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THE MERCK MANUAL MEDICAL LIBRARY: The Merck Manual of Diagnosis and Therapy
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Lidocaine Drug Information Provided by Lexi-Comp

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Medication Safety Issues

High alert medication: The Institute for Safe Medication Practices (ISMP) includes this medication (epidural administration; I.V. formulation) among its list of drugs which have a heightened risk of causing significant patient harm when used in error.

Transdermal patch may contain conducting metal (eg, aluminum); remove patch prior to MRI.

International issues:

Lidpen® may be confused with Linoten® which is a brand name for pamidronate in Spain

Pronunciation

(LYE doe kane)

U.S. Brand Names

  • Anestacon®
  • Anestafoam™ [OTC]
  • Band-Aid® Hurt-Free™ Antiseptic Wash [OTC]
  • Burn Jel® [OTC]
  • Burn-O-Jel [OTC]
  • Burnamycin [OTC]
  • L-M-X™ 4 [OTC]
  • L-M-X™ 5 [OTC]
  • LidaMantle®
  • Lidoderm®
  • LTA® 360
  • Premjact® [OTC]
  • Solarcaine® Aloe Extra Burn Relief [OTC]
  • Topicaine® [OTC]
  • Unburn®
  • Xylocaine®
  • Xylocaine® MPF
  • Xylocaine® Viscous
  • Zilactin-L® [OTC]
  • Zingo™

Index Terms

  • Lidocaine Hydrochloride
  • Lignocaine Hydrochloride

Generic Available

Yes: Cream, infusion, injection, jelly, lotion, ointment, solution

Canadian Brand Names

  • Betacaine®
  • Lidodan™
  • Lidoderm®
  • Xylocaine®
  • Xylocard®
  • Zilactin®

Pharmacologic Category

  • Analgesic, Topical
  • Antiarrhythmic Agent, Class Ib
  • Local Anesthetic

Pharmacologic Category Synonyms

  • Topical Analgesic
  • Class Ib Antiarrhythmic Agent
  • Vaughan-Williams Class Ib Antiarrhythmic
  • Anesthetic, Local

Use: Labeled Indications

Local anesthetic and acute treatment of ventricular arrhythmias from myocardial infarction, or cardiac manipulation

Intradermal: To provide local anesthesia prior to venipuncture or peripheral I.V. cannulation

Rectal: Temporary relief of pain and itching due to anorectal disorders

Topical: Local anesthetic for use in laser, cosmetic, and outpatient surgeries; minor burns, cuts, and abrasions of the skin

Lidoderm® Patch: Relief of allodynia (painful hypersensitivity) and chronic pain in postherpetic neuralgia

Use: Dental

Amide-type injectable local anesthetic and topical local anesthetic; Patch: Production of mild topical anesthesia of accessible mucous membranes of the mouth prior to superficial dental procedures

Use: Unlabeled/Investigational

ACLS guidelines (not considered drug of choice): Stable monomorphic VT (preserved ventricular function), polymorphic VT (preserved ventricular function), drug-induced monomorphic VT

Pregnancy Risk Factor

B

Pregnancy Considerations

Animal studies with lidocaine have not shown teratogenic effects. Use is not contraindicated during labor and delivery. Systemic exposure following use of the intradermal system is below the limit of detection.

Lactation

Enters breast milk (small amounts)/use caution (AAP rates “compatible”)

Contraindications

Hypersensitivity to lidocaine or any component of the formulation; hypersensitivity to another local anesthetic of the amide type; Adam-Stokes 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-related products

Warnings/Precautions

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:

• 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.

• Intradermal: For use on intact skin where adequate seal can be maintained. Do not apply to body orifices or mucous membranes. Use caution in patients with bleeding tendencies or platelet disorders; may have increased risk of superficial dermal bleeding. Safety and efficacy have not been established in children <3 years of age or adults.

• Intravenous: Constant ECG monitoring is necessary during I.V. administration. Use cautiously in hepatic impairment, any degree of heart block, Wolff-Parkinson-White syndrome, 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. 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.

• Topical: Do not leave on large body areas for >2 hours. Potentially life threatening side effects (eg, irregular heart beat, seizures, coma, respiratory depression, death) have occurred when used prior to cosmetic procedures. Observe young children closely to prevent accidental ingestion. Not for ophthalmic use. Some products are not recommended for use on mucous membranes; consult specific product labeling.

• Transdermal patch: Safety and efficacy have not been established in children.

