Mepifrin-Zdorovye, solution for and 30mg/ml in амп.по 1.7ml No. 10 (No. 10х5)

General characteristics. Structure:

Active ingredient: mepivacaine; 1 ml of drug contains a mepivakain of a hydrochloride of 30 mg; excipients: sodium chloride, 0,1 M hydroxide sodium solution, water for injections. Main physical and chemical properties: transparent colourless solution.

Pharmacological properties:

Pharmacodynamics. Mepivakaina a hydrochloride - local anesthetic of amide type which blocks passing of nervous impulses on nerve fibrils in the place of an injection. As мепивакаин has weak vasoconstrictive action, it allows to apply it without vasoconstrictor or with insignificant quantity of a vasoconstrictor. Anesthesia comes in 2-3 min. Duration of pulpal anesthesia makes 20-40 minutes. Anesthesia of soft tissues – 2-3 hours.

Pharmacokinetics. Mepivakain at introduction to a mucous membrane of a mouth reaches the peak of concentration in blood approximately in 30 minutes after an injection. The elimination half-life of a mepivakain of a hydrochloride makes about 90 minutes. Mepivakaina a hydrochloride is metabolized mainly by a liver; 5-10% of a dose are removed in an invariable view with urine.

Indications to use:

Infiltration and conduction anesthesia in stomatology. Mepifrin-Zdorovye is shown for simple exodontias, and also for preparation of cavities and processing of a stump of teeth under restorations and orthopedic designs.

Mepifrin-Zdorovye is especially recommended for patients to whom vasoconstrictive drugs are contraindicated.

Route of administration and doses:

ONLY FOR ANESTHESIA IN STOMATOLOGY.

It is intended for adults and children aged from 4 years.

The recommendation to дозированию:Для providing effective anesthesia should use a necessary minimum of solution. Adult patients have usually enough dose of 1-4 ml. Children aged from 4 years with the body weight of 20-30 kg have enough dose of 0,25-1 ml; for children with the body weight of 30-45 kg – 0,5-2 ml.

Patients of advanced age can have an increased level of a mepivakain in a blood plasma through the weakened process of metabolism and insignificant distribution. The risk of accumulation of a mepivakain increases especially at repeated injections (for example, an additional injection). The similar effect can arise at the general weakened condition of the patient, and also at an aggravation of functions of a liver and kidneys. In these cases it is recommended to reduce dosing (to enter the minimum quantity of solution for sufficient anesthesia). Dosing of a mepivakain for patients with certain diseases (stenocardia, arteriosclerosis) needs to be reduced also.

The maximum recommended dose.

Adults.

The maximum dose of a mepivakain for adults makes 4 mg/kg of body weight that corresponds to 0,133 ml of Mepifrina-Zdorovyekg of body weight. It means that to the patient with the body weight of 70 kg it is admissible to enter 300 mg of a mepivakain that makes 10 ml of Mepifrin-Zdorovye.

Children aged from 4 years.

The amount of drug which is administered has to be defined depending on age and the body weight of the child and duration of operation. Not to exceed an equivalent of 4 mg ¼Ñ»¿óá¬á¿¡á/kg (0,133 mg of Mepifrina-Zdorovyekg) body weights.

Introduction method.

For administration of drug it is necessary to use special cartridge syringes of reusable use. Just before use the karpulny rubber bung which is pressed out by an aluminum cap which is punctured a syringe needle needs to be disinfected alcohol.

It is impossible to dip karpula or ampoules into any solutions at all.

Solution for injections cannot be mixed with any other drug in one syringe.

In order to avoid intravascular injections, it is always necessary to carry out carefully the test for aspiration though the negative result of aspiration does not exclude an unintentional and unnoticed intravascular injection.

Rate of administering of drug should not exceed 0,5 ml in 15 seconds, that is 1 karpul or 1 ampoule a minute.

The majority of system reactions as result of an accidental intravascular injection can be avoided in most cases thanks to the appropriate equipment of an injection: after aspiration – a slow injection of 0,1-0,2 ml and slow introduction of the rest – not earlier than in 20-30 seconds. Karpula or an ampoule from the solution rest upon termination of dental intervention it is necessary to destroy. It is impossible to use karpula or ampoules from the solution rest for other patients.

