Mepivacain-Binergia (Solution) Instructions for Use

Marketing Authorization Holder

Binergia JSC (Russia)

Manufactured By

Armavir Biopharmaceutical Plant, FSE (Russia)

ATC Code

N01BB03 (Mepivacaine)

Active Substance

Mepivacaine (Rec.INN registered by WHO)

Dosage Form

Mepivacaine-Binergia

Solution for injection 30 mg/1 ml: 1.7 ml or 1.8 ml cartridges 10, 50 or 100 pcs., 2 ml amp. 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for injection transparent, colorless.

Excipients : sodium chloride, water for injections.

1.7 ml – cartridges (10) – contour plastic packaging (1) – cardboard packs.
1.7 ml – cartridges (10) – contour plastic packaging (5) – cardboard packs.
1.7 ml – cartridges (10) – contour plastic packaging (10) – cardboard packs.
1.8 ml – cartridges (10) – contour plastic packaging (1) – cardboard packs.
1.8 ml – cartridges (10) – contour plastic packaging (5) – cardboard packs.
1.8 ml – cartridges (10) – contour plastic packaging (10) – cardboard packs.
2 ml – ampoules (5) – contour plastic packaging (1) – cardboard packs.
2 ml – ampoules (5) – contour plastic packaging (2) – cardboard packs.

Clinical-Pharmacological Group

Local anesthetic for use in dentistry

Pharmacotherapeutic Group

Anesthetics; local anesthetics; amides

Pharmacological Action

A local anesthetic, the mechanism of action of which is associated with the stabilization of cell membranes. It causes all types of local anesthesia: terminal, infiltration, conduction. It has a rapid and strong effect.

Pharmacokinetics

When administered into the tissues of the maxillofacial area by means of conduction or infiltration anesthesia, the C_max of mepivacaine in blood plasma is reached approximately 30-60 minutes after injection. The duration of action is determined by the rate of diffusion from the tissues into the bloodstream. The distribution coefficient is 0.8. Binding to plasma proteins is 69-78% (mainly with α₁-acid glycoprotein).

The degree of bioavailability reaches 100% in the area of action.

Mepivacaine is rapidly metabolized in the liver (undergoing hydrolysis by microsomal enzymes) by hydroxylation and dealkylation to t-hydroxymepivacaine, p-hydroxymepivacaine, pipecolylxylidine; only 5-10% is excreted by the kidneys unchanged.

It undergoes enterohepatic recirculation.

It is excreted by the kidneys, mainly in the form of metabolites. Metabolites are predominantly excreted from the body with bile. T_1/2 is from 2 to 3 hours.

In patients with impaired liver function and/or in the presence of uremia, T_1/2 increases. In case of liver pathology (cirrhosis, hepatitis), accumulation of mepivacaine is possible.

Indications

Infiltration, conduction, intraligamentary, intraosseous and intrapulpal anesthesia for surgical and other painful dental interventions.

ICD codes

Dosage Regimen

The amount of solution and the total dose depend on the type of anesthesia and the nature of the surgical intervention or manipulation.

The smallest dose of mepivacaine that provides sufficient anesthesia should be used. The average single dose is 54 mg.

Adults

The recommended maximum single dose of mepivacaine for adults is 300 mg (4.4 mg/kg body weight)

For children over 4 years of age (with a body weight of more than 20 kg), the dose of mepivacaine is set depending on age, body weight and the nature of the surgical intervention. The average dose is 0.75 mg/kg body weight.

The maximum dose of mepivacaine is 3 mg/kg body weight.

Adverse Reactions

From the hematopoietic system: rarely – methemoglobinemia.

From the immune system: rarely – anaphylactic and anaphylactoid reactions, angioedema (including edema of the tongue, oral cavity, lips, throat and periorbital edema); urticaria, skin itching, rash, erythema.

From the nervous system: rarely – anxiety (including nervousness, agitation, anxiety), confusion, euphoria, numbness of the lips and tongue, oral paresthesia, drowsiness, yawning, speech disorder (dysarthria, incoherent speech, logorrhea), dizziness (including numbness, vertigo, imbalance), headaches, nystagmus, tinnitus, hyperacusis, blurred vision, diplopia, miosis, visual impairment, tremor, loss of consciousness, convulsions (including generalized). Direct local effect on efferent neurons or preganglionic neurons in the submandibular region or postganglionic neurons: oral paresthesia (lips, tongue, gums, etc.), dysesthesia, including heat or chills, dysgeusia (including metallic taste), local muscle cramps, local hyperemia, local pallor. Effect on reflexogenic zones: vasodilation, mydriasis, pallor, nausea, vomiting, hypersalivation, perspiration.

