Mepivacaine (Scandonest): effects and side effects. Use of the dental anesthetic mepivacaine Features of use in case of failure of internal organs

Pharmacotherapeutic group N01BB03 - preparations for local anesthesia.

Main Pharmacological action: amide local anesthetic, the mechanism of action is associated with the stabilization of membranes due to the blockade of sodium channels; the anesthetic effect is fast.

INDICATIONS: local anesthesia (including terminal, infiltration, conduction) in dentistry of the BNF (recommendation for the use of drugs in the British National Formulary, issue 60).

Directions for use and dosage: administer to adults 1 - 2 ml or more, depending on the requirements of the operation, by infiltration or peripheral nerve blockade, the solution must be administered in small doses, at an injection rate of approximately 1 ml / min. for a healthy adult not previously treated with sedatives, the maximum dose administered as a single dose or in repeated doses over no more than 90 minutes (minutes) is 4.4 mg/kg mepivacaine hydrochloride, but should not exceed 300 mg; MDD (maximum daily dose) - 1000 mg in pediatric practice is used with caution; the dose of the drug depends on the age and body weight of the child.

Side effects when using drugs: bradycardia, hypotension (or sometimes hypertension), ventricular arrhythmia; agitation and/or depression, headache, weakness, difficulty swallowing, blurred vision, convulsions; skin lesions, urticaria, edema or anaphylaxis, increased t ° (temperature) of the body, Quincke's edema.

Contraindications to the use of drugs: known hypersensitivity to any component of the drug; knowledge or whether pregnancy is permissible.

Drug release forms: s for injection 3%, 1.7 ml, 1.8 ml in cartridges

Visamodia with other drugs

There have been no reports of interactions between mepivacaine and other drugs. The drug is incompatible with amphotericin, methohexitone sodium, sodium sulfadiazine, mephentermine hydrochloride, alkalis, heavy metals, oxidizing agents, tannin, exposure to air and light.

Features of use in women during pregnancy and lactation

Pregnancy Do not use
Lactation: do not use

Features of use for insufficiency of internal organs

Dysfunction of the cerebrovascular system: Checking the state of the cardiovascular (cardiovascular) system.
Dysfunction of the liver:
Renal dysfunction No special recommendations
Respiratory system dysfunction: No special recommendations

Features of use in children and the elderly

Children, 12 years old Use with caution. The dose depends on age and body weight.
Elderly and senile persons: No special recommendations

Application measures

Information for the doctor: Before treatment, check the condition of the cardiovascular system. Avoid overdose; the interval between the two maximum doses should be at least 24 hours (Hour). Use the lowest doses and concentrations necessary to obtain the desired effect. At the first signs of overdose (loss of consciousness), use of the drug should be discontinued. We have emergency medical equipment at our disposal. help.
Patient Information: No special recommendations

Tradename

Mepivastezin

International nonproprietary name

Mepivacaine

Dosage form

Solution for submucosal injections in dentistry 3% 1.7 ml

Compound

1 ml of solution contains

active substance- mepivacaine hydrochloride 30 mg,

Excipients: sodium hydroxide solution 9.0%, sodium chloride, water for injection.

Description

Colorless, transparent, non-opalescent solution.

Pharmacotherapeutic group

Anesthetics. Local anesthetics. Amides. Mepivacaine.

ATX code N01BB03

Pharmacological properties

Pharmacokinetics

Mepivacaine hydrochloride is rapidly and substantially absorbed. Plasma protein binding is 60-78% and the half-life is about 2 hours.

Distribution volume 84 l. Ground clearance - 0.78 l/min.

It is mainly broken down in the liver, metabolic products are excreted through the kidneys.

Pharmacodynamics

Mepivastesin is used as a local anesthetic in dentistry. Characterized by a rapid onset of anesthesia (1 to 3 minutes after injection), a pronounced analgesic effect and good local tolerance. The duration of action for pulp anesthesia is 20 to 40 minutes, and for soft tissue anesthesia - from 45 to 90 minutes. MEPIVASTHEZINE is an amide-type local anesthetic with a rapid onset of anesthesia, which leads to reversible inhibition of the sensitivity of autonomic, sensory and motor nerve fibers. The mechanism of action is to block voltage-gated sodium channels on the nerve fiber membrane.

