LIDOCAINE HYDROCHLORIDE 0.8% IN 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.

How it works

Lidocaine is an amide-type local anesthetic that acts by blocking voltage-gated sodium channels in neuronal cell membranes, thereby inhibiting the initiation and conduction of nerve impulses. This stabilizes the neuronal membrane and produces a reversible loss of sensation.

What the body does with it

Metabolism	Primarily metabolized in the liver via oxidative N-dealkylation by CYP1A2 and CYP3A4 to monoethylglycinexylidide (MEGX) and further to glycinexylidide (GX).
Excretion	Lidocaine is primarily metabolized in the liver by CYP1A2 and CYP3A4 to active metabolites (MEGX, GX). Less than 10% is excreted unchanged in urine. Renal excretion accounts for about 20% of total clearance as metabolites and parent drug; fecal elimination is minimal (<5%).
Half-life	Terminal elimination half-life is approximately 1.5–2.0 hours after a single IV dose. In patients with heart failure or hepatic impairment, it may be prolonged to >3 hours. After continuous infusion, the half-life may increase due to accumulation.
Protein binding	60–80% bound primarily to albumin and alpha1-acid glycoprotein (AAG). Binding is saturable and decreases in conditions with low AAG (e.g., neonates) or high lidocaine concentrations.
Volume of Distribution	Vd = 1.1–2.1 L/kg. Volume increases in heart failure (due to reduced cardiac output) and decreases in hemorrhagic shock.
Bioavailability	Oral bioavailability is very low (≈35%) due to extensive first-pass metabolism. For IV administration, bioavailability is 100%. For epidural or local infiltration, bioavailability is essentially 100% as the drug is not subject to first-pass elimination at the site.
Onset of Action	IV administration: 45–90 seconds. For epidural or peripheral nerve block: 5–15 minutes. For topical application: 2–5 minutes.
Duration of Action	IV bolus (antiarrhythmic): 10–20 minutes. Infusion: during infusion and short-lived after discontinuation. Epidural: 60–90 minutes (with epinephrine). Local infiltration: 30–120 minutes (dose-dependent).

Classification & Brands

Dosing & administration

Intravenous administration: 1-1.5 mg/kg bolus, followed by 1-4 mg/min continuous infusion for ventricular arrhythmias. Max dose: 3 mg/kg bolus, 4 mg/min infusion.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for mild-moderate renal impairment. In severe renal impairment (CrCl <10 mL/min), reduce infusion rate by 25-50% due to accumulation of metabolites.
Liver impairment	Child-Pugh Class A: Reduce loading dose by 50% and infusion rate by 50%. Child-Pugh Class B or C: Contraindicated or use with extreme caution; reduce infusion rate by 75% and monitor closely.
Pediatric use	Intravenous: Loading dose 1 mg/kg, may repeat once after 5-10 min. Continuous infusion: 20-50 mcg/kg/min. Max: 100 mcg/kg/min.
Geriatric use	Reduce loading dose and infusion rate by 50% due to decreased hepatic clearance and increased risk of toxicity. Monitor for CNS and cardiac effects.

Use during pregnancy

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 with a milk-to-plasma ratio of approximately 0.4. Amount ingested is <4% of maternal weight-adjusted dose; considered compatible with breastfeeding. Monitor infant for drowsiness.
Teratogenic Risk	Lidocaine crosses the placenta. In first trimester, no major malformations reported in human studies, but risk of fetal bradycardia if high maternal levels. In second and third trimesters, placental transfer can cause fetal acidosis and CNS depression. Use only if clearly needed.

Warnings & precautions

■ FDA Black Box Warning

NOT FOR SPINAL ANESTHESIA due to risk of hypotension and cardiac arrest when used for spinal anesthesia.

