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Anesthetics (Topical)

This monograph includes information on the following:

1) Benzocaine
2) Benzocaine and Menthol
3) Butamben
4) Dibucaine
5) Lidocaine
6) Pramoxine
7) Pramoxine and Menthol
8) Tetracaine  
9) Tetracaine and Menthol 

Note: See also individual Lidocaine and Prilocaine (Topical) monograph.



INN:
{01}Dibucaine—Cinchocaine
Pramoxine—Pramocaine

BAN:
{01}Dibucaine—Cinchocaine
Lidocaine—Lignocaine
Tetracaine —Amethocaine


JAN:
{01}Benzocaine—Ethyl aminobenzoate

VA CLASSIFICATION

Note: Several of the dosage forms listed below are commercially available in more than one formulation. Because the vehicle into which a local anesthetic is incorporated may determine the appropriate usage and/or site(s) of application of a product, some of the VA classifications listed for a dosage form may apply only to specific formulations.

Benzocaine
Cream
Primary: DE700

Ointment
Primary: RS201
Secondary: DE700; RS900

Topical Aerosol
Primary: DE700
Secondary: NT300; OR600

Topical Spray Solution
Primary: DE700


Benzocaine and Menthol
Primary: DE700

Butamben
Primary: DE700

Dibucaine
Cream
Primary: DE700

Ointment
Primary: RS201
Secondary: DE700; RS900


Lidocaine
Ointment 2.5%
Primary: DE700

Ointment 5%
Primary: NT300
Secondary: DE700; OR600

Topical Spray Solution
Primary: DE700


Lidocaine Hydrochloride
Topical Aerosol
Primary: DE700

Film-forming Gel
Primary: DE700

Jelly
Primary: NT300
Secondary: GU900; DE700

Ointment
Primary: DE700


Pramoxine
Cream
Primary: RS201
Secondary: DE700; RS900

Lotion
Primary: DE700


Pramoxine and Menthol
Gel
Primary: DE700

Lotion
Primary: DE700


Tetracaine
Cream
Primary: RS201
Secondary: DE700; RE900


Tetracaine and Menthol
Ointment
Primary: RS201
Secondary: DE700; RE900




Note: For information on local anesthetics applied topically to the oral, rectal, or other mucosa, see Anesthetics (Mucosal-Local) .
In Canada, Nupercainal Cream contains domiphen bromide in addition to dibucaine.

Commonly used brand name(s): After Burn Double Strength Gel5; After Burn Double Strength Spray5; After Burn Gel5; After Burn Spray5; Almay Anti-itch Lotion7; Alphacaine5; Americaine Topical Anesthetic First Aid Ointment1; Americaine Topical Anesthetic Spray1; Butesin Picrate3; DermaFlex5; Dermoplast2; Endocaine1; Lagol1; Norwood Sunburn Spray5; Nupercainal Cream4; Nupercainal Ointment4; Pontocaine Cream8; Pontocaine Ointment9; Pramegel7; Prax6; Shield Burnasept Spray1; Tronothane6; Xylocaine5.

Other commonly used names are:
Amethocaine — Tetracaine 
Butyl aminobenzoate —Butamben
Cinchocaine —Dibucaine
Ethyl aminobenzoate —Benzocaine
Lignocaine — Lidocaine
Pramocaine —Pramoxine

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).

Not commercially available in Canada.



Category:


Anesthetic, local—

Indications

Accepted

Skin disorders, minor (treatment)—Topical anesthetics are indicated to relieve pain, pruritus, and inflammation associated with minor skin disorders, including:

• Burns, minor, including sunburn. {04} {07} {08} {10}


• Bites (or stings), insect. {03} {04} {06} {07} {08} {10}


• Dermatitis, contact, including poison ivy, poison oak, or poison sumac. {03}


• Wounds, minor, such as cuts and scratches. {04} {06} {07} {10}



Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Chemical group—
    Amides: Dibucaine, lidocaine.
    Esters, aminobenzoic acid (para-aminobenzoic acid, PABA)–derivative: Benzocaine, butamben, tetracaine.
    Unclassified: Pramoxine.
Molecular weight—
    {01}Benzocaine: 165.19
    Butamben picrate: 615.60
    Dibucaine: 343.47
    Lidocaine: 234.34
    Lidocaine hydrochloride: 288.82
    Pramoxine hydrochloride: 329.87
    Tetracaine: 264.37
    Tetracaine hydrochloride: 300.83

pKa—
    Dibucaine: 8.8
    Lidocaine: 7.9
    Tetracaine: 8.2

Mechanism of action/Effect:

Local anesthetics block both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.


