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Tetrahydrozoline Hydrochloride

Class: Vasoconstrictors
VA Class: NT100
CAS Number: 522-48-5
Brands: Murine Plus, Optigene 3, Tyzine, Visine, Visine A.C.

Warning(s)

Special Alerts:

[Posted 10/25/2012] ISSUE: FDA is warning healthcare professionals and the public that accidental ingestion by children of over-the-counter eye drops used to relieve redness and nasal decongestant sprays can result in serious and life-threatening adverse events. The eye drops and nasal sprays that have been involved in the cases of accidental ingestion contain the active ingredients tetrahydrozoline, oxymetazoline, or naphazoline. The cases of accidental ingestion reviewed by FDA occurred in children 5 years of age and younger. No deaths were reported; however, serious events requiring hospitalization such as nausea, vomiting, lethargy, tachycardia, decreased respiration, bradycardia, hypotension, hypertension, sedation, somnolence, mydriasis, stupor, hypothermia, drooling, and coma have occurred. Ingestion of only a small amount (1-2 mL; for reference, there are 5 mL in a teaspoon) of the eye drops or nasal spray can lead to serious adverse events in young children.

BACKGROUND: Most of these redness-relief eye drops and nasal decongestant sprays currently do not come packaged with child-resistant closures, so children can accidentally ingest the drug if the bottles are within easy reach. These products are sold under various brand names, as generics, and as store brands (see List of Products, included in the Drug Safety Communication, at: ).

RECOMMENDATION: Consumers should store these products out of reach of children at all times. If a child accidentally swallows OTC redness-relief eye drops or nasal decongestant spray, call your local poison control center (1-800-222-1222) immediately. Experts are available all day, every day at these centers. For more information visit the FDA website at: and .

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.101 a

Uses for Tetrahydrozoline Hydrochloride

Nasal Congestion

Temporary relief of nasal congestion.101 a

As effective as other topical vasoconstrictors.a

Nasal decongestants often preferred for short-term treatment; oral agents preferred for prolonged treatment.a (See Overuse under Cautions.)

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Reduce swelling and facilitate visualization of nasal and pharyngeal membranes prior to surgery or diagnostic procedures.a

Open obstructed eustachian ostia in ear inflammation.a

Conjunctival Congestion

Temporary relief of conjunctival congestion, itching, and minor irritation.102 a

Used alone or in fixed combination with astringents (i.e., zinc sulfate).a c

Controls hyperemia in patients with superficial corneal vascularity.a

Ineffective in the treatment of delayed hypersensitivity reactions such as contact dermatoconjunctivitis.a

Used for vasoconstrictor effect during some ocular diagnostic procedures; phenylephrine may be preferred.a

Tetrahydrozoline Hydrochloride Dosage and Administration

Administration

Apply topically to nasal mucosa 101 a or to conjunctiva.102 a c

Avoid contamination of the dropper tip or spray dispenser.102 a c

Intranasal Administration

Apply topically to the nasal mucosa as drops or spray.101 a

Nasal sprays preferable due to a decreased risk of swallowing the drug and resultant systemic absorption; however, drops are easier to administer to young children.a

Apply nasal drops to the dependent (lower) nostril with the patient in a lateral, head-low position.101 a Remain in the same position for 5 minutes, then apply drops to the other nostril in a similar manner.a Alternatively, instill drops while in a reclining position, with head tilted back as far as possible.a

Administer nasal spray into each nostril while head is erect.101 a Squeeze bottle quickly and firmly and sniff briskly;101 blow nose thoroughly after 3–5 minutes.a

Rinse tips of dispensers or droppers thoroughly with hot water following use.a

Ophthalmic Administration

Apply ophthalmic solution topically to the conjunctiva.a

Remove contact lenses before administering ophthalmic solution;102 c wait ≥15 minutes to reinsert contact lenses.b

Do not administer discolored or cloudy solution.102 c

Dosage

Available as tetrahydrozoline hydrochloride; dosage expressed in terms of the salt.a

Pediatric Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Nasal Congestion
Intranasal

Children 2–5 years of age: 2–3 drops of a 0.05% solution in each nostril every 3–6 hours (typically 4–6 hours) as needed.101

Children ≥6 years of age: 2–4 drops or 3–4 sprays of a 0.1% solution in each nostril every 3–8 hours (typically 4–8 hours) as needed.101

Conjunctival Congestion
Ophthalmic

Children ≥6 years of age: 1–2 drops of a 0.05% ophthalmic solution in the affected eye(s) up to 4 times daily.102 a c

Adults

Nasal Congestion
Intranasal

2–4 drops or 3–4 sprays of 0.1% solution in each nostril every 3–8 hours (typically 4–8 hours) as needed.101 a

Conjunctival Congestion
Ophthalmic

1–2 drops of a 0.05% ophthalmic solution in the affected eye(s) up to 4 times daily.102 a c

Prescribing Limits

Pediatric Patients

Nasal Congestion
Intranasal

Maximum of every 3 hours;101 a maximum duration of 3–5 days.a

Conjunctival Congestion
Ophthalmic

For self-medication: Maximum of 4 times daily; maximum duration of 3–4 days, unless directed by a clinician.102 a

Adults

Nasal Congestion
Intranasal

Maximum of every 3 hours;101 a maximum duration 3–5 days.a

Conjunctival Congestion
Ophthalmic

For self-medication: Maximum of 4 times daily; maximum duration of 3–4 days, unless directed by a clinician.102 a

Special Populations

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

No special population dosage recommendations at this time.a

Cautions for Tetrahydrozoline Hydrochloride

Contraindications

  • Known hypersensitivity to tetrahydrozoline or any ingredient in the formulation.101 a

  • Nasal solution: Use in infants <2 years of age.101 a

  • Nasal solution: Use of 0.1% solution in children <6 years of age.101 a

  • Nasal solution: Concomitant use of MAO inhibitors.101 (See Specific Drugs under Interactions.)

