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Lidocaine (Systemic)

Medically reviewed by Drugs.com. Last updated on Jul 25, 2020.

Pronunciation

(LYE doe kane)

Index Terms

  • Lidocaine HCl
  • Lidocaine Hydrochloride
  • Lignocaine Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Kit, Injection, as hydrochloride:

Lidomark 1/5: 1%

Lidomark 2/5: 2%

P-Care X: 1%

ReadySharp Lidocaine: 1%

Solution, Injection, as hydrochloride:

Xylocaine: 0.5% (50 mL); 1% (20 mL, 50 mL); 2% (10 mL, 20 mL, 50 mL) [contains methylparaben]

Generic: 0.5% (50 mL); 1% (2 mL, 10 mL, 20 mL, 50 mL); 2% (2 mL, 10 mL, 20 mL, 50 mL)

Solution, Injection, as hydrochloride [preservative free]:

Xylocaine-MPF: 0.5% (50 mL); 1% (2 mL, 5 mL, 10 mL, 30 mL); 1.5% (10 mL, 20 mL); 2% (2 mL, 5 mL, 10 mL) [methylparaben free]

Generic: 0.5% (50 mL); 1% (2 mL, 5 mL, 30 mL); 1.5% (20 mL); 2% (2 mL, 5 mL, 10 mL); 4% (5 mL)

Solution, Intraspinal, as hydrochloride [preservative free]:

Generic: Lidocaine 5% [50 mg/mL] and dextrose 7.5% (2 mL)

Solution, Intravenous, as hydrochloride:

Xylocaine (Cardiac): 2% [20 mg/mL] (5 mL [DSC])

Generic: 0.4% [4 mg/mL] (250 mL, 500 mL); 0.8% [8 mg/mL] (250 mL); 1% [10 mg/mL] (5 mL); 2% [20 mg/mL] (5 mL)

Solution, Intravenous, as hydrochloride [preservative free]:

Generic: 1% [10 mg/mL] (5 mL); 2% [20 mg/mL] (5 mL)

Brand Names: U.S.

  • Lidomark 1/5
  • Lidomark 2/5
  • P-Care X
  • ReadySharp Lidocaine
  • Xylocaine
  • Xylocaine (Cardiac) [DSC]
  • Xylocaine-MPF

Pharmacologic Category

  • Antiarrhythmic Agent, Class Ib
  • Local Anesthetic

Pharmacology

Class Ib antiarrhythmic; suppresses automaticity of conduction tissue, by increasing electrical stimulation threshold of ventricle, His-Purkinje system, and spontaneous depolarization of the ventricles during diastole by a direct action on the tissues; blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction

Distribution

Vd: 1.5 ± 0.6 L/kg; range: 0.7 to 2.7 L/kg; alterable by many patient factors; decreased in CHF and liver disease; crosses blood-brain barrier

Metabolism

90% hepatic; active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX) can accumulate and may cause CNS toxicity

Excretion

Urine (<10% as unchanged drug, ~90% as metabolites)

Onset of Action

Single bolus dose: 45 to 90 seconds

Duration of Action

10 to 20 minutes

Half-Life Elimination

Biphasic: Prolonged with congestive heart failure, liver disease, shock, severe renal disease; Initial: 7 to 30 minutes; Terminal: Infants, premature: 3.2 hours, Adults: 1.5 to 2 hours

Protein Binding

60% to 80% to alpha1 acid glycoprotein

Use: Labeled Indications

Local and regional anesthesia by infiltration, nerve block, epidural, or spinal techniques; acute treatment of ventricular arrhythmias (eg, due to acute myocardial infarction [MI] or during cardiac manipulation [eg, cardiac surgery]).

Note: The routine prophylactic use of lidocaine to prevent arrhythmia associated during ST-elevation MI or to suppress isolated ventricular premature beats, couplets, runs of accelerated idioventricular rhythm, and nonsustained ventricular tachycardia is not recommended (ACCF/AHA [O'Gara, 2013]).

Off Label Uses

Interstitial cystitis/bladder pain syndrome (alkalinized lidocaine)

Data from several controlled and noncontrolled trials suggest intravesical lidocaine (alkalinized) is effective in the management of interstitial cystitis/bladder pain syndrome [Nickel 2009], [Parsons 2012].

American Urological Association guidelines on the diagnosis and treatment of interstitial cystitis/bladder pain syndrome recommend intravesical lidocaine as a second-line treatment option; while evidence from controlled trials appears to support use, intravesical lidocaine offers only short-term relief (less than 2 weeks) in a subset of patients, and the procedure itself is associated with pain [AUA [Hanno 2014]].

