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Anesthetics (Mucosal-Local)

This monograph includes information on the following:

1) Benzocaine
2) Benzocaine, Butamben, and Tetracaine
3) Dibucaine
4) Dyclonine
5) Lidocaine
6) Pramoxine
7) Tetracaine

Note: See also individual Cocaine (Mucosal-Local) monograph.



INN:
{36}Dibucaine—Cinchocaine
Pramoxine—Pramocaine

BAN:
{36}Dibucaine—Cinchocaine
Dyclonine—Dyclocaine
Lidocaine—Lignocaine
Tetracaine—Amethocaine


JAN:
Benzocaine—Ethyl aminobenzoate {36}

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 for a product, some of the VA classifications listed for a dosage form may apply only to specific formulations.


Benzocaine Dental pastePrimary: OR600

Benzocaine Gel
Primary: NT300
Secondary: GU900; OR600; RS900

Benzocaine Lozenges
Primary: OR600

Benzocaine Ointment
Primary: RS201
Secondary: DE700; OR600; RS900

Benzocaine Topical aerosol
Primary: DE700
Secondary: NT300; OR600

Benzocaine Topical solution
Primary: NT300
Secondary: OR600

Benzocaine and Menthol Lozenges
Primary: OR600

Benzocaine and Phenol Gel
Primary: OR600

Benzocaine and Phenol Topical solution
Primary: OR600

Benzocaine, Butamben, and Tetracaine Gel
Primary: NT300
Secondary: GU900; OR600 ; RS900

Benzocaine, Butamben, and Tetracaine Ointment
Primary: NT300
Secondary: OR600

Benzocaine, Butamben, and Tetracaine Topical aerosol
Primary: NT300
Secondary: OR600

Benzocaine, Butamben, and Tetracaine Topical solution
Primary: NT300
Secondary: OR600

Dibucaine Ointment
Primary: RS201
Secondary: DE700; RS900

Dyclonine Lozenges
Primary: OR600

Dyclonine Topical solution
Primary: NT300
Secondary: GU900; OR600; RS900

Lidocaine Ointment
Primary: NT300
Secondary: DE700; OR600

Lidocaine Oral topical solution
Primary: OR600

Lidocaine Topical aerosol
Primary: NT300
Secondary: OR600

Lidocaine Hydrochloride Jelly
Primary: NT300
Secondary: GU900

Lidocaine Hydrochloride Oral topical solution
Primary: NT300
Secondary: OR600

Lidocaine Hydrochloride Topical solution
Primary: NT300
Secondary: OR600

Lidocaine Hydrochloride Topical spray solution
Primary: NT300

Pramoxine Aerosol foam
Primary: RS201
Secondary: RS900

Pramoxine Cream
Primary: RS201
Secondary: DE700; RS900

Pramoxine Ointment
Primary: RS201

Tetracaine Cream
Primary: RS201
Secondary: DE700; RS900

Tetracaine Hydrochloride Topical Solution
Primary: NT300

Tetracaine and Menthol Ointment
Primary: RS201
Secondary: DE700; RS900



Note: For information on local anesthetics applied topically to the skin to relieve minor dermatological conditions, see Anesthetics (Topical).
For information on use of lidocaine hydrochloride by transtracheal injection to anesthetize the larynx and trachea, see Anesthetics (Parenteral-Local) .

Commonly used brand name(s): Americaine1; Americaine Anesthetic Lubricant1; Americaine Hemorrhoidal1; Anbesol Baby Jel1; Anbesol Gel1; Anbesol Liquid1; Anbesol Maximum Strength Gel1; Anbesol Maximum Strength Liquid1; Anbesol Regular Strength Gel1; Anbesol Regular Strength Liquid1; Anbesol, Baby1; Anestacon Jelly5; Benzodent1; Cetacaine Topical Anesthetic2; Chloraseptic Lozenges1; Chloraseptic Lozenges Cherry Flavor1; Chloraseptic Lozenges, Children's1; Dent-Zel-Ite1; Dentapaine1; Dentocaine1; Dyclone4; Fleet Relief6; Hurricaine1; Num-Zit Gel1; Num-Zit Lotion1; Numzident1; Nupercainal3; Orabase, Baby1; Orabase-B with Benzocaine1; Orajel1; Orajel Extra Strength1; Orajel Liquid1; Orajel Maximum Strength1; Orajel Nighttime Formula, Baby1; Orajel, Baby1; Oratect Gel1; Pontocaine7; Pontocaine Cream7; Pontocaine Ointment7; ProctoFoam/non-steroid6; Rid-A-Pain1; SensoGARD Canker Sore Relief1; Spec-T Sore Throat Anesthetic1; Sucrets Maximum Strength4; Sucrets Regular Strength4; Sucrets, Children's4; Topicaine1; Tronolane6; Tronothane6; Xylocaine5; Xylocaine Dental Ointment5; Xylocaine Endotracheal5; Xylocaine Viscous5; Zilactin-L5.

Amethocaine—TetracaineButyl aminobenzoate —ButambenCinchocaine—DibucaineDyclocaine—DyclonineEthyl aminobenzoate —BenzocaineLignocaine—LidocainePramocaine—Pramoxine Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Anesthetic (mucosal-local)—

Indications

Note: Bracketed information in the Indications section refers to uses that are not included in U.S. product labeling.
Gel, ointment, and topical solution dosage forms of benzocaine, ointment and topical solution dosage forms of lidocaine, and topical solution dosage forms of lidocaine hydrochloride are available in more than one formulation. The vehicles present in different formulations may determine the indication(s) for which the formulations are used. Therefore, some gel, ointment, or topical solution formulations that contain the same local anesthetic cannot be used interchangeably. For additional information regarding formulations and brand name products that may be used for specific indications, see the Dosage Forms section.

Accepted

Anesthesia, local—Indicated to provide topical anesthesia of accessible mucous membranes prior to examination, endoscopy or instrumentation, or other procedures involving the
Esophagus—Benzocaine (gel {02} {12} and topical solution {12}); benzocaine, butamben, and tetracaine; {08} dyclonine (topical solution); {11} lidocaine hydrochloride (4% topical solution {23}, topical spray solution, {32} and [oral topical solution {34}]); and tetracaine hydrochloride (topical solution).

Larynx—Benzocaine (gel {02} {12} and topical solution {12}); benzocaine, butamben, and tetracaine; {08} dyclonine (topical solution); {11} lidocaine hydrochloride (4% topical solution {23} and topical spray solution {32}); and tetracaine hydrochloride (topical solution).

Mouth (in dental procedures and oral surgery)— Benzocaine (gel,{12}{20} topical aerosol,{12} and topical solution{12}); benzocaine, butamben, and tetracaine;{08} dyclonine (topical solution);{11} lidocaine (ointment,{31} topical aerosol,{26}{27} and oral topical solution{24}{25}); and lidocaine hydrochloride (oral topical solution{33} and 4% topical solution{23}).

Nasal cavity—Benzocaine (gel {02} {12}); benzocaine, butamben, and tetracaine; {08} lidocaine hydrochloride (jelly {06} {29} and 4% topical solution {23}); and tetracaine (topical solution).

Pharynx or throat—Benzocaine (gel {02} {12}, topical aerosol, {12} and topical solution {12}); benzocaine, butamben, and tetracaine; {08} dyclonine (topical solution); {11} lidocaine (ointment and topical aerosol {26}); lidocaine hydrochloride (jelly, {06} {29} oral topical solution, {23} and topical spray solution {32}); and tetracaine (topical solution).

