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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Standardized Chemical Allergen [EPC]
Benzocaine is a widely used ester-type local anesthetic designed to provide temporary pain relief by blocking nerve signals. It is commonly found in over-the-counter topical treatments for oral, throat, and skin irritation.
Name
Benzocaine
Raw Name
BENZOCAINE
Category
Standardized Chemical Allergen [EPC]
Drug Count
293
Variant Count
561
Last Verified
February 17, 2026
RxCUI
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UNII
U3RSY48JW5, 9D2RTI9KYH, ND2M416302, 3K9958V90M, EFW857872Q, 5NF5D4OPCI, L7T10EIP3A, 86Q357L16B, YUL4LO94HK, F5UM2KM3W7, PH41D05744, 13S1S8SF37, OG625Z9LEO, B6E5W8RQJ4, D9OM4SK49P, O414PZ4LPZ, V5VD430YW9, QYO8Q067D0, PDC6A3C0OX, 7EV65EAW6H, 0F32U78V2Q, 4T6H12BN9U, F05Q2T2JA0, 98PI200987, 0619F35CGV, 5TJD82A1ET, 339NCG44TV, 344S277G0Z, N20HL7Q941, 92RU3N3Y1O, BZ1R15MTK7
About Benzocaine
Benzocaine is a widely used ester-type local anesthetic designed to provide temporary pain relief by blocking nerve signals. It is commonly found in over-the-counter topical treatments for oral, throat, and skin irritation.
Detailed information about Benzocaine
This page is for informational purposes only and does not replace medical advice. Consult a qualified healthcare professional before using any medication containing Benzocaine.
Historically, Benzocaine has been a staple in dental and dermatological care since its discovery in the late 19th century. However, healthcare providers now exercise caution with its use due to the risk of rare but serious blood disorders. It is important to note that Benzocaine belongs to the same class as procaine and tetracaine, but it is distinct from amide-type anesthetics like lidocaine.
At the molecular level, Benzocaine acts as a reversible stabilizer of the neuronal membrane. It functions by binding to and inhibiting voltage-gated sodium channels located on the internal surface of nerve cell membranes. By blocking these channels, Benzocaine prevents the influx of sodium ions, which is necessary for the depolarization of the nerve cell and the subsequent propagation of an action potential (nerve impulse).
Because the nerve cannot send a signal to the brain, the patient experiences a localized loss of sensation (numbness). This effect is temporary and subsides as the drug is metabolized and cleared from the site of application.
Healthcare providers typically recommend Benzocaine for the following FDA-approved or clinical indications:
Benzocaine is available in a variety of strengths (typically 5% to 20%) and forms, including:
> Important: Only your healthcare provider can determine if Benzocaine is right for your specific condition.
Dosage varies significantly based on the concentration of the product and the area being treated. For oral pain, a 10% to 20% gel is typically applied to the affected area up to 4 times daily. For topical skin irritation, a 5% to 20% cream or spray may be applied to the affected area 3 to 4 times daily. Healthcare providers advise using the smallest amount necessary to achieve pain relief to minimize systemic absorption.
Warning: The FDA has issued safety communications stating that Benzocaine products should not be used in children under 2 years of age due to the risk of methemoglobinemia (a serious condition that reduces oxygen in the blood). For children over 2 years, use should only occur under the direct supervision of a healthcare professional and following the specific instructions on the product label.
Specific dosage adjustments for renal impairment are not typically required for topical application, but caution is advised in patients with severe kidney disease if large areas of skin are treated.
Because Benzocaine is primarily metabolized by plasma cholinesterases, hepatic impairment has a limited effect on its clearance; however, patients with severe liver disease should consult their doctor.
Elderly patients may have thinner skin or reduced systemic clearance. Healthcare providers generally recommend starting with the lowest effective concentration.
If a dose is missed, apply it as soon as remembered. If it is almost time for the next application, skip the missed dose. Do not apply double the amount to make up for a missed dose.
Signs of Benzocaine overdose or systemic toxicity include dizziness, irregular heartbeat, seizures, and respiratory distress. If you suspect an overdose or if the product is swallowed, contact a Poison Control Center or seek emergency medical care immediately.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose without medical guidance.
Most patients tolerate Benzocaine well when used as directed. Common localized reactions include:
> Warning: Stop using Benzocaine and call your doctor immediately if you experience any of these symptoms of methemoglobinemia:
Prolonged use of Benzocaine can lead to skin sensitization, making future allergic reactions more likely. It may also mask underlying conditions that require medical diagnosis, such as deep dental infections or chronic skin disorders.
While Benzocaine does not carry a traditional "Black Box Warning" in the same format as prescription antidepressants, the FDA has mandated prominent warnings on all Benzocaine labels regarding Methemoglobinemia. This warning emphasizes that the condition can occur after a single application and can lead to death if not treated promptly. The FDA specifically prohibits the use of OTC Benzocaine products for teething in infants.
