Properties
What is it?
EMLA Registration number: PN014033/01 Trade name: EMLA International Nonproprietary or Group Name: Lidocaine + Prilocaine Dosage form: Cream for topical and external use Composition (per 1 g of cream) Active substance: Lidocaine 25.0 mg, Prilocaine 25.0 mg; Excipients: Macrogol glyceryl hydroxystearate (Arlatone 289) 19.0 mg, Carbomer 974P (Carboxypolymethylene) 10.0 mg, Sodium hydroxide 5.2 mg to adjust pH to 8.7-9.7, Purified water up to 1.0 g. Description: Homogeneous white cream. Pharmacotherapeutic group: Local anesthetic ATC code: N01BB20 Pharmacodynamics EMLA cream contains lidocaine and prilocaine as active components, which are amide-type local anesthetics. Skin anesthesia is achieved by the penetration of lidocaine and prilocaine into the epidermis and dermis. The quality of anesthesia depends on the dose of the preparation and the duration of application. Intact skin After applying EMLA cream for 1-2 hours to intact skin, the duration of anesthesia after removing the occlusive dressing is 2 hours. No difference was found in efficacy (including time to achieve analgesic effect) and safety of cream use on intact skin between elderly patients (65-96 years) and younger patients. EMLA cream is expected to cause temporary pallor or redness of the skin due to its effect on superficial blood vessels. Similar reactions in patients with generalized neurodermatitis (atopic dermatitis) may occur more rapidly, as early as 30-60 minutes after cream application, indicating faster penetration of the cream into the skin. For puncture biopsy (4 mm diameter), the use of EMLA cream provides adequate anesthesia of intact skin in 90% of patients 60 minutes after application for needle insertion at a depth of 2 mm and 120 minutes after application for needle insertion at a depth of 3 mm. The efficacy of EMLA cream is not dependent on skin color or pigmentation (skin types I-IV). When using combined vaccines against infections such as measles, rubella, mumps, or intramuscular combined vaccines against diphtheria, pertussis, tetanus, poliomyelitis, and Haemophilus influenza type b infections, as well as against hepatitis B, the use of EMLA cream did not affect the mean antibody titer, the rate of appearance or disappearance of specific antibodies in blood serum, or the number of patients who achieved protective or positive antibody titers after immunization. Mucous membrane of the genital organs Anesthesia of the mucous membrane of the genital organs is achieved faster compared to anesthesia of intact skin due to faster absorption of the preparation. In women, anesthesia of the mucous membrane of the genital organs is achieved 5-10 minutes after applying EMLA cream, which is sufficient to relieve pain caused by argon laser. The duration of anesthesia is 15-20 minutes (with individual variations from 5 to 45 minutes). Trophic ulcer of the lower extremities When treating trophic ulcers of the lower extremities, the duration of anesthesia after applying the cream is 4 hours. No negative impact of the preparation on the ulcer healing process or its relationship with bacterial flora was observed. Pharmacokinetics Systemic absorption of EMLA cream depends on the dose, duration of application, and thickness of the skin cover (depending on the body part), as well as other skin characteristics, such as skin disease and shaving. When applied to the ulcerated surface of the lower extremities, the absorption of the preparation may be influenced by the characteristics of the ulcer, such as its size (absorption increases with increasing ulcer surface area). Intact skin: In adults, after applying 60 g of cream to intact skin of the hip over an area of 400 cm2 (1.5 g per 10 cm2) for 3 hours, systemic absorption of lidocaine is approximately 3% and prilocaine is 5%. Absorption is slow. The maximum concentration of lidocaine (mean value 0.12 mcg/ml) and prilocaine (mean value 0.07 mcg/ml) in blood plasma was reached approximately 4 hours after cream application. The risk of toxic symptoms exists only when the concentration of the active substance in blood plasma is 5-10 mcg/ml. After applying EMLA cream to damaged skin 8-12 hours after shaving, the maximum plasma concentration of lidocaine and prilocaine is very low in both young and elderly patients and significantly below the level of potential toxicity. Trophic ulcer of the lower extremities: The time to reach maximum concentration of lidocaine (0.05-0.84 mcg/ml) and prilocaine (0.02-0.08 mcg/ml) in