Artikain with Epinephrinum

General characteristics. Structure:

Active ingredients: 80 mg of an artikain of a hydrochloride, 0,012 mg of Epinephrinum in 1 ml of solution.

Excipients: dinatrium эдетат, sodium chloride, Acidum hydrochloricum, water for injections.

Pharmacological properties:

Pharmacodynamics. Artikain-Borimed with Epinephrinum – the combined medicine for a conduction and infiltration anesthesia in stomatology. Being its part артикаин - local anesthetic of amide type of thiafoehn group. Effect of medicine begins quickly - in 1 3 min. Duration of anesthesia makes not less than 45 min. Medicine provides the reliable anesthetizing effect. The wound repair proceeds without complications that is caused by good fabric tolerance and the minimum vasoconstrictive action.

Owing to the low maintenance of Epinephrinum (adrenaline) in drug its influence on cardiovascular system is expressed a little: almost increase in arterial pressure and increase in heart rate is not noted. Medicine possesses a hypotoxicity.

Pharmacokinetics. Artikain at submucosal introduction to oral cavities has high diffusion capacity. Linkng with proteins of plasma makes 95%. The elimination half-life makes 25,3 min. Drug in the minimum degree gets through a placental barrier, is practically not emitted with breast milk. It is brought out of an organism preferential through kidneys.

Indications to use:

Standard operations, such as, uncomplicated single or multiple extractions, preparation of a pulp cavity, preparation of tooth under a crown.

Route of administration and doses:

At an uncomplicated exodontia of an upper jaw in the absence of an inflammation usually enter in submucosal in the field of a transitional fold from the vestibular party of 1,7 ml of medicine (on each tooth). In rare instances additional introduction from 1 ml to 1,7 ml for achievement of full anesthesia is required. In most cases it is possible to refuse a painful palatal injection. Anesthesia at palatal cuts and suture for the purpose of creation of palatal depot requires about 0,1 ml of anesthetic on an injection. During removal several the quantity of injections usually manages to be limited to a number of the located teeth.

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 medicine on tooth, as a rule, is sufficient.

If in such way it was not succeeded to reach desirable effect, it is necessary to execute an additional injection of 1-1,7 ml of anesthetic in submucosal in the field of a transitional fold of a mandible from the vestibular party. If and in this case it was not succeeded to reach full anesthesia, it is necessary to carry out blockade of a mandibular nerve.

At surgical interventions Artikain with Epinephrinum depending on weight and duration of intervention is dosed individually. At implementation of one medical procedure by the adult it is possible to enter to 7 mg of an artikain on 1 kg of body weight. It is noted that patients well transferred doses to 500 mg (there correspond 12,5 ml of solution for injections).

Children. At children the dose of drug is selected depending on age and the body weight of the child, but it should not exceed 7 mg of an artikain on 1 kg of body weight.

Patients of advanced age and patients with heavy dysfunction of a liver and kidneys

Increase in plasma levels of an artikain at patients of advanced age and at patients with heavy disturbance of functions of kidneys and a liver is possible. For such patients it is especially important to use the minimum doses necessary for rather deep anesthesia.

Artikain with Epinephrinum is intended for introduction to an oral cavity.

For prevention of infections it is necessary to watch that at each intake of solution from bottles or ampoules new sterile syringes and needles were always used.

It is impossible to make an injection to the inflamed area!

Features of use:

In rare instances, in particular at patients with bronchial asthma, medicine can cause hypersensitivity reactions. These reactions can clinically be shown by vomiting, a diarrhea, a bad attack of asthma, disorders of consciousness or shock.

Medicine should be applied with care at:

- stenocardias;

- atherosclerosis;

- disturbances of coagulability of blood;

- heavy renal failures or liver.

It is impossible to carry out injections in a zone of an inflammation (infection) since medicine absorption amplifies that leads to reduction of its efficiency.

At patients with cardiovascular diseases (for example, with heart failure, coronary heart disease, stenocardia, a myocardial infarction in the anamnesis, heart arrhythmia, a hypertension), disturbances of cerebral circulation, had a stroke, with chronic bronchitis, emphysema of lungs, a diabetes mellitus or heavy alarming frustration, it is more reasonable to use drugs with the smallest maintenance of Epinephrinum.

For prevention of emergence of side effects it is necessary to consider the following:

- it is necessary to choose the best dose;

- before an injection it is necessary to carry out aspiration test in two steps (for the purpose of avoiding of intravascular administration of drug);

- it is recommended that the patient ate food only after a complete recovery of sensitivity.

