Local anesthetic articaine. Medicinal reference book geotar

Farm group:

Release form: Liquid dosage forms. Injection.

General characteristics. Compound:

Pharmacological properties:

Indications for use:

Dosage and administration:

Application Features:

Side effects:

Interaction with other drugs:

Contraindications:

Storage conditions:

In a dry, dark place at a temperature not exceeding 25 ° C. Keep out of the reach of children Shelf life 5 years. Do not use after the expiry date stated on the packaging

Leave conditions:

On prescription

Package:

Solution for injections 40 mg/ml. 2 ml in neutral glass ampoules. 5 ampoules are placed in a blister pack. 2 blister packs are placed in a cardboard box. Each pack or box contains instructions for use, an ampoule knife or an ampoule scarifier. In the case of using ampoules with notches, break rings or break points, an ampoule knife or an ampoule scarifier is not inserted.

) - dentist-therapist, dentist-periodontist. Specializes in: endodontics, aesthetic and functional restoration, professional hygiene and periodontics.

Currently, in dental practice there is a huge number of new methods and drugs used for local anesthesia. drug of choice used for local anesthesia, in dentistry is Artikain.

Articaine was first synthesized in 1969, and since 1976 it has been widely used. Now medications based on Articaine are produced by many pharmaceutical companies.

Basic requirements for local anesthetics:

• significant penetration depth of the agent;
• long duration of action;
• high degree of security.

These parameters are affected by:

• the activity of the anesthetic used;
• peripheral vascular tone.

The drug Articaine does not contain a particularly preservative - paraben, which is most often the cause of hypersensitivity reactions. Contains a minimal amount of the antioxidant adrenaline (metabisulphite).

The stability of the local anesthetic is achieved through the high quality of the glass, the rubber components of the cartridge, and the high activity of the active substance.

It is insoluble in an aqueous medium, so it is used in the form of a salt, which has water solubility. For the manifestation of the main effects, its destruction in the tissues with the formation of fat-soluble substances that are able to penetrate the lipid sheath of the nerve ending is required. Quite quickly undergoes changes in tissue structures, so the analgesic effect is noted after 1-2 minutes.

Articaine has a slight ability to expand the lumen of blood vessels, so it is advisable to use it with epinephrine (adrenaline). It quickly penetrates into soft tissues, as well as into bone structures, which ensures an early onset of the effect, as a result of which it is widely used in therapeutic, surgical, orthopedic interventions in dentistry.

Available in the form of cartridges and solutions for injection in ampoules. Packed in cardboard boxes.

pharmachologic effect

The mechanism is based on the impact on the endings of both sensory nerves and nerve fibers, which creates conditions for disrupting the generation of an exciting impulse and its conduction to other structures. Articaine interacts with receptors that are responsible for the operation of sodium channels. By influencing them, the flow of sodium ions through them is blocked, as a result of which an anesthetic effect develops.

The duration of action is about 20 minutes. It breaks down to products that are non-toxic to the body, which makes it possible to re-administer the substance. In an acidic environment, the effectiveness of the drug is reduced.

Analogues

The release of articaine-containing medicinal substances is carried out by many pharmaceutical companies. They go by the following proprietary names:

• Alfakain (manufactured in France);
• Artikain Inbisa (manufacturing country - Spain);
• Ubestezin (production - Germany);
• Primakain (producing country - France);
• Cytocorin (production - Italy);
• Ultracaine (manufacturing country - Germany);
• Septanest (manufactured in France).

Pharmacokinetics and pharmacodynamics

Artikain provides a high degree of action and a minimum number of adverse reactions of the body. It has minimal toxicity. The maximum concentration after injection into the submucosa of the oral cavity is observed 25 minutes after administration. With infiltration anesthesia, the effect is noted after 1-2 minutes, with conduction anesthesia - after 2-2.5 minutes.

Its transformation for the most part occurs in the liver, and the process of inactivation also occurs in the bloodstream and tissue structures under the action of blood plasma enzymes (cholinesterase). The resulting metabolites do not have an anesthetic effect. It binds to blood proteins, excreted by the kidneys. On the first day, about half of the administered dose is excreted.

Since it has the ability to expand blood vessels, it is most often used with adrenaline, a drug that causes vasospasm.

Adrenalin

It is an alpha, beta-adernomimetic agent. Stimulates adrenoreceptors, which leads to a cascade of biochemical reactions, the result of which is an increase or decrease in the concentration of calcium ions in the cell (increase or decrease in functional cellular activity). Functional activity directly depends on the type of ongoing biochemical processes, as well as the type of receptor that has been affected.

An example would be that in vascular walls internal organs contains smooth muscle cells that have alpha-adrenergic receptors on their surface. The impact on them leads to a reduction in cells, the result is a narrowing of the lumen of the vessels. Ability to cause vasospasm skin and mucous membranes, as a result - a slowdown in blood flow in this area, is used to reduce the rate of absorption of local anesthetics, which increases the duration of action.

