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Composition


active ingredients: 1 ml of articaine hydrochloride 40 mg and epinephrine (epinephrine) hydrochloride 0.012 mg


excipients: sodium metabisulfite (E 223), sodium chloride, water for injection.


Dosage form


Solution for injection.


Basic physical and chemical properties: transparent, colorless liquid, practically free of visible particles.


Pharmacological Group


Means for local anesthesia. Articaine, combinations.


ATX code N01B B58.


Pharmacological properties


Pharmacodynamics. Ultracaine D-S forte is a local anesthetic of the amide type, which is used in dentistry for infiltration and conduction anesthesia. The drug has a rapid onset of action (the latent period is 1-3 minutes), a strong analgesic effect. The duration of effective anesthesia is approximately 75 minutes.


It is believed that the mechanism of action of articaine is to reduce the conduction of impulses through nerve fibers by blocking the potential-free sodium channels of cell membranes.


Clinical studies involving up to 210 patients showed that the use of ultracaine D-C in doses up to 5 mg / kg of articaine and ultracaine D-C forte in doses up to 7 mg / kg of articaine in children aged 3.5 to 16 years provided reliable local anesthesia when administered by infiltration (for the lower jaw) and guide (for the upper jaw) anesthesia. The duration of anesthesia was the same in all age groups and depended on the amount of anesthetic administered.


Pharmacokinetics. The level of binding of articaine to plasma proteins is 95%. After injection under the oral mucosa, the half-life is 25.3 ± 3.3 minutes. 10% of articaine is metabolized in the liver, mainly under the action of esterases contained in blood plasma and tissues. Articaine is mainly excreted from the body by the kidneys in the form of articainic acid.


In children, the total exposure after infiltration anesthesia from the vestibular side was similar to that in adults, but the minimum blood concentrations were reached faster.


Preclinical safety data.


The results of preclinical standard studies on the pharmacology of safety, chronic toxicity, reproductive toxicity and genotoxicity indicate that there is no particular danger to humans when used at therapeutic doses. In doses higher than therapeutic, Articaine has a cardiodepresor effect and may exhibit a vasodilating effect. Epinephrine suppresses the effects of sympathomimetics.


During studies of the embryotoxicity of articaine, there was no increase in the frequency of fetal mortality or the occurrence of malformations with daily administration of the drug at doses up to 20 mg / kg (rats) and 12.5 mg / kg (rabbits). Epinephrine demonstrated a toxic effect on the reproductive function in animals at doses from 0.1 to 5 mg / kg (this is several times higher than the maximum dose of epinephrine that enters the body when using the drug Ultracaine D-S forte), which was manifested by the occurrence of congenital malformations and impaired utero-placental blood circulation.


During studies of embriophetotoxicity of articaine and epinephrine, there was no increase in the frequency of malformations with daily subcutaneous administration of articaine at doses up to 80 mg / kg (rats) and 40 mg / kg (rabbits).


During the study of the effect of the drug on fertility and early embryophetal development in rats, no negative effect on the fertility of females and males was observed when using doses that cause toxic phenomena in parental individuals.


Indications


Surgical interventions on the mucous membrane and bones that require more intensive ischemia; surgical interventions on the pulp of the tooth (amputation and extirpation) removal of periodontal or broken teeth (osteotomy) long-term surgical interventions percutaneous osteosynthesis; removal of cysts; surgical interventions on the gum mucosa; root apical resection.


Contraindications


Ultracaine D-C forte should not be used with hypersensitivity to the active substances - epinephrine and articaine, as well as to sulfites (meta bisulfite (E 223) or to any of the excipients of the drug.


Due to the presence in the composition of the drug Ultracaine D-C forte articaine, it can not be used in the following cases::


hypersensitivity to other local amide-type anesthetics;

severe violations of the formation of cardiac impulses or conduction disorders (AV block II-III degree, pronounced bradycardia)

acute decompensated heart failure (acute congestive heart failure);

severe arterial hypotension.