The drug diffuses easily through the nerve fiber membrane into the axoplasm as a base. Inside the axon, it turns into an ionized cationic form (proton) and causes a block of sodium channels. At low pH values, for example, under conditions of inflammation, the effect of the drug is reduced, since the formation of the anesthetic base is difficult.

Indications for use

Infiltration and conduction anesthesia in dentistry:

For uncomplicated tooth extraction

When preparing carious cavities and teeth for a crown

Directions for use and doses

Whenever possible, the smallest volume of solution that promotes effective anesthesia should be prescribed.

For adults, as a rule, a dose of 1-4 ml is sufficient.

For children aged 4 years and over with a body weight of 20 - 30 kg, a dose of 0.25-1 ml is sufficient; for children weighing 30 - 45 kg - 0.5-2 ml. The amount of drug administered should be determined depending on the age and body weight of the child and the duration of the operation. The average dose is 0.75 mg mepivacaine/kg body weight (0.025 ml Mepivastasin/kg body weight).

Mepivacaine plasma levels may be increased in elderly patients due to decreased metabolic processes and a lower volume of distribution of the drug.

The risk of accumulation of mepivacaine increases with repeated use. A similar effect can be observed when the patient’s general condition decreases, as well as with severe impairment of liver and kidney function. Thus, in all such cases, a lower dose of the drug (the minimum amount for sufficient anesthesia) is recommended.

The dose of Mepivastezin should be reduced in patients suffering from angina pectoris and atherosclerosis.

Adults:

For adults, the maximum dose is 4 mg mepivacaine per kg body weight and is equivalent to 0.133 ml mepivastasin per kg body weight. This means that 300 mg of mepivacaine or 10 ml of Mepivastezin is sufficient for patients weighing 70 kg.

Children aged 4 years and older:

The amount of drug administered should be determined by the age and body weight of the child and the duration of the operation; do not exceed a value equivalent to 3 mg of mepivacaine per kg of body weight (0.1 ml of Mepivastasin per kg of body weight).

The drug is intended for injection as a local anesthetic for dental purposes.

In order to exclude the possibility of intravascular injection, it is always necessary to use aspiration control in two projections (with a needle rotation of 180°), although its negative result does not always exclude unintentional or undetected intravascular injection.

The injection rate should not exceed 0.5 ml per 15 seconds, i.e. 1 cartridge per minute.

Major systemic reactions resulting from accidental intravascular injection can in most cases be avoided by using the following administration technique - after the injection, slowly inject 0.1 - 0.2 ml and after 20-30 seconds slowly inject the rest of the solution.

Opened cartridges should not be used on other patients.

The remainder must be liquidated.

Side effects

Rarely (> 0.01%)

    metallic taste in mouth

    nausea, vomiting

    noise in ears

    dizziness

    headache

    nervousness, anxiety

    excitement, anxiety

  • blurred vision

    diplopia

    feeling hot, cold, or numb

    increase in breathing rate

    drowsiness, confusion, tremors, muscle twitching, tonic-clonic seizures, loss of consciousness, coma and respiratory paralysis, respiratory arrest

    tachypnea

    bradypnea

  • cardiovascular failure

Severe cardiovascular attacks manifest themselves as:

    drop in blood pressure

    conduction disturbances

    tachycardia

    bradycardia

    hypotension

  • cardiac arrest

Very rarely (<0,01 %)

    allergic reactions, including skin rashes, urticaria, anaphylactoid reactions, anaphylactic shock, angioedema, fever.

Contraindications

Hypersensitivity to amide-type local anesthetics or allergy to amide-type local anesthetics

Malignant hyperthermia

Severe disturbances in the transmission of nerve impulses and cardiac conduction (eg: 2nd and 3rd degree AV block, severe bradycardia), disturbances in AV conduction that are not supported by a pacemaker

Decompensated heart failure

Severe hypotension

Medically uncontrolled epilepsy

Porphyria

Injections into the inflamed area

Children's age up to 4 years.

