Oticaine

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Oticaine

Classes

Bulk Agents for Compounding
Combination Topical Counterirritants (selected) and Anesthetics
Other Agents for Local Oral Treatment
Otic Analgesic Formulations
Throat Products
Topical Anti-hemorrhoidals
Topical Local Anesthetics

Administration
Topical Administration
Cream/Ointment/Lotion Formulations

Apply using a cotton applicator to the desired area.

Other Topical Formulations

Aerosol
For external use only. Avoid contact with eyes.
Shake the container each time before using.
Spray each area liberally from a distance of about 6 to 12 inches.
Contents are flammable; do not use near fire or flame, or expose to heat or temperatures above 49 degrees C (120 degrees F).
 
Solution
For external use only. Avoid contact with eyes.
Apply using a cotton applicator to the desired area.
Keep away from fire or flame. Avoid smoking during use and until product has dried.

Rectal Administration

Ointment
For external use only. Apply to cleansed affected area.

Otic Administration

Administer in external ear canal; insert cotton plug into the meatus after instillation.

Other Administration Route(s)

Dental Administration
Gel
Apply to affected area using clean fingertip or a cotton applicator. For toothache, apply to cavity and to the surrounding gums.
 
Topicale 18% Gel Formulation
Avoid contact with the eyes.
Allow to remain in place for at least 1 minute and then spit out.
 
Liquid
Avoid contact with the eyes.
Apply to the affected area using a clean fingertip, cotton, or a cotton applicator.
 
Cream/Ointment
Apply directly to the gums or to the denture surface that comes in contact with the affected area of gums. 
If you are using the dentures, wait a few minutes then reinsert dentures, and you may use your regular denture adhesive with this product.
 
Topicale 18% Ointment Formulation
Avoid contact with eyes.
Allow to remain in place for at least 1 minute and then spit out.
 
Paste
Avoid contact with eyes.
Dab paste onto the affected area using a cotton applicator. 
Allow to remain in place for at least 1 minute and then spit out.
 
Self-Adhering tablet (CankerMelts)
Place the adhesive side with a dimple against the teeth, gums, braces, or oral appliance. Affix the tablet opposite or adjacent to the sore in the mouth.
Hold the tablet in place with the cheek or tongue for 10 seconds. Adhesion will strengthen within minutes. Allow the tablet to slowly dissolve.

Adverse Reactions
Severe

angioedema / Rapid / Incidence not known
bradycardia / Rapid / Incidence not known
seizures / Delayed / Incidence not known
respiratory arrest / Rapid / Incidence not known
cardiac arrest / Early / Incidence not known
coma / Early / Incidence not known
methemoglobinemia / Early / Incidence not known

Moderate

edema / Delayed / Incidence not known
erythema / Early / Incidence not known
contact dermatitis / Delayed / Incidence not known
hypertension / Early / Incidence not known
blurred vision / Early / Incidence not known
hypotension / Rapid / Incidence not known
confusion / Early / Incidence not known
sinus tachycardia / Rapid / Incidence not known

Mild

urticaria / Rapid / Incidence not known
pruritus / Rapid / Incidence not known
photosensitivity / Delayed / Incidence not known
rash / Early / Incidence not known
drowsiness / Early / Incidence not known
dizziness / Early / Incidence not known
shivering / Rapid / Incidence not known
restlessness / Early / Incidence not known
anxiety / Delayed / Incidence not known
headache / Early / Incidence not known
tremor / Early / Incidence not known

Common Brand Names

Advocate Pain Relief Stick, Americaine, Anbesol, Anbesol Baby, Banadyne-3, Benz-O-Sthetic, Boil-Ease, Chloraseptic, Comfort Caine, Dermoplast Postpartum, Dry Socket Remedy, Freez Eez, HURRICAINE, HURRICAINE ONE, HURRICANE Snap-n-Go, Monistat Care, Orabase, OraCoat CankerMelts, Orajel, Orajel Baby, Orajel Maximum Strength, Orajel Severe Pain, Oral Pain Relief, OraMagic Plus, Outgro, Pro-Caine, Topex, Topicale, Topicale Xtra, Zilactin-B

Dea Class

OTC, Rx

Description

Short-acting local anesthetic of the ester type
Used for topical anesthesia
Contraindicated for teething pain and use in pediatric patients younger than 2 years; risk for methemoglobinemia

Dosage And Indications
For the treatment of mild pain to provide topical anesthesia or local anesthesia.
NOTE: For oral or dental uses, see dental anesthesia.
For pain and pruritus associated with minor skin abrasion, burns, sunburn, insect bites or stings, or minor skin irritations.
Topical dosage (benzocaine 5% or 20% spray)
Adults, Adolescents and Children 2 years or older

Apply gel or use spray on affected area not more than 3 to 4 times daily. If using the spray, do not exceed a spray duration of 2 seconds. If condition worsens, or if symptoms persist for more than 7 days or clear up and occur again within a few days, discontinue and consult a physician.