Due to the presence in the composition of the drug Ultracaine D-C forte epinephrine, it can not be used:

patients with closed-angle glaucoma;

patients with hyperthyroidism;

patients with paroxysmal tachycardia or absolute arrhythmia with tachycardia;

patients who recently (3 to 6 months ago) had a myocardial infarction

patients who recently (up to 3 months ago) underwent aortic bypass surgery;

patients who take non-selective beta-blockers, such as propranolol (there is a risk of developing a hypertensive crisis or severe bradycardia)

patients with pheochromocytoma;

patients with severe arterial hypertension;

with concomitant treatment with tricyclic antidepressants or MAO inhibitors, as their active ingredients can enhance the cardiovascular effects of epinephrine. This phenomenon may occur within 14 days after discontinuation of treatment with MAO inhibitors.

The administration of the drug is contraindicated.


Due to the presence of epinephrine in the composition of the drug Ultracaine D-S forte, it should not be used for anesthesia of the extremities (for example, fingers), since there is a risk of ischemia.


Ultracaine D-C forte should not be used in patients with bronchial asthma with hypersensitivity to sulfites. In such patients, the administration of the drug Ultracaine D-S forte can provoke an acute allergic reaction with symptoms of anaphylaxis, such as bronchospasm.


Interactions with other drugs and other types of interactions


Combinations of various anesthetics have an additive effect and have a more pronounced effect on the cardiovascular system and the central nervous system.


The hypertensive effects of sympathomimetic-type vasoconstrictors (e.g. epinephrine) may be enhanced by tricyclic antidepressants or MAO inhibitors. Therefore, such combinations are contraindicated (see the section "Contraindications").


The drug ultracaine D-C forte is forbidden to use in patients who take non-selective beta-blockers, such as propranolol (see the section "Contraindications").


Epinephrine can block the release of insulin a by the pancreas, which reduces the effect of oral antidiabetic drugs.


Some inhaled anesthetics, such as halothane, can increase the sensitivity of the myocardium to catecholamines, causing arrhythmia after administration of the drug Ultracaine D-C forte.


It should be remembered that in patients treated with anticoagulants (for example, heparin, acetylsalicylic acid), an accidental puncture of the vessel during local anesthesia can cause serious bleeding. Such patients generally have an increased tendency to bleed.


Application Features

Patients with a cholinesterase deficiency of ultracaine D-C forte can be prescribed only if there are absolute indications for use, since in this case there is a high probability of an increase in the duration of the drug, and sometimes an undesirable increase in its effect.


Ultracaine D-S forte should be used with caution when:


blood clotting disorders

severe renal or liver function

disorders simultaneous use of inhaled anesthesia products containing halogens (see the section " Interaction with other drugs and other types of interactions»);

the presence of a history of epilepsy (see the section "Adverse reactions").

With extreme caution, ultracaine D-C forte should also be used in patients with:

cardiovascular diseases (for example, heart failure, coronary heart disease, angina pectoris, a history of myocardial infarction, cardiac arrhythmia, arterial hypertension)

atherosclerosis;

disorders of cerebral circulation, a history of stroke

, chronic bronchitis, emphysema of the lungs,

diabetes mellitus;

significantly expressed anxiety.

In addition, Ultracaine D-C contains less epinephrine than ultracaine D-C forte, so in the cases mentioned above, it is more appropriate to use ultracaine D-C.


Do not inject in the area of inflammation (infection) (increased absorption of the drug Ultracaine D-S forte, which leads to a decrease in its effectiveness).


Before using this drug, it is necessary to interview the patient, collect a medical history, information about concomitant medications that he takes, as well as constantly maintain verbal contact with the patient during the administration of the drug. It is necessary to perform an injection test with the introduction of 5 to 10% of the dose, if there is a risk of an allergic reaction.


To avoid the appearance of side effects, it is necessary to:


apply the best dose;

before the injection, perform an aspiration test in two stages (to avoid intravascular administration of the drug).

It is recommended that the patient take food only after complete restoration of sensitivity.


Ultracaine D-C forte contains sodium, but its amount does not exceed 1 mmol (23 mg) per 1 ml.


Use for children.


