Orelk - instructions for use, doses, side effects, contraindications

Sparrow (articaine with epinephrine) is a combined preparation for infiltration and conduction anesthesia in dentistry. Included in its composition articaine - local anesthetic of the amide type of the thiafen group. Epinephrine causes vasoconstriction, especially at the injection site, which makes it difficult to absorb and prolongs the effect. The drug has a local anesthetic effect, has analgesic effect. The drug is characterized by good tolerability and minimal vasoconstrictive effect. The effect of the drug begins quickly - after 0.5-3 minutes. The duration of anesthesia is at least 45 minutes for 40 mg / ml + 5 μg / ml and not less than 75 minutes for 40 mg / ml Spray + 10 μg / ml. The mechanism of action of articaine is based on the suppression of conductivity in nerve fibers, due to the blockade of potential-dependent sodium channels in the cell membrane. Due to the low content of epinephrine in the preparation, its effect on the cardiovascular system is poorly expressed: almost no increase in blood pressure and an increase in heart rate. In connection with which it is possible to use the Spray 40 mg / ml + 5 μg / ml in patients with cardiovascular diseases.

Pharmacokinetics:

Artikain with submucosal introduction in the oral cavity has a high diffuse capacity. Binding to plasma proteins is 95%. Active substances penetrate to the minimum degree through the placental barrier, practically do not stand out from breast milk. The half-life of articaine with submucous administration is 25 minutes.

Indications:

Medicinal preparation Sparrow is indicated for local anesthesia (infiltration and conduction anesthesia) in dentistry:

In the concentration of articaine 40 mg / ml and epinephrine 5 μg / ml with planned interventions such as uncomplicated removal of one or more teeth, carious cavity treatment, teeth grinding before prosthesis.

In the concentration of articaine 40 mg / ml and epinephrine 10 μg / ml with traumatic interventions and if necessary expressed hemostasis or improve visualization of the operating field:

- dental operations on the mucous membrane or bones, requiring the creation of conditions for more severe ischemia;

- operations on the tooth pulp (amputation and 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; sulfites (including, manifested in the form of bronchial asthma); hypersensitivity to any other auxiliary ingredients of the drug.

Contraindications related to articaine

Severe dysfunction of the sinus node or severe conduction disorders (such as severe bradycardia, atrioventricular blockage of 2-3 degrees).

Acute decompensated heart failure.

Acute arterial hypotension.

Anemia (including B-12 deficiency anemia).

Methemoglobinemia.

Hypoxia.

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

Contraindications related to epinephrine

Paroxysmal tachycardia, tachyarrhythmia, angle-closure glaucoma,

The use of non-cardioselective beta-blockers, for example, propranolol (risk of developing hypertensive crisis and severe bradycardia).

Hyperthyroidism.

Pheochromocytoma.

Severe hypertension.

Postponed myocardial infarction within the last 3-6 months.

Aortocoronary bypass surgery within the last 3 months. simultaneous use of tricyclic antidepressants and monoamine oxidase inhibitors (up to 14 days after withdrawal).

Carefully:In patients with angina, atherosclerosis, previous myocardial infarction, cerebrovascular disease, a history of stroke, chronic bronchitis, emphysema, diabetes, cholinesterase insufficiency (application only possible if absolutely necessary, since it is possible prolonged and excessively strong effect of the drug), disorders coagulability of the blood, severe impairment of liver and kidney function, pronounced excitement.

Pregnancy and lactation:Artikain penetrates the placental barrier. Due to the lack of clinical data, the decision to prescribe the drug by a dentist can only be made if the potential benefit of using it for the mother justifies the potential risk to the fetus. The results of animal studies do not allow us to conclude that articaine in therapeutic doses has a direct or indirect adverse effect on the course of pregnancy, the development of the embryo / fetus, childbirth and postnatal development. 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 (i.e., Obrilok preparation 40 mg / ml + 5 μg / ml). In the short-term use of the drug, there is no need to interrupt breastfeeding, since breast milk does not show clinically significant concentrations of articaine, due to a rapid decrease in plasma concentration and excretion from the body. In studies of fertility and early embryonic development in rats, the use of toxic doses during parenteral administration did not result in undesirable effects on male or female fertility.When using the drug in therapeutic doses, there is no negative effect on human fertility.

