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

People who experience allergies regularly buy antihistamines and know what they are.

When taken in a timely manner, tablets can help relieve a debilitating cough, swelling, rash, itching and redness of the skin. The pharmaceutical industry has been producing such drugs for many years, and each new batch is issued as a separate generation.

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

General concept of antihistamines

To everyone who wants to understand in depth the question of what antihistamines are, doctors explain that these drugs are created to counteract 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. When exposed to an allergen, histamine enters an active phase and provokes allergy symptoms.

To relieve negative reactions, medications were invented at different times that could reduce the amount of histamine and neutralize its harmful effects on humans. Thus, antihistamines are a general definition of all drugs that have the indicated effectiveness. To date, their classification includes 4 generations.

The advantages of the drugs in question 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 childhood, a doctor has the right not to prescribe anti-allergy pills if their instructions list these conditions as contraindications.

All new generation antihistamines - list of new drugs:

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

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

Medicines containing cetirizine are good at removing skin manifestations of allergosis. One tablet brings significant relief within 2 hours from the moment of use. The result lasts for a long time.

The drug Erius is an improved analogue of Loratadine. But its efficiency is approximately 2.5 times higher. Erius is suitable for children over 1 year of age who are prone to allergies. They are given the drug in liquid form at a dosage of 2.5 ml once a day. From 5 years of age, 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 medicine Xyzal 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 product is not addictive. The body is affected for 24 hours.

Fexadin should not be taken during pregnancy, breastfeeding or children under 12 years of age.

Zodak (Cetrin, Zyrtec, Cetirizine)

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

In pediatrics, Zodak drops are used from 6 months. After 1 year, syrup is prescribed. Children can take tablets from 6 years of age. 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)

Xyzal drops and tablets work 40 minutes after administration.

The medication is indicated for the treatment of urticaria, allergies, and skin itching. For children, fourth-generation antihistamines for allergies called Xyzal are prescribed from 2 years and 6 years (drops and tablets, respectively). The pediatrician calculates the dosage based on the child’s age and weight.

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

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

Desloratadine (Erius, Lordestin, Dezal)

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

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

Doctors prescribe syrup for children 2–6 years old. Tablets are allowed to be used only from 6 years of age. Desloratadine is completely contraindicated for pregnant and lactating women. But for angioedema and bronchospasm, a specialist can choose a gentle option for using this medicine.

Antihistamines for babies

It is not recommended for newborns to take antihistamines. But sometimes situations arise when it is impossible to do without medication, for example, if the baby is stung by an insect. From 1 month of life, the child can be given Fenistil in drops.

Diphenhydramine, which was previously given to children on various occasions, is now prescribed by pediatricians only from the 7th month of life.

Suprastin is considered the most gentle option for the little ones. It quickly exhibits healing properties without causing the slightest harm to the body. Children are also prescribed Fenkarol and Tavegil. For urticaria, drug-induced dermatosis and food allergies, it is better to give Tavegil to the child. The tablets relieve swelling, restore skin color and work as an antipruritic agent.

Analogues of Tavegil are Donormil, Diphenhydramine, Bravegil and Clemastine. The child takes them if there are contraindications to the use of Tavegil.

From 2 to 5 years, the child’s body gradually strengthens and can normally tolerate stronger medications. For itchy skin, the names of antihistamines for this age group of patients, the specialist will consider the following:

Erius was mentioned above, now let’s focus on Tsetrin. These tablets can be used to prevent allergies in children prone to negative reactions. In case of individual intolerance to the constituent components, Cetrin is replaced with analogues - Letizen, Cetirinax, Zodak, Zetrinal. After 2 years, the child can take Astemizole.

From the age of 6, the list of antihistamines is expanded, since medications of different generations are suitable for such children - from 1 to 4. Younger schoolchildren can take Zyrtec, Terfenadine, Clemastine, Glencet, Suprastinex, Cesera tablets.

