Oxymetazoline (Monograph)

Brand names: Afrin No Drip Extra Moisturizing, Afrin No Drip Original, Afrin No Drip Severe Congestion, Afrin No Drip Sinus, Afrin Original, ... show all 14 brands 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
Drug class: Vasoconstrictors
VA class: NT100
CAS number: 2315-02-8

Medically reviewed by Drugs.com on Feb 12, 2024. Written by ASHP.

Introduction

Vasoconstrictor;^a an imidazoline-derivative sympathomimetic amine.^a

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.¹¹¹

As effective as other topical vasoconstrictors.^a

Labeled and has been used for self-medication for temporary relief of nasal congestion associated with sinusitis;^{107 111} however, efficacy data are lacking and/or controversial.^{107 108 109} In October 2005, FDA issued final rule to remove this indication from labeling of OTC nasal decongestants.¹⁰⁷ Compliance date for preparations with annual sales <$25,000 is October 11, 2007; compliance date for all other preparations is April 11, 2007.¹⁰⁷

Conjunctival Congestion

Self-medication for temporary relief of ocular redness due to minor irritation.¹¹²

Otitic Barotrauma

Has been used for self-medication for symptomatic prevention of otitic barotrauma^{† [off-label]} (aerotitis [barotitis] media);^{101 103 105} however, no more effective than placebo.¹⁰¹

Related/similar drugs

phenylephrine ophthalmic, brimonidine ophthalmic, fluorometholone ophthalmic, naphazoline ophthalmic, Upneeq, FML

Oxymetazoline Dosage and Administration

Administration

Administer topically to nasal mucosa or conjunctiva.^{a 111 112}

Intranasal Administration

Administer nasal solution intranasally as sprays or nasal pumps.^a

Prior to initial use of metered sprays, prime nasal inhaler by depressing the pump firmly several times.^a

Administer nasal spray or pump into each nostril while head is erect.^a

Ophthalmic Administration

Administer ophthalmic solution topically to the conjunctiva.^{a 112}

Avoid contamination of the dropper tip.¹¹²

Remove contact lenses before administering ophthalmic solution.^{a 112}

Do not administer discolored or cloudy solutions.¹¹²

Dosage

Available as oxymetazoline hydrochloride; dosage expressed in terms of the salt.^{111 112}

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.^{a 111}

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.¹¹²

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.^{a 111}

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.¹¹²

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.¹¹¹ (See Advice to Patients.)

Adults

Nasal Congestion

Intranasal

Self-medication: Maximum of 2 times (2 doses) in a 24-hour period.¹¹¹ (See Advice to Patients.)

Cautions for Oxymetazoline

Contraindications

• Known hypersensitivity to oxymetazoline or any ingredient in the formulation.^a

• Known sensitivity to the pharmacologic effects of adrenergic drugs.^a

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.^a Possible rebound nasal congestion or ocular hyperemia (redness);^{a 111 112} avoid prolonged use.^a (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).^{1001 1002 1003 1004 1005 1006 1007} (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.^a 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.^{a 111}

Glaucoma

Patients with narrow-angle glaucoma should consult a clinician before using ophthalmic solution.¹¹²

Specific Populations

Pregnancy

Category C.¹¹⁴

Lactation

Not known whether oxymetazoline is distributed into milk.¹¹⁴ Use with caution in nursing women.¹¹³

Pediatric Use

0.05% nasal solution or 0.025% ophthalmic solution not recommended for self-medication in children <6 years of age.^{111 112}

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.^a

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.¹⁰⁰¹ Keep out of reach of children.¹⁰⁰¹ (See Advice to Patients.)

Common Adverse Effects

Nasal solution: transient burning, stinging, sneezing, increased nasal discharge or dryness of nasal mucosa.^{a 111}

Oxymetazoline Pharmacokinetics

Absorption

Bioavailability

Occasionally, absorption may be sufficient to produce systemic effects.^a

Onset

Following intranasal administration, local vasoconstriction usually occurs within 5–10 minutes.^a

Following ocular administration, local vasoconstriction usually occurs within minutes.^a

Duration

Following intranasal administration, local vasoconstriction persists for 5–6 hours, with gradual decline over the next 6 hours.^a

Following ophthalmic administration, local vasoconstriction persists for up to 6 hours.^a

Stability

Storage

Nasal

Solution

Room temperature (<40°C); avoid freezing.^{a 111} Protect from light.¹¹¹

Ophthalmic

Solution

15–30°C;¹¹² do not store in aluminum containers.^a

Actions

• Structurally and pharmacologically related to naphazoline, tetrahydrozoline, and xylometazoline.^a

• Directly stimulates α-adrenergic receptors; exerts little or no effect on β-adrenergic receptors.^a

• Constricts dilated arterioles, reduces nasal blood flow and congestion, and opens obstructed eustachian ostia.^a Temporarily relieves nasal and conjunctival congestion following topical application.^a

Advice to Patients

• With intranasal use, importance of discontinuing drug and consulting a clinician if nasal congestion worsens or persists for >3 days.¹¹¹

• 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.¹¹²

• Overuse of nasal solution may cause recurrence or exacerbation of nasal congestion;¹¹¹ overuse of ophthalmic solution may produce increased redness of the eye.¹¹²

• Importance of removing contact lenses prior to administration of ophthalmic solution.^{a 112}

• Importance of avoiding contamination of the dropper, inhaler, or spray dispenser.^{a 111 112} Do not touch dropper tip to any surface;¹¹² rinse inhaler/spray dispenser tip with hot water or wipe clean following use.^a To minimize risk of spreading infections, do not share dropper, inhaler, or spray dispenser with other individuals.^{a 111}

• Importance of calling clinician or poison control center if ingested.¹⁰⁰¹ Importance of seeking emergency help immediately.¹⁰⁰¹

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.^a

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^a

• 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.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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