2010
DOI: 10.1111/j.1472-8206.2009.00805.x
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Alpha‐adrenoceptor agonistic activity of oxymetazoline and xylometazoline

Abstract: Oxymetazoline and xylometazoline are both used as nasal mucosa decongesting α-adrenoceptor agonists during a common cold. However, it is largely unknown which of the six α-adrenoceptor subtypes are actually present in human nasal mucosa, which are activated by the two alpha-adrenoceptor agonists and to what extent. Therefore, mRNA expression in human nasal mucosa of the six α-adrenoceptor subtypes was studied. Furthermore, the affinity and potency of the imidazolines oxymetazoline and xylometazoline at these α… Show more

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Cited by 59 publications
(60 citation statements)
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“…Xylometazoline hydrochloride (HCl) (2-[4-(1,1-dimethylethyl)-2,6-dimethylbenzyl]-4,5-dihydro-1H-imidazole HCl) is a well-established nasal decongestant that belongs to the pharmacotherapeutic group of sympathomimetic drugs and acts selectively on α-adrenergic receptors (alpha-adrenergic agonist). 1 Xylometazoline HCl is applied topically to relieve nasal congestion associated with acute or chronic rhinitis, common cold, sinusitis, hay fever or other allergies. It causes vasoconstriction in the nasal submucosa, which is manifested as a collapse of the venous sinusoids.…”
Section: Introductionmentioning
confidence: 99%
“…Xylometazoline hydrochloride (HCl) (2-[4-(1,1-dimethylethyl)-2,6-dimethylbenzyl]-4,5-dihydro-1H-imidazole HCl) is a well-established nasal decongestant that belongs to the pharmacotherapeutic group of sympathomimetic drugs and acts selectively on α-adrenergic receptors (alpha-adrenergic agonist). 1 Xylometazoline HCl is applied topically to relieve nasal congestion associated with acute or chronic rhinitis, common cold, sinusitis, hay fever or other allergies. It causes vasoconstriction in the nasal submucosa, which is manifested as a collapse of the venous sinusoids.…”
Section: Introductionmentioning
confidence: 99%
“…Forty patients with a confirmed clinical history of persistent moderate-to-severe allergic rhinitis (17 men and 23 women; age 35 years [18Ϭ49 years], mean [range]) were enrolled in the study. The sample size of 20 patients per group was calculated based on the 20% effect size, with a power of 80% and a level of significance of 0.05 (2-tailed) by using as proxy our previous work, 26 in which we measured nasal resistance for our sample size calculation. To be included in the trial, patients needed to have active moderately severe-to-severe persistent symptoms of allergic rhinitis with prominent congestion.…”
Section: Methodsmentioning
confidence: 99%
“…The pharmacologic agent that was chosen was oxymetazoline nasal spray, a potent agonist of ␣ 1 --and ␣ 2 -adrenergic receptors with an almost instantaneous onset of action and proven benefits in the management of nasal congestion. 26,27…”
mentioning
confidence: 99%
“…Oxymetazoline is an α‐adrenergic agonist that is commonly used as a topical sympathomimetic agent in over‐the‐counter decongestant sprays as well as a topical hemostatic agent in the operating room during ear, nose, and throat surgery. Its topical vasoconstrictive actions on blood vessels define its clinical utility as both a decongestant and a topical hemostatic agent . Given these effects, it is commonly used by otolaryngologists to produce vasoconstriction, thereby limiting blood loss and improving surgical field visualization during functional endoscopic sinus surgery (FESS), turbinate surgery, and adenoidectomy .…”
Section: Introductionmentioning
confidence: 99%
“…Its topical vasoconstrictive actions on blood vessels define its clinical utility as both a decongestant and a topical hemostatic agent. 1 Given these effects, it is commonly used by otolaryngologists to produce vasoconstriction, thereby limiting blood loss and improving surgical field visualization during functional endoscopic sinus surgery (FESS), turbinate surgery, and adenoidectomy. 2 Although there is generally limited vascular absorption when oxymetazoline is administered in larger doses, or when there is increased uptake due to vascular injury, this drug can lead to systemic hemodynamic effects including systemic and pulmonary hypertension.…”
Section: Introductionmentioning
confidence: 99%