Tetracaine

Class: Local Anesthetics
ATC Class: S01HA03
VA Class: OP700
CAS Number: 136-47-0
Brands: Altacaine, Pontocaine, Tetcaine, Tetravisc

Introduction

Local anesthetic.a b c

Uses for Tetracaine

Ophthalmic Anesthesia

Applied topically to the eye to produce local anesthesia for diagnostic and therapeutic procedures (e.g., tonometry, gonioscopy, removal of foreign bodies or sutures from the cornea, conjunctival and corneal scraping for diagnostic purposes, paracentesis of the anterior chamber, thorough examination and irrigation of painful injuries, short procedures involving the cornea and conjunctiva).a b c

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Rhinolaryngeal Anesthesia

Applied topically to produce anesthesia of the nose and throat.a b

Used to abolish laryngeal and esophageal reflexes prior to diagnostic procedures (e.g., bronchoscopy, bronchography, esophagoscopy).a b

Tetracaine Dosage and Administration

Administration

Apply topically to the eye as a 0.5% ophthalmic solution.a b c Apply directly to larynx, trachea, or esophagus as a 0.25 or 0.5% topical solution, or administer via oral inhalation as a nebulized 0.5% solution.a b

Do not use if solution contains crystals or is cloudy or discolored.a b c

Ophthalmic Administration

Apply 0.5% ophthalmic solution topically to eye.a c For topical anesthesia only;b do not inject.c Not for self-medication.b

May add epinephrine 0.1% to produce vascular constriction when necessary.b

Do not touch eyelids or surrounding area with dropper tip.c

Do not touch or rub eye until the anesthetic effect has worn off.c

Rhinolaryngeal Administration

Apply directly to larynx, trachea, or esophagus as a 0.25 or 0.5% topical solution, or administer via oral inhalation as a nebulized 0.5% solution.a b

Commercially available 2% topical solution contains FD&C blue No. 1 to guard against accidental injection.b

To avoid rapid absorption and high blood levels, do not administer in a coarse stream or by forceful injection.b

Manufacturer recommends adding 0.06 mL epinephrine 0.1% to each mL of anesthetic solution to retard absorption.b

Use care when measuring dose; measure dose accurately in every instance.b (See Systemic Toxicity under Cautions.)

Dosage

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

Use the lowest dose resulting in effective anesthesia.b (See Systemic Toxicity under Cautions.)

Adults

Ophthalmic Anesthesia
Ophthalmic Topical

Short-duration procedures: Instill 1–2 drops just prior to evaluation.a b c

Minor surgical procedures: Instill 1–2 drops every 5–10 minutes for 1–3 doses.c

Prolonged anesthesia: Instill 1–2 drops every 5–10 minutes for 3–5 doses.c

Not for prolonged use.b

Rhinolaryngeal Anesthesia
Rhinolaryngeal Topical

Administer as a 0.25 or 0.5% topical solution directly to larynx, trachea, or esophagus (total absorbed dose ≤20 mg).a b

Oral Inhalation

Administer as a nebulized 0.5% solution (total absorbed dose ≤20 mg).a b

Prescribing Limits

Adults

Rhinolaryngeal Anesthesia
Rhinolaryngeal Topical or Oral Inhalation

Maximum total absorbed dose: 20 mg (8 mL of a 0.25% solution or 4 mL of a 0.5% solution).a b

Special Populations

Geriatric, Debilitated, or Acutely Ill Patients

Manufacturer recommends reduced doses commensurate with weight, age, and physical status; however, no specific dosage recommendations at this time.b (See Systemic Toxicity under Cautions.)

Cautions for Tetracaine

Contraindications

  • Known hypersensitivity to tetracaine or other local anesthetics of the ester type, to p-aminobenzoic acid or its derivatives, or to any ingredient in the formulation.a b c

  • Self-administration of ophthalmic solution by patients without clinician supervision.c

Warnings/Precautions

Warnings

Systemic Toxicity

Rarely, use of local anesthetics causes reactions resulting in death.b When a local anesthetic is used (e.g., tetracaine for rhinolaryngeal anesthesia), ensure immediate availability of resuscitative equipment and drugs.b Excessive doses or rapid absorption may produce serious or fatal reactions.b (See Administration and also Prescribing Limits under Dosage and Administration).

Systemic reactions following rhinolaryngeal administration may involve the CNS (e.g., excitation, depression, nervousness, dizziness, blurred vision, tremors, drowsiness, convulsions, unconsciousness, respiratory arrest) and cardiovascular system (e.g., myocardial depression, BP changes [typically hypotension], cardiac arrest).b

Fatal reactions may occur even in the absence of a history of hypersensitivity.b (See Hypersensitivity Reactions under Cautions.)

