Mepivacaine is a substance for conducting local anesthesia, is widely used in dentistry. Belongs to the group of amide-type anesthetics. Has a strong and fast action, which lasts up to three hours.
This is crystalline powder white with no odor. It is easily soluble in water and is resistant to alkaline and acid hydrolysis. It is used for all types of local anesthesia (, terminal, etc.).
The mechanism of action of this substance is aimed at stabilizing cell membranes. By acting on nerve endings, the substance blocks the transmission of impulses to the central nervous system, promoting temporary loss of sensitivity.
All of them are used for pain relief surgical interventions in the oral cavity.
Release form and composition
The product is released in the form of an injection solution. IN cardboard box Packed in small ampoules of 1.7 or 1.8 ml. 1 milliliter of the drug contains:
- mepivacaine hydrochloride – 30 mg;
- sodium chloride – 6 mg;
- water for injections – 1 ml.
The most famous drugs based on Mepivacaine: 
- Isocaine;
- Mepicaton;
Pharmacological profile
The drug is similar in its properties and pharmacokinetics to Lidocaine. Characterized by good absorption and rapid metabolism in the liver. Up to 80% binds to plasma proteins. Penetrates through the placental barrier.
The substance is excreted by the kidneys in the form of metabolites. Up to 16% of the substance can be excreted unchanged. With a slightly alkaline balance in tissues, it quickly hydrolyzes, penetrating through cell membranes, concentrating on receptors.
The main difference from many other anesthetics is the lack of a pronounced effect on vasodilation. This determines the duration of its effect.
Indications and restrictions for use
Mepivacaine is used in dental practice in the following cases:
Suitable for patients with diabetes mellitus, cardiovascular failure.
The use of the drug is prohibited in the following cases:
- individual intolerance to anesthetic components;
- hypersensitivity;
- serious impairment of liver function;
- elderly age;
- myasthenia gravis;
- porphyria;
- pregnancy, lactation - with caution.
To avoid the solution getting into the vessel, an aspiration test must be performed before administering the entire dose. Mepivacaine should be used with caution in the following cases:
- severe forms of cardiovascular diseases;
- diabetes;
- endocrine diseases;
- pregnancy;
- lactation;
- elderly age;
- children under 12 years old.
Instructions for use
In dentistry, the drug is used in the following cases:
The anesthetic is used for pain relief in other areas of medicine.
- for example, in therapy it is used to relieve pain;
- the solution is used for caudal, lumbar, transvaginal anesthesia;
- paracervical blockade is carried out using 10 ml of a 1% solution per single injection; pain relief can be repeated no earlier than an hour and a half later.
Side effects and overdose
The medication may cause the following: side effects from the central nervous system:
- state of euphoria;
- dizziness;
- headache;
- general weakness;
- impaired coordination of movements;
- clouded consciousness;
- depressed mood;
- darkness in the eyes;
- problems with speech pronunciation;
- swallowing disorders;
- temporary loss of visual acuity;
- diplopia;
- labored breathing;
- convulsions;
- tremor;
- coma.
The cardiovascular system fails in the following ways:
Digestive system:
- nausea, vomiting;
- involuntary defecation.
Respiratory system:
- dyspnea;
- apnea.
Allergic manifestations:
- hives;
- Quincke's edema;
- skin itching;
- skin rashes;
- angioedema;
- anaphylactic shock.
In case of an overdose of the drug, the following symptoms are observed:
- drowsiness;
- pale skin;
- nausea, vomiting;
- tremor.
Severe intoxication is accompanied involuntary urination, fall vascular tone and impaired blood microcirculation.
To eliminate symptoms, short-acting tranquilizers or barbiturates are used.
Among the others side symptoms It’s worth mentioning hypothermia and decreased potency.
In dentistry, anesthesia performed with Mepivacaine can lead to the following negative symptoms:
- lack of sensitivity and paresthesia of the tongue, lips;
- prolonged anesthesia;
- fetal bradycardia;
- swelling of the gums;
- redness of the mucous membrane;
- inflammatory process at the injection site.
Special patients
Use for pain relief in special groups of patients.