Other actions/effects:

If significant quantities of topical anesthetics are absorbed, actions on the central nervous system (CNS) may lead to CNS stimulation and/or CNS depression. Actions on the cardiovascular system may cause depression of cardiac conduction and excitability, and possibly peripheral vasodilation.

Absorption:

Absorption is variable; dependent on specific drug and/or its specific salt. Benzocaine is minimally absorbed. In general, ionized forms(salts) of local anesthetics are not readily absorbed through intact skin. However, both nonionized (bases) and ionized forms of local anesthetics are readily absorbed through traumatized or abraded skin into the systemic circulation.

Biotransformation:


Amides:

Hepatic and some renal.

Lidocaine: Xylidide metabolites are active and toxic, but less so than the parent compound.



Esters, PABA-derivative:

Hydrolyzed by plasma cholinesterases, and to a much lesser extent by hepatic cholinesterases, to PABA-containing metabolites.


Onset of action:

Dibucaine—Up to 15 minutes.

Pramoxine—3 to 5 minutes.

Tetracaine—Slow.

Duration of action:

Lidocaine—Approximately 45 minutes.

Tetracaine—Approximately 30 to 45 minutes.

Elimination:


Amides—
        Renal, primarily as metabolites.
        Lidocaine: Up to 10% of an absorbed dose may be excreted unchanged.



Esters—
        Renal, as metabolites.



Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to one ester-derivative (especially a PABA-derivative) local anesthetic may be sensitive to other ester derivatives also.

Patients sensitive to PABA, parabens, or paraphenylenediamine (a hair dye) may be sensitive to PABA-derivative topical anesthetics also.

Patients sensitive to one amide derivative may rarely be sensitive to other amide derivatives also.

Cross-sensitivity between amide derivatives and ester derivatives, or between amides or esters and the chemically unrelated pramoxine, has not been reported.

Pregnancy/Reproduction

Pregnancy—
Problems in humans with topical anesthetics have not been documented.


Benzocaine, butamben, dibucaine, and pramoxine

Studies in humans have not been done.

Studies in animals have not been done.



Lidocaine

Adequate and well-controlled studies in humans have not been done.

Studies in animals given up to 6.6 times the human dose have shown no adverse effects on the fetus.

Lidocaine ointment 5%—FDA Pregnancy Category B. {11}



Tetracaine

Studies in humans have not been done.

Studies in animals have not been done.

FDA Pregnancy Category C.


Breast-feeding

Problems in humans have not been documented.

Pediatrics

Benzocaine—Benzocaine should be used with caution in infants and young children because increased absorption through the skin (with excessive use) may result in methemoglobinemia. Benzocaine-containing topical formulations should not be used in children younger than 2 years of age unless prescribed by a physician. {04}

Other topical anesthetics—No information is available on the relationship of age to the effects of these medications in pediatric patients following application to the skin. However, it is recommended that a physician be consulted before any topical local anesthetic is used in children younger than 2 years of age. {20}


Geriatrics


No information is available on the relationship of age to the effects of topical anesthetics in geriatric patients following application to the skin.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.


For ester derivatives
Cholinesterase inhibitors such as
Antimyasthenics
Cyclophosphamide
Demecarium
Echothiophate
Insecticides, neurotoxic, possibly including large quantities of topical malathion
Isoflurophate
Thiotepa    (these agents may inhibit metabolism of ester derivatives; absorption of significant quantities of ester derivatives in patients receiving a cholinesterase inhibitor may lead to increased risk of toxicity)


Sulfonamides    (metabolites of PABA-derivative topical anesthetics may antagonize antibacterial activity of sulfonamides, especially if the anesthetics are absorbed in significant quantities over prolonged periods of time)


For lidocaine
Antiarrhythmic agents, amide local anesthetic–derivative, other, such as
Mexiletine
Tocainide or
Lidocaine, systemic or parenteral-local    (risk of cardiotoxicity associated with additive cardiac effects, and, with systemic or parenteral-local lidocaine, the risk of overdose, may be increased in patients receiving these medications if large quantities of topically applied lidocaine are absorbed {12} {13})