Report any unusual symptoms to your healthcare provider.
Benzocaine should only be used topically and never ingested or injected. It is vital to use the lowest concentration necessary for the shortest duration possible. Patients with a history of breathing problems, such as asthma or COPD, may be at a higher risk for complications if methemoglobinemia occurs.
No official FDA black box warning exists, but the FDA Safety Communication (2018) serves as the highest level of caution regarding the risk of methemoglobinemia, particularly in children under 2 years of age. Labels must clearly state that the product is not for use in infants.
Routine lab tests are not typically required for short-term topical use. However, if a patient is suspected of having methemoglobinemia, healthcare providers will perform a co-oximetry test to measure methemoglobin levels in the blood.
Benzocaine generally does not interfere with the ability to drive or operate machinery. However, if used in the mouth or throat, it may cause numbness that affects swallowing; patients should wait until sensation returns before consuming hot foods or operating equipment that requires full sensory focus.
There are no direct contraindications between Benzocaine and alcohol. However, alcohol can increase the risk of gastric irritation if Benzocaine is used for oral pain, and it may impair the patient's ability to recognize signs of a serious side effect.
Benzocaine does not require a tapering period. If pain persists for more than 7 days or if the condition worsens, discontinuation and consultation with a healthcare provider are necessary.
> Important: Discuss all your medical conditions with your healthcare provider before starting Benzocaine.
There are no known major food interactions with Benzocaine. However, when used orally, it is advised to avoid eating or drinking until the numbness has worn off to prevent accidental biting of the tongue or cheeks and to ensure the gag reflex has returned to normal.
There are no well-documented interactions between Benzocaine and common herbal supplements like St. John's Wort or Ginkgo Biloba. However, patients should always inform their doctor of all supplements being taken.
Benzocaine use does not typically interfere with standard blood or urine laboratory tests. However, it can cause false readings in co-oximetry if the device is not calibrated to detect methemoglobin specifically.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking.
Patients allergic to para-aminobenzoic acid (PABA), often found in older sunscreen formulations, or certain hair dyes (paraphenylenediamine), may experience cross-allergic reactions to Benzocaine because they share a similar chemical structure.
> Important: Your healthcare provider will evaluate your complete medical history before prescribing Benzocaine.
Benzocaine is classified as FDA Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Healthcare providers typically recommend using the lowest dose for the shortest time possible.
It is not known whether Benzocaine is excreted in human milk. Because many drugs are excreted in milk, caution should be exercised when Benzocaine is administered to a nursing woman. Most experts suggest that occasional topical use is unlikely to pose a significant risk to the infant, but the application site should not be on the breast where the infant might ingest it.
Benzocaine is not approved for use in children under the age of 2. For children over 2, it is approved for minor mouth and throat irritation, but parents should be vigilant for signs of methemoglobinemia. Teething pain should be managed with non-pharmacological methods like chilled teething rings.
Elderly patients may be more susceptible to systemic toxicity and methemoglobinemia due to age-related changes in skin permeability and reduced physiological reserves. Healthcare providers often suggest lower concentrations and careful monitoring for this population.
While systemic absorption is usually low, patients with end-stage renal disease should be monitored if Benzocaine is used over large surface areas, as the metabolites are primarily cleared by the kidneys.
Since Benzocaine is primarily hydrolyzed by plasma cholinesterases, hepatic impairment does not significantly alter its metabolism. However, patients with severe liver dysfunction should still use the medication with caution.
> Important: Special populations require individualized medical assessment.
Benzocaine is a local anesthetic that acts by inhibiting the voltage-gated sodium channels on the neuronal membrane. By binding to these channels, it prevents the rapid influx of sodium ions required for the initiation and conduction of nerve impulses. This results in a reversible block of sensory nerve conduction, effectively numbing the area where the drug is applied.
The onset of action for Benzocaine is rapid, typically occurring within 1 minute of application. The duration of effect is relatively short, usually lasting between 15 to 20 minutes, depending on the site and the blood flow to the area. It does not possess significant vasodilatory properties compared to other local anesthetics.
| Parameter | Value |
|---|---|
| Bioavailability | Low (through intact skin); Moderate (mucous membranes) |
| Protein Binding | Minimal |
| Half-life | Short (Rapidly hydrolyzed) |
| Tmax | Immediate (Topical) |
| Metabolism | Plasma Cholinesterases (to PABA) |
| Excretion | Renal (Metabolites) |
Benzocaine is classified as an Ester Local Anesthetic. It is grouped with other esters like procaine and tetracaine, but it is distinct from the amide class (e.g., lidocaine, bupivacaine). It is also categorized as a standardized chemical allergen due to its potential to cause contact sensitivity.
