Allergy treatment. Review of third generation antihistamines

Antihistamines — pharmacological group agents that inhibit the action of free histamine. First, let's look at what it is from a medical point of view in professional language, this will help you understand what applies to such medications. Then we will see a simple explanation and examples.

Histamine is a mediator in the development of allergic reactions. It exerts its effect through its influence on H1, H2, H3 receptors located in smooth muscles internal organs and vessels. The level of development of histamine actions is directly proportional to the amount of the released mediator, which means that the more histamine is released, the more pronounced the allergic reaction.

The effect of medications in the body of patients

H1 receptors are found in the muscles of the respiratory system and blood vessels. The mechanism of action of histamine on H1 receptors is mediated through a cascade of reactions associated with the stimulating effect of extracellular calcium, which, when entering the cell, causes contraction smooth muscle.

Affects the lungs, causing contraction of the bronchial muscles. This leads to a narrowing of the airway lumen up to its complete obstruction. The situation is aggravated by inflammation of the mucous membrane, which further closes the lumen of the bronchus. By influencing mucus-secreting cells, histamine causes increased secretion of fluid and electrolytes into the bronchial lumen. This process provokes the development of pulmonary edema, which can be fatal.

According to a similar scheme, the effect of histamine on the trachea and uterus is realized, provoking contractions of its muscles and swelling.

The effect on blood vessels is characterized by a dilating (expanding) direction, mediated through the activation of phospholipase A2. The enzyme increases the capillary permeability of the walls of blood vessels and causes the release of fluid from microvasculature into the interstitial (intertissue) space with the development of edema. The arachidonic acid cascade is also activated. As this process develops, the connective tissue loses its density, and interstitial edema intensifies even more.

Consequently, the binding of histamine to H1 receptors causes in most cases the development of allergies.

The mechanism of action of antihistamines is associated with blocking H1 receptors instead of histamine. This process is possible due to the biochemical similarity of histamine molecules and drugs of this group. Drugs bind to histamine-tropic receptors, and the released endogenous histamine remains unbound. Thus, the influence of the mediator is blocked, and the caused processes do not develop.

Thus, pharmacological actions can be distinguished. These include:

• antipruritic (tissue swelling causes irritation of nerve endings, which is eliminated under the influence of drugs);
• decongestant;
• bronchodilator (implemented due to anticholinergic effects);
• sedative;
• local anesthetic;
• antiallergic.

Of course, most people want to know antihistamines - what they are in simple words, what they mean for patients.

Simply put, these are products that are aimed at combating allergies. They eliminate allergy symptoms and alleviate the human condition.

Generations of drugs for allergic insidiousness

The classification of antihistamines divides them by generation. Knowing this helps you understand what allergy medications are and which of them are the most effective.

1st generation medications are the very first medications in this group. They selectively bind to H1 receptors, blocking the action of free histamine. Due to their lipophilic structure, they also block serotonin and m-cholinergic receptors. This causes their undesirable effects associated with a sedative effect on the body.

List of 1st generation drugs that are used most often:

• Suprastin;
• Diphenhydramine;
• Tavegil.

Their benefit occurs within 30 minutes after administration, but the effect is quite short-lived, ranging from 4 to 12 hours. This is due to their rapid excretion from the body in urine.

Due to good absorption from the gastrointestinal tract, many of them are available in tablet form. Also, medications have the ability to penetrate the blood-brain barrier and placenta, and can be excreted in breast milk.

This generation is usually called sedative due to a side symptom. Given their ability to penetrate the blood-brain barrier, antihistamines are able to influence serotonin receptors in the brain. Blockade of central serotonin receptors leads to inhibition processes in the central nervous system, which determines the calming effect of drugs. Depending on the strength of the drug, this effect may be dominant. Doxylamine, a member of the antihistamine group, is used as a sedative.

Due to the severity of central nervous system inhibition, medications in this group should not be used in a state of alcoholic intoxication or together with sedatives and sedatives, as the effect may be potentiated.

2nd generation drugs are newer and more advanced. They block H1 receptors more specifically and do not have m-cholinergic and serotonin effects. Therefore, they are free from side effects associated with CNS inhibition. This makes it possible to prescribe drugs from group 2 to patients without limiting their ability to work. They also have a low degree of cardiotoxicity.

The prolonged effect of drugs is associated with their longer accumulation in the body. The effect is achieved after 1-2 hours and lasts up to 24 hours. Excretion of metabolic products occurs through the kidneys. Due to prolonged accumulation, the substance can accumulate in the body. Terfenadine is completely eliminated only 12 days after the last dose. This property is used when outpatient treatment urticaria, hay fever, rhinitis.

The list of the most popular means from group 2 are:

• Claritin;
• Fenistil;
• Histimet;
• Allergodil.

One of the disadvantages of second-generation antihistamines is the lack of parenteral forms. Most are sold as enteral tablets and some as topical ointments.

The official classification indicates two groups of antihistamines. The third group of pharmacologically active metabolites in pharmaceuticals is presented as the 3rd generation of H1` histamine blockers.

For those who are interested in the best drugs of the 3rd and 4th generations, as well as new drugs of the unique 5th generation, it is important to remember that this is an advertising ploy designed to attract more buyers. There are no 4th and 5th generation antihistamines. Here is a short list of drugs of group 3, which can represent both the fourth and fifth generation:

• Levocetirizine;
• Desloratadine;
• Fexofenadine.

The main thing is to know that medicines that go beyond the first two generations are the best modern drugs from allergies. The high bioavailability of drugs contributes to the rapid development of the therapeutic effect (within 30 minutes). The selectivity of action completely eliminates the effect of cardiotoxicity, which is extremely important for patients with cardiac disorders. The absence of drowsiness allows patients taking medications to remain functional. List of drugs latest generation wider, but they should also be prescribed by a doctor.