For anesthesia of unbroken skin.
Topical dosage (cream, gel, ointment, or solution)
Adults, Adolescents and Children 2 years or older

Apply to affected areas 3 to 4 times daily, or as needed. If condition worsens, or if symptoms persist for more than 7 days or clear up and occur again within a few days, discontinue and consult a physician.

Topical dosage (benzocaine 5% or 20% spray)
Adults, Adolescents and Children 2 years or older

Spray on affected areas 3 to 4 times daily, or as needed. Do not exceed a spray duration of 2 seconds. If condition worsens, or if symptoms persist for more than 7 days or clear up and occur again within a few days, discontinue and consult a physician.

For oral mucosal anesthesia to control pain and/or suppress the pharyngeal and tracheal gag reflex; or for local anesthesia of accessible mucous membranes before examination, endoscopy or instrumentation; and to facilitate passage of fiberoptic gastroscopes, laryngoscopes, proctoscopes, and sigmoidoscopes.
Topical dosage (Hurricaine Spray)
Adults and Adolescents

Spray on area for one second. May repeat if necessary. Do not exceed a spray duration of 2 seconds.

Topical dosage (gel or solution)
Adults

Apply 20% gel or topical solution either directly to mucosa or to instrument prior to examination, as needed.

For topical anesthesia in the external auditory canal to relieve ear pain related to acute otitis media and otitis externa.
Otic dosage
Adults, Adolescents, and Children

 Instill 4 to 5 drops into external ear canal; insert cotton plug. May repeat every 1 to 2 hours as needed. Do not use if there is a perforated eardrum or ear discharge.

For dental anesthesia or temporary relief of dental pain or oral pain.
Oromucosal dosage (10% or 20% gel, paste, or solution and 18% gel or ointment)
Adults

Apply a pea-size amount topically to the affected area(s) and around gum surrounding the teeth up to 4 times daily.

Children and Adolescents 2 to 17 years

Apply a pea-size amount topically to the affected area(s) and around gum surrounding the teeth up to 4 times daily.

Oromucosal dosage (disintegrating tablet)
Adults

Apply 15 mg (1 tablet) to teeth or gums or braces or appliance opposite or adjacent to the sore every 2 hours as needed.

Children and Adolescents 5 to 17 years

Apply 15 mg (1 tablet) to teeth or gums or braces or appliance opposite or adjacent to the affected area(s) every 2 hours as needed.

For the treatment of hemorrhoids.
Topical dosage (20% ointment)
Adults

Apply a thin layer topically to the external affected area(s) up to 6 times daily.

Adolescents

Apply a thin layer topically to the external affected area(s) up to 6 times daily.

