Antihistamines containing desloratadine. Desloratadine side effects. Similar facilities and cost

Desloratadine is an antihistamine drug that blocks H1-specific histamine receptors localized in smooth muscles, endothelium, CNS and causes vasodilation, spasm smooth muscle bronchi, expansion of endothelial cells (respectively, desloratadine causes back effects). Suppresses a chain of hypersensitivity reactions, causing inflammation and tissue damage. Prevents their development and makes their course less pronounced. Eliminates itching, reduces exudation, makes the walls less permeable blood vessels, prevents swelling and sharp rise smooth muscle tone, which is accompanied by contraction of the muscle itself and pain. It does not affect the central nervous system, does not cause drowsiness, does not slow down psychomotor reactions. The effect of the drug develops within half an hour after oral intake and continues throughout the day. Desloratadine is well absorbed from the gastrointestinal tract. The presence of food content in the gastrointestinal tract does not affect the rate of absorption and does not change the pharmacokinetic characteristics medicinal product. Desloratadine is indicated for seasonal allergic rhinoconjunctivitis, allergic rhinitis with persistent symptoms (year-round) to eliminate or alleviate symptoms (sneezing, difficulty nasal breathing, profuse mucus secretion from the nasal passages, hyperemia of the eyes, itching of the palate and nasal passages, lacrimation). The drug is also used for chronic urticaria unexplained etiology. In pediatric practice, the use of desloratadine is possible from the age of 12. The drug is taken 1 time per day at regular intervals. Desloratadine does not potentiate the inhibitory effect of ethanol on the central nervous system.

Clinical studies of the drug have shown it high efficiency with seasonal allergic rhinitis, bronchial asthma. The use of the drug for 4 weeks in one of these studies led to more pronounced relief of symptoms in the group taking desloratadine in contrast to the control group. The drug was well tolerated by patients and practically did not cause clinically significant side effects, with the exception of headache (developed in 5% of study participants). Desloratadine has been successfully used to treat allergic pathology in pediatric practice. One study in children aged 2 to 16 years evaluated the effectiveness of desloratadine in relieving the symptoms of persistent allergic rhinitis. The test showed good control of symptoms of allergic rhinitis by desloratadine. Best Results were achieved in relation to the symptoms induced by histamine: itching, sneezing, copious mucus from the nasal passages. The efficacy of desloratadine in patients with allergic rhinitis without associated pulmonary symptoms was higher than in patients with bronchial asthma. Desloratadine is present in European protocols for the treatment of allergic rhinitis, urticaria and atopic dermatitis(in the latter case, as aid as part of a short-term course, the purpose of which is to eliminate itching). A convenient regimen for the use of desloratadine (1 time per day, regardless of food intake) increases compliance (patients' adherence to treatment). For effective control for symptoms of allergic rhinitis and urticaria, 5 mg of desloratadine per day is sufficient.

Pharmacology

Histamine H1 receptor blocker ( long-acting). It is the primary active metabolite of loratadine. Inhibits the release of histamine and leukotriene C4 from mast cells. Prevents development and facilitates the course allergic reactions. It has antiallergic, antipruritic and antiexudative action. Reduces the permeability of capillaries, prevents the development of tissue edema, relieves spasm of smooth muscles. Has practically no sedative effect and when taken at a dose of 7.5 mg does not affect the speed of psychomotor reactions. In comparative studies of desloratadine and loratadine, there were no qualitative or quantitative differences in the toxicity of the two drugs at comparable doses (taking into account the concentration of desloratadine).

Pharmacokinetics

Release form

Blue film-coated tablets, round, biconvex; one side is inscribed with "D5" in white ink, the other side is blank.

Excipients: microcrystalline cellulose 67 mg, pregelatinized starch 25 mg, colloidal silicon dioxide 0.5 mg, talc 2.5 mg.

The composition of the film shell: Opadry II 32B30509 blue 3 mg, including lactose monohydrate 1.2 mg, hypromellose 15 cP 0.84 mg, indigo carmine aluminum lacquer 0.4332 mg, titanium dioxide 0.2868 mg, macrogol-400 0.24 mg.
Ink composition: Opacode S-1-18086 white (shellac 59%, titanium dioxide 25%, isopropanol 13.35%, butanol 1.4%, propylene glycol 1.25%).