Dosing and Administration:

With uncomplicated removal of the teeth of the upper jaw, in the absence of inflammation, 1.8 ml of the drug (per tooth) is usually injected into the submucosa in the region of the transitional fold from the vestibular side. In some cases, additional administration of 1 ml to 1.8 ml of the drug may be required to achieve complete anesthesia. In most cases, there is no need to perform painful injections from the palatal side. For anesthesia with palatine incisions and suturing with the purpose of creating a palatine depot, about 0.1 ml of the drug per shot is needed. When several adjacent teeth are removed, the number of injections is usually limited. In the case of removal of premolars of the lower jaw in the absence of inflammation, mandibular anesthesia can be dispensed with, as infiltration anesthesia, provided by injection of 1.8 ml per tooth, is usually sufficient. If this method fails to achieve the desired effect, an additional injection of 1-1.8 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, in this case, it was not possible to achieve complete anesthesia, it is necessary to blockade the mandibular nerve.

To prepare the cavity or prepare for the crown of any tooth, with the exception of lower molars, the administration of the drug in a dose of 0.5 ml to 1.8 ml per tooth as infiltration anesthesia from the vestibular side is indicated. The exact amount depends on the desired depth of the procedure.

Usually mandibular anesthesia is indicated only in cases where the above procedures do not lead to complete anesthesia.

In surgical interventions, it is recommended to use the 40 mg / ml Spray + 10 μg / ml and, depending on the severity and duration of the intervention, is dosed individually.

When performing one treatment procedure, adults can administer up to 7 mg of articaine per 1 kg of body weight. The duration of anesthesia, during which the intervention can be performed, is 30-45 minutes.

For children, the drug is administered in amounts that depend on their age, body weight and method of anesthesia.

For children aged 4 to 12 years, the dose of the drug administered is not more than 5 mg of articaine per kg of body weight.

For children with a body weight of 20 to 30 kg, the recommended dose of the drug is from 0.25 to 1 ml (from 1/6 to 1/2 cartridge). The maximum single dose of the drug should not exceed 1.5 ml. The daily dose should not exceed 2.5 ml.

For children with a body weight of 30 to 45 kg, the recommended dose of the drug is from 0.5 to 1.7 ml (from 1/3 to 1 cartridge). The maximum single dose of the drug should not exceed 1.7 ml. The daily dose should not exceed 5 ml.

In elderly patients and patients with impaired liver and kidney function, the concentration of articaine in the plasma may increase. These patients should use the minimum doses necessary to achieve sufficient depth of anesthesia.

Side effects:

The drug is usually well tolerated by patients, however, the following side effects may occur:

From the central nervous system: Depending on the dose applied, cases of impaired consciousness are described, right up to its loss; disturbances of breathing until it stops; muscular tremor; involuntary jerking of the muscles, sometimes progressing up to generalized seizures; nausea, vomiting.

From the side of the organ of vision: occasionally - blurred vision, transitory blindness, diplopia.

From the cardiovascular system: moderately expressed disorders of hemodynamics, manifested in the reduction of blood pressure, tachycardia or bradycardia, inhibition of cardiovascular activity, which in extreme manifestation can lead to collapse and cardiac arrest, which threatens the patient's life.

Allergic reactions: redness of the skin, itching, conjunctivitis, rhinitis, angioedema, swelling of various, degree of severity (including edema of the upper and / or lower lip and / or cheeks, glottis with difficulty swallowing and / or breathing, urticaria). All these phenomena can progress to the development of anaphylactic shock.

Local reactions: edema or inflammation at the injection site.

Other: headaches are often associated, probably with the presence of epinephrine in the formulation. Other side effects caused by the action of epinephrine (tachycardia, arrhythmia, increased blood pressure) are extremely rare. Extremely rare random intravascular injection can lead to the development of ischemic zones at the site of administration, sometimes progressing to tissue necrosis.