Features of use:

ONLY FOR USE IN DENTAL PRACTICE.

Athletes should be warned that this drug contains an active component which can yield positive result at a drug test.

As local anesthetics of amide type are metabolized mainly in a liver and removed by kidneys, it is necessary to apply carefully it at patients with diseases of a liver and kidneys. In case of acute hepatocellular insufficiency reduction of a dose of a mepivakain is possible. Also it is necessary to reduce doses in cases of a hypoxia, a hyperpotassemia or a metabolic acidosis.

It is necessary to pay special attention to patients who accept anticoagulants (INR monitoring).

There is a risk of an unintentional injury of a bite: different biting (lips, cheeks, mucous membrane, language); it is necessary to warn the patient that it is impossible to chew something during effect of anesthesia.

To avoid wrong injections and injections in the infected or inflamed fabrics (efficiency of local anesthesia decreases). It is necessary to consider that at patients who accept blood coagulation inhibitors (for example, heparin or aspirin) the unintentional puncture of a vessel at administration of local anesthetic can lead to serious bleeding and the general increase in a possibility of bleeding.

To apply with care to patients with supertension or a sick diabetes mellitus (risk of a local necrosis).

As мепивакаин has cardiotoxic properties, it should be applied with care to patients with repolarization disturbance (a syndrome of long AT): appointment and dosing should be selected so that to avoid any risk of too high concentration in a blood plasma which can become the reason of heavy ventrikulyarny arrhythmia.

With special care it is necessary to apply Mepifrin-Zdorovye in the following cases:

aggravation of disturbance of functions of a liver and kidneys;

stenocardia;

arteriosclerosis;

injection to the inflamed area;

considerable deterioration in a blood coagulation.

As local anesthetics of amide type are also metabolized in a liver, Mepifrin-Zdorovye patients should apply carefully with liver diseases. Patients with acute diseases of a liver have the increased risk of development of toxic concentration of an artikain in a blood plasma.

Drug should be used carefully to patients with the weakened cardiovascular function as they have smaller ability to compensate the functional changes connected with lengthening of arteriovenous conductivity that is caused by these medicines.

Drug should be used carefully to patients with epilepsy in the anamnesis. It is necessary to consider that during treatment by blood coagulation inhibitors (for example, heparin or aspirin) the unintentional puncture of a vessel at administration of local anesthetic can lead to serious bleeding and the general increase in a possibility of bleeding (see the section "Interaction with Other Medicines and Other Types of Interactions").

It is necessary to avoid accidental intravascular introduction (see the section "Route of Administration and Doses", the subsection "Introduction Method").

During processing of a pulp cavity or processing of tooth under a crown it is necessary to consider that through contents in adrenaline drug in pulpal fabrics the blood stream decreases and, thus, there is a risk not to notice accidentally open pulp.

Security measures.

Every time during use of local anesthetic there have to be available following drugs / actions of therapy:

anticonvulsive means (drugs for treatment of attacks, for example, benzodiazepine or barbiturates), muscle relaxants (drugs which reduce tension in muscles which are randomly reduced), atropine, vasoconstrictors (drugs for treatment of low blood pressure) or adrenaline for acute allergic or anaphylactic reactions;

the resuscitation equipment (especially oxygen sources) for an artificial respiration if necessary;

careful and constant tracking cardiovascular and respiratory (adequacy of breath) indicators of a condition of an organism and a condition of consciousness of the patient after each injection of local anesthetic. The concern, alarm, a sonitus, dizziness, sight easing, a shiver, a depression or drowsiness are the first signs of toxicity of TsNS (see the section "Overdoses").

Ability to influence speed of response at control of motor transport or work with other mechanisms.

This medicine can have weak or average influence on speed of response at control of motor transport or work with other mechanisms. The doctor has to solve in each special case whether the patient is capable to manage transport or mechanical means. After an injection the patient has to remain in an office of the stomatologist of at least 30 minutes.

Use during pregnancy or feeding by a breast. Pregnancy.

