Antihistamines 2nd generation for children list. Antihistamine - what does it mean? List of new generation allergy drugs

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

How does an allergy occur?

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

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

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

Features of antihistamines for children, and when to take them

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

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

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

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


First generation antihistamines

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

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

Long-term first-generation antihistamines should be replaced every 2 weeks, as they are addictive, as a result of which their effectiveness is reduced. The price of such drugs is usually very low.


The first generation of antihistamines is prescribed for children with any type of allergy, including diathesis, urticaria, rhinitis

Second generation antihistamines

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

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

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


Third generation antihistamines

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

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

Fourth generation antihistamines

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

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

The disadvantage of the newer drugs is that they are all produced in adult dosage, so it is likely that the child will have side effects.


What antihistamines are suitable for children of different ages?

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

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

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

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

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

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

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

After 6 years, children are often prescribed new drugs:

  • clemastine;
  • Zyrtec;
  • Terfenadine.

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

Every year the number of allergic reactions, including dermatitis, is steadily growing, which is associated with the deterioration of the environmental situation and the "unloading" of the immune system in the conditions of civilization.

Allergy is a hypersensitivity reaction of the body to a foreign chemical substance - an allergen. It can be food, pet hair, dust, drugs, bacteria, viruses, vaccines, and more.

In response to the entry of an allergen in the organs and cells of the immune system, an intensive production of a special substance, histamine, begins. This substance binds to H1 - histamine receptors and causes signs of allergy.

If you remove the provoking factor, the manifestations of allergies will pass over time, but the cells that store the memory of this substance will remain in the blood. At the next meeting with him, an allergic reaction may manifest itself with greater force.

How do antihistamines work?

These drugs bind to H1-histamine receptors and block them. Thus, histamine cannot bind to the receptors. Allergy phenomena subside: the rash turns pale, swelling and itching of the skin decrease, nasal breathing is facilitated and the phenomena of conjunctivitis decrease.

The first antihistamine drugs appeared in the 1930s. As science and medicine developed, the second and then the third generation of antihistamines were created. All three generations are used in medicine. The list of antihistamines is constantly updated. Analogues are produced, new forms of release appear.

Consider the most popular drugs, starting with the latest generation.

In fairness, the division into the first, second and third generations makes sense, because. substances differ in properties and side effects.

The division into the third and fourth generation is very conditional, and often carries nothing but a beautiful marketing slogan.

Sometimes these drugs are referred to both the third and fourth generations at the same time. We will not confuse you even more and call it all simpler:

Last generation - metabolites

The most modern medicines rstva. A distinctive feature of this generation is that the drugs are prodrugs. When ingested, they are metabolized - activated in the liver. Do drugs no sedative effect, also they do not affect the functioning of the heart.

Antihistamines of the new generation are successfully used to treat all types of allergies and allergic varieties of dermatitis in children, people suffering from cardiovascular diseases. Also, these funds are prescribed to people whose profession is associated with increased attention (drivers, surgeons, pilots).

Allegra (Telfast)

The active substance is fexofenadine. The drug not only blocks histamine receptors, but also reduces its production. It is used for chronic urticaria and seasonal allergies. The anti-allergic effect lasts up to 24 hours after the end of the course of treatment. Not addictive.

Available only in the form of tablets. Previously, the tablets were called Telfast, now - Allegra. They are contraindicated in children under 12 years of age, pregnant and lactating women.

cetirizine

The effect after administration develops after 20 minutes and persists for 3 days after discontinuation of the drug. It is used to treat and prevent allergies. Cetirizine does not cause drowsiness and decreased attention. It may be used for a long time. The drug is available in the form of drops (trade name "Zirtek", "Zodak"), syrup ("Cetrin", "Zodak") and tablets.

In children's practice, it is used from 6 months in the form of drops, from 1 year in the form of syrup. From the age of 6, tablets are allowed. The dosage is determined by the doctor individually.

Pregnant women Cetirizine is strictly contraindicated. For the period of use, it is desirable to stop breastfeeding.

The medicine is prescribed for the treatment of year-round and seasonal allergies, urticaria and pruritus. The action occurs 40 minutes after administration. Available in the form of drops and tablets.

In children's practice, drops are used from the age of 2 and tablets from the age of 6. The dosage is determined by the doctor in accordance with the weight and age of the child.

The drug is contraindicated for pregnant women. Acceptance during breastfeeding is allowed.

Desloratadine

Synonyms: Lordestin, Desal, Erius.

The drug has an antihistamine and anti-inflammatory effect. Well eliminates the signs of seasonal allergies and chronic urticaria. When taken in therapeutic doses, dry mouth and headache may occur. Available in the form of syrup, tablets.

Children are prescribed from 2 years in the form of syrup. Tablets are allowed for children over 6 years of age.

Pregnant and lactating Desloratadine is contraindicated. Perhaps its use in life-threatening conditions: Quincke's edema, suffocation (bronchospasm).

Antihistamines of the 3rd generation effectively eliminate the manifestations of allergies. In therapeutic doses, they do not cause drowsiness and reduce attention. However, if the recommended dosages are exceeded, dizziness, headache, and an increase in heart rate may occur.

If you have used any of their preparations, do not forget to leave a review in the comments.

Second generation - non-sedating

The drugs of this group have a pronounced antihistamine effect, the duration of which is up to 24 hours. This allows you to take them 1 time per day. Medications do not cause drowsiness or impaired attention, which is why they are called non-sedating.

Non-sedative drugs are actively used to treat:

  • urticaria;
  • hay fever;
  • eczema;

These remedies are also used to relieve severe itching in chickenpox. There is no addiction to antiallergic drugs of the 2nd generation. They are quickly absorbed from the digestive tract. They can be taken at any time, even with meals.

Loratadine

The active substance is loratadine. The drug selectively affects H1 histamine receptors, which allows you to quickly eliminate allergies and reduce the number of side effects:

  • anxiety, sleep disturbances, depression;
  • frequent urination;
  • constipation;
  • asthma attacks are possible;
  • increase in body weight.

Produced in the form of tablets and syrup (trade names "Claritin", "Lomilan"). Syrup (suspension) is convenient to dose and give to young children. The action develops 1 hour after administration.

