Naphazoline Hydrochloride

Class: Vasoconstrictors
VA Class: OP800
CAS Number: 550-99-2
Brands: Advanced Eye Relief Redness Instant Relief, Advanced Eye Relief Redness Maximum Relief, AK-Con, Clear Eyes Complete 7 Symptom Relief, Clear Eyes Cooling Comfort Itchy Eye Relief, Clear Eyes Cooling Comfort Redness Relief, Clear Eyes Maximum Itchy Eye Relief, Clear Eyes Maximum Redness Relief, Clear Eyes Redness Relief, Naphcon-A, Opcon A, Privine, Rohto Cool, Visine A

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.c

Uses for Naphazoline Hydrochloride

Nasal Congestion

Temporary relief of nasal congestion.1008

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

Apply topically to nasal mucosa or to conjunctiva.1008 a b c

Intranasal Administration

Apply topically to nasal mucosa as drops.1008

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

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.1008

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

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.1008

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

Prescribing Limits

Pediatric Patients

Nasal Congestion
Intranasal

Self-medication: Not more frequently than every 6 hours; maximum duration of 3 days.1008

Adults

Nasal Congestion
Intranasal

Self-medication: Not more frequently than every 6 hours; maximum duration of 3 days.1008

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

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

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).1001 1002 1003 1004 1005 1006 1007 (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.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

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

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.1001 Keep out of reach of children.1001 (See Advice to Patients.)

Geriatric Use

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

Common Adverse Effects

Ophthalmic: 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

Nasal

Solution

Room temperature (20–25°C).1008

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

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

  • Importance of avoiding contamination of the dropper tip.a b d To minimize risk of spreading infections, do not share dropper or container with other individuals.1008

  • Importance of calling clinician or poison control center if accidentally ingested.1001 Importance of seeking emergency help immediately.1001

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.c

  • 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

Nasal

Solution

0.05%

Privine Nasal Drops

Insight

Ophthalmic

Solution

0.1%*

AK-Con

Akorn

Naphazoline Hydrochloride Ophthalmic Solution

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

Naphazoline Hydrochloride Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.012% with Glycerin 0.25%*

Clear Eyes Redness Relief

Prestige Brands

Naphazoline Hydrochloride and Glycerin Eye Drops

0.012% with Glycerin 0.25% and Zinc Sulfate 0.25%

Clear Eyes Cooling Comfort Itchy Eye Relief

Prestige Brands

Clear Eyes Maximum Itchy Eye Relief

Prestige Brands

0.012% with Polyethylene Glycol 300 0.2%

Advanced Eye Relief Redness Instant Relief

Bausch & Lomb

0.012% with Polysorbate 80 0.2%

Rohto Cool

Mentholatum

0.025% with Hypromellose 0.2%, Polysorbate 80 0.5%, and Zinc Sulfate 0.25%

Clear Eyes Complete 7 Symptom Relief

Prestige Brands

0.025% with Pheniramine Maleate 0.3%*

Naphcon-A

Alcon

Visine A

J&J

Naphazoline Hydrochloride and Pheniramine Maleate Eye Drops

0.027% with Pheniramine Maleate 0.315%*

Naphazoline Hydrochloride and Pheniramine Maleate Eye Drops

Opcon A

Bausch & Lomb

0.03% with Glycerin 0.5%

Clear Eyes Cooling Comfort Redness Relief

Prestige Brands

Clear Eyes Maximum Redness Relief

Prestige Brands

0.03% with Hypromellose 0.5%

Advanced Eye Relief Redness Maximum Relief

Bausch & Lomb

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions February 28, 2014. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1001. US Food and Drug Administration. FDA drug safety communication: Serious adverse events from accidental ingestion by children of over-the-counter eye drops and nasal sprays. Rockville, MD; 2012 Oct 25. From FDA website.

1002. Tobias JD. Central nervous system depression following accidental ingestion of Visine eye drops. Clin Pediatr (Phila). 1996; 35:539-40. [PubMed 8902333]

1003. Katar S, Taskesen M, Okur N. Naloxone use in a newborn with apnea due to tetrahydrozoline intoxication. Pediatr Int. 2010; 52:488-9. [PubMed 20723124]

1004. Holmes JF, Berman DA. Use of naloxone to reverse symptomatic tetrahydrozoline overdose in a child. Pediatr Emerg Care. 1999; 15:193-4. [PubMed 10389957]

1005. Vitezic D, Rozmanic V, Franulovic J et al. Naphazoline nasal drops intoxication in children. Arh Hig Rada Toksikol. 1994; 45:25-9. [PubMed 8067910]

1006. Mahieu LM, Rooman RP, Goossens E. Imidazoline intoxication in children. Eur J Pediatr. 1993; 152:944-6. [PubMed 8276031]

1007. Higgins GL, Campbell B, Wallace K et al. Pediatric poisoning from over-the-counter imidazoline-containing products. Ann Emerg Med. 1991; 20:655-8. [PubMed 2039105]

1008. Insight. Privine (naphazoline hydrochloride 0.05%) product information. From Insight Pharmaceuticals website. Accessed 2013 Oct 22.

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 2014. McEvoy GK, ed. Naphazoline Hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists. From AHFS website.

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.

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