ATC Class:S01GA01
VA Class:OP800
VA Class:NT100
Naphazoline hydrochloride, an imidazoline-derivative sympathomimetic amine, is a vasoconstrictor.
Naphazoline hydrochloride is used for self-medication to temporarily relieve nasal congestion associated with the common cold or upper respiratory allergy (e.g., hay fever).1008 Topical nasal decongestants provide only temporary relief of congestion, and some degree of rebound congestion usually results.1008 (See Cautions: Adverse Effects.)
Naphazoline hydrochloride is applied topically to the conjunctiva to temporarily relieve congestion, itching, and minor irritation. Ocular decongestants are ineffective in the treatment of delayed hypersensitivity reactions such as contact dermatoconjunctivitis. The vasoconstrictor effects of naphazoline may be used during some ocular diagnostic procedures, but some clinicians prefer phenylephrine to naphazoline for this use.
Ophthalmic solutions containing naphazoline in combination with antihistamines such as antazoline phosphate or pheniramine maleate and/or astringents such as zinc sulfate are commercially available. In the concentrations usually employed, zinc sulfate is a relatively ineffective antiseptic and may promote vasodilation.
Ophthalmic solutions of naphazoline hydrochloride are applied topically to the conjunctiva. Care must be taken to avoid contamination of the dropper tip. Some manufacturers recommend that contact lenses be removed before administration of ophthalmic solutions containing naphazoline.
Naphazoline hydrochloride nasal solutions are applied topically to the nasal mucosa.1008 To minimize the risk of spreading infection, containers should not be used by more than one person.1008
To produce nasal decongestion in adults and children 12 years of age or older, 1 or 2 drops of a 0.05% naphazoline hydrochloride solution may be instilled into each nostril.1008 Doses should not be repeated more frequently than every 6 hours.1008
To produce decongestion of the conjunctiva, 1-2 drops of a 0.1% ophthalmic solution of naphazoline hydrochloride may be applied topically to the conjunctiva every 3-4 hours as needed or 1 or 2 drops of a 0.01-0.03% ophthalmic solution may be applied topically to the conjunctiva up to 4 times daily or as directed by a physician.
The incidence of serious adverse effects is low in patients receiving therapeutic dosages of ophthalmic solutions of naphazoline hydrochloride. When naphazoline hydrochloride is used in combination preparations, the cautions applicable to each ingredient in the formulation must be observed. Excessive dosage and/or prolonged or too frequent use may irritate the conjunctiva and, especially in children, cause adverse systemic effects.
After intranasal application, naphazoline hydrochloride may cause transient burning, stinging, sneezing, or increased nasal discharge.1008 Frequent or prolonged use of naphazoline nasal solution may cause recurrence or exacerbation of nasal congestion.1008 Therefore, naphazoline nasal solution should not be used for longer than 3 days.1008
Use of naphazoline in the eye may cause blurred vision, mild transient stinging and/or irritation, mydriasis, and increased or decreased intraocular pressure. Conjunctival application of naphazoline, especially when high concentrations are used in geriatric patients, may liberate pigment granules, presumably from the iris. Rebound congestion, characterized by reactive hyperemia frequently occurs with prolonged use and may result in overuse of the drug. Prolonged use of the drug should be avoided for these reasons.
Ophthalmic use of naphazoline may occasionally cause systemic sympathomimetic effects such as headache, hypertension, cardiac irregularities, nervousness, nausea, dizziness, weakness, and sweating.
In pediatric patients, accidental ingestion of imidazoline derivatives (i.e., naphazoline, oxymetazoline, tetrahydrozoline) has resulted in serious adverse events requiring hospitalization (e.g., coma, bradycardia, decreased respiration, sedation, somnolence).1001, 1002, 1003, 1004, 1005, 1006, 1007 (See Cautions: Pediatric Precautions and also see Acute Toxicity.)
Precautions and Contraindications
Naphazoline hydrochloride ophthalmic solution should be used with caution in patients with hypertension, cardiovascular abnormalities, diabetes mellitus, hyperthyroidism, infection, or injury.
