Topical anesthetics: Uses, common brands, and safety info

Topical anesthetics are medications applied to the skin or mucous membranes to numb and minimize pain. They can be used for pain relief from minor cuts, insect bites, and minor burns. Depending on the drug, topical anesthetics can be purchased as over-the-counter or prescription medications. Keep reading to learn more about the different types of topical anesthetics, what they are most commonly used for, and some common side effects associated with their use.

Other topical anesthetics

• AleveX (camphor 5.5%/menthol 16%)

• Orajel Severe Pain (benzalkonium chloride 0.13%/benzocaine 20%/menthol 0.26%/zinc chloride 0.15%)

• LET gel (lidocaine 4%/epinephrine 0.05%/tetracaine 0.5%)

• Glydo lidocaine jelly (lidocaine 2%)

• Xylocaine jelly (lidocaine 2%) 

• LidoRx (lidocaine 3%)

• ELA-Max (lidocaine 4%)

• Terocin (methyl salicylate 25%/capsaicin 0.025%/menthol 10%)

• Proctofoam (hydrocortisone 1%/pramoxine 1%)

• Topicaine (lidocaine 4%)

• Nupercainal (dibucaine 1%) 

• Sarna Sensitive (pramoxine 1%) 

• Solarcaine (lidocaine 0.5%)

• Anbesol (benzocaine 20%) 

What are topical anesthetics?

Topical anesthetics, or topical analgesics, are medicines that cause a loss of sensation on the skin or mucous membranes after direct application. This results in a numbing feeling, which can help reduce pain. 

Topical anesthesia is not the same as local anesthesia. Local anesthetics work in an identical way to topical anesthetics; however, local anesthetics are injected into the affected area instead of being applied directly to the skin or mucosa. Topical anesthetics are available as creams, lotions, gels, ointments, and patches. 

While topical anesthetics are considered safe, they should be used according to the instructions given by a healthcare provider and the information found on the drug packaging or medication insert. These medications should only be applied to intact skin and mucosa. They should not be used on broken skin, lacerations (cuts), areas with puncture wounds, or areas that are irritated. 

How do topical anesthetics work?

Topical anesthetics work by blocking nerve conduction around the site of application on the skin or mucosa. More specifically, topical anesthetics work by blocking sodium channels in the nerve endings of the skin to prevent sodium ions from flowing into the nerve cells. This action blocks the ability of the nerve cells to transmit pain messages to the brain and causes a temporary loss in sensation in the area of application. Once applied, topical anesthetics penetrate the upper layers of the skin or mucosa, providing a numbing effect.

Topical anesthetic products may contain other medications, such as steroids, epinephrine, or other topical analgesics. Steroids can help relieve inflammation and reduce tissue damage. Epinephrine is sometimes added to delay the absorption of the anesthetic and increase how long the numbing effects last.

What are topical anesthetics used for?

Topical anesthetic agents are used for different purposes. The chosen agent will generally depend on the indication it is being used for. 

Dermatological applications

Dermatologists may apply topical anesthetics before:

• Skin biopsy

• Cosmetic procedures

• Laser treatments 

• Wart removal

• Hair removal

• Skin graft removal

• Dermabrasion

• Debridement or cleaning of wounds   

Medical tattooing 

Tattoo artists may use topical anesthetics before tattooing or restorative micro pigmentation.

At-home topical pain relief

People may use topical anesthetics at home for a variety of aches and pains including:

• Postpartum pain

• Hemorrhoids

• Gum soreness 

• Toothaches

• Mild burns, cuts, and scrapes 

• Muscle or joint aches 

Pain and discomfort from injections

Topical anesthetics may be applied before giving an injection to adults or children. Topical preparations are commonly used in pediatric patients before venipuncture or other uncomfortable injections.    

Certain specialized procedures

Topical anesthetics may be used for assistance during awake intubation or for procedures that require a spray catheter or “spray-as-you-go” technique (ex. bronchoscopy) 

Procedures involving the eyes 

Topical anesthetics may be used to numb the outer layers of the cornea and conjunctiva for certain eye exams or procedures involving the eyes, including:

• Curettage 

• Laceration repair

• Removal of foreign objects from the eyes 

Dental procedures

Topical anesthetics can numb the tissues before administering an injectable local anesthetic for dental procedures.

Procedures of the ears, nose, and throat

Topical anesthetics are used for in-office procedures involving the ear, nasal cavity, oral cavity, oropharynx, and larynx.

Gastrointestinal procedures 

Topical anesthetics can aid in investigational and therapeutic procedures involving the gastrointestinal tract.

Urological procedures

Topical anesthetics may be used for the temporary treatment of premature ejaculation. They also act as numbing agents for minor penile procedures, such as circumcision. 

Types of topical anesthetics

There are two classes of anesthetics used in topical and local preparations: amino amides and amino esters.

