Ultracaine D-C Fort - instructions for use, dose, side effects, contraindications

Composition:In 1 ml of solution contains:

active substances: articaine hydrochloride - 40 mg and epinephrine hydrochloride-0.012 mg (equivalent to epinephrine base content - 0.010 mg, which corresponds to the epinephrine content in the solution of 1: 100,000);

auxiliary substances: sodium disulfite (sodium metabisulphite), sodium chloride, water for injection.

Description:Transparent colorless liquid.

Pharmacotherapeutic group:local anesthetic + α- and β-adrenomimetic

ATX: & nbsp

N.01.B.B.58 Articaine in combination with other drugs

Pharmacodynamics:

The drug Ultracaine® D-S forte, used for local infiltration and conduction anesthesia in dentistry, is a combined preparation that includes articaine (amine type local anesthetic) and epinephrine (adrenaline) (a vasoconstrictor). Epinephrine is added to composition of the drug for prolonging the action of anesthesia. Articaine has a local anesthetic effect due to the blockade of potential-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 Ultracaine® D-S forte has a fast (latent period - from 1 to 3 min) and a strong anesthetic effect and has good tissue tolerance. The duration of anesthesia is at least 75 minutes.

Children

In a clinical study involving 210 children aged 3.5 to 16 years, the use of the drug Ultracaine® D-S forte in a dose of 7 mg / kg of body weight provided sufficient local anesthetic effect when mandibular infiltration or maxillary conduction anesthesia. The duration of anesthesia was comparable in all age groups and depended on the administered volume of the drug.

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 concentrations of articaine in the blood in the area of the alveoli of the tooth after submucosal administration are hundreds of times higher than the concentrations of articaine in the systemic blood stream.

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 period of 1 yule of clearance is approximately 25 minutes.

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

Indications:

Indicated for local anesthesia (infiltration and conduction anesthesia) in dentistry with traumatic interventions and if necessary expressed hemostasis or improve visualization of the operating field: dental operations on the mucosa or bones, requiring the creation of conditions for more severe ischemia; operations on the pulp of the tooth (amputation or extirpation); removal of a broken tooth (osteotomy) or a tooth afflicted with apical periodontitis; prolonged surgical interventions; percutaneous osteosynthesis; excision of cysts; interference on the gingival mucosa; resection of the apex of the tooth root.

Contraindications:

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

Hypersensitivity to epinephrine.

Hypersensitivity to sulfites (in particular, in patients with bronchial asthma and hypersensitivity to sulfites, as possible 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 conduction disorders (such as severe bradycardia, atrioventricular blockage of the 2nd or 3rd degree).

Acute decompensated heart failure.

Severe arterial hypotension.

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

Contraindications related to epinephrine

Paroxysmal tachycardia, tachyarrhythmia.

Recently suffered (3-6 months ago) myocardial infarction.

A recent coronary artery bypass graft (3 months ago).

Simultaneous reception of non-cardioselective beta-blockers, for example, propranolol (risk of hypertensive crisis and severe bradycardia).

Closed-angle glaucoma.

Hyperthyroidism.

Pheochromocytoma.

Severe hypertension.

Carefully:

In patients with chronic heart failure, coronary heart disease, angina pectoris, atherosclerosis, myocardial infarction in history, heart rhythm disorders, arterial hypertension.

In patients with cerebrovascular disorders, a history of stroke.

In patients with chronic bronchitis, emphysema of the lungs.

In patients with diabetes mellitus (a potential risk of changes in the concentration of glucose in the blood).

In patients with cholinesterase deficiency (use is possible only in case of emergency, as prolongation is possible and the effect of the drug is clearly enhanced).

In patients with bleeding disorders.

In patients with severe impairment of liver and kidney function.

In patients with severe arousal.

In patients with epilepsy in history.

When combined with halogen-containing agents for inhalation anesthesia (see section "Interaction with drugs").