blood plasma is 1-2.5 hours after applying the preparation to the ulcerated surface (5-10 g of cream for 30 minutes). With repeated application of the cream to the ulcerated surface, no accumulation of prilocaine, lidocaine, or their metabolites in blood plasma was observed. EMLA cream in amounts of 2-10 g was applied to the ulcerated surface up to 62 cm2 for 30-60 minutes, 3 to 7 times a week (15 times a month). Mucous membrane of the genital organs: The time to reach maximum concentration of lidocaine and prilocaine in blood plasma (mean 0.18 mcg/ml and 0.15 mcg/ml, respectively) is approximately 35 minutes from the moment of application of the preparation to the vaginal mucous membrane (10 g of cream for 10 minutes). Indications for use In adults: • Superficial anesthesia of the skin during injections (including vaccinations), punctures, and vascular catheterization, and during superficial surgical interventions, including minor cosmetic procedures and epilation; • Superficial anesthesia during surgical treatment of trophic ulcers of the lower extremities (mechanical debridement), for example, removal of fibrin, pus, and necrotic tissue. • Superficial anesthesia of the mucous membrane of the genital organs during painful manipulations and for anesthesia before injection of local anesthetics. In children: • Superficial anesthesia of the skin during injections (including vaccinations), punctures, and vascular catheterization, and during superficial surgical interventions (including removal of molluscum contagiosum). Contraindications - Hypersensitivity to amide-type local anesthetics or any component of the preparation. - Premature newborns born before 37 weeks of gestation; - Newborns with a body weight less than 3 kg. Use with caution in glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, generalized neurodermatitis (atopic dermatitis), patients taking Class III antiarrhythmic drugs (e.g., amiodarone) (see section "Special Instructions"). Pregnancy and lactation Pregnancy There is insufficient data on the use of EMLA cream in pregnant women. Animal studies have not revealed direct or indirect adverse effects of the preparation on pregnancy, intrauterine fetal development, labor, or postnatal development. Lidocaine and prilocaine cross the placental barrier and may be absorbed by fetal tissues. There are no reports of specific reproductive process disorders, such as increased incidence of malformations or development of other direct or indirect adverse effects on the fetus. Lactation Lidocaine and prilocaine are excreted in breast milk in amounts that do not pose a risk to the infant when the preparation is used in therapeutic doses. Method of administration and dosage: For external use on the skin or mucous membrane. Adults Superficial anesthesia of intact skin Indications Dosage and method of application Duration of application For needle insertion, e.g., during vascular catheterization and blood sampling Apply half of a 5 g tube (approx. 2 g) thickly over a 10 cm2 area and cover with an occlusive dressing for 1 hour, maximum 5 hours For minor surgical manipulations, e.g., removal of molluscum contagiosum, wart removal, minor cosmetic procedures, and epilation Apply 1.5-2 g/10 cm2 thickly to the skin and cover with an occlusive dressing for 1 hour, maximum 5 hours On large areas of freshly shaved skin (in outpatient settings), including before epilation Maximum recommended dose 60 g, maximum recommended application area 600 cm2; apply thickly to the skin and cover with an occlusive dressing for 1 hour, maximum 5 hours For superficial procedures on large areas (in inpatient settings), e.g., skin grafting. Apply 1.5-2 g/10 cm2 thickly to the skin and cover with an occlusive dressing for 2 hours, maximum 5 hours Superficial anesthesia of trophic ulcers of the lower extremities For surgical treatment of trophic ulcers of the lower extremities (mechanical debridement): Single dose approximately 1-2 g/10 cm2; apply the cream thickly to the ulcerated surface, not exceeding 10 g per procedure. Apply an occlusive dressing. Duration of application: minimum 30 minutes. An opened tube of cream is intended for single use only; the tube with residual cream should be discarded after use on one patient. When treating ulcers where penetration of the preparation into the tissue is difficult, the application time can be extended to 60 minutes. Mechanical debridement must be started no later than 10 minutes after removing the cream. When manipulating trophic