Forms of drugs with the desired result

Antihistamines exist in the main pharmacological forms:

• pills;
• locally acting agents (and gels);
• parenteral agents for intravenous administration.

Application depends on the form. Tablets (Loratadine, Suprastin, Diphenhydramine) are prescribed to patients with allergic diseases to prevent relapses and treat chronic processes. They are prescribed in a certain dose at regular intervals to maintain the antiallergic effect.

Parenteral antiallergic drugs are more often used in emergency situations in a hospital with the development of anaphylactic shock and Quincke's edema. Due to the rapid onset of benefits (instant blockade of histamine receptors), antihistamines in ampoules are the primary drugs of choice.

Ointments and gels (Fenistil, Dermadrin) are prescribed to relieve local inflammatory processes. Most of them are used for their antipruritic effect. The effect is achieved by rubbing into skin. The effect occurs within an hour and lasts 3-5 hours.

Other forms are also used in pediatrics. They are designed for ease of administration to children:

• rectal suppositories;
• eye drops (Fenistil, Zyrtec);
• syrups (Claritin);
• drops in the nose.

Medicines for children for painful passions

Prescriptions for children are made by a pediatrician. You should not give your child medications yourself. This is due to a large number side symptoms, caused by high concentrations of conventional (adult) drugs.

Suprastin and Diphenhydramine are prescribed:

• injection for children under 1 year of age only for health reasons, the concentration of the drug is chosen by the pediatrician;
• 1-6 years - a quarter of a tablet 3 times a day;
• 6-10 years - half a tablet 3 times a day;
• 10+ - prescribed 1 tablet 3 times a day.

Claritin:

• children weighing less than 30 kg - 1 scoop;
• more than 30 kg - 2 measuring spoons;
• tablets are allowed from 4 years of age.

• one of the safest drugs for treating allergies;
• children under one year old - 2.5 ml;
• from 5 to 10 years - 5 ml;
• 10+ years - 10 ml.

For any reason side effects You should definitely consult your doctor.

Choosing products for pregnant women in advance

During pregnancy, the medicine affects not only the mother, but also the fetus. This is especially true for antihistamines of the first two generations, since they are able to penetrate the placenta, affecting the baby in the womb. In addition, histamines of the first groups have a wide range of side effects. Therefore, they are prescribed only for health reasons.

New generation antiallergic drugs are less embryotoxic due to their peripheral specific effects and they do not have a hypnotic effect. You should be especially wary of antihistamines prescribed in the 1st trimester of pregnancy. This is due to the greatest impact on the fetus in this period. The last two trimesters are more favorable in relation to appointments. A few examples:

1. Cetirizine. Belongs to the third group. Pregnancy is not a contraindication for prescribing the drug. Numerous tests have proven the absence of teratogenic effects on the fetus.
2. Telfast(second generation). The drug is prescribed by the attending physician under his supervision. Use in the 1st trimester of pregnancy is highly undesirable due to side symptoms.
3. Suprastin(first group). It is prescribed only for health reasons when assessing the harm and benefits of the drug in the 2nd and 3rd trimesters.

Proper use is the key to successful treatment

Even the best antihistamine will not bring the expected effect if it is used incorrectly. Antihistamines are in most cases sold in pharmacies without a prescription. It is important to note that self-treatment may lead to the development unwanted effects. To prevent them, you must follow some rules:

1. Before starting use, you should consult your doctor. He will prescribe the most correct and successful treatment.
2. You should not take medications of the first groups for more than 7 days unless your doctor advises using them longer, as they begin to accumulate in the body, which can lead to the development side symptoms. Medicines of the last group should not be used for more than a year.
3. During treatment, if side effects occur or worsen, you should consult your doctor.

Examples of effective antihistamines

The table shows a list of names popular drugs for adults.

Name	Generation	Price, rub	Peculiarities
Suprastin	1	85-146	Rapid onset of benefit and its short duration
Diphenhydramine	1	1,8-9	Strong sedative effect. Dries out the skin and mucous membranes. Anesthetic effect.
Claritin	2	170-200	High antihistamine activity. There is no drowsiness and potentiation effect. Can be combined with many drugs.
Desloratadine	3	130-160	High activity. Lack of sedative and cardiotoxic effects. Valid throughout the day. The benefit occurs within 30 minutes.
Tsetrin	3	150-200	High activity. Lack of sedative and cardiotoxic effects. Valid for 24 hours.

Comparing popular means

For those who are interested in which is better – Erius or Kestin, it is important to remember that they belong to the 2nd group of antihistamines. The active ingredient of Erius is loratadine, and Kestina is ebastine. The main difference is that the antihistamine effect of Erius is many times stronger. It can also be given infants, and the effect occurs within 10 minutes after administration. Erius is available in the form of syrup and tablets, while Kestin is available only in tablets.

Now let’s look at what is better – Fenkarol or Loratadine. Fenkarol belongs to the initial generation. Due to its lipophilic structure, it does not penetrate the BBB, like its generation brothers. Because of this, the sedative effect is not pronounced. A significant advantage over Loratadine and other drugs is its antiarrhythmogenic effect, while 2nd generation drugs can cause arrhythmic changes in the heart.

It's time to find out whether Tavegil or Zyrtec is better for allergies. Tavegil has a pronounced sedative effect, so its use is sharply limited. After taking it, there may be a decrease in performance, lethargy, and drowsiness. The advantage is the possibility of parenteral administration with acute allergies. Zyrtec does not have this disadvantage. He also has more long-term action and the lack of weakening of the anti-inflammatory effect over time.

