Introduction

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^{† [off-label]} (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.)

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.

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.)