What Komarovsky says

Famous pediatrician E.O. Komarovsky does not advise parents to give antihistamines to young children unless absolutely necessary and without medical prescription. If a pediatrician or allergist considers it necessary to prescribe an antiallergic drug to a child, it can be taken for no more than 7 days.

Evgeniy Olegovich also prohibits 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 DPT, but Komarovsky does not see any point in this. The children's doctor explains that the body's reaction to the vaccine has nothing to do with allergies.

Women with allergies planning to have children are always interested in what antihistamines can be taken during pregnancy and preferably during lactation, or whether it is worth enduring the inconvenience associated with hay fever, rash and swelling. Doctors say that it is better for women not to take any medications during gestation, as they are potentially dangerous to 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 connective tissue mast cells, which are part of 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 bind reversibly to H1 receptors, which explains the need for large dosages and high frequency of administration.

1st generation antihistamines 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 the drugs are changed every 2-3 weeks.

The bulk of 1st generation antihistamines are fat-soluble, can cross the blood-brain barrier and bind to H1 receptors in the brain, which explains the sedative effect of these drugs, which increases after taking alcohol or psychotropic drugs. When taking moderate therapeutic doses in children and high toxic doses in adults, psychomotor agitation may occur. Due to the 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 oral cavity, urinary retention, constipation, and blurred vision. These features can be beneficial for rhinitis, but can increase airway obstruction caused by bronchial asthma (the viscosity of sputum increases) and contribute to the exacerbation of prostate adenoma, glaucoma and other diseases. At the same time, these drugs have an antiemetic and anti-sickness effect, reducing the manifestation of parkinsonism.

A number of these antihistamines are included in combination drugs that are used for migraines, colds, motion sickness, or have a sedative or hypnotic effect.

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

Diphenhydramine

Diphenhydramine is prescribed for hay fever, urticaria, seasickness, air sickness, vasomotor runny nose, bronchial asthma, allergic reactions caused by the administration of drugs (for example, antibiotics), in the treatment of peptic ulcers, dermatoses, etc.

Advantages: high antihistamine activity, reduced severity of allergic, pseudo-allergic reactions. Diphenhydramine has an antiemetic and antitussive effect, has a local anesthetic effect, making it an alternative to Novocaine and Lidocaine if they are intolerant.

Minuses: unpredictability of the consequences of taking the drug, its effect 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 characteristics of their effects.

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

Minuses: irritates the mucous membranes of the gastrointestinal tract, causes dizziness, difficulty urinating, 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, and 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 its high antihistamine activity, a rapid therapeutic effect is observed.

Minuses: side effects - drowsiness, dizziness, inhibition of reactions, etc. - are present, although 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 preventive and therapeutic agent for allergic and pseudoallergic 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 effects.

Fenkarol

Fenkarol is prescribed when addiction to other antihistamines occurs.

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

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

Antihistamines 2nd generation

They have advantages compared to 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 and physical activity are not affected;
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 from food in the gastrointestinal tract.

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

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

Claridol

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

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

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

Clarisens

Clarisens is able to suppress the release of histamine and leukotriene C4 from mast cells. It is used for the treatment and prevention of allergy manifestations such as rhinitis, conjunctivitis, and dermatosis. The drug is included in the complex treatment of 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 functioning 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 for 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, and 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, pseudoallergic 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 nervous system disorders: 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. Damage to the respiratory system can be manifested by cough, bronchospasm, sinusitis and similar manifestations.

Lomilan

Lomilan is indicated for seasonal and permanent allergic rhinitis, 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), and prevent tissue swelling within half an hour from the moment of taking the drug. The greatest effectiveness occurs after 8-12 hours, then subsides. Lomilan is not addictive and does not have a negative effect on the activity of the nervous system.

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

LauraHexal

LauraHexal 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 an anticholinergic nor a central effect, its use does not affect the attention, psychomotor functions, performance and mental qualities of the patient.

