Rhinazal®

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT RINAZAL® (RINAZAL)

Composition:

Active substance: xylometazoline hydrochloride;

1 ml of solution contains xylometazoline hydrochloride 0.5 mg or 1.0 mg;

Excipients: sodium dihydrogen phosphate dihydrate, disodium phosphate dodecahydrate, edetate disodium, benzalkonium chloride, sorbitol liquid non-crystallizing, hypromellose, sodium chloride, purified water.

Pharmaceutical form. Nasal spray, metered.

Main physicochemical properties: clear, colorless liquid.

Pharmacotherapeutic group. Agents used in nasal cavity disorders. Anti-edematous and other agents 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 paranasal sinuses, thereby reducing swelling and hyperemia of the nasal and nasopharyngeal mucosa. It also decreases associated excessive mucus secretion and facilitates the removal of blocked nasal secretions, resulting in clearance of the nasal passages and improved nasal breathing.

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

The product is well tolerated, even by patients with sensitive mucosa, and does not impair mucociliary function. According to laboratory test results, xylometazoline reduces the infectious activity of human rhinovirus associated with the common cold.

Due to its moisturizing components (sorbitol, hypromellose), Rinazal® nasal spray, metered dose, helps relieve dryness and irritation of the nasal mucosa.

The medicinal product has a balanced pH value within the physiological range typical for the nasal cavity.

Pharmacokinetics.

After topical administration, the product is poorly absorbed; plasma concentrations of xylometazoline are so low that they are barely detectable (plasma concentration is close to the limit of detection).

Xylometazoline has no 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.

For facilitating drainage of secretions in diseases of the nasal accessory sinuses.

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

For facilitating rhinoscopy.

Contraindications.

• Hypersensitivity to xylometazoline, to any other component of the medicinal product, or to other sympathomimetic amines;
• Closed-angle glaucoma;
• Concomitant use with monoamine oxidase inhibitors (MAOIs) and within 2 weeks after discontinuation of MAOIs;
• Transsphenoidal hypophysectomy and surgical interventions involving exposure of meninges in medical history;
• Dry rhinitis (rhinitis sicca) or atrophic rhinitis.

Interaction with other medicinal products and other forms of interaction.

Monoamine oxidase inhibitors (MAOIs): xylometazoline may potentiate the effect of MAOIs and induce a hypertensive crisis.

Do not use xylometazoline in patients receiving or who have received MAOIs within the last two weeks.

Tricyclic and tetracyclic antidepressants: concomitant use of tricyclic or tetracyclic antidepressants and sympathomimetic medicinal products may enhance the sympathomimetic effect of xylometazoline, particularly in cases of overdose; therefore, concomitant use 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 medicinal product should not be used for longer than 5 consecutive days.

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

The medicinal product, like other sympathomimetics, 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 medicinal product should not be exceeded, especially when treating children and elderly patients.

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

Patients with prolonged QT syndrome who use xylometazoline are at increased risk of serious ventricular arrhythmias.

The medicinal product contains benzalkonium chloride (0.014 mg benzalkonium chloride per 0.14 ml dose, equivalent to 0.100 mg/ml), which may cause irritation of the nasal mucosa.

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 resolved or improved within a few days after appropriate treatment. The medicinal product should be discontinued immediately and medical advice sought if signs or symptoms of PRES/RCVS develop.

Use during pregnancy or breastfeeding.

The medicinal product 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 advised, and the medicinal product should be used during breastfeeding only on medical advice. Prolonged use should be avoided during breastfeeding due to the risk of adverse effects in the infant (tachycardia, excitability, increased blood pressure).

Fertility.

There are no adequate data on the effect of the medicinal product 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 speed when driving or operating machinery.

The medicinal product usually has no effect or only a negligible effect on the ability to drive or operate machinery. However, with prolonged use of high doses of xylometazoline, systemic effects with cardiovascular effects cannot be excluded.

Method of Administration and Dosage.

