Universal reference book for medicines

Active substance: articaine

Type: Local anesthetic for dental use

Composition, form of production and packaging
Solution for injections is
transparent, colorless.

1 ml

articaine hydrochloride 40 mg

Excipients: sodium chloride - 2.1 mg, water d / and - up to 1 ml.

2 ml - ampoules of colorless glass (10) - packs cardboard.

1.7 ml - colorless glass cartridges (10) - corrugated cardboard blocks (1) - cardboard packs.

1.7 ml - colorless glass cartridges (10) - corrugated cardboard blocks (10) - cardboard packs.


Description of the drug approved by the manufacturer for the printed edition of 2014.


Locally anesthetic drug.
The amide structure of articaine is similar to the structure of other local anesthetics, but its molecule contains one additional ester group, which in the human body is rapidly hydrolyzed by esterases.
Articaine blocks the sodium channels of the neuron membrane, which leads to a decrease in the conduction of impulses along the nerve fiber, thus providing a local anesthetic effect.
Local anesthetics cause a reversible loss of sensitivity due to the cessation or decrease in the conductivity of sensory nerve impulses directly at the injection site and around it. They have a membrane-stabilizing effect by reducing the permeability of nerve cell membranes for sodium ions.
Ultracaine В® D does not contain epinephrine, it is used when the addition of epinephrine to the local anesthetic is not necessary or the use of epinephrine is contraindicated.
The effect of the drug begins quickly (the latent period is 1-3 minutes). The duration of anesthesia is approximately 20 minutes. Rapid destruction of articaine to an inactive metabolite - articaine acid - is the cause of its very low systemic toxicity, which allows repeated injections of the drug.


The binding of articaine to plasma proteins is approximately 95%.

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


Articaine (as well as other amine type local anesthetics) is metabolized by microsomal enzymes of the liver.
Besides this, articaine is also inactivated by nonspecific plasma esterases in tissues and blood by hydrolyzing the ester bond in the carboxyl group. Because hydrolysis occurs very rapidly and begins immediately after administration, about 90% of articaine is inactivated by this method. The resulting main metabolite articaine - articaine acid - does not have local anesthetic activity and has no systemic toxicity.

After submucosal administration, the withdrawal of articaine occurs exponentially with T 1/2 approximately 25 minutes.
Articaine is excreted mainly by the kidneys in the form of articaine acid (64.2 В± 14.4%), arkainic acid glucuronide (13.4 В± 5%) and unchanged articaine (1.45 В± 0.77%).
After injection of the drug into the oral mucosa, the total clearance of articaine is 235 В± 27 l / h.


Infiltration and conductive anesthesia in dental operations:

uncomplicated removal of one or more teeth;

- treatment of carious cavities of the tooth;

- grinding teeth before prosthetics.


For adults, the maximum dose is 4-6 mg / kg body weight.
The total dose is not more than 400 mg.
In infiltrative anesthesia, in the absence of inflammation , 1.7 ml of Ultrakain D 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.

Before the introduction of the drug, it is recommended to always perform an aspirate test in order to avoid unintentional intravascular administration of the drug.Injection pressure during the administration of the drug should be adjusted depending on the tissue sensitivity.

The introduction of the drug into the inflamed parts of the mucosa is not recommended.


From the side of the central nervous system: dose-response reactions - stupor, sometimes progressing to loss of consciousness, respiratory disorders, sometimes progressing to stopping breathing, muscle tremor, muscle twitching sometimes progressing to generalized seizures;
possible dizziness, paresthesia, hypoesthesia, transient visual disorders (blurred vision, blindness, double vision) that occur during or shortly after injection of the local anesthetic into the head region.
Sometimes, if the correct technique of injection is violated with the introduction of a local anesthetic in dental practice, nerve damage is possible, in particular, in such cases, damage to the facial nerve can occur, which can lead to paralysis of the facial nerve.

From the digestive system: nausea, vomiting.

On the part of the cardiovascular system: lowering blood pressure, bradycardia, heart failure, shock.

Allergic reactions: possible - flushing of the skin, conjunctivitis, rhinitis and angioedema.
Angioedema may be manifested by edema of the upper and / or lower lips, cheeks, edema of the vocal cords with a sensation of "lump in the throat" and difficulty swallowing, hives, difficulty breathing. Any of these manifestations can progress to anaphylactic shock.
Local reactions: swelling or inflammation of the mucosa at the injection site.


