Tatucain (Cream) Instructions for Use

Marketing Authorization Holder

Biolab, LLC (Russia)

Manufactured By

Interpharma, LLC (Russia)

ATC Code

N01BB20 (Amides in combination)

Active Substances

Lidocaine (Rec.INN registered by WHO)

Prilocaine (Rec.INN registered by WHO)

Dosage Form

Tatucain

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 in the form of a homogeneous mass of white or almost white color; the presence of a slight specific odor is allowed.

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

5 g – aluminum tubes (1) – cardboard packs.
5 g – aluminum tubes (5) – cardboard boxes.
5 g – aluminum tubes (10) – cardboard boxes.
5 g – aluminum tubes (20) – cardboard boxes.
5 g – aluminum tubes (30) – cardboard boxes.
30 g – aluminum tubes (1) – cardboard packs.
100 g – aluminum tubes (1) – cardboard packs.

Indications

• Topical anesthesia of intact skin in procedures requiring penetration of the skin (e.g., venipuncture, venous cannulation, laser therapy, superficial surgical procedures, cosmetic interventions).
• Topical anesthesia of genital mucous membranes in adults for superficial minor surgical procedures and as an analgesic for the relief of pain associated with the mucous membranes.
• Dermal anesthesia on limited areas of skin for the management of localized neuropathic pain, such as post-herpetic neuralgia, when other treatments are not suitable.

The cream is intended for use on small, well-defined areas of skin or mucous membranes. The duration of application and the amount of cream used must be strictly controlled to minimize systemic absorption and the risk of adverse effects.

Contraindications

• Hypersensitivity to lidocaine, prilocaine, any other amide-type local anesthetic, or any of the excipients listed in the composition.
• Patients with congenital or idiopathic methemoglobinemia or in patients receiving other drugs known to induce methemoglobinemia.
• Application to broken or inflamed skin, as this can lead to significantly increased systemic absorption.
• Application on or near mucous membranes in children under the age of 12, except for specific genital mucous membrane indications in adults as directed.
• Use on large areas of skin or under occlusive dressings for prolonged periods, due to the high risk of systemic toxicity.
• Patients with significant hepatic impairment or severe renal failure, as reduced metabolism and excretion can lead to accumulation and toxicity.
• Patients with severe heart failure or shock, as systemic absorption can further depress cardiac function.

This product should not be used in infants under the age of 12 months. Special caution is required in debilitated, elderly, or acutely ill patients due to reduced physiological reserves.

Dosage Regimen

For intact skin procedures (e.g., venipuncture): A thick layer of cream is applied to the skin without rubbing and covered with an occlusive dressing. For adults and children over 1 year of age, apply 1.5 to 2.5 grams of cream per 10 cm² of skin. The maximum application time for adults is 5 hours. For children aged 1 to 12 years, the maximum application time is determined by age and weight and must not exceed 4 hours. For children under 1 year, a maximum of 2 grams applied for a maximum of 1 hour is recommended, and only on small, intact skin areas.

For genital mucous membranes in adults: A smaller quantity (up to 1 gram) is applied to the mucous membrane for 5 to 10 minutes without an occlusive dressing. The treated area may be gently wiped clean before the procedure begins. The total dose should be minimized, and the application time should be as short as possible to achieve the desired anesthetic effect.

Maximum Recommended Dose: The maximum single dose for adults should not exceed 30 grams of cream (containing 750 mg of lidocaine and 750 mg of prilocaine). In children, the maximum dose is calculated based on body weight and should not exceed 1 gram of cream per 10 kg of body weight, with absolute maximums defined by age. Repeated applications within a 24-hour period are generally not recommended.

Adverse Reactions

Local reactions at the application site are the most commonly reported adverse effects. These may include paleness, redness, swelling, itching, and transient burning or stinging sensations. These effects are usually mild and resolve spontaneously within a few hours after the cream is removed.

Systemic reactions are rare and are typically associated with excessive application, prolonged exposure, or use on compromised skin. These reactions are due to systemic absorption of the active substances and are similar to those of other local anesthetics of the amide type. Central Nervous System (CNS) effects may include dizziness, nervousness, drowsiness, tremors, blurred vision, convulsions, respiratory depression, and in severe cases, coma. Cardiovascular effects may include bradycardia, hypotension, and cardiac arrest.

A specific and serious adverse reaction, particularly in infants and young children, is methemoglobinemia. This condition reduces the oxygen-carrying capacity of the blood and can present with cyanosis (a grayish-blue discoloration of the skin, lips, and nail beds), tachycardia, headache, fatigue, and dyspnea. This is a medical emergency requiring immediate treatment.

Allergic reactions, including anaphylaxis and contact dermatitis, can occur but are infrequent. Hypersensitivity reactions may be characterized by urticaria, angioedema, or bronchospasm.

Drug Interactions

Antiarrhythmic drugs: Concurrent use of other amide-type local anesthetics (e.g., tocainide, mexiletine) or Class III antiarrhythmics (e.g., amiodarone) may have additive toxic effects, increasing the risk of CNS and cardiovascular adverse reactions.

Drugs inducing methemoglobinemia: Concomitant use with substances known to promote methemoglobin formation significantly increases the risk of clinically significant methemoglobinemia. Such drugs include sulfonamides, nitrates (e.g., nitroglycerin), nitrites, dapsone, phenacetin, phenobarbital, and phenytoin. This combination is contraindicated.

CYP450 Inhibitors and Inducers: Lidocaine and prilocaine are metabolized by the hepatic cytochrome P450 system. Drugs that inhibit these enzymes (e.g., cimetidine, fluconazole, beta-blockers like propranolol) may reduce their metabolism, leading to increased plasma concentrations and a heightened risk of toxicity. Conversely, inducers (e.g., rifampicin, phenytoin, St. John’s Wort) may increase metabolism and reduce efficacy.

Other CNS Depressants: The CNS effects of lidocaine and prilocaine may be potentiated by other CNS depressants, including opioids, sedatives, hypnotics, tranquilizers, and general anesthetics, potentially leading to enhanced sedation or respiratory depression.

Muscle Relaxants: Local anesthetics may enhance the neuromuscular blocking effect of suxamethonium and other non-depolarizing muscle relaxants.

Overdose

Symptoms of overdose are primarily related to systemic absorption of lidocaine and prilocaine and manifest as effects on the central nervous system (CNS) and the cardiovascular system. Early CNS signs include dizziness, tinnitus, blurred vision, tremors, drowsiness, and circumoral paresthesia. These may progress to convulsions, respiratory depression, and coma. Cardiovascular symptoms include bradycardia, hypotension, arrhythmias, and cardiac arrest, which can be fatal.

A specific manifestation of prilocaine overdose, especially in vulnerable populations like infants, is the development of methemoglobinemia, characterized by cyanosis, dyspnea, tachycardia, headache, and lethargy.

Management: In case of suspected overdose, the cream must be removed immediately. Management is symptomatic and supportive. Ensure a patent airway and administer oxygen. Ventilatory support may be required. Convulsions should be controlled with benzodiazepines (e.g., diazepam). Bradycardia and hypotension may require intravenous fluids and vasopressors. Methemoglobinemia is treated with intravenous methylene blue (1-2 mg/kg body weight as a 1% solution over 5 minutes), but this is contraindicated in patients with G6PD deficiency. Hemodialysis is not effective for removing lidocaine or prilocaine due to high protein binding and extensive tissue distribution.

Clinical-Pharmacological Group

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

Pharmacotherapeutic Group

Local anesthetic agent

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

Rx Only

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.