Tizin® xylol

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT TYZINE® XYLO (TYZINE® XYLO)

Composition:

Active substance: xylometazoline hydrochloride;

1 ml of solution contains 0.5 mg or 1 mg of xylometazoline hydrochloride;

Excipients: benzalkonium chloride solution; sorbitol solution, non-crystallizing (E 420); sodium chloride; sodium dihydrogen phosphate, dihydrate; disodium hydrogen phosphate, dihydrate; disodium edetate; purified water.

Pharmaceutical form. Nasal drops, solution.

Main physico-chemical characteristics: clear, colorless, odorless solution or with a slight characteristic odor.

Pharmacotherapeutic group. Anti-edematous and other agents for local use in nasal disorders. Sympathomimetics, simple preparations.

ATC code R01A A07.

Pharmacological Properties

Xylometazoline hydrochloride, an imidazole derivative, is a sympathomimetic active substance with alpha-adrenergic action. The drug exerts a vasoconstrictive effect, thereby reducing mucosal edema. Onset of action usually occurs within 5–10 minutes and lasts up to

10 hours; the drug facilitates nasal breathing by reducing mucosal swelling and improving secretion drainage.

When administered intranasally, the absorbed amount of the drug may occasionally be sufficient to cause systemic effects, particularly those affecting the central nervous and cardiovascular systems.

Clinical characteristics.

Indications.

For symptomatic relief of nasal congestion associated with acute rhinitis due to the common cold and influenza, sinusitis, allergic and non-allergic rhinitis.

Contraindications.

Tizin® Xylo should not be used in the following cases:

• hypersensitivity to the active substance xylometazoline hydrochloride or to any of the excipients of the medicinal product;
• dry inflammation of the nasal mucosa with crust formation (dry rhinitis);
• atrophic or vasomotor rhinitis;
• concomitant treatment with monoamine oxidase inhibitors (MAOIs), treatment with monoamine oxidase inhibitors (MAOIs) within two weeks prior to starting Tizin® Xylo nasal drops, or with other medicinal products capable of increasing blood pressure;
• after hypophysectomy or surgical intervention on the dura mater;
• closed-angle glaucoma;
• acute coronary diseases;
• coronary asthma;
• hyperthyroidism.

Due to the presence of benzalkonium chloride used as a preservative, Tizin® Xylo must not be used in case of established hypersensitivity to this compound.

Special precautions.

When applied locally, systemic absorption of xylometazoline hydrochloride is minimal; however, Tizin® Xylo should be used only after careful benefit-risk assessment in patients:

• with severe cardiovascular diseases (e.g., ischemic heart disease, arterial hypertension);
• with pheochromocytoma;
• with metabolic disorders (e.g., in diabetes mellitus);
• with benign prostatic hyperplasia.

Prolonged use and overdosage of sympathomimetic decongestants may lead to reactive hyperemia of the nasal mucosa. This reaction may cause airway obstruction, which in turn leads to repeated or even continuous use of the drug. This may result in chronic edema (medication-induced rhinitis), and eventually in atrophy of the nasal mucosa and anosmia.

In milder cases, treatment with sympathomimetic agents may be discontinued first in one nostril, and after complications subside, treatment may continue by administering the drug into the other nostril, thus preserving partial nasal breathing.

Tizin® Xylo contains benzalkonium chloride. This compound may cause irritation of the nasal mucosa.

Interaction with other medicinal products and other forms of interaction.

Concomitant use of Tizin® Xylo nasal drops with monoamine oxidase inhibitors of the tranylcypromine type or tricyclic antidepressants, as well as with medicinal products that increase blood pressure, may lead to arterial hypertension due to the effects of these agents on the cardiovascular system.

Due to the low systemic absorption of xylometazoline following intranasal administration, interaction with medicinal products administered by other routes is considered unlikely.

Special precautions for use

The medicinal product should be administered with caution to patients who experience strong adverse reactions such as insomnia, dizziness, tremor, cardiac arrhythmia, or increased arterial pressure during treatment with adrenergic agents.

Use during pregnancy or breastfeeding

Pregnancy

Xylometazoline hydrochloride should not be used during pregnancy, as there are insufficient studies on the effects of the medicinal product on the fetus.

Breastfeeding

The medicinal product Tizin® Ksilo should not be used during breastfeeding, as it is unknown whether the active substance passes into breast milk.

Ability to influence reaction speed when driving or operating machinery

Tizin® Ksilo generally does not affect the ability to drive vehicles or operate complex machinery when used at recommended doses. However, the possibility of adverse reactions affecting the central nervous system and visual organs should be taken into account.

Method of Administration and Dosage

Doses

The dose depends on the individual sensitivity of the patient and the clinical effect.

If not otherwise prescribed, children aged 4 to 6 years should receive 1–2 drops of Tizin® Xylo (0.05% solution) in each nostril up to 3 times daily; children aged 6 to 12 years should receive 2–3 drops (0.05% solution) in each nostril up to 3 times daily.

