"Mepivacaine" used in treatment and/or prevention the following diseases(nosological classification - ICD-10):
Gross formula: C15-H22-N2-O
CAS Code: 22801-44-1
Description
Characteristic: Amide type anesthetic.
Mepivacaine hydrochloride is a white, odorless, crystalline powder. Soluble in water, resistant to both acid and alkaline hydrolysis.
pharmachologic effect
Pharmacology: Pharmacological action - local anesthetic. Being a weak lipophilic base, it passes through the lipid layer of the membrane nerve cell and, transforming into a cationic form, binds to receptors (residues S6 of transmembrane helical domains) of membrane sodium channels located at the endings of sensory nerves. Reversibly blocks voltage-gated sodium channels, prevents the flow of sodium ions through the cell membrane, stabilizes the membrane, increases the threshold of electrical stimulation of the nerve, reduces the rate of occurrence of the action potential and reduces its amplitude, and ultimately blocks membrane depolarization, the occurrence and conduction of impulses along nerve fibers.
Calls out all kinds local anesthesia: terminal, infiltration, conduction. Has a fast and strong effect.
When it enters the systemic circulation (and creates toxic concentrations in the blood), it can have a depressant effect on the central nervous system and myocardium (however, when used in therapeutic doses, changes in conductivity, excitability, automaticity and other functions are minimal).
Dissociation constant (pK_a) - 7.6; Solubility in fats is average. The extent of systemic absorption and plasma concentration depend on the dose, route of administration, vascularization of the injection site and the presence or absence of epinephrine in the anesthetic solution. Adding a dilute solution of epinephrine (1:200,000, or 5 mcg/ml) to a mepivacaine solution usually reduces the absorption of mepivacaine and its plasma concentration. Plasma protein binding is high (about 75%). Penetrates through the placenta. Not affected by plasma esterases. Rapidly metabolized in the liver, the main metabolic pathways are hydroxylation and N-demethylation. In adults, 3 metabolites have been identified - two phenolic derivatives (excreted in the form of glucuronides) and an N-demethylated metabolite (2,6"-pipecoloxylide). T_1/2 in adults - 1.9-3.2 hours; in newborns - 8.7-9 hours. More than 50% of the dose in the form of metabolites is excreted into bile, then reabsorbed in the intestine (a small percentage is found in feces) and excreted in the urine after 30 hours, incl. unchanged (5-10%). Cumulates in case of liver dysfunction (cirrhosis, hepatitis).
Loss of sensitivity is noted after 3-20 minutes. Anesthesia lasts 45-180 minutes. The time parameters of anesthesia (start time and duration) depend on the type of anesthesia, the technique used, the concentration of the solution (dose of the drug) and individual characteristics patient. The addition of vasoconstrictor solutions is accompanied by prolongation of anesthesia.
Studies assessing carcinogenicity, mutagenicity, and effects on fertility in animals and humans have not been conducted.
Indications for use
Application: Local anesthesia for interventions in the oral cavity (all types), tracheal intubation, broncho- and esophagoscopy, tonsillectomy, etc.
Contraindications
Contraindications: Hypersensitivity, incl. to other amide anesthetics; elderly age, myasthenia gravis, severe liver dysfunction (including liver cirrhosis), porphyria.
Restrictions for use: Pregnancy, breastfeeding.
Use during pregnancy and breastfeeding: During pregnancy, it is possible if the expected effect of therapy exceeds the potential risk to the fetus (can cause narrowing of the uterine artery and fetal hypoxia). With caution during breastfeeding(no data on penetration into breast milk).
Side effects
Side effects: From the outside nervous system and sensory organs: agitation and/or depression, headache, ringing in the ears, weakness; impaired speech, swallowing, vision; convulsions, coma.
From the outside of cardio-vascular system and blood (hematopoiesis, hemostasis): hypotension (or sometimes hypertension), bradycardia, ventricular arrhythmia, possible cardiac arrest.
Allergic reactions: sneezing, urticaria, pruritis, erythema, chills, fever, angioedema.
Other: depression of the respiratory center, nausea, vomiting.
Interaction: Beta-blockers, calcium channel blockers, antiarrhythmic drugs enhance the inhibitory effect on myocardial conductivity and contractility.
Overdose: Symptoms: hypotension, arrhythmia, increased muscle tone, loss of consciousness, convulsions, hypoxia, hypercapnia, respiratory and metabolic acidosis, dyspnea, apnea, cardiac arrest.
Treatment: hyperventilation, maintenance of adequate oxygenation, assisted breathing, control of convulsions and seizures
(prescription of thiopental 50-100 mg IV or diazepam 5-10 mg IV), normalization of blood circulation, correction of acidosis.
