Introduction

Local anesthetic.

Uses for Benzocaine (EENT)

Oral Pain

Self-medication (alone or in fixed combination with various other drugs) for temporary relief of minor sore throat pain.

Self-medication (alone or in fixed combination with various other drugs) for temporary relief of pain associated with various oral or dental conditions (e.g., cold sores, ulcerations, canker sores, minor injury/irritation, toothache, sore gums, orthodontic appliances, denture irritation).

FDA states that benzocaine preparations are associated with serious risk (e.g., methemoglobinemia) and provide little to no benefit in treating oral pain. Do not use in infants and children <2 years of age. Use sparingly and only as needed in adults and children ≥2 years of age. (See Methemoglobinemia under Cautions.)

Do not use for teething pain in infants; risk of methemoglobinemia outweighs any potential benefits.

Local Anesthesia

Has been used topically for local anesthesia^{† [off-label]} of oral or other accessible mucous membranes (except eyes).

Fixed-combination preparation containing benzocaine with butamben and tetracaine also has been used for local anesthesia prior to surgical, endoscopic, or other medical procedures, and also for suppressing the gag reflex^{† [off-label]}.

However, methemoglobinemia has occurred and FDA states that benzocaine products are not approved for such uses. (See Methemoglobinemia under Cautions.)

Otic Pain

Has been used topically in fixed combination with antipyrine for temporary relief of ear pain^{† [off-label]} associated with acute otitis media of various causes. However, efficacy and safety not established.

Topical anesthetics may provide symptomatic relief but do not preclude need for appropriate anti-infective therapy when ear pain is secondary to infection.

Cerumen Removal

Has been used in fixed combination with antipyrine to facilitate removal of excessive or impacted cerumen (earwax)^{† [off-label]}. However, efficacy and safety not established.

Benzocaine (EENT) Dosage and Administration

General

• Benzocaine is commercially available (alone and in fixed combination with other drugs [e.g., antitussives, analgesics, demulcents, other local anesthetics]) in many dosage forms, some of which are intended for self-medication; consult manufacturer’s product labeling for complete directions for appropriate dosage and administration of the specific product.

Administration

Oral Administration

Administer orally as a lozenge.

Allow lozenge to slowly dissolve in the mouth.

Topical Administration

Apply topically to mucosal membranes as an aerosol spray, gel, cream, swab, solution, or ointment; consult manufacturer’s product labeling for complete directions for appropriate application of the specific product.

Avoid contact with the eye(s). Not for injection.

Manufacturer of benzocaine in fixed combination with butamben and tetracaine hydrochloride (Cetacaine) recommends application directly to site where pain control is required; not necessary to dry tissue prior to application.

Manufacturers of some topical benzocaine products intended for self-medication suggest that adults supervise children <12 years of age during drug administration.

Aerosol Spray

Amount of benzocaine contained in a single spray varies among preparations and depends on solution concentration, amount of time actuator is depressed, residual volume in can, and spatial orientation of can during administration.

Benzocaine 20% aerosol spray: Spray directly onto oral mucosa.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol spray: Apply over ≤1 second.

Gel, Liquid, Cream, Ointment, or Swab

For self-medication, apply topically using cotton swab or finger according to manufacturer’s directions.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Spread thinly and evenly over the application area using a cotton swab.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) liquid: For dental procedures (e.g., scaling, pre-injection anesthesia), apply topical liquid drop-wise into periodontal pockets using syringe and delivery device supplied by manufacturer. For surface application to mucosal membranes, apply single dip of topical liquid with a cotton or brush applicator. Do not hold applicator in position for an extended period to minimize risk of local reactions.

Dosage

Administer smallest amount required to produce desired response.

Benzocaine is commercially available (alone and in fixed combination with other drugs [e.g., antitussives, analgesics, demulcents, other local anesthetics]) in many dosage forms; consult manufacturer’s product labeling for appropriate dosage of the specific product.

Each 200 mg of Cetacaine aerosol, liquid, or gel contains 28 mg benzocaine, 4 mg butamben, and 4 mg tetracaine hydrochloride.