Rectum—Benzocaine (gel {02} {12}); benzocaine, butamben, and tetracaine (gel) {08}; and lidocaine hydrochloride (jelly). {29}

Respiratory tract or trachea—Benzocaine (gel {02} {12}, topical aerosol, {12} and topical solution {12}); benzocaine, butamben, and tetracaine; {08} dyclonine (topical solution); {11} lidocaine (ointment); lidocaine hydrochloride (jelly, {06} {29} [oral topical solution], {34} and 4% {23} and 10% {32} topical solution); and tetracaine (topical solution).

Urinary tract—Benzocaine (gel {02}); dyclonine (topical solution); {11} and lidocaine hydrochloride (jelly {06} {29}).

Vagina—Benzocaine (gel {02} {12}); benzocaine, butamben, and tetracaine (gel); {08} and dyclonine (topical solution) {11}.

Gag reflex suppression
Indicated to suppress the gag reflex and/or other laryngeal and esophageal reflexes to facilitate dental examination or procedures (including oral surgery), endoscopy, or intubation: Benzocaine (gel{02}{12}{20}, topical aerosol,{12} and topical solution);{12} benzocaine, butamben, and tetracaine (topical aerosol);{08} dyclonine (0.5% topical solution);{11} [ lidocaine (topical aerosol)];{27} lidocaine hydrochloride (oral topical solution{31} and 10% topical solution{32}); and tetracaine hydrochloride (topical solution).

Anorectal disorders (treatment)—Indicated for the symptomatic relief of
Hemorrhoids
Inflammation, anorectal and
Pain, anorectal—Benzocaine (ointment {03}); dibucaine; {13} pramoxine; {20} {21} tetracaine hydrochloride (cream); and tetracaine and menthol. These medications are effective when applied to the anal, perianal, or anorectal areas. However, they are not likely to relieve symptoms associated with conditions confined to the rectum, which lacks sensory nerve fibers. {37}

Pain, anogenital lesion–associated—Dyclonine (0.5% solution). {11}

Pain, anogenital, external and
Pruritus, anogenital—Benzocaine (ointment {03}); dibucaine; {13} pramoxine (aerosol foam and cream); tetracaine hydrochloride (cream); tetracaine and menthol.

Oral cavity disorders (treatment); and Perioral lesions (treatment)—Indicated for relief of
Canker sores or
Cold sores or
Fever blisters—Benzocaine (gel {04} and topical solution {04}); benzocaine and phenol (gel {04} and topical solution {04}); and lidocaine (2.5% topical solution). {35}

Pain, gingival or oral mucosal (i.e., pain caused by mouth or gum irritation, inflammation, lesions, or minor dental procedures)—Benzocaine (gel, {04} {16} dental paste, lozenges, {09} and topical solution {04}); dyclonine (lozenges {17} and 0.5% topical solution {11}); benzocaine and phenol (gel {04} and topical solution {04}); lidocaine (oral topical solution); {24} {25} and lidocaine hydrochloride (oral topical solution). {33} {34}

Pain, dental prosthetic (i.e., pain or irritation caused by dentures or other dental or orthodontic appliances)—Benzocaine (dental paste, gel, {04} {19} ointment, and topical solution {04}); benzocaine and phenol (gel {04} and topical solution {04}); and lidocaine (ointment) {31}.

Pain, teething—Benzocaine (7.5% and 10% gel {04} {14}).

Toothache—Benzocaine (10% and 20% gel {04} {15} and topical solution); {04} and benzocaine and phenol (gel {04} and topical solution {04}).

Pain, esophageal (treatment)
Dyclonine (topical solution); {11}and [ lidocaine hydrochloride (oral topical solution)] {34}.

Pain, pharyngeal (treatment)
Benzocaine (lozenges); {09}benzocaine and menthol (lozenges); {10} dyclonine (lozenges); {17} and lidocaine hydrochloride (oral topical solution). {33} {34}

Pain, vaginal (treatment)
Indicated to relieve pain following procedures such as episiotomy or perineorraphy: Benzocaine (topical aerosol and topical solution); and dyclonine (topical solution). {11}

Urethritis (treatment)
Indicated to relieve or control pain: Lidocaine hydrochloride (jelly {06}).


Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Chemical group—
    Amides: Dibucaine, lidocaine
    Esters, aminobenzoic acid (para-aminobenzoic acid, PABA)–derivative: Benzocaine, butamben, tetracaine
    Unclassified: Dyclonine, pramoxine
Molecular weight—
{36}    Benzocaine: 165.19
    Butamben: 193.25
    Dibucaine: 343.47
    Dyclonine hydrochloride: 325.88
    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 substantial quantities of local anesthetics are absorbed through the mucosa, actions on the central nervous system (CNS) may cause CNS stimulation and/or CNS depression. Actions on the cardiovascular system may cause depression of cardiac conduction and excitability and, with some of these agents, peripheral vasodilation.

Absorption:

Except for benzocaine, which is minimally absorbed, these agents are readily absorbed through mucous membranes into the systemic circulation. The rate of absorption is influenced by the vascularity or rate of blood flow at the site of application, the total dosage (concentration and volume) {06} {24} {26} {27} {28} {33} administered, and the duration of exposure. {06} {24} {26} {27} {28} {33} Absorption from mucous membranes of the throat or respiratory tract may be especially rapid. Addition of a vasoconstrictor to the anesthetic may not reduce or slow absorption sufficiently to protect against systemic effects.

Protein binding:

Lidocaine—Concentration-dependent, to alpha 1-acid glycoprotein; usually about 60 to 80% at concentrations of 1 to 4 mcg per mL (4.3 to 17.2 micromoles per L). {06} {23} {24} {25} {26} {27} {28} {29} {31} {32} {33}

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:

Benzocaine—About 1 minute.

Benzocaine, butamben, and tetracaine—About 30 seconds. {08}

Dibucaine—Up to 15 minutes.

Dyclonine—Up to 10 minutes.

Lidocaine—Within 1 to 5 minutes, depending on formulation. {23} {24} {25} {26} {27} {28} {29} {31} {32} {34}

Pramoxine—3 to 5 minutes.

Tetracaine—3 to 10 minutes.

Duration of action:


Benzocaine:

15 to 20 minutes.



Dibucaine:

2 to 4 hours.



Dyclonine:

Approximately 30 to 60 minutes.



Lidocaine:

Approximately 30 to 60 minutes.

Lidocaine oral topical solution: 15 to 20 minutes. {24}

Lidocaine topical aerosol: 10 to 15 minutes. {26} {27}



Tetracaine:

Approximately 30 to 60 minutes.


Elimination:


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



Esters—
        Renal, primarily as metabolites.



Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to one ester derivative (especially an aminobenzoic acid [para-aminobenzoic acid; PABA] derivative) may be sensitive to other ester derivatives also.

Patients sensitive to PABA, parabens, or paraphenylenediamine (a hair dye) may be sensitive to PABA-derivative local 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 chemically unrelated local anesthetics (i.e., dyclonine or pramoxine), has not been reported. However, some lidocaine formulations and pramoxine cream contain parabens, to which cross-sensitivity with PABA-derivative local anesthetics may exist. {20} {21} {22} {23} {28} {29} {33} {34}

Pregnancy/Reproduction
Fertility—

Dyclonine

Studies have not been done. {11}



Lidocaine

Studies have not been done. {06} {23} {24} {25} {26} {27} {28} {29} {32}


Pregnancy—

Benzocaine

Studies in humans have not been done.