Indications

In commonly used concentrations, the drug in question does not have surface anesthetic activity, but when injected, it outperforms other drugs of the same group (, Mepivacaine). Therefore, the main indication for the use of Articaine is local anesthesia of the conduction or infiltrative type.

Articaine with adrenaline is used to relieve traumatic dental interventions in the form of the following types of local anesthesia:

• infiltration (impregnation of the tissues of the surgical field);
• conductive (introduction of a substance along the nerve);
• intraligamentary (intraligamentous);
• intraseptal (intraseptal - the substance is injected into the septum of the bone between the holes of the teeth);
• intrapulpal (injection of an anesthetic into the pulp of the tooth).

It also applies to:

• uncomplicated extraction of one or more teeth;
• preparation of carious cavities and teeth before prosthetics.

Articaine in combination with epinephrine has been used in the following concentrations:

• 1:200000;
• 1:100000.

The use of a local anesthetic with a higher content of adrenaline (1:100,000) significantly increases the risk of adverse reactions in patients with pathology of periodontal tissues, as well as when injecting into the palate.

Contraindications

It is forbidden to use the local anesthetic Artikain in the following cases:

• in the presence of a hypersensitivity reaction to Artikain, Adrenaline, sulfites, as well as to any other auxiliary component of the drug;
• at various forms tachyarrhythmia, including paroxysmal tachycardia, atrial fibrillation;
• in the presence of a history of bronchial asthma with excessive sensitivity to sulfites;
• with existing angle-closure glaucoma;
• with simultaneous therapy with non-selective beta-blockers (Propranolol, Timolol, Nadolol, Carvedilol);
• violation of the functioning of the liver severe;
• excessive concentration of hormones thyroid gland in the bloodstream (hyperthyroidism);
• taking a course of therapy with drugs that inhibit monoamine oxidase (Selegiline, Pirlindol, Garmalin, Nialamide), or tricyclic antidepressants (Fluoxetine, Amitriptyline, Imipramine, Trimipramine);
• with existing B12-deficiency anemia, methemoglominemia;
• in the presence of severe disorders of cardiac conduction (severe bradycardia, atrioventricular block II-III degrees);
• in the presence of diseases of the central nervous system;
• with severe arterial hypotension;
• state of acute heart failure;
• extensive maxillofacial surgical interventions, as well as surgical procedures lasting more than 20 minutes;
• children under 4 years old.

Use with caution:

• during pregnancy;
• in puerperas with preeclampsia;
• in the presence of bleeding in the last trimester of pregnancy;
• with a lack of blood cholinesterase;
• with insufficient functioning of the kidneys;
• in the presence of diabetes;
• with hypertension.

Method of application and dosage

The main feature of Articaine is its high ability to penetrate into tissue structures when injected. Therefore, the drug allows for many interventions (for example, preparing teeth for prosthetics, surgical interventions on soft tissues, extraction of teeth) under infiltration anesthesia on the upper and lower jaws.

The absence of side effects during the local method of anesthesia for the most part depends on the correct calculation of the required dosage of the drug used for anesthesia.

In particular, attention is paid to this in pediatric dentistry, which is explained both by the lower body weight of the child, and by the peculiarities of the functioning of organs and systems that are involved in the change and elimination of drugs, as well as in high-risk patients.

The "gold" standard is the use of a minimum amount of local anesthetic with the achievement of maximum control over the pain reaction. Also, the choice of dosage is based on the depth of penetration of the required anesthesia and the time of the required intervention.

4% Articaine with Adrenaline gives a reliable analgesic effect, which manifests itself 1-3 minutes after the injection of the drug. Duration of action - 45-150 minutes. In this case note:

• good penetrating ability;
• good tolerance;
• minimal vasospasm;
• no increase in blood pressure;
• no increase in heart rate;
• minimal penetration through the placental barrier.

Therapeutic dentistry

Apply Artikain in the indicated dosage is used both for infiltration and for the following purposes:

• preparation of carious cavities;
• treatment of pulpitis;
• treatment of periodontitis;
• carrying out surgical interventions on the periodontium.

To obtain an analgesic effect lasting from 30 to 45 minutes, an injection from the outer (vestibular) side of the drug is used at a dosage of 0.5 to 1.8 ml per tooth.

Surgical dentistry

The drug is instilled into the submucosal region of the required tooth in a volume of 1.8 ml. If necessary, additional administration of the drug in the same volume is possible in order to achieve complete anesthesia. Used for conduction and infiltration anesthesia. The indication is the removal of one or more adjacent teeth.

For surgical interventions on the palate (suturing, incisions), it is sufficient to administer the drug in a volume of 0.1 ml per injection.

Orthopedic dentistry

Used for conduction and infiltration local anesthesia. Enter from 0.5 to 1.8 ml with outside jaw into the submucosa of the area of ​​the required tooth. Additional administration of the drug is possible if necessary, but not more than 7 mg per 1 kg of the patient's body weight. Indication - carrying out odontopreparation.

