Euca spray

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT EUCASPRAY (EUCASPRAY)

Composition:

Active substance: xylometazoline hydrochloride;

1 ml of solution contains 1 mg of xylometazoline hydrochloride;

Excipients: benzalkonium chloride; disodium edetate; sodium dihydrogen phosphate monohydrate; sodium hydrogen phosphate dodecahydrate; sodium chloride; polyoxyl 40 hydrogenated castor oil; sorbitol (E 420); eucalyptus oil; purified water.

Pharmaceutical form. Nasal spray.

Main physico-chemical properties: opalescent solution, from colorless to whitish, with a characteristic eucalyptol odor.

Pharmacotherapeutic group. Agents used in nasal cavity disorders. Decongestants and other agents for local use in nasal disorders. Simple sympathomimetics. Xylometazoline.

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 adjacent areas of the nasopharynx, thereby reducing edema 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 improving nasal breathing. The effect of the drug begins within 2 minutes after administration and lasts up to 12 hours. The drug is well tolerated, including by patients with sensitive mucosa, and does not impair mucociliary function. Studies have shown that xylometazoline reduces the infectious activity of human rhinovirus associated with the common cold. The drug has a balanced pH value within the physiological range of the nasal cavity.

Pharmacokinetics.

After local administration, 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).

Xylometazoline has no mutagenic properties. In addition, studies in animals 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.
• Facilitation of secretion drainage in diseases of the nasal accessory sinuses.
• Adjunctive therapy in cases of otitis media (to reduce mucosal swelling).
• Facilitation of rhinoscopy.

Contraindications.

Hypersensitivity to xylometazoline, any other component of the medicinal product, or to other sympathomimetic amines; narrow-angle glaucoma, transsphenoidal hypophysectomy, or history of surgical procedures involving exposure of the meninges; dry rhinitis (rhinitis sicca) or atrophic rhinitis. Concomitant use of monoamine oxidase inhibitors (MAOIs) or their use within 2 weeks prior to treatment with Eukaspray.

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 cause a hypertensive crisis. Xylometazoline must not be used in patients taking or who have taken MAO inhibitors within the previous two weeks (see section "Contraindications").

Tricyclic and tetracyclic antidepressants: concomitant use of tricyclic or tetracyclic antidepressants and sympathomimetic agents, including xylometazoline, may enhance sympathomimetic effects; therefore, concomitant use of such agents is not recommended.

Concomitant use with beta-adrenergic blockers may cause bronchospasm or reduced 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.

Due to the risk of developing atrophy of the nasal mucosa, this medicinal product 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 in the future may lead to atrophic rhinitis). In cases of moderate severity, administration of the product may be temporarily discontinued in one nasal passage or, alternatively, in both nasal passages 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.

The recommended dose of the 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, porphyria, or benign prostatic hyperplasia. Xylometazoline must 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 use xylometazoline are at increased risk of serious ventricular cardiac rhythm disturbances.

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 improved or resolved within several days after appropriate treatment. The medicinal product should be discontinued immediately and medical advice sought if signs or symptoms of posterior reversible encephalopathy syndrome/reversible cerebral vasoconstriction syndrome develop.

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

The product contains hydrogenated polyethoxylated castor oil, which may cause allergic reactions.

There is also evidence that sorbitol, the moisturizing component in EucaSprey, helps relieve dryness and irritation of the nasal mucosa.

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, and the product should be used during breastfeeding only on the advice of a physician. If used during breastfeeding, prolonged use should be avoided due to the risk of adverse effects in the infant (tachycardia, excitation, increased blood pressure).

Fertility
There are no adequate data on the effect of the product on fertility. 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, the medicinal product has no or negligible influence 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.

Dosage and Administration.

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.

To use the spray: insert the tip of the nozzle into the nostril and press firmly once on the bottle. During spraying, inhale through the nose. Do not tilt the head backward or turn the bottle upside down while administering the spray. To prevent the spread of infection, do not use the same bottle for multiple individuals. The last application is recommended to be performed immediately before bedtime.

Children.

Eucasept spray may be used in children aged 12 years and older.

Overdose.

Symptoms. Systemic effects after nasal administration are unlikely due to local vasoconstriction, which reduces absorption. However, in case of systemic absorption, xylometazoline, as an α2-adrenergic agonist, may exert effects similar to clonidine: a transient increase in blood pressure followed by a more 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.

Impaired consciousness may indicate severe, overt intoxication. Younger children are more sensitive to toxic effects than adults.

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

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

Treatment. Severe overdose requires hospital treatment. Since xylometazoline hydrochloride is rapidly absorbed, activated charcoal (adsorbent), sodium sulfate (laxative), or gastric lavage (after ingestion of higher doses) should be administered immediately. Reduction of blood pressure can be achieved using non-selective alpha-blockers. Vasoconstrictor agents are contraindicated. If necessary, antipyretics, anticonvulsants, and artificial oxygen ventilation should be applied. There are no specific antidotes; atropine may be used in cases of bradycardia.

Side effects.

From the immune system:

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

From the nervous system:

Rare (≥ 1/10,000, < 1/1,000): headache, insomnia, fatigue, seizures (usually in children);

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

From the visual organs:

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

From the cardiovascular system:

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

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

From the respiratory system, thorax and mediastinum:

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

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

From the gastrointestinal system:

Common (≥ 1/100, < 1/10): nausea;

Uncommon (≥ 1/1,000, < 1/100): vomiting.

General disorders and administration site reactions:

Common (≥ 1/100, < 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 5 days of treatment, and if treatment continues, it may lead to long-term mucosal damage with crust formation (dry rhinitis).

Reporting suspected adverse reactions. Reporting of suspected adverse reactions after drug registration is of great importance. It allows continuous monitoring of the benefit-risk ratio of the drug. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of drug efficacy via the Automated Pharmacovigilance Information System 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 container with a spray pump and cap, in a carton.

Prescription status.

Over-the-counter.

Manufacturer.

Ukrainian-Spanish joint venture "Sperco Ukraine".

Manufacturer's address and location of business activity.

21027, Ukraine, Vinnytsia, vul. 600-richchia, 25.

Tel.: + 38(0432)52-30-36. E-mail: [email protected]

www.sperco.ua