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

Claritin

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

Advantages: highly effective in the treatment of allergic diseases, the drug does not cause addiction or 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 component - rupatadine, characterized 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.

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, which increase vascular permeability, causing muscle spasms, leading to an allergic reaction. Used to treat allergic conjunctivitis, rhinitis and chronic idiopathic urticaria.

Advantages: the drug acts within an hour after application, the therapeutic effect lasts for 2 days. A five-day intake of Kestin allows you to maintain the 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, 3rd generation antihistamines

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 cardiotoxic or sedative effects, so they can be used by people whose activities involve high concentration.

These drugs block H1 receptors and also have an additional effect on allergic manifestations. They are highly selective, do not cross the blood-brain barrier, therefore they are not characterized by negative consequences from the central nervous system, and there are no side effects on the heart.

The presence of additional effects promotes the use of 3rd generation antihistamines for long-term treatment of most allergic manifestations.

Gismanal

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 over 24 hours and reaches its maximum after 9-12 days. Its duration depends on previous therapy.

Advantages: the drug has virtually no sedative effect and does not enhance the effect of taking sleeping pills or alcohol. It also does not affect driving ability or mental performance.

Minuses: Gismanal can cause increased appetite, dry mucous membranes, tachycardia, drowsiness, arrhythmia, prolongation of the QT interval, palpitations, collapse.

Trexil

Trexyl is a fast-acting, selectively active H1 receptor antagonist, a derivative of buterophenol, which differs in chemical structure from its analogues. Used for allergic rhinitis to relieve its symptoms, allergic dermatological manifestations (dermatographism, contact dermatitis, urticaria, atonic eczema), asthma, atonic and provoked physical activity, as well as in connection with acute allergic reactions to various irritants.

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

Telfast

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

Advantages: does not exhibit sedative properties, does not affect the speed of reactions and concentration, heart function, 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 rare 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, and neutrophils. The drug is used for allergic rhinitis, bronchial asthma, urticaria, conjunctivitis, dermatitis, fever, itching, antineurotic edema.

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

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

Antihistamines for children

To treat allergic manifestations in children, antihistamines of all three generations are used.

1st generation antihistamines are distinguished by the fact that they quickly exhibit their healing properties and are eliminated 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 are Tavegil, Suprastin, Diazolin, Fenkarol.

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

2nd generation antihistamines do not cause a sedative effect, 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.

The 3rd generation of antihistamines for children includes Gismanal, Terfen and others. They are used for chronic allergic processes, since they can remain 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: none, recommended for use from 3 years of age.

Antihistamines are produced for children in the form of ointments (allergic skin reactions), 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 are absolutely safe.

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

The safest antihistamines are Claritin, Zyrtec, Telfast, Avil, but their use must be agreed with a doctor.

There are several groups of medications used for allergic diseases. This:

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

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

What are 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 that takes part in the regulation of vital functions of the body and plays a leading role in the development of many diseases.

Under normal conditions, this substance is in the body in an inactive, bound state, however, during various pathological processes (hay fever, 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 bronchial muscles);
• dilates capillaries and reduces blood pressure;
• causes stagnation of blood in the capillaries and increased 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;
• increases the secretion of gastric juice;
• plays the role of a neurotransmitter in the central nervous system.

Externally, these effects appear in the following way:

• bronchospasm occurs;
• the nasal mucosa swells - nasal congestion and mucus discharge appear;
• itching, redness of the skin appears, all kinds of rash elements 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;
• on the part of the cardiovascular system, and may be observed.

There are special receptors in the body for which histamine has an affinity - H1, H2 and H3 histamine receptors. In the development of allergic reactions, the role played mainly by H1-histamine receptors located in the smooth muscles of internal organs, in particular the bronchi, in the inner lining - the endothelium - of blood vessels, in the skin, as well as in the central nervous system.

