allergic reactions, mainly H1-histamine receptors play a role, located in the smooth muscles of the internal organs, in particular, the bronchi, in the inner membrane - the endothelium - of the vessels, in the skin, and also in the central nervous system.

Antihistamines affect precisely this group of receptors, blocking the action of histamine by the type of competitive inhibition. That is, the drug does not displace histamine already bound to the receptor, but occupies a free receptor, preventing histamine from attaching to it.

If all receptors are occupied, the body recognizes this and gives a signal to reduce the production of histamine. Thus, antihistamines prevent the release of new portions of histamine, and are also means of preventing the occurrence of allergic reactions.

Classification of antihistamines

Several classifications of drugs in this group have been developed, but none of them is generally accepted.

Depending on the characteristics of the chemical structure, antihistamines are divided into the following groups:

• ethylenediamines;
• ethanolamines;
• alkylamines;
• quinuclidine derivatives;
• alphacarboline derivatives;
• phenothiazine derivatives;
• piperidine derivatives;
• piperazine derivatives.

In clinical practice, the classification of antihistamines by generations has become more widely used, which are currently distinguished by 3:

1. 1st generation antihistamines:

• diphenhydramine (diphenhydramine);
• doxylamine (donormil);
• clemastine (tavegil);
• chloropyramine (suprastin);
• mebhydrolin (diazolin);
• promethazine (pipolphen);
• quifenadine (fencarol);
• cyproheptadine (peritol) and others.

1. 2nd generation antihistamines:

• acrivastine (semprex);
• dimethindene (fenistil);
• terfenadine (histadine);
• azelastine (allergodil);
• loratadine (lorano);
• cetirizine (cetrin);
• bamipin (soventol).

1. 3rd generation antihistamines:

• fexofenadine (telfast);
• deslorathodine (erius);
• levocetirizine.

1st generation antihistamines

Antihistamines of the first generation have a pronounced sedative effect.

According to the predominant side effect, drugs in this group are also called sedatives. They interact not only with histamine receptors, but also with a number of other receptors, which determines their individual effects. They act for a short time, which is why they require multiple doses during the day. The effect comes quickly. Available in different dosage forms - for oral administration (in the form of tablets, drops) and parenteral administration (in the form of a solution for injection). Affordable.

With prolonged use of these drugs, their antihistamine effectiveness is significantly reduced, which necessitates a periodic change of the drug - once every 2-3 weeks.

Some 1st generation antihistamines are included in combination medicines for the treatment of colds, as well as sleeping pills and sedatives.

The main effects of 1st generation antihistamines are:

• local anesthetic - associated with a decrease in membrane permeability to sodium; the most powerful local anesthetics from the drugs of this group are promethazine and diphenhydramine;
• sedative - due to a high degree of penetration of drugs of this group through the blood-brain barrier (that is, into the brain); the degree of severity of this effect in different drugs is different, it is most pronounced in doxylamine (it is often used as a sleeping pill); the sedative effect is enhanced with the simultaneous use of alcoholic beverages or the use of psychotropic drugs; when taking extremely high doses of the drug, instead of the effect of sedation, marked excitement is noted;
• anti-anxiety, calming effect is also associated with the penetration of the active substance into the central nervous system; maximally expressed in hydroxyzine;
• anti-sickness and antiemetic - some representatives of the drugs in this group inhibit the function of the labyrinth of the inner ear and reduce the stimulation of receptors of the vestibular apparatus - they are sometimes used for Meniere's disease and motion sickness in transport; this effect is most pronounced in drugs such as diphenhydramine, promethazine;
• atropine-like action - cause dryness of the mucous membranes of the oral and nasal cavities, increased heart rate, visual disturbances, urinary retention, constipation; may exacerbate bronchial obstruction, lead to exacerbation of glaucoma and obstruction in - with these diseases are not used; these effects are most pronounced in ethylenediamines and ethanolamines;
• antitussive - drugs of this group, in particular, diphenhydramine, have an effect directly on the cough center located in the medulla oblongata;
• the antiparkinsonian effect is obtained by inhibiting the effects of acetylcholine by the antihistamine;
• antiserotonin effect - the drug binds to serotonin receptors, alleviating the condition of patients suffering from migraine; especially pronounced in cyproheptadine;
• expansion of peripheral vessels - leads to a decrease in blood pressure; maximally expressed in phenothiazine preparations.

Since drugs in this group have a number of undesirable effects, they are not the drugs of choice for the treatment of allergies, but they are still often used for it.

Below are the individual, most commonly used, representatives of the drugs in this group.

diphenhydramine (diphenhydramine)

One of the first antihistamines. It has a pronounced antihistamine activity, in addition, it has a local anesthetic effect, and also relaxes the smooth muscles of the internal organs and is a weak antiemetic. Its sedative effect is similar in strength to the effects of neuroleptics. In high doses, it also has a hypnotic effect.