In children, Loratadine is used from the age of 2 years in the form of a suspension. The dosage is selected by the doctor depending on the body weight and age of the child.

Loratadine is prohibited for use in the first 12 weeks of pregnancy. In extreme cases, it is prescribed under the strict supervision of a physician.

Synonym: Ebastine

This agent selectively blocks H1 histamine receptors. Does not cause drowsiness. The action occurs 1 hour after administration. The antihistamine effect persists for 48 hours.

In children, it is used from 12 years of age. Kestin has a toxic effect on the liver, causes rhythm disturbances, and reduces the heart rate. Pregnant women are contraindicated.

Synonym: Rupatadin

The medicine is used in the treatment of hives. After oral administration, it is rapidly absorbed. Simultaneous food intake enhances the effect of Rupafin. It is not used in children under 12 and pregnant women. Use during breastfeeding is possible only under strict medical supervision.

Antihistamines of the 2nd generation meet all modern requirements for medicines: high efficiency, safety, long-term effect, ease of use.

However, it should be remembered that exceeding the therapeutic dosage leads to the opposite effect: drowsiness appears and side effects increase.

First generation - sedatives

Sedative drugs are called because they cause a sedative, hypnotic, mind-depressing effect. Each representative of this group has a sedative effect expressed to varying degrees.

In addition, the first generation of drugs has a short-term anti-allergic effect - from 4 to 8 hours. They may become addictive.

However, the drugs are time-tested and often inexpensive. This explains their mass.

First-generation antihistamines are prescribed to treat allergic reactions, relieve skin itching in infectious rashes, to reduce the risk of post-vaccination complications.

Along with a good anti-allergic effect, they cause a number of side effects. To reduce their risk, treatment is prescribed for 7-10 days. Side effects:

  • dry mucous membranes, thirst;
  • increased heart rate;
  • drop in blood pressure;
  • nausea, vomiting, stomach discomfort;
  • increased appetite.

First generation drugs are not prescribed to people whose activities are associated with increased attention: pilots, drivers, because. they can weaken attention and muscle tone.

Suprastin

Synonyms: Chloropyramine

It is available both in the form of tablets and in ampoules. The active ingredient is chloropyramine. One of the most commonly used antiallergic drugs. Suprastin has a pronounced antihistamine effect. It is prescribed for the treatment of seasonal and chronic rhinitis, urticaria, atopic dermatitis, eczema, Quincke's edema.

Suprastin relieves itching well, including after an insect bite. It is used in the complex therapy of rashes, accompanied by skin itching and scratching. Available in the form of tablets, solutions for injection.

Suprastin is approved for the treatment of infants, starting from one month. The dosage is selected individually depending on the age and body weight of the child. These funds are used in the complex therapy of chicken pox: to relieve skin itching and as a sedative. Suprastin is also included in the lytic mixture ("troychatka"), which is prescribed at a high and not knocked down temperature.

Suprastin is contraindicated for use during pregnancy and breastfeeding.

Tavegil

Synonym: clemastine

It is used in the same cases as suprastin. The drug has a strong antihistamine effect lasting up to 12 hours. Tavegil does not lower blood pressure, the hypnotic effect is less pronounced than that of suprastin. The medicine is available in several forms: tablets and injection.

Application in children. Tavegil has been used since 1 year. The syrup is prescribed for children from 1 year old, tablets can be used from 6 years old. The dosage is determined individually depending on the age and body weight of the child. The dose is selected by the doctor.

Tavegil is prohibited for use during pregnancy.

Synonym: Quifenadine

Fenkarol blocks H-1 histamine receptors and starts an enzyme that utilizes histamine, so the effect of the drug is more stable and long lasting. Fenkarol practically does not cause a sedative and hypnotic effect. In addition, there are indications that this drug has an antiarrhythmic effect. Phencarol is available in the form of tablets and powder for suspension.

Quifenadine (Fenkarol) is used to treat all types of allergic reactions, especially seasonal allergies. This tool is included in the complex treatment of parkinsonism. In surgery, it is used as part of medical preparation for anesthesia (premedication). Fenkarol is used to prevent host-foreign reactions (when the body rejects foreign cells) during transfusions of blood components.

In pediatric practice, the drug is prescribed from 1 year. For children, the suspension is preferable, it has an orange flavor. If the child refuses to take the syrup, a tablet form may be prescribed. The dosage is determined by the doctor, taking into account the weight and age of the child.

Fencarol is contraindicated in the 1st trimester of pregnancy. In the 2nd and 3rd trimester, its use is possible under medical supervision.

Fenistil

Synonym: Dimetinden

The drug is used to treat all types of allergies, skin itching with chickenpox, rubella, prevention of allergic reactions. Fenistil causes drowsiness only at the beginning of treatment. After a few days, the sedative effect disappears. The drug has a number of other side effects: dizziness, muscle spasms, dryness of the oral mucosa.

Fenistil is available in the form of tablets, drops for children, gel and emulsion. Gel and emulsion are applied externally after insect bites, contact dermatitis, sunburn. There is also a cream, but this is a completely different drug based on a different substance and it is used for "cold on the lips".

In children's practice, Fenistil in the form of drops is used from 1 meat. Up to 12 years of age, drops are prescribed, over 12 years of age, capsules are allowed. The gel is used in children from birth. The dosage of drops and capsules is selected by the doctor.

Pregnant women are allowed to use the drug in the form of a gel and drops from 12 weeks of pregnancy. From the second trimester, Fenistil is prescribed only for life-threatening conditions: Quincke's edema and acute food allergies.

Diazolin

Synonym: Mebhydrolin

The drug has low antihistamine activity. Diazolin has a fairly large number of side effects. When it is taken, dizziness, stomach pain, nausea and vomiting, increased heart rate, and frequent urination occur. But at the same time, Diazolin does not cause drowsiness. It is approved for long-term treatment in drivers and pilots.

Available in the form of tablets, powder for suspension and dragee. The duration of antiallergic action is up to 8 hours. It is taken 1-3 times a day.

In children, the drug is prescribed from 2 years of age. Up to 5 years, Diazolin in the form of a suspension is preferable; over 5 years, tablets are allowed. The dosage is selected by the doctor individually.

Diazolin is contraindicated in the first trimester of pregnancy.

Despite all the shortcomings, first-generation drugs are widely used in medical practice. They are well studied, approved for the treatment of young children. Medicines are available in different forms: injection solutions, suspensions, tablets, which makes it convenient to use them and select an individual dosage.

Antihistamines work well for allergic dermatitis, and (in most cases) atopic dermatitis too.

It should be remembered that drugs should be taken in a strictly defined dose, according to the instructions. Otherwise, undesirable effects may occur, even (!) an increase in an allergic reaction.

The choice of medicine and its dose should be performed by a doctor. Antiallergic treatment, especially for children and pregnant women, should be carried out under strict medical supervision.

10 comments

    I have a severe allergy to ragweed (but the list of allergens is not limited to this): itchy eyes, runny nose, sneezing. I started taking levocitemeresin in addition to Avamys (nasal spray). But he does not help me well, because. A strong cough has already begun, especially at night. I didn't sleep at all for one night. Now I don't know what to drink :(

    • There are a lot of drugs, each one is better for something different. Try other drugs from the list, newer.

      Well, it is best to consult a doctor, perhaps you will be prescribed an injectable form.

    Hello! My daughter (16 years old) has frequent recurrences of allergic rhinitis. The last time the doctor prescribed a course of Desal (4 weeks) did not pass and 2 weeks later there was again nasal congestion, fever, and this time severe headaches. Thought it was low blood pressure. When they took the test, it turned out again-allergy. They started taking Desal again. Tell me, is it possible to use antihistamines so often, and what alternative and more effective treatment would you recommend?

    If any one drug from at least the second generation does not help, then you need to try another active ingredient. For example, loratadine does not help my child at all. Doctors automatically prescribe it. :(They used cetrin, drank almost the entire package - everything was fine, as long as the weather was damp and cold. As soon as the sun came out and all the alder-birch trees began to bloom, cetrin does not help. Where the promised effect for three days after the course of treatment is unclear.
    Passed 2 courses of ASIT - so far it has not helped, alas. And drugs for ASIT are very, very expensive.
    Friends say that acupuncture helps. But it is also very expensive. We need to study the issue.

To see new comments, press Ctrl+F5

All information is presented for educational purposes. Do not self-medicate, it is dangerous! An accurate diagnosis can only be made by a doctor.

Allergy is a companion of progress. The higher the level of hygiene, the more cases of allergies. The more pollution in the air, water and land, the more people suffer from this disease. Fortunately, science does not stand still, and pharmaceutical scientists create more and more new allergy medications. Most Effective of which are listed in this top 10.

Antihistamines are I, II and III generation:

  • I - effective tablets, powders, ointments, but with a large number of side effects. They quickly relieve symptoms, but are not intended for systemic treatment of allergies.
  • II - remedies for allergies of a wider spectrum. They act softer, but also have a number of side effects.
  • III - last generation allergy medicines. They act directed at the cellular level, without affecting the central nervous system. Suitable for long term treatment. Virtually devoid of side effects.

10. Donormil

Cost: 330 rubles.

Generation: I

Basically, Donormil is used as a sleeping pill, but sometimes it is also prescribed to allergy sufferers as part of complex therapy. Indeed, with an exacerbation of allergies, especially accompanied by severe skin itching, it is difficult to sleep well.

9. Suprastin

150 rub.

Generation: I

One of the oldest allergy remedies on the post-Soviet market. Even with prolonged use, it does not cause an overdose, it does not accumulate in the blood serum. Bonus: anti-emetic and anti-sickness effect.

Cons: short-term therapeutic effect. Like other antiallergic drugs of the first group of effectiveness, it has a sedative effect. It also causes side effects such as tachycardia, as well as dryness of the nasopharynx and oral cavity, which is unlikely to please those suffering from bronchial asthma.

8. Fenistil

370 rub.

Generation: II

Unlike previous medications, Fenistil comes in the form of an emulsion or gel and is applied to the skin. It is not intended to eliminate the causes of allergies, but relieves symptoms - it cools, softens, moisturizes and has a weak local anesthetic effect.

7. Loratadine

80 rub.

Generation: II

Domestic and, as a result, inexpensive drug (those who wish can buy the production of Hungary, a little more expensive). Unlike other drugs of the second group of efficiency, it is practically devoid of cardiotoxic action.

The second generation drugs have a number of advantages over the previous ones - for example, there is no sedative effect, mental activity remains at the same level. And, most importantly, the prolonged action of the drug. One tablet per day is enough for people with pollen allergy to feel quite tolerable even during the period of violent flowering of plants.

6. Claritin

200 rub.

Generation: II

The active substance of Claritin is loratadine. It acts quickly, within half an hour after ingestion, and lasts for a day, which has made Claritin one of the most popular and effective remedies for allergies. For children, the drug is available in the form of a syrup. And adult allergy sufferers will appreciate that Claritin does not enhance the effects of alcohol on the nervous system.

5. Tsetrin

240 rub.

Generation: III

In fifth place in the ranking of the best allergy remedies is Cetrin. It helps to cope with various symptoms with little or no side effects, and with mild bronchial asthma, it relieves spasms. The active substance is cetirizine, which has a high ability to penetrate the skin. This makes it especially effective for skin manifestations of allergies. In addition, cetirizine is an effective third-generation agent, which means that it has neither cardiotoxic nor sedative effects.

4. Zodak

200 rub.

Generation: III

Zodak is also made on the basis of cetirizine (like Cetrin), but is produced in the Czech Republic.

3. Zyrtec

320 rub.

Generation: III

Means based on cetirizine produced in Belgium. One of the best allergy pills, a highly effective drug that acts quickly, alleviates the course and prevents the development of an allergic attack.

2. Eden

120 rub.

Generation: III

The active substance of Eden is desloratadine, an antihistamine of the third group, a descendant of loratadine. Like all substances in this group, it practically does not cause drowsiness and does not affect the reaction rate. It helps with tissue swelling, lacrimation, itchy skin. An effective means of Ukrainian production.

1. Erius

The average cost of Erius: 500 rubles.

Generation: III

Erius is the most effective antihistamine of the third generation. The active substance of Erius is also desloratadine. The drug itself is produced by Bayer, USA, which is easy to guess when looking at the price. Acts quickly and almost immediately, effectively eliminates itching, rashes, runny nose and redness on the skin - one of the most effective allergy pills at the moment.

1. Dexamethasone

Dexamethasone price: from 50 rubles for drops to 150 for a set of ampoules.

Dexamethasone can be compared to heavy artillery among the most effective allergy remedies. It is used in emergency cases when it is necessary to stop a very strong allergic attack or severe inflammation. Along with anti-allergic, it has anti-inflammatory, immunosuppressive and anti-shock effects.

Remember that self-medication for allergies can lead to a deterioration in well-being. There are contraindications. Only an allergist can prescribe a medicine for allergies.

There are three (according to some authors - four) generations of antihistamines. The first includes drugs that, in addition to antiallergic, also have a sedative / hypnotic effect. The second includes drugs with a minimally pronounced sedative effect and a powerful antiallergic effect, but in some cases causing serious, life-threatening arrhythmias. Antihistamine drugs of the new - third - generation are metabolic products (metabolites) of second-generation drugs, and their effectiveness is 2-4 times higher than that of their predecessors. They have a number of unique positive properties and do not cause such side effects as drowsiness and negative effects on the heart. It is about the drugs of the third generation that will be discussed in this article.

New (third) generation antihistamines: mechanism of action and effects

Drugs in this group act exclusively on H1-histamine receptors, that is, they have a selective action. Their antiallergic effect is also provided by the following mechanisms of action. So, these drugs:

  • inhibit the synthesis of mediators of systemic allergic inflammation, including chemokines and cytokines;
  • reduce the number and disrupt the function of adhesion molecules;
  • inhibit chemotaxis (the process of release of leukocytes from the vascular bed into the damaged tissue);
  • inhibit the activation of allergy cells, eosinophils;
  • inhibit the formation of superoxide radical;
  • reduce the increased reactivity (hyperreactivity) of the bronchi.

All of the above mechanisms of action provide powerful anti-allergic and, to a certain extent, anti-inflammatory effects: they eliminate itching, reduce the permeability of the capillary wall, swelling and hyperemia of tissues. Do not cause drowsiness, do not have a toxic effect on the heart. They do not bind to cholinergic receptors, therefore, they do not cause such side effects as blurred vision and. They have a high security profile. It is thanks to these properties that new generation antihistamines can be recommended for long-term treatment of a number of patients.

Side effects

As a rule, these drugs are well tolerated by patients. However, occasionally, against the background of their use, the following undesirable effects may develop:

  • fatigue;
  • dry mouth (very rare);
  • hallucinations;
  • drowsiness, insomnia, agitation;
  • , heartbeat;
  • nausea, vomiting, discomfort in the epigastrium, in isolated cases -;
  • muscle pain;
  • allergic reactions: skin rash, with or without it, shortness of breath, Quincke's edema, anaphylactic reactions.

Indications and contraindications for the use of third-generation antihistamines


Foods can cause food allergies and cause illness.

Indications for the use of drugs in this group are:

  • allergic rhinitis (both year-round and seasonal);
  • (also, both seasonal and year-round);
  • chronic;
  • allergic;

New generation antihistamines are contraindicated only in case of individual hypersensitivity of the patient's body to them.

Representatives of new generation antihistamines

This group of medicines includes:

  • fexofenadine;
  • cetirizine;
  • Levocetirizine;
  • Desloratadine.

Let's consider each of them in more detail.

Fexofenadine (Altiva, Telfast, Tigofast, Fexofast, Fexofen-Sanovel)

Release form: film-coated tablets of 120 and 180 mg.

Pharmacologically active metabolite of the second generation drug, terfenadine.

After ingestion, it is rapidly absorbed in the digestive tract, reaching a maximum concentration in the blood after 1-3 hours. Almost does not bind to blood proteins, does not penetrate the blood-brain barrier. The half-life is 11-15 hours. It is excreted mainly with bile.

The antiallergic effect of the drug develops within 60 minutes after a single dose, within 6 hours the effect increases and persists throughout the day.

Adults and children over 12 years of age are recommended to take 120-180 mg (1 tablet) once a day, before meals. The tablet should be swallowed without chewing with 200 ml of water. The course of treatment is determined individually depending on the characteristics of the course of the disease. Even after regular use of fexofenadine for 28 days, there were no signs of intolerance.

For patients suffering from severe or, the drug should be used with caution.

During pregnancy should not be used, since clinical studies in this category of patients have not been conducted.

The drug passes into breast milk, so nursing mothers should not take it either.

Cetirizine (Allertec, Rolinoz, Tsetrin, Amertil, Zodak, Tsetrinal)


Avoid alcohol while taking antihistamines.

Release form: film-coated tablets, oral solution and drops, syrup.

Metabolite of hydroxyzine. The strongest antagonist of H1-histamine receptors.

The use of this drug in average therapeutic doses significantly improves the quality of life of patients suffering from seasonal and chronic allergic rhinitis.

After ingestion, the effect appears after 2 hours and lasts for a day or more.

In patients with impaired renal function, the dose of cetirizine should be adjusted depending on the magnitude of creatinine clearance: for mild renal failure, 10 mg of an antihistamine drug is prescribed 1 time per day, which is a full dose; moderate degree - 5 mg 1 time per day (half dose); if the creatinine clearance corresponds to a severe degree of renal insufficiency, it is recommended to take 5 mg of cetirizine every other day, and for patients on hemodialysis with end-stage renal failure, taking the drug is completely contraindicated.

Contraindications to the use of cetirizine are also individual hypersensitivity to it and congenital pathology of carbohydrate metabolism (glucose-galactose malabsorption syndrome and others).

Cetirizine, taken at normal doses, may cause temporary adverse reactions such as fatigue, drowsiness, central nervous system agitation, dizziness, and headache. In some cases, against the background of its reception, dry mouth, disturbance of eye accommodation, difficulty urinating and increased activity of liver enzymes are noted. As a rule, after discontinuation of the drug, these symptoms disappear on their own.

During the period of treatment, you should stop taking.

Persons suffering from convulsive syndrome and epilepsy should take the drug with extreme caution due to the increased risk of occurrence.

During pregnancy, use if absolutely necessary. Do not take during lactation as it is excreted in breast milk.

Levocetirizine (L-cet, Alerzin, Aleron, Zilola, Cetrilev, Aleron neo, Glentset, Xizal)

Presentation: film-coated tablets, oral drops, syrup (dosage form for children).

A derivative of cetirizine. The affinity for H1-histamine receptors of this drug is several times higher than that of its predecessor.
When taken orally, it is rapidly and completely absorbed, and the degree of absorption does not depend on food intake, however, its rate decreases in the presence of food in the stomach. In some patients, the effect of the drug begins within 12-15 minutes after administration, but in most patients it develops later, after 30-60 minutes. The maximum concentration in the blood is determined after 50 minutes and persists for 48 hours. The half-life is from 6 to 10 hours. Excreted by the kidneys.

In persons suffering from severe renal insufficiency, the half-life of the drug is prolonged.

It is allocated with breast milk.

Adults and children over 6 years of age are recommended to use the tablet form of the drug. 1 tablet (5 mg) is taken orally without chewing, drinking plenty of water. Multiplicity of reception - 1 time per day. If levocetirizine is prescribed in the form of drops, its dose for adult patients and children 6 years of age and older is 20 drops 1 time per day. Children under 6 years of age are prescribed in the form of syrup or drops, the dose of which depends on the age of the child.

Persons with severe renal insufficiency should calculate the creatinine clearance before prescribing the drug. If this value indicates impaired renal function of the first degree, then the recommended dose of the antihistamine drug is 5 mg per day, that is, the full dose. In case of moderate impairment of kidney function, it is 5 mg 1 time in 48 hours, that is, every other day. In severe renal impairment, the drug should be taken at 5 mg 1 time in 3 days.

The duration of the course of treatment varies widely and is selected individually depending on the disease and the severity of its course. So, with hay fever, the course of treatment, as a rule, is 3-6 months, with chronic allergic diseases - up to 1 year, in case of potential contact with an allergen - 1 week.

Contraindications to the use of levocetirizine, in addition to individual intolerance and severe chronic renal failure, are congenital (galactose intolerance, lactase deficiency, and others), as well as pregnancy and lactation.

Side effects are similar to those of other drugs in this group.

Taking levocetirizine, it is strictly contraindicated to drink alcoholic beverages.


Desloratadine (Alersis, Lordes, Trexil neo, Erius, Eden, Alergomax, Allergostop, DS-Lor, Fribris, Eridez)

Presentation: 5 mg film-coated tablets and oral solution containing 0.5 mg of active ingredient per ml (dosage form for children). Some drugs, in particular Allergomax, are also available in the form of a nasal spray.

Catad_tema Allergic diseases

Antihistamines: myths and reality

"EFFICIENT PHARMACOTHERAPY"; No. 5; 2014; pp. 50-56.

T.G. Fedoskova
SSC Institute of Immunology, FMBA of Russia, Moscow

The main drugs that affect the symptoms of inflammation and control the course of diseases of allergic and non-allergic origins include antihistamines.
The article analyzes the debatable points regarding the experience of using modern antihistamines, as well as some of their main characteristics. This will allow a differentiated approach to the choice of the optimal drug in the complex therapy of various diseases.
Keywords: antihistamines, allergic diseases, cetirizine, Cetrin

ANTIHISTAMINES: MYTHS AND REALITY

T.G. Fedoskova
State Science Center Institute of Immunology, Federal Medical and Biological Agency, Moscow

Antihistamines belong to main drugs influencing symptoms of inflammation and controlling course of both of allergic and non-allergic diseases. In this paper debatable issues regarding experience of using current antihistamines as well as some of their characteristics are analyzed. It may let to make a differential choice to administer appropriate drugs for a combination therapy of different diseases.
key words: antihistamines, allergic diseases, cetirizine, Cetrine

Type 1 antihistamines (H1-AHP), or type 1 histamine receptor antagonists, have been widely and successfully used in clinical practice for more than 70 years. They are used as part of symptomatic and basic therapy of allergic and pseudo-allergic reactions, complex treatment of acute and chronic infectious diseases of various origins, as premedication during invasive and radiopaque studies, surgical interventions, for the prevention of side effects of vaccination, etc. In other words, H 1 -AHP is advisable to use in conditions caused by the release of active mediators of inflammation of a specific and non-specific nature, the main of which is histamine.

Histamine has a wide spectrum of biological activity, realized through the activation of cell surface specific receptors. The main depot of histamine in the tissues are mast cells, in the blood - basophils. It is also present in platelets, gastric mucosa, endothelial cells, and brain neurons. Histamine has a pronounced hypotensive effect and is an important biochemical mediator in all clinical symptoms of inflammation of various origins. That is why antagonists of this mediator remain the most popular pharmacological agents.

In 1966, the heterogeneity of histamine receptors was proven. Currently, 4 types of histamine receptors are known - H 1 , H 2 , H 3 , H 4 belonging to the superfamily of receptors associated with G-proteins (G-protein-coupled receptors -GPCRs). Stimulation of H 1 receptors leads to the release of histamine and the realization of inflammation symptoms, mainly of allergic origin. Activation of H 2 receptors increases the secretion of gastric juice and its acidity. H3 receptors are predominantly present in the organs of the central nervous system (CNS). They perform the function of histamine-sensitive presynaptic receptors in the brain, regulate the synthesis of histamine from presynaptic nerve endings. Recently, a new class of histamine receptors, expressed predominantly on monocytes and granulocytes, H 4 , has been identified. These receptors are present in the bone marrow, thymus, spleen, lungs, liver, and intestines. The mechanism of action of H 1 -AHP is based on reversible competitive inhibition of histamine H 1 receptors: they prevent or minimize inflammatory reactions, preventing the development of histamine-induced effects, and their effectiveness is due to the ability to competitively inhibit the effect of histamine on the loci of specific H 1 receptor zones in effector tissue structures.

Currently, over 150 types of antihistamines are registered in Russia. These are not only H 1 -AGP, but also drugs that increase the ability of blood serum to bind histamine, as well as drugs that inhibit the release of histamine from mast cells. Due to the variety of antihistamines, it is quite difficult to make a choice between them for their most effective and rational use in specific clinical cases. In this regard, there are debatable points, and often myths are born about the use of H 1 -AHP, which are widely used in clinical practice. In the domestic literature, there are many works on this topic, however, there is no consensus on the clinical use of these drugs (PM).

The myth of three generations of antihistamines
Many are mistaken in thinking that there are three generations of antihistamines. Some pharmaceutical companies present new drugs that have appeared on the pharmaceutical market as third-generation AGPs. Attempts were made to classify metabolites and stereoisomers of modern AGPs to the third generation. Currently, these drugs are considered to be second-generation antihistamines, since there is no significant difference between them and previous second-generation drugs. According to the Consensus on Antihistamines, it was decided to reserve the name "third generation" to denote future synthesized antihistamines, which are likely to differ from known compounds in a number of key characteristics.

There are many differences between first and second generation AGPs. This is primarily the presence or absence of a sedative effect. A sedative effect when taking first-generation antihistamines is subjectively noted by 40-80% of patients. Its absence in individual patients does not exclude the objective negative effect of these drugs on cognitive functions, which patients may not complain about (the ability to drive a car, learn, etc.). Dysfunction of the central nervous system is observed even with the use of minimal doses of these drugs. The effect of first-generation antihistamines on the central nervous system is the same as when using alcohol and sedatives (benzodiazepines, etc.).

Second-generation drugs practically do not penetrate the blood-brain barrier, so they do not reduce the mental and physical activity of patients. In addition, first and second generation antihistamines differ in the presence or absence of side effects associated with stimulation of other types of receptors, the duration of action, and the development of addiction.

The first AGPs - phenbenzamine (Antergan), pyrilamine maleate (Neo-Antergan) began to be used as early as 1942. Subsequently, new antihistamines have appeared for use in clinical practice. Until the 1970s Dozens of compounds belonging to this group of drugs have been synthesized.

On the one hand, a large clinical experience has been accumulated in the use of first-generation antihistamines, on the other hand, these drugs have not been examined in clinical trials that meet the modern requirements of evidence-based medicine.

Comparative characteristics of AGP of the first and second generations are presented in Table. one .

Table 1.

Comparative characteristics of AGP of the first and second generations

Properties First generation Second generation
Sedation and effects on cognition Yes (in minimal doses) No (in therapeutic doses)
Selectivity for H 1 receptors Not Yes
Pharmacokinetic studies Few A lot of
Pharmacodynamic studies Few A lot of
Scientific studies of various doses Not Yes
Studies in newborns, children, elderly patients Not Yes
Use in pregnant women FDA Category B (diphenhydramine, chlorpheniramine), Category C (hydroxyzine, ketotifen) FDA Category B (loratadine, cetirizine, levocetirizine), Category C (desloratadine, azelastine, fexofenadine, olopatadine)

Note. FDA (US Food and Drug Administration) - Food and Drug Administration (USA). Category B - no teratogenic effect of the drug was detected. Category C - studies have not been conducted.

Since 1977, the pharmaceutical market has been replenished with new H 1 -AHPs, which have clear advantages over first-generation drugs and meet modern requirements for AGPs set out in the EAACI (European Academy of Allergology and Clinical Immunology) consensus documents.

The myth about the benefits of the sedative effect of first-generation antihistamines
Even with regard to some of the side effects of first-generation antihistamines, there are misconceptions. The sedative effect of first-generation H1-HPA is associated with the myth that their use is preferable in the treatment of patients with concomitant insomnia, and if this effect is undesirable, it can be leveled by using the drug at night. At the same time, it should be remembered that first-generation antihistamines inhibit the phase of REM sleep, due to which the physiological process of sleep is disturbed, and there is no complete processing of information in sleep. When using them, breathing and heart rhythm disturbances are possible, which increases the risk of developing sleep apnea. In addition, in some cases, the use of high doses of these drugs contributes to the development of paradoxical excitation, which also negatively affects the quality of sleep. It is necessary to take into account the difference in the duration of the preservation of the antiallergic effect (1.5-6 hours) and the sedative effect (24 hours), as well as the fact that prolonged sedation is accompanied by impaired cognitive functions.

The presence of pronounced sedative properties debunks the myth about the expediency of using H1-HPA of the first generation in elderly patients who use these drugs, guided by the prevailing stereotypes of habitual self-treatment, as well as the recommendations of doctors who are not sufficiently informed about the pharmacological properties of drugs and contraindications to their appointment. Due to the lack of selectivity of effects on alpha-adrenergic receptors, muscarinic, serotonin, bradykinin and other receptors, a contraindication to the appointment of these drugs is the presence of diseases that are quite common among the elderly patients - glaucoma, benign prostatic hyperplasia, bronchial asthma, chronic obstructive pulmonary disease, etc. . .

The myth about the absence of a place in clinical practice for first-generation antihistamines
Despite the fact that first-generation H1-AHPs (most of them developed in the middle of the last century) are capable of causing known side effects, they are still widely used in clinical practice today. Therefore, the myth that with the advent of the new generation of AHD there is no place left for the previous generation of AHD is invalid. The H 1 -AGP of the first generation has one indisputable advantage - the presence of injectable forms that are indispensable in the provision of emergency care, premedication before certain types of diagnostic examinations, surgical interventions, etc. In addition, some drugs have an antiemetic effect, reduce the state of increased anxiety, and are effective in motion sickness. An additional anticholinergic effect of a number of drugs of this group is manifested in a significant reduction in itching and skin rashes with itchy dermatoses, acute allergic and toxic reactions to food, drugs, insect bites and stings. However, it is necessary to prescribe these drugs with strict consideration of indications, contraindications, severity of clinical symptoms, age, therapeutic dosages, and side effects. The presence of pronounced side effects and the imperfection of the first generation H 1 -AGP contributed to the development of new second generation antihistamine drugs. The main directions of improvement of drugs were the increase in selectivity and specificity, the elimination of sedation and tolerance to the drug (tachyphylaxis).

Modern H 1 -AGP of the second generation have the ability to selectively affect H 1 receptors, do not block them, but, being antagonists, they transfer them to an “inactive” state without violating their physiological properties, have a pronounced anti-allergic effect, a rapid clinical effect, act long (24 hours), do not cause tachyphylaxis. These drugs practically do not penetrate the blood-brain barrier, therefore, do not cause a sedative effect, cognitive impairment.

Modern H 1 -AGP of the second generation have a significant anti-allergic effect - they stabilize the membrane of mast cells, suppress the release of interleukin-8 induced by eosinophils, granulocyte-macrophage colony-stimulating factor (Granulocyte Macrophage Colony-Stimulating Factor. GM-CSF) and soluble intercellular adhesion molecule 1 (Soluble Intercellular Adhesion Molecule-1, sICAM-1) from epithelial cells, which contributes to greater efficiency compared to first-generation H1-AHP in the basic therapy of allergic diseases, in the genesis of which mediators of the late phase of allergic inflammation play a significant role.

In addition, an important characteristic of second-generation H1-AHP is their ability to provide an additional anti-inflammatory effect by inhibiting the chemotaxis of eosinophils and neutrophilic granulocytes, reducing the expression of adhesion molecules (ICAM-1) on endothelial cells, inhibiting IgE-dependent platelet activation, and releasing cytotoxic mediators. Many doctors do not pay due attention to this, however, the listed properties make it possible to use such drugs for inflammation not only of an allergic nature, but also of an infectious origin.

The myth of the same safety of all second-generation AHDs
There is a myth among physicians that all second-generation H1-HPAs are similar in their safety. However, in this group of drugs there are differences associated with the peculiarity of their metabolism. They may depend on the variability in the expression of the CYP3A4 enzyme of the liver cytochrome P 450 system. Such variability may be due to genetic factors, diseases of the hepatobiliary system, simultaneous intake of a number of drugs (macrolide antibiotics, some antimycotic, antiviral drugs, antidepressants, etc.), products (grapefruit) or alcohol that have an inhibitory effect on the oxygenase activity of the CYP3A4 cytochrome system. P450.

Among the H1-AGP of the second generation, there are:

  • "metabolizable" drugs that have a therapeutic effect only after undergoing metabolism in the liver with the participation of the CYP 3A4 isoenzyme of the cytochrome P450 system with the formation of active compounds (loratadine, ebastine, rupatadine);
  • active metabolites - drugs that enter the body immediately in the form of an active substance (cetirizine, levocetirizine, desloratadine, fexofenadine) (Fig. 1).
  • Rice. one. Features of the metabolism of H 1 -AGP of the second generation

    The advantages of active metabolites, the intake of which is not accompanied by an additional burden on the liver, are obvious: the speed and predictability of the development of the effect, the possibility of joint administration with various drugs and foods that are metabolized with the participation of cytochrome P450.

    The myth about the higher efficiency of each new AGP
    The myth that the new H1-AGP agents that have appeared in recent years are obviously more effective than the previous ones has also not been confirmed. The works of foreign authors indicate that second-generation H1-AHP, for example, cetirizine, have a more pronounced antihistamine activity than second-generation drugs that appeared much later (Fig. 2).

    Rice. 2. Comparative antihistamine activity of cetirizine and desloratadine on the effect on the skin reaction caused by the administration of histamine within 24 hours

    It should be noted that among the H 1 -AGP of the second generation, researchers assign a special place to cetirizine. Developed in 1987, it was the first original highly selective H1 receptor antagonist based on the pharmacologically active metabolite of the previously known first-generation antihistamine, hydroxyzine. Until now, cetirizine remains a kind of standard of antihistamine and antiallergic action, used for comparison in the development of the latest antihistamine and antiallergic drugs. There is an opinion that cetirizine is one of the most effective antihistamine H 1 drugs, it has been used more often in clinical trials, the drug is preferable for patients who respond poorly to therapy with other antihistamines.

    The high antihistamine activity of cetirizine is due to the degree of its affinity for H 1 receptors, which is higher than that of loratadine. It should also be noted the significant specificity of the drug, since even at high concentrations it does not have a blocking effect on serotonin (5-HT 2), dopamine (D 2), M-cholinergic receptors and alpha-1-adrenergic receptors.

    Cetirizine meets all the requirements for modern second generation antihistamines and has a number of features. Among all known antihistamines, the active metabolite cetirizine has the smallest volume of distribution (0.56 l/kg) and provides full employment of H1 receptors and the highest antihistamine effect. The drug is characterized by a high ability to penetrate the skin. 24 hours after taking a single dose, the concentration of cetirizine in the skin is equal to or exceeds the concentration of its content in the blood. At the same time, after a course of treatment, the therapeutic effect persists for up to 3 days. The pronounced antihistamine activity of cetirizine favorably distinguishes it among modern antihistamines (Fig. 3).

    Rice. 3. Efficacy of a single dose of second-generation H 1 -AHP in suppressing histamine-induced whealing over 24 hours in healthy men

    The myth about the high cost of all modern AGPs
    Any chronic disease is not immediately amenable to even adequate therapy. As is known, insufficient control over the symptoms of any chronic inflammation leads not only to a deterioration in the patient's well-being, but also to an increase in the total cost of treatment due to an increase in the need for drug therapy. The selected drug should have the most effective therapeutic effect and be affordable. Physicians who remain committed to prescribing first-generation H1-AHP explain their choice by referring to yet another myth that all second-generation antihistamines are much more expensive than first-generation drugs. However, in addition to the original drugs on the pharmaceutical market, there are generics, the cost of which is lower. For example, at present, 13 generics are registered from cetirizine drugs in addition to the original one (Zyrtec). The results of pharmacoeconomic analysis presented in Table. 2, testify to the economic feasibility of using Cetrin, a modern second-generation AGP.

    Table 2.

    Results of comparative pharmacoeconomic characteristics of H1-AGP of the first and second generations

    A drug Suprastin 25 mg № 20 Diazolin 100 mg №10 Tavegil 1 mg № 20 Zyrtec 10 mg No. 7 Cetrin 10 mg № 20
    Average market value of 1 pack 120 rub. 50 rub. 180 rub. 225 rub. 160 rub.
    Multiplicity of reception 3 r/day 2 r / day 2 r / day 1 r / day 1 r / day
    The cost of 1 day of therapy 18 rub. 10 rub. 18 rub. 32 rub. 8 rub.
    Cost of 10 days of therapy 180 rub. 100 rub. 180 rub. 320 rub. 80 rub.

    The myth that all generics are equally effective
    The question of the interchangeability of generics is relevant when choosing the optimal modern antihistamine drug. Due to the variety of generics on the pharmacological market, a myth has arisen that all generics act approximately the same, so you can choose any, focusing primarily on price.

