Brand names: Americaine, Anbesol, Chloraseptic, Hurricaine, Mycinettes, Topex, Zilactin-B
Drug class: Local Anesthetics
CAS number: 94-09-7

Medically reviewed by Drugs.com on Apr 10, 2024. Written by ASHP.

Introduction

Local anesthetic.^{111 112 113 114 115 116 117 118 119 120 121 122 123 124 125 126 127 128 129 130 a}

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.^{114 115 124 126}

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).^{111 112 113 114 115 116 117 118 119 120 121 122}

FDA states that benzocaine preparations are associated with serious risk (e.g., methemoglobinemia) and provide little to no benefit in treating oral pain.¹⁰⁸ Do not use in infants and children <2 years of age.¹⁰⁸ Use sparingly and only as needed in adults and children ≥2 years of age.^{108 109} (See Methemoglobinemia under Cautions.)

Do not use for teething pain in infants; risk of methemoglobinemia outweighs any potential benefits.^{108 109 111 112 117}

Local Anesthesia

Has been used topically for local anesthesia^{† [off-label]} of oral or other accessible mucous membranes (except eyes).^{125 127 128 129}

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]}.^{127 128 129}

However, methemoglobinemia has occurred and FDA states that benzocaine products are not approved for such uses.¹⁰⁸ (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.¹²³ However, efficacy and safety not established.^{107 123}

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

Cerumen Removal

Has been used in fixed combination with antipyrine to facilitate removal of excessive or impacted cerumen (earwax)^{† [off-label]}.¹²³ However, efficacy and safety not established.^{107 123}

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.^{114 115 124}

Allow lozenge to slowly dissolve in the mouth.^{114 115 124}

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.^{111 112 113 116 117 118 119 120 121 127 128 129}

Avoid contact with the eye(s).^{111 112 113 127 128 129} Not for injection.^{127 128 129}

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.^{127 128 129}

Manufacturers of some topical benzocaine products intended for self-medication suggest that adults supervise children <12 years of age during drug administration.^{111 112 113 116 118}

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.¹⁰⁵

Benzocaine 20% aerosol spray: Spray directly onto oral mucosa.^{125 130}

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol spray: Apply over ≤1 second.¹²⁹

Gel, Liquid, Cream, Ointment, or Swab

For self-medication, apply topically using cotton swab or finger according to manufacturer’s directions.^{111 112 113 116 117 118 119 120 121 122}

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Spread thinly and evenly over the application area using a cotton swab.¹²⁸

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.¹²⁷ For surface application to mucosal membranes, apply single dip of topical liquid with a cotton or brush applicator.¹²⁷ Do not hold applicator in position for an extended period to minimize risk of local reactions.¹²⁷

Dosage

Administer smallest amount required to produce desired response.¹⁰⁸

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.^{127 128 129}

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.¹²⁴

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.¹¹⁵

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.^{114 126}

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.^{114 126}

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.^{111 112 113 116 117 118 119 120 121 122}

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.¹³⁰

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.^{127 128 129}

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.^{115 124}

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.^{114 126}

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.^{111 112 113 116 117 118 119 120 121 122}

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.¹³⁰

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.¹²⁹ Do not exceed 2 seconds.¹²⁹

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).¹²⁷ Do not exceed 0.4 mL (400 mg).¹²⁷

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).¹²⁸ Do not exceed 400 mg.¹²⁸

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.^{114 126}

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.^{114 126}

Benzocaine 15-mg lozenges in children ≥3 years of age: Do not use for more than 2 days unless directed by clinician.¹²⁴

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.¹¹⁵

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.^{111 112 113 116 118 119 120 121 122 130}

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.^{114 126}

Benzocaine 15-mg lozenges: Do not use for more than 2 days unless directed by clinician.^{115 124}

Topical

Benzocaine 10 or 20% gel, swabs, cream, aerosol spray, ointment, or solution: Maximum 4 applications daily for 7 days.^{111 112 113 116 117 118 119 120 121 122 130}

Local Anesthesia†

Topical

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) aerosol spray: Do not spray >2 seconds.¹²⁹

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) liquid: Do not apply >0.4 mL (12–14 drops).¹²⁷

Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel: Do not apply >400 mg.¹²⁸

Special Populations

Geriatric Patients

The manufacturers of Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) recommend reducing the dosage in debilitated geriatric patients.^{127 128 129}

Acutely Ill Patients

The manufacturers of Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) recommend reducing the dosage in acutely ill patients.^{127 128 129}

Cautions for Benzocaine (EENT)

Contraindications

• Known or suspected hypersensitivity to benzocaine, other ester-type local anesthetics, or any ingredient in the formulation.^{111 112 113 114 115 116 117 118 119 120 121 a}

• 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).^{127 128 129} Do not apply Cetacaine under dentures or cotton rolls (possible escharotic effect).^{127 128 129}

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.¹⁰⁴ Use lowest concentration likely to be effective, and use in small amounts for shortest period possible; use of FDA-approved preparations recommended.¹⁰⁴

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.^{100 101 102 103 105 106 108} Fatalities have occurred.¹⁰⁸

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.¹⁰⁶ Do not use for teething.¹⁰⁸ (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.^{100 105 106 108}

Concomitant ingestion or use of nitrite- or nitrate-containing products (e.g., foods, drugs) may be additive in inducing methemoglobin formation.^{105 106 108}

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.^{100 105 106 108}

Development of methemoglobinemia is not dose related; may occur following a single application.¹⁰⁵

Observe patients receiving aerosol benzocaine preparations for signs of methemoglobinemia during the medical procedure and for ≥2 hours after benzocaine administration.^{100 105}

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.¹⁰⁶ (See Advice to Patients.)