ulcers of the lower extremities, EMLA cream is used up to 15 times over 1-2 months without an increase in efficacy or incidence of local reactions. Superficial anesthesia of the genital organs: Skin of the genital organs: Anesthesia before injection of local anesthetics: Men: 1 g/10 cm2. Apply the cream thickly to the skin. Duration of application: 15 minutes. Women: 1-2 g/10 cm2. Apply the cream thickly to the skin. Duration of application: 60 minutes. Superficial anesthesia of the mucous membrane of the genital organs: For removal of condylomas and anesthesia before injection of local anesthetics: approximately 5-10 g of cream, depending on the area to be treated. Apply the cream to the entire surface of the mucous membrane, including folds of the mucous membrane. Occlusive dressing is not required. Duration of application: 5-10 minutes. The procedure should be performed immediately after removing the cream. Children Anesthesia during needle insertion, including for removal of molluscum contagiosum and other minor superficial surgical manipulations. Apply the cream thickly to the skin and cover with an occlusive dressing. The dose should correspond to the area to be treated and should not exceed 1 g of cream per 10 cm2. Age Application area Duration of application 0-3 months Maximum 10 cm2 (total 1 g of cream) (maximum daily dose) 1 hour (Important: not more than 1 hour). 3-12 months Maximum 20 cm2 (total 2 g of cream) 1 hour 1-6 years Maximum 100 cm2 (total 10 g of cream) 1 hour, maximum 4 hours 6-12 years Maximum 200 cm2 (total 20 g of cream) 1 hour, maximum 4 hours A 3.5 cm strip of EMLA cream corresponds to approximately 1 g dose. Increasing the application time reduces anesthesia. In children with atopic dermatitis, the application time should be reduced to 30 minutes. Apply the cream thickly to the skin and cover with an occlusive dressing. Recommendations for applying the preparation 1. Puncture the protective membrane of the aluminum tube using the threaded cap, dispense a sufficient amount of cream from the tube and apply to the area where the procedure is to be performed. For anesthesia of the skin cover, an occlusive dressing can be used (5x5 g is included in the package). 2. a) Take one occlusive dressing and remove its central part. b) Remove the paper backing from the back. For anesthesia of trophic ulcers of the lower extremities, use a PVC occlusive dressing. 3. Cover the applied cream with the dressing so that the cream remains thick and does not come out from under the dressing. Carefully adjust the edges of the dressing so that no cream leaks out. 4. When using the occlusive dressing included in the package, remove the paper frame. The application time of the preparation can be written on the dressing itself. 5. After the recommended time has elapsed, remove the dressing and residual cream. Side effects When applied to intact skin Frequent (>1%, <10%) Skin: Transient local reactions at the application site, such as pallor, redness, and swelling Uncommon (>0.1%, <1%) Skin: Mild burning, itching, and sensation of warmth at the moment of application (in the area of application of the preparation) Rare (<0.1%) General: Allergic reactions, in more severe cases - anaphylactic shock. Methemoglobinemia and/or cyanosis. Reaction at the site of application of the preparation, such as hemorrhagic rash or petechiae, especially in children with atopic dermatitis or molluscum contagiosum after prolonged application. Accidental contact with the eye causes corneal irritation. When applied to trophic ulcers of the lower extremities Frequent (>1%, <10%) Skin: Transient local reactions at the application site, such as pallor, redness, and swelling; mild burning, itching, and sensation of warmth at the moment of application (in the area of application of the preparation). Uncommon (>0.1%, <1%) Skin: Skin irritation (in the area of application of the preparation). Rare (<0.1%) General: Allergic reactions, in more severe cases - anaphylactic shock. Overdose Systemic toxic signs are unlikely to develop when maintaining the recommended dosage regimen of the preparation. Intoxication symptoms are expected, as with the use of other local anesthetics, such as central nervous system excitation, as well as severe cases of CNS and cardiac depression. In rare cases, clinically significant methemoglobinemia has been reported. Prilocaine in high doses causes an increase in methemoglobin content. Superficial application of 125 mg of prilocaine over 5 hours