Other warnings/precautions:

• CAST trial: In the Cardiac Arrhythmia Suppression Trial (CAST), recent (>6 days but <2 years ago) myocardial infarction patients with asymptomatic, nonlife-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.

Adverse Reactions

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

Frequency not defined.

Cardiovascular: Arrhythmia, bradycardia, arterial spasms, cardiovascular collapse, defibrillator threshold increased, edema, flushing, heart block, hypotension, sinus node supression, vascular insufficiency (periarticular injections)

Central nervous system: Agitation, anxiety, apprehension, coma, confusion, disorientation, dizziness, drowsiness, euphoria, hallucinations, headache, hyperesthesia, hypoesthesia, lethargy, lightheadedness, nervousness, psychosis, seizure, slurred speech, somnolence, unconsciousness

Dermatologic: Angioedema, bruising (transdermal system), contact dermatitis, depigmentation (transdermal system), edema of the skin, itching, petechia (transdermal system), pruritus, rash, urticaria

Gastrointestinal: Metallic taste, nausea, vomiting

Local: Irritation (transdermal system), thrombophlebitis

Neuromuscular & skeletal: Pain exacerbation (transdermal system), paresthesia, transient radicular pain (subarachnoid administration; up to 1.9%), tremor, twitching, weakness

Ocular: Diplopia, visual changes

Otic: Tinnitus

Respiratory: Bronchospasm, dyspnea, respiratory depression or arrest

Miscellaneous: Allergic reactions, anaphylactoid reaction, sensitivity to temperature extremes

Intradermal system: Application site reactions: Erythema (53%), petechiae (44%), edema (8%), bruising/burning/contusion/hemorrhage/pain (4%), pruritus (1%; equal to placebo)

Following spinal anesthesia: Positional headache (3%), shivering (2%) nausea, peripheral nerve symptoms, respiratory inadequacy and double vision (<1%), hypotension, cauda equina syndrome

Postmarketing and/or case reports: ARDS (inhalation), asystole, disorientation, methemoglobinemia, skin reaction

Metabolism/Transport Effects

Substrate of CYP1A2 (minor), 2A6 (minor), 2B6 (minor), 2C9 (minor), 2D6 (major), 3A4 (major); Inhibits CYP1A2 (strong), 2D6 (moderate), 3A4 (moderate)

Drug Interactions

Amiodarone: May decrease the metabolism of Lidocaine. Risk C: Monitor therapy

Bendamustine: CYP1A2 Inhibitors (Strong) may increase the serum concentration of Bendamustine. Concentrations of the active metabolites of bendamustine may be decreased. Risk C: Monitor therapy

Beta-Blockers: May decrease the metabolism of Lidocaine. Exceptions: Levobunolol; Metipranolol. Risk C: Monitor therapy

CYP1A2 Substrates: CYP1A2 Inhibitors (Strong) may decrease the metabolism of CYP1A2 Substrates. Risk D: Consider therapy modification

CYP2D6 Inhibitors (Moderate): May decrease the metabolism of CYP2D6 Substrates. Risk C: Monitor therapy

CYP2D6 Inhibitors (Strong): May decrease the metabolism of CYP2D6 Substrates. Risk D: Consider therapy modification

CYP2D6 Substrates: CYP2D6 Inhibitors (Moderate) may decrease the metabolism of CYP2D6 Substrates. Exceptions: Tamoxifen. Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification

CYP3A4 Substrates: CYP3A4 Inhibitors (Moderate) may decrease the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

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

Eplerenone: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eplerenone. Management: A lower starting dose of eplerenone (25 mg once daily) is recommended in patients with hypertension who are also taking drugs that are moderate inhibitors of CYP3A4. Risk D: Consider therapy modification

Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy

Maraviroc: CYP3A4 Inhibitors may increase the serum concentration of Maraviroc. Risk D: Consider therapy modification

P-Glycoprotein Inducers: May decrease the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy

P-Glycoprotein Inhibitors: May increase the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy

Pimecrolimus: CYP3A4 Inhibitors (Moderate) may decrease the metabolism of Pimecrolimus. Risk C: Monitor therapy

Ranolazine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ranolazine. Risk X: Avoid combination

Salmeterol: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Salmeterol. Risk C: Monitor therapy

Tamoxifen: CYP2D6 Inhibitors (Moderate) may decrease the metabolism of Tamoxifen. Specifically, CYP2D6 inhibitors may decrease the formation of highly potent active metabolites. Risk D: Consider therapy modification

Thioridazine: CYP2D6 Inhibitors may decrease the metabolism of Thioridazine. Risk X: Avoid combination

TraMADol: CYP2D6 Inhibitors (Moderate) may diminish the therapeutic effect of TraMADol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects. Risk C: Monitor therapy

Ethanol/Nutrition/Herb Interactions

Herb/Nutraceutical: St John's wort may decrease lidocaine levels; avoid concurrent use.

