Skip to Content

Naphazoline Hydrochloride

Class: Vasoconstrictors
VA Class: OP800
CAS Number: 550-99-2
Brands: AK-Con, Albalon, All Clear, All Clear AR, Clear Eyes, Clear Eyes ACR, Napha A, Napha Forte, Naphcon, Naphcon-A, Opcon A, VasoClear, VasoClear A, Vasocon-A, Visine A

Warning(s)

Special Alerts:

[Posted 10/25/2012] ISSUE: FDA is warning healthcare professionals and the public that accidental ingestion by children of over-the-counter eye drops used to relieve redness and nasal decongestant sprays can result in serious and life-threatening adverse events. The eye drops and nasal sprays that have been involved in the cases of accidental ingestion contain the active ingredients tetrahydrozoline, oxymetazoline, or naphazoline. The cases of accidental ingestion reviewed by FDA occurred in children 5 years of age and younger. No deaths were reported; however, serious events requiring hospitalization such as nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma have occurred. Ingestion of only a small amount (1-2 mL; for reference, there are 5 mL in a teaspoon) of the eye drops or nasal spray can lead to serious adverse events in young children.

BACKGROUND: Most of these redness-relief eye drops and nasal decongestant sprays currently do not come packaged with child-resistant closures, so children can accidentally ingest the drug if the bottles are within easy reach. These products are sold under various brand names, as generics, and as store brands (see List of Products, included in the Drug Safety Communication, at: ).

RECOMMENDATION: Consumers should store these products out of reach of children at all times. If a child accidentally swallows OTC redness-relief eye drops or nasal decongestant spray, call your local poison control center (1-800-222-1222) immediately. Experts are available all day, every day at these centers. For more information visit the FDA website at: and .

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.c

Uses for Naphazoline Hydrochloride

Conjunctival Congestion

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

Slideshow: View Frightful (But Dead Serious) Drug Side Effects

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

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

Naphazoline Hydrochloride Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the conjunctiva.a b c

Avoid contamination of the dropper tip.a b d

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

Do not administer discolored or cloudy solutions.b d

Dosage

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

Pediatric Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

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.c e f

Adults

Conjunctival Congestion
Ophthalmic

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

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.a c e f

Cautions for Naphazoline Hydrochloride

Contraindications

  • Angle-closure glaucoma.c d

  • Known hypersensitivity to naphazoline or any ingredient in the formulation.a d

Warnings/Precautions

Warnings

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

MAO Inhibitors

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

General Precautions

Sympathomimetic Effects

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

Overuse

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

Glaucoma

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

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).c

Specific Populations

Pregnancy

Category C.d

Lactation

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

Pediatric Use

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

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.c d

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

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

Geriatric Use

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

Common Adverse Effects

Blurred vision, mild transient stinging and/or irritation.c

Interactions for Naphazoline Hydrochloride

Specific Drugs

Drug

Interaction

Antidepressants, tricyclic

Increased pressor effects of naphazolinec

MAO inhibitors

Possible severe hypertensive reactionc d

Maprotiline

Increased pressor effects of naphazolinec

Naphazoline Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Occasionally, absorption may be sufficient to produce systemic effects.c

Onset

Local vasoconstriction usually occurs within 10 minutes.c

Duration

Local vasoconstriction may persist for 2–6 hours.c

Stability

Storage

Ophthalmic

Solution

Room temperature; protect from light.a c d e f Do not store in aluminum containers.c

Actions

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

  • Constricts small arterioles and temporarily relieves conjunctival congestion following topical application.c d

  • May produce mydriasis when applied to the conjunctiva.c

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

  • 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.a b e

  • Overuse may produce increased redness of the eye.a b

  • Importance of avoiding contamination of the dropper tip.a b d

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

  • Importance informing patients of other precautionary information.c (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

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

Naphazoline Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.012%

All Clear (with benzalkonium chloride)

Bausch & Lomb

Clear Eyes (with benzalkonium chloride and glycerin 0.2%)

Prestige Brands

Naphcon (with benzalkonium chloride)

Alcon

0.03%

All Clear AR (with benzalkonium chloride)

Bausch & Lomb

0.1%*

AK-Con (with benzalkonium chloride)

Akorn

Albalon (with benzalkonium chloride)

Allergan

Naphazoline Hydrochloride Ophthalmic Solution

Bausch & Lomb

Naphazoline Hydrochloride Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.012% with Zinc Sulfate 0.25%

Clear Eyes ACR (with benzalkonium chloride and glycerin 0.2%)

Prestige Brands

0.025% with Pheniramine Maleate 0.3%

Naphcon-A (with benzalkonium chloride)

Alcon

Visine A

Pfizer

0.027% with Pheniramine Maleate 0.315%

Opcon A

Bausch & Lomb

0.05% with Antazoline Phosphate 0.5%

Vasocon-A (with benzalkonium chloride)

Novartis

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions October 26, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

a. Bausch & Lomb. Opcon-A (naphazoline hydrochloride) 0.02675% Opthalmic Solution prescribing information. Rochester, NY; 1998 Oct.(

b. Bausch & Lomb. All Clear AR (Naphazoline Hydrochloride) 0.03% with Pheniramine maleate 0.3% Ophthalmic Solution prescribing information. Rochester, NY; 2003.

c. AHFS Drug Information 2003. McEvoy GK, ed. Naphazoline Hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2003:2697-8.

d. Allergan. Albalon (naphazoline hydrochloride) 0.1% opthalmic solution prescribing information. In: PDR.net [database online]. Montvale, NJ: Thomson Healthcare; 2004. Updated 2003 Jan.

e. Pfizer Consumer Healthcare. Visine-A (naphazoline hydrochloride) 0.025% with pheniramine maleate 0.3% Antihistamine and Redness Reliever opthalmic solution prescribing information. In: PDR.net [database online]. Montvale, NJ: Thomson Healthcare; 2004. Undated.

f. Novartis Ophthalmics. Vascon-A (naphazoline hydrochloride) 0.05% with antazoline phosphate 0.5% Itching/Redness Reliever opthalmic solution prescribing information. In: PDR.net [database online]. Montvale, NJ: Thomson Healthcare; 2004. Undated.

Hide