Articaine with adrenaline forte, 40 mg/ml+0.01mg/ml 2 ml 10 pcs

Pharmacotherapeutic group: Local anesthetic + alpha- and beta-adrenomimetic

ATC code: N01BB58

Pharmacodynamics:

Articaine with adrenaline forte used for infiltration and conduction anesthesia in dentistry is a combination drug that includes articaine (an amide type local anesthetic) and epinephrine (a vasoconstrictor) which is added to the drug to prolong anesthesia.

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

Articaine with adrenaline forte has a rapid (latency period – 1 to 3 min) and strong anesthetic effect and has good tissue tolerance. The duration of effective anesthesia including intrapulpal anesthesia is at least 75 minutes the duration of soft tissue anesthesia is from 120 to 240 minutes.

In children

Published studies have shown that in children aged 35 to 16 years, use of the drug at a dose of 7 mg articaine per 1 kg of body weight provided sufficient local anesthetic effect in mandibular infiltration

or maxillary conduction anesthesia. Duration of anesthesia was comparable in all age groups and depended on the volume of the drug administered.

Pharmacokinetics:

The blood plasma protein binding of articaine is approximately 95%. With oral submucosal injection the half-life of articaine is 253 ± 33 min.

Articaine is metabolized rapidly and almost immediately after administration through hydrolysis by non-specific plasma esterases of blood and tissues (90%). Up to 10% of articaine is metabolized in the liver. The resulting main metabolite of articaine – articoic acid – has no local anesthetic activity and systemic toxicity, which allows repeated administration of the drug. Articaine is excreted by the kidneys mainly in the form of articicic acid.

In children, the overall effect in vestibular infiltration anesthesia is comparable to that in adults, however, the maximum concentration of articaine in the blood plasma is reached faster.

Indications

The drug Articaine with adrenaline forte is indicated for local anesthesia (infiltration and conduction anesthesia) in dentistry in traumatic interventions and when pronounced hemostasis or improved visualization of the operating field is required:

– dental operations on the mucosa or bones requiring the creation of conditions of more pronounced ischemia;

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

– removal of a broken tooth (osteotomy) or a tooth affected by apical periodontitis;

Long-term surgical interventions;

Percutaneous osteosynthesis;

– Excision of cysts;

– interventions on the gum mucosa;

– resection of the apex of the tooth root.

Active ingredient

Articaine, Epinephrine

Composition

1 ml of the solution contains:

the active substances:

articaine hydrochloride (in terms of 100% substance) – 40 mg,

epinephrine hydrotartrate (in terms of 100% substance) – 0.018 mg (in terms of epinephrine – 0.010 mg, which corresponds to the content of epinephrine in the solution 1:100 000);

excipients: sodium disulfite – 0.50 mg, sodium chloride – 1.00 mg, water for injection up to 1 ml.

How to take, the dosage

The drug can only be injected into uninflamed tissues.

The product is not to be administered intravenously!

The product is intended to be used in the oral cavity.

In order to avoid accidental ingestion of the drug into the blood vessels, a two-step aspiration test with a 90 and 180° needle rotation should always be performed before administering it.

The main systemic reactions that may develop as a result of accidental intravascular injection of the drug can be avoided by observing the injection technique: after the aspiration test slowly inject 01 – 02 ml of the drug then not earlier than 20 – 30 seconds slowly inject the remaining dose of the drug. The injection pressure should be consistent with the sensitivity of the tissues.

In order to prevent infection (including hepatitis virus), care must be taken to ensure that new sterile syringes and needles are always used when taking the drug from the ampoules.

The opened cartridges must not be reused for other patients (risk of hepatitis infection)!

Damaged cartridges should not be used.

The medication should not be used if it has changed color or become cloudy.

Dosing regimen

Anesthesia in uncomplicated maxillary tooth extraction in the absence of inflammation usually requires sufficient depotting of Artikaine with adrenaline forte in the transition fold by injection into the submucosa on the vestibular side (17 ml of the drug per tooth). In some cases additional injection of 1 ml to 17 ml may be required to achieve complete anesthesia. In most cases this allows to avoid a painful palatal injection.

Anesthesia for incisions and sutures in the palatal area to create a palatal depot requires about 01 ml of the drug per injection.

If several adjacent teeth are extracted, the number of injections can usually be limited.

In the case of mandibular premolars where there is no inflammation, an injection of 17 ml per tooth is generally sufficient. If this does not achieve the desired effect, an additional injection of 1-17 ml of anesthetic should be given into the submucosa in the area of the transition fold of the lower jaw on the vestibular side.

