Aqua spray oxy

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT AQUA SPRAY OXY

Composition:

Active substance: oxymetazoline hydrochloride;

1 ml of solution contains 0,5 mg of oxymetazoline hydrochloride;

Excipients: citric acid monohydrate; sodium citrate; glycerol; benzalkonium chloride solution; purified water.

Pharmaceutical form. Nasal spray, metered.

Main physicochemical properties: almost transparent solution, ranging from colorless to slightly yellowish.

Pharmacotherapeutic group.

Anti-edematous and other locally acting drugs for nasal cavity disorders. Sympathomimetics, simple preparations.

ATC code R01A A05.

Pharmacological properties.

Pharmacodynamics.

AQUA SPRAY OXY belongs to the group of local vasoconstrictors. Oxymetazoline exerts a sympathomimetic and vasoconstrictive effect, reducing swelling of the nasal mucosa. It constricts blood vessels at the site of application, reduces swelling of the nasal mucosa and upper respiratory tract, and decreases nasal discharge. It restores nasal breathing. Reduction of nasal mucosa swelling promotes restoration of ventilation in the paranasal sinuses and the 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 acute rhinitis symptoms (nasal congestion, rhinorrhea, sneezing, and general malaise).

A double-blind, parallel-group comparative study involving 247 patients demonstrated a rapid and significant reduction in typical symptoms of acute rhinitis (nasal congestion, runny nose, sneezing, and general discomfort) (p < 0.05), attributable to the combined vasoconstrictive, antiviral, anti-inflammatory, and antioxidant effects of oxymetazoline. Thus, treatment with 0.05% oxymetazoline nasal spray significantly shortened the duration of the common cold from 6 to 4 days on average, compared to saline (p < 0.001).

Pharmacokinetics.

The effect of oxymetazoline begins within a few seconds.

The onset of action of 0.05% oxymetazoline nasal spray was measured in an open-label study and found to occur on average after 20.6 seconds. This finding was confirmed in a double-blind, parallel-group comparative study versus isotonic saline solution involving 247 patients, where the average onset of action was observed within 25 seconds. The duration of action of the drug lasts up to 12 hours.

When applied locally via the nasal route 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 oxymetazoline is excreted via the kidneys, and approximately 1.1% is excreted in feces.

Safety preclinical data.

Repeated-dose toxicity studies of intranasal oxymetazoline in dogs revealed no risks to human health. The in vitro mutagenicity test in bacteria was negative. There are no data regarding carcinogenicity. No teratogenic effects were observed in rats and rabbits. Doses exceeding the therapeutic range caused embryolethal effects or fetal growth retardation. Lactation was inhibited in rats. There are no data on fertility impairment.

Preclinical studies show that benzalkonium chloride, depending on concentration and exposure time, may suppress ciliary motility, leading to irreversible ciliary arrest, as well as histopathological changes in the nasal mucosa.

Clinical characteristics.

Indications.

Acute respiratory diseases accompanied by nasal congestion.

Allergic rhinitis.

Vasomotor rhinitis.

For restoration of drainage and nasal breathing in diseases of the nasal accessory sinuses, eustachitis.

For reduction of swelling prior to diagnostic procedures in the nasal passages.

Contraindications.

Hypersensitivity to the components of the medicinal product.

Dry rhinitis.

Do not use after transsphenoidal hypophysectomy or other surgical interventions involving the dura mater.

Children under 6 years of age.

Interaction with other medicinal products and other forms of interaction.

Concomitant use of oxymetazoline and:

• tricyclic antidepressants
• monoamine oxidase (MAO) inhibitors such as tranylcypromine
• hypertensive agents

may lead to increased blood pressure. These drugs should not be combined if possible.

In cases of oxymetazoline overdose or if swallowed, as well as when used concomitantly or immediately after tricyclic antidepressants and/or MAO inhibitors, an increase in blood pressure is possible.

Special precautions for use

The medicinal product should be used only after careful assessment of the benefit-risk ratio in the following cases:

• increased intraocular pressure, especially in angle-closure glaucoma;
• severe cardiovascular disorders (e.g. ischemic heart disease) and arterial hypertension;
• pheochromocytoma;
• metabolic disorders (e.g. hyperthyroidism, diabetes mellitus);
• benign prostatic hyperplasia;
• porphyria;
• concomitant use of MAO inhibitors and other medicinal products that potentially increase blood pressure.

Prolonged use or overdose of the nasal decongestant may lead to reduced effectiveness. Misuse of this product may cause drug-induced rhinitis, mucosal atrophy, and reactive hyperemia of the nasal mucosa (rebound effect).

