Brilokain-adrenaline forte - instructions for use, dose, side effects, contraindications

adrenaline hydrotartrate ([recalculated to 100% substance] in terms of base) - 0.0010 g, articine hydrochloride (in terms of 100% substance) - 4.0000 g

Excipients: sodium pyrosulfite-0,0500 g, sodium chloride 0.1600 g, trilon B-0.0250 g, 1 M sodium hydroxide solution up to pH 5,0, water for injection up to 100 ml.

Description:Colorless transparent liquid.

Pharmacotherapeutic group:Local anesthetic + α- and β-adrenomimetic

ATX: & nbsp

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

Pharmacodynamics:

The drug Brilokain®-epinephrine used for local infiltration and conduction anesthesia in dentistry is a combined preparation that includes articaine (amine type local anesthetic) and epinephrine (adrenaline) (vasoconstrictor), which is added to the formulation for the prolongation of anesthesia. Articaine has a local anesthetic effect due to the blockade of 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 reverse loss of sensitivity.

The drug has a fast (latent period - 1 to 3 min) and a strong anesthetic effect and has good tissue tolerance. The duration of anesthesia is at least 75 minutes.

Children

The use of the drug in children aged 4 to 16 at a dose of 5 mg / kg of body weight provides a sufficient local anesthetic effect of the drug during the mandibular infiltration and maxillary conduction anesthesia. The duration of anesthesia is comparable in all age groups and depends on the injected volume of the drug.

Pharmacokinetics:

Articaine quickly and practically immediately after administration is metabolized (by hydrolysis) with nonspecific plasma esterases in tissues and blood (90%); The remaining 10% of the dose of articaine is metabolized by microsomal enzymes of the liver. The resulting main metabolite articaine - articaine acid - does not have local anesthetic activity and systemic toxicity. This allows repeated injections of the drug.

Concentrations of articaine in the blood in the area of dental alveoli after submucosal administration are thousands of times higher than articaine concentrations in the systemic circulation. The binding of articaine to plasma proteins is 95%. Articaine is excreted through the kidneys, mainly in the form of articaine acid. After submucosal administration, the half-life of articaine (T1/2) is approximately 25 minutes.

In children, comparable pharmacokinetic data were obtained.

Artikain penetrates the placental barrier, practically does not excrete with breast milk.

Indications:

The drug Brilokain®-epinephrine forte is indicated for local anesthesia (infiltration and conduction anesthesia) in dentistry with traumatic interventions and if necessary expressed hemostasis or better visualization of the operating field:

- dental operations on the mucosa and on the bones, requiring the creation of conditions for more severe ischemia,

- operation on the tooth pulp (amputation or extirpation),

- removal of a broken tooth (osteotomy) or a tooth afflicted with apical periodontitis,

- prolonged surgical interventions,

- percutaneous osteosynthesis,

- excision of cysts,

- interference on the mucosa of the gum,

- resection of the apex of the tooth root.

Contraindications:

- Intravenous administration of the drug is contraindicated;

- Anesthesia of the distal parts of the limbs, such as the fingers and toes (because of the danger of ischemia);

- Hypersensitivity to articaine or other amido type local anesthetics, except when hypersensitivity to these agents has been allergic to articaine by appropriate studies conducted in compliance with all necessary rules and requirements;

- Hypersensitivity to epinephrine;

- Hypersensitivity to the auxiliary components of the drug, including sulfites (including manifested as bronchial asthma).

Contraindications related to articaine

- Severe dysfunction of the sinus node or severe conduction disorders (such as severe bradycardia, atrioventricular blockade of II and III degrees);

- Acute decompensated heart failure;

- Severe arterial hypotension;

- Children under 4 years (lack of clinical experience).

Contraindications related to epinephrine

- Paroxysmal tachycardia, tachyarrhythmia;

- Closed-angle glaucoma;

- Admission of nonselective beta-blockers, for example, propranolol (risk of developing hypertensive crisis and severe bradycardia);

- Hyperthyroidism;

- Pheochromocytoma;

- Severe hypertension;

- Postponed myocardial infarction within 3-6 months, aortocoronary bypass surgery within the last 3 months;

- Concomitant treatment with tricyclic antidepressants or monoamine oxidase (MAO) inhibitors, since these drugs can potentiate the cardiovascular effects of epinephrine. This can occur up to 14 days after the abolition of MAO inhibitors.

