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Xylocaine Topical Solution

Pronunciation

Generic Name: lidocaine hydrochloride
Dosage Form: topical solution

Xylocaine

Topical Solution

Rx only

Xylocaine Topical Solution Description

4% Xylocaine (lidocaine HCl) Topical Solution contains a local anesthetic agent and is administered topically.  See INDICATIONS for specific uses.

4% Xylocaine Topical Solution contains lidocaine HCl, which is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl)-, monohydrochloride and has the following structural formula:

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The 50 mL screw-cap bottle should not be autoclaved, because the closure employed cannot withstand autoclaving temperatures and pressures.  Composition of 4% Xylocaine (lidocaine HCl) Topical Solution:  Each mL contains lidocaine HCl, 40 mg, methylparaben, and sodium hydroxide and/or hydrochloric acid to adjust pH to 6.0–7.0.

An aqueous solution.  NOT FOR INJECTION.

Xylocaine Topical Solution - Clinical Pharmacology

Mechanism of Action

Lidocaine HCl stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

Hemodynamics

Excessive blood levels may cause changes in cardiac output, total peripheral resistance, and mean arterial pressure.  These changes may be attributable to a direct depressant effect of the local anesthetic agent on various components of the cardiovascular system.

Pharmacokinetics and Metabolism

Lidocaine HCl may be absorbed following topical administration to mucous membranes, its rate of absorption and percent of dose absorbed depending upon concentration and total dose administered, the specific site of application and duration of exposure.  In general, the rate of absorption of local anesthetic agents following topical application occurs most rapidly after intratracheal administration. Lidocaine HCl is well-absorbed from the gastrointestinal tract, but little intact drug appears in the circulation because of biotransformation in the liver.

Lidocaine HCl is metabolized rapidly by the liver, and metabolites and unchanged drug are excreted by the kidney. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. N-dealkylation, a major pathway of biotransformation, yields the metabolites monoethylglycinexylidide and glycinexylidide.  The pharmacological/toxicological actions of these metabolites are similar to, but less potent than, those of lidocaine HCl.  Approximately 90% of lidocaine HCl administered is excreted in the form of various metabolites, and less than 10% is excreted unchanged.  The primary metabolite in urine is a conjugate of 4-hydroxy-2,6-dimethylaniline.

The plasma binding of lidocaine HCl is dependent on drug concentration, and the fraction bound decreases with increasing concentration.  At concentrations of 1 to 4 mcg of free base per mL, 60 to 80 percent of lidocaine HCl is protein bound. Binding is also dependent on the plasma concentration of the alpha-1-acid glycoprotein.

Lidocaine HCl crosses the blood-brain and placental barriers, presumably by passive diffusion.

Studies of lidocaine HCl metabolism following intravenous bolus injections have shown that the elimination half-life of this agent is typically 1.5 to 2 hours. Because of the rapid rate at which lidocaine HCl is metabolized, any condition that affects liver function may alter lidocaine HCl kinetics.  The half-life may be prolonged two-fold or more in patients with liver dysfunction.  Renal dysfunction does not affect lidocaine HCl kinetics but may increase the accumulation of metabolites.

Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of lidocaine HCl required to produce overt systemic effects. Objective adverse manifestations become increasingly apparent with increasing venous plasma levels above 6 mcg free base per mL.  In the rhesus monkey arterial blood levels of 18 to 21 mcg/mL have been shown to be threshold for convulsive activity.

Indications and Usage for Xylocaine Topical Solution

4% Xylocaine (lidocaine HCl) Topical Solution is indicated for the production of topical anesthesia of accessible mucous membranes of the oral and nasal cavities and proximal portions of the digestive tract.

Contraindications

Lidocaine HCl is contraindicated in patients with a known history of hypersensitivity to local anesthetics of the amide type or to other components of 4% Xylocaine Topical Solution.

Warnings

IN ORDER TO MANAGE POSSIBLE ADVERSE REACTIONS, RESUSCITATIVE EQUIPMENT, OXYGEN AND OTHER RESUSCITATIVE DRUGS MUST BE IMMEDIATELY AVAILABLE WHEN LOCAL ANESTHETIC AGENTS, SUCH AS LIDOCAINE HCl, ARE ADMINISTERED TO MUCOUS MEMBRANES.

4% Xylocaine Topical Solution should be used with extreme caution if there is sepsis or severely traumatized mucosa in the area of application, since under such conditions there is the potential for rapid systemic absorption.

Precautions

General

The safety and effectiveness of lidocaine HCl depend on proper dosage, correct technique, adequate precautions, and readiness for emergencies.  Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use (see WARNINGS and ADVERSE REACTIONS).  The lowest dosage that results in effective anesthesia should be used to avoid high plasma levels and serious adverse effects.  Repeated doses of lidocaine HCl may cause significant increases in blood levels with each repeated dose because of slow accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies with the status of the patient.  Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their age and physical status. Lidocaine HCl should also be used with caution in patients with severe shock or heart block.