Dosage and method of administration
Directions for use and dosage: The amount of solution and the total dose depend on the type of anesthesia and the nature of the intervention. For injection use a 3% solution of mepivacaine (maximum dose for adults - 4.4 mg/kg, but not more than 300 mg per visit) or a 2% solution in combination with epinephrine (1: 80000, 1: 100000) or norepinephrine ( 1:200000) (maximum dose - 6.6 mg/kg, but not more than 400 mg of mepivacaine per visit). The maximum dose of mepivacaine (in mg) for children is calculated taking into account the child's body weight.
Precautions: Use with caution in patients with hepatitis, liver cirrhosis, liver failure, severe renal impairment, and acidosis.
| Mepivacaine
Analogs (generics, synonyms)
Isocaine, Mepivacaine DF, Mepivastezin, Mepidont, Mepicaton, Novocaine, Lidocaine
Recipe (international)
Rp.: Sol. Mepivacaini 2% - 1.8 ml
D.t.d. No. 10
S. For conduction anesthesia.
pharmachologic effect
Being a weak lipophilic base, it passes through the lipid layer of the nerve cell membrane and, transforming into a cationic form, binds to the receptors (residues of S6 transmembrane helical domains) of sodium channels of membranes located at the endings of sensory nerves. Reversibly blocks voltage-gated sodium channels, prevents the flow of sodium ions through the cell membrane, stabilizes the membrane, increases the threshold of electrical stimulation of the nerve, reduces the rate of occurrence of the action potential and reduces its amplitude, and ultimately blocks membrane depolarization, the occurrence and conduction of impulses along nerve fibers.
Causes all types of local anesthesia: terminal, infiltration, conduction. Has a fast and strong effect.
When it enters the systemic circulation (and creates toxic concentrations in the blood), it can have a depressant effect on the central nervous system and myocardium (however, when used in therapeutic doses, changes in conductivity, excitability, automaticity and other functions are minimal).
Dissociation constant (pKa) - 7.6; Solubility in fats is average. The extent of systemic absorption and plasma concentration depend on the dose, route of administration, vascularization of the injection site and the presence or absence of epinephrine in the anesthetic solution. Adding a dilute solution of epinephrine (1:200,000, or 5 mcg/ml) to a mepivacaine solution usually reduces the absorption of mepivacaine and its plasma concentration. Plasma protein binding is high (about 75%). Penetrates through the placenta. Not affected by plasma esterases. Rapidly metabolized in the liver, the main metabolic pathways are hydroxylation and N-demethylation. In adults, 3 metabolites have been identified - two phenolic derivatives (excreted in the form of glucuronides) and an N-demethylated metabolite. T1/2 in adults - 1.9-3.2 hours; in newborns - 8.7-9 hours. More than 50% of the dose in the form of metabolites is excreted into bile, then reabsorbed in the intestine (a small percentage is found in feces) and excreted in the urine after 30 hours, incl. unchanged (5-10%). Cumulates in case of liver dysfunction (cirrhosis, hepatitis).
Loss of sensitivity is noted after 3-20 minutes. Anesthesia lasts 45-180 minutes. The time parameters of anesthesia (onset time and duration) depend on the type of anesthesia, the technique used, the concentration of the solution (dose of the drug) and the individual characteristics of the patient. The addition of vasoconstrictor solutions is accompanied by prolongation of anesthesia.
Studies assessing carcinogenicity, mutagenicity, and effects on fertility in animals and humans have not been conducted.
Mode of application
For adults: For conduction anesthesia (brachial, cervical, intercostal, pudendal) - 5-40 ml (50-400 mg) of a 1% solution or 5-20 ml (100-400 mg) of a 2% solution.
Caudal and lumbar epidural anesthesia - 15-30 ml (150-300 mg) of 1% solution, 10-25 ml (150-375 mg) of 1.5% solution or 10-20 ml (200-400 mg) of 2% solution.
In dentistry: single anesthesia in the upper or lower jaw- 1.8 ml (54 mg) 3% solution; local infiltration anesthesia and conduction anesthesia - 9 ml (270 mg) of 3% solution; the dose required for long-term procedures should not exceed 6.6 mg/kg.
For local infiltration anesthesia (in all cases, except for use in dentistry) - up to 40 ml (400 mg) of a 0.5-1% solution.
For paracervical blockade - up to 10 ml (100 mg) of 1% solution per administration; administration can be repeated no earlier than after 90 minutes.
For cupping pain syndrome(therapeutic block) - 1-5 ml (10-50 mg) of a 1% solution or 1-5 ml (20-100 mg) of a 2% solution.
For transvaginal anesthesia (combination of paracervical and pudendal blockade) - 15 ml (150 mg) of a 1% solution.