Antihistamines act specifically on this group of receptors, blocking the action of histamine through 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 histamine production. Thus, antihistamines prevent the release of new portions of histamine, and are also a 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 generation has become more widely used, of which today there are 3:

1. 1st generation antihistamines:

• diphenhydramine (diphenhydramine);
• doxylamine (donormil);
• clemastine (tavegil);
• chloropyramine (suprastin);
• mebhydrolin (diazolin);
• promethazine (pipolfen);
• 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);
• desloratodine (erius);
• Levocetirizine.

1st generation antihistamines

First generation antihistamines have a pronounced sedative effect.

Based on 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 throughout 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 an injection solution). Affordable.

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

Some 1st generation antihistamines are included in combination medications 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 this group of drugs are promethazine and diphenhydramine;
• sedative – due to the 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 varies between drugs; it is most pronounced in doxylamine (it is often used as a hypnotic); the sedative effect increases with the simultaneous consumption of alcoholic beverages or taking psychotropic drugs; when taking extremely high doses of the drug, instead of the effect of sedation, pronounced agitation is observed;
• anti-anxiety, calming effect is also associated with the penetration of the active substance into the central nervous system; most expressed in hydroxyzine;
• anti-sickness and anti-emetic - 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 and promethazine;
• atropine-like effect - causes dryness of the mucous membranes of the oral and nasal cavities, increased heart rate, visual impairment, urinary retention, constipation; may increase bronchial obstruction, lead to exacerbation of glaucoma and obstruction in cases of – not used for these diseases; These effects are most pronounced in ethylenediamines and ethanolamines;
• antitussive - drugs of this group, in particular diphenhydramine, act directly on the cough center located in the medulla oblongata;
• the antiparkinsonian effect occurs 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;
• dilatation of peripheral vessels - leads to a decrease in blood pressure; is 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 are still often used for it.

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

Diphenhydramine (diphenhydramine)

One of the first antihistamines. It has pronounced antihistamine activity, in addition, it has a local anesthetic effect, and also relaxes the smooth muscles of 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.

It is quickly absorbed when taken orally and penetrates the blood-brain barrier. Its half-life is about 7 hours. It undergoes biotransformation in the liver and is excreted by the kidneys.

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

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

1-5 ml of 1% solution are administered intramuscularly, 0.02-0.05 g of the drug in 100 ml of 0.9% sodium chloride solution is administered intravenously.

Can be used in the form of 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 reducing the dose or completely stopping the drug.

Contraindications are pregnancy, lactation, prostate hypertrophy, and angle-closure glaucoma.

Chloropyramine (suprastin)

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

It is quickly and completely absorbed when taken orally, the maximum concentration in the blood is observed 2 hours after administration. Penetrates the blood-brain barrier. Biotransformed in the liver, excreted by the kidneys and feces.

Prescribed for all kinds of allergic reactions.

It is used orally, intravenously and intramuscularly.

Orally, take 1 tablet (0.025 g) 2-3 times a day, with meals. The daily dose can 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 speed, impaired coordination of movements, nausea, and dry mouth are possible.

Strengthens the effect of sleeping pills and sedatives, as well as narcotic analgesics and alcohol.

Contraindications are similar to those of diphenhydramine.

Clemastine (tavegil)

In 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 moderate.

Take 1 tablet (0.001 g) orally 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.

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

Side effects are rare when taking this drug. Possible headache, drowsiness, nausea and vomiting, constipation.

Prescribed with caution to persons whose profession requires intense mental and physical activity.

Contraindications are standard.

Mebhydrolin (diazolin)

In addition to the 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 and excreted in the urine.

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, the daily dose is 0.6 g.

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

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

2nd generation antihistamines

Second generation antihistamines are characterized by high efficiency, rapid onset of action and a minimum of side effects, however, some of their representatives can cause life-threatening arrhythmias.