Beta-adrenergic blocking agents    (concurrent use may slow metabolism of lidocaine because of decreased hepatic blood flow, leading to increased risk of lidocaine toxicity if large quantities are absorbed)


Cimetidine    (cimetidine inhibits hepatic metabolism of lidocaine; concurrent use may lead to lidocaine toxicity if large quantities are absorbed)



Laboratory value alterations
The following have been selected on the basis of their potential clinical significance (possible effect in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):

With diagnostic test results
Pancreatic function determinations using bentiromide    (use of PABA-derivative topical anesthetics or lidocaine prior to the bentiromide test may invalidate test results since these medications are also metabolized to PABA or other arylamines and will thus increase the real or apparent quantity of PABA recovered; patients should be advised to discontinue use of these anesthetics 3 days prior to bentiromide administration)


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
Local infection at site of application    (infection may alter the pH at the treatment site, leading to decrease or loss of local anesthetic effect)


Sensitivity to the topical anesthetic being considered for use or to chemically related anesthetics and, for the ester derivatives, to PABA, parabens, or paraphenylenediamine, or
Sensitivity to other ingredients in the formulation
Skin disorders, severe or extensive, especially if skin is abraded or broken    (increased absorption of anesthetic)




Side/Adverse Effects

Note: Adverse reactions are due to excessive dosage or rapid absorption, which produces high plasma concentrations, as well as to idiosyncrasy, hypersensitivity, or decreased patient tolerance.
Benzocaine and tetracaine are more likely to cause contact sensitization than are the other local anesthetics.

The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence less frequent
    
Angioedema (large, hive-like swellings on skin, mouth, or throat)
    
dermatitis, contact (skin rash, redness, itching, or hives; burning, stinging, swelling, or tenderness not present before therapy){11}





Overdose
For specific information on the agents used in the management of topical anesthetics overdose, see:
   • Ascorbic Acid (Systemic) monograph;
   • Benzodiazepines (Systemic) monograph;
   • Sympathomimetic Agents—Cardiovascular Use (Parenteral-Systemic) monograph; and/or


Methylene Blue (Systemic) monograph.
For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).

Clinical effects of overdose
The following effects have been selected on the basis of their potential clinical significance if excessive systemic absorption occurs (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
    
Cardiovascular system depression (low blood pressure; slow or irregular heartbeat; unusual paleness; increased sweating)—may lead to cardiac arrest
    
CNS toxicity (blurred or double vision; confusion; convulsions; dizziness or lightheadedness; drowsiness; feeling hot, cold, or numb; ringing or buzzing in the ears; shivering or trembling; unusual anxiety, excitement, nervousness, or restlessness){11}
    
methemoglobinemia (difficulty in breathing on exertion; dizziness; headache; unusual tiredness or weakness)

Note: Stimulant and/or depressant manifestations of CNS toxicity may occur. CNS stimulation usually occurs first, followed by CNS depression. However, CNS stimulation may be transient or absent, so that drowsiness may be the first symptom of toxicity in some patients. CNS depression may lead to unconsciousness and respiratory arrest. {11}



Treatment of overdose
Recommended treatment includes:


Specific treatment:
For methemoglobinemia—Administering methylene blue (1 to 2 mg per kg of body weight, intravenously) and/or ascorbic acid (100 to 200 mg orally). {14}

For circulatory depression—Administration of a vasopressor and intravenous fluids is recommended.

For convulsions—Administering an anticonvulsant, usually a benzodiazepine, {16} keeping in mind that benzodiazepines may cause respiratory {17} and circulatory {14} depression, especially when administered rapidly. {18} Medications and equipment needed for support of respiration and for resuscitation must be immediately available. {19}



Supportive Care:
For systemic reactions caused by excessive absorption—Securing and maintaining a patent airway, administering oxygen, and instituting assisted or controlled respiration as required. In some patients, endotracheal intubation may be required. {15}



Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Anesthetics (Topical).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to local anesthetics of the same chemical class, and, for ester derivatives only, aminobenzoic acid, parabens, or hair dye





Use in children—Caution that excessive quantities of benzocaine may cause methemoglobinemia in children younger than 2 years of age; consulting physician before using any topical local anesthetic in children younger than 2 years of age


Proper use of this medication
Following physician's instructions if prescribed

Following manufacturer's instructions if self-medicating

» Not using on large areas, especially if skin broken or abraded, or for prolonged periods of time, without physician's advice

