Data from FDA - Curated by EPG Health - Last updated 22 August 2017

Indication(s)

INDICATIONS AND USAGE Lidocaine and prilocaine cream USP, 2.5%/2.5% (a eutectic mixture of lidocaine 2.5% and prilocaine 2.5%) is indicated as a topical anesthetic for use on: • normal intact skin for local analgesia. • genital mucous membranes for superficial minor surgery and as pretreatment for infiltration anesthesia. Lidocaine and prilocaine cream is not recommended in any clinical situation in which penetration or migration beyond the tympanic membrane into the middle ear is possible because of the ototoxic effects observed in animal studies (see WARNINGS).

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Advisory information

contraindications
CONTRAINDICATIONS Lidocaine and prilocaine cream 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.
Special warnings and precautions
PRECAUTIONS General: Repeated doses of lidocaine and prilocaine cream may increase blood levels of lidocaine and prilocaine. Lidocaine and prilocaine cream should be used with caution in patients who may be more sensitive to the systemic effects of lidocaine and prilocaine including acutely ill, debilitated, or elderly patients. Lidocaine and prilocaine cream should not be applied to open wounds. Care should be taken not to allow lidocaine and prilocaine cream to come in contact with the eye because animal studies have demonstrated severe eye irritation. Also the loss of protective reflexes can permit corneal irritation and potential abrasion. Absorption of lidocaine and prilocaine cream in conjunctival tissues has not been determined. If eye contact occurs, immediately wash out the eye with water or saline and protect the eye until sensation returns. Patients allergic to paraaminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross sensitivity to lidocaine and/or prilocaine, however, lidocaine and prilocaine cream should be used with caution in patients with a history of drug sensitivities, especially if the etiologic agent is uncertain. Patients with severe hepatic disease, because of their inability to metabolize local anesthetics normally, are at greater risk of developing toxic plasma concentrations of lidocaine and prilocaine. Lidocaine and prilocaine have been shown to inhibit viral and bacterial growth. The effect of lidocaine and prilocaine cream on intradermal injections of live vaccines has not been determined. Information for Patients When lidocaine and prilocaine cream is used, the patient should be aware that the production of dermal analgesia may be accompanied by the block of all sensations in the treated skin. For this reason, the patient should avoid inadvertent trauma to the treated area by scratching, rubbing, or exposure to extreme hot or cold temperatures until complete sensation has returned. Lidocaine and prilocaine cream should not be applied near the eyes or on open wounds. Drug Interactions Lidocaine and prilocaine cream 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. Prilocaine may contribute to the formation of methemoglobin in patients treated with other drugs known to cause this condition (see Methemoglobinemia subsection of WARNINGS). Specific interaction studies with lidocaine/prilocaine and class III anti-arrhythmic drugs (e.g., amiodarone, bretylium, sotalol, dofetilide) have not been performed, but caution is advised (see WARNINGS). Should lidocaine and prilocaine cream be used concomitantly with other products containing lidocaine and/or prilocaine, cumulative doses from all formulations must be considered. Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis: Long-term studies in animals designed to evaluate the carcinogenic potential of lidocaine and prilocaine have not been conducted. Metabolites of prilocaine have been shown to be carcinogenic in laboratory animals. In the animal studies reported below, doses or blood levels are compared to the Single Dermal Administration (SDA) of 60 g of lidocaine and prilocaine cream to 400 cm2 for 3 hours to a small person (50 kg). The typical application of lidocaine and prilocaine cream for one or two treatments for venipuncture sites (2.5 or 5 g) would be 1/24 or 1/12 of that dose in an adult or about the same mg/kg dose in an infant. Chronic oral toxicity studies of ortho-toluidine, a metabolite of prilocaine, in mice (450 to 7,200 mg/m2; 60 to 960 times SDA) and rats (900 to 4,800 mg/m2; 60 to 320 times SDA) have shown that ortho-toluidine is a carcinogen in both species. The tumors included hepatocarcinomas/adenomas in female mice, multiple occurrences of hemangiosarcomas/hemangiomas in both sexes of mice, sarcomas of multiple organs, transitional-cell carcinomas/papillomas of urinary bladder in both sexes of rats, subcutaneous fibromas/fibrosarcomas and mesotheliomas in male rats, and mammary gland fibroadenomas/adenomas in female rats. The lowest dose tested (450 mg/m2 in mice,900 mg/m2 in rats, 60 times SDA) was carcinogenic in both species. Thus the no-effect dose must be less than 60 times SDA. The animal studies were conducted at 150 to 2,400 mg/kg in mice and at 150 to 800 mg/kg in rats. The dosages have been converted to mg/m2 for the SDA calculations above. Mutagenesis: The mutagenic potential of lidocaine HCl has been tested in a bacterial reverse (Ames) assay in Salmonella, an in vitro chromosomal aberration assay using human lymphocytes and in an in vivo micronucleus test in mice. There was no indication of mutagenicity or structural damage to chromosomes in these tests. Ortho-toluidine, a metabolite of prilocaine, at a concentration of 0.5 mcg/mL was genotoxic in Escherichia coli DNA repair and phage-induction assays. Urine concentrates from rats treated with ortho-toluidine (300 mg/kg orally; 300 times SDA) were mutagenic when examined in Salmonella typhimurium in the presence of metabolic activation. Several other tests on ortho-toluidine, including reverse mutations in five different Salmonella typhimurium strains in the presence or absence of metabolic activation