Eucazolin® aqua

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT EUCAZOLIN® AQUA (EUCAZOLIN® AQUA)

Composition:

Active substance: xylometazoline;

1 g of spray contains 1 mg of xylometazoline hydrochloride, calculated as 100% substance;

Excipients: benzalkonium chloride; eucalyptus oil; disodium edetate; propylene glycol; polyethylene glycol 1500; povidone; hypromellose; polysorbate 20; sodium hydrogen phosphate dodecahydrate; potassium dihydrogen phosphate; purified water.

Pharmaceutical form. Nasal spray.

Main physicochemical properties: the product, when dispensed from the container through a pump-dosing device with a nasal atomizer, is released as an aerosol jet with a specific odor and consists of liquid particles dispersed in the air.

Pharmacotherapeutic group.

Preparations used in nasal cavity disorders. Decongestants and other preparations for local use in nasal cavity disorders. Sympathomimetics, simple preparations. ATC code R01A A07.

Pharmacological Properties

Pharmacodynamics

Xylometazoline is a sympathomimetic agent acting on α-adrenergic receptors.

When administered intranasally, xylometazoline causes vasoconstriction of the blood vessels in the nasal mucosa and adjacent areas of the nasopharynx. This reduces edema and hyperemia of the nasal and nasopharyngeal mucosa, decreases associated excessive mucus secretion, and facilitates removal of blocked nasal secretions. As a result, nasal passages are cleared and nasal breathing is relieved.

The effect of the drug begins within 2 minutes after administration and lasts up to 12 hours (e.g., throughout the night).

The drug is well tolerated by patients with sensitive mucosa and does not impair mucociliary function. Study results have shown that xylometazoline reduces the infectious activity of human rhinovirus, which is associated with the common cold.

Pharmacokinetics

After topical administration, xylometazoline is practically not absorbed, and its plasma concentration is so low that it is virtually undetectable (plasma concentration is close to the limit of detection).

Xylometazoline does not possess mutagenic properties. In addition, animal studies have not revealed any teratogenic effects of xylometazoline.

Clinical characteristics.

Indications.

Symptomatic treatment of nasal congestion due to colds, hay fever, other allergic rhinitis, and sinusitis.

Facilitation of secretion drainage in diseases of the nasal accessory sinuses.

Adjunctive therapy in cases of otitis media (to relieve swelling of the nasal mucosa).

Facilitation of rhinoscopy.

Contraindications.

Hypersensitivity to xylometazoline or to any other component of the medicinal product, acute coronary diseases, coronary asthma, hyperthyroidism, closed-angle glaucoma, transsphenoidal hypophysectomy, and surgical interventions involving exposure of the meninges in medical history, dry rhinitis (rhinitis sicca) or atrophic rhinitis. Concomitant use of monoamine oxidase inhibitors (MAO inhibitors) and within 2 weeks after discontinuation of their use.

Interaction with other medicinal products and other forms of interaction.

Monoamine oxidase inhibitors (MAO inhibitors): xylometazoline may potentiate the effect of monoamine oxidase inhibitors and induce a hypertensive crisis. Xylometazoline should not be used in patients who are currently taking or who have taken MAO inhibitors within the previous two weeks.

Tricyclic and tetracyclic antidepressants: concomitant use of tricyclic or tetracyclic antidepressants and sympathomimetic agents may enhance the sympathomimetic effect of xylometazoline; therefore, concomitant use of these agents is not recommended.

Concomitant use with β-blockers may cause bronchospasm or reduction in blood pressure.

Special precautions for use.

The product should not be used for more than 10 consecutive days. Prolonged or excessive use may lead to rebound nasal congestion and/or atrophy of the nasal mucosa.

The product, like other sympathomimetics, should be used with caution in patients who exhibit strong reactions to adrenergic agents, such as insomnia, dizziness, tremor, cardiac arrhythmia, or increased blood pressure.

