1. Medical uses

2. Side effects and special considerations
     Rebound congestion    Use in pregnancy  

3. Overdose

4. Pharmacology
     Pharmacodynamics    Pharmacokinetics  

5. History

6. Society and culture
     Brand names  

7. References

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.^[1] Oxymetazoline is generally available as a nasal spray.

Medical uses

Oxymetazoline is available over-the-counter as a topical decongestant in the form of oxymetazoline hydrochloride in nasal sprays such as Otrivin, Afrin, Operil, Dristan, Dimetapp, Oxyspray, Facimin, Nasivin, Nostrilla, Utabon, Sudafed OM, Vicks Sinex, Zicam, SinuFrin, Drixoral^[2]

and Mucinex Full Force.^[3]

In the United States, oxymetazoline 1% cream is approved by the Food and Drug Administration for topical treatment of persistent facial erythema (redness) associated with rosacea in adults.^[4]

Due to its vasoconstricting properties, oxymetazoline is also used to treat nose bleeds^[5][6] and eye redness due to minor irritation (marketed as Visine L.R. in the form of eye drops). {{Citation needed|date=March 2018}} ^[7]

Side effects and special considerations

Rebound congestion

Use in pregnancy

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,^[10] this subject has not been studied extensively enough to draw reliable conclusions.{{or?|date=September 2018}}

Overdose

If accidentally ingested, standard methods to remove unabsorbed drugs should be considered.{{clarify|date=December 2016}} There is no specific antidote for oxymetazoline, although its pharmacological effects may be reversed by α adrenergic antagonists such as phentolamine. In the event of a possibly life-threatening overdose (such as a hypertensive crisis), benzodiazepines should be considered to decrease the likelihood of seizures and convulsions, as well as reduce anxiety and to lower blood pressure. In children, oxymetazoline may produce profound central nervous system depression due to stimulation of central α₂ receptors and imidazoline receptors, much like clonidine.{{citation needed|date=October 2011}}

Pharmacology

Pharmacodynamics

Oxymetazoline is a sympathomimetic that selectively agonizes α₁ and, partially, α₂ adrenergic receptors.^[11] 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.^[12] Vasoconstriction of vessels results in relief of nasal congestion in two ways: first, it increases the diameter of the airway lumen; second, it reduces fluid exudation from postcapillary venules.^[13] It can reduce nasal airway resistance (NAR) up to 35.7% and nasal mucosal blood flow up to 50%.^[14]

Pharmacokinetics

Imidazolines are sympathomimetic agents, with primary effects on α adrenergic receptors and little if any effect on β adrenergic receptors.{{fact|date=September 2018}} Oxymetazoline is readily absorbed orally.{{fact|date=September 2018}} Effects on α receptors from systemically absorbed oxymetazoline hydrochloride may persist for up to 7 hours after a single dose.{{fact|date=September 2018}} The elimination half-life in humans is 5–8 hours.{{fact|date=September 2018}} It is excreted unchanged both by the kidneys (30%) and in feces (10%).{{fact|date=September 2018}}

History

The oxymetazoline brand Afrin was first sold as a prescription medication in 1966. After finding substantial early success as a prescription medication, it became available as an over-the-counter drug in 1975. Schering-Plough did not engage in heavy advertising until 1986.^[15]

From the mid 1980s to mid 1990s, the brand Sinex was featured in many television advertisements. Some of these commercials showed men, women, and children using other brands of nasal sprays, and then standing upside down on a sidewalk, or against a wall, etc or hanging upside down from various playground equipment to prevent their nasal spray from dripping out. This was juxtaposed with Sinex users not having to hang upside side down or stand on their heads as it didn't drip out.

Society and culture

Brand names

Brand names include Afrin, Drixine, Dristan, Nasivin, Nasivion, Nezeril, Nostrilla, Logicin, Vicks Sinex, Visine L.R., Sudafed OM, Zicam, Otrivin Oxy, SinuFrin and Mucinex Sinus-Max.

References

• AlienBabelTech
• Alien Balbalu
• Alien (band)
• Alien Beat Club
• Alien Big Cat
• Alien blood
• Alien Bounty Hunters
• Alien Boy (EP)
• Alien Brain
• Alien breed
• Alien Breed 2004
• Alien Breed 2: Assault
• Alien breed evolution
• Alien Breed Evolution
• Alien Breed: Evolution
• Alien Breed: Impact
• Alien Brigade
• Alien Cargo
• Alien Cips
• Alien Clones (TV episode)
• Alien: Colonial Marines (2001)
• Alien (comics)
• Alien conspiracies
• Alien conspiracy
• Alien conspiracy theories