Universal reference book for medicines

Active substance: articaine, epinephrine

Type: Local anesthetic with vasoconstrictor component for use in dentistry

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

1 ml

articaine hydrochloride 40 mg

epinephrine hydrochloride 12 Ојg,

is equivalent to a content of an epinephrine base of 10 Ојg,

which corresponds to the content of epinephrine in a solution of 1: 100,000

Excipients: sodium disulfite (sodium metabisulphite), sodium chloride, water d / and.

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

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.


Combined local anesthetic preparation, which includes articaine (amine type local anesthetic) and epinephrine (vasoconstrictor), which is added to the formulation to prolong the duration of anesthesia.

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.
With the rapid destruction of articaine to its inactive metabolite (articaine acid) is associated a very low systemic toxicity of the drug, allowing repeated injections of the drug.
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.
The drug has a fast (latent period - 1 to 3 min) and a strong anesthetic effect and has good tissue tolerance.
The duration of anesthesia is at least 75 minutes.


After submucosal administration, 2 ml of the drug T max articaine in blood plasma is 10-15 minutes, and the average blood plasma C max of articaine is approximately 400 Ојg / l, T max articinic acid is 45 minutes, and the average C max articaine acid is 2000 Ојg / l.
In children, comparable pharmacokinetic data were obtained.Differences between plasma concentrations of articaine and articin acid reflect the rapid hydrolysis of articaine in tissues and blood, so that the introduced articaine enters the systemic bloodstream mainly in the form of an inactive metabolite.

After submucosal administration, the concentration of articaine in the blood in the area of ​​the dental alveoli is thousands of times higher than the articaine concentration in the systemic circulation.
The inverse relationship between the time after injection and the concentration of articaine in the alveolus of the tooth is revealed.
The binding of articaine to plasma proteins is 95%.


All local anesthetic agents of the amide type are metabolized in liver microsomes.
In addition, articaine in tissues and blood is still inactivated by nonspecific plasma esterases by hydrolysis 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 on the mucosa or bones, when it is necessary to create conditions for more severe ischemia:

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

- removal of a broken tooth (osteotomy);

- removal of the tooth, afflicted with apical periodontitis;

- prolonged surgical interventions (for example, the operation of Caldwell-Luc);

- percutaneous osteosynthesis;

excision of cysts;

- intervention on the mucosa of the gum;

- resection of the apex of the root of the tooth;

- treatment of cavities and grinding before prosthetics of highly sensitive teeth.


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 iv.

For anesthesia with uncomplicated removal of the upper jaw teeth in the absence of inflammation, it is usually sufficient to create a depot of the drug UltraCain В® D-C (Ultracaine В® D-C forte) in the region of the transitional fold by inserting 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 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 sutures 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, you can do without mandibular anesthesia.
An infiltration anesthesia provided by injecting 1.7 ml of the drug per tooth is usually sufficient. If this method fails to achieve the desired effect, an additional injection of 1-1.7 ml of the drug 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 dose of Ultraquin В® D-C Fort depends on the severity and duration of the intervention individually.

When performing one treatment procedure, adults can be administered 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).
In children older than 4 years, the dose is selected depending on the age and body weight of the child;
The dose should not exceed 5 mg of articaine per 1 kg of body weight.
In elderly patients and patients with severe renal and hepatic insufficiency, it is possible to create elevated plasma concentrations of articaine.
In these patients, the drug should be used at the minimum dose necessary to achieve sufficient depth of anesthesia.
In order to avoid accidental intravascular injection of the drug, always before it is administered, an aspirate test should be performed.

The injection pressure should correspond to the sensitivity of the tissues.


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 a local anesthetic.
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.

Often - a headache, mainly due to the presence of the drug epinephrine.

From the digestive system: nausea, vomiting.

On the part of the cardiovascular system: lowering blood pressure, bradycardia, heart failure, shock.
Very rarely due to the content of the drug epinephrine may develop tachycardia, violations of the heart rhythm, increasing blood pressure.
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.
In some cases, with occasional intravascular injection, ischemic zones may occur at the site of administration, up to tissue necrosis.

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

- hypersensitivity to epinephrine;

- hypersensitivity to the auxiliary components of the drug, incl.
to sulfites (including manifested as bronchial asthma).
Contraindications related to articaine

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

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);

Contraindications related to epinephrine

- paroxysmal tachycardia, tachyarrhythmia;

- an angle-closure glaucoma;

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

- hyperthyroidism;

- pheochromocytoma;

- severe arterial hypertension.

