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Naphazoline and antazoline (ophthalmic) (United States: Not available): Drug information

Naphazoline and antazoline (ophthalmic) (United States: Not available): Drug information
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For additional information see "Naphazoline and antazoline (ophthalmic) (United States: Not available): Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: Canada
  • Refresh Eye Allergy Relief [OTC]
Pharmacologic Category
  • Alpha1 Agonist;
  • Ethylenediamine Derivative;
  • Histamine H1 Antagonist;
  • Histamine H1 Antagonist, First Generation;
  • Imidazoline Derivative;
  • Ophthalmic Agent, Vasoconstrictor
Dosing: Adult
Ocular redness/allergies

Ocular redness/allergies: Ophthalmic: Instill 1 to 2 drops in affected eye(s) every 3 to 4 hours (or less frequently).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Liver Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions are derived from product labeling unless otherwise specified.

Frequency not defined:

Cardiovascular: Cardiac disorder, hypertension

Endocrine & metabolic: Hyperglycemia

Ophthalmic: Mydriasis (with increase in intraocular pressure)

Postmarketing: Ophthalmic: Corneal opacity (Herman 1987)

Contraindications

Hypersensitivity to naphazoline, antazoline, or any component of the formulation; glaucoma; use in children (unless under medical advice)

Warnings/Precautions

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with cardiac disease or hypertension (sympathomimetic effects may increase blood pressure).

• Diabetes: Use with caution in patients with diabetes.

• Thyroid disease: Use with caution in patients with hyperthyroidism.

Dosage form specific issues:

• Benzalkonium chloride: May contain benzalkonium chloride which may be absorbed by soft contact lenses.

Other warnings/precautions:

• 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).

• 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.

Product Availability

Not available in the US

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic:

Refresh Eye Allergy Relief: Naphazoline (as hydrochloride) 0.051% and antazoline (as phosphate) 0.51% (15 mL) [contains benzalkonium chloride]

Administration: Adult

Ophthalmic: Wash hands before use. Do not touch tip of container to eye. Remove contact lenses prior to administration. After instilling drops, wait before inserting contact lenses. Do not insert contacts if eyes are red.

Use: Labeled Indications

Note: Not approved in the US

Ocular redness/allergies: Temporary symptomatic relief of tearing, redness, swelling and itching associated with ocular allergies.

Metabolism/Transport Effects

Refer to individual components.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Atomoxetine: May increase hypertensive effects of Sympathomimetics. Atomoxetine may increase tachycardic effects of Sympathomimetics. Risk C: Monitor

Atropine (Systemic): May increase hypertensive effects of Alpha1-Agonists. Risk C: Monitor

Bornaprine: Sympathomimetics may increase anticholinergic effects of Bornaprine. Risk C: Monitor

Bromocriptine: May increase hypertensive effects of Alpha1-Agonists. Management: Consider alternatives to this combination when possible. If combined, monitor for hypertension and tachycardia, and do not coadminister these agents for more than 10 days. Risk D: Consider Therapy Modification

Cannabinoid-Containing Products: May increase tachycardic effects of Sympathomimetics. Risk C: Monitor

Cocaine (Topical): May increase hypertensive effects 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. Risk D: Consider Therapy Modification

Dihydralazine: Sympathomimetics may decrease therapeutic effects of Dihydralazine. Risk C: Monitor

Doxofylline: Sympathomimetics may increase adverse/toxic effects of Doxofylline. Risk C: Monitor

Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): May increase vasoconstricting effects of Alpha1-Agonists. Risk X: Avoid

Esketamine (Injection): May increase adverse/toxic effects of Sympathomimetics. Specifically, the risk for elevated heart rate, hypertension, and arrhythmias may be increased. Risk C: Monitor

Guanethidine: May increase hypertensive effects of Sympathomimetics. Guanethidine may increase arrhythmogenic effects of Sympathomimetics. Risk C: Monitor

Iobenguane Radiopharmaceutical Products: Alpha1-Agonists may decrease therapeutic effects 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. Risk X: Avoid

Kratom: May increase adverse/toxic effects of Sympathomimetics. Risk X: Avoid

Levothyroxine: May increase therapeutic effects of Sympathomimetics. Sympathomimetics may increase therapeutic effects of Levothyroxine. Levothyroxine may increase adverse/toxic effects of Sympathomimetics. Specifically, the risk of coronary insufficiency may be increased in patients with coronary artery disease. Risk C: Monitor

Linezolid: May increase hypertensive effects of Sympathomimetics. Management: Consider initial dose reductions of sympathomimetic agents, and closely monitor for enhanced blood pressure elevations, in patients receiving linezolid. Risk D: Consider Therapy Modification

Lisuride: May increase hypertensive effects of Alpha1-Agonists. Risk X: Avoid

Monoamine Oxidase Inhibitors: May increase hypertensive effects 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. Risk X: Avoid

Pergolide: May increase hypertensive effects of Alpha1-Agonists. Risk C: Monitor

Solriamfetol: Sympathomimetics may increase hypertensive effects of Solriamfetol. Sympathomimetics may increase tachycardic effects of Solriamfetol. Risk C: Monitor

Sympathomimetics: May increase adverse/toxic effects of Sympathomimetics. Risk C: Monitor

Tedizolid: May increase adverse/toxic effects of Sympathomimetics. Specifically, the risk for increased blood pressure and heart rate may be increased. Risk C: Monitor

Tricyclic Antidepressants: May increase therapeutic effects of Alpha1-Agonists. Tricyclic Antidepressants may decrease therapeutic effects of Alpha1-Agonists. Risk C: Monitor

Pregnancy Considerations

Refer to individual monographs.

Breastfeeding Considerations

Refer to individual monographs.

Mechanism of Action

Naphazoline stimulates alpha-adrenergic receptors in the arterioles of the conjunctiva.

Antazoline inhibits histamine induced effects on conjunctival epithelial cells.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (MX) Mexico: Midazol ofteno;
  • (PE) Peru: Red off plus;
  • (QA) Qatar: Ocured | Ophtazolin;
  • (RU) Russian Federation: Allergophtal
  1. 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. U.S. Food and Drug Administration. October 25, 2012. Available at http://www.fda.gov/Drugs/DrugSafety/ucm325257.htm. Accessed May 3, 2016.
  2. Herman DC, Bartley GB. Corneal opacities secondary to topical naphazoline and antazoline (Albalon-A). Am J Ophthalmol. 1987;103(1):110-111. doi:10.1016/s0002-9394(14)74185-6 [PubMed 3799780]
  3. Refresh Eye Allergy Relief (naphazoline and antazoline) [product monograph]. Allergan Canada Inc; received May 3, 2016.
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