Pronunciation:

(LYE doe kane)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

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

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

Use - Dental:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

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

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.

Topical: L-M-X™ 4 cream: Do not leave on large body areas for >2 hours. Observe young children closely to prevent accidental ingestion. Not for use ophthalmic use or for use on mucous membranes.

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

Adverse Reactions:

Frequency not defined:

Cardiovascular: Bradycardia, hypotension, heart block, arrhythmia, cardiovascular collapse, sinus node supression, increase defibrillator threshold, vascular insufficiency (periarticular injections), arterial spasms

Central nervous system: Drowsiness after administration is usually a sign of a high blood level. Other effects may include lightheadedness, dizziness, tinnitus, blurred vision, vomiting, twitching, tremor, lethargy, coma, agitation, slurred speech, seizure, anxiety, euphoria, hallucinations, paresthesia, psychosis.

Dermatologic: Itching, rash, edema of the skin, contact dermatitis

Gastrointestinal: Nausea, vomiting, taste disorder

Local: Thrombophlebitis

Neuromuscular & skeletal: Transient radicular pain (subarachnoid administration; up to 1.9%)

Ocular: Blurred vision, diplopia

Respiratory: Dyspnea, respiratory depression or arrest, bronchospasm

Miscellaneous: Allergic reactions, urticaria, edema, anaphylactoid reaction

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), severe back pain, methemoglobinemia, asystole

Overdosage/Toxicology:

Drug Interactions:

Cimetidine increases lidocaine blood levels; monitor levels or use an alternative H2 antagonist.

CYP1A2 substrates: Lidocaine may increase the levels/effects of CYP1A2 substrates. Example substrates include aminophylline, fluvoxamine, mexiletine, mirtazapine, ropinirole, theophylline, and trifluoperazine.

CYP2D6 inhibitors: May increase the levels/effects of lidocaine. Example inhibitors include chlorpromazine, delavirdine, fluoxetine, miconazole, paroxetine, pergolide, quinidine, quinine, ritonavir, and ropinirole.

CYP2D6 substrates: Lidocaine may increase the levels/effects of CYP2D6 substrates. Example substrates include amphetamines, selected beta-blockers, dextromethorphan, fluoxetine, mirtazapine, nefazodone, paroxetine, risperidone, ritonavir, thioridazine, tricyclic antidepressants, and venlafaxine.

CYP2D6 prodrug substrates: Lidocaine may decrease the levels/effects of CYP2D6 prodrug substrates. Example prodrug substrates include codeine, hydrocodone, oxycodone, and tramadol.

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of lidocaine. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

CYP3A4 inhibitors: May increase the levels/effects of lidocaine. Example inhibitors include amiodarone (doses >400 mg/day), azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

CYP3A4 substrates: Lidocaine may increase the levels/effects of CYP3A4 substrates. Example substrates include benzodiazepines, calcium channel blockers, cyclosporine, mirtazapine, nateglinide, nefazodone, sildenafil (and other PDE-5 inhibitors), tacrolimus, and venlafaxine. Selected benzodiazepines (midazolam and triazolam), cisapride, ergot alkaloids, selected HMG-CoA reductase inhibitors (lovastatin and simvastatin), and pimozide are generally contraindicated with strong CYP3A4 inhibitors.

Propranolol: Increases lidocaine blood levels.

Protease inhibitors (eg, amprenavir, ritonavir): May increase lidocaine blood levels.

Ethanol/Nutrition/Herb Interactions:

Stability:

Standard diluent: 2 g/250 mL D5W

Compatibility:

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:

Pharmacodynamics/Kinetics:

Onset of action: Single bolus dose: 45-90 seconds

Duration: 10-20 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

Dosage:

Antiarrhythmic:

Children:

I.V., I.O.: (Note: For use in pulseless VT or VF, give after defibrillation and epinephrine): Loading dose: 1 mg/kg; 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. (loading dose only): 2-10 times the I.V. bolus dose; dilute with NS to a volume of 3-5 mL and follow with several positive-pressure ventilations

Adults:

Ventricular fibrillation or pulseless ventricular tachycardia (after defibrillation and epinephrine): 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 over 3-5 minutes after initial dose. Total dose should not exceed 200-300 mg during a 1-hour period or 3 mg/kg total dose. 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.

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

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.

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%.

Administration:

Intratracheal: 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.

I.V.: Use microdrip (60 gtt/mL) or infusion pump to administer an accurate dose

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

Topical:

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

Patch: May be cut to appropriate size; remove immediately if burning sensation occurs; wash hands after application

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:

Patient Education:

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.

Oral: 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.

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.

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).

Cardiovascular Considerations:

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

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

Cream, topical (L-M-X™ 4): 4% (5 g, 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 benzyl alcohol, aloe vera, and jojoba]

Gel, topical, as hydrochloride: 2% (30 g)

Burn Jel: 2% (3.5 g, 120 g)

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

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] (5 mL, 20 mL, 30 mL, 50 mL); 1.5% [15 mg/mL] (20 mL); 2% [20 mg/mL] (2 mL, 5 mL, 10 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] (5 mL, 10 mL); 4% [40 mg/mL] (5 mL); 10% [100 mg/mL] (10 mL); 20% [200 mg/mL] (10 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)

Jelly, topical, as hydrochloride:

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 (LidMantle®): 3% (177 mL)

Ointment, topical: 5% (37 g)

Patch, transdermal (Lidoderm®): 5% (30s)

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

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

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]

International Brand Names: