Currently, in the special literature, opinions regarding which antiallergic drugs should be attributed to the second and third generation diverge. In this regard, the list of 2nd generation antihistamines will have its own characteristics, depending on what point of view modern pharmacists adhere to.

What are the criteria for classifying antihistamines in the second group?

According to the first point of view, second-generation drugs are all those antiallergic drugs that are devoid of sedation, because they do not penetrate the brain through the blood-brain barrier.

The second and most common point of view is that the second generation of antihistamines should include only those that, although they do not affect the nervous system, are capable of causing changes in the heart muscle. Medicines that do not act on the heart and nervous system are classified as third-generation antihistamines.

According to the third point of view, only one drug with antihistamine properties, ketotifen, belongs to the second generation, because it has a membrane-stabilizing effect. And all those drugs that stabilize the mast cell membrane, but do not cause sedation, make up the third generation of antihistamines.

Why are antihistamines given this name?

Histamine is the most important substance, which is mainly found in mast cells of the connective tissue and blood basophils. Being released under the influence of various factors from these cells, it connects to the H 1 and H 2 receptors:

  • H 1 receptors, when interacting with histamine, cause bronchospasm, contraction of smooth muscles, dilate capillaries and increase their permeability.
  • H 2 receptors stimulate an increase in acidity in the stomach, affect the heart rate.

Indirectly, histamine can cause severe itching by stimulating the release of catecholamines from adrenal cells, increase the secretion of the salivary and lacrimal glands, and also accelerate intestinal motility.

Antihistamines bind to H 1 and H 2 receptors and block the action of histamine.

List of drugs of the second group

According to the most common classification of antihistamines, the second generation includes:

  • dimethindene,
  • loratadine,
  • ebastine,
  • cyproheptadine,
  • azelastine,
  • acrivastine.

All these drugs do not penetrate the brain, so they do not cause a sedative effect. However, the possible development of cardiotoxic action limits the use of this group of drugs in the elderly and those who suffer from heart disease.

Enhances myocardial damage in the treatment of second-generation antihistamines, the simultaneous use of antifungal agents and some antibiotics with them, for example, clarithromycin, erythromycin, itraconazole and ketoconazole. You should also refrain from drinking grapefruit juice and antidepressants.

Dimetinden (Fenistil)

Available in the form of drops, gel and capsules for oral administration. It is one of the few drugs that can be used in children of the first year of life, with the exception of the neonatal period.

Fenistil is well absorbed inside and has a pronounced anti-allergic effect, lasting after 1 dose for about 6-11 hours.

The drug is effective for skin itching, eczema, drug and food allergies, insect bites, itchy dermatoses and exudative-catarrhal diathesis in children. Its other purpose is the removal of household and mild sunburns.

Application features. It is one of the few second-generation drugs that still crosses the blood-brain barrier, so it can slow down the response when driving. In this connection, it should be prescribed with extreme caution to drivers, and even more so not to be used during work that requires a quick reaction.

When applying the gel to the skin, it is necessary to protect this area from exposure to direct sunlight.

Dimetindene is contraindicated during the first trimester of pregnancy and in the neonatal period. It is used with caution in the second and third trimesters of pregnancy, with prostate adenoma, angle-closure glaucoma.

Loratadine (claritin, lomilan, lotaren)

Like other drugs in this group, it effectively treats all kinds of allergic diseases, especially allergic rhinitis, conjunctivitis, nasopharyngitis, angioedema, urticaria, endogenous itching. The drug is available in the form of tablets and syrup for oral administration, and is also part of multicomponent antiallergic gels and ointments for local treatment.

Effective for pseudo-allergic reactions, pollinosis, urticaria, itchy dermatoses. As an aid, it is prescribed for bronchial asthma.

Application features. May cause sedation in the elderly and is not recommended during pregnancy and breastfeeding. Many drugs reduce the effectiveness of loratadine or increase its side effects, so you should always consult your doctor before taking it.

Ebastin (Kestin)

It also belongs to the group of second-generation antihistamines. Its distinguishing feature is the absence of interaction with ethanol, so it is not contraindicated in the use of drugs containing alcohol. Simultaneous administration with ketoconazole increases the toxic effect on the heart, which can lead to fatal consequences.

Ebastin is prescribed for allergic rhinitis, urticaria and other diseases accompanied by excessive release of histamine.

Cyproheptadine (peritol)

This drug for the treatment of allergic reactions can be prescribed to children from 6 months. Like other drugs in this group, cyproheptadine has a strong and lasting effect, eliminating allergy symptoms. A distinctive feature of peritol is the relief of migraine headaches, a calming effect, and a decrease in the excess secretion of somatotropin in acromegaly. Cyproheptadine is prescribed for toxicoderma, neurodermatitis, in the complex therapy of chronic pancreatitis, serum sickness.

Azelastine (allergodil)

This drug copes well with such types of allergy manifestations as allergic rhinitis and conjunctivitis. Available as a nasal spray and eye drops. In pediatrics, it is prescribed for children from 4 years old (eye drops) and from 6 years old (spray). The duration of the course of treatment with azelastine on the recommendation of a doctor can last up to 6 months.

From the nasal mucosa, the drug is well absorbed into the general circulation and has a systemic effect on the body.

Acrivastine (semprex)

The drug penetrates poorly through the blood-brain barrier, therefore it does not have a sedative effect, however, drivers of vehicles and those whose work requires quick and accurate actions should refrain from taking it.

Acrivastine differs from other representatives of this group in that it begins to act within the first 30 minutes, and the maximum effect on the skin is observed already 1.5 hours after administration.

Drugs of the second group, about which there is disagreement in the scientific community

Mebhydrolin (diazolin)

Most experts attribute diazolin to the first generation of antihistamines, while others, due to the minimally pronounced sedative effect, classify this agent as the second. Be that as it may, diazolin is widely used not only in adults, but also in pediatric practice, being considered one of the most inexpensive and affordable medicines.

Desloratadine (Eden, Erius)

It is most commonly referred to as a third-generation antihistamine because it is an active metabolite of loratadine.

Cetirizine (Zodak, Cetrin, Parlazin)

Most researchers classify this drug as a second-generation antihistamine, although some confidently classify it as a third, because it is an active metabolite of hydroxyzine.

Zodak is well tolerated and rarely causes side effects. Available in the form of drops, tablets and syrup for oral administration. With a single dose of the drug, it has a therapeutic effect throughout the day, so it can be taken only 1 time per day.

Cetirizine relieves allergy symptoms, does not cause sedation, prevents the development of spasm of smooth muscles and swelling of surrounding tissues. It is effective for hay fever, allergic conjunctivitis, hives, eczema, itching is well removed.

Application features. If the drug is prescribed in large doses, then you should refrain from driving vehicles, as well as work that requires quick response. When combined with alcohol, cetirizine can enhance its negative effect.

The duration of the course of treatment with this drug can be from 1 to 6 weeks.

Fexofenadine (Telfast)

Most researchers also belong to the third generation of antihistamines, because it is an active metabolite of terfenadine. It can be used by those whose activities are related to driving vehicles, as well as those suffering from heart disease.

Content

A small number of people are fortunate enough to never experience allergic reactions in their lives. Most people have to deal with them from time to time. Effective antihistamines will help to cope with allergies for both an adult and a child. Such funds help to eliminate negative reactions on the body to certain stimuli. There is a wide range of anti-allergic drugs on the market. It is desirable for every person to be able to understand them.

What are antihistamines

These are drugs whose work is aimed at suppressing the action of free histamine. This substance is released from the connective tissue cells that enter the immune system when an allergen enters the human body. When histamine interacts with certain receptors, swelling, itching, and rashes begin. All of these are symptoms of an allergy. Drugs with an antihistamine effect block the aforementioned receptors, alleviating the patient's condition.

Indications for use

You must be prescribed antihistamines by a doctor, having made an accurate diagnosis. As a rule, their administration is advisable in the presence of such symptoms and diseases:

  • early atopic syndrome in a child;
  • seasonal or year-round rhinitis;
  • negative reaction to plant pollen, animal hair, household dust, some medications;
  • severe bronchitis;
  • angioedema;
  • anaphylactic shock;
  • food allergies;
  • enteropathy;
  • bronchial asthma;
  • atopic dermatitis;
  • conjunctivitis caused by exposure to allergens;
  • chronic, acute and other forms of urticaria;
  • allergic dermatitis.

Antihistamines - list

There are several generations of antiallergic drugs. Their classification:

  1. New generation drugs. The most modern medicines. They act very quickly, and the effect of their use lasts for a long time. Block H1 receptors, suppressing allergy symptoms. Antihistamines in this group do not worsen the functioning of the heart, therefore they are considered one of the safest.
  2. 3rd generation drugs. Active metabolites with very few contraindications. They provide a fast stable result, they are gentle on the heart.
  3. 2nd generation drugs. Not sedative drugs. They have a small list of side effects, give a big load on the heart. Do not affect mental or physical activity. Antiallergic drugs of the second generation are often prescribed for the appearance of a rash, itching.
  4. 1st generation drugs. Sedative drugs that last up to several hours. Well eliminate the symptoms of allergies, but have many side effects, contraindications. From their use always tends to sleep. At the present time, such drugs are prescribed very rarely.

New generation antiallergic drugs

It is not possible to list all the drugs in this group. Let's take a look at some of the best ones. This list opens with the following drug:

  • name: Fexofenadine (analogues - Allegra (Telfast), Fexofast, Tigofast, Altiva, Fexofen-Sanovel, Kestin, Norastemizol);
  • action: blocks H1-histamine receptors, relieves all allergy symptoms;
  • pluses: acts quickly and for a long time, is available in tablets and suspensions, is well tolerated by patients, does not have too many side effects, is dispensed without a prescription;
  • cons: not suitable for children under six years of age, pregnant women, nursing mothers, incompatible with antibiotics.

Another drug that deserves attention:

  • name: Levocetirizine (analogues - Aleron, Zilola, Alerzin, Glenset, Aleron Neo, Rupafin);
  • action: antihistamine, blocks H1 receptors, reduces vascular permeability, has antipruritic and antiexudative effects;
  • pluses: there are tablets, drops, syrup on sale, the drug acts in just a quarter of an hour, there are not many contraindications, there is compatibility with many drugs;
  • cons: a wide range of strong side effects.
  • name: Desloratadine (analogues - Lordes, Allergostop, Alersis, Fribris, Edem, Eridez, Alergomax, Erius);
  • action: antihistamine, antipruritic, decongestant, relieves rash, runny nose, nasal congestion, reduces bronchial hyperactivity;
  • pluses: the new generation allergy medicine is well absorbed and works quickly, relieves allergy symptoms for a day, does not have a negative effect on the central nervous system and reaction rate, does not harm the heart, joint use with other drugs is allowed;
  • cons: not suitable for pregnancy and lactation, prohibited for children under 12 years of age.

Antihistamine 3 generations

The following drug is popular and has many good reviews:

  • name: Desal (analogues - Ezlor, Nalorius, Elyseus);
  • action: antihistamine, relieves swelling and spasms, relieves itching, rash, allergic rhinitis;
  • pluses: it is available in tablets and solution, does not give a sedative effect and does not affect the rate of reactions, it works quickly and acts for about a day, it is quickly absorbed;
  • cons: bad effect on the heart, many side effects.

Experts respond well to this drug:

  • name: Suprastinex;
  • action: antihistamine, prevents the appearance of allergic manifestations and facilitates their course, helps with itching, peeling, sneezing, swelling, rhinitis, lacrimation;
  • pluses: it is available in drops and tablets, there is no sedative, anticholinergic and antiserotonergic effect, the drug acts in an hour and continues to work for a day;
  • cons: there are a number of strict contraindications.

The group of third-generation drugs also includes the following:

  • name: Ksizal;
  • action: pronounced antihistamine, not only relieves allergy symptoms, but also prevents their occurrence, reduces the permeability of vascular walls, fights sneezing, lacrimation, edema, urticaria, inflammation of the mucous membranes;
  • pluses: sold in tablets and drops, does not have a sedative effect, is well absorbed;
  • cons: has a wide list of side effects.

2nd generation antiallergenic drugs

A well-known series of drugs, represented by tablets, drops, syrups:

  • name: Zodak;
  • action: prolonged anti-allergic, helps against itching, skin peeling, relieves swelling;
  • pluses: subject to dosages and rules of administration, it does not cause drowsiness, quickly begins to act, is not addictive;
  • cons: prohibited for pregnant women and children.

The next second generation drug:

  • name: Cetrin;
  • action: antihistamine, well helps with edema, hyperemia, itching, peeling, rhinitis, urticaria, reduces capillary permeability, relieves spasms;
  • pluses: there are drops and syrup on sale, low cost, lack of anticholinergic and antiserotonin effects, if the dosage is observed, it does not affect concentration, is not addictive, side effects are extremely rare;
  • cons: there are a number of strict contraindications, an overdose is very dangerous.

Another very good drug in this category:

  • name: Lomilan;
  • action: systemic blocker of H1 receptors, relieves all allergy symptoms: itching, peeling, swelling;
  • pluses: does not affect the heart and central nervous system, is completely excreted from the body, helps to overcome allergies well and quickly, suitable for continuous use;
  • cons: many contraindications and side effects.

Means of the 1st generation

Antihistamines of this group appeared a very long time ago and are now used less often than others, however, they deserve attention. Here is one of the most famous:

  • name: Diazolin;
  • action: antihistamine, blocker of H1 receptors;
  • pluses: gives an anesthetic effect, acts for a long time, helps well with dermatosis with itchy skin, rhinitis, cough, food and drug allergies, insect bites, is cheap;
  • cons: there is a moderately pronounced sedative effect, many side effects, contraindications.

This one also belongs to the drugs of the 1st generation:

  • name: Suprastin;
  • action: anti-allergic;
  • pluses: available in tablets and ampoules;
  • cons: a pronounced sedative effect, the effect does not last long, there are a lot of contraindications, side effects.

The last member of this group:

  • name: Fenistil;
  • action: histamine blocker, antipruritic;
  • pluses: available in the form of a gel, emulsion, drops, tablets, relieves skin irritation well, relieves pain a little, inexpensive;
  • cons: the effect after application passes quickly.

Allergy pills for children

Most antihistamines have strict age contraindications. The question would be quite reasonable: how to treat very small allergies, who suffer at least as often as adults? As a rule, children are prescribed drugs in the form of drops, suspensions, and not tablets. Means approved for the treatment of infants and persons under 12 years of age:

  • Diphenhydramine;
  • Fenistil (drops are suitable for babies older than a month);
  • Peritol;
  • Diazolin;
  • Suprastin (suitable for babies);
  • Clarotadine;
  • Tavegil;
  • Tsetrin (suitable for newborns);
  • Zyrtec;
  • Claricens;
  • Cinnarizine;
  • Loratadine;
  • Zodak;
  • Claritin;
  • Erius (allowed from birth);
  • Lomilan;
  • Fenkarol.

Mechanism of action of antihistamines

Under the action of an allergen, an excess of histamine is produced in the body. When it is associated with certain receptors, negative reactions are caused (edema, rash, itching, runny nose, conjunctivitis, etc.). Antihistamines reduce the release of this substance into the blood. In addition, they block the action of H1-histamine receptors, thereby preventing them from binding and reacting with histamine itself.

Side effects

Each drug has its own list. The specific list of side effects also depends on which generation the remedy belongs to. Here are a few of the most common:

  • headache;
  • drowsiness;
  • confusion;
  • decreased muscle tone;
  • fast fatiguability;
  • constipation;
  • concentration disorders;
  • blurred vision;
  • abdominal pain;
  • dizziness;
  • dry mouth.

Contraindications

Each antihistamine drug has its own list, specified in the instructions. Almost every one of them is forbidden to be taken by pregnant girls and nursing mothers. In addition, the list of contraindications for therapy may include:

  • individual intolerance to the components;
  • glaucoma;
  • stomach or duodenal ulcer;
  • prostate adenoma;
  • obstruction of the bladder;
  • childhood or old age;
  • diseases of the lower respiratory tract.

Best Allergy Remedies

TOP 5 most effective drugs:

  1. Erius. A fast-acting medicine that well eliminates a runny nose, itching, rashes. It costs expensive.
  2. Eden. Drug with desloratadine. Does not give a hypnotic effect. It copes well with lacrimation, itching, swelling.
  3. Zyrtec. A drug based on cetirizine. Fast acting and efficient.
  4. Zodak. An excellent allergy medicine that instantly eliminates symptoms.
  5. Tsetrin. A drug that rarely gives side effects. Quickly eliminates allergy symptoms.

The price of antihistamines

All medicines are available for purchase, and you can easily choose the most suitable one. Sometimes they give good discounts on funds. You can buy them in pharmacies in Moscow, St. Petersburg and other cities, order their delivery by mail in online pharmacies. For an approximate price range for antihistamines, see the table:

Name of the drug, form of release, volume

Approximate cost in rubles

Suprastin, tablets, 20 pcs.

Zyrtec, drops, 10 ml

Fenistil, drops, 20 ml

Erius, tablets, 10 pcs.

Zodak, tablets, 30 pcs.

Claritin, tablets, 30 pcs.

Tavegil, tablets, 10 pcs.

Cetrin, tablets, 20 pcs.

Loratadine, tablets, 10 pcs.

Question: Can antiallergic antihistamines harm a person if taken on a regular basis?

Answer: It is better to pass tests for allergens on the machine "IMEDIS Expert", and further exclude contacts with identified bioresonance test allergens. Also, if possible, it is treated by a bioresonance therapist and for many years to take homeopathic and bioresonance preparations prescribed during the treatment of bioresonance therapy, as well as during exacerbations or during the allergic season, take new-generation antihistamine drugs selected by a bioresonance test or pendulum.

You need to drink new generation antihistamines 1 time per day until the allergy symptoms disappear. If contact with the allergen cannot be avoided, then you will have to take an antihistamine (anti-allergic drug) daily, there is nowhere to go from this, alas. When exposed to an allergen without an antiallergic drug, a severe allergic reaction can develop, which in turn can lead to death, coma, and allergies can also turn into asthma.

There are people who sit on new generations of antihistamines during their lifetime and nothing.

Of course, pills are no sweetie, and antihistamines are no exception. In a state of reaction, do not try to do without them. Allergens will need to be removed from the field of the body on time, and then it may be too late.

Antihistamines

Antihistamines are a group of drugs whose principle of action is based on the fact that they block H1 and H2-histamine receptors. This blocking helps to reduce the reaction of the human body with a special mediator histamine. What are these medicines for? Doctors prescribe them during allergic reactions. Possessing good antipruritic, antispastic, antiserotonin and local anesthetic effects, antihistamines perfectly help with allergies, and also effectively prevent bronchospasm caused by histamine.

In accordance with the time of invention and release on sale, the whole variety of allergy remedies is classified into several levels. Antihistamines are classified into first, second, third and fourth generation drugs. The medicines included in each generation have their own specific features and properties. Their classification is based on the duration of the antihistamine effect, the existing contraindications and side effects. The medicine necessary for treatment must be selected based on the characteristics of each specific case of the disease.

Generations of antihistamines

First generation antihistamines

Preparations of the 1st (first) generation include sedatives. They work at the level of H-1 receptors. The duration of their action is four to five hours, after this period it will be necessary to take a new dose of the drug, and the dose should be large enough. Sedative antihistamines, despite their strong effect, have a number of disadvantages. For example, they can provoke dry mouth, dilated pupils, blurred vision.

Drowsiness and a decrease in tone may occur, which means it is impossible to take these drugs while driving a car and other activities that require a high concentration of attention. They also enhance the effect of taking other sedatives, sleeping pills and pain medications. The effect on the body of alcohol mixed with sedatives is also enhanced. Most first generation antihistamines are interchangeable.

Their use is advisable in case of allergic problems with the respiratory system, for example, when coughing or nasal congestion. It is worth paying attention to the fact that first-generation antihistamines fight cough well. This makes it appropriate to use them in bronchitis.

They will also be useful for those people who suffer from chronic diseases associated with difficulty breathing. Their use is quite effective in bronchial asthma. They can also have a fairly good effect in the treatment of acute allergic reactions. So, for example, their use will be appropriate for urticaria. The most common among them are:

suprastin

diphenhydramine

diazolin

tavegil

Also often on sale you can find peritol, pipolfen and fenkarol.

Second generation antihistamines

Preparations of the 2nd (second) generation are called non-sedative. They do not have such a large list of side effects as the drugs that make up the first generation of antihistamines. These are drugs that do not cause drowsiness and do not reduce brain activity, and also do not have cholinergic effects. A good effect is given by their use in itchy skin and allergic rashes.

However, their significant drawback is the cardiotoxic effect that these drugs can cause. Therefore, non-sedative drugs are prescribed only on an outpatient basis. In no case should they be taken by people suffering from diseases of the cardiovascular system. Names of the most common non-sedative drugs:

trexil

histalong

zodak

semprex

fenistil

claritin

Third generation antihistamines

Antihistamines of the 3rd (third) generation are also otherwise called active metabolites. They have strong antihistamine properties and have virtually no contraindications. The standard set of these drugs includes:

cetrin

zyrtec

telfast

These drugs do not have a cardiotoxic effect, unlike second-generation drugs. Their use gives a positive effect in asthma and acute allergic reactions. They are also effective in the treatment of dermatological diseases. Quite often, third-generation antihistamines are prescribed by doctors for psoriasis.

New generation drugs are the most effective and harmless antihistamines. They are non-addictive, safe for the cardiovascular system, and also have a long period of action. They belong to the fourth generation of antihistamines.

Fourth generation antihistamines

Preparations of the 4th (fourth) generation have a small list of contraindications, which are mainly pregnancy and childhood, but, nevertheless, it is worth reading the instructions and consulting with a specialist before starting treatment. The list of these drugs includes:

levocetirizine

desloratadine

fexofenadine

Based on them, a larger number of drugs are produced, which, if necessary, can be purchased at a pharmacy. These include erius, xizal, lordestin, and telfast.

Forms of release of antihistamines

There are several forms of release of drugs that block histamine receptors. In most cases, their most convenient type to use are tablets and capsules. However, on the shelves of pharmacies you can also find antihistamines in ampoules, suppositories, drops and even syrups. The action of each of them is unique, so only a doctor can help you choose the most appropriate form of taking the medicine.

Treatment of children with antihistamines

As you know, children are more prone to allergic diseases than adults. A qualified allergist should select and prescribe drugs for children. Many of them in the list of their contraindications are of children's age, therefore, if necessary, from the application to the preparation of a course of treatment, it is necessary to be especially careful. Children's organisms can react quite sharply to the effects of the drug, so the child's well-being during the period of their use must be monitored very carefully. In case of side effects, the drug should be stopped immediately and consult a doctor.

For the treatment of children, both somewhat outdated medicines and more modern ones are suitable. The drugs that make up the first generation are mainly used to urgently relieve acute allergy symptoms. During long-term use, more modern means are usually used.

Antihistamines are not usually available in special "children's" forms. For the treatment of children, the same drugs are used as for adults, but in smaller doses. Drugs such as zyrtec and ketotifen are usually prescribed from the moment the child reaches the age of six months, all others - from two years. Do not forget that taking medicines by a child should be under the supervision of an adult.

In the case of an illness of a small child, the selection of antihistamines is much more complicated. For newborns, medications that have a slight sedative effect, that is, first-generation drugs, may be suitable. The most commonly used in the treatment of very young children is suprastin. It is safe for both babies and older children, as well as for nursing mothers and pregnant women. Depending on the disease and the condition of the child's body, the doctor may prescribe him tavegil or Phencarol, and in the case of an allergic skin reaction, an antihistamine cream. For infants, the same drugs are suitable as for newborns.

Antihistamines during pregnancy and lactation

Due to the increased production of cortisol in the body of a woman, allergies during the childbearing period are quite rare, but, nevertheless, some women still face this problem. During pregnancy, the intake of absolutely all medications must be agreed with the doctor. This also applies to allergy remedies, which have a fairly wide range of side effects and can harm the child. The use of antihistamines is strictly prohibited in the first trimester of pregnancy; in the second and third trimesters, they can be used, observing, however, the necessary precautions.

Unintentional ingestion of the drug into the child's body is possible not only during pregnancy, but also during breastfeeding. During lactation, the use of antihistamines is highly undesirable and is prescribed only in the most urgent cases. The question of which remedy a nursing woman will use can only be decided by a doctor. Even the newest and most modern medicines can cause irreparable harm, so in any case, do not self-medicate by feeding your baby with your milk.

Side effects of antihistamines

As mentioned earlier, the body of each person is individual, and only a specialist can choose the right remedy for treatment. Taking the wrong medicine for a person and violating the dosage can seriously harm health. The harm of antihistamines can manifest itself in addition to their usual side effects such as drowsiness, runny nose and cough in violation of the timing of ovulation in women, the occurrence of allergic edema and asthma. Therefore, be sure to consult your doctor before you start drinking the medicine, and strictly follow the recommendations for taking it.

Drug treatment of allergies, antihistamines

How antihistamines work

Antihistamines of the "old" and "new" generations

What is the difference between 1st, 2nd and 3rd generation antihistamines

Fundamentals of drug therapy

There is such a substance - histamine. It is released during an allergic reaction and is responsible for the development of bad symptoms, from skin manifestations to very severe life-threatening reactions, such as anaphylactic shock. That's why antiallergic drugs are called ANTIhistamines.

They block histamine receptors and thus stop the development of allergy symptoms.

Depending on the type of reaction, antihistamines are prescribed by injection (for severe forms) and orally (for milder ones). It is understandable: if we inject the drug with the help of an intramuscular or intravenous injection, it instantly enters the bloodstream and is included in the work. And if we drink this medicine, time must pass before the active substance is absorbed into the blood from the gastrointestinal tract.

All anti-allergy drugs can be divided into several groups:

1. Symptomatic drugs.

2. Medicines for the treatment of chronic allergic inflammation in the affected organ.

3. Medicines for local therapy.

Symptomatic drugs are intended to alleviate the course of allergic diseases. The leading place among them belongs to drugs called antihistamines.

These agents counteract the damaging effects of the main mediator of allergic reactions, histamine. Today, doctors are armed with three generations of antihistamines that differ in their characteristics.

The selection of antihistamines is carried out individually, taking into account the nature of food allergies, the age of the child and the nature of concomitant diseases. Symptomatic drugs also, for example, include bronchodilators. They are used for asthma attacks.

Antihistamines for the treatment of chronic allergic inflammation in the affected organ are divided into non-hormonal and hormonal. The latter drugs are more powerful and effective.

The appointment of drugs in this group is carried out depending on the clinical manifestations of food allergies, the severity of the disease, the age of the child. It must be remembered that these drugs are generally effective only with long-term regular use.

We must remember that drug therapy for food allergies is a long process, you need to patiently and persistently follow medical recommendations.

We must also remember that some treatments for food allergies are absolutely contraindicated and can harm the child. So, with food allergies, treatment with herbs and many traditional medicines is contraindicated, and psychotherapy and reflexology, except for bioresonance treatment, almost do not give a significant effect.

Treatment with herbs and preparations based on them increases the risk of developing an allergy to plant pollen in the future. The same "service" can be provided by biologically active additives, which often contain plant components.

Antihistamines are standard therapy for atopic dermatitis. They are used as an additional remedy for external treatment with severe itching and associated rashes.

Antihistamines are divided into three generations:

means of the 1st "old" generation;

means of the 2nd and 3rd generations ("new" generation).

Antihistamine drugs of the 1st "old" generation

Antihistamines of the 1st generation are more often used to treat acute reactions, in the treatment of itchy allergic dermatoses. Most of them are available in solutions in ampoules, but there are forms in tablets, syrups and powders.

Antihistamines of the 1st "old" generation (forms for oral administration)

Chloropyramine, Clemastine, Dimetindene, Quifenadine, Hifenadine, Mebhydrolin, Ketotifen.

Disadvantages of older generation antihistamines:

Incomplete connection with H1 receptors, as a result of which relatively high doses are required;

Short-term action - taking several times a day

Development of addiction - it is necessary to alternate drugs of different groups every 10-14 days

Sedative and hypnotic effect

Antihistamine drugs of the 2nd and 3rd "new" generations

Loratodin, cyterizine, fexofenadine, desloratadine.

Currently, in the treatment of atopic dermatitis, antihistamine drugs of the “new”, that is, the 2nd and 3rd generations, are widely used.

Antihistamine drugs of the 2nd and 3rd generations are used for basic and anti-relapse therapy.

Antihistamines of the "new" generation do not have sedative and hypnotic effects. They have a selective effect, causing blockade of only H1-histamine receptors. The duration of their action is up to 24 hours, so most of these drugs are prescribed once a day.

After taking most antihistamines, their residual effect may last for one week after withdrawal (this circumstance must be taken into account when conducting an allergy examination). A significant difference between the antihistamine drugs of the "new" generation is that they have not only H1-blocking action, but also anti-allergic and anti-inflammatory effects.

If long-term use is necessary, only antihistamines of the “new” generation are used.

The absence of undesirable side effects characteristic of the first antihistamines allows to significantly expand the list of indications for the appointment of modern H1-antagonists.

Benefits of 2nd generation antihistamines over 1st generation:

Rapid onset of action (from 30 minutes - acute cases);

The possibility of taking at any time of the day (including in the first half of the day) good absorption from the digestive tract the possibility of using in young children a long duration of the antihistamine effect (up to 24 hours), which allows you to take the drug once a day.

No blockade of other types of receptors

Lack of penetration through the blood-brain barrier at therapeutic doses

Lack of connection with food intake

Non-addictive, even with long-term use (3 to 6 months)

The almost complete absence of side effects associated with exposure to the nervous and cardiovascular systems.

The use of antihistamine drugs in the treatment of children with atopic dermatitis.

Children after a year, as a rule, are prescribed drugs of a new generation.

The "new" generation drugs that are approved for use in children from 6 months of age are antihistamine drugs based on cetirizine (generic active ingredient).

VACCINATION

Since allergy is an immune disorder, allergic rhinitis and bronchial asthma can be treated with vaccines from allergens to which the child is hypersensitive. Indications for vaccination are determined based on the results of skin tests with allergens.

The vaccine is administered under a special scheme subcutaneously or buried under the tongue. Such treatment is applicable only in children over 5 years of age and should be carried out by an allergist.

And finally, the most interesting question: do allergy medications cause allergies? Yes! We will not go into the technical details of the complex mechanisms that may lead to this development.

Let's just say that an allergy to antihistamines is extremely rare, but it happens. There is only one way out - to change the drug.

Antihistamines are a group of drugs that perform a competitive blockade of histamine receptors in the body, which leads to inhibition of the effects mediated by it.

Histamine is a neurotransmitter that can affect the respiratory tract (causing swelling of the nasal mucosa, bronchospasm), skin (itching, blistering hyperemic reaction), gastrointestinal tract (intestinal colic, stimulation of gastric secretion), cardiovascular system (expansion of capillary vessels, increased vascular permeability, hypotension, cardiac arrhythmias), smooth muscles.

Strengthening its influence cause allergic reactions, so antihistamines are used to combat the manifestations of allergies. Another area of ​​their application is symptomatic therapy / elimination of symptoms in colds.

Currently, there are three groups of drugs (according to the receptors they block):

H1 blockers - used in the treatment of allergic diseases.

H2-blockers - used in the treatment of diseases of the stomach (help reduce gastric secretion).

H3 blockers are used in the treatment of neurological diseases.

Among them, cetrin (cetirizine), phencarol (chifenadine), diphenhydramine, clemastine, suprastin stop the emission (for example, cromoglycic acid) or the action (like diphenhydramine) of histamines.

Available in the form of tablets, nasal spray, drops, including eye drops, solution in ampoules for intramuscular injection (usually for emergency therapy).

There are several generations of antihistamines. With each generation, the number and strength of side effects and the likelihood of addiction decrease, the duration of action increases.

First generation

Before buying a medicine - paracetamol, ibuprofen, antiallergic (antihistamine) drugs, cold and cold remedies, you need to know:

Paracetamol

Pain reliever, antipyretic, anti-inflammatory agent. The active substance is paraacetaminophen, on the basis of which many other similar drugs are produced in different countries, such as acetaminophen, panadol, efferalgan, myalgin, paramol, pilaren, etc.

Benefit. In its action, paracetamol is in many ways close to aspirin, but has less pronounced side effects. It does not reduce blood viscosity, so it is safe to use in preparation for and after surgery.

It is less likely than aspirin to cause allergic reactions and is less irritating to the stomach. Paracetamol is part of many combined preparations in combination with aspirin, analgin, caffeine, etc. It is available in the form of tablets, capsules, mixtures, syrup, "effervescent" powders (panadol, panadon).

Possible harm. When combined with alcohol, it can damage and even destroy the liver. Therefore, it, like aspirin, is dangerous for people who regularly drink alcohol. Paracetamol has a negative effect on the liver and in case of violation of the norm of its intake (in case of overdose).

Exit. Take no more than 2 g per day (4 tablets of 500 mg) - People who drink alcohol daily should stop taking paracetamol.

ibuprofen

It has an analgesic and anti-inflammatory effect. Ibuprofen is the active ingredient in drugs such as Brufen, Arthryl, Advil, Naproxen, etc. These drugs are chemically identical, but differ in the duration of the therapeutic effect.

Benefit. Help with fever, muscle and joint pain (rheumatoid arthritis, arthrosis, etc.)

Possible harm. If the body is severely dehydrated as a result of hard physical work, heat, or taking diuretics (diuretics), then ibuprofen can adversely affect the kidneys. The risk of kidney damage increases with regular use of ibuprofen.

Long-term use of ibuprofen is dangerous for the stomach. In people who constantly drink alcohol, taking ibuprofen can affect the liver.

Exit. Try to avoid dehydration. When taking ibuprofen, it is necessary to monitor the work of the kidneys. In no case should you exceed the allowable daily intake (6 tablets of ibuprofen 200 mg or 2 tablets of naproxen 220 mg).

Antiallergic (antihistamine) drugs

The drugs in this group are intended for people suffering from pollinosis (hay fever), asthma, hives or other allergic diseases.

Benefit. They relieve runny nose, sneezing, sore throat, coughing and suffocation, unbearable itching and other symptoms of these diseases.

Possible harm. Most common drugs in this group, such as suprastin, tavegil, diphenhydramine, zaditen, peritol, etc., have a sedative effect, that is, they cause drowsiness, inhibition of reactions, and general weakness. Therefore, it is dangerous to take them to car drivers, pilots, operators, dispatchers, etc., that is, people who require constant attention and quick reaction in difficult situations.

Exit. To avoid the risk, you should take a new generation of antihistamines that do not cause drowsiness and inhibition of reactions, such as claritin, kestin, which act for 12-24 hours. Sedative antihistamines are best taken in the afternoon and at night.

Remedies for the common cold

The action of drugs such as sanorin, naphthyzin, galazolin, otrivin, etc., is that they narrow the blood vessels in the swollen mucous membrane of the nasal passages, as a result of which the nasal passages themselves expand.

Benefit. With a cold, the runny nose is weakened or stops, breathing through the nose is restored, and the headache disappears.

Possible harm. When taking these drugs, blood vessels are narrowed not only in the nose, as a result of which blood pressure may increase in patients with hypertension.

This is especially dangerous for hypertensive patients, since the drugs they take to lower blood pressure will be ineffective. In addition, drugs in this group are dangerous for those who take antidepressants such as pyrazidol, pirlindol, nialamide.

Exit. For people suffering from hypertension, common cold remedies can only be taken under the control of blood pressure. In the event of an increase in pressure, the dosage of antihypertensive drugs should be increased.

Patients with depression who take the listed antidepressants or the like, drugs in this group are contraindicated.

Complex preparations for colds used with antihistamines

Among the complex anti-cold drugs, such as askofen, citramon, sedalgin, alkaseltzer plus, bicarmint, etc. are especially known.

Benefit. They help to get rid of various symptoms of the disease at the same time: cough, runny nose, pain, fever, allergic manifestations.

Possible harm. When taking complex drugs, the so-called "unforeseen overdose" is quite often allowed.

This happens when, with a severe cold or headache, in order to increase the effectiveness of treatment, a complex cold preparation containing aspirin is added to the intake of aspirin. As a result, peptic ulcer disease may worsen or even gastric bleeding occurs.

If, with an allergic rhinitis, in addition to suprastin, you also take a complex preparation containing an antihistamine, then everything together will act as a strong sleeping pill. Sometimes liver disorders are associated with a similar overdose of paracetamol or ibuprofen.

Exit. Before taking a complex preparation for a cold, you should carefully read its composition indicated on the package or in the insert, and do not take separately those medicines that are included in it.

Antiallergic drugs for children: characteristics, principle of action, benefits and harms

Diazolin (mebhydrolin);

Peritol (cyproheptadine).

In principle, the effectiveness of the above drugs has been confirmed by many years of experience, but this same experience indicates a whole bunch of side effects:

All these drugs to a greater or lesser extent affect the central nervous system, providing sedative and hypnotic effects.

Classical antihistamines dry out the mucous membranes. Dry mouth, sputum viscosity in the lungs (which is especially dangerous in acute respiratory viral infections, as it seriously increases the risk of developing pneumonia) - does not affect the child's condition in the best way.

The simultaneous use of first-generation antiallergic drugs with other drugs enhances the effect of the use of the latter. Thus, antipyretic, analgesic, hypnotic effects are enhanced. Especially dangerous is the combination of antihistamines with other drugs that actively affect the functioning of the central nervous system. In this case, the development of side effects up to fainting is possible. The combination with alcoholic beverages is highly undesirable.

The action of such drugs, although effective, is limited to 2-3 hours (some last up to 6 hours).

Of course, it does not come without advantages. Firstly, first-generation antihistamines are relatively affordable, and secondly, they are great for short-term treatment of allergies. That is, if, for example, a child ate an excessive amount of chocolate and a short-term intake of an antihistamine is required, you can safely use the same Tavegil or Fenkarol.

Most first-generation allergy remedies are forbidden to be taken orally by nursing mothers; only their local forms can be used - ointment, cream, spray. The exception is Suprastin and Fenkarol (from three months of pregnancy). Each drug has its own characteristic feature, which is important to consider when drawing up a treatment regimen. So, it is not advisable for a baby prone to constipation to use Tavegil; a child suffering from gastrointestinal diseases is prohibited from taking Suprastin; and children with impaired liver function need to be careful with the use of Phencarol.

For babies under one year old, taking first-generation antiallergic drugs is undesirable. For the smallest, there are more modern drugs that are practically safe and very effective.

The principles of action of antihistamines, the second generation on the children's body

The undoubted advantage of antiallergic drugs of the second and third generation is the absence or minimization of the sedative, hypnotic, CNS inhibitory effect.

In addition, they have a number of other advantages: they do not penetrate the fetoplacental barrier (that is, such drugs can be used during pregnancy);

do not dry mucous membranes;

do not affect the mental and physical activity of the child;

have a quick and long-lasting (up to 24 hours) therapeutic effect - one tablet is enough to forget about allergy symptoms for the whole day;

in addition to antiallergic, they have antiemetic, antiulcer and other actions (some drugs); do not reduce their effectiveness with long-term use.

Perhaps the only drawback of second-generation antiallergic drugs is their ability to have a negative impact on the children's cardiovascular system. Due to the possible cardiotoxic effect, the use of such drugs is not recommended for children with various pathologies of the heart and blood vessels.

Among the most prominent representatives of the second generation:

Claritin (loratidin);

Allergy treatment, antihistamines

Diazolin dragee 50mg №20

Diazolin tab. 100mg #10

Suprastin (chloropyramine) is one of the most widely used sedative antihistamines. It has significant antihistamine activity, peripheral anticholinergic and moderate antispasmodic action.

Effective in most cases for the treatment of seasonal and year-round allergic rhinoconjunctivitis, angioedema, urticaria, atopic dermatitis, eczema, itching of various etiologies; in parenteral form - for the treatment of acute allergic conditions requiring emergency care. It does not accumulate in the blood serum, so it does not cause an overdose with prolonged use. The effect comes on quickly, but is short-lived; to increase its duration, it is combined with non-sedating H1-blockers.

Suprastin injection 2% 1ml amp. No. 5 (Egis, Hungary)

Suprastin tab. 25mg №20 (Egis, Hungary)

Chloropyramine g / x tab. 25mg #40

Tavegil (clemastine) is a highly effective antihistamine drug similar in action to diphenhydramine. It has a high anticholinergic activity, but penetrates the blood-brain barrier to a lesser extent.

In an injectable form, which can be used as an additional remedy for anaphylactic shock and angioedema, for the prevention and treatment of allergic and pseudo-allergic reactions. However, there is an allergy to tavegil.

Peritol (cyproheptadine), along with antihistamine, has a significant antiserotonin effect. It is often used in some forms of migraine to increase appetite.

Peritol syrup 2mg/5ml 100ml (Egis, Hungary)

Peritol tab. 4mg №20 (Egis, Hungary)

Pipolfen (promethazine) - a pronounced effect on the central nervous system, is used as an antiemetic and to potentiate anesthesia.

Pipolphen other 25mg №20 (Egis, Hungary)

Pipolfen solution for injections 50mg 2ml amp. №10 (Egis, Hungary)

Diprazine tab. 25mg #20

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

Fenkarol tab. 25mg №20 (Latvia)

Second generation antihistamines (non-sedating).

Unlike the first generation, they have almost no sedative and anticholinergic effects, do not penetrate the blood-brain barrier, do not reduce mental and physical activity, are not adsorbed with food in the gastrointestinal tract, have a high affinity for H1 receptors, and have a rapid therapeutic effect. . However, for them, a cardiotoxic effect was noted to varying degrees; when they are taken, constant monitoring of cardiac activity is required (appointed on an outpatient basis). They should not be taken by patients with disorders of the cardiovascular system, elderly patients.

The effect comes on quickly and for a longer time (delayed elimination).

When using drugs in therapeutic doses, a minimal sedative effect is observed. Some particularly sensitive individuals may experience moderate drowsiness, which does not require discontinuation of the drug.

The absence of tachyphylaxis (decrease in antihistamine activity) with prolonged use.

The cardiotoxic effect occurs due to the ability to block the potassium channels of the heart muscle, the risk of a cardiotoxic effect increases when antihistamines are combined with antifungals (ketoconazole and itraconazole), macrolides (erythromycin and clarithromycin), antidepressants (fluoxetine, sertraline and paroxetine), when drinking grapefruit juice and in patients with severe hepatic impairment.

There are no parenteral forms, only enteral and local dosage forms.

The most common second-generation antihistamines are:

Trexil (terfenadine) is the first second-generation antihistamine drug that does not have an inhibitory effect on the central nervous system, but with a significant cardiotoxic effect and an increased ability to cause fatal arrhythmias.

Trexil tab. 60mg №100 (Ranbaxi, India)

Gistalong (astemizole) is one of the longest acting drugs of the group (up to 20 days). It is characterized by irreversible binding to H1 receptors. Virtually no sedative effect, does not interact with alcohol.

Effective in chronic allergic diseases, with an acute process, its use is impractical. But the risk of developing serious heart rhythm disturbances, sometimes fatal, increases. Due to these dangerous side effects, the sale of astemizole in the United States and some other countries has been suspended.

Astemizole tab. 10mg #10

Histalong tab. 10mg №20 (India)

Semprex (acrivastine) is a drug with high antihistamine activity with a minimally pronounced sedative and anticholinergic effect. The therapeutic effect is achieved quickly, but for a short time.

Semprex caps. 8mg №24 (GlaxoWellcome, UK)

Fenistil (dimetendene) is closest to first-generation antihistamines, but differs from them in a significantly lesser sedative effect, higher antiallergic activity and duration of action than first-generation drugs. There is a gel for external use.

Claritin (loratadine) is one of the best-selling second-generation drugs. Its antihistamine activity is higher than that of astemizole and terfenadine, due to the greater strength of binding to peripheral H1 receptors.

There is no sedative effect, it does not potentiate the effect of alcohol. It practically does not interact with other drugs and does not have a cardiotoxic effect. It can be taken by drivers, children from 1 year old.

Claritin syrup 5mg/5ml 120ml (Schering-Plough, USA)

Claritin tab. 10mg №10 (Schering-Plough, USA)

Loratadine tab. 10mg #10

Agistam tab. 10mg #12

Third generation antihistamines (metabolites).

They are active metabolites of second-generation antihistamines. They do not have a sedative and cardiotoxic effect. In this regard, the drugs are approved for use by persons whose activities require increased attention.

Zyrtec, cetrin (cetirizine) is a highly selective blocker of peripheral H1 receptors. Cetirizine is almost not metabolized in the body, the rate of its excretion depends on the function of the kidneys. It penetrates well into the skin, and is effective in skin manifestations of allergies.

The effect appears 2 hours after ingestion and lasts 24 hours. Do not have a sedative and cardiotoxic effect in therapeutic doses. Be wary appoint in violation of kidney function.

Cetrin tab. 10mg No. 20 (Dr. Reddy's Laboratories, India)

Telfast (fexofenadine) is a metabolite of terfenadine. Does not metabolize in the body, does not interact with drugs, does not have a sedative effect and does not affect psychomotor activity. An effective and safest drug among antihistamines.

Telfast tab. 120mg №10 (Hoechst Marion Roussel)

Telfast tab. 180mg №10 (Hoechst Marion Roussel)

Allergy is the scourge of the XXI century. The disease, the prevalence of which has been growing rapidly in recent decades, especially in the developed countries of the world, still remains incurable. World statistics, showing the number of people suffering from various manifestations of an allergic reaction, strikes even the most daring imagination. Judge for yourself: 20% of the population annually suffer from allergic rhinitis, 6% are forced to diet and take allergy pills, about 20% of the world's inhabitants experience symptoms of atopic dermatitis. No less impressive are the numbers that reflect the number of people suffering from even more severe pathologies of allergic origin. Depending on the country of residence, about 1-18% of people cannot breathe normally due to asthma attacks. Approximately 0.05-2% of the population experience or have experienced in the past a life-threatening anaphylactic shock.

Thus, at least half of the population is faced with allergic manifestations, and it is concentrated for the most part in countries with developed industry, and, therefore, in the Russian Federation. At the same time, the help of allergists, alas, does not cover all Russians in need, which, of course, aggravates the situation and contributes to the further progression of the disease. The obviously insufficient control over the release of prescription antiallergic drugs in domestic pharmacies also contributes to the not very favorable state of affairs with the treatment of allergies in Russia. This trend contributes to aggressive self-treatment, including with the help of hormonal allergy medications, which can sometimes lead patients into a blind corner and bring the development of severe stages of the disease closer.

We have drawn such an unsightly picture not to frighten the reader. We just want every person who has encountered an allergy to understand both the severity of the disease and the prognosis in case of unsuccessful treatment, and not to rush to buy the first pills “peeped” in the commercial. We, in turn, will devote a detailed article to the description of allergies, which, we hope, will help to understand the features of the disease, its therapy and the features of various drugs used for this purpose. Understand and continue to be treated only correctly.

What is an allergy?

And we will start with the basics, without which it is impossible to understand how allergy pills work. Allergy is defined as a range of conditions caused by hypersensitivity of the immune system to a substance. At the same time, most people perceive these same substances as safe and do not react to them at all. Now let's try to describe this process in a more popular way.

Imagine an army guarding the borders of a state. She is well armed and always ready for battle. Every day, enemies try to storm the carefully controlled border, but invariably receive a worthy rebuff. One fine day, confusion occurs in the ranks of our army for unknown reasons. Her experienced and courageous warriors suddenly make a serious mistake, mistaking a friendly delegation, which has always crossed the border unhindered, for an enemy. And by this, unwittingly, they cause irreparable damage to their country.

Approximately the same events develop during an allergic reaction.

The immune system of the body, which every day is on its defense against hundreds of bacteria and viruses, suddenly begins to perceive harmless substances as mortal enemies. As a result, a military operation begins, which is too expensive for the organism itself.

How does an allergic reaction develop?

First, the body begins to produce special antibodies that are not synthesized normally - class E immunoglobulins. Looking ahead, let's say that a blood test for the presence of IgE allows you to reliably establish that a person suffers from allergies and needs medicines for it. The task of immunoglobulins E is to bind a substance that is mistaken for an aggressive toxin - an allergen. As a result, a stable antigen-antibody complex is formed, which should neutralize the enemy. However, unfortunately, it is impossible to “neutralize” without consequences in case of an allergic reaction.

The formed antigen-antibody combination settles on the receptors of special cells of the immune system called mast cells.

An antigen is a molecule that is capable of binding to an antibody.

They are located in the connective tissue. There are especially many mast cells under the skin, in the region of the lymph nodes and blood vessels. Various substances are located inside the cells, including histamine, which regulates many physiological processes in the body. However, along with a positive role, histamine can also play a negative one - it is he who is a mediator, that is, a substance that triggers allergic reactions. As long as histamine is inside the mast cells, it does not pose a danger to the body. But if an antigen-antibody complex is attached to the receptors located on the surface, the mast cell wall is destroyed. Accordingly, all the contents come out, including histamine. And then his finest hour comes, and hitherto unaware of the complex processes taking place in their bodies, citizens seriously think about what kind of pills they should buy for allergies. But there is no need to rush - you should first find out what kind of allergic reaction will take on.

What is an allergy?

And there may be several options depending on the allergen and individual sensitivity. Most often, allergies develop on the pollen of grasses and flowers. In this case, they talk about hay fever, or hay fever. Symptoms that indicate a disease and require the appointment of tablets or allergy sprays include:

  • manifestations of allergic rhinitis - runny nose, sneezing, itching in the nose, rhinorrhea;
  • manifestations of allergic conjunctivitis - lacrimation, itching in the eyes, redness of the sclera;


Much less often, treatment with tablets or ointments for allergies requires dermatitis that is allergic in nature. These include a number of diseases, including:

  • atopic dermatitis, characterized by excessive dryness and irritation of the skin;
  • contact dermatitis develops as a reaction to contact with materials that cause allergies. Most often it is latex (latex gloves), less often - metal products and jewelry;
  • urticaria, may appear due to reactions to various foods.

Severe chronic disease of allergic nature - bronchial asthma. Even more dangerous conditions associated with a risk to life are Quincke's edema and anaphylactic shock. They are immediate allergic reactions, have a fulminant onset and require immediate medical attention. Well, now let's start describing the drugs that are used to treat various types of allergies.

Antihistamines as Allergy Drugs: Popular and Economical

Means of this group are among the most well-known and commonly used drugs for the treatment of food, seasonal allergies, various dermatitis, less often - emergency conditions.

The mechanism of action of antihistamines is to block the receptors to which the main mediator of allergy, histamine, binds. They are called H1-histamine receptors, and drugs that inhibit them, respectively, blockers of H1-histamine receptors, or H1-antihistamines.

To date, three generations of antihistamines are known, used both for the treatment of allergies and for some other conditions.

Here is a list of the most famous antihistamines that are used against allergies.

Table 1. Three generations of antihistamine antiallergic drugs

First generation antihistamines

They have been used for several decades and, nevertheless, still have not lost their relevance. Distinctive features of these drugs are:

  • sedative, that is, a sedative effect. It is due to the fact that drugs of this generation can bind to H1 receptors located in the brain. Some drugs, such as Diphenhydramine, are much better known for their sedative than antiallergic properties. Other pills that could theoretically be prescribed for allergies have found use as a safe sleeping pill. We are talking about doxylamine (Donormil, Somnol);
  • anxiolytic (mild tranquilizing) action. It is associated with the ability of certain drugs to suppress activity in certain areas of the central nervous system. As a safe tranquilizer, the first generation antihistamine tablets hydroxyzine, known under the trade name Atarax, are used;
  • anti-sickness and antiemetic action. It is manifested, in particular, by diphenhydramine (Dramina, Aviamarin), which, along with the H-histamine blocking effect, also inhibits m-cholinergic receptors, which reduces the sensitivity of the vestibular apparatus.

Another distinguishing feature of first-generation antihistamine tablets for allergies is a quick, but short-term anti-allergic effect. In addition, the first generation drugs are the only antihistamines that are available in injectable form, that is, in the form of injection solutions (Diphenhydramine, Suprastin and Tavegil). And if the solution (and tablets, by the way, too) of Dimedrol has a rather weak anti-allergic effect, then the injection of Suprastin and Tavegil allows you to quickly provide first aid for an immediate type of allergy.

With an allergic reaction to insect bites, urticaria, Quincke's edema, intramuscular or intravenous Suprastin or Tavegil is used along with injection as a powerful antiallergic agent of a glucocorticosteroid drug, most often Dexamethasone.

Second generation antihistamines

Preparations of this series can be called modern new-generation allergy pills that do not cause drowsiness. Their names often appear in TV commercials and media brochures. They are characterized by several properties that distinguish among other H1-histamine blockers and antiallergic drugs in general, including:

  • rapid onset of antiallergic effect;
  • duration of action;
  • minimal or complete absence of a sedative effect;
  • lack of injection forms;
  • the ability to have a negative effect on the heart muscle. By the way, we can dwell on this effect in more detail.

Do allergy pills work on the heart?

Yes, indeed, some antihistamines can adversely affect the functioning of the heart. This is due to blockage of the potassium channels of the heart muscle, leading to a prolongation of the QT interval on the electrocardiogram and a violation of the heart rhythm.

The likelihood of developing a similar effect increases when second-generation antihistamines are combined with a number of other drugs, in particular:

  • the antifungals ketoconazole (Nizoral) and itraconazole (Orungal);
  • macrolide antibiotics erythromycin and clarithromycin (Klacid);
  • antidepressants fluoxetine, sertraline, paroxetine.

In addition, the risk of a negative effect of second-generation antihistamines on the heart increases if allergy pills are combined with the use of grapefruit juice, as well as in patients suffering from liver diseases.

Among the wide range of second-generation antiallergic drugs, several drugs should be distinguished that are considered relatively safe for the heart. First of all, it is dimethindene (Fenistil), which can be used for children from 1 month of age, as well as inexpensive loratadine tablets, which are also widely used for allergy therapy in pediatric practice.

third generation antihistamine

And finally, we come to the smallest, latest generation of drugs prescribed for allergies, from the group of H1-histamine blockers. They fundamentally differ from other drugs in the absence of a negative effect on the heart muscle against the background of a powerful anti-allergic effect, fast and prolonged action.

The drugs in this group include Cetirizine (Zyrtec), as well as Fexofenadine (trade name Telfast).

About metabolites and isomers

In recent years, two new H1-histamine blockers, which are close "relatives" of already well-known drugs of the same group, have gained popularity. We are talking about desloratadine (trade names Erius, analogues Lordestin, Ezlor, Edem, Elisey, Nalorius) and levocetirizine, which belong to a new generation of antihistamines and are used to treat allergies of various origins.

Desloratadine is the primary active metabolite of loratadine. Just like its predecessor, desloratadine tablets are prescribed once a day, preferably in the morning for allergic rhinitis (both seasonal and year-round) and chronic urticaria for the treatment of adults and children over one year old.

Levocetirizine (Xyzal, Suprastinex, Glentset, Zodak Express, Cezera) is a levorotatory isomer of cetirizine, used for allergies of various origins and types, including those accompanied by itching and rashes (dermatoses, urticaria). The drug is also used in pediatric practice for the treatment of children older than 2 years.

It should be noted that the appearance of these two drugs on the market was enthusiastically received. Many experts believed that levocetirizine and desloratadine would finally help to effectively solve the problem of insufficient response to traditional antihistamine therapy, including severe allergy symptoms. However, in fact, expectations, alas, did not materialize. The effectiveness of these drugs did not exceed the effectiveness of other H1-histamine blockers, which, by the way, is almost identical.

The choice of an antihistamine is often based on the patient's tolerance and price preferences, as well as ease of use (ideally, the drug should be used once a day, such as Loratadine).

When are antihistamines used for allergies?

It should be noted that antihistamines are distinguished by a rather large variety of active substances and dosage forms. They can be produced in the form of tablets, solutions for intramuscular and intravenous injections and external forms - ointments and gels, and all are used for various types of allergies. Let's figure out in which cases the advantage is given to one or another medicine.

Hay fever, or polynosis, food allergy

The drugs of choice for allergic rhinitis (inflammation of the nasal mucosa of an allergic nature) are allergy pills of the II or last, III generation (the full list is given in Table 1). When it comes to allergies in a small child, dimethindene (Fenistil in drops), as well as Loratadine, Cetirizine in children's syrups or solutions are often prescribed.

Skin manifestations of allergies (food, various types of dermatitis, insect bites)

In such cases, it all depends on the severity of the manifestations. With mild irritation and a small area of ​​​​lesion, external forms can be limited, in particular, Psilo-balm gel preparations (Dimedrol is included) or Fenistil gel (external emulsion). If the allergic reaction in an adult or a child is strong enough, accompanied by severe itching and / or a significant area of ​​​​the skin is affected, in addition to local drugs, tablets (syrups) for allergies of the H1-histamine blockers group can also be prescribed.

allergic conjunctivitis

With inflammation of the mucous membrane of the eye of an allergic nature, eye drops are prescribed and, with insufficient effect, tablets. The only eye drops today that contain exactly the antihistamine component are Opatanol. They contain the substance olapatadin, which provides a local anti-allergic effect.

Mast Cell Membrane Stabilizers: Allergy Pills Are Not for Everyone

Another group of allergy drugs acts by preventing calcium ions from entering mast cells and thus inhibiting the destruction of cell walls. Thanks to this, it is possible to prevent the release of histamine into the tissues, as well as some other substances involved in the development of an allergic and inflammatory reaction.

Only a few allergy remedies for this group are registered on the modern Russian market. Among them:

  • ketotifen, an allergy drug in tablets;
  • cromoglycic acid and sodium cromoglycate;
  • lodoxamide.


All preparations containing cromoglycic acid and sodium cromoglycate are conditionally called cromoglycates in pharmacology. Both active ingredients have similar properties. Let's consider them.

cromoglycates

These drugs are available in several forms of release, which, in turn, are indicated for various types of allergies.

Dosed nasal spray (Kromoheksal) is prescribed for seasonal or year-round allergic rhinitis. It is prescribed for adults and children over five years of age.

It should be noted that the noticeable effect of the use of cromoglycates in the spray occurs after one week of continuous use, reaching a peak by four weeks of continuous treatment.

Inhalations are used to prevent asthma attacks. An example of inhalation agents against allergies, which was complicated by bronchial asthma, are Intal, KromoGeksal, Kromogen Easy Breathing. The mechanism of action of drugs in such cases is aimed at interrupting the allergic reaction, which is a "trigger" in the pathogenesis of bronchial asthma.

Capsules of cromoglycic acid (KromoGeksal, Cromolyn) are prescribed for food allergies and some other diseases, one way or another associated with allergies.


Eye drops with cromoglycates (Allergo-Komod, Ifiral, Dipolkrom, Lekrolin) are the most prescribed anti-allergic drugs for conjunctivitis caused by sensitivity to plant pollen.

Ketotifen

A tableted remedy for allergies, from the group of mast cell stabilizers. Just like cromoglycates, it prevents or at least slows down the release of histamine and other biologically active substances that provoke inflammation and allergies from mast cells.

It has a fairly low price. In the Russian Federation, several preparations containing ketotifen are registered, and one of the highest quality is the French Zaditen. By the way, it is available in the form of tablets, as well as syrup for children and eye drops, which are prescribed for allergies of various origins and types.

It should be borne in mind that Ketotifen is a drug that exhibits a cumulative effect. With its constant use, the result develops only after 6-8 weeks. Therefore, Ketotifen is prescribed preventively, for the prevention of allergies in bronchial asthma, allergic bronchitis. In some cases, cheap Ketotifen tablets are used to prevent the development of seasonal allergic rhinitis, as indicated in the instructions for the drug. However, it is important to start taking the medication in advance, ideally at least 8 weeks before the expected start of the allergen bloom, and, of course, not stop the course of therapy until the season is over.

lodoxamide

This active substance is produced as part of eye drops, which are prescribed for allergic conjunctivitis, Alomida.

Glucocorticosteroids in tablets and injections in the treatment of allergies

The most important group of drugs that are used to relieve the symptoms of allergies are steroid hormones. Conventionally, they can be divided into two large subgroups: local agents that are used to irrigate the nasal cavity, tablets and injections for oral administration. There are also eye and ear drops with corticosteroids, which are used for ENT pathologies of various origins, including allergic conjunctivitis and otitis media, as well as ointments and gels sometimes used to treat allergic dermatitis. However, in the treatment of these diseases, corticosteroids are far from the first place: rather, they are prescribed as a means of temporary relief, for the rapid relief of symptoms, after which they switch to therapy with other antiallergic drugs. Means for local (nasal sprays) and internal use (tablets), on the contrary, are used quite widely for the treatment of various diseases of an allergic nature, and it is worth talking about them in more detail.

The difference between these categories of drugs, first of all, is tolerability. If local and external preparations have close to zero bioavailability and are practically not absorbed into the systemic circulation, exerting only an effect at the site of application (application), then injection and tablet preparations, on the contrary, penetrate the blood in the shortest possible time, and, therefore, exhibit systemic effects. Therefore, the safety profile of the first and second is fundamentally different.

Despite such significant differences in the characteristics of absorption and distribution, the mechanism of action of both local and internal glucocorticosteroids is the same. Let's talk in more detail, due to which tablets, sprays or ointments containing hormones have a therapeutic effect in case of allergies.

Hormonal steroids: mechanism of action

Corticosteroids, glucocorticosteroids, steroids - all these names describe a category of steroid hormones that are synthesized by the adrenal cortex. They exhibit a very powerful triple healing effect:

Due to these abilities, corticosteroids are indispensable drugs used for a wide variety of indications in different fields of medicine. Among the diseases in which corticosteroid preparations are prescribed are not only allergies, regardless of origin and type, but also rheumatoid arthritis, osteoarthritis (with a pronounced inflammatory process), eczema, glomerulonephritis, viral hepatitis, acute pancreatitis, as well as shock, including anaphylactic.

However, unfortunately, despite the severity and variety of therapeutic effects, not all glucocorticosteroids are equally safe.

Side effects of hormonal steroids

It was not for nothing that we immediately made a reservation about the different safety profile of glucocorticosteroids for internal and local (external) use.

Oral and injectable hormonal preparations have many side effects, including serious ones, sometimes requiring drug withdrawal. We list the most common of them:

  • headache, dizziness, blurred vision;
  • hypertension, chronic heart failure, thrombosis;
  • nausea, vomiting, gastric ulcer (duodenal ulcer), pancreatitis, loss of appetite (both improvement and deterioration);
  • decreased function of the adrenal cortex, diabetes mellitus, menstrual irregularities, growth retardation (in childhood);
  • muscle weakness and/or pain, osteoporosis;
  • acne disease.

“Good,” the reader will ask. “Why are you describing all these terrible side effects?” Just so that a person who is going to treat allergies with the same Diprospan thinks about the consequences of such a “treatment”. Although this should be discussed in more detail.

Diprospan for allergies: a hidden danger!

Many experienced allergy sufferers know: the introduction of one (two, or even more) ampoules of Diprospan or its analogue, for example, Flosteron or Celeston, saves from severe symptoms of seasonal allergies. They advise this "magic remedy" to acquaintances and friends who are desperate to find a way out of the allergic vicious circle. And they do them oh what a disservice. “Well, why bearish? - the skeptic will ask. “It’s getting easier, and fast.” Yes, it does, but at what cost!

The active substance of Disprospan ampoules, which are often used to relieve allergy symptoms, including without a doctor's prescription, is a classic glucocorticosteroid betamethasone.

It exhibits a powerful and rapid anti-allergic, anti-inflammatory and antipruritic effect, indeed in a short time alleviating the condition with allergies of various origins. What happens next?

The further scenario largely depends on the severity of the allergic reaction. The fact is that the effects of Diprospan cannot be called long-term. They can last for several days, after which their severity weakens and finally disappears. A person who has already managed to feel a significant relief of allergy symptoms naturally tries to continue the “treatment” with another Diprospan ampoule. He does not know or does not think about the fact that the likelihood and severity of side effects of glucocorticosteroids depend on their dose and frequency of use, and, therefore, the more often Diprospan or its analogues are administered to correct allergy manifestations, the higher the risk of experiencing the full force of its side effect. actions.

There is another extremely negative side of the use of glucocorticosteroids for internal use in seasonal allergies, which most patients have no idea about - a gradual decrease in the effect of classic anti-allergic tablets or sprays. Applying Diprospan, especially from year to year, regularly during the manifestation of allergies, the patient literally leaves no alternative for himself: against the background of a strong, powerful effect shown by an injectable glucocorticosteroid, the effectiveness of antihistamine tablets and, especially, mast cell membrane stabilizers, decreases catastrophically. The same picture persists after the end of the action of steroids.

Thus, a patient who uses Diprospan or its analogues to alleviate allergy symptoms practically dooms himself to constant hormone therapy with all its side effects.

That is why doctors are categorical: self-medication with injectable steroids is dangerous. "Passion" for drugs of this series is fraught not only with resistance to therapy with safe drugs, but also with the need for a constant increase in the dose of hormones to achieve an adequate effect. However, in some cases, treatment with corticosteroids is still necessary.

When are steroid pills or injections used to treat allergies?

First of all, tablets or injections of Dexamethasone (less often, Prednisolone or other glucocorticosteroids) are used to stop an acute allergic reaction. So, with anaphylactic shock or Quincke's edema, it is advisable to administer the hormone intravenously, in less urgent cases - intramuscularly or orally. In this case, the doses of the drug can be high, approaching the highest daily or even exceeding it. Such a tactic justifies itself with a single use of drugs, one or two times, which, as a rule, is sufficient to obtain the desired effect. In such cases, you should not be afraid of the notorious side effects, because they begin to manifest themselves in full force only against the background of a course or regular administration.

There is another important indication for the use of hormones in tablets or injections as drugs for the treatment of allergies. These are severe stages or types of the disease, for example, bronchial asthma in the acute stage, severe allergies that are not amenable to standard therapy.

Hormone therapy for allergic diseases can only be prescribed by a doctor who is able to evaluate both the benefits and risks of treatment. He carefully calculates the dose, controls the patient's condition, side effects. Only under the vigilant supervision of a doctor, corticosteroid therapy will bring real results and will not harm the patient. Self-medication with hormones for oral administration or injection is strictly unacceptable!

When should you not be afraid of hormones?

As dangerous as glucocorticosteroids can be for systemic use, steroids intended for injection into the nasal cavity are just as innocent drugs. Their field of activity is limited exclusively to the mucous membrane of the nasal cavity, where they, in fact, should work in the case of allergic rhinitis.

“However, some of the medicine can be accidentally swallowed!” - the meticulous reader will say. Yes, this possibility is not excluded. But in the gastrointestinal tract, the absorption of intranasal steroids (absorption) is minimal. Most of the hormones are completely "neutralized" when passing through the liver.

Having an anti-inflammatory and powerful anti-allergic effect, nasal corticosteroids quickly stop the symptoms of allergies, stopping the pathological reaction.

The effect of intranasal steroids appears 4-5 days after the start of therapy. The peak effectiveness of this group of drugs for allergies is achieved after a few weeks of continuous use.

Today, there are only two hormonal corticosteroids on the domestic market, which are available in the form of intranasal sprays:

  • Beclomethasone (trade names Aldecin, Nasobek, Beconase)
  • Mometasone (trade name Nasonex).

Beclomethasone preparations are prescribed for the treatment of mild to moderate allergies. They are approved for use by children over 6 years of age and adults. As a rule, beclomethasone is well tolerated and does not cause side effects. However, in some (fortunately extremely rare) cases, especially with long-term treatment, damage (ulceration) of the nasal septum is possible. To minimize its risk, it is necessary, when irrigating the nasal mucosa, not to direct the jet of the drug to the nasal septum, but to spray the medicine on the wings.

Occasionally, the use of beclomethasone spray can lead to minor nosebleeds, which is not dangerous and does not require discontinuation of the drug.

"Heavy artillery"

I would like to pay special attention to the next representative of hormonal corticosteroids. Mometasone is recognized as the most powerful drug for the treatment of allergies, which, along with very high efficacy, has an extremely favorable safety profile. Mometasone, the original Nasonex spray, has a powerful anti-inflammatory and anti-allergic effect, practically not being absorbed into the blood: its systemic bioavailability does not exceed 0.1% of the dosage.

The safety of Nasonex is so high that in some countries of the world it is approved for use in pregnant women. In the Russian Federation, mometasone is officially contraindicated during pregnancy due to the lack of clinical studies studying its use in this category of patients.

It should be noted that not a single tablet or spray that is used to treat allergies in a wide range of patients is approved for use during pregnancy - expectant mothers suffering from hay fever or other types of allergies are advised to avoid the action of the allergen, for example, leaving for another climatic zone at the time of flowering. And to the frequent question: which allergy pills can be taken during pregnancy, there is only one correct answer - none, during this crucial period you will have to do without medication. But the nursing ones were more fortunate. For allergies while breastfeeding, you can take some pills, but before starting treatment, it is better to consult a doctor.

But the drug is widely used in pediatric practice for the treatment and prevention of allergies in children over the age of 2 years.

Mometasone begins to act 1-2 days after the start of treatment, and its maximum effect is achieved after 2-4 weeks of continuous use. The drug is prescribed for the prevention of seasonal allergies, starting to irrigate the nasal mucosa a few weeks before the expected period of pollination. And, of course, mometasone is one of the most "favorite" and frequently prescribed drugs for the treatment of allergies. As a rule, treatment with them is not accompanied by side effects, only in rare cases, dryness of the nasal mucosa and the occurrence of minor nosebleeds may occur.

Allergy treatment with pills and more: a stepwise approach

As you can see, there are quite a lot of drugs with anti-allergic properties. Most often, patients select pills for the treatment of allergies, based on the reviews of friends, advertising statements that sound on TV screens and pour from the pages of magazines and newspapers. And, of course, it is quite difficult to get in this way “with a finger in the sky”. This leads to the fact that a person suffering from allergies seems to be treated by taking pills or a spray, but does not see the result and continues to suffer from a runny nose and other symptoms of the disease, complaining that the medicines do not help. In fact, there are quite strict rules of treatment, the observance of which largely depends on the effectiveness.

First of all, the treatment regimen for allergies (we will speak on the example of its most common form, allergic rhinitis) is based on an assessment of the severity of the disease. There are three levels of severity: mild, moderate and severe. What drugs are used for each of them?

  1. Step one.
    Treatment of mild allergies.

    As a rule, therapy begins with the appointment of an antihistamine of the II or III generation. Most often, Loratadine (Claritin, Lorano) or Cetirizine (Cetrin, Zodak) tablets are used as first-line drugs for allergies. They are quite inexpensive and easy to use: they are prescribed only once a day. In the absence of a clinical effect or an insufficient result, they proceed to the second stage of allergy therapy.
  2. Step two.
    Treatment of moderate allergies.

    An intranasal corticosteroid (Baconase or Nasonex) is added to the antihistamine.
    If symptoms of allergic conjunctivitis remain during treatment, antiallergic eye drops are prescribed. Insufficient effect on the combined treatment regimen is the basis for more thorough diagnosis and therapy, which should be dealt with by an allergist.
  3. Step three.
    Treatment of severe allergies.

    Additional drugs may be added to the therapy regimen, for example, leukotriene receptor inhibitors (Montelukast). They block the receptors to which inflammatory mediators bind, thus reducing the severity of the inflammatory process. The target indication for their appointment is bronchial asthma, as well as allergic rhinitis. In very severe cases, systemic glucocorticosteroids are introduced into the therapy regimen. If even then the result is not achieved, a decision is made on the need for allergen-specific immunotherapy and other methods of treatment. Only an experienced doctor should prescribe treatment. The lack of medical care in such situations can lead to uncontrolled progression of allergies and the development of its extremely severe form, bronchial asthma.

Thus, the selection of tablets, sprays and other anti-allergy products is not as easy as it seems after watching the next commercial. To choose the right scheme, it is better to use the help of a doctor or at least an experienced pharmacist, and not rely on the opinion of a neighbor or girlfriend. Remember: with allergies, as with most other diseases, the doctor's experience, individual approach and thoughtful solutions are important. Subject to these conditions, you will be able to breathe easily and freely all year round, forgetting about the endless runny nose and other allergic "joys".

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 oral administration, 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, Cetrin, 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: in 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.