From the cardiovascular system: rarely – cardiac arrest, cardiac conduction disturbance (AV block), arrhythmia (ventricular extrasystole and ventricular fibrillation), myocardial depression, tachycardia, bradycardia, vascular collapse, arterial hypotension, vasodilation.

From the respiratory system: rarely – respiratory depression (from bradypnea to respiratory arrest).

From the digestive system: rarely – edema of the lips, tongue, gums, nausea, vomiting, gum ulceration, gingivitis.

Local reactions necrosis at the injection site.

Other edema in the head and neck area.

Contraindications

Hypersensitivity to mepivacaine and other local anesthetics of the amide group; severe liver diseases (cirrhosis, hereditary or acquired porphyria); myasthenia gravis; children under 4 years of age (body weight less than 20 kg); cardiac rhythm and conduction disorders; acute decompensated heart failure; arterial hypotension; intravascular administration (an aspiration test must be performed before administering mepivacaine).

With caution conditions accompanied by reduced hepatic blood flow (for example, chronic heart failure, diabetes mellitus, liver diseases); progression of cardiovascular failure; inflammatory diseases or infection of the injection site; pseudocholinesterase deficiency; renal failure; hyperkalemia; acidosis; elderly age (over 65 years); atherosclerosis; vascular embolism; diabetic polyneuropathy.

Use in Pregnancy and Lactation

During pregnancy, it should be used only after consultation with a doctor, in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

Local anesthetics, including Mepivacaine, are excreted in breast milk to a small extent. With a single use of mepivacaine, a negative effect on the child is unlikely. It is not recommended to breastfeed for 10 hours after using mepivacaine.

Use in Hepatic Impairment

Contraindicated in patients with severe liver diseases (cirrhosis, hereditary or acquired porphyria). Use with caution in patients with liver diseases. In this group of patients, it is necessary to use the minimum dose that provides sufficient anesthesia.

Use in Renal Impairment

Use with caution in patients with renal failure. In this group of patients, it is necessary to use the minimum dose that provides sufficient anesthesia.

Pediatric Use

Contraindicated in children under 4 years of age (body weight less than 20 kg).

Geriatric Use

Use with caution in elderly patients (over 65 years of age). In this group of patients, it is necessary to use the minimum dose that provides sufficient anesthesia.

Special Precautions

MAO inhibitors should be discontinued 10 days before the planned use of mepivacaine.

Mepivacaine should be used only in a healthcare facility setting.

Mepivacaine must be administered slowly and continuously. When using mepivacaine, it is necessary to monitor the patient’s blood pressure, pulse and pupil diameter. Before using mepivacaine, access to resuscitation equipment must be ensured.

In patients receiving treatment with anticoagulants, the risk of bleeding occurrence and development is increased.

The anesthetic effect of mepivacaine may be reduced when administered into an inflamed or infected area.

When using mepivacaine, unintentional injury to the lips, cheeks, mucous membrane and tongue is possible, especially in children, due to reduced sensitivity.

The patient should be warned that food intake is possible only after sensitivity is restored.

Before administering mepivacaine, an aspiration control must always be performed to avoid intravascular administration.

Regional and local anesthesia should be performed by experienced specialists in an appropriately equipped room with readily available equipment and drugs necessary for monitoring cardiac activity and resuscitation. The personnel performing anesthesia must be qualified and trained in anesthesia techniques, and must be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

Effect on the ability to drive vehicles and mechanisms

When using mepivacaine, patients must exercise caution when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

The use of mepivacaine while taking MAO inhibitors (furazolidone, procarbazine, selegiline) increases the risk of decreased blood pressure. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect of mepivacaine.

Mepivacaine enhances the depressant effect on the central nervous system caused by other drugs. When used concomitantly with sedatives, a reduction in the dose of mepivacaine is required.

Anticoagulants (ardeparin sodium, dalteparin, enoxaparin, warfarin) and low molecular weight heparin preparations increase the risk of bleeding.

When treating the mepivacaine injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.

Mepivacaine enhances and prolongs the action of muscle relaxant drugs.

When prescribed concomitantly with narcotic analgesics, an additive depressant effect on the central nervous system develops.

Antagonism with antimyasthenic drugs in their effect on skeletal muscles is manifested, especially when used in high doses, which requires additional correction of myasthenia treatment.

Cholinesterase inhibitors (antimyasthenic drugs, cyclophosphamide, thiotepa) reduce the metabolism of mepivacaine.

When used concomitantly with H₂-histamine receptor blockers (cimetidine), an increase in the level of mepivacaine in the blood serum is possible.

When used concomitantly with antiarrhythmic drugs (tocainide, sympatholytics, digitalis preparations), an increase in side effects is possible.

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.