Nazonol

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

Composition:

Active substance: xylometazoline hydrochloride;

1 ml of solution contains 1 mg of xylometazoline hydrochloride;

Excipients: benzalkonium chloride; disodium edetate; sorbitol solution, non-crystallizing (E 420); hypromellose; sodium chloride; sodium dihydrogen phosphate, dihydrate; disodium phosphate, dodecahydrate; purified water.

Pharmaceutical form. Nasal spray, metered solution.

Main physicochemical properties: clear, colorless or slightly yellow liquid, practically odorless.

Pharmacotherapeutic group.

Agents used in diseases of the nasal cavity. 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 nasal mucosa and paranasal sinuses, thereby reducing edema and hyperemia of the nasal and nasopharyngeal mucosa. It also decreases associated excessive mucus secretion and facilitates the removal of blocked nasal secretions, promoting clearance of the nasal passages and improving nasal breathing.

The effect begins within a few minutes after administration and lasts up to 12 hours.

The medicinal product is well tolerated, including by patients with sensitive mucosa, and does not impair mucociliary function.

Pharmacokinetics.

After topical application, the drug is practically not absorbed, and plasma concentrations of xylometazoline are so low that they are practically undetectable (plasma concentration is close to the limit of detection).

Clinical Characteristics.

Indications.

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

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

Used as an adjunctive therapy in otitis media (to reduce mucosal swelling).

For facilitating rhinoscopy.

Contraindications.

• Hypersensitivity to xylometazoline or to any other component of the medicinal product;
• Closed-angle glaucoma;
• Transsphenoidal hypophysectomy and surgical interventions involving exposure of the meninges in medical history;
• Dry rhinitis (rhinitis sicca) or atrophic rhinitis;
• Hyperthyroidism.

Concomitant use with monoamine oxidase inhibitors (MAOIs) is contraindicated, as well as within two weeks after discontinuation of such treatment.

Interaction with other medicinal products and other forms of interaction.

Monoamine oxidase inhibitors (MAOIs): xylometazoline may potentiate the effect of monoamine oxidase inhibitors and may induce a hypertensive crisis. Xylometazoline should not be used in patients taking MAOIs or who have taken them 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.

When used concomitantly with β-blockers, xylometazoline may cause bronchospasm or reduction in blood pressure.

Special precautions for use.

This medicinal product should not be used for longer than 7 consecutive days. Prolonged or excessive use may lead to rebound nasal congestion and/or atrophy of the nasal mucosa.

Due to the risk of developing atrophy of the nasal mucosa, this preparation should be used in patients with chronic inflammation of the nasal mucosa only under medical supervision.

Repeated or chronic use of this medicinal product may lead to rebound congestion syndrome and narrowing of the upper airways. This may manifest as chronic hyperemia of the nasal mucosa (which may eventually lead to atrophic rhinitis). In moderate cases, administration of the drug may be temporarily discontinued in one nostril, or alternatively in both nostrils, until symptom intensity decreases, in order to maintain nasal passage patency.

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

This medicinal product should be used with caution in patients with cardiovascular disorders, arterial hypertension, diabetes mellitus, pheochromocytoma, porphyria, or benign prostatic hyperplasia.

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

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

The formulation includes an auxiliary substance (a moisturizing component) — non-crystallizing sorbitol solution — which helps reduce symptoms of nasal mucosal dryness.

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

Use during pregnancy or breastfeeding.

This medicinal product should not be used during pregnancy due to its potential vasoconstrictive effects.

Lactation. 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 product should be used during breastfeeding only under medical supervision.

Fertility. Adequate data on the effect of Nazonol on fertility are lacking. However, since systemic exposure to xylometazoline hydrochloride is very low, the likelihood of an effect on fertility is extremely small.

Ability to affect reaction speed when driving or operating machinery.

Generally, this medicinal product has no effect or only a negligible effect on the ability to drive or operate machinery. However, with prolonged use at high doses, undesirable effects on the cardiovascular system may occur, which could negatively affect the ability to drive or operate machinery.

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 use more than 3 sprays into each nostril per day. The duration of treatment depends on the course of the disease and should not exceed 7 consecutive days.