Sudden cardiac arrest due to ventricular fibrillation or pulseless ventricular tachycardia

The 2015 American Heart Association (AHA) guidelines for the cardiopulmonary resuscitation and emergency cardiovascular care (adult advanced cardiovascular life support) and the 2018 AHA focused update on advanced cardiovascular life support use of antiarrhythmic drugs during and immediately after cardiac arrest support the use of lidocaine for treatment of sudden cardiac arrest due to ventricular fibrillation or pulseless ventricular tachycardia unresponsive to CPR, defibrillation, and vasopressor therapy (ACLS [Link 2015]; ACLS [Panchal 2018]).

Contraindications

Hypersensitivity to lidocaine or any component of the formulation; hypersensitivity to another local anesthetic of the amide type; Adam-Stokes syndrome; Wolff-Parkinson-White syndrome; severe degrees of SA, AV, or intraventricular heart block (except in patients with a functioning artificial pacemaker); premixed injection may contain corn-derived dextrose and its use is contraindicated in patients with allergy to corn or corn-related products

Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to ester local anesthetics (paraben-containing solutions only); antimicrobial preservative-containing solutions should not be used intra-or retro-ocularly or for epidural or spinal anesthesia or any route that would introduce solution into the cerebrospinal fluid or in doses ≥15 mL for other types of blockades.

Dosing: Adult

Anesthesia, local injectable: Varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient.

Cutaneous infiltration: Maximum: 4.5 mg/kg/dose not to exceed 300 mg; do not repeat within 2 hours.

Intraosseous line or infusion pain: Lidocaine 1% or 2% preservative-free solution: Intraosseous: Initial dose: 40 mg over 1 to 2 minutes; usual adult dose range and maximum: 20 to 50 mg/dose; after allowing lidocaine to dwell for up to 1 minute, follow with NS flush; immediately following the NS flush, some centers administer a second lower (50% dose reduction) lidocaine dose over 30 to 60 seconds (usual adult maximum repeat dose: 20 mg/dose); if discomfort reoccurs, may repeat doses at a maximum frequency of every 45 minutes during intraosseous access; maximum total dose not established (Philbeck 2010; Schalk 2011). Note: Intraosseous access devices have a minimum weight and age for a particular device in addition to specific instruction for insertion and validation; consult product specific information for more detail.

Interstitial cystitis (bladder pain syndrome) (off-label use): Intravesical:

Various dosage regimens of alkalinized lidocaine alone or with heparin (20,000 to 50,000 units) have been used. There is a risk of precipitation if proper alkalinization does not occur. Lidocaine stability and pH should be determined after the components have been mixed, prior to administration (Parsons 2012).

Single instillation: Single intravesical administration of lidocaine (200 mg)/heparin (50,000 units)/sodium bicarbonate (420 mg) in 15 mL of sterile water, instilled into the bladder via catheter and allowed to dwell for 30 minutes before drainage (Parsons 2012).

Weekly instillation: Weekly bladder instillations for 12 consecutive weeks with lidocaine 4% (5 mL)/heparin (20,000 units)/sodium bicarbonate 7% (25 mL), instilled into an empty bladder via catheter and allowed to dwell for 30 minutes before drainage (Nomiya 2013).

Daily instillation: Daily bladder instillations for 5 days with lidocaine (200 mg)/sodium bicarbonate 8.4% solution (final volume of 10 mL), instilled into an empty bladder and allowed to dwell for 1 hour before drainage (Nickel 2009).

Ventricular arrhythmias:

Sudden cardiac arrest due to ventricular fibrillation or pulseless ventricular tachycardia, unresponsive to cardiopulmonary resuscitation, defibrillation, and epinephrine (off-label use):

IV, intraosseous: Initial: 1 to 1.5 mg/kg bolus. If refractory ventricular fibrillation or pulseless ventricular tachycardia, repeat 0.5 to 0.75 mg/kg bolus every 5 to 10 minutes (maximum cumulative dose: 3 mg/kg). Follow with continuous infusion (1 to 4 mg/minute) after return of perfusion (ACLS [Link 2015]; ACLS [Neumar 2010]; ACLS [Panchal 2018]; AHA/ACC/HRS [Al-Khatib 2018]).

Reappearance of arrhythmia during continuous infusion: Give an additional 0.5 mg/kg bolus then increase infusion (Zipes 2000).