Following ophthalmic administration, systemic toxicity (mainly CNS stimulation followed by depression) occurs very rarely.a

Use caution when administering to patients with abnormal or reduced levels of plasma esterases.b

Prolonged Ophthalmic Use

Avoid prolonged use of ophthalmic solution.a b c Corneal epithelial erosions, retardation or prevention of healing of corneal erosions, severe keratitis, and permanent corneal opacification and scarring with accompanying reduction of visual acuity or visual loss have occurred.a b c

Ocular Effects

Protect anesthetized eye from irritating chemicals, foreign bodies, and rubbing to prevent corneal and conjunctival damage.b c

Rarely, local idiosyncratic reactions (e.g., lacrimation, photophobia, chemosis) may occur.a b

Serious Adverse Effects associated with Local Anesthetics

Risk of serious adverse effects (e.g., seizures, coma, irregular heart beat, respiratory depression) with use of topical local anesthetics; generally reported following application of extemporaneously prepared topical preparations containing high concentrations of anesthetics.k

Potential for life-threatening adverse effects (e.g., irregular heart beat, seizures, breathing difficulties, coma, death) when topical local anesthetics are applied to a large area of skin, when the area of application is covered with an occlusive dressing, if a large amount of topical anesthetic is applied, if the anesthetic is applied to irritated or broken skin, or if the skin temperature increases (from exercise or use of a heating pad).101 102

Lidocaine 4% gel has been investigated to reduce discomfort during mammography.101 103 Whether such use could result in serious reactions has not been determined.101 103 Patients should speak with their clinician if they are considering using a topical anesthetic before obtaining a mammogram.101

When a topical anesthetic is needed for a procedure, use of an FDA-approved preparation has been recommended.k Use a preparation containing the lowest concentration of anesthetic likely to be effective; apply a small amount of the preparation to the affected area for the shortest period necessary for the desired effect,k and do not apply to broken or irritated skin.101

Sensitivity Reactions

Hypersensitivity Reactions

Following ophthalmic administration, rare, severe, immediate allergic corneal reaction reported (acute diffuse epithelial keratitis with filament formation and/or sloughing of large areas of necrotic epithelium, diffuse stromal edema, descemetitis, and iritis).c Discontinue use if signs or symptoms of allergy or sensitivity occur.a b

Following rhinolaryngeal administration, systemic allergic reactions may occur (e.g., cutaneous lesions [e.g., urticaria], edema, other allergic manifestations); possibly caused by hypersensitivity, idiosyncrasy, or diminished tolerance.b Skin testing is of limited value in detecting sensitivity.b

Rarely, severe allergic reactions, including anaphylaxis, have occurred following rhinolaryngeal administration; not typically dose related.b

Specific Populations

Pregnancy

Category C.b

Lactation

Not known whether tetracaine is distributed into milk.b Use caution.b

Pediatric Use

Safety and efficacy of ophthalmic and topical solutions not established.a b

Common Adverse Effects

Ophthalmic topical: Stinging, burning, conjunctival redness.c

Tetracaine Pharmacokinetics

Absorption

Onset

Ophthalmic solution: 25–30 seconds.a c

Rhinolaryngeal topical solution: 5–10 minutes.a b

Duration

Ophthalmic solution: ≥15 minutes.a

Rhinolaryngeal topical solution: 30 minutes.a b

Elimination

Metabolism

Systemically absorbed drug is detoxified in blood by plasma esterases.b

Stability

Storage

Ophthalmic

Solution

Tight, light-resistant containers at 15–30°C; avoid freezing.a c

Topical

Solution

Tight, light-resistant containers at 2–8°C.a b

Actions

  • Local anesthetic of the ester type, related to procaine.a b c

  • Stabilizes neuronal membrane; prevents initiation and transmission of nerve impulses thereby effecting local anesthesia.b c

  • Usually does not dilate the pupil, disturb accommodation, or increase intraocular pressure when applied to conjunctiva.a b

  • Approximately equipotent to proparacaine hydrochloride.a

Advice to Patients

  • Importance of not touching or rubbing eye(s) until anesthesia from ophthalmic solution has worn off.a b c

  • Advise patient not to instill ophthalmic solution repeatedly; risk of severe eye damage.b c

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.b

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

  • 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

Tetracaine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution*

0.5%*

Altacaine

Altaire

Pontocaine Hydrochloride

Hospira

Tetcaine

Ocusoft

Tetracaine Hydrochloride Ophthalmic Solution

Tetravisc

Ocusoft

Topical

Solution

2%

Pontocaine Hydrochloride

Hospira

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 1, 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

a. AHFS Drug Information 2008. McEvoy GK, ed. Tetracaine hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; 2008:2902-3.

b. Hospira, Inc. Pontocaine (tetracaine hydrochloride, USP) ophthalmology 0.5% solution and rhinolaryngology 2% solution prescribing information. Lake Forest, IL; 2004 Nov.

c. Bausch & Lomb Incorporated. Tetracaine hydrochloride ophthalmic solution USP, 0.5% prescribing information. Tampa, FL; 2004 Jan.

k. Food and Drug Administration. FDA Public Health Advisory: Life-threatening side effects with use of skin products containing numbing ingredients for cosmetic procedures. 2007 Feb 6, updated 2007 Feb 9. From FDA website ().

101. Food and Drug Administration. FDA Public Health Advisory: Potential hazards of skin products containing numbing ingredients for relieving pain from mammography and other medical tests and conditions. 2009 Jan 16. From FDA website ().

102. Food and Drug Administration. Topical Anesthetics. MedWatch alert. Rockville, MD; 2009 Jan 16. From FDA website (

103. Lambertz CK, Johnson CJ, Montgomery PG et al. Premedication to reduce discomfort during screening mammography. Radiology. 2008; 248:765-72. [PubMed 18647845]

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