Regarding which medicine is better - Fenkarol or Suprastin, it is worth clarifying that they are from the same group - the first. However, due to the difference in chemical composition their effects are different. Suprastin has a whole range of side effects, including a pronounced sedative effect. Fenkarol does not have these disadvantages due to its inability to penetrate the BBB. It also does not have a pronounced cardiotoxic effect, but has an antiarrhythmic effect.

To find the most powerful allergy remedy for a specific patient, you need to consult a doctor. He will tell you not only which drugs are antihistamines, but which ones are best for eliminating the observed symptoms.

Today we will talk about:

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

1st generation antihistamines

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

1st generation antihistamines are characterized by the following pharmacological properties:

Reduce muscle tone;
have a sedative, hypnotic and anticholinergic effect;
potentiate the effects of alcohol;
have a local anesthetic effect;
give a quick and strong, but short-term (4-8 hours) therapeutic effect;
long-term use reduces antihistamine activity, so the drugs are changed every 2-3 weeks.

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

The anticholinergic properties of these drugs cause atropine-like reactions, such as tachycardia, dryness of the nasopharynx and oral cavity, urinary retention, constipation, and blurred vision. These features can be beneficial for rhinitis, but can increase airway obstruction caused by bronchial asthma (the viscosity of sputum increases) and contribute to the exacerbation of prostate adenoma, glaucoma and other diseases. At the same time, these drugs have an antiemetic and anti-sickness effect, reducing the manifestation of parkinsonism.

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

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

Diphenhydramine

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

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

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

Diazolin

Diazolin has the same indications for use as other antihistamines, but differs from them in the characteristics of their effects.

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

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

Suprastin

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

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

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

Tavegil

Tavegil in injection form is used for angioedema, as well as anaphylactic shock, as a preventive and therapeutic agent for allergic and pseudo-allergic reactions.

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

Cons: may itself cause an allergic reaction, has some inhibitory effects.

Fenkarol

Fenkarol is prescribed when addiction to other antihistamines occurs.

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

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

Antihistamines 2nd generation

They have advantages compared to first generation drugs:

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

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

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

Claridol

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

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

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

Clarisens

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

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

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

Clarotadine

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

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

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

Lomilan

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

Advantages: Lomilan is able to relieve itching, reduce the tone of smooth muscles and the production of exudate (a special liquid that appears when inflammatory process), prevent tissue swelling within half an hour from the moment of taking the drug. The greatest effectiveness occurs after 8-12 hours, then subsides. Lomilan is not addictive and does not have any negative impact on the activity of the nervous system.

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

LauraHexal

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

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

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

Claritin

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

Advantages: highly effective in the treatment of allergic diseases, the drug does not cause addiction or drowsiness.

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

Rupafin

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

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

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

Kestin

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

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

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

New, 3rd generation antihistamines

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

All 3rd generation antihistamines do not have cardiotoxic or sedative effects, so they can be used by people whose activities involve high concentration of attention.

These drugs block H1 receptors and also have additional influence for allergic manifestations. They are highly selective, do not cross the blood-brain barrier, and therefore are not characteristic of negative consequences from the central nervous system, there is no side effect on the heart.

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

Gismanal

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

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

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

Trexil

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

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

Telfast

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

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

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

Zyrtec

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

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

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

Antihistamines for children

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

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

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

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

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

Negative consequences:

1st generation: headache, constipation, tachycardia, drowsiness, dry mouth, blurred vision, urinary retention and lack of appetite;
2nd generation: negative influence on the heart and liver;
3rd generation: none, recommended for use from 3 years of age.

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

Antihistamines during pregnancy

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

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

The safest antihistamines are Claritin, Zyrtec, Telfast, Avil, but their use should also be mandatory agreed with the doctor.

To understand what antihistamines are, you need to understand what histamines are and how antihistamines act on them.

Histamines are substances contained in the so-called “mast cells”. After contact with an allergen, histamines are released from mast cells in order to neutralize the provoking substance. It is histamines that affect the penetrating ability of blood vessels and cause the manifestation of all known symptoms allergies (itching, swelling, redness, watery eyes, blisters, rashes, etc.) There are three types of receptors that, when reacting to a compound with histamine, have different effects:

1. H1 receptors. When combined with histamine, they cause itching, bronchopulmonary spasms, and increase the permeability of vascular walls.

2. H2 receptors. They respond to histamines by relaxing the muscles of the uterus, increasing gastric secretion, and increasing contractility myocardium.

3. H3 receptors. They are able to inhibit the production of histamine and prevent it from entering the nervous system.

Now it will be much easier to understand what antihistamines are and exactly how they work.

Mechanism of action

Antihistamines are substances that have the property of blocking (inhibiting) the sensitivity of receptors to histamine and stopping acute immune reaction. Various substances aimed at inhibiting different types receptors and accordingly have various fields Applications:

• H1 blockers. Relieves allergy symptoms;
• H2 blockers. Helps reduce gastric secretion and is used in the treatment of stomach diseases;
• H3 blockers. Used in the treatment of diseases of the central nervous system.

Medicines containing H1 receptor inhibitors were invented back in 1936 and have been constantly improved since then. Today there are antihistamines of the 1st, 2nd and 3rd generations.

First generation antihistamines

The main advantage of first generation drugs is the ability to quickly stop the immune reaction. At the same time, the effect does not last long - about 4-6 hours.

The main disadvantage is the ability to penetrate the blood-brain barrier. As a result, depression of the central nervous system occurs. The sedative effect can vary in severity and manifests itself in such signs as: drowsiness, loss of attention, apathy. Psychomotor agitation is also possible.

The sedative effect of first generation drugs causes contraindications for use for people whose activities require special care or involve high physical activity.

