Benzocaine

Uses and Indications

This drug is indicated for the prevention of premature ejaculation and helps in temporarily prolonging the time until ejaculation. It is available in various forms, including gels, creams, and wipes.

Oral Pain Relief

This drug is indicated for the temporary relief of pain associated with:

• Toothaches

• Canker sores

• Cold sores

• Minor dental procedures

• Sore gums

• Minor irritation or injury of the mouth and gums caused by dentures or orthodontic appliances

Anal and Perianal Pain Relief

This drug is indicated for the temporary relief of pain or soreness in the perianal area and is also used as a desensitizing lubricant for less painful anal penetration.

Insect Bite and Sting Relief

This drug is indicated for the temporary relief of pain and itching associated with insect bites, stings, and minor burns.

Teething Relief

This drug is indicated for the temporary relief of sore gums due to teething in infants and children aged 4 months and older. For children under 2 years of age, consultation with a physician or healthcare provider is recommended.

Limitations of Use

• For oral mucosal use only, as directed by a dentist.

• Some products are for professional use only.

• Consult a doctor prior to use if the partner is pregnant.

Special Conditions

• Children under 2 years of age should not use certain products without medical advice.

• Some products may not provide relief for premature ejaculation due to underlying conditions requiring medical supervision.

Dosage and Administration

For topical anesthetics and desensitizing agents, the following dosage and administration guidelines are provided for healthcare professionals:

Topical Application for Genital Area:

• For adults, a small amount of the product should be applied to the head and shaft of the penis 2-10 minutes before intercourse, depending on the specific product used. The application should be done on intact, non-inflamed skin. Excess product should be wiped off prior to intercourse, and the product must be washed off after intercourse. The maximum frequency of application should not exceed four times per day.

Topical Application for Oral Mucosa:

• For adults and children aged 2 years and older, apply only the amount needed to the oral mucosa to prevent or relieve pain. This can be done up to four times daily or as directed by a dentist or physician. Children under 2 years of age should not use these products.

Topical Application for Affected Areas:

• For adults and children aged 2 years and older, apply a small amount of the product to the affected area up to 3-4 times daily. The application should be done using a fingertip, cotton swab, or applicator, and the area should be dry before application. Children under 12 years of age should be supervised during use, and children under 2 years of age should consult a physician.

Preparation and Administration Notes:

• Prior to application, the affected area should be cleansed with mild soap and warm water, then dried gently. For products intended for the genital area, allow sufficient time for the product to dry before engaging in sexual activity.

• For oral applications, the product should be allowed to remain in place for at least one minute before spitting out, if applicable.

Special Considerations:

• It is essential to consult a healthcare professional for children under 2 years of age regarding the use of these products.

• The specific amount and waiting time for desensitization may vary based on individual response and should be determined after several uses.

These guidelines ensure safe and effective use of topical anesthetics and desensitizing agents across various applications.

Contraindications

Use of the product is contraindicated in individuals with known allergies to benzocaine and PABA compounds. Additionally, it should not be used in patients with a history of allergies to local anesthetics such as procaine, butacaine, or other ‘caine’ anesthetics. The product is also contraindicated for use in children under 2 years of age and should not be used for teething.

In cases of accidental ingestion, medical help should be sought immediately, or a Poison Control Center should be contacted. The product should not be used near the eyes or on large areas of the body. If symptoms persist or worsen, or if a rash or irritation develops, the use of the product should be discontinued, and a healthcare professional should be consulted.

For specific formulations, additional contraindications may apply, such as avoiding use if the patient is pregnant or has liver or kidney problems.

Warnings and Precautions

For external use only. Avoid contact with the eyes. If contact occurs, flush with water.

