Brand names: Lidoderm, Ztlido
Drug class: Antipruritics and Local Anesthetics

Medically reviewed by Drugs.com on Oct 10, 2024. Written by ASHP.

Introduction

Amide local anesthetic; a nonselective voltage-gated sodium channel inhibitor.

Uses for Lidocaine (Topical)

Postherpetic Neuralgia

Lidocaine 1.8% and 5% patches are used topically for treatment of pain associated with postherpetic neuralgia (PHN) in adults.

Following topical application as recommended, produces analgesia, but not anesthesia. Has been shown to modestly decrease pain in patients with PHN and is well-tolerated.

The 1.8% patch has greater bioavailability, allowing for a lower strength; however, the preparations are considered to be bioequivalent.

First-line treatments for neuropathic pain include gabapentinoids (gapapentin and pregabalin), tricyclic antidepressants (TCAs), and serotonin-norepinephrine reuptake inhibitors (SNRIs; duloxetine and venlafaxine). Lidocaine patches are recommended as a first-line treatment in some guidelines, and second-line in others. May be considered in certain patients such as the elderly who may not be able to tolerate the adverse effects of gabapentinoids, TCAs, or SNRIs.

Lidocaine (Topical) Dosage and Administration

General

Dispensing and Administration Precautions

Handling and Disposal

• Wash hands immediately after handling lidocaine patches; avoid contact with eyes.

• Store patches outside the sealed envelope out of reach of children, pets, and others.

• Apply patches immediately after removal from their protective envelope. Fold used patches so that the adhesive side sticks to itself and safely discard used patches or pieces of cut patches where children and pets cannot get to them.

Administration

Apply topically to intact skin.

Apply immediately after removal from the protective envelope. May cut into smaller sizes with scissors prior to removal of the release liner.

Up to 3 patches may be applied at one time as prescribed; application of more than the recommended number of patches or for longer durations than recommended can result in increased blood concentrations of lidocaine, resulting in adverse reactions.

Clothing may be worn over the area of application.

If irritation or a burning sensation occurs during application, remove patch(es) and do not reapply until irritation subsides.

Lidocaine 5% (Lidoderm) patches may not stick if they get wet. Manufacturer states to avoid contact with water, such as bathing, swimming or showering.

Manufacturer of Ztlido states that the patches may be used during moderate exercise, such as biking for 30 minutes and may be exposed to water, such as showering, for 10 minutes or immersion for 15 minutes. To dry the topical system after water exposure, gently pat skin; do not rub skin or topical system.

Do not apply external heat sources, such as heating pads or electric blankets, directly to lidocaine patches, since this may increase plasma lidocaine levels. Manufacturer of Ztlido states that the patches can be applied to an administration site after moderate heat exposure, such as 15 minutes of heating pad exposure on a medium setting.

Dosage

Adults

Postherpetic Neuralgia

Topical

Lidocaine 1.8% patches (Ztlido) are bioequivalent to lidocaine 5% patches (Lidoderm and generics); one Ztildo topical system provides equivalent lidocaine exposure to one Lidoderm (or generic equivalent) patch.

Lidocaine 5%: Each patch contains 700 mg of lidocaine. Apply up to 3 patches to most painful area of skin. Apply once for up to 12 hours within a 24 hour period.

Lidocaine 1.8%: Each patch contains 36 mg of lidocaine. Apply up to 3 patches to the most painful area of the skin. Apply once for up to 12 hours within a 24 hour period.

Smaller areas of treatment are recommended in debilitated patients and patients with impaired elimination.

When used concomitantly with other products containing local anesthetic agents, consider the amount absorbed from all formulations.

Special Populations

Geriatric Patients

Select dosage with caution in geriatric patients, usually starting at the low end of the dosing range (e.g., a single topical system).

Cautions for Lidocaine (Topical)

Contraindications

• Known history of sensitivity to local anesthetic of the amide type, or to any other component of the product.

Warnings/Precautions

Risk of Methemoglobinema

Methemoglobinemia reported in association with local anesthetic use. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants <6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations.

Symptoms may include cyanotic skin discoloration and/or abnormal blood color.

Discontinue lidocaine patch and any other oxidizing agents if methemoglobinemia occurs. Depending on severity, supportive care (e.g., oxygen therapy, hydration) or more aggresive treatments (e.g., methylene blue, exchange transfusion, hyperbaric oxygen) may be necessary.

Accidental Exposure

A used lidocaine patch contains a residual amount of drug after use. Potential exists for a small child or a pet to suffer serious adverse effects from chewing or ingesting a new or used patch.

Store and dispose of lidocaine patches out of reach of children, pets, and others.

Excessive Dosing

Application to larger areas or for longer than recommended durations could result in increased absorption of lidocaine and high blood concentrations causing serious adverse effects.

Lidocaine toxicity can be expected at blood concentrations >5 mcg/mL. Blood concentration is determined by rate of systemic absorption and elimination. Longer duration of application, application of more than the recommended number of patches, smaller patients, or impaired elimination may all contribute to increasing blood concentration of lidocaine.

Application Site Reactions

Application site reactions (e.g., blisters, bruising, burning sensation, depigmentation, dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia, pruritus, vesicles) may occur. Generally mild and transient, resolving spontaneously within a few minutes to hours.

If application site reactions occur, remove patch; do not reapply until skin reaction subsides.

Apply only on intact skin. Application to broken or inflamed skin may result in higher blood concentrations of lidocaine from increased absorption.

Hypersensitivity Reactions

Allergic and anaphylactoid reactions reported rarely. Signs and symptoms have included angioedema, bronchospasm, dermatitis, dyspnea, hypersensitivity, laryngospasm, pruritus, shock, and urticaria.

If a hypersenstivity reaction occurs, manage with conventional measures.