Maximum doses in adult patients: in dentistry - 6.6 mg/kg, but not more than 400 mg per administration; for other indications - 7 mg/kg, but not more than 400 mg.
Maximum doses for children: 5-6 mg/kg.
Indications
infiltration and transtracheal anesthesia, peripheral, sympathetic, regional (Beers method) and epidural nerve blockade during surgical and dental interventions. Not recommended for subarachnoid administration.
Contraindications
hypersensitivity to amide local anesthetics, coagulopathy, simultaneous use of anticoagulants, thrombocytopenia, infections, sepsis, shock. Relative contraindications are AV blockade, increased duration QT interval, serious illnesses heart and liver, eclampsia, dehydration, arterial hypotension, myasthenia gravis, pregnancy and lactation.
Side effects
From the nervous system and sensory organs: agitation and/or depression, headache, ringing in the ears, weakness; impaired speech, swallowing, vision; convulsions, coma.
From the cardiovascular system and blood (hematopoiesis, hemostasis): hypotension (or sometimes hypertension), bradycardia, ventricular arrhythmia, possible cardiac arrest.
Allergic reactions: sneezing, urticaria, pruritis, erythema, chills, fever, angioedema.
Other: depression of the respiratory center, nausea, vomiting
Release form
1 ml mepivacaine hydrochloride 30 mg;
ATTENTION!
The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to provide healthcare workers with additional information about certain medications, thereby increasing their level of professionalism. Use of the drug "" in mandatory involves consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.
N01BB53 (Mepivacaine in combination with other drugs)
N01BB03 (Mepivacaine)
Analogues of the drug according to ATC codes:
You should consult your doctor before using MEPIVACAIN. These instructions for use are for informational purposes only. To get more complete information Please refer to the manufacturer's instructions.
Clinical and pharmacological group
21.009 (Local anesthetic for use in dentistry)
pharmachologic effect
A local anesthetic whose mechanism of action is related to stabilization cell membranes. Causes all types of local anesthesia: terminal, infiltration, conduction. Has a fast and strong effect.
MEPIVACAIN: DOSAGE
The amount of solution and the total dose depend on the type of anesthesia and the nature surgical intervention or manipulation. Average single dose- 1.3 ml; if necessary, the dose can be increased.
Maximum daily doses: for adults and children weighing more than 30 kg - 5.4 ml; for children weighing 20-30 kg - 3.6 ml; for children weighing less than 20 kg - 1.8 ml.
Drug interactions
With the simultaneous use of mepivacaine with beta-blockers, calcium channel blockers and other antiarrhythmic drugs, the inhibitory effect on myocardial conductivity and contractility increases.
Pregnancy and lactation
During pregnancy, the use of mepivacaine is possible only under strict indications.
MEPIVACAIN: SIDE EFFECTS
Possible: (especially if the dose is exceeded or with accidental intravascular administration) euphoria, depression, disturbances in speech, swallowing, vision, convulsions, respiratory depression, coma, bradycardia, arterial hypotension; allergic reactions(urticaria, Quincke's edema).
Indications
For local anesthesia for various therapeutic and surgical interventions in the oral cavity (lubrication of mucous membranes during tracheal intubation, bronchoesophagoscopy, tonsillectomy; in dentistry).
Contraindications
Increased sensitivity to local anesthetics of the amide type and to alkyl-4-hydroxybenzoates (parabens).
special instructions
Use with caution in elderly patients.
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
Mepivastezin is used as 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 values pH, 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 reducing general condition patient, also with severe violations liver and kidney functions. 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
headache
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 dysfunction of the central nervous system (metallic taste in the mouth, nausea, vomiting, tinnitus, dizziness, agitation, anxiety, increased respiratory rate, drowsiness, confusion, tremor, muscle twitching, tonic-clonic seizures, coma and respiratory paralysis) and/or vascular symptoms (drop in blood pressure, conduction disturbances, bradycardia, cardiac arrest).
Treatment: If side effects occur, immediately stop administering the local anesthetic.
Basic general measures
Diagnostics (respiration, circulation, consciousness), maintenance/restoration of vital functions of breathing and circulation, administration of oxygen, intravenous access.
Special measures
Hypertension: Elevate the patient's upper body and, if necessary, give sublingual nifedipine.
Convulsions: Protect the patient from associated bruises, injuries, if necessary, diazepam intravenously.
Hypotension: Horizontal position of the patient's body, if necessary, intravascular infusion of electrolyte solutions, vasopressors (eg, intravenous epinephrine).
Bradycardia: Atropine IV.
Anaphylactic shock: Contact an emergency physician. Meanwhile, place the patient in a horizontal position and elevate the lower part of the body. Intensive infusion of electrolyte solutions, if necessary - intravenous epinephrine, intravenous glucocorticoid.
