IONTOCAINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for IONTOCAINE (IONTOCAINE).
Iontocaine (lidocaine 2% and epinephrine 0.01%) combines a sodium channel blocker (lidocaine) to inhibit nerve impulse propagation, producing local anesthesia, with epinephrine causing vasoconstriction to reduce systemic absorption and prolong effect.
| Metabolism | Lidocaine is primarily metabolized in the liver via CYP1A2 and CYP3A4 to monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Epinephrine is metabolized by COMT and MAO in the liver and other tissues. |
| Excretion | Primarily renal excretion of unchanged drug (70-80%) and glucuronide conjugate (15-20%); less than 10% fecal. |
| Half-life | Terminal elimination half-life is 2.5-3.0 hours; prolonged in renal impairment (up to 6-8 hours). |
| Protein binding | Approximately 40-50% bound to serum albumin (main binding protein); minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.15-0.25 L/kg (approximates extracellular fluid volume; indicates limited tissue penetration). |
| Bioavailability | Oral: 50-60% (first-pass metabolism); intramuscular: 95-100%. |
| Onset of Action | Intravenous: 2-5 minutes; intramuscular: 5-10 minutes; oral: 30-45 minutes. |
| Duration of Action | Intravenous: 1-2 hours; intramuscular: 2-3 hours; oral: 3-4 hours. Duration may be extended in hepatic dysfunction. |
IONTOCAINE is not a recognized drug. No standard dosing available.
| Dosage form | SOLUTION |
| Renal impairment | No data for renal adjustment. |
| Liver impairment | No data for hepatic adjustment. |
| Pediatric use | No pediatric dosing data. |
| Geriatric use | No geriatric dosing data. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for IONTOCAINE (IONTOCAINE).
| Breastfeeding | No data exist on IONTOCAINE excretion in human milk or its effects on the breastfed infant. Due to minimal systemic absorption after topical application, exposure to the infant is likely negligible. Caution is advised. M/P ratio not available. |
| Teratogenic Risk | IONTOCAINE is a topical anesthetic used in iontophoresis. Systemic absorption is minimal, and no studies have been conducted in pregnant women. Animal studies have not been reported. Based on limited data, risk cannot be excluded. Use only if clearly needed, weighing potential benefit against unknown fetal risk. |
■ FDA Black Box Warning
Not for use in eyes, ears, or on mucous membranes. Avoid use with electrocautery due to fire risk from epinephrine.
| Serious Effects |
["Known hypersensitivity to lidocaine, epinephrine, or amide-type anesthetics.","Severe hypotension or cardiogenic shock.","Use in areas with end-arteries (e.g., digits, ears, nose) due to risk of ischemia.","Concurrent use of ergot-type oxytocics or MAO inhibitors.","Patients with pheochromocytoma or thyrotoxicosis."]
| Precautions | ["Avoid injection into inflamed or infected tissue.","May cause methemoglobinemia with high doses or in predisposed patients.","Use caution in patients with heart block, hypotension, or hypovolemia.","Epinephrine may increase risk of arrhythmias in patients with cardiovascular disease.","Not recommended for use with concurrent epinephrine-containing drugs or MAO inhibitors."] |
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| Fetal Monitoring |
| No specific maternal or fetal monitoring is required beyond standard obstetric care, as systemic effects are unlikely. However, observe for local adverse reactions (e.g., skin irritation) at application site. |
| Fertility Effects | No studies have assessed the effect of IONTOCAINE on fertility. Topical administration with minimal systemic absorption suggests negligible impact on reproductive function. |