MEDICATION SAFETY ISSUES
Sound-alike/look-alike issues:
Orabase®-B may be confused with Orinase®
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
U.S. BRAND NAMES — Americaine® Hemorrhoidal [OTC]; Anbesol® Baby [OTC]; Anbesol® Cold Sore Therapy [OTC]; Anbesol® Jr. [OTC]; Anbesol® Maximum Strength [OTC]; Anbesol® [OTC]; Benzodent® [OTC]; Bi-Zets; Boil-Ease® Pain Relieving; Cepacol® Sore Throat [OTC]; Chiggerex® Plus; Chiggerex® [OTC]; Chiggertox® [OTC]; Cylex® [OTC]; Dent’s Extra Strength Toothache [OTC]; Dentapaine [OTC]; Dermoplast® Antibacterial [OTC]; Dermoplast® Pain Relieving [OTC]; Detane® [OTC]; Foille® [OTC]; HDA® Toothache [OTC]; Hurricaine® [OTC]; Ivy-Rid® [OTC]; Kank-A® Soft Brush™ [OTC]; Lanacane® Maximum Strength [OTC]; Lanacane® [OTC]; Little Teethers® [OTC]; Mycinettes® [OTC]; Orabase® with Benzocaine [OTC]; Orajel PM® Maximum Strength [OTC]; Orajel® Baby Daytime and Nighttime [OTC]; Orajel® Baby Teething Nighttime [OTC]; Orajel® Baby Teething [OTC]; Orajel® Denture Plus [OTC]; Orajel® Maximum Strength [OTC]; Orajel® Medicated Toothache [OTC]; Orajel® Mouth Sore [OTC]; Orajel® Multi-Action Cold Sore [OTC]; Orajel® Ultra Mouth Sore [OTC]; Outgro® [OTC]; Red Cross™ Canker Sore [OTC]; Rid-A-Pain Dental [OTC]; Sepasoothe®; Skeeter Stik [OTC]; Sting-Kill [OTC]; Tanac® [OTC]; Thorets [OTC]; Trocaine® [OTC]; Zilactin Toothache and Gum Pain® [OTC]; Zilactin®-B [OTC]
PHARMACOLOGIC CATEGORY
Local Anesthetic
DOSING: ADULTS — Note: These are general dosing guidelines; Refer to specific product labeling for dosing instructions.
Bee stings, insect bites, minor burns, sunburn: Topical 5% to 20%: Apply to affected area 3-4 times a day as needed. In cases of bee stings, remove stinger before treatment.
Lubricant for passage of catheters and instruments: Topical 20%: Apply evenly to exterior of instrument prior to use.
Mouth and gum irritation: Topical (oral) 10% to 20%: Apply thin layer to affected area up to 4 times daily
Sore throat: Oral: Allow 1 lozenge (10-15 mg) to dissolve slowly in mouth; may repeat every 2 hours as needed
Hemorrhoids: Rectal 5% to 20%: Apply externally to affected area up to 6 times daily
DOSING: PEDIATRIC — Note: These are general dosing guidelines; refer to specific product labeling for dosing instructions.
(For additional information see “Benzocaine: Pediatric drug information”)
Teething pain: Children ≥ 4 months: Topical (oral): 7.5% to 10%: Apply to affected gum area up to 4 times daily
Bee stings, insect bites, minor burns, sunburn: Topical: Children ≥ 2 years: Refer to adult dosing.
Lubricant for passage of catheters and instruments: Topical: Children ≥ 2 years: Refer to adult dosing.
Mouth and gum irritation: Topical (oral) 10% to 20%: Children ≥ 2 years: Refer to adult dosing.
Sore throat: Oral: Children ≥ 5 years: Refer to adult dosing.
Hemorrhoids: Rectal 5% to 20%: Children ≥ 12 years: Refer to adult dosing.
DOSING: ELDERLY — Refer to adult dosing.