Adults and children aged 12 years and older should receive 2–3 drops of Tizin® Xylo (0.1% solution) in each nostril up to 3 times daily as needed.

Method of Administration

To administer Tizin® Xylo nasal drops, 0.05% and 0.1% solutions, slightly tilt the head backward. Do not release the rubber bulb until after removing the pipette from the nose to prevent nasal secretions from entering the bottle. Wipe the dosing pipette after each use.

Treatment Duration

Tizin® Xylo should not be used for longer than 7 consecutive days, except when recommended by a physician.

Repeated use should only be initiated after an interval of several days and consultation with a physician. The treatment duration for children should be determined individually by a physician.

In cases of chronic rhinitis, Tizin® Xylo should be used only under medical supervision due to the risk of developing nasal mucosal atrophy.

Children

Tizin® Xylo 0.05% is indicated for the treatment of children aged 4 to 12 years.

Tizin® Xylo 0.05% is not recommended for children under 4 years of age.

Tizin® Xylo 0.1% is indicated for the treatment of adults and children aged 12 years and older.

Overdose

Symptoms

With nasal administration, systemic effects are unlikely due to local vasoconstriction, which reduces absorption. However, in the case of systemic absorption, xylometazoline, as an α2-adrenergic agonist, may exert effects similar to clonidine: transient increase in arterial pressure followed by prolonged hypotension and sedation.

Symptoms of intoxication with 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, bradycardia, cardiac arrest, arterial hypertension, shock-like hypotension, pulmonary edema, respiratory disturbances, and apnea.

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

Treatment

Severe overdose requires hospital treatment. Since xylometazoline hydrochloride is rapidly absorbed, activated charcoal (adsorbent), sodium sulfate (laxative), or gastric lavage (in cases of higher doses) should be administered immediately. Hypotension can be managed with non-selective alpha-blockers. Vasoconstrictors are contraindicated. If necessary, antipyretics and anticonvulsants should be used, along with artificial oxygen ventilation.

Adverse Reactions

Undesirable effects were categorized by frequency 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;
Frequency not known: cannot be estimated from available data.

Respiratory, thoracic and mediastinal disorders

Tyzine® Xylo may cause temporary mild signs of irritation (burning sensation or dryness of the nasal mucosa), particularly in sensitive patients, as well as nasal and throat pain.

Common: Reactive hyperemia.
Uncommon: Nasal bleeding, sneezing, epistaxis.

Prolonged or frequent use of higher doses of xylometazoline hydrochloride may lead to burning, stinging, itching, sensitivity, dryness, or irritation of the nasal mucosa, as well as rebound congestion and drug-induced rhinitis. This effect may occur as early as 7 days after treatment initiation, and with prolonged use may result in irreversible damage to the nasal mucosa with crust formation (dry rhinitis).

Occasionally, nausea, headache, and transient visual disturbances may occur.

Rebound nasal congestion after discontinuation of treatment, particularly following prolonged use of xylometazoline, has been reported.

Nervous system disorders

Rare: Headache, dizziness, rebound effect, insomnia, increased fatigue.
Very rare: Hallucinations, predominantly in children.

Cardiovascular system disorders

Uncommon: Systemic sympathomimetic effects (tachycardia, accelerated pulse, increased blood pressure).
Very rare: Arrhythmia.

Musculoskeletal and connective tissue disorders

Very rare: Seizures, particularly in children.

Immune system disorders

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

Post-marketing data

The following adverse effects have been reported spontaneously: burning sensation of the mucosa, nasal dryness; prolonged treatment may lead to rebound effect.

Shelf life. 3 years.

Shelf life of the product after first opening of the bottle – 24 weeks.

Storage conditions.

Store at temperatures not exceeding 25°C, in a place inaccessible to children.

Do not freeze.

Packaging.

Nasal drops, solution 0.05% and 0.1%, 10 ml in bottles; 1 bottle per cardboard pack.

Supply category. Over-the-counter.

Manufacturer. DELPHARM ORLEANS / DELPHARM ORLEANS.

Manufacturer's address

5 avenue de Concyr, ORLEANS CEDEX 2, 45071, France / 5 avenue de Concyr, ORLEANS CEDEX 2, 45071, France.

Marketing Authorization Holder.

McNeil Products Limited.

Address of Marketing Authorization Holder.

50-100 Holmers Farm Way, High Wycombe, HP12 4EG, England / 50-100 Holmers Farm Way, High Wycombe, HP12 4EG, England.

Representative of Marketing Authorization Holder. Johnson & Johnson Ukraine LLC.

Address of Representative.

32/2 Ostrizkykh Knyaziv St., Kyiv, 01010, Ukraine.

+38 (044) 498 0888
+38 (044) 498 7392