Ксилен актив Uses, Dosage, Side Effects and more

Ксилен актив is a sympathomimetic agent with marked alphaadrenergic activity, and is intended for use in the nose. It constricts the nasal blood vessels, thereby decongesting the mucosa of the nose and neighboring regions of the pharynx. This enables patients suffering from colds to breathe more easily through the nose. The effect of Ксилен актив begins within a few minutes and persists for several hours. Ксилен актив is generally well tolerated and does not impair the function of ciliated epithelium. Systemic absorption may occur following nasal application of Ксилен актив.

Ксилен актив is a sympathomimetic agent that causes vasoconstriction of the nasal mucosa. In one study comprising subjects with nasal congestion associated with the common cold, the median time of onset of subjective relief of nasal congestion was about 1.7 minutes and the time of subjective peak relief of nasal congestion was 30 minutes. Previous studies reported rebound swelling, rebound nasal congestion, rhinitis medicamentosa, and shorter duration of decongestant effect from the long-term use of xylometazoline in healthy volunteers, suggesting that the drug is most effective if used temporarily.

An early in vitro study demonstrated xylometazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that xylometazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation.

Attribute	Details
Trade Name	Ксилен актив
Generic	Xylometazoline
Xylometazoline Other Names	Xylometazoline, Xylometazolinum, Xylomethazoline
Type
Formula	C₁₆H₂₄N₂
Weight	Average: 244.3752 Monoisotopic: 244.193948778
Protein binding	No information is available on xylometazoline pharmacokinetics.
Groups	Approved, Investigational
Therapeutic Class	Nasal Anti-histamine preparations
Manufacturer
Available Country	Russia
Last Updated:	January 7, 2025 at 1:49 am

Uses

For the symptomatic relief of nasal congestion, perennial allergic rhinitis (including hay fever), sinusitis.

Ксилен актив is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Nasal Congestion, Seasonal Allergic Rhinitis

How Ксилен актив works

Nasal congestion is caused by various etiologies, such as rhinosinusitis and allergic or non-allergic rhinitis, leading to congestion of the venous sinusoids lining the nasal mucosa. Activation of α-adrenergic receptors leads to vasoconstriction of the blood vessels of the nasal mucosa and resumption of nasal airflow. As the most abundantly expressed in the human nasal mucosa, α_1A- and α_2B-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Ксилен актив is a more selective agonist at α_2B-adrenoceptors, with affinity at α_1A-, α_2A-, α_2C-, α_1B-, and α_1D-adrenoceptors. Ксилен актив decreases nasal resistance during inspiration and expiration and increases the volume of nasal airflow. Compared to oxymetazoline, another imidazoline nasal decongestant, xylometazoline had a slightly faster onset of action although they had a similar duration of action. In one study, subjects with nasal congestion reported relief of earache and sore throat in addition to nasal decongestion: it is speculated that oxymetazoline mediates this effect by causing vasoconstriction of the nasal mucosa that contains the venous sinuses and nasal decongestion allows breathing through the nose, providing relief from sore throat caused by mouth breathing that dries and irritates the throat.

Dosage

Adults: 2 or 3 drops of Ксилен актив Adult formula (0.1%) two to three times daily. This adult formula should not be used for children under the age of 12 years.Children under 12 years: 1 or 2 drops of the Ксилен актив children's formula (0.05%) in each nostril once or twice daily. Not to be used in infants less than 3 months.

Side Effects

The following side effects have occasionally been encountered: a burning sensation in the nose and throat, local irritation, nausea, headache, and dryness of the nasal mucosa. Systemic cardiovascular effects have occurred, and this should be kept in mind when giving Ксилен актив to people with cardiovascular disease.

Toxicity

The oral LD₅₀ is 230 mg/kg in rats and 75 mg/kg in mice. The subcutaneous LD₅₀ is 90 mg/kg in rats and 53 mg/kg in mice. The intraperitoneal LD₅₀ is 43 mg/kg in rats.

Ксилен актив poisoning is documented in three pediatric patients who were exposed to a drug concentration 40 times above the adequate dosage for children due to a compounding error: these patients experienced bradypnea and sinus bradycardia with supraventricular extrasystoles and were managed with fluid management.

Precaution

Each Ксилен актив pack should be used by one person only to prevent any cross-infection. Patients are advised not to take decongestants for more than seven consecutive days.

Interaction

No drug interactions have been reported.