Overdose:

When the first signs of the development of side effects or toxic effects (dizziness,motor disturbance, impaired consciousness), it is necessary to urgently stop the injection and give the patient a horizontal position. Careful monitoring of the parameters of hemodynamics (pulse, arterial pressure) and patency of the respiratory tract is necessary. Even if the symptoms do not seem heavy, you should prepare everything you need for intravenous infusion and, at the very least, carry out venipuncture. Depending on the degree of disturbance of breathing, oxygen, carry out artificial respiration and, if necessary, endotracheal intubation with controlled ventilation of the lungs. The use of analeptic drugs of central action is contraindicated. In case of involuntary, muscle twitching or generalized convulsions, intravenous administration of short or ultrashort barbiturates is indicated. The introduction should be carried out slowly, under the constant control of parameters of hemodynamics and respiration. At the same time, intravenous fluid infusion through a pre-established cannula should be performed.

With tachycardia, bradycardia, or a marked decrease in blood pressure,with severe circulatory disturbances and shock the patient should be given a horizontal position with raised legs, oxygen inhalation and intravenous infusion of balanced electrolyte and plasma-substituting solutions, intravenously injecting glucocorticoids (250-1000 mg methylprednisolone). In case of threatening vascular collapse and increasing bradycardia, administer 25-100 μg of epinephrine intravenously (0.25-1.0 ml of a solution with a concentration of 100 μg / ml). Introduction is carried out slowly, under the control of pulse and blood pressure. Do not administer more than 100 μg of epinephritis (1 ml of solution per time). With the introduction of additional amounts of epinephrine, it should be added to the infusion solution. The infusion rate should correlate with the heart rate and blood pressure level.

Severe forms of tachycardia and tachyarrhythmias can be eliminated by the use of antiarrhythmic drugs, however, non-selective beta-blockers should not be used.

With increasing blood pressure in patients with arterial hypertension should, if necessary, use peripheral, vasodilators.

Interaction:

The hypertensive effect of sympathomimetic amines for epinephrine may be enhanced by tricyclic antidepressants and MAO inhibitors. It is necessary to abolish MAO inhibitors 10 days before the introduction of a local anesthetic.

Do not prescribe the drug on the background of treatment with non-selective beta-blockers, since in this case the risk of hypertensive crisis and severe bradycardia is high.

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

Special instructions:

The drug contains sulfites, which can provoke an anaphylactic reaction.

Increased sensitivity to sulfites is more often observed in patients with bronchial asthma. The drug can not be administered intravenously. Do not inject into the area of inflammation.

In patients with cholinesterase deficiency, the drug can be used only with urgent indications, as these patients have a chance of prolonging and sometimes enhancing the effect of the drug.

To prevent infection (including viral hepatitis), you should not use open cartridges again for other patients.

In patients with cardiovascular disease (chronic heart failure, coronary artery disease, angina pectoris, rhythm disturbance, history of myocardial infarction, arterial hypertension), cerebrovascular disorders, history of stroke, chronic bronchitis, emphysema, diabetes, hyperthyroidism, and if, in the presence of severe anxiety, it is advisable to use a preparation containing a smaller amount of epinephrine.

Effect on the ability to drive transp. cf. and fur:Local anesthesia with Obrlok, as studies have shown, does not lead to significant deviations from the usual ability to drive and participate in traffic. However, the decision on when a patient after dental intervention with the drug Obrlok can return to driving vehicles or managing mechanisms, should take a dentist.

Form release / dosage:

Solution for injection 40 mg / ml + 5 μg / ml and 40 mg / ml + 10 μg / ml.

Packaging:

1.8 ml are placed in a cartridge of clear, colorless glass of hydrolytic class 1, on the one side ukuporenny plunger of brombutyl rubber,on the opposite side ukuporenny brombutilovoy stopper and crimped aluminum cap. Each label is labeled. For 10 cartridges are placed in a blister (pallet) made of plastic and polyethylene. For 10 blisters (pallets), along with instructions for use, put in a pack of cardboard.

Storage conditions:

Store in a 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

Obsolete name of the trade product: & nbspArtikain Perrell with adrenaline

Date renamed: & nbsp26.03.2015

Registration number:LSR-004839/10

Date of registration:27.05.2010 / 26.03.2015

Expiration Date:Unlimited

The owner of the registration certificate:Perrell Farma Sr.L.Perrell Farma Sr.L.

Manufacturer: & nbsp

PIERREL FARMACEUTICI, S.p.A. Italy

Information update date: & nbsp10.06.2017

Illustrated instructions

Instructions

Orablok® (Orabloc®)