LIDOCAINE HYDROCHLORIDE 0.1% AND DEXTROSE 5% IN PLASTIC CONTAINER
Clinical safety rating: safe
Beta-blockers may increase the risk of lidocaine toxicity Can cause CNS toxicity (seizures) and cardiovascular collapse.
Lidocaine is a sodium channel blocker, which stabilizes neuronal membranes and inhibits the initiation and conduction of nerve impulses. Dextrose 5% provides caloric support.
| Metabolism | Lidocaine undergoes extensive first-pass metabolism in the liver via cytochrome P450 (CYP1A2 and CYP3A4) to monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Dextrose is metabolized to glucose. |
| Excretion | Renal: approximately 10% unchanged; hepatic metabolism to 4-hydroxy-2,6-xylidine and glycylxylidide, which are excreted renally. Total renal excretion of metabolites and parent drug accounts for >95% of the dose. Fecal excretion is minimal (<5%). |
| Half-life | Terminal elimination half-life: 1.5–2.0 hours in adults with normal hepatic function. In patients with hepatic impairment or heart failure, half-life may be prolonged (>3 hours). Clinical context: short half-life requires continuous infusion for sustained antiarrhythmic effect. |
| Protein binding | 70–80% bound primarily to alpha-1-acid glycoprotein (AAG). Binding is concentration-dependent and can be affected by conditions altering AAG levels (e.g., inflammation, pregnancy). |
| Volume of Distribution | 1.1–1.6 L/kg. Distribuited widely into well-perfused tissues (brain, heart, liver, kidneys). Clinical meaning: reflects rapid distribution; loading dose required to achieve therapeutic levels quickly. |
| Bioavailability | Intravenous: 100%; Intramuscular: approximately 85–90% (due to first-pass metabolism); Oral: <35% (extensive first-pass hepatic metabolism); Topical (mucosal): variable 10–40% depending on site and integrity. |
| Onset of Action | Intravenous: 45–90 seconds; Intramuscular: 5–15 minutes; Epidural: 5–15 minutes; Topical: 2–5 minutes (mucous membranes). |
| Duration of Action | Intravenous: 10–20 minutes (antiarrhythmic effect); Epidural: 60–90 minutes; Infiltration: 30–120 minutes (with epinephrine up to 2 hours). Clinical note: duration is dose-dependent and may be prolonged in patients with reduced clearance. |
Intravenous: 50-100 mg bolus (1-2 mg/kg) over 2-3 minutes, followed by continuous infusion at 1-4 mg/min (20-50 mcg/kg/min). Total maximum dose: 300 mg over 1 hour.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR >30 mL/min. For GFR 15-30 mL/min: reduce infusion by 25% and monitor for toxicity. For GFR <15 mL/min: reduce infusion by 50% and monitor closely. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated or use with extreme caution; consider alternative. |
| Pediatric use | Loading dose: 1 mg/kg IV bolus; infusion: 20-50 mcg/kg/min. Maximum loading dose: 5 mg/kg. Use with caution in neonates; reduce dose by 50%. |
| Geriatric use | Reduce loading dose to 0.5-1 mg/kg; reduce infusion rate by 25-50% due to decreased clearance and increased risk of toxicity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Beta-blockers may increase the risk of lidocaine toxicity Can cause CNS toxicity (seizures) and cardiovascular collapse.
| FDA category | Animal |
| Breastfeeding | Lidocaine is excreted into breast milk in small amounts. Milk-to-plasma (M/P) ratio: approximately 0.4. Oral bioavailability in infants is low due to first-pass metabolism; clinically insignificant at maternal therapeutic doses. Dextrose 5% does not pose risk. American Academy of Pediatrics considers lidocaine compatible with breastfeeding. |
| Teratogenic Risk |
■ FDA Black Box Warning
Not applicable for this formulation (lidocaine HCl 0.1% and dextrose 5% in plastic container is not typically associated with FDA black box warnings; however, lidocaine solutions for systemic use may carry warnings for cardiac toxicity and resuscitative equipment must be available).
| Common Effects | ventricular arrhythmias |
| Serious Effects |
Absolute: Known hypersensitivity to lidocaine or amide-type anesthetics; severe heart block (second- or third-degree) without a pacemaker; severe hepatic disease. Relative: Hypovolemic states; concurrent use with Class I antiarrhythmic agents (e.g., tocainide, mexiletine).
| Precautions | Risk of cardiac toxicity (bradycardia, hypotension, arrhythmias) at high doses; caution in patients with hepatic impairment, heart failure, or hypovolemia; use with caution in elderly and debilitated patients; avoid intravascular injection; monitor for signs of CNS toxicity (dizziness, confusion, seizures). |
Loading safety data…
| Lidocaine crosses the placenta. First trimester: No well-controlled studies; animal studies not clearly indicative of risk. Second and third trimesters: Use in obstetrics (e.g., epidural anesthesia) is common; no evidence of major teratogenicity. High doses or prolonged use may cause fetal bradycardia or CNS depression. Dextrose 5% is standard maintenance solution without known teratogenic risk. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and oxygen saturation during intravenous infusion. Assess for signs of lidocaine toxicity (perioral numbness, metallic taste, tinnitus, seizures). Fetal heart rate monitoring recommended during obstetric use to detect bradycardia. Monitor maternal glucose levels if prolonged infusion of dextrose 5% is used, especially in diabetic patients. |
| Fertility Effects | No evidence of adverse effects on human fertility from lidocaine or dextrose 5%. Animal studies show no impairment of fertility at clinically relevant doses. |