7 pcs. - blisters (1) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
7 pcs. - blisters (2) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
7 pcs. - blisters (3) made of OPA/Al/PVC and aluminum foil - cardboard packs.
7 pcs. - blisters (4) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
10 pieces. - blisters (1) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
10 pieces. - blisters (2) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
10 pieces. - blisters (3) made of OPA/Al/PVC and aluminum foil - cardboard packs.
10 pieces. - blisters (4) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
10 pieces. - blisters (5) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
10 pieces. - blisters (6) made of OPA/Al/PVC and aluminum foil - packs of cardboard.
10 pieces. - blisters (9) made of OPA/Al/PVC and aluminum foil - cardboard packs.
10 pieces. - blisters (10) made of OPA/Al/PVC and aluminum foil - cardboard packs.

Dosage

Adults and adolescents aged 12 years and older are prescribed orally, regardless of food intake, at a dose of 5 mg / day.

Children aged 1 to 5 years - 1.25 mg 1 time / day, aged 6 to 11 years - 2.5 mg 1 time / day.

Interaction

The study of interaction with ketoconazole and erythromycin did not reveal clinically significant changes.

Does not affect the effects of ethanol.

For the symptomatic treatment of allergies, antihistamines are used, which can be divided into 2 groups depending on the ability to have a sedative effect. Desloratadine is a non-sedating antihistamine because it does not cross the blood-brain barrier and does not affect brain activity. The substance desloratadine is the active product of the breakdown of loratadine, which is formed in the liver. It is classified as a 3rd generation antihistamine.

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Composition of Desloratadine

The active substance desloratadine (INN - desloratadine) is contained in the preparation at a concentration of 5 mg in each biconvex tablet with a blue shell. Auxiliary substances are:

• calcium hydrophosphate dihydrate;
• microcrystalline cellulose;
• corn starch;
• talc;
• sodium stearate.

The medicine is also produced in the form of a syrup, 1 ml of which contains 0.5 mg of the active ingredient and a number of additional substances:

• propylene glycol;
• sorbitol;
• citric acid and its sodium salt;
• sodium benzoate;
• disodium edetate;
• crystalline sugar;
• raspberry flavor;
• dye carmoisine.

Desloratadine syrup should not be used by people with fructose intolerance as it contains sorbitol.



pharmachologic effect

Desloratadine selectively blocks specific histamine receptors ( H1 receptors) involved in the development of allergy symptoms. The drug has 3 proven properties:

1. 1. antihistamine;
2. 2. antiallergic;
3. 3. anti-inflammatory.

The drug prevents the release of signaling substances involved in the development of allergies (pro-inflammatory cytokines and chemokines), P-selectin. The agent affects the activity of immune cells involved in the development of allergies: it inhibits the interaction and movement of eosinophils and the production of superoxide anion by neutrophils. An allergic reaction often occurs with the participation of class E immunoglobulins (IgE). Desloratadine slows down the IgE-dependent release of histamine and other signaling substances.



Clinical studies of the efficacy and safety of this drug have shown that its use does not cause significant damage to the health of the cardiovascular system and intestines.

Desloratadine has the potential to relieve acute allergic bronchospasm.



Indications

Desloratadine is indicated for the treatment of manifestations of allergic rhinitis (seasonal and perennial) and the chronic form of idiopathic urticaria. The medicine is taken for the following allergic manifestations:

• sneeze;
• runny nose;
• rashes;
• nasal congestion;
• eye redness;
• increased tearing;
• cough.

The effectiveness of this drug in the symptomatic treatment of bronchial asthma has been proven.

The activity of the drug is not affected by the intake of certain antibiotics (erythromycin, azithromycin), antifungal agents (ketoconazole), antidepressants (fluoxetine) and antihistamines (cimetidine).



Method of application and dosage

Desloratadine quickly enters the blood - no later than half an hour after ingestion, and after 3 hours the maximum amount of the drug enters the bloodstream. The half-life of the drug is 27 hours. The drug has an effect on allergy symptoms within 1 day, so it is recommended to take it 1 time during this period.

Medication is not tied to food intake. Recommended dosages are given in the table.

Allergic reactions are familiar to many people. They can occur on drugs, cosmetics, food. A harmless, at first glance, condition can be complicated by anaphylactic shock and lead to death. Therefore, every allergy sufferer should have a remedy in his home medicine cabinet that can help relieve unpleasant symptoms. Desloratadine is considered one of the most popular antiallergic drugs. Analogues are also widely used. However, it is worth taking any medication after consulting a doctor.