DOSAGE FORMS — Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Aerosol, oral spray:
Hurricaine®: 20% (60 mL) [dye free; cherry flavor]
Aerosol, topical spray:
Dermoplast® Antibacterial: 20% (83 mL) [contains aloe vera, benzethonium chloride, menthol]
Dermoplast® Pain Relieving: 20% (60 mL, 83 mL) [contains menthol]
Foille®: 5% (92 g) [contains chloroxylenol 0.63% and corn oil]
Ivy-Rid®: 2% (83 mL)
Lanacane® Maximum Strength: 20% (120 mL) [contains ethanol 36%]
Combination package (Orajel® Baby Daytime and Nighttime):
Gel, oral [Daytime Regular Formula]: 7.5% (5.3 g)
Gel, oral [Nighttime Formula]: 10% (5.3 g)
Cream, oral:
Benzodent®: 20% (7.5 g, 30 g)
Orajel PM® Maximum Strength: 20% (5.3 g, 7 g) [contains menthol]
Cream, topical:
Lanacane®: 6% (30 g, 60 g)
Lanacane® Maximum Strength: 20% (30 g)
Gel, oral:
Anbesol®: 10% (7.5 g) [contains benzyl alcohol; cool mint flavor]
Anbesol® Baby: 7.5% (7.5 g) [contains benzoic acid; grape flavor]
Anbesol® Jr.: 10% (7 g) [contains benzyl alcohol; bubble gum flavor]
Anbesol® Maximum Strength: 20% (7.5 g, 10 g) [contains benzyl alcohol]
Dentapaine: 20% (11 g) [contains clove oil]
HDA® Toothache: 6.5% (15 mL) [contains benzyl alcohol]
Hurricaine®: 20% (5 g) [dye free; wild cherry flavor]; (30 g) [dye free; mint, pina colada, watermelon, and wild cherry flavors]
Kank-A® Soft Brush™ : 20% (2 mL) [packaged in applicator with brush tip]
Little Teethers®: 7.5% (9.4 g) [cherry flavor]
Orabase® with Benzocaine®: 20% (7 g) [contains ethanol 48%; mild mint flavor]
Orajel®: 10% (5.3 g, 7 g, 9.4 g)
Orajel® Baby Teething: 7.5% (9.4 g, 11.9 g) [cherry flavor]
Orajel® Baby Teething Nighttime: 10% (5.3 g)
Orajel® Denture Plus: 15% (9 g) [contains menthol 2%, ethanol 66.7%]
Orajel® Maximum Strength: 20% (5.3 g, 7 g, 9.4 g, 11.9 g)
Orajel® Mouth Sore: 20% (5.3 g, 9.4 g, 11.9 g) [contains allantoin, benzalkonium chloride 0.02%, zinc chloride 0.1%]
Orajel® Multi-Action Cold Sore: 20% (9.4 g) [contains allantoin 0.5%, camphor 3%, dimethicone 2%]
Orajel® Ultra Mouth Sore: 15% (9.4 g) [contains ethanol 66.7%, menthol 2%]
Zilactin®-B: 10% (7.5 g)
Gel, topical:
Detane®: 7.5% (15 g)
Liquid, oral:
Anbesol®: 10% (9 mL) [cool mint flavor; contains benzyl alcohol]
Anbesol® Maximum Strength: 20% (9 mL) [contains benzyl alcohol]
Hurricaine®: 20% (30 mL) [pina colada and wild cherry flavors; dye free]
Orajel® Baby Teething: 7.5% (13 mL) [very berry flavor]
Orajel® Maximum Strength: 20% (13 mL) [contains ethanol 44%, tartrazine]
Tanac®: 10% (13 mL) [contains benzalkonium chloride]