Dosing Considerations
Hepatic Impairment

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Renal Impairment

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Drug Interactions

Adapalene; Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Articaine; EPINEPHrine: (Moderate) Use articaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Benzocaine; Butamben; Tetracaine: (Moderate) Use tetracaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Benzoyl Peroxide; Clindamycin: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Benzoyl Peroxide; Erythromycin: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Benzoyl Peroxide; Sulfur: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
BUPivacaine Liposomal: (Major) Avoid use of other local anesthetics for 96 hours after liposomal bupivacaine administration. Use benzocaine and other formulations of bupivacaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
BUPivacaine: (Major) Avoid use of other local anesthetics for 96 hours after liposomal bupivacaine administration. Use benzocaine and other formulations of bupivacaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
BUPivacaine; EPINEPHrine: (Major) Avoid use of other local anesthetics for 96 hours after liposomal bupivacaine administration. Use benzocaine and other formulations of bupivacaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
BUPivacaine; Meloxicam: (Major) Avoid use of other local anesthetics for 96 hours after liposomal bupivacaine administration. Use benzocaine and other formulations of bupivacaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Calamine; Pramoxine: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed.
Chloroprocaine: (Moderate) Use chloroprocaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Clindamycin; Adapalene; Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.
Dapsone: (Moderate) Coadministration of dapsone with benzocaine may increase the risk of developing methemoglobinemia. Advise patients to discontinue treatment and seek immediate medical attention with any signs or symptoms of methemoglobinemia.
Dibucaine: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed.
Ethyl Chloride: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed.
hydrALAZINE; Isosorbide Dinitrate, ISDN: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Nitrates may also induce methemoglobin formation that will be additive to that formed by benzocaine products. Therefore, caution is warranted when combining nitrate medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Hydrocortisone; Pramoxine: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed.
Isosorbide Dinitrate, ISDN: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Nitrates may also induce methemoglobin formation that will be additive to that formed by benzocaine products. Therefore, caution is warranted when combining nitrate medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Isosorbide Mononitrate: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Nitrates may also induce methemoglobin formation that will be additive to that formed by benzocaine products. Therefore, caution is warranted when combining nitrate medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
lamoTRIgine: (Moderate) Consider ECG monitoring before and during concomitant use of lamotrigine with other sodium channel blockers known to impair atrioventricular and/or intraventricular cardiac conduction, such as benzocaine. Concomitant use of benzocaine with lamotrigine may increase the risk of proarrhythmia, especially in patients with clinically important structural or functional heart disease. In vitro testing showed that lamotrigine exhibits class IB antiarrhythmic activity at therapeutically relevant concentrations.
Lidocaine: (Moderate) Use lidocaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Lidocaine; EPINEPHrine: (Moderate) Use lidocaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Lidocaine; Prilocaine: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed. (Moderate) Use lidocaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Lidocaine; Tetracaine: (Moderate) Use tetracaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Mafenide: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Examples of other drugs that can cause methemoglobinemia include the sulfonamides. Therefore, caution is warranted when combining such medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Menthol; Pramoxine: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed.
Mepivacaine: (Moderate) Use mepivacaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Nitrates: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Nitrates may also induce methemoglobin formation that will be additive to that formed by benzocaine products. Therefore, caution is warranted when combining nitrate medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Nitroglycerin: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Nitrates may also induce methemoglobin formation that will be additive to that formed by benzocaine products. Therefore, caution is warranted when combining nitrate medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Penicillin G Benzathine; Penicillin G Procaine: (Moderate) Coadministration of penicillin G procaine with other local anesthetics, such as benzocaine, may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue penicillin G procaine and any other local anesthetic. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Penicillin G Procaine: (Moderate) Coadministration of penicillin G procaine with other local anesthetics, such as benzocaine, may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue penicillin G procaine and any other local anesthetic. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Pramoxine: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed.
Pramoxine; Zinc Acetate: (Moderate) Caution is advised if combining topical local anesthetics. The toxic effects of local anesthetics are additive. In addition, rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine-containing products. Clinicians should closely monitor patients for the development of methemoglobinemia when a combination local anesthetic is used during a procedure. If a patient becomes cyanotic or if elevated methemoglobin concentrations are suspected, immediately institute treatment to counteract methemoglobinemia (such as administration of methylene blue) as oxygen delivery is ineffective throughout the body until the condition is reversed.
ROPivacaine: (Moderate) Use ropivacaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
sulfADIAZINE: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Examples of other drugs that can cause methemoglobinemia include the sulfonamides. Therefore, caution is warranted when combining such medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Sulfamethoxazole; Trimethoprim, SMX-TMP, Cotrimoxazole: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Examples of other drugs that can cause methemoglobinemia include the sulfonamides. Therefore, caution is warranted when combining such medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
sulfaSALAzine: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Examples of other drugs that can cause methemoglobinemia include the sulfonamides. Therefore, caution is warranted when combining such medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Sulfonamides: (Moderate) Rare and sometimes fatal cases of methemoglobinemia have been reported with the use of topical or oromucosal benzocaine products. Examples of other drugs that can cause methemoglobinemia include the sulfonamides. Therefore, caution is warranted when combining such medications with topical or oromucosal benzocaine products. Patients using OTC benzocaine gels and liquids should be advised to seek immediate medical attention if signs or symptoms of methemoglobinemia develop. In addition, clinicians should closely monitor patients for the development of methemoglobinemia when benzocaine sprays are used during a procedure.
Tetracaine: (Moderate) Use tetracaine and benzocaine together with caution. Monitor cardiovascular and respiratory vital signs, as well as the patient's state of consciousness if used concurrently due to potential for additive CNS and/or cardiovascular toxic effects. Manifestations of toxicity may include CNS excitation and/or depression, cardiac conduction depression, or peripheral vasodilation. Additionally, coadministration may increase the risk of developing methemoglobinemia. Monitor patients closely for signs and symptoms of methemoglobinemia if coadministration is necessary. If methemoglobinemia occurs or is suspected, discontinue local anesthetic use. Depending on the severity of symptoms, patients may respond to supportive care; more severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.
Tretinoin; Benzoyl Peroxide: (Moderate) Concurrent use of benzoyl peroxide and topical anesthetics may decrease the efficacy of the anesthetic. In a clinical study, an estimated 75% increase in patient-reported, prick-induced pain was noted in areas treated with both 5% benzoyl peroxide and 6% benzocaine cream as compared to areas treated with 6% benzocaine cream alone. Investigators attributed the decreased anesthetic effect to a breakdown of the benzocaine molecule by either or both benzoyl peroxide or benzoyl peroxide-derived free radicals. It is recommended that the skin area that is to be topically anesthetized have no previous treatment with benzoyl peroxide or that the skin is thoroughly washed prior to the application of the anesthetic.