The goal of developing drugs in this group was to minimize sedation and other side effects while maintaining or even stronger antiallergic activity. And it was a success! Antihistamines 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 protein, which ensures longer circulation in the body; in addition, it accumulates in organs and tissues, and is also slowly excreted);
• additional mechanisms of antiallergic effects (suppress the accumulation of eosinophils in the respiratory tract associated with the entry of the allergen into the body, and also stabilize the membranes of mast cells), causing a wider range of indications for their use (,);
• with long-term use, the effectiveness of these drugs does not decrease, that is, there is no tachyphylaxis effect - 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 the blocking of potassium channels of the heart muscle by an antiallergic drug, 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 combining their use with antidepressants (paroxetine, fluoxetine), antifungals (intraconazole 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 2nd generation antihistamines is tablets, but parenteral ones are not available. Some drugs (such as levocabastine, azelastine) are available in the form of creams and ointments and are intended for topical administration.

Let's take a closer look at the main drugs in this group.

Acrivastine (Semprex)

It is well absorbed when taken orally and begins to act within 20-30 minutes after administration. The half-life is 2-5.5 hours, it penetrates the blood-brain barrier in small quantities and is excreted unchanged in the urine.

It blocks H1-histamine receptors and has a slight sedative and anticholinergic effect.

It is used for all kinds of allergic diseases.

In some cases, while taking it, drowsiness and a decrease in reaction speed are possible.

The drug is contraindicated during pregnancy, lactation, severe, severe coronary heart disease, and children under 12 years of age.

Dimetindene (fenistil)

In addition to antihistamine, it has weak anticholinergic, antibradykinin and sedative effects.

It is quickly and completely absorbed when taken orally, the 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 administration, the half-life is 6 hours for the regular form and 11 hours for the retard form. It penetrates the blood-brain barrier and is excreted in bile and urine in the form of metabolic products.

The drug is used orally and topically.

Adults take 1 capsule of retard orally 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.

Strengthens the effects of alcohol, sleeping pills and tranquilizers on the central nervous system.

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 is 70%). The maximum concentration of the active substance in the blood is observed after 60 minutes. Does not penetrate the blood-brain barrier. Biotransformed in the liver to form fexofenadine, excreted in feces and urine.

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

The indications are the same as for other drugs in this group.

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

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

Contraindications include pregnancy and breastfeeding.

Azelastine (allergodil)

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

It is quickly absorbed in the digestive tract and from the mucous membranes, the half-life is as much as 20 hours. Excreted in the form of metabolites in the urine.

Used, as a rule, for allergic rhinitis and.

When taking the drug, side effects are possible such as dryness and irritation of the nasal mucosa, bleeding from it and taste disorders when administered intranasally; 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 continues throughout the day.

There is no pronounced sedative effect.

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

Indications include any allergic diseases.

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

Contraindications include hypersensitivity to loratadine and lactation.

Prescribed with caution to pregnant women.

Bamipin (Soventol)

H1-histamine receptor blocker for topical use. Prescribed for allergic skin lesions (urticaria), contact allergies, as well as frostbite and burns.

The gel is applied in a thin layer to the affected areas of the skin. After half an hour, the drug can be reapplied.

Cetirizine (Cetrin)

Metabolite of hydroxyzine.

It has the ability to easily penetrate the skin and quickly accumulate in it - this determines the 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 administration. The half-life is 7-10 hours, but if renal function is impaired, it extends to 20 hours.

The range 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. These are drowsiness, dizziness and headache, dry mouth, nausea.

3rd generation antihistamines

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

These drugs are active metabolites (metabolic products) of previous generation drugs. They are devoid of cardiotoxic (arrhythmogenic) effect, but retain 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.

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 in feces.

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

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

Desloratadine (erius, eden)

It is an active metabolite of loratadine.

Has anti-allergic, anti-edematous and antipruritic effects. When taken in therapeutic doses, it has virtually no sedative effect.

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

In 2% of cases, while taking the drug, headaches, increased fatigue and dry mouth may occur.

In case of renal failure, prescribe with caution.

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

Levocetirizine (aleron, L-cet)

Cetirizine derivative.

