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Lidocaine (Systemic)

Class: Class Ib Antiarrhythmics
Molecular Formula: C25H28N6O3S•½C4H4 O4
CAS Number: 6108-05-0

Medically reviewed by Drugs.com. Last updated on Oct 20, 2020.

Introduction

Antiarrhythmic agent; an amide-type local anesthetic, class Ib agent.

Uses for Lidocaine (Systemic)

Ventricular Arrhythmias

Alternative to other antiarrhythmic drugs (e.g., amiodarone, procainamide, sotalol) for the acute treatment of life-threatening ventricular arrhythmias such as those that occur following MI or during cardiac manipulative procedures such as cardiac surgery.

Used during cardiac arrest for treatment of refractory (i.e., resistant to CPR, defibrillation, and a vasopressor [epinephrine]) VF or pulseless VT. Considered an alternative to amiodarone for this use in current ACLS guidelines in adults; in pediatric patients, current evidence supports use of either amiodarone or lidocaine.

Alternative to other antiarrhythmic agents or synchronized electrical cardioversion in the treatment of hemodynamically stable monomorphic VT; however, other agents (e.g., procainamide, sotalol, amiodarone) preferred.

Status Epilepticus

Treatment of status epilepticus, as a last resort.

Lidocaine (Systemic) Dosage and Administration

General

Ventricular Arrhythmias

  • Solutions containing epinephrine must not be used to treat arrhythmias.

  • Adjust dosage carefully according to individual requirements and response; constant ECG monitoring is recommended.

  • Terminate infusion as soon as the basic cardiac rhythm appears to be stable or at the earliest sign of toxicity. Immediately stop infusion if signs of excessive cardiac depression occur (e.g., prolongation of PR interval and QRS complex, appearance or aggravation of arrhythmias).

  • Infusions continued for >24 hours should be rarely necessary.

Administration

Administer IV. Has been administered IM (IM formulation no longer commercially available in the US).

Also has been administered via endotracheal tube or by intraosseous (IO) injection during cardiac resuscitation when IV administration is not possible. Although endotracheal administration also is possible, IV or IO administration is preferred because of more predictable drug delivery and pharmacologic effect. (See Absorption under Pharmacokinetics.)

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer as a bolus IV injection for initial treatment of ventricular arrhythmias. Maintenance IV infusions may be required to maintain normal sinus rhythm if oral antiarrhythmic therapy is not feasible.

Injections containing preservatives should not be given IV.

Do not introduce additives into solutions of lidocaine in 5% dextrose, since dosage is titrated to response.

Do not add to blood transfusion assemblies.

Do not use commercially available solutions of lidocaine in 5% dextrose in series connections with other plastic containers; such use could result in air embolism.

Rate of Administration

Administer IV bolus dose at a rate of 25–50 mg/minute.

Administer maintenance infusions at a rate of 1–4 mg/minute (14–57 mcg/kg per minute) in adults or 10–50 mcg/kg per minute in pediatric patients.

For other populations, see Special Populations under Dosage and Administration.

Endotracheal Administration

For endotracheal administration in adults, dilute dose in 5–10 mL of 0.9% sodium chloride injection or sterile water.

In pediatric patients, flush with 5 mL of 0.9% sodium chloride injection after dose is administered.

Dilution in sterile water may increase absorption of lidocaine.

Dosage

Available as lidocaine hydrochloride; dosage is expressed in terms of the salt.

Pediatric Patients

Ventricular Arrhythmias
IV

Controlled clinical studies to establish pediatric dosing have not been performed.

Some clinicians have suggested initial dose of 0.5–1 mg/kg as a rapid IV injection (i.e., bolus); dose may be repeated according to patient response, up to a maximum total dose of 3–5 mg/kg. Maintenance infusion of 10–50 mcg/kg per minute.

Pediatric Resuscitation
IV/IO

For shock-refractory VF or pulseless VT: 1 mg/kg initially, followed by maintenance infusion of 20–50 mcg/kg per minute. If time between initial bolus dose and onset of IV infusion >15 minutes, repeat bolus dose.

Endotracheal

Optimal dose not established, but usually 2–2.5 times the recommended IV dosage.

Adults

Ventricular Arrhythmias
IV

Usual initial dose is 50–100 mg administered as a direct IV injection. If desired response is not achieved, a second dose may be administered 5 minutes after completion of the first injection.

For hemodynamically stable monomorphic VT: AHA recommends initial dose of 1–1.5 mg/kg, followed by 0.5–0.75 mg/kg repeated at 5- to 10-minute intervals as necessary, up to a maximum total dose of 3 mg/kg.

