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Special Alerts
Chondrolysis Reported With Continuous Intra-articular Infusions of Local Anesthetics - November 2009
The U.S. Food and Drug Administration (FDA) is notifying healthcare professionals and patients of the recent reporting of 35 cases of chondrolysis following continuous intra-articular infusion of local anesthetics (eg, bupivacaine, chloroprocaine, lidocaine, mepivacaine, procaine, ropivacaine) via elastomeric infusion devices; some of these patients were otherwise healthy young adults. Affected patients received these agents (with and without epinephrine) for extended periods of time (eg, 48-72 hours) to control postsurgical pain, mainly following shoulder surgery. The onset of symptoms of chondrolysis occurred as early as 2 months following treatment (median: 5 months); symptoms included joint pain, stiffness, and loss of motion. More than half of these patients required repeat surgery (eg, arthroscopy, arthroplasty) as a result of the chondrolysis.
The mechanism by which the intra-arterial infusion of local anesthetics results in chondrolysis has not been identified; possible factors may include the drug, elastomeric infusion device, and/or other unknown factors. Clinicians should note that single intra-articular injections of local anesthetics have been used safely during orthopedic procedures for years without resulting in chondrolysis.
Healthcare professionals are reminded that the intra-articular administration of local anesthetics is not an FDA-approved route of administration. In addition, no infusion device, including elastomeric infusion devices, are FDA-approved for continuous intra-articular infusions. The FDA has encouraged clinicians to consult and follow the approved drug and device labeling recommendations with regard to proper administration.
In the event that a patient receives a continuous intra-articular infusion of local anesthetic, the patient should be monitored for the development of chondrolysis; symptoms may take months to develop.
Further information may be found at http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm190302.htm
Transdermal Patches: Risk of Burns During MRI - March 2009
The U.S. Food and Drug Administration (FDA) has issued a public health advisory regarding the risk of burns associated with the use of transdermal medication patches containing aluminum or other metals during MRI screening. The package labeling for certain metal-containing patches includes a warning related to the risk of burns if the patches are not removed prior to MRI procedures. However, not all transdermal medication patches with metallic backings have this warning in the labeling. Although metal materials are present in certain patches, it may not be visible. The FDA is currently reviewing the components of all transdermal medication systems to ensure that proper warnings are present in the labeling of those patches that do contain metal materials. In the interim, the FDA recommends that healthcare professionals who refer patients to have an MRI procedure should identify patients who are wearing a transdermal medication patch prior to the scan. Those patients who are wearing a transdermal medication patch should be advised on the proper removal of the patch prior to the procedure as well as reapplication following the scan.
Additional information can be found at http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm111493.htm
Topical Anesthetic Use for Cosmetic or Medical Procedures: Public Health Advisory - January 2009; Updated March 2009
Health Canada has issued a “Dear Healthcare Professional” letter and a notice to the Canadian public regarding important safety information associated with the use of topical anesthetic agents. Recently in the U.S., the The Food and Drug Administration (FDA) issued 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, methemoglobinemia, irregular heart beats, seizures, coma, respiratory depression, death). Children may be at an increased risk for adverse effects, as well as individuals who, without the supervision of trained professionals, 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.
Both the FDA and Health Canada are recommending that when topical anesthetics are needed prior to procedures, consumers ask their healthcare provider for instructions on safe use of these products, use only 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 alternative techniques for pain control.
