Allerway Express dispersible tablets 5mg, No. 10

• Treating symptoms of allergic rhinitis (including perennial (persistent) and seasonal (intermittent) allergic rhinitis) and allergic conjunctivitis, such as itching, sneezing, nasal congestion, rhinorrhea (nasal discharge), lacrimation, conjunctival hyperemia (redness of the eyes).

• Pollinosis (hay fever).

• Hives.

• Other allergic dermatoses, accompanied by itching and rashes.

Inside.

Place the tablet on your tongue, where it begins to dissolve immediately. Keep in the mouth for a few seconds until completely absorbed.

Taking tablets dispersed in the oral cavity does not require drinking water, does not affect the increase in saliva production, and allows patients with deviations in the act of swallowing with behavioral and neurological disorders to take the drug.

Special instructions for handling the drug

Do not squeeze tablets through the foil of the packaging! To remove the orodispersible tablets, proceed as follows:

1. Bend 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 old

The daily dose is 5 mg (1 tablet) as a single dose.

Duration of taking the drug

In the treatment of seasonal (intermittent) allergic rhinitis (the presence of symptoms less than 4 days a week or their total duration is less than 4 weeks), the duration of treatment depends on the duration of the symptomatology; treatment can be stopped when symptoms disappear and resumed when symptoms appear.

In the treatment of perennial (persistent) allergic rhinitis (the presence of symptoms more than 4 days a week and their total duration of more than 4 weeks), treatment can be continued during the entire period of exposure to allergens.

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

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

If you forget to take a drug, do not take a double dose to compensate for the missed dose, take the next dose at the usual time.

Special patient groups

The main way of excretion of levocetirizine from the body is renal excretion, therefore, when using the drug in elderly patients and with renal insufficiency, the dose should be adjusted depending on the degree of renal failure, based on the assessment of creatinine clearance (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 from 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 every 3 days.

For patients with renal and hepatic insufficiency, dosing is carried out according to the above scheme.

Patients with impaired liver function alone do not require dosage adjustment.

Each orodispersible tablet contains:

active substance: levocetirizine dihydrochloride 5.00 mg;

excipients: betadex, mannitol, anhydrous colloidal silicon dioxide, corn starch, anhydrous citric acid, microcrystalline cellulose (102), crospovidone, aspartame, magnesium stearate.

• Hypersensitivity to the active substance, cetirizine, hydroxyzine, any piperazine derivative or to any other excipient of the drug.

• End-stage renal failure (CC <10 ml / min).

• Homozygous phenylketonuria (the drug contains aspartame).

• Children under 6 years of age (for this dosage form).

  Carefully

• With chronic renal failure (correction of the dosage regimen is necessary). In elderly patients (with age-related decrease in glomerular filtration). In patients with spinal cord injury, prostatic hyperplasia, as well as in the presence of other predisposing factors to urinary retention, since levocetirizine may increase the risk of urinary retention. With simultaneous use with alcohol (see section 'Interaction with other medicinal products'). In patients with epilepsy and increased convulsive readiness, since levocetirizine can exacerbate seizures.

Pharmacodynamics

Levocetirizine is the active ingredient of Allerway Express - the (R) -enantiomer of cetirizine, a powerful and selective histamine antagonist that blocks histamine H1 receptors.

Levocetirizine affects the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators.

Levocetirizine prevents the development and facilitates the course of allergic reactions, has an anti-exudative and antipruritic effect, practically does not have an anticholinergic and antiserotonin effect. In therapeutic doses, it does not have a sedative effect.

With a single use of levocetirizine, binding to receptors is 90% after 4 hours and 57% after 24 hours.

The use of levocetirizine at a dose of 5 mg significantly reduces the formation of urticarial elements (blisters) in the first 12 hours, this effect lasts up to 24 hours, compared with placebo.

Pharmokinetics

Pharmacokinetic parameters of levocetirizine vary linearly.

Suction

After oral administration, the drug is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although it reduces its speed. The maximum concentration (Cmax) in blood plasma is reached after 0.9 hours and is 270 ng / ml, the equilibrium concentration is reached after 2 days.

After taking Allerway Express 5 mg tablets by healthy volunteers on an empty stomach, levocetirizine was determined in the blood after 24 hours at a concentration exceeding 10% of Cmax.

Distribution

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

Metabolism

In small amounts (less than 14%), levocetirizine is metabolized in the body by N- and O-dealkylation (unlike other antagonists of H1-histamine receptors, which are metabolized in the liver by the cytochrome system) with the formation of a pharmacologically inactive metabolite. Due to the insignificant metabolism and lack of metabolic potential, the interaction of levocetirizine with other drugs seems unlikely.

Withdrawal

The half-life (T1 / 2) in adults is 7.9 ± 1.9 hours. In young children, T1 / 2 is shorter. In adults, the total clearance is 0.63 ml / min / kg.

About 85.4% of the taken dose of the drug is excreted by the kidneys unchanged by glomerular filtration and tubular secretion; about 12.9% - through the intestines.

Separate patient groups

Patients with renal impairment

In patients with renal insufficiency (creatinine clearance (CC) <40 ml / min), the clearance of the drug decreases. In patients on hemodialysis, the total clearance is reduced by 80%.

Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

Patients with hepatic impairment

The pharmacokinetics of levocetirizine in patients with hepatic impairment has not been studied. In patients with chronic liver diseases (hepatocellular, cholestatic and biliary cirrhosis) who received the racemic compound cetirizine at a dose of 10 mg or 20 mg once, there was an increase in T1 / 2 by 50% and a decrease in drug clearance by 40%, compared with healthy people.