Caregivers of young children should be warned about the possibility of soft tissue damage due to biting as a result of prolonged numbness of the soft tissues after anesthesia.


Use during pregnancy or lactation.


Pregnancy. There is no experience of using articaine in pregnant women, except for its use during childbirth. In animal studies, no evidence of direct or indirect negative effects of articaine on pregnancy, embryophetal development, childbirth, or postnatal development was found. Animal studies have shown that epinephrine at doses higher than the maximum permissible dose has a toxic effect on reproductive function (see the section "Preclinical safety data"). Epinephrine and Articaine pass through the placental barrier, although Articaine passes to a much lesser extent compared to other local anesthetics. The concentrations of articaine in the blood serum of newborns were approximately 30% of its concentration in the mother's blood. In the case of accidental intravascular injection of the mother, epinephrine (epinephrine) can reduce the rate of blood flow in the uterus. The use of the drug Ultracaine D-S forte during pregnancy is possible only after a thorough analysis of the benefit-risk ratio.


Ultracaine D-C is preferred because it contains less epinephrine (1: 200000) than ultracaine D-C forte.


Breast-feeding. Due to the rapid decrease in plasma concentrations and the rapid elimination of articaine from the body, it does not appear in breast milk in quantities that should be of clinical significance. Epinephrine penetrates into breast milk, but it also breaks down quickly. With short-term use of the drug, there is no need to stop breastfeeding.


Fertility.


Studies on laboratory animals that were administered Articaine 40 mg / ml + epinephrine 0.01 mg / ml did not reveal any negative effect on fertility (see the section "Pharmacological properties"). When using the drug in therapeutic doses, the negative effect of the drug on human fertility is not expected.


The ability to influence the reaction speed when driving vehicles or other mechanisms.


Only the dentist should decide how long after the administration of the drug Ultracaine D-S forte, the patient can again drive a vehicle or work with mechanisms. The fear associated with waiting for dental manipulation, and the stress that accompanies it, can lead to a change in the ability to act effectively, but relevant studies have shown that local anesthesia of articaine does not cause any noticeable deterioration in the ability to drive a vehicle.


Method of administration and dosage


In the case of uncomplicated removal of the upper jaw tooth with forceps in the absence of inflammation, it is enough to inject 1.7 ml of the drug per tooth from the vestibular side into the transitional fold. Sometimes,to achieve complete anesthesia, an additional vestibular injection of 1-1. 7 ml of the drug may be required. In most cases, there is no need to perform a painful palatinal injection.


If it is necessary to make an incision in the palate or to put stitches on it, then in order to create a depot of anesthetic from the palate, it is enough to inject 0.1 ml of the drug.


With multiple extractions of adjacent teeth, the number of vestibular depot injections can be reduced in most cases.


In the case of uncomplicated removal of the premolars of the lower jaw with forceps in the absence of inflammation, Mandibular anesthesia can not be performed, since infiltration anesthesia, which is provided with the introduction of 1.7 ml of the drug per tooth, is usually sufficient. If this does not allow for complete analgesia,an additional vestibular injection at a dose of 1-1. 7 ml is performed first. And only when this also did not give full anesthesia, standard mandibular anesthesia is indicated.


For surgical procedures, the dosage of D-S forte Ultracaine should be selected depending on the severity and duration of the operation.


During one course of treatment, adults can be administered up to 7 mg of ultracaine (articaine) per 1 kg of body weight. After the preliminary aspiration test, doses up to 500 mg (which is 12.5 ml of solution for injection) were well tolerated.


Children.


The drug ultracaine D-S forte should be administered to children in a minimum amount that allows for proper anesthesia; the amount of the drug administered should be adjusted individually, depending on the age and body weight of the child. Do not exceed the maximum dose, which is 7 mg of articaine per 1 kg of body weight.


The use of this drug in children under the age of 1 year has not been studied.


Elderly patients and patients with severe liver and kidney dysfunction.


In elderly patients and patients with severe hepatic and renal impairment, an increase in the concentration of articaine in blood plasma is possible. For such patients, special care should be taken and the minimum dose necessary to achieve sufficient depth of anesthesia should be applied.