Storage

Lidocaine injection is stable at room temperature. Stability of parenteral admixture at room temperature (25°C) is the expiration date on premixed bag; out of overwrap stability is 30 days.

Reconstitution

Standard diluent: 2 g/250 mL D5W.

Compatibility

Stable in D5LR, D51/2NS, D5NS, D5W, LR, 1/4NS, NS.

Y-site administration: Compatible: Alteplase, amiodarone, cefazolin, ciprofloxacin, cisatracurium, clarithromycin, diltiazem, dobutamine, dobutamine with dopamine, dobutamine with nitroglycerin, dobutamine with sodium nitroprusside, dopamine, dopamine with nitroglycerin, dopamine with sodium nitroprusside, enalaprilat, etomidate, famotidine, gatifloxacin, haloperidol, heparin, heparin with hydrocortisone sodium succinate, inamrinone, labetalol, levofloxacin, linezolid, meperidine, morphine, nitroglycerin, nitroglycerin with sodium nitroprusside, potassium chloride, propofol, remifentanil, sodium nitroprusside, streptokinase, theophylline, tirofiban, vitamin B complex with C, warfarin. Incompatible: Amphotericin B cholesteryl sulfate complex, thiopental.

Compatibility in syringe: Compatible: Clonidine with fentanyl, glycopyrrolate, heparin, hydroxyzine, ketamine with morphine, metoclopramide, milrinone, moxalactam, nalbuphine. Incompatible: Cefazolin. Variable (consult detailed reference): Ampicillin, ceftriaxone, sodium bicarbonate.

Compatibility when admixed: Compatible: Alteplase, aminophylline, amiodarone, atracurium, bretylium, bupivacaine, calcium chloride, calcium gluconate, chloramphenicol, chlorothiazide, cimetidine, clonidine, dexamethasone sodium phosphate, digoxin, diphenhydramine, dobutamine, dopamine, ephedrine, erythromycin lactobionate, fentanyl, floxacillin, flumazenil, furosemide, heparin, hydrocortisone sodium succinate, hydroxyzine, insulin (regular), ketamine, mephentermine, metaraminol, morphine, nafcillin, nitroglycerin, penicillin G potassium, pentobarbital, phenylephrine, potassium chloride, procainamide, prochlorperazine edisylate, promazine, propafenone, ranitidine, sodium bicarbonate, sodium lactate, tetracaine, theophylline, verapamil, vitamin B complex with C. Incompatible: Amphotericin B, dacarbazine, methohexital, phenytoin. Variable (consult detailed reference): Epinephrine, isoproterenol, norepinephrine.

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: 45-90 seconds; Intradermal: 1-3 minutes

Duration: 10-20 minutes; Intradermal: decreases after 10 minutes

Absorption: Intradermal: Below limit of detection (<5 ng/mL)

Distribution: Vd: 1.1-2.1 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: 7-30 minutes; Terminal: Infants, premature: 3.2 hours, Adults: 1.5-2 hours

Dosage

Antiarrhythmic:

Children:

I.V., I.O.: Note: For use in pulseless VT or VF, give after defibrillation, CPR, and epinephrine:

Loading dose: 1 mg/kg (maximum 100 mg); follow with continuous infusion; may administer second bolus of 0.5-1 mg/kg if delay between bolus and start of infusion is >15 minutes

Continuous infusion: 20-50 mcg/kg/minute. Use 20 mcg/kg/minute in patients with shock, hepatic disease, cardiac arrest, mild CHF; moderate-to-severe CHF may require 1/2 loading dose and lower infusion rates to avoid toxicity.

