Perkain (Solution) Instructions for Use

Marketing Authorization Holder

Pierrel Farmaceutici, S.p.A. (Italy)

Manufactured By

Pierrel, S.p.A. (Italy)

ATC Code

N01BB03 (Mepivacaine)

Active Substance

Mepivacaine (Rec.INN registered by WHO)

Dosage Form

Perkain

Injection solution 30 mg/ml: 1.8 ml cartridges 50 or 100 pcs.

Dosage Form, Packaging, and Composition

Solution for injection is a clear, colorless solution, free from visible particles.

Excipients: sodium chloride, water for injections.

1.8 ml – cartridges (10) – tray (5) – carton packs.
1.8 ml – cartridges (10) – tray (10) – carton packs.

Clinical-Pharmacological Group

Local anesthetic

Pharmacotherapeutic Group

Local anesthetic agent

Pharmacological Action

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

Pharmacokinetics

When administered into the tissues of the maxillofacial area via 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) through hydroxylation and dealkylation to t-hydroxymepivacaine, p-hydroxymepivacaine, and 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 ranges from 2 to 3 hours.

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

Indications

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

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 (weighing 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

Hematopoietic system: rarely – methemoglobinemia.

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.

Nervous system: rarely – anxiety (including nervousness, agitation, anxiety), confusion, euphoria, numbness of lips and tongue, oral paresthesia, drowsiness, yawning, speech disorder (dysarthria, incoherent speech, logorrhea), dizziness (including stupor, vertigo, balance disorder), 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 area 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.

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.

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

Digestive system: rarely – edema of 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 (e.g., chronic heart failure, diabetes mellitus, liver diseases); progression of cardiovascular failure; inflammatory diseases or infection at 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. Breastfeeding is not recommended for 10 hours after the use of 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 anticoagulant treatment, the risk of bleeding onset 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 the sensitivity has been restored.

Before administering mepivacaine, an aspiration check must always be performed to avoid intravascular injection.

Regional and local anesthesia should be performed by experienced specialists in an appropriately equipped room with readily available equipment and drugs necessary for cardiac monitoring and resuscitation measures. 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 operate machinery

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 relaxants.

When co-administered with narcotic analgesics, an additive depressant effect on the central nervous system develops.

Antagonism with antimyasthenic drugs on skeletal muscle 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 serum level of mepivacaine is possible.

When used concomitantly with antiarrhythmic agents (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.