Emla cream for local and external use 30g

Pharmacological properties of the drug Emla

EMLA cream contains lidocaine and prilocaine, amide-type local anesthetics. Due to the penetration of lidocaine and prilocaine into the layers of the epidermis and dermis, skin anesthesia occurs. The degree of anesthesia depends on the time of application and dose. Intact skin When EMLA cream is applied to intact skin for 1–2 hours, anesthesia lasts about 2 hours after removing the occlusive sticker. There were no differences in efficacy (including time to achieve analgesic effect) and safety when applied to intact skin between young and elderly patients. Due to the effect of the cream on the superficial vessels, temporary pallor or redness of the skin area is possible. Vasomotor reactions develop faster (already 30–60 minutes after applying the cream) in patients with widespread neurodermatitis (atopic neurodermatitis), which indicates a faster penetration of the cream through the changed skin. During a puncture biopsy (up to 4 mm in diameter), the use of the cream provides adequate anesthesia of intact skin in 90% of patients 60 minutes after applying the cream when the needle is inserted into the skin to a depth of 2 mm and after 120 minutes - to a depth of 3 mm. The effectiveness of the cream does not depend on the color and pigmentation of the skin (skin types I–IV). The cream can be used for pain relief before vaccination when administering the vaccine subcutaneously or intramuscularly. Genital mucosa The anesthetic effect of the mucous membrane appears earlier, since absorption occurs faster than in cases of application to intact skin. In women, after applying EMLA cream to the mucous membrane of the genital organs, after 5–10 minutes an analgesic effect is achieved that is sufficient for manipulations using an argon laser. The duration of anesthesia is 15–20 minutes (taking into account individual characteristics - from 5 to 45 minutes). Trophic ulcers of the lower extremities After applying the cream when treating trophic ulcers of the lower extremities, the duration of the analgesic effect is about 4 hours. The cream does not have a negative effect on the wound healing process and bacterial flora. Systemic absorption depends on the amount of cream, duration of application, skin thickness (which varies in different areas of the body) and other skin characteristics. Intact skin In adults, after applying 60 g of EMLA cream to 400 cm2 of intact skin on the thigh (1.5 g per 10 cm2) over 3 hours, systemic absorption was 3% for lidocaine and 5% for prilocaine. Absorption occurs slowly. At the above dose, the maximum plasma concentration of lidocaine (average 0.12 mcg/ml) and prilocaine (average 0.07 mcg/ml) was achieved approximately 4 hours after application. The risk of developing toxic symptoms exists only at doses of 5–10 mcg/ml. Trophic ulcers of the lower extremities After applying 5–10 g of EMLA cream to trophic ulcers with an exposure of 30 minutes, the maximum levels of lidocaine and prilocaine in the blood plasma were achieved after 1–2.5 hours (lidocaine concentration in the range of 0.05–0.84 μg/ml , prilocaine - 0.02–0.08 mcg/ml). After repeated application of EMLA cream to trophic ulcers, no significant accumulation of lidocaine, prilocaine or their metabolites in the blood plasma was noted (EMLA cream was applied at a dose of 2–10 g for 30–60 min to an area of ​​62 cm2 15 times a month for 3–7 sessions per week). Genital mucosa The maximum plasma concentration is achieved approximately 35 minutes after applying 10 g of EMLA cream to the vaginal mucosa with an exposure of 10 minutes (the average concentration of lidocaine was 0.18 mcg/ml; prilocaine - 0.15 mcg/ml) .

Emla cream for local and external use 30g

Compound

For 1 g of cream, active ingredients: lidocaine 25.0 mg, prilocaine 25.0 mg;
excipients: macrogol glyceryl hydroxystearate (ARLATON 289) 19.0 mg, carbomer 974 P (carboxypolymethylene) 10.0 mg, sodium hydroxide 5.2 mg to bring the pH to 8.7 -9.7, purified water to 1.0 g .