Liquid, oral [drops]:
Rid-A-Pain Dental: 6.3% (30 mL) [contains ethanol 70%]
Liquid, topical:
Chiggertox®: 2% (30 mL)
Outgro®: 20% (9 mL)
Skeeter Stik: 5% (14 mL) [contains menthol]
Lozenge: 6 mg (18s) [contains menthol]; 15 mg (10s)
Bi-Zets: 15 mg (10s)
Cepacol® Sore Throat: 15 mg (18s) [contains cetylpyridinium, menthol; cherry, citrus, and honey lemon flavors]
Cepacol® Sore Throat: 15 mg (16s) [sugar free; contains cetylpyridinium, menthol; cherry and menthol flavors]
Cylex®: 15 mg (12s) [sugar free; contains cetylpyridinium chloride 5 mg; cherry flavor]
Mycinettes®: 15 mg (12s) [sugar free; contains sodium 9 mg; cherry or regular flavor]
Sepasoothe®: 10 mg (6s, 24s, 100s, 250s, 500s) [sugar free; contains cetylpyridium 0.5 mg/lozenge; wild cherry flavor]
Thorets: 18 mg (300s) [sugar free]
Trocaine®: 10 mg (50s, 300s)
Ointment, oral:
Anbesol® Cold Sore Therapy: 20% (7.1 g) [contains benzyl alcohol, allantoin, aloe, camphor, menthol, vitamin E]
Red Cross™ Canker Sore: 20% (7.5 g) [contains coconut oil]
Ointment, rectal:
Americaine® Hemorrhoidal: 20% (30 g)
Ointment, topical:
Boil-Ease® Pain Relieving: 20% (30 g)
Chiggerex®: 2% (50 g) [contains aloe vera] [DSC]
Chiggerex® Plus: 6% (50 g) [contains aloe]
Foille®: 5% (3.5 g, 14 g, 28 g) [contains chloroxylenol 0.1%, benzyl alcohol; corn oil base]
Pads, topical:
Sting-Kill: 20% (8s) [contains menthol and tartrazine]
Paste, oral:
Orabase® with Benzocaine: 20% (6 g)
Swabs, oral:
Hurricaine®: 20% (6s, 100s) [dye free; wild cherry flavor]
Orajel® Baby Teething: 7.5% (12s) [berry flavor]
Orajel® Medicated Mouth Sore, Orajel® Medicated Toothache: 20% (8s, 12s) [contains tartrazine]
Zilactin® Toothache and Gum Pain: 20% (8s) [grape flavor]
Swabs, topical:
Boil-Ease® Pain Relieving: 20% (12s) [contains tartrazine]
Sting-Kill: 20% (5s) [contains menthol and tartrazine]
Wax, oral:
Dent’s Extra Strength Toothache Gum: 20% (1 g)
DOSAGE FORMS: CONCISE
Aerosol, oral spray:
Hurricaine® [OTC]: 20% (60 mL)
Aerosol, topical spray:
Dermoplast® Antibacterial [OTC]: 20% (83 mL)
Dermoplast® Pain Relieving [OTC]: 20% (60 mL, 83 mL)
Foille® [OTC]: 5% (92 g)
Ivy-Rid® [OTC]: 2% (83 mL)
Lanacane® Maximum Strength [OTC]: 20% (120 mL)
Combination package:
Orajel® Baby Daytime and Nighttime [OTC]:
Gel, oral [Daytime Regular Formula]: 7.5% (5.3 g)
Gel, oral [Nighttime Formula]: 10% (5.3 g)
Cream, oral:
Benzodent® [OTC]: 20% (7.5 g, 30 g)
Orajel PM® Maximum Strength [OTC]: 20% (5.3 g, 7 g)
Cream, topical:
Lanacane® [OTC]: 6% (30 g, 60 g)
