Oxymetazoline

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Oxymetazoline is a selective adrenergic receptor agonist? ₁ and? ₂ adrenergic receptor partial agonist. This is a topical decongestant, used in the form of oxymetazoline hydrochloride. It was developed from xylometazoline in E. Merck Darmstadt by Fruhstorfer in 1961. Oxymetazoline is generally available as a nasal spray.

Video Oxymetazoline

Medical use

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, Naprilla, Sudafed OM, Vicks Sinex, Zicam, SinuFrin, Drixoral and Mucinex Full Force.

In the United States, 1% oxymethazoline cream is approved by the Food and Drug Administration for the topical treatment of facial erythema associated with rosacea in adults.

Due to its vasoconstricting nature, oxymetazoline is also used to treat nose bleeding and redness eyes due to mild irritation (marketed as Visine L.R. in the form of eye drops).

Maps Oxymetazoline

Side effects and special considerations

Rebound congestion

Rebound congestion, or rhinitis medicamentosa, can occur if oxymetazoline is used for more than three days. Patients who continue to use oxymetazoline beyond this point can become dependent on drugs to reduce their chronic congestion.

Use in pregnancy

The Food and Drug Administration puts oxymetazoline in category C, indicating the risk to the fetus can not be excluded. Although it has been shown that a single dose does not significantly alter the mother or fetal circulation, the subject has not been studied broad enough to draw reliable conclusions.

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Overdose

If accidentally ingested, standard methods for removing unabsorbed drugs should be considered. There is no specific antidote for oxymetazoline, although its pharmacological effects can be reversed by? adrenergic antagonists such as phentolamine. In cases of potentially life-threatening overdose (such as hypertensive crises), benzodiazepines should be considered to reduce the possibility of seizures and seizures, and reduce anxiety and lower blood pressure. In children, oxymetazoline can produce deep depression of the central nervous system due to stimulation of central receptors? ₂ and imidazoline receptors, such as clonidine.

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Pharmacology

Action mechanism

Oxymetazoline is sympathomimetic that selectively tortures? ₁ and, in part,? ₂ adrenergic receptors. Because the bed veins are widely express? ₁ receptor, the action of oxymetazoline produces vasoconstriction. In addition, local application of this drug also produces vasoconstriction because of its action on postcasinaps endotaps? ₂ receptors; systemic agonist application? ₂ , in contrast, causes vasodilatation because of the inhibition of centralized sympathetic tones via presinaptic receptors? ₂ . Vasoconstriction of vessels results in a clogged nasal relief in two ways: first, increasing the lumen diameter of the airway; second, reducing fluid exudation from the postcapillary venule. May decrease nasal airway resistance (NAR) up to 35.7% and nasal mucosal blood flow up to 50%.

Pharmacokinetics

Imidazoline is a sympathomimetic agent, with the main effect? adrenergic receptor and little if any effect? adrenergic receptors. Oxymetazoline is readily absorbed orally. Works on? receptors of systemically absorbed oxymetazoline hydrochloride can last up to 7 hours after a single dose. The elimination half-life in humans is 5-8 hours. It is excreted unchanged both by the kidney (30%) and in the stool (10%).

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History

The Afrin oxymetazoline brand was first sold as a prescription drug in 1966. After finding a substantial initial success as a prescription drug, it became available as an over-the-counter drug in 1975. Schering-Plow was not involved in heavy advertising until 1986. From from the late 1980s to the mid-1990s, Afrin appeared in many famous television commercials. Some of these ads show men, women, and children using other brands of nasal sprays, and then stand upside down or hung upside down from play gear to prevent their nose sprays from dripping out. This is paired with Afrin users who have no issues.

Society and culture

Brand name

The 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

Source of the article : Wikipedia