Naphazoline (Ophthalmic)


VA CLASSIFICATION
Primary: OP802

Commonly used brand name(s): Ak-Con; Albalon; Albalon Liquifilm; Allerest; Allergy Drops; Clear Eyes Lubricating Eye Redness Reliever; Comfort Eye Drops; Degest 2; Estivin II; I-Naphline; Muro's Opcon; Nafazair; Naphcon; Naphcon Forte; Ocu-Zoline Sterile Ophthalmic Solution; VasoClear; VasoClear A; Vasocon; Vasocon Regular.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Decongestant (ophthalmic)—

Indications

Accepted

Ocular redness{04}{15} (treatment)—Naphazoline is indicated for the temporary relief of redness {04} {15} associated with minor irritations of the eye, {04} such as those caused by pollen-related allergies, colds, dust, smog, wind, swimming, or wearing contact lenses.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    246.74

Mechanism of action/Effect:

A direct-acting sympathomimetic amine. Acts on alpha-adrenergic receptors in the arterioles of the conjunctiva to produce vasoconstriction, resulting in decreased conjunctival congestion.

Onset of action:

Within 10 minutes.

Duration of action:

2 to 6 hours.


Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to other ophthalmic sympathomimetics may be sensitive to this medication also.

Pregnancy/Reproduction

Pregnancy—
Naphazoline may be systemically absorbed.

Studies have not been done in either animals or humans.

FDA Pregnancy Category C.

Breast-feeding

It is not known whether naphazoline is distributed into breast milk and problems in humans have not been documented; however, naphazoline may be systemically absorbed.

Pediatrics

Use in infants and children is not recommended, since central nervous system (CNS) depression leading to coma and severe reduction in body temperature may result. {29}


Geriatrics


Appropriate studies on the relationship of age to the effects of ophthalmic naphazoline have not been performed in the geriatric population. However, no geriatrics-specific problems have been documented to date.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

Antidepressants, tricyclic or
Maprotiline    (if significant systemic absorption of ophthalmic naphazoline occurs, concurrent use of maprotiline or tricyclic antidepressants may potentiate the pressor effect of naphazoline)


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Except under special circumstances, this medication should not be used when the following medical problem exists:
» Glaucoma, narrow-angle, or predisposition to    (naphazoline may cause significant mydriasis, which may precipitate an acute attack of narrow-angle glaucoma)


Risk-benefit should be considered when the following medical problems exist
Cardiovascular disease    (systemic absorption of naphazoline may cause cardiac irregularities)


Diabetes mellitus    (systemic absorption of naphazoline may cause minimal hyperglycemia)


Eye disease, serious, or infection or injury
Hypertension    (systemic absorption of naphazoline may cause hypertension)


Hyperthyroidism
Sensitivity to naphazoline


Side/Adverse Effects

Note: Serious side/adverse effects occur rarely with ophthalmic naphazoline. However, excessive dosage and/or prolonged use may cause increased irritation of the conjunctiva and systemic side effects.
Prolonged use may cause reactive hyperemia, which may result in overuse of the medication.
This medication may cause liberation of pigment granules, presumably from the iris, especially when high concentrations are used in elderly patients.

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
With excessive dosage and/or prolonged use
    
Hyperemia, reactive (increase in eye irritation)

Symptoms of systemic absorption
    
Dizziness
    
headache
    
increased sweating
    
nausea
    
nervousness
    
weakness



Those indicating need for medical attention only if they continue or are bothersome
Incidence less frequent or rare
    
Blurred vision
    
large pupils





Overdose
For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).

