Lidocaine

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Special Alerts

Topical Anesthetic Use for Cosmetic or Medical Procedures: Public Health Advisory -
January 2009

The Food and Drug Administration (FDA) is issuing a Public Health Advisory to remind
consumers, caregivers, and healthcare professionals of potential life-threatening side effects
associated with the use of topical anesthetics available as prescription and over-the-counter
(OTC) products for a variety of uses, including numbing skin prior to cosmetic or medical
procedures (topical lidocaine has been recently evaluated to relieve mammography discomfort).
Topical application can result in high systemic levels and lead to toxic effects (eg, irregular heart
beats, seizures, coma, respiratory depression, death). At risk are consumers, particularly without
the supervision of trained professionals, who apply large amounts of anesthetics (or cover large
areas of the skin), leave these products on for long periods of time, or use materials, wraps, or
dressings to cover the skin after anesthetic application. The FDA is working with healthcare
professional organizations and other media to spread the message about the potential hazards and
safe use of topical anesthetics. The FDA is recommending that if topical anesthetics are needed
prior to procedures, consumers ask their healthcare provider for instructions on safe use of these
products, use only FDA-approved products, and use products with the lowest amount of
anesthetic while applying the least amount possible to relieve pain. If a high degree of pain is
expected that is not controlled by appropriate amounts of topical anesthetics, consumers should
ask their physician for alternatives techniques for pain control.

Additional information can be found at

http://www.fda.gov/medwatch/safety/2009/safety09.htm#Anesthetics

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

Akten™; 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™

Canadian Brand Names

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

Pharmacologic Category

Analgesic, Topical; Antiarrhythmic Agent, Class Ib; Local Anesthetic; Local Anesthetic,
Ophthalmic

Use: Labeled Indications

Local anesthetic and acute treatment of ventricular arrhythmias (such as from myocardial
infarction or cardiac manipulation)

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

Ophthalmic: To provide local anesthesia to ocular surface during ophthalmologic

procedures

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: Unlabeled/Investigational

ACLS guidelines (not considered drug of choice): Stable monomorphic VT (preserved

ventricular function), polymorphic VT (preserved ventricular function), drug-induced
monomorphic VT

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

Dosing: Adults

Antiarrhythmic:

I.V.: 1-1.5 mg/kg bolus over 2-3 minutes; may repeat doses of 0.5-0.75 mg/kg in 5-10
minutes up to a total of 3 mg/kg; continuous infusion: 1-4 mg/minute

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 I.V. dose

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

Anesthesia, local injectable: 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.

Anesthesia, ocular: Apply 2 drops to ocular surface in area where procedure will occur; may
reapply to maintain effect
Anesthetic, topical:

Cream:

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

L-M-Xâ„¢ 4: 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-Xâ„¢ 5: Relief of anorectal pain and itching: Rectal: Apply topically to clean, dry
area or using applicator, insert rectally, up to 6 times/day

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

Jelly: Maximum dose: 30 mL (600 mg) in any 12-hour period:

Anesthesia of male urethra: 5-30 mL (100-600 mg)

Anesthesia of female urethra: 3-5 mL (60-100 mg)

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

Liquid: Cold sores and fever blisters: Apply to affected area every 6 hours as needed

Patch: Postherpetic neuralgia: 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.

Dosing: Elderly

Refer to adult dosing.

Dosing: Pediatric

Antiarrhythmic:

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

Anesthetic, ocular: Refer to adult dosing

Anesthetic, topical:

Cream:

LidaMantle®: Skin irritation: Refer to adult dosing.

L-M-X™ 4: Children ≥2 years: Refer to adult dosing.

L-M-X™ 5: Relief of anorectal pain and itching: Rectal: Children ≥12 years:
Refer to adult dosing.

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

Liquid: Cold sores and fever blisters: Children ≥5 years: Refer to adult dosing.

Injectable local anesthetic: Refer to adult dosing.

Anesthesia, intradermal: Children 3-18 years: Zingoâ„¢: 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.

Dosing: Renal Impairment

Not dialyzable (0% to 5%) by hemo- or peritoneal dialysis; supplemental dose is not necessary.

