Class: Vasoconstrictors
VA Class: NT100
CAS Number: 2315-02-8
Brands: Afrin No Drip Extra Moisturizing, Afrin No Drip Original, Afrin No Drip Severe Congestion, Afrin No Drip Sinus, Afrin Original, Afrin Severe Congestion, Afrin Sinus, Dristan 12 Hour, Neo-Synephrine 12 Hour Severe Sinus Congestion, Nostrilla 12 Hour Nasal Decongestant, Vicks Sinex 12 Hour Nasal Decongestant, Visine L.R. Eye Drops, Zicam Extreme Congestion Relief, Zicam Intense Sinus Relief
Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.
Uses for Oxymetazoline
Nasal Congestion
Self-medication for temporary relief of nasal congestion associated with the common cold, hay fever, or other upper respiratory allergies.
As effective as other topical vasoconstrictors.
Labeled and has been used for self-medication for temporary relief of nasal congestion associated with sinusitis; however, efficacy data are lacking and/or controversial. In October 2005, FDA issued final rule to remove this indication from labeling of OTC nasal decongestants. Compliance date for preparations with annual sales <$25,000 is October 11, 2007; compliance date for all other preparations is April 11, 2007.
Conjunctival Congestion
Self-medication for temporary relief of ocular redness due to minor irritation.
Otitic Barotrauma
Has been used for self-medication for symptomatic prevention of otitic barotrauma† (aerotitis [barotitis] media); however, no more effective than placebo.
Oxymetazoline Dosage and Administration
Administration
Administer topically to nasal mucosa or conjunctiva.
Intranasal Administration
Administer nasal solution intranasally as sprays or nasal pumps.
Prior to initial use of metered sprays, prime nasal inhaler by depressing the pump firmly several times.
Administer nasal spray or pump into each nostril while head is erect.
Ophthalmic Administration
Administer ophthalmic solution topically to the conjunctiva.
Avoid contamination of the dropper tip.
Remove contact lenses before administering ophthalmic solution.
Do not administer discolored or cloudy solutions.
Dosage
Available as oxymetazoline hydrochloride; dosage expressed in terms of the salt.
Pediatric Patients
Nasal Congestion
Intranasal
For self-medication in children ≥6 years of age: 2 or 3 sprays of a 0.05% nasal solution in each nostril every 10–12 hours (usually in the morning and evening), up to 2 times daily.
Conjunctival Congestion
Ophthalmic
For self-medication in children ≥6 years of age: 1 or 2 drops of a 0.025% ophthalmic solution in the affected eye(s) every 6 hours as needed.
Adults
Nasal Congestion
Intranasal
For self-medication: 2 or 3 sprays of a 0.05% nasal solution in each nostril every 10–12 hours (usually in the morning and evening), up to 2 times daily.
Conjunctival Congestion
Ophthalmic
For self-medication: 1 or 2 drops of a 0.025% ophthalmic solution in the affected eye(s) every 6 hours as needed.
Prescribing Limits
Pediatric Patients
Nasal Congestion
Intranasal
Self-medication in children ≥6 years of age: Maximum of 2 times (2 doses) in a 24-hour period. (See Advice to Patients.)
Adults
Nasal Congestion
Intranasal
Self-medication: Maximum of 2 times (2 doses) in a 24-hour period. (See Advice to Patients.)
Cautions for Oxymetazoline
Contraindications
- Known hypersensitivity to oxymetazoline or any ingredient in the formulation.
- Known sensitivity to the pharmacologic effects of adrenergic drugs.
Warnings/Precautions
General Precautions
Overuse
Possible irritation of nasal mucosa and adverse systemic effects (particularly in children) with excessive dosage and/or prolonged or too frequent intranasal use. Possible rebound nasal congestion or ocular hyperemia (redness); avoid prolonged use. (See Advice to Patients.)
Accidental ingestion of imidazoline derivatives (i.e., oxymetazoline, naphazoline, tetrahydrozoline) in children has resulted in serious adverse events requiring hospitalization (e.g., coma, bradycardia, decreased respiration, sedation, somnolence). (See Pediatric Use under Cautions and also see Advice to Patients.)
Sympathomimetic Effects
With intranasal use, possible headache, hypertension, cardiac irregularities (e.g., palpitation, reflex bradycardia), nervousness, nausea, dizziness, and insomnia. Use with caution and under direction of a clinician in patients with thyroid disease (e.g., hyperthyroidism), heart disease (including angina), hypertension, advanced arteriosclerotic conditions, or diabetes mellitus; in patients experiencing difficulty in urination secondary to prostatic enlargement; or in patients receiving monoamine oxidase (MAO) inhibitors.
