Oxymetazoline, sold under the brand name Afrin among others, is a topical decongestant and vasoconstrictor medication. It is available over-the-counter as a nasal spray to treat nasal congestion and nosebleeds, as eyedrops to treat eye redness due to minor irritation, and (in the United States) as a prescription topical cream to treat persistent facial redness due to rosacea in adults. Its effects begin within minutes and last for up to six hours. Intranasal use for longer than three days may cause congestion to recur or worsen, resulting in physical dependence. It is estimated that 700,000 people in Norway could be dependent on nasal sprays.[1]
Oxymetazoline is a derivative of imidazole.[2] It was developed from xylometazoline at Merck by Wolfgang Fruhstorfer and Helmut Müller-Calgan in 1961.[3] A direct sympathomimetic, oxymetazoline binds to and activates α1 adrenergic receptors and α2 adrenergic receptors, most notably.[2] One study classified it in the following order: α(2A) > α(1A) ≥ α(2B) > α(1D) ≥ α(2C) >> α(1B), but this is not universally agreed upon.[4] There is little consistency across the (relatively large) number of in-vitro studies with respect to binding affinity/selectivity.
Another study classified it with selectivity ratios in alpha 2 adrenergic receptors of 200 for a2A vs a2B, 7.1 a2A vs a2C, and 28.2 a2B vs a2C.[5] Making it a highly selective a2A agonist.
In 2021, it was the 292nd most commonly prescribed medication in the United States, with more than 600,000 prescriptions.[6][7]
^Rhea C (5 March 2024). "In Norway, 700,000 people are dependent on nasal sprays". Newsendip.
^ ab"Oxymetazoline". PubChem. Bethesda (MD): National Library of Medicine (US), National Center for Biotechnology Information. CID 4636.
^DE 1117588, Fruhstorfer W, Müller-Calgan H, "2-(2,6-dimethyl-3-hydroxy-4-tert-butyl-benzyl)-2-imidazoline,and acid addition salts thereof,and process for their manufacture", issued 23 November 1961, assigned to E Merck AG.
^Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, et al. (December 2010). "Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline". Fundamental & Clinical Pharmacology. 24 (6): 729–739. doi:10.1111/j.1472-8206.2009.00805.x. PMID 20030735. S2CID 25064699.
^Proudman RG, Akinaga J, Baker JG (October 2022). "The signaling and selectivity of α-adrenoceptor agonists for the human α2A, α2B and α2C-adrenoceptors and comparison with human α1 and β-adrenoceptors". Pharmacology Research & Perspectives. 10 (5): e01003. doi:10.1002/prp2.1003. PMC 9471048. PMID 36101495.
^"The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
^"Oxymetazoline - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
Oxymetazoline, sold under the brand name Afrin among others, is a topical decongestant and vasoconstrictor medication. It is available over-the-counter...
these areas. Decongestant nasal sprays and eye drops often contain oxymetazoline and are used for topical decongestion. Pseudoephedrine acts indirectly...
suspected to be brought on by extended use of topical decongestants (e.g., oxymetazoline, phenylephrine, xylometazoline, and naphazoline nasal sprays) and certain...
or "Otriven" (Germany). A product marketed as "Otrivin Oxy" contains oxymetazoline instead of xylometazoline. Other product names used include Antazol...
chewing tobacco or gum Imidazolines such as clonidine, naphazoline, oxymetazoline and tetrahydrozoline Antipsychotics, including risperidone, haloperidol...
support this interpretation. Use of intranasal decongestants (such as oxymetazoline) for more than three days leads to tachyphylaxis of response and rebound...
useful in reversing this condition. Topical nasal decongestants include: Oxymetazoline Phenylephrine Xylometazoline Combination use of two medications as nasal...
Nasal Spray is a nasal decongestant, the active ingredient of which is oxymetazoline hydrochloride 0.05%. Dristan Cold Multi-Symptom Tablets contain three...
the stomach and cause vomiting. Vasoconstrictive medications such as oxymetazoline (Afrin) or phenylephrine are widely available over the counter for treatment...
eye dryness. These formulations use active ingredients ranging from oxymetazoline to naphazoline. Some Visine products cater specifically to contact lens...
nocturnal symptoms, intranasal corticosteroids can be combined with nightly oxymetazoline, an adrenergic alpha-agonist, or an antihistamine nasal spray without...
the warning against unsupervised use with hypertension. This includes oxymetazoline (e.g., Afrin), phenylephrine (e.g., Neo-Synephrine), naphazoline (e...
airways. Other causes are side effects of topical decongestants such as oxymetazoline and phenylephrine. Both of these medications activate alpha-1 adrenergic...
congestion brought on by extended use of topical decongestants (e.g., oxymetazoline, phenylephrine, xylometazoline, and naphazoline nasal sprays) Sinusitis...
all drugs that produce physical dependence are addictive drugs, e.g., oxymetazoline. Many professionals, self-help groups, and businesses specialize in...
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