Universal reference book for medicines
Product name: LORDESTIN (LORDESTIN)

Active substance: desloratadine

Type: The blocker of histamine H 1 -receptors.
Anti-allergic drug
Composition, form of production and packaging
? The syrup is transparent, colorless, with the smell of almonds.
1 ml

desloratadine hemisulphate 0.578 mg,

which corresponds to the content of desloratadine 0.5 mg

Auxiliary substances: propylene glycol 150 mg, sorbitol (liquid non-crystallizing) 70% 150 mg, citric acid 4.6 mg, sodium citrate dihydrate 1.26 mg, sodium cyclamate 5 mg, hypromellose -2910 3.5 mg, disodium edetate dihydrate 0.25 mg, almond flavoring - 0.75 mg, water - up to 1 ml.

60 ml - bottles of dark glass (1) complete with a dosing cup - packs of cardboard.

120 ml - bottles of dark glass (1) complete with a dosing cup - packs of cardboard.

150 ml - bottles of dark glass (1) complete with a dispensing cup - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2016.

PHARMACHOLOGIC EFFECT

Desloratadine is a long-acting histamine antagonist.
It is the primary active metabolite of loratadine. Inhibits a whole cascade of reactions of allergic inflammation, incl. - release of pro-inflammatory cytokines, such as interleukins IL-4. IL-6, IL-8 and IL-13, release of pro-inflammatory chemokines (RANTES), production of superoxide anions by activated polymorphonuclear neutrophils, chemotaxis and adhesion of eosinophils, isolation of adhesion molecules such as P-selectin, IgE-dependent release of histamine, prostaglandin D2 and leutrotrieia C4. Thus, desloratadin prevents development and facilitates the course of allergic reactions, and also possesses antipruritic and antiexclusive action, reduces permeability of capillaries, prevents the development of edema of tissues and spasm of smooth muscles.
The drug has no effect on the central nervous system, almost no sedative effect (does not cause drowsiness) and does not affect the rate of psychomotor reactions.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

Suction

Desloratadine is well absorbed into the digestive tract.
It is determined in the blood plasma 30 minutes after ingestion.
Distribution

C max in blood plasma is achieved, on average, 3 h after administration.
Does not penetrate the blood-brain barrier. 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 was no clinically significant cumulation of the drug. Simultaneous intake of food or grapefruit juice did not affect the distribution of desloratadine when administered at a dose of 7.5 mg 1 time / day.
Metabolism

Desloratadine nc is an inhibitor of CYP3A4 and CYP2D6 isoenzymes and is not a substrate or an inhibitor of P-glycoprotein.
Intensively metabolized in the liver by hydroxylation to form 3-OH-desloratadine glucuronide.
Excretion

Only a small part of the dose taken internally is excreted unchanged by the kidneys (<2%) and through the intestine (<7%), the largest part is excreted as metabolites by the kidneys and through the intestine in approximately equal amounts.
T 1/2 is 20-30 hours (on the average - 27 hours).
INDICATIONS

- Allergic rhinitis (relief or elimination of sneezing, nasal congestion, removal of mucus from the nose, itching of the nose, itching of the palate, redness and itching of the eyes, lachrymation);

- urticaria (reduction or elimination of itching, rash).

DOSING MODE

Inside.
Syrup should be taken regardless of food intake, washed down with a small amount of water.
Children aged 1 to 5 years: 1.25 mg (2.5 ml syrup) 1 time / day.

Children aged 6 to 11 years: 2.5 mg (5 ml syrup) 1 time / day.

Adults and adolescents from 12 years: 5 mg (10 ml of syrup) 1 time / day.

For proper dosing, use the supplied plastic dispensing cup, graduated from 2.5 ml to 20 ml.

SIDE EFFECT

In children less than 2 years old, when using Lordestine syrup 0.5 mg / ml, the following undesirable reactions were noted, the frequency of which was higher than with placebo: diarrhea, fever, insomnia.

In children aged 2 to 11 years with the use of lordestine syrup 0.5 mg / ml, the incidence of side effects was the same as with placebo.

In adults and adolescents (12 years and older) with the use of Lordestine syrup 0.5 mg / ml, the following adverse events were observed, the frequency of which was higher than with placebo: increased fatigue (1.2%), dry mouth (0.8%), headache (0.6%).

