Active substanceArticaine + EpinephrineArticaine + Epinephrine
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  • Dosage form: & nbspinjection
    Composition:

    At 1 ml solution:

    Active substances: articaine hydrochloride (in terms of 100% substance) 40.00 mg; epinephrine (in terms of 100% substance) 0.01 mg

    Excipients: sodium metabisulphite (sodium disulphite) 0.31 mg, glycine (in terms of 100% substance) 8.00 mg, sodium chloride 0.40 mg, 1 M solution of hydrochloric acid to pH 3.5, water for injection up to 1.0 ml.

    Description:Transparent colorless or slightly yellowish-greenish solution.
    Pharmacotherapeutic group:Local anesthetic + α- and β-adrenomimetic
    ATX: & nbsp

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

    Pharmacodynamics:

    Combined preparation of articaine (amniotic-type local anesthetic) and epinephrine (vasoconstrictor, epinephrine content in a 1: 100,000 solution), which is added to the formulation to prolong the duration of anesthesia. Articaine causes a reversible loss of sensitivity due to the cessation or reduction of sensory nerve impulses near the site of injection.Has a membrane-stabilizing effect by reducing the permeability of nerve cell membranes for sodium ions. Artifrin forte has a rapid (latent period of 1 to 3 min) and a strong anesthetic effect, has good tissue tolerance. The duration of anesthesia of tooth pulp is at least 75 minutes, the duration of anesthesia of soft tissues is not less than 120-240 minutes.

    Pharmacokinetics:

    After submucosal administration, 2 ml of Artifrin Fort preparation time to reach the maximum concentration of articaine in the blood (Tmax) is 10-15 minutes, the average value of the maximum concentration of articaine in the blood plasma (CmOh) is approximately 400 μg / l. Tmax The main metabolite of articaine - articine acid, is 45 min, CmOh - 2000 μg / l, as a result introduced articaine enters the systemic circulation mainly in the form of an inactive metabolite. The connection of articaine with plasma proteins is 95%. In children, comparable pharmacokinetic data were obtained.

    The concentration of articaine in the area of ​​dental alveoli after submucosal administration is thousands of times higher than the concentration of articaine in the systemic circulation.The inverse relationship between the time after injection and the concentration of articaine in the alveoli of the tooth is revealed.

    10% articaine metabolized in the liver, 90% of articaine is inactivated in tissues and blood by nonspecific plasma esterases by hydrolysis in the carboxyl group. The main metabolite articaine acid, formed as a result of hydrolysis, does not have local anesthetic activity and systemic toxicity. The total clearance of articaine after submucosal injection into the oral cavity is

    Excretion of articaine after submucosal administration occurs exponentially with a half-life (T1/2) about 25 minutes. Displayed articaine mainly through the kidneys in the form of artic acid (64.2 ± 14.4%), arkainic acid glucuronide (13.4 ± 5.0%) and unchanged articaine (1.45 ± 0.77%).

    Indications:

    Infiltration and conductive anesthesia during dental operations on the mucous membrane or bones, which require the creation of conditions for more severe ischemia; operations on the tooth pulp (amputation or extirpation), removal of a broken tooth (osteotomy) or tooth afflicted with apical periodontitis,prolonged surgical interventions (eg, Caldwell-Luke surgery), percutaneous osteosynthesis, excision of cysts, gingival mucosal interference, resection of the apex of the tooth root.

    Contraindications:

    - Intravenous introduction;

    - Hypersensitivity to articaine or other amido type local anesthetics, except in cases where hypersensitivity to amine type local anesthetics is known, an allergy to articaine has been ruled out by appropriate studies conducted in accordance with the necessary rules and requirements. Hypersensitivity to epinephrine; to sulfites (including manifested as bronchial asthma) and / or to other components of the drug;

    - Acute decompensated heart failure, severe dysfunction of the sinus node or conduction (pronounced bradycardia, atrioventricular block of 2-3 degrees), severe arterial hypertension or hypotension; paroxysmal tachycardia, tachyarrhythmia; reception of nonselective beta-blockers, for example, propranolol;

    - Closed-angle glaucoma;

    - Hyperthyroidism;

    - Pheochromocytoma;

    - Use in patients who had experienced acute myocardial infarction 3-6 months ago, coronary artery bypass grafting - 3 months ago;

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

    Carefully:

    Angina pectoris, atherosclerosis, postinfarction cardiosclerosis, cerebrovascular accident, stroke in the anemia, chronic bronchitis, pulmonary emphysema, diabetes mellitus, cholinesterase insufficiency (application is possible only in case of emergency, probably prolongation and excessive strengthening of the drug), bleeding disorders, severe violations of liver and kidney function, marked excitement, simultaneous use of MAO inhibitors or tricyclic antidepressants.

