Beautycaine^® (Cream) Instructions for Use

Marketing Authorization Holder

Intelbio LLC (Russia)

Manufactured By

Flora Kavkaza, JSC (Russia)

ATC Code

N01BB20 (Amides in combination)

Active Substances

Lidocaine (Rec.INN registered by WHO)

Prilocaine (Rec.INN registered by WHO)

Dosage Form

Beautycaine®

Cream for topical and external use 2.5 g+2.5 g/100 g: tubes 5 g, 30 g or 100 g

Dosage Form, Packaging, and Composition

Cream for topical and external use is homogeneous, white or almost white in color; a faint specific odor is allowed.

Excipients: PEG-54 hydrogenated castor oil – 1.9 g, carbomer 934R – 1 g, sodium hydroxide – 0.52 g, purified water – up to 100 g.

5 g – aluminum tubes (1) – cardboard boxes.
30 g – aluminum tubes (1) – cardboard boxes.
100 g – aluminum tubes (1) – cardboard boxes.

Clinical-Pharmacological Group

Agent for topical anesthesia of the skin and mucous membranes of the genital organs

Pharmacotherapeutic Group

Local anesthetic agent

Pharmacological Action

A combined local anesthetic agent for external and topical use. It contains Lidocaine and Prilocaine, which are local anesthetics of the amide type.

Anesthesia of the skin is caused by the penetration of lidocaine and prilocaine into the layers of the epidermis and dermis.

When applied to the mucous membrane of the genital organs, anesthesia is achieved faster than when applied to intact skin due to the faster absorption of the active substances.

The degree of anesthesia depends on the dose and duration of application.

Pharmacokinetics

The systemic absorption of the active substances depends on the dose, duration of application, and skin thickness (which varies by body area), as well as other skin characteristics, such as skin diseases and shaving.

When applied to an ulcerative surface of the lower extremities, the absorption of the active substances can be influenced by the characteristics of the ulcers, for example, their size (absorption increases with increasing ulcer area).

Intact skin. In adults, after applying an amount of the drug containing this combination in a single dose for 3 hours, the systemic absorption of lidocaine was approximately 3% and prilocaine – 5%. Absorption is slow. The C_max of lidocaine (mean value 0.12 µg/ml) and prilocaine (mean value 0.07 µg/ml) in blood plasma was reached approximately 4 hours after application. The risk of toxic symptoms exists only when the plasma concentration of the active substances is 5-10 µg/ml.

Trophic ulcers of the lower extremities. The time to reach C_max of lidocaine (0.05-0.84 µg/ml) and prilocaine (0.02-0.08 µg/ml) in blood plasma is 1-2.5 hours from the moment of applying the drug to the ulcer surface for 30 minutes.

No accumulation of prilocaine, lidocaine, or their metabolites in the blood plasma was observed after repeated application to the ulcer surface.

Mucous membrane of the genital organs. The time to reach C_max of lidocaine and prilocaine in blood plasma (on average 0.18 µg/ml and 0.15 µg/ml, respectively) is approximately 35 minutes from the moment of application to the vaginal mucosa for 10 minutes.

Indications

In adults: superficial anesthesia of the skin for injections (including vaccination), punctures and vascular catheterization, 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 tissues; superficial anesthesia of the mucous membrane of the genital organs before performing painful manipulations and for pain relief before injections of local anesthetics.

In children: superficial anesthesia of the skin for injections (including vaccination), punctures and vascular catheterization, and superficial surgical interventions (including removal of molluscum contagiosum).

ICD codes

Dosage Regimen

Apply externally to the skin or topically to the genital mucous membranes.

Determine the dose and application time based on the indication, clinical situation, and patient age.

For superficial anesthesia of intact skin in adults and children over 1 year: apply a thick layer of cream to the required area. Cover the application site with an occlusive dressing.

For minor dermatological procedures (e.g., needle punctures, superficial surgery): apply for at least 1 hour.