Uncomplicated tooth extraction, preparation for filling, preparation for placement under the crown should be accompanied by the introduction of 0.5 to 1.8 ml of local anesthetic with a vasoconstrictor preparation (no more than 1 cartridge). If there is a need to administer Articaine from the palatal side, then 0.1 ml of a local anesthetic is used.

The maximum dosage allowed for the injection of Articaine is:

• for childhood from 4 to 12 years old - 5 mg / kg;
• for children over 12 years old and adults - 7 mg / kg.

Before the direct administration of the drug, an aspiration test is required to avoid intravascular administration of the drug. The pressure exerted on the piston during the introduction of the agent must be corrected depending on the sensitivity of the tissues. Do not recommend the introduction of the drug into areas of the mucosa, on which there are signs inflammatory process.

Side effects

Articaine can cause a number of adverse effects:

• from the nervous system: stupor, loss of consciousness, respiratory disorders, respiratory arrest, tremor, twitching of muscle groups, generalized convulsions, dizziness, cephalgia, hypesthesia (change pain sensitivity), paresthesia (burning sensations, indications), damage facial nerve(paralysis of the muscles of the face);
• on the part of the organ of vision: blurred vision, diplopia (double vision), decreased visual acuity, blindness;
• from the side of the cardiovascular system: decrease blood pressure, insufficient functioning of the heart, cardiogenic shock;
• from the digestive tract: nausea, vomiting;
• from the side immune system: hypersensitivity reactions, at the injection site - hyperemia, edema, hyperemia of the skin, angioedema (swelling of the upper and lower lips, cheeks, vocal cords), rhinitis, conjunctivitis, urticaria, impaired respiratory function.

Overdose

The introduction of an excess amount of the drug can lead to a variety of manifestations from various organ systems:

• Nervous system. Both her oppression and excitement can be observed. In the first case, dizziness, shortness of breath, impaired consciousness up to its complete loss are observed. Excitation is characterized by anxiety, unreasonable anxiety, tremor of the limbs, convulsions, an increase in the frequency of respiratory movements, and an increase in heart rate.
• The cardiovascular system. Detect violations heart rate, ventricular fibrillation, arterial hypotension, cardiac arrest.

• stopping the administration of the drug;
• the patient is placed on a horizontal surface;
• patency is provided respiratory tract, supply of oxygen;
• control of respiratory rate and heart rate, blood pressure;
• in case of respiratory failure - oxygen supply, intubation, artificial ventilation of the lungs;
• in the presence of convulsions, short-acting barbiturates (Cyclobarbital, Thiopental, Hexobarbital, Kemital) are administered intravenously with simultaneous oxygen supply and blood circulation control;
• with significant circulatory disorders and shock states- intravenous infusion of electrolytes (Ringer's, Aminol, Ringer-Locke solutions), glucocorticosteroid hormones (Dexamethasone, Prednisolone, Methylprednisolone), plasma-substituting solutions (crystalloids - saline, 5% glucose, colloids - dextrans, starches, gelatins; Reopoliglyukin, blood plasma , Fluorodecalins), albumin;
• in collaptoid states and bradycardia - slow intravenous administration 0.1 ml of Epinephrine, then drip into a vein under the control of blood pressure and heart rate;
• with tachycardia and tachyarrhythmias - beta-blockers (Metoprolol, Propranolol, Esmolol, Atenolol), blood pressure control and oxygen supply into the vein.

drug interaction

With the simultaneous use of Articaine with:

• drugs that depress the nervous system (general anesthetics - Halothane, Fluorotan, hypnotics - Zopiclone, Zolpidem) increase the effect of the latter;
• anticoagulants (Heparin, Warfarin, Fraxiparin, Clexane) note an increased risk of bleeding and hemorrhage;
• monoamine oxidase inhibitors (Selegelin, Pirlindol, Nialamide) increase the risk of developing arterial hypotension, therefore, stopping these drugs is indicated 10 days before the planned dental procedure;
• muscle relaxants (Suxamethonium, Tubocurarine, Orphenandrin, Dantrolene) reveal an increase in the duration of action of the last drugs;
• narcotic analgesics (Tramadol, Fentanyl, Codeine, Buprenorphine) observe an increase in the effects of these medications, note depression of respiratory function;
• vasoconstrictor drugs (Oxymetazoline, Xylometazoline, Caffeine, Naphazoline) enhance and lengthen the local anesthetic effect of Articaine;
• cholinesterase blockers (Neostigmine, Galantamine, Physostigmine, Pyridostigmine), Thiotepa, Cyclophosphamide reduce the intensity of Articaine's metabolism.

Articaine is an antagonist of drugs used to treat myasthenia gravis by its action on striated muscles, especially when used in high doses, as a result, additional correction of the treatment of myasthenia is required.