Side Effect Profile

Common Effects	ventricular arrhythmias
Serious Effects

Absolute Contraindications

["Hypersensitivity to lidocaine or amide-type local anesthetics","Severe heart block (second- or third-degree) without pacemaker","Severe hypotension or cardiogenic shock","Use for spinal anesthesia (contraindicated in formulation)"]

Clinical Precautions

Precautions

["Risk of systemic toxicity with inadvertent intravascular injection","Use caution in patients with heart block, hepatic impairment, or severe hypotension","Epidural or caudal anesthesia may cause hypotension, bradycardia, or respiratory arrest","Potential for methemoglobinemia (rare)","Monitor for signs of CNS toxicity (dizziness, confusion, seizures) and cardiac toxicity (arrhythmias, cardiac arrest)"]

Clinical Tips & Counseling

Drug interactions

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LIDOCAINE HYDROCHLORIDE 0.8% IN 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.

How it works

What the body does with it

Metabolism	Primarily metabolized in the liver via oxidative N-dealkylation by CYP1A2 and CYP3A4 to monoethylglycinexylidide (MEGX) and further to glycinexylidide (GX).
Excretion	Lidocaine is primarily metabolized in the liver by CYP1A2 and CYP3A4 to active metabolites (MEGX, GX). Less than 10% is excreted unchanged in urine. Renal excretion accounts for about 20% of total clearance as metabolites and parent drug; fecal elimination is minimal (<5%).
Half-life	Terminal elimination half-life is approximately 1.5–2.0 hours after a single IV dose. In patients with heart failure or hepatic impairment, it may be prolonged to >3 hours. After continuous infusion, the half-life may increase due to accumulation.
Protein binding	60–80% bound primarily to albumin and alpha1-acid glycoprotein (AAG). Binding is saturable and decreases in conditions with low AAG (e.g., neonates) or high lidocaine concentrations.
Volume of Distribution	Vd = 1.1–2.1 L/kg. Volume increases in heart failure (due to reduced cardiac output) and decreases in hemorrhagic shock.
Bioavailability	Oral bioavailability is very low (≈35%) due to extensive first-pass metabolism. For IV administration, bioavailability is 100%. For epidural or local infiltration, bioavailability is essentially 100% as the drug is not subject to first-pass elimination at the site.
Onset of Action	IV administration: 45–90 seconds. For epidural or peripheral nerve block: 5–15 minutes. For topical application: 2–5 minutes.
Duration of Action	IV bolus (antiarrhythmic): 10–20 minutes. Infusion: during infusion and short-lived after discontinuation. Epidural: 60–90 minutes (with epinephrine). Local infiltration: 30–120 minutes (dose-dependent).

Classification & Brands

Dosing & administration

Intravenous administration: 1-1.5 mg/kg bolus, followed by 1-4 mg/min continuous infusion for ventricular arrhythmias. Max dose: 3 mg/kg bolus, 4 mg/min infusion.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for mild-moderate renal impairment. In severe renal impairment (CrCl <10 mL/min), reduce infusion rate by 25-50% due to accumulation of metabolites.
Liver impairment	Child-Pugh Class A: Reduce loading dose by 50% and infusion rate by 50%. Child-Pugh Class B or C: Contraindicated or use with extreme caution; reduce infusion rate by 75% and monitor closely.
Pediatric use	Intravenous: Loading dose 1 mg/kg, may repeat once after 5-10 min. Continuous infusion: 20-50 mcg/kg/min. Max: 100 mcg/kg/min.
Geriatric use	Reduce loading dose and infusion rate by 50% due to decreased hepatic clearance and increased risk of toxicity. Monitor for CNS and cardiac effects.

Use during pregnancy

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 with a milk-to-plasma ratio of approximately 0.4. Amount ingested is <4% of maternal weight-adjusted dose; considered compatible with breastfeeding. Monitor infant for drowsiness.
Teratogenic Risk	Lidocaine crosses the placenta. In first trimester, no major malformations reported in human studies, but risk of fetal bradycardia if high maternal levels. In second and third trimesters, placental transfer can cause fetal acidosis and CNS depression. Use only if clearly needed.

Warnings & precautions

■ FDA Black Box Warning

NOT FOR SPINAL ANESTHESIA due to risk of hypotension and cardiac arrest when used for spinal anesthesia.

Side Effect Profile

Common Effects	ventricular arrhythmias
Serious Effects