anesthetics (topical/mucosal)

High Alert

Topical Relief of pruritus or pain associated with minor skin disorders including burns, abrasions, bruises, insect stings/bites, dermatitis, hemorrhoids, or other forms of skin irritation.

Mucosal

Provide local anesthesia to mucosal surfaces before instrumentation, minor procedures, or endoscopy. Decrease irritation caused by minor mouth and throat conditions including sore throat, gingivitis, stomatitis, or teething. Also used to suppress the gag reflex during endoscopy or intubation.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity. Cross-sensitivity may occur among related agents (amide types—dibucaine; ester types—benzocaine, tetracaine);
Hypersensitivity to any components of preparations including stabilizers, colorants, or bases;
Active, untreated infection of affected area;
Not to be used in the eye;
Some products contain alcohol and should be avoided in patients with known alcohol intolerance;
Pedi: Topical benzocaine products should not be used in children <2 yr.

Use Cautiously in:

Large or severely abraded areas of skin or mucous membrane;
Prolonged use (not recommended);
Pedi: ↑risk of systemic toxicity in children, safety not established for some products; use smaller doses due to potential for methemoglobinemia;;
Geri: ↑risk of toxicity in older adults; use smaller doses.

Adv. Reactions/Side Effects ⬆ ⬇

EENT: mucosal use↓or absent gag reflex

Derm: topical useburning, edema, irritation, stinging, tenderness, urticaria

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Toxicity of ester-type agents may be ↑ by concurrent use of cholinesterase inhibitors.

Availability ⬆ ⬇

Benzocaine
- Lozenges: 15 mg^OTC
- Topical swab: 20%^OTC
- Oral gel: 7.5%^OTC; 10%^OTC; 20%^OTC
- Oral liquid: 20%^OTC
- Oral aerosol: 20%^OTC
- Topical aerosol: 2%^OTC
- Topical solution: 20%^OTC
- In combination with:
- benzalkonium chloride (Orajel Cold Sore); butamben and tetracaine (Cetacaine), and phenol^OTC. See Combination Drugs.
Dibucaine
- Topical ointment: 1%^OTC
Dyclonine
- Lozenges: 2 mg^OTC
- Topical solution: 0.5%^OTC
Pramoxine
- Topical gel: 1%^OTC
- Topical lotion: 1%^OTC
- Rectal aerosol foam: 1%^OTC
- In combination with:
- hydrocortisone (Analpram HC, Epifoam, PramCort, Pramosome, ProCort, ProctoFoam HC); phenylephrine (Preparation H). See Combination Drugs.

Route/Dosage ⬆ ⬇

Benzocaine

Topical/Mucosal(Adults and Children ): Apply cream, ointment, topical solutions, or dental/oral products as needed. Lozenges may be used hourly (not to exceed 12 lozenges/day). Rectal products may be used twice daily.

Dibucaine

(Adults and Children ): Apply as needed (not to exceed 30 g/day in adults or 7.5 g/day in children). Can be used 3–4 times daily.

Dyclonine

Mucosal(Adults ): 2- or 3-mg lozenge may be dissolved in the mouth every 2 hr (not to exceed 10 lozenges/day), or solution may be used 4 times daily.
Mucosal(Children ≥2 yr): 1.2-mg lozenge may be dissolved in mouth every 2 hr (not to exceed 10 lozenges/day).

Pramoxine

Topical/Mucosal(Adults ): Topical products may be used every 3 hr as needed. Rectal products may be used up to 5 times daily.

US Brand Names ⬆ ⬇

benzocaine: Anbesol, Anbesol Baby, Anbesol Cold Sore Therapy, Anbesol Maximum Strength, Cepacol Sore Throat Pain Relief, Hurricaine, Orabase, Zilactin-B,

dibucaine: Nupercainal,

dyclonine: DycloPro, Sucrets,

pramoxine: Caladryl Clear, ProctoFoam, Sarna Sensitive

Action ⬆ ⬇

Inhibit initiation and conduction of sensory nerve impulses.

Therapeutic effects:

Local anesthesia with subsequent loss of sensation or relief of pain and/or pruritus.

Classifications ⬆ ⬇

Therapeutic Classification: anesthetics (topical/local)

Pharmacokinetics ⬆ ⬇

Absorption: Benzocaine is poorly absorbed through intact skin. Other agents may be readily absorbed. Degree of absorption ↑ with surface area; presence of lesions, cuts, or abrasions; and amount of agent applied.

Distribution: Unknown.

Metabolism/Excretion: Ester-type agents (PABA derivatives, benzocaine) are metabolized by plasma and liver cholinesterases. Small amounts of amide-type agents (dibucaine) that may be absorbed are mostly metabolized by the liver.

Half-Life: Unknown.

Time/Action Profile ⬆ ⬇

(mucosal anesthetic effects)

ROUTE	ONSET	PEAK	DURATION
Benzocaine	about 1 min	unknown	15–20 min
Dibucaine	within 15 min	unknown	2–4 hr
Dyclonine	up to 10 min	unknown	60 min
Pramoxine	3–5 min	unknown	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Instruct patient on correct application technique. High Alert: Inform patient of potential harm from overuse. Emphasize need to avoid contact with eyes.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications, especially topical formulations.
- Advise patient to discontinue use and notify health care professional if erythema, rash, or irritation at site of administration occurs; area becomes infected; medication is swallowed; or condition worsens or does not improve within 7 days.
- Advise adults using liquid form around the mouth to avoid smoking until solution is dry.
Teething Gel: Instruct patients to notify health care professional if pain is excessive or prolonged. Advise caregiver to avoid feeding immediately after application to prevent choking from diminished gag reflex.
Lozenge: Instruct patient to suck on lozenge and allow it to slowly dissolve. Consult health care professional if throat pain persists >2 days. Avoid use in young children because of danger of choking.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.

Pronunciation ⬆

benzocaine: BEN-zoe-kane

dibucaine: DYE-byoo-kane

dyclonine: DYE-klon-een

pramoxine: pra-MOX-een

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Indications ⬇