Studies in animals have not been done.

Benzocaine gel: FDA Pregnancy Category C. {02}



Dyclonine

Studies in humans have not been done.

Studies in animals have not been done.

Dyclonine topical solution: FDA Pregnancy Category C. {11}



Lidocaine

Adequate and well-controlled studies in humans have not been done. {06} {23} {24} {25} {26} {27} {28} {29} {32} {33} {34}

Studies in rats given up to 6.6 times the human dose have not shown evidence of teratogenicity or harm to the fetus. {06} {23} {24} {25} {26} {27} {28} {29} {32} {33} {34}

FDA Pregnancy Category B. {06} {24} {26} {28} {33}



Other mucosal-local anesthetics

Problems in humans have not been documented.


Breast-feeding


Lidocaine:

—Distributed into breast milk in very small quantities that pose no risk to the infant. {23} {25} {27} {29} {31} {32} {34}



Other mucosal-local anesthetics:

—Problems in humans have not been documented.


Pediatrics


Benzocaine:

—Benzocaine should be used with caution in infants and young children because increased absorption may result in methemoglobinemia. Nonprescription teething products (i.e., 7.5% or 10% benzocaine gel) should not be used in infants younger than 4 months of age unless prescribed by a physician or dentist. {04} {14} Other nonprescription products that contain benzocaine for relief of dental pain, perioral lesions, or sore throat (e.g., gel, lozenges, ointment, or topical solution and combinations containing benzocaine with menthol or phenol) should not be used in children younger than 2 years of age unless prescribed by a physician or dentist. {04} {09} {10}



Other mucosal-local anesthetics:

—Pediatric patients may be more susceptible to systemic toxicity with these medications. Nonprescription products that contain dyclonine or lidocaine for relief of sore throat or perioral lesions should not be used in children younger than 2 years of age unless prescribed by a physician or dentist. {17} {35} Dosage of other mucosal-local anesthetic formulations should be individualized, based on the child's age, weight, and physical condition. {06} {23} {24} {25} {28} {29} {31} {32} {34}



Geriatrics


Systemic toxicity may be more likely to occur in geriatric patients, who may require lower concentrations and/or lower total dosages of mucosal-local anesthetics, especially for endoscopic procedures.

Drug interactions and/or related problems
See also Laboratory value alterations.

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 only
Cholinesterase inhibitors    (metabolism of an ester-derivative local anesthetic may be inhibited, leading to increased risk of systemic toxicity, when it is administered to a patient receiving a cholinesterase inhibitor)


Sulfonamides    (metabolites of PABA-derivative local anesthetics may antagonize antibacterial activity of sulfonamides)


For lidocaine only
Antiarrhythmic agents, amide local anesthetic–derivative, other,{23}{25}{27}{29}{31} such as:
Mexiletine
Tocainide or
Lidocaine, systemic or parenteral-local{30}    (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 when lidocaine is applied to the mucosa, especially if it is applied in large quantities, used repeatedly, used in the oral or pharyngeal area, or swallowed)


Beta-adrenergic blocking agents    (concurrent use may slow metabolism of lidocaine because of decreased hepatic blood flow, leading to increased risk of lidocaine toxicity, especially if lidocaine is applied to the mucosa in large quantities, used repeatedly, used in the oral or pharyngeal area, or swallowed)


Cimetidine    (cimetidine may inhibit hepatic metabolism of lidocaine, leading to increased risk of lidocaine toxicity, especially if lidocaine is applied to the mucosa in large quantities, used repeatedly, used in the oral or pharyngeal area, or swallowed)



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
Cystoscopic procedures following pyelography    (dyclonine interferes with visualization by reacting with iodine-containing contrast agents, resulting in precipitation of iodine)


Pancreatic function determination using bentiromide    (administration of PABA-derivative anesthetics or lidocaine prior to the bentiromide test will invalidate test results [if the anesthetics are absorbed in sufficient quantity] since they are also metabolized to arylamines and will thus increase the apparent quantity of PABA recovered; discontinuation of these medications at least 3 days prior to the test is recommended)


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
Hemorrhoids, bleeding—for rectal use
Local infection at area of treatment    (may alter pH at site of application, leading to decrease or loss of local anesthetic effect)


Sensitivity to the local anesthetic being considered for use and/or chemically related anesthetics or other compounds, history of
Traumatized mucosa, severe    (increased absorption of anesthetic, leading to increased risk of systemic toxicity)


Caution is also advised in pediatric, geriatric, acutely ill, or debilitated patients, who may be more susceptible to systemic toxicity with these medications.


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 mucosal-local anesthetics. Also, tetracaine is more toxic than other mucosal-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
    
Allergic contact dermatitis (skin rash, redness, itching, or hives)
    
angioedema (large, hive-like swellings on skin or in mouth or throat)
    
burning, stinging, swelling, or tenderness not present before therapy{06}{11}{23}{24}{25}{26}{27}{28}{29}{31}{32}{33}{34}

Incidence rare
    
Urethritis (blood in urine, increased frequency of urination, pain or burning during urination)—with urethral application





Overdose
For specific information on the agents used in the management of an overdose, see:    • Ascorbic Acid (Systemic) monograph;
   • Benzodiazepines (Systemic) monograph;
   • Methylene Blue (Systemic) monograph; and/or
   • Sympathomimetic Agents—Cardiovascular Use (Parenteral-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 (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:
Acute and chronic effects
    
Cardiovascular system depression (increased sweating, low blood pressure, pale skin, slow or irregular heartbeat)—may lead to cardiac arrest{06}{11}{23}{24}{25}{26}{27}{28}{29}{31}{32}{33}{34}
    
CNS toxicity (blurred or double vision; confusion; convulsions; dizziness or lightheadedness; drowsiness; feeling hot, cold, or numb; ringing or buzzing in ears; shivering or trembling; unusual anxiety, excitement, nervousness, or restlessness){06}{11}{23}{24}{25}{26}{27}{28}{29}{31}{32}{33}{34}
    
methemoglobinemia (difficulty in breathing on exertion, dizziness, headache, tiredness, weakness){49}

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. {06} {11} {23} {24} {25} {26} {27} {28} {29} {31} {32} {33} {34}



Treatment of overdose


Specific treatment:
For circulatory depression—Administering a vasopressor and intravenous fluids. {39}

For convulsions—Administering a benzodiazepine anticonvulsant, keeping in mind that intravenously administered benzodiazepines may cause respiratory {42} and circulatory {38} depression, especially when administered rapidly. {41} {43} Medications and equipment needed for support of respiration and for resuscitation must be immediately available. {44}

For methemoglobinemia—Administering methylene blue (1 to 2 mg per kg of body weight, intravenously) and/or ascorbic acid (100 to 200 mg orally). {38}



Supportive care:
Securing and maintaining a patent airway, administering 100% oxygen, and instituting assisted or controlled respiration as required. In some patients, endotracheal intubation may be required. {39}



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

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

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





Use in children—Caution recommended, especially with use of benzocaine or lidocaine in infants and young children






Use in the elderly—Increased risk of side effects

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

Following manufacturer's instructions if self-medicating

» Not using more, more often, or for a longer period of time than prescribed by physician or dentist or recommended on package label

» Checking with physician or dentist before using for problems other than those for which medication was prescribed or those stated on package label

Proper administration technique

For lidocaine hydrochloride oral topical solution {33} {34}
» Measuring dose accurately