Pharmacokinetics

Systemic absorption of EMLA cream depends on the dose, duration of application and thickness of the skin (depending on the body area), as well as other skin characteristics such as skin diseases and shaving. When applied to the ulcerative surface of the lower extremities, the absorption of the drug may be influenced by the characteristics of the ulcers, for example, the size (with an increase in the area of ​​the ulcer, absorption increases).

Intact skin: In adults, after applying 60 g of cream to an area of ​​400 cm2 of intact thigh skin (1.5 g per 10 cm2) for 3 hours, systemic absorption for lidocaine was approximately 3% and for prilocaine 5%.

Absorption is slow. The maximum concentration of lidocaine (average value 0.12 μg/ml) and prilocaine (average value 0.07 μg/ml) in blood plasma was reached approximately 4 hours after application of the cream. The risk of toxic symptoms exists only when the concentration of active substances in the blood plasma is 5-10 mcg/ml. When EMLA cream is applied to intact skin 8-12 hours after shaving, the maximum plasma concentration of lidocaine and prilocaine in both young and elderly patients is very low and well below possible toxic levels.

Trophic ulcers of the lower extremities: The time to reach the maximum concentration of lidocaine (0.05-0.84 mcg/ml) and prilocaine (0.02-0.08 mcg/ml) in the blood plasma is 1-2.5 hours from the moment of application of the drug on the ulcer surface (5 - 10 g of cream for 30 minutes). With repeated application of the cream to the ulcerative surface, there was no accumulation of prilocaine, lidocaine or their metabolites in the blood plasma. 2-10 g of EMLA cream were applied to the ulcer surface with an area of ​​up to 62 cm2 for 30-60 minutes from 3 to 7 times a week (15 times within a month).

Genital mucosa: The time to reach the maximum concentration of lidocaine and prilocaine in the blood plasma (on average 0.18 mcg/ml and 0.15 mcg/ml, respectively) is approximately 35 minutes from the moment the drug is applied to the vaginal mucosa (10 g of cream for 10 min).

Indications for use

In adults:
-superficial anesthesia of the skin during punctures (including vaccinations), punctures and catheterization of blood vessels and superficial surgical interventions, including minor cosmetic procedures and hair removal;

-superficial anesthesia of trophic ulcers of the lower extremities during surgical treatment (mechanical cleaning), for example, to remove fibrin, pus and necrotic tissue;

-superficial anesthesia of the mucous membrane of the genital organs before painful manipulations and for pain relief before injections of local anesthetics.

In children:

— superficial anesthesia of the skin during injections (including vaccinations), punctures and catheterization of blood vessels and superficial surgical interventions (including removal of molluscum contagiosum).

Contraindications

- Hypersensitivity to amide-type local anesthetics or any other component of the drug; - premature newborns born at a gestational age of less than 37 weeks; - newborns weighing less than 3 kg.

With caution: Glucose-6-phosphate dehydrogenase deficiency, hereditary or idiopathic methemoglobinemia, common neurodermatitis (atopic dermatitis), patients taking class III antiarrhythmic drugs (for example, amiodarone) (see section “Special Instructions”).

Directions for use and doses

Externally, on the skin or mucous membrane.

Adults. Superficial anesthesia of intact skin

Superficial anesthesia of trophic ulcers of the lower extremities: During surgical treatment (mechanical cleaning) of trophic ulcers of the lower extremities: a single dose of about 1-2 g/10 cm2; Apply the cream in a thick layer to the ulcer surface, no more than 10 g of cream per procedure. Apply an occlusive dressing. Application time: minimum 30 min. An opened tube of cream is intended for single use; the tube with any remaining cream should be discarded after use on one patient. In the case of treating ulcers, into the tissues of which penetration of the drug is difficult, the duration of application can be increased to 60 minutes. Mechanical cleaning must begin no later than 10 minutes after removing the cream.

