Xylometazoline, also spelled xylomethazoline, is a medication used to reduce symptoms of
nasal congestion,
allergic rhinitis, and
sinusitis.[2] Use is not recommended for more than seven days.[3] Use is also not recommended in those less than three months of age and some say not less than 6 years of age.[3][4] It is used directly in the
nose as a spray or drops.[3]
Side effects include trouble sleeping, irritation of the nose, nausea, nosebleed (3%), period pain (10%) and headache (3%).[5][2][3] Long term use (> 10 days) is not recommended due to a
rhinitis medicamentosa when stopped.[5][6] Use is not recommended during
pregnancy.[2] Xylometazoline is in the
decongestant and
alpha-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]
The drug works by stimulating
adrenergic receptors on the
lamina propria of
blood vessels in the nose. The decongestant effect is due to
constriction 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 nasal
epithelium to be visibly paler after dosage.
Xylometazoline is an
imidazole derivative which is designed to mimic the molecular shape of
adrenaline. It binds to
α1 and
α2 adrenergic receptors[12] in the nasal mucosa. Due to its
sympathomimetic effects, it should not be used by people with high
blood pressure, or other
heart 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 called
rhinitis medicamentosa, commonly referred to as rebound congestion. Moreover, long-term overdosing can cause degenerative changes in nasal
mucous membranes that pose another health problem.[citation needed]
Society and culture
Brand names
The most common name for over-the-counter products containing xylometazoline internationally is "Otrivin" (used in Australia,[14] Canada, Estonia, Finland, Greece, Hungary, India,[15] Israel, Jordan, Netherlands, New Zealand, Norway, Poland, South Africa, Sweden, Vietnam, Hong Kong), "Otrivine" (United Kingdom, Ireland, Turkey, Belgium), or "Otriven" (Germany). A product marketed as "Otrivin Oxy" contains
oxymetazoline instead of xylometazoline.
Other product names used include Antazol (Square, in
Bangladesh), Xylomet (Opsonin,
Bangladesh), Cirovin, Klarigen (in Denmark), Nasolin, Neo-Rinoleina, Novorin, Olynth, Otrinoz, Galazolin[16] (Russia, Ukraine, Belarus), Nasomist-X, Otrix, Rhinoset, Zenfresh, Naphthyzinium, Xymelyn (in
Latvia), Sinutab Nasal Spray, Snup akut, Sudafed, Xylo-COMOD, Xylolin (in the United Abar Emirates), Xylovit, Olynth (in Serbia, the Czech Republic and Slovakia), Meralys (in
Croatia) Xynosine (in
Pakistan,
Afghanistan,
Kyrgyzstan and
Kazakhstan), Xymelin, Zymelin, Xylostar, Xylorin (in Poland), Nasobol, Xylo Mepha and others (Switzerland), Decozal (in Jordan), Nasic, Orinox (Romania), Narhimed (Italy), nasa Rhinathiol (Belgium) and Zolinol,[17] Nasorhinathiol[18] and Vibrocil[19] (Portugal].
As of 2021, a number of consumer products containing xylometazoline are marketed in the United States.[20]
Formulations
The standard adult solution strength is 0.1%
w/v xylometazoline (or 1 mg per 1 mL solution), and the dose for children under 12 is usually 0.05% (0.5 mg/mL).[21]
^{{Fulga, Ana, Andrei Zenovia, Doriana Cristea Ene, Constantin Stan, Dorel Firescu, and Iuliu Fulga. 2021. “Addiction to Nasal Decongestants Based on Α-Adrenoceptor Agonists Case Series and Literature Review: Array”. EuroEconomica 40 (2).
https://dj.univ-danubius.ro/index.php/EE/article/view/1455}}
^
abcdeBritish national formulary : BNF 69 (69 ed.). British Medical Association. 2015. p. 786.
ISBN978-0-85711-156-2.
^
abWorld Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization.
hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
^
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 1959-01-13, assigned to Ciba Pharmaceutical Products Inc., Summit, N. J.
^World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization.
hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
^Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bönisch H (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.