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Special Alerts
Topical Anesthetic Use for Cosmetic or Medical Procedures: Public Health Advisory - January 2009; Updated March 2009
Health Canada has issued a “Dear Healthcare Professional” letter and a notice to the Canadian public regarding important safety information associated with the use of topical anesthetic agents. Recently in the U.S., the The Food and Drug Administration (FDA) issued a Public Health Advisory to remind consumers, caregivers, and healthcare professionals of potential life-threatening side effects associated with the use of topical anesthetics available as prescription and over-the-counter (OTC) products for a variety of uses, including numbing skin prior to cosmetic or medical procedures (topical lidocaine has been recently evaluated to relieve mammography discomfort).
Topical application can result in high systemic levels and lead to toxic effects (eg, methemoglobinemia, irregular heart beats, seizures, coma, respiratory depression, death). Children may be at an increased risk for adverse effects, as well as individuals who, without the supervision of trained professionals, apply large amounts of anesthetics (or cover large areas of the skin), leave these products on for long periods of time, or use materials, wraps, or dressings to cover the skin after anesthetic application.
Both the FDA and Health Canada are recommending that when topical anesthetics are needed prior to procedures, consumers ask their healthcare provider for instructions on safe use of these products, use only approved products, and use products with the lowest amount of anesthetic while applying the least amount possible to relieve pain. If a high degree of pain is expected that is not controlled by appropriate amounts of topical anesthetics, consumers should ask their physician for alternative techniques for pain control.
Additional information can be found at:
U.S.: http://www.fda.gov/Drugs/DrugSafety/PublicHealthAdvisories/ucm110625.htm
Canada: Canada: http://www.hc-sc.gc.ca/dhp-mps/medeff/advisories-avis/prof/_2009/emla_ametop_hpc-cps-eng.php
Pronunciation
(TET ra kane)
U.S. Brand Names
Index Terms
Generic Available
Yes: Ophthalmic solution, solution for injection
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Spinal anesthesia; local anesthesia in the eye for various diagnostic and examination purposes; topically applied to nose and throat for diagnostic procedures
Use: Dental
Ester-type local anesthetic; applied topically to throat for various diagnostic procedures and on cold sores and fever blisters for pain
Pregnancy Risk Factor
C
Pregnancy Considerations
Animal reproduction studies have not been conducted.
Lactation
Excretion in breast milk unknown/use caution
Contraindications
Hypersensitivity to tetracaine, ester-type anesthetics, aminobenzoic acid, or any component of the formulation; injection should not be used when spinal anesthesia is contraindicated
Warnings/Precautions
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with cardiovascular disease.
• Decreased plasma esterase levels: Use with caution in patients with abnormal or decreased levels of plasma esterases.
• Hyperthyroidism: Use with caution in patients with hyperthyroidism.
Special populations:
• Acutely ill patients: Use with caution in acutely ill patients; dose reduction may be required.
• Debilitated patients: Use with caution in debilitated patients; dose reduction may be required.
• Elderly: Use with caution in the elderly; dose reduction may be required.
• Obstetric patients: Use with caution in obstetric patients; dose reduction may be required.
• Patients with increased intra-abdominal pressure: Use with caution in patients with increased intra-abdominal pressure; dose reduction may be required.
Dosage form specific issues:
• Ophthalmic: May delay wound healing. Prolonged use is not recommended. The anesthetized eye should be protected from irritation, foreign bodies, and rubbing to prevent inadvertent damage.
• Sodium bisulfite: Products may contain sodium bisulfite which may cause allergic reactions in some individuals.
• Trained personnel: Dental practitioners and/or clinicians using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.
Adverse Reactions
Frequency not defined.
Injection: Note: Adverse effects listed are those characteristics of local anesthetics.
Cardiovascular: Cardiac arrest, hypotension
Central nervous system: Chills, convulsions, dizziness, drowsiness, nervousness, unconsciousness
Gastrointestinal: Nausea, vomiting
Neuromuscular & skeletal: Tremors
Ocular: Blurred vision, pupil constriction
Otic: Tinnitus
Respiratory: Respiratory arrest
Miscellaneous: Allergic reaction
Ophthalmic: Ocular: Chemosis, lacrimation, photophobia, transient stinging
With chronic use: Corneal erosions, corneal healing retardation, corneal opacification (permanent), corneal scarring, keratitis (severe)
Drug Interactions
There are no known significant interactions.
Storage
Injection: Store solution under refrigeration. Protect from light.
Ophthalmic and topical solutions: Store under refrigeration at 2°C to 8°C.
Reconstitution
Solution for injection: Hyperbaric solution: May be made by mixing equal volumes of the 1% solution and D10W.
Powder for injection:
Hyperbaric solution: Dissolve 10 mg of Pontocaine® Niphanoid® in 1 mL D10W. Further dilute with equal volume of spinal fluid. Resulting solution is D5W with tetracaine 5 mg/mL.
Hypobaric solution: Dissolve 1 mg of Pontocaine® Niphanoid® in 1 mL SWFI.
Mechanism of Action
Ester local anesthetic blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction
Pharmacodynamics/Kinetics
Onset of action: Anesthetic: Rhinolaryngology: 5-10 minutes
Duration: Rhinolaryngology: ~30 minutes
Metabolism: Hepatic; detoxified by plasma esterases to aminobenzoic acid
Excretion: Urine
Dosage
Adults:
Ophthalmic: Short-term anesthesia of the eye: 0.5% solution: Instill 1-2 drops; prolonged use (especially for at-home self-medication) is not recommended
Injection: Spinal anesthesia: Note: Dosage varies with the anesthetic procedure, the degree of anesthesia required, and the individual patient response; it is administered by subarachnoid injection for spinal anesthesia.