When treating the injection site of a local anesthetic with disinfectant solutions that contain heavy metals, the risk of developing an adverse local reaction in the form of swelling, hyperemia and painful sensitivity increases.

special instructions

When using Artikain, some points should be observed:

• intravenous administration is contraindicated;
• in order to prevent infectious and inflammatory complications, the sterility of the used needles and syringes should be monitored when taking the drug from the ampoule;
• infiltration mandibular anesthesia of the tongue and soft palate does not work (a conductive method of anesthesia is required);
• infiltration anesthesia has the effect of conduction anesthesia when removing the premolars of the lower jaw;
• it is required to control the functions of the cardiovascular, nervous systems, respiratory tract;
• monoamine oxidase inhibitors should be canceled 10 days before the introduction of Articaine.

Articaine during pregnancy and lactation

The use of Articaine during pregnancy has not been established due to insufficient clinical data. Possible use the specified drug if the potential therapeutic effect outweighs the potential risk of adverse effects on the fetus.

Articaine (Articaine) refers to local anesthetics, is a representative of the amide group, is used in dentistry for and.

Available in two forms - with and without adrenaline.

Composition features

The composition of the drug contains the following compounds:

• articaine hydrochloride;
• sodium chloride;
• water for injections.

A variant of Artikain is also produced with the content of a vasoconstrictor in the composition:

• articaine hydrochloride;
• epinephrine hydrotartrate;
• sodium chloride;
• sodium hydroxide;
• disodium edetate;
• sodium disulfite;
• water for injections.

The amount of vasoconstrictor can be either 0.005 mg per 1 ml of solution or 0.01 mg.

Release form - carpula containing 1.7 ml of anesthetic. Each box contains 50 pieces. Ampoules with a volume of 2 ml are also produced, 10 pieces per pack. Artikain is produced by domestic CJSC Binergia, Russia and foreign INIBSA.

Pharmacological properties

Main active substance begins its transformation, getting into the tissues. There it is hydrolyzed, which promotes the release of a base with lipophilic properties. As a result, the metabolite passes through the nerve membrane and affects the functioning of cell wall receptors.

The main target is sodium channels, since they are responsible for the transmission of a nerve impulse. Articaine blocks them, thereby providing an analgesic effect.

The effect appears 2-3 minutes after anesthesia. It stays on for about 20-30 minutes. Adding adrenaline changes the duration. It increases to 45-60 minutes.

The drug is rapidly transformed with the formation of a passive metabolite called articaic acid. It is with this that the low general toxicity is associated, due to which repeated administration of the anesthetic is possible.

Excretion is carried out by the kidneys. The elimination half-life when using the drug in the oral cavity is 25 minutes.

When the drug can and cannot be used

Articaine is used in the following dental interventions:

• processing of teeth for orthopedic constructions;
• carried out on the teeth, oral mucosa or bone;
• closure of communication with the maxillary sinus;
• delete ;
• installation of metal plates at.

An anesthetic is not used for:

• hypersensitivity to the substances included in the drug;
• megaloblastic B12 deficiency anemia;
• methemoglobinemia;
• hypoxia;
• angle-closure glaucoma;
• diseases of the central nervous system;
• chronic hypoxia;
• bronchial asthma;
• paroxysmal tachycardia;
• atrial fibrillation;
• severe atrioventricular block;
• bradycardia;
• acute insufficiency of cardiac activity;
• high blood pressure;
• pheochromocetoma;
• treatment of children under 4 years of age.

How to use?

Before the introduction of an anesthetic, it is important to conduct an aspiration test. Thus, the doctor checks whether he got into the vessel. Also, the use is recommended only in those areas where there is no bright inflammatory process. The injection should never be given into inflamed tissues because it will be ineffective.

Features of the use of Articaine depending on the goals:

The maximum possible amount of medication administered per visit is 4 ml/kg. 1 ml contains 40 mg of active ingredient.

If Articaine with epinephrine was chosen for injection, then the maximum dose would be 7 ml/kg in patients over 18 years of age. The amount of the drug for children will be selected according to the age and weight of each child. But the maximum amount is still limited to 5 ml / kg.

What to look out for

Before the introduction of an anesthetic, it is very important to conduct an aspiration test in order to control the ingress of the agent outside the vascular bed. If this happens, then the injection is carried out slowly.

To prevent transmission infectious diseases each sampling from an ampoule or vial must be carried out using new needles and a syringe. The cartridge is disposable. Its repeated use in other patients is excluded.

A few days before the proposed manipulation, anticoagulants are canceled to reduce the risk of bleeding and hemorrhage. Patients should stop taking monoamine oxidase inhibitors 10 days before visiting the dentist to reduce the chance of developing hypotension.

The anesthetic must be applied with special attention at:

• preeclampsia;
• angina;
• atherosclerosis;
• violations of the level of platelets;
• severe renal and hepatic failure.