E.T.: 2-3 mg/kg; flush with 5 mL of NS and follow with 5 assisted manual ventilations

Adults:

Ventricular fibrillation or pulseless ventricular tachycardia (after defibrillation, CPR, and vasopressor administration): I.V.: Initial: 1-1.5 mg/kg. Refractory ventricular tachycardia or ventricular fibrillation, a repeat 0.5-0.75 mg/kg bolus may be given every 5-10 minutes after initial dose for a maximum of 3 doses. Total dose should not exceed 3 mg/kg. Follow with continuous infusion (1-4 mg/minute) after return of perfusion. Reappearance of arrhythmia during constant infusion: 0.5 mg/kg bolus and reassessment of infusion.

E.T. (loading dose only): 2-2.5 times the recommended I.V. dose; dilute in 10 mL NS or distilled water. Note: Absorption is greater with distilled water, but causes more adverse effects on PaO2.

Hemodynamically stable VT: 0.5-0.75 mg/kg followed by synchronized cardioversion

Note: Decrease dose in patients with CHF, shock, or hepatic disease.

Anesthesia, topical:

Cream:

LidaMantle®: Skin irritation: Children and Adults: Apply to affected area 2-3 times/day as needed

L-M-X™ 4: Children ?2 years and Adults: Apply 1/4 inch thick layer to intact skin. Leave on until adequate anesthetic effect is obtained. Remove cream and cleanse area before beginning procedure.

L-M-X™ 5: Relief of anorectal pain and itching: Children ?12 years and Adults: Rectal: Apply topically to clean, dry area or using applicator, insert rectally, up to 6 times/day

Gel, ointment, solution: Adults: Apply to affected area ?3 times/day as needed (maximum dose: 4.5 mg/kg, not to exceed 300 mg)

Jelly:

Children ?10 years: Dose varies with age and weight (maximum dose: 4.5 mg/kg)

Adults (maximum dose: 30 mL [600 mg] in any 12-hour period):

Anesthesia of male urethra: 5-30 mL

Anesthesia of female urethra: 3-5 mL

Lubrication of endotracheal tube: Apply a moderate amount to external surface only

Liquid: Cold sores and fever blisters: Children ?5 years and Adults: Apply to affected area every 6 hours as needed

Patch: Postherpetic neuralgia: Adults: Apply patch to most painful area. Up to 3 patches may be applied in a single application. Patch may remain in place for up to 12 hours in any 24-hour period.

Anesthesia, intradermal: Children 3-18 years: Zingo™: 0.5 mg to site of venipuncture or peripheral I.V. cannulation, 1-3 minutes prior to procedure. Procedure should be started within 10 minutes of application.

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; do not repeat within 2 hours.

Dosage adjustment in renal impairment: Not dialyzable (0% to 5%) by hemo- or peritoneal dialysis; supplemental dose is not necessary.

Dosage adjustment in hepatic impairment: Reduce dose in acute hepatitis and decompensated cirrhosis by 50%.

Dental Usual Dosing

Anesthesia, topical:

Cold sores and fever blisters: Children ?5 years and Adults: Liquid: Apply to affected area every 6 hours as needed

Postherpetic neuralgia: Adults: Patch: Apply patch to most painful area. Up to 3 patches may be applied in a single application. Patch may remain in place for up to 12 hours in any 24-hour period.

Administration: I.V.

Use microdrip (60 drops/mL) or infusion pump to administer an accurate dose.

Infusion rates: 2 g/250 mL D5W (infusion pump should be used):

1 mg/minute: 7.5 mL/hour

2 mg/minute: 15 mL/hour

3 mg/minute: 22.5 mL/hour

4 mg/minute: 30 mL/hour

Buffered lidocaine for injectable local anesthetic: Add 2 mL of sodium bicarbonate 8.4% to 18 mL of lidocaine 1%

Administration: Topical

Gel (Topicaine®): Avoid mucous membranes; remove prior to laser treatment.

Transdermal: Apply to painful area of skin immediately after removal from protective envelope. May be cut to appropriate size. After removal from skin, fold used transdermal systems so the adhesive side sticks to itself. Remove immediately if burning sensation occurs. Wash hands after application.

Intradermal (Zingo™): Apply to intact skin do not use on mucous membranes. When placing intradermal injection system on skin, hold device perpendicular to skin and seal to avoid gaps between system and skin which would impair drug delivery. A “popping” sound will indicate dose has been discharged. If needed, may apply at a new location following failed attempt at venous access; do not apply multiple times at the same site.

Administration: Other

Endotracheal: Dilute in NS or distilled water. Absorption is greater with distilled water, but causes more adverse effects on PaO2. Pass catheter beyond tip of tracheal tube, stop compressions, spray drug quickly down tube. Follow immediately with several quick insufflations and continue chest compressions.

