Oxyspray

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

Composition:

Active substance: oxymetazoline;

1 ml of solution contains 0.5 mg of oxymetazoline hydrochloride;

Excipients: benzalkonium chloride; levomenthol; racemic camphor; eucalyptol; sodium dihydrogen phosphate monohydrate; disodium edetate; propylene glycol; purified water.

Pharmaceutical form. Nasal spray.

Main physicochemical properties: colorless or slightly yellowish clear liquid with a specific odor.

Pharmacotherapeutic group. Decongestants and other agents for local use in nasal cavity disorders. Sympathomimetics.

ATC code R01A A05.

Pharmacological properties.

Pharmacodynamics.

Oxyspray belongs to the group of local vasoconstrictive agents. Oxymetazoline exerts sympathomimetic and vasoconstrictive effects, reducing nasal mucosal edema. It constricts blood vessels at the site of application, decreases swelling of the nasal and upper respiratory tract mucosa, and reduces nasal discharge. It restores nasal breathing. Relief of nasal mucosal edema promotes restoration of ventilation in the paranasal sinuses and middle ear cavity, thus preventing the development of bacterial complications.

Oxymetazoline exerts antiviral, anti-inflammatory, immunomodulatory, and antioxidant effects. Due to this combined mechanism of action, clinical studies have demonstrated faster and more effective relief of symptoms of acute rhinitis (nasal congestion, rhinorrhea, sneezing, and general malaise).

When applied locally as a nasal spray at therapeutic concentrations, it does not irritate the nasal mucosa or cause hyperemia. The elimination half-life is approximately 35 hours after administration. About 2.1% of the drug is excreted by the kidneys, and approximately 1.1% is excreted in feces.

Treatment with 0.05% oxymetazoline as a nasal spray significantly reduced the duration of the common cold compared to placebo saline solution: from an average of 6 days down to 4 days (P < 0.001). In a double-blind, parallel-group comparative study involving 247 adult patients, faster and more effective reduction of typical symptoms of acute rhinitis [nasal congestion, rhinorrhea, sneezing, and general malaise (P < 0.05)] was demonstrated, attributable to the combined vasoconstrictive, antiviral, anti-inflammatory, and antioxidant effects of oxymetazoline.

Pharmacokinetics.

Duration of action of the drug – up to 12 hours.

Following intranasal administration, the absorbed amount may sometimes be sufficient to produce systemic effects, for example, on the central nervous and cardiovascular systems.

Additional pharmacokinetic data in humans are lacking.

Preclinical safety data

In toxicity studies in dogs, repeated nasal administration of oxymetazoline revealed no risks to human safety. Results of the in vitro bacterial mutagenicity test were negative. Data on carcinogenicity of this medicinal product are currently unavailable. No teratogenic effects were observed in rats and rabbits. Doses higher than the therapeutic level were embryolethal or caused delayed fetal growth. In rats, suppression of maternal milk production was observed. There were no signs of impaired fertility.

Clinical characteristics.

Indications.

• Acute rhinitis.
• Allergic rhinitis.
• Episodes of non-infectious vasomotor rhinitis.
• Restoration of drainage and nasal breathing in diseases of the nasal paranasal sinuses, eustachian tube inflammation associated with rhinitis.
• Relief of swelling prior to diagnostic procedures in the nasal passages.

Contraindications.

Hypersensitivity to oxymetazoline, other adrenomimetics, or to any component of the drug; atrophic rhinitis; increased intraocular pressure, especially in closed-angle glaucoma; pheochromocytoma; severe forms of cardiovascular diseases (arterial hypertension, ischemic heart disease), pronounced atherosclerosis, acute cardiovascular disorders or cardiac asthma, tachysystolic cardiac arrhythmias, angina pectoris; metabolic disorders (hyperthyroidism, diabetes mellitus, porphyria); renal insufficiency. Do not use after transsphenoidal hypophysectomy or other surgical interventions involving opening of the dura mater. Skin inflammation or damage around the nasal passages or nasal mucosa. Concomitant use with monoamine oxidase inhibitors (MAOIs) is contraindicated, as well as within 2 weeks after discontinuation of MAOI therapy. Also contraindicated is concomitant use with other agents that may increase blood pressure. Prostate hyperplasia.

Interaction with other medicinal products and other types of interactions.

Prior to using other medicinal products, consultation with a physician is recommended. This drug should not be used simultaneously with other local vasoconstrictors (regardless of the route of administration), with other nasal decongestants, or with tricyclic antidepressants and maprotiline, due to the possible increase in blood pressure. Such combined use is permissible only after consultation with a physician. Concomitant use with monoamine oxidase inhibitors (MAOIs) may lead to increased blood pressure. Do not use Oxyspray concurrently with MAOIs or within 2 weeks after discontinuation of MAOI therapy (see section "Contraindications"). Concurrent use of oxymetazoline with tricyclic antidepressants increases the risk of arterial hypertension and arrhythmias. Oxymetazoline may reduce the effectiveness of β-adrenergic blockers, methyldopa, or other antihypertensive agents. Concomitant use of sympathomimetics and antiparkinsonian agents may increase toxic effects on the cardiovascular system.

Special precautions for use.

Prolonged use and overdosage of the drug should be avoided. Prolonged use or overdosage of a nasal decongestant may lead to diminished effect (tachyphylaxis). If the drug is used for an extended period or overdosed, treatment with this medicinal product should be discontinued immediately. Abuse of this product may cause atrophy of the mucous membrane, reactive hyperemia with drug-induced rhinitis, as well as epithelial damage and inhibition of its activity. Special monitoring is required in patients with chronic rhinitis and when nasal congestion is relieved prior to diagnostic procedures. Doses higher than recommended should be used only under medical supervision. Continuous use of the drug should not exceed 7 days.