Adverse reactions

Injections of the drug are usually well tolerated by all patients, but the following undesirable side reactions sometimes develop:

1. Effect on the nervous system. Consciousness, breathing are disturbed, tremors appear, twitching of the limbs, convulsions. In addition, headache, dizziness, paresthesia and hypoesthesia develop. With a gross violation of the anesthesia technique, damage to the nerve trunk is possible, which leads to paralysis and prolonged sensory disturbances.
2. Influence on the senses. Perhaps a temporary violation of visual acuity or diplopia.
3. Effect on the heart and blood vessels. The level of arterial pressure decreases. Against this background, heart failure and a state of shock develop.
4. Influence on the gastrointestinal tract. Nausea, vomiting, and diarrhea are likely.
5. Allergies in the form of local hyperemia. Of the systemic manifestations, urticaria, allergic conjunctivitis and rhinitis are possible. A more complex course is expressed by angioedema and anaphylactic shock.

What to do in case of an overdose

An excess amount of administered medication manifests itself differently in each of the organ systems:

1. Central nervous system can react with both excitation and oppression. In the first case, anxiety, anxiety, tremors, convulsions appear, consciousness becomes confused, the frequency of breathing and heart rate increases. With oppression, dizziness, shortness of breath develop, consciousness is lost until it is completely lost, breathing is disturbed.
2. Heart and blood vessels respond with bradycardia, arrhythmia, ventricular fibrillation, arterial hypotension and cardiac arrest.

What to do:

• firstly, the administration of the drug is stopped;
• the patient is given a supine position;
• oxygen access and airway patency are provided;
• if breathing is disturbed, an air duct and artificial ventilation of the lungs are used;
• if the level of blood pressure rises, then peripheral vasodilators are used;
• with convulsions, short-acting barbiturates are administered, the injection is carried out intravenously, slowly;
• in shock, solutions of electrolytes, plasma substitutes, albumin and glucocorticosteroids are administered;
• if bradycardia has developed, then adrenaline is used in an amount of 0.1 mg;
• with tachycardia and tachyarrhythmia, intravenous administration of selective beta-blockers is mandatory.

If the pressure has not decreased to critical values, and there is practically no arrhythmia, then the correction is possible with the patient lying down and legs raised above the level of the head. All manipulations are carried out under constant control of the pulse and respiration.

Application in special cases

The safety of the use of Articaine during pregnancy and lactating women has not been established, since not enough studies have been conducted. The penetration of metabolites through the hemato-placental barrier has been proven.

Therefore, the use of an anesthetic is possible only when the positive effect of the manipulation outweighs the likely risk to the fetus (bradycardia may develop).

After anesthesia, breastfeeding is possible, since no substances penetrate into breast milk.

In the treatment of the elderly and patients with insufficient liver and kidney function, the use of minimal doses of the drug is recommended.

Issue price and analogues

The price of one package of the drug Articain is approximately 1500-1700 rubles, the medication with adrenaline and the Forte series cost the same.

The non-adrenaline drug can be replaced with the following anesthetics:

• Scandonest;
• Ultracain D;
• Markain.

Similar remedies that can be used instead of Articaine with adrenaline:

• Ubistezin;
• Primakain;
• Brilocaine-adrenaline;
• Artifrin;
• Septanest.

The active substance is 40 mg Articaine hydrochloride.

Auxiliary ingredients: 2.1 mg sodium chloride and up to 1 ml of water for injection.

Release form

The domestic pharmaceutical industry produces the drug Articaine in the form of an injection containing 40 mg / 1 ml of the active substance.

One package contains 5 or 10 ampoules of 2 ml solution.

pharmachologic effect

Local anesthetic.

Pharmacodynamics and pharmacokinetics

Articaine is a derivative thiophene and has a local anesthetic effect. Is used for conductive and infiltration . Articaine exposed hydrolysis in a slightly alkaline environment of tissues with the release of a base with lipophilic properties, and therefore, it easily penetrates through the cell membrane into the nerve fiber.

Influencing receptors, blocks delivery sodium ions into the cell and conduct impulses along the nerve fibers. The action of the drug is observed immediately after its administration and lasts from 1 to 3 hours. Efficiency is reduced in an acidic environment.

At intramuscular injection Cmax is reached in 20 - 40 minutes.

When introduced under the mucous membrane of the oral cavity, it exhibits a high diffusion ability.

It binds to plasma proteins by 95%.

Exposed to metabolism in the liver, T½ approximately 60 - 80 minutes.

Within 6 hours, it is excreted by the kidneys by 54 - 63%.

Can penetrate the placental barrier (to a lesser extent than other local anesthetics), through the blood-brain barrier penetrates in small quantities. It is practically not excreted with breast milk.

Indications for use

Articaine is used for local anesthesia, mainly during dental procedures.

Contraindications

• children's age up to 4 years;
• hypersensitivity to local anesthetics of the amide group;
• paroxysmal;
• B12 deficiency anemia (megaloblastic);
• angle-closure glaucoma;
• atrial tachyarrhythmia;
• chronic .

