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Benzocaine topical

Pronunciation

Class: Antipruritics and Local Anesthetics
VA Class: NT300
CAS Number: 94-09-7
Brands: Americaine, Anacaine, Chiggerex, Chiggertox, Dermoplast, Foille, Ivarest, Outgro, Solarcaine

Introduction

Local anesthetic.a

Uses for Benzocaine

Dermatologic Conditions

Self-medication for temporary relief of pain and itching associated with minor burns, sunburn, minor cuts or scrapes, insect bites, or minor skin irritations.e h i j

Usually used in fixed-combination with an antibacterial (e.g., benzethonium chloride), antipruritic (e.g., menthol), or skin protectant (e.g., calamine).h i j

Hemorrhoids

Self-medication for temporary relief of pain and itching associated with hemorrhoids.c

Premature Ejaculation

Self-medication, as a male genital desensitizer, to aid in slowing the onset of ejaculation.b

Anesthetic Lubricant

Has been used as a water-soluble lubricant (no longer commercially available in US) for topical anesthesia on intratracheal catheters and pharyngeal and nasal airways to obtund pharyngeal and tracheal reflexes and on nasogastric and endoscopic tubes, urinary catheters, laryngoscopes, proctoscopes, sigmoidoscopes, and vaginal specula;a d however, methemoglobinemia has occurred when applied to mucous membranes.104 105 106 a

Benzocaine Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as an aerosol spray, cream, lotion, ointment, or solution.a

Avoid contact with the eye(s) and do not apply to e deep or puncture wounds or to serious burns.a

Aerosol Spray

Shake well prior to use.h

Hold spray canister approximately 6–12 inches away from the affected area.h

To avoid contact with eyes when applying to face, first spray the drug into the palm of hand and then apply.h

Dosage

Pediatric Patients

Dermatologic Conditions
Topical

Children ≥2 years of age (self-medication): Apply 5–20% aerosol spray, cream, lotion, ointment, or solution 3 or 4 times daily or as directed by a clinician.e

Hemorrhoids
Topical

Children ≥12 years of age (self-medication): Apply 20% ointment to cleansed, affected area up to 6 times daily.c

Adults

Dermatologic Conditions
Topical

Self-medication for the temporary relief of pain and itching associated with various skin conditions, apply 5–20% aerosol spray, cream, lotion, ointment, or solutions 3 or 4 times daily or as directed by a clinician.e

Hemorrhoids
Topical

Self-medication for the temporary relief of pain and itching associated with hemorrhoids, apply 20% ointment to cleansed, affected area up to 6 times daily.c

Premature Ejaculation
Topical

Self-medication to aid in slowing the onset of ejaculation, apply a small amount of a preparation containing 3–7.5% benzocaine in a water-soluble base to the head and shaft of the penis before intercourse.b

After intercourse, wash off any remaining benzocaine to minimize the chance of an allergic reaction occurring.b

Cautions for Benzocaine

Contraindications

  • Known hypersensitivity to benzocaine, other ester-type local anesthetics, or any ingredient in the formulation.a

Warnings/Precautions

Warnings

Administration

For external use only.a

Avoid contact with the eyes.a e

Not intended for prolonged use (e.g., >1 week).a i

When used for self-medication, discontinue the drug and consult a clinician if the condition worsens or symptoms persist for >7 days or clear and occur again within a few days, if infection or bleedingc occurs, or if rash or irritation occurs.a b

When used for genital desensitization, recognize that premature ejaculation may be due to a condition requiring medical attention.b

Sensitivity Reactions

Possible sensitization.a d

If a rash or irritation develops during therapy, discontinue the drug and consult a clinician.a d

When used for self-medication as a male genital desensitizer, advise the male to use the drug with caution if his sexual partner is sensitive to local anesthetics, sunscreens, sulfa drugs, or hair dyes.a Discontinue therapy if rash or irritation (e.g., burning, itching) occurs; consult clinician if symptoms persists.b

