Naphazoline (EENT)

AHFS Class: Vasoconstrictors (52:32)

VA Class: OP800

View the associated AHFS monograph.

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 ^®; also available generically.

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.^c

Uses

Conjunctival Congestion

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

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

Dosage and Administration

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.

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}

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

Contraindications

• Angle-closure glaucoma.^{c d}

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

Warnings/Precautions

MAO Inhibitors. Concomitant use with MAO inhibitor may result in severe hypertensive crisis.^{c d}

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

Pregnancy.

Category C.^d

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

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.^{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

Specific Drugs

Pharmacokinetics

Absorption

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

Local vasoconstriction usually occurs within 10 minutes.^c

Local vasoconstriction may persist for 2–6 hours.^c

Stability

Storage

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

• 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

Naphazoline Hydrochloride

Routes	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

* available by nonproprietary name

Naphazoline Hydrochloride Combinations

Routes	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

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit www.drugstore.com.

Albalon 0.1% Solution (ALLERGAN): 15/$29.99 or 45/$75.97

© Copyright, May 2004, American Society of Health-System Pharmacists, Inc. 7272 Wisconsin Avenue, Bethesda, MD 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.