Prescribe with caution:

• with pathologies of the central nervous system;
• at pseudocholinesterase deficiency;
• at pernicious anemia;
• at hypoxia.

Side effects

Peripheral and central nervous system:

• headache;
• dyspnea;
• visual impairment;
• muscle twitching;
• convulsions;
• diplopia;
• disturbance of consciousness.

The cardiovascular system:

• bradycardia;
• decrease in blood pressure.

Digestive system:

• nausea;
• vomit.

Allergic manifestations:

• itching;
• skin rash;
• very rarely - .

Application instruction of Artikain (Way and dosage)

The instruction for Articaine in dentistry suggests an individual dosing regimen, depending on the severity of the procedure, the time of its implementation and the tolerance of the drug by the patient.

The maximum single dose of the drug is 6 mg per kilogram of body weight.

For surgical intervention, which requires more time than Articaine can provide, a combined preparation is used - Articaine Inibsa containing as active ingredients - Artikain and . Epinephrine exhibits a vasoconstrictor effect at the injection site, thereby increasing its absorption time, prolonging the action.

Instructions for use of the drug Articaine Epinephrine in dentistry recommends the following doses of the drug.

In the procedure for removing the teeth of the upper jaw without complications and inflammation - 1.7 ml of the drug per tooth, with inefficiency - 1 ml - 1.7 ml.

With a palatine incision or suturing - 0.1 ml.

When turning teeth to install crowns or prepare cavities, a vestibular injection is made at a dose of 0.5 ml - 1.7 ml for each tooth.

In the procedure for the removal of premolars of the lower jaw without complications, infiltration anesthesia , which acts as a conductive anesthesia.

The maximum dose in dentistry for adult patients is 7 mg per kilogram of body weight. For pediatric patients older than 4 years - 5 mg per kilogram of body weight.

Overdose

In case of overdose, it appears dizziness, loss of consciousness, motor agitation, lowering blood pressure, bradycardia, tachycardia.

If the first symptoms of an overdose are detected during the administration of the drug, it is necessary to interrupt the injection, put the patient in a horizontal position, monitor the airway, and also control blood pressure and heart rate.

With increasing bradycardia and vascular collapse give intravenous injection Epinephrine (0.1 mg) with slow administration. If necessary, continue to enter epinephrine in the form of infusion under the control of blood pressure and heart rate.

Interaction

Local anesthetics enhance the effects of drugs that depress the central nervous system.

When Articaine is administered to patients who are receiving Acetylsalicylic acid or, increased risk of local bleeding.

Narcotic potentiate the action of local anesthetic drugs and can lead to respiratory depression.

Artikain DF
Instructions for medical use- RU No. LP-001074

Last Modified Date: 28.04.2017

Dosage form

Injection

Compound

1 ml contains:

Active ingredients: 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 of the dosage form

Clear, colorless solution, odorless.

Pharmacological group

Local anesthetic + alpha and beta adrenomimetic.

Pharmacodynamics

Articaine DF, used for local infiltration and conduction anesthesia in dentistry, is combination drug, which includes articaine (an amide-type local anesthetic) and epinephrine (adrenaline) (a vasoconstrictor). Epinephrine is added to the composition of the drug to prolong the action of anesthesia. Articaine has a local anesthetic effect due to the blockade of voltage-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 rapid 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 drug, its effect on cardiovascular system it is expressed slightly: there is almost no increase in blood pressure and an increase in heart rate.

Pharmacokinetics

Articaine is quickly and almost immediately after administration metabolized (by hydrolysis) by nonspecific plasma esterases in tissues and blood (90%); the remaining 10% dose of articaine is metabolized by microsomal liver enzymes. The main metabolite of articaine formed in this case, articaic acid, does not have local anesthetic activity and systemic toxicity, which allows for repeated injections of the drug. The concentration of articaine in the blood in the area of ​​the alveoli of the tooth after submucosal administration is hundreds of times higher than the concentration of articaine in the systemic circulation. The binding of articaine to plasma proteins is approximately 95%.

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

Articaine crosses the placental barrier and is practically not excreted in breast milk.

Indications

The drug Articaine DF is indicated for local anesthesia (infiltration and conduction anesthesia) in dentistry with traumatic interventions and, if necessary, pronounced hemostasis or improved visualization of the surgical field:

• Dental operations on the mucous membrane or bones, requiring the creation of conditions for more pronounced ischemia;
• Operations on the pulp of the tooth (amputation or extirpation);
• Removal of a broken tooth (osteotomy) or a tooth affected by apical periodontitis;
• Prolonged surgical interventions;
• Transosseous osteosynthesis;
• Excision of cysts;
• Interventions on the mucous membrane of the gums;
• Resection of the apex of the tooth root.