Perineal anesthesia: 5 mg
Perineal and lower extremities: 10 mg
Anesthesia extending up to costal margin: 15 mg; doses up to 20 mg may be given, but are reserved for exceptional cases
Low spinal anesthesia (saddle block): 2-5 mg
Topical mucous membranes (rhinolaryngology): Used as a 0.25% or 0.5% solution by direct application or nebulization; total dose should not exceed 20 mg
Dental Usual Dosing
Topical mucous membranes (rhinolaryngology): Adults: Used as a 0.25% or 0.5% solution by direct application or nebulization; total dose should not exceed 20 mg
Patient Education
Topical or ophthalmic anesthesia effects may last for some time following use; you will need to observe appropriate safety precautions to prevent injury. Pregnancy precaution: Inform prescriber if you are pregnant.
Ophthalmic: Do not rub or touch your eye, scratch your nose, or attempt to apply eye make-up until all sensation returns. May cause temporary rash or stinging when used. Report any ringing in ears, feeling of weakness or faintness, chest pain or palpitation, or increased restlessness.
Topical: Do not eat or drink anything until full sensation returns to lips, mouth, and throat. Use caution with heat or cold; you will not have accurate hot or cold sensation until full effects of anesthesia have worn off.
Additional Information
Approximately 10 times more potent than procaine
Anesthesia and Critical Care Concerns/Other Considerations
Local anesthetic toxicity: Cardiac arrest: Lipid infusion has been used in animal studies and several human cases (Bupivacaine: Rosenblatt, 2006; Levobupivacaine: Foxall, 2007; Ropivacaine: Litz, 2006) where cardiovascular toxicity, unresponsive to conventional resuscitation, resulted. Additional information is available at http://www.lipidrescue.org. The protocol from the website is: 20% Fat Emulsion: 1.5 mL/kg administered over 1 minute, followed immediately by an infusion of 0.25 mL/kg/minute. Continue chest compressions (lipid must circulate). Repeat bolus every 3-5 minutes up to 3 mL/kg total dose until circulation restored. Continue infusion until hemodynamic stability is restored. Increase the infusion rate to 0.5 mL/kg/minute if BP declines. A maximum total dose of 8 mL/kg is recommended.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause dizziness, drowsiness, or nervousness
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
Note: Tetracaine is 10 times as potent as procaine. Explain use, monitor vital signs, and monitor patient safety before, during, and following use according to formulation used and procedure being done. Caution patient that anesthetic effects of topical or ophthalmic preparation may last for some time after procedure (1-5 hours). Instruct in appropriate safety precautions.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Injection, powder for reconstitution, as hydrochloride [preservative free]:
Pontocaine® Niphanoid®: 20 mg
Injection, solution, as hydrochloride [preservative free]: 1% [10 mg/mL] (2 mL)
Pontocaine®): 1% [10 mg/mL] (2 mL) [contains sodium bisulfite]
Solution, ophthalmic, as hydrochloride: 0.5% [5 mg/mL] (2 mL, 15 mL)
Solution, topical, as hydrochloride:
Pontocaine®: 2% [20 mg/mL] (30 mL, 118 mL) [for rhinolaryngology]
Pricing: U.S. (www.drugstore.com)
Solution (Tetracaine HCl)
0.5% (15): $17.82
References
Bartfield JM, Lee FS, Raccio-Robak N, et al, “Topical Tetracaine Attenuates the Pain of Infiltration of Buffered Lidocaine,” Acad Emerg Med, 1996, 3(11):1001-5.
Bonadio WA, “Safe and Effective Method for Application of Tetracaine, Adrenaline, and Cocaine to Oral Lacerations,” Ann Emerg Med, 1996, 28(4):396-8.
Corcoran W, Butterworth J, Weller RS, et al, “Local Anesthetic-Induced Cardiac Toxicity: A Survey of Contemporary Practice Strategies Among Academic Anesthesiology Departments,” Anesth Analg, 2006, 103(5):1322-6.
Duffin RM and Olson RJ, “Tetracaine Toxicity,” Ann Ophthalmol, 1984, 16(9):836, 838.
Foxall G, McCahon R, Lamb J, et al, “Levobupivacaine-Induced Seizures and Cardiovascular Collapse Treated With Intralipid,” Anaesthesia, 2007, 62(5):516-8.
Garfield JM, Andriole GL, Vetto JL, et al, “Prolonged Diabetes Insipidus Subsequent to an Episode of Chemical Meningitis,” Anesthesiology, 1986, 64(2):253-4.
Grant SA and Hoffman RS, “Use of Tetracaine, Epinephrine, and Cocaine as a Topical Anesthetic in the Emergency Department,” Ann Emerg Med, 1992, 21(8):987-97.
Kintner JC, Grossniklaus HE, Lass JH, et al, “Infectious Crystalline Keratopathy Associated With Topical Anesthetic Abuse,” Cornea, 1990, 9(1):77-80.
Litz RJ, Popp M, Stehr SN, et al, “Successful Resuscitation of a Patient With Ropivacaine-Induced Asystole After Axillary Plexus Block Using Lipid Infusion," Anaesthesia, 2006, 61(8):800-1.
Rosenblatt MA, Abel M, Fischer GW, et al, “Successful Use of a 20% Lipid Emulsion to Resuscitate a Patient After a Presumed Bupivacaine-Related Cardiac Arrest," Anesthesiology, 2006, 105(1):217-8.
Skidmore RA, Patterson JD, and Tomsick RS, “Local Anesthetics,” Dermatol Surg, 1996, 22(6):511-22.
van Kan JH, Egberts AC, Rijnvos WP, et al, “Tetracaine Versus Lidocaine-Prilocaine for Preventing Venipuncture-Induced Pain in Children,” Am J Health Syst Pharm, 1997, 54(4):388-92.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2010
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