Rhinazal®, nasal spray, metered, 0.5 mg/mL:

For children aged 2 to 5 years (under adult supervision): 1 spray into each nostril once or twice daily. Do not exceed 3 sprays per nostril per day.

For children aged 6 to 11 years (under adult supervision): 1 to 2 sprays into each nostril 2 to 3 times daily. Do not exceed 3 sprays per nostril per day.

The duration of treatment depends on the course of the disease and should not exceed 5 consecutive days.

Rhinazal®, nasal spray, metered, 1.0 mg/mL:

For adults and children aged 12 years and older: 1 spray into each nostril up to 3 times daily. The interval between administrations should be at least 8–10 hours. Do not exceed 3 sprays per nostril per day.

The duration of treatment depends on the course of the disease and should not exceed 5 consecutive days.

If symptoms worsen or new symptoms appear, consult a physician.

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

Before use, prime the dosing device by performing several actuations until the spray is released into the air. If the spray does not dispense when the nozzle is pressed, or if the product has not been used for more than 7 days, re-prime the spray by performing several actuations until a fine mist is produced.

Once primed, the device will be ready for immediate use during subsequent applications.

To use the spray correctly:

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

The last dose should be taken immediately before bedtime.

Children.

Rhinazal®, nasal spray, metered, 0.5 mg/mL, must not be used in children under 2 years of age.

Use in children aged 2 years and older is recommended only under adult supervision.

Rhinazal®, nasal spray, metered, 1 mg/mL, must not be used in children under 12 years of age.

Overdose.

Excessive local use of xylometazoline hydrochloride or accidental ingestion may lead to sympatholytic effects, including central nervous system depression (e.g., drowsiness, coma), pronounced dizziness, excessive sweating, significant decrease in body temperature, pallor, headache, tachycardia, bradycardia, arterial hypertension, respiratory depression, miosis, seizures, ataxia, and agitation. Elevated blood pressure may be followed by hypotension. Altered consciousness may indicate severe overt intoxication. Gastrointestinal symptoms such as nausea and vomiting may also occur. Younger children are more sensitive to the toxic effects than adults.

Severe symptoms have not been commonly observed after accidental use; however, in newborns (2 weeks of age), administration of 1 drop of 0.1% solution into each nostril may result in coma.

In cases of severe intoxication, hospitalize the patient and provide emergency symptomatic treatment under medical supervision. Medical care should include observation of the patient for several hours. There is no specific antidote; atropine may be used in cases of bradycardia. In cases of severe overdose with cardiac arrest, resuscitation efforts should continue for at least 1 hour. At home, activated charcoal may be administered as an emergency measure prior to hospitalization.

Adverse Reactions

All adverse reactions are listed by system organ classes and frequency: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), frequency not known (cannot be estimated from the available data).

Eye disorders: very rare – temporary visual disturbances.

Respiratory, thoracic and mediastinal disorders: common – dryness or discomfort of the nasal mucosa, burning sensation, drug-induced rhinitis; uncommon – nasal bleeding.

Gastrointestinal disorders: common – nausea; uncommon – vomiting.

Nervous system disorders: common – headache; uncommon – insomnia.

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

Immune system disorders: very rare – hypersensitivity reactions, including angioneurotic edema, rash, pruritus.

General disorders and administration site conditions: common – burning sensation at the application site.

Reporting of suspected adverse reactions.

Reporting of suspected adverse reactions after marketing authorization is important. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and patients, or their legal representatives, are encouraged to report any suspected adverse reactions and/or lack of efficacy of the medicinal product via the Pharmacovigilance Automated Information System at: https://aisf.dec.gov.ua.

Shelf life. 3 years.

Storage conditions.

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

Keep out of reach of children.

Packaging.

10 ml in a bottle, 1 bottle with a dosing pump in a carton.

Availability category. Over-the-counter (without prescription).

Manufacturer. JSC "Pharmaceutical Company "Darnytsia".

Manufacturer's address and location of its business activities.

13, Borispilska Street, Kyiv, 02093, Ukraine.