Contraindications

• Hypersensitivity to articaine or other local anesthetics of the amide type, except in cases where hypersensitivity to local anesthetics of the amide type, allergy to articaine has been excluded using appropriate studies carried out in compliance with all necessary rules and requirements.
• Hypersensitivity to epinephrine.
• Hypersensitivity to sulfites (particularly in patients with bronchial asthma and hypersensitivity to sulfites, since 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 violations conduction (such as severe bradycardia, atrioventricular blockade of the 2nd or 3rd degree).
• Acute decompensated heart failure.
• Severe arterial hypotension.
• Children's age up to 4 years (lack of sufficient clinical experience).

Contraindications related to epinephrine

• Paroxysmal tachycardia, tachyarrhythmia.
• Recent (3-6 months ago) myocardial infarction.
• Recent (3 months ago) coronary artery bypass grafting.
• Simultaneous use of non-cardioselective beta-blockers, for example, propranolol (risk of developing a hypertensive crisis and severe bradycardia).
• Angle-closure glaucoma.
• Hyperthyroidism.
• Pheochromocytoma.
• heavy arterial hypertension.

Carefully

chronic heart failure, ischemic disease heart disease, angina pectoris, atherosclerosis, history of myocardial infarction, cardiac arrhythmias, arterial hypertension, cerebrovascular disorders, history of stroke, chronic bronchitis, pulmonary emphysema, bleeding disorders, intraventricular and atrioventricular heart block, inflammation in the area of ​​proposed anesthesia, cholinesterase deficiency ( the use is possible only in case of emergency, since prolongation and a pronounced increase in the effect of the drug are possible), severe liver dysfunction, kidney failure, diabetes, elderly age, heavy general state, debilitated patients, severe agitation, history of epilepsy, simultaneous use with halogen-containing agents during inhalation anesthesia (see section "Interaction with other drugs").

Use during pregnancy and lactation

Pregnancy

Articaine and epinephrine cross the placental barrier. The concentration of articaine in blood serum in newborns (after administration of the drug to the mother) is approximately 30% of the concentration of articaine in the mother's blood serum.

The decision to use the drug can only be made if the potential benefit to the mother outweighs the potential risk to the fetus.

In case of accidental intravascular injection, epinephrine can reduce the blood supply to the uterus.

Period breastfeeding

With short-term use of the drug during breastfeeding, as a rule, it is not necessary to interrupt feeding, since in breast milk no clinically significant concentrations of articaine and epinephrine are detected.

Fertility

Animal studies using articaine 40 mg/ml and epinephrine 0.01 mg/ml showed no effect on fertility in males and females. No effect on human fertility is expected with the use of articaine and epinephrine at therapeutic doses.

Dosage and administration

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

Do not inject into inflamed tissues.

The drug should not be administered intravenously.

In order to avoid accidental entry of the drug into the blood vessels, an aspiration test (in two stages) should always be performed before its administration.

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

For anesthesia with uncomplicated extraction of the teeth of the upper jaw in the absence of inflammation, it is usually sufficient to create a depot of the drug in the region of the transitional fold by introducing it into the submucosa from the vestibular side (1.7 ml of the drug 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 avoids a painful palatal injection. When removing several adjacent teeth, the number of injections can usually be limited.

For anesthesia with incisions and suturing in the sky in order to create a palatine depot, about 0.1 ml of the drug is needed for each injection.

In the case of extraction of mandibular premolars in the absence of inflammation, mandibular anesthesia can be dispensed with, since infiltration anesthesia provided by an injection of 1.7 ml per tooth is usually sufficient. If in this way it was not possible to achieve the desired effect, an additional injection of 1-1.7 ml of anesthetic should be performed into the submucosa in the region of the transitional fold of the lower jaw from the vestibular side. If, in this case, it was not possible to achieve complete anesthesia, it is necessary to conduct a blockade of the mandibular nerve.

At surgical interventions the drug, depending on the severity and duration of the intervention, is dosed individually.

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

For pediatric patients (over 4 years of age), 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 under 1 year of age 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 necessary to achieve sufficient depth of anesthesia should be used.

Side effects

Side effects are grouped by systems and organs in accordance with the MedDRA dictionary and the WHO classification of the incidence of adverse reactions: very often (≥1/10), often (≥1/100 to<1/10), нечасто (≥1/1000 до <1/100), редко (≥1/10000 до <1/1000), очень редко (<1/10000), частота неизвестна (частота не может быть определена на основе имеющихся данных).

Nervous system disorders: often - paresthesia, hypesthesia, headache caused mainly by the presence of epinephrine; infrequently - dizziness; the 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 respiratory arrest, muscle tremor, muscle twitching, sometimes progressing to generalized convulsions).

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

Violations of the organ of vision: frequency is unknown - visual disorders (blurred visual perception, mydriasis, blindness, double vision

eyes), usually reversible and occurring during or shortly after injection of a local anesthetic.

Gastrointestinal disorders: often - nausea, vomiting.

