Ultracaine® D (Ultracain® D)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceArticaineArticaine
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  • Ultracaine® D
    solution for injections 
    Sanofi-Aventis Deutschland GmbH     Germany
    • Dosage form: & nbspinjection
    Composition:In 1 ml of the drug contains the active substance: articaine hydrochloride - 40.0 mg;
    auxiliary substances: sodium chloride - 2.1 mg, water for injection - up to 1 ml.
    Description:Transparent colorless liquid.
    Pharmacotherapeutic group:local anesthetic
    ATX: & nbsp

    N.01.B.B.08   Articaine

    Pharmacodynamics:

    Artikain is an amine type local anesthetic used for infiltration and conduction anesthesia in dentistry.

    Artikain has a local anesthetic effect due to blockade of potential-dependent sodium channels in the cell membrane of neurons, which leads to reversible inhibition of conduction of impulses along the nerve fiber and reversible loss of sensitivity.

    The effect of the drug begins quickly, within 1-3 minutes. The duration of anesthesia is approximately 20 minutes. The drug Ultracaine® D does not contain epinephrine and is used when the addition of epinephrine to the topical anesthetic is not necessary or the use of epinephrine is contraindicated.

    Pharmacokinetics:

    Articaine quickly and almost immediately after administration 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 of articaine, articaine acid, does not have local anesthetic activity and systemic toxicity, which allows repeated injections of the drug.

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

    Articaine is excreted through kidney, mainly in the form of articaine acid. After submucosal administration period elimination half-life is approximately 25 minutes.

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

    Indications:

    Local anesthetic for infiltration and conduction anesthesia in dentistry.

    Artikain without epinephrine is used primarily for short procedures in patients in whom the use of epinephrine is unacceptable (for example, in cardiovascular diseases), or when small amounts of the drug are needed (in the region of the anterior teeth, palate).
    Contraindications:

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

    - Severe dysfunction of the sinus node or severe conduction disorders (such as severe bradycardia, atrioventricular block II-III degree).

    - Acute decompensated heart failure.

    - Severe arterial hypotension.

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

    Carefully:

    - Insufficiency of cholinesterase (application is possible only in case of emergency, since prolongation and pronounced increase in the action of the drug are possible);

    - Epilepsy in the anamnesis (see section "Side effect").

    Pregnancy and lactation:

    Pregnancy

    Artikain penetrates the placental barrier. The concentration of articaine in the serum in newborns (after the introduction of the mother drug) is approximately 30% of concentration of articaine in the mother's blood serum. In view of the lack of clinical decision to use preparation by a dentist can be taken only in the case, if the potential benefit from its application to the mother justifies the potential risk to the fetus.

    Breastfeeding period

    In the short term during the period of the breast breastfeeding, as a rule, not it is necessary to interrupt feeding breast, since in breast milk not found clinically significant concentrations of articaine.

    Fertility

    In fertility studies, rats, when using articaine in toxic doses, there was no effect on fertility in males and females. No effect on fertility in humans is expected with articaine 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 infiltrative anesthesia, in the absence of inflammation, 1.7 ml of Ultrakain® D solution per tooth or twoadjacent teeth.

    With conductor anesthesia of the lower alveolar nerve, approximately 1-1.7 ml of the drug solution is required. For additional injections, half the dose or the full dose should be used.

    The maximum dose for adults is 4 mg of articaine hydrochloride per kg of body weight.

    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 injection pressure during the administration of the drug should be adjusted depending on the tissue sensitivity.

    Side effects:

    The incidence of side effects is presented in accordance with the classification recommended by the World Health Organization: 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.

    Infrequently

    Dizziness.

    Frequency unknown

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

    Disorders from the gastrointestinal tract

    Often

    Nausea, vomiting.

    Violations from the heart and blood vessels

    Frequency unknown

    Reduction of blood pressure, bradycardia, heart failure, 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 edema 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.

    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 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 drop in blood pressure can be eliminated by simply moving the patient to a horizontal position with raised lower limbs.

    In severe circulatory disorders 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 of methylprednisolone), if necessary, plasma substitutes, including albumin.

    With the development of collapse and increased bradycardia showed a slow intravenous injection of epinephrine (0.0025-0.1 mg) under controlheart rate and blood pressure. 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.

    Interaction:

    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 action of local anesthetics and increase the risk of respiratory depression.

    With heparin, acetylsalicylic acid

    When carrying out injections of the drug Ultracaine® Patients receiving heparin or acetylsalicylic acid may develop bleeding at the injection site.

    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 vasoconstrictor

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

    Special instructions:

    The drug is not intended for long-term administration (more than 20 minutes).

    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 are required to monitor the condition of the cardiovascular system, respiratory system, CNS. Care should be taken when using the drug in patients with angina pectoris, atherosclerosis, blood clotting disorders, severe impairment of liver or kidney function.

    In order to avoid the risk of adverse reactions, it is necessary to use the minimum effective doses of the preparation and, prior to its introduction, a two-stage aspiration test should be performed.

    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 with teeth (biting) due to a 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.
    Effect on the ability to drive transp.cf. and fur:

    The decision on when a patient after dental surgery can return to driving or 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.

    Packaging:

    Ampoules: 2 ml per ampoule of clear, colorless glass (type 1). 10 ampoules are placed in a cardboard box together with instructions for use.

    Cartridges: 1.7 ml per cartridge transparent, colorless glass (type 1). For 10 cartridges are placed in a block of corrugated cardboard. For 1 or 10 blocks of corrugated cardboard is placed in a cardboard box together with an instruction for use.
    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children!

    Shelf life:

    5 years.

    Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-001358
    Date of registration:03.04.2011
    The owner of the registration certificate:Sanofi-Aventis Deutschland GmbHSanofi-Aventis Deutschland GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspSanofi Aventis GroupSanofi Aventis Group
    Information update date: & nbsp30.01.2015
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