Mepivacaine in dentistry. Experience in the clinical use of local anesthetics based on mepivacaine. side effects of mepivacaine

A. V. Kuzin

Candidate of Medical Sciences, Dentist-Surgeon of the Federal State Institution "TsNIIS and ChLH" of the Ministry of Health of the Russian Federation, consultant of the 3M ESPE company on pain relief in dentistry

M. V. Stafeeva

dentist-therapist, private practice (Moscow)

V. V. Voronkova

Candidate of Medical Sciences, Dentist-Therapist of the Department of Therapeutic Dentistry of the Clinical and Diagnostic Center of the First Moscow State Medical University. I. M. Sechenov” of the Ministry of Health of Russia

Often in clinical practice there is a need for the use of short-acting anesthetics. There are many small-scale dental interventions that require anesthesia. The use of long-acting anesthetics is not entirely legitimate, since the patient leaves the dentist with numbness in a certain area of ​​​​the oral cavity lasting from 2 to 6 hours.

Taking into account the labor and social burden on the patient, it is justified to use short-acting anesthetics, which can reduce the duration of soft tissue numbness to 30-45 minutes. Today, local anesthetics based on mepivacaine meet these requirements in dentistry.

Mepivacaine is the only amide-type anesthetic that can be used without the addition of a vasoconstrictor. Most amide anesthetics (articaine, lidocaine) dilate blood vessels at the injection site, which leads to their rapid absorption into the bloodstream. This reduces the duration of their action, so anesthetic dosage forms are produced with epinephrine. In the Russian Federation, lidocaine is produced without vasoconstrictors in ampoules, which requires dilution with epinephrine before use. According to modern standards of anesthesia in dentistry, the preparation of a local anesthetic solution by staff is a violation of anesthesia technique. 3% mepivacaine has a less pronounced local vasodilating effect, which allows it to be effectively used to anesthetize the teeth and soft tissues of the oral cavity (Table No. 1).

The duration of action of mepivacaine-containing anesthetics (mepivastezin) is different in certain parts of the oral cavity. This is due to some features of its pharmacological action and features of the anatomy of the oral cavity. According to the instructions of the local anesthetic, the duration of anesthesia of the dental pulp is an average of 45 minutes, anesthesia of soft tissues - up to 90 minutes. These data were obtained as a result of an experimental study in practically healthy patients with anesthesia of single-rooted teeth, mainly in the upper jaw. Naturally, such studies do not reflect the real clinical conditions in which the dentist is faced with inflammation in tissues, chronic neuropathic pain, and individual characteristics of the patient's anatomy. According to Russian scientists, it was found that the average duration of dental pulp anesthesia using 3% mepivacaine is 20-25 minutes, and the duration of soft tissue anesthesia depends on the amount of anesthetic administered and the anesthesia technique (infiltration, conduction) and is 45-60 min.

The question of the speed of onset of local anesthesia is also important. So, when using 3% mepivacaine, the speed of onset of anesthesia of the dental pulp is 5-7 minutes. Therapeutic dental treatment will be most painless for the patient from the 5th to the 20th minute after anesthesia. Surgical treatment will be painless from the 7th to the 20th minute after local anesthesia.

There are some features in the anesthesia of certain groups of teeth with 3% mepivacaine. Numerous studies have proven that it is most effective in the anesthetization of single-rooted teeth. The incisors of the upper and lower jaws are anesthetized with infiltration anesthesia with 3% mepivacaine in a volume of 0.6 ml. At the same time, it is important to take into account the topography of the tops of the roots of the teeth and, accordingly, the depth of advancement of the carpule needle in the tissue. To anesthetize the canines, premolars and molars of the upper jaw, the authors recommend creating an anesthetic depot of 0.8-1.2 ml. Mandibular premolars respond well to anesthesia with 3% mepivacaine: chin anesthesia is performed in various modifications, where an anesthetic depot of up to 0.8 ml is created. It is important after mental anesthesia to carry out finger pressing of soft tissues over the mental foramen for better diffusion of the anesthetic. Infiltration anesthesia in the area of ​​the mandibular molars with 3% mepivacaine is ineffective in comparison with articaine. Anesthesia of mandibular molars with 3% mepivacaine is advisable only in patients with contraindications to the use of articaine-containing anesthetics with epinephrine: in these cases, it is necessary to perform mandibular anesthesia (1.7 ml of 3% mepivacaine). The mandibular canine teeth are also anesthetized with chin or mandibular anesthesia in patients with the above contraindications.

As a result of many years of experience in the clinical use of mepivacaine, indications and clinical recommendations for its use have been developed. Of course, mepivacaine is not an "every day" anesthetic, however, there are a number of clinical cases when its use is most appropriate.

Patients with chronic general somatic diseases. First of all, the use of mepivacaine is most justified in patients with cardiovascular pathology and a restriction on the use of a vasoconstrictor. If a low-traumatic intervention lasting less than 20-25 minutes is planned, there are indications for the use of 3% mepivacaine, which does not affect the patient's hemodynamic parameters (BP, heart rate). If a longer treatment or intervention in the region of the mandibular molars is planned, the use of only articaine-containing anesthetics with a vasoconstrictor 1:200,000 is justified from a clinical point of view.

