Lidocaine Hydrochloride

Pronunciation: (LYE-doe-kane HYE-droe-KLOR-ide)
Class: Antiarrhythmic agent, Local anesthetic

Trade Names

Akten
- Gel, ophthalmic 3.5%

Anestafoam
- Foam; topical 4%

Lida Mantle
- Cream; topical 3%
- Lotion; topical 3%

Lidocaine
- Ointment; topical 5%

Lidocaine Viscous
- Solution; oral 2%

Lidocream
- Cream; topical 4%

Lidoderm
- Patch, topical 5%

LMX
- Cream; topical 4%
- Cream; rectal 5%

Regenecare HA
- Gel; topical 2%
- Pads; topical 2%

Topicaine
- Gel 4%
- Gel 5%

Xylocaine
- Jelly; topical 2%
- Injection 0.5%
- Injection 1%
- Injection 1.5%
- Injection 2%
- Solution; topical 4%

Xylocaine Hydrochloride IV for Cardiac Arrhythmias
- Injection for direct IV administration 2%

Xylocaine-MPF
- Injection 0.5%
- Injection 1%
- Injection 1.5%
- Injection 2%
- Injection 4%

Lidodan Endotracheal (Canada)
Lidodan Ointment (Canada)
Lidodan Viscous (Canada)
Xylocaine Ointment 5% (Canada)
Xylocaine Parenteral without Epinephrine (Canada)
Xylocaine Topical 4% (Canada)
Xylocard (Canada)

Pharmacology

Attenuates phase 4 diastolic depolarization, decreases automaticity, decreases action potential duration, and raises ventricular fibrillation threshold; inhibits conduction of nerve impulses from sensory nerves.

Indications and Usage

Acute management of ventricular arrhythmias; topical anesthesia in local skin disorders; local anesthesia of accessible mucous membranes; topical anesthesia prior to venipuncture or peripheral IV cannulation; ocular surface anesthesia during ophthalmic procedures.

Unlabeled Uses

Intraosseous or endotracheal administration to children with cardiac arrest.

Contraindications

Hypersensitivity to amide local anesthetics; Stokes-Adams syndrome; Wolff-Parkinson-White syndrome; severe degrees of sinoatrial, AV, or intraventricular block in absence of pacemaker.

Dosage and Administration

Adults IM

300 mg. May be repeated after 60 to 90 min.

IV bolus

50 to 100 mg at rate of 25 to 50 mg/min; may repeat, but do not exceed 200 to 300 mg/h.

Continuous infusion

1 to 4 mg/min.

Intradermal

Apply 0.5 mg via intradermal injection system 1 to 3 min prior to procedure. May repeat 1 additional injection at a new location after failed attempt at venous access.

Ophthalmic

2 drops applied to ocular surface in the area of the planned procedure. May reapply to maintain anesthetic effect.

Topical

Apply as needed to affected area; use lowest dose possible when applying to mucous membranes.

Foam

Apply no more than 3 to 4 times daily.

Transdermal patch

Apply up to 3 patches, only once for up to 12 h within a 24-h period. Smaller treatment areas are recommended for patients who are debilitated and who have hepatic impairment.

Children IV bolus/intratracheal

1 mg/kg/dose every 5 to 10 min (max, 5 mg/kg). Maintenance dose is 20 to 50 mcg/kg/min.

Topical

Apply as needed to affected area; use lowest dose possible when applying to mucous membranes.

Foam

Apply no more than 3 to 4 times daily.

Ophthalmic

2 drops applied to ocular surface in the area of the planned procedure. May reapply to maintain anesthetic effect.

General Advice

• IM
• Use IM route for emergency situations (eg, no IV access, no ECG monitoring) only. Only use 10% solution for injection. Deltoid muscle is preferred IM site. Switch to IV route as soon as possible.

• IV
• When giving by IV route, use only 1% to 2% solutions of drug. Use only lidocaine specifically labeled for IV use (without preservatives or epinephrine). Do not administer with other agents.
• For continuous infusion, use prediluted solution or add lidocaine 1 g to 500 mL of dextrose 5% in water to prepare 0.2% solution. Rate of administration should not exceed 1 to 4 mg/min. Adjust rate according to cardiac response.
• Use diluted solutions within 24 h.

• Intradermal
• Use only on intact skin.
• Follow instructions for use for proper application of injection system.
• Do not use around the eyes, on body orifices, or on mucous membranes.

• Foam
• Spray foam into palm of hand, then apply to affected area.

