Oxymetazoline Hydrochloride

Class: Vasoconstrictors
VA Class: NT100
CAS Number: 2315-02-8
Brands: Afrin No Drip Extra Moisturizing, Afrin No Drip Original, Afrin No Drip Severe Congestion, Afrin No Drip Sinus, Afrin Original, Afrin Severe Congestion, Afrin Sinus, Dristan 12 Hour, Neo-Synephrine 12 Hour Severe Sinus Congestion, Nostrilla 12 Hour Nasal Decongestant, Vicks Sinex 12 Hour Nasal Decongestant, Visine L.R. Eye Drops, Zicam Extreme Congestion Relief, Zicam Intense Sinus Relief

Introduction

Vasoconstrictor;a an imidazoline-derivative sympathomimetic amine.a

Uses for Oxymetazoline Hydrochloride

Nasal Congestion

Self-medication for temporary relief of nasal congestion associated with the common cold, hay fever, or other upper respiratory allergies.111

As effective as other topical vasoconstrictors.a

Labeled and has been used for self-medication for temporary relief of nasal congestion associated with sinusitis;107 111 however, efficacy data are lacking and/or controversial.107 108 109 In October 2005, FDA issued final rule to remove this indication from labeling of OTC nasal decongestants.107 Compliance date for preparations with annual sales <$25,000 is October 11, 2007; compliance date for all other preparations is April 11, 2007.107

Slideshow: Fact or Fiction? The Top 15 Osteoarthritis Myths

Conjunctival Congestion

Self-medication for temporary relief of ocular redness due to minor irritation.112

Otitic Barotrauma

Has been used for self-medication for symptomatic prevention of otitic barotrauma (aerotitis [barotitis] media);101 103 105 however, no more effective than placebo.101

Oxymetazoline Hydrochloride Dosage and Administration

Administration

Administer topically to nasal mucosa or conjunctiva.a 111 112

Intranasal Administration

Administer nasal solution intranasally as sprays or nasal pumps.a

Prior to initial use of metered sprays, prime nasal inhaler by depressing the pump firmly several times.a

Administer nasal spray or pump into each nostril while head is erect.a

Ophthalmic Administration

Administer ophthalmic solution topically to the conjunctiva.a 112

Avoid contamination of the dropper tip.112

Remove contact lenses before administering ophthalmic solution.a 112

Do not administer discolored or cloudy solutions.112

Dosage

Available as oxymetazoline hydrochloride; dosage expressed in terms of the salt.111 112

Pediatric Patients

Nasal Congestion
Intranasal

For self-medication in children ≥6 years of age: 2 or 3 sprays of a 0.05% nasal solution in each nostril every 10–12 hours (usually in the morning and evening), up to 2 times daily.a 111

Conjunctival Congestion
Ophthalmic

For self-medication in children ≥6 years of age: 1 or 2 drops of a 0.025% ophthalmic solution in the affected eye(s) every 6 hours as needed.112

Adults

Nasal Congestion
Intranasal

For self-medication: 2 or 3 sprays of a 0.05% nasal solution in each nostril every 10–12 hours (usually in the morning and evening), up to 2 times daily.a 111

Conjunctival Congestion
Ophthalmic

For self-medication: 1 or 2 drops of a 0.025% ophthalmic solution in the affected eye(s) every 6 hours as needed.112

Prescribing Limits

Pediatric Patients

Nasal Congestion
Intranasal

Self-medication in children ≥6 years of age: Maximum of 2 times (2 doses) in a 24-hour period.111 (See Advice to Patients.)

Adults

Nasal Congestion
Intranasal

Self-medication: Maximum of 2 times (2 doses) in a 24-hour period.111 (See Advice to Patients.)

Cautions for Oxymetazoline Hydrochloride

Contraindications

  • Known hypersensitivity to oxymetazoline or any ingredient in the formulation.a

  • Known sensitivity to the pharmacologic effects of adrenergic drugs.a

Warnings/Precautions

General Precautions

Overuse

Possible irritation of nasal mucosa and adverse systemic effects (particularly in children) with excessive dosage and/or prolonged or too frequent intranasal use.a Possible rebound nasal congestion or ocular hyperemia (redness);a 111 112 avoid prolonged use.a (See Advice to Patients.)

