Xylometazoline

Xylometazoline
ATC Code R01AA07, R01AB06, S01GA03
Formula C16H24N2
Molar Mass (g·mol−1) 244,38
Physical State solid
Melting Point (°C) 131–133
CAS Number 526-36-3
PUB Number 5709
Drugbank ID DB06694
Solubility practically insoluble in water

Basics

Xylometazoline is a medication used to reduce the symptoms of nasal congestion, allergic rhinitis, and sinusitis. It belongs to the group of α1-adrenoceptor agonists. It is used directly in the nose as a spray or drops. Its use is not recommended for more than seven days at a time.

Pharmacology

Pharmacodynamics

Xylometazoline is an imidazole derivative designed to mimic the molecular shape of epinephrine. This drug acts by stimulating adrenergic receptors (α1-adrenoceptors) on the lamina propria of blood vessels in the nose. The decongestant effect is due to constriction of the large veins in the nose, which swell during inflammation of an infection or allergy of the nose. The smaller arteries are also constricted, causing the color of the nasal epithelium to become visibly paler after dosing.
Aufgrund seiner sympathomimetischen Wirkung sollte es nicht von Personen mit Bluthochdruck oder anderen Herzproblemen verwendet werden.

Toxicity

Side effects

Side effects include sleep disturbance, nasal irritation, nausea, nosebleeds (3%), period pain (10%), and headache (3%).

Long-term use (>10days) is not recommended due to rhinitis medicamentosa on discontinuation.

Use is not recommended during pregnancy.

Toxicological data

LD50 (rat, oral, hydrochloride): 230 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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