Брилокаин®-адреналин forte

General characteristics. Structure:

Active ingredient: 0,001 g of adrenaline of hydrotartrate ([in terms of 100% substance] in terms of the basis), 4 g of an artikain of a hydrochloride (in terms of 100% substance).

Excipients: sodium pyrosulphite, sodium of chloride, Trilonum of B, 1 M of solution of sodium caustic to pH 5,0, water for injections.

Pharmacological properties:

Pharmacodynamics. The drug Brilokain®-adrenalin used for local infiltration and conduction anesthesia in stomatology is kombinirovanyony drug which part is артикаин (mestnoanesteziruyushchy means of amide type) and Epinephrinum (adrenaline) (a vasoconstrictive sredyostvo) which is added to composition of drug for anesthesia prolongation. Artikain has mestnoanesteziruyushchy effect due to blockade potential - dependent natrium channels in a cellular membrane of neurons that leads to reversible oppression of conductivity of impulses on nerve fibril and the return anesthesia.

Drug renders bystry (stage of latency - from 1 to 3 min.) and strong anesthetic effect and has good fabric tolerance. Duration of anesthesia makes not less than 75 min.

Children. Use of drug for children aged from 4 up to 16 years in a dose of 5 mg/kg of body weight provides sufficient mestnoanesteziruyushchy effect of drug when carrying out mandibular infiltration and maxillary conduction anesthesia. Duration of anesthesia is comparable in all age groups and depends on the entered drug volume.

Pharmacokinetics. Artikain quickly and practically right after introduction is metabolized (puyoty hydrolysis) by nonspecific plasma esterases in fabrics and blood (90%); other 10% of a dose of an artikain are metabolized by microsomal enzymes of a liver. The main metabolite of an artikayoin which is formed at the same time - artikainovy acid - does not possess mestnoanesteziruyushchy активно­стью and system toxicity. That the drug vvedeyoniya allows to carry out repeated.

Concentration of an artikain in blood in the field of tooth sockets after podsliziyosty introduction to thousands of times exceeds concentration of an artikain in a sistemyony blood-groove. Linkng of an artikain with proteins of plasma makes 95%. Artikain is brought through kidneys, mainly, in the form of artikainovy acid. After submucosal introduction the elimination half-life of an artikain (T1/2) makes about 25 min.

At children comparable pharmacokinetic data were obtained.

Artikain gets through a placental barrier, practically not выделяет­ся with breast milk.

Indications to use:

Brilokain®-adrenalin medicine is forte shown for local anesthesia (infiltration and conduction anesthesia) in stomatology at traumatic interventions and in need of the expressed geyomostaz or improvement of visualization of a surgery field:

- dental a mucous membrane operations and on bones, treyobuyushchy creations of conditions of more expressed ischemia,

- operation on a tooth pulp (amputation or an extirpation),

- removal of the broken tooth (osteotomy) or the tooth affected with an apiyokalny periodontal disease

- long surgical interventions,

- transdermal osteosynthesis,

- excision of cysts,

- interventions on a mucous membrane of a gingiva,

- radectomy.

Route of administration and doses:

Drug is intended for use in an oral cavity and can вводить­ся only in fabric where there is no inflammation.

It is impossible to carry out an injection to the inflamed fabrics.

The drug cannot be administered intravenously.

Anesthesia at cuts and suture in the field of the sky on purpose a sozdayoniya of palatal depot requires about 0,1 ml of drug on each injection.

In case of removal of premolar tooths of a mandible in the absence of an inflammation it is possible to do without mandibular anesthesia as the infiltration anesthesia provided with an injection of 1,7 ml of drug on tooth is usually sufficient. If in such way it was not succeeded to reach a desirable effekyot, it is necessary to execute an additional injection of 1-1,7 ml of anesthetic in a podyoslizisty cover in the field of a transitional fold of a mandible from the vestiyobulyarny party. If and in this case the full aneyosteziya did not manage to reach, it is necessary to carry out conduction blockade of a mandibular neyorv.
At surgical interventions the drug Brilokain®-adrenalin dose forte depending on weight and duration of intervention ustanavlivayotsya individually.

At implementation of one medical procedure by the adult it is possible to enter артикаин in a dose to 7 mg on 1 kg of body weight. It is noted that patients well peyorenosit doses to 500 mg (there correspond 12,5 ml of solution for injections).

At children 4 years a dose of drug are more senior select depending on age and the body weight of the child; the dose should not exceed 5 mg of an artikain on 1 kg of body weight.

At patients of advanced age and patients with heavy renal and pechenochyony failure creation of the raised plasma kontsenyotration of an artikain is possible. At these patients drug should be used in the miniyomalny dose necessary for achievement of sufficient depth of anesthesia. In order to avoid accidental hit of drug in blood vessels, before its introduction it is always necessary to carry out two-stage aspiration test with turn of a needle on 90 and 180 ° (see. Special instructions).