If full anesthesia cannot still be achieved in this case, a guided blockade of the mandibular nerve must be performed.

In surgical interventions, depending on their severity and duration, the drug Artikaine with adrenaline forte is dosed individually.

In a single treatment procedure in adults, up to 7 mg of articaine per 1 kg of body weight can be administered. Patients have been observed to tolerate doses up to 500 mg (corresponding to 125 ml of the drug) well.

Elderly patients and patients with severe renal and hepatic impairment

In elderly patients and all patients with severe renal and hepatic impairment, elevated plasma concentrations of articaine may occur. For these patients the minimum doses necessary to achieve sufficient depth of anesthesia should be used.

Children

In pediatric patients (over 4 years of age), the minimum doses necessary to achieve adequate anesthesia should be used. The dose of Articaine with Adrenaline Forte is adjusted according to the child’s age and body weight but must not exceed 7 mg articaine per 1 kg of body weight (0175 ml/kg). The use of the drug in children younger than 1 year old has not been studied.

Interaction

Combinations of different local anesthetics cause additional cardiovascular and central nervous system effects.

Contraindicated combinations

With non-selective beta-adrenoblockers such as propranololol

Risk of hypertensive crisis and marked bradycardia.

Interactions to be taken into consideration

With tricyclic antidepressants or monoamine oxidase inhibitors (MAOIs)

The effects of vasoconstrictors (adrenomimetics) that increase blood pressure, such as epinephrine, may be enhanced by tricyclic antidepressants or MAO inhibitors. Similar observations have been described for norepinephrine concentrations of 1:25,000 and epinephrine concentrations of 1:80,000 when used as vasoconstrictors. Although the concentration of epinephrine in Articaine with epinephrine forte is significantly lower (1:100,000), the possibility of enhancing the hypertensive effects of epinephrine should nevertheless be considered.

With drugs depressing the central nervous system Local anesthetic agents increase the effect of drugs depressing the central nervous system. Narcotic analgesics increase the effect of local anesthetic agents, but increase the risk of respiratory depression.

With anticoagulants and other drugs that reduce blood clotting

Injections of Artikaine with adrenaline forte in patients receiving, for example, heparin or acetylsalicylic acid may cause bleeding at the injection site.

With cholinesterase inhibitors

Cholinesterase inhibitors decrease the metabolism of local anesthetic drugs, which may result in prolongation and pronounced enhancement of the effects of articaine.

With oral hypoglycemic agents

Epinephrine may inhibit insulin release from pancreatic beta cells and reduce the effects of oral hypoglycemic agents.

With some agents for inhalation anesthesia (halothane)

Halothane may increase myocardial sensitivity to catecholamines and increase the risk of cardiac rhythm disturbances after injections of Articaine with Adrenaline Forte.

With disinfectant solutions containing heavy metals

The treatment of the injection site of local anesthetic with disinfectant solutions containing heavy metals increases the risk of local reactions – swelling of soreness.

Special Instructions

Anesthesia must be administered by experienced personnel in an appropriately equipped room with immediately available equipment and medications for cardiac monitoring and resuscitation. Personnel performing anesthesia must be qualified and trained in anesthesia techniques and be familiar with the diagnosis and management of systemic toxic reactions, adverse events and reactions and other complications.

Only with a strict indication should the drug be used in patients with cholinesterase deficiency, as prolongation and under certain circumstances enhancement of its action is possible.

Particin with adrenaline forte should be used with particular caution in patients with blood clotting disorders with severe renal or hepatic impairment when used together with halogenated inhaled narcotics (see section “Interaction with other drugs”) with a history of epilepsy.

. In patients with cardiovascular disease (chronic heart failure coronary heart disease stenocardia myocardial infarction in a history of heart rhythm disorders arterial hypertension) atherosclerosis cerebrovascular failure stroke in a history of chronic bronchitis pulmonary emphysema diabetes mellitus severe forms of anxiety neurosis it is appropriate to use preparations containing no epinephrine or with epinephrine concentration 0005 mg/ml.

The injection should not be given in an inflamed area.

Before administering the drug, inquire about the patient’s history and current concomitant drug therapy. The physician should maintain verbal contact with the patient and administer a test dose of 5% or 10% of the estimated dose if there is a risk of allergy.

The following conditions must be followed to avoid adverse events:

– choose the minimum doses necessary to achieve sufficient depth of anesthesia;

– a two-plane aspiration test should be performed before injection (to avoid accidental intravascular injection).

