Articaine (Monograph)

Brand name: Septocaine
Drug class: Local Anesthetics
Chemical name: 4-Methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-2-thiopenecarboxylic acid methyl ester monohydrochloride
Molecular formula: C₁₃H₂₀N₂O₃S•HCl
CAS number: 23964-57-0

Introduction

Intermediate-acting local anesthetic (amide type).

Uses for 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.

Articaine Dosage and Administration

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.

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.

Cautions for Articaine

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.

Drug Interactions

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

Specific Drugs

Articaine Pharmacokinetics

Absorption

Bioavailability

Peak plasma concentrations achieved approximately 25 minutes following single dose and 48 minutes following 3 doses.

Onset

1–6 minutes following submucosal injection. Average onset of anesthesia following articaine administration appears to be similar to that of prilocaine but slightly faster than that of other local anesthetics (e.g., lidocaine).

Duration

Complete anesthesia lasts approximately 1 hour.

Distribution

Plasma Protein Binding

Approximately 60–80% (albumin and γ-globulins).

Elimination

Metabolism

Systemically absorbed articaine is rapidly metabolized by plasma carboxyesterase to articainic acid (inactive); approximately 5–10% of available articaine is metabolized to articainic acid by CYP enzymes.

Elimination Route

Excreted principally in urine as inactive metabolites and small amounts (2%) of unchanged drug; approximately 53–57% of administered dose excreted within 24 hours following submucosal administration.

Half-life

Approximately 1.8 hours.

Stability

Storage

Parenteral

Injection

25°C (may be exposed to 15–30°C). Protect from light.

Compatibility

May be incompatible with strong oxidizing agents.

Actions

• Local anesthetics block the generation and conduction of nerve impulses by increasing the threshold for electrical excitation, slowing the propagation of the nerve impulse, and reducing the rate of rise of the action potential.

• Formulated with epinephrine to decrease articaine’s rate and extent of systemic absorption and to prolong its duration of action.

• Has intermediate duration of action (approximately 1 hour).

Advice to Patients

• Prior to administration, advise patients of the possibility of temporary loss of sensation and muscle function following infiltration and nerve block injections.

• Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular disease).

• Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Reload page with references included

Medical Disclaimer