Rapidly absorbed when taken orally, penetrates the blood-brain barrier. Its half-life is about 7 hours. Undergoes biotransformation in the liver, excreted by the kidneys.

It is used for all kinds of allergic diseases, as a sedative and hypnotic, as well as in the complex therapy of radiation sickness. Less commonly used for vomiting of pregnant women, seasickness.

Inside is prescribed in the form of tablets of 0.03-0.05 g 1-3 times a day for 10-14 days, or one tablet at bedtime (as a sleeping pill).

Intramuscularly injected 1-5 ml of a 1% solution, intravenous drip - 0.02-0.05 g of the drug in 100 ml of a 0.9% sodium chloride solution.

Can be used as eye drops, rectal suppositories or creams and ointments.

Side effects of this drug are: short-term numbness of the mucous membranes, headache, dizziness, nausea, dry mouth, weakness, drowsiness. Side effects go away on their own, after a dose reduction or complete discontinuation of the drug.

Contraindications are pregnancy, lactation, prostatic hypertrophy, angle-closure glaucoma.

Chloropyramine (suprastin)

It has antihistamine, anticholinergic, myotropic antispasmodic activity. It also has antipruritic and sedative effects.

Quickly and completely absorbed when taken orally, the maximum concentration in the blood is observed 2 hours after ingestion. Penetrates through the blood-brain barrier. Biotransformirovatsya in the liver, excreted by the kidneys and faeces.

It is prescribed for all kinds of allergic reactions.

It is used orally, intravenously and intramuscularly.

Inside should be taken 1 tablet (0.025 g) 2-3 times a day, with meals. The daily dose may be increased to a maximum of 6 tablets.

In severe cases, the drug is administered parenterally - intramuscularly or intravenously, 1-2 ml of a 2% solution.

When taking the drug, side effects such as general weakness, drowsiness, decreased reaction rate, impaired coordination of movements, nausea, dry mouth are possible.

Enhances the effect of hypnotics and sedatives, as well as narcotic analgesics and alcohol.

Contraindications are similar to those of diphenhydramine.

Clemastine (tavegil)

By structure and pharmacological properties, it is very close to diphenhydramine, but it acts longer (within 8-12 hours after administration) and is more active.

The sedative effect is expressed moderately.

It is used orally 1 tablet (0.001 g) before meals with plenty of water, 2 times a day. In severe cases, the daily dose can be increased by 2, maximum - 3 times. The course of treatment is 10-14 days.

It can be used intramuscularly or intravenously (within 2-3 minutes) - 2 ml of a 0.1% solution per dose, 2 times a day.

Side effects with this drug are rare. Headache, drowsiness, nausea and vomiting, constipation are possible.

Be wary appoint persons whose profession requires intense mental and physical activity.

Contraindications are standard.

Mebhydrolin (diazolin)

In addition to antihistamine, it has anticholinergic and. Sedative and hypnotic effects are extremely weak.

When taken orally, it is slowly absorbed. The half-life is only 4 hours. Biotransformed in the liver, excreted in the urine.

It is used orally, after meals, in a single dose of 0.05-0.2 g, 1-2 times a day for 10-14 days. The maximum single dose for an adult is 0.3 g, daily - 0.6 g.

Generally well tolerated. Sometimes it can cause dizziness, irritation of the gastric mucosa, blurred vision, urinary retention. In very rare cases - when taking a large dose of the drug - a slowdown in the rate of reactions and drowsiness.

Contraindications are inflammatory diseases of the gastrointestinal tract, angle-closure glaucoma and prostatic hypertrophy.

2nd generation antihistamines

Antihistamines of the second generation are characterized by high efficacy, rapid onset of action and a minimum of side effects, however, some of their representatives can cause life-threatening arrhythmias.

The purpose of the development of drugs in this group was to minimize sedative and other side effects while maintaining or even stronger antiallergic activity. And it succeeded! Antihistamine drugs of the 2nd generation have a high affinity specifically for H1-histamine receptors, with virtually no effect on choline and serotonin receptors. The advantages of these drugs are:

• rapid onset of action;
• long duration of action (the active substance binds to the protein, which ensures its longer circulation in the body; in addition, it accumulates in organs and tissues, and is also slowly excreted);
• additional mechanisms of anti-allergic effects (suppress the accumulation of eosinophils in the respiratory tract associated with the intake of an allergen, and also stabilize mast cell membranes), causing a wider range of indications for their use (,);
• with prolonged use, the effectiveness of these drugs does not decrease, that is, there is no effect of tachyphylaxis - there is no need to periodically change the drug;
• since these drugs do not penetrate or penetrate in extremely small quantities through the blood-brain barrier, their sedative effect is minimal and is observed only in patients who are particularly sensitive in this regard;
• do not interact with psychotropic drugs and ethyl alcohol.

