Artikain DF - instructions for use, dose, side effects, contraindications

Active substances: articaine hydrochloride 40.0 mg + epinephrine 0.010 mg; Excipients: sodium disulfite 0.5 mg, sodium chloride 1.6 mg, water for injection up to 1 ml.

Description:Transparent colorless solution, odorless.

Pharmacotherapeutic group:Local anesthetic + alpha and beta-adrenomimetic

ATX: & nbsp

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

Pharmacodynamics:

Artikain DF, applied to the local infiltration and conductive anesthesia in dentistry, is a combined preparation, which includes articaine (amine type local anesthetic) and epinephrine (adrenaline) (a vasoconstrictor). Epinephrine is added to the formulation for prolongation of the action of anesthesia. Articaine has a local anesthetic effect due to 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 reversible loss of sensitivity. The drug has a quick effect (latent period - from 1 to 3 minutes). The duration of anesthesia is at least 75 minutes. Due to the low content of epinephrine in the preparation, its effect on the cardiovascular system is not significantly expressed: there is almost no increase in blood pressure and an increase in the heart rate.

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, which allows repeated injections of the drug. The concentrations of articaine in the blood in the area of the alveoli of the tooth after submucosal administration are hundreds of times higher than the concentrations of articaine in the systemic blood stream. The binding of articaine to plasma proteins is approximately 95%.

Articaine is excreted through the kidneys, mainly in the form of articaine acid. After submucosal administration, the elimination half-life is approximately 25 minutes.

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

Indications:

Drug Artikain DF is indicated for local anesthesia (infiltration and conduction anesthesia) in dentistry at traumatic interventions and if necessary expressed hemostasis or improve visualization of the operating field:

- Dental operations on the mucous membrane or bones, requiring the creation of conditions for more severe ischemia;

- Operations on the tooth pulp (amputation or extirpation);

- Removal of a broken tooth (osteotomy) or a tooth afflicted with apical periodontitis;

- Prolonged surgical interventions;

- Transosseous osteosynthesis;

- Excision of cysts;

- Interventions on the gingival mucosa;

- Resection of the apex of the root of the tooth.

Contraindications:

- Hypersensitivity to articaine or other amido type local anesthetic agents,when hypersensitivity to amnestic type local anesthetics, an allergy to articaine has been ruled out with the help of appropriate studies conducted in compliance with all the necessary rules and requirements.

- Hypersensitivity to epinephrine.

- Hypersensitivity to sulfites (in particular, in patients with bronchial asthma and hypersensitivity to sulfites, as possible the development of acute allergic reactions, such as bronchospasm) and any other auxiliary components of the drug.

Contraindications related to articaine

- Severe dysfunction of the sinus node or severe conduction disorders (such as severe bradycardia, atrioventricular blockage of the 2nd or 3rd degree).

- Acute decompensated heart failure.

- Severe arterial hypotension.

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

Contraindications related to epinephrine

Paroxysmal tachycardia, tachyarrhythmia.

- Recently moved (3-6 months ago) myocardial infarction.

- Recently conducted (3 months ago) coronary artery bypass graft.

- Simultaneous reception of non-cardioselective beta-blockers, for example, propranolol (risk of hypertensive crisis and severe bradycardia).

- Closed-angle glaucoma.

- Hyperthyroidism.

- Pheochromocytoma.

- Severe hypertension.

Carefully:

Chronic heart failure, coronary heart disease, angina pectoris, atherosclerosis, myocardial infarction in history, heart rhythm disturbances, arterial hypertension, cerebrovascular disorders, a history of stroke, chronic bronchitis, emphysema, coagulation disorders, intraventricular and atrioventricular heart block, inflammation in the area suspected anesthesia, cholinesterase deficiency (use is only possible in case of emergency, since prolongation and pronounced enhancement may be possible ystviya drug), severe liver function, renal failure, diabetes, old age, severe general condition, weakened patients, expressed excitation history of epilepsy, the simultaneous application with halogenated agents during inhalation anesthesia (see.section "Interaction with other 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.

The decision to use the drug can be taken only if the potential benefit from the use for the mother exceeds the potential risk to the fetus.

