Allerwei Express oral dispersible pills 5mg, 10pcs

Composition

Each tablet dispersed in the oral cavity contains:

Active ingredient: levocetirizine dihydrochloride 5.00 mg;

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

Pharmacological action

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

ATX code: R06AE09

Pharmacological properties

Pharmacodynamics

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

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

Levocetirizine prevents the development and eases the course of allergic reactions, has an antipruritic and anti-exudative effect. Practically does not affect cholinergic and serotonin receptors, in therapeutic doses it does not have a sedative effect.

Pharmacokinetics

The pharmacokinetics of levocetirizine vary linearly.

Suction

After oral use, the drug is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although its rate decreases. In adults, after a single dose of the drug in a therapeutic dose (5 mg), the maximum concentration (Cmax) in blood plasma is 270 ng / ml and is reached in 0.9 hours, after repeated use at a dose of 5 mg – 308 ng / ml. Equilibrium plasma concentration (Css) is reached after 2 days. Distribution

Levocetirizine is 90% bound to plasma proteins. The 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 by the cytochrome system) to form a pharmacologically inactive metabolite.

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

Deduction

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

Features of pharmacokinetics in individual patients

Patients with impaired renal function

In patients with renal insufficiency (creatinine clearance (CC)) In patients undergoing hemodialysis, total clearance is reduced by 80%, which requires a change in the dosage regimen. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

Indications

• for the treatment of symptoms of allergic rhinitis, including year-round (persistent) and seasonal (intermittent) allergic rhinitis, and allergic conjunctivitis, such as itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia;
• pollinosis (hay fever);
• urticaria;
• other allergic dermatoses accompanied by itching and rashes.

Use during pregnancy and lactation

Pregnancy

Data on the use of levocetirizine during pregnancy are almost nonexistent or limited (less than 300 pregnancy outcomes). However, the use of cetirizine, levocetirizine racemate, during 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 fetal development, delivery, or postnatal development were found in animal studies.

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

Breast-feeding period

Cetirizine, a racemate of levocetirizine, is excreted in breast milk. Therefore, the excretion of levocetirizine in breast milk is also likely. Children who are breastfed may experience adverse reactions to levocetirizine. Therefore, caution should be exercised when prescribing levocetirizine during breastfeeding.

Fertility

There are no clinical data on levocetirizine.

Before using the drug, if you are pregnant, or think that you might be pregnant, or are planning to become pregnant, you should consult your doctor.

Contraindications

• Hypersensitivity to the Active ingredient, cetirizine, hydroxyzine, any piperazine derivative or to any excipient of the drug.
• Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
• End-stage renal failure (CC 
• Children under 6 years of age (due to limited safety and efficacy data).

With caution

• In case of chronic renal failure (correction of the dosage regimen is necessary).
• In elderly patients (with an age-related decrease in glomerular filtration).
• In patients with spinal cord injury, prostatic hyperplasia, or other predisposing factors to urinary retention, levocetirizine may increase the risk of urinary retention.
• When used concomitantly with alcohol (see the section “Interaction with other medicinal products”).
• When prescribed to pregnant women and during breastfeeding.

Side effects

Clinical trials

During clinical trials, men and women aged 12-71 years with a frequency of 1% or more (often ≥ 1/100, < 1/10) experienced the following side effects: headache, drowsiness, dry mouth, fatigue, infrequently (≥ 1/1000,

During clinical trials in children aged 6 to 12 years with a frequency of 1% or more (often ≥ 1/100,

Post-registration studies:

• The frequency of side effects is not known (cannot be estimated from the available data).
• Immune system disorders
• Hypersensitivity reactions, including anaphylaxis.
• Metabolic disorders and eating disorders
• Increased appetite.
• Mental disorders
• Anxiety, aggression, agitation, depression, hallucinations, insomnia, suicidal thoughts.
• Nervous system disorders
• Seizures, dura mater sinus thrombosis, paresthesia, dizziness, fainting, tremor, dysgeusia.
• Hearing disorders and labyrinth disorders
• Vertigo 
• Visual disturbances
• Visual impairment, blurred vision, inflammatory manifestations.
• Disorders of the cardiovascular system
• Angina pectoris, tachycardia, palpitation, jugular vein thrombosis.
• Respiratory system disorders
• Shortness of breath, increased symptoms of rhinitis.
• Disorders of the gastrointestinal tract
• Nausea, vomiting, diarrhea.
• Liver and biliary tract disorders 
• Hepatitis, changes in liver function tests.
• Disorders of the kidneys and urinary system
• Dysuria, urinary retention.
• Skin and subcutaneous tissue disorders
• Angioedema, persistent drug-induced erythema, rash, pruritus, urticaria, hypotrichosis, cracks, photosensitization.
• Musculoskeletal and connective tissue disorders
• Muscle pain, arthralgia.

General violations:  

• Peripheral edema, weight gain.
• Cross-reactivity.

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

Interaction

The interaction of levocetirizine with other drugs has not been studied.

When studying the drug interaction of cetirizine racemate with antipyrine, azithromycin, cimetidine, diazepam, erythromycin, glipizide, ketoconazole, pseudoephedrine and phenazone, no clinically significant adverse interactions were detected.

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

In a study with simultaneous use of ritanovir (600 mg twice daily) and cetirizine (10 mg daily), it was shown that cetirizine exposure increased by 40%, while ritonavir exposure changed slightly (-11%).

In some cases, concomitant use of levocetirizine with alcohol or drugs that have an overwhelming effect on the central nervous system (CNS) can cause lethargy and deterioration of performance.

How to take it, course of use and dosage

Inside.

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

Taking tablets dispersed in the oral cavity does not require mandatory washing down with 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 product

Do not squeeze tablets through the foil of the packaging! Remove tablets dispersed in the oral cavity 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 of age

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

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 symptoms; treatment can be discontinued when symptoms disappear and resumed when they appear.

In the treatment of year-round (persistent) allergic rhinitis (the presence of symptoms more than 4 days a week and their total duration is more than 4 weeks), treatment can continue for the entire period of exposure to allergens.

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

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

If you forget to take the 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 route of elimination of levocetirizine from the body is excretion by the kidneys, so when using the drug in elderly patients and with renal insufficiency, the dose should be adjusted depending on the degree of renal insufficiency, based on the assessment of creatinine clearance (ml/min).

In patients with mild renal impairment (creatinine clearance 50-79 ml/min), no dose adjustment is required.

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

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

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

No dosage adjustment is required for patients with hepatic impairment alone.

Overdose

Symptoms: drowsiness (in adults), first may appear agitation and anxiety, then give way to drowsiness (in children).

Treatment: it is necessary to wash the stomach or take activated charcoal if little time has passed since taking the drug. Symptomatic and supportive care is recommended. There is no specific antidote. Hemodialysis is not effective.

Description

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

Special instructions

The intervals between doses should be selected individually, depending on renal function.

Caution is recommended when used concomitantly with alcohol.

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

Caution should be exercised if patients have predisposing factors to urinary retention (for example, spinal cord injury, prostatic hyperplasia), as levocetirizine may increase the risk of urinary retention.

Caution should be exercised in patients with epilepsy and increased convulsive readiness, as levocetirizine can cause exacerbation of seizures.

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

Itching may occur after discontinuation of levocetirizine, even if such symptoms were not present 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 a resumption of treatment.

After resuming treatment, these symptoms should disappear.

Children

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

Influence on the ability to drive vehicles and mechanisms

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

Form of production

Tablets dispersed in the oral cavity,5 mg.

10 tablets in a blister of (PA/Al/PVC) foils / / aluminum foils laminated with PET/paper. 1 or 3 blisters with instructions for use in a cardboard pack.

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Levocetirizine

Dosage form

Tablets