Gross formula
C15H22N2OPharmacological group of the substance Mepivacaine
Nosological classification (ICD-10)
CAS Code
22801-44-1Characteristics of the substance Mepivacaine
Amide type anesthetic.
Mepivacaine hydrochloride is a white, odorless, crystalline powder. Soluble in water, resistant to both acid and alkaline hydrolysis.
Pharmacology
pharmachologic effect- local anesthetic.Being a weak lipophilic base, it passes through the lipid layer of the nerve cell membrane and, transforming into a cationic form, binds to the receptors (residues of S6 transmembrane helical domains) of sodium channels of membranes located at the endings of sensory nerves. Reversibly blocks voltage-gated sodium channels, prevents the flow of sodium ions through the cell membrane, stabilizes the membrane, increases the threshold of electrical stimulation of the nerve, reduces the rate of occurrence of the action potential and reduces its amplitude, and ultimately blocks membrane depolarization, the occurrence and conduction of impulses along nerve fibers.
Causes all types of local anesthesia: terminal, infiltration, conduction. Has a fast and strong effect.
When it enters the systemic circulation (and creates toxic concentrations in the blood), it can have a depressant effect on the central nervous system and myocardium (however, when used in therapeutic doses, changes in conductivity, excitability, automaticity and other functions are minimal).
Dissociation constant (pK a) - 7.6; Solubility in fats is average. The extent of systemic absorption and plasma concentration depend on the dose, route of administration, vascularization of the injection site and the presence or absence of epinephrine in the anesthetic solution. Adding a dilute solution of epinephrine (1:200,000, or 5 mcg/ml) to a mepivacaine solution usually reduces the absorption of mepivacaine and its plasma concentration. Plasma protein binding is high (about 75%). Penetrates through the placenta. Not affected by plasma esterases. Rapidly metabolized in the liver, the main metabolic pathways are hydroxylation and N-demethylation. In adults, 3 metabolites have been identified - two phenolic derivatives (excreted in the form of glucuronides) and an N-demethylated metabolite (2,6"-pipecoloxylide). T1/2 in adults - 1.9-3.2 hours; in newborns - 8.7-9 hours. More than 50% of the dose in the form of metabolites is excreted into bile, then reabsorbed in the intestine (a small percentage is found in feces) and excreted in the urine after 30 hours, incl. unchanged (5-10%). Cumulates in case of liver dysfunction (cirrhosis, hepatitis).
Loss of sensitivity is noted after 3-20 minutes. Anesthesia lasts 45-180 minutes. The time parameters of anesthesia (onset time and duration) depend on the type of anesthesia, the technique used, the concentration of the solution (dose of the drug) and the individual characteristics of the patient. The addition of vasoconstrictor solutions is accompanied by prolongation of anesthesia.
Studies assessing carcinogenicity, mutagenicity, and effects on fertility in animals and humans have not been conducted.
Use of the substance Mepivacaine
Local anesthesia for interventions in the oral cavity (all types), tracheal intubation, broncho- and esophagoscopy, tonsillectomy, etc.
Contraindications
Hypersensitivity, incl. to other amide anesthetics; old age, myasthenia gravis, severe liver dysfunction (including liver cirrhosis), porphyria.
Restrictions on use
Pregnancy, breastfeeding.
Use during pregnancy and breastfeeding
During pregnancy, it is possible if the expected effect of therapy exceeds the potential risk to the fetus (can cause narrowing of the uterine artery and fetal hypoxia). With caution during breastfeeding (no data on penetration into breast milk).
Side effects of the substance Mepivacaine
From the nervous system and sensory organs: agitation and/or depression, headache, ringing in the ears, weakness; impaired speech, swallowing, vision; convulsions, coma.
From the cardiovascular system and blood (hematopoiesis, hemostasis): hypotension (or sometimes hypertension), bradycardia, ventricular arrhythmia, possible cardiac arrest.
Allergic reactions: sneezing, urticaria, pruritus, erythema, chills, fever, angioedema.
Other: depression of the respiratory center, nausea, vomiting.
Interaction
Beta-blockers, calcium channel blockers, and antiarrhythmic drugs enhance the inhibitory effect on myocardial conductivity and contractility.
Overdose
Symptoms: hypotension, arrhythmia, increased muscle tone, loss of consciousness, convulsions, hypoxia, hypercapnia, respiratory and metabolic acidosis, dyspnea, apnea, cardiac arrest.
Treatment: hyperventilation, maintenance of adequate oxygenation, assisted breathing, control of convulsions and seizures
(prescription of thiopental 50-100 mg IV or diazepam 5-10 mg IV), normalization of blood circulation, correction of acidosis.
