Elisei - instructions for use, dose, side effects, contraindications

Excipients: sorbitol (E 420) - 110 mg; sucrose 420 mg; sodium hydrophosphate dodecahydrate - 20.18 mg; sodium benzoate (E 211) 1.0 mg; disodium edetate dihydrate 0.25 mg; propylene glycol 100 mg; citric acid monohydrate - 4.375 mg; dye sunset sunset yellow (E 110) - 0.02 mg; water purified to 1.0 ml.

Description:

Transparent, viscous liquid of orange color.

Pharmacotherapeutic group:antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.X Other antihistamines for systemic use

R.06.A.X.27 Desloratadine

Pharmacodynamics:

Desloratadine is a selective blocker of peripheral histamine H₁-receptors that do not cause sedation. Desloratadine is the primary active metabolite of loratadine. After oral administration, selectively blocks peripheral H₁-gistaminovye receptors.

In addition to antihistamine activity, desloratadine has anti-allergic and anti-inflammatory effect. Determined that desloratadine oppresses the cascade of various reactions underlying the development of allergic inflammation, namely:

- release of anti-inflammatory cytokines, including IL-4, IL-6, IL-8, IL-13;

- release of anti-inflammatory chemokines, such as RANTES;

- production of superoxide anion by activated polymorphonuclear neutrophils;

- adhesion and chemotaxis of eosinophils;

- expression of adhesion molecules, such as P-selectin;

- IgE-dependent release of histamine, prostaglandin D2 and leukotriene C4;

- acute allergic bronchospasm in animal studies.

The safety of desloratadine in children has been demonstrated in three clinical studies. The drug was prescribed for children from 6 months to 11 years who needed antihistamine therapy at a daily dose of 1 mg (age group from 6 to 11 months), 1.25 mg (age group from 1 to 5 years), or 2.5 mg from 6 to 11 years). The treatment was well tolerated, which was confirmed by the results of clinical laboratory studies and the state of vital body functions. In clinico-pharmacological studies of the use of desloratadine in the recommended therapeutic dose there was no longer lengthening of the interval QT on the ECG.

During clinical trials, daily usedesloratadine in a dose of up to 20 mg for 14 days was not accompanied by statistically clinically significant changes in the cardiovascular system. In a clinical pharmacological study, the use of desloratadine 45 mg / day (9 times the therapeutic dose) for 10 days did not cause an elongation of the interval QT.

When using the recommended dose of 5 mg, the incidence of drowsiness did not exceed that in the placebo group. In clinical trials desloratadine did not affect the psychomotor function when taking a dose of up to 7.5 mg.

Pharmacokinetics:

Desloratadine begins to be detected in the blood plasma for 30 minutes after application. Elisei effectively controls the symptoms within 24 hours. The maximum concentration of desloratadine in blood plasma is reached on average after 3 hours, the half-life period averages 27 hours. The degree of cumulation of desloratadine corresponds to its half-life (approximately 27 hours) and the frequency of application (1 time per day). The bioavailability of desloratadine was proportional to the dose in the range of 5 to 20 mg.

Desloratadine moderately (83-87%) binds to blood plasma proteins.With the use of desloratadine in a dose of 5 to 20 mg once a day for 14 days, no signs of clinically significant cumulation of the drug were detected.

Desloratadine does not penetrate the blood-brain barrier.

Intensively metabolized in the liver by hydroxylation to form 3-OH-desloratadine. linked to glucuronide. Only a small part of the dose taken internally is excreted by the kidneys (<2%) and through the intestine (<7%) in unchanged form.

When conducting pharmacokinetic studies in pediatric practice, it was found that the indicators AUC and FROM_mOh desloratadine (when used in the recommended doses) can be equated to the same indicators in adults who took desloratadine in the form of a syrup in a dose of 5 mg.

The results of the studies showed that desloratadine Do not depress CYP3A4 or CYP2D6 and is neither a substrate nor an inhibitor of the P-glycoprotein.

Food (fatty high-calorie breakfast) or grapefruit juice does not affect the distribution of desloratadine.

Indications:

To eliminate the symptoms associated with allergic rhinitis, such as sneezing, nasal discharge, itching, edema and nasal congestion, and itching and redness of the eyes, lacrimation, itching of the palate and coughing.

To eliminate symptoms associated with hives, such as itching and rashes.

Contraindications:

Hypersensitivity to the active substance or to any of the components of the drug.

Pregnancy and the period of breastfeeding.

Children up to 6 months.

Hereditary transmitted - intolerance to fructose, a violation of absorption of glucose-galactose or insufficiency of sucrose-isomaltase in the body (due to the presence of sucrose and sorbitol in the composition).

Carefully:

Severe kidney failure.

Pregnancy and lactation:

The safety of the drug during pregnancy is not established, so the use of Elisei in this period is not recommended.

Desloratadine penetrates into breast milk, so the use of Elisei in women breastfeeding is not recommended.

Dosing and Administration:

Take inside regardless of food intake, washing down with a small amount of water.

