Xylorif

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT XILORIF (XILORIF)

Composition:

Active substance: xylometazoline hydrochloride;

1 ml of solution contains xylometazoline hydrochloride 1 mg;

Excipients: sodium dihydrogen phosphate, dihydrate; sodium hydrogen phosphate, dodecahydrate; sodium chloride; benzalkonium chloride solution; disodium edetate; menthol (levomenthol); eucalyptus oil; sorbitol (E 420); polyoxylated hydrogenated castor oil; purified water.

Pharmaceutical form. Nasal spray, metered.

Main physicochemical properties: clear or opalescent solution, from colorless to white, with the odor of menthol and eucalyptus.

Pharmacotherapeutic group.

Agents used in diseases of the nasal cavity. Decongestants and other agents for local use in nasal diseases.

Simple sympathomimetics. ATC code R01A A07.

Pharmacological Properties

Pharmacodynamics

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

When applied intranasally, xylometazoline causes vasoconstriction of the blood vessels in the nasal mucosa and adjacent areas of the nasopharynx, thereby reducing swelling and hyperemia of the nasal and nasopharyngeal mucosa. It also decreases associated excessive mucus secretion, facilitates clearance of blocked nasal secretions, promotes opening of the nasal passages, and eases nasal breathing.

The effect of the drug begins within 2 minutes after administration and lasts up to 12 hours.

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

The product contains evaporating cooling aromatic substances—menthol and eucalyptol.

Pharmacokinetics

When applied locally, the drug is practically not absorbed; plasma concentrations of xylometazoline are so low that they are practically undetectable (plasma concentration is close to the limit of detection).

Xylometazoline has no mutagenic properties. In animal studies, xylometazoline showed no teratogenic effects.

Clinical characteristics.

Indications.

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

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

Adjunctive therapy in cases of otitis media (to reduce mucosal swelling).

Facilitation of rhinoscopy.

Contraindications.

Hypersensitivity to xylometazoline, to any of the excipients, or to other sympathomimetic amines; closed-angle glaucoma; transsphenoidal hypophysectomy; transnasal or transoral surgical procedures involving exposure of the meninges or history thereof; atrophic rhinitis (rhinitis sicca) or atrophic rhinitis. Patients receiving concomitant treatment with monoamine oxidase inhibitors (MAOIs) (see section "Interaction with other medicinal products and other types of interactions").

Interaction with other medicinal products and other types of interactions.

MAO inhibitors: xylometazoline may potentiate the effect of MAO inhibitors and may induce a hypertensive crisis. Xylometazoline must not be used in patients receiving or who have received 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 administration of these medicinal products is not recommended.

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

Special precautions for use.

The drug should not be used for longer than 5 consecutive days.

Prolonged or excessive treatment with xylometazoline may cause secondary swelling of the nasal mucosa, with risk of chronic rhinitis and/or atrophy of the nasal mucosa.

Like other sympathomimetics, the drug should be prescribed with caution to patients who exhibit strong reactions to adrenergic agents, manifested as insomnia, dizziness, tremor, cardiac arrhythmia, or increased blood pressure.

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

The drug should be prescribed with caution to patients with cardiovascular disorders, arterial hypertension, diabetes mellitus, hyperthyroidism, pheochromocytoma, or prostate hyperplasia. The drug must not be used in patients who have received concomitant treatment with monoamine oxidase inhibitors (MAOIs) or within 2 weeks after discontinuation of such therapy.

Patients with prolonged QT syndrome who receive xylometazoline may be at increased risk of serious ventricular arrhythmias. Nasal irrigation with physiological saline is recommended as first-line therapy. The medicinal product Xylorif may be used as a second-line medicinal product.

The product contains benzalkonium chloride, which may cause swelling of the nasal mucosa, particularly with prolonged use.

Rare cases of posterior reversible encephalopathy syndrome (PRES)/reversible cerebral vasoconstriction syndrome (RCVS) have been reported with the use of sympathomimetic drugs. Reported symptoms include sudden severe headache, nausea, vomiting, and visual disturbances. In most cases, symptoms resolve or improve within a few days after appropriate treatment. The drug should be discontinued immediately and medical advice sought if signs or symptoms of PRES/RCVS develop.