» Checking with physician before using for problems other than prescribed or recommended on package label, or if any suspicion of infection

» Not using products containing alcohol, which is flammable, near fire or open flame or while smoking; not smoking until area completely dry

» Using care not to get in eyes, mouth, or nose; if using topical aerosol or spray dosage forms, applying to face with hand or other suitable applicator

» Proper dosing
Missed dose (if on scheduled dosing): Applying as soon as possible; not applying if almost time for next dose

» Proper storage

For butamben
Butamben may permanently stain clothing and hair; covering area with a loose bandage after application to protect clothing and not allowing hair to come into contact with the medication {22}

For lidocaine film-forming gel
Proper application technique: Drying area before applying; applying medication, then waiting 60 seconds until transparent film forms
{06}
Precautions while using this medication
» Taking precautions to prevent children from transferring medication to their mouths after application
»
Discontinuing use and checking with physician
If condition does not improve within 7 days or worsens

If problem area becomes infected

If rash, irritation, or other symptoms not present before use occur

If medication is swallowed


Side/adverse effects
Signs and symptoms of potential side effects, especially angioedema, contact dermatitis, and overdose


General Dosing Information
These medications should not be applied over large areas, or for prolonged periods of time, especially to broken or abraded skin, because of the increased risk of systemic absorption and toxicity.

Topical anesthetic–containing medications may be sprayed or applied directly to the affected area, or applied with a suitable applicator (for example, a sterile gauze pad or cotton swab).



BENZOCAINE

Summary of Differences


Physicochemical characteristics:
An ester-type (PABA-derivative) local anesthetic.



Precautions:


Cross-sensitivity and/or related problems—
May occur with other ester-type anesthetics, especially other PABA derivatives, with PABA or parabens, and with paraphenylenediamine.



Pediatrics—
Excessive use may cause methemoglobinemia in infants and young children.



Drug interactions and/or related problems—
Cholinesterase inhibitors may inhibit metabolism of benzocaine.

Benzocaine may antagonize antibacterial activity of sulfonamides.




Side/adverse effects:
More likely to cause contact sensitization than most other topical anesthetics.

See also Side/Adverse Effects .



Topical Dosage Forms

BENZOCAINE CREAM USP

Usual adult and adolescent dose
Anesthetic, local
Topical, to the affected area three or four times a day {21} as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


5% (OTC)[Generic]{05}

Packaging and storage:
Store below 30 °C (86 °F). Store in a tight container. Protect from light. Protect from freezing.

Auxiliary labeling:
   • For external use only.


BENZOCAINE OINTMENT USP

Usual adult and adolescent dose
Anesthetic, local
Topical, to the affected area three or four times a day {21} as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


5% (OTC) [Lagol{05}]


20% (OTC) [Americaine Topical Anesthetic First Aid Ointment{04}]

Packaging and storage:
Store below 30 °C (86 °F). Store in a tight container. Protect from light. Protect from freezing.

Auxiliary labeling:
   • For external use only.


BENZOCAINE TOPICAL AEROSOL USP

Usual adult and adolescent dose
Anesthetic, local
Topical, sprayed on or applied to affected area three or four times a day {21} as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


20% (OTC) [Americaine Topical Anesthetic Spray{04}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer.

Auxiliary labeling:
   • Shake well.
   • For external use only.


BENZOCAINE TOPICAL SPRAY SOLUTION

Usual adult and adolescent dose
Anesthetic, local
Topical, sprayed on or applied to affected area three or four times a day {21} as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—

Canada—


2% (OTC) [Shield Burnasept Spray{02}]


20% (OTC) [Endocaine{01}{02}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer.

Auxiliary labeling:
   • For external use only.


BENZOCAINE AND MENTHOL

Summary of Differences


Physicochemical characteristics:
An ester-type (PABA-derivative) local anesthetic.



Precautions:


Cross-sensitivity and/or related problems—
May occur with other ester-type anesthetics, especially other PABA derivatives, with PABA or parabens, and with paraphenylenediamine.



Pediatrics—
Excessive use may cause methemoglobinemia in infants and young children.



Drug interactions and/or related problems—
Cholinesterase inhibitors may inhibit metabolism of benzocaine.

Benzocaine may antagonize antibacterial activity of sulfonamides.




Side/adverse effects:
More likely to cause contact sensitization than most other topical anesthetics.

See also Side/Adverse Effects .