Pediatric Patients

Oral Pain

Oral

Benzocaine 15-mg lozenge: For self-medication in children ≥3 years of age, take 1 lozenge; repeat every 2 hours as necessary or as directed by a clinician.

Benzocaine 15-mg lozenge (in fixed combination with menthol): For self-medication in children ≥5 years of age, take 1 lozenge; repeat every 2 hours as necessary or as directed by a clinician.

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol): For self-medication in children 6–12 years of age, take 1 lozenge; repeat every 4 hours as needed up to 6 lozenges daily or as directed by a clinician.

Benzocaine 6 or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol): For self-medication in children ≥12 years of age, take 2 lozenges (1 immediately after the other); repeat every 4 hours as necessary up to 12 lozenges daily or as directed by a clinician.

Topical

Benzocaine 10 and 20% gel, swabs, cream, or liquid: For self-medication in children ≥2 years of age, apply up to 4 times daily to affected oral area(s) or as directed by a clinician or dentist.

Benzocaine 20% aerosol spray: For self-medication in children ≥2 years of age, spray for 0.5 seconds by pressing and immediately releasing actuator; use up to 4 times daily or as directed by a clinician or dentist.

Local Anesthesia† [off-label]

Topical

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol, liquid, or gel: Manufacturer states that an appropriate pediatric dosage has not been established; dosage should be reduced in very young patients.

Adults

Oral Pain

Oral

Benzocaine 15-mg lozenge (alone or in fixed combination with menthol): For self-medication, take 1 lozenge; repeat every 2 hours as necessary or as directed by a clinician.

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol): For self-medication, take 2 lozenges (1 immediately after the other); repeat every 4 hours as necessary up to 12 lozenges daily or as directed by a clinician.

Topical

Benzocaine 10 and 20% gel, swabs, ointments, creams, topical aerosols, or liquid: For self-medication, apply to affected oral area up to 4 times daily or as directed by a clinician or dentist.

Benzocaine 20% aerosol spray: For self-medication, spray for 0.5 seconds by pressing and immediately releasing actuator; use up to 4 times daily or as directed by a clinician or dentist.

Local Anesthesia†

Topical

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol: Spray onto site(s) for ≤1 second; at normal temperatures, the average expulsion rate is approximately 200 mg of solution per second. Do not exceed 2 seconds.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) liquid: Apply 0.2 mL (200 mg of solution) with a cotton applicator or directly to the site(s). Do not exceed 0.4 mL (400 mg).

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Apply 200 mg of gel (a bead approximately 0.2–0.5 inches long) to site(s). Do not exceed 400 mg.

Prescribing Limits

Pediatric Patients

Oral Pain

Oral

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol) in children 6–12 years of age: Do not exceed 6 lozenges in 24 hours for a maximum of 2 days for sore throat or 7 days for sore mouth.

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg) in children ≥12 years of age: Do not exceed 12 lozenges in 24 hours for a maximum of 2 days for sore throat or 7 days for sore mouth.

Benzocaine 15-mg lozenges in children ≥3 years of age: Do not use for more than 2 days unless directed by clinician.

Benzocaine 15-mg lozenges (in fixed combination with menthol) in children ≥5 years of age: Do not use for more than 2 days unless directed by clinician.

Topical

Benzocaine 10 or 20% gel, swabs, cream, aerosol spray, ointment, or solution in children ≥2 years of age: Maximum 4 applications daily for 7 days.

Adults

Oral Pain

Oral

Benzocaine 6- or 7.5-mg lozenges (in fixed combination with dextromethorphan with or without menthol): Do not exceed 12 lozenges in 24 hours.

Benzocaine 15-mg lozenges: Do not use for more than 2 days unless directed by clinician.

Topical

Benzocaine 10 or 20% gel, swabs, cream, aerosol spray, ointment, or solution: Maximum 4 applications daily for 7 days.

Local Anesthesia†

Topical

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol spray: Do not spray >2 seconds.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) liquid: Do not apply >0.4 mL (12–14 drops).