Applying with cotton swab or swishing around in mouth (for mouth or gum conditions) or gargling (for throat conditions)

» Not swallowing unless specifically directed by physician or dentist

For benzocaine film-forming gel {16}
Drying affected area with one of the swabs provided before applying

Applying gel to a second swab, then rolling the swab over the affected area

Keeping mouth open and dry for 30 to 60 seconds after applying, while film forms

Not removing film, which will slowly disintegrate over 6 hours

For other nonprescription gel and solution dosage forms {35}
Applying to affected area(s) with a clean finger, a cotton-tipped applicator, or gauze

If using for pain caused by dental appliances, applying to sore area and, after relief is obtained, rinsing mouth before reinserting appliance; not applying directly to or using under appliance unless directed to do so by dentist

For benzocaine dental paste
Dabbing small amounts onto affected areas with cotton-tipped applicator; not rubbing or spreading, to prevent crumbling or grittiness

For topical aerosol or spray dosage forms
Using care not to inhale medication

Avoiding spraying back of throat or mouth unless specifically directed by physician or dentist

For lozenges
Dissolving slowly in mouth; not biting or chewing lozenges or swallowing them whole

For rectal cream or ointment
Reading patient directions

If applying externally: Cleansing area with mild soap and water or a cleansing wipe, rinsing thoroughly, and drying gently before applying

If inserting into anal canal: Using special applicator provided; lubricating applicator with a small amount of cream or ointment before inserting; washing reusable applicator after each use; discarding pre-filled disposable applicator

For rectal aerosol foam
Reading patient directions before use

Not inserting container into rectum; shaking container, attaching and filling the applicator provided, then detaching applicator from container prior to use

Applying a small amount of foam to lubricate the applicator before inserting

Taking applicator apart and washing thoroughly after each use

» Proper dosing
Missed dose (if prescribed for scheduled dosing)—Using as soon as possible; not using if almost time for next dose; not doubling doses of dental-local anesthetics

» Proper storage

Precautions while using this medication
» Contacting physician:

• if using for sore throat and sore throat is severe, persists for more than 2 days, or is accompanied or followed by other symptoms such as fever, headache, rash, swelling, nausea, or vomiting {09} {10} {17}


• if using for hemorrhoids or other perianal conditions and condition does not improve within 7 days, bleeding occurs, or symptoms such as redness, irritation, swelling, or pain develop or worsen during treatment {03} {20}


» Contacting physician or dentist if using for perioral lesions and symptoms do not improve within 7 days, irritation or pain persists or worsens, or swelling, rash, or fever develops {04}

» Contacting dentist:

• as soon as possible to arrange an appointment if using to relieve toothache; medication is a temporary measure only


• at regular intervals when medication used to relieve pain during adjustment of new dentures or other dental appliances {19} {31}


Not using benzocaine, lidocaine, or tetracaine for 72 hours prior to having pancreatic function test using bentiromide because of potential interference with test results

For use in mouth or throat area
» Not eating for one hour following use of medication because may impair swallowing, leading to risk of aspiration

» Not chewing gum or food while numbness persists because of risk of biting tongue or buccal mucosa


Side/adverse effects
Signs and symptoms of potential side effects, especially allergic contact dermatitis; angioedema; and burning, stinging, swelling, or tenderness not present before therapy


General Dosing Information
The safety and effectiveness of local anesthetics, when they are used for examination or instrumentation procedures (especially those involving the esophagus, larynx, pharynx, respiratory tract, or urinary tract) depend upon proper dosage, correct administration technique, adequate precautions, and readiness for emergencies. Resuscitative equipment, oxygen, and other required medications should be immediately available.

The dosage of mucosal-local anesthetics, when they are used for examination or instrumentation procedures, depends on the technique of anesthesia, the area to be anesthetized, the vascularity of the tissues at the application site, and the patient's tolerance.

For use in examination or instrumentation procedures, the recommended adult doses are given as a guideline for use in the average adult. The actual dosage and maximum dosage must be individualized, based on the age, size, and physical status of the patient and the expected rate of systemic absorption from the administration site.

Depending on the area to be anesthetized, lower concentrations and/or lower total dosage may be required for pediatric, geriatric, acutely ill, or debilitated patients.

A standard textbook should be consulted for specific techniques and procedures applicable to the use of mucosal-local anesthetics for individual diagnostic and treatment procedures.

BENZOCAINE

Summary of Differences


Pharmacology/pharmacokinetics:


Physicochemical characteristics—
Benzocaine is a PABA derivative ester-type local anesthetic.



Absorption—
Minimally absorbed.




Precautions:


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



Pediatrics—
May cause methemoglobinemia in infants.



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

May antagonize antibacterial activity of sulfonamides.




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

See also Side/Adverse Effects.



Dental Dosage Forms

Note: The gel, ointment, and topical solution dosage forms included in this section are specifically formulated for application only to the gingival or buccal mucosa or to perioral tissues. Gel and topical solution formulations that may be applied to other mucosal tissues (in addition to the gingival or buccal mucosa) are included in the Topical Dosage Forms section.


BENZOCAINE GEL (DENTAL)

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, as a 10 or 20% gel, applied to affected area(s) up to four times a day or as directed by a physician or dentist. {04}

Note: The medication may be applied with cotton, a cotton swab, or a fingertip. {04}
The gel should not be applied directly to, or used beneath, a dental appliance {04} unless the patient is under the supervision of a dentist. {19} Patients using this medication without the supervision of a dentist for relief of dental appliance pain should apply the medication directly to the affected gum area, wait until relief is obtained, and rinse the mouth before reinserting the appliance. {04}


Usual pediatric dose
Anesthetic, mucosal-local


For teething pain:
Infants up to 4 months of age—Dosage must be individualized by a physician or dentist. {04} {14}

Infants and children 4 months to 2 years of age—Topical, as a 7.5 or 10% gel, applied to affected area(s) up to four times a day as needed or as directed by a physician or dentist. {04} {14}

Children 2 years of age and older—Topical, as a 7.5% or stronger gel, applied to affected area(s) up to four times a day or as directed by a physician or dentist. {04}



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



Note: Product may be applied with cotton, a cotton swab, or a fingertip. {04}


Strength(s) usually available
U.S.—


7.5% (OTC) [Anbesol, Baby{04}] [Num-Zit Gel] [Orabase, Baby{01}{07}] [Orajel, Baby{14}]


10% (OTC) [Numzident] [{07}Orajel] [Orajel Nighttime Formula, Baby] [{07}Rid-A-Pain{01}]


20% (OTC) [Anbesol Maximum Strength Gel (alcohol 60%){04}] [Orajel Maximum Strength{15}] [SensoGARD Canker Sore Relief]

Canada—


7.5% (OTC) [Anbesol Baby Jel{05}]


20% (OTC) [Orajel Extra Strength{05}] [Topicaine{19}]

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.


BENZOCAINE FILM-FORMING GEL

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, as a 15% gel, applied with a cotton swab to affected area(s) up to four times a day or as directed by a physician or dentist. The area should be dried with a cotton swab prior to application. {16}

Usual pediatric dose
Anesthetic, mucosal-local
Infants and children up to 2 years of age: Dosage must be individualized by a physician or dentist. {16}

Children 2 years of age and older: See Usual adult and adolescent dose . {16}


Note: To ensure that this medication is applied correctly, children up to 12 years of age should apply it under the supervision of an adult. {16}


Strength(s) usually available
U.S.—


15% (OTC) [Oratect Gel]{16}

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.