• Transdermal patch
• Apply to intact skin.
• Patches may be cut into smaller sizes with scissors prior to removal of the release liner.
• Clothing may be worn over the area of application.
• Wash hands after handling the patch and avoid contact with eyes.
• The used patch should be disposed of immediately upon removal in such a way as to prevent access by children or pets.

Storage/Stability

Store at room temperature.

Drug Interactions

Beta-adrenergic blockers

Increased lidocaine levels.

Cimetidine

Decreased lidocaine Cl.

Class I antiarrhythmic agents (eg, mexiletine, tocainide)

Toxic effects are additive and potentially synergistic.

CYP450

CYP3A4 to 3A7 and CYP2D6 inhibitors may elevate systemic lidocaine levels.

Procainamide

Additive neurological and cardiac effects.

Succinylcholine

Prolongation of neuromuscular blockade.

Incompatibility

Amphotericin B, cephalosporins (parenteral), doxycycline, epinephrine, isoproterenol, methohexital, nitroprusside, norepinephrine, phenytoin, sodium bicarbonate, sulfadiazine.

Laboratory Test Interactions

IM administration may increase CPK levels.

Adverse Reactions

Cardiovascular

Bradycardia, cardiac arrest, CV collapse, hypotension.

CNS

Apprehension; confusion; convulsions; dizziness; drowsiness; euphoria; hallucinations; headache; light-headedness; mood changes; nervousness; sensations of heat, cold, or numbness; tremors; twitching; unconsciousness.

EENT

Blurred or double vision, conjunctival hyperemia, corneal epithelial changes, diplopia, tinnitus, visual disturbances.

GI

Nausea, vomiting.

Local

Erythema (53%); petechiae (44%); edema (8%); injection-site reactions, including bruising, burning, contusion, hemorrhage, pain (4% [intradermal]); burning, sloughing, stinging, tenderness; extravasation; local reactions, including soreness at IM injection site; venous thrombosis or phlebitis (with topical application).

Respiratory

Respiratory depression or arrest.

Miscellaneous

Hypersensitivity reactions. Burning upon installation (ophthalmic). Difficulty in speaking, breathing, and swallowing; numbness of lips or tongue; other paresthesias, including heat and cold.

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

If used, reduce dose. IM autoinjector device not recommended in children weighing less than 50 kg.

Transdermal

Safety and efficacy not established.

Intradermal

Safety and efficacy not established in children younger than 3 yr of age.

Elderly

Safety and efficacy not established (intradermal). Give reduced doses commensurate with their age and physical status.

Hypersensitivity

May occur.

Renal Function

Use caution with repeated doses or prolonged use.

Hepatic Function

Use caution with repeated doses or prolonged use.

Bleeding tendencies

May have higher risk of dermal bleeding (intradermal).

Cardiac effects

Use with caution and in lower doses in patients with CHF, reduced cardiac output, or digitalis toxicity, and in elderly patients.

IV use

May result in excessive depression of cardiac conductivity.

Malignant hyperthermia

Has been reported with administration of amide local anesthetics.

Methemoglobinemia

Do not use in patients with congenital or idiopathic methemoglobinemia or in infants younger than 12 mo of age who are receiving methemoglobin-inducing drugs.

Ophthalmic use

Prolonged use may produce permanent corneal opacification and ulceration with accompanying visual loss.

Pseudocholinesterase deficiency

Greater risk of developing toxic lidocaine plasma levels.

Topical use

Systemic effects can occur following topical use; use lowest possible dose to avoid serious toxicity, shock, or heart block.

Overdosage

Symptoms

Bradycardia, cardiac arrest, confusion, convulsions, CV collapse, diplopia, drowsiness, hypotension, tinnitus, tremors, unconsciousness.

Patient Information

• Explain to patient that adverse reactions related to the CNS (eg, confusion, convulsions, drowsiness, paresthesias, respiratory arrest) can occur and are a result of CNS toxicity.
• Emphasize importance of not allowing topical solution to come in contact with eyes or broken skin.
• Advise patient not to chew gum or eat food until 60 min after oral anesthetic has been administered.
• Advise patient that drug may cause dizziness or drowsiness and to avoid getting out of bed or walking without assistance.
• For patients receiving ophthalmic gel, advise them to avoid rubbing or touching the eye until the anesthesia has worn off because inadvertent damage may be done to the anesthetized cornea and conjunctiva.
• Advise patients that skin reactions, including edema, erythema, and petechiae, may occur with the intradermal injection system.

Copyright © 2009 Wolters Kluwer Health.