Patients using naphazoline hydrochloride ophthalmic solutions should be advised to discontinue the drug and consult a physician if ocular pain or visual changes occur, they experience continued ocular redness or irritation, the condition worsens or persists for more than 48 hours, or they experience manifestations of systemic absorption (e.g., headache, nausea, decrease in body temperature). Patients also should be informed that overuse of ophthalmic vasoconstrictors may produce increased redness of the eye (rebound hyperemia).
Serious adverse events requiring hospitalization have been reported in children following accidental ingestion of nonprescription (over-the-counter, OTC) ophthalmic or nasal solutions containing imidazoline derivatives (i.e., naphazoline, oxymetazoline, tetrahydrozoline).1001 (See Cautions: Pediatric Precautions and also see Acute Toxicity.) If accidental ingestion of naphazoline hydrochloride ophthalmic or nasal solution occurs, a poison control center should be contacted, and patients should be advised to seek emergency help immediately.1001
Naphazoline is contraindicated in patients with known hypersensitivity to the drug. Patients with glaucoma should be advised not to use naphazoline hydrochloride ophthalmic solutions except under the advice and supervision of a physician. Ophthalmic solutions of the drug should not be used in patients with angle-closure glaucoma. Fixed combinations containing naphazoline hydrochloride and antazoline are contraindicated while soft contact lenses are being worn.
Excessive dosage of topically applied naphazoline hydrochloride may cause marked sedation in children, and, if severe, symptomatic and supportive therapy should be initiated. One manufacturer states that 0.1% naphazoline hydrochloride ophthalmic solution is contraindicated in infants and children, since CNS depression possibly progressing to coma and hypothermia may occur in children, especially infants.
Serious adverse events requiring hospitalization have been reported in children following accidental ingestion of small amounts (1-2 mL) of nonprescription ophthalmic solutions or nasal sprays containing imidazoline derivatives (i.e., naphazoline, oxymetazoline, tetrahydrozoline).1001 Patients should be advised to keep naphazoline hydrochloride ophthalmic and nasal solutions out of the reach of children.1001 (See Cautions: Precautions and Contraindications and also see Acute Toxicity.)
Pregnancy, Fertility, and Lactation
Animal studies have not been conducted with naphazoline hydrochloride, and it is not known whether the drug can cause fetal harm when administered to a pregnant woman. Therefore, naphazoline hydrochloride should be used during pregnancy only when clearly needed.
It is not known whether naphazoline hydrochloride can affect reproduction capacity in humans.
It is not known whether naphazoline hydrochloride is distributed into milk. Because many drugs are distributed into milk, caution should be exercised when this drug is administered to a breast-feeding woman.
Concurrent use of maprotiline or tricyclic antidepressants with naphazoline hydrochloride may potentiate the pressor effects of naphazoline.
Patients being treated with monoamine oxidase (MAO) inhibitors may experience a severe hypertensive reaction if administered with a sympathomimetic drug. Although this reaction has not specifically been reported with naphazoline, the possibility of such an interaction should be considered.
