Articaine

Brand names: Septocaine
Drug class: Antineoplastic Agents

Usage of Articaine

Dental Anesthesia

Local, infiltrative, or regional (i.e., nerve block) anesthesia in simple and complex dental and periodontal procedures.

Anesthetic activity comparable to that of lidocaine, mepivacaine, and prilocaine.

Relate drugs

How to use Articaine

General

  • Determine dosage based on type and extent of surgical procedure, depth of anesthesia, degree of muscular relaxation, and condition of the patient. Use smallest dose required to produce the desired effect.
  • For pediatric patients, determine dosage based on age, weight, physical condition of the patient, and type and extent of surgical procedure.

    • Administration

    Submucosal Injection

    For solution and drug compatibility information, see Compatibility under Stability.

    Administer by submucosal infiltration or by nerve block.

    Aspirate prior to administration to guard against intravascular injection.

    For chemical disinfection of the cartridge unit, use isopropyl (rubbing) alcohol (91%) or ethyl alcohol (70%). Do not use brands that are not of USP grade, since these preparations may contain denaturants that may be injurious to rubber.

    Dosage

    Available as fixed combination containing articaine hydrochloride and epinephrine bitartrate; dosage expressed in terms of articaine hydrochloride.

    Pediatric Patients

    Dental Anesthesia Submucosal Injection

    Children ≥4 years of age: Use lower dosages than those suggested for healthy adults (see Adults under Dosage and Administration).

    Simple procedures: 0.76–5.65 mg/kg used in clinical trials.

    Complex procedures: 0.37–7.48 mg/kg used in clinical trials.

    Approximately 13% of pediatric patients in clinical trials required additional injections for complete anesthesia.

    Adults

    Dental Anesthesia Submucosal Injection

    Usual dosage range: 20–204 mg.

    Recommended Dosages (as articaine hydrochloride 4% with epinephrine 1:100,000) for Dental Anesthesia in Healthy Adults1

    Procedure

    Volume of Injection (mL)

    Total Dose of Articaine Hydrochloride (mg)

    Infiltration

    0.5–2.5

    20–100

    Nerve block

    0.5–3.4

    20–136

    Oral surgery

    1–5.1

    40–204

    Prescribing Limits

    Pediatric Patients

    Dental Anesthesia Submucosal Injection

    Maximum 7 mg/kg (0.175 mL/kg).

    Adults

    Dental Anesthesia Submucosal Injection

    Maximum 7 mg/kg (0.175 mL/kg).

    Special Populations

    Hepatic Impairment

    Reduce dosage in patients with hepatic disease.

    Geriatric Patients

    Reduce dosage in patients ≥65 years of age.

    Patients 65–74 Years of Age

    Simple procedures: 0.43–4.76 mg/kg used in clinical trials.

    Complex procedures: 1.05–4.27 mg/kg used in clinical trials.

    Approximately 6% of patients in clinical trials required additional injections for complete anesthesia.

    Patients ≥75 Years of Age

    Simple procedures: 0.78–4.76 mg/kg used in clinical trials.

    Complex procedures: 1.12–2.17 mg/kg used in clinical trials.

    None of the patients in clinical trials required additional injections for complete anesthesia.

    Other Populations

    Reduce dosage in patients with cardiac disease, debilitated patients, and patients with acute illnesses.

    Warnings

    Contraindications

  • Known hypersensitivity to local anesthetics of the amide type or to sodium metabisulfite.

    • Warnings/Precautions

    Warnings

    Epinephrine Administration

    Injection contains epinephrine, which may cause tissue necrosis or systemic toxicity. Consider usual precautions associated with epinephrine administration.

    Accidental Intravascular Injection

    Accidental intravascular injection may result in confusion, seizures, CNS or cardiorespiratory depression, coma, and/or respiratory arrest.

    Aspirate prior to administration to guard against intravascular injection.

    Should be used only by clinicians who are sufficiently knowledgeable in the diagnosis and management of dose-related toxicity and other acute emergencies that might arise. Resuscitative equipment and drugs must be available for immediate use.

    Sensitivity Reactions

    Sulfite Sensitivity

    Articaine injection contains sodium metabisulfite, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals.

    General Precautions

    CNS Effects

    Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse CNS effects (e.g., restlessness, anxiety, tinnitus, lightheadedness, dizziness, disorientation, excitement, blurred vision, tremors, depression, drowsiness).

    Carefully monitor level of consciousness after each local anesthetic injection.

    Cardiovascular Effects

    Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse cardiovascular effects (e.g., reduced myocardial contractility, peripheral vasodilation, depressed cardiac conduction and excitability). Possible atrioventricular block, ventricular arrhythmia, cardiac arrest, and, rarely, death. Carefully monitor cardiovascular and respiratory vital signs after each local anesthetic injection.

    Cardiac arrhythmias may occur in patients receiving potent general anesthetics; use with caution in such patients.

    Articaine hydrochloride injection contains epinephrine; risk of exaggerated vasoconstrictor response in patients with hypertension or peripheral vascular disease. Risk of ischemic injury or necrosis.

    Use with caution in patients with heart block or other cardiovascular disease.

    Specific Populations

    Pregnancy

    Category C.

    Lactation

    Not known whether articaine or its metabolites are distributed into milk. Caution advised if used in nursing women.

    Pediatric Use

    Safety and efficacy not established in children <4 years of age.

    Geriatric Use

    No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.

    Hepatic Impairment

    Not studied in patients with hepatic impairment. Use with caution in patients with severe hepatic impairment.

    Common Adverse Effects

    Pain, headache, facial edema, gingivitis, paresthesia, infection.

    What other drugs will affect Articaine

    Approximately 5–10% of available articaine is metabolized by CYP enzymes.

    Specific Drugs

    Drug

    Interaction

    Comments

    Anesthetics, general

    Possible cardiac arrhythmias when articaine is administered during or following administration of potent general anesthetics

    Use with caution

    Antidepressants, tricyclics

    Possible severe, prolonged hypertension due to epinephrine component

    Avoid concomitant use; if must be used concomitantly, careful monitoring is required

    Butyrophenones

    Possible reduction or reversal of pressor effect of epinephrine

    Avoid concomitant use; if must be used concomitantly, careful monitoring is required

    MAO inhibitors

    Possible severe, prolonged hypertension due to epinephrine component

    Avoid concomitant use; if must be used concomitantly, careful monitoring is required

    Phenothiazines

    Possible reduction or reversal of pressor effect of epinephrine

    Avoid concomitant use; if must be used concomitantly, careful monitoring is required

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