For more extensive procedures (e.g., split-thickness skin grafting): apply for 2 to 5 hours.

For genital mucous membranes in women (e.g., minor surgical procedures, pre-injection anesthesia): apply 5 to 10 grams for 5 to 10 minutes.

For trophic ulcers on lower extremities: apply for 30 to 60 minutes prior to mechanical cleaning or debridement.

In children aged 1 to 12 years, apply a maximum of 10 grams for up to 4 hours.

In infants aged 3 to 12 months weighing over 3 kg, apply a maximum of 2 grams for up to 2 hours.

Do not use on premature infants born before 37 weeks gestation or on newborns weighing less than 3 kg.

Avoid application to open wounds, damaged eardrums, or areas where penetration into the middle ear is possible.

Reduce application time to 15-30 minutes when treating skin affected by atopic dermatitis.

After the required application time, remove the occlusive dressing and wipe off the cream. The anesthetized area will be ready for the procedure.

Adverse Reactions

Local reactions: transient local reactions such as pallor, redness, and swelling may occur at the application site; immediately after application – mild burning, itching, and a sensation of warmth. Hemorrhagic rash or petechiae, especially after prolonged application in children with atopic dermatitis or molluscum contagiosum.
Corneal irritation due to accidental contact of the drug with the eyes.

General reactions: allergic reactions, in the most severe cases – anaphylactic shock. Methemoglobinemia and/or cyanosis.

Contraindications

Premature newborns born at less than 37 weeks of gestation; newborns weighing less than 3 kg; hypersensitivity to local anesthetics of the amide type.

Use in Pregnancy and Lactation

Animal studies have not revealed any direct or indirect negative effects of this combination on pregnancy, embryonic/fetal development, the birth process, or postnatal development.

Lidocaine and Prilocaine cross the placental barrier and can be absorbed into fetal tissues. No specific impairments of the reproductive process, such as an increased frequency of malformations or other direct or indirect negative effects on the fetus, have been reported.

Lidocaine and Prilocaine are excreted in breast milk in amounts that do not pose a risk to the child when drugs containing this combination are used according to the indications in recommended doses.

Use in Hepatic Impairment

There are no specific restrictions for use.

Use in Renal Impairment

There are no specific restrictions for use.

Pediatric Use

Premature newborns born at less than 37 weeks of gestation; newborns weighing less than 3 kg.

Geriatric Use

Use with caution to avoid exacerbation of concomitant diseases.

Special Precautions

Use with caution in: glucose-6-phosphate dehydrogenase deficiency, hereditary or idiopathic methemoglobinemia, widespread neurodermatitis (atopic dermatitis), patients taking class III antiarrhythmic drugs (e.g., amiodarone).

Patients with glucose-6-phosphate dehydrogenase deficiency or hereditary or idiopathic methemoglobinemia are more susceptible to drug-induced methemoglobinemia.

Caution should be exercised when applying the drug to the skin in atopic dermatitis; the application time should be reduced (15-30 minutes).

Patients taking class III antiarrhythmic drugs (e.g., amiodarone) should be under constant supervision and ECG monitoring, as an effect on cardiac activity is possible.

The drug should not be applied to a damaged eardrum or in other cases where penetration of the drug into the middle ear is possible.

The drug containing this combination should not be applied to open wounds.

Lidocaine and Prilocaine in concentrations above 0.5-2% have bactericidal and antiviral properties. In this regard, special attention is recommended when using the drug before the subcutaneous administration of a live vaccine (e.g., BCG).

Due to a lack of data on absorption, application to the mucous membrane of the genital organs in children is not recommended.

Drug Interactions

In patients receiving drugs that induce methemoglobinemia (e.g., drugs containing sulfogroups), the use of drugs containing this combination may contribute to an increase in 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 this combination in high doses 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 the drugs concomitantly.

Drugs that reduce the clearance of lidocaine (e.g., cimetidine or beta-blockers) may cause potentially toxic plasma concentrations when repeated high doses of lidocaine are used over a prolonged period.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.