ACLS
IV/IO

For refractory VF or pulseless VT: 1–1.5 mg/kg as initial loading dose, then 0.5–0.75 mg/kg repeated at 5- to 10-minute intervals as necessary, up to a total of 3 doses (or up to 3 mg/kg).

Endotracheal

Optimal dose not established, but usually 2–2.5 times the recommended IV dosage.

Status Epilepticus†
IV

Initially, 1 mg/kg. After 2 minutes, administer 0.5 mg/kg if seizure is not terminated. Maintenance infusion of 30 mcg/kg per minute for prevention of seizure recurrence.

Prescribing Limits

Adults

Ventricular Arrhythmias
IV

Maximum total dose of 200–300 mg over a 1-hour period.

Special Populations

Hepatic Impairment

Careful and individualized dosing recommended.

Renal Impairment

Dosage modification not required.

Decreased Cardiac Output

Smaller bolus doses may be required.

Some clinicians recommend infusion rates <30 mcg/kg per minute in patients with CHF.

Patients Requiring Prolonged Therapy

Possible increased half-life following infusions lasting>24 hours; reduce dosage accordingly (e.g., by 50%) to avoid accumulation of the drug and potential toxicity.

Cautions for Lidocaine (Systemic)

Contraindications

  • Adams-Stokes syndrome; severe degrees of SA, AV, or intraventricular heart block (unless a functioning pacemaker is present). Some manufacturers state that lidocaine is contraindicated in patients with Wolff-Parkinson-White syndrome.

  • Known hypersensitivity to amide-type local anesthetics.

Warnings/Precautions

Warnings

Cardiac Monitoring

Constant ECG monitoring is necessary during IV administration. Discontinue infusion if signs of excessive cardiac depression occur (e.g., prolongation of PR interval and QRS complex, appearance or aggravation of arrhythmias).

Severe Reactions

Resuscitative equipment and drugs should be immediately available for the management of severe adverse cardiovascular, respiratory, or CNS effects. Discontinue therapy if severe reactions occur; institute emergency resuscitative procedures and other supportive measures as required.

Severe reactions may be preceded by somnolence and paresthesia.

Sensitivity Reactions

Hypersensitivity

Possible hypersensitivity reactions (e.g., skin lesions, urticaria, edema, anaphylactoid reactions).

General Precautions

Prolonged Therapy

Possible increased half-life following infusions lasting >24 hours; reduce dosage accordingly (see Patients Requiring Prolonged Therapy under Dosage and Administration).

If maintenance therapy is necessary, an oral antiarrhythmic agent is recommended.

Nervous System Effects

Possible muscle twitching or tremors, seizures, unconsciousness, and coma; may be associated with high doses or overdosage.

Cardiovascular Effects

Possible hypotension, arrhythmias, heart block, cardiovascular collapse, and bradycardia, which may lead to cardiac arrest in patients with high plasma lidocaine concentrations or myocardial conduction defects.

Possible serious ventricular arrhythmias or heart block in patients with sinus bradycardia.

Possible increased sensitivity to cardiac depressant effects in patients with a diseased or abnormal sinus node.

Possible increased ventricular rate in patients with atrial fibrillation.

Possible increased coronary blood flow in patients with recent MI.

Possible myocardial and circulatory depression.

Cautious use recommended in patients with any form of heart block, CHF, marked hypoxia, severe respiratory depression, hypovolemia, or shock.

Respiratory Effects

Possible respiratory depression and arrest; may be associated with high doses or overdosage.

Local Effects

Possible local thrombophlebitis in patients receiving prolonged IV infusions.

Tissue infiltration may lead to local ischemia, tissue injury, and ulceration.

Laboratory Test Interference

Possible increased serum CK (CPK) concentrations associated with IM injections. Isoenzyme separation is necessary when CK determinations are used in the diagnosis of acute MI.

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk. Use with caution.

Pediatric Use

Safety and efficacy not established in controlled clinical studies; however, lidocaine has been used for treatment of ventricular arrhythmias in infants and children.

Hepatic Impairment

Use with caution. (See Pharmacokinetics and also see Hepatic Impairment under Dosage and Administration.)

Renal Impairment

Use with caution in severe renal impairment. (See Elimination: Special Populations, under Pharmacokinetics.)

Common Adverse Effects

Adverse CNS effects (e.g., drowsiness, dizziness, disorientation, confusion, lightheadedness, tremulousness, psychosis, nervousness, apprehension, agitation, euphoria, tinnitus, visual disturbances, paresthesia, difficulty swallowing, dyspnea, slurred speech, sensations of heat, cold, or numbness), nausea, vomiting.