How Supplied

Advocate Pain Relief Stick/Banadyne-3/Outgro Topical Sol: 5%, 10%, 20%
Americaine/Boil-Ease Topical Ointment: 20%
Americaine/Dermoplast Postpartum/Monistat Care Topical Spray: 20%
Anbesol/Benzocaine/Benz-O-Sthetic/Boil-Ease/Comfort Caine/Freez Eez/HURRICAINE/Orajel/Orajel Maximum Strength/Orajel Severe Pain/Oral Pain Relief/Pro-Caine/Topicale/Topicale Xtra/Zilactin-B Periodontal Gel: 10%, 18%, 20%
Anbesol/Benzocaine/HURRICAINE/HURRICANE Snap-n-Go/Orajel/Orajel Maximum Strength/OraMagic Plus Periodontal Sol: 10%, 20%
Benzocaine/Benz-O-Sthetic/Topex Oropharyngeal Spray: 20%
Benzocaine/Dermoplast Postpartum/HURRICAINE/HURRICAINE ONE Periodontal Spray: 20%
Chloraseptic Oropharyngeal Lozenge: 15mg
HURRICANE Snap-n-Go Periodontal Swab: 20%
Orabase Buccal Paste: 20%
Orabase Periodontal Paste: 20%
OraCoat CankerMelts Oral Tab Orally Dis: 15mg
Topicale Periodontal Ointment: 18%

Maximum Dosage
Adults

The maximum dosage is dependent on route of administration and indication for therapy.

Geriatric

The maximum dosage is dependent on route of administration and indication for therapy.

Adolescents

The maximum dosage is dependent on route of administration and indication for therapy.

Children

2 to 12 years: The maximum dosage is dependent on route of administration and indication for therapy.
1 year: OTC benzocaine products are contraindicated.

Infants

OTC benzocaine products are contraindicated.

Mechanism Of Action

Like all local anesthetics, benzocaine causes a reversible blockade of nerve conduction by decreasing nerve membrane permeability to sodium. This decreases the rate of membrane depolarization, thereby increasing the threshold for electrical excitability. The blockade affects all nerve fibers in the following sequence: autonomic, sensory, and motor, with effects diminishing in reverse order. Clinically, loss of function occurs as follows: pain, temperature, touch, proprioception, and skeletal muscle tone. Direct nerve membrane penetration is necessary for effective anesthesia, which is achieved by applying the anesthetic topically to the area to be anesthetized.

Pharmacokinetics

Benzocaine is applied topically. Benzocaine is metabolized hepatically. Metabolites are renally excreted.

Topical Route

Benzocaine is minimally absorbed after topical administration. Systemic absorption is favored by broken skin or mucosa. Onset of action is rapid with initial effects obtained in about 1 minute and action lasting about 15—20 minutes.

Pregnancy And Lactation
Pregnancy

There are no adequate data on the developmental risk associated with benzocaine use during human pregnancy. Animal reproduction studies with benzocaine have not been performed. Use during pregnancy only if the maternal condition justifies the potential fetal risks. An increased risk of congenital anomalies was not demonstrated among the children of 47 women treated with benzocaine during the first 4 lunar months of pregnancy or among the children of 238 women treated any time during pregnancy in the Collaborative Perinatal Project. Based upon these data, the use of benzocaine in early in pregnancy may be associated with a low risk of teratogenic effects in humans.

Benzocaine may be taken during breast-feeding. It is not known whether benzocaine is excreted in human breast milk, however in general, topically applied benzocaine is unlikely to affect the nursing infant if it is applied away from the breast. Benzocaine has been associated with life-threatening cases of methemoglobin; products should be applied and used only as directed and the drug should never be applied to the breast or nipple in order to avoid infant ingestion.