Among the side effects:

• weakness;
• headache;
• nausea, vomiting;
• changes in stool;
• dry mucous membranes;
• fall blood pressure;
• muscle weakness;
• drowsiness;
• arrhythmia.

Almost every one of us actually knows what first generation antihistamines are. They are the most accessible, widespread and are often used for emergency relief from allergy symptoms, treatment of allergies of unknown origin, to relieve itching and reduce skin reactions, for allergic rhinitis, motion sickness, migraines, and asthma.

First generation drugs are addictive, so long-term use is unacceptable. The course of treatment cannot exceed 7-10 days.

In the first generation group: “Suprastin”, “Daizolin”, “Diphenhydramine”, “Tavegil”, “Fenkarol”.

II generation antihistamines

Second generation drugs are more advanced and do not have an inhibitory effect on the central nervous system. The antihistamine effect occurs quickly and lasts 24 hours, that is, a single dose per day is sufficient.

The main disadvantage is the cardiotoxic effect. Second generation antihistamines are capable of blocking potassium channels in the heart muscle. As a consequence, disruptions in the functioning of the heart. This effect is enhanced by concurrent use of antidepressants, macrolides, antifungal drugs, grapefruit juice.

II generation drugs are not prescribed to older people, patients with heart disease, or people with pronounced violations in liver function.

Possible side effects:

• dry mucous membranes;
• nausea and vomiting;
• anxiety;
• depression;
• stool disorders;
• headache;
• gastritis.

Second generation antihistamines are used in the treatment of allergic rhinitis, eczema, and atopic diseases.

The duration of treatment can be up to 12 months.

The group of drugs of the second generation includes: Loratadine, Fenistil, Claritin, Lomilan, Cladidol, Rupafin, etc.

III generation antihistamines

What are third generation antihistamines? These are special substances - metabolic products of second generation drugs, the so-called “active metabolites”. Metabolites do not have the disadvantages of I and II generation drugs: CNS depression and cardiotoxic effects are eliminated, negative effects on the liver, kidneys and gastrointestinal tract are eliminated.

Active metabolites are acceptable for use in a wide range of patients for treatment allergic conjunctivitis, rhinitis, hay fever, atopic dermatitis, urticaria, eczema, asthma.

Side effects are practically reduced to zero. However, occasionally it is possible:

• headache;
• muscle pain;
• weakness;
• gastritis;
• nausea, vomiting;
• arrhythmia;
• dry mucous membranes.

III generation drugs are acceptable for use on an ongoing basis.

Contraindications for taking metabolites are pregnancy, early childhood, and individual intolerance to any of the components.

The group of metabolites includes the following drugs: Zyrtec, Telfast, Erius.

Medicines for children

Most antihistamines are contraindicated for use in early childhood. However, it is infants who are often susceptible. Therefore, only an experienced specialist should select a medicine.

For quick disposal For allergy symptoms in early childhood, it is permissible to take first generation drugs. To eliminate skin manifestations, it is possible to use antihistamine ointments and creams.

During the entire course of taking antihistamines, the child’s condition should be carefully monitored and if adverse reactions occur, you should immediately seek medical help!

Only a specialist knows in detail what antihistamines are, and only an experienced allergist can choose the drug and dosage that is right for you. Self-medication can lead to irreparable consequences!

Choosing a competent specialist

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

Answer: It is better to undergo tests for allergens on the device "Imedis Expert" and further exclude contacts with identified bioresonance test allergens. Also, if possible, be treated by a bioresonance therapist and for many years take homeopathic and bioresonance medications prescribed during the treatment of bioresonance therapy, as well as during exacerbations or during the allergic season, take new generation antihistamines selected by a bioresonance test or pendulum.

You need to take new generation antihistamines once a day until allergy symptoms disappear. If contact with the allergen cannot be avoided, then you will have to take an antihistamine (anti-allergy drug) every day, unfortunately there is no escape from this. When contacting an allergen without an antiallergic drug, a severe allergic reaction can develop, which in turn can lead to death, coma, and the allergy can also develop into asthma.

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

Of course, pills are not candy, and antihistamines are no exception. In a state of reaction, do not try to do without them. In any case, allergens will need to be removed from the body in 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 reduce the reaction of the human body with a special mediator histamine. What are these medications taken for? Doctors prescribe their use during allergic reactions. Having good antipruritic, antispastic, antiserotonin and local anesthetic effects, antihistamines are excellent for allergies, and also effectively prevent bronchospasms caused by histamine.

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

Generations of antihistamines

First generation antihistamines

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

Drowsiness and decreased tone may occur, which means it is impossible to take these drugs while driving a car or other activities that require high concentration attention. They also enhance the effect of taking other sedatives, hypnotics and painkillers. The effect of alcohol mixed with sedatives is also intensifying. Most first generation antihistamines are interchangeable.

Their use is advisable when allergic problems arise with respiratory system, for example, with a cough or nasal congestion. It is worth paying attention to the fact that antihistamines belonging to the first generation are good at fighting cough. This makes it advisable to use them for bronchitis.

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

suprastin

diphenhydramine

diazolin

tavegil

You can also often find peritol, pipolfen and fenkarol on sale.

Second generation antihistamines

2nd (second) generation drugs are called non-sedatives. They do not have such a large list of side effects as the drugs that make up the first generation of antihistamines. These are medications that do not cause drowsiness or reduce brain activity, and do not have anticholinergic effects. Good effect gives their use for 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 in outpatient setting. Under no circumstances 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 medications includes:

cetrin

Zyrtec

telfast

These drugs do not have a cardiotoxic effect, unlike second-generation drugs. Their use gives positive effect for 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 medications are the most effective and harmless antihistamines. They are non-addictive, safe for the cardiovascular system, and also have long period actions. They are classified as the fourth generation of antihistamines.

