Allerway Express, 5 mg 10 pcs

Pharmacotherapeutic group: anti-allergic agent – H1-histamine receptor blocker.

The ATC code: R06AE09

Pharmacological properties

Pharmacodynamics

Levocetirizine (R)-enantiomer of cetirizine is an inhibitor of peripheral H1-histamine receptors.

Levocetirizine has a pronounced antihistamine and anti-allergic effect. It influences the histamine-dependent phase of the allergic reaction, decreases migration of eosinophils, reduces the permeability of the vascular wall and limits the release of inflammatory mediators.

Levocetirizine prevents the development and facilitates allergic reactions, has antipruritic and antiexudative actions. It has practically no effect on cholinergic and serotonin receptors and has no sedative effect in therapeutic doses.

Pharmacokinetics

The pharmacokinetics of levocetirizine changes linearly.

Intake

After oral administration, the drug is quickly and completely adsorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although the speed of absorption is reduced. In adults, after a single therapeutic dose (5 mg) the maximum concentration (Cmax) in plasma is 270 ng/ml, reached after 0.9 hours, after reuptake in 5 mg dose – 308 ng/ml. The equilibrium plasma concentration (Css) is reached after 2 days.
Distribution

Levocetirizine is 90% bound to blood plasma proteins. Volume of distribution (Vd) is 0.4 l/kg. Bioavailability reaches 100%.

Metabolism

Less than 14% of the drug is metabolized in the body by N- and O-dealkylation (unlike other H1-histamine receptor antagonists, which are metabolized in the liver via the cytochrome system) to form a pharmacologically inactive metabolite.

Owing to limited metabolism and absence of metabolic inhibitory activity, interaction of levocetirizine at the metabolic level with other substances is unlikely.

Elimination

In adults the half-life (T1/2) is 7.9±1.9 hours, total clearance is 0.63 ml/min/kg.
About 85.4% of the administered dose is excreted unchanged by kidneys via glomerular filtration and tubular secretion; about 12.9% – via intestine.

Peculiarities of pharmacokinetics in individual patients

Patients with impaired renal function

. In patients with renal impairment (creatinine clearance (CK) < 40 ml/min) the drug clearance is decreased and T1/2 is prolonged. In patients on hemodialysis total clearance is decreased by 80%, which requires a change in dosing regimen. Less than 10% of levocetirizine is eliminated during a standard 4-hour hemodialysis procedure.

Indications

Active ingredient

Composition

Each tablet dispersible in the mouth contains:

The active ingredient: levocetirizine dihydrochloride 5.00 mg;

Auxiliary substances: Betadex, mannitol, colloidal anhydrous silica, corn starch, anhydrous citric acid, microcrystalline cellulose (102), crospovidone, aspartame, magnesium stearate.

How to take, the dosage

Ingestion.

Place the tablet on the tongue where it will immediately begin to dissolve. Hold it in the mouth for a few seconds until it is completely dissolved.

The oral tablet does not require water to swallow, does not increase saliva production, and is appropriate for patients with swallowing difficulties and behavioral and neurologic disorders.

Special instructions for handling the drug

Do not squeeze the tablets through the foil of the package! Remove tablets dispersed in the mouth as follows:

1. Fold the blister along the tear line.

2. open the blister by gently pulling on the edge of the foil.

3. Carefully remove the tablet.

Adults and children over 6 years of age

The daily dose is 5 mg (1 tablet) once.

The duration of treatment with the drug

When treating seasonal (intermittent) allergic rhinitis (presence of symptoms less than 4 days per week or their total duration of less than 4 weeks), the duration of treatment depends on the duration of symptoms; treatment can be stopped when symptoms disappear and restarted when they appear.

When treating year-round (persistent) allergic rhinitis (presence of symptoms more than 4 days per week and their total duration of more than 4 weeks), treatment may continue for the duration of allergen exposure.

There is clinical experience with continuous use of levocetirizine in adult patients for up to 6 months.

If you are taking or have recently taken other medications, tell your doctor.

If you forget to take the medication, do not take a double dose to make up for a missed dose, take the next dose at the usual time.

Particular patient groups

The main route of levocetirizine excretion from the body is by the kidneys, so when using the drug in elderly patients and patients with renal failure, the dose must be adjusted according to the degree of renal failure, based on the creatinine clearance score (ml/min).