caused a moderate increase in methemoglobinemia in a 3-month-old infant. Superficial application of lidocaine at a dose of 8.6-17.2 mg/kg caused severe intoxication in newborns. Treatment Severe neurological symptoms (convulsions, central nervous system depression) require symptomatic treatment, including administration of anticonvulsants and, if necessary, artificial ventilation of the lungs. In case of methemoglobinemia, the antidote is methylthionine chloride (methylene blue). Due to the slow systemic absorption of the preparation, patients should be monitored for several hours after starting intoxication treatment. Interaction with other medicinal products and other types of interaction Patients taking drugs that induce methemoglobinemia (e.g., sulfa-containing drugs) may experience an increase in blood methemoglobin concentration with EMLA cream. When treating with other local anesthetics and structurally similar preparations (including tocainide), the risk of potentiation of systemic effects should be considered when using high doses of EMLA cream. No specific studies have been conducted to assess the interaction of lidocaine/prilocaine with Class III antiarrhythmic drugs; caution should be exercised when using the preparations simultaneously. Pharmaceutical interactions: Not established. Preparations that reduce lidocaine clearance (e.g., cimetidine or beta-blockers) may lead to potentially toxic concentrations of lidocaine in plasma with repeated high-dose use over a prolonged period. This interaction is not clinically significant with short-term therapy with lidocaine (e.g., EMLA cream) at recommended doses. Special instructions Patients with glucose-6-phosphate dehydrogenase deficiency or congenital or idiopathic methemoglobinemia are more susceptible to drug-induced methemoglobinemia. The efficacy of cream use in newborns during heel blood sampling procedures has not been established. Caution should be exercised when applying EMLA cream around the eyes, as the preparation causes eye irritation. The loss of protective reflexes may lead to corneal irritation or damage. In case of accidental contact with the eye, the eye should be immediately washed with water or 0.9% sodium chloride solution, and the eye should be protected until protective reflexes are restored. Caution must be exercised when applying the preparation to the skin in atopic dermatitis; the application time may be reduced (15-30 minutes). The efficacy and safety of EMLA cream use in children up to 3 months of age have been determined after a single dose application. In such infants, a temporary increase in blood methemoglobin content lasting up to 13 hours has often been observed after cream application. However, the increase in blood methemoglobin content is not clinically significant. Patients taking Class III antiarrhythmic drugs (e.g., amiodarone) should be under constant observation and ECG monitoring, as effects on cardiac function are possible. EMLA cream must not be applied to a perforated tympanic membrane or in other cases where there is a possibility of cream entering the middle ear. Do not apply the cream to open wounds. Due to insufficient data on absorption, it is not recommended to apply the cream to the mucous membrane of the genital organs in children. Lidocaine and prilocaine at concentrations above 0.5-2% have bactericidal and antiviral properties. Therefore, special attention should be paid to the use of live vaccines subcutaneously (e.g., BCG) when using the cream. Due to lack of data, simultaneous use of EMLA cream and preparations that cause methemoglobinemia is not recommended in children aged 0 to 12 months. Effect on ability to drive and operate machinery Does not affect the ability to drive and operate machinery. Dosage form Cream for topical and external use (aluminum tube) 5 g and 30 g. 5 g aluminum tube, sealed with an aluminum membrane and closed with a screw cap. 1 tube or 5 tubes with occlusive dressings and instructions for use are placed in a cardboard box, with a cardboard divider, with/without first opening control. 30 g aluminum tube, sealed with an aluminum membrane and closed with a screw cap. 1 tube with instructions for use is placed in a cardboard box, with/without first opening control. Shelf life 3 years. Do not use after the expiry date indicated on the packaging. Storage conditions Store below 30°C, out of reach of children. Do not freeze. Dispensing category Pharmaceutical product group III, available without prescription.