Actisep

Drug overview for ACTISEP (benzocaine/menthol/cetylpyridinium chloride):

Generic name: benzocaine/menthol/cetylpyridinium chloride
Drug class: Oral Topical Anesthetics
Therapeutic class: Mouth-Throat-Dental - Preparations

Benzocaine is a local anesthetic.

Benzocaine is used in the form of oral lozenges for the temporary relief of minor sore throat pain or in the form of topical aerosols, gels, creams, ointments, or solutions for the temporary relief of pain associated with various oral or dental conditions (e.g., toothache, sore gums, orthodontic appliances, denture irritation, cold sores, ulcerations, canker sores, minor injury/irritation); benzocaine is commercially available in a variety of over-the-counter (OTC) preparations as a single entity or in fixed combination with other drugs (e.g., dextromethorphan, menthol) for self-medication of these conditions. However, FDA states that OTC benzocaine products are associated with serious risk (e.g., methemoglobinemia) and provide little to no benefit in treating oral pain. (See Methemoglobinemia under Cautions: Precautions and Contraindications.) Benzocaine or other local anesthetics should not be used for the treatment of teething pain in infants because such therapy is not useful and is associated with a risk of methemoglobinemia that outweighs any potential benefit of the drug.

Because of the risk of methemoglobinemia, OTC benzocaine preparations should not be used in infants and children younger than 2 years of age and should be used sparingly and only as needed in adults and children 2 years of age or older. Benzocaine also has been used topically in the form of aerosols, gels, or solutions for local anesthesia+ of oral and other accessible mucous membranes (except the eyes). The fixed-combination preparation containing benzocaine, butamben, and tetracaine hydrochloride (Cetacaine(R)) has been used topically for local anesthesia prior to surgical, endoscopic, or other medical procedures; the aerosol formulation also has been used for suppressing the gag reflex+.

However, FDA states that benzocaine is not approved for these uses. (See Methemoglobinemia under Cautions: Precautions and Contraindications.) Benzocaine (in fixed combination with antipyrine) has been used topically in the external auditory canal for the temporary relief of ear pain+ associated with acute otitis media of various causes. Topical anesthetics may provide symptomatic relief, but they do not preclude the need for appropriate anti-infective therapy when ear pain is secondary to infection.

The efficacy and safety of benzocaine for relief of ear pain have not been established. The fixed combination of benzocaine and antipyrine also has been used topically in the external auditory canal to facilitate removal of excessive or impacted cerumen (earwax)+; however, efficacy and safety of the drug for this use have not been established. For other uses of benzocaine as a topical anesthetic, see 84:08.

DRUG IMAGES

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The following indications for ACTISEP (benzocaine/menthol/cetylpyridinium chloride) have been approved by the FDA:

Indications:
Aphthous stomatitis
Denture stomatitis
Gingivostomatitis
Mouth irritation
Sore throat

Professional Synonyms:
Aphthous ulcer
Burning sensation of throat
Denture sore mouth
Oral irritation
Pharyngeal pain
Pharyngeal soreness
Sore throat symptom
Ulcerative stomatitis

The following dosing information is available for ACTISEP (benzocaine/menthol/cetylpyridinium chloride):

Dosing
Administration
Dosing Information
Generic

No enhanced Dosing information available for this drug.

Benzocaine is administered orally as a lozenge or applied topically to mucous membranes as an aerosol spray, swab, gel, solution, cream, or ointment. The drug should not be administered as an injection. Benzocaine is commercially available alone or 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; the manufacturer's product labeling should be consulted for complete directions for appropriate dosage and administration of the specific product.

The smallest amount required to produce the desired response should be administered. Benzocaine lozenges are administered orally by dissolving the lozenge slowly in the mouth. For topical application, benzocaine may be applied to any accessible mucous membrane except for the eyes.

When using aerosol preparations, the amount of benzocaine contained in a single spray varies based on the concentration of the solution, amount of time the actuator is depressed, residual volume in the can, and spatial orientation of the can during administration. The manufacturer of benzocaine in fixed combination with butamben and tetracaine hydrochloride (Cetacaine(R)) recommends application directly to the site where pain control is required; it is not necessary to dry the tissue prior to application. The manufacturers of some topical benzocaine products intended for self-medication suggest that adults supervise children younger than 12 years of age during drug administration.

No dosing information available.

No generic dosing information available.

The following drug interaction information is available for ACTISEP (benzocaine/menthol/cetylpyridinium chloride):

Contraindicated
Severe
Moderate

There are 0 contraindications.

There are 1 severe interactions. These drug interactions can produce serious consequences in most patients. Actions required for severe interactions include, but are not limited to, discontinuing one or both agents, adjusting dosage, altering administration scheduling, and providing additional patient monitoring. Review the full interaction monograph for more information.