Children

Data on the study of the pharmacokinetics of the drug in 14 children aged 6 to 11 years with a body weight of 20 to 40 kg with a single oral intake of 5 mg of levocetirizine showed that the Cmax values ??and the area under the concentration-time pharmacokinetic curve (AUC) were approximately two times higher than those in healthy adults with crossover control. The average Cmax was 450 ng / ml, the maximum concentration was reached on average after 1.2 hours, the total clearance, taking into account body weight, was 30% higher, and T1 / 2 was 24% shorter in children than the corresponding indicators in adults. Special pharmacokinetic studies have not been performed in children under 6 years of age. Retrospective pharmacokinetic analysis was performed in 323 patients (181 children aged 1 to 5 years,18 children aged 6 to 11 years and 124 adults aged 18 to 55) who received one or more doses of levocetirizine from 1.25 mg to 30 mg. The data obtained during the analysis showed that taking the drug at a dose of 1.25 mg in children aged 6 months to 5 years leads to a plasma concentration corresponding to that in adults when taking 5 mg of the drug once a day.

Elderly patients

Pharmacokinetic data in elderly patients are limited. With repeated administration of 30 mg of levocetirizine once a day for 6 days in 9 elderly patients (age 65 to 74 years), the total clearance was approximately 33% lower than that in younger adults. The distribution of cetirizine racemate has been shown to be more dependent on renal function than age. This statement can also be applied to levocetirizine, since both drugs - both levocetirizine and cetirizine - are excreted primarily by the kidneys.

Therefore, in elderly patients, the dose of levocetirizine should be adjusted depending on renal function.

Overdose

Symptoms: drowsiness (in adults), at first excitement and anxiety may appear, then alternating with drowsiness (in children).

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

Side effects

Uncommon (0.1-1%): Abdominal pain.

Post-registration studies

During the period of post-registration use of the drug, the following side effects were observed.

Immune system disorders

Hypersensitivity reactions, including anaphylaxis.

Metabolic and nutritional disorders

Increased appetite.

Mental disorders

Anxiety, aggression, agitation, hallucinations, depression, insomnia, suicidal ideation, nightmares.

Nervous system disorders

Convulsions, sinus thrombosis of the dura mater, paresthesia, dizziness, fainting, tremor, dysgeusia.

Violations of the organ of vision

Inflammatory manifestations, visual impairment, blurred vision, involuntary movements of the eyeballs (nystagmus).

Heart disorders

Angina pectoris, tachycardia, palpitations.

Vascular disorders

Jugular vein thrombosis.

Respiratory, Chest and Mediastinal Disorders

Increased symptoms of rhinitis, shortness of breath.

Skin and subcutaneous tissue disorders

Angioedema, exanthema, hypotrichosis, pruritus, rash, cracks, urticaria, photosensitivity / toxicity, persistent drug erythema.

Gastrointestinal disorders

Nausea, vomiting.

Liver and biliary tract disorders

Hepatitis.

Musculoskeletal and connective tissue disorders

Muscle pain, arthralgia.

Kidney and urinary tract disorders

Dysuria, urinary retention.

General disorders and disorders at the injection site

Edema, ineffectiveness of the product and its interactions, dryness of the mucous membranes.

Laboratory and instrumental data

Increase in body weight, changes in liver function tests, cross-reactivity.

Description of selected adverse reactions

A small number of patients experienced pruritus after discontinuation of levocetirizine.

If you have any side effects indicated in the instructions, or they are aggravated, or you notice any other side effects not listed in the instructions, inform your doctor.

Special conditions

The intervals between doses should be adjusted individually depending on the renal function.

It is recommended to be careful when used with alcohol.

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

If patients have predisposing factors for urinary retention (eg, spinal cord injury, prostatic hyperplasia), caution should be exercised, since levocetirizine may increase the risk of urinary retention.

Caution should be observed in patients with epilepsy and increased convulsive readiness, since levocetirizine can exacerbate seizures.

The reaction to allergic skin tests is suppressed by antihistamines, and before testing, you must refrain from taking the drug for 3 days.

Itching may appear after stopping levocetirizine, even if there were no such symptoms at the beginning of treatment. Symptoms may go away on their own.

In some cases, symptoms can be severe and may require resumption of treatment.

These symptoms should go away after treatment resumes.

Children

Levocetirizine in orodispersible tablets is contraindicated in children under 6 years of age, as this dosage form does not allow the use of an appropriate dosage for this age group. It is recommended to use a pediatric dosage form (oral drops).

Influence on the ability to drive vehicles, mechanisms

Levocetirizine can lead to increased drowsiness, therefore, Allerway Express may affect the ability to drive a car or work with equipment. During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

The study of the interaction of levocetirizine with other drugs has not been conducted. When studying the drug interaction of cetirizine racemate with antipyrine, azithromycin, cimetidine, diazepam, erythromycin, glipizide, ketoconazole and pseudoephedrine, no clinically significant undesirable interactions were revealed.

When used simultaneously with theophylline (400 mg / day), the total clearance of cetirizine decreases by 16% (the theophylline kinetics does not change).

In a study with the simultaneous administration of ritonavir (600 mg 2 times a day) and cetirizine (10 mg per day), it was shown that the exposure to cetirizine increased by 40%, while the exposure to ritonavir changed slightly (-11%).

In sensitive patients, the simultaneous use of levocetirizine and alcohol or drugs that have a suppressive effect on the central nervous system (CNS) can cause lethargy and impairment of performance.