Persistence of nasal congestion after the third day of treatment may indicate the presence of a deviated nasal septum, purulent sinusitis, adenoids, allergic rhinitis, persistent bacterial infection, or other undiagnosed conditions requiring medical consultation and specialized comprehensive therapy.

Medical advice should be sought before starting treatment with this drug in the following cases: high blood pressure, cardiovascular disorders, or hepatic or renal impairment.

Use during pregnancy or breastfeeding.

Oxymetazoline has not been associated with adverse pregnancy outcomes. The drug should be used with caution in patients with arterial hypertension or signs of reduced placental perfusion. Frequent or prolonged use of high doses may reduce placental blood flow. During pregnancy, the drug may be used only if, in the physician’s opinion, the expected benefit to the mother outweighs the potential risk to the fetus/infant. In such cases, special caution is required; exceeding the recommended dosage must be avoided.

It is unknown whether oxymetazoline passes into breast milk. Due to the lack of data, oxymetazoline should not be used during breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

With prolonged use of the drug in doses exceeding the recommended levels, systemic effects on the cardiovascular system cannot be ruled out. In such cases, the ability to drive or operate machinery may be impaired.

Method of Administration and Dosage

Adults and children aged 6 years and older

One spray of OxySpray in each nostril 2–3 times daily. The single dose should not be used more than 3 times daily or for longer than 7 consecutive days. Doses higher than recommended should not be used.

Method of Administration

The spray mechanism operates by pressing the container. Before first use, remove the protective cap, hold the nasal spray in hand, and press the container several times until a consistent aerosol mist is formed. Insert the tip of the nozzle into each nostril and press the container sharply once. During spraying, inhale air through the nose. When administering into the nasal cavity, do not tilt the head back or invert the container. It is not recommended for multiple individuals to use the same container to avoid spreading infection. After use, clean the spray nozzle and cover the container with the protective cap.

Children

The medication may be used in children aged 6 years and older.

Overdose

In case of significant overdose of oxymetazoline or accidental ingestion, the following symptoms may occur: mydriasis, nausea, vomiting, cyanosis, elevated body temperature, spasms, tachycardia, arrhythmia, palpitations, cardiovascular insufficiency, arterial hypertension, dyspnea, respiratory disorders, pulmonary edema, cardiac arrest, excessive sweating, agitation, fear sensation, seizures, pallor, miosis, hyposmia, hallucinations, psychiatric disorders, physical discomfort. Very rarely, central nervous system (CNS) depression may be observed, manifesting as drowsiness, decreased body temperature, bradycardia, arterial hypotension, collapse, shock, respiratory disturbances, apnea, loss of consciousness, potentially progressing to coma.

Clinical manifestations of overdose in children include CNS-related symptoms: seizures and coma, hallucinations, bradycardia, apnea, arterial hypertension changing to hypotension.

Emergency measures: in case of suspected oxymetazoline overdose, immediate hospitalization to an intensive care unit is required. Immediate administration of activated charcoal (adsorbent), sodium sulfate (laxative), or gastric lavage (in case of overdose with a large amount of the drug) is recommended, as oxymetazoline may be rapidly absorbed. In case of arterial hypertension, vasodilators (phentolamine, sodium nitroprusside) should be administered. Vasopressor agents should not be used. Non-selective α-blockers may be used as an antidote. If necessary, measures to reduce body temperature should be taken; benzodiazepines may be administered for agitation; anticonvulsant therapy should be performed with benzodiazepines and/or barbiturates. In severe cases, tracheal intubation and artificial ventilation of the lungs may be required.

Adverse Reactions

With frequent and prolonged use, sensations of burning, tingling in the nose, facial flushing, sneezing, and dryness of the mucous membrane may occur. Prolonged continuous use of vasoconstrictive agents may lead to tachyphylaxis or the development of drug-induced rhinitis. Generally, severe adverse effects are not expected.

The frequency of adverse reactions is classified as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1,000 to < 1/100), rare (≥ 1/10,000 to < 1/1,000), very rare (< 1/10,000), and not known (cannot be estimated from available data).

Cardiovascular system.

Rare: palpitations (awareness of heartbeat), tachycardia, increased blood pressure, chest pain.

Very rare: arrhythmias.

Eye disorders.

Rare: eye irritation, discomfort or redness, blurred vision.

Gastrointestinal disorders.

Rare: nausea.

Immune system disorders.

Uncommon: hypersensitivity reactions (angioneurotic edema, rash, itching).

Nervous system disorders.

Very rare: headache, nausea, dizziness, sedation, drowsiness or insomnia, restlessness, nervousness, anxiety, tremor, increased fatigue, hallucinations (especially in children).

Musculoskeletal and connective tissue disorders.

Very rare: seizures (especially in children).

Respiratory, thoracic and mediastinal disorders.

Rare: nasal, oral or throat discomfort or irritation, burning sensation or dryness of the nasal mucosa, sneezing, epistaxis. After the effect of the drug wears off, a sensation of severe nasal congestion may occur (rebound hyperemia).

General disorders.

Very rare: weakness.

Frequency not known: tachyphylaxis (with prolonged use or overdose).

Reporting suspected adverse reactions.

Reporting of suspected adverse reactions after authorization of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and patients, as well as their legal representatives, are encouraged to report any suspected adverse reactions and lack of efficacy through 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 30 °C. Keep out of reach and sight of children.

Packaging.

10 ml in a polyethylene container with a spray pump and a cap with a first-opening control, packed in a cardboard box.

Supply category.

Over-the-counter (without prescription).

Manufacturer.

Ukrainian-Spanish joint venture "Sperko Ukraine".

Manufacturer's address and location of operations.

21027, Ukraine, Vinnytsia, 600-richchya St., 25.