Heavy system reactions owing to inadvertent vnutrisosudiyosty introduction can be prevented by slow introduction: at first enter 0,1-0,2 ml of drug, then, 20-30 seconds later slowly enter the drug rest.

Pressure of an injection has to correspond to sensitivity of fabrics.

Features of use:

Pregnancy and lactation. Artikain and Epinephrinum get through a placental barrier.

In view of insufficiency of clinical data drug use vozmozhyono only if the potential advantage of its use for a mayotera justifies potential risk for a fruit. In need of a priyomeneniye of an artikain during pregnancy, it is better to use the drugs which are not containing Epinephrinum or with concentration of Epinephrinum of 0,005 mg/ml. At accidental intravascular introduction Epinephrinum can reduce a krovoyosnabzheny uterus.

In preclinical trials toxic influence on reproductive system, fertility and an embryogenesis at rats and rabbits is not revealed. The Epinephrinum-induced anomalies of fruits at animals observed at introduction it in the doses considerably exceeding the most rekomenduyeyomy as a part of this drug. Influence on fertility at the person at use of an artikain and Epinephrinum in therapeutic doses is not expected.

In the period of a lactation there is no need to interrupt breastfeeding as in breast milk clinically significant kontsenyotration of an artikain are not found. Nursing mothers should decant and delete the first maternal milk after anesthesia with use of an artikain.

The drug cannot be administered intravenously. It is impossible to carry out an injection to the inflamed area. In order to avoid an intravascular injection before administration of drug sleyodut surely to carry out the double aspiration test.

Injection pressure has to correspond to sensitivity of fabric. For prevention of entering of infections (including a viral hepatitis) it is necessary to watch that at a solution intake from cartridges new sterile syringes and needles were always used. Open cartridges cannot be used for other patients again.

It is impossible to use the damaged cartridge for injections. At patients with diseases of cardiovascular system (chronic heart failure, atherosclerosis, pathology of coronary vessels, stenocardia, disturbances of a heart rhythm, a myocardial infarction in the anamnesis, arteyorialny hypertensia), cerebrovascular frustration, existence of an inyosult in the anamnesis, chronic bronchitis, emphysema, a diabetes mellitus, and also in the presence of heavy alarm it is reasonable to apply артикаин without Epinephrinum. These states have to be applied with care. Drug has to be used with care at frustration of a svertyyovaniye of blood, a heavy renal and liver failure, odnovremenyony use of means for the general anesthesia (derivative halogenated hydrocarbons), epilepsy in the anamnesis.

1 ml of drug contains 0,781 mg of sodium. Due to the content in drug of sulfites development of reactions of hypersensitivity is possible.

At patients with deficit of cholinesterase use of drug is possible only in urgent cases as probably prolongation and excessive strengthening of effect of drug.

At implementation of preliminary procedures and anesthesia the patient's poll on the case history accompanying therapy, and also a constant game a step with the patient (inquiry of the patient, the specifying questions which poyoyavlyatsya in process of a statement by the patient of complaints and feelings) is necessary.

For prevention of emergence of undesirable reactions it is necessary to carry out the twofold aspiration test and the choice of minimum possible dose.

In case of risk of developing of an allergy enter 5-10% of a dose of drug.

In case of development of heavy allergic and anaphylactic reactions are necessary for resuscitation activity: adrenaline, atropine, phosphodiesterase inhibitors (an Euphyllinum, theophylline, Aminophyllinum), antihistaminic drugs (Suprastinum, tavegil), corticosteroids (a hydrocortisone, Methylprednisolonum), Cordiaminum, Epinephrinum, Relanium, liquid ammonia and other drugs, and also the resuscitation equipment (in particular an isyotochnik of oxygen) providing opportunities for artificial a dykhayoniya in necessary cases.

It is possible to eat food only after cancellation of a local anesteyoziya (sensitivity recovery).

Parents (trustees) of children of younger age have to watch that poyosledny did not put themselves damage of soft tissues at a sting in the period of an anesthesia deyyostviye.

Influence on ability to manage vehicles and mechanisms. Local anesthesia the drug Brilokain®-adrenalin forte as showed researches, does not cause any noticeable disturbance of ability to manage vehicles. However the decision on when the patient after dental intervention is able to return to driving of an avyototransport and occupations potentially dangerous types of activity, treyobuyushchy the increased concentration of attention and speed of psychomotor reactions, the doctor has to accept.