4% Xylocaine Topical Solution should be used with caution in patients with known drug sensitivities.  Patients allergic to para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross sensitivity to lidocaine HCl.

Although it has been shown that the rate of absorption of lidocaine HCl after spraying the laryngotracheal mucosa with a solution of the local anesthetic agent is normally relatively slow, there is the attendant risk that occasionally some of the solution may gravitate into the lower respiratory tract where surface area for absorption and tissue blood flow are markedly greater.  This can result in unexpectedly rapid and high blood levels, and this possibility must be kept in mind whenever 4% Xylocaine Topical Solution is administered.

Many drugs used during the conduct of anesthesia are considered potential triggering agents for familial malignant hyperthermia.  Since it is not known whether amide-type local anesthetics may trigger this reaction and since the need for supplemental general anesthesia cannot be predicted in advance, it is suggested that a standard protocol for management should be available.  Early unexplained signs of tachycardia, tachypnea, labile blood pressure and metabolic acidosis may precede temperature elevation. Successful outcome is dependent on early diagnosis, prompt discontinuance of the suspect triggering agent(s) and institution of treatment, including oxygen therapy, indicated supportive measures and dantrolene (consult dantrolene sodium intravenous package insert before using).

Information for Patients

When topical anesthetics are used in the mouth, the patient should be aware that the production of topical anesthesia may impair swallowing and thus enhance the danger of aspiration.  For this reason, food should not be ingested for 60 minutes following use of local anesthetic preparations in the mouth or throat area.  This is particularly important in children because of their frequency of eating.

Numbness of the tongue or buccal mucosa may enhance the danger of unintentional biting trauma.  Food and chewing gum should not be taken while the mouth or throat area is anesthetized.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Studies of lidocaine HCl in animals to evaluate the carcinogenic and mutagenic potential or the effect on fertility have not been conducted.

Use in Pregnancy

Pregnancy Category B. Reproduction studies have been performed in rats at doses up to 6.6 times the human dose and have revealed no evidence of harm to the fetus caused by lidocaine HCl.  There are, however, no adequate and well-controlled studies in pregnant women.  Animal reproduction studies are not always predictive of human response. General consideration should be given to this fact before administering lidocaine HCl to women of childbearing potential, especially during early pregnancy when maximum organogenesis takes place.

Labor and Delivery

Lidocaine HCl is not contraindicated in labor and delivery. Should 4% Xylocaine Topical Solution be used concomitantly with other products containing lidocaine HCl, the total dose being administered must be kept in mind.

Nursing Mothers

It is not known whether this drug is excreted in human milk.  Because many drugs are excreted in human milk, caution should be exercised when lidocaine HCl is administered to a nursing woman.

Pediatric Use

Dosages in children should be reduced, commensurate with age, body weight and physical condition (see DOSAGE AND ADMINISTRATION).

Adverse Reactions

Adverse experiences following the administration of lidocaine HCl are similar in nature to those observed with other amide local anesthetic agents.  These adverse experiences are, in general, dose-related and may result from high plasma levels caused by excessive dosage or rapid absorption, or may result from a hypersensitivity, idiosyncrasy or diminished tolerance on the part of the patient.  Serious adverse experiences are generally systemic in nature.  The following types are those most commonly reported:

Central Nervous System

CNS manifestations are excitatory and/or depressant and may be characterized by lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression and arrest.  The excitatory manifestations may be very brief or may not occur at all, in which case the first manifestation of toxicity may be drowsiness merging into unconsciousness and respiratory arrest.

Drowsiness following the administration of lidocaine HCl is usually an early sign of a high blood level of the drug and may occur as a consequence of rapid absorption.

Cardiovascular System

Cardiovascular manifestations are usually depressant and are characterized by bradycardia, hypotension, and cardiovascular collapse, which may lead to cardiac arrest.

Allergic

Allergic reactions are characterized by cutaneous lesions, urticaria, edema or anaphylactoid reactions. Allergic reactions may occur as a result of sensitivity either to the local anesthetic agent or to other ingredients in the formulation.  Allergic reactions as a result of sensitivity to lidocaine HCl are extremely rare and, if they occur, should be managed by conventional means.  The detection of sensitivity by skin testing is of doubtful value.

Overdosage

Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics (see ADVERSE REACTIONS, WARNINGS, and PRECAUTIONS).

Management of Local Anesthetic Emergencies

The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs and the patient’s state of consciousness after each local anesthetic administration.  At the first sign of change, oxygen should be administered.

The first step in the management of convulsions consists of immediate attention to the maintenance of a patent airway and assisted or controlled ventilation with oxygen and a delivery system capable of permitting immediate positive airway pressure by mask. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should be evaluated, keeping in mind that drugs used to treat convulsions sometimes depress the circulation when administered intravenously.  Should convulsions persist despite adequate respiratory support, and if the status of the circulation permits, small increments of an ultra-short acting barbiturate (such as thiopental or thiamylal) or a benzodiazepine (such as diazepam) may be administered intravenously.  The clinician should be familiar, prior to use of local anesthetics, with these anticonvulsant drugs. Supportive treatment of circulatory depression may require administration of intravenous fluids and, when appropriate, a vasopressor as directed by the clinical situation (eg, ephedrine).