Children:

- from 6 to 12 months: 2 ml of syrup (1 mg desloratadine) once a day;

- from 1 to 5 years: 2.5 ml of syrup (1.25 mg desloratadine) once a day;

- from 6 to 11 years: 5 ml of syrup (2.5 mg desloratadine) once a day.

Adults and teenagers from age 12: 10 ml of syrup (5 mg desloratadine) once a day.

To dispense the drug, it is recommended to use a dispensing spoon or a dispensing glass with the appropriate divisions.

The duration of treatment depends on the severity and course of the disease.

Treatment of intermittent allergic rhinitis (the presence of symptoms less than 4 days a week or less than 4 weeks) should be done taking into account the history of the patient: stop after the disappearance of symptoms and resume after their re-occurrence.

With persistent allergic rhinitis (the presence of symptoms more than 4 days a week or more than 4 weeks) it is necessary to continue treatment throughout the period of contact with the allergen.

Side effects:

In children under 2 years, the following adverse events were noted, the frequency of which was slightly higher than with placebo (≥ 1/100 to <1/10): diarrhea (3.7% of cases), body temperature increase (2, 3%), insomnia (2.3%).

In children between the ages of 2 and 11 years with the use of the drug Elisei, syrup, the incidence of side effects was the same as with the placebo.

In adults and adolescents (12 years and older) the incidence of side effects was slightly higher compared with placebo (≥ 1/100 to <1/10), of which the most common were: increased fatigue (1.2%), dry mouth (0.8%), headache ( 0.6%).

When using the drug Elisei, syrup in adults and adolescents at the recommended dose of 5 mg per day, the incidence of drowsiness was not higher than with placebo.

Among the very rare side effects (<1/10 000) are the following:

from the nervous system: hallucinations, dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions;

from the liver and biliary tract: increased activity of liver enzymes, increased concentrations of bilirubin, hepatitis:

from the digestive system: abdominal pain, nausea, vomiting, indigestion, diarrhea;

from the cardiovascular system: tachycardia, palpitations, lengthening of the interval QT;

from the musculoskeletal system: myalgia;

allergic reactions: anaphylaxis, angioedema, dyspnea, pruritus, rash, including urticaria.

From the skin and subcutaneous tissues photosensitivity is possible.

Postpayment period

Children.

Frequency unknown: lengthening interval QT, arrhythmia, bradycardia.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms. Taking a dose that exceeds the recommended dose by 5 times did not lead to any symptoms. In clinical trials, the daily use of desloratadine in adults and adolescents at a dose of up to 20 mg for 14 days was not accompanied by statistically or clinically significant changes in the cardiovascular system. In the clinico-pharmacological study, the use of desloratadine at a dose of 45 mg / day (9 times higher than recommended) for 10 days did not cause lengthening of the interval QT and there were no serious side effects.

Treatment. If you ingest large amounts of the drug, you should immediately consult a doctor. Recommended gastric lavage, reception of activated charcoal; if necessary, symptomatic therapy. Desloratadine not excreted in hemodialysis; the effectiveness of peritoneal dialysis is not established.

Interaction:

Clinically significant changes in the plasma concentration of desloratadine with repeated combined use together with ketoconazole. erythromycin, azithromycin, fluoxetine, cimetidine was not detected.

Due to the fact that the enzyme responsible for the metabolism of desloratadine. not established, the possibility of interaction with other drugs can not be completely ruled out.

Eating or grapefruit juice does not affect the effectiveness of desloratadine.

Elisei does not increase the effect of alcohol on the central nervous system. Nevertheless, during the post-registration use cases of alcohol and alcohol intolerance were reported. therefore desloratadine Alcohol should be used with caution.

Special instructions:

Elisei does not enhance alcohol effects such as impairment of psychomotor function and drowsiness.

In patients with high renal insufficiency, the use of Elisei should be performed under the supervision of a physician.

The drug contains sorbitol, so it is contraindicated to use in patients with congenital intolerance to fructose.

Studies of the effectiveness of desloratadine in rhinitis of infectious etiology were not conducted.

Children. The effectiveness and safety of the use of Elisei syrup for children under 6 months are not established, therefore it is contraindicated to apply it to patients of this age category.

Effect on the ability to drive transp. cf. and fur:

Consideration should be given to the potential for the development of side effects such as dizziness and drowsiness. When these undesirable phenomena appear, one should refrain from performing these activities.

Form release / dosage:

Syrup, 0.5 mg / ml.

Packaging:

For 60 ml or 100 ml in glass bottles with a screw neck of brown color, capped with screw caps with a thread with an opening control ring.

The label is self-adhesive on the vial.

Each vial with a spoon, a dosing, a dispensing glass and instructions for medical use is placed in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use the product after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003759

Date of registration:27.07.2016

Expiration Date:27.07.2021

The owner of the registration certificate:FARMAK, PAO FARMAK, PAO Ukraine

Manufacturer: & nbsp

FARMAK, PAO Ukraine

Representation: & nbspFARMAK PAOFARMAK PAO

Information update date: & nbsp21.08.2016

Illustrated instructions

Instructions

The Elisei (Elizey)