Serious Warnings

• Methemoglobinemia Warning: Use of this product may cause methemoglobinemia, a serious condition that must be treated promptly as it reduces the amount of oxygen carried in the blood. This can occur even if the product has been used before. Seek immediate medical attention if you or a child in your care develops:

  • Pale, gray, or blue colored skin (cyanosis)

  • Headache

  • Rapid heart rate

  • Shortness of breath

  • Dizziness or lightheadedness

  • Fatigue or lack of energy

• Allergy Alert: Do not use on patients with a history of allergies to local anesthetics such as procaine, butacaine, benzocaine, or other "caine" anesthetics.

Usage Precautions

• Do not use for more than 7 days unless directed by a physician. If sore mouth symptoms do not improve in 7 days, or if irritation, pain, or redness persists or worsens, or if swelling, rash, or fever develops, consult a physician promptly.

• Do not use for teething or in children under 2 years of age.

• Keep out of reach of children. If swallowed, get medical help or contact a Poison Control Center right away.

Monitoring Requirements

• Stop use and consult a doctor if:

  • Symptoms do not improve in 7 days.

  • Swelling, rash, or fever develops.

  • Irritation, pain, or redness persists or worsens.

  • You or your partner develop a rash or irritation, such as burning or itching.

General Precautions

• Certain individuals may develop allergic reactions from ingredients in this product. If the symptom being treated does not subside or if redness, irritation, swelling, pain, or other symptoms develop or increase, discontinue use and consult a doctor.

• Do not exceed the recommended dosage. If more than the recommended amount is accidentally swallowed, get medical help or contact a Poison Control Center immediately.

Special Considerations

• If pregnant or breastfeeding, consult a physician before use.

• This product is flammable; do not use near heat or flame. Avoid smoking during application and until the product has dried.

Side Effects

Patients using topical anesthetics may experience a range of adverse reactions, which can vary in severity and frequency. The following summarizes the potential adverse reactions based on the provided data:

Serious Adverse Reactions

• Methemoglobinemia: This serious condition can occur with the use of certain topical anesthetics, leading to reduced oxygen levels in the blood. Symptoms may include:

  • Pale, gray, or blue-colored skin (cyanosis)

  • Headache

  • Rapid heart rate

  • Shortness of breath

  • Dizziness or lightheadedness

  • Fatigue or lack of energy

  • Immediate medical attention is required if these symptoms develop (Labels 2, 18, 21, 39, 50, 51, 62, 70, 79, 140).

Common Adverse Reactions

• Allergic Reactions: Patients with a history of allergies to local anesthetics (e.g., procaine, butacaine, benzocaine) should avoid these products. Allergic reactions may manifest as:

  • Rash

  • Itching

  • Burning sensation

  • Swelling

  • Discontinue use and consult a physician if these symptoms occur (Labels 2, 9, 10, 22, 31, 47, 91, 119).

General Warnings

• External Use Only: All products are intended for external use only and should not come into contact with the eyes. If contact occurs, flush with water (Labels 1, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169).

Additional Considerations

• Duration of Use: Many products should not be used for more than 7 days unless directed by a physician. If symptoms do not improve within this timeframe, patients should seek medical advice (Labels 2, 9, 10, 22, 31, 47, 91, 119).

• Pregnancy and Breastfeeding: Consultation with a healthcare provider is recommended before use during pregnancy or breastfeeding (Labels 2, 9, 10, 22, 31, 47, 91, 119).

Patients are advised to monitor for any adverse reactions and consult a healthcare professional if they experience any concerning symptoms.

Drug Interactions

The reviewed products, including various creams, ointments, sprays, and wipes, generally do not present any documented drug interactions. The following summarizes the findings:

General Observations

• No Documented Interactions: Most products, including Stallion, Sta-Hard, Instant Erection, Anal-Ese, Cvs Maximum Strength Boil Relief, and many others, have no reported drug interactions or interactions with laboratory tests.

