Pharmacologic Category
Antiarrhythmic Agent, Class Ib; Local Anesthetic
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.
* See Dosage and Administration in AHFS Essentials for additional information.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Renal Impairment: Adult
eGFR <30 mL/minute/1.73 m2: Administer lower maintenance infusion rate with close monitoring for toxicity.
Dosing: Hepatic Impairment: Adult
Administer lower maintenance infusion rate with close monitoring for toxicity.
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.
Dosing: Renal Impairment: Pediatric
Infants, Children, and Adolescents: There are no dosage adjustments provided in the manufacturer's labeling; however, accumulation of metabolites may be increased in renal dysfunction. Not dialyzable (0% to 5%) by hemo- or peritoneal dialysis; supplemental dose is not necessary (Aronoff 2007)
Dosing: Hepatic Impairment: Pediatric
Infants, Children and Adolescents: Use with caution; reduce dose. Monitor lidocaine concentrations closely and adjust infusion rate as necessary; consider alternative therapy. Maximum rate of continuous IV infusion: 20 mcg/kg/minute
Calculations
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]).
* See Uses in AHFS Essentials for additional information.
Use: Off-Label: Adult
Interstitial cystitis/bladder pain syndrome (alkalinized lidocaine)Level of Evidence [B, G]
Data from several controlled and noncontrolled trials suggest intravesical lidocaine (alkalinized) is effective in the management of interstitial cystitis/bladder pain syndrome Ref.
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 Ref. Access Full Off-Label Monograph
Sudden cardiac arrest due to ventricular fibrillation or pulseless ventricular tachycardiaLevel of Evidence [G]
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]).
Level of Evidence Definitions
Level of Evidence Scale
Class and Related Monographs
Clinical Practice Guidelines
Advanced Cardiac Life Support (ACLS)/Emergency Cardiovascular Care (ECC):
AHA, "2018 American Heart Association Focused Update on Advanced Cardiovascular Life Support Use of Antiarrhythmic Drugs During and Immediately After Cardiac Arrest," December 2018
AHA, “2015 American Heart Association Guidelines Update for Cardiopulmonary Resuscitation and Emergency Cardiovascular Care,” October 2015
AHA, "2010 Guidelines for Cardiopulmonary Resuscitation and Emergency Cardiovascular Care,” November 2010
AHA, “Cardiac Arrest in Pregnancy,” October 2015
Arrhythmias:
AHA/ACC/HRS, “2017 AHA/ACC/HRS Guideline for Management of Patients with Ventricular Arrhythmias and the Prevention of Sudden Cardiac Death,” October 2017
Trigeminal Neuralgia:
European Academy of Neurology, “European Academy of Neurology Guideline on Trigeminal Neuralgia,” 2019
Usual Infusion Concentrations: Pediatric
Note: Premixed solutions available
IV infusion: 8000 mcg/mL
Usual Infusion Concentrations: Adult
Note: Premixed solutions available
IV infusion: 1000 mg in 250 mL (concentration: 4 mg/mL) or 2000 mg in 250 mL (concentration: 8 mg/mL) of D5W
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.
Administration: Injectable Detail
pH: 5 to 7 (injection); 3.5 to 6 (premixed infusion solution in D5W)
Administration: Other
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).
Administration: Endotracheal
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.
Administration: Intraosseous
Intraosseous (off-label administration route): Intraosseous administration is a reasonable alternative when quick IV access is not feasible (ACLS, 2010).
Administration: Pediatric
Endotracheal: Infants, Children, and Adolescents: May administer dose undiluted, followed by flush with 5 mL of NS after endotracheal administration or may further dilute prior to administration; follow with 5 assisted manual ventilations (Hegenbarth 2008; PALS [Kleinman 2010]).
Parenteral:
IV push, Intraosseous: The manufacturer recommends that the rate of administration should not exceed 0.7 mg/kg/minute or 50 mg/minute, whichever is less; however, during acute situations (eg, pulseless VT or VF), administration by rapid IV push has been used by some clinicians in practice.
Continuous IV infusion: Administer via an infusion pump.
Dietary Considerations
Premixed injection may contain corn-derived dextrose and its use is contraindicated in patients with allergy to corn-related products.
Storage/Stability
Injection: Store at controlled room temperature. For products with an overwrap, do not remove overwrap until ready for use.
Preparation for Administration: Adult
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).
Preparation for Administration: Pediatric
Endotracheal: Pediatric patients: May dilute in 1 to 5 mL NS based on patient size (Hegenbarth 2008).
Parenteral:
IV:
Bolus: Preparation dependent upon product; solutions containing 40 to 200 mg/mL must be diluted prior to use to a concentration not to exceed 20 mg/mL. The injectable solution of 20 mg/mL may be administered undiluted.
