Articaine-Binergia with adrenaline - instructions for use, doses, side effects, contraindications

active ingredients: articaine hydrochloride (in terms of 100% substance) - 10 mg and epinephrine hydrotartrate (in terms of 100% substance) - 0.009 mg (in terms of epinephrine 0.005 mg, which corresponds to the epinephrine content in the solution of 1: 200,000);

Excipients: sodium disulfite 0.50 mg, sodium chloride 7.0 mg, disodium edetate 0.25 mg, 1 M sodium hydroxide solution to pH 5.0, water for injection up to 1 ml.

1 ml of the drug with a dosage (20 mg + 0.005 mg) / ml contains:

active ingredients: articaine hydrochloride (in terms of 100% substance) - 20 mg and epinephrine hydrotartrate (in terms of 100% substance) - 0,009 mg (in terms of epinephrine - 0,005 mg, which corresponds to the content of epinephrine in a solution of 1: 200,000);

Excipients: sodium disulfite 0.50 mg, sodium chloride 5.2 mg, disodium edetate 0.25 mg, 1M sodium hydroxide solution to pH 5.0, water for injection up to 1 ml.

Description:

Transparent, colorless or with a yellowish tinge solution.

Pharmacotherapeutic group:Local anesthetic + alpha and beta-adrenomimetic

ATX: & nbsp

N.01.B.B.58 Articaine in combination with other drugs

Pharmacodynamics:

Articaine-Binergia with adrenaline is a combined preparation, which includes articaine (amine type local anesthetic) and epinephrine (vasoconstrictor), which is added to the formulation for the prolongation of anesthesia.

Artikain has a local anesthetic effect by blocking potential-dependent sodium channels in the cell membrane of neurons, which leads to a reversible inhibition of the conduction of impulses along the nerve fiber and a reversible loss of sensitivity.

With all methods of administration articaine has a fast (latent period - from 1 to 11 minutes) and a strong anesthetic effect and has good tissue tolerance. The duration of anesthesia for solutions with the addition of epinephrine is 120 to 420 minutes. For superficial anesthesia articaine has very little anesthetic effect.

Pharmacokinetics:

The binding of articaine to plasma proteins is approximately 95%. Articaine quickly and practically immediately after administration, is metabolized (by hydrolysis) with nonspecific plasma esterases in tissues and blood (90%); The remaining 10% dose of articaine is metabolized by microsomal enzymes of the liver. Articaine is excreted by the kidneys, mainly in the form of articaine acid.

After intramuscular administration, the maximum concentration of articaine in the blood is reached after 20-40 minutes, the half-life is 39.8 ± 3.1 minutes.

Indications:

Articaine-Binergia with adrenaline is used for local and regional blockade of nerve endings.

Contraindications:

Hypersensitivity to articaine, epinephrine, sulfites (in particular, in patients suffering from bronchial asthma with increased susceptibility to sulfites, since there may be acute allergic reactions with symptoms of anaphylactic shock, such as bronchospasm), or to any of the other auxiliary components of the drug.

Contraindications, articaine

- Pincreased sensitivity to other amine type local anesthetics;

- severe violations of the sinus node function or severe conduction disorders (such as severe bradycardia, atrioventricular blockage of the 2nd or 3rd degree);

- acute decompensated heart failure (acute violation of the functional state of the heart);

- severe arterial hypotension, shock.

Contraindications, epinephrine

- Anesthesia of terminal phalanges of the fingers and toes (risk of ischemia);

- paroxysmal tachycardia, tachyarrhythmia;

- recently transferred (3-6 months ago) myocardial infarction;

- recently conducted (3 months ago) coronary artery bypass graft;

- simultaneous reception of non-selective beta-blockers, for example, propranolol (risk of hypertensive crisis and severe bradycardia);

- an angle-closure glaucoma;

- hyperthyroidism;

- pheochromocytoma;

- severe arterial hypertension;

- simultaneous administration of tricyclic antidepressants or monoamine oxidase (MAO) inhibitors, since these active substances can enhance the effect of epinephrine on the cardiovascular system. This concerns the time period up to 14 days after the end of treatment with MAO inhibitors.

Intravenous injection is contraindicated.

