Yes

Analgesic, Topical; Antiarrhythmic Agent, Class I-B; Local Anesthetic

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

Medical: Local anesthetic and acute treatment of ventricular arrhythmias from myocardial infarction, cardiac manipulation, digitalis intoxication; topical local anesthetic: relief od pain associated with postherpetic neuralgia; drug of choice for ventricular ectopy, ventricular tachycardia, ventricular fibrillation; for pulseless VT or VF preferably administer after defibrillation and epinephrine; control of premature ventricular contractions, wide-complex PSVT

B (Per manufacturer); C (per expert analysis)

Hypersensitivity to lidocaine or any component of the product; 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)

Intravenous: Constant EKG 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.

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

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

Neuromuscular & Skeletal: Transient radicular pain (subarachnoid administration; 0-1.9%)

Local:Thrombophlebitis

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, tremors, lethargy, coma, agitation, slurred speech, seizures, anxiety, euphoria, hallucinations, paresthesia, psychosis

Dermatologic: Itching, rash, edema of the skin, contact dermatitis. EMLA ® cream can cause blanching, erythema, altered temperature sensation,and edema of the skin.

Gastrointestinal: Nausea, vomiting, taste disorder

Miscellaneous: Allergic reactions, urticaria, edema, anaphylactoid reaction

Respiratory: Dyspnea, respiratory depression or arrest, bronchospasm

Ocular: Blurred vision, diplopia

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

Case reports: ARDS (inhalation), severe back pain, methemoglobinemia, asystole

Has a narrow therapeutic index and severe toxicity may occur slightly above the therapeutic range, especially with other antiarrhythmic drugs; symptoms of overdose include sedation, confusion, coma, seizures, respiratory arrest and cardiac toxicity (sinus arrest, A-V block, asystole, and hypotension); the QRS and Q-T intervals are usually normal, although they may be prolonged after massive overdose; other effects include dizziness, paresthesias, tremor, ataxia, and GI disturbance.

Treatment is supportive, using conventional therapies (fluids, positioning, vasopressors, antiarrhythmics, anticonvulsants); sodium bicarbonate may reverse QRS prolongation, bradyarrhythmias and hypotension; enhanced elimination with dialysis, hemoperfusion or repeat charcoal is not effective.

CYP3A3/4 enzyme substrate

Drugs which inhibit CYP3A3/4 may increase lidocaine blood levels.

Protease inhibitors like amprenavir and ritonavir may increase lidocaine blood levels.

Propranolol increases lidocaine blood levels.

Lidocaine injection is stable at room temperature

Stability of parenteral admixture at room temperature (25°C): Expiration date on premixed bag; out of overwrap stability: 30 days

Standard diluent: 2 g/250 mL D₅W

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

Onset of action (single bolus dose): 45-90 seconds

Duration: 10-20 minutes

Distribution: V_d: Alterable by many patient factors; decreased in CHF and liver disease

Protein binding: 60% to 80%; binds to alpha₁ acid glycoprotein

Metabolism: 90% metabolized in liver; active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX) can accumulate and may cause CNS toxicity

Half-life (biphasic): Increased with CHF, liver disease, shock, severe renal disease

Initial: 7-30 minutes

Terminal: Infants, premature: 3.2 hours; Adults: 1.5-2 hours

Topical: Apply to affected area as needed; maximum: 3 mg/kg/dose; do not repeat within 2 hours.

Injectable local anesthetic: 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.

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.

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

I.V. (2 g/250 mL D₅W) infusion rates (infusion pump should be used for I.V. infusion administration):

1 mg/minute: 7 mL/hour

2 mg/minute: 15 mL/hour

3 mg/minute: 21 mL/hour

4 mg/minute: 30 mL/hour

Ventricular fibrillation (after defibrillation and epinephrine): Initial: 1.5 mg/kg may repeat boluses as above; follow with continuous infusion after return of perfusion.

Prevention of ventricular fibrillation: I.V.: Initial bolus: 0.5 mg/kg; repeat every 5-10 minutes to a total dose of 2 mg/kg

Refractory ventricular fibrillation: Repeat 1.5 mg/kg bolus may be given 3-5 minutes after initial dose.

Endotracheal: 2-2.5 times the I.V. dose

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

Therapeutic: 1.5-5.0 mg/mL (SI: 6-21 mmol/L)

Potentially toxic: >6 mg/mL (SI: >26 mmol/L)

Toxic: >9 mg/mL (SI: >38 mmol/L)

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 doses 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).

May rarely cause agitation, anxiety, euphoria, or hallucinations

None reported

No information available to require special precautions

No effects or complications reported

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 difficulty breathing.

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.

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 precautions: Inform prescriber if you are pregnant.

Local thrombophlebitis may occur in patients receiving prolonged I.V. infusions Patch may be cut to appropriate size. remove immediately if burning sensation occurs. Wash hands after application.

Cream, as hydrochloride: 2% (56 g)

Injection, as hydrochloride: 0.5% [5 mg/mL] (50 mL); 1% [10 mg/mL] (2 mL, 5 mL, 10 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, 30 mL, 50 mL); 4% [40 mg/mL] (5 mL); 10% [100 mg/mL] (10 mL); 20% [200 mg/mL] (10 mL, 20 mL)

Injection, as hydrochloride:

I.M.: 10% [100 mg/mL] (3 mL, 5 mL)

Direct I.V.: 1% [10 mg/mL] (5 mL, 10 mL); 20 mg/mL (5 mL)

I.V. admixture, preservative free: 4% [40 mg/mL] (25 mL, 30 mL); 10% [100 mg/mL] (10 mL); 20% [200 mg/mL] (5 mL, 10 mL)

I.V. infusion, in D₅W: 0.2% [2 mg/mL] (500 mL); 0.4% [4 mg/mL] (250 mL, 500 mL, 1000 mL); 0.8% [8 mg/mL] (250 mL, 500 mL)

Gel, , as hydrochloride, topical: 2% (30 mL); 2.5% (15 mL)

Liquid, as hydrochloride, topical: 2.5% (7.5 mL)

Liquid, as hydrochloride, viscous: 2% (20 mL, 100 mL)

Ointment, as hydrochloride, topical: 2.5% [OTC], 5% (35 g)

Solution, as hydrochloride, topical: 2% (15 mL, 240 mL); 4% (50 mL)

Transdermal patch: 5%

Amitai Y, Whitesell L, and Lovejoy FH Jr, "Death Following Accidental Lidocaine Overdose in a Child," N Engl J Med, 1986, 314(3):181-2.

Carnel SB, Blakeslee DB, Oswald SG, et al, "Treatment of Radiation- and Chemotherapy-Induced Stomatitis," Otolaryngol Head Neck Surg, 1990, 102(4):326-30.

Emergency Cardiac Care Committee and Subcommittees, American Heart Association, "Guidelines for Cardiopulmonary Resuscitation and Emergency Cardiac Care, III: Adult Advanced Cardiac Life Support" and "VI: Pediatric Advanced Life Support," JAMA, 1992, 268(16):2199-241 and 2262-75.

Gonzalez del Rey J, Wason S, and Druckenbrod RW, "Lidocaine Overdose: Another Preventable Case," Pediatr Emerg Care, 1994, 10(6):344-6.

Noble J, Kennedy DJ, Latimer RD, et al, "Massive Lignocaine Overdose During Cardiopulmonary Bypass. Successful Treatment With Cardiac Pacing," Br J Anaesth, 1984, 56(12):1439-41.