If not treated immediately, both convulsions and cardiovascular depression can result in hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest. If cardiac arrest should occur, standard cardiopulmonary resuscitative measures should be instituted.

Dialysis is of negligible value in the treatment of acute overdosage with lidocaine HCl.

The intravenous LD50 of lidocaine HCl in female mice is 26 (21 to 31) mg/kg and the subcutaneous LD50 is 264 (203 to 304) mg/kg.

Xylocaine Topical Solution Dosage and Administration

When 4% Xylocaine Topical Solution is used concomitantly with other products containing lidocaine HCl, the total dose contributed by all formulations must be kept in mind.

The dosage varies and depends upon the area to be anesthetized, vascularity of the tissues, individual tolerance, and the technique of anesthesia.  The lowest dosage needed to provide effective anesthesia should be administered.  Dosages should be reduced for children and for elderly and debilitated patients.  The maximum dose should not exceed 4.5 mg/kg (2 mg/lb) of body weight.  Although the incidence of adverse effects with 4% Xylocaine Topical Solution is quite low, caution should be exercised, particularly when employing large volumes, since the incidence of adverse effects is directly proportional to the total dose of local anesthetic agent administered.

The dosages recommended below are for normal, healthy adults:

When used as a spray, or when applied by means of cotton applicators or packs, as when instilled into a cavity, the suggested dosage of 4% Xylocaine Topical Solution is 1 to 5 mL (40 to 200 mg lidocaine HCl), ie, 0.6 to 3 mg/kg or 0.3 to 1.5 mg/lb body weight.

NOTE: The solution may be applied with a sterile swab which is discarded after a single use.  When spraying, transfer the solution from the original container to an atomizer.

MAXIMUM RECOMMENDED DOSAGES

Normal Healthy Adults

The maximum recommended dose of 4% Xylocaine Topical Solution should be such that the dose of lidocaine HCl is kept below 300 mg and in any case should not exceed 4.5 mg/kg (2 mg/lb) body weight.

Children

It is difficult to recommend a maximum dose of any drug for children since this varies as a function of age and weight.  For children of less than ten years who have a normal lean body mass and normal body development, the maximum dose may be determined by the application of one of the standard pediatric drug formulas (eg, Clark’s rule).  For example, in a child of five years weighing 50 lbs, the dose of lidocaine HCl should not exceed 75 to 100 mg when calculated according to Clark’s rule.  In any case, the maximum dose of 4% Xylocaine Topical Solution with epinephrine should not exceed 7 mg/kg (3.2 mg/lb) of body weight.  When used without epinephrine, the amount of 4% Xylocaine Topical Solution administered should be such that the dose is kept below 300 mg and in any case should not exceed 4.5 mg/kg (2 mg/lb) of body weight.

How is Xylocaine Topical Solution Supplied

4% Xylocaine (lidocaine HCl) Topical Solution NOT FOR INJECTION.

Product No.
 NDC No.
 Strength  
 491750  63323-497-50  4% (40 mg/mL)
 50 mL screw-cap bottle, packaged individually.

Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

All trademarks are the property of APP Pharmaceuticals, LLC

Manufactured for:

451173

Revised: March 2009

PACKAGE LABEL - PRINCIPAL DISPLAY - Xylocaine® 50 mL Vial Label

NDC 63323-497-50

491750

Xylocaine® (lidocaine HCl)

4% Topical Solution

Not for Injection

50 mL

 



PACKAGE LABEL - PRINCIPAL DISPLAY - Xylocaine® 50 mL Carton Label

NDC 63323-497-50

491750

Xylocaine® (lidocaine HCl)

Topical Solution

4% (40 mg/mL)

Not for Injection

Rx only

50 mL


XYLOCAINE 
lidocaine hydrochloride solution
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:63323-497
Route of Administration TOPICAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
LIDOCAINE HYDROCHLORIDE (LIDOCAINE) LIDOCAINE HYDROCHLORIDE 40 mg  in 1 mL
Inactive Ingredients
Ingredient Name Strength
METHYLPARABEN 1 mg  in 1 mL
SODIUM HYDROXIDE  
HYDROCHLORIC ACID  
Packaging
# Item Code Package Description
1 NDC:63323-497-50 1 BOTTLE (1 BOTTLE) in 1 BOX
1 50 mL in 1.0 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
NDA NDA010417 11/11/2009
Labeler - APP Pharmaceuticals, LLC (608775388)
Establishment
Name Address ID/FEI Operations
AstraUSA, Inc 176500158 MANUFACTURE
Revised: 11/2009
 
APP Pharmaceuticals, LLC
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