Carefully:

- In patients with impaired coagulation;

- in patients with severe impairment of liver or kidney function;

- when used simultaneously with halogen-containing agents in the conduct of inhalation anesthesia (see section "Interaction with other drugs");

- in patients with epilepsy in the anamnesis;

- in patients with chronic heart failure, ischemic heart disease, angina pectoris, myocardial infarction in history, heart rhythm disturbances, arterial hypertension;

- in patients with atherosclerosis;

- in patients with cerebrovascular disorders, a history of stroke;

- in patients with chronic bronchitis, emphysema;

- in patients with diabetes mellitus;

- in patients with severe forms of anxious neurosis.

Pregnancy and lactation:

Pregnancy

The experience of using articaine in pregnant women is not available, except for its use during childbirth.

In experimental studies on animals any signs of direct or indirect negative impact artikaina pregnancy, development of the embryo / fetus, childbirth or postnatal development were found. The results of the study in animals demonstrated that epinephrine has a reproductive toxicity in animals at doses exceeding the maximum recommended dose. Articaine and epinephrine penetrate the placental barrier to a lesser extent than other local anesthetics.

The concentration of articaine in the serum in newborns (after the administration of the mother's drug) is approximately 30% of the concentration of articaine in the mother's blood serum.

In case of accidental intravascular injection epinephrine can reduce blood supply to the uterus.

The decision to use the drug Articaine-Binergia with epinephrine can be taken by a doctor only if the potential benefit from its use for the mother justifies the potential risk to the fetus.

The negative effect of articaine on newborns with the use of obstetric anesthesia has not been revealed.

Breastfeeding period

Due to the short half-life of epinephrine, as well as the very rapid drop in serum levels and rapid elimination of articaine from the body, breast milk does not show clinically significant concentrations of articaine and epinephrine. Therefore, in the short-term use of the drug during breastfeeding, as a rule, it is not necessary to interrupt breastfeeding.

Fertility

Experimental studies using articaine 40 mg / ml + epinephrine 0.01 mg / ml in animals (which is several times greater than in the drug Artikain-Binergiya with epinephrine) showed no effect on fertility. When used in therapeutic doses, the negative effect of the drug on human fertility is absent.

Dosing and Administration:

Articaine-Binergia with epinephrine is used for epidural and directed local anesthesia.

A minimum dose should be administered, with which the desired sufficient anesthesia is achieved.

Dosage should be carried out individually in accordance with the peculiarities of each specific case.

For children and elderly patients a dose selection is necessary.

Recommended maximum dose for adults: 5-6 mg / kg body weight (not more than 600 mg). Below are the estimated doses that need to be adjusted depending on the depth of anesthesia and the patient's condition.

Type of anesthesia	Quantity, ml
Type of anesthesia	For dosage 10 mg / ml	For dosage 20 mg / ml
Blockade of the brachial plexus	10-30	10-15
Peribulbar or retrobulbar anesthesia	2-5	2-5
Peridural (epidural) anesthesia	10-30	10-15
Infiltration anesthesia	10-40	10-30

To avoid accidental intravascular injection, an aspiration test should always be performed before the drug is administered and during the administration of the main dose. The injection pressure should correspond to the sensitivity of the tissues.

Side effects:

The incidence of side effects is presented in accordance with the classification recommended by the World Health Organization: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000), including individual messages; frequency is unknown (can not be determined from available data).

Disturbances from the nervous system

Often

Paresthesia, hypoesthesia, headache (due to the presence of epinephrine in the formulation).

Infrequently

Dizziness.

Frequency unknown

Dose-dependent reactions from the central nervous system (especially when injected too large a dose or with occasional intravascular injection): a sense of anxiety, nervousness, stupor, confusion down to loss of consciousness, coma, respiratory distresses, sometimes progressing to a stop in breathing, muscle tremor, twitchings, sometimes progressing to generalized seizures.

Disturbances on the part of the organ of sight

Frequency unknown

Visual disorders (blurred vision, mydriasis, blindness, double vision), usually reversible and occurring during or shortly after injection of a local anesthetic.

Disorders from the gastrointestinal tract

Often

Nausea, vomiting.

Disorders from the cardiovascular system

Infrequently

Tachycardia.

Frequency unknown

Heart palpitations, arrhythmias, signs of angina pectoris, increased blood pressure, hypotension, bradycardia, heart failure and shock (under certain circumstances with a life threat).

In the process of obstetric anesthesia, in particular, with paracervical blockade, the fetus may have a bradycardia. It is recommended to closely monitor the fetal heart tones.