Perhaps the development of acute allergic reactions with anaphylactic symptoms, such as bronchospasm in persons with hypersensitivity to sulfites, manifested in the form of bronchial asthma.

Carefully:

Angina pectoris, atherosclerosis, postinfarction cardiosclerosis (myocardial infarction> 6 months ago), cerebral circulatory disorders, a history of stroke, other cardiovascular diseases (not described in the section "Contraindications"), chronic bronchitis, emphysema,diabetes mellitus, cholinesterase insufficiency (the use is possible only in case of emergency, as the prolonged and excessively strong effect of the drug is possible), blood clotting disorders, severe liver and kidney dysfunction, simultaneous use of general anesthetic agents (halogenated hydrocarbon derivatives), epilepsy in anamnesis, severe anxiety.

Pregnancy and lactation:

Articaine and epinephrine penetrate through the placental barrier.

In view of the lack of clinical data, the use of the drug is possible only if the potential benefit from its use for the mother justifies the potential risk to the fetus. If articaine is needed during pregnancy, it is better to use drugs that do not contain epinephrine or with an epinephrine concentration of 0.005 mg / ml. In case of accidental intravascular injection epinephrine can reduce blood supply to the uterus.

Pre-clinical studies showed no toxic effects on the reproductive system, fertility, and embryogenesis in rats and rabbits. Epinephrine-induced fetal anomalies in animals were observed when administered at doses significantly exceeding the maximum recommended in the formulation.It is not expected that human fertility will be affected by the use of articaine and epinephrine in therapeutic doses.

During lactation, there is no need to interrupt breastfeeding, since breast milk does not show clinically significant concentrations of articaine. Breastfeeding mothers should express and remove the first breast milk after anesthesia using articaine.

Dosing and Administration:

The drug is intended for use in the oral cavity and can be administered only in tissues where there is no inflammation.

Do not inject into inflamed tissues.

The drug can not be administered intravenously.

For anesthesia with incisions and sutures in the palate with the aim of creating a palatine depot you need about 0.1 ml of the drug for each injection.

In the case of removal of premolars of the lower jaw in the absence of inflammation it is possible to do without mandibular anesthesia, since infiltration anesthesia provided by injecting 1.7 ml of the drug per tooth is usually sufficient. If this method fails to achieve the desired effect, an additional injection of 1-1.7 ml of anesthetic into the submucosa should be performed in the region of the transitional fold of the lower jaw from the vestibular side.If, however, in this case, it was not possible to achieve complete anesthesia, it is necessary to conduct a conductive blockade of the mandibular nerve.

In surgical interventions, the dose of Brilokain®-adrenaline forte depends on the severity and duration of the intervention individually.

When performing one treatment procedure, adults can enter articaine in a dose of up to 7 mg per 1 kg of body weight. It was noted that patients well tolerated doses up to 500 mg (corresponding to 12.5 ml of solution for injection).

In children older than 4 years, the dose is selected depending on the age and body weight of the child; The dose should not exceed 5 mg of articaine per 1 kg of body weight.

In elderly patients and patients with severe renal and hepatic insufficiency, it is possible to create elevated plasma concentrations of articaine. In these patients, the drug should be used at the minimum dose necessary to achieve sufficient depth of anesthesia. In order to avoid accidental ingestion of the drug into blood vessels, a two-stage aspiration test should always be carried out before insertion, with a needle rotation of 90 and 180 ° (see Special instructions).

Severe systemic reactions due to unintentional intravascular administration can be prevented by slow administration: first, 0.1-0.2 ml of the drug is administered, then, after 20-30 seconds, the remainder of the drug is slowly introduced.

The injection pressure should correspond to the sensitivity of the tissues.

Side effects:

The frequency of adverse reactions is determined by the following categories: very often (≥1/10), often (≥1/100, <1/10), infrequently (≥1/1000, <1/100), rarely (≥1/10000, <1/1000), and very rarely (<1/10000), including individual messages, the frequency is unknown (can not be determined by the available data).

