Mepivacaine DF - instructions for use, dose, side effects, contraindications

Active substanceMepivacaineMepivacaine

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Mepivacaine DF

solution for injections

HIRATRADE, JV LLC Russia

Mepivastezin

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3M Deutschland GmbH

Scandinibes

solution for injections

Laboratory of Inibes SA Spain

Scandonaut

solution for injections

The Septodont France

Dosage form: & nbspinjection

Composition:

1 ml of the preparation contains:

active substance: mepivacaine hydrochloride 30 mg; Excipients: sodium chloride 6 mg, water for injection up to 1 ml.

Description:

A clear, colorless solution.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B.03 Mepivacaine

N.01.B.B Amides

Pharmacodynamics:

Mepivacaine is an amine type local anesthetic. Introduced by injection next to sensitive nerve endings or nerve fibers, mepivacaine reversibly blocks voltage-dependent sodium channels, prevents the generation of pulses in the endings of the sensory nerves and painful pulses in the central nervous system. Mepivacaine is lipophilic - the pKa value is 7.6. Mepivacaine penetrates the membrane of the nerve in the basic form, then, after the repetition has a pharmacological action in ionized form.The ratio of these forms of mepivacaine is determined by the pH value of the tissues in the anesthetized area. At low pH values of the tissue, for example, in inflamed tissues, the main form of mepivacaine is present in small amounts, and therefore anesthesia may be insufficient.

Unlike most local anesthetics, which have vasodilator properties, mepivacaine has no pronounced effect on the vessels and can be used in dentistry without a vasoconstrictor.

With peripheral neural blockade the effect of the drug comes in 2-4 minutes. The duration of pulp anesthesia is 20-40 minutes, the duration of anesthesia of soft tissues is 2-3 hours. The duration of motor blockade does not exceed the duration of anesthesia.

Pharmacokinetics:

Suction, distribution

When administered to the tissues of the maxillofacial area by means of a conductive or infiltration anesthesia, the maximum concentration of mepivacaine in the blood plasma is reached approximately 30 minutes after the injection. The duration of action is determined by the rate of diffusion from the tissues into the bloodstream. The distribution coefficient is 0.8.The connection with plasma proteins is high (from 65% to 79%). Metabolism

Mepivacaine is metabolized in the liver by hydroxylation and dealkylation to mhydroxypepivacaine, p-hydroxymepivacaine, pipecolylxylidine.

Mepivacaine is subjected to hepatic intestinal recirculation.

Excretion

It is excreted by the kidneys, mainly in the form of metabolites. The half-life (T_1/2) is long and is about 2-4 hours.

Plasma clearance - 0,78 l / min.

The elimination half-life increases in patients with liver disease and in patients with uremia. With liver pathology (cirrhosis, hepatitis), cumulation of mepivacaine is possible.

Indications:

Infiltration, conductive, intraligamentary, intraosseous and intrapulpic anesthesia in surgical and other painful dental interventions.

The drug does not contain a vasoconstrictor component, which allows its use in patients with diseases of the cardiovascular system, diabetes, closed-angle glaucoma.

Contraindications:

- Hypersensitivity to mepivacaine (including other locally anesthetic drugs of the amide group) or other excipients,included in the preparation;

- Severe liver disease: cirrhosis, hereditary or acquired porphyria;

- Myasthenia gravis gravis;

- Children under 4 years old (body weight less than 20 kg);

- Heart rhythm and conduction disorders;

- Acute decompensated heart failure;

- Arterial hypotension;

- Intravascular injection (before the administration of the drug, an aspiration test should be performed, see section "Special instructions").

Carefully:

- Conditions accompanied by a decrease in hepatic blood flow (eg, chronic heart failure, diabetes mellitus, liver disease);

- Progression of cardiovascular failure;

- Inflammatory diseases or infection of the injection site;

- Deficiency of pseudocholinesterase;

- Renal failure;

- Hyperkalemia;

- Acidosis;

- Elderly age (over 65 years);

- Atherosclerosis;

- Embolism of vessels;

- Diabetic polyneuropathy.

Pregnancy and lactation:

Pregnancy.

