Xylazol

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT KSYLAZOL (XYLAZOL)

Composition:

Active substances: xylometazoline, dexpanthenol;

1 ml of solution contains 1 mg of xylometazoline hydrochloride and 50 mg of dexpanthenol;

Excipients: sodium hydrogen phosphate heptahydrate; sodium dihydrogen phosphate monohydrate; benzalkonium chloride; purified water.

Pharmaceutical form. Nasal spray, solution.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group

Anti-edematous and other rhinological preparations for local use. Sympathomimetics, combinations, excluding corticosteroids. ATC code R01A B06.

Pharmacological Properties

Pharmacodynamics

The nasal medicinal product is a combination of an alpha-sympathomimetic agent with a vitamin B5 analogue (pantothenic acid) for local application to the nasal mucosa. Xylometazoline has vasoconstrictor activity, thereby reducing swelling of the mucous membrane. Dexpanthenol is a derivative of pantothenic acid (vitamin B5) that promotes wound healing and protects mucous membranes.

Xylometazoline

Xylometazoline, an imidazole derivative, is an alpha-adrenergic sympathomimetic agent. The onset of action usually occurs within 5–10 minutes, manifested by relief of nasal congestion and improved drainage of secretions, resulting in easier nasal breathing.

Dexpanthenol

Dexpanthenol (D-(+)-pantothenyl alcohol) is an alcohol analogue of pantothenic acid and, through intermediate conversion, exhibits the same biological activity as pantothenic acid. However, only the dextrorotatory D-configuration is biologically active. Pantothenic acid and its salts are water-soluble vitamins that, as coenzyme A, participate in numerous metabolic processes, including supporting the synthesis of proteins and corticoids, as well as antibody production. Coenzyme A also participates in the formation of lipids, which, in particular, constitute the secretion of sebaceous glands and have an important protective function. Furthermore, coenzyme A plays a role in the acetylation of aminosugars, which are the primary building blocks for various mucopolysaccharides.

Dexpanthenol protects epithelial layers and promotes wound healing.

Pharmacokinetics

Xylometazoline

In some cases, intranasal administration of xylometazoline results in significant absorption, leading to systemic effects, for example on the central nervous system (CNS) and the cardiovascular system.

Pharmacokinetic data in humans are lacking.

Dexpanthenol

Dexpanthenol is absorbed through the skin and undergoes enzyme-catalyzed oxidation to pantothenic acid in the body and in skin cells. The vitamin is transported in blood plasma in protein-bound form. As an essential structural component, pantothenic acid combines with coenzyme A and is distributed throughout the body. Detailed studies on metabolism in the skin and mucous membranes are lacking. 60–70% of an orally administered dose is excreted in urine and 30–40% in feces.

Clinical characteristics

Indications

• Nasal congestion in acute rhinitis;
• Promoting healing of the skin around the nasal passages and injuries of the mucous membrane in the nasal cavity;
• Vasomotor rhinitis;
• Impaired nasal breathing after surgical interventions in the nasal cavity.

Contraindications

• Hypersensitivity to the active substance and/or to any of the excipients of the medicinal product;
• Dry inflammation of the nasal mucosa;
• Acute coronary conditions, including cardiac asthma;
• Hyperthyroidism;
• Closed-angle glaucoma;
• Transsphenoidal hypophysectomy and surgical interventions exposing the meninges in medical history;
• Concomitant use with MAO inhibitors and within 2 weeks after discontinuation of their use;
• Children under 6 years of age.

The medicinal product contains benzalkonium chloride; therefore, it should not be used in patients with known hypersensitivity to this substance.

Interaction with other medicinal products and other forms of interaction

Xylometazoline

Concomitant use of the drug with tranylcypromine, monoamine oxidase inhibitors, tricyclic or tetracyclic antidepressants, or β-adrenoblockers may lead, due to the effect of these drugs on the cardiovascular system, to an increase in blood pressure.

Dexpanthenol

No data available.

Special precautions for use

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

• those taking monoamine oxidase inhibitors or other medicinal products capable of increasing blood pressure;
• patients with elevated intraocular pressure, especially with closed-angle glaucoma;
• patients with phaeochromocytoma;
• patients with benign prostatic hyperplasia;
• patients with porphyria.

The medicinal product should be used with caution in patients with cardiovascular disorders, arterial hypertension, diabetes mellitus, thyroid disorders, or prostatic hyperplasia.

Patients with the long QT syndrome who are receiving xylometazoline may be at increased risk of serious ventricular arrhythmias.

Use of the medicinal product during chronic rhinitis is possible only under medical supervision due to the risk of nasal mucosal atrophy.

Decongestant sympathomimetics (including xylometazoline) may, especially with prolonged use or in cases of overdose, lead to reactive hyperemia of the nasal mucosa. This reversible effect leads to nasal passage constriction, forcing the patient to reapply the sympathomimetic. This may result in chronic edema (medication-induced rhinitis), up to atrophy of the nasal cavity mucosa (atrophic rhinitis).

In mild cases, it may be sufficient to discontinue the sympathomimetic in one nostril initially, and then, once symptoms resolve, repeat this with the other nostril, in order to maintain at least partial nasal breathing.

As with other drugs in this class, the medicinal product should be used with caution in patients who exhibit strong reactions to sympathomimetics, such as insomnia, dizziness, tremor, cardiac arrhythmia, or increased blood pressure.