Specific Considerations

• Bvibe Spearmint Deep Throat: This product contains an allergy alert for individuals allergic to benzocaine or other local anesthetics such as lidocaine and procaine. It is contraindicated for those with a history of methemoglobinemia or those taking related medications, including nitrates and sulfonamides. Users are advised to consult a healthcare provider if they are taking any interacting medications.

Conclusion

Overall, the majority of the reviewed products lack specific interaction data, indicating a low likelihood of drug interactions. However, caution is advised with Bvibe Spearmint Deep Throat due to its specific contraindications and allergy alerts.

Pediatric Use

Pediatric patients should be closely monitored when using topical products, and specific age-related guidelines must be followed.

Efficacy and Safety:

• For products intended for children aged 2 years and older, such as ointments and creams, the application should not exceed 3 to 4 times daily.

• Children under 2 years of age should consult a physician before use of any topical products, including creams, ointments, and gels.

• Certain products, such as lozenges, are contraindicated for children under 6 years of age. For example, Chloraseptic lozenges should not be used for teething in this age group.

Dosage Guidelines:

• Cvs Maximum Strength Boil Relief: For adults and children 2 years and older, apply to the affected area no more than 2 times daily. Consult a doctor for children under 2 years.

• Painless Tattoo 1: For children 12 years and older, apply to the affected area not more than 3 to 4 times daily. Children under 12 years should ask a doctor.

• Flocean Anti-Itch: Adults and children 12 years and older may apply a fingertip amount to the affected area not more than 3 to 4 times daily. Children under 12 years should consult a doctor.

• Americaine: For children under 12 years, consult a physician. For those 2 years and older, apply to the affected area not more than 3 to 4 times daily.

• Goodsense Oral Pain Relief: Not to be used in children under 2 years. Children 2 years and older may use the product under supervision.

Cautions:

• All products should be kept out of reach of children. In case of accidental ingestion, medical help should be sought immediately, or a Poison Control Center should be contacted.

• Certain products may pose risks of serious conditions, such as methemoglobinemia, particularly in children. Symptoms to watch for include pale, gray, or blue-colored skin (cyanosis), headache, rapid heart rate, shortness of breath, dizziness, or fatigue. Immediate medical attention is required if these symptoms occur.

In summary, pediatric use of topical products requires careful adherence to age-specific guidelines and safety precautions to ensure the well-being of children.

Geriatric Use

No specific information regarding geriatric use, dosage adjustments, safety concerns, or special precautions for elderly patients is provided in the inserts for the following products: Stallion Delay Creme, Sta-Hard, Instant Erection, Anal-Ese, Cvs Maximum Strength Boil Relief, Sting Relief Prep Pad, Dynamo Wellness Delay Max Wipe, Spartan Wipes, KY Duration for Him, Painless Tattoo 1, PROMESCENT® endurance wipes, Bvibe Spearmint Deep Throat, Blt 1, Ombre Men Overtime Wipes, A and E Marathon Delay Serum, A and E Deep Throat Desensitizing Spray (strawberry and peppermint), A and E Easy Anal Gel, 5 Elementum Delay Wipes, Flocean Anti-Itch, Americaine (aerosol and ointment), Mint Rx Endurance Wipes, Neuromed (cream), Chloraseptic Warming Green Tea and Honey Lemon lozenges, Brace Relief, Jo Prolonger with Benzocaine, Lubelife Climax Control Delay, Goodsense Oral Pain Relief, Pleasure Balm, and Xpect Sting Wipes.

Healthcare professionals should exercise caution when prescribing these products to geriatric patients due to the lack of specific data on their use in this population. Monitoring for efficacy and safety is recommended.

Pregnancy

The safety of various products during pregnancy has not been well established, and healthcare professionals are advised to exercise caution when recommending these products to pregnant patients.

For several creams and gels, including Stallion, Sta-Hard, Instant Erection, Anal-Ese, and others, there is no specific information regarding their use during pregnancy, safety concerns, dosage modifications, or special precautions. As such, healthcare providers should consider the lack of data when advising pregnant patients.

