Articaine DF (Solution) Instructions for Use

Marketing Authorization Holder

Hiratrade SP, LLC (Russia)

Manufactured By

Industria E Comercio Dfl S.A. (Brazil)

ATC Code

N01BB58 (Articaine in combination with other drugs)

Active Substances

Articaine (Rec.INN WHO registered)

Epinephrine (Rec.INN WHO registered)

Dosage Form

Articaine DF

Injection solution 40 mg+0.01 mg/1 ml: cartridges 1.8 ml 50 pcs.

Dosage Form, Packaging, and Composition

Solution for injection transparent, colorless, odorless.

Excipients : sodium disulfite – 0.5 mg, sodium chloride – 1.6 mg, water for injection – up to 1 ml.

1.8 ml – cartridges of colorless glass (10) – PVC/aluminum foil blisters (5) – cardboard packs.

Clinical-Pharmacological Group

Local anesthetic for use in dentistry

Pharmacotherapeutic Group

Local anesthetic agent + alpha- and beta-adrenomimetic

Pharmacological Action

Articaine DF is a local anesthetic for infiltration and conduction anesthesia in dental practice.

It has a rapid onset of action (latent period – from 1 to 3 minutes). The duration of anesthesia is at least 75 minutes. Due to the low epinephrine content in the drug, its effect on the cardiovascular system is insignificant: there is almost no increase in blood pressure or increase in heart rate.

Pharmacokinetics

Absorption

After injection into the oral submucosa: time to reach C_max– about 25 min. Onset of action: in case of infiltration administration — 1-2 min, in case of mandibular anesthesia administration – 2-2.5 min. Duration of action – 45 min.

Distribution

Plasma protein binding of articaine is 95%. The drug minimally penetrates the placental barrier and is practically not excreted in breast milk.

Elimination

Articaine is excreted primarily by the kidneys unchanged (about 10%) and in the form of metabolites (about 90%). Approximately 53-57% of the dose is excreted within the first 24 hours after administration into the submucosa. After injection into the oral submucosa, T_1/2 averages 25 min.

Indications

Local infiltration and conduction anesthesia in dentistry (including in patients with concomitant severe somatic diseases)

• Uncomplicated extraction of one or several teeth;
• Cavity preparation and tooth grinding before prosthetics.

ICD codes

Dosage Regimen

For uncomplicated extraction of maxillary teeth in a non-inflammatory stage, 1.8 ml of Articaine DF is injected into the submucosa in the area of the transitional fold from the vestibular side (for each tooth). In rare cases, additional administration of 1 ml to 1.8 ml is required to achieve complete anesthesia.

For anesthesia during palatal incisions and suture placement to create a palatal depot, about 0.1 ml of anesthetic per injection is needed. Painful palatal injection can be avoided in most cases. When extracting several adjacent teeth, the number of injections can usually be limited.

For extraction of mandibular premolars in the absence of inflammation, mandibular anesthesia can be dispensed with, as infiltration anesthesia provided by an injection of 1.8 ml per tooth is usually sufficient.

If the desired effect is not achieved in this way, an additional injection of 1-1.8 ml of anesthetic should be performed into the submucosa in the area of the mandibular transitional fold from the vestibular side. If complete anesthesia is still not achieved, a mandibular nerve block should be performed. For cavity preparation and tooth preparation for crowns, except for mandibular molars, – vestibular injection of 0.5-1.7 ml per tooth. Maximum dose 7 mg/kg.

For surgical interventions, Articaine DF is dosed individually depending on the severity and duration of the intervention. The table below shows the recommended volumes and doses of the drug for several types of anesthesia. The proposed doses are intended for healthy patients.

Precautions for use

Intravenous use is contraindicated!

To avoid intravascular injection, an aspiration test must be performed.

Injection pressure should correspond to tissue sensitivity.

Do not inject into an inflamed area!

Food intake is possible only after sensitivity is restored.

Opened cartridges must not be reused for other patients. Do not use a damaged cartridge.

Adverse Reactions

From the digestive system nausea; vomiting, diarrhea.

From the nervous system headache, confusion up to loss of consciousness, respiratory disturbances up to life-threatening arrest, muscle tremor and twitching, up to generalized convulsions, nausea, vomiting.

From the cardiovascular system: drop in blood pressure and cardiac arrest can also occur with drug administration.

