Emla, cream 30 g

Pharmacotherapeutic group:A local anesthetic
ATX code: N01BB20

Pharmacodynamics

EMLA cream contains as active ingredients lidocaine and prilocaine, which are local anesthetic amide type. Anesthesia of the skin 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. No differences in efficacy (including time of achieving anesthetic effect) and safety were found when applying the cream to intact skin between elderly (65-96 years) and younger patients.
Due to the action of EMLA cream on the surface vessels, temporary paling or reddening of the skin is possible. Such reactions in patients with widespread neurodermatitis (atopic dermatitis) may occur more quickly, 30-60 minutes after application of the cream, indicating faster penetration of the cream through the skin.
In case of puncture biopsy (4 mm in diameter) the use of EMLA cream provides adequate anesthesia of the intact skin in 90% of patients in 60 minutes after applying the cream in case of needle insertion to a depth of 2 mm, and in 120 minutes after the needle insertion to a depth of 3 mm. The efficiency of EMLA cream does not depend on skin color or pigmentation (skin type I-IV).
When using combined vaccines against such infections as measles, rubella, mumps, or intramuscular combined vaccines against diphtheria, pertussis, tetanus, polio and infection caused by Haemophilius influenzae type b, as well as during 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 reached a protective or positive antibody titer after immunization.

Genital mucosa
Anesthesia of the genital mucosa is achieved faster compared to anesthesia of intact skin due to faster absorption of the drug.
In women 5-10 minutes after applying EMLA cream to the genital mucosa anesthesia is achieved sufficient to relieve pain caused by the use of an argon laser; anesthesia lasts 15-20 minutes (taking into account individual characteristics from 5 to 45 minutes).

Trophic ulcers of the lower extremities
After the application of the cream in the treatment of trophic ulcers of the lower extremities the duration of anesthesia is up to 4 hours. No negative effect of the drug on the healing process of ulcers or with respect to bacterial flora was noted.

Pharmacokinetics

Systemic absorption of EMLA cream depends on the dose, duration of application and thickness of the skin (depending on body area) as well as other skin conditions such as skin diseases and shaving. When applied to the ulcerous surface of the lower extremities, the absorption of the drug may be affected by features of the ulcers, such as the size (absorption increases with increasing area of the ulcer).

Intact skin:
In adults, after applying 60 g of cream to 400 cm2 (1.5 g per 10 cm2) intact thigh skin for 3 hours, systemic absorption for lidocaine was approximately 3% and for prilocaine 5%. Absorption was slow. Maximum plasma concentrations of lidocaine (mean 0.12 µg/ml) and prilocaine (mean 0.07 µg/ml) were reached approximately 4 hours after application of the cream. There is a risk of toxic symptoms only at plasma concentrations of the active substances of 5-10 µg/ml. When EMLA cream is applied to intact skin 8-12 hours after shaving, the maximum plasma concentrations of lidocaine and prilocaine in both young and elderly patients are very low and well below possible toxic levels.

Trophic ulcers of the lower extremities:
The time to reach maximum plasma concentrations of lidocaine (0.05-0.84 µg/ml) and prilocaine (0.02-0.08 µg/ml) is 1-2.5 hours from application to the ulcerous surface (5-10 g cream for 30 min).
No cumulation in plasma of prilocaine, lidocaine or their metabolites was observed during repeated application of the cream on the ulcerous surface. 2-10 g of EMLA cream was applied to the ulcerous surface up to 62 cm2 for 30-60 minutes from 3 to 7 times a week (15 times during the month).

Genital mucosa:
Time to reach maximum plasma concentrations of lidocaine and prilocaine (0.18 µg/mL and 0.15 µg/mL on average, respectively) is approximately 35 min from application to the vaginal mucosa (10 g cream for 10 min).