One of the most adverse effects of 2nd generation antihistamines is their ability to cause fatal arrhythmias. The mechanism of their occurrence is associated with blocking the potassium channels of the heart muscle with an antiallergic agent, which leads to a prolongation of the QT interval and the occurrence of arrhythmia (usually ventricular fibrillation or flutter). This effect is most pronounced in drugs such as terfenadine, astemizole and ebastine. The risk of its development increases significantly with an overdose of these drugs, as well as in the case of a combination of taking them with antidepressants (paroxetine, fluoxetine), antifungals (itraconazole and ketoconazole) and some antibacterial agents (antibiotics from the macrolide group - clarithromycin, oleandomycin, erythromycin), some antiarrhythmics (disopyramide, quinidine), when the patient consumes grapefruit juice and severe.

The main form of release of antihistamines of the 2nd generation is tableted, while parenteral ones are absent. Some drugs (such as levocabastine, azelastine) are available as creams and ointments and are intended for topical administration.

Consider the main drugs of this group in more detail.

Acrivastine (semprex)

Well absorbed when taken orally, begins to act within 20-30 minutes after ingestion. The half-life is 2-5.5 hours, it penetrates the blood-brain barrier in a small amount, is excreted in the urine unchanged.

Blocks H1-histamine receptors, to a small extent has a sedative and anticholinergic effect.

It is used for all kinds of allergic diseases.

Against the background of admission, in some cases, drowsiness and a decrease in the reaction rate are possible.

The drug is contraindicated during pregnancy, during lactation, with severe, severe coronary and, as well as children under 12 years of age.

Dimetinden (Fenistil)

In addition to antihistamine, it has a weak anticholinergic, anti-bradykinin and sedative effects.

It is quickly and completely absorbed when taken orally, while bioavailability (degree of digestibility) is about 70% (in comparison, when using cutaneous forms of the drug, this figure is much lower - 10%). The maximum concentration of the substance in the blood is observed 2 hours after ingestion, the half-life is 6 hours for the usual and 11 hours for the retard form. Through the blood-brain barrier penetrates, excreted in the bile and urine in the form of metabolic products.

Apply the drug inside and topically.

Inside, adults take 1 capsule of retard at night or 20-40 drops 3 times a day. The course of treatment is 10-15 days.

The gel is applied to the affected areas of the skin 3-4 times a day.

Side effects are rare.

Contraindication is only the 1st trimester of pregnancy.

Enhances the effect on the central nervous system of alcohol, sleeping pills and tranquilizers.

Terfenadine (histadine)

In addition to antiallergic, it has a weak anticholinergic effect. It does not have a pronounced sedative effect.

Well absorbed when taken orally (bioavailability delivers 70%). The maximum concentration of the active substance in the blood is observed after 60 minutes. It does not penetrate the blood-brain barrier. Biotransformed in the liver with the formation of fexofenadine, excreted in faeces and urine.

The antihistamine effect develops after 1-2 hours, reaches a maximum after 4-5 hours, and lasts for 12 hours.

Indications are the same as for other drugs in this group.

Assign 60 mg 2 times a day or 120 mg 1 time per day in the morning. The maximum daily dose is 480 mg.

In some cases, when taking this drug, the patient develops such side effects as erythema, fatigue, headache, drowsiness, dizziness, dry mucous membranes, galactorrhea (outflow of milk from the mammary glands), increased appetite, nausea, vomiting, in case of an overdose - ventricular arrhythmias.

Contraindications are pregnancy and lactation.

Azelastine (allergodil)

It blocks H1-histamine receptors, and also prevents the release of histamine and other allergy mediators from mast cells.

It is rapidly absorbed in the digestive tract and from the mucous membranes, the half-life is as long as 20 hours. Excreted as metabolites in the urine.

They are used, as a rule, for allergic rhinitis and.

When taking the drug, side effects such as dryness and irritation of the nasal mucosa, bleeding from it and taste disorders during intranasal use are possible; irritation of the conjunctiva and a feeling of bitterness in the mouth - when using eye drops.

Contraindications: pregnancy, lactation, children under 6 years of age.

Loratadine (lorano, claritin, lorizal)

Long-acting H1-histamine receptor blocker. The effect after a single dose of the drug lasts for a day.

There is no pronounced sedative effect.

When taken orally, it is absorbed quickly and completely, reaches a maximum concentration in the blood after 1.3-2.5 hours, and is half excreted from the body after 8 hours. Biotransformed in the liver.

Indications are any allergic diseases.

It is usually well tolerated. In some cases, dry mouth, increased appetite, nausea, vomiting, sweating, pain in the joints and muscles, hyperkinesis may occur.

Contraindication is hypersensitivity to loratadine and lactation.