Drug interactions

β-blockers and calcium channel blockers increase the inhibition of myocardial conductivity and contractility. If sedatives are used to reduce the patient's fear, the dose of the anesthetic should be reduced, since the latter, like sedatives, depresses the central nervous system.

During treatment with anticoagulants, the risk of bleeding increases (see section "Special instructions").

Patients receiving antiarrhythmic drugs may experience additive side effects following the use of MEPIVASTHEZINE.

Toxic synergism is observed when used together with central analgesics, sedatives, chloroform, ether and sodium thiopental.

special instructions

FOR PROFESSIONAL USE IN DENTAL PRACTICE ONLY.

Before injection, it is necessary to conduct a skin test for hypersensitivity to the drug. An anamnesis should be obtained regarding the simultaneous use of other drugs. If necessary, use benzodiazepines for premedication. The drug should be administered slowly. Administration of low doses may cause insufficient anesthesia and lead to increased drug levels in the blood as a result of accumulation of the drug or its metabolites.

Athletes should be warned that this drug contains an active ingredient that may give a positive result during doping control. Since amide-type local anesthetics are metabolized primarily in the liver and excreted by the kidneys, the drug should be used with caution in patients with liver and kidney diseases. In case of liver failure, it is necessary to reduce the dose of mepivacaine. The dose should also be reduced in cases of hypoxia, hyperkalemia or metabolic acidosis. Increased attention should be paid to patients taking anticoagulants (INR monitoring).

There is a risk of unintentional injury to the mucous membrane due to biting the lip, cheek, or tongue. The patient should be warned not to perform chewing movements during the duration of anesthesia. Avoid erroneous injections and injections into infected or inflamed tissue (the effectiveness of local anesthesia is reduced).

Accidental intravascular administration should be avoided (see section “Dosage and Administration”).

The drug should be used with caution in patients with a history of epilepsy, diabetes mellitus, and cardiovascular diseases, since they have less ability to compensate for the functional changes associated with prolongation of arteriovenous conduction that are caused by drugs.

Precautionary measures

Whenever a local anesthetic is used, the following drugs/therapy measures should be available:

Anticonvulsants (medicines used to treat seizures, such as benzodiazepines or barbiturates), muscle relaxants, atropine, vasoconstrictors, epinephrine for acute allergic or anaphylactic reactions;

Resuscitation equipment (especially oxygen sources) for artificial respiration if necessary;

Carefully and continuously monitor the patient's cardiovascular and respiratory (adequacy of breathing) parameters and state of consciousness after each local anesthetic injection. Restlessness, anxiety, tinnitus, dizziness, blurred vision, trembling, depression or drowsiness are the first signs of CNS toxicity (see section "Overdose").

Mepivastezin should be used with extreme caution in the following cases:

Severe renal dysfunction

Severe liver diseases

Angina pectoris

Atherosclerosis

Marked decrease in blood clotting

In patients taking anticoagulants (eg, heparin) or acetylsalicylic acid, accidental intravascular administration during injection may increase the likelihood of serious bleeding and hemorrhage (see section "Drug Interactions").

Directions for use and doses

Pregnancy and lactation

Pregnancy

There are no sufficient clinical studies regarding the use of Mepivastezin during pregnancy. Animal studies have not provided adequate insight into the effects of use during pregnancy, fetal development, childbirth and postpartum development.

Mepivastezin penetrates the placental barrier and reaches the fetus in the womb.

When using Mepivastezin in the first trimester of pregnancy, the possibility of a risk of malformations cannot be excluded; In early pregnancy, Mepivastezin should be used only if other local anesthetics cannot be used.

Lactation period

There is no sufficient data in what doses Mepivastezin passes into breast milk. If its use is necessary during lactation, breastfeeding should be discontinued and can be resumed after 24 hours.

Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms

In sensitive patients, after injection of Mepivastezin, a temporary worsening of the reaction may occur, for example, during road traffic. The question of whether a patient is allowed to drive a vehicle or work with potentially dangerous mechanisms is decided by the doctor individually in each specific case.

Overdose

Symptoms: may occur immediately, with accidental intravascular injection or under conditions of pathological absorption (eg: inflamed or vascularized tissue) and at a later period and manifest as symptoms of dysfunction of the central nervous system (metallic taste in the mouth, nausea, vomiting, tinnitus, dizziness, agitation, anxiety, increased respiratory rate, drowsiness, confusion, tremor, muscle twitching, tonic-clonic seizures, coma and respiratory paralysis) and/or vascular symptoms (drop in blood pressure, conduction disturbances, bradycardia, cardiac arrest).

Treatment: If side effects occur, immediately stop administering the local anesthetic.

Basic general measures

Diagnostics (respiration, circulation, consciousness), maintenance/restoration of vital functions of breathing and circulation, administration of oxygen, intravenous access.

Special measures

Hypertension: Elevate the patient's upper body and, if necessary, give sublingual nifedipine.

Convulsions: Protect the patient from associated bruises, injuries, if necessary, diazepam intravenously.

Hypotension: Horizontal position of the patient's body, if necessary, intravascular infusion of electrolyte solutions, vasopressors (eg, intravenous epinephrine).

Bradycardia: Atropine IV.

Anaphylactic shock: Contact an emergency physician. Meanwhile, place the patient in a horizontal position and elevate the lower part of the body. Intensive infusion of electrolyte solutions, if necessary - intravenous epinephrine, intravenous glucocorticoid.

Local anesthetic of medium duration of action of the amide group. Causes a reversible block of nerve conduction by reducing the permeability of neuronal membranes to sodium ions. Compared with lidocaine, mepivacaine causes less vasodilation and has a more rapid onset and longer duration of action.
Systemic absorption of mepivacaine depends on the dose, concentration, route of administration, degree of tissue vascularization, and degree of vasodilation. When anesthetizing the teeth of the upper and lower jaw, the effect develops after 0.5-2 and 1-4 minutes, respectively. Anesthesia of the dental pulp lasts for 10-17 minutes, anesthesia of soft tissues in adults lasts 60-100 minutes. With epidural administration, the effect of mepivacaine develops after 7-15 minutes, the duration of action is 115-150 minutes.
Distributed in all tissues, maximum concentrations are created in well-perfused organs, including the liver, lungs, heart and brain. Mepivacaine undergoes rapid metabolism in the liver and is inactivated by hydroxylation and N-demethylation. Three inactive metabolites are known: two phenolic derivatives, which are excreted in the form of glucuronic conjugates, and 2",6"-pipcolokilide. Approximately 50% of pepivacaine is excreted in the bile as metabolites and undergoes enterohepatic recirculation followed by renal excretion. Only 5-10% is excreted unchanged in urine. A certain amount of the drug is metabolized in the lungs. The metabolism of mepivacaine in newborns is limited; the drug is excreted in unchanged form. The half-life is 1.9-3.2 hours in adults and 8.7-9 hours in newborns. Penetrates the placenta through passive diffusion.

Indications for use of the drug Mepivacaine

Infiltration and transtracheal anesthesia, peripheral, sympathetic, regional (Beers method) and epidural nerve blockade for surgical and dental interventions. Not recommended for subarachnoid administration.

