Side effects include trouble sleeping, irritation of the nose, nausea, nosebleed (3%), period pain (10%) and headache (3%).[5][3][4] Long term use (> 10 days) is not recommended due to arhinitis medicamentosa when stopped.[5][6] Use is not recommended duringpregnancy.[3] Xylometazoline is in thedecongestant andalpha-adrenergic agonist families of medication.[6][7]
One study classified it with selectivity ratios in alpha 2 adrenergic receptors of 151 for a2A vs a2B, 4.5 a2A vs a2C, and 33.9 a2B vs a2C. Making it a highly selective a2A agonist.[8]
Xylometazoline works by stimulatingadrenergic receptors on thelamina propria ofblood vessels in the nose. The decongestant effect is due toconstriction of large veins in the nose which swell up during the inflammation of any infection or allergy of the nose. The smaller arteries are also constricted and this causes the colour of the nasalepithelium to be visibly paler after dosage.
Xylometazoline is animidazole derivative which is designed to mimic the molecular shape ofadrenaline. It binds toα1 andα2 adrenergic receptors[12] in the nasal mucosa. Due to itssympathomimetic effects, it should not be used by people with highblood pressure, or otherheart problems.
Extended usage of xylometazoline can result in decreased effectiveness or a buildup of tolerance against the drug.[13] The number of receptors decreases, and when the administration of the drug is ceased, chronic congestion can occur; this is calledrhinitis medicamentosa, commonly referred to as rebound congestion. Moreover, long-term overdosing can cause degenerative changes in nasalmucous membranes that pose another health problem.[citation needed]
In 2021, a US FDA Drug Safety Communication stated that, while a US Consumer Product Safety Commission (CPSC) proposed rule regarding child-resistant packaging covered products containing xylometazoline, no such products were marketed in the United States at that time.[14]
The most common name for over-the-counter products containing xylometazoline internationally is "Otrivin" (used in Australia,[15] Canada, Estonia, Finland, Greece, Hungary, India,[16] Israel, Jordan, Netherlands, New Zealand, Norway, Poland, South Africa, Egypt, Sweden, Vietnam, Hong Kong), "Otrivine" (United Kingdom, Ireland, Turkey, Belgium), or "Otriven" (Germany). A product marketed as "Otrivin Oxy" containsoxymetazoline instead of xylometazoline.
Other product names used include Antazol (Square, inBangladesh), Xylomet (Opsonin,Bangladesh), Cirovin, Klarigen (in Denmark), Nasolin (in Finland), Neo-Rinoleina, Novorin, Olynth, Otrinoz, Galazolin (Russia, Ukraine, Belarus), Nasomist-X, Otrix, Rhinoset, Zenfresh, Naphthyzinium, Xymelyn (inLatvia), Sinutab Nasal Spray, Snup akut, Sudafed, Xylo-COMOD, Xylolin (in the United Arab Emirates), Xylovit, Olynth (in Serbia, the Czech Republic, Lithuania and Slovakia), Meralys (inCroatia) Xynosine (inPakistan,Afghanistan,Kyrgyzstan andKazakhstan), Xymelin, Zymelin, Xylostar, Xylorin (in Poland), Nasobol, Xylo Mepha and others (Switzerland), Decozal (in Jordan), Nasic, Orinox (Romania), Narhimed, Actifed (Italy), nasa Rhinathiol (Belgium), Zolinol, Nasorhinathiol, and Vibrocil (Portugal).
^abcBritish national formulary : BNF 69 (69 ed.). British Medical Association. 2015. p. 786.ISBN978-0-85711-156-2.
^abEccles R, Martensson K, Chen SC (April 2010). "Effects of intranasal xylometazoline, alone or in combination with ipratropium, in patients with common cold".Current Medical Research and Opinion.26 (4):889–899.doi:10.1185/03007991003648015.PMID20151787.S2CID34728458.
^US patent 2868802A, Hüni, Albrecht, "2-(γ-TERT-BUTYL-O,O'-DIMETHYL-PHENYL-METHYL)-IMIDAZOLINE AND SALTS", issued 13 January 1959, assigned to Ciba Pharmaceutical Products Inc., Summit, N. J.
^World Health Organization (2023).The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization.hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
^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.
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