Compound

The drug is considered a blocker of histamine H1 receptors. Belongs to the group Available in the form of blue tablets. The main substance in the composition of the drug is desloratadine. One tablet contains 5 mg of the active ingredient. The tool has a long-term effect, prevents the patient from developing allergies, alleviates the symptoms of the disease. The drug reduces swelling, itching, pain, has a pronounced antispasmodic effect on smooth muscles.

The drug does not affect the activity of the central nervous system, does not cause drowsiness. The action of the tablets begins 30 minutes after ingestion. The therapeutic effect persists for a day when taking Desloratadine. Instructions, price in pharmacies, application features - all this information can be obtained from your doctor.

The drug belongs to the low price category. For one package of tablets you will have to pay about 200 rubles.

Indications and contraindications

The drug is prescribed for severe which is accompanied by mucosal edema, sneezing, redness and general malaise. The remedy is also widely used for symptoms of urticaria, when there are rashes on the skin, itching.

A contraindication to drug treatment is hypersensitivity to the individual components of the drug, the period of childbearing and breastfeeding. It is not recommended to take children under 12 years of age, as well as patients with severe renal insufficiency. You should not use Desloratadine tablets without the recommendation of a specialist. Analogues (their price may be slightly higher) can also be used after consulting a doctor.

Dosage

The tablet should be taken without chewing, with plenty of liquid. For adults and children over 12 years of age, the dose is 5 mg once a day. It is advisable to take the medicine at the same time. The course of treatment depends on the condition of the patient. During the flowering period, when allergic rhinitis appears, it is worth taking pills for at least one week.

What if the pharmacy could not find the drug "Desloratadine Teva"? Analogues can recommend a doctor. The most popular means will be described below.

"Erius"

The drug belongs to the group of antihistamines. Blocks production. The composition of the drug includes desloratadine. Available in the form of blue tablets or syrup. The drug prevents the development and eliminates the symptoms of an allergic reaction. It does not have a sedative effect and does not affect the functioning of the nervous system. It is used to treat the symptoms of allergic rhinitis and urticaria. Contraindications to treatment are pregnancy and lactation. Also, do not take pills under the age of 12 years. The drug is contraindicated in case of hypersensitivity to the components of the drug.

With caution, the remedy "Erius" is prescribed for pathologies of the kidneys and liver. In most cases, take one tablet per day. Syrup for adults is dosed in 10 ml per dose. Young children, depending on age, are given to drink from 2.5 ml to 5 ml of medication per day. The drug has the same performance as the drug "Desloratadine". Instructions for use, price, drug analogues - every allergic person should know all this.

Elisey tablets

The drug has antiallergic properties. Does not cause drowsiness and does not affect the work of the central nervous system. Reduces capillary permeability, relaxes smooth muscles, relieves swelling. The medicine relieves the symptoms of pain, itching, redness. Urticaria and other types of allergies are prescribed. The therapeutic effect occurs 30 minutes after taking the medicine and lasts for a day.

Do not use the product in case of hypersensitivity to the components, as well as during pregnancy and lactation. The dose per dose is 5 mg. Tablets are taken once a day. The drug has the same effect as Desloratadine tablets. Analogues are similar in composition.

If allergic itching occurs, doctors prescribe Desloratadine, which is a histamine blocker. For adults, the drug is available in the form of tablets, for children - in the form of a syrup. Both types of drugs suppress the manifestation of allergy symptoms, they act safely. Check out their instructions for use for proper use of medications.

The drug Desloratadine

According to the pharmacological classification of drugs, Desloratadine belongs to histamine receptor blockers and antiallergic drugs. This means that it is used as a medicine that eliminates itching, redness and rashes on the skin. This action is ensured by the work of the active substance of the drug - desloratadine.

Compound

The drug is available in the form of tablets for adults and syrup for children. Their description and composition are given in the table:

Pharmacodynamics and pharmacokinetics

The antihistamine drug is a blocker of histamine receptors, has a long-term effect. The active substance belongs to the primary active metabolites of loratadine. The drug inhibits the cascade of allergic inflammation, releases pro-inflammatory cytokines, chemokines, interleukins. The drug inhibits production:

• superoxide anions activated by neutrophils;
• adhesion of eosinophils, release of histamine, prostaglandin and leukotriene;
• expression of selectin molecules;
• immunoglobulin dependent release of histamine by peripheral receptors;
• acute allergic bronchospasm.