Pregnancy
It has been established that the substance is able to penetrate the placental barrier. The use of the drug during pregnancy is allowed in exceptional cases, if the effect is therapeutic actions significantly exceeds possible risk from injection.
May affect intrauterine development fetus During the use of the drug during pregnancy, fetal hypoxia was observed, and the expectant mother experienced narrowing of the uterine artery.
Lactation period
When breastfeeding, women are allowed to use pain relief with this substance, but only after mandatory consultation with the attending physician and subsequent monitoring of the patient's condition.
There is no data on the possible penetration of the drug into breast milk.
Price of the product and its analogues
If you need to stop using Mepivacaine, you can replace it with the following: similar drugs based on it, having the same operating principle:
Mepivacaine is represented quite widely on the pharmaceutical market; the price of the drug ranges from 1200 to 1400 rubles per package, depending on pricing policy pharmacy chain.
Mepivacaine ( international name Mepivacaine) is a local anesthetic of the amide group, derived from xylidine. Mepivacaine is used in infiltration for peripheral transthoracic anesthesia and for sympathetic, regional and epidural nerve blocks in surgical and dental procedures. It is available commercially with and without adrenaline. Compared to mepivacaine, it produces less vasodilation and has a faster onset and longer duration of action.
Commercially known as: mepivastezin (JEPHARM, Palestine), scandonest (Septodont, France), scandicaine, carbocaine (Caresteam Health, Inc., USA).
Mepivacaine has a faster onset of action and is more long term than lidocaine. Its duration of action is about 2 hours and it is twice as effective as procaine. Used for local anesthesia in dentistry and spinal anesthesia. At a concentration of 3% it is produced without a vasoconstrictor, at 2% with a vasoconstrictor, brand name levonordefrin, concentration 1:20000. The anesthetic is recommended for use in patients for whom anesthetics with a vasoconstrictor are contraindicated.
Mepivacaine in dentistry
Local anesthetic is used in dentistry to perform the following types of anesthesia on the lower and lower extremities:
Mepivacaine in dentistry
Mechanism of action
Like all drugs, mepivacaine causes a reversible block of nerve conduction, reducing the permeability of the nerve membrane to sodium ions (Na+). This reduces the rate of membrane depolarization, thereby increasing the threshold of electrical excitability. The blockage affects all nerve fibers in the following sequence: autonomic, sensory, and motor, with diminishing effects as reverse order. Clinically, loss of nerve function follows the following order: pain, temperature, touch, proprioception, and tone skeletal muscles. For anesthesia to be effective, direct penetration of the nerve membrane is necessary, which is achieved by injecting a local anesthetic solution subcutaneously, intradermally, or submucosally around the nerve trunks or ganglia. For mepivacaine, the degree of motor blockade depends on the concentration and can be summarized as follows:
- 0.5% is effective in blocking small superficial nerves;
- 1% will block sensory and sympathetic conduction without affecting performance motor system;
- 1.5% will provide extensive and often complete blockage of the motor system
- 2% will ensure complete blocking of the motor system by any group of nerves.
Pharmacokinetics
Systemic absorption of mepivacaine depends on the dose, concentration, route of administration, tissue vascularization and degree of vasodilation. The use of mixtures containing vasoconstrictors will counteract the vasodilation produced by mepivacaine. This reduces the rate of absorption, prolongs the duration of action and maintains hemostasis. For dental anesthesia, onset of action for upper and lower jaw occurs in 0.5-2 minutes and 1-4 minutes, respectively. lasts for 10-17 minutes, and soft tissue anesthesia lasts about 60-100 minutes after administration of the adult dose. When performing the epidural method of pain relief, mepivacaine has an effect of 7-15 minutes and a duration of approximately 115-150 minutes.
Mepivacaine crosses the placenta by passive diffusion and is distributed throughout all tissues with high concentrations in well-perfused organs such as the liver, lungs, heart and brain. Mepivacaine undergoes rapid metabolism in the liver and deactivation through hydroxylation and N-demethylation. Three were found in adults inactive metabolite: two are phenols, which are isolated as glucuronide conjugates, and one is 2′, 6′-picloxidine. Approximately 50% of mepivacaine is excreted into the bile as metabolites that enter the enterohepatic circulation and are subsequently excreted. Only 5-10% of mepivacaine is excreted unchanged in the urine. Some metabolism may occur in the lungs.