Method of administration and duration of use.


Before using the drug, it is necessary to make a skin test to exclude hypersensitivity. Ultracaine D-S forte is intended for administration under the oral mucosa.


To avoid intravascular administration of the drug, it is always recommended to perform an aspiration test before injection. The aspiration test is carried out in two stages, that is, by turning the needle by 90 ° or even better by 180 °. If cartridges are used, then the "Unijet K" or "Unijet K vario"syringes are best suited for performing this test.


The development of serious systemic reactions resulting from accidental intravascular administration of the drug can be avoided in most cases if such an injection technique is used after aspiration, 0.1-0.2 ml is slowly administered, and then, no earlier than 20-30 seconds later, the remaining drugs are slowly administered. The injection pressure must match the sensitivity of the tissue.


The use of appropriate syringes (for infiltration anesthesia - "Unijet K" or "Unijet K vario", for intraligmental anesthesia - "Ultrajet ") provides maximum protection against damage to the cartridge glass and guarantees smooth insertion. Do not use a damaged cartridge for injection.


To avoid infection (for example, transmission of the hepatitis virus), new sterile needles and syringes should always be used for the solution set.


This drug should not be used if it is cloudy or has changed color.


Children


The drug ultracaine D-S forte should be administered to children in a minimum amount that allows for proper anesthesia; the amount of the drug administered should be adjusted individually, depending on the age and body weight of the child. Do not exceed the maximum dose, which is 7 mg of articaine per 1 kg of body weight.


The use of this drug in children under the age of 1 year has not been studied.

Overdose


Symptoms of overdose.


Signs of central nervous system arousal: restlessness, anxiety, confusion, rapid breathing, tachycardia, increased blood pressure, which is accompanied by redness of the face, nausea, vomiting, tremor, involuntary muscle contractions, tonic-clonic convulsions.


Signs of CNS depression: dizziness, hearing loss, loss of the ability to speak, stupor, loss of consciousness, muscle atony, vasomotor paralysis (weakness, pallor of the skin), shortness of breath, death as a result of paralysis of the respiratory center.


Signs of cardiovascular depression: bradycardia, arrhythmia, ventricular fibrillation, decreased blood pressure, cyanosis, cardiac arrest.


Urgent measures and antidotes.


If the first signs of an adverse reaction or toxic effect appear (for example, dizziness, motor excitement or stupor), stop the injection and move the patient to a horizontal position. It is necessary to ensure the patency of the patient's airways, monitor the pulse and blood pressure.


Even when the symptoms of intoxication are not severe, it is recommended to install a catheter to ensure immediate access, if necessary.


In case of respiratory disorders, depending on the severity of the condition, it is recommended to use oxygen, as well as artificial respiration if necessary. If necessary, tracheal intubation is performed in combination with controlled ventilation of the lungs.


Involuntary muscle contractions or generalized convulsions are stopped by intravenous administration of short-acting anticonvulsants (for example, suxamethonium chloride, diazepam). It is also recommended to use artificial respiration (oxygen).


A decrease in blood pressure, tachycardia, or bradycardia can be eliminated by moving the patient to a horizontal position or to a position where the legs are raised just above the head.


In severe circulatory disorders, as well as in shock, regardless of the cause, after stopping the injection, urgent measures should be taken, namely:


move the patient to a horizontal position or to a position in which the legs are raised slightly above the head, and also ensure the patency of the respiratory tract (oxygen insufflation)


start intravenous infusion of a balanced electrolyte solution;


apply the administration of glucocorticoids (for example, 250-1000 mg of prednisolone or an appropriate amount of its derivative, for example, methylprednisolone)


restore the volume of circulating blood (additionally, if necessary, use plasma substitutes, human albumin).


In the event of a threat of circulatory collapse and increasing bradycardia, an immediate intravenous injection of epinephrine (epinephrine) is performed. To do this, dilute 1 ml of epinephrine solution 1: 1000 to 10 ml (instead, you can use epinephrine solution 1: 10000) and slowly inject 0.25-1 ml of this solution (contains 0.025-0.1 mg of epinephrine), monitoring the pulse rate and blood pressure (attention: heart arrhythmia may occur). Do not administer more than 1 ml of this solution (0.1 mg of epinephrine) during a single injection. If this amount of epinephrine is not enough, then it is recommended to add infusion solutions (the infusion rate is adjusted according to the pulse rate and blood pressure).


