anesthetics (Topical/Mucosal)

section name header

Indications ⬇

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:

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

Adv. Reactions/Side Effects ⬆ ⬇

EENT: mucosal use: ↓or absent gag reflex.

Derm: topical use: burning, edema, irritation, stinging, tenderness, urticaria.

Misc: ALLERGIC REACTIONS INCLUDING ANAPHYLAXIS.

Interactions ⬆ ⬇

Drug-Drug:

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

Availability ⬆ ⬇

Benzocaine

Lozenges: 6 mg^OTC; 10 mg^OTC; 15 mg^OTC; 18 mg^OTC;
Oral ointment: 20%^OTC;
Oral paste: 20%^OTC;
Oral swab: 7.5%^OTC; 20%^OTC;
Topical swab: 20%^OTC;
Rectal ointment: 20%^OTC;
Oral gel: 6.5%^OTC; 7.5%^OTC; 10%^OTC; 15%^OTC; 20%^OTC;
Oral cream: 20%^OTC;
Oral liquid: 6.3%^OTC;
Oral aerosol: 20%^OTC;
Topical aerosol: 20%^OTC;
Topical cream: 6%^OTC; 20%^OTC;
Topical gel: 7.5%^OTC; 10%^OTC; 20%^OTC;
Topical ointment: 5%^OTC; 6%^OTC; 20%^OTC;
Topical solution: 2%^OTC; 5%^OTC; 20%^OTC;
In combination with: butamben and tetracaine (Cetacaine), and phenol^OTC. See Appendix [not included in this PDA edition].

Dibucaine

Topical ointment: 1%^OTC;

Dyclonine

Lozenges: 1.2 mg^OTC; 2 mg^OTC; 3 mg^OTC;

Pramoxine

Topical cream: 1%^OTC;
Topical gel: 1%^OTC;
Topical solution: 1%^OTC;
Topical spray: 1%^OTC;
Rectal aerosol foam: 1%^OTC;
Rectal ointment: 1%^OTC;
In combination with: hydrocortisone (Analpram HC, Pramosome, ProctoFoam HC). See Appendix [not included in this PDA edition].

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
Topical (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 q 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 q 2 hr (not to exceed 10 lozenges/day).
Pramoxine
Topical/Mucosal (Adults): Topical products may be used q 3 hr as needed. Rectal products may be used up to 5 times daily.

US Brand Names ⬆ ⬇

benzocaine: Americaine Hemorrhoidal, Anbesol, Anbesol Baby, Anbesol Cold Sore Therapy, Anbesol Jr., Anbesol Maximum Strength, Benzodent, Cepacol Sore Throat Pain Relief, Dentapaine, Dermoplast Pain Relieving, Hurricaine, Lanacane, Orajel Mouth Sore, Orabase, Medicone Hemorrhoidal, Mycinettes, Zilactin-B
dibucaine: Nupercainal
dyclonine: Sucrets Children's, Sucrets Maximum Strength, Sucrets Regular Strength
pramoxine: Caladryl Clear, ProctoFoam NS, Sarna Ultra, Tronolane, Tucks Hemorrhoidal

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.

Canadian Brand Names ⬆ ⬇

benzocaine: Baby Orajel, Dentocaine, Orajel Liquid

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 ⬆ ⬇

Instruct patient on correct application technique. High Alert: Inform patient of potential harm from overuse. Emphasize need to avoid contact with eyes.
Caution patient that these agents should not be applied for prolonged periods or to large areas, especially if skin is abraded or broken, without consulting health care professional. Patient should also consult health care professional before using these agents for conditions other than indicated.
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.
Caution patient to read list of active ingredients on OTC products. Brand names frequently change and may be misleading as to actual contents.
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 parents 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 more than 2 days. Avoid use in young children because of danger of choking.

Pronunciation ⬆

benzocaine: BEN-zoe-kane
dibucaine: DYE-byoo-kane
dyclonine: DYE-klon-een
pramoxine: pra-MOX-een

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