and a study to detect single strand breaks in DNA of V79 Chinese hamster cells, were negative. Impairment of Fertility: See Use in Pregnancy. Use in Pregnancy: Teratogenic Effects: Pregnancy Category B. Reproduction studies with lidocaine have been performed in rats and have revealed no evidence of harm to the fetus (30 mg/kg subcutaneously; 22 times SDA). Reproduction studies with prilocaine have been performed in rats and have revealed no evidence of impaired fertility or harm to the fetus (300 mg/kg intramuscularly; 188 times SDA). There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, lidocaine and prilocaine cream should be used during pregnancy only if clearly needed. Reproduction studies have been performed in rats receiving subcutaneous administration of an aqueous mixture containing lidocaine HCl and prilocaine HCl at 1:1 (w/w). At 40 mg/kg each, a dose equivalent to 29 times SDA lidocaine and 25 times SDA prilocaine, no teratogenic, embryotoxic or fetotoxic effects were observed. Labor and Delivery Neither lidocaine nor prilocaine are contraindicated in labor and delivery. Should lidocaine and prilocaine cream be used concomitantly with other products containing lidocaine and/or prilocaine, cumulative doses from all formulations must be considered. Nursing Mothers Lidocaine, and probably prilocaine, are excreted in human milk. Therefore, caution should be exercised when lidocaine and prilocaine cream is administered to a nursing mother since the milk: plasma ratio of lidocaine is 0.4 and is not determined for prilocaine. Pediatric Use Controlled studies of lidocaine and prilocaine cream in children under the age of seven years have shown less overall benefit than in older children or adults. These results illustrate the importance of emotional and psychological support of younger children undergoing medical or surgical procedures. Lidocaine and prilocaine cream should be used with care in patients with conditions or therapy associated with methemoglobinemia (see Methemoglobinemia subsection of WARNINGS). When using lidocaine and prilocaine cream in young children, especially infants under the age of 3 months, care must be taken to insure that the caregiver understands the need to limit the dose and area of application, and to prevent accidental ingestion (see DOSAGE AND ADMINISTRATION and Methemoglobinemia). In neonates (minimum gestation: 37 weeks) and children weighing less than 20 kg, the area and duration of application should be limited (see TABLE 2 in Individualization of Dose). Studies have not demonstrated the efficacy of lidocaine and prilocaine cream for heel lancing in neonates. Geriatric Use Of the total number of patients in clinical studies of lidocaine and prilocaine cream, 180 were age 65 to 74 and 138 were 75 and over. No overall differences in safety or efficacy were observed between these patients and younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Plasma levels of lidocaine and prilocaine in geriatric and non-geriatric patients following application of a thick layer of lidocaine and prilocaine cream are very low and well below potentially toxic levels. However, there are no sufficient data to evaluate quantitative differences in systemic plasma levels of lidocaine and prilocaine between geriatric and non-geriatric patients following application of lidocaine and prilocaine cream. Consideration should be given for those elderly patients who have enhanced sensitivity to systemic absorption. (See PRECAUTIONS.) After intravenous dosing, the elimination half-life of lidocaine is significantly longer in elderly patients (2.5 hours) than in younger patients (1.5 hours). (See CLINICAL PHARMACOLOGY.)
Adverse reactions
ADVERSE REACTIONS Localized Reactions: During or immediately after treatment with lidocaine and prilocaine cream on intact skin, the skin at the site of treatment may develop erythema or edema or may be the locus of abnormal sensation. Rare cases of discrete purpuric or petechial reactions at the application site have been reported. Rare cases of hyperpigmentation following the use of lidocaine and prilocaine cream have been reported. The relationship to lidocaine and prilocaine cream or the underlying procedure has not been established. In clinical studies on intact skin involving over 1,300 lidocaine and prilocaine cream-treated subjects, one or more such local reactions were noted in 56% of patients, and were generally mild and transient, resolving spontaneously within 1 or 2 hours. There were no serious reactions which were ascribed to lidocaine and prilocaine cream. Two recent reports describe blistering on the foreskin in neonates about to undergo circumcision. Both neonates received 1.0 g of lidocaine and prilocaine cream. In patients treated with lidocaine and prilocaine cream on intact skin, local effects observed in the trials included: paleness (pallor or blanching) 37%, redness (erythema) 30%, alterations in temperature sensations 7%, edema 6%, itching 2% and rash, less than 1%. In clinical studies on genital mucous membranes involving 378 lidocaine and prilocaine cream-treated patients, one or more application site reactions, usually mild and transient, were noted in 41% of patients. The most common application site reactions were redness (21%), burning sensation (17%) and edema (10%). Allergic Reactions: Allergic and anaphylactoid reactions associated with lidocaine or prilocaine can occur. They are characterized by urticaria, angioedema, bronchospasm, and shock. If they occur they should be managed by conventional means. The detection of sensitivity by skin testing is of doubtful value. Systemic (Dose Related) Reactions: Systemic adverse reactions following appropriate use of lidocaine and prilocaine cream are unlikely due to the small dose absorbed (see Pharmacokinetics subsection of CLINICAL PHARMACOLOGY). Systemic adverse effects of lidocaine and/or prilocaine 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, 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.