Patients with aggravated allergic anamnesis. There is a group of patients with bronchial asthma in whom the use of articaine with a vasoconstrictor is contraindicated due to the risk of developing status asthmaticus on the preservatives contained in the carp. Mepivacaine does not contain preservatives (sodium bisulfite), so it can be used for short-term interventions in this group of patients. With longer interventions in this group of patients, it is advisable to carry out dental treatment in specialized institutions under the guidance of an anesthesiologist. Mepivacaine can be used in patients with multivalent allergies and those allergic to a known anesthetic. Outpatient dental treatment of such patients is carried out after the conclusion of the allergist about the tolerability of the drug. According to the clinical experience of the authors of this article, the frequency of positive allergy tests to mepivacaine 3% is significantly lower compared to other carpool anesthetics.

AT therapeutic dentistry mepivacaine is used in the treatment of uncomplicated caries: enamel caries, dentine caries. It is important to consider that the required duration of anesthesia is limited to the stage of preparation of hard tissues of the tooth. After covering the formed cavity with an adhesive material, further restoration will be painless. Accordingly, any planned invasive treatment should not exceed 15 minutes after the onset of anesthesia. Also, when planning treatment, one should take into account the low effectiveness of mepivacaine in anesthesia of the canines and molars of the lower jaw with infiltration anesthesia and with intraligamentary anesthesia of the teeth of the lower jaw.

AT surgical dentistry mepivacaine is used for short-term surgical interventions. The highest efficiency was found in the extraction of teeth with chronic periodontitis and in the extraction of intact teeth for orthodontic indications. The role of mepivacaine in anesthesia during surgical dressings is also important. Often, the procedure for removing sutures, changing the wound dressing in the tooth socket, and changing the iodoform dressing are painful for patients. The use of long-acting anesthetics is unjustified due to the subsequent prolonged numbness of the soft tissues, which can lead to self-injury to the surgical area when eating. In these cases, infiltration anesthesia is used in a volume of 0.2-0.4 ml of 3% mepivacaine, and for dressings after extensive surgical interventions (cystectomy, excision of soft tissue formations, removal of an impacted third molar), conduction anesthesia is performed. The use of mepivacaine in outpatient surgical dressings can reduce patient discomfort and stress.

Dentistry of children's age. Short-acting anesthetics have proven themselves well when used in pediatric dentistry. When using mepivacaine, the dosage of this drug should be considered when performing local anesthesia in children. Mepivacaine is more toxic to the CNS than articaine because it is rapidly absorbed into the bloodstream. Also, the clearance of mepivacaine is higher than the clearance of articaine by several hours. The maximum dosage of 3% mepivacaine is 4 mg/kg in a child over 4 years of age (Table 2). However, in pediatric dentistry there are no indications for the use of such high volumes of anesthetic. According to current safety standards, the dosage of administered 3% mepivacaine should not exceed half the maximum dose for all dental treatments. With this application, cases of local anesthetic overdose (weakness, drowsiness, headaches) in pediatric practice are excluded.

When using mepivacaine, cases of self-injury of the soft tissues of the oral cavity by a child after treatment by a dentist are practically excluded. According to statistics, up to 25-35% of preschool children injure the lower lip after the treatment of the lower teeth, and in most cases this is associated with the use of long-acting anesthetics based on articaine with a vasoconstrictor. Short-acting local anesthetics can be used when sealing tooth fissures, treating initial forms of caries, and removing temporary teeth. Especially justified is the use of mepivacaine in children with polyvalent allergies, bronchial asthma, since the drug does not contain preservatives (EDTA, sodium bisulfite).

Pregnancy and lactation. Mepivacaine can be safely used in pregnant women during routine oral hygiene at the dentist for the above indications. In most cases, 3% mepivacaine is used for short-term and minimally invasive interventions lasting up to 20 minutes. The most favorable for treatment is the second trimester of pregnancy.

Mepivacaine can be used in breastfeeding women, it is found in the mother's breast milk in a small concentration for the child. Nevertheless, the patient is advised to refrain from feeding the child for 10-12 hours after anesthesia with 3% mepivacaine and for 2 hours after anesthesia with 4% articaine with epinephrine, which completely eliminates the effect of the anesthetic on the child.

conclusions

Thus, mepivacaine-containing anesthetics (Mepivastezin) have found their application in various fields of dentistry. For a separate group of patients, these anesthetics are the only drugs for local anesthesia due to general somatic features. As a short-acting anesthetic, the drug can be well used for minimally invasive short-term interventions.

Table No. 1. Features of the clinical use of 3% mepivacaine (Mepivastezin)

Table No. 2. Dosage of 3% mepivacaine based on patient weight (adult/child)

Catad_pgroup Local anesthetics

Mepivacaine-Binergia - instructions for use

Registration number:

Trade name:

Mepivacaine-Bynergia

International non-proprietary name:

mepivacaine

Dosage form:

injection

Compound

1 ml of the drug contains:
active substance: mepivacaine hydrochloride - 30 mg;
Excipients: sodium chloride, water for injection.