Topical Dosage Forms

BENZOCAINE AND MENTHOL LOTION

Usual adult and adolescent dose
Anesthetic, local
Topical, to the affected area three or four times a day as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


8% of benzocaine and 0.5% of menthol (OTC) [Dermoplast (methylparaben )]{05}

Packaging and storage:
Store below 30 °C (86 °F). Protect from freezing.

Auxiliary labeling:
   • For external use only.


BENZOCAINE AND MENTHOL TOPICAL AEROSOL

Usual adult and adolescent dose
Anesthetic, local
Topical, sprayed on or applied to affected area three or four times a day {21} as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


8% of benzocaine and 0.5% of menthol (OTC) [Dermoplast (methylparaben ){05}]

Canada—


4.5% of benzocaine and 0.5% of menthol (OTC) [Dermoplast ( methylparaben) (isopropyl alcohol){21}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer.

Auxiliary labeling:
   • Shake well.
   • For external use only.


BUTAMBEN

Summary of Differences


Physicochemical characteristics:
Butamben is an ester-type (PABAderivative) local anesthetic.



Precautions:


Cross-sensitivity and/or related problems—
May occur with other ester-type anesthetics, especially other PABA derivatives, with PABA or parabens, and with paraphenylenediamine.



Drug interactions and/or related problems—
Cholinesterase inhibitors may inhibit metabolism of butamben.

Butamben may antagonize antibacterial activity of sulfonamides.




Topical Dosage Forms

BUTAMBEN PICRATE OINTMENT

Usual adult and adolescent dose
Anesthetic, local
Topical, to the skin, as a 1% ointment three or four times a day as needed {21}.


Note: Area should be loosely bandaged to protect clothing from staining.


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


1% (OTC) [Butesin Picrate{05}]

Packaging and storage:
Store below 25 °C (77 °F), unless otherwise specified by manufacturer. {22} Protect from freezing.

Auxiliary labeling:
   • For external use only.


DIBUCAINE

Summary of Differences


Physicochemical characteristics:
Dibucaine is an amide-type local anesthetic.



Precautions:
Cross-sensitivity and/or related problems—Rarely, may occur with other amide-type local anesthetics.

Laboratory value alterations—No interference with bentiromide test for pancreatic function.



Topical Dosage Forms

DIBUCAINE CREAM USP

Usual adult and adolescent dose
Anesthetic, local
Topical, to the skin, as a 0.5% cream three or four times a day as needed {21}.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


0.5% (OTC) [Nupercainal Cream{07} (acetone sodium bisulfite)][Generic]{07}

Note: In Canada, Nupercainal Cream also contains domiphen bromide. {02}


Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a collapsible tube or a tight, light-resistant container. Protect from freezing.

Auxiliary labeling:
   • For external use only.


DIBUCAINE OINTMENT USP

Usual adult and adolescent dose
Anesthetic, local
Topical, to the skin, as a 1% ointment three or four times a day as needed {21}.


Note: Area may be lightly covered for protection.


Usual adult prescribing limits
Not more than 30 grams in a twenty-four-hour period. {07}

Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Usual pediatric prescribing limits
Not more than 7.5 grams in a twenty-four-hour period. {07}

Strength(s) usually available
U.S.—


1% (OTC) [Nupercainal Ointment{07}][Generic]

Canada—


1% (OTC) [Nupercainal Ointment]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a collapsible tube or in a tight, light-resistant container. Protect from freezing.

Auxiliary labeling:
   • For external use only.


LIDOCAINE

Summary of Differences


Physicochemical characteristics:
Lidocaine is an amide-type local anesthetic.



Precautions:
Cross-sensitivity and/or related problems—Rarely, may occur with other amide-type local anesthetics.

Drug interactions—Possibility of toxicity in patients receiving local anesthetic–derivative antiarrhythmic agents, lidocaine via other routes of administration, beta-adrenergic blocking agents, or cimetidine if large quantities of topically administered lidocaine are absorbed.



Topical Dosage Forms

LIDOCAINE OINTMENT USP

Usual adult and adolescent dose
Anesthetic, local
Topical, as a 2.5% or 5% ointment, to the affected area three or four times a day {21} as needed.