Be wary appoint pregnant women.

Bamipin (Soventol)

Blocker of H1-histamine receptors for local use. It is prescribed for allergic skin lesions (urticaria), contact allergies, as well as for frostbite and burns.

The gel is applied in a thin layer to the affected areas of the skin. After half an hour, it is possible to re-apply the drug.

Cetirizine (Cetrin)

Metabolite of hydroxyzine.

It has the ability to freely penetrate the skin and quickly accumulate in it - this leads to a rapid onset of action and high antihistamine activity of this drug. There is no arrhythmogenic effect.

It is rapidly absorbed when taken orally, its maximum concentration in the blood is observed 1 hour after ingestion. The half-life is 7-10 hours, but in case of impaired renal function, it is extended to 20 hours.

The spectrum of indications for use is the same as for other antihistamines. However, due to the characteristics of cetirizine, it is the drug of choice in the treatment of diseases manifested by skin rashes - urticaria and allergic dermatitis.

Take 0.01 g in the evening or 0.005 g twice a day.

Side effects are rare. This is drowsiness, dizziness and headache, dry mouth, nausea.

3rd generation antihistamines

III generation antihistamines have high antiallergic activity and are devoid of arrhythmogenic effect.

These drugs are active metabolites (metabolites) of the previous generation. They are devoid of cardiotoxic (arrhythmogenic) effect, but retained the advantages of their predecessors. In addition, 3rd generation antihistamines have a number of effects that enhance their antiallergic activity, which is why their effectiveness in treating allergies is often higher than that of the substances from which they are produced.

Fexofenadine (Telfast, Allegra)

It is a metabolite of terfenadine.

It blocks H1-histamine receptors, prevents the release of allergy mediators from mast cells, does not interact with cholinergic receptors, and does not depress the central nervous system. It is excreted unchanged with feces.

The antihistamine effect develops within 60 minutes after a single dose of the drug, reaches a maximum after 2-3 hours, lasts for 12 hours.

Side effects such as dizziness, headache, weakness are rare.

Desloratadine (erius, edema)

It is an active metabolite of loratadine.

It has anti-allergic, anti-edematous and antipruritic effects. When taken in therapeutic doses, it practically does not have a sedative effect.

The maximum concentration of the drug in the blood is reached 2-6 hours after ingestion. The half-life is 20-30 hours. Does not penetrate the blood-brain barrier. Metabolized in the liver, excreted in the urine and feces.

In 2% of cases, against the background of taking the drug, headache, increased fatigue and dry mouth may occur.

In renal failure appoint with caution.

Contraindications are hypersensitivity to desloratadine. As well as periods of pregnancy and lactation.

Levocetirizine (Aleron, L-cet)

A derivative of cetirizine.

The affinity for H1-histamine receptors of this drug is 2 times higher than that of its predecessor.

Facilitates the course of allergic reactions, has anti-edematous, anti-inflammatory, antipruritic effect. Practically does not interact with serotonin and cholinergic receptors, does not have a sedative effect.

When taken orally, it is rapidly absorbed, its bioavailability tends to 100%. The effect of the drug develops 12 minutes after a single dose. The maximum concentration in blood plasma is observed after 50 minutes. It is excreted mainly by the kidneys. It is allocated with breast milk.

Contraindicated in case of hypersensitivity to levocetirizine, severe renal insufficiency, severe galactose intolerance, deficiency of the lactase enzyme or impaired absorption of glucose and galactose, as well as during pregnancy and lactation.

Side effects are rare: headache, drowsiness, weakness, fatigue, nausea, dry mouth, muscle pain, palpitations.

Antihistamines and pregnancy, lactation

Therapy of allergic diseases in pregnant women is limited, since many drugs are dangerous for the fetus, especially in the first 12-16 weeks of pregnancy.

When prescribing antihistamines to pregnant women, the degree of their teratogenicity should be taken into account. All medicinal substances, in particular anti-allergic ones, are divided into 5 groups depending on how dangerous they are to the fetus:

A - special studies have shown that there is no harmful effect of the drug on the fetus;

B - when conducting experiments on animals, no negative effects on the fetus were found, special studies on humans have not been conducted;

C - animal experiments have revealed a negative effect of the drug on the fetus, but it has not been proven in relation to humans; drugs of this group are prescribed to a pregnant woman only when the expected effect exceeds the risk of its harmful effects;

D - the negative effect of this drug on the human fetus has been proven, however, its administration is justified in certain life-threatening situations for the mother, when safer drugs were ineffective;

X - the drug is certainly dangerous for the fetus, and its harm exceeds any theoretically possible benefit to the mother's body. These drugs are absolutely contraindicated in pregnant women.

Systemic antihistamines during pregnancy are used only when the expected benefit outweighs the possible risk to the fetus.

