Oxymetazoline (Ophthalmic)


VA CLASSIFICATION
Primary: OP802

Commonly used brand name(s): OcuClear; Visine L.R.

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



Category:


Decongestant (ophthalmic){02}

Indications

Accepted

Ocular redness{16}{17} (treatment)—Oxymetazoline is indicated for the temporary relief of redness {16} {17} {28} associated with minor irritations of the eye, {16} such as those caused by pollen-related allergies, colds, dust, smog, wind, swimming, or wearing contact lenses.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Molecular weight—
    260.37 {07}

Mechanism of action/Effect:

Oxymetazoline is a direct-acting sympathomimetic amine. It acts on alpha-adrenergic receptors in the arterioles of the conjunctiva to produce vasoconstriction, resulting in decreased conjunctival congestion. {01} {02} {07} {10}

Onset of action:

Within 5 minutes. {01}

Duration of action:

Approximately 6 hours. {01}


Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to other ophthalmic sympathomimetics may be sensitive to this medication also. {02}

Pregnancy/Reproduction

Pregnancy—
Oxymetazoline may be systemically absorbed.

Studies have not been done in humans or animals.

Breast-feeding

Problems in humans have not been documented; however, oxymetazoline may be systemically absorbed. {10}

Pediatrics

Check with physician before using oxymetazoline ophthalmic solution in children up to 6 years of age. Eye redness in children can occur with illnesses, such as allergies, fevers, colds, and measles, that may require medical attention. {01} {24} {25}


Geriatrics


Appropriate studies on the relationship of age to the effects of oxymetazoline 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):

Antidepressants, tricyclic or{12}
Maprotiline    (if significant systemic absorption of ophthalmic oxymetazoline occurs, concurrent use may potentiate the pressor effect of oxymetazoline {10})


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).


Risk-benefit should be considered when the following medical problems exist
Coronary artery disease or{02}{10}
Heart disease, including angina or{02}{10}
Hypertension{02}{10}    (if significant systemic absorption of ophthalmic oxymetazoline occurs, condition may be exacerbated due to drug-induced cardiovascular effects)


Eye disease, infection, or injury{01}{02}    (may mask symptoms and delay treatment {14})


Glaucoma, narrow-angle, or predisposition to{01}{02}    (may precipitate an attack by dilating pupil {14})


Hyperthyroidism{02}{10}    (may exacerbate existing tachycardia or elevated blood pressure {14})


Sensitivity to oxymetazoline


Side/Adverse Effects

Note: Excessive dosage and/or prolonged use may cause increased irritation of the conjunctiva. {02} Prolonged use may also cause reactive hyperemia. {01} {02} {23}

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{01}{02} (increase in irritation or redness of eyes)

Symptoms of systemic absorption {10}
    
Fast, irregular, or pounding heartbeat{10}
    
headache or lightheadedness{10}
    
nervousness{10}
    
trembling{10}
    
trouble in sleeping{10}





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

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

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to oxymetazoline or any other eye decongestant





Use in children—Checking with physician before using medication in children up to 6 years of age; eye redness in children can occur with illnesses, such as allergies, fevers, colds, and measles, that may require medical attention


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

Proper administration technique

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

» Importance of not using more medication than the amount recommended and not using for more than 72 hours, unless directed to do so by physician; overuse may increase eye irritation and the chance of side effects

» 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
Side effects usually are rare when medication is used for short periods of time at low doses

Signs of potential side effects, especially reactive hyperemia or symptoms of systemic absorption


General Dosing Information
Treatment should not be continued for more than 72 hours {17} unless otherwise directed by physician. {02} {14}

Although the manufacturer recommends that patients remove soft contact lenses before using oxymetazoline ophthalmic solution, USP medical experts do not believe this precaution is necessary unless the patient has corneal epithelial problems. 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 eye drops in patients with no significant corneal surface problem. {02} {14}


Ophthalmic Dosage Forms

OXYMETAZOLINE HYDROCHLORIDE OPHTHALMIC SOLUTION USP{04}

Usual adult and adolescent dose
Topical, to the conjunctiva, 1 drop of a 0.025% solution every six hours as needed, or as directed by physician. {28}

Usual pediatric dose
Children up to 6 years of age—Dosage must be individualized by physician. {01} {28}

Children 6 years of age and older—See Usual adult and adolescent dose{28} .

Strength(s) usually available
U.S.—


0.025% (OTC) [Visine L.R.{28} (boric acid) (edetate disodium) (sodium borate) (sodium chloride){28}]

Canada—


0.025% (OTC) [OcuClear{29} (boric acid) (disodium edetate) (hydrochloric acid and/or sodium hydroxide) (sodium chloride){29}]

Packaging and storage:
Store between 15 and 30 °C (59 and 86 °F), {28} unless otherwise specified by manufacturer. Store in a tight container. {01} {08} Protect from freezing. {02}

Stability:
Do not use if solution contains a precipitate or changes color. {01} {02}

Auxiliary labeling:
   • For the eye.
   • Keep container tightly closed. {01} {02}



Revised: 08/13/1998



References
  1. OcuClear package insert (Schering—US), Rev 1988, Rec 6/88.
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  1. The United States pharmacopeia. The national formulary. 22nd revision (January 1, l990). Rockville, MD: The United States Pharmacopeial Convention, Inc.; 1990. p. 993.
  1. OPEN.
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  1. Budavar S, editor. The Merck index. An encyclopedia of chemicals, drugs, and biological. 10th ed. Rahway, NJ: Merck Research Laboratories; l983. p. 6838.
  1. Reynolds JEF, editor. Martindale, the extra pharmacopeia. 28th ed. London: The Pharmaceutical Press; 1982. p. 23.
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  1. Panel comments, 3/26/87.
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  1. FDC Reports, March 7, l988.
  1. FDA Bulletin, 3/28/88.
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  1. OPEN.
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  1. Reviewer's comment.
  1. OcuClear eye drops (Schering). In: PDR Physicians' desk reference for ophthalmology. 19th ed. Montvale, NJ: Medical Economics Data; 1991.
  1. Visine L.R. eye drops (Pfizer Consumer). In: PDR Physicians' desk reference for ophthalmology. 19th ed. 1991. Montvale, NJ: Medical Economics Data; 1991.
  1. OPEN.
  1. OPEN.
  1. Visine L.R. (Pfizer). In: PDR Physicians' desk reference for nonprescription products. 19th ed. 1998. Montvale, NJ: Medical Economics Company; 1998. p. 724.
  1. Ocuclear (Schering). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 33rd. ed. Ottawa: Canadian Pharmaceutical Association; 1998. p. 1202.
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