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 a decongestant, anti-inflammatory, antipruritic effect. Practically does not interact with serotonin and cholinergic receptors, does not have a sedative effect.

When taken orally, it is quickly 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 primarily by the kidneys. Excreted in breast milk.

Contraindicated in cases of hypersensitivity to levocetirizine, severe renal failure, 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 for allergic diseases in pregnant women is limited, since many drugs are dangerous to 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 antiallergic 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 – experiments on animals did not reveal any negative effects on the fetus; no special studies were conducted on humans;

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

D – the negative effect of this drug on the human fetus has been proven, but its use is justified in certain situations that threaten the life of the mother, when safer drugs were ineffective;

X – the drug is certainly dangerous for the fetus, and its harm exceeds any theoretically possible benefit for 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 are included in category A. Category B includes 1st generation drugs - tavegil, diphenhydramine, peritol; 2nd generation – loratadine, cetirizine. Category C includes Allergodil, Pipolfen.

The drug of choice for the treatment of allergic diseases during pregnancy is cetirizine. 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 are therefore strictly contraindicated for use by pregnant women.

Regarding the lactation period, we can say the following... Again, uncontrolled use of these drugs by a nursing mother is unacceptable, since no human studies have been conducted on the extent of their penetration into breast milk. If these medications are needed, the young mother is allowed to take the one that is approved for her child to take (depending on age).

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

Which doctor should I contact?

If acute allergy symptoms appear, you can contact a therapist or pediatrician, and then an allergist. If necessary, a consultation with an ophthalmologist, dermatologist, ENT doctor, or pulmonologist is scheduled.

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

Antihistamines 4th generation, list of these drugs in tablets, drops

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

These medications are prescribed to adults and children to treat hay fever, 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 and suspension. An hour after taking this medication, patients begin to experience symptoms of allergic reactions. Fexofenadine is not prescribed to children under six years of age, patients with renal or hepatic pathology, pregnant or 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 over two days. It passes into breast milk, so it should not be consumed during breastfeeding. Levocetirizine is taken for the effective treatment of various forms of allergic rhinitis, seasonal allergies, urticaria, and allergic dermatosis. You should not drink alcoholic beverages while you are taking this medicine. If patients have impaired kidney function, the daily dosage of the drug is determined after testing.
3. Cetirizine. This medicine is sold in the form of drops, syrup, and tablets. It copes well with any manifestations of allergies - skin rashes, severe itching. It is most often prescribed for the treatment of itchy dermatosis and urticaria. The dosage is selected by the doctor depending on age and indications. During pregnancy, Cetirizine is prescribed only in rare cases.
4. Desloratadine. It can be purchased in the form of tablets and drops for oral administration. The substances included in the composition are quickly absorbed and 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 effectiveness for 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 inflammatory processes on the skin and penetrate deeply into it.

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

1. Galcinonide. This medicine works great for eczema that appears due to a nervous or allergic reaction. Acute inflammatory processes in areas of the skin are in most cases accompanied by swelling and excessive itching. The ointment has a gentle effect on inflamed skin and quickly relieves all allergy symptoms.
2. Hydrocortisone ointment. This is a fairly effective antiallergic agent that relieves itching, swelling, irritation and other skin rashes. Prescribed to patients who have hypersensitivity to individual components of the drug.
3. Deperzolon is available as an ointment for external use. It helps relieve allergic reactions, constricts blood vessels, and relieves excessive itching. In most cases, this ointment is prescribed for the treatment of dermatitis, dermatosis, allergies to insect bites, and various skin reactions.
4. Beloderm. This is an effective and efficient ointment for external use. Within an hour after use, it relieves itching, constricts blood vessels, and relieves inflammation.
5. Sinaflan is an effective antiallergic drug that is intended to relieve inflammatory processes. It is prescribed to patients diagnosed with atopic dermatitis, lichen, allergic skin reactions and swelling.

