Lidocan V

Lidocan™ V 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.

• 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 Lidocan™ V 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 lidocaine patch 5% 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 5%, although the risk with this formulation has not been evaluated.
• It is important for patients to store and dispose of Lidocan™ IV out of the reach of children, pets, and others (see HANDLING AND DISPOSAL).
• Excessive Dosing Excessive dosing by applying Lidocan™ V 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 lidocaine patch 5%, 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.
• General 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, Lidocan™ V should be used with caution in patients with a history of drug sensitivities, especially if the etiologic agent is uncertain.
• Non-intact Skin Application to broken or inflamed skin, although not tested, may result in higher blood concentrations of lidocaine from increased absorption.
• Lidocan™ V is only recommended for use on intact skin.
• External Heat Sources Placement of external heat sources, such as heating pads or electric blankets, over lidocaine patch 5% is not recommended as this has not been evaluated and may increase plasma lidocaine levels.
• Eye Exposure The contact of Lidocan™ V with eyes, although not studied, should be avoided based on the findings of severe eye irritation 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.
• Information for Patients Methemoglobinemia Inform patients that use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly.
• Drug Interactions Antiarrhythmic Drugs - Lidocan™ V should be used with caution in patients receiving Class I antiarrhythmic drugs (such as tocainide and mexiletine) since the toxic effects are additive and potentially synergistic.
• Drug 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 negligible following application of Lidocan™ V .
• Mutagenesis Lidocaine HCl is not mutagenic in Salmonella/mammalian microsome test nor clastogenic in chromosome aberration assay with human lymphocytes and mouse micronucleus test.
• Impairment of Fertility The effect of lidocaine on fertility has not been studied.
• Pregnancy Teratogenic Effects Pregnancy Category B.
• Labor and Delivery Lidocan™ V has not been studied in labor and delivery.
• Lidocaine is not contraindicated in labor and delivery.
• Should Lidocan™ V be used concomitantly with other products containing lidocaine, total doses contributed by all formulations must be considered.
• Nursing Mothers Lidocan™ V has not been studied in nursing mothers.
• Pediatric Use Safety and effectiveness in pediatric patients have not been established.
• General 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, Lidocan™ V should be used with caution in patients with a history of drug sensitivities, especially if the etiologic agent is uncertain.
• Non-intact Skin Application to broken or inflamed skin, although not tested, may result in higher blood concentrations of lidocaine from increased absorption.
• Lidocan™ V is only recommended for use on intact skin.
• External Heat Sources Placement of external heat sources, such as heating pads or electric blankets, over lidocaine patch 5% is not recommended as this has not been evaluated and may increase plasma lidocaine levels.
• Eye Exposure The contact of Lidocan™ V with eyes, although not studied, should be avoided based on the findings of severe eye irritation 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.

• Teratogenic Effects Pregnancy Category B.
• Lidocan™ V has not been studied in pregnancy.
• Reproduction studies with lidocaine have been performed in rats at doses up to 30 mg/kg subcutaneously and have revealed no evidence of harm to the fetus due to lidocaine.
• There are, however, no adequate and well-controlled studies in pregnant women.
• Because animal reproduction studies are not always predictive of human response, Lidocan™ V should be used during pregnancy only if clearly needed.
• Lidocan™ V has not been studied in nursing mothers. Lidocaine is excreted in human milk, and the milk:plasma ratio of lidocaine is 0.4. Caution should be exercised when Lidocan™ V is administered to a nursing woman.

• Antiarrhythmic Drugs - Lidocan™ V should be used with caution in patients receiving Class I antiarrhythmic drugs (such as tocainide and mexiletine) since the toxic effects are additive and potentially synergistic.
• Local Anesthetics - When Lidocan™ V is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered.
• Drugs That May Cause Methemoglobinemia When Used with Lidocan™ V Patients who are administered local anesthetics are at increased risk of developing methemoglobinemia when concurrently exposed to the following drugs, which could include other local anesthetics:
• Examples of Drugs Associated with Methemoglobinemia:
• Drug

• 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 50 of 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.