Articaine (Solution) Instructions for Use

ATC Code

N01BB08 (Articaine)

Active Substance

Articaine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Local anesthetic for use in dentistry

Pharmacotherapeutic Group

Local anesthetic agent

Pharmacological Action

Articaine is a local anesthetic of the amide type, used for infiltration and conduction anesthesia in dentistry.

Articaine exerts its local anesthetic effect by blocking voltage-gated sodium channels in the neuronal cell membrane, leading to reversible inhibition of impulse conduction along the nerve fiber and reversible loss of sensation.

The drug’s effect begins rapidly, within 1-3 minutes. The duration of anesthesia is approximately 20 minutes.

The drug Articaine does not contain epinephrine and is used when the addition of epinephrine to a local anesthetic is not necessary or when the use of epinephrine is contraindicated.

Pharmacokinetics

Absorption, Distribution, Metabolism

Articaine is rapidly and almost immediately after administration metabolized (via hydrolysis) by non-specific plasma esterases in tissues and blood (90%); the remaining 10% of articaine is metabolized by hepatic microsomal enzymes. The main metabolite of articaine formed in this process, articainic acid, does not possess local anesthetic activity or systemic toxicity, which allows for repeated administration of the drug.

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

Articaine crosses the placental barrier and is practically not excreted in breast milk.

In children, the overall effect after vestibular infiltration anesthesia is comparable to that in adults, but the C_max in blood serum is reached faster.

Elimination

Articaine is eliminated mainly by the kidneys in the form of articainic acid. After submucosal administration, the T_1/2 is approximately 25 minutes.

Indications

• Infiltration and conduction anesthesia in dentistry.

Articaine without epinephrine is used primarily for short procedures in patients for whom the use of epinephrine is unacceptable (for example, in cardiovascular diseases), or when small volumes of the drug need to be administered (in the area of the anterior teeth, palate).

ICD codes

Dosage Regimen

Solution

The drug is intended for use in the oral cavity and can only be injected into tissue that is not inflamed.

Injection into inflamed tissues is not allowed.

The drug must not be administered intravenously.

To avoid accidental entry of the drug into blood vessels, a two-step aspiration test with rotation of the needle by 90°C (194°F) and 180° should always be performed before its administration.

Major systemic reactions that may develop as a result of accidental intravascular administration of the drug can be avoided by following the injection technique: after performing the aspiration test, 0.1-0.2 ml of the drug is slowly injected, then, no earlier than 20-30 seconds later, the remaining dose of the drug is slowly injected. The injection pressure should correspond to tissue sensitivity.

For infiltration anesthesia in the absence of inflammation, 1.7 ml of the drug is usually administered per tooth or per two adjacent teeth. For conduction anesthesia of the inferior alveolar nerve, approximately 1-1.7 ml of the drug is required.

For additional injections, half the dose or a full dose should be used.

The maximum dose for adults is 4 mg/kg of body weight.

Adverse Reactions

The frequency of adverse effects is presented in accordance with the classification recommended by WHO: very common (≥1/10); common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10000, <1/1000); very rare (<1/10000), including isolated reports; frequency unknown (cannot be estimated from the available data).

Nervous system disorders: common – paresthesia, hypesthesia; uncommon – dizziness; frequency unknown – dose-dependent reactions from the CNS, including agitation, nervousness, stupor sometimes progressing to loss of consciousness, coma, respiratory disorders sometimes progressing to respiratory arrest, muscle tremor, muscle twitching sometimes progressing to generalized convulsions.

Sometimes, if the correct injection technique is violated during the administration of a local anesthetic in dental practice, nerve damage may occur, which can lead to the development of facial nerve paralysis.

Eye disorders frequency unknown – transient visual disturbances (blurred vision, diplopia, mydriasis, blindness), usually reversible, and occurring during or shortly after injection of the local anesthetic in the head area.

Gastrointestinal disorders common – nausea, vomiting.

Cardiac and vascular disorders frequency unknown – decreased BP, heart failure, shock (under certain circumstances life-threatening).

Immune system disorders frequency unknown – allergic and allergy-like reactions. At the injection site, they may manifest as swelling or inflammation of the mucous membrane. Manifestations not related to the injection site may include skin redness, itching, conjunctivitis, rhinitis, and angioedema. Angioedema may present as swelling of the upper and/or lower lips, cheeks, swelling of the vocal cords with a sensation of a “lump in the throat” and difficulty swallowing, urticaria, and difficulty breathing. Any of these manifestations can progress to anaphylactic shock.

Contraindications

• Hypersensitivity to articaine or other local anesthetics of the amide type, except in cases where, in the presence of hypersensitivity to local anesthetics of the amide type, allergy to articaine has been ruled out through appropriate studies conducted in compliance with all necessary rules and requirements;
• Severe sinus node dysfunction or severe conduction disorders (such as marked bradycardia, atrioventricular block II-III degree);
• Acute decompensated heart failure;
• Severe arterial hypotension;
• Children under 4 years of age (lack of sufficient clinical experience).

With caution

• Cholinesterase deficiency (use is possible only in case of extreme necessity, as prolonged and excessively strong action of the drug is possible);
• History of epilepsy (see section “Adverse Reactions”).

Use in Pregnancy and Lactation

Pregnancy

Articaine crosses the placental barrier.

The concentration of articaine in the blood serum of newborns (after administration of the drug to the mother) is approximately 30% of the concentration of articaine in the mother’s blood serum.