Administration: I.V. Detail

Local thrombophlebitis may occur in patients receiving prolonged I.V. infusions.

pH: 5-7 (injection); 3.5-6.0 (premixed infusion solution in D5W)

Reference Range

Therapeutic: 1.5-5.0 mcg/mL (SI: 6-21 ?mol/L)

Potentially toxic: >6 mcg/mL (SI: >26 ?mol/L)

Toxic: >9 mcg/mL (SI: >38 ?mol/L)

Dietary Considerations

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

Patient Education

I.V.: You will be monitored during infusion. Do not get up without assistance. Report dizziness, numbness, double vision, nausea, pain or burning at infusion site, nightmares, hearing strange noises, seeing unusual visions, or respiratory difficulty.

Dermatologic: You will experience decreased sensation to pain, heat, or cold in the area and/or decreased muscle strength (depending on area of application) until effects wear off; use necessary caution to reduce incidence of possible injury until full sensation returns. Report irritation, pain, persistent numbness, tingling, swelling; restlessness, dizziness, acute weakness; blurred vision; ringing in ears; or respiratory difficulty.

Dental/local anesthetic: Lidocaine can cause numbness of tongue, cheeks, and throat. Do not eat or drink for 1 hour after use. Take small sips of water at first to ensure that you can swallow without difficulty. Your tongue and mouth may be numb; use caution avoid biting yourself. Immediately report swelling of face, lips, or tongue

Transdermal patch: Patch may be cut to appropriate size. Apply patch to most painful area. Up to 3 patches may be applied in a single application. Patch may remain in place for up to 12 hours in any 24-hour period. Remove immediately if burning sensation occurs. Wash hands after application.

Pregnancy precaution: Inform prescriber if you are pregnant.

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.

Anesthesia and Critical Care Concerns/Other Considerations

Cardiac Arrest: Amiodarone was recently compared to lidocaine (ALIVE trial) in out-of-hospital cardiac arrest victims whose ventricular fibrillation was resistant to 3 defibrillation attempts in addition to epinephrine and a fourth defibrillation attempt (Dorian, 2002). Other inclusion criteria included ventricular fibrillation unrelated to trauma (or with other arrhythmias that converted to ventricular fibrillation) and recurrent ventricular fibrillation after successful initial defibrillation. This was a randomized, double-blind comparison. The primary endpoint was the number of patients who were admitted to the hospital intensive care unit alive. Three hundred and forty-seven patients were enrolled. The initial amiodarone dose was 5 mg/kg and the lidocaine dose was 1.5 mg/kg. If ventricular fibrillation persisted after another shock, then the study drug could be administered again (amiodarone 2.5 mg/kg, lidocaine 1.5 mg/kg). Significantly more amiodarone patients (?23%) were admitted to the hospital alive than lidocaine patients (12%). The majority (>90%) of patients in the ALIVE trial had ventricular fibrillation as the initial arrhythmia. The authors concluded that intravenous amiodarone is superior to lidocaine in the treatment of shock-resistant, out-of-hospital ventricular fibrillation. Lidocaine is not as effective as amiodarone for improving intermediate outcomes, but neither has improved survival until hospital discharge among patients with VF cardiac arrest.

Monitoring: Great care is needed in administration of lidocaine in the elderly and in patients with heart failure, shock, or hepatic disease, as toxic effects of lidocaine may become evident earlier in these patients. The half-life of lidocaine increases after 24-48 hours as the drug inhibits its own hepatic metabolism. The dose should be reduced after 24 hours or blood levels should be monitored. While lidocaine toxicity may elicit seizures, lidocaine may also cause respiratory arrest and cardiac toxicity (eg, sinus arrest, AV block, asystole, and hypotension).

Local anesthetic toxicity: Cardiac arrest: Lipid infusion has been used in animal studies and several human cases (Bupivacaine: Rosenblatt, 2006; Levobupivacaine: Foxall, 2007; Ropivacaine: Litz, 2006) where cardiovascular toxicity, unresponsive to conventional resuscitation, resulted. Additional information is available at http://www.lipidrescue.org. The protocol from the website is: 20% Fat Emulsion: 1.5 mL/kg administered over 1 minute, followed immediately by an infusion of 0.25 mL/kg/minute. Continue chest compressions (lipid must circulate). Repeat bolus every 3-5 minutes up to 3 mL/kg total dose until circulation restored. Continue infusion until hemodynamic stability is restored. Increase the infusion rate to 0.5 mL/kg/minute if BP declines. A maximum total dose of 8 mL/kg is recommended.