Glaucoma
Patients with narrow-angle glaucoma should consult a clinician before using ophthalmic solution.
Specific Populations
Pregnancy
Category C.
Lactation
Not known whether oxymetazoline is distributed into milk. Use with caution in nursing women.
Pediatric Use
0.05% nasal solution or 0.025% ophthalmic solution not recommended for self-medication in children <6 years of age.
Possible irritation of nasal mucosa and adverse systemic effects (including profound CNS depression) associated with excessive dosage, prolonged or too frequent use, or inadvertent ingestion of nasal solution.
Accidental ingestion of OTC ophthalmic solutions or nasal sprays containing imidazoline derivatives (i.e., oxymetazoline, naphazoline, tetrahydrozoline) in children has resulted in serious adverse events requiring hospitalization, including nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma. Keep out of reach of children. (See Advice to Patients.)
Common Adverse Effects
Nasal solution: transient burning, stinging, sneezing, increased nasal discharge or dryness of nasal mucosa.
Oxymetazoline Pharmacokinetics
Absorption
Bioavailability
Occasionally, absorption may be sufficient to produce systemic effects.
Onset
Following intranasal administration, local vasoconstriction usually occurs within 5–10 minutes.
Following ocular administration, local vasoconstriction usually occurs within minutes.
Duration
Following intranasal administration, local vasoconstriction persists for 5–6 hours, with gradual decline over the next 6 hours.
Following ophthalmic administration, local vasoconstriction persists for up to 6 hours.
Stability
Storage
Nasal
Solution
Room temperature (<40°C); avoid freezing. Protect from light.
Ophthalmic
Solution
15–30°C; do not store in aluminum containers.
Actions
- Structurally and pharmacologically related to naphazoline, tetrahydrozoline, and xylometazoline.
- Directly stimulates α-adrenergic receptors; exerts little or no effect on β-adrenergic receptors.
- Constricts dilated arterioles, reduces nasal blood flow and congestion, and opens obstructed eustachian ostia. Temporarily relieves nasal and conjunctival congestion following topical application.
Advice to Patients
- With intranasal use, importance of discontinuing drug and consulting a clinician if nasal congestion worsens or persists for >3 days.
- With ophthalmic use, importance of discontinuing drug and consulting a clinician if ocular pain or visual changes occur or if ocular redness or irritation worsens or persists for >72 hours.
- Overuse of nasal solution may cause recurrence or exacerbation of nasal congestion; overuse of ophthalmic solution may produce increased redness of the eye.
- Importance of removing contact lenses prior to administration of ophthalmic solution.
- Importance of avoiding contamination of the dropper, inhaler, or spray dispenser. Do not touch dropper tip to any surface; rinse inhaler/spray dispenser tip with hot water or wipe clean following use. To minimize risk of spreading infections, do not share dropper, inhaler, or spray dispenser with other individuals.
- Importance of calling clinician or poison control center if ingested. Importance of seeking emergency help immediately.
- Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.
- Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
- Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
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Oxymetazoline Hydrochloride |
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Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
|
Nasal |
Solution |
0.05%* |
Afrin No Drip Extra Moisturizing 12 Hour Pump Mist |
Schering-Plough |
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Afrin No Drip Original 12 Hour Pump Mist |
Schering-Plough |
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Afrin No Drip Severe Congestion 12 Hour Pump Mist |
Schering-Plough |
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Afrin No Drip Sinus 12 Hour Pump Mist |
Schering-Plough |
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Afrin Original 12 Hour Spray |
Schering-Plough |
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Afrin Severe Congestion 12 Hour Spray |
Schering-Plough |
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Afrin Sinus 12 Hour Spray |
Schering-Plough |
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Dristan 12 Hour Nasal Spray |
Pfizer |
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Neo-Synephrine 12 Hour Severe Sinus Congestion Spray |
Bayer |
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Nostrilla 12 Hour Nasal Decongestant Metered Pump Spray |
Insight |
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Oxymetazoline Hydrochloride Nasal Solution |
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Vicks Sinex 12 Hour Nasal Decongestant Spray (with regular or metered pump mist spray) |
Procter & Gamble |
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Zicam Extreme Congestion Relief Nasal Gel |
Matrixx |
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Zicam Intense Sinus Relief Nasal Gel |
Matrixx |
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Ophthalmic |
Solution |
0.025% |
Visine L.R. Eye Drops |
Pfizer |