Allerway, 5 mg 30 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.

Intestation

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

Elimination

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 taken is excreted unchanged by kidney through glomerular filtration and tubular secretion; about 12.9% – through intestine.

Particular pharmacokinetics in selected 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

Allerway, film-coated tablets, 5 mg indicated in adults and children 6 years and older:

Active ingredient

How to take, the dosage

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.

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.

Impact on driving and operating machinery

Levocetirizine may lead to increased somnolence; therefore, the drug 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 quick psychomotor reactions.

Synopsis

Contraindications

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 greater (often ≥ 1/100, < 1/10) in children aged 6 years to 12 years during clinical trials.

Post-registration studies

The incidence of side effects is not known (cannot be estimated from 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

Convulsions, dura sinus thrombosis, paresthesia, dizziness, fainting, tremor, dysgeusia.

Hearing and labyrinth disorders

Vertigo

Visual disturbances

Visual disturbances, blurred vision, inflammatory manifestations.

Cardiovascular system disorders

Stenocardia, tachycardia, palpitations, jugular vein thrombosis.

Respiratory system disorders

Dyspnea, increased symptoms of rhinitis.

Gastrointestinal disorders

Nausea, vomiting, diarrhea.

Hepatic and biliary tract disorders

Hepatitis, changes in liver function tests.

Renal and urinary system disorders

Dysuria, urinary retention.

Skin and subcutaneous tissue disorders

Angioneurotic edema, persistent erythema drug, rash, pruritus, urticaria, hypotrichosis, cracks, photosensitization.

Muscular and connective tissue disorders

Muscle pain, arthralgia.

General disorders

Peripheral edema, weight gain.

Other

Cross-reactivity.

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), 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.

Similarities