Description

Clear colorless solution

Pharmacotherapeutic group

Local anesthetic

ATC code:

Pharmacological properties

Pharmacodynamics
Mepivacaine is an amide-type local anesthetic. Injected near sensory nerve endings or nerve fibers, mepivacaine reversibly blocks voltage-dependent sodium channels, prevents the generation of impulses at the endings of sensory nerves and the conduction of pain impulses in the nervous system. Mepivacaine is lipophilic with a pKa value of 7.6. Mepivacaine penetrates the nerve membrane in the basic form, then, after reprotonation, it has a pharmacological effect in the ionized form. The ratio of these forms of mepivacaine is determined by the pH value of the tissues in the anesthetized area. At low tissue pH values, such as in inflamed tissues, the main form of mepivacaine is present in small amounts, and therefore anesthesia may be insufficient.
Unlike most local anesthetics with vasodilating properties, mepivacaine does not have a pronounced effect on blood vessels and can be used in dentistry without a vasoconstrictor.
The time parameters of anesthesia (start time and duration) depend on the type of anesthesia, the technique used for its implementation, the concentration of the solution (dose of the drug) and the individual characteristics of the patient.
With peripheral nerve blockade, the effect of the drug occurs after 2-3 minutes.
The average duration of action for pulp anesthesia is 20-40 minutes, and for soft tissue anesthesia - 2-3 hours.
The duration of motor blockade does not exceed the duration of anesthesia.

Pharmacokinetics
suction, distribution
When injected into the tissues of the maxillofacial region by conduction or infiltration anesthesia, the maximum concentration of mepivacaine in the blood plasma is reached approximately 30-60 minutes after the injection. The duration of action is determined by the rate of diffusion from the tissues into the bloodstream. The distribution coefficient is 0.8. Plasma protein binding is 69-78% (mainly with alpha-1-acid glycoprotein).
The degree of bioavailability reaches 100% in the field of action.
Metabolism
Mepivacaine is rapidly metabolized in the liver (subject to hydrolysis by microsomal enzymes) by hydroxylation and dealkylation to m-hydroxymepivacaine, p-hydroxymepivacaine, pipecolylxylidine, and only 5-10% is excreted unchanged by the kidneys.
It undergoes hepato-intestinal recirculation.
breeding
Excreted by the kidneys, mainly in the form of metabolites. Metabolites are mainly excreted from the body with bile. The half-life (T 1/2) is long and ranges from 2 to 3 hours. The plasma half-life of mepivacaine is increased in patients with impaired hepatic function and/or in the presence of uremia. In liver pathology (cirrhosis, hepatitis), mepivacaine may accumulate.

Indications for use

Infiltration, conduction, intraligamentary, intraosseous and intrapulpal anesthesia in surgical and other painful dental interventions.
The drug does not contain a vasoconstrictor component, which allows it to be used in patients with diseases of the cardiovascular system, diabetes mellitus, angle-closure glaucoma.

Contraindications

• hypersensitivity to mepivacaine (including other local anesthetic drugs of the amide group) or other excipients that make up the drug;
• severe liver disease: cirrhosis, hereditary or acquired porphyria;
• myasthenia gravis;
• children's age up to 4 years (body weight less than 20 kg);
• heart rhythm and conduction disturbances;
• acute decompensated heart failure;
• arterial hypotension;
• intravascular administration (before the administration of the drug, it is necessary to conduct an aspiration test, see the section "Special Instructions").

Carefully

• conditions accompanied by a decrease in hepatic blood flow (for example, chronic heart failure, diabetes mellitus, liver disease);
• progression of cardiovascular insufficiency;
• inflammatory diseases or infection of the injection site;
• pseudocholinesterase deficiency;
• kidney failure;
• hyperkalemia;
• acidosis;
• old age (over 65 years);
• atherosclerosis;
• vascular embolism;
• diabetic polyneuropathy.

Use during pregnancy and during breastfeeding

Pregnancy
During pregnancy, local anesthesia is considered the safest method for relieving pain during dental procedures. The drug does not affect the course of pregnancy, however, due to the fact that mepivacaine can cross the placenta, it is necessary to evaluate the benefit to the mother and the risk to the fetus, especially in the first trimester of pregnancy.
breastfeeding period
Local anesthetics, including mepivacaine, are excreted to a small extent into breast milk. With a single use of the drug, a negative effect on the child is unlikely. It is not recommended to breastfeed within 10 hours after using the drug.

Dosage and administration

The amount of solution and the total dose depend on the type of anesthesia and the nature of the surgical intervention or manipulation.
The rate of administration should not exceed 1 ml of the drug in 1 minute.
Aspiration control should always be performed to avoid intravenous administration.
Use the smallest dose of the drug that provides sufficient anesthesia.
The average single dose is 1.8 ml (1 cartridge).
Do not use already opened cartridges to treat other patients. Cartridges with unused residue of the drug must be disposed of.
adults
The recommended maximum single dose of mepivacaine hydrochloride is 300 mg (4.4 mg/kg body weight), which corresponds to 10 ml of the drug (about 5.5 cartridges).
Children over 4 years of age (weighing over 20 kg)
The amount of the drug depends on age, body weight and the nature of the surgical intervention. The average dose is 0.75 mg / kg of body weight (0.025 ml of the drug / kg of body weight).
The maximum dose of mepivacaine is 3 mg/kg of body weight, which corresponds to 0.1 ml of the drug/kg of body weight.