BENZOCAINE LOZENGES

Usual adult and adolescent dose
Anesthetic, mucosal-local—Oral, one 10-mg lozenge to be dissolved slowly in the mouth. May be repeated at two-hour intervals as needed.

Usual pediatric dose
Anesthetic, mucosal-local
Children up to 2 years of age: Dosage must be individualized by a physician. {10}

Children 2 years of age and older: Oral, one 5-mg lozenge to be dissolved slowly in the mouth. May be repeated at two-hour intervals, if needed. {10}


Usual pediatric prescribing limits
Not to exceed twelve 5-mg lozenges per day.

Strength(s) usually available
U.S.—


5 mg (OTC) [Chloraseptic Lozenges, Children's{10}]


10 mg (OTC) [Spec-T Sore Throat Anesthetic{01}]

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


BENZOCAINE OINTMENT (DENTAL) USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied to cleaned and dried dentures up to four times a day.

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


20% (OTC) [Benzodent] [Dentapaine]{01}{07}

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


BENZOCAINE DENTAL PASTE

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied to the affected area as needed.

Usual pediatric dose
Anesthetic, mucosal-local
Children up to 6 years of age: Dosage must be individualized by physician or dentist.

Children 6 years of age and older: See Usual adult and adolescent dose.


Strength(s) usually available
U.S.—


20% (OTC) [Orabase-B with Benzocaine]{01}{07}

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.


BENZOCAINE TOPICAL SOLUTION (DENTAL) USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, as a 20% solution, applied to affected area(s) up to four times a day or as directed by a physician or dentist. {04}

Note: The medication may be applied with cotton, a cotton swab, or a fingertip.


Usual pediatric dose
Anesthetic, mucosal-local
Infants and children up to 2 years of age: Dosage must be individualized by a physician or dentist. {04}

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


Strength(s) usually available
U.S.—


0.2% (OTC) [Num-Zit Lotion (alcohol 12.6%)]{48}


5% (OTC) [Dent-Zel-Ite (alcohol 81%)]{07}


20% (OTC) [Anbesol Maximum Strength Liquid (alcohol 60%)]{04}

Note: In Canada, Anbesol Maximum Strength Liquid also contains 0.45% of phenol. See Benzocaine and Phenol Topical Solution .


Canada—


6.5% (OTC) [Dentocaine]{05}{07}


7.5% (OTC) [Orajel, Baby]{05}


20% (OTC) [Orajel Liquid]{05}

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


BENZOCAINE AND MENTHOL LOZENGES

Usual adult and adolescent dose
Anesthetic, mucosal-local—Oral, one lozenge dissolved slowly in the mouth every two hours as needed or as directed by a physician or dentist. {09}

Usual pediatric dose
Anesthetic, mucosal-local
Children up to 2 years of age: Dosage must be individualized by a physician or dentist. {09}

Children 2 years of age and older: See Usual adult and adolescent dose . {09}


Strength(s) usually available
U.S.—


6 mg of benzocaine and 10 mg of menthol (OTC) [Chloraseptic Lozenges]{09}

Canada—


6 mg of benzocaine and 10 mg of menthol (OTC) [Chloraseptic Lozenges Cherry Flavor]{47}

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


BENZOCAINE AND PHENOL GEL

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied to affected area(s) up to four times a day or as directed by a physician or dentist. {04}

Note: The medication may be applied with cotton, a cotton swab, or a fingertip.
The gel should not be applied directly to, or used beneath, a dental appliance {04} unless the patient is under the supervision of a dentist. Patients using this medication without the supervision of a dentist for relief of dental appliance pain should apply the medication directly to the affected gum area, wait until relief is obtained, and rinse the mouth before reinserting the appliance. {04}


Usual pediatric dose
Anesthetic, mucosal-local
Infants and children up to 2 years of age: Dosage must be individualized by a physician or dentist. {04}

Children 2 years of age and older: See Usual adult and adolescent dose . {04}


Strength(s) usually available
U.S.—


6.3% of benzocaine and 0.5% of phenol (OTC) [Anbesol Regular Strength Gel (alcohol 70%)]{04}

Canada—


6.4% of benzocaine and 0.5% of phenol (OTC) [Anbesol Gel ( alcohol)]{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.


BENZOCAINE AND PHENOL TOPICAL SOLUTION

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied to affected area(s) up to four times a day or as directed by a physician or dentist. {04}

Note: The medication may be applied with cotton, a cotton swab, or a fingertip.


Usual pediatric dose
Anesthetic, mucosal-local
Infants and children up to 2 years of age: Dosage must be individualized by a physician or dentist. {04}

Children 2 years of age and older: See Usual adult and adolescent dose . {04}


Strength(s) usually available
U.S.—


6.3% of benzocaine and 0.5% of phenol (OTC) [Anbesol Regular Strength Liquid (alcohol 70%)]{04}

Canada—


6.5% of benzocaine and 0.45% of phenol (OTC) [Anbesol Liquid ( alcohol)]{47}


20% of benzocaine and 0.45% of phenol (OTC) [Anbesol Maximum Strength Liquid (alcohol)]{47}

Note: In the U.S., Anbesol Maximum Strength Liquid does not contain phenol. See Benzocaine Topical Solution USP (Dental) .


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.



Rectal Dosage Forms

BENZOCAINE OINTMENT (RECTAL) USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied to the perianal area up to six times a day after the area has been cleansed and dried. Medication should not be inserted into the rectum. {03}

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


20% (OTC) [Americaine Hemorrhoidal]{03}

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



Topical Dosage Forms

BENZOCAINE GEL

Usual adult and adolescent dose
Anesthetic, mucosal-local
Dental procedures: Topical, as a 20% gel, applied to area with a cotton applicator as needed.

Other examination or instrumentation procedures: Topical, as a 20% gel, applied to area with a cotton applicator, or to instrument prior to insertion.


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


20% (OTC) [Americaine Anesthetic Lubricant{02}] [Hurricaine{12}]

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.


BENZOCAINE TOPICAL AEROSOL USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, as a 20% solution, sprayed on area for one second. May be repeated if necessary.

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


20% (OTC) [Americaine{01}] [Hurricaine{12}]

Packaging and storage:
Store below 40 °C (104 °F), unless otherwise specified by manufacturer.


BENZOCAINE TOPICAL SOLUTION USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, as a 20% solution, applied to area with a cotton applicator as needed.

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


20% (OTC) [Hurricaine]{12}

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


BENZOCAINE, BUTAMBEN, AND TETRACAINE

Summary of Differences


Pharmacology/pharmacokinetics:


Physicochemical characteristics—
Benzocaine, butamben, and tetracaine are all PABA-derivative ester-type local anesthetics.




Precautions:


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



Drug interactions and/or related problems—
Cholinesterase inhibitors inhibit metabolism of these local anesthetics.

May antagonize antibacterial activity of sulfonamides.




Side/adverse effects:
Benzocaine and tetracaine are more likely to cause contact sensitization than other local anesthetics.

Tetracaine is more toxic than other mucosal-local anesthetics.

See also Side/Adverse Effects.



Additional Dosing Information
See also General Dosing Information.

In dentistry, this medication should not be used under dentures or cotton rolls, because retention under these materials may result in sloughing of tissue.


Topical Dosage Forms

BENZOCAINE, BUTAMBEN, AND TETRACAINE HYDROCHLORIDE GEL USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied directly to desired area, or to instrument prior to insertion.

