Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Ophthalmic, as hydrochloride:
Clear Eyes Redness Relief: Naphazoline 0.0125% and glycerin 0.2% (6 mL) [contains benzalkonium chloride]
GoodSense Redness Relief Plus: Naphazoline 0.03% and glycerin 0.5% (15 mL) [contains benzalkonium chloride, edetate disodium]
Generic: 0.1% (15 mL [DSC])
Pharmacology
Mechanism of Action
Stimulates alpha-adrenergic receptors in the arterioles of the conjunctiva and the nasal mucosa to produce vasoconstriction
Use: Labeled Indications
Decrease in eye redness (vasoconstrictor):
Rx: Topical ocular vasoconstrictor.
OTC: Relief of redness of the eye due to minor irritation; temporary relief of burning and irritation due to dry eyes; as a protectant against further irritation or dryness of the eye.
Contraindications
Hypersensitivity to naphazoline or any component of the formulation; narrow-angle glaucoma or anatomically narrow angle
Documentation of allergenic cross-reactivity for ophthalmic vasoconstrictors is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity can not be ruled out with certainty.
Dosage and Administration
Dosing: Adult
Decrease in eye redness (vasoconstrictor): Ophthalmic:
Rx: 0.1% solution: 1 to 2 drops into conjunctival sac every 3 to 4 hours as needed
OTC: 0.012% or 0.03% solution: 1 to 2 drops into affected eye(s) up to 4 times daily
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Ocular redness, irritation: Limited data available: Children ≥6 years and Adolescents: Ophthalmic solution 0.012% to 0.03% (OTC products): Instill 1 to 2 drops in affected eye up to four times daily (Kliegman 2016)
Administration
For topical ophthalmic use only. Remove contact lenses prior to administration. Do not touch tip of container to any surface, the eyelids, or the surrounding area. Do not use if solution changes color or becomes cloudy.
Storage
Store at room temperature.
Drug Interactions
Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Monitor therapy
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Consider therapy modification
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Monitor therapy
Ergot Derivatives: May enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. Avoid combination
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Monitor therapy
Iobenguane Radiopharmaceutical Products: Alpha1-Agonists may diminish the therapeutic effect of Iobenguane Radiopharmaceutical Products. Management: Discontinue all drugs that may inhibit or interfere with catecholamine transport or uptake for at least 5 biological half-lives before iobenguane administration. Do not administer these drugs until at least 7 days after each iobenguane dose. Avoid combination
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of Alpha1-Agonists. While linezolid is expected to interact via this mechanism, management recommendations differ from other monoamine oxidase inhibitors. Refer to linezolid specific monographs for details. Exceptions: Linezolid. Avoid combination
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Tricyclic Antidepressants: May enhance the therapeutic effect of Alpha1-Agonists. Tricyclic Antidepressants may diminish the therapeutic effect of Alpha1-Agonists. Monitor therapy
Adverse Reactions
Frequency not defined: Ophthalmic: Blurred vision, eye discomfort, eye irritation, eye redness, increased intraocular pressure, lacrimation, mydriasis, punctuate keratitis
Warnings/Precautions
Disease-related concerns:
- Cardiovascular disease: Use with caution in patients with cardiovascular abnormalities or hypertension.
- Diabetes: Use with caution in patients with diabetes mellitus.
- Hyperthyroidism: Use with caution in patients with hyperthyroidism.
- Infection/injury: Use with caution in patients with local infection or injury.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Dosage form specific issues:
- Benzalkonium chloride: May contain benzalkonium chloride which may be absorbed by soft contact lenses.
Other warnings/precautions:
- Appropriate use: For topical ophthalmic use only. Do not touch tip of container to any surface, the eyelids, or the surrounding area. Discontinue use and notify health care provider if symptoms worsen or persist >48 hours (>72 hours [OTC]) or if symptoms of systemic absorption occur (ie, dizziness, headache, nausea, decrease in body temperature, drowsiness). Overuse may produce increased redness of the eye; pupils may become enlarged temporarily.
- Self-medication (OTC use): Discontinue use and contact health care provider if eye pain or changes in vision occur.
- Accidental ingestion: Accidental ingestion by children of nonprescription (OTC) imidazoline-derivative eye drops and nasal sprays may result in serious harm. Serious adverse reactions (eg, coma, bradycardia, respiratory depression, sedation) requiring hospitalization have been reported in children ≤5 years of age who had ingested even small amounts (eg, 1 to 2 mL). Contact a poison control center and seek emergency medical care immediately for accidental ingestion (FDA Drug Safety Communication, 2012).
Pregnancy
Pregnancy Risk Factor
C
Pregnancy Considerations
Animal reproduction studies have not been conducted.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience enlarged pupils. Have patient report immediately to prescriber vision changes, eye pain, or severe eye irritation (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