Continuous IV infusion: Dilute in D5W or other compatible solution to a concentration of 1,000 to 8,000 mcg/mL (1 to 8 mg/mL) (Klaus 1989; Murray 2014; Phillips 2011); premix solution available for 4,000 and 8,000 mcg/mL (4 and 8 mg/mL).
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).
Compatibility
See Trissel’s IV Compatibility Database
Open Trissel's IV Compatibility
Medication Patient Education with HCAHPS Considerations
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.
Frequently reported side effects of this drug
• Pinpoint red spots on skin
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
• 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 a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of 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 brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
Medication Safety Issues
High alert medication:
International issues:
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.
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.
* See Cautions in AHFS Essentials for additional information.
Geriatric Considerations
Due to decreases in Phase I metabolism and possibly decrease in splanchnic perfusion with age, there may be a decreased clearance or increased half-life in the elderly and increased risk for CNS side effects and cardiac effects.
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]).
Breast-Feeding Considerations
Lidocaine is present in breast milk.
The relative infant dose (RID) of lidocaine is 4.9% when calculated using the highest breast milk concentration located and compared to a weight-adjusted maternal dose of 183 mg for epidural anesthesia.
In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
The RID of lidocaine was calculated using a mean milk concentration of 0.86 mcg/mL, providing an estimated daily infant dose via breast milk of 129 mcg/kg/day. This milk concentration was obtained following maternal administration lidocaine via local regional anesthesia to 22 women undergoing cesarean delivery. Milk was sampled 2 hours after the injection. Breast milk concentrations of lidocaine decreased over 12 hours (Ortega 1999). Lidocaine metabolites have also been detected in breast milk (Giuliani 2001; Lebedevs 1993; Puente 2001). Lower concentrations of lidocaine have been reported in breast milk following dental procedures, infusion for arrhythmias, and liposuction (Dryden 2000; Giuliani 2001; Lebedevs 1993; Zeisler 1986). Oral bioavailability to the breastfeeding infant is expected to be low (Lebedevs 1993; Ortega 1999).
Available guidelines consider lidocaine to be compatible with breastfeeding when used as an antiarrhythmic or local anesthetic (ABM [Reece-Stremtan 2017]; WHO 2002). Cumulative exposure from all routes of administration should be considered.
Briggs' Drugs in Pregnancy & Lactation
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
* See Cautions in AHFS Essentials for additional information.
Allergy and Idiosyncratic Reactions
Toxicology
Metabolism/Transport Effects
Substrate of CYP1A2 (major), CYP2A6 (minor), CYP2B6 (minor), CYP2C9 (minor), CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions Open Interactions
Amiodarone: May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy
Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Beta-Blockers: May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy
Bosentan: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy
Broccoli: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Risk C: 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. Risk D: Consider therapy modification
Cannabis: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Risk C: Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
CYP1A2 Inducers (Moderate): May decrease the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy
CYP1A2 Inhibitors (Strong): May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: 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. Risk D: Consider therapy modification
CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Risk D: 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). Risk D: Consider therapy modification
Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Risk C: Monitor therapy
Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: 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. Risk C: Monitor therapy
Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: 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. Risk D: Consider therapy modification
Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy
Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Etravirine: May decrease the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Risk C: Monitor therapy
Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: 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. Risk C: Monitor therapy
Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Local Anesthetics: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: 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. Risk D: 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. Risk D: Consider therapy modification
Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: 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. Risk C: Monitor therapy
Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: 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. Risk C: Monitor therapy
Saquinavir: May enhance the arrhythmogenic effect of Lidocaine (Systemic). Saquinavir may increase the serum concentration of Lidocaine (Systemic). Risk X: Avoid combination
Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy
Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: 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. Risk C: 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. Risk D: 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. Risk C: Monitor therapy
Tobacco (Smoked): May decrease the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy
Genes of Interest
Monitoring Parameters
Liver function tests, lidocaine concentrations, ECG; in patients requiring drug >24 hrs, blood level monitoring recommended; consult individual institutional policies and procedures
Reference Range
Therapeutic: 1.5 to 5.0 mcg/mL (SI: 6 to 21 micromole/L)
Potentially toxic: >6 mcg/mL (SI: >26 micromole/L)
Toxic: >9 mcg/mL (SI: >38 micromole/L)
Advanced Practitioners Physical Assessment/Monitoring
Dental/local anesthetic: Use caution to prevent gagging or choking. Avoid food or drink for 1 hour. Antiarrhythmic: IV: ECG and vital signs must be closely and continually monitored. Keep patient supine to reduce hypotensive effects. Assess frequently for adverse reactions or signs of CNS toxicity.
Nursing Physical Assessment/Monitoring
Dental/local anesthetic: Use caution to prevent gagging or choking. Avoid food or drink for 1 hour. Antiarrhythmic: IV: Monitor ECG, blood pressure, and respirations closely and continually. Keep patient supine to reduce hypotensive effects. Assess frequently for adverse reactions or signs of CNS toxicity (eg, drowsiness, lightheadedness, dizziness, tinnitus, blurred vision, vomiting, twitching, tremor, lethargy, coma, agitation, slurred speech, seizure, anxiety, euphoria, hallucinations, paresthesia, psychosis).
Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Kit, Injection, as hydrochloride:
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); 4% (5 mL [DSC]) [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)
Dosage Forms: Canada
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Injection, as hydrochloride:
Xylocaine: 0.5% (20 mL)
Xylocaine: 1% (20 mL, 50 mL); 2% (20 mL, 50 mL) [contains methylparaben]
Xylocaine Plain: 1% (2 mL, 5 mL, 10 mL); 2% (2 mL, 5 mL, 10 mL)
Generic: 10 mg/mL (5 mL, 10 mL, 20 mL, 50 mL); 1% (2 mL, 5 mL, 10 mL, 20 mL, 50 mL); 2% (2 mL, 5 mL, 10 mL, 20 mL, 50 mL)
Solution, Intravenous, as hydrochloride:
Xylocard: 2% [20 mg/mL] (5 mL)
Generic: 0.4% [4 mg/mL] (250 mL, 500 mL); 2% [20 mg/mL] (5 mL)
Anatomic Therapeutic Chemical (ATC) Classification
Generic Available (US)
Yes
Pricing: US
Kit (ReadySharp Lidocaine Injection)
1% (per each): $283.11
Solution (Lidocaine HCl (Cardiac) PF Intravenous)
100 mg/5 mL (per mL): $0.66
Solution (Lidocaine HCl (PF) Injection)
0.5% (per mL): $0.09
1% (per mL): $0.30 - $0.81
1.5% (per mL): $0.55
2% (per mL): $0.27 - $0.72
4% (per mL): $1.04
Solution (Lidocaine HCl Injection)
0.5% (per mL): $0.10
1% (per mL): $0.07 - $0.15
2% (per mL): $0.09 - $0.19
Solution (Lidocaine in D5W Intravenous)
4 mg/mL 5% (per mL): $0.01
8 mg/mL 5% (per mL): $0.02 - $0.04
Solution (Lidocaine in Dextrose Intraspinal)
5-7.5% (per mL): $5.47
Solution (Xylocaine Injection)
0.5% (per mL): $0.13
1% (per mL): $0.18
2% (per mL): $0.20
Solution (Xylocaine-MPF Injection)
0.5% (per mL): $0.30
1% (per mL): $0.38
1.5% (per mL): $0.80
2% (per mL): $0.75
Solution Prefilled Syringe (Lidocaine HCl (Cardiac) Intravenous)
50 mg/5 mL (per mL): $2.36
100 mg/5 mL (per mL): $0.81 - $1.38
Solution Prefilled Syringe (Lidocaine HCl (Cardiac) PF Intravenous)
50 mg/5 mL (per mL): $1.67
100 mg/5 mL (per mL): $0.78
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Mechanism of Action
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
Pharmacodynamics/Kinetics
Onset of action: Single bolus dose: 45 to 90 seconds
Duration: 10 to 20 minutes
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
Protein binding: 60% to 80% to alpha1 acid glycoprotein
Metabolism: 90% hepatic; active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX) can accumulate and may cause CNS toxicity
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
Excretion: Urine (<10% as unchanged drug, ~90% as metabolites)
Dental Use
Amide-type injectable local anesthetic
* See Uses in AHFS Essentials for additional information.
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Metallic taste.
Effects on Bleeding
No information available to require special precautions
Dental Usual Dosing
Dosage varies with the anesthetic procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient.
Anesthetic, local injectable: Children and Adults: Varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient; maximum: 4.5 mg/kg/dose not to exceed 300 mg; do not repeat within 2 hours.
Related Information
Index Terms
Lidocaine HCl; Lidocaine Hydrochloride; Lignocaine Hydrochloride
FDA Approval Date
November 30, 1948
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Brand Names: International
Anocaine (LB); Chalocaine (TH); Dequaspray (GB); Dolocaine (PH); Ecocain (AE, QA); Esracain (IL); Ke Ze Pu (CN); Lidocard (DK); Lignotox (ZW); Lignox (ZW); Locaine (PH); Locana (TH); Lox (ET); Lydocan (MY); Peterkaien (ZA); Procomil (LB); Rapidocain (CH); Roxicaina (EC); Sensinal (LB); Sensinil (CO); Themicain (IN); Xilonest (PE); Xylo-Efa 10% Cardiologica (UY); Xylobex (BD); Xylocaine (AE, BB, BH, CY, EG, JO, JP, KW, NZ, QA, SA); Xylocaine IV (TW); Xylocard (AT, BE, FR, IN, IS, NO, NZ, SE, SG, VN); Xylone (BD)
Last Updated 3/23/20