Co side of the immune system

Frequency unknown: allergic reactions or pseudoallergic reactions (hypersensitivity). They may manifest as edema and / or inflammation at the injection site, but may also occur regardless of the site of injection and manifest as erythema, pruritus, conjunctivitis, rhinitis, angioedema, edema of the upper lip and / or lower lip and / or swelling cheeks, swelling of the larynx with difficulty swallowing, hives and difficulty breathing, which can reach anaphylactic shock.

From the nervous system

Often: paresthesia, hypesthesia, headache, probably due to the presence of epinephrine in the formulation.

Infrequently: dizziness.

Frequency unknown: dose-dependent reactions from the central nervous system (including at excessively high doses or after a random intravascular injection): agitation, anxiety, stupor, progressing in some cases to unconsciousness, coma, respiratory failure (in some cases, up to stopping breathing) , muscle tremor and muscle twitching, sometimes progressing to generalized seizures. Reactions at the injection site: nerve damage (eg facial nerve paresis), decreased taste sensations.

From the side of the organs of sight

Frequency unknown: transient visual impairment (blurred vision, blindness, diplopia).

From the side of the cardiovascular system

Infrequently: tachycardia

Frequency unknown: violation of the heart rate, increase or decrease in blood pressure, bradycardia, heart failure and shock.

From the digestive system

Often: nausea, vomiting.

General disorders and reactions at the site of administration

Frequency unknown: a random intravascular injection can lead to the onset of ischemia at the injection site, sometimes progressing to tissue necrosis.

Perhaps the development of hypersensitivity reactions (acute allergic reactions with anaphylactic symptoms, such as bronchospasm) in connection with the content of the sulfites in the preparation.

Children

Published studies show that the safety profile of children and adolescents aged 4 to 18 years is comparable to that of adults. Nevertheless, casual injuries of soft tissues are more common in children (up to 16% of children), especially at the age of 4 to 7 years (due to prolonged anesthesia of soft tissues).

Overdose:

Symptoms

symptoms of CNS stimulation: (anxiety, anxiety, confusion, hyperpnoea, tachycardia, increased blood pressure with red face, nausea, vomiting, tremor, convulsive twitching, tonic-clonic convulsions);

Symptoms of CPP depression: (dizziness, hearing loss, loss of ability to speak, loss of consciousness, muscle atony, vasomotor paralysis (weakness, pallor), shortness of breath, death due to respiratory paralysis);

symptoms of cardiovascular depression, bradycardia, arrhythmia, ventricular fibrillation, drop in blood pressure, cyanosis, cardiac arrest.

Treatment: at the first manifestations of symptoms of toxic effects during the administration of the drug, it should 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 always recommended, even if the symptoms of intoxication appear to be mild, to put an intravenous catheter 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 is recommended, and if there are indications for carrying out artificial respiration, an endotracheal intubation and artificial ventilation of the lungs is recommended.

The introduction of central action analeptics is contraindicated.

Muscular twitching and generalized convulsions can be stopped by intravenous injection of barbiturates of short or ultrashort action.It is recommended to inject these drugs slowly, under constant medical supervision (risk of hemodynamic disorders and respiratory depression) and with simultaneous oxygen supply and monitoring of hemodynamic parameters.

Often bradycardia or a sharp drop in blood pressure can be eliminated by simply moving the patient to a horizontal position with raisedlower extremities.

With severe circulatory disturbances and shock, regardless of their cause, the drug should be discontinued and the patient should be placed in a horizontal position with raised lower limbs. It is necessary to provide oxygen supply, intravenous administration of solutions of electrolytes, glucocorticosteroids (250-1000 mg of methylprednisolone), if necessary, plasma substitutes, albumin.

With the development of collapse and increased bradycardia, a slow intravenous injection of a solution of epinephrine (0.0025-0.1 mg) under the control of cardiac rhythm and blood pressure was shown. If it is necessary to administer doses exceeding 0.1 mg, epinephrine should be administered infusion, adjusting the rate of administration under the control of the number of heartbeats and blood pressure.

Severe tachycardias and tachyarrhythmias can be stopped by the administration of antiarrhythmic drugs, with the exception of cardioselective beta-blockers (see section "Contraindications").

Increased blood pressure in patients with arterial hypertension, if necessary, should be reduced with the help of vasodilators.

Interaction:

Joint use of various anesthetics causes summation of effects from the cardiovascular system and the central nervous system.