Fourth generation antihistamines

4th (fourth) generation drugs have a small list of contraindications, which mainly include 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 they produce more medications that can be purchased at a pharmacy if necessary. These include erius, xysal, lordestin and telfast.

Release forms of antihistamines

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

Treatment of children with antihistamines

As is known, children are more susceptible to allergic diseases than adults. A qualified allergist should select and prescribe medications for children. Many of them have children in their list of contraindications, so if necessary, they must be used with particular care when planning a course of treatment. Children's bodies can react quite sharply to the effects of the medicine, so the child's well-being during the period of their use must be monitored very carefully. If side effects occur, you should immediately stop taking the drug and consult a doctor.

Both somewhat outdated medications and more modern ones are suitable for treating children. The drugs included in the first generation are mainly used for urgent relief of acute allergy symptoms. During long-term use, more modern means are usually used.

Antihistamines are usually not available in special “children’s” forms. The same medications are used to treat children as for adults, but in smaller doses. Drugs such as Zyrtec and ketotifen are usually prescribed from the time the child reaches the age of six months, all others - from two years. Do not forget that a child should take medications under the supervision of an adult.

In case of illness small child the selection of antihistamines becomes 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 condition of the child’s body, the doctor may prescribe him to take Tavegil or Fenkarol, and in case of an allergic skin reaction, an antihistamine cream. The same medications are suitable for infants as for newborns.

Antihistamines during pregnancy and lactation

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

Unintentional penetration of the medicine into the child’s body is possible not only during pregnancy, but also during breastfeeding. During lactation, the use of antihistamines is extremely undesirable and is prescribed only in the most in case of emergency. The question of what product a nursing woman will use can only be decided by a doctor. Even the newest and modern medicines can cause irreparable harm, so under no circumstances self-medicate by feeding your baby your milk.

Side effects of antihistamines

As mentioned earlier, each person’s body is individual, and only a specialist can choose the right treatment. Taking the wrong medicine for a person and violating the dosage can seriously harm your health. The harm of antihistamines can manifest itself, in addition to the usual side effects for them 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 taking the medicine, and strictly follow the instructions for taking it.

Drug treatment of allergies, antihistamines

How do antihistamines work?

Antihistamines of the “old” and “new” generations

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

Basics of drug therapy

There is such a substance - histamine. It is released during an allergic reaction and is responsible for the development of unpleasant symptoms: from skin manifestations to very severe life-threatening reactions such as anaphylactic shock. This is why antiallergy drugs are called ANTIhistamine.

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

Depending on the type of reaction, antihistamines are prescribed by injection (if severe forms) and inside (for milder cases). This is understandable: if we administer medicine using intramuscular or intravenous injection, it instantly enters the bloodstream and starts working. And if we take this medicine, time must pass before active substance absorbed into the blood from the gastrointestinal tract.

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

1. Symptomatic medications.

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

3. Medicines for local therapy.

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

These drugs counteract the damaging effects of the main mediator of allergic reactions, histamine. Today, doctors have three generations of antihistamines, differing in their characteristics.

The selection of antihistamines is carried out individually, taking into account the nature of the food allergy, the child’s age and character concomitant diseases. TO symptomatic drugs also, for example, include bronchodilators. They are used for attacks of bronchial asthma.

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

The prescription of drugs in this group depends on clinical manifestations food allergies, severity of the disease, 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 Food allergies are a long process, you need to patiently and persistently follow your doctor’s recommendations.

We must also remember that some treatment methods for food allergies are absolutely contraindicated and can be harmful to the child. Thus, for food allergies, treatment with herbs and many traditional medicines is contraindicated, and psychotherapy and reflexology, in addition to bioresonance treatment, have almost no significant effect.

Treatment with herbs and drugs based on them increases the risk of developing an allergy to pollen in the future. The same “service” can be provided by dietary supplements, which often contain plant components.

Antihistamines are standard therapy for atopic dermatitis. They are used as additional remedy for external treatment for severe itching and accompanying 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

1st generation antihistamines 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 (oral forms)

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

Disadvantages of old generation antihistamines:

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

Short duration of action - taken several times a day

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

Sedative and hypnotic effect

Antihistamine drugs of the 2nd and 3rd “new” generations

Loratodine, cyterizine, fexofenadine, desloratadine.

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

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. Their duration of action is up to 24 hours, so most of these drugs are prescribed once a day.

After taking most antihistamines, their residual effect can continue for one week after discontinuation (this circumstance must be taken into account when conducting an allergy examination). A significant difference between the “new” generation of antihistamines is that they have not only an H1-blocking effect, but also antiallergic and anti-inflammatory effects.

If long-term use is necessary, use only “new” generation antihistamines

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

Advantages of 2nd generation antihistamines compared to 1st:

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

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

No blockade of other types of receptors

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

Lack of connection with food intake

No addiction, even with long-term use (3 to 6 months)

Almost complete absence of side effects associated with effects on the nervous and cardiovascular systems.

The use of antihistamines in the treatment of children with atopic dermatitis.

Children after one year of age are usually prescribed new generation drugs.

Drugs of the “new” generation, which are approved for use in children from 6 months of age, are antihistamines based on cetirizine (generic active ingredient).

VACCINATION

Since allergies are an immune disorder, allergic rhinitis and bronchial asthma can be treated with vaccines made 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 according to a special scheme subcutaneously or instilled under the tongue. This treatment is only applicable to 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 technical details of the complex mechanisms that can lead to such a development of events.

Let's just say that allergies to antihistamines are extremely rare, but they do happen. There is only one way out - change the drug.

Antihistamines are a group of drugs that competitively block histamine receptors in the body, which leads to inhibition of the effects mediated by them.