None of the drugs in this group is included in category A. Category B includes drugs of the 1st generation - tavegil, diphenhydramine, peritol; 2nd generation - loratadine, cetirizine. Category C includes allergodil, pipolfen.

Cetirizine is the drug of choice for the treatment of allergic diseases during pregnancy. Loratadine and fexofenadine are also recommended.

The use of astemizole and terfenadine is unacceptable due to their pronounced arrhythmogenic and embryotoxic effects.

Desloratadine, suprastin, levocetirizine cross the placenta, and therefore are strictly contraindicated for pregnant women.

With regard to the lactation period, the following can be said ... Again, the uncontrolled intake of these drugs by a nursing mother is unacceptable, since no human studies have been conducted on the degree of their penetration into breast milk. If necessary, in these drugs, a young mother is allowed to take the one that is allowed to be taken by her child (depending on age).

In conclusion, I would like to note that even though this article describes in detail the most commonly used drugs in therapeutic practice and indicates their dosages, the patient should start taking them only after consulting a doctor!

Which doctor to contact

If acute allergy symptoms appear, you can contact a general practitioner or pediatrician, and then an allergist. If necessary, a consultation of an ophthalmologist, dermatologist, ENT doctor, pulmonologist is appointed.

The list of 4th generation antihistamines is quite large. They are modern means that gently affect any irritants and allergens in the body. The main difference is long-term therapy, minimal side effects.

4th generation antihistamines, a list of these drugs in tablets, drops

These drugs are metabolites - these are metabolic products of active substances.

These medicines are prescribed for adults and children to treat pollinosis, skin rashes or bronchial asthma. Only a doctor can prescribe drugs after a comprehensive diagnosis of the patient.

List of new generation antihistamines in the form of tablets and drops:

1. Fexofenadine. The drug is available in two dosage forms - tablets, suspension. An hour after taking this medication, the symptoms of allergic reactions begin to disappear in patients. Fexofenadine is not prescribed for children under six years of age, patients with renal or hepatic pathology, pregnant women, nursing mothers.
2. Levocetirizine. It is available in the form of tablets, drops, syrup. The maximum level of concentration of the active substance in the body is determined for two days. It passes into breast milk, so it is forbidden to use it during the feeding period. Levocetirizine is taken for the effective treatment of various forms of allergic rhinitis, seasonal allergies, urticaria, allergic dermatosis. Do not drink alcoholic beverages while taking this medicine. If the correct functioning of the kidneys is impaired in patients, then the daily dosage of the drug is determined after passing the tests.
3. Cetirizine. This drug is sold in the form of drops, syrup, tablets. It copes well with any manifestations of allergies - these are skin rashes, severe itching. It is most often prescribed for the treatment of itchy dermatosis, urticaria. The dosage is selected by the doctor depending on the age, indications. During pregnancy, cetirizine is prescribed only in rare cases.
4. Desloratadine. It can be bought in the form of tablets and drops for oral administration. The substances included in the composition are quickly absorbed, begin to act an hour after consumption. This drug is prescribed to patients diagnosed with allergic rhinitis, skin rash, urticaria, hay fever.
5. Hifenadine. It shows high efficiency in dermatosis, acute or chronic urticaria, food allergies, hay fever, allergic conjunctivitis, rhinitis, angioedema.

Options in ointments, gels

Fourth generation drugs in the form of ointments and gels have a potent effect. They quickly relieve inflammation on the skin, penetrate deeply into it.

There are several powerful drugs that are used in modern medicine:

1. Galcinonide. This medicine is excellent for eczema that occurs due to a nervous or allergic reaction. Acute inflammatory processes in areas of the skin in most cases are accompanied by edema, excessive itching. The ointment gently affects the inflamed skin, quickly removes all allergy symptoms.
2. Hydrocortisone ointment. This is a fairly effective anti-allergic agent that relieves itching, swelling, irritation and other skin rashes. It is prescribed to patients who have hypersensitivity to individual components of the drug.
3. Deperzolon is available as an ointment for external use. It helps to remove the manifestations of allergic reactions, constricts blood vessels, relieves excessive itching. In most cases, this ointment is prescribed for the treatment of dermatitis, dermatosis, insect sting allergies, and a variety of skin reactions.
4. Beloderm. This is an effective and effective ointment for external use. Within an hour after use, it relieves itching, constricts blood vessels, relieves inflammation.
5. Sinaflan is an effective anti-allergic drug that is designed to relieve inflammation. It is prescribed to patients diagnosed with atopic dermatitis, lichen, allergic skin reactions and swelling.

Spray treatment is the most effective way to deal with allergic rhinitis.