Usual adult prescribing limits
For the 5% ointment—Not more than 5 grams per single application or 20 grams per day. {11}

Usual pediatric dose
Anesthetic, local
Dosage must be individualized, depending on the child"s age, weight, and physical condition, up to a maximum of 4.5 mg per kg of body weight. {11}


Strength(s) usually available
U.S.—


2.5% (OTC) [Xylocaine{10}]


5% (Rx) [Xylocaine][Generic]{11}

Canada—


5% (OTC) [Alphacaine{02}] [Xylocaine{02}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in a tight container. Protect from freezing.

Auxiliary labeling:
   • For external use only.


LIDOCAINE TOPICAL SPRAY SOLUTION

Usual adult and adolescent dose
Anesthetic, local
Topical, sprayed on or applied to affected area three or four times a day {21} as needed.


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—

Canada—


2% (OTC) [Norwood Sunburn Spray{02}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


LIDOCAINE HYDROCHLORIDE TOPICAL AEROSOL

Usual adult and adolescent dose
Anesthetic, local
Topical, sprayed on or applied to the affected area three or four times a day {21} as needed.


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—

Canada—


0.5% (OTC) [After Burn Spray{02}]


1% (OTC) [After Burn Double Strength Spray{02}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • Shake well.
   • For external use only.


LIDOCAINE HYDROCHLORIDE FILM-FORMING GEL

Usual adult and adolescent dose
Anesthetic, local
Topical, applied to affected area three or four times a day as needed. {06}


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


2.5% (OTC) [DermaFlex{06}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


LIDOCAINE HYDROCHLORIDE JELLY USP

Usual adult and adolescent dose
Anesthetic, local
Topical, to the affected area three or four times a day {21} as needed.


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—

Canada—


0.5% (OTC) [After Burn Gel{02}]


1% (OTC) [After Burn Double Strength Gel{02}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


LIDOCAINE HYDROCHLORIDE OINTMENT

Usual adult and adolescent dose
Anesthetic, local
Topical, as a 5% ointment, to the affected area three or four times a day {21} as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage has not been established.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


5% (Rx)[Generic]{05}

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


PRAMOXINE

Summary of Differences
Physicochemical characteristics: Pramoxine is an unclassified(neither an amide-type nor an ester-type) local anesthetic.

Precautions: Diagnostic interference—No interference with bentiromide test for pancreatic function.


Topical Dosage Forms

PRAMOXINE HYDROCHLORIDE CREAM USP

Usual adult and adolescent dose
Anesthetic, local
Topical, as a 1% cream, every three to four hours as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage has not been established.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


1% (OTC) [Prax] [Tronothane{05}]

Canada—


1% (OTC) [Tronothane{02}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Store in tight container. Protect from freezing.

Auxiliary labeling:
   • For external use only.


PRAMOXINE HYDROCHLORIDE LOTION

Usual adult and adolescent dose
Anesthetic, local
Topical, as a 1% lotion, every three or four hours as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage has not been established.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


1% (OTC) [Prax{09}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


PRAMOXINE HYDROCHLORIDE AND MENTHOL

Summary of Differences
Physicochemical characteristics: Pramoxine is an unclassified(neither an amide-type nor an ester-type) local anesthetic.

Precautions: Diagnostic interference—No interference with bentiromide test for pancreatic function.


Topical Dosage Forms

PRAMOXINE HYDROCHLORIDE AND MENTHOL GEL

Usual adult and adolescent dose
Anesthetic, local
—Topical, applied to affected areas three or four times a day as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage has not been established.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


1% of pramoxine hydrochloride and 0.5% of menthol (OTC) [Pramegel{08}]

Canada—


1% of pramoxine hydrochloride and 0.5% of menthol (OTC) [Pramegel{02}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


PRAMOXINE HYDROCHLORIDE AND MENTHOL LOTION

Usual adult and adolescent dose
Anesthetic, local
Topical, applied to affected areas three or four times a day {21} as needed.


Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage has not been established.

Children 2 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


1% of pramoxine hydrochloride and 0.2% of menthol (OTC) [Almay Anti-itch Lotion{03}]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


TETRACAINE

Summary of Differences


Physicochemical characteristics:
An ester-type (PABA-derivative) local anesthetic.



Precautions:
Cross-sensitivity and/or related problems—May occur with other ester-type anesthetics, especially other PABA derivatives, with PABA or parabens, and with paraphenylenediamine.



Drug interactions and/or related problems:
Cholinesterase inhibitors may inhibit metabolism of tetracaine.

Tetracaine may antagonize antibacterial activity of sulfonamides.