    Pregnancy and lactation:

    Artikain passes through the placental barrier in less quantity than other local anesthetics. Pre-clinical studies showed no toxic effects of articaine on the reproductive system, fertility and embryogenesis in rats and rabbits. Epinephrine-induced fetal anomalies in animals were observed when administered at doses significantly exceeding the maximum recommended in the formulation.Due to the lack of clinical data, the decision to prescribe the drug by a dentist can be made after a thorough assessment of the relationship of benefit to the mother and the risk to the fetus. If it is necessary to use pregnancy time, it is better to use articaine preparations without epinephrine or preparations with a lower concentration of epinephrine.

    The abolition of breastfeeding with short-term use of the drug, as a rule, is not required.

    Dosing and Administration:

    The drug is intended for use in the oral cavity and can be administered only in tissues in which there is no inflammation. Do not inject into inflamed tissues.

    When performing preliminary procedures and anesthesia, a constant verbal contact of the dentist with the patient is required (questioning the patient, clarifying the questions that appear as the patient complains of complaints and sensations).

    To prevent intravascular injection, an aspirate test (sample) is performed: before injecting the drug solution, the syringe piston must be pulled by itself. With a positive aspiration sample, you need to pull the needle, then re-push it forward.The injection pressure should correspond to the sensitivity of the tissue.

    When applying the drug for the first time, a skin test is performed: 0.02 ml of drug is intradermally injected and the local reaction is observed for 15 minutes. In the presence of severe hyperemia, pruritus and other intolerance, the use of the drug in this patient is contraindicated.

    With uncomplicated removal of the upper jaw teeth in the absence of inflammation, it is usually sufficient to create the Artifrin forte depot in the region of the transitional fold by inserting it into the submucosa from the vestibular side 1.7 ml per each tooth. In rare cases, in order to achieve complete anesthesia, additional administration of 1 to 1.7 ml of the drug may be required. In most cases this allows you not to carry a painful palatine injection.

    With incisions and suturing in the palate with the goal of creating a palatine depot, about 0.1 ml of the drug for each injection is needed.

    If you remove the premolars of the lower jaw in the absence of inflammation, you can avoid mandibular anesthesia, since infiltration anesthesia provided by injection of 1.7 ml per tooth is usually sufficient.If this is not the way 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.

    To prepare the cavity and prepare the teeth for the crowns, it is enough to inject 0.5 to 1.7 ml of the drug per tooth for the oral mucosa.

    During surgical interventions, Artifrin forte dosages individually depending on the severity and duration of the intervention. When performing one treatment procedure, adults can administer up to 7 mg of articaine per 1 kg of body weight. In clinical studies, patients well tolerated doses up to 500 mg (corresponding to 12.5 ml of the drug).

    Children older than 4 years of the drug is administered in doses, depending on the age, body weight and method of anesthesia. For children with a body weight of 20-30 kg, a dose of 0.25 ml to 1 ml is sufficient, for children with a body weight of 30-45 kg, from 0.5 ml to 2 ml. For children aged 4 to 12 years, the dose of the drug administered should not exceed 5 mg of articaine per 1 kg of body weight.

    In elderly patients and / or patients with severe and renal insufficiency, it is possible to create increased plasma concentrations of articaine, so these patients should be treated minimum doses necessary to achieve sufficient depth of anesthesia.

    Side effects:

    From the central nervous system: often - headache; rarely - dizziness, anxiety, nervousness, paresthesia; very rarely - hypoesthesia. Dose-dependent adverse reactions: rarely - stupor, progressing to loss of consciousness, coma, breathing disorders until it stops; muscular tremor, involuntary muscle twitching, generalized convulsions.

    If the correct injection technique is violated, the nerve, in particular the facial nerve, can be damaged by injecting the drug, which can lead to the development of its paralysis.

    From the side of the organ of vision: rarely - transient visual disorders (blurred vision, blindness, double vision, mydriasis) that occur during or shortly after the injection.

    From the gastrointestinal tract: infrequently - nausea, rarely - vomiting.

    From the cardiovascular system: seldom - moderately pronounced violations of hemodynamics, manifested in a decrease in blood pressure, bradycardia, heart failure, which in extreme manifestation can lead to life-threatening shock. Due to the content in the preparation of epinephrine, it is rarely possible to increase blood pressure, tachycardia.

    Allergic reactions: infrequently - edema or inflammation at the injection site, non-local reactions - skin flushing, itching, conjunctivitis, rhinitis, angioedema, of varying severity (may be manifested by edema of the upper and / or lower lip, cheeks, glottis with a sensation of "lump in the throat" and with difficulty swallowing, hives, difficulty breathing). All these phenomena can progress to the development of anaphylactic shock.

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

    Overdose:

    Symptoms: nausea, vomiting, agitation, motor anxiety, anxiety, muscle twitching, convulsions, respiratory failure, impaired consciousness, stupor,coma; violation of the heart rhythm (bradycardia or tachycardia), a sharp decrease or increase in blood pressure, circulatory disturbance, shock.

