Generic Name: oxymetazoline nasal

Uses

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.

Dosage and Administration

Administration

Administer topically to nasal mucosa or conjunctiva.

Intranasal Administration

Administer nasal solution intranasally as drops, sprays, or nasal pumps. Nasal sprays may be preferable to drops due to decreased risk of swallowing of drug and resultant systemic absorption.

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

Apply drops to dependent (lower) nostril while in a lateral, head-low position. Remain in the same position for 5 minutes, then apply drops to the other nostril in a similar manner. Alternatively, instill drops while in a reclining position, with head tilted back as far as possible.

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 drops or 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 drops or 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

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.)

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.

Common Adverse Effects

Nasal solution: transient burning, stinging, sneezing, increased nasal discharge or dryness of nasal mucosa.

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 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.

AHFS Drug Information. © Copyright, 1959-2009, Selected Revisions June 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.