|Systematic (IUPAC) name|
|Biological half-life||5-6 hours|
|ATC code||R01AA05 (WHO) R01, S01|
|Molar mass||260.375 g·mol−1[[Script error: No such module "String".]]|
|Melting point||301.5 °C (574.7 °F)|
Oxymetazoline is available over-the-counter as a topical decongestant in the form of oxymetazoline hydrochloride in nasal sprays such as Afrin, Sudafed OM, Dristan, Vicks Sinex, and Mucinex Full Force. It was developed from Xylometazoline at E.Merck Darmstadt by Fruhstorfer in 1961 (German Patent 1,117,588).
Mechanism of action
Oxymetazoline is an adrenomimetic that nonselectively agonizes α1 and α2 adrenergic receptors. Since vascular beds widely express α1 receptors, the action of oxymetazoline results in vasoconstriction. 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, causes vasodilation because of centrally-mediated inhibition of sympathetic tone via presynaptic α2 receptors. Vasoconstriction of vessels results in relief of nasal congestion in two ways: firstly, it increases the diameter of the airway lumen; secondly, it reduces fluid exudation from postcapillary venules.
Side effects and special considerations
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 reliant on the medication to relieve their chronic congestion.
Effects of benzalkonium chloride
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.
Use in pregnancy
The Food and Drug Administration places oxymetazoline in category C, indicating there may be some risk to the fetus. 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.
If accidentally ingested, standard methods to remove unabsorbed drugs should be considered. There is no specific antidote for oxymetazoline, although its pharmacological effects may be reversed by alpha adrenergic antagonists such as phentolamine. In children, oxymetazoline may produce profound central nervous system depression due to stimulation of central alpha-2 receptors and imidazoline receptors, much like clonidine.
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