Overview
Articaine is an amide-type local anesthetic used primarily in dental procedures. It has a rapid onset of action (1-3 minutes) and intermediate duration of anesthesia (approximately 1 hour). Articaine contains epinephrine (adrenaline) as a vasoconstrictor to prolong its effect and reduce systemic absorption. It is metabolized primarily in plasma by plasma esterases and has a short elimination half-life of approximately 20 minutes.
Mechanism of Action
Articaine blocks voltage-gated sodium channels in neuronal membranes, preventing depolarization and propagation of action potentials, thereby inhibiting nerve conduction and producing local anesthesia. The epinephrine component causes vasoconstriction, reducing systemic absorption and prolonging anesthetic effect.
Indications
- Local anesthesia for dental procedures including restorative dentistry, oral surgery, and periodontal treatment
- Infiltration and nerve block anesthesia in dentistry
Dosage
Dosage varies based on procedure, patient age, and physical status. Typical adult dose: 0.5-2.7 mL (containing 20-108 mg articaine) per injection site. Maximum recommended dose: 7 mg/kg (not to exceed 500 mg articaine). For children: Maximum dose of 5 mg/kg. Always use the smallest effective dose.
Contraindications
- Hypersensitivity to articaine, other amide-type anesthetics, or sulfites
- Patients with methemoglobinemia
- Severe hypotension or shock
- Patients with severe heart block or severe bradycardia without pacemaker
- Epinephrine-containing formulations contraindicated in patients with uncontrolled hyperthyroidism, pheochromocytoma, or severe cardiovascular disease
Side Effects
- Common: Paresthesia, pain at injection site, headache, dizziness
- Neurological: Seizures, syncope, anxiety, tremors
- Cardiovascular: Tachycardia, bradycardia, hypertension, hypotension, arrhythmias
- Gastrointestinal: Nausea, vomiting
- Allergic: Urticaria, pruritus, angioedema, anaphylaxis
- Other: Methemoglobinemia, tinnitus, blurred vision
Interactions
- MAO inhibitors, tricyclic antidepressants, phenothiazines: May potentiate pressor effects of epinephrine
- Beta-blockers: May increase risk of hypertension and bradycardia
- Vasoconstrictors: Additive effects with other vasoconstrictors
- Antiarrhythmic drugs: Additive cardiac effects
- Sulfonamides: Increased risk of methemoglobinemia