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Do not apply >400 mg.

Special Populations

Geriatric Patients

The manufacturers of Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) recommend reducing the dosage in debilitated geriatric patients.

Acutely Ill Patients

The manufacturers of Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) recommend reducing the dosage in acutely ill patients.

Contraindications

• Known or suspected hypersensitivity to benzocaine, other ester-type local anesthetics, or any ingredient in the formulation.

• Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination): Injection or use in eyes; patients with cholinesterase deficiency; application to large areas of denuded or inflamed tissue (excessive systemic absorption could result). Do not apply Cetacaine under dentures or cotton rolls (possible escharotic effect).

Warnings/Precautions

Warnings

Serious Adverse Effects Associated with Local Anesthetics

Serious adverse effects (e.g., seizures, coma, irregular heartbeat, respiratory depression) reported following topical application of local anesthetics to skin; reported after application of extemporaneously compounded topical preparations containing high concentrations of anesthetics for cosmetic procedures and following use for FDA-approved indications. Use lowest concentration likely to be effective, and use in small amounts for shortest period possible; use of FDA-approved preparations recommended.

Methemoglobinemia

Methemoglobinemia, a rare but serious blood disorder, reported after topical benzocaine application; reported mostly with use of aerosol preparations during medical procedures (e.g., intubation, endoscopic, or bronchoscopic procedures), but also with topical application of OTC preparations to oral mucosa. Fatalities have occurred.

Most reported cases with OTC gel and liquid preparations involved children <2 years of age who received benzocaine gel for teething; however, cases also reported in adults using a gel or liquid preparation for toothache relief. Do not use for teething. (See Advice to Patients.)

Manifestations of methemoglobinemia (e.g., pale, gray, or blue-colored skin, lips, or nail beds; headache, lightheadedness, anxiety, confusion, or fatigue; tachycardia; dyspnea, increased respiratory rate, or decreased blood oxygen saturation) may occur within minutes to 1–2 hours following application.

Concomitant ingestion or use of nitrite- or nitrate-containing products (e.g., foods, drugs) may be additive in inducing methemoglobin formation.

Patients with asthma, bronchitis, emphysema, or heart disease and those who smoke may be at risk for methemoglobinemia-related complications; infants <4 months of age, geriatric adults, and individuals with certain inborn defects (e.g., glucose-6-phosphate dehydrogenase deficiency, hemoglobin M disease, NADH methemoglobin reductase deficiency, pyruvate kinase deficiency) may be predisposed to methemoglobinemia.

Development of methemoglobinemia is not dose related; may occur following a single application.

Observe patients receiving aerosol benzocaine preparations for signs of methemoglobinemia during the medical procedure and for ≥2 hours after benzocaine administration.

Do not use benzocaine preparations in children <2 years of age, and use sparingly, only when needed, and not more than 4 times daily in adults and children ≥2 years of age. (See Advice to Patients.)

May obtain a direct measure of methemoglobin through cooximetry (arterial blood gas and standard 2-wavelength pulse oximetry are unreliable). Promptly treat patients who develop methemoglobinemia (e.g., administer methylene blue if appropriate).

Sensitivity Reactions

Tartrazine Sensitivity

Some commercially available formulations of benzocaine (e.g., Orajel Double Medicated Toothache and Gum Relief Plus Liquid, Orajel Mouth Sore Swabs) contain the dye tartrazine (FD&C yellow No. 5), which may cause allergic reactions including bronchial asthma in susceptible individuals. Although the incidence of tartrazine sensitivity is low, it frequently occurs in patients who are sensitive to aspirin.

Hypersensitivity

Hypersensitivity reactions, including anaphylaxis, rarely reported.

Possible dehydration of epithelium and escharotic effect; therefore, do not apply topical benzocaine under dentures or cotton rolls.

Possible localized allergic reactions or contact dermatitis characterized by erythema and pruritus that may progress to vesiculation and oozing; most common after prolonged or repeated use. If rash, urticaria, edema, irritation, or other manifestations of allergy develop, discontinue the drug and consult a clinician. Avoid prolonged use except under continual supervision.

