Tetrahydrozoline (Monograph)

Brand names: Clear Eyes Triple Action Relief, Rohto Arctic, Rohto Ice, Rohto Relief, Visine Original
Drug class: Vasoconstrictors
CAS number: 522-48-5

Medically reviewed by Drugs.com on Feb 12, 2024. Written by ASHP.

Introduction

Vasoconstrictor; an imidazoline-derivative sympathomimetic amine.

Uses for Tetrahydrozoline

Conjunctival Congestion

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

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

Controls hyperemia in patients with superficial corneal vascularity.

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

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

Tetrahydrozoline Dosage and Administration

Administration

Ophthalmic Administration

Apply ophthalmic solution topically to the conjunctiva.

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

Do not administer discolored or cloudy solution.

Avoid contamination of the dropper tip.

Dosage

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

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.

Adults

Conjunctival Congestion

Ophthalmic

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

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.

Adults

Conjunctival Congestion

Ophthalmic

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

Special Populations

No special population dosage recommendations at this time.

Cautions for Tetrahydrozoline

Contraindications

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

Warnings/Precautions

Warnings

Glaucoma

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

General Precautions

Overuse

Possible irritation of conjunctiva and adverse systemic effects (particularly in children) with excessive dosage and/or prolonged or too frequent use. Possible ocular hyperemia (redness); avoid prolonged use. (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). (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.

Sympathomimetic Effects

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

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.

Specific Populations

Pregnancy

Category C.

Lactation

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

Pediatric Use

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

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. 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. Keep out of reach of children. (See Advice to Patients.)

Common Adverse Effects

Ophthalmic: Blurred vision, irritation, mydriasis.

Tetrahydrozoline Pharmacokinetics

Absorption

Bioavailability

Absorption may occasionally be sufficient to produce systemic effects.

Onset

Following ocular administration, local vasoconstriction usually occurs within minutes.

Duration

Local vasoconstriction may persist for 4–8 hours.

Stability

Storage

Ophthalmic

Solution

Tight containers at 15–25°C.

Actions

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

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

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

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.

• Overuse of ophthalmic solution may produce increased redness of the eye.

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

• Importance of avoiding contamination of the dropper or spray dispenser. Do not touch dropper tip to any surface. To minimize risk of spreading infections, do not share dropper with other individuals.

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

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

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

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

• 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.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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

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

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