It is not recommended to eat until the local anesthesia has ceased (recovery of sensitivity).

Please note that 1 ml of the drug contains less than 1 mmol (23 mg) of sodium. The drug is intended for use in dentistry. It should not be used for anesthesia of the distal extremities (risk of ischemia due to epinephrine in the drug).

Children

Parents (caregivers) of young children need to watch out for soft tissue injuries caused by biting (biting) due to the long-term de-sensitization of the tissue caused by the drug.

Effects on driving ability:

The use of Articaine with Adrenaline Forte does not cause any noticeable deviation from normal driving ability. However, the decision as to when the patient can return to driving and engaging in other potentially hazardous activities requiring increased concentration and quick psychomotor reactions should be made by the physician after the dental intervention.

Contraindications

Hypersensitivity to articaine or other local anesthetic agents of the amide type epinephrine sulfites (in particular in patients with bronchial asthma with hypersensitivity to sulfites as acute allergic reactions with anaphylactic shock symptoms such as bronchospasm are possible) or to any of the other excipients of the drug.

Persistent contraindications due to the presence of articaine in the product

Severe sinus node dysfunction or severe conduction disorders (e.g., severe bradycardia atrioventricular block of grade II or III);

– acute decompensated heart failure;

– severe arterial hypotension;

– children under 4 years of age (insufficient clinical experience).

Contraindications due to the presence of epinephrine in the drug

– Closed angle glaucoma;

– hyperthyroidism;

– paroxysmal tachyarrhythmia;

– recent myocardial infarction (within 6 months);

p> – recent aortocoronary bypass surgery (up to 3 months);

– taking non-selective beta-adrenoblockers such as propranololol (risk of hypertensive crisis and severe bradycardia);

Pheochromocytoma;

Severe arterial hypertension.

Cautions: – In patients with chronic heart failure coronary heart disease angina atherosclerosis myocardial infarction in a history of cardiac rhythm disorders arterial hypertension;

– In patients with a history of cerebrovascular disorders stroke;

Patients with chronic bronchitis pulmonary emphysema;

Patients with diabetes (potential risk of changes in blood glucose concentration);

– In patients with cholinesterase deficiency (use only if absolutely necessary, as prolongation and marked potentiation of the drug may occur);

– In patients with blood clotting disorders;

– patients with severe hepatic or renal impairment;

– in patients with severe agitation;

– in patients with a history of epilepsy;

– when combined with halogen-containing agents during inhalational anesthesia (see “Interaction with other agents”).

In co-administration with halogen-containing drugs during inhalation anesthesia (see section “Interaction with other medicinal products”).

Side effects

The incidence of side effects is presented according to the classification recommended by the World Health Organization: very common (≥ 1/10); common (≥ 1/100 < 1/10); infrequent (≥ 1/1000 < 1/100); rare (≥ 1/10000 < 1/1000); very rare (< 1/10000) including individual reports; frequency unknown (cannot be determined from available data).

Particular system disorders

Frequency unknown

Allergic or allergy-like reactions. Can manifest as swelling and/or inflammation at the injection site, but can also occur regardless of the injection site and can be manifested as redness of the skin itching conjunctivitis rhinitis angioedema of the face with swelling of the upper and/or lower lip cheeks swelling of the throat with a “lump in the throat” feeling and difficulty in swallowing urticaria and difficulty in breathing which can go as far as anaphylactic shock.

Central nervous system disorders

Often

Paresthesia hypoesthesia headache (due to the presence of epinephrine in the drug).

Infrequent

Dizziness.

Frequency unknown

– Dose-dependent central nervous system reactions (including at excessively high doses or after accidental intravascular injection): anxiety feeling nervousness stupor mental confusion up to loss of consciousness coma respiratory disorders up to respiratory arrest muscle tremor and twitching of muscles up to generalized convulsions;

– if the correct technique of drug administration is violated or due to anatomical features in the injection area, damage of the facial nerve is possible which can lead to paralysis of the facial nerve and reduction of taste sensation.

Visual disturbances

Prevalence unknown

Visual disturbances (blurred vision mydriasis blindness double vision) are usually reversible and occur during or shortly after injection of the local anesthetic agent.

Heart and vascular disorders

Infrequent

Tachycardia.

Prevalence unknown

Heart rhythm disorders increased blood pressure arterial hypotension bradycardia heart failure and shock.

Gastrointestinal disorders

Often

Nausea vomiting.

