LIDOCAINE HYDROCHLORIDE 0.4% 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 amide-type local anesthetic that blocks voltage-gated sodium channels in neuronal membranes, inhibiting the initiation and conduction of nerve impulses. Dextrose provides calories and does not have pharmacological activity.
| Metabolism | Lidocaine is primarily metabolized in the liver via oxidative N-dealkylation (CYP1A2, CYP3A4) to monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Dextrose is metabolized via glycolysis and the citric acid cycle. |
| Excretion | Renal: Approximately 90% of lidocaine is metabolized in the liver, and less than 10% is excreted unchanged in urine. The major metabolites (monoethylglycinexylidide and glycinexylidide) are excreted renally. Biliary/fecal excretion is minimal (<1%). |
| Half-life | Terminal elimination half-life: 1.5–2 hours after a single dose in healthy adults. In patients with hepatic impairment, heart failure, or prolonged infusion, half-life can increase to >3 hours due to reduced clearance. Neonates: 3–6.3 hours. |
| Protein binding | 60–80% bound primarily to alpha-1-acid glycoprotein (AAG). Binding is concentration-dependent and saturable at high doses. In conditions with elevated AAG (e.g., trauma, myocardial infarction), free fraction decreases. |
| Volume of Distribution | Vd: 1.1–1.6 L/kg. Rapid distribution to well-perfused tissues (brain, heart, liver, kidneys). Reflects extensive tissue binding; increased Vd in obesity (due to adipose tissue) and neonates (due to low protein binding). |
| Bioavailability | Oral: <35% due to extensive first-pass hepatic metabolism (dealkylation). Intramuscular: ~100% bioavailability (but slower absorption; peak at 10–15 min). Topical: Variable (5–20% depending on site and integrity of skin/mucosa). Epidural: Dosed to produce local effect; systemic absorption occurs with similar bioavailability to IM. |
| Onset of Action | Intravenous: 30–90 seconds (antiarrhythmic effect). Epidural: 5–15 minutes. Subcutaneous infiltration: <1 minute. Topical (e.g., on mucous membranes): 2–5 minutes. |
| Duration of Action | Intravenous: 10–20 minutes (antiarrhythmic effect). Epidural: 60–90 minutes. Subcutaneous: 30–120 minutes (depending on vasoconstrictor addition). Topical: 15–30 minutes. |
Intravenous administration: 1-1.5 mg/kg bolus, followed by 1-4 mg/min continuous infusion for ventricular arrhythmias. Maximum total dose: 3 mg/kg bolus; infusion for up to 24 hours. Note: 0.4% concentration = 4 mg/mL, 5% dextrose as diluent.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required for GFR; lidocaine is extensively hepatically metabolized. However, accumulation of metabolites may occur in severe renal impairment (GFR < 10 mL/min) but clinical significance is unclear. Caution advised. |
| Liver impairment | Child-Pugh Class A: Reduce infusion rate by 50%. Child-Pugh Class B: Reduce infusion rate by 75%. Child-Pugh Class C: Contraindicated or use only with extreme caution; reduce dose by 75-90% and monitor closely. Avoid loading doses in severe hepatic impairment. |
| Pediatric use | Loading dose: 1 mg/kg IV bolus, may repeat once after 5-10 minutes if needed (total max 2 mg/kg). Continuous infusion: 20-50 mcg/kg/min (0.02-0.05 mg/kg/min). Adjust based on response and toxicity. Use preservative-free formulations. |
| Geriatric use | Initiate at lower end of dosing range: reduce infusion rate by 50% due to decreased hepatic clearance and increased risk of toxicity. Monitor for CNS and cardiac adverse effects closely. |
| 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 low concentrations; the milk-to-plasma ratio (M/P) is approximately 0.4. The relative infant dose is estimated to be less than 1% of the maternal weight-adjusted dose. It is considered compatible with breastfeeding; however, monitor the infant for signs of lidocaine toxicity (e.g., irritability, drowsiness). |
| Teratogenic Risk |
■ FDA Black Box Warning
Not for IV or intra-arterial administration due to risk of systemic toxicity and neurological injury. Solutions containing dextrose are contraindicated in patients with known allergy to corn or corn products.
| Common Effects | ventricular arrhythmias |
| Serious Effects |
["Hypersensitivity to lidocaine, amide-type anesthetics, or any component.","Severe sinoatrial block, second- or third-degree AV block without a pacemaker.","Adams-Stokes syndrome.","Untreated hypovolemia."]
| Precautions | ["Use with extreme caution in patients with severe hepatic disease, heart block, or hypovolemia.","Monitor for signs of CNS toxicity (dizziness, confusion, seizures) and cardiovascular depression (bradycardia, hypotension).","Avoid extravasation (dextrose solutions can cause tissue necrosis)."] |
Loading safety data…
| Lidocaine hydrochloride is classified as FDA Pregnancy Category B. No teratogenic effects have been observed in animal studies, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed. In the first trimester, risk is low but not zero; second and third trimesters: fetal bradycardia may occur with high maternal serum levels or inadvertent intravascular injection. |
| Fetal Monitoring | Monitor maternal vital signs, ECG, and neurological status during administration. Fetal heart rate monitoring is recommended if administered during labor. After epidural or spinal use, assess maternal motor block, blood pressure, and signs of systemic toxicity (e.g., dizziness, perioral numbness, metallic taste). |
| Fertility Effects | No adverse effects on fertility have been reported in animal studies. Lidocaine is not known to impair human reproductive function at therapeutic doses. |