Endotracheal (loading dose only) (off-label route): 2 to 3.75 mg/kg (2 to 2.5 times the recommended IV dose); dilute in 5 to 10 mL NS or sterile water. Note: Absorption is greater with sterile water and results in less impairment of PaO2 (ACLS [Neumar 2010]).

Ventricular tachycardia, hemodynamically stable:

IV: 1 to 1.5 mg/kg; repeat with 0.5 to 0.75 mg/kg every 5 to 10 minutes as necessary (maximum cumulative dose: 3 mg/kg). Follow with continuous infusion of 1 to 4 mg/minute (AHA/ACC/HRS [Al-Khatib 2018]) or 20 to 50 mcg/kg/minute.

Note: For prolonged infusion (after 24 hours), reduce the rate of infusion by approximately one-half to compensate for the reduced elimination rate. Administer under constant ECG monitoring.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Ventricular fibrillation (VF) or pulseless ventricular tachycardia (VT), shock-refractory: Infants, Children, and Adolescents:

IV, Intraosseous (PALS [de Caen 2015]; PALS [Duff 2018]; PALS [Kleinman 2010]):

Loading dose: 1 mg/kg/dose; follow with continuous IV infusion; may administer second bolus if delay between initial bolus and start of infusion is >15 minutes.

Continuous IV infusion: 20 to 50 mcg/kg/minute. Per manufacturer, do not exceed 20 mcg/kg/minute in patients with shock, hepatic disease, cardiac arrest, or CHF.

Endotracheal: Loading dose: 2 to 3 mg/kg/dose; flush with 5 mL of NS and follow with 5 assisted manual ventilations (PALS [Kleinman 2010]).

Anesthesia, local injectable: Dose varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient.

Cutaneous infiltration: Children and Adolescents: Typically solutions with concentration <2% should be used (allow for larger volumes); maximum dose: 5 mg/kg/dose not to exceed the recommended adult maximum dose of 300 mg/dose; do not repeat within 2 hours (Kliegman 2016).

Intraosseous line or infusion pain: Infants, Children, and Adolescents: Lidocaine 1% or 2 % preservative-free solution: Intraosseous: Initial dose: 0.5 mg/kg over 1 to 2 minutes; usual adult dose range and maximum: 20 to 50 mg/dose; follow with NS flush; immediately following the NS flush, some centers administer a second lower (50% dose reduction) lidocaine dose over 30 to 60 seconds (usual adult maximum repeat dose: 20 mg/dose); if discomfort reoccurs, may repeat doses at a maximum frequency of every 45 minutes during intraosseous access; maximum total dose not established, some centers suggest that dose should not exceed: 3 mg/kg/24 hours (Hartholt 2010; Nagler 2011; Philbeck 2010; Schalk 2011). Note: Intraosseous access devices have a minimum weight and age for a particular device in addition to specific instruction for insertion and validation; consult product specific information for more detail.

Reconstitution

Local infiltration: Buffered lidocaine for injectable local anesthetic may be prepared: Add 2 mL of sodium bicarbonate 8.4% to 18 mL of lidocaine 1% (Christoph 1988).

Administration

IV:

Bolus: According to the manufacturer, may administer at 25 to 50 mg/minute. In the setting of cardiac arrest (eg, ventricular fibrillation or pulseless ventricular tachycardia), may be infused rapidly into a peripheral vein (Dorian, 2002).

Continuous infusion: After initial bolus dosing, may administer as a continuous infusion; refer to indication-specific infusion rates in dosing for detailed recommendations. In the setting of cardiac arrest, infusion may be initiated once patient has return of spontaneous circulation resulting from lidocaine administration; however, there is no evidence to support subsequent continuous infusion to prevent recurrence (ACLS [Peberdy 2010]). Local thrombophlebitis may occur in patients receiving prolonged IV infusions.

Endotracheal (off-label administration route): Dilute in NS or sterile water. Absorption is greater with sterile water and results in less impairment of PaO2 (Hahnel 1990). Stop compressions, spray drug quickly down tube. Flush with 5 mL of NS and follow immediately with several quick insufflations and continue chest compressions.

Intraosseous (IO; off-label administration route): Intraosseous administration is a reasonable alternative when quick IV access is not feasible (ACLS, 2010).

Intravesical (off-label use): Various regimens of alkalinized lidocaine (with or without heparin) have been instilled into the bladder

The On-Q® infusion pump is used to slowly administer local anesthetics (eg, bupivacaine, lidocaine, ropivacaine) to or around surgical wound sites and/or in close proximity to nerves for pre- or postoperative regional anesthesia. When infused directly into the shoulder, destruction of articular cartilage (chondrolysis) has occurred. On-Q® pumps should never be placed directly into any joint (see https://www.ismp.org/Newsletters/acutecare/archives/May09.asp).