When manipulating ulcers of the lower extremities, EMLA cream was used up to 15 times over 1-2 months without reducing the effectiveness and increasing the incidence of local reactions. Superficial anesthesia of the genital organs: Skin of the genital organs: Anesthesia before injections of local anesthetics: Men: 1 g/10 cm2. Apply the cream in a thick layer to the skin. Application time: 15 min. Women: 1-2 g/10 cm2. Apply the cream in a thick layer to the skin. Application time: 60 min. Superficial anesthesia of the genital mucosa: When removing condylomas and for pain relief before injections of local anesthetics: approximately 5-10 g of cream, depending on the area of ​​the treated surface. The cream should be applied to the entire surface of the mucous membrane, including the folds of the mucous membrane. No occlusive dressing is required. Application time: 5-10 min. Carry out the procedure immediately after removing the cream.

Children Pain relief during needle insertion (including vaccination), curettage of molluscum contagiosum and other minor superficial surgical procedures. Apply the cream in a thick layer to the skin and cover with an occlusive dressing. The dose should correspond to the surface being treated and should not exceed 1 g of cream per 10 cm.

Storage conditions

Store at temperatures below 30°C, out of the reach of children. Do not freeze.

Best before date

3 years. Do not use after the expiration date stated on the package.

special instructions

Patients with glucose-6-phosphate dehydrogenase deficiency or hereditary or idiopathic methemoglobinemia are more susceptible to drug-dependent methemoglobinemia. The effectiveness of using the cream in newborns during the procedure of taking blood samples from the heel has not been established. Caution should be used when applying EMLA cream around the eyes as the drug causes eye irritation.

Elimination of protective reflexes can cause irritation or damage to the cornea. If the cream gets into your eyes, immediately rinse your eyes with water or 0.9% sodium chloride solution and protect your eyes until protective reflexes are restored. Caution must be exercised when applying the drug to the skin with atopic dermatitis; Application time should be reduced (15-30 minutes).

In children under 3 months of age, the safety and effectiveness of EMLA cream was determined after a single dose. In such children, after applying the cream, a temporary increase in the level of methemoglobin in the blood was often observed, lasting up to 13 hours. However, the observed increase in blood methemoglobin levels is probably not clinically significant. Patients taking class III antiarrhythmic drugs (for example, amiodarone) should be under constant monitoring and ECG monitoring, because Possible effect on cardiac activity.

EMLA cream should not be applied to a damaged eardrum or in other cases of possible penetration of the cream into the middle ear.

The cream should not be applied to open wounds. Due to the lack of data on the absorption of the drug, it is not recommended to apply the cream to the genital mucosa in children. Lidocaine and prilocaine in concentrations above 0.5-2% have bactericidal and antiviral properties.

In this regard, it is recommended to take special care when applying the cream before subcutaneous administration of a live vaccine (for example, BCG). Due to the lack of data, the combined use of EMLA cream and drugs that cause methemoglobinemia is not recommended in children aged 0 to 12 months.

Description

Homogeneous white cream.

Conditions for dispensing from pharmacies

Over the counter

Dosage form

Cream for local and external use.

Manufacturer and organization accepting consumer complaints

AstraZeneca AB

Pharmacodynamics

EMLA cream contains lidocaine and prilocaine, which are amide-type local anesthetics, as active ingredients. Skin anesthesia is caused by the penetration of lidocaine and prilocaine into the layers of the epidermis and dermis. The degree of anesthesia depends on the dose of the drug and the duration of application.

Intact skin. After applying EMLA cream to intact skin for 1-2 hours, the duration of anesthesia after removing the occlusive dressing is 2 hours. There were no differences in efficacy (including time to achieve analgesic effect) and safety when applying the cream to intact skin between elderly (65-96 years) and younger patients. Due to the effect of EMLA cream on superficial vessels, temporary paleness or redness of the skin is possible. Similar reactions in patients with widespread neurodermatitis (atopic dermatitis) may occur faster, within 30-60 minutes after applying the cream, which indicates faster penetration of the cream through the skin.