    Meanwhile, generics differ from each other, and not only pharmacoeconomic characteristics. The stability of the therapeutic effect and the therapeutic activity of the reproduced drug are determined by the features of the technology, packaging, the quality of active substances and excipients. The quality of the active substances of drugs from different manufacturers can vary significantly. Any change in the composition of excipients can contribute to a decrease in bioavailability and the occurrence of side effects, including hyperergic reactions of various nature (toxic, etc.). A generic drug must be safe to use and equivalent to the original drug. Two medicinal products are considered to be bioequivalent if they are pharmaceutically equivalent, have the same bioavailability and, when administered at the same dose, are similar, providing adequate efficacy and safety. According to the recommendations of the World Health Organization, the bioequivalence of a generic should be determined in relation to the officially registered original drug. The study of bioequivalence is one of the stages in the study of therapeutic equivalence. The FDA (Food and Drug Administration - Food and Drug Administration (USA)) annually publishes and publishes the "Orange Book" with a list of drugs that are considered therapeutically equivalent to the original. Thus, any doctor can make the optimal choice of a safe antihistamine drug, taking into account all the possible characteristics of these drugs.

    One of the highly effective generics of cetirizine is Cetrin. The drug acts quickly, for a long time, has a good safety profile. Cetrin is practically not metabolized in the body, the maximum serum concentration is reached one hour after ingestion, with prolonged use it does not accumulate in the body. Cetrin is available in 10 mg tablets, indicated for adults and children from 6 years of age. Cetrin is completely bioequivalent to the original drug (Fig. 4).

    Rice. four. The average dynamics of the concentration of cetirizine after taking the compared drugs

    Cetrin is successfully used as part of the basic therapy of patients with allergic rhinitis with sensitization to pollen and household allergens, allergic rhinitis associated with atopic bronchial asthma, allergic conjunctivitis, urticaria, including chronic idiopathic urticaria, pruritic allergic dermatoses, angioedema, and also as symptomatic therapy for acute viral infections in patients with atopy. When comparing the performance indicators of cetirizine generics in patients with chronic urticaria, the best results were noted with the use of Cetrin (Fig. 5).

    Rice. 5. Comparative evaluation of the clinical efficacy of cetirizine preparations in patients with chronic urticaria

    Domestic and foreign experience in the use of Cetrin indicates its high therapeutic efficacy in clinical situations where the use of second-generation H 1 antihistamines is indicated.

    Thus, when choosing the optimal H 1 -antihistamine drug from all drugs on the pharmaceutical market, one should not be based on myths, but on selection criteria that include maintaining a reasonable balance between efficacy, safety and availability, the presence of a convincing evidence base, and high quality production. .

    BIBLIOGRAPHY:

    1. Luss L.V. The choice of antihistamines in the treatment of allergic and pseudo-allergic reactions // Russian Allergological Journal. 2009. No. 1. S. 78-84.
    2. Gushchin I.S. Potential of antiallergic activity and clinical efficacy of H1-antagonists // Allergology. 2003. No. 1. C. 78-84.
    3. Takeshita K., Sakai K., Bacon K.B., Gantner F. Critical role of histamine H4 receptor in leukotriene B4 production and mast cell-dependent neutrophil recruitment induced by zymosan in vivo // J. Pharmacol. Exp. Ther. 2003 Vol. 307. No. 3. P. 1072-1078.
    4. Gushchin I.S. Diversity of the antiallergic action of cetirizine // Russian Allergological Journal. 2006. No. 4. S. 33.
    5. Emelyanov A.V., Kochergin N.G., Goryachkina L.A. To the 100th anniversary of the discovery of histamine. History and modern approaches to the clinical use of antihistamines // Clinical dermatology and venereology. 2010. No. 4. S. 62-70.
    6. Tataurshchikova N.S. Modern aspects of the use of antihistamines in the practice of a general practitioner // Farmateka. 2011. No. 11. S. 46-50.
    7. Fedoskova T.G. The use of cetirizine (Cetrin) in the treatment of patients with perennial allergic rhinitis // Russian Allergological Journal. 2006. No. 5. C. 37-41.
    8. Holgate S. T., Canonica G. W., Simons F. E. et al. Consensus Group on New-Generation Antihistamines (CONGA): present status and recommendations // Clin. Exp. Allergy. 2003 Vol. 33. No. 9. P. 1305-1324.
    9. Grundmann S.A., Stander S., Luger T.A., Beissert S. Antihistamine combination treatment for solar urticaria // Br. J. Dermatol. 2008 Vol. 158. No. 6. P. 1384-1386.
    10. Brik A., Tashkin D.P., Gong H. Jr. et al. Effect of cetirizine, a new histamine H1 antagonist, on airway dynamics and responsiveness to inhaled histamine in mild asthma // J. Allergy. Clin. Immunol. 1987 Vol. 80. No. 1. P. 51-56.
    11. Van De Venne H., Hulhoven R., Arendt C. Cetirizine in perennial atopic asthma // Eur. Resp. J. 1991. Suppl. 14. P. 525.
    12. An open randomized crossover study of comparative pharmacokinetics and bioequivalence of Cetrin tablets 0.01 (Dr. Reddy's Laboratories LTD, India) and Zyrtec tablets 0.01 (UCB Pharmaceutical Sector, Germany).
    13. Fedoskova T.G. Features of the treatment of acute respiratory viral infections in patients with year-round allergic rhinitis // Russian Allergological Journal. 2010. No. 5. P. 100-105.
    14. Medicines in Russia, Vidal's Handbook. M.: AstraPharmService, 2006.
    15. Nekrasova E.E., Ponomareva A.V., Fedoskova T.G. Rational pharmacotherapy of chronic urticaria // Russian Allergological Journal. 2013. No. 6. S. 69-74.
    16. Fedoskova T.G. The use of cetirizine in the treatment of patients with year-round allergic rhinitis associated with atopic bronchial asthma // Russian Allergological Journal. 2007. No. 6. C. 32-35.
    17. Elisyutina O.G., Fedenko E.S. Experience with the use of cetirizine in atopic dermatitis // Russian Allergological Journal. 2007. No. 5. S. 59-63.