Amino Amides

The amino amides include:

• Mepivacaine 

• Lidocaine

• Etidocaine

• Bupivacaine

• Levobupivacaine

• Ropivacaine 

• Dibucaine 

• Prilocaine 

• Articaine

Amino Esters

The amino esters include: 

• Procaine

• Cocaine 

• Chloroprocaine 

• Tetracaine

• Benzocaine 

Methyl Salicylate 

Methyl salicylate is the methyl ester of salicylic acid. It is typically compounded with menthol or camphor and used to relieve minor body aches or pains. It can be identified by its aromatic, wintergreen smell.  

Menthol and Camphor

Menthol provides a mild cooling sensation while camphor helps relieve pain. These active ingredients may be used alone or in combination with other medications, such as over-the-counter itch and burn creams.  

Herbal Compounds 

There is a significant and growing body of evidence, including some clinical trials and case reports, demonstrating that some herbal compounds are as effective at providing analgesia as more traditional medicines. These include:

• Capsaicin

• Neem 

• Cannabis-derived products (CBD and THC)

• Clove 

Who can take topical anesthetics?

Can men take topical anesthetics?

Yes, men can use topical anesthetics. In addition to other uses, topical anesthetics for men can be used for certain procedures of the penis, including circumcision, short frenulum plasty, meatotomy, and removal of penile or urethral warts. Clinical trials have also shown that preparations like EMLA and lidocaine gel can safely be placed on the glans of the penis to treat premature ejaculation. 

Can women take topical anesthetics?

Yes, women can use topical anesthetics. In addition to other uses, topical anesthetics are commonly used by women who undergo cosmetic procedures, such as microneedling facials, injectables, laser treatments, and hair removal procedures. Topical anesthetics can also be used safely for gynecologic procedures, including genital wart removal, resurfacing procedures, or placement of various cervical agents.   

Can you take topical anesthetics while pregnant or breastfeeding?

Yes, many topical anesthetics can be used while pregnant and breastfeeding. Topical anesthetics are less absorbed into the bloodstream and thus cause fewer side effects than injected local anesthetics. Lidocaine and prilocaine are classified as Pregnancy Category B and are considered safe options for pregnancy. Preparations containing benzocaine and tetracaine are considered Pregnancy Category C and may need to be used with caution. 

Lidocaine and bupivacaine are the preferred topical anesthetics in nursing mothers. Certain topical anesthetics like benzocaine and dibucaine are toxic when ingested orally and should not be applied to the breasts, especially during breastfeeding. 

Can children take topical anesthetics?

Yes, children can take topical anesthetics. It is very common for topical anesthesia to be used in pediatric populations for minor cuts, scrapes, and burns. They may also be used clinically for blood draws, dental procedures, and numbing before injections. Consult with a healthcare provider before applying topical anesthetics to children.  

Can seniors take topical anesthetics?

Yes, seniors can use topical anesthetics for any indication they are normally used for in other adults. However, as we age, the skin can lose thickness and the supporting muscle can lose tone. This means there may be increased absorption of topical agents through the skin of older people, which can increase the risk of toxicity from topical anesthetics.  

Are topical anesthetics safe?

Topical anesthetics are considered a safe class of medications due to their minimal absorption into the bloodstream. Topical anesthetics are not controlled substances, and in many cases, they are used to replace the need for opioid pain medications. Topical anesthetics are rarely abused or misused.  

Common topical anesthetics side effects

As with any medication, the use of topical anesthetics is associated with possible side effects. Most side effects occur due to toxicity, sensitivity, or misuse of the medication. Notify a healthcare provider if you experience any side effects with topical anesthetics. Common side effects may include:

• Mild burning or stinging at or around the site of application

• Itching or rash

• Discoloration of the skin where the medication was applied

Severe side effects of topical anesthetics may include:

• Severe burning or stinging at the application site

• Swelling or redness around the area of application

• Allergic reactions with signs or symptoms that include:

  • Hives

  • Swelling of the face or throat

  • Trouble breathing

• Unusual sensations or prolonged loss of sensation on the skin

• Systemic effects, if too much of the drug is absorbed through the skin into the bloodstream, which includes:

  • Dizziness

  • Drowsiness

  • Confusion 

  • Blurred vision 

  • Ringing in the ears

  • Unusual hot or cold sensations on the skin 

Topical anesthetics are generally used for short-term relief of pain, as directed by a healthcare provider. A healthcare provider can help determine whether a topical anesthetic is appropriate for a given condition and how long it should be used. 

How much do topical anesthetics cost?

Topical anesthetics are available at a wide range of prices depending on the medication. On the low end, some over-the-counter preparations, such as Cepacol lozenges, LMX cream, and AleveX can be found for under $10. Most over-the-counter preparations are between $5 and $20. Some prescription topical anesthetics, such as the Synera patch, can cost up to $200. 

Prices can vary depending on the quantity prescribed and whether the medication is covered by insurance. With a SingleCare discount card, patients can get up to 80% off the retail price of brand and generic medications.