Due to insufficient clinical data, the decision to use the drug by a dentist can only be made if the potential benefit of its use for the mother justifies the potential risk to the fetus.

Breastfeeding period

Articaine is practically not excreted in breast milk.

With short-term use of the drug during breastfeeding, it is generally not necessary to interrupt breastfeeding, as clinically significant concentrations of articaine are not detected in breast milk.

Fertility

In fertility studies in rats, no effect on fertility in males and females was observed when articaine was used in toxic doses. No effect on human fertility is expected when articaine is used in therapeutic doses.

Pediatric Use

The efficacy and safety of the drug in children under 4 years of age have not been studied, therefore its use in this age group is contraindicated.

Special Precautions

The drug is not intended for prolonged administration (more than 20 minutes). To prevent infection (including hepatitis virus), care must be taken to ensure that new syringes and needles are always used when withdrawing the solution from ampoules. Opened cartridges must not be reused for other patients!

Do not use a damaged cartridge for injection.

Regional and local anesthesia should be performed by experienced specialists in an appropriately equipped room with readily available equipment and drugs necessary for monitoring cardiac activity and resuscitation. The personnel performing anesthesia must be qualified and trained in anesthesia techniques, and must be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

Patients require monitoring of the cardiovascular system, respiratory system, and CNS.

Caution should be exercised when using the drug in patients with angina pectoris, atherosclerosis, bleeding disorders, severe impairment of liver or kidney function, history of epilepsy (see section “Adverse Reactions”). To avoid the risk of adverse reactions, the minimum effective doses of the drug should be used and a two-step aspiration test should be performed before its administration.

It should be taken into account that 1 ml of the drug contains less than 1 mmol (23 mg) of sodium.

Food can be taken only after the local anesthesia has worn off (sensation has returned). Children and their parents should be warned about the risk of accidental damage to soft tissues by teeth (biting) due to reduced tissue sensitivity caused by the drug.

Effect on ability to drive vehicles and operate machinery

The decision on when a patient can return to driving vehicles or engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions after a dental intervention should be made by the doctor.

Overdose

Symptoms

From the CNS: CNS excitation – feeling of anxiety, fear, confusion, hyperpnea, tachycardia, increased BP with facial flushing, nausea, vomiting, tremor, twitching, tonic-clonic convulsions;

CNS depression – dizziness, hearing impairment, loss of speech, stupor, unconsciousness, atony, paralysis of vasomotor nerves (weakness, pallor), shortness of breath, death from paralysis of respiratory muscles.

From the cardiovascular system: bradycardia, arrhythmia, ventricular fibrillation, drop in BP, cyanosis, cardiac arrest.

Treatment

At the first signs of intoxication or adverse drug effects, such as dizziness, motor agitation, or stupor during drug administration, its administration should be stopped and the patient should be placed in a horizontal position with lower limbs elevated. Airway patency should be ensured and hemodynamic parameters (heart rate and BP) should be monitored. It is recommended to always, even if the symptoms of intoxication seem mild, secure venous access in order to be able to immediately administer necessary medications intravenously if needed.

In case of respiratory disturbances, depending on their severity, oxygen supply is recommended, and if indications for artificial respiration arise, endotracheal intubation and mechanical ventilation should be performed.

Muscle twitching and generalized convulsions can be controlled by intravenous administration of fast-acting drugs with muscle relaxant and anticonvulsant effects (e.g., diazepam, suxamethonium chloride). Mechanical ventilation (oxygen supply) is also recommended.

A sharp decrease in BP, bradycardia, or tachycardia can often be eliminated by simply placing the patient in a horizontal position with elevated lower limbs.

In case of severe circulatory disorders and shock, regardless of their cause, the administration of the drug should be discontinued and the patient should be placed in a horizontal position with elevated lower limbs. Oxygen supply, intravenous administration of electrolyte solutions, corticosteroids (e.g., 250-1000 mg prednisolone or an equivalent amount of its derivative, e.g., methylprednisolone), replacement infusion therapy (if necessary, additionally, plasma substitutes, including human albumin) should be carried out.

If collapse develops and bradycardia increases, epinephrine (adrenaline) should be administered intravenously immediately. After diluting 1 ml of 0.1% epinephrine solution (1:1000) to 10 ml or using a 0.01% epinephrine solution (1:10000), slowly administer 0.25-1 ml (0.025-0.1 mg epinephrine) intravenously, monitoring heart rhythm and BP (caution: cardiac arrhythmias may occur!).

Do not exceed a single intravenous dose of 1 ml (0.1 mg epinephrine). If subsequent administration of doses exceeding 0.1 mg is necessary, epinephrine should be administered by infusion, adjusting the rate of administration under the control of heart rate and BP.

Drug Interactions

With drugs that depress the CNS

Local anesthetics enhance the effect of drugs that depress the CNS. Narcotic analgesics enhance the effect of local anesthetics and increase the risk of respiratory depression.

With anticoagulants and other drugs that reduce blood clotting

When administering Articaine injections to patients receiving, for example, heparin or acetylsalicylic acid, bleeding may develop at the injection site.

With cholinesterase inhibitors

Slowing of the metabolism of local anesthetics, as a result of which prolongation and pronounced enhancement of the effect of articaine is possible.

With vasoconstrictors

The local anesthetic effect of articaine is enhanced and prolonged by vasoconstrictor drugs.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F); do not allow freezing.

Shelf Life

Shelf life – 5 years. Do not use after the expiration date printed on the packaging.

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.