Lidoderm (Lidocaine Patch 5%): Side Effects, Uses, Dosage, Interactions, Warnings (2024)

Description for Lidoderm

LIDODERM (lidocaine patch 5%) is comprised of an adhesive material containing 5% lidocaine, which is applied to a non-woven polyester felt backing and covered with a polyethylene terephthalate (PET) film release liner. The release liner is removed prior to application to the skin. The size of the patch is 10 cm x 14 cm.

Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), has an octanol: water partition ratio of 43 at pH 7.4, and has the following structure:

Each adhesive patch contains 700 mg of lidocaine (50 mg per gram adhesive) in an aqueous base. It also contains the following inactive ingredients: dihydroxyaluminum aminoacetate, disodium edetate, gelatin, glycerin, kaolin, methylparaben, polyacrylic acid, polyvinyl alcohol, propylene glycol, propylparaben, sodium carboxymethylcellulose, sodium polyacrylate, Dsorbitol, tartaric acid, and urea.

Uses for Lidoderm

LIDODERM is indicated for relief of pain associated withpost-herpetic neuralgia. It should be applied only to intact skin.

Dosage for Lidoderm

Apply LIDODERM to intact skin to cover the most painfularea. Apply the prescribed number of patches (maximum of 3), only once for upto 12 hours within a 24 hour period. Patches may be cut into smaller sizes withscissors prior to removal of the release liner. (See Handling And Disposal)Clothing may be worn over the area of application. Smaller areas of treatmentare recommended in a debilitated patient, or a patient with impairedelimination.

If irritation or a burning sensation occurs duringapplication, remove the patch (es) and do not reapply until the irritationsubsides.

When LIDODERM is used concomitantly with other productscontaining local anesthetic agents, the amount absorbed from all formulationsmust be considered.

LIDODERM may not stick if it gets wet. Avoid contact withwater, such as bathing, swimming or showering.

Handling And Disposal

Hands should be washed after the handling of LIDODERM,and eye contact with LIDODERM should be avoided. Do not store patch outside thesealed envelope. Apply immediately after removal from the protective envelope.Fold used patches so that the adhesive side sticks to itself and safely discardused patches or pieces of cut patches where children and pets cannot get tothem. LIDODERM should be kept out of the reach of children.

HOW SUPPLIED

LIDODERM (lidocaine patch 5%) is available as thefollowing:

Carton of 30 patches, packaged into individualchild-resistant envelopes

NDC 63481-687-06

Store at 25°C (77°F); excursions permitted to 15°-30°C(59°-86°F). [See USP Controlled Room Temperature].

For more information, call Endo Pharmaceuticals at1-800-462-3636.

Manufactured for: Endo Pharmaceuticals Inc.Malvern, PA 19355. January 2015

Side Effects for Lidoderm

Application Site Reactions

During or immediately after treatment with LIDODERM(lidocaine patch 5%), the skin at the site of application may develop blisters,bruising, burning sensation, depigmentation, dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia, pruritus, vesicles, ormay be the locus of abnormal sensation. These reactions are generally mild andtransient, resolving spontaneously within a few minutes to hours.

Allergic Reactions

Allergic and anaphylactoid reactions associated withlidocaine, although rare, can occur. They are characterized by angioedema,bronchospasm, dermatitis, dyspnea, hypersensitivity, laryngospasm, pruritus, shock, and urticaria. If they occur, they should be managed by conventionalmeans. The detection of sensitivity by skin testing is of doubtful value.

Other Adverse Events

Due to the nature and limitation of spontaneous reportsin postmarketing surveillance, causality has not been established foradditional reported adverse events including:

Asthenia, confusion, disorientation, dizziness, headache,hyperesthesia, hypoesthesia, lightheadedness, metallic taste, nausea,nervousness, pain exacerbated, paresthesia, somnolence, taste alteration,vomiting, visual disturbances such as blurred vision, flushing, tinnitus, and tremor.

Systemic (Dose-Related) Reactions

Systemic adverse reactions following appropriate use ofLIDODERM are unlikely, due to the small dose absorbed (see CLINICALPHARMACOLOGY, Pharmaco*kinetics). Systemic adverse effects oflidocaine are similar in nature to those observed with other amide local anesthetic agents, including CNS excitation and/or depression(light-headedness, nervousness, apprehension, euphoria, confusion, dizziness,drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat,cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratorydepression and arrest). Excitatory CNS reactions may be brief or not occur atall, in which case the first manifestation may be drowsiness merging intounconsciousness. Cardiovascular manifestations may include bradycardia, hypotension and cardiovascular collapse leading to arrest.

Drug Interactions for Lidoderm

Antiarrhythmic Drugs

LIDODERM should be used with caution in patientsreceiving Class I antiarrhythmic drugs (such as tocainide and mexiletine) sincethe toxic effects are additive and potentially synergistic.