During pregnancy, local anesthesia is considered the safest method for relieving pain during dental interventions. The drug does not affect the course of pregnancy, however, due to the fact that mepivacaine can penetrate the placenta, it is necessary to evaluate the benefit to the mother and the risk to the fetus, especially in the first trimester of pregnancy.

Breastfeeding period

Local anesthetics, including mepivacaine, to a small extent are excreted in breast milk. With a single use of the drug, a negative effect on the child is unlikely. It is recommended that breastfeeding be performed 10 hours after the drug is administered.

Dosing and Administration:

The amount of solution and the total dose depend on the type of anesthesia and the nature of the surgery or manipulation.

The rate of administration should not exceed 1 ml of the drug in 1 minute.

To avoid intravenous injection, always perform aspiration control.

Use the lowest dose of the drug, providing sufficient anesthesia. The average single dose is 1.8 ml (1 cartridge).

Do not use already opened cartridges to treat other patients. Cartridges with unused residue of the drug must be destroyed.

Adults

The recommended maximum single dose of mepivacaine hydrochloride is 300 mg (4.4 mg / kg body weight), which corresponds to 10 ml of the drug (about 5.5 cartridges).

Children older than 4 years (with a body weight of more than 20 kg)

The amount of the drug depends on the age, body weight and the nature of the surgery. The average dose is 0.75 mg / kg body weight (0.025 ml drug / kg body weight).

The maximum dose of mepivacaine is 3 mg / kg body weight, which corresponds to 0.1 ml drug / kg body weight.

Depending on body weight, the following maximum doses of the drug are recommended:

Body weight, kg	Dose of mepivacaine, mg	Volume of the preparation, ml	The number of cartridges of the drug (1.8 ml each)
20	60	2	1,1
30	90	3	1,7
40	120	4	2,2
50	150	5	2,8

Special patient groups

In elderly people, an increase in the concentration of the drug in the blood plasma is possible due to a slowing of the metabolism. This group of patients requires the use of a minimal dose that provides sufficient anesthesia.

In patients with renal or hepatic insufficiency, as well as in patients with hypoxia, hyperkalemia or metabolic acidosis, it is also necessary to use a minimal dose that provides sufficient anesthesia.

In patients with such diseases as vascular embolism, atherosclerosis or diabetic polyneuropathy, a dose reduction of one third is necessary.

Side effects:

Possible side effects when using Mepivacaine DF are similar to side effects arising from the use of amine type local anesthetics. The most common disorders are the nervous system and the cardiovascular system. Serious side effects are systemic. Side effects are grouped according to systems and organs according to the dictionary MedDRA and classification of the frequency of development of adverse reactions WHO: very often (≥1 / 10), often (≥1 / 100 to <1/10), infrequently (≥1 / 1000 to <1/100), rarely (≥1 / 10000 to <1/1000), very rarely (<1/10000), the frequency is unknown (the frequency can not be determined from the available data).

