Nazopas

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT Nazopass (Nazopass®)

Composition:

Active substance: oxymetazoline;

1 ml of solution contains oxymetazoline hydrochloride 0.25 mg or 0.5 mg;

Excipients: sodium citrate (E 331); citric acid, monohydrate (E 330); disodium edetate (E 386); benzalkonium chloride; glycerol (E 422); water for injections.

Pharmaceutical form. Nasal drops, solution.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group.

Anti-edematous and other drugs for local use in nasal cavity disorders. Sympathomimetics, single preparations. ATC code R01A A05.

Pharmacological Properties

Pharmacodynamics

Oxymetazoline belongs to the group of local vasoconstrictor agents. Oxymetazoline exerts sympathomimetic and vasoconstrictive effects, reducing edema of the nasal mucosa. 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 re-aeration of 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 symptoms of acute rhinitis (nasal congestion, rhinorrhea, sneezing, malaise).

Clinical efficacy

A double-blind, parallel-group comparative study involving 247 patients demonstrated faster and greater improvement in typical symptoms of acute rhinitis (nasal congestion, rhinorrhea, sneezing, malaise) (p < 0.05), attributable to the combined vasoconstrictive, antiviral, anti-inflammatory, and antioxidant effects of oxymetazoline. Thus, treatment with 0.05% oxymetazoline nasal drops significantly reduced the duration of the common cold compared to placebo (physiological saline), from an average of 6 days down to 4 days (p < 0.001).

Pharmacokinetics

The effects of oxymetazoline manifest within several minutes after instillation.

When applied topically to the nasal mucosa 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 via the kidneys, and approximately 1.1% is excreted in feces.

The duration of the drug's effect lasts several hours (on average, 6–8 hours), with a maximum duration of up to 12 hours.

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 paranasal sinuses, eustachitis.
• To relieve swelling prior to diagnostic procedures in the nasal passages.

Contraindications.

• Hypersensitivity to oxymetazoline or to any other component of the medicinal product.
• Atrophic rhinitis.
• Should not be used after transsphenoidal hypophysectomy or other surgical interventions exposing the meninges.
• Use of monoamine oxidase inhibitors (MAOIs) and within 2 weeks after discontinuation of MAOI therapy, as well as use of other agents causing increased blood pressure.
• Elevated intraocular pressure, especially in angle-closure glaucoma.
• Severe forms of cardiovascular diseases (e.g., ischemic heart disease) and arterial hypertension.
• Pheochromocytoma.
• Metabolic disorders (e.g., hyperthyroidism, diabetes mellitus).
• Prostatic hyperplasia.
• Porphyria.

Nasopass 0.25 mg is contraindicated in infants and children under 1 year of age; Nasopass 0.5 mg is contraindicated in children under 6 years of age.

Interaction with other medicinal products and other forms of interactions.

Concomitant use of oxymetazoline and:

• tricyclic antidepressants;
• tranilcypramine-type MAO inhibitors;
• hypertensive agents

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

Special precautions for use

Prolonged use and overdosing of the medicinal product should be avoided. In particular, the effect of nasal decongestants may diminish with prolonged use or overdosing (tachyphylaxis). This may lead to the need for higher doses or more frequent administration, potentially resulting in dependence on continuous use of the drug. If prolonged use or overdosing occurs, the use of this medicinal product should be discontinued immediately.

Improper use of rhinological preparations may lead to the following conditions:

• Reactive hyperemia of the nasal mucosa (rebound effect);
• Chronic swelling of the nasal mucosa (medicamentous rhinitis);
• Atrophy of the nasal mucosa.

Use in chronic rhinitis or at doses higher than recommended should be carried out only under medical supervision.

This product contains 0.040 mg of benzalkonium chloride per milliliter. Prolonged use may cause swelling of the nasal mucosa.

Use during pregnancy or breastfeeding.

Pregnancy

Data from a limited number of women exposed during the first trimester of pregnancy do not indicate the occurrence of adverse reactions affecting the course of pregnancy or the health of the fetus/newborn. Other epidemiological data are currently lacking. Animal studies have shown reproductive dose-dependent toxicity when doses exceeding therapeutic levels were administered. This medicinal product should be used during pregnancy only with caution, strictly after consultation with a physician and careful assessment of the benefit-risk ratio for the mother and fetus. The recommended dosage should not be exceeded during pregnancy, as overdosing may impair fetal blood supply.

Breastfeeding period

Data on the passage of oxymetazoline into breast milk are not available. The product should be used during breastfeeding only after consultation with a physician and careful evaluation of the benefit-risk ratio. The recommended dosage should not be exceeded during breastfeeding, as overdosing may reduce the amount of breast milk in women.