This leads to the prevention of the development and alleviation of the course of allergic reactions. The drug has antipruritic and antiexudative action, reduces capillary permeability, prevents the development of tissue edema, spasm of smooth muscles. Desloratadine does not affect the central nervous system, does not have a sedative effect and does not slow down the speed of psychomotor reactions. It begins to act within half an hour after administration and works for a day.

The active substance is well absorbed from the gastrointestinal tract, is determined in the blood plasma after half an hour, and reaches a maximum concentration within three hours. The drug binds to plasma proteins by 85%, does not accumulate, does not penetrate the blood-brain barrier, its bioavailability is not affected by the use of grapefruit juice and food intake. Metabolism of the substance occurs in the liver by hydroxylation, excreted by the kidneys and intestines in 40-60 hours.

Indications for use

You can use the drug to eliminate the symptoms of allergic rhinitis (sneezing, nasal discharge, itching, swelling, congestion), itching and redness of the eyes, tearing, coughing. The drug treats hives, associated symptoms - rashes and burning of the skin. The drug is prescribed by the doctor after the doctor finds out the individual characteristics of the patient.

Instructions for use Desloratadine

Taking the drug differs depending on the form of release. Tablets and syrup are taken orally at the dose prescribed by the doctor. The volume of dosage is affected by the age of the patient, the severity of the allergy, the individual characteristics of the patient. It is impossible to prescribe a medicine for yourself, this threatens the development of negative reactions from many organ systems.

Desloratadine syrup

Desloratadine syrup is intended for children older than six months. It is used to eliminate the symptoms of allergic rhinitis, intermittent (symptoms last less than 4 days in a row or for 4 weeks) and persistent form (signs are noticeable for more than 4 days in a row or for more than 4 months), urticaria throughout the time of allergy symptoms.

The use of the drug does not depend on food intake. Children 6-11 months old are given 2 ml of syrup once, 1-5 years old - 2.5 ml each, 6-11 years old - 5 ml each, over 12 years old and adults are prescribed 10 ml / day. Dosing is carried out with a measuring spoon. The course of treatment lasts until the symptoms disappear completely or during the entire period of contact with allergens that cause symptoms.

According to the instructions, Desloratadine tablets are taken orally, swallowed whole, washed down with a small amount of liquid. It is desirable to take the drug at the same time of day, regardless of food. Adults and children over 12 years of age are given a tablet / day. The duration of therapy depends on the type of disease, treatment continues until the symptoms disappear.

Desloratadine for children

Taking tablets is contraindicated in children under 12 years of age, and syrup - up to six months. The dosage of the drug for adults differs from that for children, in the latter it is several times less and depends on age and body weight. The restriction on the age categories of patients is due to the lack of information on the efficacy and safety of the drug for young children.

Interaction with other drugs

There was no drug interaction with Azithromycin, Erythromycin, Cimetidine, Ketoconazole and Fluoxetine. When taking alcohol, the drug does not increase the effect of alcohol on the central nervous system and does not increase the negative effect of ethanol on psychomotor functions. The drug is ineffective in the treatment of rhinitis of infectious etiology; cases of reduced concentration of attention when driving can rarely occur.

Side effects

Taking the medication, the patient may experience side effects. These include the following:

• anaphylaxis, angioedema;
• shortness of breath, skin itching;
• rash, idiopathic urticaria;
• headache, dizziness, drowsiness;
• insomnia, psychomotor hyperactivity;
• hallucinations, convulsions;
• tachycardia, palpitations;
• dry mouth, stomach pain;
• nausea, vomiting, diarrhea;
• hepatitis, dyspepsia;
• myalgia, fatigue;
• pharyngitis;
• dysmenorrhea.

Overdose

Taking a dose five times higher than the recommended one did not lead to the negative effects of the drug and overdose. Daily use of a dose of 20 mg for two weeks was also not marked by changes in the cardiovascular system, as well as 45 mg for a course of 10 days. If these figures are exceeded, vomiting and nausea may develop. Treatment consists of gastric lavage, activated charcoal, and symptomatic therapy. Hemodialysis and peritoneal dialysis are ineffective.

