Nazivin® sensitive

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NASIVIN® SENSITIVE (NASIVIN® SENSITIVE)

Composition:

Active substance: oxymetazoline;

1 ml of 0.025% solution contains 0.25 mg of oxymetazoline hydrochloride;

1 ml of 0.05% solution contains 0.5 mg of oxymetazoline hydrochloride;

Excipients: citric acid monohydrate; sodium citrate; glycerol (85%); purified water.

Pharmaceutical form. Nasal spray.

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

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

ATC code R01A A05.

Pharmacological Properties

Pharmacodynamics

Nazivin® Sensitive belongs to the group of local vasoconstrictive agents. Oxymetazoline exerts sympathomimetic and vasoconstrictive effects, reducing swelling of the nasal mucosa. It constricts blood vessels at the site of application, decreases edema of the nasal and upper respiratory tract mucosa, and reduces nasal discharge. It restores nasal breathing. Reduction of nasal mucosal swelling promotes re-establishment 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 symptoms of acute rhinitis (nasal congestion, rhinorrhea, sneezing, and general malaise).

When applied locally as a nasal formulation at therapeutic concentrations, oxymetazoline 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% via feces.

Treatment with 0.05% oxymetazoline as a nasal spray, compared to physiological saline, significantly reduced the duration of the common cold: 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, runny nose, 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 is up to 12 hours.

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

Additional pharmacokinetic data in humans are lacking.

Preclinical Safety Data

In toxicity studies conducted in dogs, repeated nasal administration of oxymetazoline revealed no risks to human safety. Results of the in vitro bacterial mutagenicity test were negative. Currently, there are no data available on the carcinogenic potential of this medicinal product. No teratogenic effects were observed in rats and rabbits. However, doses higher than the therapeutic level were embryolethal or caused delayed fetal growth. In rats, inhibition of maternal milk production was observed. There were no signs of impaired fertility.

Clinical characteristics.

Indications.

• Acute rhinitis.
• Allergic rhinitis.
• Attacks of non-infectious vasomotor rhinitis.
• To restore drainage and nasal breathing in diseases of the nasal accessory sinuses, eustachian tube inflammation associated with rhinitis.
• To reduce swelling prior to diagnostic procedures in nasal passages.

Contraindications.

• Hypersensitivity to oxymetazoline or any other component of the medicinal product.
• Atrophic rhinitis.
• Do not use after transsphenoidal hypophysectomy or other surgical interventions involving exposure of the meninges.
• Use of monoamine oxidase inhibitors (MAOIs) and within 2 weeks after discontinuation of MAOI therapy, as well as use of other drugs promoting 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).
• Prostate hyperplasia.
• Porphyria.

Nasivin® Sensitive 0.025% is contraindicated in infants and children under 1 year of age; Nasivin® Sensitive 0.05% is contraindicated in children under 6 years of age.

Interaction with other medicinal products and other types of interactions.

Concomitant use of oxymetazoline with MAO inhibitors of the tranylcypromine type, tricyclic antidepressants, and hypertensive agents may lead to increased blood pressure. Therefore, these drugs should not be used concurrently.

Special precautions for use.

Prolonged use and overdosing of the medicinal product should be avoided. In particular, the effect of nasal decongestants may decrease 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, treatment with this medicinal product should be discontinued immediately.

Improper use of intranasal medications may lead to the following conditions:

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

Use in chronic rhinitis, as well as at doses higher than recommended, should only occur under medical supervision.

Use during pregnancy or breastfeeding.

Pregnancy.

Data from a limited number of women exposed during the first trimester of pregnancy do not indicate adverse reactions affecting the course of pregnancy or the health of the fetus/newborn. Other epidemiological data are currently unavailable. Animal studies have shown dose-dependent reproductive toxicity at doses exceeding the therapeutic dose. The 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.

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

Ability to influence reaction rate while driving or operating machinery.

When used at therapeutic doses, the medicinal product does not affect reaction speed while driving or operating machinery. However, a general effect on the cardiovascular and nervous systems cannot be completely ruled out.

Method of Administration and Dosage

Nasivin® Sensitive, nasal spray, is intended for nasal use.

Children aged 1 to 6 years
– 1 spray of Nasivin® Sensitive 0.025% into each nostril 2–3 times daily. The single dose should not be used more than 3 times a day or for longer than 7 days. Doses higher than recommended should not be used.

Adults and children aged 6 years and older
– 1 spray of Nasivin® Sensitive 0.05% into each nostril 2–3 times daily. The single dose should not be used more than 3 times a day or for longer than 7 consecutive days. Doses higher than recommended should not be used.

The spray mechanism activates when pressing the dosing device. Before the first use, remove the protective cap and periodically press the dosing device to ensure consistent spray performance. Hold the bottle upright under the nostril and administer 1 spray. Afterwards, clean the dosing device and replace the protective cap.

Children
Nasivin® Sensitive 0.025% is indicated for children aged 1 to 6 years; Nasivin® Sensitive 0.05% is indicated for children aged 6 years and older.

Overdose

With 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 drug. If prolonged use or overdose occurs, 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 hypothermia, lethargy, drowsiness, and potentially coma.

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

In particular, in children, overdose may predominantly cause effects on the central nervous system: seizures and coma, bradycardia, apnea, as well as arterial hypertension that may progress 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 case 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.

Adverse Reactions

Undesirable 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: arrhythmias.

From the respiratory system.

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

Uncommon: after the effect of Nazivin® Sensitive wears off – sensation of strong nasal congestion, epistaxis (nosebleed).

Very rare: apnea in infants and newborns.

From the musculoskeletal system.

Very rare: convulsions (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 unknown: tachyphylaxis (with prolonged use or overdose).

Reporting suspected adverse reactions after medicine authorization is very important. It allows continuous monitoring of the benefit-risk balance of the medicine. Healthcare professionals are encouraged to report suspected adverse reactions via the national reporting system.

Shelf life.
3 years.

After first opening – no more than 12 months.

Storage conditions.
No special storage conditions required. Keep out of reach of children!

Packaging.
10 ml or 15 ml of solution in a bottle; 1 bottle per cardboard box.

Supply category.
Over-the-counter (without prescription).

Manufacturer.

1. P&G Health Austria GmbH & Co. OG (Batch release authorization)
2. Sofarimex – Indústria Química e Farmacêutica, S.A. (Full-cycle manufacturing)
3. Famar Health Care Services Madrid, S.A.U. (Full-cycle manufacturing)

Manufacturer's address and place of business.

1. Hosslgasse 20, 9800 Spittal an der Drau, Austria
2. Av. das Indústrias – Alto do Colaride, Cacém, 2735-213, Portugal
3. Avda. Leganés, 62, Alcorcón, 28923 Madrid, Spain