Use during pregnancy or breastfeeding.

The drug should not be used during pregnancy due to its potential vasoconstrictive effects. 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 drug should be used during breastfeeding only on medical advice. During breastfeeding, prolonged use should be avoided due to the risk of adverse effects in the infant (tachycardia, excitation, increased blood pressure).

Fertility.

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

Ability to affect reaction rate while driving or operating machinery.

The drug usually has no effect or has a negligible effect on the ability to drive or operate machinery. However, with excessively prolonged use or use at high doses, an effect on the cardiovascular system cannot be ruled out.

Method of Administration and Dosage

The medication should be administered to adults and children aged 12 years and older as one spray into each nostril, up to three times daily. Do not administer more than three times per day into each nostril. The interval between administrations should be at least 8–10 hours. The duration of treatment depends on the course of the illness and should not exceed 5 consecutive days without interruption.

Do not cut off the spray nozzle. The nasal spray is a metered dose spray and is ready for immediate use.

The metered-dose spray ensures accurate dosing and proper distribution of the solution over the nasal mucosal surface. Each spray delivers 0.14 mL of solution, corresponding to 0.14 mg of xylometazoline.

Before the first use, prime the spray pump by pressing it 4 times. After this, the spray pump is ready for use throughout the entire treatment period. If the spray does not dispense when the pump is pressed, or if the spray has not been used for more than 7 days, the spray pump must be re-primed by actuating it 4 times into the air.

To use the spray:

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

The last administration is recommended to be performed immediately before bedtime.

Children.

This medicinal product is not intended for use in children under 12 years of age.

Overdose.

Excessive local use of xylometazoline hydrochloride or accidental ingestion may lead to pronounced dizziness, excessive sweating, significant decrease in body temperature, headache, bradycardia, and less frequently, tachycardia, arterial hypertension, respiratory depression, coma, and seizures. Elevated arterial blood pressure may later shift to hypotension. Impaired consciousness may indicate severe, overt intoxication. Younger children are more sensitive to toxic effects than adults. At home, activated charcoal may be administered as an emergency measure prior to hospitalization.

In cases of severe intoxication, the patient should be hospitalized and receive immediate symptomatic treatment under medical supervision. Medical care should include monitoring of the patient's condition for several hours. In cases of severe overdose accompanied by cardiac arrest, resuscitation efforts should continue for at least 1 hour.

Side effects

Side effects are classified by frequency of occurrence into the following categories: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1000 to < 1/100); rare (≥ 1/10,000 to < 1/1000); very rare (< 1/10,000).

Immune system disorders:

very rare: hypersensitivity reactions, including angioedema, rash, pruritus.

Nervous system disorders:

common: headache; uncommon: insomnia.

Eye disorders:

very rare: transient visual disturbances.

Cardiovascular system disorders:

very rare: irregular or rapid heartbeat, arterial hypertension, arrhythmia.

Respiratory, thoracic and mediastinal disorders:

common: dryness or discomfort of the nasal mucosa; burning sensation; drug-induced rhinitis; uncommon: epistaxis.

Gastrointestinal disorders:

common: nausea; uncommon: vomiting.

General disorders and administration site conditions:

common: burning sensation at the application site.

Reporting of side effects after marketing authorization of the medicinal product is of great importance. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all suspected side effects and lack of efficacy through the automated pharmacovigilance information system at: https://aisf.dec.gov.ua.

Shelf life.

2 years.

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

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Packaging.

10 ml in a glass bottle with a nasal spray pump or in a polymer bottle with a nasal spray pump. 1 bottle per cardboard box.

Supply classification.

Over-the-counter.

Manufacturer.

JSC "CHEMICAL PHARMACEUTICAL PLANT "CHERVONA ZIRKA".

Manufacturer's address and location of its business activity.

1 Gordienkovskaya Street, Kharkiv, Kharkiv Oblast, 61010, Ukraine.