Lanacane® Maximum Strength [OTC]: 20% (30 g)
Gel, oral:
Anbesol® [OTC], Zilactin®-B [OTC]: 10% (7.5 g)
Anbesol® Baby [OTC]: 7.5% (7.5 g)
Anbesol® Jr. [OTC]: 10% (7 g)
Anbesol® Maximum Strength [OTC]: 20% (7.5 g, 10 g)
Dentapaine [OTC]: 20% (11 g)
HDA® Toothache [OTC]: 6.5% (15 mL)
Hurricaine® [OTC]: 20% (5 g, 30 g)
Kank-A® Soft Brush™ [OTC]: 20% (2 mL)
Little Teethers® [OTC]: 7.5% (9.4 g)
Orabase® with Benzocaine [OTC]: 20% (7 g)
Orajel® [OTC]: 10% (5.3 g, 7 g, 9.4 g)
Orajel® Baby Teething [OTC]: 7.5% (9.4 g, 11.9 g)
Orajel® Baby Teething Nighttime [OTC]: 10% (5.3 g)
Orajel® Denture Plus [OTC]: 15% (9 g)
Orajel® Maximum Strength [OTC]: 20% (5.3 g, 7 g, 9.4 g, 11.9 g)
Orajel® Mouth Sore [OTC]: 20% (5.3 g, 9.4 g, 11.9 g)
Orajel® Multi-Action Cold Sore [OTC]: 20% (9.4 g)
Orajel® Ultra Mouth Sore [OTC]: 15% (9.4 g)
Gel, topical:
Detane® [OTC]: 7.5% (15 g)
Liquid, oral:
Anbesol® [OTC], Tanac® [OTC]: 10%
Anbesol® Maximum Strength [OTC], Hurricaine® [OTC], Orajel® Maximum Strength [OTC]: 20%
Orajel® Baby Teething [OTC]: 7.5%
Liquid, oral [drops]:
Rid-A-Pain Dental [OTC]: 6.3%
Liquid, topical:
Chiggertox® [OTC]: 2% (30 mL)
Outgro® [OTC]: 20% (9 mL)
Skeeter Stik [OTC]: 5% (14 mL)
Lozenge: 6 mg (18s), 15 mg (10s)
Bi-Zets: 15 mg (10s)
Cepacol® Sore Throat [OTC]: 15 mg (16s, 18s)
Cylex® [OTC], Mycinettes® [OTC]: 15 mg (12s)
Sepasoothe®: 10 mg (6s, 24s, 100s, 250s, 500s)
Thorets [OTC]: 18 mg (300s)
Trocaine® [OTC]: 10 mg (50s, 300s)
Ointment, oral:
Anbesol® Cold Sore Therapy [OTC]: 20% (7.1 g)
Red Cross™ Canker Sore [OTC]: 20% (7.5 g)
Ointment, rectal:
Americaine® Hemorrhoidal [OTC]: 20% (30 g)
Ointment, topical:
Boil-Ease® Pain Relieving: 20% (30 g)
Chiggerex® Plus: 6% (50 g)
Foille® [OTC]: 5% (3.5 g, 14 g, 28 g)
Pads, topical:
Sting-Kill [OTC]: 20% (8s)
Paste, oral:
Orabase® with Benzocaine [OTC]: 20% (6 g)
Swabs, oral:
Hurricaine® [OTC]: 20% (6s, 100s)
Orajel® Baby Teething [OTC]: 7.5% (12s)
Orajel® Mouth Sore [OTC], Orajel® Medicated Toothache [OTC]: 20% (8s, 12s)
Zilactin Toothache and Gum Pain® [OTC]: 20% (8s)
Swabs, topical:
Boil-Ease® Pain Relieving: 20% (12s)
Sting-Kill [OTC]: 20% (5s)
Wax, oral:
Dent’s Extra Strength Toothache Gum [OTC]: 20% (1 g)
GENERIC EQUIVALENT AVAILABLE — Yes: Lozenge
ADMINISTRATION — Avoid application to large areas of broken skin, especially in children. When possible, apply to clean, dry area. When administering a spray formulation, the number of sprays administered and the length of each spray should be monitored and recorded.
