Lidothol ES

INDICATIONS AND USAGE Lidothol® ES is a formulation used to assist patients in the treatment of mild to moderate acute or chronic aches or pain. Muscle or joint pain can be due to muscle or ligament strains, simple backache, tendonitis, osteoarthritis, rheumatoid arthritis, peripheral neuropathies such as diabetic neuropathy or post-herpetic neuralgia, and other complex regional pains. It can also be used to help with certain types of headaches, but use with caution when applying in order to avoid eye contact. Other uses may be considered if deemed clinically relevant.

DOSAGE AND ADMINISTRATION Apply Lidothol® ES to intact skin to cover the most painful area. Apply no more than two systems per day. Each system should not be applied for more than 12 hours in a given 24-hour period. Lidothol® ES may be cut into smaller sizes with scissors prior to the removal of the protective film. Clothing may be worn over the area of application. Smaller treatment areas are recommended for debilitated patients or those with impaired elimination. If irritation or a burning sensation occurs during application, remove the system and do not reapply until the irritation subsides. When Lidothol® ES is used concurrently with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered.

CONTRAINDICATIONS Lidothol® ES 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 AND PRECAUTIONS Excessive dosage or short intervals between doses can result in high plasma levels and serious adverse effects. Patients should be instructed to strictly adhere to the recommended dosage and administration guidelines set forth in this literature and on their prescription label. The management of serious adverse reactions may require the use of resuscitative equipment, oxygen, or other resuscitative drugs. 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 and symptoms of methemoglobinemia may occur immediately or may be delayed for some hours after exposure and are characterized by cyanotic skin discoloration and 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 Lidothol® ES and any other oxidizing agents. Depending on the severity of the symptoms, patients may respond to supportive care, i.e., oxygen therapy, hydration. More severe symptoms may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen. Accidental Exposure in Children Even a used Lidothol® ES contains a large amount of lidocaine. The potential exists for a small child or a pet to suffer serious adverse effects from chewing or ingesting a new or used Lidothol® ES. However, the risk with this formulation has not been evaluated. It is important for patients to store and dispose of Lidothol® ES beyond the reach of children, pets, and others. (See HANDLING AND DISPOSAL) Excessive Dosing Excessive dosing by applying Lidothol® ES to larger areas for longer than the recommended wearing time could result in increased absorption of lidocaine and high blood concentrations, leading to serious adverse effects. Lidocaine toxicity could be expected at lidocaine blood concentrations above 5 µg/mL. The rate of systemic absorption and elimination determines the blood concentration of lidocaine. Longer duration of application, application of more than the recommended number of systems, smaller patients, or impaired elimination may all contribute to increasing the blood concentration of lidocaine. With recommended dosing of Lidothol® ES, the average blood concentration is about 0.13 µg/mL, but concentrations higher than 0.25 µg/mL have been observed in some patients. Sedation and Impaired Alertness Because of the possibility of sedation, patients should be cautioned regarding the use of heavy machinery or automobiles, or any activities made hazardous by decreased alertness. Hepatic Disease Patients with severe hepatic disease are at greater risk of developing toxic blood concentrations of lidocaine, because of their inability to metabolize lidocaine normally. Allergic Reactions Patients allergic to para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross-sensitivity to lidocaine. However, Lidothol® ES should be used with caution in patients with a history of drug sensitivities, especially if the etiologic agent is uncertain. 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, consult your doctor. Non-intact Skin Although not tested, application to broken or inflamed skin may result in higher blood concentrations of lidocaine from increased absorption. Lidothol® ES is only recommended for use on intact skin. Eye Exposure The contact of Lidothol® ES with the eyes, although not studied, should be avoided based on the findings of severe eye irritations with the use of similar products in animals. If eye contact occurs, immediately wash out the eye with water or saline and protect the eye until sensation returns. External Heat Sources Placement of external heat sources, such as heating pads or electric blankets, over Lidothol® ES is not recommended, as this has not been evaluated and may increase plasma lidocaine levels.

DRUG INTERACTIONS Antiarrhythmic Drugs Lidothol® ES should be used with caution in patients receiving Class 1 antiarrhythmic drugs (such as tocainide and mexiletine) since the toxic effects are additive and potentially synergistic. Local Anesthetics When Lidothol® ES is used concurrently with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered. Methemoglobinemia Patients that are administered local anesthetics may be at increased risk of developing methemoglobinemia when concurrently exposed to the following oxidizing agents: a di table

ADVERSE REACTIONS The most common adverse reactions occur at the application site, including dermatitis, itching, or scaling. These tend to be dose-limiting and diminish with time. Serious adverse experiences following the administration of Lidothol® ES are similar in nature to those observed in other amide local anesthetic-containing agents. These adverse experiences are, in general, dose-related and may result from high plasma levels caused by excessive dosage, rapid absorption, or may result from hypersensitivity, idiosyncrasy, or a diminished tolerance on the part of the patient. Serious adverse experiences are generally systemic in nature. During or immediately after treatment with Lidothol® ES, the skin at the site of application may develop redness, blisters, bruising, burning sensation, depigmentation, dermatitis, or mild irritation.

USE IN SPECIFIC POPULATIONS Pregnancy The safety of Lidothol® ES has not been established during pregnancy. There are no well-controlled studies in pregnant women. Discuss with a physician prior to using Lidothol® ES during pregnancy. Lactation The effect of Lidothol® ES on breastfed infants has not been evaluated. Lidothol® ES has not been studied during lactation. Discuss with a physician prior to using Lidothol® ES while breastfeeding. Pediatric/Geriatric Use Safety and effectiveness in pediatric and geriatric patients have not been established.