Researches on animals did not find teratogenecity signs. In the absence of teratogenecity at animals defects of development and in the person are not expected. Really, till this time of substance which are responsible for defects of development in the person found teratogenecity in animals in well controlled researches on two types.

In clinical aspect there are no enough relevant clinical data for today to estimate possible influence of defects of development or fetotoksichesky influence of a mepivakain at its introduction to pregnancy time.

Thus, in stomatology pregnant women should allow purpose of a mepivakain only in case of extreme requirement, at impossibility of use of other local anesthetics.

Feeding by a breast. As well as any other local anesthetic, мепивакаин can get to breast milk in very small quantities. However feeding can be continued after effect of drug ends in 24 hours.

Children. Children need to apply this product only aged 4 years as anesthesia of this type is inappropriate for children of younger age are more senior.

Special security measures. Before using this drug, it is necessary:

• to ask about existence of a case history of the patient with the indication of treatment which he passes at present;
• if necessary to carry out premedication by a benzodiazepine dose;
• at possible risk of an allergy to execute a trial injection from 5% to 10% of a dose;
• to carry out an injection slowly, carrying out often aspiration, in order to avoid an intravascular injection;
• to support verbal contact with the patient and to control his state;
• introduction of low doses can predetermine insufficient anesthesia and lead to increase in level of drug in blood owing to accumulation of drug or its metabolites.

Side effects:

Side reactions after introduction of a mepivakain are similar with side reactions to other local anesthetics of amide type.

In general these side effects are connected with dosing and can result from increase in level of plasma in blood at excess dosing, bystry absorption, as a result of an unintentional intravascular injection or through low metabolism. Also they can arise through hypersensitivity, an idiosyncrasy or reduced resistance of the patient to medicamentous means. In general serious side reactions are essentially system. The most widespread of them following:

Central nervous system. Signs is excitement and/or oppression TsNS, metal smack, a headache, disturbance of the speech, swallowing, nervousness, concern, yawning, a shiver, uneasiness, euphoria, a logorrhea, deterioration in consciousness, dizziness, drowsiness, a sonitus, a nystagmus, deterioration in sight, a diplopia, feeling of heat, cold or numbness, convulsive reductions, a tremor, convulsions, consciousness disturbances, a loss of consciousness, deterioration and an apnoea, a coma. At emergence of these signs it is necessary to put the patient in a prone position and to make ventilation oxygen, and also to watch constantly a condition of the patient to prevent possible deterioration, such as convulsions with the subsequent depression of TsNS. Manifestations of excitement can be very short or not arise at all, in such cases drowsiness which passes into an unconscious state and an apnoea can be the first sign. Usually emergence of drowsiness after introduction of a mepivakain is a precursory symptom of increase in level of drug in blood and can result from bystry absorption.

Cardiovascular system.

Usually this oppression of cardiovascular system which signs is bradycardia, arterial hypotonia which can lead to a collapse, cardiovascular insufficiency which can lead to a cardiac standstill. Also the following clinical signs can be observed: tachycardia, cardiac arrhythmia (ventrikulyarny extrasystoles and ventrikulyarny fibrillation), disturbance of conductivity of heart (atrioventricular block). These manifestations can entail a cardiac standstill.

These signs and symptoms of oppression of cardiovascular function can usually be results of vazovagalny reaction, especially if the patient is in vertical position. They can sometimes be result of direct effect of drug. Inability to distinguish antecedent signs, such as sweat, dizziness, feeling of weakness, change of pulse, can lead to the progressing cerebral hypoxia and spasms or serious cardiovascular frustration.

Auxiliary actions or circulatory unefficiency can demand intravenous infusion and if there are no contraindications, introductions of vasoconstrictive agents (for example, ephedrine) if it is demanded by a clinical situation.

Respiratory system. A tachypnea, брадипноэ that can lead to an apnoea.

Allergic reactions.

In general allergic reactions on мепивакаин arise seldom and can be result of hypersensitivity. They are characterized by damage of skin in the form of rashes, a small tortoiseshell, hypostasis, anaphylactoid reactions, an acute anaphylaxis, Quincke's disease, fervescence. As well as in a case with other local anesthetics, anaphylactic reactions on мепивакаин arise seldom. Reaction can be unexpected and acute, usually it is not connected with dosing. There can be local hypostasis or a tumor.

