Xylometazoline HCl

Xylometazoline is an α-adrenoceptor agonist commonly used as nasal decongestant, exhibits highest potency at α_2B-adrenoceptor subtype with EC50 of 99 μM. Phase 4.

Topical glucocorticoid reduces the topical decongestant-induced histologic changes in an animal model nasal mucosa.[Pubmed:22374848]

Laryngoscope. 2012 Apr;122(4):741-6.

OBJECTIVES/HYPOTHESIS: To investigate the histologic consequences of simultaneous nasal glucocorticosteroid and Xylometazoline HCl administration in the rabbit nasal mucosa. STUDY DESIGN: Prospective randomized study. METHODS: Twenty New Zealand male rabbits were randomly placed into three groups: group I, control (n = 6); group II, Xylometazoline HCl (n = 8); or group III, Xylometazoline HCl-fluticasone furoate (n = 6). Group I received no treatment. Groups II and III received two intranasal puffs of Xylometazoline HCl 0.5 mg/mL twice daily or two puffs of Xylometazoline HCl 0.5 mg/mL twice daily plus one puff of 27.5 mug fluticasone furoate twice daily to each nostril (110 mug), respectively. At the end of 3 weeks, the rabbits were sacrificed. The mucosa of the nasal cavities was excised. Specimen sections (5 mum) were stained with hematoxylin and eosin, mucicarmine, and Gomori one-step trichrome and were examined under a light microscope. The presence of edema, congestion, inflammatory cell infiltration, nasociliary loss, epithelial and nerve-ending degeneration, and goblet cell increase were evaluated semiquantitatively (grades 0-3). RESULTS: Statistically significant differences were detected between groups II and III in terms of edema, congestion, inflammatory cell infiltration, nasociliary loss, and epithelial degeneration (P = .006, P = .049, P = .015, P = .014, and P = .049, respectively). Nerve-ending degeneration, goblet cell increase, and quantitative goblet and neutrophil cell counts did not yield statistically significant differences between groups II and III (P = .137, P = .580, P = .770, and P = .616, respectively). CONCLUSIONS: The combined simultaneous intranasal administration of Xylometazoline HCl and fluticasone furoate appears to be beneficial in minimizing the long-term usage-associated congestion, edema, inflammatory cell infiltration, epithelial degeneration, and nasociliary loss in the rabbit model nasal mucosa.

Correlation between the sensitivity of the ciliary beat frequency of human adenoid tissue and chicken embryo tracheas for some drugs.[Pubmed:6180466]

Rhinology. 1982 Jun;20(2):81-7.

The effects of benzalkonium chloride, chlorbutol,xylometazoline and naphazoline on the ciliary beat frequency of human adenoids and chicken embryo tracheas have been determined and compared. Chlorbutol 0.5% appeared to arrest ciliary motion in both tissues within 5 minutes. Rinsing with Locke Ringer solution (LR) restored the ciliary motion almost completely in both cases. Benzalkonium chloride 0.006% +EDTA 0.1% decreased the ciliary beat frequency 35% for the human tissues and 50% for the chicken tissues after a contact of 20 minutes. In both cases the frequency hardly changed after rinsing with LR. Naphazoline nitrate 0.1% and Xylometazoline HCl 0.05% have reversible effects on the ciliary beat frequency of both human adenoids and chicken embryo tracheas. Cilia of human adenoids appeared to be more sensitive for xylometazoline than for naphazoline; whereas cilia of chicken embryo tracheas were more affected by naphazoline than by xylometazoline. The results with human adenoids and chicken embryo tracheas show a correlation (correlation coeff. = 0.82, p less than 0.005). In the initial response the differences in sensitivity to preservatives and drugs were in many cases statistically significant, but the final effects were similar.