For puncture biopsy (4 mm in diameter), the use of EMLA cream provides adequate anesthesia of intact skin in 90% of patients 60 minutes after application of the cream when the needle is inserted to a depth of 2 mm and after 120 minutes when the needle is inserted to a depth of 3 mm. The effectiveness of EMLA cream does not depend 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, whooping cough, tetanus, polio and infection caused by Haemophilius influenzae type B, as well as vaccination against hepatitis B, the use of EMLA cream had no effect on the average antibody titer, the rate of appearance or disappearance of specific antibodies in the blood serum, or the number of patients who achieved a protective or positive antibody titer after immunization. Genital mucosa Anesthesia of the genital mucosa is achieved more quickly compared to anesthesia of intact skin due to faster absorption of the drug.

In women, 5-10 minutes after applying EMLA cream to the mucous membrane of the genital organs, anesthesia sufficient to relieve pain caused by the use of an argon laser is achieved; The duration of anesthesia is 15-20 minutes (taking into account individual characteristics from 5 to 45 minutes).

Trophic ulcers of the lower extremities. After applying the cream when treating trophic ulcers of the lower extremities, the duration of pain relief is up to 4 hours. There was no negative effect of the drug on the healing process of ulcers or on bacterial flora.

Use during pregnancy and breastfeeding

Pregnancy. There is insufficient data on the use of EMLA cream in pregnant women. Animal studies did not reveal any direct or indirect negative effects of the drug on pregnancy, intrauterine development of the fetus, the process of childbirth or postnatal development. Lidocaine and prilocaine penetrate the placental barrier and can be absorbed into fetal tissues. No specific reproductive effects, such as increased incidence of malformations or other direct or indirect adverse effects on the fetus, have been reported.

Lactation. Lidocaine and prilocaine are excreted in breast milk in quantities that do not pose a risk to the baby when the drug is used in therapeutic doses.

Interaction

In patients receiving drugs that induce the development of methemoglobinemia (for example, drugs containing a sulfo group), EMLA® cream may help increase the concentration of methemoglobin in the blood. When treating with other local anesthetics and structurally similar drugs (including tocainide), the risk of increased systemic effects when using high doses of EMLA cream should be taken into account. No specific studies have been conducted to evaluate the interaction of lidocaine/prilocaine with class III antiarrhythmic drugs; caution should be exercised when using drugs together.

Pharmaceutical interaction: not detected. Drugs that reduce the clearance of lidocaine (eg, cimetidine or beta-blockers) may cause potentially toxic plasma concentrations when repeated high doses of lidocaine are administered over an extended period of time. This interaction is not clinically significant during short-term therapy with lidocaine (eg, EMLA® cream) at recommended doses.

Overdose

If the recommended dosage regimen is followed, the development of signs of systemic toxicity is unlikely. Symptoms of intoxication are likely to be the same as with other local anesthetics, such as central nervous system (CNS) stimulation and, in severe cases, CNS and cardiac depression.

In rare cases, the development of clinically significant methemoglobinemia has been observed. Prilocaine in high doses can cause an increase in methemoglobin levels. Superficial application of prilocaine 125 mg for 5 hours caused the development of moderate methemoglobinemia in a 3-month-old child. Superficial application of lidocaine at a dose of 8.6 - 17.2 mg/kg caused serious intoxication in newborns.

Treatment. Severe neurological symptoms (convulsions, depression of the central nervous system) require symptomatic treatment, including the prescription of anticonvulsants and, if necessary, artificial ventilation. In case of development of methemoglobinemia, the antidote is methylthioninium chloride (methylene blue). Due to the slow systemic absorption of the drug, patients should be monitored for several hours after starting treatment for intoxication.

Impact on the ability to drive vehicles and operate machinery

Does not affect the ability to drive vehicles or operate equipment.

