Xylometazoline

Xylometazoline
Clinical data
Pronunciation /ˌzaɪloʊˌmɛtəˈzoʊliːn/
ZY-lo-MET-ə-ZOH-leen
Trade names Otrivin, Otrivine, others
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy
category
  • C
Dependence
liability		 moderate
Routes of
administration		 intranasal (spray or drops)
ATC code
Legal status
Legal status
Pharmacokinetic data
Elimination half-life >10 seconds
Excretion Urinary
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
ECHA InfoCard 100.007.629 Edit this at Wikidata
Chemical and physical data
Formula C16H24N2
Molar mass 244.37516 g/mol
3D model (JSmol)
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Xylometazoline, also spelled xylomethazoline, is a medication which is used to improve symptoms of nasal congestion, allergic rhinitis, and sinusitis.[1] Use is not recommended for more than seven days.[2] Use is also not recommended in those less than three months of age and some say not less than 6 years of age.[2][3] It is used directly in the nose as a spray or drops.[2]

Side effects include trouble sleeping, irritation of the nose, nausea, and headache.[1][2] Long term use is not recommended due to a rhinitis medicamentosa when stopped.[4] Use is not recommended during pregnancy.[1] Xylometazoline is in the decongestant and alpha-adrenergic agonist families of medication.[4][5]

Xylometazoline was patented in 1956 and came into medical use in 1959.[6] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[3] Xylometazoline is available as a generic medication.[2] The wholesale cost in the developing world is about 0.75 USD for a 10 ml bottle.[7] In the United Kingdom that dose costs the NHS about 2.10 pounds.[2]

Mechanism of action

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[8] 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.[9] 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.

Society and culture

Brand names

Xylometazoline is sold under a number of brand names worldwide, including: Antazol (Square, in Bangladesh), Xylomet (Opsonin, Bangladesh) Cirovin, Klarigen (in Denmark), Nasolin, Neo-Rinoleina, Novorin, Olynth, Otrinoz, Otriven, Otrivin (Greece, New Zealand, Norway, Netherlands, Russia, South Africa, Sweden, Vietnam), Otrivine (United Kingdom, Turkey), Nasomist-X, Otrivin (in India)[10], Otrix, Rhinoset, Zenfresh, Naphthyzinium, Xymelyn (in Latvia), Sinutab Nasal Spray, Snup akut, Sudafed, Xylo-COMOD, Xylolin (in UAE), Xylovit, Olynth (in Serbia), Xynosine (in Pakistan, Afghanistan, Kyrgyzstan and Kazakhstan), Xymelin, Zymelin, Xylostar, Xylorin (in Poland), Nasobol, Xylo Mepha and others (Switzerland), Otrivin and Decozal (in Jordan), Nasic (Romania).

No products containing xylometazoline are currently marketed or available in the United States.[11]

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).[12]

See also

References

  1. 1 2 3 "Otrivine Adult Measured Dose Sinusitis Spray - Summary of Product Characteristics (SPC) - (eMC)". www.medicines.org.uk. 13 April 2016. Archived from the original on 29 December 2016. Retrieved 28 December 2016.
  2. 1 2 3 4 5 6 British national formulary : BNF 69 (69 ed.). British Medical Association. 2015. p. 786. ISBN 9780857111562.
  3. 1 2 "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
  4. 1 2 Graf, P (1997). "Rhinitis medicamentosa: aspects of pathophysiology and treatment". Allergy. 52 (40 Suppl): 28–34. doi:10.1111/j.1398-9995.1997.tb04881.x. PMID 9353558.
  5. ↑ "Xylometazoline nasal medical facts from Drugs.com". www.drugs.com. Archived from the original on 29 December 2016. Retrieved 28 December 2016.
  6. ↑ Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 552. ISBN 9783527607495. Archived from the original on 2016-12-29.
  7. ↑ "Xylometazoline". International Drug Price Indicator Guide. Retrieved 8 December 2016.
  8. ↑ Haenisch, B.; Walstab, J.; Herberhold, S.; Bootz, F.; Tschaikin, M.; Ramseger, R.; Bönisch, H. (2009). "Alpha-adrenoceptor Agonistic Activity of Oxymetazoline and Xylometazoline". Fundamental & Clinical Pharmacology. 24 (6): 729–39. doi:10.1111/j.1472-8206.2009.00805.x. PMID 20030735.
  9. ↑ Gold Standard Clinical Pharmacology Archived 2008-05-25 at the Wayback Machine.
  10. ↑ "Otrivin | GSK Consumer Healthcare INDIA". Retrieved 2018-06-17.
  11. ↑ https://www.fda.gov/Drugs/DrugSafety/ucm325257.htm
  12. ↑ "Archived copy". Archived from the original on 2015-02-22. Retrieved 2015-02-22.
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