ANESTACON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANESTACON (ANESTACON).
Local anesthetic that stabilizes the neuronal membrane by inhibiting sodium ion influx, thereby blocking nerve impulse conduction.
| Metabolism | Not available. |
| Excretion | Renal (90% as unchanged drug and metabolites; 10% fecal/biliary). |
| Half-life | Terminal elimination half-life is 1.5–2.5 hours; clinically relevant for dosing interval. |
| Protein binding | 85–95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd = 1.5–2.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 30–40% (first-pass effect); IM: 100%; IV: 100%. |
| Onset of Action | IV: immediate; IM: 5–10 minutes; oral: 30–60 minutes. |
| Duration of Action | IV: 30–60 min for analgesic effect; IM: 1–2 hours; oral: 2–4 hours. |
5% lidocaine ointment, apply topically 3-4 times daily as needed; maximum single dose 20 g of ointment (1 g lidocaine), maximum total daily dose 60 g (3 g lidocaine).
| Dosage form | JELLY |
| Renal impairment | No dose adjustment required for topical lidocaine; systemic absorption is minimal. In severe renal impairment (eGFR <30 mL/min), monitor for lidocaine accumulation with prolonged use. |
| Liver impairment | In Child-Pugh Class B or C, reduce dose frequency to apply once or twice daily; avoid large surface area application. For severe hepatic impairment, consider alternative therapy. |
| Pediatric use | Apply a thin layer to affected area not more than 3-4 times daily; maximum single dose 4.5 mg/kg lidocaine, maximum total daily dose 12 mg/kg lidocaine. Not recommended for infants under 2 years due to risk of methemoglobinemia. |
| Geriatric use | Use with caution; apply smaller amount to limited area. Monitor for increased systemic absorption due to thinner skin and reduced clearance. Maximum single dose 15 g of ointment per application. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANESTACON (ANESTACON).
| Breastfeeding | Lidocaine is excreted into breast milk in small amounts. The milk-to-plasma ratio is approximately 0.4. At therapeutic maternal doses, the dose received by a nursing infant is less than 4% of the maternal weight-adjusted dose, which is considered compatible with breastfeeding. Caution is advised if high doses or prolonged use is required. |
| Teratogenic Risk | ANESTACON (lidocaine) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated teratogenic effects. There are no adequate and well-controlled studies in pregnant women. Use during first trimester should be avoided unless clearly necessary. In second and third trimesters, use is considered low risk when administered appropriately. Potential for fetal bradycardia exists with high maternal serum levels. |
■ FDA Black Box Warning
Not available.
| Serious Effects |
["Hypersensitivity to any component","Bacteremia","Use in eyes or ears"]
| Precautions | ["Excessive dosage may cause systemic toxicity including CNS and cardiovascular effects","Use with caution in patients with hepatic impairment","Avoid application to broken skin or large areas"] |
| Food/Dietary | No significant food interactions. Avoid concurrent consumption of grapefruit juice as it may theoretically increase systemic lidocaine levels, though clinical relevance is minimal. |
| Clinical Pearls |
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| Fetal Monitoring | Monitor maternal vital signs (heart rate, blood pressure, respiratory rate) and ECG during administration. Assess for signs of local anesthetic systemic toxicity (LAST). Fetal heart rate monitoring is recommended during labor and delivery if used as an epidural or spinal anesthetic. Observe for neonatal respiratory depression if high doses are used near delivery. |
| Fertility Effects | No known adverse effects on fertility in animal studies. In humans, no specific data on fertility impairment. Lidocaine is not expected to affect reproductive function at therapeutic doses. |
| ANESTACON (lidocaine/prilocaine) is a eutectic mixture of local anesthetics. Apply thickly to intact skin under occlusion for at least 1 hour for adequate dermal analgesia. Onset is slower on hairy or calloused skin. Avoid use on broken skin or mucous membranes due to risk of systemic absorption. Maximum application area is 600 cm² in adults. Methemoglobinemia risk is increased in patients with G6PD deficiency or concurrent use of sulfonamides. |
| Patient Advice | Apply a thick layer of cream to the treatment area and cover with the provided occlusive dressing. · Do not rub the cream into the skin; leave it in place for at least 1 hour before procedure. · Remove the cream and dressing just before the procedure; wash the area with soap and water. · Do not use on open wounds, rashes, or near the eyes or mouth. · Seek emergency care if you experience difficulty breathing, blue discoloration of lips or nails, or severe dizziness. |