Naphazoline (Monograph)

Brand names: AK-Con, Privine, Rohto Cool
Drug class: Vasoconstrictors
VA class: OP800
CAS number: 550-99-2

Medically reviewed by Drugs.com on Feb 19, 2024. Written by ASHP.

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.

Uses for Naphazoline

Nasal Congestion

Temporary relief of nasal congestion.

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.

Naphazoline Dosage and Administration

Administration

Apply topically to nasal mucosa or to conjunctiva.

Intranasal Administration

Apply topically to nasal mucosa as drops.

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

Nasal Congestion

Intranasal

For self-medication in children ≥12 years of age, 1 or 2 drops of a 0.05% solution in each nostril not more frequently than every 6 hours.

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

Nasal Congestion

Intranasal

For self-medication, 1 or 2 drops of a 0.05% solution in each nostril not more frequently than every 6 hours.

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.

Prescribing Limits

Pediatric Patients

Nasal Congestion

Intranasal

Self-medication: Not more frequently than every 6 hours; maximum duration of 3 days.

Adults

Nasal Congestion

Intranasal

Self-medication: Not more frequently than every 6 hours; maximum duration of 3 days.

Cautions for Naphazoline

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.

Accidental ingestion of imidazoline derivatives (i.e., naphazoline, oxymetazoline, 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.)

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.

Accidental ingestion of OTC ophthalmic solutions or nasal sprays containing imidazoline derivatives (i.e., naphazoline, oxymetazoline, 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.)

Geriatric Use

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

Common Adverse Effects

Ophthalmic: Blurred vision, mild transient stinging and/or irritation.

Drug Interactions

Specific Drugs

Naphazoline 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

Nasal

Solution

Room temperature (20–25°C).

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

• Importance of avoiding contamination of the dropper tip. To minimize risk of spreading infections, do not share dropper or container with other individuals.

• Importance of calling clinician or poison control center if accidentally 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 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.

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

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

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