Composition, form of production and packaging
? The solution for oral administration is clear, colorless, free from foreign particles.
1 ml
desloratadine 0.5 mg
Auxiliary substances: sorbitol 147.15 mg, propylene glycol 102.3 mg, citric acid monohydrate 21.06 mg, sodium citrate dihydrate 16.38 mg, hypromellose 2910 mg 2 mg, sucralose 1 mg, disodium edetate 0.04 mg, flavor tutti-frutti, - 0.03 mg.
50 ml - bottles of dark glass (1) complete with a measuring spoon with a volume of 2.5 ml or 5 ml or a 5 ml syringe dispenser - packs of cardboard.
60 ml - bottles of dark glass (1) complete with a measuring spoon with a volume of 2.5 ml or 5 ml or a syringe dispenser with a volume of 5 ml - packs of cardboard.
100 ml - bottles of dark glass (1) complete with a measuring spoon with a volume of 2.5 ml or 5 ml or a syringe dispenser with a volume of 5 ml - packs of cardboard.
120 ml - bottles of dark glass (1) complete with a measuring spoon with a volume of 2.5 ml or 5 ml or a 5 ml syringe dispenser - packs of cardboard.
150 ml - bottles of dark glass (1) complete with a measuring spoon with a volume of 2.5 ml or 5 ml or a syringe dispenser with a volume of 5 ml - packs of cardboard.
300 ml - bottles of dark glass (1) complete with a measuring spoon with a volume of 2.5 ml or 5 ml or a 5 ml syringe dispenser - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
An antihistamine long-acting drug, a blocker of peripheral histamine H 1 -receptors. Desloratadine is the primary active metabolite of loratadine. Inhibits a cascade of reactions of allergic inflammation, incl. release of pro-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, release of pro-inflammatory chemokines, production of superoxide anions by activated polymorphonuclear neutrophils, adhesion and chemotaxis of eosinophils, isolation of adhesion molecules such as P-selectin, IgE- mediated release of histamine, prostaglandin D 2 and leukotriene C 4 . Thus, the drug prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action, reduces permeability of capillaries, prevents the development of edema of tissues, spasm of smooth muscles.
The drug has no effect on the central nervous system, has almost no sedative effect (does not cause drowsiness) and does not affect the rate of psychomotor reactions when taken in the recommended doses. Does not cause an extension of the QT interval on the ECG.
The action of desloratadine begins within 30 minutes after ingestion and lasts for 24 hours.
PHARMACOKINETICS
The use of desloratadine in the form of a solution for oral administration is equivalent to its use in the form of tablets containing a similar amount of active substance.
Suction
After taking the drug inside desloratadine is well absorbed from the digestive tract. It is determined in the blood plasma after 30 minutes, and C max is reached after about 3 hours. There were no clinically significant changes in the concentration of desloratadine in the blood plasma with multiple administration of ketoconazole and erythromycin. Bioavailability of desloratadine is proportional to the dose when taking a dose in the range from 5 mg to 20 mg.
Distribution
Binding to plasma proteins 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 a clinically significant cumulation of desloratadine. The degree of cumulation of desloratadine is consistent with the value of T 1/2 and the frequency of its application 1 time / day.The values ​​of AUC and C max in children were similar to those in adults receiving 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
Enzymes responsible for the metabolism of desloratadine are not yet known, so it is impossible to completely exclude interactions with certain drugs. It is not an inhibitor of CYP3A4 and CYP2D6 and is not a substrate or an inhibitor of P-glycoprotein. Intensively metabolized in the liver by hydroxylation to form 3-OH-desloratadine, which is then glucuronized.
Excretion
T 1/2 is about 27 hours. Desloratadine is excreted from the body in the form of a glucuronide compound and in small amounts in unchanged form (with urine less than 2% and through the intestine - less than 7%).
INDICATIONS
To ease or eliminate symptoms:
- Allergic rhinitis (sneezing, stuffy nose, rhinorrhea, itching in the nose, itching of the palate, itching and redness of the eyes, lacrimation);
- urticaria (skin itching, rash).
