Tyzine^® Alergy (Spray) Instructions for Use

Marketing Authorization Holder

J&JTL, LLC (Russia)

Manufactured By

Janssen Pharmaceutica, NV (Belgium)

Contact Information

J&JTL LLC (Russia)

ATC Code

R01AC02 (Levocabastine)

Active Substance

Levocabastine (Rec.INN WHO registered)

Dosage Form

Tyzine® Alergy

Metered-dose nasal spray 50 mcg/1 dose: 10 ml bottle (100 doses) with sprayer

Dosage Form, Packaging, and Composition

Metered-dose nasal spray 50 mcg/dose, in the form of a homogeneous white suspension.

Excipients: propylene glycol, anhydrous disodium phosphate, sodium phosphate monohydrate, hypromellose (2910 5 mPa.s), polysorbate 80, benzalkonium chloride 50% solution recalculated to benzalkonium chloride, disodium edetate, purified water.

10 ml (100 doses) – high-density polyethylene bottles (1) with a sprayer and a low-density polyethylene protective cap – cardboard packs.

Clinical-Pharmacological Group

An antiallergic drug – a histamine H₁-receptor blocker

Pharmacotherapeutic Group

Drugs for the treatment of nasal diseases; decongestants and other preparations for topical use; antiallergic agents, other than corticosteroids

Pharmacological Action

Levocabastine is a selective, long-acting blocker of H₁-histamine receptors.

After intranasal application, Tyzine^® Alergy relieves the symptoms of allergic rhinitis: nasal discharge, sneezing, itching in the nasal cavity.

The local effect occurs within 5 minutes. The action lasts for 12 hours.

Pharmacokinetics

Absorption

With each intranasal administration at a rate of 50 mcg/dose, approximately 30-40 mcg of levocabastine is absorbed.

The C_max of levocabastine in blood plasma is reached approximately 3 hours after nasal administration.

Distribution

Levocabastine binds to plasma proteins by approximately 55%.

Metabolism

The main metabolite of levocabastine, acylglucuronide, is formed by glucuronidation, which is the main metabolic pathway.

Excretion

The T_1/2 of levocabastine is about 35-40 hours.

Levocabastine is excreted primarily in the urine unchanged (about 70% of the absorbed amount).

Indications

• Symptomatic treatment of seasonal and perennial allergic rhinitis.

ICD codes

Dosage Regimen

Intranasally.

Adults

2 doses (100 mcg) into each nostril 2 times/day.

The use of the drug should be continued until the symptoms are relieved.

In case of severe symptoms, it can be applied 3-4 times/day.

Children from 6 to 18 years

2 doses (100 mcg) into each nostril 2 times/day.

The use of the drug should be continued until the symptoms are relieved.

Instructions for use

Shake the bottle before each use.

Inhale the drug through the nose.

Patients should be advised to clear the nasal passages before using the spray and to inhale through the nose during administration.

Before first use, remove the protective cap and press the spray nozzle several times until a cloud of “mist” appears.

The bottle is ready for further use.

Adverse Reactions

Definition of the frequency of adverse reactions: very common (>1/10), common (>1/100, <1/10), uncommon (>1/1000, <1/100), rare (>1/10,000, <1/1000), very rare (<1/10,000, including isolated reports), frequency unknown (frequency cannot be estimated from the available data).

Adverse events observed in patients during clinical studies

Infections and infestations common – sinusitis.

Immune system disorders uncommon – hypersensitivity; frequency unknown – anaphylactic reactions.

Nervous system disorders very common – headache; common – drowsiness, dizziness.

Eye disorders frequency unknown – eyelid edema.

Cardiac disorders uncommon – palpitations; rare – tachycardia.

Respiratory, thoracic and mediastinal disorders common – pharyngeal and laryngeal pain, epistaxis; uncommon – dyspnea, nasal congestion; rare – nasal mucosal edema; frequency unknown – bronchospasm, cough.

Gastrointestinal disorders: common – nausea.

General disorders and administration site conditions common – fatigue, administration site pain; uncommon – administration site irritation, administration site dryness, anxiety; rare – administration site burning, administration site discomfort.

Post-marketing data

Immune system disorders: very rare – anaphylactic reactions, hypersensitivity.

Eye disorders : very rare – eyelid edema.

Cardiac disorders: very rare – palpitations, tachycardia.

Respiratory, thoracic and mediastinal disorders very rare – bronchospasm, dyspnea, nasal mucosal edema.

General disorders and administration site conditions : uncommon – malaise.

Contraindications

• Hypersensitivity to levocabastine and any of the excipients included in the drug;
• Children under 6 years of age.

With caution

Patients with impaired renal function and elderly patients.

Use in Pregnancy and Lactation

Pregnancy

Reliable data on the use of Tyzine^® Alergy nasal spray in pregnant women are not available.

Therefore, the drug should not be used during pregnancy, except in cases where the intended benefit to the mother justifies the potential risk to the fetus.

Lactation

Based on the determination of levocabastine concentration in the saliva and breast milk of nursing women who received a single oral dose of 0.5 mg of levocabastine, it is expected that approximately 0.6% of the total intranasal dose of levocabastine may enter the infant’s body during breastfeeding.

Due to the limited number of clinical and experimental data, caution is recommended when using Tyzine^® Alergy nasal spray in nursing women.

If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.

Use in Renal Impairment

The drug should be used with caution in patients with impaired renal function.

Pediatric Use

Contraindicated for use in children under 6 years of age.

Geriatric Use

The drug should be used with caution in elderly patients.

Special Precautions

Excipients

Tyzine^® Alergy contains benzalkonium chloride, which is an irritant and may cause irritation of the nasal mucosa and skin reactions.

Tyzine^® Alergy contains propylene glycol, which may cause irritation of the nasal mucosa and irritate the skin.

Effect on ability to drive vehicles and operate machinery

The drug at the recommended dose usually does not have a clinically pronounced sedative effect and does not reduce the speed of reaction compared to placebo.

If drowsiness occurs while using the drug, one should not engage in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug disposal rules

If the medicine is no longer usable or the expiration date has passed, it should not be disposed of in sewage or on the street.

The medicine should be placed in a bag and put into a trash container.

These measures will help protect the environment.

Overdose

No reports of levocabastine overdose have been received.

Symptoms: in case of accidental ingestion, decreased blood pressure, tachycardia, and mild sedation are possible.

Treatment in case of ingestion, the patient should drink plenty of fluids to accelerate the excretion of levocabastine by the kidneys.

Drug Interactions

No interaction with alcohol was observed in clinical studies.

No enhancement of the effect of diazepam or alcohol was observed when using Tyzine^® Alergy nasal spray at usual doses.

Concomitant use of the CYP3A4 isoenzyme inhibitors ketoconazole or erythromycin did not affect the pharmacokinetics of levocabastine upon intranasal administration.

Possible local interaction with other intranasal drugs has not been sufficiently studied, except for interaction with oxymetazoline, which can transiently reduce the absorption of levocabastine upon intranasal administration.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

The shelf life is 2 years. Do not use after the expiration date printed on the package.

Dispensing Status

The drug is available without a prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.