Use of the drug Mepivacaine

Infiltration anesthesia:
Adults: up to 40 ml of 1% solution (400 mg) or 80 ml of 0.5% solution (400 mg) in divided doses over 90 minutes.
For blockade of cervical nerves, brachial plexus, intercostal nerves:
Adults - 5-40 ml of 1% solution (50-400 mg) or 5-20 ml of 2% solution (100-400 mg).
Paracervical blockade:
Adults up to 10 ml of 1% solution on each side. Inject slowly with an interval of 5 minutes between injections on the other side.
Peripheral nerve block:
Adults: 1-5 ml of 1-2% solution (10-100 mg) or 1.8 ml of 3% solution (54 mg).
Infiltration anesthesia in dentistry: Adults - 1.8 ml of 3% solution (54 mg). Infiltration is performed slowly with frequent aspiration. In adults, 9 ml (270 mg) of 3% solution is usually sufficient to anesthetize the entire oral cavity. The total dose should not exceed 400 mg.
Children: 1.8 ml of 3% solution (54 mg). Infiltration is performed slowly with frequent aspiration. The maximum dose should not exceed 9 ml (270 mg) of 3% solution.
Epidural or caudal anesthesia:
Adults - 15-30 ml of 1% solution (150-300 mg), 10-25 ml of 1.5% solution (150-375 mg) or 10-20 ml of 2% solution (200-400 mg ).
Maximum doses:
Adults: 400 mg as a single dose for regional administration; the maximum daily dose is 1000 mg.
Children: 5-6 mg/kg. For children under 3 years of age or weighing less than 13.6 kg, mepivacaine solutions are used in concentrations up to 2%.

Contraindications to the use of the drug Mepivacaine

Hypersensitivity to amide local anesthetics, coagulopathy, simultaneous use of anticoagulants, thrombocytopenia, infections, sepsis, shock. Relative contraindications are AV blockade, increased duration Q-T, severe heart and liver diseases, eclampsia, dehydration, arterial hypotension, myasthenia gravis, pregnancy and lactation.

Side effects of the drug Mepivacaine

Nausea, vomiting, hypotension, dizziness, headache, agitation, sinus bradycardia, atrial fibrillation, prolongation P-R And Q-T, AV block, cardiac arrest, respiratory depression, inhibition of uterine contractions, fetal acidosis and bradycardia, injection site reactions, anaphylactic reactions, itching, rash, urticaria, tremor, seizures, urinary incontinence.

Special instructions for the use of Mepivacaine

IV, IV, and intrathecal administration of mepivacaine is prohibited.

Drug interactions Mepivacaine

Local anesthetics (especially when prescribed in large doses) may have an antagonistic effect on neuromuscular transmission compared to cholinesterase inhibitors.
The use of local anesthetics with ganglion blockers may increase the risk of arterial hypotension and bradycardia.
Patients taking MAO inhibitors concomitantly with local anesthetics have an increased risk of developing arterial hypotension.
Local anesthetics may have an additive hypotensive effect in patients taking antihypertensive agents and organic nitrates.

List of pharmacies where you can buy Mepivacaine:

  • Saint Petersburg

International name

Mepivacaine

Group affiliation

Local anesthetic

Dosage form

Injection

pharmachologic effect

Local anesthetic. Blocks voltage-gated sodium channels, which prevents the generation of impulses at the endings of sensory nerves and the conduction of impulses along nerve fibers. Has a fast and strong effect. Duration of effect – 1-3 hours.

Indications

Caudal and lumbar epidural anesthesia, local infiltration anesthesia (for interventions on the oral cavity, tracheal intubation, bronchoesophagoscopy, tonsillectomy; in dentistry), intravenous regional anesthesia (Bayer block), conduction anesthesia (including in dentistry), anesthesia during intubation.

Contraindications

Hypersensitivity (including to other local anesthetic drugs of the amide group), severe liver disease, porphyria, myasthenia gravis.

Side effects

From the central and peripheral nervous system: headache, dizziness, drowsiness, weakness, motor restlessness, disturbances of consciousness, up to its loss, convulsions, trismus, tremor, visual and auditory disturbances, loss of vision, blurred vision, diplopia, nystagmus, cauda equina syndrome (leg paralysis, paresthesia), motor and sensory block.

From the cardiovascular system: decreased blood pressure, collapse (peripheral vasodilation), bradycardia, arrhythmias, chest pain.

From the urinary system: involuntary urination.

From the digestive system: nausea, vomiting, involuntary bowel movements.

Blood disorders: methemoglobinemia.

From the respiratory system: shortness of breath, apnea.

Allergic reactions: skin itching, skin rash, angioedema, other anaphylactic reactions (including anaphylactic shock), urticaria (on the skin and mucous membranes).