Treatment with sprays is the most effective way to combat allergic rhinitis.

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

Differences from previous generations

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

They have a minimal 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 effect.

When histamine goes from a bound state to a free one, a viral effect is created in the body. Therefore, many patients confuse allergies with the flu or a common runny nose.

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

• spasm of the soft tissues of the intestines and bronchi occurs;
• increased levels of adrenaline, so people’s blood pressure increases and their heart rate increases;
• the production of digestive enzymes, mucus in the bronchi and nasal cavity increases;
• large blood vessels narrow, so the nasal mucosa increases significantly, redness on the skin, small rashes appear, and blood pressure drops;
• anaphylactic shock develops with convulsions, vomiting, and loss of consciousness.

Fourth generation antihistamines can be used while driving a vehicle or working on machines where a quick reaction is required. In most cases, they do not react with other medications, including antibiotics.

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

Composition, therapeutic effect of new products

The presented drugs block H1 and H2 histamine receptors. Thanks to this effect in the human body, the reaction to the presence of the mediator histamine is reduced, and the allergic reaction is relieved.

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

They can be taken for a long time and do not cause drowsiness or worsening of the condition.

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

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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, it is important to consult with your doctor and 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 considered to be 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 medical 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 recorded.


The following undesirable effects may occur while taking it:

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

Drugs that do not cause adverse reactions

List of 4th generation antihistamines that do not cause coughing or other side effects:

• fexofenadine;
• desloratadine;
• Levocetirizine.

There are several benefits of using these medications:

1. Maximum high level effects on the patient’s body, the onset of a therapeutic effect. After consumption, a person feels relief after 20-30 minutes.
2. The effect lasts for two days. Therefore, patients do not need to take medications frequently.
3. There is no need to harm your health and take topical corticosteroids.
4. Lack of tachyphylaxis effect.
5. Long-term use does not have a negative effect on the functioning of the central nervous system and does not cause disturbances in the myocardium.
6. These medications can be used as allergy prevention.

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

Features of use in children and the elderly

4th generation antihistamines are safe and have minimal side effects after use. They are manufactured using innovative developments from the best pharmaceutical companies. Such drugs act on H1 receptors, thereby gently and quite effectively removing the body’s high susceptibility to histamine.

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

Newborns 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, and drug-induced dermatitis should use the new drug Tavegil.

It effectively relieves puffiness, reduces itching, and restores the natural shade of the skin.

The safest and most harmless drugs:

• xysal;
• desloratidine;
• levocetirizine;
• fexofenadine.

These drugs may be prescribed for older people. New generation medications are less harmful to the body with long-term use and effectively eliminate any clinical manifestations.

Antihistamines of the 4th generation do not cause addiction to the body, so there is no need to increase the dosage if the effectiveness decreases. During treatment, older people need to drink more fluid so that the active substance is well absorbed into 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 rapid action and the absence of side effects. But there are those who are afraid to experience the effects of these new medications.

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

Antihistamines 4th generation

5 (100%) 6 votes

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In the window of any pharmacy you can find a variety of allergy pills, the prices of which vary markedly, which misleads an inexperienced buyer who has not previously dealt with allergies.

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

Anti-allergy tablets - list

During an allergic reaction, histamine is released into the blood, a substance that can narrow the airways and dilate blood vessels, thereby causing tissue swelling or swelling, as well as a decrease in blood pressure.

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

Which allergy pills to choose?

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

To treat and relieve the symptoms of skin manifestations and allergic rhinoconjunctivitis, most often, the latest generation of allergy tablets are used, which can be purchased at the pharmacy without a doctor's prescription.

Let's take a closer look at the most effective and inexpensive allergy pills.

Antihistamine allergy tablets fall into two categories:

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

The first generation includes older antiallergy drugs that relieve symptoms but cause drowsiness, which makes them difficult to use when driving or doing work that requires high concentration. In addition, the concentration of active substances is quickly eliminated from the blood, which requires taking the drug two or three times a day.