Immune system disorders

Frequency unknown

Allergic or allergic reactions. At the injection site, they can manifest as swelling / swelling and / or inflammation. Manifestations not associated with the place of administration may be flushing of the skin, itching, conjunctivitis, rhinitis, swelling of the face (angioedema).

Angioedema may be manifested by swelling of the upper and / or lower lip, and / or cheeks, edema of the vocal cords with a sensation of "lump in the throat" and difficulty swallowing, hives and difficulty breathing until anaphylactic shock.

Other

Due to the presence of sodium disulfite (sodium metabisulphite) in the preparation of the sodium, allergic reactions in the form of vomiting, diarrhea, heavy breathing, acute asthma attack, consciousness disorder or shock, in particular, in patients suffering from bronchial asthma, are very rare.

Overdose:

Overdose Symptoms

From the central nervous system

Excitation of the central nervous system: anxiety, fear, confusion, hyperpnoea, tachycardia, increased blood pressure with reddening face, nausea, vomiting, tremor, twitching, tonic-clonic convulsions.

Inhibition of the central nervous system: dizziness, hearing loss, loss of speaking ability, stupor, unconsciousness, atony, paresis of the vasomotor nerves (weakness, pallor), dyspnea, death from paralysis of the respiratory tract.

From the side of the cardiovascular system

Depression of the cardiovascular system: bradycardia, arrhythmia, fibrillation of the ventricles, a drop in blood pressure, cyanosis, cardiac arrest.

Emergency help and countermeasures

If there are first signs of side effects or intoxication, such as dizziness, motor agitation, confusion or stupor during the administration of the drug, stop its administration and move the patient to a horizontal position with raised lower limbs. It is necessary to ensure the patency of the airways and monitor the parameters of hemodynamics (the number of heartbeats and blood pressure).

It is recommended to release access to the veins (even with symptoms that do not seem serious) in order, if necessary, to be able to immediately carry out intravenous administration of necessary medications.

In case of breathing disorders, depending on their severity, oxygen supply is recommended, if necessary - artificial respiration, and under certain circumstances - endotracheal intubation and controlled artificial ventilation of the lungs.

Muscular jerking and generalized convulsions can be stopped by intravenous injection of a high-speed antispasmodic agent (for example, suxamethonium chloride, diazepam). It is also recommended to carry out artificial ventilation (oxygen supply).

A sharp drop in blood pressure, tachycardia or a bradycardia can be eliminated by simply moving the patient to a horizontal position with raised lower limbs.

In severe circulatory disorders and shock of any origin, the drug should be discontinued. It is necessary to move the patient to a horizontal position with raised lower limbs and release the airways (insufflation of oxygen). Intravenous administration of balanced solutions of electrolytes, glucocorticosteroids (250-1000 mg of prednisolone or an equivalent amount of a derivative, for example, methylprednisolone), replacement infusion therapy (if necessary, additional plasma substitutes, for example, human albumin).

With the development of circulatory collapse and increased bradycardia intravenously is immediately introduced epinephrine (adrenalin).After diluting 1 ml of a 0.1% solution of epinephrine (1: 1000) to 10 ml, using the resulting 0.01% solution of epinephrine (1: 10,000), slowly introduce first 0.25-1 ml (0.025-0.1 mg epinephrine), controlling the pulse and blood pressure (carefully: there may be heart rhythm disturbances!). Do not exceed a single intravenous dose of 1 ml (0.1 mg epinephrine). If it is necessary to administer doses exceeding a single intravenous dose of epinephrine 0.1 mg, epinephrine should be administered with the infusion solution, adjusting the dropping rate of administration in accordance with the pulse rate and arterial pressure.

Strong tachycardia and tachyarrhythmia can be removed with antiarrhythmic drugs, excluding non-selective beta-blockers, such as, for example, propranolol. In such cases, oxygen supply and circulation control are necessary.

Increased blood pressure in patients with arterial hypertension, if necessary, is stopped with the help of peripheral vasodilators.

Interaction:

Combinations of various local anesthetics cause additional effects on the cardiovascular system and the central nervous system.

Contraindicated combinations

With nonselective beta-blockers, for example, propranolol

Risk of developing a hypertensive crisis and severe bradycardia.

With tricyclic antidepressants or monoamine oxidase inhibitors

It is possible to increase the hypertensive effect of epinephrine (up to 14 days after discontinuation of treatment with monoamine oxidase inhibitors).