Local Anesthetics

When LIDODERM is used concomitantly with other productscontaining local anesthetic agents, the amount absorbed from all formulationsmust be considered.

Warnings for Lidoderm

Accidental Exposure In Children

Even a used LIDODERM patch contains a large amountof lidocaine (at least 665 mg). The potential exists for a small child or a petto suffer serious adverse effects from chewing or ingesting a new or usedLIDODERM patch, although the risk with this formulation has not been evaluated.It is important for patients to store and dispose of LIDODERM out of thereach of children, pets and others. (See Handling And Disposal)

Excessive Dosing

Excessive dosing by applying LIDODERM to larger areas orfor longer than the recommended wearing time could result in increasedabsorption of lidocaine and high blood concentrations, leading to seriousadverse effects (see ADVERSE REACTIONS, Systemic Reactions).Lidocaine toxicity could be expected at lidocaine blood concentrations above 5μg/mL. The blood concentration of lidocaine is determined by the rate ofsystemic absorption and elimination. Longer duration of application, applicationof more than the recommended number of patches, smaller patients, or impairedelimination may all contribute to increasing the blood concentration oflidocaine. With recommended dosing of LIDODERM, the average peak blood concentrationis about 0.13 μg/mL, but concentrations higher than 0.25 μg/mL havebeen observed in some individuals.

Precautions for Lidoderm

General

Hepatic Disease

Patients with severe hepatic disease are at greater riskof developing toxic blood concentrations of lidocaine, because of theirinability to metabolize lidocaine normally.

Allergic Reactions

Patients allergic to para-aminobenzoic acid derivatives(procaine, tetracaine, benzocaine, etc.) have not shown cross sensitivity tolidocaine. However, LIDODERM should be used with caution in patients with ahistory of drug sensitivities, especially if the etiologic agent is uncertain.

Non-intact Skin

Application to broken or inflamed skin, although nottested, may result in higher blood concentrations of lidocaine from increasedabsorption. LIDODERM is only recommended for use on intact skin.

External Heat Sources

Placement of external heat sources, such as heating padsor electric blankets, over LIDODERM patches is not recommended as this has notbeen evaluated and may increase plasma lidocaine levels.

Eye Exposure

The contact of LIDODERM with eyes, although not studied,should be avoided based on the findings of severe eye irritation with the useof similar products in animals. If eye contact occurs, immediately wash out theeye with water or saline and protect the eye until sensation returns.

Carcinogenesis, Mutagenesis, Impairment Of Fertility

Carcinogenesis

A minor metabolite, 2, 6-xylidine, has been found to be carcinogenic in rats. The blood concentration of this metabolite is negligiblefollowing application of LIDODERM.

Mutagenesis

Lidocaine HC1 is not mutagenic in Salmonella/mammalianmicrosome test nor clastogenic in chromosome aberration assay with humanlymphocytes and mouse micronucleus test.

Impairment of Fertility

The effect of LIDODERM on fertility has not been studied.

Pregnancy

Teratogenic Effects

Pregnancy Category B

LIDODERM (lidocaine patch 5%) has not been studied inpregnancy. Reproduction studies with lidocaine have been performed in rats atdoses up to 30 mg/kg subcutaneously and have revealed no evidence of harm tothe fetus due to lidocaine. There are, however, no adequate and well-controlledstudies in pregnant women. Because animal reproduction studies are not alwayspredictive of human response, LIDODERM should be used during pregnancy only ifclearly needed.

Labor And Delivery

LIDODERM has not been studied in labor and delivery.Lidocaine is not contraindicated in labor and delivery. Should LIDODERM be usedconcomitantly with other products containing lidocaine, total doses contributedby all formulations must be considered.

Nursing Mothers

LIDODERM has not been studied in nursing mothers.Lidocaine is excreted in human milk, and the milk: plasma ratio of lidocaine is0.4. Caution should be exercised when LIDODERM is administered to a nursingwoman.

Pediatric Use

Safety and effectiveness in pediatric patients have notbeen established.

Overdose Information for Lidoderm

Lidocaine overdose from cutaneous absorption is rare, butcould occur. If there is any suspicion of lidocaine overdose (see ADVERSEREACTIONS, Systemic Reactions), drug blood concentration should bechecked. The management of overdose includes close monitoring, supportive care,and symptomatic treatment. Dialysis is of negligible value in the treatment ofacute overdose with lidocaine.

In the absence of massive topical overdose or oral ingestion,evaluation of symptoms of toxicity should include consideration of otheretiologies for the clinical effects, or overdosage from other sources oflidocaine or other local anesthetics.