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 feeding, since breast milk does not show clinically significant concentrations of articaine and epinephrine.

Fertility

In studies on animals using articaine 40 mg / ml and epinephrine 0.01 mg / ml, there was no effect on fertility in males and females. It is not expected that human fertility will be affected by the use of articaine and epinephrine in therapeutic doses.

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.

In order to avoid accidental ingestion of the drug into blood vessels, an aspirate test (in two steps) should always be performed before it is administered.

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 the remaining dose is slowly introduced in 20-30 seconds preparation. The injection pressure should correspond to the sensitivity of the tissues.

For anesthesia with uncomplicated removal of the upper jaw teeth in the absence of inflammation, it is usually sufficient to create a drug depot in the region of the transitional fold by inserting it into the submucosa from the vestibular side (1.7 ml per tooth). In rare cases, an additional injection of 1 ml to 1.7 ml may be required to achieve complete anesthesia.In most cases this allows you not to carry a painful palatine injection. When several adjacent teeth are removed, the number of injections is usually limited.

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

In the case of removal of premolars of the lower jaw in the absence of inflammation, mandibular anesthesia can be dispensed with, as infiltration anesthesia provided by injection of 1.7 ml per tooth is usually sufficient. If this is not the way to achieve the desired effect, an additional injection of 1 to 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 drug is dosed individually, depending on the severity and duration of the intervention.

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).

For patients of child age (over 4 years), the minimum doses necessary to achieve adequate anesthesia should be used. The dose of the drug 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.

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

Side effects:

Side effects are grouped according to systems and organs according to the dictionary MedDRA and classification of the frequency of development of adverse reactions WHO: very often (≥1 / 10), often (≥1 / 100 to <1/10), infrequently (≥1 / 1000 to <1/100), rarely (≥1 / 10000 to <1/1000), very rarely (<1/10000), the frequency is unknown (the frequency can not be determined from the available data).

Impaired nervous system: often - paresthesia, hypoesthesia, headache, caused, mainly,the presence of epinephrine; infrequently - dizziness; frequency is unknown - dose-dependent reactions from the central nervous system (agitation, nervousness, stupor, sometimes progressing to loss of consciousness, coma, respiratory disorders, sometimes progressing to stopping breathing, muscle tremor, muscle twitching, sometimes progressing to generalized seizures).

Sometimes, if the correct technique of injection is violated with the introduction of a local anesthetic in dental practice, damage to the facial nerve is possible, which can lead to paralysis of the facial nerve.

Disorders from the side of the organ of vision: frequency unknown - visual disorders (blurred vision, mydriasis, blindness, double vision), usually reversible and occurring during or shortly after injection of the local anesthetic.

Disorders from the gastrointestinal tract: often - nausea, vomiting.

Violations from the heart and blood vessels: infrequently - a tachycardia, disturbance of a warm rhythm, rising of arterial pressure; the frequency is unknown - lowering blood pressure, bradycardia, heart failure and shock.

Immune system disorders: frequency unknown - allergic reactions (swelling and inflammation at the injection site), hyperemia of the skin, itching, conjunctivitis, rhinitis, angioedema (swelling of the upper and / or lower lip, cheeks, swelling of the vocal cords with a sensation of "lump in the throat", difficulty swallowing, urticaria, difficulty breathing). Any of these manifestations can progress to anaphylactic shock.

General disorders and disorders at the site of administration: frequency is unknown - with occasional intravascular injection, ischemic zones may occur at the site of administration, up to tissue necrosis.

Children

In the studies conducted, the safety profile in children and adolescents aged 4 to 18 years was comparable to that in adult patients. However, due to prolonged anesthesia of the oral cavity, children suffered more frequent soft tissue damage (in 16% of children), especially at the age of 3 to 7 years.

Overdose:

Symptoms: The most common symptoms are the reactions of the cardiovascular system and nervous system, nausea, motor anxiety, blurred consciousness during injection, breathing disorders, muscle twitching, convulsions, shock.

