Xylometazoline

ATC CodeR01AA07, R01AB06, S01GA03
CAS number526-36-3
PUB number5709
Drugbank IDDB06694
Empirical formulaC16H24N2
Molar mass (g·mol−1)244,38
Physical statesolid
Melting point (°C)131–133

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, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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