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 is indicated for adults and children aged 6 years and older with:

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;
hay fever (hay fever);
hives;
other allergic dermatoses accompanied by itching and rashes.

Pharmacological effect

Pharmacotherapeutic group:

antiallergic agent – ​​H1-histamine receptor blocker.

ATX code: R06AE09

Pharmacological properties

Pharmacodynamics

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

Levocetirizine has a pronounced antihistamine and antiallergic effect. It affects the histamine-dependent phase of the 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 alleviates the course of allergic reactions, has antipruritic and antiexudative effects. It has virtually no effect on cholinergic and serotonin receptors, and does not have a sedative effect in therapeutic doses.

Pharmacokinetics

The pharmacokinetics of levocetirizine varies linearly.

Suction

After oral administration, the drug is quickly and completely absorbed from the gastrointestinal tract. Eating does not affect the completeness of absorption, although its speed decreases. In adults, after a single dose of the drug in a therapeutic dose (5 mg), the maximum concentration (Cmax) in the blood plasma is 270 ng/ml and is achieved after 0.9 hours, after repeated administration at a dose of 5 mg – 308 ng/ml. Equilibrium plasma concentration (Css) is achieved 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 using the cytochrome system) to form a pharmacologically inactive metabolite. Due to limited metabolism and the absence of metabolic inhibitory activity, interaction of levocetirizine at the metabolic level with other substances is unlikely.

Removal

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 administered dose of the drug is excreted unchanged by the kidneys through glomerular filtration and tubular secretion; about 12.9% – through the intestines.

Features of pharmacokinetics in individual patients

Patients with impaired renal function

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

Special instructions

The intervals between doses should be individualized depending on renal function.

Caution is recommended when used concomitantly with alcohol.

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

Impact on the ability to drive vehicles and machinery

Levocetirizine may cause increased drowsiness; therefore, the drug may affect the ability to drive a car or operate machinery. During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Levocetirizine

Composition

Each film-coated tablet contains:

Contraindications

Hypersensitivity to the active substance, cetirizine, hydroxyzine, any piperazine derivative or to any excipient of the drug. Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
End-stage renal failure (CC < 10 ml/min). Children under 6 years of age (due to limited data on safety and effectiveness). 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 in the presence of other factors predisposing to urinary retention, since levocetirizine may increase the risk of urinary retention.
When used simultaneously with alcohol (see section “Interaction with other drugs”).
When prescribed to pregnant women and during breastfeeding.

Side Effects

Clinical studies

During clinical studies in men and women 12-71 years of age, the following side effects occurred with a frequency of 1% or more (often ≥ 1/100, < 1/10): headache, drowsiness, dry mouth, fatigue; infrequently (≥ 1/1000, < 1/100) asthenia and abdominal pain occurred.

During clinical studies in children aged 6 to 12 years, headache and drowsiness occurred with a frequency of 1% or more (common ≥ 1/100, < 1/10).

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 and eating disorders

Increased appetite.

Mental disorders

Anxiety, aggression, agitation, depression, hallucinations, insomnia, suicidal thoughts.

Nervous system disorders

Convulsions, thrombosis of the dural sinuses, paresthesia, dizziness, fainting, tremor, dysgeusia.

Hearing and labyrinth disorders

Vertigo

Visual disorders

Visual impairment, blurred vision, inflammatory manifestations.

Cardiovascular disorders

Angina pectoris, tachycardia, palpitations, jugular vein thrombosis.

Respiratory system disorders

Shortness of breath, increased symptoms of rhinitis.

Gastrointestinal disorders

Nausea, vomiting, diarrhea.

Disorders of the liver and biliary tract

Hepatitis, changes in liver function tests.

Renal and urinary system disorders

Dysuria, urinary retention.

Skin and subcutaneous tissue disorders

Angioedema, persistent drug erythema, rash, itching, urticaria, hypotrichosis, fissures, photosensitivity.

Musculoskeletal and connective tissue disorders

Muscle pain, arthralgia.

General violations

Peripheral edema, weight gain.

Other

Cross reactivity.

If any of the side effects indicated 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 interactions of cetirizine racemate with antipyrine, azithromycin, cimetidine, diazepam, erythromycin, glipizide, ketoconazole, pseudoephedrine and phenazone, no clinically significant adverse interactions were identified.

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

In a study with simultaneous administration of ritanovir (600 mg 2 times a day) and cetirizine (10 mg per day), cetirizine exposure increased by 40%, and ritonavir exposure changed slightly (-11%).

In some cases, when levocetirizine is used simultaneously with alcohol or drugs that have a suppressive effect on the central nervous system (CNS), it can cause lethargy and deterioration in performance.

Overdose

Symptoms: drowsiness (in adults), agitation and anxiety, followed by drowsiness (in children).

Treatment: it is necessary to rinse 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.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children!

Shelf life

2 years.

Manufacturer

Dr. Reddy’s Laboratories Ltd, India