Medications containing this ingredient
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Everlit Survival Sting Relief Pad
Cetacaine Anesthetic
Cetacaine Topical Anesthetic
Orajel Gum Pain 3x Medicated
Vagisil Anti-itch Creme Regular Strength
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+ 38 more drugs
Common questions about Benzocaine
Benzocaine is a local anesthetic primarily used for the temporary relief of pain and itching associated with minor medical conditions. Healthcare providers often recommend it for oral issues like toothaches, canker sores, or gum irritation, as well as for sore throats in the form of lozenges. It is also found in topical creams for minor burns, sunburns, and insect bites. Its primary function is to numb the area by blocking nerve signals locally. Always consult your doctor to ensure it is appropriate for your specific symptoms.
The most common side effects of Benzocaine are localized and mild, including stinging, burning, or redness at the site of application. Some individuals may also experience itching or a mild rash, which is often a sign of local irritation. These symptoms usually disappear shortly after the medication is discontinued. In rare cases, more significant skin irritation or an allergic reaction can occur. If you notice any persistent or worsening symptoms, you should contact your healthcare provider for further evaluation.
There is no known direct chemical interaction between Benzocaine and alcohol that would cause immediate harm. However, if you are using Benzocaine for oral pain, alcohol may irritate the sensitive tissues in your mouth and delay healing. Additionally, alcohol can impair your judgment, making it harder to notice serious side effects like difficulty breathing. It is generally best to avoid alcohol until the underlying condition being treated with Benzocaine has improved. Always discuss your lifestyle habits with your doctor when starting a new medication.
Benzocaine is classified as FDA Pregnancy Category C, meaning its safety during pregnancy has not been established through rigorous clinical trials. It should only be used if the potential benefit to the mother outweighs the potential risk to the developing fetus. Most healthcare providers suggest avoiding its use during pregnancy unless specifically directed by a medical professional. If you are pregnant or planning to become pregnant, talk to your doctor about safer alternatives for pain relief. Minimal topical application is generally considered low-risk, but professional guidance is essential.
Benzocaine has a very rapid onset of action, typically providing a numbing effect within one minute of application. This makes it highly effective for immediate, short-term relief of sharp pains or intense itching. However, the duration of this effect is relatively short, usually lasting only 15 to 30 minutes. Because it wears off quickly, it is often formulated into products that allow for multiple applications throughout the day. If the pain returns quickly and is severe, consult your healthcare provider rather than over-applying the medication.
Yes, Benzocaine can be stopped suddenly without the risk of withdrawal symptoms or rebound effects. Since it is a topical anesthetic used for symptomatic relief, you can simply stop using it once the pain or irritation has resolved. There is no need to taper the dose or follow a specific discontinuation schedule. However, if you stop using it and your symptoms return or worsen, it may indicate an underlying issue that needs medical attention. Always follow the advice of your healthcare provider regarding the duration of treatment.
If you miss a dose of Benzocaine, you should apply it as soon as you remember, provided it is not almost time for your next scheduled application. If it is nearly time for the next dose, simply skip the missed one and continue with your regular routine. You should never apply extra Benzocaine or double the amount to make up for a missed application, as this increases the risk of systemic absorption and side effects. Since it is used 'as needed' for many conditions, missing a dose is generally not a cause for concern. Consult your doctor if you have specific questions about your dosing schedule.
There is no clinical evidence to suggest that Benzocaine causes weight gain. Because it is applied topically and has very limited systemic absorption, it does not affect the metabolic processes or hormonal balances that typically lead to changes in body weight. Any weight changes experienced while using Benzocaine are likely due to other factors, such as underlying health conditions or other medications. If you are concerned about weight gain, you should discuss your overall health and medication regimen with your healthcare provider. Benzocaine is considered weight-neutral for the vast majority of patients.
Benzocaine can interact with certain other medications, particularly 'sulfa' drugs (sulfonamides), as it may reduce their antibacterial effectiveness. It also carries an increased risk of methemoglobinemia when used alongside other drugs that affect oxygen in the blood, such as nitrates or other local anesthetics like prilocaine. You should always provide your healthcare provider with a full list of your current medications, including over-the-counter drugs and supplements. Most topical interactions are minor, but systemic risks must be evaluated by a professional. Your doctor can help you determine the safest way to use Benzocaine with your other treatments.
Yes, Benzocaine is widely available as a generic medication and is found in many store-brand over-the-counter products. Generic versions are required by the FDA to have the same quality, strength, and purity as brand-name products. You can find generic Benzocaine in various forms, such as gels for toothaches, sprays for sunburns, and lozenges for sore throats. Using a generic version is often a cost-effective way to achieve the same pain-relieving results. Your pharmacist or healthcare provider can help you select a generic product that is appropriate for your needs.