Use of Emla

Adults:

Trophic ulcers of the lower extremities During surgical treatment (mechanical cleansing) of trophic ulcers, apply 1–2 g of cream per 10 cm2 of surface. The cream is applied in a thick layer to the surface of the ulcer, no more than 10 g of cream per procedure. Cover the surface of the ulcer with an occlusive sticker. Duration of cream application is 30 minutes. The open tube is intended for one-time use; after each procedure, the unused cream is thrown away. When treating ulcers into which tissue penetration of the drug is difficult, the duration of application can be increased to 60 minutes. Surgical treatment of the wound surface should begin no later than 10 minutes after removing the cream. In the treatment of trophic ulcers of the lower extremities, EMLA cream is used up to 15 times over 1–2 months without reducing effectiveness or increasing the incidence of local reactions. Superficial anesthesia of the genital organs Skin of the genital organs Application of local anesthetics before injection:

• men: 1 g per 10 cm2. A thick layer of cream is applied to the skin. Duration of application - 15 minutes;
• women: 1–2 g per 10 cm2. A thick layer of cream is applied to the skin. Duration of application - 60 minutes.

Mucous membrane of the genital organs To remove condylomas or before injection of local anesthetics: 5–10 g of cream, depending on the area of ​​treatment, is applied to the entire surface, including the folds of the mucous membrane. No occlusal adhesive is required. Application duration is 5–10 minutes. The surgical procedure should begin immediately after removing the cream. Children When performing percutaneous injections, removal of molluscum contagiosum and other superficial surgical manipulations: the dose of EMLA cream should not exceed 1 g per 10 cm2 of surface, the cream is applied in a thick layer to the surface of the skin and covered with an occlusive sticker.

Children with atopic dermatitis need to reduce the duration of application to 30 minutes. Recommendations regarding the method of use Pierce the sealed membrane of the tube with a spike located in the upper outer part of the lid. Squeeze out the required amount of cream and apply to the procedure site. When anesthetizing the skin, occlusive stickers are used, included in the kit with the cream (12 pieces, size 6x7 cm).

Where is topical anesthesia used?

Most often it is used for pain relief when puncturing the skin during catheter insertion, injections, blood sampling, as well as in the following areas of medicine, such as:

• dentistry (for removing teeth and tartar, to relieve the gag reflex during procedures);
• surgery (for superficial surgical interventions. For example, when harvesting a flap for skin grafting, during mechanical cleaning of trophic ulcers);
• dermatology (for removal of molluscum contagiosum);
• cosmetology (before tattooing, hair removal, mesotherapy, laser therapy);
• gynecology (for removal of condylomas);
• pediatrics (for blood sampling, vaccinations).

Side effects of Emla

True adverse reactions caused by the use of local anesthetics occur with a frequency of 1/1000 patients.

Isolated cases of local reactions at the site of application of the cream, such as hemorrhagic rashes or petechiae, have been reported, especially after prolonged application in children with atopic dermatitis or warts. If the drug accidentally gets into the eyes, corneal irritation may occur.