Allergic reactions in the form of edema or inflammation at the injection site, skin hyperemia, itching, conjunctivitis, rhinitis, facial swelling (angioedema) with swelling of the upper and/or lower lip, swelling of the vocal cords with a feeling of a lump in the throat and difficulty swallowing, urticaria, difficulty breathing up to anaphylactic shock.

Other tachycardia, cardiac arrhythmias, increased blood pressure with low epinephrine concentration (0.005 mg/ml) are rare. With accidental intravascular injection, areas of ischemia up to tissue necrosis at the injection site may appear. Due to the sodium disulfite content, in some cases, patients with bronchial asthma may experience hypersensitivity reactions, manifested as vomiting, diarrhea, rapid breathing, acute asthma attack, impaired consciousness or shock.

Contraindications

• Paroxysmal ventricular tachycardia and other tachyarrhythmias;
• Bronchial asthma with hypersensitivity to sulfites;
• Closed-angle glaucoma;
• Concomitant use of non-selective beta-blockers;
• Severe hepatic insufficiency (porphyria);
• Hyperthyroidism;
• Concomitant therapy with MAO inhibitors or tricyclic antidepressants;
• Cardiogenic shock;
• Children under 4 years of age;
• Hypersensitivity to articaine, epinephrine or any other component of the drug.

With caution : chronic heart failure, intraventricular and AV heart block, inflammation in the area of intended anesthesia, cholinesterase deficiency, renal failure, diabetes mellitus, arterial hypertension, elderly age, severe general condition, debilitated patients.

Use in Pregnancy and Lactation

For surgical interventions during pregnancy, local anesthesia is considered a gentle method of pain relief. Articaine passes through the placental barrier in smaller quantities than other local anesthetics. Due to the very rapid drop in articaine levels and its rapid elimination from the body, it enters breast milk in clinically insignificant amounts. Therefore, interruption of breastfeeding is not required.

Use in Hepatic Impairment

Contraindicated

• Severe hepatic insufficiency (porphyria).

Pediatric Use

Contraindicated

• Children under 4 years of age.

Special Precautions

Effect on ability to drive vehicles and operate machinery

The patient’s eligibility to drive vehicles and operate machinery is determined by the doctor.

Overdose

Symptoms the most common symptoms are reactions of the cardiovascular system and nervous system nausea, motor restlessness, confusion during injection, respiratory disturbances, muscle twitching, convulsions, shock.

Treatment: treatment is symptomatic. At the first signs of overdose or adverse reactions, such as nausea, motor restlessness, confusion during injection, it should be interrupted, the patient should be placed in a horizontal position, the airways should be cleared, and pulse and blood pressure should be monitored. It is recommended, even if the symptoms do not seem too pronounced, to ensure intravenous access. For respiratory disturbances, depending on the severity, administer oxygen, in some cases perform artificial respiration. Central analeptics are contraindicated. Muscle twitching or generalized convulsions are relieved by intravenous injection of short or ultra-short-acting barbiturates. A drop in blood pressure, tachycardia or bradycardia is often eliminated by placing the patient in a horizontal position. In case of severe circulatory disorders and shock of any origin, after stopping the injection, emergency measures are indicated: ensuring airway patency (oxygen insufflation), intravenous fluid infusion (electrolyte solution), glucocorticosteroids. Additionally, plasma substitutes and albumin can be administered. In case of threatening circulatory disturbance and increasing bradycardia, 0.25 ml to 1 ml of epinephrine is administered. Intravenous injection of epinephrine should be performed slowly under the control of pulse rate and blood pressure. A single dose of intravenous epinephrine injection should not exceed 0.1 mg. Subsequently, if necessary, Epinephrine can be administered by drip (the infusion rate through the dropper is regulated depending on the pulse rate and blood pressure). Severe forms of tachycardia and tachyarrhythmia can be eliminated by the use of antiarrhythmic drugs, but non-selective beta-blockers should not be used. Oxygen supply and circulation monitoring are necessary in any case. In case of increased blood pressure in patients suffering from arterial hypertension, peripheral vasodilators should be used if necessary.

Drug Interactions

Tricyclic antidepressants, MAO inhibitors enhance the hypertensive effect.

Vasoconstrictor drugs enhance and prolong the local anesthetic effect of articaine.

Non-selective beta-blockers increase the risk of hypertensive crisis and severe bradycardia.

Storage Conditions

Store in a light-protected place at a temperature not exceeding 30°C (86°F). Keep out of reach of children.

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.