Additional information can be found at:
U.S.: http://www.fda.gov/Drugs/DrugSafety/PublicHealthAdvisories/ucm110625.htm
Canada: Canada: http://www.hc-sc.gc.ca/dhp-mps/medeff/advisories-avis/prof/_2009/emla_ametop_hpc-cps-eng.php
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
Index Terms
Generic Available
Yes: Cream, infusion, injection, jelly, lotion, ointment, solution
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Local and regional anesthesia by infiltration, nerve block, epidural, or spinal techniques; acute treatment of ventricular arrhythmias from myocardial infarction or cardiac manipulation
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 oral muscous membrane; use in laser/cosmetic surgeries; minor burns, cuts, and abrasions of the skin
Oral solution (viscous): Topical anesthesia of irritated oral mucous membranes and pharyngeal tissue
Patch (Lidoderm®): Relief of allodynia (painful hypersensitivity) and chronic pain in postherpetic neuralgia
Use: Dental
Topical local anesthetic
Patch: Production of mild topical anesthesia of accessible mucous membranes of the mouth prior to superficial dental procedures
Oral solution (viscous): Reduce gagging during dental impressions and x-rays
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; I.V. infusion for chronic pain syndrome
Pregnancy Risk Factor
B
Pregnancy Considerations
Animal studies with lidocaine have not shown teratogenic effects. Lidocaine and the MEGX metabolite cross the placenta. Use is not contraindicated during labor and delivery. Topical lidocaine is used locally to provide analgesia prior to episiotomy and during repair of obstetric lacerations. Administration by the perineal route may result in greater absorption than administration by the epidural route. Adverse events have been reported in the infant following maternal administration, however, when used in appropriate doses, the risk to the fetus is low. Cumulative exposure from all routes of administration should be considered.
Lactation
Enters breast milk/use caution (AAP rates “compatible”)
Breast-Feeding Considerations
Small amounts of lidocaine and the MEGX metabolite are found in breast milk. The actual amount may depend on route and duration of administration. When administered topically at recommended doses, the amount of lidocaine available to the nursing infant would not be expected to cause adverse events. Cumulative exposure from all routes of administration should be considered.
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.
• 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.
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
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, chondrolysis (continuous intra-articular administration), 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
Colchicine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Colchicine. Management: Reduce colchicine (adult) dose as directed when using with a moderate CYP3A4 inhibitor, and increase monitoring for colchicine-related toxicity. Use extra caution in patients with impaired renal and/or hepatic function. Risk D: Consider therapy modification
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 for adults) is recommended in patients with hypertension who are also taking drugs that are moderate inhibitors of CYP3A4. Risk D: Consider therapy modification
Everolimus: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Everolimus. Risk X: Avoid combination
Fesoterodine: CYP2D6 Inhibitors may increase serum concentrations of the active metabolite(s) of Fesoterodine. Risk C: Monitor therapy
Halofantrine: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Halofantrine. Risk D: Consider therapy modification
Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
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 adult dose to a maximum of 500 mg 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
Saxagliptin: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Saxagliptin. 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
Tolvaptan: CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tolvaptan. 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
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.
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; Ophthalmic: 20 seconds to 5 minutes (median: 40 seconds)
Duration: 10-20 minutes; Ophthalmic: 5-30 minutes (median: 15 minutes)
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)
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.
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.
Anesthesia, ocular: Children and Adults: Apply 2 drops to ocular surface in area where procedure will occur; may reapply to maintain effect.
Anesthesia, topical: Unless otherwise noted, the following traditional pediatric guideline for topical lidocaine dosage may be observed: Apply to affected area as needed; maximum dose: 3 mg/kg/dose; do not repeat within 2 hours (Benitz, 1988)
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 (topical): Cold sores and fever blisters: Children ?5 years and Adults: Apply to affected area every 6 hours as needed
Oral solution (viscous):
Infants and Children <3 years: 1.25 mL applied to area with a cotton-tipped applicator every 3-8 hours (maximum: 4 doses per 12-hour period)
Children ?3 years: Should not exceed 4.5 mg/kg/dose (not to exceed 300 mg/dose); swished in the mouth and spit out every 3-8 hours; patient should not swallow viscous solution
Adults: 15 mL swished in the mouth and spit out every 3-8 hours (maximum: 8 doses per 24-hour period); patient should not swallow viscous solution
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.
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.
Oral solution: Have patient swish medication around mouth and then spit it out; patient should not swallow medication.
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.
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. Remove patch while having MRI scan; can cause burns.
Ophthalmic: May cause burning when applied.
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: In out-of-hospital cardiac arrest victims, lidocaine is not as effective as amiodarone for improving intermediate outcomes, but neither has improved survival to hospital discharge among patients with shock-resistant VF cardiac arrest (Dorian, 2002).
Monitoring: Toxic effects of lidocaine may appear earlier in the elderly and in patients with heart failure, shock, or hepatic disease. 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. Lidocaine toxicity may elicit seizures, 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.