The preservative (benzalkonium chloride) contained in the medicinal product may cause swelling of the nasal mucosa, especially with prolonged use. If such a reaction (chronically blocked nose) is suspected, a preservative-free nasal preparation should be used. If such a preparation is not available, consideration should be given to using another pharmaceutical form.

Use during pregnancy or breastfeeding.

Pregnancy. Data from a limited number of pregnant women exposed to this medicinal product during the first trimester do not indicate adverse effects of oxymetazoline on pregnancy or on the health of the fetus and newborn. Currently, there are no adequate epidemiological data available. Animal studies have shown reproductive toxicity at doses exceeding the therapeutic range.

The product should be used with particular caution during pregnancy or breastfeeding, following a careful benefit-risk assessment. Exceeding the recommended dosage is not recommended, as overdose may impair fetal blood supply.

Breastfeeding. It is unknown whether oxymetazoline passes into breast milk; therefore, the use of the product is possible only after a careful benefit-risk assessment. Exceeding the recommended dosage is not recommended, as it may reduce breast milk production.

Ability to affect reaction speed when driving or operating machinery.

When used at recommended doses, the product is not expected to affect reaction speed when driving or operating machinery. However, after prolonged use at doses exceeding the recommended levels, a systemic effect 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

For adults and children aged 6 years and older — 1 spray into each nostril 2–3 times daily. Do not use the stated single dose more than 3 times per day. Do not exceed the recommended doses. The medicinal product should not be used for longer than 7 days.

Method of Administration

The spray mechanism operates by pressing on the finger rest. Before first use, remove the protective cap, hold the bottle in hand, and press the pump several times until a consistent aerosol mist is produced. With the spray nozzle held close to the entrance of the nostril, administer one spray into each nostril. After use, clean the spray nozzle and, if necessary, the protective cap.

Children

Do not use the medicinal product in children under 6 years of age.

Overdose

Overdose may occur following nasal administration or accidental oral ingestion of the medicinal product. The clinical picture caused by intoxication with imidazole derivatives may be diffuse, as hyperreactive phases may alternate with phases of depression of the central nervous system, cardiovascular system, and respiratory system.

Stimulation of the central nervous system may manifest as anxiety, agitation, hallucinations, and seizures. Depression of the central nervous system may present as decreased body temperature, lethargy, drowsiness, and coma.

Other possible symptoms include miosis, mydriasis, elevated body temperature, excessive sweating, pallor, cyanosis, palpitations, tachycardia, bradycardia, arrhythmia, cardiac arrest, arterial hypertension, shock hypotension, nausea and vomiting, respiratory depression, and apnea, as well as psychogenic disorders.

In children, overdose often leads to predominant central nervous system effects, including seizures and coma, bradycardia, apnea, and arterial hypertension, which may follow an initial phase of hypotension.

Therapeutic measures are indicated in cases of severe overdose. Administration of activated charcoal (adsorbent), sodium sulfate (laxative), or gastric lavage (in case of ingestion of a large amount of the medicinal product) should be performed immediately, as oxymetazoline may be rapidly absorbed. Vasopressor agents are contraindicated. Non-selective alpha-blockers may be used as an antidote. If necessary, anticonvulsant therapy, lung ventilation, and antipyretic measures should be initiated.

Side effects

The frequency of adverse reactions is defined according to the following categories: 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); frequency not known (cannot be estimated from the available data).

From the nervous system

Very rare: restlessness, insomnia, fatigue (drowsiness, sedative effect), headache, hallucinations (especially in children).

From the cardiovascular system

Rare: palpitations, tachycardia, arterial hypertension.

Very rare: arrhythmias.

From the respiratory system, thorax and mediastinum

Common: burning sensation and dryness of the nasal mucosa, sneezing.

Uncommon: rebound effect, increased swelling of the mucous membrane, nasal bleeding after discontinuation.

Very rare: apnea in newborns and young children.

From the musculoskeletal and connective tissue system

Very rare: convulsions (mainly in children).

From the immune system

Uncommon: hypersensitivity reactions (angioedema, rash, itching).

Reporting of adverse reactions after marketing authorization is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the automated pharmacovigilance information system at: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Shelf life after first opening — 6 months.

Do not use after the expiry date.

Storage conditions.

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

Keep out of reach and sight of children.

Packaging.

10 ml in a polymer bottle with a nasal spray pump. 1 bottle per cardboard box.

Supply category.

Over-the-counter.

Manufacturer.

JSC "CHEMICAL PHARMACEUTICAL PLANT "CHERVONA ZIRKA".

Manufacturer's address.

1, Gordienkivska Street, Kharkiv, Kharkiv Oblast, 61010, Ukraine.