SEPTOCAINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SEPTOCAINE (SEPTOCAINE).
Articaine is a local anesthetic of the amide type that stabilizes the neuronal membrane by inhibiting sodium ion influx, thereby blocking nerve impulse conduction.
| Metabolism | Primarily metabolized by plasma esterases (nonspecific) and hepatic CYP450 enzymes (minor). |
| Excretion | Primarily hepatic metabolism; less than 10% excreted unchanged in urine. Biliary/fecal elimination is negligible. |
| Half-life | Terminal elimination half-life in adults is 2-4 hours. In neonates, it may be prolonged to 8-12 hours due to immature hepatic function. |
| Protein binding | About 55-75% bound primarily to alpha1-acid glycoprotein. |
| Volume of Distribution | Approximately 1.0 L/kg, indicating extensive distribution into tissues. |
| Bioavailability | Intravenous: 100%; Subcutaneous or topical: Not applicable due to vasoconstriction and first-pass metabolism. |
| Onset of Action | Infiltration: 1-2 minutes; Nerve block: 2-5 minutes; Epidural: 5-15 minutes. |
| Duration of Action | Infiltration: 30-60 minutes; Nerve block: 45-90 minutes; Epidural: 60-120 minutes. Duration can be prolonged 2-3 times with epinephrine-containing solutions. |
SEPTOCAINE (articaine HCl 4% with epinephrine 1:100,000 or 1:200,000) dental infiltration or nerve block: 0.5–1.7 mL (20–68 mg articaine) per injection site; maximum adult dose: 7 mg/kg (up to 500 mg total).
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment for mild-to-moderate renal impairment; caution in severe renal impairment (GFR <30 mL/min) with extended monitoring for methemoglobinemia. |
| Liver impairment | Child-Pugh A and B: no adjustment; Child-Pugh C: avoid use or reduce dose by 50% with monitoring due to reduced hepatic clearance. |
| Pediatric use | Pediatric weight-based dosing: articaine 4% with epinephrine 1:100,000 or 1:200,000; maximum dose 7 mg/kg; typical infiltration 0.5–1.7 mL per site; adjust volume to age and weight; not recommended under 4 years of age. |
| Geriatric use | Elderly: start with lower doses (minimum effective volume) due to possible decreased hepatic/renal function; maximum dose 7 mg/kg; monitor for prolonged effect and cardiovascular stress. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SEPTOCAINE (SEPTOCAINE).
| Breastfeeding | Articaine is excreted into breast milk in small amounts; the milk-to-plasma ratio (M/P) is approximately 0.8. Relative infant dose is estimated at 2-5% of maternal weight-adjusted dose, considered safe. Epinephrine has poor oral bioavailability. However, monitor infant for signs of local anesthetic toxicity (e.g., irritability, drowsiness). |
| Teratogenic Risk | Septocaine (articaine with epinephrine) is classified as FDA Pregnancy Category C. Animal studies have shown fetal harm at doses 1.3 to 2.6 times the maximum recommended human dose, but no adequate human studies exist. Risk cannot be ruled out. Use only if potential benefit justifies potential risk. First trimester: Avoid elective procedures; risk of teratogenicity cannot be excluded. Second and third trimesters: Use with caution; potential for fetal bradycardia due to epinephrine or maternal hypotension. |
■ FDA Black Box Warning
Not FDA approved for use in children under 4 years of age. Methemoglobinemia has been reported; risk increases with total dose and in patients with glucose-6-phosphate dehydrogenase deficiency.
| Serious Effects |
Hypersensitivity to articaine or any component of the formulation; hypersensitivity to amide-type local anesthetics; sulfite allergy; severe hypotension; atrioventricular block; uncontrolled epilepsy; myasthenia gravis (relative).
| Precautions | Methemoglobinemia risk; avoid in patients with congenital or idiopathic methemoglobinemia. Use with caution in patients with impaired cardiovascular function, hepatic or renal disease, and in elderly or debilitated patients. Contains sulfites which may cause allergic reactions including anaphylaxis. |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and oxygen saturation. Fetal heart rate monitoring is recommended during prolonged procedures or high doses. Observe for signs of maternal hypotension, tachycardia, or allergic reaction. In near-term, avoid excessive doses due to risk of fetal acidosis. |
| Fertility Effects | No adequate studies on fertility. Animal studies with articaine did not show impaired fertility. Epinephrine at high systemic doses may affect uterine blood flow, but local injection with epinephrine at recommended doses is unlikely to impact fertility. |