Clinical effects of overdose
The following effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Acute and chronic
    
Decrease in body temperature
    
drowsiness
    
slow heartbeat
    
weakness, severe



Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Naphazoline (Ophthalmic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to naphazoline





Use in children—Use in infants and children is not recommended

Other medical problems, especially narrow-angle glaucoma or predisposition to narrow-angle glaucoma

Proper use of this medication
Not using if solution becomes cloudy or changes color

» Not using in infants and children

» Importance of not using more medication than the amount recommended; or using for more than 72 hours, unless otherwise directed by physician

Proper administration technique

Preventing contamination: Not touching applicator tip to any surface and keeping container tightly closed

» Proper dosing

» Proper storage

Precautions while using this medication
» Stopping medication and checking with physician if eye pain or change in vision occurs or if redness or irritation continues, gets worse, or lasts for more than 72 hours


Side/adverse effects
Signs of potential side effects, especially reactive hyperemia or systemic absorption


General Dosing Information
Treatment should not be continued for more than 72 hours {15}, unless otherwise directed by physician.

Although some of the manufacturers recommend that patients not wear soft contact lenses during treatment with naphazoline ophthalmic solution, USP medical experts do not believe this precaution is necessary, unless the patient has corneal epithelial problems and the medication is to be used more often than once every 1 to 2 hours. No significant problems have been documented with ophthalmic solutions containing 0.03% or less of benzalkonium chloride as a preservative when they are used as eyedrops in patients with no significant corneal surface problem.


Ophthalmic Dosage Forms

NAPHAZOLINE HYDROCHLORIDE OPHTHALMIC SOLUTION USP

Usual adult and adolescent dose
Ophthalmic decongestant
Topical, to the conjunctiva, 1 drop of a 0.012% {05} {06} {08} {09} {13} {22} solution up to four times a day {05} {06} {08} {09} {13} {22} as needed, or 1 drop of a 0.1% {07} {10} {11} {12} {14} {19} {23} solution every three to four hours {07} {10} {11} {12} {19} {23} as needed.


Usual pediatric dose
Use is not recommended.

Strength(s) usually available
U.S.—


0.012% (OTC) [Allerest] [Allergy Drops{42}] [Clear Eyes Lubricating Eye Redness Reliever{30}] [Degest 2{33}] [Estivin II] [Naphcon{34}]


0.02% (OTC) [VasoClear{38}] [VasoClear A{39}]


0.025% (OTC)[Generic]{41}


0.03% (OTC) [Comfort Eye Drops{32}]


0.1% (Rx) [Ak-Con{28} (benzalkonium chloride 0.01%)] [Albalon (polyvinyl alcohol 1.4%) (benzalkonium chloride 0.004%)] [I-Naphline] [Muro's Opcon] [Nafazair] [Naphcon Forte{35} (benzalkonium chloride 0.01%)] [Ocu-Zoline Sterile Ophthalmic Solution{36}] [Vasocon Regular{37}][Generic]

Canada—


0.1% (OTC) [Ak-Con{44} (polyvinyl alcohol)] [Albalon Liquifilm{45} (polyvinyl alcohol 1.4%)] [Naphcon Forte{46}] [Vasocon{47} (polyvinyl alcohol)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. Protect from freezing.

Stability:
Do not use if solution contains a precipitate or changes color.

Auxiliary labeling:
   • For the eye.
   • Keep container tightly closed.



Revised: 02/24/1994



References
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  1. FDC Reports. March 7, l988.
  1. Degest 2 package insert (Barnes-Hind—US), Rec 4/88.
  1. Vaso Clear package insert (CooperVision—US), Rev 1/82, Rec 4/86.
  1. Vasocon Regular package insert (Iolab—US), Rev 8/87, Rec 5/88.
  1. Allergy Drops package insert (Bausch & Lomb—US), Rec 5/87.
  1. Naphcon package insert (Alcon—US), Rec 4/87.
  1. Naphcon Forte package insert (Alcon—US), Rec 4/87.
  1. Albalon package insert (Allergan—US), Rev 7/85, Rec 3/87.
  1. Ak-Con package insert (Akorn—US), Rev 2/86, Rec 4/88.
  1. Clear Eyes package insert (Ross Laboratories—US), Rec 6/88.
  1. I-Naphline product list (International Pharmaceutical Products—US), Rev 1989.
  1. FDA Bulletin 3/28/88.
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  1. Allerest package insert (Pharmacraft—US), Rec 5/88.
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