Newborns may have limited ability to the metabolism of mepivacaine, but they are able to eliminate the unmodified drug. The half-life of mepivacaine is 1.9 to 3.2 hours in adults and 8.7 to 9 hours in newborns.
Local ester anesthetics are metabolized in plasma by the enzyme pseudocholinesterase, and one of the main metabolites is para-aminobenzoic acid, which appears to be responsible for allergic reactions. Anesthetics of the amide group are metabolized in the liver and do not form para-aminobenzoic acid.
Indications for use
For cervical nerve block, blockade brachial plexus, blockade of the intercostal nerve. Adults: 5-40 ml of a 1% solution (50-400 mg) or 5-20 ml of a 2% solution (100-400 mg). Dose increases should not be made more frequently than every 90 minutes.
For anesthesia peripheral nerves and cupping severe pain. Adults: 1-5 ml of a 1-2% solution (10-100 mg) or 1.8 ml of a 3% solution (54 mg). Dose increases should not be made more frequently than every 90 minutes.
For dental anesthesia by infiltration. Adults: 1.8 ml of 3% solution (54 mg). Infiltration should be done slowly with frequent aspirations. In adults, 9 ml (270 mg) of a 3% solution is usually sufficient to cover the entire mouth. The total dose should not exceed 400 mg. Incremental doses should not be administered more frequently than every 90 minutes.
Children: 1.8 ml of 3% solution (54 mg). Infiltration should be done slowly with frequent aspirations. The maximum dose should not exceed 9 ml (270 mg) of a 3% solution. The maximum dose can be calculated using the following formula, based on Clark's rule: Maximum dose (mg) = weight (in pounds) / 150 x 400 mg. 1 pound = 0.45 kilograms.
The dose of local anesthetics differs depending on the anesthetic procedure, the area to be anesthetized, the vascularity of the tissue and the number of nerves blocked, the intensity of the blockade, the required degree of muscle relaxation, the desired duration of anesthesia, individual indications and physical condition patient.
Mepivacaine is predominantly metabolized in the liver. Lower doses of mepivacaine administration may be required in patients with hepatic dysfunction due to prolonged effects and systemic accumulation. Specific dosing recommendations are not available.
Contraindications for use
Local anesthetics should only be prescribed by a physician trained in the diagnosis and treatment of analgesic toxicity and the management of serious emergencies that may result from the administration of a regional anesthetic. Before starting the administration of the drug, it is necessary to ensure the immediate availability of oxygen, equipment for cardiopulmonary resuscitation, appropriate medications, support personnel to treat toxic reactions or emergencies. Any delay in correct provision emergency care may lead to acidosis, cardiac arrest and possibly death.
Intravenous or intra-arterial administration of mepivacaine should be avoided. Forced intravenous or intra-arterial administration may cause cardiac arrest and require prolonged resuscitation. To avoid intravascular administration of mepivacaine during local anesthetic procedures, aspiration should be performed before local anesthetic administration and after needle changes. During epidural administration, a control dose should be administered first, and the patient's CNS status and cardiovascular toxicity should be monitored, as well as signs of accidental intrathecal administration.
For head and neck anesthesia, including ophthalmic and dental anesthesia, small doses of local anesthetics can cause adverse reactions, similar to the systemic toxicity observed with accidental intravascular injections of higher doses.
When local anesthetics used for retrobulbar blockade in ophthalmic surgery, lack of corneal sensation should not be taken as a basis for determining whether a patient is ready for surgery. Lack of corneal sensation usually precedes clinically acceptable akinesia of the external ocular muscles.
Mepivacaine epidural and nerve injections are contraindicated in patients with the following characteristics: infection or inflammation at the injection site, bacteremia, platelet abnormalities, thrombocytopenia<100 000 / мм3, увеличение времени свертывания крови, неконтролируемая коагулопатия и терапия антикоагулянтами. Поясничную анестезию и каудальную анестезию следует использовать с особой осторожностью у пациентов с неврологическими заболеваниями, деформациями позвоночника, сепсисом или тяжелой гипертонией.
