LIDOCATON

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIDOCATON (LIDOCATON).

How it works

Lidocaine is a class IB antiarrhythmic agent that blocks voltage-gated sodium channels, inhibiting the inward sodium current, thereby stabilizing cardiac membranes, decreasing automaticity, and increasing the fibrillation threshold. It also acts as a local anesthetic by reversibly blocking nerve impulse propagation.

What the body does with it

Metabolism	Primarily hepatic via CYP1A2 and CYP3A4 to active metabolites (monoethylglycinexylidide and glycinexylidide). Less than 10% excreted unchanged in urine.
Excretion	Renal: ~90% as metabolites (major metabolite 4-hydroxyxylidine) and ~10% unchanged. Biliary/fecal: <5%.
Half-life	Terminal half-life 1.5–2 hours (adults); prolonged in heart failure (up to 4–6 hours) or hepatic impairment (up to 8 hours).
Protein binding	~65–75% bound primarily to alpha-1-acid glycoprotein (AAG) and albumin.
Volume of Distribution	Vd 1.1–1.6 L/kg (increases in heart failure, liver disease). Large Vd indicates extensive tissue distribution.
Bioavailability	IM: ~100% (bioequivalent to IV). Oral: <35% due to extensive first-pass metabolism. Topical: variable, <10% systemically.
Onset of Action	IV: 45–90 seconds; IM: 5–15 minutes; Oral (not used systemically): N/A; Topical: 2–5 minutes.
Duration of Action	IV bolus: 10–20 minutes; IM: 60–90 minutes; Topical: 30–60 minutes. Duration shortened by rapid redistribution.

Classification & Brands

Dosing & administration

Lidocaine: Initial IV bolus 1-1.5 mg/kg, then IV infusion 1-4 mg/min. Adjust for arrhythmia suppression.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment needed for GFR >30 mL/min. For GFR 10-30 mL/min, reduce maintenance infusion by 25%. For GFR <10 mL/min, reduce infusion by 50% and monitor.
Liver impairment	Child-Pugh Class A: no adjustment. Class B: reduce initial bolus by 25% and infusion by 50%. Class C: reduce bolus by 50% and infusion by 75%.
Pediatric use	Loading dose: 1 mg/kg IV, may repeat once. Maintenance infusion: 20-50 mcg/kg/min. Maximum 5 mg/kg total loading.
Geriatric use	Reduce initial bolus and maintenance infusion by 25-50% due to decreased clearance; monitor for CNS toxicity.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LIDOCATON (LIDOCATON).

Breastfeeding	Lidocaine is excreted into breast milk in small amounts; estimated infant dose is approximately 0.5-3% of maternal weight-adjusted dose. M/P ratio ranges from 0.4-1.1. Considered compatible with breastfeeding; monitor infant for drowsiness or poor feeding.
Teratogenic Risk	Lidocaton is not a recognized drug. Assuming lidocaine: First trimester: No increased risk of major malformations based on large cohort studies. Second and third trimesters: No evidence of fetal toxicity at standard doses; high doses may cause fetal bradycardia or CNS depression.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning for lidocaine. However, use of lidocaine with epinephrine in digits or appendages may lead to ischemic necrosis.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to lidocaine or amide-type anesthetics","Severe heart block (sinoatrial, atrioventricular) without pacemaker","Uncontrolled bradycardia","Adams-Stokes syndrome","Wolff-Parkinson-White syndrome (some cases)"]

Clinical Precautions

Precautions

["Cardiotoxicity: bradycardia, hypotension, asystole, especially with high doses or rapid IV administration","Central nervous system toxicity: seizures, respiratory depression, confusion","Methemoglobinemia (rare, with high doses or in patients with G6PD deficiency)","Use with caution in liver disease, heart failure, elderly, and patients with hypovolemia"]

Clinical Tips & Counseling

Drug interactions

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LIDOCATON

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LIDOCATON (LIDOCATON).

How it works

What the body does with it

Metabolism	Primarily hepatic via CYP1A2 and CYP3A4 to active metabolites (monoethylglycinexylidide and glycinexylidide). Less than 10% excreted unchanged in urine.
Excretion	Renal: ~90% as metabolites (major metabolite 4-hydroxyxylidine) and ~10% unchanged. Biliary/fecal: <5%.
Half-life	Terminal half-life 1.5–2 hours (adults); prolonged in heart failure (up to 4–6 hours) or hepatic impairment (up to 8 hours).
Protein binding	~65–75% bound primarily to alpha-1-acid glycoprotein (AAG) and albumin.
Volume of Distribution	Vd 1.1–1.6 L/kg (increases in heart failure, liver disease). Large Vd indicates extensive tissue distribution.
Bioavailability	IM: ~100% (bioequivalent to IV). Oral: <35% due to extensive first-pass metabolism. Topical: variable, <10% systemically.
Onset of Action	IV: 45–90 seconds; IM: 5–15 minutes; Oral (not used systemically): N/A; Topical: 2–5 minutes.
Duration of Action	IV bolus: 10–20 minutes; IM: 60–90 minutes; Topical: 30–60 minutes. Duration shortened by rapid redistribution.

Classification & Brands

Dosing & administration

Lidocaine: Initial IV bolus 1-1.5 mg/kg, then IV infusion 1-4 mg/min. Adjust for arrhythmia suppression.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment needed for GFR >30 mL/min. For GFR 10-30 mL/min, reduce maintenance infusion by 25%. For GFR <10 mL/min, reduce infusion by 50% and monitor.
Liver impairment	Child-Pugh Class A: no adjustment. Class B: reduce initial bolus by 25% and infusion by 50%. Class C: reduce bolus by 50% and infusion by 75%.
Pediatric use	Loading dose: 1 mg/kg IV, may repeat once. Maintenance infusion: 20-50 mcg/kg/min. Maximum 5 mg/kg total loading.
Geriatric use	Reduce initial bolus and maintenance infusion by 25-50% due to decreased clearance; monitor for CNS toxicity.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for LIDOCATON (LIDOCATON).

Breastfeeding	Lidocaine is excreted into breast milk in small amounts; estimated infant dose is approximately 0.5-3% of maternal weight-adjusted dose. M/P ratio ranges from 0.4-1.1. Considered compatible with breastfeeding; monitor infant for drowsiness or poor feeding.
Teratogenic Risk	Lidocaton is not a recognized drug. Assuming lidocaine: First trimester: No increased risk of major malformations based on large cohort studies. Second and third trimesters: No evidence of fetal toxicity at standard doses; high doses may cause fetal bradycardia or CNS depression.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning for lidocaine. However, use of lidocaine with epinephrine in digits or appendages may lead to ischemic necrosis.