Tetrahydrozoline Hydrochloride

Class: Vasoconstrictors
CAS Number: 522-48-5
Brands: Clear Eyes Triple Action Relief, Rohto Arctic, Rohto Ice, Rohto Relief, Visine A.C., Visine Advanced, Visine Maximum, Visine Original, Visine Totality

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.101 a

Uses for Tetrahydrozoline Hydrochloride

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

Slideshow: Fact or Fiction? The Top 15 Osteoarthritis Myths

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

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

Avoid contamination of the dropper tip.102 a c

Dosage

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

Pediatric Patients

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

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

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

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

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

Warnings/Precautions

Warnings

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 conjunctiva and adverse systemic effects (particularly in children) with excessive dosage and/or prolonged or too frequent use.a Possible ocular hyperemia (redness); avoid prolonged use.101 102 a c (See Advice to Patients.)

Overdose may produce CNS depression with drowsiness, decreased body temperature, bradycardia, shock-like hypotension, apnea, and coma.

Accidental ingestion of imidazoline derivatives (i.e., tetrahydrozoline, naphazoline, oxymetazoline) in children has resulted in serious adverse events requiring hospitalization (e.g., coma, bradycardia, decreased respiration, sedation, somnolence).101 1001 1002 1003 1004 1005 1006 1007 (See Pediatric Use under Cautions and also see Advice to Patients.)

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

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

Accidental ingestion of OTC ophthalmic solutions or nasal sprays containing imidazoline derivatives (i.e., tetrahydrozoline, naphazoline, oxymetazoline) 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 Respiratory depression, CNS depression, and/or lethargy reportedly occurred in infants following accidental ingestion of small amounts (≤6 mL) of 0.05% tetrahydrozoline ophthalmic solution.1002 1007 Keep out of reach of children.1001 (See Advice to Patients.)

Common Adverse Effects

Ophthalmic: Blurred vision, irritation, mydriasis.a

Tetrahydrozoline Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Absorption may occasionally be sufficient to produce systemic effects.a

Onset

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

Duration

Local vasoconstriction may persist for 4–8 hours.a

Stability

Storage

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

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

Advice to Patients

  • 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 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 To minimize risk of spreading infections, do not share dropper with other individuals.a

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

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

  • 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

Ophthalmic

Solution

0.05%*

Tetrahydrozoline Hydrochloride Eye Drops

Visine Original

J&J

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

Tetrahydrozoline Hydrochloride Combinations

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.05% with Dextran 70 0.1%, Polyethylene Glycol 400 1%, and Povidone 1%*

Tetrahydrozoline Hydrochloride, Dextran, Polyethylene Glycol, and Povidone Eye Drops

Visine Advanced

J&J

0.05% with Glycerin 0.2%, Hypromellose 0.36%, and Polyethylene Glycol 400 1%

Visine Maximum

J&J

0.05% with Glycerin 0.2%, Hypromellose 0.36%, Polyethylene Glycol 400 1%, and Zinc Sulfate 0.25%

Visine Totality

J&J

0.05% with Hypromellose 0.35%

Rohto Arctic

Mentholatum

0.05% with Hypromellose 0.2% and Zinc Sulfate 0.25%

Rohto Ice

Mentholatum

Rohto Relief

Mentholatum

0.05% with Polyethylene Glycol 400 1%*

Tetrahydrozoline Hydrochloride and Polyethylene Glycol Eye Drops

0.05% with Polyvinyl Alcohol 0.5% and Povidone 0.6%

Clear Eyes Triple Action Relief

Prestige Brands

0.05% with Zinc Sulfate 0.25%*

Tetrahydrozoline Hydrochloride and Zinc Sulfate Eye Drops

Visine A.C.

J&J

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions February 20, 2014. 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.

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. Tetrahydrozoline hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists. From AHFS website.

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.

Hide
(web3)