With caution should be used in patients with angina pectoris, atherosclerosis, postinfarction cardiosclerosis, cerebral circulatory disorders, anamnesis, chronic bronchitis, pulmonary emphysema, diabetes mellitus, cholinesterase deficiency (use is possible only in case of emergency, because it is possible to prolong and excessively strong effect of the drug), disorders of blood clotting, severe impairment of liver and kidney function, pronounced excitation


Artikain penetrates the placental barrier.

In view of the lack of clinical data, the decision to prescribe the dentist can be made only if the potential benefit from its use justifies the potential risk to the fetus.
If it is necessary to use articaine in pregnancy, it is preferable to use preparations that do not contain epinephrine (Ultracaine В® D) or with a lower concentration of epinephrine (Ultracaine В® D-C).
During lactation, there is no need to interrupt breastfeeding, because
in breast milk there are no clinically significant concentrations of articaine.

Caution should be used in patients with severe renal dysfunction.


Caution should be used in patients with severe impairment of liver function.


Contraindicated in children under 4 years of age (lack of clinical experience).


In elderly patients, it is possible to create elevated plasma concentrations of articaine.
In these patients, the drug should be used at the minimum dose necessary to achieve sufficient depth of anesthesia.

The drug can not be administered iv.
Do not inject into an inflamed area. To avoid intravascular injection, an aspiration test should always be performed.
The injection pressure should correspond to the sensitivity of the tissue.

To prevent the introduction of infections (including viral hepatitis), 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 used again for other patients.
Do not use a damaged cartridge for injections.

Patients with diseases of the cardiovascular system (chronic heart failure, coronary artery disease, angina pectoris, cardiac arrhythmias, history of myocardial infarction, hypertension), cerebrovascular disorders, the presence of a history of a stroke, chronic bronchitis, emphysema, diabetes, hyperthyroidism, and also in the presence of the expressed concern expedient use of the drug articaine В® D-C containing minimal amount of epinephrine or articaine В® a preparation not containing
his epinephrine.
Take food can only after the termination of the local anesthesia (restoration of sensitivity).

Impact on the ability to drive vehicles and manage mechanisms

Local anesthesia with Ultracaine В® D-S Fort, as the tests showed, does not cause any noticeable deviation from the usual ability to drive and participate in traffic.However, the decision on when a patient after dental surgery can return to driving vehicles and engaging in potentially dangerous activities that require increased concentration and speed of psychomotor reactions should be made by the 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 bradycardia or a sharp decrease 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 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.
Severe tachycardias and tachyarrhythmias can be suppressed by the administration of antiarrhythmic drugs, with the exception of cardioselective beta-blockers.

Increasing blood pressure in patients with hypertension should be reduced with vasodilators if necessary.


Contraindicated combinations

Contraindicated combination with cardioselective beta-blockers, for example, propranolol, t.
there is a risk of developing a hypertensive crisis and severe bradycardia.
Interactions that should be taken into account

It is possible to intensify the action of vasoconstrictors, increasing blood pressure, such as epinephrine, while using 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.
The concentration of epinephrine in the preparation of Ultracaine В® D-S forte is lower - 1: 100 000. However, it is necessary to take into account the possibilities of such amplification of the action.
Local anesthetics enhance the effect of drugs that depress the central nervous system.
Opioid analgesics increase the effect of local anesthetics, but increase the risk of respiratory depression.
When injecting the drug Ultracaine В® D-S forte, patients who receive heparin or acetylsalicylic acid may develop bleeding at the injection site.

Ultrakain В® D-S forte increases the intensity and duration of the action of muscle relaxants.

Ultracaine В® D-C forte shows antagonism with respect to the effect on the sclerotic musculatrus 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-S forte causes a slowing of the metabolism of local anesthetics.

When used simultaneously with cholinesterase inhibitors, the metabolism of locally anesthetized drugs slows down.

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

Halothane can increase the sensitivity of the heart to catecholamines and therefore increase the risk of heart rhythm disturbances after injections of the drug UltrakainВ® D-C Fort.

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.


The drug is released by prescription.


List B.

Ampoules should be stored in a dark place at a temperature of no higher than 25 В° C.
Shelf life - 36 months.
Cartridges should be stored in a dark place at a temperature of no higher than 30 В° C.
Shelf life - 30 months.
The drug should be stored out of the reach of children.

Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y

Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!