Organs and Systems	Frequency	Adverse events
Violations of the blood and lymphatic system	Rarely	Methemoglobinemia.
Immune system disorders	Rarely	- Anaphylactic and anaphylactoid reactions - Angioedema (including swelling of the tongue, mouth, lips, throat and periorbital edema) - Hives - Itchy itching - Rash, erythema
Disturbances from the nervous system	Rarely	1. Effects on the central nervous system (CNS) In connection with the increased concentration of anesthetic in the blood entering the brain,It is possible to load the central nervous system and affect the regulatory centers of the brain and cranial nerves. Concomitant side effects are agitation or depression, which are dose-dependent and are accompanied by the following symptoms: - Anxiety (including nervousness, excitement, anxiety) - Confusion of consciousness - Euphoria - Numbness of the lips and tongue, paresthesia of the mouth - Drowsiness, yawning - Speech disorder (dysarthria, incoherent speech, logoreia) - Dizziness (including numbness, vertigo, imbalance) - Headache - Nystagmus - Noise in the ears, hyperacusis - Blurred vision, diplopia, miosis These symptoms should not be considered as symptoms of a neurosis. The following side effects are also possible: - Impairment of vision - Tremor - Muscle cramps These effects are symptoms of the following conditions: - Loss of consciousness - Convulsions (including generalized) Seizures can be accompanied by CNS depression, coma, hypoxia and hypercapnia, which can lead to respiratory depression and respiratory arrest. Symptoms of an excited state are temporary, but the symptoms of depression (eg, drowsiness) can lead to an unconscious condition or a stopping of breathing. 2.Effects on the peripheral nervous system (PNS) The impact on PNS is associated with an increased concentration of anesthetic in the blood plasma. Molecules of the anesthetic can penetrate from the systemic blood stream into the synaptic cleft and have a negative effect on the heart, blood vessels and gastrointestinal tract. 3. Direct local / local effects on efferent neurons or preganglionic neurons in the submaxillary region or postganglionic neurons. Paresthesia of the mouth, lips, tongue, gums, etc. - Loss of sensitivity of the oral cavity (lips, tongue, etc.) - Decreased sensitivity of the oral cavity, lips, tongue, gums, etc. - Dysaesthesia, including fever or chills, dysgeusia (including metallic taste) - Local muscle cramps - Local / local hyperemia - Local / local pallor 4. Effects on reflexogenic zones Local anesthetics can cause vomiting and vasovagal reflex, accompanied by the following effects: - Vascular expansion - mydriasis - Pale - Nausea, vomiting - Hyper-salivation - Perspiration
Heart Disease	Rarely	Possible development of cardiac toxicity, accompanied by the following symptoms: - Cardiac arrest - Impaired cardiac conduction (atrioventricular block) - Arrhythmia (ventricular extrasystole and ventricular fibrillation) - Cardiovascular disorder - Disorder of cardiovascular system - Inhibition of the myocardium - Tachycardia, bradycardia
Vascular disorders	Rarely	- Vascular collapse - Hypotonia - Vascular expansion
Disturbances from the respiratory system, chest and mediastinal organs	Frequency unknown	Inhibition of breathing (from bradypnoea to respiratory arrest)
Disorders from the gastrointestinal tract	Frequency unknown	- Edema of the tongue, lips, gums - Nausea, vomiting - Ulceration of the gums, gingivitis
Are common disorders and disorders at the site of administration	Frequency unknown	- Necrosis at the site of administration - Edema in the head and neck

Overdose:

Overdose is possible with the unintentional intravenous administration of the drug or as a result of exceptionally rapid absorption of the drug. The critical threshold dose is the concentration of 5-6 μg mepivacaine hydrochloride per 1 ml of blood plasma.

Symptoms:

1. From the central nervous system

Intoxication of mild degree - paresthesia and numbness of the oral cavity, tinnitus, "metallic" taste in the mouth, fear, anxiety, tremor, muscle twitching, vomiting, disorientation.

Intoxication of an average degree - dizziness, nausea, vomiting, speech disorder, numbness, drowsiness, confusion, tremor, choreiform movements, tonic-clonic convulsions, pupil dilated, rapid breathing.

Intoxication of severe degree - vomiting (risk of suffocation), paralysis of the sphincter, loss of muscle tone, lack of response and akinesia (stupor), irregular breathing, stopping breathing, coma, death.

2. From the side of the heart and blood vessels

Intoxication of mild degree - increase of arterial pressure, palpitation, rapid breathing.

Intoxication of the middle degree - heart palpitations, arrhythmia, hypoxia, pallor. Intoxication of severe degree - severe hypoxia, violation of the heart rhythm (bradycardia, lowering blood pressure, primary heart failure, ventricular fibrillation, asystole).

Treatment:

At the appearance of the first signs of an overdose, it is necessary to immediately stop the administration of the drug, and also to provide support for respiratory function, if possible with the use of oxygen, monitoring the pulse and blood pressure.

If there is a violation of breathing - oxygen, endotracheal intubation, artificial ventilation (central analeptics are contraindicated).

When hypertension is necessary to raise the upper part of the patient's trunk, if necessary - nifedipine sublingually.

In case of hypotension, the position of the patient's body should be brought to the horizontal position, if necessary - intravascular injection of electrolyte solution, vasoconstrictor drugs. If necessary, compensate the volume of circulating blood (for example, solutions of crystalloids).