General Precautions

Methemoglobinemia

Possible methemoglobinemia; closely adhere to dosing recommendations.g

Serious Adverse Effects associated with Local Anesthetics

Risk of serious adverse effects (e.g., seizures, coma, irregular heart beat, respiratory depression) with use of topical local anesthetics; generally reported following application of extemporaneously prepared topical preparations containing high concentrations of anesthetics.k

Potential for life-threatening adverse effects (e.g., irregular heart beat, seizures, breathing difficulties, coma, death) when topical local anesthetics are applied to a large area of skin, when the area of application is covered with an occlusive dressing, if a large amount of topical anesthetic is applied, if the anesthetic is applied to irritated or broken skin, or if the skin temperature increases (from exercise or use of a heating pad).101 102

Lidocaine 4% gel has been investigated to reduce discomfort during mammography.101 103 Whether such use could result in serious reactions has not been determined.101 103 Patients should speak with their clinician if they are considering using a topical anesthetic before obtaining a mammogram.101

When a topical anesthetic is needed for a procedure, use of an FDA-approved preparation has been recommended.k Use a preparation containing the lowest concentration of anesthetic likely to be effective; apply a small amount of the preparation to the affected area for the shortest period necessary for the desired effect,k and do not apply to broken or irritated skin.101 fn

Specific Populations

Pregnancy

Category C.d

Lactation

Not known whether benzocaine is distributed into milk; use with caution.d

Pediatric Use

Safety and efficacy of topical aerosol spray, cream, lotion, ointment, or solution not established in children <2 years of age;e use only under the direction of a clinician.106 a

Common Adverse Effects

Generally nontoxic when applied topically, but sensitization can occur.a Contact dermatitis and/or hypersensitivity can result in burning, stinging, pruritus, tenderness, erythema, rash, urticaria, and edema.d

Male genital desensitization preparations usually do not adversely affect female orgasm in the sexual partner, but sensitization can occur.a (See Sensitivity Reactions under Cautions.)

Stability

Storage

Topical

Aerosol

<40°C, preferably between 15–30°C.a

Do not puncture, use, or store aerosol containers near heat or an open flame, expose to temperatures >49°C, or place into a fire or incinerator for disposal.a

Creams

Tight, light-resistant containers at <40°C, preferably between 15–30°C.a Avoid prolonged exposure to temperatures >30°C.a

Ointments

Tight, light-resistant containers at <40°C, preferably between 15–30°C.a Avoid prolonged exposure to temperatures >30°C.a

Solutions

<40°C, preferably 15–30°C.a Do not freeze.a

Actions

  • Blocks the initiation and conduction of nerve impulses by inhibiting the depolarization of the neuronal membrane.d

  • Structurally similar to procaine (no longer commercially available in US).g (See Methemoglobinemia under Cautions.)

Advice to Patients

  • Risk of sensitization.a Importance of discontinuing therapy and consulting clinician if a rash or irritation develops during therapy.a

  • Importance of avoiding contact with the eyes.a e

  • Importance of using as directed and not applying in large quantities, particularly over raw surfaces or blistered areas.e

  • When a topical anesthetic is used for a procedure, importance of applying the preparation as directed by a clinician.k

  • Before recommending use of benzocaine preparations, inform patients or caregivers of the signs and symptoms of methemoglobinemia (e.g., pale, gray, or blue colored skin, lips, or nail beds; headache, lightheadedness, anxiety, confusion, or fatigue; tachycardia; shortness of breath) and advise them to seek immediate medical attention if such manifestations occur.104 106 Advise patients to store benzocaine preparations out of reach of children.106

  • Importance of discontinuing therapy and consulting clinician if dermatologic condition worsens or symptoms persist for >7 days or clear and occur again within a few days, if infection or bleedingc occurs, or if rash or irritation occurs.a b e

  • Advise patients using benzocaine for genital desensitization that premature ejaculation may be due to a condition requiring medical attention.b Discontinue and consult a clinician if relief is not obtained following use as directed or if the patient or their sexual partner develops a rash or irritation.b