Local anesthetics should be used with caution in patients with hypotension, hypovolemia or dehydration, myasthenia gravis, shock, or cardiac disease. Patients with impaired cardiac function, especially AV block, may be less able to compensate for the functional changes associated with prolonged AV conduction (QT interval prolongation) caused by local anesthetics.
Mepivacaine is contraindicated in patients with known hypersensitivity to amide-type local anesthetics. Elderly patients, especially those receiving treatment for hypertension, may be at greater risk of the hypotensive effects of mepivacaine.
No long-term animal studies have been conducted to evaluate carcinogenic and mutagenic potential in fertility settings. There is no human data to suggest that mepivacaine is mutagenic or carcinogenic.
- Contraindicated in patients with hypersensitivity to amide local anesthetics or any other component of the drug formula
- Serious liver disorders: cirrhosis, porphyrin disease. Patients receiving these blocks should have their ventilatory and circulatory systems closely monitored, and recommended doses should not be exceeded in these patients.
- For patients with myasthenia gravis
General precautions
- Patients under anesthesia should delay eating until sensation in the lips, cheeks, and tongue is fully restored.
- In pediatric, elderly and malnourished patients, the dose of anesthetic should be reduced
High doses of the drug are prohibited for patients with epilepsy - Use extreme caution in patients with liver disease due to the liver's metabolism of amides - this may precipitate the development of anemia
- When using any type of local anesthetic, oxygen equipment and resuscitative drugs must be available for immediate use.
- Injection into a swollen or infected area should be avoided as it may change the pH and thus alter the effect of the anesthetic.
Mepivacaine during pregnancy and lactation
There is significant transfer of mepivacaine across the maternal placenta, and the ratio between fetal drug concentrations and maternal concentrations is approximately 0.7. Although neonates have a very limited ability to metabolize mepivacaine, they appear to be able to eliminate this drug. The safety of mepivacaine hydrochloride during breastfeeding is unknown. The medicine should be prescribed with caution!
Mepivacaine rapidly crosses the placenta and, when used in epidural, paracervical, caudal, or pudendal anesthesia, may cause maternal, fetal, or neonatal toxicity. Mepivacaine should be used with caution in women who are breastfeeding as it is not known whether mepivacaine is excreted in milk.
Adverse reactions
Like all local anesthetics, mepivacaine can cause significant CNS and cardiovascular toxicity, especially when high serum concentrations are achieved. CNS toxicity occurs at lower doses and at lower plasma concentrations than those associated with cardiac toxicity. CNS-induced toxicity typically presents with stimulation symptoms such as restlessness, anxiety, nervousness, disorientation, confusion, dizziness, blurred vision, nausea/vomiting, tremors, and seizures. Subsequently, depressive symptoms may occur, including drowsiness, unconsciousness, and respiratory depression (which may lead to respiratory arrest).
In some patients, symptoms of CNS toxicity may be mild and short-lived. Seizures can be treated with intravenous benzodiazepines, although this should be done with caution as these agents are also CNS depressants.
The cardiac effects of local anesthetics are due to conduction interference in the myocardium. Cardiac effects are observed at very high doses and usually occur after the onset of CNS toxicity. Adverse cardiovascular effects caused by mepivacaine include myocardial depression, AV block, PR prolongation, QT prolongation, atrial fibrillation, sinus bradycardia, cardiac arrhythmias, hypotension, cardiovascular collapse, and cardiac arrest.
Maternal seizures and cardiovascular collapse may occur following paracervical blockade in early pregnancy (eg, anesthesia for elective abortion) due to rapid systemic absorption.
Cardiovascular side effects from mepivacaine administration should be managed with general physiologic support measures such as oxygen, assisted ventilation, and intravenous fluids.
There may be a burning sensation at the injection site. Pre-existing inflammation or infection increases the risk of developing serious skin side effects. Patients should be monitored for injection site reactions.
Allergic reactions are characterized by rash, hives, swelling, itching, etc. may result from sensitivity to local anesthesia or methipaben, which is used as a preservative in some medications.