Pregnancy and lactation:

Pregnancy

Articaine and epinephrine penetrate through 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.

Due to 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. If it is necessary to use articaine during pregnancy, it is better to use drugs that do not contain epinephrine or with a lower concentration of epinephrine (that is, preparations of Ultracaine® D and Ultracaine® D-C). In case of accidental intravascular injection epinephrine can reduce blood supply to the uterus. 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 and epinephrine.

Fertility

Studies on animals using articaine 40 mg / ml and epinephrine 0.01 mg / ml showed no effect on fertility in males and females. It is not expected that human fertility will be affected by the use of articaine and epinephrine 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 order to avoid accidental ingestion of the drug into blood vessels, an aspirate test (in two steps) should always be performed before it is administered. The main systemic reactions that can develop as a result of a random intravascular injection of the drug can be avoided by observing the technique of injection: after the aspiration test, slowly inject 0.1-0.2 ml of the drug, then the remaining dose of the drug is slowly introduced after 20-30 seconds. The injection pressure should correspond to the sensitivity of the tissues. For anesthesia with uncomplicated removal of the upper jaw teeth in the absence of inflammation, it is usually sufficient to create a drug depot

Ultracaine® D-C forte in the region of the transitional fold by inserting it into the submucosa from the vestibular side (1.7 ml 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 out a painful palatine injection. When several adjacent teeth are removed, the number of injections is usually limited.

For anesthesia in the incision and suturing in the palate with the goal of creating a palatine depot, it is necessary about 0.1 ml of the preparation for each injection.

In the case of removal of premolars of the lower jaw in the absence of inflammation, you can do without mandibular anesthesia, since infiltration is usually sufficient anesthesia provided by injection of 1.7 ml per tooth. If this is not the way to achieve the desired effect,an additional injection of 1-1.7 ml of anesthetic should be performed in the submucosa 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 drug Ultracaine® D-S forte, depending on the severity and duration of the intervention, is dosed individually.

When performing one treatment procedure, adults can enter 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).

For patients of child age (over 4 years), the minimum doses necessary to achieve adequate anesthesia should be used. The dose of Ultrakaink D-C Fort 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 younger than 1 year 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 needed to achieve sufficient depth of anesthesia should be used.

Side effects:

The incidence of adverse events listed below was determined according to the following gradation: 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; headache, mainly due to the presence of epinephrine in the formulation.

Infrequently

Dizziness.

Frequency unknown

Dose-dependent reactions from the central nervous system: agitation, nervousness, stupor, sometimes progressing to loss of consciousness, coma, respiratory disorders, sometimes progressing to a stop in 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, mydriasis, blindness, double vision), usually reversible and occurring during or shortly after injection of a local anesthetic.

Disorders from the gastrointestinal tract

Often

Nausea, vomiting.

Violations from the heart and blood vessels

Infrequently

Due to the content of epinephrine in the formulation, it is very rare to develop tachycardia, heart rhythm disturbances, increase blood pressure.

Frequency unknown

Reduced blood pressure, bradycardia, heart failure and 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 swelling 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.

General disorders and disorders at the site of administration

Frequency unknown

In some cases, with occasional intravascular injection, ischemic zones may occur at the site of administration, up to tissue necrosis.

Children

In the 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 soft tissues of the oral cavity, soft tissue damage was more frequent in children (in 16% of children), especially in the age of 3-7 beds. In a retrospective study in 211 children aged 1 to 4 years, dental interventions performed using 4.2 ml of 4% articaine and 0.01 mg / ml epinephrine did not cause adverse reactions.

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 introduction of central action 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 administer these drugs slowly under the constant supervision of a doctor (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 placed in a horizontal position with raised lower limbs. There should be oxygen supply, intravenous electrolyte solutions, glucocorticosteroids (250-1000 mg methylprednisolone), if necessary plasma substitutes, albumin.