Interactions for Lidocaine (Systemic)

Antiarrhythmic Agents

Potential pharmacologic interaction (additive or antagonistic cardiac effects and additive toxicity) with concomitant administration of antiarrhythmic agents (e.g., phenytoin, procainamide, propranolol, quinidine).

Specific Drugs

Drug

Interaction

Comments

Cimetidine

Decreased lidocaine clearance

Monitor serum lidocaine concentrations and observe closely for signs of lidocaine toxicity

Phenytoin

Possible increased lidocaine metabolism

Clinical importance unknown

Propranolol

Decreased lidocaine clearance

Monitor serum lidocaine concentrations and observe closely for signs of lidocaine toxicity

Succinylcholine

Increased neuromuscular blocking effect

Appears to be important only at lidocaine doses higher than those used clinically

Lidocaine (Systemic) Pharmacokinetics

Absorption

Bioavailability

Absorbed from the GI tract, but passes into hepatic circulation and only about 35% of an oral dose reaches the systemic circulation unchanged. Toxic effects appear at oral doses that fail to produce therapeutic plasma concentrations.

Following IM (deltoid) injection, peak plasma concentrations are achieved in 10 minutes.

Absorbed in trachea; when administered endotracheally, plasma concentrations generally lower than those achieved with vascular administration. Absorption is biphasic. Endotracheal absorption may be increased by diluting the drug in sterile water instead of 0.9% sodium chloride injection.

Onset

Following direct IV (bolus) administration of 50–100 mg, onset of action is 45–90 seconds.

Duration

Following direct IV (bolus) administration of 50–100 mg, duration is 10–20 minutes.

Plasma Concentrations

Plasma lidocaine concentrations of 1–5 mcg/mL are required to suppress ventricular arrhythmias; concentrations exceeding 5 mcg/mL associated with toxicity.

Distribution

Extent

Widely distributed into body tissues. Readily crosses the blood-brain barrier. Crosses the placenta and is distributed into milk.

Early, rapid decline in plasma concentrations is associated with distribution into highly perfused tissues (e.g., kidneys, lungs, liver, heart); slower elimination phase associated with metabolism and redistribution into skeletal muscle and adipose tissue.

Plasma Protein Binding

Binding is variable and concentration dependent; 60 –80% bound to plasma proteins at concentrations of 1–4 mcg/mL. Partially bound to α1-acid glycoprotein.

Special Populations

Volume of distribution is decreased in patients with CHF and increased in patients with liver disease.

Elimination

Metabolism

Approximately 90% of a parenteral dose is metabolized rapidly in the liver by de-ethylation to the active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX). Rate of metabolism appears to be limited by hepatic blood flow.

Elimination Route

Excreted in urine principally as metabolites.

Half-life

Lidocaine has an initial half-life of 7–30 minutes and a terminal half-life of 1.5–2 hours. Elimination half-lives of MEGX and GX are 2 and 10 hours, respectively.

Special Populations

Rate of metabolism of lidocaine may be decreased and the half-life increased in patients with liver disease. Major differences may exist in pharmacokinetics for different types of liver disease (e.g., cirrhosis, hepatitis); no consistent correlation established between clearance and severity of liver disease (as determined by liver function tests).

GX may accumulate in patients with renal failure.

In patients with MI, the half-lives of lidocaine and its metabolites appear to be prolonged.

In patients with CHF, half-life of lidocaine may be prolonged.

In individuals receiving continuous IV infusions lasting >24 hours, half-life of lidocaine may be prolonged.

Stability

Storage

Parenteral

Injection

25°C; may be exposed briefly to temperatures up to 40°C. Do not freeze; protect from excessive heat.

Extemporaneously prepared solutions (1–4 mg/mL in 5% dextrose injection) appear to be stable at room temperature for at least 24 hours.

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution CompatibilityHID

Compatible

Amino acids 4.25%, dextrose 25%

Dextrose 5% in Ringer’s injection, lactated

Dextrose 5% in sodium chloride 0.45 or 0.9%

Dextrose 5% in water

Ringer’s injection, lactated

Sodium chloride 0.45 or 0.9%

Drug Compatibility

Drugs that require low pH for stability (e.g., dopamine, epinephrine, norepinephrine, isoproterenol) may be adversely affected by the pH of lidocaine (5–7). Use such mixtures promptly after preparation or consider separate administration of the drugs. The manufacturers state that commercially available solutions of lidocaine hydrochloride in 5% dextrose should not be mixed with other drugs.