Side effects:

Frequency of side reactions is determined by the following categories: very often (> 1/10), it is frequent (> 1/100, <1/10), infrequently (> 1/1000, <1/100), is rare (> 1/10000, <1/1000), and is very rare (<1/10000), including a separate soobshcheyoniya, frequency is unknown (it cannot be defined but to the available data).

From immune system. Frequency is unknown: allergic reactions or pseudo-allergic reyoaktion (hypersensitivity). Can be shown in the form of hypostasis and/or a vosyopaleniye in the place of an injection, but also can arise irrespective of the place of an injection and be shown in the form of an erythema, a skin itch, conjunctivitis, a riyonit, a Quincke's disease of the person with hypostasis of an upper lip and/or an under lip and/or hypostasis of a cheek, throat hypostasis with swallowing difficulty, krapivniyoets and difficulties of breath which can reach an acute anaphylaxis.

From a nervous system. Often: paresthesias, a hypesthesia, a headache probably owing to existence in composition of drug of Epinephrinum. Not often: dizziness. Frequency is unknown: dozozavisimy reactions from the central nervyony system (including at excessively high doses or after an accidental intravascular injection): agitation, concern, a stupor, progressiyoruyushchy in certain cases to a loss of consciousness, a lump, breath disturbance (in certain cases up to an apnoea), the muscular tremor and muscular twitchings sometimes progressing to generalized suyodorog. Reactions in an injection site: damage of a nerve (for example, paresis лицево­го nerve), decrease in flavoring feelings.

From organs of sight. Frequency is unknown: passing vision disorders (sight misting, blindness, diplopia).

From cardiovascular system. Infrequently: tachycardia. Frequency is unknown: disturbance of a cordial rhythm, increase or snizheyony arterial pressure, bradycardia, heart failure and shock.

From the alimentary system. Often: nausea, vomiting. The general disturbances and reactions in an injection site. Frequency is unknown: accidental intravascular introduction can lead to developing of ischemia in the place of the injection sometimes progressing to a necrosis of fabrics. Development of reactions of hypersensitivity (acute allergic reactions with anaphylactic symptoms, such as a bronchospasm) in connection with the content in drug of sulfites is possible.

Children. The published researches show that the safety profile at deyoty and teenagers aged from 4 up to 18 years is comparable to that at adults. Nevertheless, accidental injuries of soft tissues are more often observed at children (to 16% of children), especially aged from 4 up to 7 years (in connection with a long aneyosteziya of soft tissues).

Interaction with other medicines:

Combined use of various anesthetics causes summing of efyofekt from cardiovascular system and TsNS.

Contraindicated simultaneous use with cardionon-selective beta adrenoblockers, for example, propranolol, in view of development of gipertonicheyosky crisis and heavy bradycardia.

Combined use with tricyclic antidepressants or ingibiyotor of MAO is contraindicated in view of strengthening of action of the vasoconstrictors raising the ABP including adrenomimetik, such as Epinephrinum.

When carrying out injections of the drug Brilokain®-adrenalin forte to the patsiyenyota receiving heparin or acetylsalicylic acid, perhaps razyovity bleedings in the place of an injection.

Epinephrinum is capable to inhibit release of insulin from beta cells of a pancreas and to reduce effects of hypoglycemic means for intake.

The halothane can increase sensitivity of a myocardium to catecholamines and poyoety to increase risk of development of disturbances of a cordial rhythm after drug Brilokain®-adrenalin injections forte.

Contraindications:

- intravenous administration of drug is contraindicated;

- anesthesia of distal departments of extremities, such as fingers of hands and legs (because of danger of ischemia);

- hypersensitivity to an artikain or to other mestnoanesteziruyushchy means of amide type, except for cases when at hypersensitivity to these means the allergy to an artikain was excluded with по­мощью the corresponding researches conducted with observance of all necessary rules and requirements;

- hypersensitivity to Epinephrinum;

- hypersensitivity to auxiliary components of drug, including to sulfites (including shown in the form of bronchial asthma).

The contraindications relating to an artikain:
- heavy dysfunctions of a sinus node or heavy disturbances of conductivity (such as heavy bradycardia, atrioventricular bloyokada of II and III degrees);

- acute dekompensirovanny heart failure;

- heavy arterial hypotension;

- children's age up to 4 years (lack of clinical experience).

The contraindications relating to Epinephrinum:
- Bouveret's disease, tachyarrhythmia;

- closed-angle glaucoma;

- reception of non-selective beta adrenoblockers, for example, propranolol (risk of development of hypertensive crisis and heavy bradycardia);

- hyperthyroidism;

- pheochromocytoma;

- heavy arterial hypertension;

- the postponed myocardial infarction within 3-6 months, aortocoronary shunting within the last 3 months;

- the accompanying treatment by tricyclic antidepressants or ingiyobitor of monoamine oxidase (MAO) as these drugs can potenyotsirovat cardiovascular effects of Epinephrinum. It can occur up to 14 days after cancellation of MAO inhibitors.