Cardiovascular Considerations

The prophylactic use of lidocaine in patients after myocardial infarction confers no benefit and in fact may be harmful. Great care is needed in administration of lidocaine in the elderly and in patients with heart failure, shock, or hepatic disease, as toxic effects of lidocaine may become evident earlier in these patients. This is especially problematic since lidocaine-induced seizures may induce extension of underlying myocardial infarction. It is important to recognize that lidocaine has a narrow therapeutic index. Severe toxicity may occur at levels slightly above the therapeutic range, particularly when lidocaine is administered together with other antiarrhythmic drugs. While lidocaine toxicity may elicit seizures, lidocaine may also cause respiratory arrest and cardiac toxicity (AV block, asystole, and hypotension).

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Metallic taste.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May rarely cause agitation, anxiety, euphoria, or hallucinations

Mental Health: Effects on Psychiatric Treatment

None reported

Nursing: Physical Assessment/Monitoring

Assess other medications patient may be taking for adverse interactions. Local anesthetic: Monitor for effectiveness of anesthesia and adverse reactions. Dental/local anesthetic: Use caution to prevent gagging or choking. Avoid food or drink for 1 hour. Teach patient adverse reactions to report; use and teach appropriate interventions to promote safety. Antiarrhythmic: I.V.: 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. Teach patient adverse reactions to report and appropriate interventions to promote safety.

Dosage Forms

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

Aerosol, topical [foam]:

Anestafoam™: 4% (30 g) [contains benzalkonium chloride and benzyl alcohol]

Cream, rectal (L-M-X™ 5): 5% (15 g) [contains benzyl alcohol; packaged with applicator]; (30 g) [contains benzyl alcohol]

Cream, topical (L-M-X™ 4): 4% (5 g) [contains benzyl alcohol; packaged with Tegaderm™ dressing]; (15 g, 30 g) [contains benzyl alcohol]

Cream, topical, as hydrochloride: 3% (30 g)

LidaMantle®: 3% (30 g, 85 g)

Gel, topical:

Burn-O-Jel: 0.5% (90 g)

Topicaine®: 4% (10 g, 30 g, 113 g) [contains alcohol 35%, benzyl alcohol, aloe vera, and jojoba]

Gel, topical, as hydrochloride:

Burn Jel®: 2% (3.5 g, 120 g)

Solarcaine® Aloe Extra Burn Relief: 0.5% (113 g, 226 g) [contains aloe vera gel and tartrazine]

Unburn®: 2.5% (3.5 g, 59 mL, 118 mL) [contains vitamin E]

Infusion, as hydrochloride [premixed in D5W]: 0.4% [4 mg/mL] (250 mL, 500 mL); 0.8% [8 mg/mL] (250 mL, 500 mL)

Injection, solution, as hydrochloride: 0.5% [5 mg/mL] (50 mL); 1% [10 mg/mL] (2 mL, 10 mL, 20 mL, 30 mL, 50 mL); 2% [20 mg/mL] (2 mL, 5 mL, 20 mL, 50 mL)

Xylocaine®: 0.5% [5 mg/mL] (50 mL); 1% [10 mg/mL] (10 mL, 20 mL, 50 mL); 2% [20 mg/mL] (1.8 mL, 10 mL, 20 mL, 50 mL)

Injection, solution, as hydrochloride [preservative free]: 0.5% [5 mg/mL] (50 mL); 1% [10 mg/mL] (2 mL, 5 mL, 30 mL); 1.5% [15 mg/mL] (20 mL); 2% [20 mg/mL] (2 mL, 5 mL, 10 mL); 4% [40 mg/mL] (5 mL)

Xylocaine®: 10% [100 mg/mL] (5 mL) [for ventricular arrhythmias]

Xylocaine® MPF: 0.5% [5 mg/mL] (50 mL); 1% [10 mg/mL] (2 mL, 5 mL, 10 mL, 30 mL); 1.5% [15 mg/mL] (10 mL, 20 mL); 2% [20 mg/mL] (2 mL, 5 mL, 10 mL); 4% [40 mg/mL] (5 mL)

Injection, solution, as hydrochloride [premixed in D7.5W, preservative free]: 5% (2 mL)