1. Flixonaz. It relieves not only allergies, but also inflammation of the nasal mucosa.
2. Avamis. The effect of the drug is achieved 7 hours after use. After use, manifestations of unpleasant side effects are possible - this is excessive dryness of the mucous membrane, thirst increases, nosebleeds may open.
3. Nasonex. The drug belongs to the steroid group, so it is quite effective for the treatment of allergic rhinitis. It is prescribed for adults and young children. The dosage is selected after a comprehensive examination of patients.

Differences from previous generations

Fourth generation antihistamines differ from previous medicines in their high effectiveness in combating various allergy symptoms.

They have a minimum number of side effects, so in most cases they are prescribed even to pregnant patients.

The following pharmacological properties can be distinguished:

• prevention of bronchial spasms;
• elimination of severe itching;
• antispastic effect on the body;
• removal of puffiness;
• sedative action.

When histamine passes from a bound state to a free state, the effect of a viral action is created in the body. Therefore, many patients confuse allergies with the flu or the common cold.

In the presence of a pathogen in the body, the following negative processes are observed:

• there is a spasm of the soft tissues of the intestine and bronchi;
• increased levels of adrenaline, so people have increased blood pressure, heart rate increases;
• increases the production of digestive enzymes, mucus in the bronchi, nasal cavity;
• large blood vessels narrow, so the nasal mucosa increases significantly, redness on the skin, a small rash appear, blood pressure drops;
• anaphylactic shock develops with convulsions, vomiting, loss of consciousness.

Fourth-generation antihistamines can be used while driving or working on machines where a quick response is needed. In most cases, they do not react with other drugs, including antibiotics.

For this reason, many doctors prescribe them for the treatment of inflammatory processes, diseases.

Composition, therapeutic effect of new sample products

Presented drugs perform blocking of H1 and H2-histamine receptors. Due to this effect in the human body, the reaction to the presence of the histamine mediator decreases, and the allergic reaction is stopped.

They quickly act on the symptoms, retain their effect for a long time. These are safe drugs that do not harm the functioning of the heart and blood vessels.

They can be taken for a long time, do not cause drowsiness, deterioration.

The composition of fourth-generation antihistamine drugs includes an active ingredient. This may be levocetirizine hydrochloride, the primary metabolite of loratadine, cetirizine dihydrochloride and others.

Video

Indications for use

Taking 4th generation antihistamines is necessary for patients who are faced with the following problems:

• allergic rhinitis (it can manifest itself in a certain season or throughout the year);
• allergic form of conjunctivitis (this problem is seasonal or year-round);
• chronic urticaria;
• allergic contact dermatitis;
• atopic dermatitis.

Before taking it is important to consult with your doctor, undergo a comprehensive examination. The main task of an allergist is to find the pathogen that provokes a negative reaction in the body.

Contraindications for use and side effects

The main contraindication to the use of new generation antihistamines is individual intolerance to the active substance, hypersensitivity to individual components.

Medicines are taken under the strict supervision of the attending physician. Before prescribing the drug, allergists carefully study the history of each patient and prescribe a comprehensive examination.

In most cases, 4th generation antihistamines are well tolerated by patients. Isolated cases of adverse reactions have been reported.


Against the background of the reception, the following undesirable effects may occur:

• fatigue, decreased activity;
• headache;
• increased dry mouth, regular thirst;
• hallucinations;
• dizziness, drowsiness, sleep disturbance, agitation, irritation, convulsions;
• accelerated heart rate, heart rate;
• pain in muscle tissue;
• skin rash, excessive itching, shortness of breath, Quincke's edema, anaphylactic reaction.

Means that do not cause adverse reactions

List of 4th generation antihistamines that do not cause cough and other side effects:

• fexofenadine;
• desloratadine;
• levocetirizine.

There are several benefits of using these drugs:

1. Maximum high level impact on the patient's body, the onset of a therapeutic effect. After use, a person feels relief after 20-30 minutes.
2. The effect lasts for two days. Therefore, patients do not need to take drugs frequently.
3. No need to harm your health and drink topical corticosteroids.
4. No tachyphylaxis effect.
5. Long-term use does not adversely affect the functioning of the central nervous system, does not cause disturbances in the myocardium.
6. These medicines can be used as an allergy prophylaxis.

Loratidine and Xizal are distinguished by their maximum therapeutic effect. They block the release of mediators in the inflammatory process. Patients will be able to get rid of the negative manifestation of an allergic reaction for a long time.

Features of use in children and the elderly

Antihistamines of the 4th generation are safe, have a minimum number of side effects after their use. They are manufactured according to the innovative developments of the best pharmaceutical companies. Such drugs act on H1 receptors, thereby gently, quite effectively removing the body's high susceptibility to histamine.

Already after the first application in young children, any clinical manifestations of an allergic reaction disappear. Inflammatory processes are completely stopped two weeks after the start of treatment.

Newborn children are not recommended to use antihistamines. But there are times when it is impossible to cure a child without them. Infants diagnosed with food allergies, urticaria, drug dermatitis should use the new drug Tavegil.