Side/adverse effects:
More likely to cause contact sensitization than most other topical anesthetics.

See also Side/Adverse Effects .



Topical Dosage Forms

TETRACAINE HYDROCHLORIDE CREAM USP

Usual adult and adolescent dose
Anesthetic, local
Topical, applied as a 1% cream to affected areas three or four times a day as needed {21}.


Usual adult prescribing limits
Not more than 28.35 grams in a twenty-four-hour period.

Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Usual pediatric prescribing limits
Not more than 7 grams in a twenty-four-hour period.

Strength(s) usually available
U.S.—


1% (OTC) [Pontocaine Cream{04}]

Canada—
Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.


TETRACAINE AND MENTHOL

Summary of Differences


Physicochemical characteristics:
An ester-type (PABA-derivative) local anesthetic.



Precautions:
Cross-sensitivity and/or related problems—May occur with other ester-type anesthetics, especially other PABA derivatives, with PABA or parabens, and with paraphenylenediamine.



Drug interactions and/or related problems:
Cholinesterase inhibitors may inhibit metabolism of tetracaine.

Tetracaine may antagonize antibacterial activity of sulfonamides.



Side/adverse effects:
More likely to cause contact sensitization than most other topical anesthetics.

See also Side/Adverse Effects .



Topical Dosage Forms

TETRACAINE AND MENTHOL OINTMENT USP

Usual adult and adolescent dose
Anesthetic, local
Topical, applied to affected area as a 0.5% ointment three or four times a day as needed {21}.


Usual adult prescribing limits
Not more than 28.35 grams in a twenty-four-hour period.

Usual pediatric dose
Anesthetic, local
Children up to 2 years of age: Dosage must be individualized by a physician.

Children 2 years of age and older: See Usual adult and adolescent dose.


Usual pediatric prescribing limits
Not more than 7 grams in a twenty-four-hour period.

Strength(s) usually available
U.S.—


0.5% of tetracaine and 0.5% of menthol (OTC) [Pontocaine Ointment{04}]

Canada—
Not commercially available.

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For external use only.



Revised: 08/29/94



References

Note: All references used in the development and earlier revisions of this monograph have not yet been incorporated into the computer database and, therefore, are not listed below. Citations for information not yet referenced in the monograph will be provided upon request.

  1. Fleeger CA, editor. USAN 1994. USAN and the USP dictionary of drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1993: 79, 207, 378, 540, 653.
  1. Krogh CME, editor. Self-Medication Product Information. 4th ed Volume 2. Ottawa: Canadian Pharmaceutical Association, 1993: 380, 384, 390-2.
  1. Almay Anti-itch Lotion (Almay). In: PDR Physicians' desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 503.
  1. Americaine formulations. In: PDR Physicians' desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 562.
  1. Red book 1994. Montvale, NJ: Medical Economics Data, 1994: 437, 461, 469, 497, 499, 562, 625, 679.
  1. DermaFlex (Zila). In: PDR Physicians' desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 789.
  1. Nupercainal (Ciba). In: PDR Physicians' desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 832.
  1. Pramegel (GenDerm). In: PDR Physicians' desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 999.
  1. Prax (Ferndale). In: PDR Physicians' desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 923.
  1. Xylocaine Ointment 2.5% (Astra—US). Rev 11/93, Rec 2/94.
  1. Xylocaine Ointment 5% (Astra—US). Rev 1/94, Rec 5/94.
  1. Xylocaine 4% Topical Solution (Astra). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 1375-6.
  1. Xylocaine 5% Topical Solution (Astra). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 1384-5.
  1. Ellenhorn MJ, Barceloux DG. Medical toxicology. Diagnosis and treatment of human poisoning. New York: Elsevier, 1988: 1263-5, 1317-24.
  1. Reviewers' consensus on Anesthetics (Mucosal-Local) monograph revision for USP DI 1985.
  1. Reviewers' consensus, Benzodiazepines (Systemic) monograph, USP DI.
  1. Panel comments, Lidocaine and Prilocaine (Topical) monograph draft 6/93.
  1. Panel comment, Lidocaine and Prilocaine (Topical) ballot 6/93.
  1. Panel comments, Lidocaine and Prilocaine (Topical) monograph draft 6/93 and ballot 6/93.
  1. Reviewers' consensus on monograph revision 6/94.
  1. Reviewers' responses on monograph revision 6/94.
  1. Manufacturer comment, 6/94.
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