Special instructions for the use of Emla

Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia are more likely to develop drug-dependent methemoglobinemia. EMLA cream should be used with caution on the skin in the eye area, since the drug irritates the mucous membrane of the eyes. In addition, loss of protective reflexes due to anesthetic contact with the cornea can lead to irritation and damage to the cornea. If EMLA cream gets into your eyes, they should be immediately rinsed with water or saline (sodium chloride solution) and protected until sensitivity of the cornea is restored. In patients with atopic dermatitis, the cream should be used with caution, and the duration of application should be reduced to 15–30 minutes. The effectiveness of using the cream in newborns when taking blood from the heel has not been established. The safety and effectiveness of the drug in children under 3 months of age have been studied only using a single dose. In such children, after applying the cream, a temporary increase in the level of methemoglobin in the blood is often observed, lasting up to 13 hours. However, this fact is probably not clinically significant. The cream should not be applied to a damaged eardrum and should not be used in situations where the drug may penetrate into the middle ear cavity. The cream should not be applied to open wounds. The drug should not be applied to the genital mucosa in children due to insufficient data regarding absorption. At concentrations exceeding 0.5–2.0%, lidocaine and prilocaine exhibit bactericidal and antiviral properties. Therefore, if the drug is used during vaccination (intradermal administration of a live vaccine, for example BCG), careful monitoring of the results of vaccination is necessary. EMLA cream should not be used in children aged 0 to 12 months receiving concomitant therapy with drugs that induce methemoglobinemia due to the lack of sufficient clinical experience with its use. It is necessary to monitor patients receiving antiarrhythmic drugs belonging to class III (for example, amiodarone), taking into account the results of the ECG in such patients, since lidocaine and class III antiarrhythmic drugs have additive effects. Pregnancy and lactation period Data regarding treatment of pregnant women with EMLA cream are insufficient. The results of studies conducted on animals do not contain sufficiently complete and reliable information regarding the effect on pregnancy, embryonic/fetal development, childbirth and development after birth. Lidocaine and prilocaine penetrate the placental barrier and can be absorbed by fetal tissues. There were no reports of reproductive disturbances, such as an increased incidence of malformations or direct or indirect effects on the fetus. However, when using the drug during pregnancy, it is necessary to weigh the benefit/risk ratio. Lidocaine and, probably, prilocaine pass into breast milk, but in such small quantities that the effect of therapeutic doses of the drug on the child is unlikely. Does not affect the ability to drive vehicles and operate machinery.

Lidocaine spray and EMLA: what is the difference?

The drugs differ in composition. If the spray contains only one substance - lidocaine, then EMLA cream contains lidocaine along with prilocaine.

Lidocaine and prilocaine belong to the class of amides of intermediate action. Their effect lasts on average 1-1.5 hours.

The anesthetic effect of lidocaine is 4 times higher than that of novocaine. It does not penetrate well through the surface epithelium of the skin. Therefore, the spray is more often used when performing manipulations on the mucous membranes - there the effectiveness of pain relief is higher.

Prilocaine is slower but longer acting than lidocaine and is less toxic. The combination of two anesthetics in EMLA cream allows you to prolong the effect of the drug and provide it with additional functions. For example, with ELMA the depth of pain relief depends on the duration of application, while with lidocaine spray the effect extends only to the superficial layers of the skin and then only when additional conditions are created (applying a patch or film that prevents moisture evaporation). Thus, the cream is suitable for both procedures performed on the skin and those performed on the mucous membranes.

Emla drug interactions

EMLA cream may increase the formation of methemoglobin in patients receiving treatment with methemoglobin-inducing drugs (eg, sulfonamides). When using EMLA cream in high doses in patients receiving local anesthetics or drugs structurally similar to local anesthetics, such as tocainide, the risk of systemic additive effects must be considered. Specific studies of the interaction of the drug with local anesthetics and antiarrhythmic drugs belonging to class III have not been conducted, so caution is recommended when using them together.

Emla drug overdose, symptoms and treatment

If the recommended dosage regimen is followed, the development of systemic toxicity is unlikely. The probable symptoms of intoxication are the same as with the use of other local anesthetics: at the beginning, stimulation of the central nervous system, in severe cases, depression of the central nervous system and cardiac activity. Cases of clinically significant methemoglobinemia have been very rarely reported in children, as prilocaine in high doses can increase methemoglobin levels. Superficial application of 125 mg of prilocaine for 5 hours caused the development of moderate methemoglobinemia in a three-month-old child. Topical application of 8.6–17.2 mg/kg lidocaine led to the development of severe intoxication in infants. Severe neurological symptoms (convulsions, central nervous system depression) require symptomatic treatment: the use of mechanical ventilation and anticonvulsants. The antidote for methemoglobinemia is methylthionine. Due to the slow systemic absorption of the drug, the patient's condition must be monitored for several hours after the symptoms of intoxication have resolved.