With the development of circulatory collapse and increased bradycardia, a slow intravenous injection of a solution 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 infusion, adjusting the rate of administration under the control of the number of heartbeats and blood pressure.

Severe tachycardias and tachyarrhythmias can be stopped by the administration of antiarrhythmic drugs, with the exception of cardioselective beta-blockers (see section "Contraindications").

Increased blood pressure in patients with arterial hypertension, if necessary, should be reduced with the help of vasodilators.

Interaction:

Contraindicated combinations

With non-cardioselective beta-blockers, for example, propranolol

Risk of developing a hypertensive crisis and severe bradycardia.

Interaction, which should be taken into account

With tricyclic antidepressants or monoamine oxidase (MAO) inhibitors,

The action of vasoconstrictors (adrenomimetics), increasing blood pressure, for example, epinephrine, may be enhanced by 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. Although the concentration of epinephrine in the drug Ultrakain® D-S forte is much lower (1: 100000), nevertheless, the possibility of increasing the hypertensive effect of epinephrine should be considered.

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 effect of local anesthetics, but increase the risk of respiratory depression.

With heparin, acetylsalicylic acid

When carrying out injections of the drug Ultracaine® For patients receiving heparin or acetylsalicylic acid, development of bleeding at the injection site is possible.

With cholinesterase inhibitors

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

With hypoglycemic agents for oral administration

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

With some means for inhalation anesthesia (halothane)

Halothane can increase the sensitivity of the myocardium to catecholamines and increase the risk of heart rhythm disturbances after injections of the drug Ultracaine® Д-С forte.

With disinfecting solutions containing heavy metals

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.

Special instructions:

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.

Open cartridges can not be reused 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, arterial hypertension), atherosclerosis, cerebrovascular disorders, history of history of chronic bronchitis, emphysema, diabetes mellitus, hyperthyroidism, as well as in the presence of severe anxiety, it is advisable to use drugs Ultracaine® D, not containing epinephrine, or Ultracaine® D-S, hack as compared to the drug Ultracaine® D-S forte it contains smaller doses of epinephrine.

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

In order to avoid the risk of adverse reactions, the minimum effective doses of the drug should be used and, before the administration of the drug, a two-stage aspiration test should be performed (see Fig.See section "Dosing and Administration").

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 by teeth (biting) due to a prolonged 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.

The drug is intended for use in dentistry. The use of distal limbs for anesthesia is unacceptable (the risk of developing ischemia due to epinephrine).

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

The decision on when a patient after dental surgery can return to driving and 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 + 0.010 mg / 1 ml.

Packaging:Solution for injection 40 mg / ml + 0.010 mg / 1 ml, in ampoules of 2 ml and cartridges of 1.7 ml. Ampoules: 2 ml per ampoule of clear, colorless glass (type I).10 ampoules are placed in a cardboard box together with instructions for use.

Cartridges: 1.7 ml per cartridge transparent, colorless glass (type I). For 10 cartridges are placed in a block of corrugated cardboard. 10 blocks of corrugated cardboard are placed in a cardboard box together with instructions for use.

Storage conditions:Ampoules. At a temperature of no higher than 25 ° C in a dark place.

Cartridges. At a temperature of no higher than 30 ° C in a dark place.

Keep the drug out of the reach of children.

List B.

Shelf life:Ampoules - 36 months. Cartridges - 30 months.

After the expiration date, the drug can not be used.

Terms of leave from pharmacies:On prescription

Registration number:П N015117 / 01

Date of registration:13.08.2008

The owner of the registration certificate:Sanofi-Aventis Deutschland GmbHSanofi-Aventis Deutschland GmbH Germany

Manufacturer: & nbsp

SANOFI-AVENTIS Deutschland, GmbH Germany

Representation: & nbspSanofi Russia, JSCSanofi Russia, JSCRussia

Information update date: & nbsp10.03.2015

Illustrated instructions

Instructions

Ultrakain® D-C Fort (Ultracain® D-S forte)