Children. At medicine use children need to adjust amount of the administered drug individually depending on age and the body weight of the child. It is impossible to exceed the maximum dose which makes 7 mg of an artikain on 1 kg of body weight.

Ability to influence speed of response at control of motor transport or other mechanisms. Only the stomatologist has to decide since what time after administration of medicine the patient can manage the vehicle again or work with mechanisms. The fear is connected with expectation of dental manipulation and the stress by which it is followed can be led to ability change to work effectively, however the corresponding researches showed that the HP local anesthesia does not cause any noticeable deterioration in ability to manage the vehicle. At sensitive patients emergence of undesirable reactions from the central nervous system is possible (see the section "Side reactions").

Use during pregnancy and in the period of a lactation. In view of insufficiency of clinical data, the decision on purpose of drug can be made by the doctor only after careful studying of a ratio advantage risk.

In need of use of an artikain during pregnancy, use of medicine in view of the smaller maintenance of Epinephrinum is more preferable.

Artikain passes through a placental barrier in smaller quantity, than other local anesthetics. Due to very bystry falling of level of an artikain and its bystry removal from an organism it comes to maternal milk in clinically insignificant quantities. Therefore it is not required to interrupt feeding with a breast.

Side effects:

Medicine is usually well transferred by patients. However development of by-effects is possible.

Apply the following categories to classification of frequency of emergence of side effects: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); seldom (> 1/10000, <1/1000); very seldom (<1/10000); it is unknown (frequency cannot be calculated according to the available data).

From the central nervous system:

- depending on a dosage there can come disturbances of activity of the central nervous system: opacification of consciousness up to its loss, disturbance of breath to the stop menacing for life, a muscular tremor and twitchings of muscles up to generalized spasms;

- dizziness, paresthesia, hypesthesia;

- the temporary vision disorder (an illegibility of visual perception, a blindness, doubling in eyes) arising in time or through short time after an injection of mestnoanesteziruyushchy means;

- the frequent headache arising, mainly, owing to existence of Epinephrinum as a part of drug; at the wrong introduction of a mestnoanesteziruyushchy stredstvo in dental practice injury of a nerve, in particular, front which can lead to development of paralysis of a facial nerve is sometimes possible.

From digestive tract:

- nausea, vomiting.

From cardiovascular system:

- lowering of arterial pressure, bradycardia, heart failure and shock.

- other side effects caused by Epinephrinum - tachycardia, disturbances of a cordial rhythm, increase in arterial pressure – at small concentration 1:200000 (0,5 mg / 100 ml) and 1: 100 000 (1,0 mg / 100 ml) meet seldom.

From immune system:

- allergic reactions can be shown: in the form of hypostasis or an inflammation in the place of an injection, dermahemia, an itch, conjunctivitis, rhinitis, puffiness of the person (Quincke's edema) with swelling of an upper and/or under lip, hypostasis of phonatory bands with feeling of a lump in a throat and the complicated swallowing, small tortoiseshells, breath difficulties. All these manifestations can develop into an acute anaphylaxis.

From behind the content of sodium of disulphite in some cases patients with bronchial asthma can have hypersensitivity reactions which are shown in the form of vomiting, a diarrhea, hurried breathing, a bad attack of asthma, disturbances of consciousness or shock.

The general disturbances and undesirable reactions in an injection site: occasionally at an accidental intravascular injection ischemia zones up to a necrosis of fabrics in the place of an injection can appear (see also "Special instructions").

Interaction with other medicines:

Combinations of various anesthetics have the additive effect and exert more expressed impact on cardiovascular system and TsNS.

Hypertensive effects of vasoconstrictors of sympathomimetic type (for example, Epinephrinum) can be strengthened by tricyclic antidepressants or MAO inhibitors. Therefore such combinations are contraindicated (see the section "Contraindications").

Epinephrinum can block insulin release by a pancreas owing to what effect of peroral antidiabetic drugs decreases.

Some inhalation narcotic drugs, such as halothane, can increase sensitivity of a myocardium to catecholamines, causing arrhythmia after administration of medicine.

It is necessary to remember that at the patients receiving treatment by antitrombotichesky means (for example, heparin, acetylsalicylic acid), the accidental puncture of a vessel during local anesthesia can cause serious bleeding. Such patients have an increased tendency to bleedings.

About simultaneous use of non-selective beta-blockers see the section "Contraindications".

Contraindications:

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

Hypersensitivity to Epinephrinum, sulfites or to any other component of drug.