Cardiac and vascular disorders: infrequently - tachycardia, cardiac arrhythmias, increased blood pressure; the frequency is unknown - lowering blood pressure, bradycardia, heart failure and shock.

Immune system disorders: the frequency is 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 , hives, difficulty breathing). Any of these manifestations can progress to anaphylactic shock.

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

Children

In 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 in children, soft tissue damage was more often noted (in 16% of children), especially at the age of 3 to 7 years.

Overdose

Symptoms: The most common symptoms are reactions of the cardiovascular system and the nervous system, nausea, restlessness, clouding of consciousness during injection, respiratory failure, muscle twitching, convulsions, shock.

Treatment: Treatment is symptomatic. At the first signs of an overdose or side effects, such as nausea, motor

anxiety, clouding of consciousness during the injection, it should be interrupted, the patient should be transferred to a horizontal position, the airways should be cleared, the pulse and blood pressure should be monitored. It is recommended that intravenous access be provided even if the symptoms do not seem too severe. In case of respiratory disorders, depending on the severity, give oxygen, in some cases, carry out artificial respiration. Central analeptics are contraindicated. Muscle twitches or generalized convulsions are relieved by intravenous injection of short-acting or ultra-short-acting barbiturates. A drop in blood pressure, tachycardia, or bradycardia often resolves when the patient is placed in the supine position. In case of severe circulatory disorders and shock of any origin, emergency measures are indicated after stopping the injection: ensuring the patency of the respiratory tract (oxygen insufflation), intravenous infusion of fluid (electrolyte solution), glucocorticosteroids. Additionally, you can enter plasma substitutes, albumin.

With a threatening circulatory disorder and increasing bradycardia, 0.25 ml to 1 ml of epinephrine is administered. Intravenous injection of epinephrine should be given slowly under the control of pulse rate and blood pressure.

A single dose of intravenous injection of epinephrine should not exceed 0.1 mg, in the future, if necessary, epinephrine can be administered drip (the rate of infusion through a dropper is regulated depending on the pulse rate and blood pressure). Severe forms of tachycardia and tachyarrhythmia can be eliminated by the use of antiarrhythmic drugs, but non-selective beta-blockers should not be used. Oxygen supply and circulation control are necessary in any case. With an increase in blood pressure in patients suffering from arterial hypertension, peripheral vasodilators should be used, if necessary.

Interaction

Simultaneous use is contraindicated

With simultaneous use with non-cardioselective beta-blockers, for example, propanolol, it is possible to develop a hypertensive crisis and severe bradycardia.

Simultaneous use is possible with caution

The action of vasoconstrictors that increase blood pressure, such as epinephrine, may be enhanced by tricyclic antidepressants or monoamine oxidase inhibitors.

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

When using the drug Articaine DF in patients taking heparin or acetylsalicylic acid possible development of bleeding at the injection site.

When used simultaneously with inhibitors cholinesterase, it is possible to slow down the metabolism of local anesthetics, as a result of which prolongation and a pronounced increase in the action of articaine are possible. Epinephrine may inhibit the release of insulin from pancreatic beta cells and reduce the effects of oral hypoglycemic agents.

Some inhalation anesthetics, such as halothane, may increase myocardial sensitivity to catecholamines and increase the risk of cardiac arrhythmias following injections of Articaine DF.

When treating the injection site of local anesthetic disinfectant solutions containing heavy metals, the risk of development of local reactions - hypostasis, morbidity increases.

special instructions

Regional and local anesthesia should be performed by experienced professionals in an appropriately equipped room with the availability of equipment and preparations ready for immediate use, necessary for cardiac monitoring and resuscitation. Anesthesia personnel should be qualified and trained in anesthesia technique and 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), it is necessary to ensure that new sterile syringes and needles are always used when taking the solution from the ampoules.

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

In order to avoid the development of adverse reactions, it is necessary to use the minimum effective doses of the drug and conduct a two-stage aspiration test before administering the drug (see section "Method of application and doses").

When using the drug, unintentional injury to the lips, cheeks, mucous membrane and tongue is possible, especially in children, due to a decrease in

sensitivity. The patient should be warned that food intake is possible only after the termination of the local anesthesia and the restoration of sensitivity.

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

Influence on the ability to drive vehicles, mechanisms

The possibility of allowing the patient to drive vehicles and mechanisms is determined by the doctor.

Release form

Solution for injection 40 mg + 0.010 mg / ml.

1.8 ml 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 raised symbols. The neck of the cartridge is sealed with a gray rubber stopper and an aluminum cap. A transparent self-adhesive label with marking is pasted on the cartridge.

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

5 blisters with instructions for use in a cardboard box with first opening control.

Storage conditions

In a place protected from light at a temperature not exceeding 30 ° C. Keep out of the reach of children.

Best before date

Do not use after the expiration date.

Terms of dispensing from pharmacies

Released by prescription.

Artikain DF - instructions for medical use - RU No.