Accidental ingestion of imidazoline derivatives (i.e., oxymetazoline, naphazoline, tetrahydrozoline) in children has resulted in serious adverse events requiring hospitalization (e.g., coma, bradycardia, decreased respiration, sedation, somnolence).1001 1002 1003 1004 1005 1006 1007 (See Pediatric Use under Cautions and also see Advice to Patients.)

Sympathomimetic Effects

With intranasal use, possible headache, hypertension, cardiac irregularities (e.g., palpitation, reflex bradycardia), nervousness, nausea, dizziness, and insomnia.a Use with caution and under direction of a clinician in patients with thyroid disease (e.g., hyperthyroidism), heart disease (including angina), hypertension, advanced arteriosclerotic conditions, or diabetes mellitus; in patients experiencing difficulty in urination secondary to prostatic enlargement; or in patients receiving monoamine oxidase (MAO) inhibitors.a 111

Glaucoma

Patients with narrow-angle glaucoma should consult a clinician before using ophthalmic solution.112

Specific Populations

Pregnancy

Category C.114

Lactation

Not known whether oxymetazoline is distributed into milk.114 Use with caution in nursing women.113

Pediatric Use

0.05% nasal solution or 0.025% ophthalmic solution not recommended for self-medication in children <6 years of age.111 112

Possible irritation of nasal mucosa and adverse systemic effects (including profound CNS depression) associated with excessive dosage, prolonged or too frequent use, or inadvertent ingestion of nasal solution.a

Accidental ingestion of OTC ophthalmic solutions or nasal sprays containing imidazoline derivatives (i.e., oxymetazoline, naphazoline, tetrahydrozoline) in children has resulted in serious adverse events requiring hospitalization, including nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma.1001 Keep out of reach of children.1001 (See Advice to Patients.)

Common Adverse Effects

Nasal solution: transient burning, stinging, sneezing, increased nasal discharge or dryness of nasal mucosa.a 111

Oxymetazoline Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Occasionally, absorption may be sufficient to produce systemic effects.a

Onset

Following intranasal administration, local vasoconstriction usually occurs within 5–10 minutes.a

Following ocular administration, local vasoconstriction usually occurs within minutes.a

Duration

Following intranasal administration, local vasoconstriction persists for 5–6 hours, with gradual decline over the next 6 hours.a

Following ophthalmic administration, local vasoconstriction persists for up to 6 hours.a

Stability

Storage

Nasal

Solution

Room temperature (<40°C); avoid freezing.a 111 Protect from light.111

Ophthalmic

Solution

15–30°C;112 do not store in aluminum containers.a

Actions

  • Structurally and pharmacologically related to naphazoline, tetrahydrozoline, and xylometazoline.a

  • Directly stimulates α-adrenergic receptors; exerts little or no effect on β-adrenergic receptors.a

  • Constricts dilated arterioles, reduces nasal blood flow and congestion, and opens obstructed eustachian ostia.a Temporarily relieves nasal and conjunctival congestion following topical application.a

Advice to Patients

  • With intranasal use, importance of discontinuing drug and consulting a clinician if nasal congestion worsens or persists for >3 days.111

  • With ophthalmic use, importance of discontinuing drug and consulting a clinician if ocular pain or visual changes occur or if ocular redness or irritation worsens or persists for >72 hours.112

  • Overuse of nasal solution may cause recurrence or exacerbation of nasal congestion;111 overuse of ophthalmic solution may produce increased redness of the eye.112

  • Importance of removing contact lenses prior to administration of ophthalmic solution.a 112

  • Importance of avoiding contamination of the dropper, inhaler, or spray dispenser.a 111 112 Do not touch dropper tip to any surface;112 rinse inhaler/spray dispenser tip with hot water or wipe clean following use.a To minimize risk of spreading infections, do not share dropper, inhaler, or spray dispenser with other individuals.a 111

  • Importance of calling clinician or poison control center if ingested.1001 Importance of seeking emergency help immediately.1001

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.a

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.a

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Oxymetazoline Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Solution

