Galazolin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT GALEZOLINE® (GALAZOLIN®)

Composition:

Active substance: xylometazoline hydrochloride;

1 g of nasal gel contains 0.5 mg or 1 mg of xylometazoline hydrochloride;

Excipients: sodium chloride, disodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate monohydrate, disodium edetate, benzalkonium chloride solution 50%, sorbitol (E 420), hydroxyethylcellulose, glycerol, purified water.

Pharmaceutical form. Nasal gel.

Main physicochemical properties: colorless or almost colorless, transparent or slightly opalescent viscous liquid.

Pharmacotherapeutic group. Medicinal products used in nasal disorders. Sympathomimetics, simple preparations.

ATC code R01A A07.

Pharmacological Properties

Pharmacodynamics

Xylometazoline is an imidazoline derivative with sympathomimetic action. It is a direct agonist of α-adrenergic receptors.

The drug causes vasoconstriction of the mucosal blood vessels, reduces swelling, alleviates mucosal hyperemia in the nasal cavity and nasopharynx, and decreases exudate production. GELAZOLINE® is formulated as a gel, which enables moisturizing of the nasal mucosa and prevents the drug from running down into the nasal cavity floor and throat.

Pharmacokinetics

The drug begins to act within 5–10 minutes, and its effect lasts up to 10 hours. When applied to the nasal mucosa, the drug induces local vasoconstriction. It is generally not absorbed in clinically significant amounts and does not produce systemic effects.

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 swelling of the mucous membrane).

Contraindications.

• Hypersensitivity to any component of the drug.
• Should not be used in patients after hypophysectomy or after other surgical interventions involving opening of the dura mater.
• Atrophic rhinitis or dry rhinitis (rhinitis sicca).
• Acute coronary conditions, coronary asthma, hyperthyroidism, closed-angle glaucoma.
• Concomitant treatment with monoamine oxidase inhibitors (MAOIs) and within 2 weeks after discontinuation of such treatment.

Interaction with other medicinal products and other forms of interaction.

MAO inhibitors: xylometazoline may potentiate the effect of MAO inhibitors and induce a hypertensive crisis. Xylometazoline should not be used in patients taking or who have taken MAO inhibitors within the previous 2 weeks.

Tricyclic and tetracyclic antidepressants: concomitant use of tricyclic or tetracyclic antidepressants and sympathomimetic agents may enhance the sympathomimetic effect of xylometazoline; therefore, simultaneous administration of these agents is not recommended.

Concomitant use of xylometazoline with other sympathomimetic agents (e.g., ephedrine, pseudoephedrine) should be avoided due to their additive effects.

β-adrenergic blockers: when used concomitantly with β-blockers, may cause bronchospasm or reduction in blood pressure.

Special precautions for use

The medicinal product should be used with caution in patients who experience strong reactions to adrenergic agents, such as insomnia, dizziness, tremor, cardiac arrhythmia, or increased arterial pressure.

The product should not be used in patients with chronic or vasomotor rhinitis, as they may use it for longer than 5 days. Prolonged use beyond the recommended duration may lead to secondary vasodilation and consequently to secondary drug-induced rhinitis (rhinitis medicamentosa). This condition is likely caused by inhibition of norepinephrine release from nerve endings due to stimulation of presynaptic α2-receptors.

Caution is advised when using the product in patients with cardiovascular disorders, arterial hypertension, diabetes mellitus, thyroid disorders, pheochromocytoma, prostate hyperplasia, or those experiencing difficulty in urination. The product should not be used in patients who have received concomitant treatment with monoamine oxidase inhibitors (MAOIs) or within 2 weeks after discontinuation of such therapy.

Doses higher than recommended should not be used, especially in children and elderly patients.

GALAZOLINE® 0.05% should not be used in children under 3 years of age.

GALAZOLINE® 0.1% should not be used in children under 12 years of age.

Due to the presence of benzalkonium chloride, the product may cause irritation of the nasal mucosa.