Special patient groups
In the elderly, an increase in the concentration of the drug in the blood plasma is possible due to a slowdown in metabolism. In this group of patients, it is necessary to use the minimum dose that provides sufficient anesthesia.
In patients with renal or hepatic insufficiency, as well as in patients with hypoxia, hyperkalemia or metabolic acidosis, it is also necessary to use the minimum dose that provides sufficient anesthesia.
In patients with diseases such as vascular embolism, atherosclerosis or diabetic polyneuropathy, it is necessary to reduce the dose of the drug by a third.

Side effect

Possible side effects when using the drug Mepivacaine-Binergia are similar to the side effects that occur when taking local anesthetics of the amide type. The most common disorders are those of the nervous system and the cardiovascular system. Serious side effects are systemic.
Side effects are grouped by systems and organs in accordance with the MedDRA dictionary and the WHO classification of the incidence of adverse reactions: very often (≥1/10), often (≥1/100 to<1/10), нечасто (≥1/1000 до <1/100), редко (≥1/10000 до <1/1000), очень редко (<1 /10000), частота неизвестна (частота не может быть определена на основе имеющихся данных).

Overdose

Overdose is possible with unintentional intravascular administration of the drug or as a result of exceptionally rapid absorption of the drug. The critical threshold dose is a concentration of 5-6 micrograms of mepivacaine hydrochloride per 1 ml of blood plasma.
Symptoms
From the side of the central nervous system
Mild intoxication - paresthesia and numbness of the oral cavity, tinnitus, "metallic" taste in the mouth, fear, anxiety, tremor, muscle twitching, vomiting, disorientation.
Moderate intoxication - dizziness, nausea, vomiting, speech disorder, numbness, drowsiness, confusion, tremor, choreiform movements, tonic-clonic convulsions, dilated pupils, rapid breathing.
Severe intoxication - vomiting (risk of suffocation), sphincter paralysis, loss of muscle tone, lack of reaction and akinesia (stupor), irregular breathing, respiratory arrest, coma, death.
From the side of the heart and blood vessels
Mild intoxication - increased blood pressure, rapid heartbeat, rapid breathing.
Moderate intoxication - palpitations, arrhythmia, hypoxia, pallor. Severe intoxication - severe hypoxia, cardiac arrhythmia (bradycardia, lowering blood pressure, primary heart failure, ventricular fibrillation, asystole).
Treatment
When the first signs of an overdose appear, it is necessary to immediately stop the administration of the drug, as well as provide support for respiratory function, if possible with the use of oxygen, monitor pulse and blood pressure.
In case of respiratory failure - oxygen, endotracheal intubation, artificial ventilation of the lungs (central analeptics are contraindicated).
In case of hypertension, it is necessary to raise the upper part of the patient's torso, if necessary - nifedipine sublingually.
In case of hypotension, it is necessary to bring the position of the patient's body to a horizontal position, if necessary, intravascular administration of an electrolyte solution, vasoconstrictor drugs. If necessary, the volume of circulating blood is compensated (for example, with crystalloid solutions).
With bradycardia, atropine (0.5 to 1 mg) is administered intravenously.
With convulsions, it is necessary to protect the patient from concomitant injuries, if necessary, intravenous diazepam (5 to 10 mg) is administered. With prolonged convulsions, sodium thiopental (250 mg) and a short-acting muscle relaxant are administered, after intubation, artificial ventilation of the lungs with oxygen is performed.
In severe circulatory disorders and shock - intravenous infusion of electrolyte solutions and plasma substitutes, glucocorticosteroids, albumin.
With severe tachycardia and tachyarrhythmia - intravenous beta-blockers (selective).
In cardiac arrest, cardiopulmonary resuscitation should be performed immediately.
When using local anesthetics, it is necessary to provide access to a ventilator, drugs that increase blood pressure, atropine, anticonvulsants.

Interaction with other drugs

Appointment while taking monoamine oxidase (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. With simultaneous use with sedatives, a dose reduction of mepivacaine is required.
Anticoagulants (sodium ardeparin, dalteparin, enoxaparin, warfarin) and low molecular weight heparin preparations increase the risk of bleeding.
When treating the injection site of mepivacaine with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.
Enhances and prolongs the action of muscle relaxant drugs.
When administered with narcotic analgesics, an additive inhibitory effect on the central nervous system develops.
There is antagonism with antimyasthenic drugs in terms of action 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.
With simultaneous use with blockers of H 2 -histamine receptors (cimetidine), an increase in the level of mepivacaine in the blood serum is possible.
With simultaneous use with antiarrhythmic drugs (tocainide, sympatholytics, digitalis preparations), side effects may increase.