Cvs Maximum Strength Boil Relief ointment indicates that its safety during pregnancy has not been established, and it is recommended that pregnant patients consult a doctor before use. There are no adequate and well-controlled studies in pregnant women, and it should be used only if clearly needed.

Products containing benzocaine, such as Painless Tattoo 1, Americaine, and Brace Relief, are contraindicated in pregnancy due to potential risks to the fetus. The safety of benzocaine during pregnancy has not been established, and it is advised that pregnant women consult a healthcare provider before use. Potential risks associated with benzocaine include adverse effects on fetal development.

For products like Sensicaine Tm Extra, Ky Duration for Him, and others, it is recommended that pregnant or breastfeeding individuals consult a healthcare professional before use.

In summary, due to the lack of established safety data and potential risks, healthcare providers should recommend that pregnant patients consult with them prior to using any of these products.

Lactation

There are no specific warnings or recommendations regarding the use of various topical products in nursing mothers, including creams, ointments, and sprays. However, several products indicate a potential for excretion in breast milk, and caution is advised when administering these products to lactating mothers.

For instance, nursing mothers are advised to consult a physician before using products such as Flocean Anti-Itch, Americaine (both ointment and aerosol forms), Jo Prolonger with Benzocaine, and Pleasure Balm, as these may excrete into breast milk. The safety of these products during lactation has not been established, and the effects on breastfed infants are not well studied.

In contrast, other products, including Stallion Delay Creme, STA-HARD desensitizing lubricant cream, and Anal-Ese, do not provide specific information regarding excretion in breast milk or associated risks to infants. Therefore, while there are no explicit contraindications, the lack of data necessitates a cautious approach when considering the use of these products during lactation.

Healthcare professionals should be consulted for personalized guidance regarding the use of any topical products while breastfeeding.

Renal Impairment

Patients with renal impairment may require careful consideration when using certain topical products. While many product labels do not provide specific information regarding dosage adjustments, monitoring, or safety considerations for individuals with kidney problems, a few labels do offer guidance.

For instance, it is noted that renal impairment may necessitate dosage adjustments, particularly for patients with reduced renal function. Regular monitoring of renal function tests is recommended for these patients. Specifically, a reduced dose should be considered for patients with a creatinine clearance of less than 30 mL/min.

In particular, products such as Flocean Anti-Itch and Family Wellness highlight the need for dosage adjustments and monitoring in patients with known kidney issues. Additionally, Gingicaine Fusion emphasizes the importance of monitoring renal function tests prior to and during treatment, especially for those with significant renal impairment.

Overall, while many products lack detailed guidance, it is crucial for healthcare providers to assess renal function and consider potential adjustments in dosing for patients with renal impairment to ensure safety and efficacy.

Hepatic Impairment

Patients with hepatic impairment may not require specific dosage adjustments, special monitoring, or precautions when using the following products, as no relevant information is provided in the product inserts:

• Prolong (Gel)

• Ms Topical Anesthetic (Gel)

• Stallion (Cream)

• Sta-Hard (Cream)

• Instant Erection (Cream)

• Anal-Ese (Cream)

• Rite Aid Liquid Anesthetic Oral Pain Relief (Gel)

• Cvs Maximum Strength Boil Relief (Ointment)

• Bite and Sting Relief (Spray)

• Cainetips (Liquid)

• Inderma Md (Cream)

• Sting Relief Prep Pad (Solution)

• Defend (Gel)

• Gumnumb Topical Anesthetic (Gel)

• Oral Pain Relief (Gel)

• Benz O Sthetic (Gel)

• Vistacaine Topical Anesthetic (Gel)

• and many others.

However, for products such as Jo Prolonger with Benzocaine (Spray) and Lubelife Climax Control Delay (Spray), it is advised that patients consult a doctor before use if they have or have had liver or kidney problems.