Dosing: Hepatic Impairment

Reduce dose in acute hepatitis and decompensated cirrhosis by 50%.

Calculations

 Lidocaine

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: 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)

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 (Zingoâ„¢): 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.
 Dietary Considerations

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

Storage

Injection: 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.

Ophthalmic: Store at 15°C to 25°C (59°F to 77°F). Protect from light. Discard after use.

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.

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

Allergy Considerations

 Local Anesthetic Hypersensitivity/Allergy

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.

• Ophthalmic: For ophthalmic use only; not for injection. Prolonged use may cause
permanent corneal ulceration and/or opacification with loss of vision.

• 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, 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.

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 Risk Factor

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”)

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: Burning (ophthalmic), irritation (transdermal system), thrombophlebitis

Neuromuscular & skeletal: Pain exacerbation (transdermal system), paresthesia, transient

radicular pain (subarachnoid administration; up to 1.9%), tremor, twitching, weakness

Ocular: Conjunctival hyperemia (ophthalmic), corneal epithelial changes (ophthalmic),

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

Darunavir: May increase the serum concentration of Lidocaine. Risk C: Monitor therapy

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Risk C: Monitor
therapy

Deferasirox: May decrease the serum concentration 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

Fesoterodine: CYP2D6 Inhibitors may increase serum concentrations of the active metabolite(s)
of Fesoterodine. Risk C: Monitor therapy

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. Management: Limit the ranolazine dose to a maximum of 500mg twice daily in
patients concurrently receiving moderate CYP3A4 inhibitors (e.g., diltiazem, verapamil,
erythromycin, etc.). Risk D: Consider therapy modification

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.

Reference Range

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

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

Toxic: >9 mcg/mL (SI: >38 μmol/L)

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.

Monitoring: Lab Tests

I.V.: Serum lidocaine levels. Therapeutic levels range from 1.5-5 mcg/mL; >6 mcg/mL is
associated with toxicity.

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.

Ophthalmic: May cause burning when applied.

Pregnancy precaution: Inform prescriber if you are pregnant.

Dosage Forms

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

Aerosol, topical [foam]:

Anestafoamâ„¢: 4% (30 g) [contains benzalkonium chloride and benzyl alcohol]

Cream, rectal (L-M-Xâ„¢ 5): 5% (15 g) [contains benzyl alcohol; packaged with applicator]; (30
g) [contains benzyl alcohol]
Cream, topical (L-M-Xâ„¢ 4): 4% (5 g) [contains benzyl alcohol; packaged with Tegadermâ„¢
dressing]; (15 g, 30 g) [contains benzyl alcohol]

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

LidaMantle®: 3% (30 g, 85 g)

Gel, ophthalmic:

Aktenâ„¢: 3.5% (5 mL) [preservative free]

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:

Zingoâ„¢: 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)

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

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

Cream (LidaMantle)

3% (85): $139.15

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): $195.39

Ointment (Lidocaine)

5% (35.44): $15.99

Patch (Lidoderm)

5% (30): $206.47

Solution (Lidocaine HCl)

4% (50): $16.99

4% (100): $235.41

Solution (Lidocaine Viscous)

2% (100): $13.99

Solution (Xylocaine)

2% (50): $16.99
 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; Ophthalmic: 20
seconds to 5 minutes (median: 40 seconds)

Duration: 10-20 minutes; Intradermal: Decreases after 10 minutes; Ophthalmic: 5-30 minutes
(median: 15 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

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

Related Information

 Antiarrhythmic Drugs

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

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).

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.

Index Terms

Lidocaine Hydrochloride; Lignocaine Hydrochloride

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. [PubMed 16314375]

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.[PubMed 17056977]

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.[PubMed 11907287]

Foxall G, McCahon R, Lamb J, et al, "Levobupivacaine-Induced Seizures and Cardiovascular

Collapse Treated With Intralipid," Anaesthesia, 2007, 62(5):516-8.[PubMed 17448066]

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.[PubMed 16867094]

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.[PubMed 16810015]
 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)

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