The recommended dose of the product should not be exceeded, especially when treating children and elderly patients.

The product should be prescribed with caution to patients with cardiovascular disorders, arterial hypertension, diabetes mellitus, pheochromocytoma, or benign prostatic hyperplasia. It should not be used in patients receiving treatment with MAO inhibitors or within 2 weeks after discontinuation of such treatment.

The product contains benzalkonium chloride, which may cause irritation of the nasal mucosa.

Use during pregnancy or breastfeeding.

The product must not be used during pregnancy due to its potential vasoconstrictive effect.

There is no evidence of any adverse effect on the infant. It is unknown whether xylometazoline is excreted in breast milk; therefore, caution is required and the product should be used during breastfeeding only under medical supervision.

Fertility.

There are no adequate data on the effect of the product on fertility. Since systemic exposure to xylometazoline hydrochloride is very low, the likelihood of an effect on fertility is extremely low.

Ability to affect reaction speed when driving or operating machinery.

The product usually has no effect or only a negligible effect on the ability to drive or operate machinery.

Method of Administration and Dosage

Eukazolin® Aqua, nasal spray, is intended for use in adults and children aged 12 years and older.

Adults and children aged 12 years and older:

1 spray into each nostril up to 3 times daily as needed. Do not use more than 3 times per day into each nostril. The duration of treatment depends on the course of the disease and should not exceed 10 consecutive days.

The metered spray ensures accurate dosing and proper distribution of the solution over the nasal mucosal surface.

Before first use, prime the spray pump by actuating it several times until a fine spray is produced. After initial priming, the spray device will be ready for immediate use.

The spray should be used as follows:

• thoroughly clear the nasal passages before using the medication;
• hold the bottle vertically, supporting the bottom with the thumb and placing the nozzle between two fingers;
• slightly tilt the bottle and insert the nozzle into the nostril;
• administer a spray while simultaneously inhaling gently through the nose;
• after use, before replacing the cap, clean and dry the nozzle;
• to prevent infection, each bottle should be used by only one person.

The last dose should preferably be administered immediately before bedtime.

Children. The medication should not be used in children under 12 years of age.

Overdose.

Excessive local use of xylometazoline hydrochloride or accidental ingestion may lead to pronounced dizziness, sweating, significant decrease in body temperature, headache, bradycardia, arterial hypertension, respiratory depression, coma, and convulsions. Elevated arterial pressure may be followed by a drop in pressure. Younger children are more sensitive to toxicity than adults.

All patients suspected of overdose should receive appropriate supportive measures and, if necessary, immediate symptomatic treatment under medical supervision. Medical assistance should include monitoring of the patient for several hours. In cases of severe overdose accompanied by cardiac arrest, resuscitation efforts should continue for at least 1 hour.

Side effects.

Immune system:

Rare (<1/10,000): hypersensitivity reaction, including angioneurotic edema, rash, itching.

Nervous system:

Common (≥1/100, <1/10): headache.

Eye disorders:

Rare (<1/10,000): temporary visual disturbances.

Cardiovascular system:

Rare (<1/10,000): irregular or rapid heartbeat.

Respiratory, thoracic and mediastinal disorders:

Common (≥1/100, <1/10): dryness or discomfort of the nasal mucosa;

Uncommon (≥1/1,000 – <1/100): epistaxis.

Gastrointestinal disorders:

Common (≥1/100, <1/10): nausea.

General disorders and administration site conditions:

Common (≥1/100, <1/10): burning sensation at the application site.

Shelf life.

2 years.

Do not use the medication after the expiry date stated on the packaging.

Storage conditions.

Store in a protected from light place at a temperature not exceeding 25 ºC.

Keep out of the reach of children.

Packaging.

10 g in a bottle. 1 bottle in a box.

Availability. Over-the-counter.

Manufacturer. JSC "Farmak".

Manufacturer's name and address of the place of business.

74, Kyrylivska Street, Kyiv, 04080, Ukraine.