Heavy dysfunctions of a sinus node or heavy disturbances of conductivity (such, as: the expressed bradycardia, an atrioventricular block 2-3 degrees).

Acute noncompensated heart failure, sharply expressed arterial hypotension.

As drug contains Epinephrinum, it is contraindicated in the following cases:

- at a Bouveret's disease and other disturbances of a cordial rhythm, and also at a closed-angle form of glaucoma;

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

- the patient with a hyperthyroidism;

- the patient with a pheochromocytoma;

- the patient with heavy arterial hypertension;

- at anesthesia of final nervous branches.

It is not necessary to apply at anemia (including V-12 of scarce anemia), methemoglobinemias, hypoxias.

It is impossible to use at patients with bronchial asthma at hypersensitivity to sulfites.

Contraindicated intravenous administration of medicine.

With care. Deficit of cholinesterase, a renal failure, bronchial asthma, a diabetes mellitus, a hyperthyroidism, arterial hypertension, children's age (up to 4 years - efficiency and safety are not defined). When carrying out paracerebral blockade - a preeclampsia, bleedings in the last trimester, an amnionitis.

Overdose:

Symptoms: signs of excitement of TsNS: concern, alarm, confusion of consciousness, hurried breathing, tachycardia, increase in arterial pressure which is followed by face reddening, nausea, vomiting, a tremor, involuntary muscular contractions, toniko-clonic spasms.

Signs of oppression of TsNS: dizziness, decrease in hearing, loss of ability to speak, a loss of consciousness, a muscular atony, vasculomotor paralysis (weakness, pallor of integuments), an asthma, a lethal outcome owing to paralysis of a respiratory center.

Signs of oppression of cardiovascular activity: bradycardia, arrhythmia, fibrillation of ventricles, lowering of arterial pressure, cyanosis, cardiac standstill.

Urgent measures and antidotes: at emergence of the first signs of side reaction or toxic action (for example, dizziness, motive concern or a stupor) it is necessary to stop an injection and to transfer the patient to horizontal position. It is necessary to provide passability of respiratory tracts of the patient, to control pulse and arterial pressure.

Even in that case when symptoms of intoxication do not seem heavy, it is recommended to establish a catheter for ensuring immediate intravenous access if it is required.

At breath disturbances, depending on weight of a state, it is recommended to apply oxygen, and also, in case of need, to apply an artificial respiration. If necessary carry out a trachea intubation in combination with controlled ventilation of the lungs.

Involuntary muscular contractions or generalized spasms stop introduction of anticonvulsants of short action (for example, succinylcholine of chloride, diazepam). Also it is recommended to apply an artificial respiration (oxygen).

Decrease in the ABP, tachycardia or bradycardia can be eliminated by transfer of the patient in horizontal position or in situation at which legs are raised slightly above the head.

At heavy disturbances of blood circulation, and also at shock, irrespective of the reason, after the termination of an injection it is necessary to take the following urgent measures:

- to transfer the patient to horizontal position or situation with the raised legs, and also to provide passability of respiratory tracts (oxygen insufflation);

- to begin intravenous infusional administration of the balanced electrolytic solution;

- intravenous administration of glucocorticoids (for example, 250-1000 mg of Prednisolonum or corresponding quantity of its derivative, for example, Methylprednisolonum);

- to recover the volume of the circulating blood (in addition, if necessary, apply plasma substitutes, albumine of the person).

In case of threat of a circulator collapse and the accruing bradycardia carry out an immediate intravenous injection of Epinephrinum (adrenaline). For this purpose it is necessary to part 1 ml of solution of Epinephrinum 1:1000 to 10 ml (instead solution of Epinephrinum 1:10000 can be applied) and to slowly enter 0,25-1 ml of this solution (= 0,025-0,1 mg of adrenaline) under control of pulse rate and arterial pressure (attention: developing of arrhythmia of heart is possible). Not to enter more than 1 ml of this solution (0,1 mg of adrenaline) during one injection. If this quantity of Epinephrinum is not enough, then it is recommended to be added to infusion solution (speed of infusion is adjusted with pulse rate and arterial pressure).

Severe forms of tachycardia and tachyarrhythmia can be liquidated by use of antiarrhytmic drugs (but not non-selective beta-blockers, for example, of a propanolol) (see the section "Contraindications"). In such cases use of oxygen and control of blood circulation is necessary.

At increase in arterial pressure at patients with arterial hypertension if necessary it is necessary to apply peripheral vazodilatator.

Storage conditions:

In the place protected from light, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

In ampoules of 2 ml in packaging No. 10, No. 10 x 1.