Development of acute allergic reactions with anaphylactic symptoms, such as a bronchospasm at persons with hypersensitivity to sulfites, shown in the form of bronchial asthma is possible.

With care. Stenocardia, atherosclerosis, a postinfarction cardiosclerosis (prescription of an inyofarkt of a myocardium> of 6 months), disturbances of cerebral circulation, a stroke in the anamnesis, other cardiovascular diseases (which are not described in the section "Contraindications"), chronic bronchitis, emphysema of lungs, a diabetes mellitus, insufficiency of cholinesterase (use is possible only in an emergency sluyochaa, as perhaps prolonged and chrezmeryono strong effect of drug), disturbances of coagulability of blood, heavy abnormal liver functions and kidneys, simultaneous use of means for the general anesthesia (derivatives of halogenated hydrocarbons), an epilepyosiya in the anamnesis, heavy alarm.

Overdose:

Symptoms. symptoms of stimulation of TsNS: (concern, alarm, confusion of consciousness, a hyperpnea, tachycardia, increase in arterial pressure with face reddening, nausea, vomiting, a tremor, convulsive twitchings, toniko-clonic spasms); symptoms of oppression of TsPS: (dizziness, a hearing disorder, loss of a spoyosobnost to speak, a loss of consciousness, a muscular atony, vasculomotor пара­лич (weakness, pallor), an asthma, death because of breath paralysis); symptoms of oppression of cardiovascular system, bradycardia, arrhythmia, fibrillation of ventricles, falling of arterial pressure, cyanosis, ostanovyoka of heart.

Treatment: at the first manifestations of symptoms of toxic action in вре­мя administrations of drug, it is necessary to stop its introduction and to transfer a patsiyenyot to horizontal position with the raised lower extremities. It is necessary to provide passability of respiratory tracts and to monitorirovat poyokazatel of a hemodynamics (number of cordial reductions and arterial davleyony). It is recommended always even if symptoms of intoxication seem not heavy, to put an intravenous catheter in order that in case of need, to have an opportunity immediately to carry out an intravenous vveyodeniye of necessary medicines.

At breath disturbances, depending on their weight, the poyodacha of oxygen is recommended, and at emergence of indications to carrying out искусственно­го breath - carrying out an endotracheal intubation and artificial venyotilyation of lungs.

Introduction of analeptics of the central action is contraindicated. Muscular twitchings and generalized spasms can be kupiroyovana intravenous administration of barbiturates of short or ultrashort action. It is recommended to administer these drugs slowly, under constant medical control (risk of hemodynamic frustration and oppression of a dyyokhaniye) and with simultaneous supply of oxygen and monitoring of gemodiyonamichesky indicators.

Often bradycardia or a sharp lowering of arterial pressure can be eliminated at simple convertion of the patient in horizontal position with at the raised lower extremities.

At heavy disturbances of blood circulation and shock, regardless of their reason, administration of drug should be stopped and the patient has to be пе­реведен in horizontal position with raised lower konechnostyayom. It is necessary to provide oxygen supply, intravenous administration of rasyotvor of electrolytes, glucocorticosteroids (250-1000 mg of Methylprednisolonum), if necessary, plasma substitutes, albumine.

At development of a collapse and strengthening of bradycardia slow vnutriyovenny administration of solution of Epinephrinum (0,0025-0,1 mg) under control of a serdechyony rhythm and arterial pressure is shown. In need of introduction of the doses exceeding 0,1 mg, Epinephrinum should be entered infusionally, отрегулиро­вав rate of administering under control of number of cordial reductions and arteriyoalny pressure.

Heavy tachycardias and tachyarrhythmias can be stopped by administration of antiarrhytmic drugs, except for cardionon-selective beta adrenoblockers (see the section "Contraindications").

Increase in arterial pressure at patients with arterial gipertenziyoy if necessary has to decrease by means of vazodilatator.

Storage conditions:

In the place protected from light, at a temperature not above 25 °C. Not to allow freezing. To store in the place, unavailable to children. A period of validity - 2 years. Not to use drug after expiry date, указанно­го on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections 1:100000. On 1,7 or 1,8 ml in inserts glass (cartridges). On 5, 10 inserts place in a blister strip packaging from a film of the polyvinyl chloride and aluminum foil or paper thermowelded. Packaging in a blister strip packaging from a film poliviyonilkhloridny is allowed. On 1, 2, 3, 4, 5 blister strip packagings together with the instruction on a priyomeneniye place in a pack from a cardboard. On 20, 25, 30, 35, 40, 50 blister strip packagings together with 5-10 application instructions place in a box from a cardboard (an upakovyok for hospitals).