The recommended dose of the medicinal product should not be exceeded, especially when treating children and elderly patients.

The medicinal product contains benzalkonium chloride, which may cause irritation of the nasal mucosa.

The medicinal product is not intended for use in children under 6 years of age. For children under 6 years of age, a different dosage formulation of the drug should be used.

Each package should be used by only one person to avoid the risk of infection.

Use during pregnancy or breastfeeding

Pregnancy

The medicinal product should not be used during pregnancy, as there are insufficient data on the use of xylometazoline for treatment in pregnant women.

Breastfeeding

The medicinal product should not be used during breastfeeding, as it is unknown whether xylometazoline passes into breast milk.

Fertility

No adverse effects on fertility have been observed during treatment with xylometazoline hydrochloride.

Ability to affect reaction speed when driving or operating machinery

When used according to the instructions, the medicinal product is not expected to affect the ability to drive or operate machinery.

Method of Administration and Dosage

Dosing

Adults and children aged 6 years and older

The nasal spray should be sprayed once into each nostril no more than 3 times daily. Dosage depends on individual sensitivity and clinical response.

The medicinal product should not be used for longer than 7 days, except when recommended by a physician.

Regarding duration of use in children, consultation with a physician is always required.

Repeated use should only be initiated after a several-day break and following consultation with a physician. The duration of treatment in children is determined individually by a physician.

In cases of chronic rhinitis, the medicinal product may be used only under medical supervision due to the risk of developing nasal mucosal atrophy.

Method of Administration

The medicinal product is intended for nasal use.

During application, the bottle should be held vertically. The patient should gently inhale through the nose while spraying.

Before use, remove the plastic protective semi-ring from the spray bottle. Remove the protective cap from the spray nozzle. Before first use, prime the nasal spray by pressing the pump several times until a fine, uniform mist is produced. Insert the nozzle into one nostril and press once; repeat for the other nostril. After use, cover the spray nozzle with the protective cap.

Children

The medicinal product should not be used in children under 6 years of age. For children aged 2 to 6 years, Ksilazol-kids should be used.

Overdose

Xylometazoline

Symptoms

Symptoms of intoxication with imidazole derivatives (including xylometazoline) may be clinically unclear, as periods of stimulation may alternate with periods of central nervous system (CNS) and cardiovascular system depression.

Overdose, especially in children, may lead to significant CNS effects, including seizures, coma, bradycardia, apnea, and arterial hypertension, which may progress to arterial hypotension.

Symptoms of CNS stimulation include anxiety, agitation, hallucinations, and convulsions.

Symptoms of CNS depression include hypothermia, lethargy, drowsiness, and coma.

Additional possible symptoms include miosis, mydriasis, sweating, nausea, cyanosis, fever, pallor, tachycardia, bradycardia, cardiac arrest, cardiac arrhythmia, arterial hypertension, shock-like hypotension, pulmonary edema, respiratory depression, apnea, and occasionally impaired consciousness.

Treatment

Severe overdose requires hospital treatment. Since xylometazoline is rapidly absorbed, absorbents (activated charcoal) should be administered immediately, along with laxatives (sodium sulfate), or gastric lavage (in cases of high doses). Reduction of blood pressure can be achieved using non-selective alpha-blockers. Vasoconstrictors are contraindicated. If necessary, antipyretics and anticonvulsants should be administered, as well as artificial oxygen ventilation.

Dexpanthenol

Pantothenic acid and its derivatives, such as dexpanthenol, have very low toxicity. In case of overdose, no therapeutic measures are required.

Side effects

Adverse reactions are classified by organ systems and frequency of occurrence according to MedDRA: very common (≥ 1/10); common (≥ 1/100 – <1/10); uncommon (≥ 1/1000 – <1/100); rare (≥ 1/10,000 – <1/1000); very rare (<1/10,000); not known (frequency cannot be estimated from available data).

Immune system disorders:

uncommon – hypersensitivity reactions (angioedema, rash, pruritus).

Psychiatric disorders:

very rare – anxiety, insomnia, hallucinations (mainly in children).

Nervous system disorders:

very rare – fatigue (drowsiness, sedative effect), headache.

Cardiovascular disorders:

rare – palpitations, tachycardia, arterial hypertension; very rare – arrhythmia.

Respiratory, thoracic and mediastinal disorders:

very rare – after the effect subsides, increased mucosal swelling; epistaxis; not known – burning and dryness of nasal mucosa, sneezing.

Musculoskeletal and connective tissue disorders:

very rare – convulsions (especially in children).

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after marketing authorization is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and patients, or their legal representatives, should report any suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life

3 years.

After opening the bottle, the product can be used for up to 12 weeks.

Storage conditions

Store at temperatures not exceeding 25 °C. Keep out of reach of children.

Packaging

10 ml in a bottle with a spray pump and protective cap; 1 bottle per cardboard box.

Prescription status

Over-the-counter (without prescription).

Manufacturer

UORLД MEDICINE ILAC SAN. VE TIC. A.Ş. /
WORLD MEDICINE ILAC SAN. VE TIC. A.S.

Manufacturer's address and location of operations

15 Temmuz Mahallesi Cami Yolu Caddesi No:50 Gunesli Bagcilar/Istanbul, Turkey /
15 Temmuz Mahallesi Cami Yolu Caddesi No:50 Gunesli Bagcilar/Istanbul, Turkey.