Xylocaine® MPF: 1.5% (2 mL) [DSC]

Jelly, topical, as hydrochloride: 2% (5 mL, 30 mL)

Anestacon®: 2% (15 mL) [contains benzalkonium chloride]

Xylocaine®: 2% (5 mL, 30 mL)

Liquid, topical (Zilactin®-L): 2.5% (7.5 mL)

Lotion, topical, as hydrochloride (LidaMantle®): 3% (177 mL)

Ointment, topical: 5% (37 g, 50 g)

Powder, intradermal, as hydrochloride:

Zingo™: 0.5 mg

Solution, topical, as hydrochloride: 4% [40 mg/mL] (50 mL)

Band-Aid® Hurt-Free™ Antiseptic Wash: 2% (180 mL)

LTA® 360: 4% [40 mg/mL] (4 mL) [packaged with cannula for laryngotracheal administration]

Xylocaine®: 4% [40 mg/mL] (50 mL)

Solution, viscous, as hydrochloride: 2% [20 mg/mL] (20 mL, 100 mL)

Xylocaine® Viscous: 2% [20 mg/mL] (100 mL, 450 mL)

Spray, topical:

Burnamycin: 0.5% (60 mL) [contains aloe vera gel and menthol]

Premjact®: 9.6% (13 mL)

Solarcaine® Aloe Extra Burn Relief: 0.5% (127 g) [contains aloe vera]

Transdermal system, topical (Lidoderm®): 5% (30s)

Pricing: U.S. (www.drugstore.com)

Cream (LidaMantle)

3% (85): $121.00

Cream (LMX 5)

5% (30): $59.99

Gel (Lidocaine HCl)

2% (10): $10.99

Kit (LMX 4 Plus)

4% (1): $47.59

Lotion (LidaMantle)

3% (177): $169.90

Ointment (Lidocaine)

5% (35.44): $15.99

Patch (Lidoderm)

5% (30): $197.58

Solution (Lidocaine HCl)

4% (50): $15.99

4% (100): $235.41

Solution (Lidocaine Viscous)

2% (100): $13.99

Solution (Xylocaine)

2% (50): $16.99

References

“2005 American Heart Association Guidelines for Cardiopulmonary Resuscitation and Emergency Cardiovascular Care. Part 12: Pediatric Advanced Life Support,” Circulation, 2005, 112(24 Suppl):167-87.

Corcoran W, Butterworth J, Weller RS, et al, "Local Anesthetic-Induced Cardiac Toxicity: A Survey of Contemporary Practice Strategies Among Academic Anesthesiology Departments," Anesth Analg, 2006, 103(5):1322-6.

Dorian P, Cass D, Schwartz B, et al, “Amiodarone as Compared With Lidocaine for Shock-Resistant Ventricular Fibrillation,” N Engl J Med, 2002, 346(12):884-90.

Foxall G, McCahon R, Lamb J, et al, "Levobupivacaine-Induced Seizures and Cardiovascular Collapse Treated With Intralipid," Anaesthesia, 2007, 62(5):516-8.

Litz RJ, Popp M, Stehr SN, et al, "Successful Resuscitation of a Patient With Ropivacaine-Induced Asystole After Axillary Plexus Block Using Lipid Infusion," Anaesthesia, 2006, 61(8):800-1.

Rosenblatt MA, Abel M, Fischer GW, et al, "Successful Use of a 20% Lipid Emulsion to Resuscitate a Patient After a Presumed Bupivacaine-Related Cardiac Arrest," Anesthesiology, 2006, 105(1):217-8.