The new generation of anti-allergy tablets do not cause drowsiness, which is why they are used even in 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 can be taken even by children from 6 months.

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

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, and Quincke's edema. Contraindications: age under 6 years.

• LEVOCETIRIZINE TEVA No. 14 from 360 rub.
• KYZAL No. 7 from 316 rub.
• GLENCET No. 7 from 290 rub.
• SUPRASTINEX No. 7 from 261 rub.
• ELTSETT No. 7 from 112 rub.

LORATADINE (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. Effective for insect allergies (to poison and insect bites) and pseudo-allergies. Contraindications – age under 2 years.

• CLARITIN No. 10 from 206 rub.
• LOMILAN No. 7 from 112 rub.
• CLARICENS No. 10 from 68 rub.
• CLARIDOL No. 7 from 62 rub.
• LORAGEXAL No. 10 from 50 rub.
• LORATADINE VERTE No. 10 from 26 rub.

DESLORATADINE (5 mg)

Used in the treatment of allergic rhinitis and idiopathic urticaria. Contraindications – age under 12 years.

• ELIZEUS No. 30 from 350 rub.
• LORDESTIN No. 10 from 270 rub.
• ERIUS No. 7 from 235 rub.
• DEZAL No. 10 from 227 rub.
• BLOGGER-3 No. 10 from 164 rub.
• DESLORATADINE No. 10 from 120 rub.

FEXOPHENADINE (120 mg)

Taken to eliminate the symptoms of rhinoconjunctivitis, various allergic rashes and relieve angioedema. Contraindications – age under 6 years.

• ALLEGRA No. 10 from 697 rub.
• FEXADIN No. 10 from 247 rub.
• FEXOFAST No. 10 from 215 rub.

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 No. 10 from 58 rub.

DIPHENGYDRAMINE (50 mg)

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

• DIMEDROL No. 20 from 10 rub.

EBASTINE (10 mg)

Allergic rhinitis and urticaria of various etiologies. Contraindicated for children under 6 years of age.

• KESTIN No. 5 from 216 rub.

KETOTIFEN (1 mg)

Relieves and prevents symptoms of rhinoconjunctivitis associated with seasonal allergies, effective for atopic dermatitis and urticaria. Contraindications – age under 3 years.

• KETOTIFEN No. 30 from 57 rub.

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 rub.

CHLOROPYRAMINE (25 mg)

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

• SUPRASTIN No. 20 from 123 rub.

CLEMASTINE (1 mg)

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

• TAVEGIL No. 10 from 158 rub.

Corticosteroid drugs

Corticosteroid medications (hormonal allergy pills), made from synthetic hormones, are effective against serious allergic reactions. Allows you to achieve effective relief of inflammatory processes and eliminate swelling.

Corticosteroids in tablet form prevent and treat nasal congestion, seasonal and year-round runny nose (rhinitis), sneezing, and itching. They also help reduce inflammation and swelling in other types of allergies: drug, food, cat, etc.

Because they are potent, oral corticosteroids are usually used short-term. Long-term use of these drugs may increase the risk of side effects, such as high blood pressure, joint pain, etc. Therefore, you should not prescribe and drink these drugs yourself; you should seek advice from a specialist.

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

Indications: Quincke's edema, contact and atopic dermatitis, rhinoconjunctivitis, bronchial asthma.

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

Indications: allergic rhinoconjunctivitis, dermatitis of various origins, Quincke's edema.

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

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

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

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

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

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

• PREDNISOONE (Prednisolone) 5 mg No. 100 from 98 rub.

For 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 tablets

Decongestants are used to constrict blood vessels and relieve nasal congestion due to allergic rhinitis and 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 also called generics (cheap analogues). The low price of the drug is due to the fact that no studies have been conducted to prove their effectiveness, unlike patented products. Therefore, in this case, it is difficult to say whether cheap drugs will have the desired effect in treating 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.