Contraindicated concurrent use with cardioselective beta-blockers, for example, propranolol, due to the development of hypertensive crisis and severe bradycardia.

Co-administration with tricyclic antidepressants or MAO inhibitors is contraindicated due to the increased effect of vasoconstrictors that increase blood pressure, including adrenomimetics, such as epinephrine.

When injecting Brilokain®-epinephrine forte, patients who receive heparin or acetylsalicylic acid may develop bleeding at the injection site.

Epinephrine can inhibit the release of insulin from the beta cells of the pancreas and reduce the effects of hypoglycemic agents for oral administration.

Halothane can increase the sensitivity of the myocardium to catecholamines and therefore increase the risk of heart rhythm disturbances after injections of the drug Brilokain®-adrenaline forte.

Special instructions:

The drug can not be administered intravenously.

Do not inject into an inflamed area.

To avoid intravascular injection, a two-time aspiration test should be performed prior to administration of the drug.

The injection pressure should correspond to the sensitivity of the tissue. To prevent the introduction of infections (including viral hepatitis), care should be taken to ensure that new sterile syringes and needles are always used when taking a solution from the cartridges. Open cartridges can not be used again for other patients.

Do not use a damaged cartridge for injections.

Patients with diseases of the cardiovascular system (chronic heart failure, atherosclerosis, coronary artery disease, angina pectoris, cardiac arrhythmias, history of myocardial infarction, hypertension), cerebrovascular disorders, the presence of a history of history, chronic bronchitis, emphysema, diabetes,and in the presence of severe anxiety, it is advisable to apply articaine without epinephrine. These conditions should be used with caution. The drug should be used with caution in disorders of blood clotting, severe renal and hepatic insufficiency, simultaneous use of funds for general anesthesia (derivatives of halogenated hydrocarbons), epilepsy in the anamnesis.

1 ml of the drug contains 0.781 mg of sodium. In connection with the content of sulfites in the preparation, it is possible to develop hypersensitivity reactions.

In patients with cholinesterase deficiency, the use of the drug is possible only in case of emergency, since prolongation and excessive strengthening of the drug effect are likely.

When performing preliminary procedures and anesthesia, a patient should be interviewed on the medical history, concomitant therapy, and constant contact with the patient (patient inquiry, clarifying questions that appear as the patient complains of complaints and sensations).

To avoid the occurrence of unwanted reactions, a two-time aspiration test and the choice of the lowest possible dose should be performed.

In case of risk of allergy, 5-10% of the dose is administered.

In the case of the development of severe allergic and anaphylactic reactions for resuscitation, adrenaline, atropine, phosphodiesterase inhibitors (euphyllin, theophylline, aminophylline), antihistamines (suprastin, tavegil), corticosteroids (hydrocortisone, methylprednisolone), cordiamine, epinephrine, Relanium, ammonia and other preparations, as well as resuscitation equipment (especially oxygen source), which provides opportunities for artificial respiration in necessary cases.

Take food can only after the termination of the local anesthesia (restoration of sensitivity).

Parents (guardians) of young children should ensure that the latter do not damage themselves soft tissue when bitten during the period of anesthesia.

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

Local anesthesia with the drug Brilokain®-adrenaline forte, as studies have shown, does not cause any noticeable impairment of the ability to drive vehicles.However, the decision on when a patient after dental surgery can return to driving vehicles and engaging in potentially dangerous activities that require increased concentration and speed of psychomotor reactions should be made by the doctor.

Form release / dosage:

Solution for injection 1: 100000.

Packaging:

By 1,7 or 1,8 ml in liners of glass (cartridges).

For 5, 10 liners are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil or heat-sealable paper. It is allowed to pack in a contour mesh box made of a polyvinylchloride film.

By 1,2, 3, 4, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

20, 25, 30, 35, 40, 50 contour cell packs, together with 5-10 instructions for use, are placed in a cardboard box (packing for hospitals).

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

2 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:For hospitals

Registration number:P N000689 / 01-2001

Date of registration:04.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia

Manufacturer: & nbsp

BRYNTSALOV-A, CJSC Russia

Information update date: & nbsp24.02.2017

Illustrated instructions

Instructions

Brilokain®-adrenaline forte (Brilocaine®-adrenaline forte)