Patients with mild renal impairment (creatinine clearance 50-79 ml/min) do not require dose adjustment.

In patients with moderate renal impairment (creatinine clearance 30 to 49 mL/min), the recommended dose is 5 mg every other day.

In patients with severe renal impairment (creatinine clearance less than 30 mL/min), the recommended dose is 5 mg once every 3 days.

In patients with renal and hepatic impairment, the dosing regimen is as described above.

Patients with hepatic impairment only do not need to adjust the dosing regimen.

Interaction

The study of interaction of levocetirizine with other medicinal products has not been conducted.

In the study of drug interactions of cetirizine racemate with antipyrine, azithromycin, cimetidine, diazepam, erythromycin, glipizide, ketoconazole, pseudoephedrine and phenazone no clinically significant adverse interactions were found.

Concomitant administration with theophylline (400 mg/day) decreases total clearance of cetirizine by 16% (theophylline kinetics is not changed).

In a study with concomitant administration of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), cetirizine exposure was shown to increase by 40% and ritonavir exposure was not significantly altered (-11%).

In some cases, concomitant use of levocetirizine with alcohol or medications that have an inhibitory effect on the central nervous system (CNS) may cause lethargy and impaired performance.

Special Instructions

Dose intervals should be adjusted individually depending on renal function.

Cautious use with alcohol is recommended.

The drug contains aspartame, a source of phenylalanine, which may be dangerous for patients with phenylketonuria.

In patients with predisposing factors to urinary retention (e.g., spinal cord injury, prostatic hyperplasia), caution should be exercised because levocetirizine may increase the risk of urinary retention.

Caution should be exercised in patients with epilepsy and increased seizure readiness because levocetirizine may cause exacerbation of seizures.

The reaction to skin allergy tests is suppressed by antihistamines, and the drug should be withheld for 3 days before testing.

Itching may occur after discontinuation of levocetirizine, even if there were no such symptoms at the beginning of treatment. The symptoms may go away on their own.

In some cases the symptoms may be severe, and this may require resuming treatment.

The symptoms should go away when treatment resumes.

Children

Levocetirizine oral dispersible tablets are contraindicated in children under 6 years of age because this dosage form does not allow for a suitable dosage for this age group. It is recommended to use the pediatric dosage form (oral drops).

Impact on the ability to drive, operate machinery

Levocetirizine may lead to increased somnolence; therefore, Allerwei Express may affect the ability to drive or operate machinery. During treatment it is necessary to refrain from engaging in potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Synopsis

Circular, flat tablets with beveled edges, white to almost white in color.

Contraindications

With caution

Side effects

Clinical Studies

During clinical trials in men and women 12-71 years of age, the following side effects occurred with an incidence of 1% or greater (often ≥ 1/100, < 1/10): headache, drowsiness, dry mouth, fatigue, infrequent (≥ 1/1000, < 1/100) occurrence of asthenia and abdominal pain.

Headache and somnolence occurred with an incidence of 1% or more (often ≥ 1/100, < 1/10) in children aged 6 years to 12 years during clinical trials.

Post-registration studies:

General disorders:

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

Overdose

Symptoms: drowsiness (in adults), at first there may be agitation and restlessness, followed by drowsiness (in children).

Treatment: It is necessary to flush the stomach or take activated charcoal if little time has passed after taking the drug. Symptomatic and supportive therapy is recommended. There is no specific antidote. Hemodialysis is not effective.

Pregnancy use

Pregnancy

The data on the use of levocetirizine in pregnancy are scarce or limited (less than 300 pregnancy outcomes). However, the use of cetirizine, the racemate of levocetirizine, in pregnancy (more than 1000 pregnancy outcomes) was not accompanied by malformations and intrauterine and neonatal toxic effects. No direct or indirect adverse effects on pregnancy, fetal and foetal development, labor and postnatal development were found in animal studies.

The use of levocetirizine in pregnancy may be considered if necessary.

Breastfeeding period

Cetirizine, the racemate of levocetirizine, is excreted with breast milk. Therefore, excretion of levocetirizine with breast milk is also likely. Breast-fed children may have adverse reactions to levocetirizine. Therefore, caution should be exercised when prescribing levocetirizine during breastfeeding.

Fertility

There are no clinical data on levocetirizine.

Consult your doctor before using the drug if you are pregnant, or if you think you might be pregnant, or are planning to become pregnant.