Dietary Considerations

Premixed injection may contain corn-derived dextrose and its use is contraindicated in patients with allergy to corn-related products.

Storage

Injection: Store at controlled room temperature. For products with an overwrap, do not remove overwrap until ready for use.

Drug Interactions

Abametapir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Abametapir: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Avoid combination

Amiodarone: May increase the serum concentration of Lidocaine (Systemic). Monitor therapy

Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Beta-Blockers: May increase the serum concentration of Lidocaine (Systemic). Monitor therapy

Broccoli: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Monitor therapy

Bupivacaine (Liposomal): Lidocaine (Systemic) may enhance the adverse/toxic effect of Bupivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with topical lidocaine. Liposomal bupivacaine may be administered 20 minutes or more after the administration of lidocaine. Consider therapy modification

Cannabis: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Monitor therapy

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

CYP1A2 Inducers (Moderate): May decrease the serum concentration of Lidocaine (Systemic). Monitor therapy

CYP1A2 Inhibitors (Strong): May increase the serum concentration of Lidocaine (Systemic). Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Management: Consider avoiding this combination. Some combinations are specifically contraindicated by manufacturers; others may have recommended dose adjustments. If combined, monitor for increased substrate effects. Consider therapy modification

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Disopyramide: May enhance the arrhythmogenic effect of Lidocaine (Systemic). Disopyramide may increase the serum concentration of Lidocaine (Systemic). Specifically, the unbound/free fraction of lidocaine. Monitor therapy

Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Etravirine: May decrease the serum concentration of Lidocaine (Systemic). Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Monitor therapy

Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Lacosamide: Lidocaine (Systemic) may enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Monitor therapy

Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Local Anesthetics: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Monitor therapy

Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification

Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Monitor therapy

Nitric Oxide: May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Prilocaine: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents. Monitor therapy

Saquinavir: May enhance the arrhythmogenic effect of Lidocaine (Systemic). Saquinavir may increase the serum concentration of Lidocaine (Systemic). Avoid combination

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Sodium Nitrite: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Monitor therapy

Tobacco (Smoked): May decrease the serum concentration of Lidocaine (Systemic). Monitor therapy

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Adverse Reactions

Effects vary with route of administration. Many effects are dose-related.

1% to 10%:

Central nervous system: Headache (positional headache following spinal anesthesia: 3%), shivering (following spinal anesthesia: 2%), radiculopathy (≤2%; transient pain; subarachnoid administration)

Frequency not defined:

Cardiovascular: Bradycardia, cardiac arrhythmia, circulatory shock, coronary artery vasospasm, edema, flushing, heart block, hypotension (including following spinal anesthesia), local thrombophlebitis, vascular insufficiency (periarticular injections)

Central nervous system: Agitation, anxiety, apprehension, cauda equina syndrome (following spinal anesthesia), coma, confusion, disorientation, dizziness, drowsiness, euphoria, hallucination, hyperesthesia, hypoesthesia, intolerance to temperature, lethargy, loss of consciousness, metallic taste, nervousness, paresthesia, peripheral neuropathy (following spinal anesthesia), psychosis, seizure, slurred speech, twitching

Gastrointestinal: Nausea (including following spinal anesthesia), vomiting

Hypersensitivity: Anaphylactoid reaction, anaphylaxis, hypersensitivity reaction

Neuromuscular & skeletal: Tremor, weakness

Otic: Tinnitus

Respiratory: Bronchospasm, dyspnea, respiratory depression, respiratory insufficiency (following spinal anesthesia)

<1%, postmarketing, and/or case reports: Asystole, dermatological reaction, diplopia (following spinal anesthesia), methemoglobinemia

Warnings/Precautions

Concerns related to adverse effects:

• Intra-articular infusion related chondrolysis: Continuous intra-articular infusion of local anesthetics after arthroscopic or other surgical procedures is not an approved use; chondrolysis (primarily in the shoulder joint) has occurred following infusion, with some cases requiring arthroplasty or shoulder replacement.

• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).

Disease-related concerns:

• Hepatic dysfunction: Use extreme caution in patients with severe hepatic dysfunction; may have increased risk of lidocaine toxicity.