Drug Interaction	Drug Names
Long-acting Bupivacaine/Local Anesthetics SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction. MECHANISM OF ACTION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1) CLINICAL EFFECTS: Concurrent or use of local anesthetics with 96 hours of use of long-acting bupivacaine may result in neurologic and cardiovascular toxicity. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also result in methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1) PREDISPOSING FACTORS: Use of additional agents that are associated with methemoglobinemia may further increase the risk of methemoglobinemia.(1) Patients who are at increased risk of developing methemoglobinemia include those with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended.(1) PATIENT MANAGEMENT: Avoid the use of other local anesthetics within 96 hours following the administration of long-acting bupivacaine. In patients for whom use is required, monitor for neurologic and cardiovascular effects. Also monitor for methemoglobinemia with use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine.(1,2) Non-liposomal bupivacaine may be administered in the same syringe as bupivacaine liposomal or injected immediately before bupivacaine liposomal as long as the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1) DISCUSSION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposome bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally. Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1)	BUPIVACAINE LIPOSOME, EXPAREL, XARACOLL, ZYNRELEF

Drug Interaction

Drug Names

Long-acting Bupivacaine/Local Anesthetics

SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.

MECHANISM OF ACTION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1)

CLINICAL EFFECTS: Concurrent or use of local anesthetics with 96 hours of use of long-acting bupivacaine may result in neurologic and cardiovascular toxicity. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also result in methemoglobinemia.(1,2) Non-liposomal bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally.(1)

PREDISPOSING FACTORS: Use of additional agents that are associated with methemoglobinemia may further increase the risk of methemoglobinemia.(1) Patients who are at increased risk of developing methemoglobinemia include those with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended.(1)

PATIENT MANAGEMENT: Avoid the use of other local anesthetics within 96 hours following the administration of long-acting bupivacaine. In patients for whom use is required, monitor for neurologic and cardiovascular effects. Also monitor for methemoglobinemia with use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine.(1,2)

Non-liposomal bupivacaine may be administered in the same syringe as bupivacaine liposomal or injected immediately before bupivacaine liposomal as long as the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1) Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1)

DISCUSSION: Concurrent use of other local anesthetics or use of other local anesthetics within 96 hours following long-acting bupivacaine may result in additive neurologic and cardiovascular effects. Use of articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, and tetracaine may also increase the risk of methemoglobinemia.(1,2) Non-liposome bupivacaine may impact the pharmacokinetic and/or physicochemical properties of the liposomal formulation when administered in the same syringe or used simultaneously unless the ratio of mg of non-liposomal bupivacaine to mg of bupivacaine liposomal does not exceed 1:2.(1)

Local anesthetics other than bupivacaine may trigger the immediate release of bupivacaine from the liposomal formulation when administered together locally. Lidocaine may be administered 20 minutes or more prior to bupivacaine. It is unknown if other local anesthetics may be used without compromising the release characteristic of bupivacaine liposomal.(1)

BUPIVACAINE LIPOSOME, EXPAREL, XARACOLL, ZYNRELEF

There are 0 moderate interactions.

The following contraindication information is available for ACTISEP (benzocaine/menthol/cetylpyridinium chloride):

Overview
Contraindicated
Severe
Moderate

Drug contraindication overview.

No enhanced Contraindications information available for this drug.

There are 1 contraindications. Absolute contraindication.

Contraindication List
Methemoglobinemia

There are 5 severe contraindications. Adequate patient monitoring is recommended for safer drug use.

Severe List
Glucose-6-phosphate dehydrogenase (g6Pd) deficiency
Hemolytic anemia from pyruvate kinase and g6PD deficiencies
NADH methemoglobin reductase deficiency
Pregnancy
Systemic mastocytosis

There are 0 moderate contraindications.

The following adverse reaction information is available for ACTISEP (benzocaine/menthol/cetylpyridinium chloride):

Overview
Severe
Less Severe

Adverse reaction overview.

No enhanced Common Adverse Effects information available for this drug.

There are 2 severe adverse reactions.

More Frequent	Less Frequent
None.	Angioedema

Rare/Very Rare
Methemoglobinemia

There are 6 less severe adverse reactions.

More Frequent	Less Frequent
None.	Contact dermatitis Erythema Mouth irritation Pruritus of skin Skin rash Urticaria

Rare/Very Rare
None.

The following precautions are available for ACTISEP (benzocaine/menthol/cetylpyridinium chloride):

Pediatric
Pregnant
Lactation
Geriatric

No enhanced Pediatric Use information available for this drug.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None

No enhanced Pregnancy information available for this drug.

No enhanced Lactation information available for this drug.

No enhanced Geriatric Use information available for this drug.

Aphthous stomatitis
K12.0	Recurrent oral aphthae
Denture stomatitis
K12.1	Other forms of stomatitis
Gingivostomatitis
K05.10	Chronic gingivitis, plaque induced
Mouth irritation
K13.79	Other lesions of oral mucosa
Sore throat
R07.0	Pain in throat