Ability to affect reaction speed when driving or operating machinery.

When used at therapeutic doses, the product does not affect the ability to drive or operate machinery. However, a general effect on the cardiovascular and nervous systems cannot be completely ruled out.

Method of Administration and Dosage

Nazopas, nasal drops, is intended for intranasal use.

The head should be tilted backward, and normal breathing should be maintained during administration into both nostrils.

Adults, adolescents, and children aged 6 years and older

Administer Nazopas 0.5 mg/mL, 1–2 drops into each nostril 2–3 times daily.

The single dose should not be used more than 3 times per day.

The effect of the medication develops within 25 seconds after administration and lasts for several hours (on average 6–8 hours, up to 12 hours maximum).

Children aged 1 to 6 years

Administer Nazopas 0.25 mg/mL, 1–2 drops into each nostril 2–3 times daily.

The single dose should not be used more than 3 times per day.

The effect of the medication develops within a few minutes after administration and lasts for several hours (on average 6–8 hours, up to 12 hours maximum).

Doses higher than recommended should only be used under medical supervision.

The medication Nazopas should not be used for longer than 5–7 days without consulting a physician.

Children

Do not use Nazopas 0.25 mg/mL in children under 1 year of age.

Do not use Nazopas 0.5 mg/mL in children under 6 years of age.

Overdose

Following prolonged use or overdose of nasal decongestants, their effect may diminish (tachyphylaxis). This may lead to increased dosing or more frequent administration, potentially resulting in dependence on the medication. In cases of prolonged use or overdose, treatment with this medication should be discontinued immediately.

Overdose may occur after nasal or accidental oral administration. The clinical picture of intoxication with imidazole derivatives may be unclear, as periods of stimulation may alternate with periods of depression of the central nervous, cardiovascular, and respiratory systems.

Stimulation of the central nervous system may manifest as anxiety, agitation, hallucinations, and seizures.

Depression of the central nervous system may manifest as decreased body temperature, lethargy, drowsiness, and possible development of coma.

Other possible symptoms include: miosis, mydriasis, elevated body temperature, increased sweating, pallor, cyanosis, rapid heartbeat, tachycardia, bradycardia, cardiac arrhythmia, cardiac arrest, arterial hypertension, shock-like hypotension, nausea, vomiting, respiratory insufficiency, and apnea, as well as psychiatric disturbances.

In particular, in children, overdose may predominantly cause effects on the central nervous system: seizures and development of coma, bradycardia, apnea, as well as arterial hypertension possibly progressing to arterial hypotension.

Intensive supportive therapy is indicated in cases of severe overdose. Immediate administration of activated charcoal (adsorbent), sodium sulfate (laxative), or gastric lavage (in cases of overdose with a large amount of the drug) is recommended, as oxymetazoline may be rapidly absorbed.

Vasopressor agents are contraindicated. Non-selective α-blockers may be used as an antidote. If necessary, measures to reduce body temperature, anticonvulsant therapy, and lung ventilation should be implemented.

Side effects

Side effects are classified by frequency of occurrence as follows: very common (≥ 10%), common (≥ 1% and < 10%), uncommon (≥ 0.1% and < 1%), rare (≥ 0.01% and < 0.1%), very rare (< 0.01%), and isolated cases.

From the nervous system

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

From the cardiovascular system

Rare: palpitations (awareness of heartbeat), tachycardia, arterial hypertension, chest pain.

Very rare: arrhythmia.

From the respiratory system

Common: nasal discomfort (e.g. burning sensation) or dryness of the nasal mucosa, sneezing.

Uncommon: after the effect of the medication wears off – sensation of severe nasal congestion, epistaxis (nosebleed).

Very rare: apnea in infants and newborns.

From the musculoskeletal system

Very rare: cramps (especially in children).

From the immune system

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

General disorders and administration site reactions

Very rare: increased fatigue (drowsiness), weakness.

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

Shelf life

Closed vial: 3 years.

After first opening of the vial, the solution is suitable for use within 1 month. Store in the original packaging in a place protected from light. Do not refrigerate or freeze.

Storage conditions

Store in the original packaging to protect from light. Do not refrigerate or freeze.

After first opening, store the vial in the original packaging in a place protected from light.

Keep out of reach of children.

Packaging

10 ml in a dropper bottle; 1 dropper bottle in a cardboard box.

Prescription category

Over-the-counter (without prescription).

Manufacturer

ALKALOID AD Skopje.

ALKALOID AD Skopje.

Manufacturer's address and location of business activity

Boulevard Aleksandar Makedonski 12, Skopje, 1000, Republic of North Macedonia.

Boulevard Aleksandar Makedonski 12, Skopje, 1000, Republic of North Macedonia.