Cross-sensitivity not shown between para-aminobenzoic acid (PABA) derivatives (e.g., procaine, tetracaine, benzocaine) and lidocaine. However, use lidocaine patch with caution in patients with a history of drug sensitivities.

Eye Exposure

Avoid contact with eyes; severe eye irritation observed in animal studies.

If eye contact occurs, immediately wash the eye with water or saline and protect the eye until sensation returns.

External Heat Sources

Do not apply external heat sources to lidocaine patches during administration; may increase drug exposure.

No effect on pharmacokinetics of the 1.8% patch observed when applied to the administration site after external heat exposure (heating pad at medium setting applied for 15 minutes prior to the topical system application) or after engagement in exercise (walking at a moderate pace on a treadmill for approximately 20 minutes beginning approximately 30 minutes prior to the topical system application).

Specific Populations

Pregnancy

Lidocaine 5% patch not studied in pregnancy. Limited human data with the 1.8% patch insufficient to inform a drug-associated risk for major birth defects and miscarriage.

Use during pregnancy only if clearly needed.

Not studied and contraindicated in labor and delivery.

If used concomitantly with other products containing lidocaine, consider total doses contributed by all formulations.

Lactation

Excreted into human milk in low concentrations following topical application. Use caution in nursing woman, especially when administered with other local anesthetics.

Females and Males of Reproductive Potential

Effect of lidocaine patches on fertility not studied.

Pediatric Use

Safety and effectiveness not established.

Geriatric Use

Clinical studies of lidocaine 1.8% patch did not include sufficient number of patients ≥65 years of age to determine whether they respond differently from younger patients. No differences in response identified in other clinical experience.

Hepatic Impairment

Patients with severe hepatic disease are at increased risk of lidocaine toxicity because they are unable to metabolize lidocaine normally.

Common Adverse Effects

Common adverse effects of lidocaine 1.8 and 5% patches include mild and transient application site reactions (e.g., blisters, bruising, burning sensation, depigmentation, dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia, pruritus, vesicles).

Systemic adverse reactions following topical use of lidoderm patch unlikely due to minimal drug absorption.

Drug Interactions

Antiarrhythmic Drugs

Use with caution in patients receiving class I antiarrhythmic drugs (e.g., tocainide, mexiletine); additive and potentially synergistic toxic effects can occur.

Local Anesthetics

When used concomitantly with other products containing local anesthetic agents, consider the amount absorbed from all formulations.

Drugs Associated with Methemoglobinemia

Patients receiving local anesthetics are at increased risk of developing methemoglobinemia when taking other drugs that can cause methemoglobinemia. These drugs include nitrate/nitrites (nitric oxide, nitroglycerin, nitroprusside, nitrous oxide), local anesthetics (articaine, benzocaine, bupivacaine, lidocaine, mepivacaine, prilocaine, procaine, ropivacaine, tetracaine), antineoplastic agents (cyclophosphamide, flutamide, hydroxyurea, ifosfamide, rasburicase), antibiotics (dapsone, nitrofurantoin, para-aminosalicylic acid, sulfonamides), antimalarials (chloroquine, primaquine), anticonvulsants (phenobarbital, phenytoin, sodium valproate), acetaminophen, metoclopramide, quinine, and sulfasalazine.

Lidocaine (Topical) Pharmacokinetics

Absorption

Bioavailability

Amount of lidocaine systemically absorbed from a lidocaine patch is directly related to both duration of application and surface area over which it is applied.

Minimal systemic absorption (approximately 3%) when the 5% patches are used topically as recommended; maximum blood concentrations are about 1/10 of the therapeutic concentration required to treat cardiac arrhythmias.

Mean lidocaine blood concentrations after 3 consecutive days of daily use (3 patches applied at the same time for 12 hours once daily for 3 days) remain the same.

Lidocaine 1.8% patches (Ztlido) are bioequivalent to lidocaine 5% patches (Lidoderm and generics).

Distribution

Plasma Protein Binding

Approximately 70% bound to plasma proteins (primarily alpha-1-acid glycoprotein) at concentrations achieved from topical application; at higher concentrations, plasma protein binding is concentration dependent.

Extent

Crosses placental and blood brain barriers, presumably by diffusion.

Distributes into human milk.

Elimination

Metabolism

Not known if lidocaine is metabolized in the skin.

Extensively metabolized in liver to several pharmacologically active metabolites and excreted by kidneys (<10% as unchanged drug).

Stability

Storage

Topical

Lidoderm and generics: Store at 25°C; excursions permitted to 15–30°C.

Ztlido: Store at 20–25°C; excursions permitted to 15–30°C.

Actions

• Amide-type local anesthetic that blocks sodium ion channels required for the initiation and conduction of neuronal impulses. Analgesic effects of lidocaine are thought to result from these effects.

• Penetration of lidocaine into intact skin is sufficient to produce an analgesic effects; however, the amount is insufficient to product a complete sensory block.

Advice to Patients

• Inform patients that use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly. Advise patients or caregivers to stop use and seek immediate medical attention if they or someone in their care experience the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue.

• Instruct patients on proper application, storage, and disposal of the lidocaine patches.

• Advise patients that skin irritation may occur at the site of application. If skin reactions occur, advise patients to remove the patch and do not reapply until the skin reaction subsides.

• Advise patients to not place external heat sources, such as heating pads or electric blankets, over lidocaine patches as this has not been evaluated and may increase plasma lidocaine levels.

• Advise patients to wash hands immediately after handling the lidocaine patches and to avoid contact with eyes. If contact occurs, instruct patients to immediately wash out the eye with water or saline and protect the eye until sensation returns.

• Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.

• Advise women to inform their clinician if they are or plan to become pregnant or plan to breast-feed.

• Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

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

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

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

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