Usage information

Dosing and administration
DOSAGE AND ADMINISTRATION Adult Patients-Intact Skin: A thick layer of lidocaine and prilocaine cream is applied to intact skin and covered with an occlusive dressing (see INSTRUCTIONS FOR APPLICATION). Minor Dermal Procedures: For minor procedures such as intravenous cannulation and venipuncture, apply 2.5 grams of lidocaine and prilocaine cream (1/2 the 5 g tube) over 20 to 25 cm2 of skin surface for at least 1 hour. In controlled clinical trials using lidocaine and prilocaine cream, two sites were usually prepared in case there was a technical problem with cannulation or venipuncture at the first site. Major Dermal Procedures: For more painful dermatological procedures involving a larger skin area such as split thickness skin graft harvesting, apply 2 grams of lidocaine and prilocaine cream per 10 cm2 of skin and allow to remain in contact with the skin for at least 2 hours. Adult Male Genital Skin: As an adjunct prior to local anesthetic infiltration, apply a thick layer of lidocaine and prilocaine cream (1 g/10 cm2) to the skin surface for 15 minutes. Local anesthetic infiltration should be performed immediately after removal of lidocaine and prilocaine cream. Dermal analgesia can be expected to increase for up to 3 hours under occlusive dressing and persist for 1 to 2 hours after removal of the cream. The amount of lidocaine and prilocaine absorbed during the period of application can be estimated from the information in TABLE 2, ** footnote, in Individualization of Dose. Adult Female Patients-Genital Mucous Membranes: For minor procedures on the female external genitalia, such as removal of condylomata acuminata, as well as for use as pretreatment for anesthetic infiltration, apply a thick layer (5 to 10 grams) of lidocaine and prilocaine cream for 5 to 10 minutes. Occlusion is not necessary for absorption, but may be helpful to keep the cream in place. Patients should be lying down during the lidocaine and prilocaine cream application, especially if no occlusion is used. The procedure or the local anesthetic infiltration should be performed immediately after the removal of lidocaine and prilocaine cream. Pediatric Patients-Intact Skin: The following are the maximum recommended doses, application areas and application times for lidocaine and prilocaine cream based on a child's age and weight: Age and Body Weight Requirements Maximum Total Dose of Lidocaine and Prilocaine Cream Maximum Application Area Maximum Application Time 0 up to 3 months or < 5 kg 1 g 10 cm2 1 hour 3 up to 12 months and > 5 kg 2 g 20 cm2 4 hours 1 to 6 years and > 10 kg 10 g 100 cm2 4 hours 7 to 12 years and > 20 kg 20 g 200 cm2 4 hours Please note: If a patient greater than 3 months old does not meet the minimum weight requirement, the maximum total dose of lidocaine and prilocaine cream should be restricted to that which corresponds to the patient's weight (see INSTRUCTIONS FOR APPLICATION). Practitioners should carefully instruct caregivers to avoid application of excessive amounts of lidocaine and prilocaine cream (see PRECAUTIONS). When applying lidocaine and prilocaine cream to the skin of young children, care must be taken to maintain careful observation of the child to prevent accidental ingestion of lidocaine and prilocaine cream, or the occlusive dressing. A secondary protective covering to prevent inadvertent disruption of the application site may be useful. Lidocaine and prilocaine cream should not be used in neonates with a gestational age less than 37 weeks nor in infants under the age of twelve months who are receiving treatment with methemoglobin-inducing agents (see Methemoglobinemia subsection of WARNINGS). When lidocaine and prilocaine cream is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered (see Individualization of Dose). The amount absorbed in the case of lidocaine and prilocaine cream is determined by the area over which it is applied and the duration of application under occlusion (see TABLE 2, ** footnote, in Individualization of Dose). Although the incidence of systemic adverse reactions with lidocaine and prilocaine cream is very low, caution should be exercised, particularly when applying it over large areas and leaving it on for longer than 2 hours. The incidence of systemic adverse reactions can be expected to be directly proportional to the area and time of exposure (see Individualization of Dose). INSTRUCTIONS FOR APPLICATION To measure 1 gram of lidocaine and prilocaine cream, the cream should be gently squeezed out of the tube as a narrow strip that is 1.5 inches (3.8 cm) long and 0.2 inches (5 mm) wide. The strip of lidocaine and prilocaine cream should be contained within the lines of the diagram shown below. ≈ 1 g strip 1.5 x 0.2 inches Use the number of strips that equals your dose, like the examples in the table below. Dosing Information 1 gram = 1 strip 2 grams = 2 strips 2.5 grams = 2.5 strips For adult and pediatric patients, apply ONLY as prescribed by your physician. If your child is below the age of 3 months or small for their age, please inform your doctor before applying lidocaine and prilocaine cream, which can be harmful, if applied over too much skin at one time in young children. When applying lidocaine and prilocaine cream to the intact skin of young children, it is important that they be carefully observed by an adult in order to prevent the accidental ingestion of or eye contact with lidocaine and prilocaine cream. Lidocaine and prilocaine cream must be applied to intact skin at least 1 hour before the start of a routine procedure and for 2 hours before the start of a painful procedure. A protective covering of the cream is not necessary for absorption but may be helpful to keep the cream in place. If using a protective covering, your doctor will remove it, wipe off the lidocaine and prilocaine cream, and clean the entire area with an antiseptic solution before the procedure. The duration of effective skin anesthesia will be at least 1 hour after removal of the protective covering. PRECAUTIONS: 1. Do not apply near eyes or on open wounds. 2. Keep out of reach of children. 3. If your child becomes very dizzy, excessively sleepy, or develops duskiness of the face or lips after applying lidocaine and prilocaine cream, remove the cream and contact your physician at once. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Pregnancy and lactation
Nursing Mothers Lidocaine, and probably prilocaine, are excreted in human milk. Therefore, caution should be exercised when lidocaine and prilocaine cream is administered to a nursing mother since the milk: plasma ratio of lidocaine is 0.4 and is not determined for prilocaine.

Interactions

Drug Interactions Lidocaine and prilocaine cream 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. Prilocaine may contribute to the formation of methemoglobin in patients treated with other drugs known to cause this condition (see Methemoglobinemia subsection of WARNINGS). Specific interaction studies with lidocaine/prilocaine and class III anti-arrhythmic drugs (e.g., amiodarone, bretylium, sotalol, dofetilide) have not been performed, but caution is advised (see WARNINGS). Should lidocaine and prilocaine cream be used concomitantly with other products containing lidocaine and/or prilocaine, cumulative doses from all formulations must be considered.

More information

Category Value
Agency product number 98PI200987
Orphan designation No
Product NDC 76420-313
Date Last Revised 08-03-2017
Type HUMAN PRESCRIPTION DRUG
RXCUI 197877
Marketing authorisation holder Asclemed USA, Inc.