Articaine with adrenaline - instructions for use, dose, side effects, contraindications

1 ml of the solution contains: active ingredients: articaine hydrochloride 40 mg and epinephrine hydrotartrate 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 disulphite - 0.50 mg, sodium chloride - 1.00 mg, water for injection up to 1 ml.

Description:

Transparent colorless or with a yellowish tinge solution.

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

ATX: & nbsp

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

Pharmacodynamics:Articaine with adrenaline, used for infiltration and conductive anesthesia in dentistry, 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.

Articaine with adrenaline has a fast (latent period - from 1 to 3 min) and a strong anesthetic effect and has good tissue tolerance. The duration of effective anesthesia is at least 45 minutes.

Children

Published studies have shown that in children aged 3.5 to 16 years, the use of the drug at a dose of 5 mg of articaine per kg of body weight provided sufficient local anesthetic effect with mandibular infiltration or maxillary conduction anesthesia. The duration of anesthesia was comparable in all age groups and depended on the amount of drug administered.

Pharmacokinetics:

The connection of articaine with plasma proteins is approximately 95%. With submucosal introduction into the oral cavity, the half-life of articaine is 25.3 ± 3.3 min.

Articaine quickly and practically immediately after administration is metabolized by hydrolysis with nonspecific plasma esterases of blood and tissues (90%). Up to 10% of articaine is metabolized in the liver.The resulting main metabolite articaine - articaine acid - does not have local anesthetic activity and systemic toxicity, which allows repeated injections of the drug. Articaine is excreted by the kidneys, mainly in the form of articaine acid.

In children, the overall effect on infiltration anesthesia from the vestibular side is comparable to that in adults, but the maximum concentration of articaine in the blood plasma is reached more quickly.

Indications:

Medicinal preparation Articaine with adrenaline is indicated for local anesthesia (infiltration and conduction anesthesia) in dentistry.

Planned interventions, such as uncomplicated removal of one or more teeth, carious cavity treatment, teeth grinding before prosthetics.

Contraindications:

Hypersensitivity to articaine or other amine type local anesthetic agents, epinephrine, sulfites (in particular, in patients suffering from bronchial asthma with increased susceptibility to sulfites, since acute allergic reactions with symptoms of anaphylactic shock such as bronchospasm are possible), or to anyone another of the auxiliary components of the drug.

Contraindications due to the presence of articaine in the formulation

- severe dysfunction of the sinus node or severe conduction disorders (eg, severe bradycardia, atrioventricular blockade of degree II or III);

- acute decompensated heart failure;

- severe form of arterial hypotension.

Contraindications due to the presence of epinephrine in the formulation

- angle-closure glaucoma;

- hyperthyroidism;

- paroxysmal tachycardia, tachyarrhythmia;

- recently suffered myocardial infarction (up to 6 months);

- recently transferred coronary artery bypass graft (up to 3 months);

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

- pheochromocytoma;

- severe form of hypertension.

Carefully:- In patients with chronic heart failure, ischemic heart disease, angina pectoris, atherosclerosis, myocardial infarction in history, heart rhythm disorders, arterial hypertension;

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

- in patients with chronic bronchitis, emphysema;

- in patients with diabetes mellitus (potential risk of changes in blood glucose concentration);

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

- in patients with coagulation disorders;

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

- in patients with marked agitation;

- in patients with epilepsy in the anamnesis;

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

Pregnancy and lactation:

Pregnancy

Articaine and epinephrine penetrate through the placental barrier.

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.

Due to the lack of clinical data, the decision to use the drug by a dentist can be made only if the potential benefit from using it for the mother justifies the potential risk to the fetus.If articaine is needed during pregnancy, it is better to use medicines 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.

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 and epinephrine.

Fertility

Experimental studies of articaine 40 mg / ml + epinephrine 0.01 mg / ml in animals showed no effect on fertility in males and females. When used in therapeutic doses, the negative effect of the drug on human fertility is absent.

Dosing and Administration:The drug can be injected only into non-inflamed tissues.

The drug is not allowed to be administered intravenously!

The drug is intended for use in the oral cavity.

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 °.

The main systemic reactions that can develop as a result of accidental intravascular injection of the drug can be avoided by observing the technique of injection: after the aspiration test, slowly inject 0.1-0.2 ml of the drug, then slowly inject, not earlier than 20-30 seconds later the rest of the drug. The injection pressure should correspond to the sensitivity of the tissues.

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

Open cartridges can not be reused for other patients (risk of contracting hepatitis)!

Do not use damaged cartridges.

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

Dosing regimen

For anesthesia with uncomplicated removal of the upper jaw teeth in the absence of inflammation, it is usually sufficient to create a drug depot Articaine with adrenaline in the region of the transitional fold by introducing it into the submucosa from the vestibular side (1.7 ml per tooth).In some cases, in order to achieve complete anesthesia, an additional administration of 1 ml to 1.7 ml may be required. In most cases this allows you not to carry out a painful palatine injection.

For anesthesia in the incision and suturing in the palate with the goal of creating a palatine depot, about 0.1 ml of the drug per injection is needed.