Other: hypothermia, decreased potency; during anesthesia in dentistry: insensitivity and paresthesia of the lips and tongue, prolongation of anesthesia, fetal bradycardia.

Local reactions: swelling and inflammation at the injection site.

Application and dosage

For conduction anesthesia (brachial, cervical, intercostal, pudendal) - 5-40 ml (50-400 mg) of a 1% solution or 5-20 ml (100-400 mg) of a 2% solution.

Caudal and lumbar epidural anesthesia - 15-30 ml (150-300 mg) of 1% solution, 10-25 ml (150-375 mg) of 1.5% solution or 10-20 ml (200-400 mg) of 2% solution.

In dentistry: single anesthesia in the upper or lower jaw - 1.8 ml (54 mg) of a 3% solution; local infiltration anesthesia and conduction anesthesia – 9 ml (270 mg) of a 3% solution; the dose required for long-term procedures should not exceed 6.6 mg/kg.

For local infiltration anesthesia (in all cases, except for use in dentistry) - up to 40 ml (400 mg) of a 0.5-1% solution.

For paracervical blockade - up to 10 ml (100 mg) of 1% solution per administration; administration can be repeated no earlier than after 90 minutes.

To relieve pain (therapeutic block) - 1-5 ml (10-50 mg) of a 1% solution or 1-5 ml (20-100 mg) of a 2% solution.

For transvaginal anesthesia (a combination of paracervical and pudendal blockade) – 15 ml (150 mg) of a 1% solution.

Maximum doses in adult patients: in dentistry – 6.6 mg/kg, but not more than 400 mg per administration; for other indications – 7 mg/kg, but not more than 400 mg.

Maximum doses for children: 5-6 mg/kg.

special instructions

It is necessary to discontinue MAO inhibitors 10 days before the planned administration of a local anesthetic.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Interaction

Prescription while taking MAO inhibitors (furazolidone, procarbazine, selegiline) increases the risk of lowering blood pressure.

Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect of mepivacaine.

Mepivacaine enhances the inhibitory effect on the central nervous system caused by other drugs.

Anticoagulants (ardeparin sodium, dalteparin sodium, enoxaparin sodium, heparin, warfarin) 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.

When using mepivacaine for epidural anesthesia with guanethidine, mecamylamine, trimethaphan camsilate, the risk of a pronounced decrease in blood pressure and a decrease in heart rate increases.

Strengthens and prolongs the effect of muscle relaxants.

When prescribed with narcotic analgesics, an additive effect develops, which is used during epidural anesthesia, but this increases respiratory depression.

It exhibits antagonism with antimyasthenic drugs in its effect on skeletal muscles, especially when used in high doses, which requires additional correction in the treatment of myasthenia gravis.

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

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"Mepivacaine" used in the treatment and/or prevention of the following diseases (nosological classification - ICD-10):

Gross formula: C15-H22-N2-O

CAS Code: 22801-44-1

Description

Characteristic: Amide type anesthetic.

Mepivacaine hydrochloride is a white, odorless, crystalline powder. Soluble in water, resistant to both acid and alkaline hydrolysis.

pharmachologic effect

Pharmacology: Pharmacological action - local anesthetic. Being a weak lipophilic base, it passes through the lipid layer of the nerve cell membrane and, transforming into a cationic form, binds to the receptors (residues of S6 transmembrane helical domains) of sodium channels of membranes located at the endings of sensory nerves. Reversibly blocks voltage-gated sodium channels, prevents the flow of sodium ions through the cell membrane, stabilizes the membrane, increases the threshold of electrical stimulation of the nerve, reduces the rate of occurrence of the action potential and reduces its amplitude, and ultimately blocks membrane depolarization, the occurrence and conduction of impulses along nerve fibers.

Causes all types of local anesthesia: terminal, infiltration, conduction. Has a fast and strong effect.

When it enters the systemic circulation (and creates toxic concentrations in the blood), it can have a depressant effect on the central nervous system and myocardium (however, when used in therapeutic doses, changes in conductivity, excitability, automaticity and other functions are minimal).