special instructions

It is necessary to cancel MAO inhibitors 10 days before the planned introduction of a local anesthetic.
Use only in a medical institution.
After opening the ampoule, immediate use of the contents is recommended.
The drug must be administered slowly and continuously. When using the drug, it is necessary to control the patient's blood pressure, pulse and diameter of the pupils.
Before using the drug, it is necessary to provide access to resuscitation equipment.
Patients treated with anticoagulants have an increased risk of bleeding and bleeding.
The anesthetic effect of the drug may be reduced when injected into an inflamed or infected area.
When using the drug, unintentional injury to the lips, cheeks, mucous membrane and tongue is possible, especially in children, due to a decrease in sensitivity.
The patient should be warned that eating is possible only after the restoration of sensitivity.
Before the introduction of the drug, it is always necessary to carry out aspiration control to avoid intravascular injection.
Regional and local anesthesia should be performed by experienced professionals in an appropriately equipped room with the availability of equipment and preparations ready for immediate use, necessary for cardiac monitoring and resuscitation. Anesthesia personnel should be qualified and trained in anesthesia technique and should be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.
1 ml of the drug contains 0.05 mmol (1.18 mg) of sodium.

Influence on the ability to drive vehicles, mechanisms

The drug has a slight effect on the ability to drive vehicles and mechanisms. During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

Release form

Solution for injections 30 mg/ml.
1.7 ml, 1.8 ml of the drug in transparent colorless glass cartridges of the 1st hydrolytic class, sealed on one side with plungers made of elastomeric material, and on the other hand with combined caps for dental cartridges for local anesthesia, consisting of a disk of elastomeric material and anodized aluminum cap.
10 cartridges in a contour plastic package (pallet) or in a contour cell package; or in an insert for fixing the cartridges.
1.5, 10 blister packs (pallets) or blister packs or inserts with cartridges along with instructions for use in a cardboard pack.
Two protective labels with the company logo are glued onto the pack with cartridges (first opening control).
2 ml of the drug in ampoules of transparent colorless glass of the 1st hydrolytic class or neutral glass of the HC-3 brand.
5 ampoules in a contour plastic package (pallet).
1, 2 contour plastic packages (pallets) with ampoules along with instructions for use and an ampoule knife or an ampoule scarifier in a cardboard pack.
When using ampoules with a colored break point and a notch or a colored break ring, the ampoule knife or ampoule scarifier is not inserted.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Do not freeze.
Keep out of the reach of children.

Best before date

5 years
Do not use after the expiry date stated on the package.

Holiday conditions

Released by prescription.

Legal entity in whose name the registration certificate is issued / Organization accepting claims:

CJSC "Binergia", Russia, 143910, Moscow region, Balashikha, st. Krupeshina, d. 1.

Manufacturer and place of production:

FKP "Armavir biofactory", Russia, 352212, Krasnodar Territory, Novokubansky district, Progress settlement, st. Mechnikova, 11.

A. V. Kuzin

Candidate of Medical Sciences, Dentist-Surgeon of the Federal State Institution "TsNIIS and ChLH" of the Ministry of Health of the Russian Federation, consultant of the 3M ESPE company on pain relief in dentistry

M. V. Stafeeva

dentist-therapist, private practice (Moscow)

V. V. Voronkova

Candidate of Medical Sciences, Dentist-Therapist of the Department of Therapeutic Dentistry of the Clinical and Diagnostic Center of the First Moscow State Medical University. I. M. Sechenov” of the Ministry of Health of Russia

Often in clinical practice there is a need for the use of short-acting anesthetics. There are many small-scale dental interventions that require anesthesia. The use of long-acting anesthetics is not entirely legitimate, since the patient leaves the dentist with numbness in a certain area of ​​​​the oral cavity lasting from 2 to 6 hours.

Taking into account the labor and social burden on the patient, it is justified to use short-acting anesthetics, which can reduce the duration of soft tissue numbness to 30-45 minutes. Today, local anesthetics based on mepivacaine meet these requirements in dentistry.

Mepivacaine is the only amide-type anesthetic that can be used without the addition of a vasoconstrictor. Most amide anesthetics (articaine, lidocaine) dilate blood vessels at the injection site, which leads to their rapid absorption into the bloodstream. This reduces the duration of their action, so anesthetic dosage forms are produced with epinephrine. In the Russian Federation, lidocaine is produced without vasoconstrictors in ampoules, which requires dilution with epinephrine before use. According to modern standards of anesthesia in dentistry, the preparation of a local anesthetic solution by staff is a violation of anesthesia technique. 3% mepivacaine has a less pronounced local vasodilating effect, which allows it to be effectively used to anesthetize the teeth and soft tissues of the oral cavity (Table No. 1).