May obtain a direct measure of methemoglobin through cooximetry (arterial blood gas and standard 2-wavelength pulse oximetry are unreliable).^{100 103 105 106 108} Promptly treat patients who develop methemoglobinemia (e.g., administer methylene blue if appropriate).¹⁰⁰

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.^{119 121 a} Although the incidence of tartrazine sensitivity is low, it frequently occurs in patients who are sensitive to aspirin.^a

Hypersensitivity

Hypersensitivity reactions, including anaphylaxis, rarely reported.¹²⁷

Possible dehydration of epithelium and escharotic effect; therefore, do not apply topical benzocaine under dentures or cotton rolls.¹²⁷

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.¹²⁷ If rash, urticaria, edema, irritation, or other manifestations of allergy develop, discontinue the drug and consult a clinician.^{111 112 116 117 118 119 120} Avoid prolonged use except under continual supervision.¹²⁷

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.^{111 112 113 114 115 118 119}

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.^{111 112 114 115}

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).^{113 114 115 118 120 121 122 127}

Specific Populations

Pregnancy

Effects on fetal development not known.¹²⁷ Do not use during pregnancy unless benefits outweigh risks.¹²⁷

Pediatric Use

FDA states that benzocaine preparations should not be used in children <2 years of age.¹⁰⁸

Benzocaine 15 mg (in fixed combination with menthol) lozenges should not be used in children <5 years of age.¹¹⁵

Benzocaine 7.5 mg (in fixed combination with dextromethorphan) lozenges should not be used in children <6 years of age.¹¹⁴

Appropriate pediatric dosage not established for Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) preparations.¹²⁷

Common Adverse Effects

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

Benzocaine (EENT) Pharmacokinetics

Absorption

Onset

Following Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel, liquid, or spray administration, anesthesia occurs within approximately 30 seconds to 1 minute.^{127 128 129}

Following topical application of benzocaine 20% aerosol, anesthesia occurs within approximately 20 seconds.¹³⁰

Duration

Following Cetacaine (benzocaine, butamben, and tetracaine hydrochloride fixed combination) gel, liquid, or spray administration, anesthesia lasts approximately 30–60 minutes.^{127 128 129}

Stability

Storage

Oral

Lozenges

20–25°C.^{114 115} Protect from humidity.^{114 115}

Topical

Gel, Liquid, and Ointment

20–25°C.^{111 112 113 117} Do not refrigerate.¹¹⁷

Aerosol

20% aerosol: 15–30°C.¹²⁵

Actions

• Alleviates pain and discomfort.^{111 112 113 114 115 116 118}

Advice to Patients

• Before recommending use of benzocaine preparations, inform patients or caregivers of the signs and symptoms of methemoglobinemia and advise them to seek immediate medical attention if such manifestations occur.^{106 108}

• Advise parents and caregivers not to use benzocaine or other local anesthetics for treatment of teething pain in infants and children, and to follow recommendations by AAP for alternative treatment options (e.g., rubbing or massaging gums with fingers, using a firm rubber teething ring).^{108 109} Advise adults experiencing mouth soreness or pain to follow treatment strategies recommended by the American Dental Association.¹⁰⁸

• Advise patients not to use OTC benzocaine products in children <2 years of age and to use sparingly, only as needed, and no more than 4 times a day in adults and children ≥2 years of age.¹⁰⁸

• Advise patients, parents, and caregivers to store benzocaine preparations out of reach of children.¹⁰⁶

• Importance of discontinuing therapy and consulting clinician if swelling, rash, irritation, or fever develops during therapy.^{111 112 114 115 116 118}

• Importance of avoiding contact with the eyes.^{111 112 113 127}

• Importance of using as directed and not applying topical preparations in large quantities, particularly over raw surfaces or blistered areas.¹²⁷

• Advise patients using benzocaine preparations for self-medication not to exceed the recommended dosage or duration of therapy and to carefully read the manufacturer’s product labeling; importance of following directions for appropriate dosage and administration.^{111 114 115 116 118 119 120 121 122}

• Advise patients using benzocaine for self-medication of mouth soreness or toothache to discontinue the drug and consult a clinician if symptoms do not improve after 7 days or if irritation, pain, or redness persists or worsens.^{111 112 113 114 115 116 118 119}

• Advise patients using benzocaine for self-medication of sore throat to consult a clinician if sore throat is severe, persists for >2 days, or is accompanied or followed by fever, headache, rash, swelling, nausea, or vomiting.^{114 115}

• Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.¹²⁷

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹²⁷

• 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.

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