Usual adult prescribing limits
For the tetracaine component—20 mg. {08}

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


14% of benzocaine, 2% of butamben, and 2% of tetracaine hydrochloride (Rx) [Cetacaine Topical Anesthetic]{08}

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.


BENZOCAINE, BUTAMBEN, AND TETRACAINE HYDROCHLORIDE OINTMENT USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied with a cotton pledget or directly to tissue.

Note: Cotton pledget should not be held in position for extended periods of time, because of increased risk of local reactions to the anesthetics.


Usual adult prescribing limits
For the tetracaine component—20 mg. {08}

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


14% of benzocaine, 2% of butamben, and 2% of tetracaine hydrochloride (Rx) [Cetacaine Topical Anesthetic]{08}

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.


BENZOCAINE, BUTAMBEN, AND TETRACAINE HYDROCHLORIDE TOPICAL AEROSOL USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, sprayed on desired area for approximately one second or less.

Usual adult prescribing limits
Duration of spray should not exceed two seconds.

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


14% of benzocaine, 2% of butamben, and 2% of tetracaine hydrochloride (Rx) [Cetacaine Topical Anesthetic]{08}

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.


BENZOCAINE, BUTAMBEN, AND TETRACAINE HYDROCHLORIDE TOPICAL SOLUTION USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, applied with a cotton pledget or directly to tissue.

Note: Cotton pledget should not be held in position for extended periods of time, because of increased risk of local reactions to the anesthetics.


Usual adult prescribing limits
For the tetracaine component—20 mg. {08}

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


14% of benzocaine, 2% of butamben, and 2% of tetracaine hydrochloride (Rx) [Cetacaine Topical Anesthetic]{08}

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.


DIBUCAINE

Summary of Differences


Indications:
Indicated for treatment of hemorrhoids and other anorectal disorders.



Pharmacology/pharmacokinetics:


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 pancreatic function test using bentiromide.



Rectal Dosage Forms

DIBUCAINE OINTMENT USP

Usual adult and adolescent dose
Anesthetic, mucosal-local
Rectal, a comfortable quantity, inserted three or four times a day, in the morning, in the evening, and after bowel movements; and/or

Topical, to the perianal area three or four times a day, in the morning, in the evening, and after bowel movements. {13}


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


1% (OTC) [Nupercainal (acetone sodium bisulfite)][Generic]{13}

Canada—


1% (OTC) [Nupercainal (bisulfite)]{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. Store in a collapsible tube or in a tight, light-resistant container. Protect from freezing.


DYCLONINE

Summary of Differences


Pharmacology/pharmacokinetics:


Physicochemical characteristics—
Dyclonine is neither an ester-type nor an amide-type local anesthetic.




Precautions:


Cross-sensitivity and/or related problems—
Does not occur with either ester-type or amide-type local anesthetics.



Laboratory value alterations—
May cause precipitation of iodine from contrast agents used in cystoscopic procedures following pyelography.

No interference with pancreatic function test using bentiromide.




Dental Dosage Forms

DYCLONINE HYDROCHLORIDE LOZENGES

Usual adult and adolescent dose
Anesthetic, mucosal-local—Oral, one 2-mg or 3-mg lozenge to be dissolved slowly in the mouth. May be repeated at two-hour intervals, if needed. {17}

Usual pediatric dose
Anesthetic, mucosal-local
Children up to 2 years of age: Dosage has not been established. {17}

Children 2 years of age and older: Oral, one 1.2-mg lozenge to be dissolved slowly in the mouth. May be repeated at two-hour intervals, if needed. {17}


Strength(s) usually available
U.S.—


1.2 mg (OTC) [Sucrets, Children's]


2 mg (OTC) [Sucrets Regular Strength]


3 mg (OTC) [Sucrets Maximum Strength]{17}

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



Topical Dosage Forms

DYCLONINE HYDROCHLORIDE TOPICAL SOLUTION USP

Usual adult and adolescent dose
Anesthetic, mucosal-local
Topical, 40 to 200 mg as a 0.5 or 1% solution; specifically: —
For anogenital pain
Topical, as a 0.5% solution, applied with sponges or cotton pledgets. {11}

For dental procedures
Topical, as a 0.5% solution, used as a mouthwash or gargle and the excess expelled. {11}

For otorhinolaryngologic examinations
Topical, as a 0.5% solution, used as a spray or gargle. {11}

For perioral lesion pain
Topical, to the affected area(s), as a 0.5% solution, used as a rinse or swab. {11}

For vaginal pain
Topical, a 0.5 or 1% solution, applied as a wet compress or spray. {11}

For esophageal lesion pain
Oral, 25 to 150 mg (5 to 15 mL of a 0.5 or 1% solution).



Usual adult prescribing limits
Up to 300 mg (30 mL of a 1% solution) per examination, although this dose is rarely required. Adequate anesthesia is usually achieved with smaller quantities.

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


0.5% (Rx) [Dyclone]{11}


1% (Rx) [Dyclone]{11}

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, light-resistant container. Protect from freezing.


LIDOCAINE
{22}{23}{24}{25}{26}{27}{28}{29}{30}{31}
Summary of Differences


Pharmacology/pharmacokinetics:
Physicochemical characteristics—Lidocaine is an amide-type local anesthetic.

Protein binding—Concentration-dependent; 60 to 80% at nontoxic plasma concentrations.



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

Breast-feeding—Distributed into breast milk in very small quantities.

Drug interactions and/or related problems—Also interacts with beta-adrenergic blocking agents, cimetidine, and amide local anesthetic–derivative antiarrhythmic agents.



Dental Dosage Forms

Note: The topical solution formulations included in this section are specifically formulated for application only to gingival or buccal mucosa or to perioral tissues. Topical solution formulations that are applied to other mucosal tissues (in addition to the gingival or buccal mucosa) are included in the Topical Dosage Forms section.


LIDOCAINE TOPICAL AEROSOL USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, to gingival and oral mucous membranes, 20 mg (two metered sprays) per quadrant of gingiva and oral mucosa. {26}

Usual adult prescribing limits
Not to exceed 30 mg of lidocaine (three metered sprays) per quadrant of gingiva and oral mucosa over a one-half-hour period {26} or 200 mg (twenty metered sprays) in twenty-four hours. {27}

Usual pediatric dose
Anesthetic, mucosal-local—Topical, to gingival and oral mucous membranes, up to a total of 3 mg per kg of body weight. {27}

Strength(s) usually available
U.S.—


10% (10 mg per metered spray) (Rx) [Xylocaine]{26}

Canada—


10% (10 mg per metered spray) (OTC) [Xylocaine]{27}

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.


LIDOCAINE ORAL TOPICAL SOLUTION USP

Usual adult and adolescent dose
Anesthesia, mucosal-local
Dental procedures: Topical, 50 to 200 mg as a 5% solution, applied to the oral mucosa with a cotton applicator. {25}

Perioral lesions: Topical, as a 2.5% solution, applied to affected area(s) with a cotton swab every one or two hours for the first three days, then as needed. {35}


Usual adult prescribing limits
Dental procedures—Not to exceed a total of 250 mg (5 mL of a 5% solution) for all quadrants in a three-hour period. {24}

Usual pediatric dose
Anesthesia, mucosal-local—Dental procedures: Topical, the dosage being individualized, based on the child's age, weight, and physical condition {24} up to a maximum of 4.5 mg per kg of body weight as 5% solution. {24} {25}

Strength(s) usually available
U.S.—


2.5% (OTC) [Zilactin-L{35}]


5% (Rx) [Xylocaine{24}][Generic]

Canada—


5% (OTC) [Xylocaine{25}]

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.