Administration issue: 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 joint instead of the tissue around the shoulder, destruction of articular artilage (chondrolysis) has occurred. On-Q® pumps should never be placed directly into any joint (see https://www.ismp.org/Newsletters/acutecare/archives/May09.asp).
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: 5% (15 g)
L-M-X™ 5: 5% (15 g) [contains benzyl alcohol; packaged with applicator]; (30 g) [contains benzyl alcohol]
Cream, topical: 4% (5 g, 15, g, 30 g)
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, ophthalmic, as hydrochloride [preservative free]:
Akten™: 3.5% (5 mL)
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, 60 mL, 120 mL)
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] (10 mL, 20 mL, 50 mL)
Injection, solution, as hydrochloride [for dental use]:
Xylocaine® Dental: 2% (1.8 mL)
Injection, solution, as hydrochloride [premixed in D7.5W, preservative free]: 5% [50 mg/mL] (2 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)
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: 3% (177 mL)
LidaMantle®: 3% (177 mL)
Ointment, topical: 5% (30 g, 37 g, 50 g)
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, topical [spray]:
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]
Solution, viscous, oral, as hydrochloride: 2% [20 mg/mL] (20 mL, 100 mL)
Xylocaine® Viscous: 2% [20 mg/mL] (100 mL, 450 mL)
Transdermal system, topical:
Lidoderm®: 5% (30s)
Pricing: U.S. (www.drugstore.com)
Cream (LidaMantle)
3% (85): $159.45
Cream (LMX 5)
5% (30): $59.99
Gel (Lidocaine HCl)
2% (10): $17.99
2% (30): $17.99
Kit (LMX 4 Plus)
4% (1): $55.99
Lotion (LidaMantle)
3% (177): $223.89
Ointment (Lidocaine)
5% (35.44): $18.99
Patch (Lidoderm)
5% (30): $206.48
Solution (Lidocaine HCl)
4% (50): $16.99
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.
American Pain Society, Principles of Analgesic Use in the Treatment of Acute Pain and Cancer Pain, 6th ed, Glenview, IL: American Pain Society, 2008.
Benitz WE and Tatro DS, The Pediatric Drug Handbook, 2nd ed, Chicago, IL: Year Book Medical Publishers Inc, 1988.
Cavalli RdeC, Lanchote VL, Duarte G, et al, “Pharmacokinetics and Transplacental Transfer of Lidocaine and Its Metabolite for Perineal Analgesic Assistance to Pregnant Women,” Eur J Clin Pharmacol, 2004, 60(8):569-74.
Chow T, Galvin J, and McGovern B, “Antiarrhythmic Drug Therapy in Pregnancy and Lactation,” Am J Cardiol, 1998, 82(4A):58I-62I.
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.
Dryden RM and Lo MW, “Breast Milk Lidocaine Levels in Tumescent Liposuction,” Plast Reconstr Surg, 2000, 105(6):2267-8.
Foxall G, McCahon R, Lamb J, et al, “Levobupivacaine-Induced Seizures and Cardiovascular Collapse Treated With Intralipid,” Anaesthesia, 2007, 62(5):516-8.
Goetzl LM and ACOG Committee on Practice Bulletins-Obstetrics, “ACOG Practice Bulletin. Clinical Management Guidelines for Obstetrician-Gynecologists Number 36, July 2002. Obstetric Analgesial and Anesthesia,” Obstet Gynecol, 2002, 100(1):177-91.
Giuliani M, Grossi GB, Pileri M, et al, “Could Local Anesthesia While Breast-Feeding Be Harmful to Infants?” J Pediatr Gastroenterol Nutr, 2001, 32(2):142-4.
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.
Marchettini P, Lacerenza M, Marangoni C, et al, “Lidocaine Test in Neuralgia,” Pain, 1992, 48(3):377-82.
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.
Schnider TW, Gaeta R, Brose W, et al,“Derivation and Cross-Validation of Pharmacokinetic Parameters for Computer-Controlled Infusion of Lidocaine in Pain Therapy,” Anesthesiology, 1996, 84(5):1043-50.
International Brand Names
Lexi-Comp.com
Last full review/revision November 2009
Content last modified November 2009
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