0.05%*

Afrin No Drip Extra Moisturizing 12 Hour Pump Mist

Schering-Plough

Afrin No Drip Original 12 Hour Pump Mist

Schering-Plough

Afrin No Drip Severe Congestion 12 Hour Pump Mist

Schering-Plough

Afrin No Drip Sinus 12 Hour Pump Mist

Schering-Plough

Afrin Original 12 Hour Spray

Schering-Plough

Afrin Severe Congestion 12 Hour Spray

Schering-Plough

Afrin Sinus 12 Hour Spray

Schering-Plough

Dristan 12 Hour Nasal Spray

Pfizer

Neo-Synephrine 12 Hour Severe Sinus Congestion Spray

Bayer

Nostrilla 12 Hour Nasal Decongestant Metered Pump Spray

Insight

Oxymetazoline Hydrochloride Nasal Solution

Vicks Sinex 12 Hour Nasal Decongestant Spray (with regular or metered pump mist spray)

Procter & Gamble

Zicam Extreme Congestion Relief Nasal Gel

Matrixx

Zicam Intense Sinus Relief Nasal Gel

Matrixx

Ophthalmic

Solution

0.025%

Visine L.R. Eye Drops

Pfizer

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions February 20, 2014. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

100. Csortan E, Jones J, Haan M et al. Efficacy of pseudoephedrine for the prevention of barotrauma during air travel. Ann Emerg Med. 1994; 23:1324-7. [IDIS 330837] [PubMed 8198308]

101. Jones JS, Sheffield W, White LJ et al. A double-blind comparison between oral pseudoephedrine and topical oxymetazoline in the prevention of barotrauma during air travel. Am J Emerg Med. 1998; 16:262-4. [IDIS 407003] [PubMed 9596428]

102. Brown M, Jones K, Krohmer J. Pseudoephedrine for the prevention of barotitis media: a controlled clinical trial in underwater divers. Ann Emerg Med. 1992; 21:849-52. [PubMed 1610044]

103. Capes JP and Tomaszewski C. Prophylaxis against middle ear barotrauma in US in hyperbaric oxygen therapy centers. Am J Emerg Med. 1996; 14:645-8. [PubMed 8906761]

104. Newton HB. Neurologic complications of scuba diving. Am Fam Physician. 2001; 63:2211-8. [PubMed 11417773]

105. Carlson S, Jones J, Brown M et al. Prevention of hyperbaric-associated middle ear barotrauma. Ann Emerg Med. 1992; 21:1468-71. [PubMed 1443845]

106. Bettes TN and McKenas DK. Medical advice for commercial air travelers. Am Fam Physician. 1999; 60:801-10. [PubMed 10498108]

107. Food and Drug Administration. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; amendment of final monograph for over-the-counter nasal decongestant drug products. 21 CFR Parts 310 and 341. Final rule. [Docket No. 2004N- 0289] Fed Regist. 2005; 70:58974-7.

108. Spector SL, Bernstein IL, Li JT et al for the Joint Task Force on Practice Parameters, representing the American Academy of Allergy, Asthma and Immunology, the American College of Allergy, Asthma and Immunology, and the Joint Council of Allergy, Asthma and Immunology. Parameters for the diagnosis and management of sinusitis. J Allergy Clin Immunol. 1998; 102(Suppl):S107-44. [PubMed 9847450]

109. American Academy of Pediatrics: subcommittee on management of sinusitis and committee on quality improvement. Clinical practice guideline: Management of sinusitis. Pediatrics. 2001; 108:798-808. [PubMed 11533355]

110. Benninger MS, Anon J, Mabry RL. The medical management of rhinosinusitis. Otolaryngol Head Neck Surg. 1997; 117(Suppl):S41-9. [PubMed 9334787]

111. Neo-Synephrine 12 Hour (oxymetazoline hydrochloride) 0.05% nasal solution prescribing information. In PDR.net [database online]. Montvale, NJ: Thomson Healthcare; 2003. Updated 2003 Oct.

112. Visine L.R. Long Lasting (oxymetazoline hydrochloride) 0.025% ophthalmic solution prescribing information. In PDR.net [database online]. Montvale, NJ: Thomson Healthcare; 2003. Updated 2003 Oct.

113. Wickersham, RM. Drug Facts and Comparisons. 2003. St Louis, MO: Facts and Comparisons; 2003: page 685.

114. Briggs GG, Freeman RK, Yaffe SJ. Drugs in pregnancy and lactation. 7th ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2005:1227-8.

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.

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]

a. AHFS Drug Information 2014. McEvoy GK, ed. Oxymetazoline Hydrochloride. Bethesda, MD: American Society of Health System Pharmacists.

Hide
(web1)