Oxymetazoline
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| Trade names | Afrin, Ocuclear, Drixine |
| AHFS/Drugs.com | Monograph |
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| Dependence liability |
Moderate |
| Routes of administration |
Intranasal |
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| Pharmacokinetic data | |
| Metabolism | Kidney (30%), fecal (10%) |
| Biological half-life | 5–6 hours |
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| ChEMBL | |
| ECHA InfoCard | 100.014.618 |
| Chemical and physical data | |
| Formula | C16H24N2O |
| Molar mass | 260.375 g·mol−1 |
| 3D model (Jmol) | |
| Melting point | 301.5 °C (574.7 °F) |
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Oxymetazoline is a selective α1 adrenergic receptor agonist and α2 adrenergic receptor partial agonist. It is a topical decongestant, used in the form of oxymetazoline hydrochloride. It was developed from xylometazoline at E. Merck Darmstadt by Fruhstorfer in 1961. Oxymetazoline is generally available as a nasal spray.
Oxymetazoline is available over-the-counter as a topical decongestant in the form of oxymetazoline hydrochloride in nasal sprays such as Afrin, Operil, Dristan, Dimetapp, oxyspray, Facimin, Nasivin, Nostrilla, Sudafed OM, Vicks Sinex, Zicam, SinuFrin, and Mucinex Full Force.
Due to its vasoconstricting properties, oxymetazoline is also used to treat nose bleeds and eye redness due to minor irritation (marketed as Visine L.R. in the form of eye drops).
It is recommended that oxymetazoline not be used for more than three days, as rebound congestion, or rhinitis medicamentosa, may occur. Patients who continue to use oxymetazoline beyond this point may become dependent on the medication to relieve their chronic congestion.
Some studies have found that benzalkonium chloride, a common additive to oxymetazoline nasal sprays, may damage nasal epithelia and exacerbate rhinitis medicamentosa. However, the majority of studies find benzalkonium chloride to be a safe preservative.
The Food and Drug Administration places oxymetazoline in category C, indicating risk to the fetus cannot be ruled out. While it has been shown that a single dose does not significantly alter either maternal or fetal circulation, this subject has not been studied extensively enough to draw reliable conclusions.
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Wikipedia