The medicinal product's spray dispenser 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 first use, prime the spray pump by pressing it several times until a fine mist is released into the air. After priming, the dispenser will be ready for use.

How to use the spray:

• Thoroughly clear the nasal passages before using the spray;
• Hold the bottle vertically, supporting the bottom with the thumb and positioning the nozzle between the other fingers;
• Slightly tilt the bottle and insert the nozzle into a nostril;
• Administer 1 spray while gently inhaling through the nose;
• After use, before replacing the spray nozzle cap, clean and dry the nozzle;
• To prevent infection, the bottle should be used by only one person.

The last spray is recommended to be administered immediately before bedtime.

Children

The medicinal product must not be used in children under 12 years of age.

Overdose

Symptoms

Systemic effects following nasal administration are unlikely due to local vasoconstriction, which limits absorption. However, in case of systemic absorption, xylometazoline, as an α2-adrenergic agonist, may exert effects similar to clonidine: transient increase in blood pressure followed by prolonged hypotension and sedation.

Intoxication symptoms caused by imidazole derivatives may be clinically unclear, as periods of stimulation may alternate with periods of depression of the central nervous and cardiovascular systems.

Symptoms of central nervous system stimulation include anxiety, excitement, hallucinations, and seizures.

Symptoms of central nervous system depression include decreased body temperature, lethargy, drowsiness, and coma.

Additional possible symptoms include miosis, mydriasis, sweating, nausea, cyanosis, fever, pallor, central nervous system paralysis, sedation, dry mouth, arrhythmia, tachycardia, ataxia, bradycardia, cardiac arrest, arterial hypertension, shock-like hypotension, pulmonary edema, respiratory disturbances, and apnea. Gastrointestinal symptoms such as nausea and vomiting may also occur.

Overdose, especially in children, may significantly affect the central nervous system, causing spasms, coma, bradycardia, apnea, and arterial hypertension, which may later shift to arterial hypotension.

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

Treatment

Severe overdose requires hospitalization. Since xylometazoline hydrochloride is rapidly absorbed, activated charcoal (adsorbent), sodium sulfate (laxative), or gastric lavage (in cases of higher doses) should be administered immediately. Reduction of arterial blood pressure can be achieved using non-selective alpha-blockers. Vasoconstrictors are contraindicated. If necessary, antipyretics and anticonvulsants should be administered, along with artificial oxygen supply. No specific antidotes exist; atropine may be used in cases of bradycardia.

Side effects.

Immune system disorders:

Uncommon (≥1/1,000 to <1/100): hypersensitivity reactions, including angioneurotic edema, rash, itching.

Nervous system disorders:

Rare (≥1/10,000 to <1/1,000): headache, insomnia, fatigue, convulsions (usually in children).

Very rare (<1/10,000): restlessness, drowsiness/sedation (usually in children).

Eye disorders:

Uncommon (≥1/1,000 to <1/100): transient visual disturbances.

Cardiovascular system disorders:

Uncommon (≥1/1,000 to <1/100): palpitations, tachycardia.

Very rare (<1/10,000): arrhythmia, arterial hypertension.

Respiratory, thoracic and mediastinal disorders:

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

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

Gastrointestinal disorders:

Common (≥1/100, <1/10): nausea.

General disorders and administration site conditions:

Common (≥1/100 to <1/10): burning sensation at the application site, drug-induced rhinitis.

Prolonged or frequent use of high doses of xylometazoline may cause burning sensation or dryness of the mucous membrane and increased swelling of the mucous membrane, which intensify with continued use of the drug (drug-induced rhinitis). This effect may occur as early as 7 days of treatment, and if treatment continues, it may lead to long-term damage of the mucous membrane with crust formation (dry rhinitis).

If any adverse reactions occur, treatment should be discontinued and medical advice should be sought.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Keep out of the reach of children.

Packaging. 10 ml solution in a polymer bottle with a spray pump; 1 bottle per cardboard box.

Pharmaceutical category. Over-the-counter.

Manufacturer. LLC "Micropharm".

Manufacturer's address and place of business.

20 Shevchenka Street, Kharkiv, Ukraine, 61013.