Articaine

SEPTOCAINE

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Articaine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Articaine ballicule

What it isPeripheral sodium-channel blocker with amide and ester features; dental anesthesia.

Why this oneRapid onset and good bone penetration make it a dental workhorse, and plasma esterases clear it quickly.

What limits itParesthesia after mandibular block is reported more often with articaine than with lidocaine.

Articaine molecular structure (skeletal formula) — Molecular structure: Articaine

FDA-approved for

dental anesthesia (2000)

FDA label

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FDA dosing	Population	Start	Target	Max
Local/regional anesthesia for dental procedures (infiltration or nerve block)	adults	Infiltration 0.5-2.5 mL (20-100 mg); nerve block 0.5-3.4 mL (20-136 mg); oral surgery 1-5.1 mL (40-204 mg)	lowest effective dose	7 mg/kg (0.175 mL/kg)
Local/regional dental anesthesia	peds 4-16 y	per procedure	lowest effective dose	7 mg/kg (0.175 mL/kg)

Renal Undefined

Hepatic Undefined

Maximum 7 mg/kg articaine HCl (healthy adults and children 4-16 y).

Instructions

Intraoral submucosal infiltration or nerve block only.
Aspirate before injecting to avoid intravascular injection; reposition needle until no blood returns.
Use the lowest dose that produces the desired effect.
1:200,000 epinephrine preferred for routine procedures; 1:100,000 when more hemostasis/visualization is needed.

Available strengths

inj 40/0.005, 40/0.01, 40/5, 40/10 mg/mL

Contraindications

Hypersensitivity to sulfites

Cautions

Accidental intravascular injection — convulsions, coma, respiratory arrest
Systemic toxicity affecting CNS and cardiovascular systems
Vasoconstrictor toxicity — caution in impaired cardiovascular function or vascular disease
Methemoglobinemia

Adverse reactions

Headache
Pain
Face edema
Paresthesia
Gingivitis

Pregnancy Pregnancy Category C; no adequate studies; use only if benefit justifies risk (animal fetal death/skeletal variations).

Lactation Exercise caution when administering to a nursing woman.

Cost

Articaine (SEPTOCAINE)

Strength		#/mo	CostPlus
40/0.005 mg/mL	inj	per unit	not offered
40/0.01 mg/mL	inj	per unit	not offered
40/5 mg/mL	inj	per unit	not offered
40/10 mg/mL	inj	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Articaine is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskParaesthesia after mandibular block is reported more with articaine than with lidocaine

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Sedation liability1 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

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