Severe forms of tachycardia and tachyarrhythmia can be eliminated by the use of antiarrhythmic drugs (but not non-selective beta-blockers, such as propanolol) (see the section "Contraindications"). In such cases, it is necessary to use oxygen and monitor blood circulation.


In the case of increased blood pressure in patients with arterial hypertension, if necessary, peripheral vasodilators should be used.


Adverse reactions


The following categories are used to classify the frequency of side effects: very common (≥ 1/10); common (≥1/100, <1/10); infrequent (≥1/1, 000, <1/100); rare (≥1/10, 000, <1/1, 000) very rare (<1/10, 000) frequency unknown (frequency cannot be calculated from available data).


On the part of the immune system.


The frequency is unknown hypersensitivity reactions (allergic and pseudoallergic) may occur. They can manifest as edema and / or inflammation at the injection site, as well as independently of the injection site in the form of redness of the skin, itching, conjunctivitis, rhinitis, facial edema such as angioedema, including edema of the upper and / or lower lip and / or cheeks, edema of the vocal cords with a feeling of a lump in the throat and difficulty swallowing, urticaria and difficulty breathing, which can turn into anaphylactic shock.


From the nervous system.


Often paresthesia, hypesthesia, headaches, caused mainly by the presence of epinephrine.


Infrequently: dizziness.


Frequency unknown:


When using too large doses of the drug or with accidental intravascular administration, there may be dose-dependent reactions from the central nervous system: anxiety, nervousness, stupor (which can sometimes progress to unconsciousness), coma, respiratory failure, which sometimes progresses to respiratory arrest, muscle tremor, involuntary muscle contractions, which sometimes progress to generalized convulsions.


The theoretical possibility of nerve damage exists during any dental interventions due to violations of the injection technique or due to the peculiarities of the anatomical structure of the injection site. In such cases, it is possible to damage the facial nerve and cause paresis of the facial nerve. This can lead to a decrease in taste sensitivity.


On the part of the visual organs.


The frequency is unknown: during the injection of a local anesthetic (or shortly after) in the head area, it is also possible to develop temporary visual impairment (blurred vision, double vision, mydriasis, blindness).


From the cardiovascular system.


Infrequently tachycardia.


The frequency is unknown: cardiac arrhythmias, increased blood pressure, hypotension, bradycardia, heart failure, and shock (which may be life-threatening).


From the gastrointestinal tract.


Often: nausea, vomiting.


Violation of the general condition and reaction at the site of administration of the drug.


The frequency is unknown: with unintentional intravascular injection, areas of ischemia may appear at the site of administration of the drug, sometimes progressing to the appearance of tissue necrosis (see the section "Method of administration and doses").


In the post-marketing period, cases of chills, mainly related to anxiety due to dental procedures, sweating, tinnitus, and mydriasis, were reported.

Special warnings.


In rare cases, especially in patients with bronchial asthma, the drug can cause hypersensitivity reactions due to the presence of sodium metabisulfite in its composition. These reactions can be clinically manifested by vomiting, diarrhea, shortness of breath, acute asthma attack, disorders of consciousness, or shock.


Methyl-4-hydroxybenzoate (Ph. Eur.) May cause allergic reactions (possibly delayed type), in isolated cases - bronchospasm.


Pediatric population.


According to the published research results, the safety profile in children aged 4 to 18 years was similar to the safety profile in adults. However, more often (up to 16% of children) there were accidental soft tissue injuries due to prolonged soft tissue anesthesia, especially in children aged 3 to 7 years. In a retrospective study that included 211 children aged 1 to 4 years, dental treatment was performed with up to 4.2 ml of the drugs ultracaine D-C or ultracaine D-C forte, with no reported side effects.

Tags: Ultracaine® [Articaine, Epinephrine]