The duration of action of mepivacaine-containing anesthetics (mepivastezin) is different in certain parts of the oral cavity. This is due to some features of its pharmacological action and features of the anatomy of the oral cavity. According to the instructions of the local anesthetic, the duration of anesthesia of the dental pulp is an average of 45 minutes, anesthesia of soft tissues - up to 90 minutes. These data were obtained as a result of an experimental study in practically healthy patients with anesthesia of single-rooted teeth, mainly in the upper jaw. Naturally, such studies do not reflect the real clinical conditions in which the dentist is faced with inflammation in tissues, chronic neuropathic pain, and individual characteristics of the patient's anatomy. According to Russian scientists, it was found that the average duration of dental pulp anesthesia using 3% mepivacaine is 20-25 minutes, and the duration of soft tissue anesthesia depends on the amount of anesthetic administered and the anesthesia technique (infiltration, conduction) and is 45-60 min.

The question of the speed of onset of local anesthesia is also important. So, when using 3% mepivacaine, the speed of onset of anesthesia of the dental pulp is 5-7 minutes. Therapeutic dental treatment will be most painless for the patient from the 5th to the 20th minute after anesthesia. Surgical treatment will be painless from the 7th to the 20th minute after local anesthesia.

There are some features in the anesthesia of certain groups of teeth with 3% mepivacaine. Numerous studies have proven that it is most effective in the anesthetization of single-rooted teeth. The incisors of the upper and lower jaws are anesthetized with infiltration anesthesia with 3% mepivacaine in a volume of 0.6 ml. At the same time, it is important to take into account the topography of the tops of the roots of the teeth and, accordingly, the depth of advancement of the carpule needle in the tissue. To anesthetize the canines, premolars and molars of the upper jaw, the authors recommend creating an anesthetic depot of 0.8-1.2 ml. Mandibular premolars respond well to anesthesia with 3% mepivacaine: chin anesthesia is performed in various modifications, where an anesthetic depot of up to 0.8 ml is created. It is important after mental anesthesia to carry out finger pressing of soft tissues over the mental foramen for better diffusion of the anesthetic. Infiltration anesthesia in the area of ​​the mandibular molars with 3% mepivacaine is ineffective in comparison with articaine. Anesthesia of mandibular molars with 3% mepivacaine is advisable only in patients with contraindications to the use of articaine-containing anesthetics with epinephrine: in these cases, it is necessary to perform mandibular anesthesia (1.7 ml of 3% mepivacaine). The mandibular canine teeth are also anesthetized with chin or mandibular anesthesia in patients with the above contraindications.

As a result of many years of experience in the clinical use of mepivacaine, indications and clinical recommendations for its use have been developed. Of course, mepivacaine is not an "every day" anesthetic, however, there are a number of clinical cases when its use is most appropriate.

Patients with chronic general somatic diseases. First of all, the use of mepivacaine is most justified in patients with cardiovascular pathology and a restriction on the use of a vasoconstrictor. If a low-traumatic intervention lasting less than 20-25 minutes is planned, there are indications for the use of 3% mepivacaine, which does not affect the patient's hemodynamic parameters (BP, heart rate). If a longer treatment or intervention in the region of the mandibular molars is planned, the use of only articaine-containing anesthetics with a vasoconstrictor 1:200,000 is justified from a clinical point of view.

Patients with aggravated allergic anamnesis. There is a group of patients with bronchial asthma in whom the use of articaine with a vasoconstrictor is contraindicated due to the risk of developing status asthmaticus on the preservatives contained in the carp. Mepivacaine does not contain preservatives (sodium bisulfite), so it can be used for short-term interventions in this group of patients. With longer interventions in this group of patients, it is advisable to carry out dental treatment in specialized institutions under the guidance of an anesthesiologist. Mepivacaine can be used in patients with multivalent allergies and those allergic to a known anesthetic. Outpatient dental treatment of such patients is carried out after the conclusion of the allergist about the tolerability of the drug. According to the clinical experience of the authors of this article, the frequency of positive allergy tests to mepivacaine 3% is significantly lower compared to other carpool anesthetics.

AT therapeutic dentistry mepivacaine is used in the treatment of uncomplicated caries: enamel caries, dentine caries. It is important to consider that the required duration of anesthesia is limited to the stage of preparation of hard tissues of the tooth. After covering the formed cavity with an adhesive material, further restoration will be painless. Accordingly, any planned invasive treatment should not exceed 15 minutes after the onset of anesthesia. Also, when planning treatment, one should take into account the low effectiveness of mepivacaine in anesthesia of the canines and molars of the lower jaw with infiltration anesthesia and with intraligamentary anesthesia of the teeth of the lower jaw.

AT surgical dentistry mepivacaine is used for short-term surgical interventions. The highest efficiency was found in the extraction of teeth with chronic periodontitis and in the extraction of intact teeth for orthodontic indications. The role of mepivacaine in anesthesia during surgical dressings is also important. Often, the procedure for removing sutures, changing the wound dressing in the tooth socket, and changing the iodoform dressing are painful for patients. The use of long-acting anesthetics is unjustified due to the subsequent prolonged numbness of the soft tissues, which can lead to self-injury to the surgical area when eating. In these cases, infiltration anesthesia is used in a volume of 0.2-0.4 ml of 3% mepivacaine, and for dressings after extensive surgical interventions (cystectomy, excision of soft tissue formations, removal of an impacted third molar), conduction anesthesia is performed. The use of mepivacaine in outpatient surgical dressings can reduce patient discomfort and stress.