International Brand Names

  • Aeroderm (ES)
  • Anelok (HR)
  • Anestecidan (ES)
  • Betacaine (IL, MX)
  • Cidancaina (ES)
  • Cuivasil Spray (IL)
  • Curadent (ES)
  • Dentinox (LU)
  • Dimecaina (CN)
  • Dube Spray (SG)
  • Dynexan (FR)
  • Esracain Jelly (IL)
  • Farmacaina (CO)
  • Gesicain Jelly (IN)
  • Gesicain Ointment (IN)
  • Gesicain Viscous (IN)
  • Hipoden (MX)
  • Lecasin (KP)
  • Leostesin Jelly (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE)
  • Leostesin Ointment (AE, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, IL, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, NE, NG, OM, QA, SA, SC, SD, SL, SN, SY, TN, TZ, UG, YE, ZA, ZM, ZW)
  • Lidocain (HU, PL)
  • Lidocain Braun (LU)
  • Lidocain Gel (BG, DE, FI, HN)
  • Lidocain Ointment (BG)
  • Lidocain Spray (BG, HN)
  • Lidocaina IV Braun (ES)
  • Lidocainhydrochlorid-Braun (LU)
  • Lidogel (PL)
  • Lidokain (HR)
  • Lidokaina (EE)
  • Lidokain[inj.] (HR)
  • Lidonest (ID)
  • Lignocain (PL)
  • Lignocaine Gel (AU)
  • Lignocainum (PL)
  • Lignocainum Hydrochloricum (PL)
  • Lignox (PL)
  • Ora (TW)
  • Otoralgyl (LU)
  • Penles (JP)
  • Peterkaien (ZA)
  • Plidocain (PL)
  • Roxicaina (CO)
  • Sedodent (HR)
  • Sensipharma (MX)
  • Solarcaine (HK)
  • Sunicaine (MX)
  • Uvega (MX)
  • Versatis Plaster (GB, IE)
  • Xilina (PL)
  • Xilocaina Viscosa (PT)
  • Xilonest Pomada (PE)
  • Xilotane Gel (PT)
  • Xilotane Oral (PT)
  • Xylocain (CZ)
  • Xylocain Aerosol (DK, SE)
  • Xylocain Creme (DK, NO)
  • Xylocain Gargle (FI, SE)
  • Xylocain Gel (AT, CH, DE, DK, FI, NO, SE)
  • Xylocain Liniment (DK)
  • Xylocain Ointment (AT, CH, DE, FI, SE)
  • Xylocain Salve (DK)
  • Xylocain Spray (AT, CH, DE, NO)
  • Xylocain Viscous (AT, CH)
  • Xylocain Viskos (DE, SE)
  • Xylocain Visks (FI)
  • Xylocaina (MX)
  • Xylocaina Ointment (IT)
  • Xylocaina Pomada (AR, BR)
  • Xylocaina Spray (IT)
  • Xylocaine (LU, PL)
  • Xylocaine Aerosol (AU, FR, HK, NL)
  • Xylocaine Gel (AE, BE, BH, CY, EG, FR, GB, GR, IE, IL, IQ, IR, JO, KW, LB, LY, OM, PK, QA, SA, SY, YE)
  • Xylocaine Heavy (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE)
  • Xylocaine Jalea (UY)
  • Xylocaine Jelly (BF, BJ, CI, ET, GH, GM, GN, HK, ID, IN, KE, LR, MA, ML, MR, MU, MW, NE, NG, NZ, PH, SC, SD, SL, SN, TN, TW, TZ, UG, ZA, ZM, ZW)
  • Xylocaine Ointment (AE, AU, BF, BH, BJ, CI, CY, EG, ET, GH, GM, GN, GR, IL, IN, IQ, IR, JO, KE, KW, LB, LR, LY, MA, ML, MR, MU, MW, MY, NE, NG, NL, OM, PH, QA, SA, SC, SD, SL, SN, SY, TH, TN, TW, TZ, UG, YE, ZA, ZM, ZW)
  • Xylocaine Pomada (VE)
  • Xylocaine Solution (FR)
  • Xylocaine Spray (BE, BF, BJ, CI, ET, FR, GH, GM, GN, GR, HK, ID, IL, KE, KP, LR, MA, ML, MR, MU, MW, MY, NE, NG, NL, PH, SC, SD, SL, SN, TH, TN, TW, TZ, UG, ZA, ZM, ZW)
  • Xylocaine Topical Solution (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LY, OM, QA, SA, SY, YE)
  • Xylocaine Viscosa (PY, VE)
  • Xylocaine Viscous (GB, IE, IN, MY, TH, TW)
  • Xylocaine Viscous Topical Solution (AU, GB)
  • Xylocaine Viscus (GR)
  • Xylocaine Viskeus Topical Solution (NL)
  • Xylocaine Visquese (FR)
  • Xylocaine Visqueuse (BE)
  • Xylocaine-Astra (LU)
  • Xylocard (AE, BH, CY, EG, IL, IQ, IR, JO, KW, LB, LU, LY, OM, QA, SA, SY, YE)
  • Xyloctin (DE)
  • Xylonibsa (ES)
  • Xylonor (ES)

Lexi-Comp.com

Last full review/revision September 2008

Content last modified September 2008

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