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(dilation of capillary vessels, increased vascular permeability, hypotension, cardiac arrhythmia), smooth muscles.

An increase in its influence is caused by allergic reactions, so antihistamines are used to combat allergy symptoms. Another area of ​​their use is symptomatic therapy/elimination of symptoms for 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 stomach diseases (help reduce gastric secretion).

H3 blockers - used in the treatment of neurological diseases.

Among them, cetrin (cetirizine), fenkarol (hifenadine), diphenhydramine, clemastine, suprastin stop the emission (for example, cromoglicic 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 decreases, and the duration of action increases.

First generation

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

Paracetamol

Analgesic, antipyretic, anti-inflammatory agent. The active substance is paraacetaminophenol, based on which different countries They produce many other similar drugs, 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 to cause allergic reactions than aspirin and is less irritating to the stomach. Paracetamol is part of many combination drugs in combination with aspirin, analgin, caffeine, etc. It is available in the form of tablets, capsules, mixtures, syrup, “effervescent” powders (panadol, panadone).

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

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

Ibuprofen

Has analgesic and anti-inflammatory effects. Ibuprofen is the active ingredient in drugs such as Brufen, Arthril, 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 severe physical work, heat or taking diuretics, then ibuprofen can have a negative effect on 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 regularly drink alcohol, taking ibuprofen can affect the liver.

Exit. Try to avoid dehydration. When taking ibuprofen, you need to monitor your kidney function. In no case exceed the permissible daily intake (6 tablets of ibuprofen, 200 mg each, or 2 tablets of naproxen, 220 mg each).

Antiallergic (antihistamine) drugs

Drugs in this group are intended for people suffering from hay fever (hay fever), asthma, urticaria or other allergic diseases.

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

Possible harm. Most of the 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, they are dangerous for car drivers, pilots, operators, dispatchers, etc., that is, people who require constant attention and quick reaction in difficult situations.

Exit. To avoid this risk, you should take new generation antihistamines, not drowsy and inhibition of reactions, such as claritin, kestin, which act for 12-24 hours. Antihistamines, which have a sedative effect, are best taken in the afternoon and at night.

Remedies for runny nose

The effect of drugs such as sanorin, naphthyzin, galazolin, otrivin, etc. is that they constrict 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 weakens or stops, breathing through the nose is restored, and the headache goes away.

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

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

Exit. People suffering from hypertension can take common medications for the common cold only under blood pressure control. In case of increased blood pressure, the dosage of antihypertensive drugs should be increased.

For patients with depression taking the listed antidepressants or similar ones, drugs from this group are contraindicated.

Complex cold preparations using antihistamines

Among the complex anti-cold drugs, the most famous are askofen, citramon, sedalgin, alka-seltzer plus, bicarmint, etc.

Benefit. They help get rid of different symptoms illnesses: cough, runny nose, pain, fever, allergic manifestations.

Possible harm. When taking complex drugs, the so-called “unexpected overdose” is quite often allowed.

This happens when severe cold or headache, in order to increase the effectiveness of treatment, they also add a complex cold medicine containing aspirin to taking aspirin. As a result, peptic ulcer disease may worsen or even gastric bleeding may occur.

If, in case of allergic rhinitis, in addition to suprastin, you also take a complex drug containing an antihistamine, then all together it 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 drug for colds, you should carefully read its composition indicated on the package or in the insert, and do not take separately the medications 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 in use, but this same experience indicates a whole bunch of side effects:

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

Classic antihistamines dry out the mucous membranes. Dry mouth, viscosity of sputum in the lungs (which is especially dangerous during ARVI, as it seriously increases the risk of developing pneumonia) - not in the best possible way affects the child's condition.

Concomitant use of first generation antiallergic drugs with other medicines enhances the effect of using the latter. Thus, antipyretic, analgesic, sleeping pills. The combination of antihistamines with other drugs that actively affect the functioning of the central nervous system is especially dangerous. In this case, side effects may develop, including fainting. Combination with alcoholic drinks is highly undesirable.

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

Of course, there are some advantages too. Firstly, first-generation antihistamines are relatively affordable, and secondly, they are excellent for short-term treatment of allergies. That is, if, for example, a child has eaten an excessive amount of chocolate and a short-term antihistamine is required, you can safely use the same Tavegil or Fenkarol.

Most first-generation allergy remedies are prohibited from being 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 when using Fenkarol.

For babies under one year of age, taking first-generation antiallergic drugs is not advisable. For the little ones, there are more modern drugs that are practically safe and very effective.

Principles of action of second-generation antihistamines on the child’s body

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

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 out 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 effects (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 effect 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 (loratidine);

Allergy treatment, antihistamines

Diazolin tablets 50 mg No. 20

Diazolin tab. 100 mg No. 10

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

Effective in most cases for the treatment of seasonal and year-round allergic rhinoconjunctivitis, Quincke's edema, 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, therefore it does not cause an overdose with long-term use. The effect occurs quickly, but is short-lived; to increase the duration, it is combined with non-sedating H1 blockers.

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

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

Chloropyramine hydrochloride tablet. 25 mg No. 40

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

IN injection form, which can be used as an additional remedy for anaphylactic shock and angioedema, for the prevention and treatment of allergic and pseudoallergic reactions. However, allergies can also occur to tavegil.

Peritol (cyproheptadine), along with an antihistamine, has a significant antiserotonin effect. It is often used for some forms of migraine and increases appetite.

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

Peritol tab. 4 mg No. 20 (Egis, Hungary)

Pipolfen (promethazine) - pronounced effect on the central nervous system, used as antiemetic and for potentiation of anesthesia.