Dissociation constant (pK_a) - 7.6; Solubility in fats is average. The extent of systemic absorption and plasma concentration depend on the dose, route of administration, vascularization of the injection site and the presence or absence of epinephrine in the anesthetic solution. Adding a dilute solution of epinephrine (1:200,000, or 5 mcg/ml) to a mepivacaine solution usually reduces the absorption of mepivacaine and its plasma concentration. Plasma protein binding is high (about 75%). Penetrates through the placenta. Not affected by plasma esterases. Rapidly metabolized in the liver, the main metabolic pathways are hydroxylation and N-demethylation. In adults, 3 metabolites have been identified - two phenolic derivatives (excreted in the form of glucuronides) and an N-demethylated metabolite (2,6"-pipecoloxylide). T_1/2 in adults - 1.9-3.2 hours; in newborns - 8.7-9 hours. More than 50% of the dose in the form of metabolites is excreted into bile, then reabsorbed in the intestine (a small percentage is found in feces) and excreted in the urine after 30 hours, incl. unchanged (5-10%). Cumulates in case of liver dysfunction (cirrhosis, hepatitis).

Loss of sensitivity is noted after 3-20 minutes. Anesthesia lasts 45-180 minutes. The time parameters of anesthesia (onset time and duration) depend on the type of anesthesia, the technique used, the concentration of the solution (dose of the drug) and the individual characteristics of the patient. The addition of vasoconstrictor solutions is accompanied by prolongation of anesthesia.

Studies assessing carcinogenicity, mutagenicity, and effects on fertility in animals and humans have not been conducted.

Indications for use

Application: Local anesthesia for interventions in the oral cavity (all types), tracheal intubation, broncho- and esophagoscopy, tonsillectomy, etc.

Contraindications

Contraindications: Hypersensitivity, incl. to other amide anesthetics; old age, myasthenia gravis, severe liver dysfunction (including liver cirrhosis), porphyria.

Restrictions for use: Pregnancy, breastfeeding.

Use during pregnancy and breastfeeding: During pregnancy, it is possible if the expected effect of therapy exceeds the potential risk to the fetus (can cause narrowing of the uterine artery and fetal hypoxia). With caution during breastfeeding (no data on penetration into breast milk).

Side effects

Side effects: From the nervous system and sensory organs: agitation and/or depression, headache, ringing in the ears, weakness; impaired speech, swallowing, vision; convulsions, coma.

From the cardiovascular system and blood (hematopoiesis, hemostasis): hypotension (or sometimes hypertension), bradycardia, ventricular arrhythmia, possible cardiac arrest.

Allergic reactions: sneezing, urticaria, pruritis, erythema, chills, fever, angioedema.

Other: depression of the respiratory center, nausea, vomiting.

Interaction: Beta-blockers, calcium channel blockers, antiarrhythmic drugs enhance the inhibitory effect on myocardial conductivity and contractility.

Overdose: Symptoms: hypotension, arrhythmia, increased muscle tone, loss of consciousness, convulsions, hypoxia, hypercapnia, respiratory and metabolic acidosis, dyspnea, apnea, cardiac arrest.

Treatment: hyperventilation, maintenance of adequate oxygenation, assisted breathing, control of convulsions and seizures

(prescription of thiopental 50-100 mg IV or diazepam 5-10 mg IV), normalization of blood circulation, correction of acidosis.

Dosage and method of administration

Directions for use and dosage: The amount of solution and the total dose depend on the type of anesthesia and the nature of the intervention. For injection use a 3% solution of mepivacaine (maximum dose for adults - 4.4 mg/kg, but not more than 300 mg per visit) or a 2% solution in combination with epinephrine (1: 80000, 1: 100000) or norepinephrine ( 1:200000) (maximum dose - 6.6 mg/kg, but not more than 400 mg of mepivacaine per visit). The maximum dose of mepivacaine (in mg) for children is calculated taking into account the child's body weight.

Precautions: Use with caution in patients with hepatitis, liver cirrhosis, liver failure, severe renal impairment, and acidosis.