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

Active substanceArticaineArticaine

Similar drugsTo uncover

Articaine

solution for injections

Promomed Rus, Open Company Russia

Articaine-Binergia

solution for injections

BINERGIYA, CJSC Russia

Ultracaine® D

solution for injections

Sanofi-Aventis Deutschland GmbH Germany

Dosage form: & nbspinjection

Composition:

Active substance: articaine hydrochloride 40.0 mg.

Excipients: sodium chloride - 2.1 mg, water for injection - up to 1.0 ml.

Description:Colorless transparent liquid.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B.08 Articaine

Pharmacodynamics:

Artikain is an amine type local anesthetic used for infiltration and conduction anesthesia in dentistry. Articaine has a local anesthetic effect due to blockade of potential-dependent sodium channels in the cell membrane of neurons, which leads to reversible inhibition of conduction of impulses along the nerve fiber and reversible loss of sensitivity. The effect of the drug begins quickly, within 1-3 minutes. The duration of anesthesia is approximately 20 minutes. A drug Articaine does not contain epinephrine and is used when the addition of epinephrine to the topical anesthetic is not necessary or the use of epinephrine is contraindicated.

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 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:Local anesthetic for infiltration and conduction anesthesia in dentistry. Artikain without epinephrine is used primarily for short procedures in patients who use epinephrine inadmissible (for example, for cardiovascular diseases), or when small amounts of the drug are needed (in the region of the anterior teeth, the palate).

Contraindications:

- Hypersensitivity to articaine or other amido type local anesthetics, except when hypersensitivity to amine type local anesthetics, an allergy to articaine has been ruled out by appropriate studies conducted in compliance with all necessary rules and requirements.

- Severe dysfunction of the sinus node or severe conduction disorders (such as severe bradycardia, atrioventricular block II-III degree).

- Acute decompensated heart failure.

- Severe arterial hypotension.

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

Carefully:- Insufficiency of cholinesterase (application is possible only in case of emergency, since prolongation and pronounced increase in the action of the drug are possible);

- Epilepsy in the anamnesis (see section "Side effect").

Pregnancy and lactation:

Pregnancy

Artikain penetrates 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.

In view of 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.

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.

Fertility

In studies of fertility in rats, when applying articaine in toxic doses, there was no effect on fertility in males and males female. No effect on fertility in humans is expected with articaine 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 infiltration anesthesia, in the absence of inflammation, 1.7 ml of the Artikain solution per tooth or two adjacent teeth are usually administered.With conductor anesthesia of the lower alveolar nerve, approximately 1-1.7 ml of the drug solution is required. For additional injections, half the dose or the full dose should be used.

The maximum dose for adults is 4 mg of articaine hydrochloride per kg of body weight.

In order to avoid accidental ingestion of the drug in blood vessels. Before its introduction always it is necessary to conduct an aspirate test (in two stages). The injection pressure during the administration of the drug should be adjusted depending on the tissue sensitivity.

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; the frequency is unknown (it is not possible to determine the frequency of occurrence according to the available data).

Disturbances from the nervous system

Often

Paresthesia, hypoesthesia.

Infrequently

Dizziness.

Frequency unknown

Dose-dependent reactions from the central nervous system: agitation, nervousness, stupor, sometimes progressing to loss of consciousness, coma, respiratory distress,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.

Disturbances on the part of the organ of sight

Frequency unknown

Visual disorders (blurred vision, double vision, mydriasis, blindness), usually reversible, and occurring during or shortly after injection of a local anesthetic into the head region.

Disorders from the gastrointestinal tract

Often

Nausea, vomiting.

Violations from the heart and blood vessels

Frequency unknown

Reduction of blood pressure, bradycardia, heart failure, shock.

Immune system disorders

Frequency unknown

Allergic and allergic reactions can develop. At the injection site, they can manifest as swelling or inflammation of the mucous membrane. Manifestations not associated with the place of administration may include skin flushing, itching, conjunctivitis, rhinitis and angioedema.

Angioedema may be manifested by edema of the upper and / or lower lip, cheeks, edema of the vocal cords with a sensation of "lump in the throat" and difficulty swallowing, hives and difficulty breathing. Any of these manifestations can progress to anaphylactic shock.

Overdose:At the first manifestations of toxic effects, 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 put an intravenous catheter in order, if necessary, to be able to immediately carry out intravenous administration of the necessary medicines. 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.

The management of central analeptics is contraindicated.

Muscular twitching and generalized convulsions can be stopped by intravenous injection of barbiturates of short or ultrashort action. It is recommended to inject these drugs slowly, under constant medical supervision (risk of hemodynamic disorders and respiratory depression) and with simultaneous oxygen supply and monitoring of hemodynamic parameters.

Often bradycardia or a sharp drop in blood pressure can be eliminated by simply moving the patient to a horizontal position with raised lower limbs.

With severe circulatory disturbances and shock, regardless of their cause, the drug should be discontinued and the patient should be moved to a horizontal position with raised lower limbs. There should be oxygen supply, intravenous electrolyte solutions, glucocorticosteroids (250-1000 mg of methylprednisolone), if necessary, plasma substitutes, including albumin. With the development of collapse and increased bradycardia, a slow intravenous injection of epinephrine solution (0.0025-0.1 mg)under the control of heart rate and blood pressure. If necessary, the administration of 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.

Interaction:

With drugs that depress the central nervous system (CNS)

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

With heparin, acetylsalicylic acid

When injecting the drug Articaine patients receiving heparin or acetylsalicylic acid may develop bleeding at the injection site.

With cholinesterase inhibitors

The slowing of the metabolism of the local anesthetic drugs, as a result of which prolongation and the pronounced increase in the action of articaine are possible.

With vasoconstrictor

The local anesthetic effect of articaine is enhanced and lengthened by vasoconstrictive drugs.

With disinfecting solutions containing heavy metals

When treating the injection site of a local anesthetic with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain sensitivity, edema increases.

Special instructions:

The drug is not intended for long-term administration (more than 20 minutes).

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.

Patients are required to monitor the condition of the cardiovascular system, respiratory system, CNS. Care should be taken when using the drug in patients with angina pectoris, atherosclerosis, blood clotting disorders, severe impairment of liver or kidney function.

In order to avoid the risk of adverse reactions, it is necessary to use the minimum effective doses of the preparation and, prior to its introduction, a two-stage aspiration test should be performed.

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.

Take food can only after the termination of the local anesthesia (restoration of sensitivity). Children and their parents should be warned about the risk of accidental damage to soft tissues with teeth (biting) due to a decrease in the sensitivity of tissues due to the action of the drug.

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

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

The decision on when a patient after dental surgery can return to driving or other potentially dangerous activities that require increased concentration and speed of psychomotor reactions should be made by the doctor.

Form release / dosage:

Solution for injection 40 mg / ml.

Packaging:2 ml into ampoules from neutral glass grade HC-3 or from glass of the first hydrolytic class.

5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

1 or 2 contour squares are placed in a pack of cardboard.

10 ampoules are placed in a box of cardboard.

In each pack or box, put the instructions for use and the ampoule scaler.

When using ampoules with an incision, a ring of fracture or a break point, the ampoule scaper is not inserted.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:5 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001151

Date of registration:11.11.2011 / 22.11.2016

Expiration Date:Unlimited

The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp09.10.2017

Illustrated instructions

Instructions

Articaine (Articaine)