Admixture CompatibilityHID

Compatible

Alteplase

Aminophylline

Amiodarone HCl

Atracurium besylate

Calcium chloride

Calcium gluconate

Chloramphenicol sodium succinate

Chlorothiazide sodium

Ciprofloxacin

Dexamethasone sodium phosphate

Digoxin

Diphenhydramine HCl

Dobutamine HCl

Dopamine HCl

Ephedrine sulfate

Erythromycin lactobionate

Flumazenil

Furosemide

Heparin sodium

Hydrocortisone sodium succinate

Hydroxyzine HCl

Nafcillin sodium

Nitroglycerin

Penicillin G potassium

Pentobarbital sodium

Phenylephrine HCl

Potassium chloride

Procainamide HCl

Prochlorperazine edisylate

Ranitidine HCl

Sodium bicarbonate

Sodium lactate

Theophylline

Verapamil HCl

Incompatible

Methohexital sodium

Phenytoin sodium

Variable

Fentanyl citrate

Y-Site Injection CompatibilityHID

Compatible

Alteplase

Amiodarone HCl

Argatroban

Bivalirudin

Cefazolin sodium

Ceftaroline fosamil

Ciprofloxacin

Cisatracurium besylate

Clarithromycin

Daptomycin

Dexmedetomidine HCl

Diltiazem HCl

Dobutamine HCl

Dobutamine HCl with dopamine HCl

Dobutamine HCl with nitroglycerin

Dobutamine HCl with sodium nitroprusside

Dopamine HCl

Dopamine HCl with dobutamine HCl

Dopamine HCl with nitroglycerin

Dopamine HCl with sodium nitroprusside

Enalaprilat

Etomidate

Famotidine

Fenoldopam mesylate

Haloperidol lactate

Heparin sodium

Heparin sodium with hydrocortisone sodium succinate

Hetastarch in lactated electrolyte injection (Hextend)

Labetalol HCl

Levofloxacin

Linezolid

Meperidine HCl

Micafungin sodium

Morphine sulfate

Nicardipine HCl

Nitroglycerin

Nitroglycerin with dobutamine HCl

Nitroglycerin with dopamine HCl

Nitroglycerin with sodium nitroprusside

Palonosetron HCl

Potassium chloride

Propofol

Remifentanil HCl

Sodium nitroprusside

Sodium nitroprusside with dobutamine HCl

Sodium nitroprusside with dopamine HCl

Sodium nitroprusside with nitroglycerin

Theophylline

Tigecycline

Tirofiban HCl

Vasopressin

Warfarin sodium

Incompatible

Amphotericin B cholesteryl sulfate complex

Metoprolol tartrate

Actions

  • Membrane-stabilizing antiarrhythmic agent. Combines with fast sodium channels in their inactive state and inhibits recovery after repolarization in a time- and voltage-dependent manner. Exhibits rapid rates of attachment to and dissociation from transmembrane sodium channels.

  • Controls ventricular arrhythmias by suppressing automaticity in His-Purkinje system and by suppressing spontaneous depolarization of the ventricles during diastole.

  • Little effect on AV node conduction and His-Purkinje conduction in normal heart at therapeutic concentrations. Affects conducting tissues of ventricles more than atria. Variable effect on the effective refractory period (ERP) of the AV node; ERP and action potential duration of the His-Purkinje system are shortened.

  • Cardiac actions appear to be similar to those of phenytoin.

  • CNS depressant. Produces sedative, analgesic, and anticonvulsant effects. Suppresses cough and gag reflexes.

  • Produces little effect on autonomic tone; generally does not produce a substantial fall in BP, decreased myocardial contractility, or diminished cardiac output. Usually has little effect on heart rate.

Advice to Patients

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, and of concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Lidocaine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection, for direct IV injection

10 mg/mL*

Lidocaine Hydrochloride Injection for Cardiac Arrhythmias

20 mg/mL*

Lidocaine Hydrochloride Injection for Cardiac Arrhythmias

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Lidocaine Hydrochloride in Dextrose

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Parenteral

Injection, for IV infusion

4 mg/mL (1 or 2 g) Lidocaine Hydrochloride in 5% Dextrose*

0.4% Lidocaine Hydrochloride and 5% Dextrose Injection

8 mg/mL (2 or 4 g) Lidocaine Hydrochloride in 5% Dextrose*

0.8% Lidocaine Hydrochloride and 5% Dextrose Injection

AHFS DI Essentials™. © Copyright 2021, Selected Revisions October 30, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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