- Severe dysfunction of the sinus node or severe conduction disorders (such as severe bradycardia, AV-blockade II-III degree);

acute decompensated heart failure;

- severe arterial hypotension;

- Anemia (including in 12- deficiency anemia);

- Methemoglobinemia;

- hypoxia;

- Children under 4 years of age (lack of clinical experience);

- hypersensitivity to articaine or other amido type local anesthetics, except in cases when hypersensitivity to these agents allergy to articaine has been excluded through appropriate studies conducted in compliance with all necessary rules and requirements.

With caution , use the drug in case of cholinesterase insufficiency (they are used only in case of emergency, because prolonged and excessively strong action of the drug is possible).


Artikain penetrates the placental barrier.

In view of the lack of clinical data, the decision to prescribe the drug by a dentist can be made only if the potential benefit of using it justifies the potential risk to the fetus.

During lactation, there is no need to interrupt breastfeeding, because
in breast milk there are no clinically significant concentrations of articaine, but for the sake of precaution, breastfeeding should be discontinued for 4 hours after the last dose of articaine.

Contraindicated in children under 4 years.


To avoid intravascular injection, an aspiration test should always be performed.

To prevent the introduction of infections (including viral hepatitis), care must be taken to ensure that new sterile syringes and needles are always used when taking a solution from ampoules.
Open cartridges can not be used again for other patients. Do not use a damaged cartridge for injections.
Patients are required to monitor the condition of the cardiovascular system, respiratory system, CNS.

Take food can only after the termination of the local anesthesia (restoration of sensitivity).

Impact on the ability to drive vehicles and manage mechanisms

The decision on when a patient after dental surgery can return to driving vehicles and engage in potentially dangerous activities that require increased concentration and speed of psychomotor reactions should be taken by a doctor.


Symptoms: the first manifestations of toxic effects - dizziness, motor agitation or stupor;
possible bradycardia, a sharp decrease in blood pressure, breathing disorders, muscle twitching, generalized convulsions, severe circulatory disorders, shock.
Treatment: at the first manifestations of symptoms of toxic effects 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 (heart rate and blood pressure). It is recommended always, even if the symptoms of intoxication seem to be mild, put the IV in the catheter in order, if necessary, to be able to immediately carry out / in the introduction of the necessary medications.
If breathing is disturbed, depending on their severity, oxygen is recommended, and if there are indications for carrying out artificial respiration, endotracheal intubation and ventilation should be performed.

The introduction of central action analeptics is contraindicated.

Muscular twitching and generalized convulsions can be stopped in / with the introduction 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 a bradycardia or a sharp decrease in blood pressure can be eliminated by simply transferring 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 placed in a horizontal position with raised lower limbs.
It is necessary to provide oxygen supply, iv injection of solutions of electrolytes, GCS (250-1000 mg of methylprednisolone), if necessary, plasma substitutes, incl. albumin.
With the development of collapse and increased bradycardia, a slow intravenous injection of epinephrine (0.0025-0.1 mg) under the control of cardiac rhythm and blood pressure was shown.
If it is necessary to administer doses exceeding 0.1 mg, epinephrine should be administered by infusion, adjusting the rate of administration under the control of heart rate and blood pressure.

Use with MAO inhibitors increases the risk of lowering blood pressure;
It is necessary to abolish MAO inhibitors 10 days before the injection of anesthetic.
Local anesthetics enhance the effect of drugs that depress the central nervous system.
Opioid analgesics increase the effect of local anesthetics and increase the risk of respiratory depression.
When injecting Ultrakain В® D, patients who receive heparin or acetylsalicylic acid may develop bleeding at the injection site.

Ultrakain В® D causes the enhancement and lengthening of the action of muscle relaxants.

Ultracaine В® D antagonizes the effect on the sclerotic musculature with preparations for the treatment of myasthenia gravis, therefore, when it is used, especially in high doses, an additional correction of the treatment of myasthenia is required.

Ultracaine В® D causes a slowing of the metabolism of local anesthetics.

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


The drug is released by prescription.


The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C.
Shelf life - 5 years.
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