Pipolfen etc. 25 mg No. 20 (Egis, Hungary)

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

Diprazine tab. 25 mg No. 20

Fenkarol (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 when developing addiction to other sedating antihistamines.

Fenkarol tab. 25 mg No. 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, and do not reduce mental and physical activity, are not adsorbed from food products V gastrointestinal tract, have a high affinity for H1 receptors, have fast therapeutic effect. However, they exhibit a cardiotoxic effect to varying degrees; when taking them it is required constant monitoring cardiac activity (prescribed on an outpatient basis). They should not be taken by patients with cardiovascular disorders or elderly patients.

The effect occurs quickly and for a longer time (slow release).

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

Absence of tachyphylaxis (decreased antihistamine activity) with long-term use.

Cardiotoxic effect occurs due to the ability to block potassium channels of the heart muscle; the risk of cardiotoxic effect increases when antihistamines are combined with antifungals (ketoconazole and intraconazole), macrolides (erythromycin and clarithromycin), antidepressants (fluoxetine, sertraline and paroxetine), and when drinking grapefruit juice , as well as in patients with severe liver dysfunction.

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

The most common second generation antihistamines are:

Trexyl (terfenadine) is the first second-generation antihistamine, no CNS depressant, but with significant cardiotoxicity and an increased ability to cause fatal arrhythmias.

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

Gistalong (astemizole) is one of the longest active drugs groups (up to 20 days). It is characterized by irreversible binding to H1 receptors. It has virtually no sedative effect and does not interact with alcohol.

Effective for chronic allergic diseases, at acute process its use is inappropriate. 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

Gistalong tab. 10mg No. 20 (India)

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

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

Fenistil (dimetenden) is closest to first-generation antihistamines, but differs from them by a significantly less severe 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 most widely purchased second-generation drugs. Its antihistamine activity is higher than that of astemizole and terfenadine due to greater binding strength 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 and children from 1 year old.

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

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

Loratadine tab. 10mg №10

Agistam tab. 10 mg No. 12

Third generation antihistamines (metabolites).

They are active metabolites of second generation antihistamines. They do not have a sedative or 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 elimination depends on renal function. It penetrates well into the skin and is effective for skin allergies.

The effect appears 2 hours after administration and lasts 24 hours. They do not have a sedative or cardiotoxic effect in therapeutic doses. Prescribe with caution in case of impaired renal function.

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

Telfast (fexofenadine) is a metabolite of terfenadine. Does not metabolize in the body, does not interact with medications, does not have a sedative effect and does not affect psychomotor activity. Efficient and maximum safe drug among antihistamines.

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

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

Every person experiences an allergic reaction from time to time, and some people suffer from allergies almost all the time, so new generation drugs are relevant for most people. Statistics show that the number of allergy sufferers is steadily increasing every year. This is due to the environmental situation and weakening.

Antihistamines - what are they in simple words?

Medicines help fight allergies. They are medications that weaken the effects of histamine in the human body. Histamine is a special substance produced by cells immune system body and designed to fight bacteria and viruses. But since an allergy is a “mistake” of the immune system, histamine does not bring any benefit, but acts on the receptors, causing swelling of the mucous membranes, redness and itching of the skin, etc. Antihistamines act on H1-histamine receptors and block them. Thus, histamine cannot influence the receptors, as a result of which the manifestations of allergies are reduced: itching, tearing, swelling of the mucous membranes, etc. are reduced.

There are several generations of antihistamines, each of which has its own differences. The first generation was created in the 30s of the last century and became a real breakthrough in the fight against allergies. After some time, second and third generation drugs were created.

Generations of antihistamines differ significantly from each other: they have different properties and side effects. This applies to drugs of three generations. 4th generation antihistamines are very conventional; most often this is an advertising ploy by manufacturers who want to emphasize the innovativeness of their products. Which ones are better? Let's take a look at the features of each category to choose the best antihistamines.

1st generation antihistamines

This is the most common group of anti-allergy drugs that have a pronounced sedative effect: they cause drowsiness and calm. They are quite powerful and do not last long, usually 4-5 hours, can be found in any pharmacy, their price is quite low, and their quality and effectiveness are time-tested. The use of first-generation antihistamines lasts no more than 7-10 days, after this period addiction begins and the effectiveness of the drugs noticeably decreases. These drugs are prescribed after some vaccines, during treatment skin diseases, as well as in case of acute allergic reaction to a temporary external irritant.

TO side effects This group includes:

• decline ;
• increased appetite;
• rapid heartbeat;
• discomfort in the stomach, vomiting and nausea;
• thirst, drying of mucous membranes;
• weakening of attention and muscle tone.

• Suprastin. Available in ampoules and tablets, the active substance is chloropyramine. Used to treat edema, eczema, hives, allergic rhinitis, swelling of the mucous membranes. Also used to eliminate skin itching, incl. after an insect bite. Suprastin can be given to children starting from one month, but it is important to calculate the dosage. This remedy can be used for high temperature, which is difficult to knock down, and also as a sedative for colds and viral diseases.

Suprastin should not be used during pregnancy and lactation.

• Diazolin. That's enough mild remedy, which does not cause drowsiness and is suitable for long-term use. Diazolin can be used during pregnancy, with the exception of the first trimester, and is also suitable for children from two years of age. This product is available in the form of tablets, ampoules, and suspensions with various dosages.
• Fenistil. Very effective universal remedy, which is used for all types of allergies. Causes drowsiness only in the first few days of treatment, then the sedative effect disappears. Can be used externally (gel) for insect bites. Suitable for children from 1 month (externally), it can be taken by pregnant women from the second trimester if their condition due to allergies causes serious concern. Available in the form of capsules, suspensions, tablets, gel.
• Fenkarol. An effective remedy, often used in the fight against seasonal allergies, as well as in blood transfusions. Prescribed to children from 1 year and pregnant women from the 2nd trimester (under medical supervision).
• Tavegil. One of the most powerful drugs with long period action (12 hours). Causes drowsiness. Available in tablets and syrup form, it is approved for children from 1 year of age. Pregnant women should not take this medicine.