Dentistry of children's age. Short-acting anesthetics have proven themselves well when used in pediatric dentistry. When using mepivacaine, the dosage of this drug should be considered when performing local anesthesia in children. Mepivacaine is more toxic to the CNS than articaine because it is rapidly absorbed into the bloodstream. Also, the clearance of mepivacaine is higher than the clearance of articaine by several hours. The maximum dosage of 3% mepivacaine is 4 mg/kg in a child over 4 years of age (Table 2). However, in pediatric dentistry there are no indications for the use of such high volumes of anesthetic. According to current safety standards, the dosage of administered 3% mepivacaine should not exceed half the maximum dose for all dental treatments. With this application, cases of local anesthetic overdose (weakness, drowsiness, headaches) in pediatric practice are excluded.

When using mepivacaine, cases of self-injury of the soft tissues of the oral cavity by a child after treatment by a dentist are practically excluded. According to statistics, up to 25-35% of preschool children injure the lower lip after the treatment of the lower teeth, and in most cases this is associated with the use of long-acting anesthetics based on articaine with a vasoconstrictor. Short-acting local anesthetics can be used when sealing tooth fissures, treating initial forms of caries, and removing temporary teeth. Especially justified is the use of mepivacaine in children with polyvalent allergies, bronchial asthma, since the drug does not contain preservatives (EDTA, sodium bisulfite).

Pregnancy and lactation. Mepivacaine can be safely used in pregnant women during routine oral hygiene at the dentist for the above indications. In most cases, 3% mepivacaine is used for short-term and minimally invasive interventions lasting up to 20 minutes. The most favorable for treatment is the second trimester of pregnancy.

Mepivacaine can be used in breastfeeding women, it is found in the mother's breast milk in a small concentration for the child. Nevertheless, the patient is advised to refrain from feeding the child for 10-12 hours after anesthesia with 3% mepivacaine and for 2 hours after anesthesia with 4% articaine with epinephrine, which completely eliminates the effect of the anesthetic on the child.

conclusions

Thus, mepivacaine-containing anesthetics (Mepivastezin) have found their application in various fields of dentistry. For a separate group of patients, these anesthetics are the only drugs for local anesthesia due to general somatic features. As a short-acting anesthetic, the drug can be well used for minimally invasive short-term interventions.

Table No. 1. Features of the clinical use of 3% mepivacaine (Mepivastezin)

Table No. 2. Dosage of 3% mepivacaine based on patient weight (adult/child)

5685 0

Mepivacainum
Local anesthetics of the amide group

Release form

Mechanism of action

It is used in the form of hydrochloric acid salt, which undergoes hydrolysis in a slightly alkaline environment of tissues. The liberated lipophilic base of the anesthetic penetrates the membrane of the nerve fiber, passes into the active cationic form, which interacts with the membrane receptors. The permeability of the membrane for sodium ions is disturbed, and the conduction of an impulse along the nerve fiber is blocked.

Mepivacaine, unlike most local anesthetics, does not have a pronounced vasodilating effect, which leads to a longer duration of its effect and the possibility of using it without a vasoconstrictor.

Pharmacokinetics

Hydroxylation and N-demethylation play an important role in the process of biotransformation. T1 / 2 is about 90 minutes. In newborns, the activity of liver enzymes is not high enough, which significantly lengthens T1 / 2. Mepivacaine is excreted by the kidneys, mainly as metabolites. In unchanged form, from 1 to 16% of the administered dose is excreted.

The dissociation constant of mepivacaine (pK 7.8), in connection with which it is rapidly hydrolyzed at a slightly alkaline pH of tissues, easily penetrates tissue membranes, creating a high concentration on the receptor.

Indications

Dosage and administration

Contraindications

Precautions, therapy control

Prescribe with caution:
■ in severe cardiovascular diseases;
■ with diabetes;
■ during pregnancy and lactation;
■ children and elderly patients;
■ all mepivacaine solutions containing vasoconstrictors should be used with caution in patients with cardiovascular and endocrine diseases (thyrotoxicosis, diabetes mellitus, heart defects, arterial hypertension, etc.), as well as those receiving β-blockers, tricyclic antidepressants and MAO inhibitors.

Side effects

Allergic reactions (urticaria, angioedema) are rare. Cross-allergy with other local anesthetics has not been noted.

Overdose

Treatment: CNS symptoms are corrected with the use of short-acting barbiturates or tranquilizers of the benzodiazepine group; for the correction of bradycardia and conduction disorders, anticholinergics are used, with arterial hypotension - adrenomimetics.

Interaction

Synonyms

G.M. Barer, E.V. Zoryan

Tradename

Mepivastezin

International non-proprietary 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 largely absorbed. Plasma protein binding is 60-78% and the elimination half-life is about 2 hours.

The volume of distribution is 84 liters. Clearance - 0.78 l / min.

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

Pharmacodynamics

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

The drug easily diffuses 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 an anesthetic base is difficult.

Indications for use

Infiltration and conduction anesthesia in dentistry:

Uncomplicated tooth extraction

When preparing carious cavities and teeth for a crown

Dosage and administration

As far as possible, the smallest volume of solution that promotes effective anesthesia should be prescribed.