During caudal or lumbar epidural nerve blocks, inadvertent penetration of the subarachnoid space may occur.
During labor and delivery, local anesthetics can cause varying degrees of toxicity in the mother, fetus, and neonates. The potential for toxicity is related to the procedure performed, the type and amount of drug used, and the technique of administration. The fetal heart rate will be constantly monitored because fetal bradycardia may occur and may be associated with fetal atherosis. Maternal hypotension may result from regional anesthesia, which may alleviate this problem.
Although the anesthetic does not affect the ability to drive a vehicle, the dentist must decide when the patient can drive a car.
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%)
-
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
metallic taste in mouth
nausea, vomiting
noise in ears
dizziness
nervousness, anxiety
excitement, anxiety
Severe cardiovascular attacks manifest themselves as:
-
cardiac arrest
drop in blood pressure
conduction disturbances
tachycardia
bradycardia
hypotension
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: AV block II and III degrees, 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 central nervous system dysfunction (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.
A. V. Kuzin
Candidate of Medical Sciences, dental surgeon of the Federal State Institution "Central Research Institute of Infrastructure and Maxillofacial Surgery" of the Ministry of Health of the Russian Federation, consultant physician at 3M ESPE on pain management in dentistry
M. V. Stafeeva
dentist-therapist, private practice (Moscow)
V. V. Voronkova
Candidate of Medical Sciences, Dentist-Therapist, Department of Therapeutic Dentistry, Clinical Diagnostic Center, First Moscow State Medical University named after. I. M. Sechenov" of the Ministry of Health of Russia
Often in clinical practice there is a need to use short-acting anesthetics. There are many low-volume dental procedures that require pain relief. The use of long-acting anesthetics is not entirely legal, 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 load on the patient, the use of short-acting anesthetics is justified, which can reduce the duration of soft tissue numbness to 30-45 minutes. Today in dentistry, local anesthetics based on mepivacaine meet these requirements.
Mepivacaine is the only amide anesthetic that can be used without the addition of a vasoconstrictor. Most amide anesthetics (articaine, lidocaine) dilate the blood vessels at the injection site, which leads to their rapid absorption into the bloodstream. This shortens the duration of their action, which is why dosage forms of anesthetics are available with epinephrine. In the Russian Federation, lidocaine is produced in ampoules without vasoconstrictors, which requires its dilution with epinephrine before use. According to modern standards of pain management in dentistry, the preparation of a local anesthetic solution by staff is a violation of the anesthesia technique. 3% mepivacaine has a less pronounced local vasodilator effect, which allows it to be effectively used to anesthetize teeth and soft tissues of the oral cavity (Table No. 1).
The duration of action of mepivacaine-containing anesthetics (mepivastezin) varies in individual areas 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 for the dental pulp is on average 45 minutes, anesthesia for soft tissues - up to 90 minutes. These data were obtained as a result of an experimental study in practically healthy patients during anesthesia of single-rooted teeth, mainly in the upper jaw. Naturally, such studies do not reflect real clinical conditions in which a dentist is faced with inflammatory phenomena in tissues, chronic neuropathic pain, and the individual characteristics of the patient’s anatomy. According to domestic scientists, it was found that the average duration of dental pulp anesthesia when using 3% mepivacaine is 20-25 minutes, and the duration of soft tissue anesthesia depends on the volume of anesthetic administered and the anesthesia technique (infiltration, conduction) and is 45-60 min.
An important issue is the speed of onset of local anesthesia. Thus, when using 3% mepivacaine, the rate of onset of dental pulp anesthesia 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 peculiarities in the anesthesia of certain groups of teeth with 3% mepivacaine. Numerous studies have proven that it is most effective in relieving pain in 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. In this case, it is important to take into account the topography of the apexes of the roots of the teeth and, accordingly, the depth of advancement of the carpule needle into the tissue. For anesthesia of 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: submental anesthesia is performed in various modifications, where an anesthetic depot of up to 0.8 ml is created. It is important after submental anesthesia to apply digital pressure to the soft tissues above the mental foramen for better diffusion of the anesthetic. Infiltration anesthesia in the area of mandibular molars with 3% mepivacaine is ineffective compared to 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, mandibular anesthesia (1.7 ml of 3% mepivacaine) must be performed. Mandibular canines are also anesthetized with chin or mandibular anesthesia in patients with the contraindications described above.