Topical Dosage Forms

LIDOCAINE OINTMENT USP

Usual adult and adolescent dose
Anesthetic, mucosal-local


Oral mucosa:
Topical, as a 5% ointment, to previously dried oral mucosa.

For use during fitting of new dentures—Apply to all denture surfaces that contact the mucosa, up to a maximum of 5 grams of ointment (250 mg of lidocaine) per single dose or 20 grams of ointment (1000 mg of lidocaine) per day. {30}

Note: The patient should be advised to consult the prescribing dentist at intervals not exceeding 48 hours throughout the fitting period. {30}




Oropharynx:
Topical, as a 5% ointment, applied to desired area, or to instrument prior to insertion.



Usual pediatric dose
Anesthetic, mucosal-local—Topical, the dosage being individualized, based on the child's age, weight, and physical condition, up to a maximum of 4.5 mg per kg of body weight or 2.5 grams of ointment in a six-hour period. {31}

Strength(s) usually available
U.S.—


5% (Rx) [Xylocaine][Generic]{30}

Canada—


5% (OTC) [Xylocaine Dental Ointment]{31}

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.


LIDOCAINE HYDROCHLORIDE JELLY USP

Usual adult and adolescent dose
Anesthetic, mucosal-local


Esophagus, larynx, trachea:
Topical, as a 2% jelly, applied to the outer surface of the instrument prior to insertion.

Note: Care should be taken to avoid depositing any of the medication on the inner surface of an endoscope or other instrument. It may dry on the inner surface and leave a residue that may cause narrowing or, rarely, occlusion of the lumen. {06} {28} {29}




Urinary tract:


Female—
Urethral, 3 to 5 mL, as a 2% jelly, several minutes prior to examination. {06} {28}

Note: Jelly may be deposited on a cotton swab and introduced into urethra. {06} {28}




Male {06} {28} {29}
Prior to catheterization: Urethral, 100 to 200 mg (5 to 10 mL) as a 2% jelly.

Prior to sounding or cystoscopy: Urethral, 600 mg (30 mL) to fill and dilate urethra. The medication is usually administered in two divided doses, with a penile clamp applied for several minutes between doses.




Usual adult prescribing limits
Not more than 600 mg (30 mL) in a twelve-hour period. {06} {28} {29}

Usual pediatric dose
Anesthetic, mucosal-local—Topical, as a 2% jelly, dosage to be individualized, based on the child's age, weight, and physical condition, up to a maximum of 4.5 mg per kg of body weight. {06} {28} {29}

Strength(s) usually available
U.S.—


2% (Rx) [Anestacon Jelly{06}] [Xylocaine{28}][Generic]

Canada—


2% (OTC) [Xylocaine]{29}

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.


LIDOCAINE HYDROCHLORIDE ORAL TOPICAL SOLUTION USP

Note: Previous name—Lidocaine Hydrochloride Viscous Solution.


Usual adult and adolescent dose
Anesthetic, mucosal-local
Oral cavity disorders: Topical, 300 mg (15 mL) swished around in the mouth, then expelled, or applied with a cotton-tipped applicator, every three hours as needed. {33} {34}

Pharyngeal pain: Topical, 300 mg (15 mL) used as a gargle every three hours as needed. May be swallowed if necessary. {33} {34}


Usual adult prescribing limits
Single dose—Not to exceed 4.5 mg per kg of body weight or 300 mg (15 mL). This dose should not be repeated more often than every three hours. {33} {34}

Multiple doses—Not to exceed 8 doses (2.4 grams or 120 mL) in twenty-four hours.

Usual pediatric dose
Anesthetic, mucosal-local


Infants and children up to 3 years of age:
Topical, up to 1.25 mL of a 2% solution, applied to affected area(s) with a cotton-tipped applicator every three hours. {33} {34}

Note: It is recommended that the dosage be accurately measured and applied to the immediate area or specific lesion with a cotton-tipped applicator. The risk of systemic toxicity, especially convulsions, is increased if dosage is not carefully controlled and/or if the patient swallows significant quantities of the medication.




Children 3 years of age and older:
Topical, the dosage being individualized, based on the child's age, weight, and physical condition, {33} up to a maximum of 4.5 mg per kg of body weight as 2% solution in a three-hour period. {34}



Strength(s) usually available
U.S.—


2% (Rx) [Xylocaine Viscous][Generic]{33}

Canada—


2% (OTC) [Xylocaine Viscous]{34}

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.


LIDOCAINE HYDROCHLORIDE TOPICAL SOLUTION USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Oral or nasal cavity or esophagus: Topical, as a 4% solution, 600 mcg (0.6 mg) to 3 mg per kg of body weight; or 40 to 200 mg (1 to 5 mL). {23}

Note: May be applied as a spray, with cotton applicators or packs, or instilled directly into cavity. {23}


Usual adult prescribing limits
For use in oral or nasal cavities or upper gastrointestinal tract—Not to exceed 4.5 mg per kg of body weight or 300 mg (7.5 mL of a 4% solution). {23}

Usual pediatric dose
Dosage must be individualized by physician.

Strength(s) usually available
U.S.—


4% (Rx) [Xylocaine][Generic]{22}

Canada—


4% (OTC) [Xylocaine]{23}

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.


LIDOCAINE HYDROCHLORIDE TOPICAL SPRAY SOLUTION

Note: The dosing and strength of this dosage form are expressed in terms of lidocaine base.


Usual adult and adolescent dose
Anesthetic, mucosal-local—Endoscopic procedures: Topical, up to 20 metered sprays (200 mg [base]) as a 10% (base) solution, sprayed onto the oropharyngeal or tracheal mucosa. {32}

Usual pediatric dose
Anesthetic, mucosal-local


Infants and children up to 3 years of age:
Use is not recommended; a less concentrated solution should be used instead. {32}



Children 3 to 12 years of age:
Larynx or trachea—Topical, up to 1.5 mg (base) per kg of body weight. {32}

Other mucosa—Topical, up to 3 mg (base) per kg of body weight. {32}



Strength(s) usually available
U.S.—
Not commercially available.

Canada—


10% (base; 12 mg of lidocaine hydrochloride equivalent to 10 mg of lidocaine base per metered spray) (OTC) [Xylocaine Endotracheal{32}]

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.


PRAMOXINE

Summary of Differences


Indications:
Indicated for the treatment of hemorrhoids and other anorectal disorders.



Pharmacology/pharmacokinetics:


Physicochemical characteristics—
Pramoxine is neither an amide-type nor an ester-type local anesthetic.




Precautions:
Cross-sensitivity and/or related problems—Does not occur with either ester-type or amide-type local anesthetics.

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



Rectal Dosage Forms

PRAMOXINE HYDROCHLORIDE AEROSOL FOAM

Usual adult and adolescent dose
Anesthetic, mucosal-local
Rectal, one applicatorful two to three times a day; or

Topical, to the external anorectal area two to three times a day.


Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


1% (OTC) [ProctoFoam/non-steroid{46} (propylparaben )]{07}

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 anorectal use only. {04}


PRAMOXINE HYDROCHLORIDE CREAM USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Topical, to the anorectal area, up to five times a day, after the area has been cleansed and dried. {20}

Usual pediatric dose
Children up to 12 years of age—Dosage must be individualized by physician. {20} {21}

Strength(s) usually available
U.S.—


1% (OTC) [Tronolane{20}] [Tronothane]

Canada—


1% (OTC) [Tronothane]{21}{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. Store in tight container. Protect from freezing.


