Oxymetazoline

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Oxymetazoline
Systematic (IUPAC) name
3-(4,5-dihydro-1H-imidazol-2-ylmethyl)- 2,4-dimethyl-6-tert-butyl-phenol
Identifiers
CAS number	1491-59-4
ATC code	R01AA05 R01AB07, S01GA04
PubChem	4636
DrugBank	APRD01158
Chemical data
Formula	C16H24N2O
Mol. mass	260.375 g·mol−1
Physical data
Melt. point	301.5 °C (575 °F)
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Oxymetazoline is a topical decongestant used, in the form of Oxymetazoline hydrochloride, in products such as Nasivion, Vicks Sinex and Afrin. Oxymetazoline is generally available as a nasal spray. If overused (usually for a period of more than 3 days) it can cause a "rebound congestion" (rhinitis medicamentosa) where the tissues of the sinuses are damaged, become swollen, and therefore become congested after the drug wears off. As a result, a user can develop physiological tolerance to the drug, manifested by prolonged nasal congestion without continued use of the medication. (See the discussion of the effect of benzalkonium chloride, a common additive to oxymetazoline nasal sprays, in the article Rhinitis medicamentosa.)

The medication has sympathomimetic properties, and thus constricts the blood vessels of the nose and sinuses via activation of alpha1 adrenergic receptors, in turn causing less production of mucous. It is frequently used by anaesthesiologists to reduce nasal bleeding during nasal endotracheal intubations. This drug, not unlike most sympathomimetic amines, has adrenaline-releasing properties due to its mode of action. However, since the application is topical, it has practically no CNS stimulation as of the systemic application of decongestants such as pseudoephedrine.

Since no clinical data on exposed pregnancies are available with oxymetazoline, the safe use of oxymetazoline during pregnancy has not been established.

If accidentally ingested, standard methods to remove unabsorbed drugs should be considered. There is no specific antidote for oxymetazoline. In children, oxymetazoline may produce profound central nervous system depression.