Generic Name: naphazoline ophthalmic

Uses

Conjunctival Congestion

Temporary relief of conjunctival congestion, itching, and minor irritation.

Used alone or in fixed combination with antihistamines (e.g., antazoline phosphate, pheniramine maleate) and/or astringents (e.g., zinc sulfate).

Ineffective in the treatment of delayed hypersensitivity reactions such as contact dermatoconjunctivitis.

Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the conjunctiva.

Avoid contamination of the dropper tip.

Some manufacturers recommend that contact lenses be removed before administering the ophthalmic solution.

Do not administer discolored or cloudy solutions.

Dosage

Available as naphazoline hydrochloride; dosage expressed in terms of the salt.

Pediatric Patients

Conjunctival Congestion

Ophthalmic

For self-medication in children ≥6 years of age, 1 or 2 drops of a 0.01–0.05% ophthalmic solution up to 4 times daily or as directed by clinician.

Adults

Conjunctival Congestion

Ophthalmic

1 or 2 drops of a 0.1% ophthalmic solution every 3–4 hours as needed.

For self-medication, 1 or 2 drops of a 0.01–0.05% ophthalmic solution up to 4 times daily or as directed by clinician.

Cautions

Contraindications

• Angle-closure glaucoma.
• Known hypersensitivity to naphazoline or any ingredient in the formulation.

Warnings/Precautions

Warnings

MAO Inhibitors

Concomitant use with MAO inhibitor may result in severe hypertensive crisis.

General Precautions

Sympathomimetic Effects

Possible headache, hypertension, cardiac irregularities, nervousness, nausea, dizziness, weakness, and sweating. Use with caution in patients with hypertension, cardiovascular abnormalities, diabetes mellitus, hyperthyroidism, infection, or injury.

Overuse

Possible conjunctival irritation and adverse systemic effects with excessive dosage and/or prolonged or too frequent use. Possible rebound congestion, characterized by reactive hyperemia. Avoid prolonged use.

Glaucoma

Use not recommended in patients with glaucoma except under the advice and supervision of a physician.

Use of Fixed Combinations

When used in fixed combination with antihistamines (e.g., antazoline phosphate, pheniramine maleate) and/or astringents (e.g., zinc sulfate), consider the cautions, precautions, and contraindications associated with the concomitant drug(s).

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether naphazoline is distributed into milk. Use with caution in nursing women.

Pediatric Use

Safety and efficacy of 0.1% ophthalmic solution not established in infants and children; potential for CNS depression, possibly progressing to coma and hypothermia, especially in infants.

0.01–0.05% ophthalmic solutions not recommended for self-medication in children <6 years of age.

Possible conjunctival irritation and adverse systemic effects (including marked sedation) associated with excessive dosage and/or prolonged or too frequent use.

Geriatric Use

Possible liberation of pigment granules, presumably from the iris following conjunctival application of naphazoline, especially high concentrations.

Common Adverse Effects

Blurred vision, mild transient stinging and/or irritation.

Interactions

Specific Drugs

Pharmacokinetics

Absorption

Bioavailability

Occasionally, absorption may be sufficient to produce systemic effects.

Onset

Local vasoconstriction usually occurs within 10 minutes.

Duration

Local vasoconstriction may persist for 2–6 hours.

Stability

Storage

Ophthalmic

Solution

Room temperature; protect from light. Do not store in aluminum containers.

Actions

• Directly stimulates α-adrenergic receptors; exerts little or no effect on β-adrenergic receptors.
• Constricts small arterioles and temporarily relieves conjunctival congestion following topical application.
• May produce mydriasis when applied to the conjunctiva.

Advice to Patients

• Importance of discontinuing drug and consulting a clinician if ocular pain or visual changes occur, ocular redness or irritation worsens or persists for >72 hours, or manifestations of systemic absorption (e.g., headache, nausea, decrease in body temperature) occur.
• Overuse may produce increased redness of the eye.
• Importance of avoiding contamination of the dropper tip.
• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
• Importance informing patients of other 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 May 2004. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

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.