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Oxymetazoline and xylometazoline are alpha-adrenoceptor agonists used topically as nasal decongestants [ ]. They have higher affinities for most α-adrenoceptor subtypes than adrenaline and noradrenaline. Oxymetazoline has a significantly higher affinity for α 1A receptors than xylometazoline but a lower affinity for α 2B receptors.
During a period of 32 months, 101 cases of xylometazoline exposure were observed in children aged under 6 years, among whom follow-up information was available in 63; there were no severe symptoms after exposure to doses of xylometazoline below 0.4 mg/kg [ ].
A 56-year-old man developed a cardiomyopathy after having used a xylometazoline nasal spray 3–5 times a day for 17 years; he stopped using xylometazoline, and 6 months later his cardiac function was completely normal [ ].
Nasal irritation, with dryness of the mouth and throat, can occur; a rebound effect on the nasal mucosa was found in some 5% of cases studied [ ]. See also Drug tolerance below.
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