USE — Temporary relief of pain associated with pruritic dermatosis, pruritus, minor burns, acute congestive, bee stings, and insect bites; mouth and gum irritations (toothache, minor sore throat pain, canker sores, dentures, orthodontia, teething, mucositis, stomatitis); sunburn; hemorrhoids; anesthetic lubricant for passage of catheters and endoscopic tubes
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Hematologic: Methemoglobinemia
Local: Burning, contact dermatitis, edema, erythema, pruritus, rash, stinging, tenderness, urticaria
Miscellaneous: Hypersensitivity
CONTRAINDICATIONS — Hypersensitivity to benzocaine, other ester-type local anesthetics, or any component of the formulation; secondary bacterial infection of area; ophthalmic use
WARNINGS / PRECAUTIONS
Concerns related to adverse effects: Methemoglobinemia: Has been reported following topical use (rare), particularly with higher concentration (14% to 20%) spray formulations applied to the mouth or mucous membranes. When applied as a spray to the mouth or throat, multiple sprays (or sprays of longer than indicated duration) are not recommended. Use caution with breathing problems (asthma, bronchitis, emphysema, in smokers), inflamed/damaged mucosa, heart disease, children <6 months of age, and hemoglobin or enzyme abnormalities (glucose-6-phosphate dehydrogenase deficiency, hemoglobin-M disease, NADH-methemoglobin reductase deficiency, pyruvate-kinase deficiency). Alternatives to benzocaine sprays, such as topical lidocaine preparations, should be considered for patients at higher risk of this reaction. The classical clinical finding of methemoglobinemia is chocolate brown-colored arterial blood. However, suspected cases should be confirmed by co-oximetry, which yields a direct and accurate measure of methemoglobin levels. Standard pulse oximetry readings or arterial blood gas values are not reliable. Clinically significant methemoglobinemia requires immediate treatment.
Other warnings/precautions: Self-medication (OTC use): When used for self-medication, notify healthcare provider if condition worsens or does not improve within 7 days, or if swelling, rash, or fever develops. Do not use on open wounds. Avoid contact with the eyes.
DRUG INTERACTIONS — There are no known significant interactions.
PREGNANCY RISK FACTOR — C (show table)
PREGNANCY IMPLICATIONS — Reproduction studies have not been conducted.
LACTATION — Excretion in breast milk unknown/use caution
MONITORING PARAMETERS — Monitor patients for signs and symptoms of methemoglobinemia such as pallor, cyanosis, nausea, muscle weakness, dizziness, confusion, agitation, dyspnea and tachycardia. The classical clinical finding of methemoglobinemia is chocolate brown-colored arterial blood. However, suspected cases should be confirmed by co-oximetry, which yields a direct and accurate measure of methemoglobin levels. Standard pulse oximetry readings or arterial blood gas values are not reliable. Clinically significant methemoglobinemia requires immediate treatment.
CANADIAN BRAND NAMES — Anbesol® Baby; Zilactin Baby®; Zilactin-B®
INTERNATIONAL BRAND NAMES — AAA Spray (GB); Anaestherit (AT); Anaesthesin (DE); Auralyt (MX); Baby Orajel (PL); Babydent (CZ); Claudemor (PT); Dentispray (ES, PL); Dermopur (PL); Dolodent (DK); Etylu Aminobenzoesan (PL); Gartricin (ES); Gengivarium (IT); Graneodin-B (MX); Hurricaine (ES, LU); Lanacane (ES); Lodoc (AR); Nani Pre Dental (ES); Octicaina (CO); Orajel (CH, PL); Oramed Gel (IL); Otisyn (FI); Topicaine (AU)
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
Absorption: Topical: Poor to intact skin; well absorbed from mucous membranes and traumatized skin
Metabolism: Hepatic (to a lesser extent) and plasma via hydrolysis by cholinesterase
Excretion: Urine (as metabolites)
PATIENT INFORMATION — Do not eat for 1 hour after application to oral mucosa; chemical burns should be neutralized before application of benzocaine; avoid application to large areas of broken skin, especially in children