Suprastin is prescribed for the treatment of seasonal and chronic allergies, urticaria, atopic dermatitis, edema, itching of various etiologies, eczema

Antihistamines 2nd generation

These are improved antihistamines that do not have a sedative effect and have a prolonged effect. You need to take them once a day, the use can be long-term, since these medications are not addictive. Their price is usually low. They are quite effective in the treatment of skin diseases, eliminating Quincke's edema, and are used to alleviate the condition of chicken pox. These medications are not recommended for older people and those with heart disease. Below is a list of the most effective second generation products.

• Loratadine. An effective product available in the form of syrup and tablets. Helps fight allergies and their consequences - anxiety, sleep disturbances, weight gain. The medicine can be given to children from three years of age; pregnant women can take the drug in the second and third trimesters. In critical situations, the doctor may prescribe Loratadine up to 12 weeks of pregnancy.
• Rupafin. Enough strong drug, which is used in the treatment of skin allergic reactions. The product is safe, acts quickly, and the effect lasts throughout the day. It cannot be used during pregnancy; use by children under 12 years of age is also prohibited. During lactation, Rupafin can be taken only as prescribed by a doctor.
• Kestin. The most powerful drug in this group, the effect of which lasts for two days. Used in the most difficult cases, it quickly removes angioedema, relieves suffocation, reduces skin rashes. At the same time, Kestin is toxic to the liver, so it cannot be taken systematically. It is contraindicated for pregnant women and children under 1 year of age.

Also effective second generation drugs include Claritin, Zodak, Cetrin, Parlazin, Lomiran, Cetrisin, Terfanadine, Semprex.

Important! Long-term use (more than a month) of these drugs is dangerous without a doctor’s permission, especially for powerful drugs. Therefore, do not forget to consult a specialist.

Antihistamines 3rd generation

Third-generation antihistamines are considered the newest, but, in fact, they are an improved version of the second generation. They have the same long-lasting effect, do not have a sedative effect, but are completely harmless to the heart and non-toxic to the liver. Thanks to these properties, they can be taken for a long time (for example, when seasonal allergies, psoriasis, bronchial). These are the safest antihistamines for pregnant women, but you should still consult your doctor before taking them.

Important: Antihistamines during pregnancy can be dangerous in the first trimester, so you should consult with. If there is a threat, then you should refrain from such means if possible. Antihistamines for breastfeeding It is also necessary to agree with the pediatrician. If appointed powerful drugs, it makes sense to stop breastfeeding for a while.

3rd generation antihistamines are considered the most powerful and fastest-acting. A list of the names of the best of them is given below.

• Telfast (Allegra). A new drug that not only reduces the response of receptors to histamine, but also suppresses the production of this substance. As a result, allergy symptoms disappear very quickly. It acts within 24 hours and does not cause addiction when taken for a long time. Children under 12 years of age and expectant mothers cannot use Telfast; it is also contraindicated during lactation.
• Cetrizine. This remedy is often classified as the fourth generation, in in this case The division into categories is very arbitrary. This is a drug of the latest generation, which begins to act almost instantly (20 minutes after administration), and you can take tablets once every three days. In the form of syrup, Cetrizine can be given to children from six months of age, but it is contraindicated for pregnant women. If the medicine was prescribed by a doctor during lactation, then feeding should be stopped for the period of treatment for allergies. This drug can be taken for a long time.
• Desloratadine. A strong antihistamine and anti-inflammatory agent. In therapeutic doses it is well tolerated, but if the dosage is exceeded, it can lead to dry mouth, frequent heart rate, insomnia. It cannot be taken during pregnancy, but in critical cases (suffocation from bronchospasm, Quincke's edema) it can be treated under the supervision of a doctor.
• Xizal. Xyzal and its analogues are effective antihistamines for skin allergies and itching, seasonal allergic manifestations, urticaria and chronic year-round allergies. They have a prolonged effect and relieve allergy symptoms 40 minutes after administration. Xyzal is available in the form of drops and tablets and is safe for children over 2 years of age.

Also good third generation products include Desal, Lordestin, Erius, Suprastinex.

Antihistamines 4th generation

Such drugs are a new word in the fight against allergies, since they are practically free of side effects, despite their high efficiency. They are not harmful to the heart, like most earlier antihistamines, do not cause drowsiness or addiction, and are easy to use (taken every 1-3 days). The only contraindication is pregnancy and early age child. As for the disadvantages of fourth generation antihistamines, these are high price medications.

The most popular and effective means this generation:

• Fexofenadine. An effective remedy in the fight against all types of allergies, it is as safe as possible and has virtually no side effects. Available in tablets and syrup form, it can be given to children over 6 years old.
• Levocetrizine. Strong remedy, which is used to treat year-round and seasonal allergies, reduces symptoms. It is non-toxic to the liver and heart, so it can be taken for months.

How to choose the best allergy remedy

The best antihistamines are not always the most expensive and modern; it is important to understand how relevant a particular drug is in a certain situation. For example, during an illness accompanied by insomnia or restless sleep, first generation drugs will be preferred. They will eliminate allergy symptoms, and their sedative effect will be very useful. If an allergy has overtaken a person who does not want to get out of the usual rhythm of life, then he should pay attention to the newest metabolite drugs. In any case, before long-term use of the drug, you should consult your doctor, especially if you need to treat a child or a pregnant woman.