Articaine-Binergia - instructions for use, dose, side effects, contraindications

Active substanceArticaineArticaine

Similar drugsTo uncover

Articaine

solution for injections

Promomed Rus, Open Company Russia

Articaine-Binergia

solution for injections

BINERGIYA, CJSC Russia

Ultracaine® D

solution for injections

Sanofi-Aventis Deutschland GmbH Germany

Dosage form: & nbspinjection

Composition:

1 ml of the drug with a dosage of 10 mg / ml contains:

active substance: articaine hydrochloride (in terms of 100% substance) - 10 mg;

Excipients: sodium chloride - 7.0 mg and water for injection up to 1 ml.

1 ml of the drug with a dosage of 20 mg / ml contains:

active substance: articaine hydrochloride (in terms of 100% substance) - 20 mg;

Excipients: sodium chloride - 5.2 mg and water for injection up to 1 ml.

Description:Colorless or colorless with a slightly yellowish tint transparent liquid.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B.08 Articaine

Pharmacodynamics:

Articaine is an amine type local anesthetic.

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.

Articaine has very little anesthetic effect for surface anesthesia. 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 without the addition of a vasoconstrictor (eg, epinephrine) is 60 to 225 minutes.

Articaine-Binergia does not contain epinephrine and is used when the addition of epinephrine to the topical anesthetic is not necessary or the use of epinephrine is contraindicated.

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 is used for local and regional blockade of nerve endings.

Contraindications:

- Hypersensitivity to articaine, other amido type local anesthetics or to any of the auxiliary components of the preparation;

- severe sinus node dysfunction or severe conduction disorders (such as bradycardia, atrioventricular block 2nd or 3rd degree);

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

- severe arterial hypotension, shock.

Carefully:

- In patients with cholinesterase deficiency (use is possible only in case of emergency, as prolongation and pronounced increase in the effect of the drug are possible);

- in patients with angina pectoris, atherosclerosis;

- in patients with coagulation disorders;

- in patients with severe hepatic / renal impairment;

- in patients with epilepsy in the anamnesis.

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.

Artikain penetrates the placental barrier to a lesser extent than other local anesthetics.

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

In view of the lack of clinical data, the decision to use the drug by a doctor can be taken only if the potential benefit from its use for the mother justifies the potential risk to the fetus.

With the use of obstetric anesthesia, no adverse effects of articaine on newborns have been observed.

Breastfeeding period

In the short-term use of the drug during breastfeeding, as a rule, it is not necessary to interrupt breastfeeding, since breast milk does not show clinically significant concentrations of articaine.

Fertility

In studies on animals using articaine 40 mg / ml + epinephrine 0.01 mg / ml no effect on fertility was noted. When used in therapeutic doses, the negative effect of the drug on human fertility is absent.

Dosing and Administration:

Articaine-Binergia, depending on the type of anesthesia chosen, is used for in-filtration, conductive, epidural and intravenous regional 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, dose selection is necessary.

The recommended maximum dose for adults is 5-6 mg / kg body weight (not more than 400 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 a dosage of 10 mg / ml	For a dosage of 20 mg / ml
Brachial plexus blockade	10-30	10-15
Epidural (epidural) anesthesia	10-30	10-15
Intravenous regional anesthesia	30-40	-

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; the frequency is unknown (it is not possible to determine the frequency of occurrence according to the available data).

Disturbances from the nervous system

Often

Paresthesia, hypoesthesia.

Infrequently

Dizziness.

Frequency unknown

Dose-dependent reactions from the central nervous system (especially when administered too large a dose or with a random intravascular injection): a sense of anxiety, nervousness, stupor, confusion, sometimes progressing to loss of consciousness, coma, respiratory disorders, sometimes progressing to stopping breathing, muscle tremor , muscle 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) that occur during or shortly after injection of the drug in the head region. As a rule, these symptoms are transient.

Disorders from the gastrointestinal tract

Often

Nausea, vomiting.

Disorders from the cardiovascular system

Frequency unknown

Reduction of blood pressure, bradycardia, heart failure and shock (under certain circumstances with a threat to life).

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

Immune system disorders

Frequency unknown

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

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 asphyxia due to paralysis of the respiratory muscles.

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 the first signs of side effects or intoxication, such as dizziness, motor agitation, confusion or stupor during the introduction of the drug, stop its introduction 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 free 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 the necessary medicines.

If breathing is disturbed, depending on their severity, oxygen supply is recommended, if necessary - artificial respiration, and under certain circumstances - endotracheal intubation and artificial ventilation of the lungs under control.

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 of the lungs (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% epinephrine solution (1: 10,000), slowly introduce first 0.25-1 ml (0.025-0.1 mg epinephrine), controlling the pulse and blood pressure (carefully: possible violations of the heart rate!). 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.

Interaction:

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

With anticoagulants and other drugs that reduce blood coagulation When injecting the drug Articaine-Binergia patients who receive, for example, heparin or acetylsalicylic acid, may develop serious bleeding with unintentional perforation of the vessel, as in such patients there is a higher tendency to bleeding.

The drug Artikain-Binergiya is incompatible with alkaline solutions.

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.

Only in the presence of strict indications Articaine-Binergia can be used in patients with cholinesterase deficiency, since prolongation is possible and, under certain circumstances, an increase in its effect.

Do not administer Artikain-Binergia to 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 (monitoring the cardiovascular system and consciousness).

For application in ophthalmology and with neuroaxial anesthesia, the drug can be withdrawn only from newly opened ampoules and vials (the drug does not contain preservatives).

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 and vials can not be reused for other patients!

In 1 ml of the drug Articaine-Binergia injection for 10 mg / ml contains 0.12 mmol (2.75 mg) of sodium.

In 1 ml of the drug Articaine-Binergia injection for 20 mg / ml contains 0.09 mmol (2.04 mg) of sodium.

These data should be considered when using the drug Articaine-Binergia in patients controlling 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:Solution for injection 10 mg / ml or 20 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 transparent colorless glass, hermetically sealed with rubber stoppers, 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. If you use ampoules with a colored break point and a notch or a colored ring, the ampoule opener or ampoule ampoule opener is not inserted.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

5 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-003910

Date of registration:18.10.2016

Expiration Date:18.10.2021

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 (Articaine-Binergia)