It effectively removes puffiness, reduces itching, restores the natural tone of the skin.

The safest and most harmless drugs:

• xyzal;
• desloratidine;
• levocetirizine;
• fexofenadine.

These drugs may be prescribed for older people. New generation drugs do not harm the body so much with prolonged use and well eliminate any clinical manifestations.

Antihistamines of the 4th generation are not addictive, so there is no need to increase the dosage with a decrease in effectiveness. During treatment, older people need to drink more liquid so that the active substance is well absorbed in the body.

General opinion of those who have used them

4th generation antihistamines have recently appeared in pharmacies, but are already in high demand and popularity. Many patients were able to appreciate their fast action, lack of side effects. But there are those who are afraid to experience the effect of these newest drugs.

They are successfully used by people whose professions are associated with the need for increased attention. These are the drivers Vehicle, pilots, surgeons, seamstresses and others.

4th generation antihistamines

5 (100%) 6 votes

String(10) "error stat" string(10) "error stat" string(10) "error stat"

In the window of any pharmacy, there are a variety of allergy pills, the price of which varies markedly, which misleads an inexperienced buyer who has not previously dealt with allergies.

Today, thanks to a wide selection of medicines, you can buy both good, but quite expensive, and the cheapest drugs. How to make the right choice and why the new product may be better than the old ones, read the article.

Allergy pills - a list

During an allergic reaction, histamine is released into the bloodstream, a substance that can lead to narrowing of the airways and dilation of blood vessels, thereby causing swelling or swelling of tissues, as well as a decrease in blood pressure.

All antihistamines act as blockers of H1 and H2 histamine receptors, thereby preventing or reducing the characteristic symptoms of allergies.

Which allergy pills to choose?

Treatment of various types of allergies can be done both with the cheapest drugs and with the more expensive ones provided by the pharmaceutical industry.

For the treatment and relief of symptoms of skin manifestations and allergic rhinoconjunctivitis, most often, the latest generation allergy pills are used, which can be purchased at a pharmacy without a doctor's prescription.

Consider the most effective and inexpensive allergy pills in more detail.

Antihistamine tablets for allergies fall into two categories:

1. having a sedative effect;
2. non-sedating allergy pills that do not cause drowsiness.

The first generation are older anti-allergic drugs that relieve symptoms but cause drowsiness, making it difficult to use these drugs when driving motor vehicles or in work that requires high concentration. In addition, the concentration of active substances is quickly excreted from the blood, which requires taking the drug two or three times a day.

New generation allergy pills do not cause drowsiness, so they are used even for long courses, for example, during the dusting season of grasses and trees.

Antihistamines

CETIRIZINE (10 mg)

Tablets for skin allergies with this active ingredient are very popular among allergy sufferers, they are also taken for the treatment of hay fever, seasonal manifestations of rhinoconjunctivitis and Quincke's edema. The best allergy pills that even children from 6 months old can take.

• ZIRTEK No. 7 from 189 rubles.
• CETRIN No. 20 from 160 rubles.
• ZODAK №10 from 142 rubles.
• PARLAZIN №10 from 110 rubles.
• LETIZEN No. 10 from 82 rubles.
• CETIRIZINE No. 10 from 60 rubles.

LEVOCETIRIZINE (5 mg)

Preparations with levocetirizine are used to eliminate the manifestations of year-round and seasonal allergic rhinoconjunctivitis, hay fever, various allergic skin rashes, Quincke's edema. Contraindications - age up to 6 years.

• LEVOCETIRIZINE TEVA №14 from 360 rubles.
• KSIZAL №7 from 316 rubles.
• GLENCET №7 from 290 rub.
• SUPRASTINEX №7 from 261 rubles.
• ELTSET No. 7 from 112 rubles.

LORATADIN (10 mg)

It is used to relieve symptoms of seasonal and year-round allergic rhinoconjunctivitis, as well as to eliminate allergic skin rashes and Quincke's edema. It is effective for insect allergies (to poison and insect bites) and pseudo-allergies. Contraindications - age up to 2 years.

• CLARITIN №10 from 206 rubles.
• LOMILAN №7 from 112 rubles.
• CLARICENSE №10 from 68 rubles.
• CLARIDOL No. 7 from 62 rubles.
• LORAGEXAL №10 from 50 rubles.
• LORATADIN VERTE №10 from 26 rubles

DESLORATADINE (5 mg)

It is used in the treatment of allergic rhinitis and idiopathic urticaria. Contraindications - age up to 12 years.

• ELIZEA №30 from 350 rubles.
• LORDESTIN №10 from 270 rub.
• ERIUS №7 from 235 rubles.
• DEZAL No. 10 from 227 rubles.
• BLOGIR-3 №10 from 164 rubles.
• DEZLORATADINE No. 10 from 120 rubles.