    At the first manifestations of the toxic effect of the drug, it is necessary to stop the injection and give the patient a horizontal position with raised lower limbs and provide airway patency. It is necessary to monitor the parameters of hemodynamics (number of heartbeats, blood pressure). It is always recommended, even if the symptoms of intoxication do not seem to be severe, to put an intravenous catheter in order, if necessary, to be able to immediately perform intravenous administration of the required medications.

    In the case of breathing disorders, depending on their severity, oxygen is recommended, if there is an indication for an artificial respiration, an endotracheal intubation and artificial ventilation of the lungs is recommended. The use of analeptic drugs of central action is contraindicated.

    In case of involuntary muscular twitching or generalized convulsions, intravenous administration of barbiturates of short or ultrashortactions. Introduction should be done slowly under constant monitoring of hemodynamic and respiratory parameters and with simultaneous feed of oxygen.

    Often a bradycardia or a sharp drop in blood pressure can be eliminated by giving the patient a horizontal position with raised legs. With severe circulatory disturbances and shock, regardless of their cause, injection of the drug should be stopped, provide the patient with a horizontal position with raised legs, oxygen inhalation and intravenous infusion of balanced electrolyte solutions, glucocorticosteroids (250-1000 mg methylprednisolone), if necessary plasma substitutes, albumin . With the development of circulatory collapse and increasing bradycardia, a slow intravenous injection of an epinephrine solution (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, the infusion rate should correlate with the heart rate and blood pressure level.

    Severe tachycardias and tachyarrhythmias can be stopped by the administration of antiarrhythmic drugs, with the exception of nonselective beta-blockers.

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

    Interaction:

    Appointment of the drug on the background of treatment with non-cardioselective beta-blockers, for example propranolol, is contraindicated, since in this case the risk of hypertensive crisis and severe bradycardia is high.

    The hypertensive effect of epinephrine can be enhanced by tricyclic antidepressants and monoamine oxidase 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 Artifrin forte is lower than indicated (1: 100,000), however, the possibility of increasing its hypertensive effect should be taken into account.

    With the simultaneous use of antithrombotic agents (heparin, acetylsalicylic acid) accidental puncture of the vessel during local anesthesia can cause bleeding at the injection site.

    When used simultaneously with cholinesterase inhibitors, the metabolism of articaine slows down.

    Epinephrine can inhibit the secretion of insulin by the pancreas, thereby reducing the effectiveness of oral antidiabetic drugs.

    Some means for inhalation anesthesia (for example, halothane) can increase the sensitivity of the myocardium to catecholamines and the risk of arrhythmia after the injection of Artifrin forte.

    When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing local reactions - edema, tenderness - increases.

    Special instructions:

    The drug is intended for use only for local anesthesia in dentistry. The drug can not be administered intravenously, and also into the inflamed area! To avoid intravascular injection, an aspiration test is mandatory.

    To prevent infection (including viral hepatitis), when taking a solution from an ampoule, new sterile syringes and needles should always be used. Open cartridges can not be reused for other patients, nor can a damaged cartridge be used.

    In patients with diseases of the cardiovascular system (chronic heart failure, arteriosclerosis, exertional angina,cardiac arrhythmias, myocardial infarction, arterial hypertension), cerebrovascular disorders, a history of stroke, chronic bronchitis, emphysema, diabetes, hyperthyroidism, and also when the patient expressed concern, it is advisable to use a combination of drugs articaine with fewer epinephrine or containing epinephrine.

    With careful use of the drug in patients with a history of epilepsy, as well as in patients with blood clotting disorders and severe liver or kidney functions.

    In each case of anesthesia, the minimum doses of the drug necessary to achieve sufficient depth of anesthesia should be used.

    1 ml of the drug contains 0.232 mg of sodium.

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

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

    In special tests, there was no clear effect of the drug on operator activity. However, due to the fact that preoperative anxiety of the patient and the stress caused by surgery, can affect the efficiency,the dentist should individually, in each case, decide on the admission of the patient to the management of transport or work with mechanisms.

    Form release / dosage:

    Solution for injection (40 mg + 0.01 mg) / ml.

    Packaging:By 1.7 ml in the cartridges.

    10 cartridges per circuit cell packaging made of polyvinylchloride film and flexible packaging on the basis of aluminum foil or paper with a polymer coating, or paper laminated.

    1 or 5 circuit cells per 10 cartridges, together with instructions for use, are placed in a pack of cardboard.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000626/10
    Date of registration:03.02.2010 / 27.12.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:HEALTH PHARMACEUTICAL COMPANY, LTD. HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine
    Manufacturer: & nbsp
    Information update date: & nbsp25.09.2017
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