Rinostop

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT RINOSTOP (RINOSTOP)

Composition:

Active ingredient: xylometazoline hydrochloride;

1 ml of solution contains 1.0 mg of xylometazoline hydrochloride;

Excipients: benzalkonium chloride; polyoxyl hydrogenated castor oil; sodium hydrogen phosphate, dodecahydrate; sodium dihydrogen phosphate, monohydrate; eucalyptus oil; disodium edetate; sodium chloride; sorbitol (E 420); purified water.

Pharmaceutical form. Nasal spray, metered.

Main physicochemical properties: opalescent solution, colorless to whitish, with a characteristic eucalyptol odor.

Pharmacotherapeutic group. Medicinal products used in nasal cavity disorders. Decongestants and other preparations for local use in nasal cavity disorders. 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 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 removal of blocked secretions from the nose, promotes clearance of nasal passages, and improves 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, including by patients with sensitive mucosa, and does not impair mucociliary function. Laboratory analyses have shown that xylometazoline reduces the infectious activity of human rhinovirus associated with the common cold.

The medicinal product contains a volatile cooling aromatic substance — eucalyptol.

Pharmacokinetics. When applied locally, the preparation is practically not absorbed, and the concentration of xylometazoline in blood plasma is so low that it is practically undetectable (plasma concentration is close to the limit of detection).

Xylometazoline has no mutagenic properties. Animal studies have also shown no evidence of teratogenic effects of xylometazoline.

Clinical characteristics

Indications. Use for symptomatic relief of nasal congestion due to colds, hay fever, other allergic rhinitis, and sinusitis.

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

Use as an adjunctive therapy in cases of otitis media (to reduce mucosal swelling).

For facilitating rhinoscopy.

Contraindications. Hypersensitivity to xylometazoline, any other component of the medicinal product, 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 (MAO inhibitors) (see section "Interaction with other medicinal products and other forms of interaction").

Interaction with other medicinal products and other forms of interaction

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

Tricyclic and tetracyclic antidepressants: concomitant use of tricyclic or tetracyclic antidepressants and sympathomimetic agents, particularly xylometazoline, may enhance sympathomimetic effects; therefore, concomitant use of these medicinal products is not recommended.

Concomitant use with beta-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 or excessive 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 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 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, 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 long QT syndrome who receive xylometazoline are at increased risk of serious ventricular arrhythmias. As first-line therapy, nasal irrigation with physiological saline is recommended. Rhinostop may be used as a second-line medicinal product.

The medicinal product contains benzalkonium chloride (0.007 mg of benzalkonium chloride per 0.14 mL dose, equivalent to 0.05 mg/mL), which may cause irritation 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 agents. 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 use of the product should be discontinued immediately and medical advice sought if signs or symptoms of posterior reversible encephalopathy syndrome / reversible cerebral vasoconstriction syndrome develop.

Use during pregnancy or breastfeeding

The medicinal product should 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. During breastfeeding, the product should be used only on medical advice. Breastfeeding mothers should avoid prolonged use due to the risk of adverse effects in the infant (tachycardia, excitability, increased blood pressure).

Fertility. Adequate data on the effect of the medicinal product Rhinostop on fertility are lacking. Since systemic exposure to xylometazoline hydrochloride is very low, the likelihood of an effect on fertility is very small.

Ability to affect reaction speed when driving or operating machinery. Generally, the medicinal product does not affect 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 excluded.

Method of Administration and Dosage

The medicinal product should be administered to adults and children aged 12 years and older as 1 spray into each nostril up to 3 times daily. Do not exceed 3 applications into each nostril per day. The interval between administrations should be at least 8–10 hours. The duration of treatment depends on the course of the disease and should not exceed 5 consecutive days.

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 will remain ready for use throughout the entire treatment period. If no spray is released when pressing the pump, or if the spray has not been used for more than 7 days, re-prime the spray pump by actuating it 4 times into the air.

The spray should be used as follows:

• thoroughly clean the nose before application;
• 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 simultaneously taking a gentle inhalation through the nose;
• after use, before replacing the cap, clean and dry the nozzle;
• to prevent infection, the bottle should be used by only one person.

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

Children. Rhinostop should be used in children aged 12 years and older.

Overdose. Excessive local use of xylometazoline hydrochloride or accidental ingestion may lead to pronounced dizziness, excessive sweating, significant decrease in body temperature, headache, bradycardia, less commonly tachycardia, arterial hypertension, respiratory depression, coma, and seizures. Elevated arterial pressure may be followed by decreased pressure. 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 emergency symptomatic treatment should be administered 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).

Reporting of suspected adverse reactions. Reporting of adverse reactions following registration of the medicinal product is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the following link: https://aisf.dec.gov.ua

Shelf life. 3 years. Do not use the medicinal product after the expiry date stated on the packaging.

Storage conditions. Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging. 10 ml in a polyethylene container with a pump spray dispenser, in a carton.

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

Manufacturer. Ukrainian-Spanish joint enterprise "Sperko Ukraine".

Manufacturer's location and address of its business site. 25, 600-richchia St., Vinnytsia, 21027, Ukraine.