General disorders and disorders at the site of administration

Area of unknown frequency

In some cases accidental intravascular administration may cause areas of ischemia at the site of administration up to and including tissue necrosis (see “Dosage and administration” section).

Children

The safety profile in children and adolescents aged 4 to 18 years is similar to that of adults in published studies. However, accidental oral soft tissue injuries are more common in children (up to 16% of children) especially between the ages of 3 and 7 years (due to longer duration of soft tissue anesthesia). There is evidence of a retrospective study of children aged 1 to 4 years in which dental interventions were performed using preparations containing 40 mg/ml artikaine + 001 mg/ml epinephrine in a dose of up to 42 ml. No adverse effects were reported from this study.

Overdose

Symptoms of overdose

Central nervous system disorders

Anxiety of the central nervous system: anxiety fear confusion hyperpnea tachycardia increased blood pressure with facial flushing nausea vomiting tremors twitching tonic-clonic convulsions.

Central nervous system depression: dizziness hearing impairment loss of ability to speak stupor unconsciousness atonia vasomotor nerve paralysis (weakness pallor) dyspnea death from respiratory paralysis.

Cardiovascular system disorders

Bradycardia arrhythmia ventricular fibrillation drop in blood pressure cyanosis cardiac arrest.

Treatment

At the first signs of intoxication or adverse effects of the drug, such as dizziness, motor agitation, or stupor during drug administration, discontinue the administration and place the patient in a horizontal position with the lower extremities elevated. Airway patency should be ensured and hemodynamic parameters (heart rate and blood pressure) should be monitored. It is always recommended that, even if symptoms of intoxication appear to be mild, access to veins be made available, so that the necessary medications can be administered immediately, if necessary.

In respiratory disorders, depending on their severity, the administration of oxygen is recommended, and if artificial respiration is indicated, endotracheal intubation and artificial lung ventilation.

Muscular twitching and generalized convulsions may be relieved by intravenous administration of a rapid-acting muscle spasm reliever (e.g., diazepam suxamethonium chloride). Artificial respiration (oxygen supply) is also recommended.

In severe circulatory disorders and shock, regardless of their cause, the drug administration should be stopped and the patient should be transferred to a horizontal position with the lower extremities elevated. Oxygen supply should be given intravenous administration of electrolyte solutions of glucocorticosteroids (e.g. 250 – 1000 mg prednisolone or an equivalent amount of its derivative such as methylprednisolone) replacement infusion therapy (if necessary, additional plasma substitutes such as human albumin).

In case of collapse and increased bradycardia intravenous epinephrine (adrenaline) is administered immediately. After diluting 1 ml of 01% epinephrine solution (1:1000) to 10 ml using the resulting 001% epinephrine solution (1:10000), slowly administer 025 – 1 ml (0025 – 01 mg epinephrine) intravenously, controlling the heart rate and blood pressure (caution: possible cardiac arrhythmias!).

Do not exceed the single dose for intravenous administration of 01 mg of epinephrine. If it is necessary to administer doses exceeding 01 mg epinephrine should be administered by infusion adjusting the rate of administration under control of the number of heartbeats and blood pressure.

Severe tachycardia and tachyarrhythmia can be treated with antiarrhythmic agents excluding non-selective beta-adrenoblockers such as propranolol. Oxygen supply and hemodynamic monitoring are necessary in these cases. Increased blood pressure in patients with arterial hypertension is relieved with peripheral vasodilators if necessary.

Pregnancy use

Pregnancy

Articaine and epinephrine penetrate the placental barrier.

The serum concentration of articaine in newborns (after maternal administration) is approximately 30% of the maternal serum concentration of articaine.

In view of the lack of clinical data, the decision to use the drug by the dentist can only be made if the potential benefit to the mother justifies the potential risk to the fetus. If it is necessary to use articaine during pregnancy, it is better to use preparations containing no epinephrine or with an epinephrine concentration of 0005 mg/ml.

In accidental intravascular administration, epinephrine may decrease the blood supply to the uterus.

Breastfeeding period

Breastfeeding usually does not need to be interrupted when the drug is used for short-term use during breastfeeding because no clinically significant concentrations of articaine and epinephrine are detected in breast milk.

Fertility

Experimental studies of articaine 40 mg/ml + epinephrine 001 mg/ml in animals have shown no effect on fertility in male and female individuals. There were no adverse effects of the drug on human fertility when used in therapeutic doses.

Similarities

Ultracaine D-S, Ultracaine D-S Forte