FEXOPHENADINE (120 mg)

It is taken to eliminate the symptoms of rhinoconjunctivitis, various allergic rashes and relieve angioedema. Contraindications - age up to 6 years.

• ALLEGRA №10 from 697 rubles
• FEKSADIN №10 from 247 rubles.
• FEXOFAST №10 from 215 rubles.

MEBHYDROLINE (50 mg)

Indications: hay fever, skin rashes accompanied by itching, allergic rhinoconjunctivitis, allergic reactions to insect venom. Contraindicated in children under 2 years of age.

• DIAZOLIN №10 from 58 rubles.

DIPHENGYDRAMINE (50 mg)

Application: allergic rhinoconjunctivitis, angioedema, allergic reactions to drugs, complex therapy of anaphylactic shock. Contraindicated in newborns.

• DIMEDROL №20 from 10 rubles.

EBASTINE (10 mg)

Allergic rhinitis and urticaria of various etiologies. Children under 6 years of age are contraindicated.

• KESTIN №5 from 216 rubles.

KETOTIFEN (1 mg)

Relieves and prevents the symptoms of rhinoconjunctivitis associated with seasonal allergies, is effective in atopic dermatitis and urticaria. Contraindications - age up to 3 years.

• KETOTIFEN №30 from 57 rubles.

RUPATADINE FUMARATE (10 mg)

Symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria. Age under 12 years is a contraindication.

• RUPAFIN No. 7 from 362 rubles.

CHLOROPYRAMINE (25 mg)

Indications: allergic rashes, rhinoconjunctivitis, hay fever symptoms, angioedema. Contraindications - early infancy up to 1 month.

• SUPRASTIN №20 from 123 rubles.

CLEMASTINE (1 mg)

Indications: skin rashes, rhinoconjunctivitis, hay fever, itchy dermatitis, contact dermatitis, eczema, insect allergy (to insect venom). Contraindicated in children under 6 years of age.

• TAVEGIL №10 from 158 rubles.

Corticosteroid drugs

Corticosteroid drugs (hormonal allergy pills) based on synthetic hormones are effective against serious allergic reactions. They allow to achieve effective removal of inflammatory processes and elimination of puffiness.

Corticosteroid tablets prevent and treat nasal congestion, seasonal and year-round runny nose (rhinitis), sneezing, and itching. Also, they help reduce inflammation and swelling in other types of allergies: drug, food, cats, etc.

Because of their strong action, oral corticosteroids are usually used for a short time. Long-term use of these drugs can increase the risk of side effects, such as high blood pressure, joint pain, etc. Therefore, you should not prescribe and drink these drugs on your own, you need to seek the advice of a specialist.

• DEXAMETHASONE (Dexamethasone) 0.5 mg № 10 from 37 rubles.

Indications: angioedema, contact and atopic dermatitis, rhinoconjunctivitis, bronchial asthma.

• KENALOG (Triamcinolone) 4 mg №50 from 380 rubles.

Indications: allergic rhinoconjunctivitis, dermatitis of various origins, angioedema.

• CORTEF (Hydrocortisone) 10 mg № 100 from 359 rubles.

Indications: severe allergic conditions, seasonal or year-round rhinoconjunctivitis, bronchial asthma, contact and atopic dermatitis.

• MEDROL (Methylprednisolone) 4 mg №30 from 166 rubles
• METIPRED (Methylprednisolone) 4 mg №30 from 199 rubles.

Application: seasonal or year-round rhinoconjunctivitis, bronchial asthma, contact and atopic dermatitis, angioedema.

• POLCORTOLONE (Triamcinolone) 4 mg №50 from 400 rubles.

It is used for severe allergic diseases, various dermatitis, year-round or seasonal rhinuconjunctivitis.

• PREDNISOLONE (Prednisolone) 5 mg № 100 from 98 rubles.

With food and drug allergies, you can take Prednisolone, as it relieves the symptoms of skin manifestations, allergic rhinoconjunctivitis, angioedema, and is also effective for hay fever.

Allergy decongestant pills

Decongestants are used to constrict blood vessels and relieve nasal congestion in allergic rhinitis, as well as other swelling caused by allergic reactions. Some allergy medications include both an antihistamine and a decongestant.

How do analogues differ from patented drugs?

Cheap allergy pills are called generics (cheap analogues) in a different way. The low price of the drug is due to the fact that no studies have been conducted proving their effectiveness, unlike patented drugs. Therefore, in this case it is difficult to say whether cheap drugs will have the desired effect in the treatment of allergies.

It is unlikely that you will be able to take a pill and forget about allergies, since long-term suppression of symptoms without rational treatment can lead to unpredictable consequences on the part of the immune system. Therefore, you should definitely visit an allergist and identify the culprits of allergic reactions.