Treatment: Treatment is symptomatic. When the first signs of an overdose or side effects, for example, nausea, motor anxiety, clouding of consciousness during the injection, it should be interrupted, the patient moved to a horizontal position, cleanse the airways, monitor the pulse and blood pressure. It is recommended, even if the symptoms seem not too pronounced, to provide intravenous access. If breathing is disturbed, depending on the degree of severity, give oxygen, in some cases, carry out artificial respiration. Central analeptics are contraindicated. Muscle twitching or generalized seizures are removed intravenous injection barbiturates of short or ultrashort action. The drop in blood pressure, tachycardia, or bradycardia is often eliminated when the patient is moved to a horizontal position. With severe circulatory disturbances and shock of any genesis after stopping the injection, emergency measures are shown: ensuring airway patency (oxygen insufflation), intravenous fluid infusion (electrolyte solution), glucocorticosteroids.In addition, it is possible to introduce plasma substitutes, albumin.

With a threatening violation of blood circulation and increasing bradycardia, from 0.25 ml to 1 ml of epinephrine is injected. Intravenous injection of epinephrine should be performed slowly under the control of pulse and blood pressure.

A single dose of intravenous injection of epinephrine should not exceed 0.1 mg, further if necessary epinephrine can be administered drip (the infusion rate through the dropper is adjusted depending on the pulse rate and blood pressure). Severe forms of tachycardia and tachyarrhythmias can be eliminated by the use of antiarrhythmic drugs, but non-selective beta-blockers should not be used. Supply of oxygen and control of blood circulation are necessary in any case. With an increase in blood pressure in patients with arterial hypertension, it is necessary, if necessary, to use peripheral vasodilators.

Interaction:

Simultaneous use is contraindicated

When used simultaneously with non-cardioselective beta-blockers, for example, propranolol, it is possible to develop a hypertensive crisis and severe bradycardia.

Simultaneous application is possible with caution

The action of vasoconstrictors that increase blood pressure, for example, epinephrine, can be amplified tricyclic antidepressants or monoamine oxidase inhibitors.

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

When using Artikain DF in patients taking heparin or acetylsalicylic acid, possibly development of bleeding at the injection site.

When used simultaneously with cholinesterase inhibitors possibly slowing the metabolism of local anesthetics, as a result of which prolongation and pronounced increase in the action of articaine are possible. Epinephrine can inhibit the release of insulin from the beta cells of the pancreas and reduce the effects hypoglycemic agents for oral administration.

Some means for inhalation anesthesia, for example, halothane, can increase the sensitivity of the myocardium to catecholamines and increase the risk of cardiac disordersrhythm after injections of Artikain DF.

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

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

The drug contains sodium disulfite, therefore its use is contraindicated in patients with bronchial asthma and hypersensitivity to sulfites, since it is possible to develop acute allergic reactions such as bronchospasm (see section "Contraindications")

To avoid the development of adverse reactions, it is necessary to apply the minimum effective doses of the preparation and, before the administration of the drug, to carry out a two-stage aspiration test (see the section "Dosing and Administration").

When using the drug, unintentional injury to the lips, cheeks, mucous membrane and tongue, especially in children, is possible, due to the reduction sensitivity. The patient should be warned that eating is possible only after the local anesthesia has ceased and sensitivity is restored.

The drug is intended for use in dentistry. The use of distal limbs for anesthesia is unacceptable due to the risk of developing ischemia due to the content of epinephrine in the preparation.

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

The possibility of the patient's admission to the management of vehicles and mechanisms is determined by the doctor.

Form release / dosage:

Solution for injection 40 mg + 0.010 mg / ml.

Packaging:

1.8 ml of solution in a colorless glass cartridge. The bottom of the cartridge is sealed with a rubber piston, on the outside of which there may be convex symbols. The neck of the cartridge is sealed with a gray rubber stopper and an aluminum cap.The cartridge is glued with a transparent self-adhesive label with a marking.

For 10 cartridges in a blister of aluminum foil and PVC film.

For 5 blisters together with instructions for use in a cardboard pack with the control of the first opening.

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001074

Date of registration:28.10.2011 / 24.01.2017

Expiration Date:Unlimited

The owner of the registration certificate:HIRATRADE, JV LLC HIRATRADE, JV LLC Russia

Manufacturer: & nbsp

INDUSTRIA E COMERCIO DFL S.A. Brazil

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Artikain DF (Articaine DF)