General Precautions

Self-Medication

When used for self-medication for mouth soreness, discontinue drug and consult a clinician if the condition worsens or symptoms persist for >7 days or resolve and occur again within a few days.

When used for self-medication for sore throat, discontinue drug and consult a clinician if sore throat is severe, persists for >2 days, or is accompanied or followed by fever, headache, rash, pain, redness, swelling, nausea, or vomiting.

Fixed-Combination Preparations

When used in fixed combination with other drugs (e.g., antitussives, analgesics, demulcents, other local anesthetics), consider the cautions, precautions, and contraindications associated with the other drug(s).

Specific Populations

Pregnancy

Effects on fetal development not known. Do not use during pregnancy unless benefits outweigh risks.

Pediatric Use

FDA states that benzocaine preparations should not be used in children <2 years of age.

Benzocaine 15 mg (in fixed combination with menthol) lozenges should not be used in children <5 years of age.

Benzocaine 7.5 mg (in fixed combination with dextromethorphan) lozenges should not be used in children <6 years of age.

Appropriate pediatric dosage not established for Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) preparations.

Common Adverse Effects

Generally nontoxic when applied topically, but sensitization and methemoglobinemia may occur. (See Warnings/Precautions under Cautions.)

General

• Benzocaine is commercially available (alone and in fixed combination with other drugs [e.g., antitussives, analgesics, demulcents, other local anesthetics]) in many dosage forms, some of which are intended for self-medication; consult manufacturer’s product labeling for complete directions for appropriate dosage and administration of the specific product.

Administration

Oral Administration

Administer orally as a lozenge.

Allow lozenge to slowly dissolve in the mouth.

Topical Administration

Apply topically to mucosal membranes as an aerosol spray, gel, cream, swab, solution, or ointment; consult manufacturer’s product labeling for complete directions for appropriate application of the specific product.

Avoid contact with the eye(s). Not for injection.

Manufacturer of benzocaine in fixed combination with butamben and tetracaine hydrochloride (Cetacaine) recommends application directly to site where pain control is required; not necessary to dry tissue prior to application.

Manufacturers of some topical benzocaine products intended for self-medication suggest that adults supervise children <12 years of age during drug administration.

Aerosol Spray

Amount of benzocaine contained in a single spray varies among preparations and depends on solution concentration, amount of time actuator is depressed, residual volume in can, and spatial orientation of can during administration.

Benzocaine 20% aerosol spray: Spray directly onto oral mucosa.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol spray: Apply over ≤1 second.

Gel, Liquid, Cream, Ointment, or Swab

For self-medication, apply topically using cotton swab or finger according to manufacturer’s directions.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Spread thinly and evenly over the application area using a cotton swab.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) liquid: For dental procedures (e.g., scaling, pre-injection anesthesia), apply topical liquid drop-wise into periodontal pockets using syringe and delivery device supplied by manufacturer. For surface application to mucosal membranes, apply single dip of topical liquid with a cotton or brush applicator. Do not hold applicator in position for an extended period to minimize risk of local reactions.

Dosage

Administer smallest amount required to produce desired response.

Benzocaine is commercially available (alone and in fixed combination with other drugs [e.g., antitussives, analgesics, demulcents, other local anesthetics]) in many dosage forms; consult manufacturer’s product labeling for appropriate dosage of the specific product.

Each 200 mg of Cetacaine aerosol, liquid, or gel contains 28 mg benzocaine, 4 mg butamben, and 4 mg tetracaine hydrochloride.

Pediatric Patients

Oral Pain

Oral

Benzocaine 15-mg lozenge: For self-medication in children ≥3 years of age, take 1 lozenge; repeat every 2 hours as necessary or as directed by a clinician.

Benzocaine 15-mg lozenge (in fixed combination with menthol): For self-medication in children ≥5 years of age, take 1 lozenge; repeat every 2 hours as necessary or as directed by a clinician.