Digestive tract. Nausea, vomiting.

At emergence of side reactions administration of local anesthetic should be stopped.

Interaction with other medicines:

Mapivakain it is necessary to apply very carefully at patients with the known allergy or hypersensitivity to drugs. Patients with an allergy to methylparaben or derivatives of para-aminobenzoic acid (novocaine, pantocain, benzocaine, etc.) did not show cross sensitivity on agents of amide type, such as мепивакаин. Beta-blockers, blockers of calcium channels, antiarrhythmic drugs strengthen the oppressing action on conductivity and contractility of a myocardium.

In case of simultaneous use of an aprindin and a mepivakain accumulation of side effect as априндин has similar side effect through the chemical structure is possible. During treatment the general increase in a possibility of bleeding arises anticoagulants. Are described a toxic synergism for the central analgetik, chloroform, ether and thiopental. There are messages on increase in level in blood serum of amide anesthetics at the accompanying introduction of Cimetidinum. If sedatives are applied to reduction of fear of the patient, it is necessary to reduce an anesthetic dose as the local anesthetizing agents, as well as soothing, are depressants of the central nervous system that in a combination can give a cooperative effect. At patients who accept antiarrhythmic drugs strengthening of manifestations of side effects after Mepifrin-Zdorovye's introduction is observed.

Contraindications:

This drug is contraindicated in case of hypersensitivity to local anesthetics of amide type, and also in the following cases:

• patients with a malignant hyperthermia in the anamnesis;
• serious violations of atrioventricular conductivity which are not supported by a pacemaker;
• the medicamentous not controlled epilepsy;
• acute dekompensirovanny heart failure;
• the acute alternating porphyria;
• heavy arterial hypotension;
• children's age up to 4 years.

Overdose:

Toxic reactions at overdose of local anesthetic can arise under two conditions: or immediately, through overdose as a result of an unintentional intravascular injection, or later, as a result of overdose from an excess dose of local anesthetic. These undesirable effects are shown as symptoms of TsNS and/or cardiovascular symptoms.

The symptoms caused by active agent mepivakainy.

Insignificant symptoms of TsNS, such, as: metal smack, a ring in ears, dizziness, concern, alarm, the accelerated breath (tachypnea).

More acute symptoms: drowsiness, concern, shiver, myotonia, convulsive reduction of muscles, lump and paralysis of respiratory system.

Acute cardiovascular symptoms: lowering of arterial pressure, disturbances of conductivity of heart, bradycardia, cardiac standstill.

Acute symptoms from digestive tract: nausea, vomiting.

Therapy.

At emergence of side effects of administration of local anesthetic it is necessary to stop.

Actions of the first acute management.

Diagnosis (breath, blood circulation, consciousness) support/resuming of vital signs of breath and blood circulation, oxygen access, intravenous access. At manifestation of a myoclonus it is necessary to carry out oxygenation and an injection of benzodiazepine.

Special events:

Hypertension:	to raise an upper body, if necessary nifedipine under language.
Convulsions:	protection of patients against possible damages, if necessary diazepam intravenously.
Hypotonia:	horizontal position, if necessary inside vascular infusion of solution of electrolyte, vasoconstrictive agents (for example, Epinephrinum, cortisone intravenously).
Bradycardia:	atropine intravenously.
Acute anaphylaxis:	to call the ambulance, to meanwhile provide intravenous administration of solutions of electrolytes, if necessary – Epinephrinum intravenously, a cortisone intravenously.
Cordial shock:	to raise an upper body, to call the ambulance.
Stop of cardiovascular system:	artificial ventilation of the lungs, indirect cardiac massage, resuscitation actions. To call the ambulance.

Storage conditions:

To store in original packaging at a temperature of not Vichy of 25 to the °sena to allow freezings. To store in the place, unavailable to children. Karpula or an ampoule needs to be used right after opening.

Period of validity. 3 years.

 

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 30 mg/ml in karpula on 1,7 ml No. 10 or No. 10x5 in the blister in a box; in ampoules on 1,7 ml No. 10 in a box; No. 5x2 in the blister in a box.