Desal tablets p / o 5mg, No. 10

To relieve or eliminate symptoms:

• allergic rhinitis (sneezing, nasal congestion, rhinorrhea, itchy nose, itchy palate, itching and redness of the eyes, watery eyes);

• hives (itching, rash).

Inside, regardless of the meal.

Adults and adolescents (12 years and older) - 5 mg (1 tab.) 1 time / day.

Blue film-coated tablets, round, biconvex, engraved with 'LT' on one side.

1 tab.

desloratadine - 5 mg

Excipients: microcrystalline cellulose - 55 mg, pregelatinized corn starch - 15 mg, mannitol - 22 mg, talc - 2.5 mg, magnesium stearate - 0.5 mg.

The composition of the film shell: opadry blue 03F20404 (hypromellose 6cP - 1.9 mg, titanium dioxide (E171) - 0.61 mg, macrogol 6000 - 0.34 mg, dye indigo carmine aluminum varnish (E132) - 0.14 mg) - about 3 mg.

• pregnancy;

• breastfeeding period;

• children under 12 years of age (efficacy and safety have not been established);

• hypersensitivity to the active or any auxiliary substance of the drug.

The drug should be used with caution in severe renal failure.

Clinical and pharmacological group: Histamine H1 receptor blocker. Antiallergic drug

Pharmaco-therapeutic group: H1-histamine receptor blocker

pharmachologic effect

Long-acting antihistamine, blocker of peripheral histamine H1 receptors. Desloratadine is the primary active metabolite of loratadine. Inhibits the cascade of reactions of allergic inflammation, incl. release of pro-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, release of proinflammatory chemokines, production of superoxide anions by activated polymorphonuclear neutrophils, adhesion and chemotaxis of eosinophils, release of adhesion molecules such as P-IgE mediated release of histamine, prostaglandin D2 and leukotriene C4.

Thus, it prevents the development and facilitates the course of allergic reactions, has an antipruritic and antiexudative effect, reduces capillary permeability, prevents the development of tissue edema, spasm of smooth muscles.

The drug has no effect on the central nervous system, practically does not have a sedative effect (does not cause drowsiness) and does not affect the speed of psychomotor reactions when taken in recommended doses. Does not cause prolongation of the QT interval on the ECG.

The action of desloratadine begins within 30 minutes after ingestion and lasts for 24 hours.

Pharmacokinetics

Suction

After taking the drug inside, desloratadine is well absorbed from the gastrointestinal tract. It is determined in blood plasma after 30 minutes, and Cmax is reached after about 3 hours. There were no clinically significant changes in the concentration of desloratadine in blood plasma with repeated administration of ketoconazole and erythromycin. The bioavailability of desloratadine is dose proportional with a dose ranging from 5 mg to 20 mg.

Distribution

Plasma protein binding is 83-87%. When used in adults and adolescents for 14 days at a dose of 5 mg to 20 mg 1 time / day, there are no signs of clinically significant cumulation of desloratadine. The degree of cumulation of desloratadine is consistent with the T1 / 2 value and the frequency of its use 1 time / day. AUC and Cmax values ??in children were similar to those in adults who received 5 mg desloratadine.

Simultaneous intake of food or grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg 1 time / day). Does not penetrate the BBB.

Metabolism

The enzymes responsible for the metabolism of desloratadine are not yet known, so interactions with some drugs cannot be completely ruled out. It is not an inhibitor of CYP3A4 and CYP2D6 and is not a substrate or inhibitor of P-glycoprotein. It is extensively metabolized in the liver by hydroxylation to form 3-OH-desloratadine, which is then glucuronized.

Withdrawal

The terminal phase T1 / 2 is about 27 hours. Desloratadine is excreted from the body in the form of a glucuronide compound and in a small amount unchanged (with urine - less than 2% and through the intestines - less than 7%).

Indications

To relieve or eliminate symptoms:

• allergic rhinitis (sneezing, nasal congestion, rhinorrhea, itchy nose, itchy palate, itching and redness of the eyes, watery eyes);

• hives (itching, rash).

Dosage regimen

Inside, regardless of the meal.

Adults and adolescents (12 years and older) - 5 mg (1 tab.) 1 time / day.

Side effect

More often than others, the following undesirable reactions are noted: increased fatigue (1.2%), dryness of the oral mucosa (0.8%), headache (0.6%).

When using the drug in adults and adolescents at the recommended dose of 5 mg / day, the incidence of drowsiness is not higher than when using placebo.

In the course of post-marketing surveillance, the following adverse reactions were very rarely observed.

Mental disorders: hallucinations.

From the side of the central nervous system: dizziness, drowsiness, insomnia, psychomotor hyperactivity.

On the part of the cardiovascular system: tachycardia, palpitations.

From the digestive system: abdominal pain, nausea, vomiting, dyspepsia, diarrhea.

From the liver and biliary tract: increased activity of liver enzymes, increased concentration of bilirubin, hepatitis.

From the musculoskeletal system: myalgia.

Allergic reactions: anaphylaxis, angioedema, itching, rash, urticaria.

Contraindications for use

• pregnancy;

• breastfeeding period;

• children under 12 years of age (efficacy and safety have not been established);

• hypersensitivity to the active or any auxiliary substance of the drug.

The drug should be used with caution in severe renal failure.

Application during pregnancy and lactation

Prescribing the drug during pregnancy is not recommended due to the lack of clinical data on the safety of its use during this period.

Desloratadine is excreted in breast milk, so its use during breastfeeding is not recommended.

Application for impaired renal function

The drug should be used with caution in severe renal failure.

Application in children

Prescribing for children under 12 years of age is contraindicated, because efficacy and safety have not been established.

special instructions

In case of severe renal dysfunction, Desal should be taken with caution.

Influence on the ability to drive vehicles and mechanisms

In studies, there was no effect of desloratadine on driving. However, it should be borne in mind that very rarely some patients may develop drowsiness, in this case, care should be taken when driving and working with mechanisms.

Overdose

Symptoms: Taking a dose 9 times the recommended dose (45 mg) did not lead to the appearance of any clinically significant symptoms. Drowsiness may develop.

Treatment: it is necessary to wash the stomach, take activated charcoal; if necessary, symptomatic therapy. Desloratadine is not excreted during hemodialysis, the effectiveness of peritoneal dialysis has not been established.

In case of accidental ingestion of a large amount of the drug, the patient should immediately consult a doctor.

Drug interactions

No clinically significant interactions with other drugs have been identified (including with ketoconazole and erythromycin).

Desloratadine does not enhance the effect of ethanol on the central nervous system.

Storage conditions

The drug should be stored out of the reach of children, dry, protected from light, at a temperature not exceeding 25 ? C.

Shelf life

Shelf life is 2 years.

Terms of sale

The drug is approved for use as a means of OTC.