• Pseudocholinesterase deficiency: Use caution in patients with pseudocholinesterase deficiency; may have increased risk of lidocaine toxicity

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

• Injectable anesthetic: Follow appropriate administration techniques so as not to administer any intravascularly. Solutions containing antimicrobial preservatives should not be used for epidural or spinal anesthesia. Some solutions contain a bisulfite; avoid in patients who are allergic to bisulfite. Resuscitative equipment, medicine and oxygen should be available in case of emergency. Use products containing epinephrine cautiously in patients with significant vascular disease, compromised blood flow, or during or following general anesthesia (increased risk of arrhythmias). Adjust the dose for the elderly, pediatric, acutely ill, and debilitated patients.

• Intravenous: Constant ECG monitoring is necessary during IV administration. Use cautiously in hepatic impairment, HF, marked hypoxia, severe respiratory depression, hypovolemia, history of malignant hyperthermia, or shock. Increased ventricular rate may be seen when administered to a patient with atrial fibrillation. Use is contraindicated in patients with Wolff-Parkinson-White syndrome and severe degrees of SA, AV, or intraventricular heart block (except in patients with a functioning artificial pacemaker). Correct electrolyte disturbances, especially hypokalemia or hypomagnesemia, prior to use and throughout therapy. Correct any underlying causes of ventricular arrhythmias. Monitor closely for signs and symptoms of CNS toxicity. The elderly may be prone to increased CNS and cardiovascular side effects. Reduce dose in hepatic dysfunction and CHF.

Other warnings/precautions:

• CAST trial: In the Cardiac Arrhythmia Suppression Trial (CAST), recent (>6 days but <2 years ago) myocardial infarction patients with asymptomatic, non-life-threatening ventricular arrhythmias did not benefit and may have been harmed by attempts to suppress the arrhythmia with flecainide or encainide. An increased mortality or nonfatal cardiac arrest rate (7.7%) was seen in the active treatment group compared with patients in the placebo group (3%). The applicability of the CAST results to other populations is unknown. Antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmias.

Monitoring Parameters

Liver function tests, lidocaine concentrations, ECG; in patients requiring drug >24 hrs, blood level monitoring recommended; consult individual institutional policies and procedures

Pregnancy Considerations

Lidocaine and its metabolites cross the placenta and can be detected in the fetal circulation following maternal injection for anesthesia prior to delivery (Cavalli 2004; Mitani 1987).

Adverse reactions in the fetus/neonate may affect the CNS, heart, or peripheral vascular tone. Fetal heart monitoring is recommended by the manufacturer.

Lidocaine injection is approved for obstetric analgesia (eg, prior to epidural or spinal anesthesia). Lidocaine administered by local infiltration is used to provide analgesia prior to episiotomy and during repair of obstetric lacerations (ACOG 209 2019). Administration by the perineal route may result in greater absorption than administration by the epidural route (Cavalli 2004). Cumulative exposure from all routes of administration should be considered. The ACOG recommends that pregnant women should not be denied medically necessary surgery regardless of trimester. If the procedure is elective, it should be delayed until after delivery (ACOG 775 2019).

Medications used for the treatment of cardiac arrest in pregnancy are the same as in the nonpregnant woman. Doses and indications should follow current Advanced Cardiovascular Life Support guidelines. Appropriate medications should not be withheld due to concerns of fetal teratogenicity (AHA [Jeejeebhoy 2015]).

Patient Education

What is this drug used for?

• It is used to numb an area before a procedure.

• It is used to treat certain types of abnormal heartbeats.

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Pinpoint red spots on skin

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Injection site bleeding

• Burning

• Bruising

• Methemoglobinemia like blue or gray color of the lips, nails, or skin; abnormal heartbeat; seizures; severe dizziness or passing out; severe headache; fatigue; loss of strength and energy; or shortness of breath.

• Acidosis like confusion, fast breathing, fast heartbeat, abnormal heartbeat, severe abdominal pain, nausea, vomiting, fatigue, shortness of breath, or loss of strength and energy.

• Trouble breathing

• Slow breathing

• Shallow breathing

• Lightheadedness

• Fatigue

• Confusion

• Blurred vision

• Slow heartbeat

• Severe anxiety

• Burning or numbness feeling

• Restlessness

• Anxiety

• Vision changes

• Noise or ringing in the ears

• Dizziness

• Passing out

• Severe headache

• Twitching

• Sensation of warmth

• Sensation of cold

• Tremors

• Chest pain

• Mood changes

• Sexual dysfunction

• Inability to move

• Leaking of urine

• Bowel incontinence

• Trouble urinating

• Seizures

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.