The minimum toxic dose of imidazoline derivatives (e.g., naphazoline, oxymetazoline, tetrahydrozoline) has not been established in pediatric patients;1003 however, ingestion of 2-5 mL of a 0.05% tetrahydrozoline solution is capable of producing coma.1001
Serious adverse events requiring hospitalization have been reported in pediatric patients following accidental ingestion of nonprescription (over-the-counter, OTC) ophthalmic solutions or nasal sprays containing imidazoline derivatives (i.e., naphazoline, oxymetazoline, tetrahydrozoline).1001 Between 1985 and October 2012, 96 cases of accidental ingestion were reported in children 1 month to 5 years of a the amount of drug ingested ranged from 0.6-45 mL.1001 While no deaths were reported, more than half of these cases reported serious adverse events requiring hospitalization, including nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma.1001 Respiratory depression, CNS depression, and/or lethargy were reported in a 23-month-old and a 2-year-old infant following accidental ingestion of 6 and 2-3 mL, respectively, of 0.05% tetrahydrozoline ophthalmic solution;1002, 1007 in addition, urinary incontinence was reported in a 36-month-old child following accidental ingestion of 30 mL of 0.05% tetrahydrozoline ophthalmic solution.1004
Symptoms develop rapidly in children (i.e., within 15 minutes to 4 hours following ingestion) and generally resolve within 24 hours.1002, 1003, 1004 Imidazoline derivatives stimulate central and peripheral α-adrenergic receptors; therefore, symptoms of acute intoxication in children may alternate between CNS depression and agitation or hyperactivity.1006
Treatment of acute toxicity associated with imidazoline derivatives (e.g., naphazoline) is primarily symptomatic and supportive and is aimed at reversing the toxic cardiovascular and CNS effects of the drugs.1002 Cardiorespiratory resuscitation, including tracheal intubation and mechanical ventilation, is considered a mainstay of care for imidazoline-derivative intoxication.1002 Neurologic and hemodynamic status of the patient should be closely observed for at least 24 hours.1006
Because imidazoline derivatives are rapidly absorbed following ingestion, GI decontamination (e.g., activated charcoal, ipecac-induced emesis, gastric lavage) appears to have limited value.1002, 1006, 1007 However, if GI decontamination is used, some clinicians state that gastric lavage is preferred over induction of emesis.1002, 1007 Administration of activated charcoal and a cathartic is recommended by some clinicians; however, safety and efficacy of repeated administration of activated charcoal have not been established.1007
There is no known specific antidote for imidazoline-derivative intoxication.1006, 1007 Because symptoms of imidazoline-derivative and clonidine intoxication are similar and are mediated via the same central α2-adrenergic receptors, and because naloxone has been effective in reversing CNS depression in some instances of clonidine overdose, some clinicians have hypothesized that naloxone may be useful for the management of imidazoline-derivative intoxication.1003, 1004, 1006, 1007 However, data are limited and conflicting, and the role of naloxone in the management of imidazoline-derivative intoxication remains to be established.1002, 1004, 1006, 1007
The mechanism of action of naphazoline has not been conclusively determined. Most pharmacologists believe that the drug directly stimulates α-adrenergic receptors of the sympathetic nervous system and exerts little or no effect on β-adrenergic receptors. Following topical application of naphazoline to the conjunctiva, small arterioles are constricted and conjunctival congestion is temporarily relieved, but reactive hyperemia may occur. The drug also may produce mydriasis when applied to the conjunctiva, but this effect is usually minimal with the concentrations used as ocular decongestants.
Following topical application of naphazoline hydrochloride solutions to the conjunctiva, local vasoconstriction usually occurs within 10 minutes and may persist for 2-6 hours. Occasionally, enough naphazoline may be absorbed to produce systemic effects. Information on the distribution and elimination of the drug in humans is not available.
Naphazoline hydrochloride is an imidazoline derivative sympathomimetic amine which is structurally and pharmacologically related to oxymetazoline, tetrahydrozoline, and xylometazoline. Naphazoline hydrochloride occurs as a white, odorless, crystalline powder having a bitter taste and is freely soluble in water and in alcohol. Naphazoline hydrochloride ophthalmic solutions are sterile, buffered solutions of the drug in water adjusted to a suitable pH and tonicity; the commercially available ophthalmic solutions also contain a suitable preservative (e.g., benzalkonium chloride). Naphazoline hydrochloride ophthalmic solutions have a pH of 5.5-7.
Naphazoline hydrochloride ophthalmic solutions should be protected from light and should be stored in tight, light-resistant containers. The drug is degraded in the presence of aluminum and, therefore, should not be stored in aluminum containers. Discolored or cloudy solutions of the drug should not be used. Fixed combinations containing naphazoline hydrochloride and antazoline phosphate should be stored at temperatures less than 25°C.
Naphazoline hydrochloride nasal solutions should be stored at room temperature (20-25°C).1008
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
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
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 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 |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions February 28, 2014. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
Only references cited for selected revisions after 1984 are available electronically.
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. [Web]
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. Insight Pharmaceuticals website. Accessed 2013 Oct 22. [Web]