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 restrictions 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, HR). If longer-term treatment or intervention is planned in the area of the mandibular molars, from a clinical point of view, the use of only articaine-containing anesthetics with a vasoconstrictor of 1:200,000 is justified.
Patients with a history of allergies. 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 due to the preservatives contained in the carpule. Mepivacaine does not contain preservatives (sodium bisulfite) and can therefore be used for short-term interventions in this group of patients. For 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 an allergist on the tolerability of the drug. According to the clinical experience of the authors of this article, the frequency of positive allergy tests for 3% mepivacaine is significantly lower in comparison with other carpulal anesthetics.
IN therapeutic dentistry mepivacaine is used in the treatment of uncomplicated caries: enamel caries, dentin caries. It is important to consider that the required duration of anesthesia is limited to the stage of preparation of hard dental tissues. After covering the formed cavity with 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 canines and molars of the lower jaw with infiltration anesthesia and with intraligamentary anesthesia of the teeth of the lower jaw.
IN surgical dentistry mepivacaine is used for short-term surgical interventions. The greatest effectiveness was found when removing teeth with chronic periodontitis and when removing intact teeth for orthodontic indications. The role of mepivacaine in pain relief during surgical dressings is important. Often, the procedure for removing sutures, changing the wound covering in the tooth socket, and changing the iodoform dressing is painful for patients. The use of long-acting anesthetics is unjustified due to the subsequent long-term numbness of soft tissues, which can lead to self-injury of the surgical site 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 during outpatient surgical dressings can reduce patient discomfort and stress.
Pediatric dentistry. Short-acting anesthetics have proven themselves well when used in pediatric dentistry. When using mepivacaine, the dosage of this drug should be taken into account when performing local anesthesia in children. Mepivacaine is more toxic to the central nervous system than articaine because it is rapidly absorbed into the bloodstream. Also, the clearance of mepivacaine is higher than the clearance of articaine for several hours. The maximum dosage of 3% mepivacaine is 4 mg/kg of body weight for a child over 4 years of age (Table No. 2). However, in pediatric dentistry there are no indications for the use of such high volumes of anesthetic. According to modern safety standards, the dosage of administered 3% mepivacaine should not exceed half the maximum dose for all dental treatment. With this use, 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 at the dentist are practically excluded. According to statistics, up to 25-35% of preschool children injure the lower lip after 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 dental fissures, treating initial forms of caries, and removing temporary teeth. The use of mepivacaine in children with polyvalent allergies and bronchial asthma is especially justified, since the drug does not contain preservatives (EDTA, sodium bisulfite).
Pregnancy and breastfeeding. Mepivacaine can be safely used in pregnant women during routine sanitation of the oral cavity at the dentist according to the indications described above. In most cases, 3% mepivacaine is used for short-term and minimally invasive interventions lasting up to 20 minutes. The second trimester of pregnancy is most favorable for treatment.
Mepivacaine can be used in breastfeeding women; it is found in mother's breast milk in concentrations that are insignificant for the baby. However, the patient is recommended 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 use in various fields of dentistry. For a certain 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)
|
Weight |
Mg |
Ml |
Carpools |
|
1.5 |
0.8 |
||
|
2.2 |
1.2 |
||
|
2.8 |
1.4 |
||
|
110 |
3.6 |
1.7 |
|
|
132 |
4.4 |
2.4 |
|
|
154 |
5.1 |
2.9 |
|
|
176 |
5.9 |
3.2 |
|
|
198 |
6.6 |
3.6 |
|
|
220 |
7.3 |
4.0 |
|
|
Mepivacaine 3% without vasoconstrictor. Maximum dose 4.4 mg/kg; 3% solution in 1 carpule 1.8 ml (54 mg) |
|||
Local anesthetic of medium duration of action of the amide group. Causes a reversible block of nerve conduction by reducing the permeability of neuron 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 block:
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