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol): For self-medication in children 6–12 years of age, take 1 lozenge; repeat every 4 hours as needed up to 6 lozenges daily or as directed by a clinician.

Benzocaine 6 or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol): For self-medication in children ≥12 years of age, take 2 lozenges (1 immediately after the other); repeat every 4 hours as necessary up to 12 lozenges daily or as directed by a clinician.

Topical

Benzocaine 10 and 20% gel, swabs, cream, or liquid: For self-medication in children ≥2 years of age, apply up to 4 times daily to affected oral area(s) or as directed by a clinician or dentist.

Benzocaine 20% aerosol spray: For self-medication in children ≥2 years of age, spray for 0.5 seconds by pressing and immediately releasing actuator; use up to 4 times daily or as directed by a clinician or dentist.

Local Anesthesia† [off-label]

Topical

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol, liquid, or gel: Manufacturer states that an appropriate pediatric dosage has not been established; dosage should be reduced in very young patients.

Adults

Oral Pain

Oral

Benzocaine 15-mg lozenge (alone or in fixed combination with menthol): For self-medication, take 1 lozenge; repeat every 2 hours as necessary or as directed by a clinician.

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol): For self-medication, take 2 lozenges (1 immediately after the other); repeat every 4 hours as necessary up to 12 lozenges daily or as directed by a clinician.

Topical

Benzocaine 10 and 20% gel, swabs, ointments, creams, topical aerosols, or liquid: For self-medication, apply to affected oral area up to 4 times daily or as directed by a clinician or dentist.

Benzocaine 20% aerosol spray: For self-medication, spray for 0.5 seconds by pressing and immediately releasing actuator; use up to 4 times daily or as directed by a clinician or dentist.

Local Anesthesia†

Topical

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol: Spray onto site(s) for ≤1 second; at normal temperatures, the average expulsion rate is approximately 200 mg of solution per second. Do not exceed 2 seconds.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) liquid: Apply 0.2 mL (200 mg of solution) with a cotton applicator or directly to the site(s). Do not exceed 0.4 mL (400 mg).

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Apply 200 mg of gel (a bead approximately 0.2–0.5 inches long) to site(s). Do not exceed 400 mg.

Prescribing Limits

Pediatric Patients

Oral Pain

Oral

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg with or without menthol) in children 6–12 years of age: Do not exceed 6 lozenges in 24 hours for a maximum of 2 days for sore throat or 7 days for sore mouth.

Benzocaine 6- or 7.5-mg lozenge (in fixed combination with dextromethorphan hydrobromide 5 mg) in children ≥12 years of age: Do not exceed 12 lozenges in 24 hours for a maximum of 2 days for sore throat or 7 days for sore mouth.

Benzocaine 15-mg lozenges in children ≥3 years of age: Do not use for more than 2 days unless directed by clinician.

Benzocaine 15-mg lozenges (in fixed combination with menthol) in children ≥5 years of age: Do not use for more than 2 days unless directed by clinician.

Topical

Benzocaine 10 or 20% gel, swabs, cream, aerosol spray, ointment, or solution in children ≥2 years of age: Maximum 4 applications daily for 7 days.

Adults

Oral Pain

Oral

Benzocaine 6- or 7.5-mg lozenges (in fixed combination with dextromethorphan with or without menthol): Do not exceed 12 lozenges in 24 hours.

Benzocaine 15-mg lozenges: Do not use for more than 2 days unless directed by clinician.

Topical

Benzocaine 10 or 20% gel, swabs, cream, aerosol spray, ointment, or solution: Maximum 4 applications daily for 7 days.

Local Anesthesia†

Topical

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol spray: Do not spray >2 seconds.

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) liquid: Do not apply >0.4 mL (12–14 drops).

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Do not apply >400 mg.

Special Populations

Geriatric Patients

The manufacturers of Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) recommend reducing the dosage in debilitated geriatric patients.

Acutely Ill Patients

The manufacturers of Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) recommend reducing the dosage in acutely ill patients.