DOSING MODE
Is taken orally, regardless of food intake.
Children aged 1 to 5 years - 2.5 ml of the solution (1.25 mg) 1 time / day.
Children aged 6 to 11 years - 5 ml of solution (2.5 mg) 1 time / day.
Adults and adolescents (12 years and older) - 10 ml of solution (5 mg) 1 time / day.
SIDE EFFECT
In children aged 2 to 11 years with the use of desloratadine, the incidence of side effects was the same as with placebo.
In children younger than 2 years with the use of desloratadine, the following side effects were observed, the frequency of which was slightly higher than with placebo: diarrhea (3.7%), fever (2.3%), insomnia (2.3%).
In adults and adolescents aged 12 years and over, the following side effects were observed with the use of desloratadine, the frequency of which was slightly higher than with placebo: fatigue (1.2%), dry mouth (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 with placebo.
In the course of post-marketing surveillance, it is very rare The following adverse reactions were noted.
Mental disturbances: hallucinations.
From the side of the central nervous system: dizziness, drowsiness, insomnia, psychomotor hyperactivity.
From the cardiovascular system: tachycardia, a feeling of palpitations.
On the part of the digestive system: abdominal pain, nausea, vomiting, indigestion, diarrhea.
From the liver and bile ducts: increased activity of liver enzymes, increased bilirubin concentration, hepatitis.
From the musculoskeletal system: myalgia.
Allergic reactions: anaphylaxis, angioedema, itching, rash, urticaria.
CONTRAINDICATIONS
- hypersensitivity to the active or any auxiliary substance of the drug;
- Pregnancy;
- the period of lactation (breastfeeding);
- Children under 1 year of age (efficacy and safety not established);
- hereditary diseases - intolerance to fructose, impaired absorption of glucose / galactose or insufficiency of sugarase / isomaltase in the body (due to the presence of sorbitol in the formulation).
With caution should be used in patients with severe renal failure.
PREGNANCY AND LACTATION
The purpose of the drug during pregnancy is contraindicated in connection with the lack of clinical data on the safety of its use in this period.
Desloratadine is excreted in breast milk, therefore its use during breastfeeding is contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should be used in severe renal failure.
APPLICATION FOR CHILDREN
Contraindicated appointment of children under 12 years of age, tk. efficiency and safety are not established.
SPECIAL INSTRUCTIONS
The effectiveness and safety of the drug Dezal in children under the age of 1 year is not established.
Differential diagnosis between allergic rhinitis and rhinitis of a different origin in children under 2 years of age presents certain difficulties. When making a differential diagnosis, attention should be paid to the presence or absence of foci of infection or structural anomalies of the upper respiratory tract, to conduct a careful history, examination, as well as appropriate laboratory tests and skin tests.
Approximately 6% of adults and children aged 2 to 11 years experience a low ability of desloratadine to metabolize, desloratadine is slower in this group of patients.The safety profile of desloratadine in children aged 2 to 11 years with a low level of metabolism is similar to that in children with normal metabolism of desloratadine. The effect of desloratadine on children younger than 2 years with a low level of metabolism has not been studied.
In the case of severe renal dysfunction, Dezal should be taken with caution.
Impact on the ability to manage vehicles and mechanisms
AT studies of the influence of desloratadine on the ability to drive vehicles there was no violation of concentration. However, it should be borne in mind that very rarely some patients develop drowsiness, in this case care should be taken when driving vehicles and when working with mechanisms.
OVERDOSE
Symptoms: taking in a dose exceeding the recommended dose 9 times (45 mg) did not lead to the appearance of any clinically significant symptoms. Possible development of drowsiness.
Treatment: it is necessary to wash the stomach, taking activated charcoal; if necessary, symptomatic therapy. Desloratadine is not excreted in hemodialysis, the effectiveness of peritoneal dialysis is not established.
If a large amount of the drug is ingested inadvertently, the patient should urgently consult a doctor.
DRUG INTERACTION
Clinically significant interaction with other drugs has not been identified (including with ketoconazole and erythromycin).
Desloratadine does not enhance the effect of ethanol on the central nervous system.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 3 years.