In 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 the administered drug 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 mepivastezin/kg body weight).

Plasma levels of mepivacaine may be increased in elderly patients due to reduced metabolic processes and a lower volume of distribution of the drug.

The risk of accumulation of mepivacaine increases with repeated applications. A similar effect can be observed with a decrease in the general condition of the patient, as well as with severe violations of the liver and kidneys. 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, atherosclerosis.

Adults:

For adults, the maximum dose is 4 mg mepivacaine per kg of body weight and is equivalent to 0.133 ml of mepivastezin per kg of 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 over:

The amount of the administered drug 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 mepivastezin 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 apply aspiration control in two projections (with a rotation of the needle by 180 °), although its negative result does not always rule out unintentional or unnoticed intravascular injection.

The injection rate should not exceed 0.5 ml in 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 injection technique - after the injection, slowly inject 0.1-0.2 ml and slowly inject the rest of the solution after 20-30 seconds.

Opened cartridges should not be used in other patients.

The rest must be liquidated.

Side effects

Rare (> 0.01%)

metallic taste in the mouth

nausea, vomiting

noise in ears

dizziness

headache

nervousness, anxiety

agitation, anxiety

• blurred vision

  diplopia

  feeling hot, cold, or numb

  increase in respiratory rate

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

  tachypnea

  bradypnea

• cardiovascular failure

Severe cardiovascular attacks are manifested in the form of:

falling blood pressure

conduction disorders

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 disorders of the transmission of nerve impulses and conduction of the heart (for example: AV block II and III degree, severe bradycardia), AV conduction disorders that are not supported by a pacemaker

Decompensated heart failure

severe hypotension

Medically uncontrolled epilepsy

porfiria

Injections into the inflamed area

Children's age up to 4 years.

Drug Interactions

β-blockers, calcium channel blockers increase the inhibition of conduction and myocardial contractility. If sedatives are used to reduce the patient's fear, the dose of 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").

In patients receiving antiarrhythmic drugs, there may be a summation of side effects after the use of MEPIVASTESIN.

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

special instructions

FOR PROFESSIONAL USE ONLY In dental practice.

Before the injection, it is necessary to conduct a skin test for hypersensitivity to the drug. An anamnesis should be collected regarding the simultaneous use of other drugs. Use benzodiazepines for premedication if necessary. The drug should be administered slowly. The introduction of low doses can cause insufficient anesthesia and lead to an increase in the level of the drug in the blood as a result of the accumulation of the drug or its metabolites.

Athletes should be warned that this preparation contains an active ingredient that may give a positive result in doping controls. Since local anesthetics of the amide type are metabolized mainly in the liver and excreted by the kidneys, the drug should be used with caution in patients with liver and kidney disease. In hepatic insufficiency, 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 of the lip, cheek, tongue. The patient should be warned not to chew during the anesthesia. Erroneous injections and injections into infected or inflamed tissues should be avoided (the effectiveness of local anesthesia decreases).

It is necessary to avoid accidental intravascular injection (see section "Method of administration and doses".

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

Precautionary measures

Each time a local anesthetic is applied, the following drugs/treatments should be available:

Anticonvulsants (seizure medications such as benzodiazepines or barbiturates), muscle relaxants, atropine, vasoconstrictors, adrenaline for acute allergic or anaphylactic reactions;

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

Careful and continuous monitoring of the cardiovascular and respiratory (breathing adequacy) indicators of the state of the body and the state of consciousness of the patient after each injection of local anesthetic. 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 cases of:

Severe renal dysfunction

Severe liver disease

angina pectoris

atherosclerosis

Marked decrease in blood clotting

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

Dosage and administration

Pregnancy and lactation

Pregnancy

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

Mepivastezin crosses 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 are no sufficient data at what doses Mepivastezin passes into breast milk. If its use is necessary during lactation, breastfeeding should be stopped and it can be resumed after 24 hours.

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

In sensitive patients, after an injection of mepivastezin, a temporary worsening of the reaction may occur, for example, during traffic. The issue of allowing a patient 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 abnormal absorption (eg, inflamed or vascularized tissue) and later, and manifest as symptoms of central nervous system dysfunction (metallic taste in the mouth, nausea, vomiting, tinnitus, dizziness, agitation, restlessness, increased respiratory rate, drowsiness, confusion, tremors, muscle twitches, tonic-clonic convulsions, coma and respiratory paralysis) and / or vascular symptoms (drop in blood pressure, conduction disturbances, bradycardia, cardiac arrest).

Treatment: in case of side effects, immediately stop the introduction of local anesthetic.

Basic general measures

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

Special Measures

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

Convulsions: Protect the patient from concomitant bruising, injury, if necessary, diazepam IV.

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

Bradycardia: Atropine IV.

Anaphylactic shock: Contact an emergency doctor. In the meantime, put the patient in a horizontal position, raise the lower part of the body. Intensive infusion of electrolyte solutions, if necessary, i.v. epinephrine, i.v. glucocorticoid.