With the use of lordestine syrup 0.5 mg / ml in adults and adolescents at the recommended dose of 5 mg per day, the incidence of drowsiness was not higher than with placebo.

During post-marketing use, other side effects were very rare (1/10 000 prescriptions (less than 0.01%)):

On the part of the immune system: allergic reactions (anaphylaxis, angioedema, itching, rash, urticaria, dyspnea).

From the nervous system: dizziness, drowsiness, hallucinations, psychomotor hyperactivity, convulsions.

From the heart: tachycardia, palpitations.

From the gastrointestinal tract: abdominal pain, nausea, vomiting, indigestion, diarrhea.

From the liver and bile ducts: increased bilirubin concentration in the blood plasma, increased activity of "hepatic" enzymes, hepatitis.

From the musculoskeletal and connective tissue: myalgia.

From the skin and subcutaneous tissues: photosensitization.

If you worsen the course of any of these reactions or if a new one occurs, you should immediately consult a doctor.

CONTRAINDICATIONS

- hypersensitivity to the components of the drug;

- Pregnancy and lactation;

- age up to 1 year;

- hereditarily transmitted disorders - intolerance or impairment of absorption of sorbitol, sorbitol dehydrogenase deficiency (lordestin syrup 0/5 mg / ml contains sorbitol, intolerance or impairment of absorption of sorbitol is often accompanied by intolerance to other sugars, for example, fructose).

Carefully

- severe renal failure.

PREGNANCY AND LACTATION

The use of the drug in pregnant women is contraindicated due to the lack of clinical data on the safety of the application of lordestine syrup 0.5 mg / ml during pregnancy.

Desloratadine is excreted in breast milk, therefore it is contraindicated to administer lordestin * 0.5 mg / ml syrup during breastfeeding.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution apply the drug to patients with severe renal failure.

APPLICATION FOR CHILDREN

Contraindicated in children under the age of 1 year.

Children aged 1 to 5 years: 1.25 mg (2.5 ml syrup) 1 time / day.

Children aged 6 to 11 years: 2.5 mg (5 ml syrup) 1 time / day.

Adults from 12 years: 5 mg (10 ml of syrup) 1 time / day.

SPECIAL INSTRUCTIONS

The shelf life of the drug after the first opening of the vial is 28 days.

Use in children

The effectiveness and safety of the use of lordestin syrup 0.5 mg / ml in children under the age of 1 year is not established.

In most cases, rhinitis in children under 2 years of age is of an infectious nature.
Studies of the efficacy of lordestine syrup 0.5 mg / ml in rhinitis of infectious etiology were not conducted.
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, as well as physical examination, laboratory tests and skin tests.
Severe kidney failure

In patients with severe renal failure or on hemodialysis, the concentration of desloratadine in the blood plasma increases by 1.7 and 2.5 times, respectively.
A minimal change in the concentration of 3-hydroxydesloragadine was detected. Desloratadine and 3-hydroxydesloratedadine are poorly derived from dialysis. Impaired renal function does not affect the binding of desloratadine and 3-hydroxydeslorotadine to plasma proteins. Based on the pharmacokinetics of lordestine syrup 0.5 mg / ml, caution should be exercised when using the drug in patients with renal insufficiency.
Influence on the ability to drive and work with machinery

In recommended doses, lordestin syrup 0.5 mg / ml does not affect the ability to drive vehicles and work with mechanisms.

OVERDOSE

Symptoms

Taking a dose that exceeds the recommended dose five times does 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 a clinical pharmacological study, the use of desloratadine at a dose of 45 mg / day (9 times higher than recommended) for 10 days did not cause prolongation of the QT interval and was not accompanied by 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 is not excreted in hemodialysis, the effectiveness of peritoneal dialysis is not established.
DRUG INTERACTION

In the study of drug interaction with repeated combined use of desloratadine with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine, clinically significant changes in the concentration of desloratadine in plasma ns have been revealed.
Eating does not affect the effectiveness of the drug. Lordestine syrup 0.5 mg / ml does not enhance the effect of alcohol on the central nervous system.
No interaction with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine



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 in a place protected from light and inaccessible to children at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
Do not use after the expiry date shown on the package.

Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!