When bradycardia is administered atropine (from 0.5 to 1 mg) intravenously.

With convulsions, it is necessary to protect the patient from concomitant damage, if necessary, intravenously diazepam (from 5 to 10 mg). With prolonged seizures, sodium thiopental (250 mg) and a short-acting muscular relaxant are injected, followed by mechanical ventilation of the lungs with oxygen.

In severe disorders of blood circulation and shock - intravenous infusion of solutions of electrolytes and plasma substitutes, glucocorticosteroids, albumin.

With severe tachycardia and tachyarrhythmias, intravenous beta-blockers (selective).

When cardiac arrest, cardiopulmonary resuscitation should be performed immediately.

When using local anesthetics, it is necessary to provide access to the device for artificial ventilation, pressure-enhancing drugs, atropine, anticonvulsants.

Interaction:

Appointment against the background of monoamine oxidase (MAO) inhibitors (furazolidone, procarbazine, selegiline) increases the risk of lowering blood pressure. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect of mepivacaine.

Mepivacaine increases the inhibitory effect on the central nervous system caused by other drugs. When used simultaneously with sedatives, a reduction in the dose of mepivacaine is required.

Anticoagulants (ardeparin sodium, dalteparin, enoxaparin, heparin, warfarin) increase the risk of bleeding.

When treating the place of injection of mepivacaine with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.

Strengthens and lengthens the action of myorelaxing drugs.

When administered with narcotic analgesics, an additive inhibitory effect on the central nervous system develops, which is used in epidural anesthesia, but respiratory depression is taken into account.

There is antagonism with antimiasthenic drugs on the effect on skeletal muscles, especially when used in high doses, which requires an additional correction of the treatment of myasthenia gravis.

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

When used simultaneously with blockers H₂-gistaminovyh receptors (cimetidine) may raise the level of mepivacaine in the blood serum.

When used simultaneously with antiarrhythmics (tokainid, sympatholytics, digitalis preparations) may increase the side effects.

Special instructions:

It is necessary to abolish monoamine oxidase inhibitors 10 days before the planned introduction of a local anesthetic.

Apply only in a medical institution.

After opening the cartridge, immediate use of the contents is recommended.

The drug must be administered slowly and continuously.When using the drug, it is necessary to monitor the blood pressure, pulse and diameter of the pupils of the patient. Before using the drug, it is necessary to provide access to resuscitative equipment.

Anesthesia with a drug with simultaneous administration of low molecular weight heparin for the prevention of thrombosis should be carried out with caution.

In patients receiving anticoagulant treatment, the risk of bleeding and the development of bleeding is increased.

The anesthetic effect of the drug can be reduced when injected into an inflamed or infected area.

When using the drug, unintentional injury to the lips, cheeks, mucous membrane and tongue, especially in children, is possible due to a decrease in sensitivity.

The patient should be warned that eating is possible only after restoring sensitivity.

Before the introduction of the drug, always perform aspiration control to avoid intravenous administration.

The drug contains less than 1 mmol (23 mg) of sodium per cartridge.

With repeated use of the drug, there may be a lack of pharmacological action in connection with the development of tolerance to the drug.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:

Solution for injection 30 mg / ml.

Packaging:

1.8 ml of solution in a colorless glass cartridge. The bottom of the cartridge is sealed with a rubber piston, on the outside of which there may be convex symbols. The neck of the cartridge is sealed with a gray rubber stopper and an aluminum cap. The cartridge is glued with a transparent self-adhesive label with a marking.

For 10 cartridges in a blister of aluminum foil and PVC film.

For 5 blisters together with instructions for use in a cardboard pack with the control of the first opening.

Storage conditions:

Store in a dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004091

Date of registration:23.01.2017

Expiration Date:23.01.2022

The owner of the registration certificate:HIRATRADE, JV LLC HIRATRADE, JV LLC Russia

Manufacturer: & nbsp

INDUSTRIA E COMERCIO DFL S.A. Brazil

Information update date: & nbsp06.02.2017

Illustrated instructions

Instructions

Mepivacaine DF (Mepivacaine DF)