The oral LD50 of lidocaine HCl is 459 (346-773) mg/kg (asthe salt) in non-fasted female rats and 214 (159-324) mg/kg (as the salt) infasted female rats, which are equivalent to roughly 4000 mg and 2000 mg,respectively, in a 60 to 70 kg man based on the equivalent surface area dosageconversion factors between species.

Contraindications for Lidoderm

LIDODERM is contraindicated in patients with a knownhistory of sensitivity to local anesthetics of the amide type, or to any othercomponent of the product.

Clinical Pharmacology for Lidoderm

Pharmacodynamics

Lidocaine is an amide-type local anesthetic agent and issuggested to stabilize neuronal membranes by inhibiting the ionic fluxesrequired for the initiation and conduction of impulses.

The penetration of lidocaine into intact skin afterapplication of LIDODERM is sufficient to produce an analgesic effect, but lessthan the amount necessary to produce a complete sensory block.

Pharmaco*kinetics

Absorption

The amount of lidocaine systemically absorbed from LIDODERMis directly related to both the duration of application and the surface areaover which it is applied. In a pharmaco*kinetic study, three LIDODERM patcheswere applied over an area of 420 cm² of intact skin on the back ofnormal volunteers for 12 hours. Blood samples were withdrawn for determinationof lidocaine concentration during the application and for 12 hours afterremoval of patches. The results are summarized in Table 1.

Table 1 : Absorption of lidocaine from LIDODERM Normalvolunteers (n= 15, 12-hour wearing time)

When LIDODERM is used according to the recommended dosinginstructions, only 3 ± 2% of the dose applied is expected to be absorbed. Atleast 95% (665 mg) of lidocaine will remain in a used patch. Mean peak bloodconcentration of lidocaine is about 0.13 μg/mL (about 1/10 of the therapeuticconcentration required to treat cardiac arrhythmias). Repeated application ofthree patches simultaneously for 12 hours (recommended maximum daily dose),once per day for three days, indicated that the lidocaine concentration doesnot increase with daily use. The mean plasma pharmaco*kinetic profile for the 15healthy volunteers is shown in Figure 1.

Figure 1 : Mean lidocaine blood concentrations afterthree consecutive daily applications of three LIDODERM patches simultaneouslyfor 12 hours per day in healthy volunteers (n = 15).

Distribution

When lidocaine is administered intravenously to healthyvolunteers, the volume of distribution is 0.7 to 2.7 L/kg (mean 1.5 ± 0.6 SD,n=15). At concentrations produced by application of LIDODERM, lidocaine isapproximately 70% bound to plasma proteins, primarily alpha-1-acid glycoprotein. At much higher plasma concentrations (1 to 4 μg/mL of freebase), the plasma protein binding of lidocaine is concentration dependent.Lidocaine crosses the placental and blood brain barriers, presumably by passivediffusion.

Metabolism

It is not known if lidocaine is metabolized in the skin.Lidocaine is metabolized rapidly by the liver to a number of metabolites,including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both ofwhich have pharmacologic activity similar to, but less potent than that of lidocaine.A minor metabolite, 2, 6-xylidine, has unknown pharmacologic activity but is carcinogenic in rats. The blood concentration of this metabolite is negligiblefollowing application of LIDODERM (lidocaine patch 5%). Following intravenousadministration, MEGX and GX concentrations in serum range from 11 to 36% andfrom 5 to 11% of lidocaine concentrations, respectively.

Excretion

Lidocaine and its metabolites are excreted by thekidneys. Less than 10% of lidocaine is excreted unchanged. The half-life oflidocaine elimination from the plasma following IV administration is 81 to 149minutes (mean 107 ± 22 SD, n = 15). The systemic clearance is 0.33 to 0.90L/min (mean 0.64 ± 0.18 SD, n = 15).

Clinical Studies

Single-dose treatment with LIDODERM was compared totreatment with vehicle patch (without lidocaine), and to no treatment(observation only) in a double-blind, crossover clinical trial with 35post-herpetic neuralgia patients. Pain intensity and pain relief scores wereevaluated periodically for 12 hours. LIDODERM performed statistically betterthan vehicle patch in terms of pain intensity from 4 to 12 hours.

Multiple-dose, two-week treatment with LIDODERM wascompared to vehicle patch (without lidocaine) in a double-blind, crossoverclinical trial of withdrawal-type design conducted in 32 patients, who wereconsidered as responders to the open-label use of LIDODERM prior to the study.The constant type of pain was evaluated but not the pain induced by sensorystimuli (dysesthesia). Statistically significant differences favoring LIDODERMwere observed in terms of time to exit from the trial (14 versus 3.8 days atp-value < 0.001), daily average pain relief, and patient's preference oftreatment. About half of the patients also took oral medication commonly usedin the treatment of post-herpetic neuralgia. The extent of use of concomitantmedication was similar in the two treatment groups.

Patient Information for Lidoderm

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.