Rinosan

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT RINOSAN

Composition:

Active substance: xylometazoline hydrochloride;

1 ml of solution contains xylometazoline hydrochloride 1 mg;

Excipients: benzalkonium chloride 1 % solution; disodium edetate; disodium hydrogen phosphate, dodecahydrate; sodium chloride; sodium dihydrogen phosphate, dihydrate; water for injections.

Pharmaceutical form. Nasal spray, solution.

Main physicochemical properties: clear, colourless or almost colourless solution.

Pharmacotherapeutic group. Agents used in nasal disorders. Decongestants and other agents for local use in nasal 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 the blood vessels in the mucous membranes of the nose 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 secretions from the nose, promoting clearance of the nasal passages and easing nasal breathing.

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

The medicinal product 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.

Pharmacokinetics.

After topical application, the drug is practically not absorbed, and xylometazoline concentrations in blood plasma are so low that they are virtually undetectable (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.

The medicinal product is indicated for:

• symptomatic relief of nasal congestion associated with colds, hay fever, other allergic rhinitis, and sinusitis;
• facilitating drainage of secretions in diseases of the nasal accessory sinuses;
• adjunctive therapy in cases of otitis media (to reduce mucosal swelling);
• facilitating rhinoscopy.

Contraindications.

Hypersensitivity to xylometazoline or to any other component of the medicinal product; closed-angle glaucoma; transsphenoidal hypophysectomy; history of surgical procedures involving exposure of meninges; dry rhinitis or atrophic rhinitis.

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 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 agents is not recommended.

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

Special precautions for use

The duration of treatment should not exceed 7 days. Prolonged use of xylometazoline may cause drug-induced rhinitis and swelling of the nasal mucosa, with symptoms resembling those of a common cold.

Xylometazoline, 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 medicinal product should not be exceeded, especially when treating children and elderly patients.

The product should be used with caution in patients with cardiovascular disorders, arterial hypertension, diabetes mellitus, hyperthyroidism, pheochromocytoma, or benign prostatic hyperplasia. Do not use in patients who are receiving or have received treatment with monoamine oxidase inhibitors (MAOIs) within the previous 2 weeks.

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

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

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 adverse effects on the infant. It is unknown whether xylometazoline is excreted in breast milk. Therefore, during breastfeeding, the product should be used with caution and only under medical supervision.

Fertility

There are no adequate data on the effect of the medicinal product Rhinosan 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 medicinal product usually has no effect or has 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

Do not cut off the spray pump nozzle. The nasal spray is ready for immediate use.

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 sprays per nostril per day. The duration of treatment depends on the course of the disease and should not exceed 7 consecutive days.

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, corresponding to 0.14 mg of xylometazoline.

Before 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 product has not been used for more than 7 days, the spray pump must be re-primed by actuating it 4 times into the air.

How to use the spray:

• thoroughly clean the nose before applying 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 simultaneously inhaling gently through the nose;
• after use, before covering the nozzle with the cap, clean and dry the nozzle thoroughly;
• to prevent contamination, the medication bottle should be used by only one person.

The last dose should preferably be administered immediately before bedtime.

Children. The medicinal product 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, convulsions, ataxia, and agitation. Elevated arterial pressure may be followed by a drop in blood pressure. Gastrointestinal symptoms such as nausea and vomiting may also occur. Younger children are more sensitive to toxicity than adults. Severe symptoms after accidental use have not been commonly observed; however, in neonates (aged 2 weeks), administration of 1 drop of 0.1% solution into each nostril may result in coma.

All patients suspected of overdose should receive appropriate supportive measures and, if necessary, immediate 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 accompanied by cardiac arrest, resuscitation efforts should continue for at least 1 hour.

Adverse Reactions

Undesirable effects listed below are categorized by organ systems and frequency of occurrence: 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), frequency not known (frequency cannot be determined from available data, includes also isolated cases).

Immune system:

very rare: hypersensitivity reactions, including angioneurotic edema, rash, pruritus.

Nervous system:

common: headache.

Eye disorders:

very rare: transient visual disturbances.

Cardiovascular system:

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

Respiratory, thoracic and mediastinal disorders:

common: dryness or discomfort of nasal mucosa, burning sensation, drug-induced rhinitis.

Gastrointestinal disorders:

common: nausea.

General disorders and administration site conditions:

common: burning sensation at the application site.

Shelf life. 3 years.

Shelf life after first opening — 1 month.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging. 10 ml of solution in a glass bottle with a plastic pump-sprayer and protective cap, in a cardboard box.

Availability category. Over-the-counter.

Manufacturer.

Basic Pharma Manufacturing B.V.

Manufacturer's address and place of business.

Burgemeester Lemmensstraat 352, 6163 JT, GELEEN, The Netherlands.