Contraindications

The drug is prescribed with caution to patients with severe renal insufficiency, disorders of the kidneys or liver. Contraindications for taking it are pregnancy, breastfeeding (lactation), because. the substance passes into breast milk, age up to 12 years for tablets and up to six months for syrup, hypersensitivity to the components of the composition, loratadine or its derivatives.

Terms of sale and storage

You can buy Desloratadine without a prescription. It is stored in a dry, dark place without children's access at temperatures up to 25 degrees for three years for tablets and two for syrup.

Analogues

Synonyms for the drug are similar to it in terms of the active substance, the therapeutic effect. Substitutes have a different active ingredient, but they have the same effect. Direct and indirect analogues of the drug are the following drugs:

• Desal;
• Erius;
• Ezlor;
• Lordestin;
• Desloratadine-Teva;
• Desloratadine Canon;
• Allergomax;
• Desradin.

What is the difference between loratadine and desloratadine

A popular analogue of Desloratadine is Loratadine. Both drugs belong to histamine blockers, do not have cardiotoxic and hypnotic effects. Desloratadine contains the active substance of the same name, which is a metabolite of loratadine, the active component of the compared drug. Desloratadine acts faster, more efficiently (4-5 times difference). Loratadine is not available in the form of a syrup, so it can only be used by adults.

Desloratadine price

You can buy the drug through pharmacies or online platforms at prices that are influenced by the form of release of the drug and the level of trade margins. The approximate cost of medicines on the shelves of Moscow, St. Petersburg pharmacies is shown in the table:

Video

Desloratadine is a 4th generation modern antiallergic agent. Its main advantages are safety, coupled with a minimum of side effects and the possibility of long-term treatment.

Indications

The active substance - Desloratadine - has the following effect on the human body:

• antipruritic;
• anti-exudative - that is, it prevents the formation of inflammatory effusion in the tissues and on the mucous membranes;
• decongestant;
• mild antispasmodic.

Desloratadine can be used to prevent allergic reactions and alleviate their course in the following cases:

• with chronic or acute allergic rhinitis or lacrimation;
• with hay fever - an allergic reaction to the flowering of plants;
• with urticaria, including idiopathic;
• with dermatitis, including allergic and atopic;
• with the threat or development of Quincke's edema.

Dosage and administration

Desloratadine is available in the form of 5 mg tablets packed in blisters of 10 pieces. Tablets are taken orally and washed down with water, regardless of the meal.

Treatment can be quite lengthy. If you need to take the drug for more than 2 weeks, you must first consult with your doctor.

Contraindications

Absolute contraindications to taking Desloratadine tablets are:

• children under 12 years of age (small patients are recommended to take this drug in the form of a syrup);
• hypersensitivity to the drug or its components, including lactase deficiency;
• During pregnancy and lactation, the drug is contraindicated, because. there are no data on the safety of its use during these periods.

Desloratadine should be used with caution in patients with kidney disease, as this drug may aggravate existing renal failure.

Side effects

The most common side effects of taking Desloratadine are:

• increased fatigue (in 12 out of 1000 patients);
• dry mouth (in 8 out of 1000 patients);
• headache or migraine (in 6 out of 1000 patients).

Extremely rarely recorded cases of tachycardia and increased levels of bilirubin in the blood.

Not a single case has been recorded when the result of taking Desloratadine was a hypnotic effect or a decrease in the level of attention.

Compound

Pharmacokinetics

Desloratadine is absorbed in the gastrointestinal tract and enters the bloodstream, after which it blocks H1-histamine receptors and suppresses the allergic inflammatory reaction at the very beginning of its development. A pronounced therapeutic effect occurs half an hour after taking the medicine, reaches its maximum within 3-4 hours and lasts a day.

The bioavailability of the drug is high. It is not affected by any food or drinks taken at the same time.

The drug does not accumulate in the body, but breaks down in the liver to a glucuronide compound and is excreted in the urine and feces within a few days.

drug interaction

Desloratadine does not affect the effectiveness of other drugs when taken simultaneously.

Overdose

Cases of overdose with Desloratadine have not been recorded. It has been proven that a one-time excess of the dose by 5-8 times will not significantly affect the state of human health and will not have a cardiotoxic effect.

If taking an unreasonably high dose of the drug still led to intoxication, it is necessary to take gastrointestinal adsorbents and call a doctor.

Other

Released without a prescription. Shelf life - 3 years. Store in a place protected from light and out of the reach of children, at a temperature not exceeding 25°C.