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Oxymetazoline hydrochloride is classified as a nasal decongestant, and it is mostly used to treat nasal congestion caused by hay fever, common colds, flu, sinusitis, and other allergic sinusitis. Nasal congestion, commonly known as stuffy nose, occurs when the nasal passages swell with extra mucus and fluid. It includes a nasal decongestant, compressing and restricting the blood vessels that line the nose passageways. Thus, oxymetazoline relieves congestion while decreasing mucus production. The FDA authorized oxymetazoline as a nasal decongestant in 1964.
Additionally, oxymetazoline is used to treat a number of illnesses, like
Face redness: Rosacea, a skin disorder that results in pimples and facial redness, can be treated with metronidazole if it is causing persistent facial redness. It functions by constricting the skin's blood vessels.
Dental anesthesia: Intranasal spray with oxymetazoline and tetracaine is useful for providing regional anesthesia to patients, including adults and children, during dental treatments.
Ptosis: Adults with acquired blepharoptosis or ptosis can be treated with oxymetazoline ophthalmic drops. This was the first medical procedure for this illness that the FDA allowed.
BRAND NAMES
Dristan 12-hour Nasal spray: It contains the active ingredient of oxymetazoline. It is available as a nasal spray used to fast-acting relieve sinus and nasal congestion.
Kovanaze: It contains a combination of tetracaine HCL and oxymetazoline HCL used as anesthesia during dental treatment.
Upneeq: It contains the active ingredient of oxymetazoline. It is available in the form of an ophthalmic solution used to treat ptosis.
Nostrila: It contains the active ingredients of oxymetazoline. It is available in the form of a solution used to treat colds, hay fever, and upper respiratory allergies.
Rhofade: It contains the active ingredient of oxymetazoline. It is available in the form of gel-based cream used to treat redness of the face.
Afrin: It contains the active ingredients of oxymetazoline. It is available in the form of nasal spray used to fast congestion relief from allergies and reduce the swelling of nasal passages.
MECHANISM OF ACTION
Oxymetazoline binds to α1 and α2 adrenoceptors, which are Gq- and Gi-protein-coupled receptors. α1-adrenoceptor antagonism activates phospholipase C to increase intracellular calcium levels, while α2-adrenoceptor antagonism inhibits adenyl cyclase and causes vasoconstriction. Oxymetazoline reduces nasal congestion by vasoconstricting the respiratory microvasculature, which includes both resistance and capacitance blood vessels on the human nasal mucosa. This results in reduced nasal mucosal blood flow, edema, and airflow resistance.
PHARMACOKINETICS
Absorption
Following nasal administration of a 0.6-ml combination product containing tetracaine and oxymetazoline in adult subjects, the maximum concentrations of oxymetazoline were reached within approximately 10 minutes.
Distribution
Oxymetazoline nasal spray increases nasal cross-sectional area and decreases nasal resistance throughout the nasal cavity.
Metabolism
Oxymetazoline is metabolized through the liver.
Excretion
Renal excretion is the main method of elimination at clinically significant oxymetazoline concentrations.
PHARMACODYNAMICS
Oxymetazoline reduced nasal congestion and improved nasal airflow in individuals with acute coryzal rhinitis for up to 12 hours after a single dosage. Oxymetazoline hydrochloride is a nasal decongestant that constricts and narrows the blood vessels in the nasal passages. Thus, oxymetazoline hydrochloride clears the clogged nose and reduces mucus production.
DOSAGE AND ADMINISTRATION
Oxymetazoline is available in the form of a nasal spray. It is often administered every 10 to 12 hours as needed, but never more than twice in 24 hours.
Oxymetazoline is available as an intranasal solution.
DRUG INTERACTIONS
- Drug interactions with oxymetazoline may include
- Anti-depressants: imipramine, despiramine
- Ergot alkaloids: ergotamine, dihydroergotamine
- MAO inhibitors: linezolid, selegiline, tranylcypromine
CONTRAINDICATIONS
It is contraindicated in patients with high blood pressure, arrhythmias, thyroid problems, diabetes, and glaucoma.
SIDE EFFECTS
Side effects of oxymetazoline may include
- Increased nasal discharge
- Sneezing
- Burning
- Dryness inside the nose
- Nervousness
- Nausea
- Headache
- Dizziness
Some serious side effects may include
- Fast heartbeat
- Slow heartbeat
OVERDOSE
Symptoms of overdose may include
- Dizziness
- Chest pain
- Myocardial infarction
- Headache
- Visual disturbance
- Stroke
- Hypertension
- arrhythmia
TOXICITY
Excessive dosage can cause poisoning. Over dosage and extended or excessive usage of oxymetazoline have been linked to rebound nasal congestion, mucosal irritation, and significant systemic effects, including major cardiovascular adverse events.
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