Interaction, which should be taken into account

With hypoglycemic agents for oral administration

Epinephrine can inhibit the release of insulin from pancreatic β cells and reduce the effects of hypoglycemic agents for oral ingestion.

With some means for inhalation anesthesia (halothane)

Halothane can increase the sensitivity of the myocardium to catecholamines and increase the risk of heart rhythm disturbances after injections of the drug Articaine-Binergia with epinephrine.

With anticoagulants and other drugs that reduce blood coagulability

When injecting Artikain-Binergia with adrenaline, patients receiving, for example, heparin or acetylsalicylic acid, may develop serious bleeding with unintentional perforation of the vessel,as in such patients the tendency to bleeding is higher.

Special instructions:

Regional and local anesthesia should be carried out by experienced specialists in an appropriately equipped room with availability of ready-to-use equipment and preparations necessary for cardiac monitoring and resuscitation. Personnel performing anesthesia should be qualified and trained in the technique of performing anesthesia, should be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

Intravenous injections are contraindicated!

Do not administer Artikain-Binergia with epinephrine in inflamed (infected) tissue sites (increased absorption of articaine with reduced efficacy).

In order to avoid the risk of adverse reactions, the following conditions must be observed:

- in patients at risk and with higher doses (more than 25% of the maximum single dose), access to the veins should be free, so that if necessary, an intravenous injection should be made;

- apply the minimum effective dose of the drug;

- before the introduction of the drug, carry out a two-stage aspiration test in two planes (to avoid accidental intravascular injection);

- regularly monitor vital signs (control of the cardiovascular system and consciousness).

To prevent infection (including viral hepatitis), care should be taken to ensure that new sterile syringes and needles are always used when taking the drug from ampoules and vials.

Open ampoules can not be reused.

The drug should not be used if the solution changes color or becomes cloudy.

The drug Articaine-Binergia with adrenaline contains sodium disulphite, therefore its use is contraindicated in patients with bronchial asthma with increased sensitivity to sulfites, since it is possible to develop acute allergic reactions such as bronchospasm (see section "Contraindications").

In 1 ml of the drug Articaine-Binergia with an adrenaline injection (10 mg + 0.005 mg / ml) contains 0.127 mmol (2.9 mg) of sodium.

In 1 ml of the drug Articaine-Binergia with an adrenaline solution for injection (20 mg + 0.005 mg / ml) contains 0.096 mmol (2.2 mg) of sodium.

These data should be taken into account when using the drug Articaine-Binergia with epinephrine in patients who control sodium intake (diet low in table salt).

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

A decision should be made by the doctor when the patient can return to the management of vehicles and other potentially dangerous activities requiring increased attention and speed of psychomotor reactions.

Neurosis waiting and postoperative stress can lead to a change in the ability to drive vehicles or other activities, despite the fact that local anesthesia with articaine, according to the results of the relevant tests, did not show a determined deviation from the usual ability to drive vehicles.

Form release / dosage:

Injection, 10 mg / ml + 0.005 mg / ml, 20 mg / ml + 0.005 mg / ml.

Packaging:

For 5 ml, 10 ml or 20 ml of the drug in ampoules of clear, colorless glass.

For 10 ml of the drug in bottles of clear, colorless glass, hermetically sealed with stoppers made of rubber,Crimped aluminum caps or caps with aluminum combined or combined caps with plastic discs.

5 bottles or ampoules in contour plastic packaging (pallet). 1 or 2 contour plastic packages (pallet) with ampoules of 5 ml or 1 contour plastic packaging (pallet) with ampoules of 10 ml or 20 ml or with 10 ml bottles together with instructions for use in a pack of cardboard.

1 contour plastic packaging (pallet) with ampoules of 20 ml together with instructions for use in a cardboard box.

In packs and boxes with ampoules, an ampoule knife or ampoule scarifier is additionally placed. When using ampoules with a color fracture point and a notch or a colored ring of a knife, an ampoule knife or an ampoule scarifier do not.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004013

Date of registration:08.12.2016

Expiration Date:08.12.2021

The owner of the registration certificate:BINERGIYA, CJSC BINERGIYA, CJSC Russia

Manufacturer: & nbsp

Armavir Biofactory, FKP

Information update date: & nbsp25.09.2017

Illustrated instructions

Instructions

Articaine-Binergia with adrenaline (Articaine-Binergia with adrenaline)