When several adjacent teeth are removed, the number of injections is usually limited.

In the case of removal of premolars of the lower jaw in the absence of inflammation, as a rule, it is sufficient to administer 1.7 ml of the drug per tooth. If this is not the way 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.

When treating cavities and grinding teeth for crowns, with the exception of the lower molars, depending on the volume and duration of treatment, the administration of the preparation Articaine with adrenaline in the region of the transitional fold from the vestibular side in a dose of 0.5-1.7 ml per tooth.

When performing one treatment procedure, adults can administer up to 7 mg of articaine 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).

Elderly patients and patients with severe renal and hepatic impairment

In elderly patients and all patients with severe renal and hepatic insufficiency, it is possible to create increased plasma concentrations articaine. For these patients, the minimum doses needed to achieve sufficient depth of anesthesia should be used.

Children

For children, the minimum doses needed to achieve adequate anesthesia should be used. Dose of the drug Articaine with adrenaline is selected depending on the age and body weight of the child, but it should not exceed 7 mg of articaine per 1 kg of body weight (0.175 ml / kg). The use of the drug in children younger than 1 year has not been studied.

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).

Immune system disorders

Frequency unknown

Allergic or allergic reactions. They can be expressed as edema and / or inflammation at the injection site, but can also occur regardless of the injection site and manifest as redness, itchy, conjunctivitis, rhinitis, angioedema, edema of the upper and / or lower lip, cheeks, swelling of the larynx with a sensation of "lump in the throat" and difficulty swallowing, urticaria and difficulty breathing, which can reach anaphylactic shock.

From the central 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 (including at excessively high doses or after a random intravascular injection): a sense of anxiety, nervousness, stupor, confusion, even loss of consciousness, coma, respiratory depression, even respiratory arrest, muscle tremor and twitching of the muscles, up to generalized seizures;

- if the correct technique of drug administration is violated or because of anatomical features in the area of injection, damage to the facial nerve is possible, which can lead to paralysis of the facial nerve. Perhaps a decrease in taste.

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.

Violations from the heart and blood vessels

Infrequently

Tachycardia.

Frequency unknown

Violations of the heart rate, increased blood pressure, hypotension, bradycardia, heart failure and shock.

Disorders from the gastrointestinal tract

Often

Nausea, vomiting.

General disorders and disorders at the site of administration

Frequency unknown

In some cases, with occasional intravascular injection, ischemic zones may occur at the site of administration, up to the necrosis of the tissues (see section "Method of administration and dose").

Children

In published papers, the safety profile of children and adolescents aged 4 to 18 years is similar to that of adults. However, the accidental injury of soft tissues of the oral cavity are more common in children (up to 16% of children), especially between the ages of 3 to 7 years (due to the longer soft tissue anesthesia).There is evidence of a retrospective study of children aged 1 to 4 years, during which dental interventions were performed using drugs containing articaine 40 mg / ml + epinephrine 0,005 mg / ml in a dose up to 4,2 ml. According to the results of this study, there were no reported side effects.

Overdose:Overdose Symptoms

From the central nervous system

Excitation of the central nervous system: a sense of 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

Bradycardia, arrhythmia, fibrillation of the ventricles, a drop in blood pressure, cyanosis, cardiac arrest.

Treatment

At the first signs of intoxication or side effects of the drug,such as dizziness, motor agitation 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 always recommended, even if the symptoms of intoxication appear to be mild, to free access to the veins in order to be able to immediately carry out the intravenous administration of necessary medications.

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.

Muscular twitching and generalized convulsions can be stopped by intravenous injection of a high-speed drug that relieves muscular spasm (for example, diazepam, suxamethonium chloride). It is also recommended to carry out artificial ventilation (oxygen supply).

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

In severe circulatory disorders 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. There should be oxygen supply, intravenous electrolyte solutions, glucocorticosteroids (for example, 250-1000 mg of prednisolone or an equivalent amount of its derivative, for example, methylprednisolone), replacement infusion therapy (if necessary, additionally, plasma substitute, human albumin).

With the development of 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 a 0.01% solution of epinephrine (1: 10,000), a slow intravenous injection of 0.25-1 ml (0.025-0.1 mg epinephrine), controlling the heart rate and blood pressure (carefully: possible violations of the heart rhythm!).

Do not exceed a single dose for intravenous administration of 1 ml (0.1 mg epinephrine).

With the subsequent need 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.

Strong tachycardia and tachyarrhythmia can be treated with antiarrhythmic drugs, excluding non-selective beta-blockers, such as, for example, propranolol. In such cases, oxygen supply and control of the circulatory system is necessary. Increase in blood pressure in patients with hypertension, if necessary, is removed 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-adrenoblockers, for example, propranolol

Risk of developing a hypertensive crisis and severe bradycardia.