Warnings/Precautions

Warnings

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Glaucoma

Patients with narrow-angle glaucoma or other serious eye disease should consult a clinician before using ophthalmic solution.102 a c

General Precautions

Overuse

Possible irritation of nasal mucosa or conjunctiva and adverse systemic effects (particularly in children) with excessive dosage and/or prolonged or too frequent use.a Possible rebound congestion (rhinitis, chronic redness, and swelling of the nasal mucosa) or ocular hyperemia (redness); avoid prolonged use.101 102 a c (See Advice to Patients.)

Overdose in children may produce profound sedation, profuse sweating, hypotension, and/or shock.101

High concentrations of ophthalmic solution may liberate pigment granules; more common in the elderly.a

Sympathomimetic Effects

Possible headache, hypertension, weakness, sweating, cardiac irregularities (e.g., palpitations), tremors, drowsiness, lightheadedness, and insomnia.101 a Use with caution in patients with thyroid disease (e.g., hyperthyroidism), heart disease (e.g., coronary artery disease), hypertension, or diabetes mellitus.101 a

Use of Fixed Combinations

When used in fixed combination with astringents (i.e., zinc sulfate), consider the cautions, precautions, and contraindications associated with the concomitant drug.c

Specific Populations

Pregnancy

Category C.101

Lactation

Not known whether tetrahydrozoline is distributed into milk.101 a Caution if used in nursing women.101 a

Pediatric Use

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Safety and efficacy of 0.05% nasal solution not established in children <2 years of age;101 safety and efficacy of 0.1% nasal solution not established in children <6 years of age.101

Safety and efficacy of ophthalmic solution not established in children <6 years of age.102

Common Adverse Effects

Intranasal: Mucosal burning, stinging, dryness, sneezing.101 a

Ophthalmic: Blurred vision, irritation, mydriasis.a

Interactions for Tetrahydrozoline Hydrochloride

Specific Drugs

Drug

Interaction

Comments

MAO Inhibitors

Nasal solution: possible severe hypertensive reaction101

Concomitant use contraindicated101

Tetrahydrozoline Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Absorption may occasionally be sufficient to produce systemic effects.a

Onset

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

Duration

Local vasoconstriction may persist for 4–8 hours.a

Stability

Storage

Nasal

Solution

Tight containersa at <30°C.101

Ophthalmic

Solution

Tight containersa at 15–25°C.102 a c

Actions

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

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

  • Intranasal application constricts dilated arterioles, reduces nasal blood flow and congestion, and may open obstructed eustachian ostia.101 a Temporarily improves nasal ventilation.a

  • Conjunctival application constricts small arterioles and temporarily relieves conjunctival congestion.a

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

  • With intranasal use, importance of discontinuing drug and consulting a clinician if nasal congestion worsens or persists for >3–5 days.a

  • 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.102 a c

  • Overuse of nasal solution may cause recurrence or exacerbation of nasal congestion; overuse of ophthalmic solution may produce increased redness of the eye. 101 a

  • Importance of removing contact lenses prior to administration of ophthalmic solution; wait ≥15 minutes after instillation to replace lenses.102 b

  • Importance of avoiding contamination of the dropper or spray dispenser.102 a c Do not touch dropper tip to any surface;102 c rinse nasal spray dispenser tip with hot water.a To minimize risk of spreading infections, do not share dropper or spray dispenser with other individuals.a

  • Advise patients not to use ophthalmic solution if solution is cloudy.102 c

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.101

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.101 102 c

  • 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

Tetrahydrozoline Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Solution

0.05%

Tyzine (with benzalkonium chloride; drops)

Kenwood

0.1%

Tyzine (with benzalkonium chloride; drops and spray)

Kenwood

Ophthalmic

Solution

0.05%*

Murine Plus (with benzalkonium chloride and povidone)

Prestige Brands

Optigene 3 (with benzalkonium chloride and glycerin)

Pfeiffer

Tetrahydrozoline Hydrochloride Eye Drops (with benzalkonium chloride)

Rugby

Visine (with benzalkonium chloride)

McNeil

Visine Advanced Relief (with benzalkonium chloride and povidone)

McNeil

Tetrahydrozoline Hydrochloride Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.05% with Zinc Sulfate 0.25%

Visine A.C. (with benzalkonium chloride)

McNeil

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions October 26, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

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

101. Tyzine (tetrahydrozoline hydrochloride) nasal solution prescribing information. Fairfield, NJ; 1999 Apr.

102. Pfizer. Visine (tetrahydrozoline hydrochloride 0.05%) product information. From Pfizer Visine website (). Accessed 2006 Oct 25.

a. AHFS drug information 2007. McEvoy GK, ed. Tetrahydrozoline hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2007:2868-9.

b. McNeil-PPC, Inc. Frequently asked questions. Available at: . Accessed 2007 Nov 29.

c. McNeil-PPC, Inc. Visine A.C. (tetrahydrozoline hydrochloride 0.05% and zinc sulfate 0.25%) product information. From McNeil Visine website (. Accessed 2007 Nov 21.

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