PRAMOXINE HYDROCHLORIDE OINTMENT

Usual adult and adolescent dose
Anesthetic, mucosal-local
Rectal, introduced into the rectum as a 1% ointment up to five times per day, in the morning, at night, and after bowel movements; or

Topical, to the anorectal area as a 1% ointment up to five times a day.


Usual pediatric dose
Children up to 12 years of age—Dosage must be individualized by physician.

Strength(s) usually available
U.S.—


1% (OTC) [Fleet Relief]{01}

Note: Available in tubes and in pre-filled 4-mL disposable applicators.


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.


TETRACAINE

Summary of Differences


Pharmacology/pharmacokinetics:


Physicochemical characteristics—
Tetracaine is a PABA-derivative ester-type local anesthetic.




Precautions:


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



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

May antagonize antibacterial activity of sulfonamides.




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

More toxic than other mucosal-local anesthetics.

See also Side/Adverse Effects.



Rectal Dosage Forms

TETRACAINE HYDROCHLORIDE CREAM USP

Note: The dosing and strength of this dosage form are expressed in terms of tetracaine base.


Usual adult and adolescent dose
Anesthetic, mucosal-local—Rectal, introduced into rectum as a 1% (base) cream up to six times a day. {45}

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

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


1% (base) (OTC) [Pontocaine Cream{01}]

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.


TETRACAINE AND MENTHOL OINTMENT USP

Usual adult and adolescent dose
Anesthetic, mucosal-local
Rectal, introduced into rectum as a 0.5% ointment up to six times a day. {45}

Topical, applied as a 0.5% ointment spread with gauze or cotton, to anorectal area up to six times a day. {45}


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

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


0.5% of tetracaine and 0.5% of menthol (OTC) [Pontocaine Ointment{01}]

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.



Topical Dosage Forms

TETRACAINE HYDROCHLORIDE TOPICAL SOLUTION USP

Usual adult and adolescent dose
Anesthetic, mucosal-local—Larynx, trachea, or esophagus
Topical, as a 0.25 or 0.5% solution prior to procedure; or

Oral inhalation, as a nebulized 0.5% solution.


Note: 0.06 mL of 0.1% (1:1000) epinephrine may be added to each mL of tetracaine solution, to reduce absorption.


Usual adult prescribing limits
Not to exceed 20 mg.

Usual pediatric dose
Dosage has not been established.

Strength(s) usually available
U.S.—


2% (Rx) [Pontocaine]{01}

Canada—
Not commercially available.

Packaging and storage:
Store between 2 and 8 °C (36 and 46 °F), unless otherwise specified by manufacturer. Store in a tight, light-resistant container. Protect from freezing.

Stability:
Do not use if solution is cloudy or discolored or contains crystals.



Revised: 06/13/2000



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. Red book 1993. Montvale, NJ: Medical Economics Data, 1993: 90, 128, 197, 250, 407, 416, 450, 487, 521, 573, 576.
  1. Americaine Anesthetic Lubricant (Fisons), Rev 6/92. In: PDR Physicians' desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 926.
  1. Americaine Hemorrhoidal (Fisons Consumer). In: PDR Physicians' desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 562.
  1. Anbesol Formulations (Whitehall). In: PDR Physicians' desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 775.
  1. Krogh CME, editor. Self-Medication Product Information. 4th ed Volume 2. Ottawa: Canadian Pharmaceutical Association, 1992: T54, T103.
  1. Anestacon Jelly (Webcon). In: PDR Physicians' desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 2486.
  1. Covington TR, editor. Handbook of nonprescription drugs. 10th ed. Washington, DC: American Pharmaceutical Association, 1993: 817, 818, 826.
  1. Cetacaine formulations (Cetylite). In: PDR Physicians" desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 804.
  1. Chloraseptic Lozenges, Children's (Procter & Gamble). In: PDR Physicians" desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 643.
  1. Chloraseptic Lozenges (Procter & Gamble). In: PDR Physicians" desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 644.
  1. Dyclone (Astra), Rev 8/89. In: PDR Physicians" desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 543-4.
  1. Hurricaine formulations (Beutlich). In: PDR Physicians" desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 607.
  1. Nupercainal Ointment (Ciba), Rev 8/86. In: PDR Physicians" desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 832.
  1. Orajel, Baby (Del). In: PDR Physicians" desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 558-9.
  1. Orajel Maximum Strength (Del). In: PDR Physicians" desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 559.
  1. Oratect Gel (MGI Pharma). In: PDR Physicians" desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 1274.
  1. Sucrets formulations (SmithKline Beecham Consumer). In: PDR Physicians" desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 733.
  1. Not used.
  1. Topicaine (Hoechst). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 1241.
  1. Tronolane (Ross). In: PDR Physicians" desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 686.
  1. Tronothane (Abbott). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 1269.
  1. Xylocaine 4% Topical Solution (Astra), Rev 7/84. In: PDR Physicians" desk reference. 48th ed. 1994. Montvale, NJ: Medical Economics Data Production Company, 1994: 565.
  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% Liquid package insert (Astra—US), Rev 9/84, Rec 5/93.
  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. Xylocaine 10% Oral Spray package insert (Astra—US), Rev 11/93, Rec 2/94.
  1. Xylocaine 10% Oral Aerosol product monograph (Astra—Canada), Rev 12/93, Rec 1/94.
  1. Xylocaine Jelly package insert (Astra—US), Rev 6/86, Rec 5/93.
  1. Xylocaine Jelly (Astra). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 1377-8.
  1. Xylocaine 5% Ointment (Astra—US), Rev 1/94, Rec 5/94.
  1. Xylocaine 5% Ointment and 5% Dental Ointment (Astra). In: CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 1378-9.
  1. Xylocaine Endotracheal product monograph (Astra—Canada), Rev 12/93, Rec 1/94.
  1. Xylocaine 2% Viscous Solution package insert (Astra—US), Rev 7/92, Rec 11/93.
  1. Xylocaine 2% Viscous Solution (Astra). In: Krogh CME, editor. CPS Compendium of pharmaceuticals and specialties. 28th ed. Ottawa: Canadian Pharmaceutical Association, 1993: 1385-6.
  1. Zilactin-L(Zila). In: PDR Physicians" desk reference for nonprescription drugs. 14th ed. 1993. Montvale, NJ: Medical Economics Data Production Co, 1993: 789.
  1. Fleeger CA, editor. USAN 1994. USAN and the USP dictionary of drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1994: 79, 104, 207, 236, 378, 540, 653.
  1. Federal Register 1988; 53: 30758-62.
  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 monograph draft, 1984.
  1. Reviewers" consensus on Benzodiazepines (Systemic) monograph.
  1. Panel comment, Lidocaine and Prilocaine (Topical) ballot 6/93.
  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. Federal Register 1990; 55: 31780.
  1. Product information ProctoFoam/non-steroid (Reed & Carnrick—US) (undated), Rec 7/83.
  1. Krogh CME, editor. Self-Medication Product Information. 4th ed Volume 2. Ottawa: Canadian Pharmaceutical Association, 1993: 15, 43.
  1. Manufacturer comment (Goody's—US), 6/94.
  1. Panel comment, 6/94.
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