Lidotral I Patch: Package Insert / Prescribing Info

Lidotral I Patch Description

Lidotral® I- Lidocaine Patch 4.88% is comprised of an adhesive material containing 4.88% 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 lidocaine 683 mg (48.8 mg per gram adhesive) in an aqueous base. It also contains the following inactive ingredients: purified water, glycerin, sorbitol, polyacrylic acid, sodium carboxymethylcellulose, sodium polyacrylate, propylene glycol, urea, kaolin, tartaric acid, gelatin, polyvinyl alcohol, dihydroxyaluminum aminoacetate, edetate disodium, methylparaben, and propylparaben.

Lidotral I Patch - Clinical Pharmacology

Clinical Studies

Single-dose treatment with Lidotral® I - Lidocaine Patch 4.88% / Lidocaine Patch 5% was compared to treatment with vehicle patch (without lidocaine), and to no treatment (observation only) in a double-blind, crossover clinical trial with 35 post-herpetic neuralgia patients. Pain intensity and pain relief scores were evaluated periodically for 12 hours. Lidocaine patch performed statistically better than vehicle patch in terms of pain intensity from 4 to 12 hours.

Multiple-dose, two-week treatment with Lidotral® I - Lidocaine Patch 4.88%/ Lidocaine Patch 5%, was compared to vehicle patch (without lidocaine) in a double-blind, crossover clinical trial of withdrawal-type design conducted in 32 patients, who were considered as responders to the open-label use of lidocaine patch prior to the study. The constant type of pain was evaluated but not the pain induced by sensory stimuli (dysesthesia). Statistically significant differences favoring lidocaine patch were observed in terms of time to exit from the trial (14 versus 3.8 days at p-value <0.001), daily average pain relief, and patient's preference of treatment. About half of the patients also took oral medication commonly used in the treatment of post-herpetic neuralgia. The extent of use of concomitant medication was similar in the two treatment groups.

Indications and Usage for Lidotral I Patch

Lidotral® I - Lidocaine Patch 4.88% is indicated for relief of pain associated with post-herpetic neuralgia. It should be applied only to intact skin.

Contraindications

Lidotral® I - Lidocaine Patch 4.88% is contraindicated in patients with a known history of sensitivity to local anesthetics of the amide type, or to any other component of the product.

Warnings

Risk of Methemoglobinemia

Cases of methemoglobinemia have been reported in association with local anesthetic use. Although all patients are at risk for methemoglobinemia, patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition. If local anesthetics must be used in these patients, close monitoring for symptoms and signs of methemoglobinemia is recommended.

Signs of methemoglobinemia may occur immediately or may be delayed some hours after exposure, and are characterized by a cyanotic skin discoloration and/or abnormal coloration of the blood. Methemoglobin levels may continue to rise; therefore, immediate treatment is required to avert more serious central nervous system and cardiovascular adverse effects, including seizures, coma, arrhythmias, and death. Discontinue Lidotral® I - Lidocaine Patch 4.88% and any other oxidizing agents. Depending on the severity of the signs and symptoms, patients may respond to supportive care, i.e., oxygen therapy, hydration. A more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen.

Accidental Exposure in Children

Even a used patch contains a large amount of lidocaine (at least 665 mg). The potential exists for a small child or a pet to suffer serious adverse effects from chewing or ingesting a new or used lidocaine patch 4.88%, although the risk with this formulation has not been evaluated. It is important for patients to store and dispose of Lidotral® I - Lidocaine Patch 4.88% out of the reach of children, pets, and others (see HANDLING AND DISPOSAL).

Excessive Dosing

Excessive dosing by applying Lidotral® I - Lidocaine Patch 4.88% to larger areas or for longer than the recommended wearing time could result in increased absorption of lidocaine and high blood concentrations, leading to serious adverse effects (see ADVERSE REACTIONS, Systemic Reactions). Lidocaine toxicity could be expected at lidocaine blood concentrations above 5 mcg/mL. The blood concentration of lidocaine is determined by the 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 the blood concentration of lidocaine. With recommended dosing of Lidotral® I - Lidocaine Patch 4.88%, the average peak blood concentration is about 0.13 mcg/mL, but concentrations higher than 0.25 mcg/mL have been observed in some individuals.

Precautions

Adverse Reactions/Side Effects

Application Site Reactions

During or immediately after treatment with Lidotral® I - Lidocaine Patch 4.88%, the skin at the site of application may develop blisters, bruising, burning sensation, depigmentation, dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia, pruritus, vesicles, or may be the locus of abnormal sensation. These reactions are generally mild and transient, resolving spontaneously within a few minutes to hours.

Allergic Reactions

Allergic and anaphylactoid reactions associated with lidocaine, 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 conventional means. The detection of sensitivity by skin testing is of doubtful value.

Other Adverse Events

Due to the nature and limitation of spontaneous reports in postmarketing surveillance, causality has not been established for additional 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 of Lidotral® I - Lidocaine Patch 4.88% are unlikely, due to the small dose absorbed (see CLINICAL PHARMACOLOGY, Pharmacokinetics). Systemic adverse effects of lidocaine are similar in nature to those observed with other amide local anesthetic agents, including CNS excitation and/or depression (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). Excitatory CNS reactions may be brief or not occur at all, in which case the first manifestation may be drowsiness merging into unconsciousness. Cardiovascular manifestations may include bradycardia, hypotension, and cardiovascular collapse leading to arrest.

Overdosage

Lidocaine overdose from cutaneous absorption is rare, but could occur. If there is any suspicion of lidocaine overdose (see ADVERSE REACTIONS, Systemic Reactions), drug blood concentration should be checked. The management of overdose includes close monitoring, supportive care, and symptomatic treatment. Dialysis is of negligible value in the treatment of acute overdose with lidocaine.

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

The oral LD 50of lidocaine HCl is 459 (346 to 773) mg/kg (as the salt) in non-fasted female rats and 214 (159 to 324) mg/kg (as the salt) in fasted 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 dosage conversion factors between species.

Lidotral I Patch Dosage and Administration

Apply Lidotral® I - Lidocaine Patch 4.88% to intact skin to cover the most painful area. Apply the prescribed number of patches (maximum of 3), only once for up to 12 hours within a 24-hour period. Patches may be cut into smaller sizes with scissors prior to removal of the release liner (see HANDLING AND DISPOSAL). Clothing may be worn over the area of application. Smaller areas of treatment are recommended in a debilitated patient, or a patient with impaired elimination.

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

When Lidotral® I - Lidocaine Patch 4.88% is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered .

Lidotral® I - Lidocaine Patch 4.88% may not stick if it gets wet. Avoid contact with water, such as bathing, swimming, or showering.

HANDLING AND DISPOSAL

Hands should be washed after the handling of Lidotral® I - Lidocaine Patch 4.88%, and eye contact with Lidotral® I - Lidocaine Patch 4.88% should be avoided. Do not store patch outside the sealed envelope. Apply immediately after removal from the 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. Lidotral® I - Lidocaine Patch 4.88% should be kept out of the reach of children.

How is Lidotral I Patch supplied

Lidotral® I - Lidocaine Patch 4.88% is available as the following:
Package of 30 patches..... NDC 59088-974-54
(packaged into individual child-resistant envelope)
Single patch..... NDC 59088-974-84
(packaged into individual child-resistant envelope)

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

Manufactured by:
PureTek Corporation
Panorama City, CA 91402
For questions or information
call toll-free : 877-921-7873

Lidotral® I - Lidocaine Patch 4.88%