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

Use during pregnancy or breastfeeding

GALAZOLINE® should not be used during pregnancy due to its possible vasoconstrictive effects.

There is no evidence of any adverse effect on the nursing infant. There are no data indicating that xylometazoline passes into breast milk; however, caution is advised, and the product should be used during breastfeeding only under medical supervision.

Fertility

There are no adequate data on the effect of the drug on fertility. Since systemic exposure to xylometazoline hydrochloride is very low, the potential for effects on fertility is extremely low.

Ability to affect reaction speed when driving or operating machinery

The product usually has no effect or only a minimal effect on the ability to drive vehicles or operate machinery.

However, with prolonged use or use at high doses, adverse reactions affecting the cardiovascular and central nervous systems may occur.

Method of Administration and Dosage

The medication is intended for nasal use.

The medication should be administered onto the nasal mucosa by a quick, single press of the bottle's dispenser.

Before each use, the cap must be removed.

Before the first use of a new bottle, after removing the cap, press the dispenser 3–5 times until the medication (gel) appears.

GAZALOLINE® 0.05% Nasal Gel (one press releases 0.05 mg of xylometazoline hydrochloride) is indicated for children aged 3 years and older.

Children aged 3 to 12 years:

1 dose of gel into each nostril every 8–10 hours.

GAZALOLINE® 0.1% Nasal Gel (one press releases 0.1 mg of xylometazoline hydrochloride) is indicated for adults and children aged 12 years and older.

Adults and children aged 12 years and older:

1 dose of gel into each nostril every 8–10 hours.

GAZALOLINE® should not be used for longer than 3–5 days.

For hygienic reasons, the medication package should be used by only one patient.

Children.

GAZALOLINE® 0.05% should not be used in children under 3 years of age.

GAZALOLINE® 0.1% should not be used in children under 12 years of age.

Overdose.

Excessive local use of xylometazoline hydrochloride or its accidental ingestion may lead to pronounced dizziness, excessive sweating, significant decrease in body temperature, headache, bradycardia, arterial hypertension, respiratory depression, coma, and seizures. Elevated arterial pressure may be followed by a drop in pressure. Young children are more sensitive to toxicity than adults.

All patients suspected of overdose should receive appropriate supportive measures and, if necessary, immediate symptomatic treatment under medical supervision. Medical care should include patient observation for several hours. In cases of severe overdose associated with cardiac arrest, resuscitation efforts should continue for at least 1 hour.

Adverse reactions.

The following undesirable effects are associated with the use of xylometazoline.

Immune system disorders: hypersensitivity reactions, including angioneurotic edema, dyspnea, allergic reactions, rash, pruritus.

Nervous system disorders: headache, drowsiness.

Eye disorders: transient visual disturbances.

Cardiovascular system disorders: palpitations, tachycardia, arterial hypertension (especially in patients with cardiovascular diseases).

Respiratory, thoracic and mediastinal disorders: sneezing, epistaxis (rare).

Prolonged use beyond the recommended duration and/or use in doses higher than recommended may lead to secondary drug-induced inflammation of the nasal mucosa.

Gastrointestinal disorders: nausea.

General disorders and administration site conditions: fatigue, feeling of weakness. Dryness of the nasal mucosa, irritation of the nasal mucosa, burning sensation in the nose and throat, discomfort related to the nasal mucosa may occur.

Shelf life. 3 years.

The shelf life after first opening of the bottle is not more than 12 weeks.

Storage conditions.

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

Keep out of the reach of children.

Incompatibilities. Not known.

Packaging. 10 g of 0.05% or 0.1% gel in bottles with a pump dispenser and an applicator with a safety nozzle. 1 bottle in a cardboard box.

Availability.

Over-the-counter (without prescription).

Manufacturer.

Pharmaceutical Works “POLPHARMA” S.A., Poland

Manufacturer's address and place of business.

Medana Branch in Sieradz, 10 Wladyslawa Lokietka Str., 98-200 Sieradz, Poland