Oxymetazoline is a derivative ofimidazole.[1] It was developed fromxylometazoline atMerck by Wolfgang Fruhstorfer and Helmut Müller-Calgan in 1961.[2] A directsympathomimetic, oxymetazoline binds to and activatesα1 adrenergic receptors andα2 adrenergic receptors, most notably.[1] 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.[3]
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.[4]
In 2022, it was the 305th most commonly prescribed medication in the United States, with more than 300,000 prescriptions.[5]
Due to its vasoconstricting properties, oxymetazoline is also used to treatnose bleeds[7][8] and eye redness due to minor irritation (marketed asVisine L.R. in the form of eye drops).[citation needed]
In the United States, oxymetazoline 1% cream was approved by the Food and Drug Administration (FDA) in January 2017 for topical treatment of persistent facial erythema (redness) associated with rosacea in adults.[9][10]
In July 2020, oxymetazoline received approval by the FDA for the treatment of acquiredblepharoptosis (drooping eyelid).[11][12]
Rebound congestion, orrhinitis medicamentosa, may occur. A 2006 review of the pathology of rhinitis medicamentosa concluded that use of oxymetazoline for more than three days may result in rhinitis medicamentosa and recommended limiting use to three days.[13]
Although Oxymetazoline can be used for treatment ofnosebleeds, it can also cause them under certain conditions, especially when nasal passages are dry. Oxymetazoline is a nasal decongestant that constricts blood vessels in the nasal mucosa, thereby reducing swelling and improving airflow. However, its use can lead to dryness and irritation of the nasal lining, which can increase the likelihood of nosebleeds.[14]
Novartis recommended a five day maximum usage period, rather than three days, in a submission to theTherapeutic Goods Administration. Novartis suggested that "The justification [for 3 days] was not based on evidence" and cited an extensive body of evidence, and noting a range of recommended periods from five to ten days, which coincides with the typical duration of the common cold.[15]
There is no specific antidote for oxymetazoline, although its pharmacological effects may be reversed by an adrenergic antagonists such asphentolamine.[medical citation needed]
Oxymetazoline is asympathomimetic that selectively agonizesα1 and, partially,α2adrenergic receptors.[16] Since vascular beds widely express α1 receptors, the action of oxymetazoline results invasoconstriction. In addition, the local application of the drug also results in vasoconstriction due to its action on endothelial postsynaptic α2 receptors; systemic application of α2 agonists, in contrast, causesvasodilation because of centrally-mediated inhibition of sympathetic tone via presynaptic α2 receptors.[17] Vasoconstriction of vessels results in relief of nasal congestion in two ways: first, it increases the diameter of the airway lumen; second, it reduces fluid exudation from postcapillary venules.[18] It can reduce nasal airway resistance (NAR) up to 35.7% and reduce nasal mucosal blood flow up to 50%.[19]
When used for treating acquired blepharoptosis, oxymetazoline is believed to work by stimulating the α1 and α2 adrenergic receptors of Müller's muscle, which helps to lift the eyelid and improve vision.[12]
Since imidazolines are sympathomimetic agents, their primary effects appear on α adrenergic receptors, with little if any effect onβ adrenergic receptors.[20] Like other imidazolines, Oxymetazoline is readily absorbed orally.[20] Effects on α receptors from systemically absorbed oxymetazoline hydrochloride may persist for up to 7 hours after a single dose.[21] The elimination half-life in humans is 5–8 hours.[22] It is excreted unchanged both by the kidneys (30%) and in feces (10%).[21]
The oxymetazoline brand Afrin was first sold as a prescription medication in 1966. After finding substantial early success as a prescription medication, it became available as an over-the-counter drug in 1975.Schering-Plough did not engage in heavy advertising until 1986.[23]
Brand names for Oxymetazoline include Afrin, ClariClear,Dristan, Drixine, Drixoral, Nasivin, Nasivion, Nezeril, Nostrilla, Logicin, Vicks Sinex,Visine L.R., Sudafed OM, Otrivin, Oxy, SinuFrin, Vicks Sinex Severe (Spray), and Mucinex Sinus-Max.[citation needed] A topical cream formulation is sold under the brand name Rhofade.[24] Oxymetazoline ophthalmic solution for the treatment of acquired blepharoptosis is marketed as Upneeq.[11][12]
^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.PMID20030735.S2CID25064699.
^"Oxymetazoline".Lexi-Comp: Merck Manual Professional. Merck.com. Retrieved15 April 2013.
^Katz RI, Hovagim AR, Finkelstein HS, Grinberg Y, Boccio RV, Poppers PJ (1990). "A comparison of cocaine, lidocaine with epinephrine, and oxymetazoline for prevention of epistaxis on nasotracheal intubation".Journal of Clinical Anesthesia.2 (1):16–20.doi:10.1016/0952-8180(90)90043-3.PMID2310576.
^Krempl GA, Noorily AD (September 1995). "Use of oxymetazoline in the management of epistaxis".The Annals of Otology, Rhinology, and Laryngology.104 (9 Pt 1):704–706.doi:10.1177/000348949510400906.PMID7661519.S2CID37579139.
^Westfall TC, Westfall DP."Chapter 6. Neurotransmission: The Autonomic and Somatic Motor Nervous Systems". In Brunton LL, Lazo JS, Parker KL (eds.).Goodman & Gilman's The Pharmacological Basis of Therapeutics (11th ed.). Archived fromthe original on 30 September 2011. Retrieved24 January 2015 – via AccessMedicine.Anatomy and General Functions of the Autonomic and Somatic Motor Nervous Systems.
^Biaggioni I, Robertson D. "Chapter 9. Adrenoceptor Agonists & Sympathomimetic Drugs". In Katzung BG (ed.).Basic & Clinical Pharmacology (11th ed.). Archived fromthe original on 30 September 2011. Retrieved30 November 2011.
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