Interaction, which should be taken into account

With tricyclic antidepressants or monoamine oxidase (MAO) inhibitors, The action of vasoconstrictors (adrenomimetics), increasing blood pressure, for example, epinephrine, may be enhanced by tricyclic antidepressants or MAO inhibitors. Similar observations were described for concentrations of norepinephrine 1: 25,000 and epinephrine 1: 80,000 when used as vasoconstrictors. Although the concentration of epinephrine in the preparation Articaine with adrenaline significantly lower (1: 200000), nevertheless, the possibility of increasing the hypertensive effect of epinephrine should be considered.

With drugs that depress the central nervous system Local anesthetics enhance the effect of drugs that depress the central nervous system. Narcotic analgesics strengthen the effect of local anesthetics, but increase the risk of respiratory depression.

With anticoagulants and other drugs that reduce blood coagulability

When injecting the drug Articaine with adrenaline patients receiving, for example, heparin or acetylsalicylic acid, may develop bleeding at the injection site.

With cholinesterase inhibitors

Cholinesterase inhibitors reduce the metabolism of topical anesthetics, as a result of which prolongation and a pronounced increase in the action of articaine are possible.

With hypoglycemic agents for oral administration

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

FROM some means for inhalation anesthesin (halothane)

Halothane can increase the sensitivity of the myocardium to catecholamines and increase the risk of heart rhythm disturbances after injection of the drug Articaine with adrenaline.

With disinfecting solutions containing heavy metals

When treating the site of injection of a local anesthetic with disinfecting solutions containing heavy metals, the risk of developing local reactions - edema, soreness - increases.

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, the drug can be used in patients with a deficiency of cholinesterase, since prolongation is possible and, under certain circumstances, an increase in its effect.

With extreme caution Articaine with adrenaline should be used in patients with impaired blood clotting, severe impairment of kidney or liver function, when combined with halogenated inhaled drugs (see section "Interaction with other drugs"), epilepsy in the anamnesis.

Patients with diseases of the cardiovascular system (chronic heart failure, coronary heart disease, angina pectoris, myocardial infarction in history, heart rhythm disturbances, arterial hypertension), atherosclerosis, cerebral vascular insufficiency, anamnesis history, chronic bronchitis, pulmonary emphysema, diabetes mellitus, severe forms of anxious neurosis, it is advisable to use drugs that do not contain epinephrine or with an epinephrine concentration of 0.005 mg / ml.

Do not inject into an inflamed area.

Before using the drug, you should know about the patient's history and ongoing concomitant drug therapy. The doctor should maintain a verbal contact with the patient and, in case of a risk of allergy, introduce a test dose of 5 or 10% of the estimated dose.

To avoid side effects, the following conditions must be observed:

- choose the minimum doses necessary to achieve sufficient depth of anesthesia;

- Before injection, it is necessary to perform an aspirate test in two planes (to avoid accidental intravascular injection).

It is not recommended to eat until the local anesthesia ceases (restores sensitivity).

It should be noted that 1 ml of the drug solution contains less than 1 mmol (23 mg) of sodium.

The drug is intended for use in dentistry. The use of distal limbs for anesthesia is unacceptable (the risk of developing ischemia due to the presence of epinephrine in the formulation).

Children

Parents (guardians) of young children should ensure that the latter do not damage themselves soft tissue when bitten by teeth (biting) because of a long decrease in the sensitivity of tissues due to the actionpreparation.

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

Application of the drug Articaine with adrenaline does not cause any noticeable deviation from the usual ability to drive vehicles. However, it is up to the doctor to decide when the patient, after dental surgery, can return to driving and other potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection (40 mg + 0.005 mg) / ml.

Packaging:

According to 1.7 ml or 1.8 ml of the preparation in cartridges of transparent colorless glass 1 or 2 of hydrolytic class, sealed on one side by elastomeric material plungers, and on the other hand combined caps for dental cartridges for local anesthesia consisting of an elastomeric disk material and aluminum anodized cap. For 10 cartridges in contour plastic packaging (pallet) or in the insert for fixing cartridges from cardboard. 1, 5, 10 contour plastic packages (pallets) or inserts with cartridges together with instructions for use in a pack of cardboard.On a pack of cartridges, two protective labels with the logo of the company are glued (control of the first opening).

1ml or 2ml of the drug in ampoules of clear, colorless glass: 1 or 2 hydrolytic class or neutral glass grade HC-3. 5 ampoules in contour plastic packaging (pallet). 1.2 contour plastic packages

(pallets) together with an instruction for use and a knife ampoule or scarifier ampullum in a pack of cardboard. 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.

Packing for hospitals

For 20, 50 contour plastic packages (pallets) with ampoules together with an equal number of instructions for use in a cardboard box.

Storage conditions:

Ampoules. In the dark place at a temperature of no higher than 25 ° C, do not allow freezing.

Cartridges. In the dark place at a temperature of no higher than 30 ° C, do not allow freezing. Keep out of the reach of children.

Shelf life:

Cartridges - 2,5 years.

Ampoules - 3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-001943

Date of registration:20.12.2012 / 06.02.2017

Expiration Date:Unlimited

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

Manufacturer: & nbsp

ARMAVIRSK BIOLOGICAL FACTORY, FSUE Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Articaine with adrenaline (Articaine with adrenaline)