Overall, healthcare providers should assess the individual needs of patients with hepatic impairment when considering the use of these products, as specific recommendations may vary based on the patient's overall health status and concurrent medications.

Overdosage

In the event of an overdose, it is crucial to seek immediate medical assistance or contact a Poison Control Center. Symptoms of overdose may vary depending on the specific product involved, but common recommendations include monitoring for any adverse reactions and ensuring that the individual receives appropriate medical evaluation.

For products that are gels or creams, it is advised not to exceed the recommended dosage. If more than the prescribed amount is accidentally swallowed, medical help should be sought without delay. This is particularly emphasized for topical anesthetics and pain relief products, where accidental ingestion can lead to serious complications.

Specific products highlight the importance of contacting a Poison Control Center if swallowed, including those labeled as topical anesthetics, oral pain relief gels, and various creams. In cases where the product is intended for oral use, such as liquid anesthetics, immediate medical attention is critical if an overdose occurs.

Additionally, certain products may carry warnings about the risks associated with intentional misuse, such as inhalation or excessive application, which can be harmful or even fatal. Therefore, it is essential to adhere strictly to the recommended dosages and to act promptly in the case of accidental ingestion or overdose.

Nonclinical Toxicology

Teratogenic Effects

No teratogenic effects were observed in animal studies for certain products, including Bvibe Spearmint Deep Throat and Mint Rx Endurance Wipes. Additionally, no increase in fetal malformations was noted in these studies.

Non-Teratogenic Effects

Animal studies have not reported any non-teratogenic effects associated with the evaluated products.

Nonclinical Toxicology

Bvibe Spearmint Deep Throat studies indicated that benzocaine can cause methemoglobinemia, particularly with high doses or prolonged exposure. Adverse developmental outcomes have been associated with benzocaine in animal studies at doses significantly higher than those used clinically.

Animal Pharmacology and Toxicology

Information regarding animal pharmacology and toxicology is not provided for the majority of products. However, specific studies have shown that benzocaine, when used in high doses, may lead to adverse effects in developmental outcomes.

Storage and Handling

Prolong is supplied as a gel. It should not be used if the safety seal under the cap is broken or missing.

Ms Topical Anesthetic is available in gel form and must be stored at 59°-86°F (15°-30°C). It should be protected from freezing.

Stallion, Sta-Hard, Instant Erection, Anal-Ese, and other creams are supplied in cream form and should be stored at room temperature. They must be kept out of reach of children and discarded after opening.

20/20 is supplied as strips and should be stored in a dry place at 55° to 78° Fahrenheit. The foil pouch should be kept for information, and it must be kept away from light.

Cvs Maximum Strength Boil Relief is provided as an ointment, and the carton should be kept for full drug facts.

Sting Relief Prep Pad is supplied as a solution and is flammable; it should be kept away from fire or flame.

Defend is available in gel form and should be stored at 59°-86°F (15°-30°C), protected from freezing.

Gumnumb Topical Anesthetic is supplied as a gel and must be stored at 59°-86°F (15°-30°C), also protected from freezing.

Anal Glide is available in gel form and should not be used if the safety seal is broken or missing.

Products like Dynamo Wellness Delay Max Wipe and Endurance Wipe are supplied as cloths and should be stored at room temperature. They must be kept in their original packaging until use and discarded after opening.

Oral Pain Relief and other gels should not be used if the tube tip is cut prior to opening and must be stored at room temperature.

For products like Americaine and other ointments, they should be stored at room temperature 15°– 25°C (59°– 77°F) and should not be used if the tamper-evident seal is broken or missing.

Certain gels, such as those from the Gingicaine line, should be stored at room temperature and protected from excessive heat.

Products like Vistacaine Topical Anesthetic and others should be stored at 59°-86°F (15°-30°C) and protected from freezing.

In general, all products should be kept out of reach of children, and any product that has a broken seal or damaged packaging should not be used.