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.d

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.d

  • Importance of informing patients of other important precautionary information.d (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Benzocaine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Aerosol

5%

Foille Medicated First Aid

Blistex

20%

Americaine First Aid Spray

Insight

Dermoplast

MedTech

Solarcaine

Schering-Plough

Cream

5%*

Benzocaine Cream

Ivarest

Blistex

Lotion

0.5%

Solarcaine

Schering-Plough

5%

Ointment

2%

Chiggerex

Scherer

5%

Foille Medicated First Aid

Blistex

10%

Anacaine

Gordon

20%

Americaine Hemorrhoidal Ointment

Insight

Solution

2.1%

Chiggertox

Scherer

20%

Outgro

MedTech

AHFS DI Essentials. © Copyright, 2004-2016, Selected Revisions December 10, 2015. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

101. Food and Drug Administration. FDA Public Health Advisory: Potential hazards of skin products containing numbing ingredients for relieving pain from mammography and other medical tests and conditions. 2009 Jan 16. From FDA website ().

102. Food and Drug Administration. Topical Anesthetics. MedWatch alert. Rockville, MD; 2009 Jan 16. From FDA website (

103. Lambertz CK, Johnson CJ, Montgomery PG et al. Premedication to reduce discomfort during screening mammography. Radiology. 2008; 248:765-72. [PubMed 18647845]

104. Food and Drug Administration. FDA Public Health Advisory: Benzocaine sprays marketed under different names, including Hurricane, Topex, and Cetacaine. 2006 Feb 10. From FDA website.

105. Food and Drug Administration. FDA drug safety communication: FDA continues to receive reports of a rare, but serious and potentially fatal adverse effect with the use of benzocaine sprays for medical procedures. 2011 Apr 7. From FDA website.

106. Food and Drug Administration. FDA drug safety communication: Reports of a rare, but serious and potentially fatal adverse effect with the use of over-the-counter (OTC) benzocaine gels and liquids applied to the gums or mouth. 2011 Apr 7. From FDA website.

a. AHFS drug information 2016. McEvoy GK, ed. Benzocaine. Bethesda, MD: American Society of Health-System Pharmacists; 2016:.

b. Food and Drug Administration. Male genital desensitizing drug products for over the counter human use. 21 CFR Part 348. From the FDA website: (. Revised 2003 Apr.

c. Insight Pharmaceuticals. Americaine (benzocaine 20%) hemorrhoidal ointment prescribing information. From the Insight website: (. Accessed 2004 Jan 23.

d. Celltech pharmaceuticals, Inc. Americaine (benzocaine) anesthetic lubricant prescribing information. Rochester, NY; 2001 Jul.

e. Food and Drug Administration. External analgesic drug products for over-the-counter human use; tentative final monograph. 21 CFR Part 348. Fed Regist. 1983; 48:5867-9.

g. Catterall W, Mackie K. Local anesthetics. In: Gilman AG, Goodman LS, Rall TW et al eds. Goodman and Gilman’s the pharmacologic basis of therapeutics. 10th ed. New York: Macmillan Publishing Company. 2001:376.

h. Medtech. Dermoplast (benzocaine) hospital strength pain relieving spray prescribing information. In: Physician’s desk reference for nonprescription drugs and dietary supplements. 23rd. ed. Montvale, NJ; Medical Economics Company, Inc.; 2002:689.

i. Medtech. Dermoplast (benzocaine) antibacterial spray prescribing information. In: Physician’s desk reference for nonprescription drugs and dietary supplements. 23rd. ed. Montvale, NJ; Medical Economics Company, Inc.; 2002:689-70.

j. Blistex. Ivarest medicated cream & lotion prescribing information. In: Physician’s desk reference for nonprescription drugs. 8th. ed. Montvale, NJ; Medical Economics Company, Inc.; 1987:521.

k. Food and Drug Administration. FDA Public Health Advisory: Life-threatening side effects with use of skin products containing numbing ingredients for cosmetic procedures. 2007 Feb 6, updated 2007 Feb 9. From FDA website ().

fn. Other references apply.

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