LIDOCAINE HYDROCHLORIDE

LIDOCAINe HYDROCHLORIDE
(lye'doe-kane)
Anestacon, Dilocaine, L-Caine, Lidoderm, Lida-Mantle, Lidoject-1, LidoPen Auto Injector, Nervocaine, Octocaine, Xylocaine, Xylocard 
Classifications: antiarrhythmic, class ib; local anesthetic (amide type);
Therapeutic: antiarrhythmic, class ib
; local anesthetic (amide type); anticonvulsant
Pregnancy Category: B

Availability

Antidysrhythmic: 300 mg/3 mL auto-injector; 0.2%, 0.4%, 0.8%, 1%, 2%, 4%, 10%, 20% injections

Local Anesthetic: 0.5%, 1%, 1.5%, 2%, 4% injection

Topical: 2%, 2.5%, 4%, 5% solution; 2.5%, 5% ointment; 0.5%, 4% cream; 0.5%, 2.5% gel; 0.5%, 10% spray; 2% jelly; 0.5% patch

Action

Exerts antiarrhythmic action (Class IB) by suppressing automaticity in His-Purkinje system. Combines with fast sodium channels in myocardial cell membranes, thus inhibiting sodium influx into myocardial cells. Thus it decreases ventricular depolarization, automaticity, and excitability during diastole. Action as local anesthetic is more prompt, more intense, and longer lasting than that of procaine.

Therapeutic Effect

Suppresses automaticity in His-Purkinje system and elevates electrical stimulation threshold of ventricle during diastole. Prompt, intense, and long-lasting local anesthetic. It decreases pain through a reversible nerve conduction blockade.

Uses

Rapid control of ventricular arrhythmias occurring during acute MI, cardiac surgery, and cardiac catheterization and those caused by digitalis intoxication. Also as surface and infiltration anesthesia and for nerve block, including caudal and spinal block anesthesia and to relieve local discomfort of skin and mucous membranes. Patch for relief of pain associated with post-herpetic neuralgia.

Unlabeled Uses

Refractory status epilepticus.

Contraindications

History of hypersensitivity to amide-type local anesthetics; application or injection of lidocaine anesthetic in presence of severe trauma or sepsis, blood dyscrasias, supraventricular arrhythmias, Stokes-Adams syndrome, untreated sinus bradycardia, severe degrees of sinoatrial, atrioventricular, and intraventaricular heart block.

Cautious Use

Liver or kidney disease, CHF, marked hypoxia, respiratory depression, hypovolemia, shock; myasthenia gravis; debilitated patients, older adults; family history of malignant hyperthermia (fulminant hypermetabolism); pregnancy (category B). Topical use in eyes, over large body areas, over prolonged periods, in severe or extensive trauma or skin disorders.

Route & Dosage

Ventricular Arrhythmias
Adult: IV 50–100 mg bolus at a rate of 20–50 mg/min, may repeat in 5 min, then start infusion of 1–4 mg/min immediately after first bolus, not more than 300 mg/h IM/SC 200–300 mg IM, may repeat once after 60–90 min
Child: IV 1 mg/kg bolus dose, then 20–50 mcg/kg/min infusion

Anesthetic Uses
Adult: Infiltration 0.5–1% solution Nerve Block 1–2% solution Epidural 1–2% solution Caudal 1–1.5% solution Spinal 5% with glucose Saddle Block 1.5% with dextrose Topical 2.5–5% jelly, ointment, cream, or solution

Post-Herpetic Neuralgia
Adult: Topical Apply up to 3 patches over intact skin in most painful areas once for up to 12 h per 24 h period

Administration

Intramuscular
  • Give in deltoid muscle as preferred site.
Topical
  • Do not apply topical lidocaine to large areas of skin or to broken or abraded surfaces. Consult physician about covering area with a dressing.
  • Avoid topical preparation contact with eyes.
Intravenous
  • Note: Do not use lidocaine solutions containing preservatives for spinal or epidural (including caudal) block. Use ONLY lidocaine HCl injection without preservatives or epinephrine that is specifically labeled for IV injection or infusion.

PREPARE: Direct: Give undiluted.  IV Infusion: ??Use D5W for infusion. For adults, add 1 g to 250 or 500 mL to yield 2 or 4 mg/mL, respectively; for children, add 120 mg to 100 m to yield 1.2 mg/mL.??Do not use solutions with particulate matter or discoloration. 

ADMINISTER: Direct: Give at a rate of 50 mg or fraction thereof over 1 min.  IV Infusion: Use microdrip and infusion pump. Rate of flow is usually ≤4 mg/min.  

INCOMPATIBILITIES Solution/additive: Ampicillin, cefazolin, methohexital, phenytoin. Y-site: Amphotericin B cholesteryl complex, phenytoin, thiopental.

  • Discard partially used solutions of lidocaine without preservatives.

Adverse Effects (≥1%)

CNS: Drowsiness, dizziness, light-headedness, restlessness, confusion, disorientation, irritability, apprehension, euphoria, wild excitement, numbness of lips or tongue and other paresthesias including sensations of heat and cold, chest heaviness, difficulty in speaking, difficulty in breathing or swallowing, muscular twitching, tremors, psychosis. With high doses: convulsions, respiratory depression and arrest. CV: With high doses, hypotension, bradycardia, conduction disorders including heart block, cardiovascular collapse, cardiac arrest. Special Senses: Tinnitus, decreased hearing; blurred or double vision, impaired color perception. Skin: Site of topical application may develop erythema, edema. GI: Anorexia, nausea, vomiting. Body as a Whole: Excessive perspiration, soreness at IM site, local thrombophlebitis (with prolonged IV infusion), hypersensitivity reactions (urticaria, rash, edema, anaphylactoid reactions).

Diagnostic Test Interference

Increases in creatine phosphokinase (CPK) level may occur for 48 h after IM dose and may interfere with test for presence of MI.

Interactions

Drug: Lidocaine patch may increase toxic effects of tocainide, mexiletine; barbiturates decrease lidocaine activity; cimetidine, beta blockers, quinidine increase pharmacologic effects of lidocaine; phenytoin increases cardiac depressant effects; procainamide compounds neurologic and cardiac effects.

Pharmacokinetics

Absorption: Topical application is 3% absorbed through intact skin. Onset: 45–90 sec IV; 5–15 min IM; 2–5 min topical. Duration: 10–20 min IV; 60–90 min IM; 30–60 min topical; >100 min injected for anesthesia. Distribution: Crosses blood–brain barrier and placenta; distributed into breast milk. Metabolism: In liver via CYP3A4 and 2D6. Elimination: In urine. Half-Life: 1.5–2 h.

Nursing Implications

Assessment & Drug Effects

  • Stop infusion immediately if ECG indicates excessive cardiac depression (e.g., prolongation of PR interval or QRS complex and the appearance or aggravation of arrhythmias).
  • Monitor BP and ECG constantly; assess respiratory and neurologic status frequently to avoid potential overdosage and toxicity.
  • Auscultate lungs for basilar rales, especially in patients who tend to metabolize the drug slowly (e.g., CHF, cardiogenic shock, hepatic dysfunction).
  • Watch for neurotoxic effects (e.g., drowsiness, dizziness, confusion, paresthesias, visual disturbances, excitement, behavioral changes) in patients receiving IV infusions or with high lidocaine blood levels.
  • Note: Lidocaine blood levels of 1.5–6 mcg/mL are reported to provide "usually effective" antiarrhythmic activity. Blood levels greater than 7 mcg/mL are potentially toxic.

Patient & Family Education

  • Swish and spit out when using lidocaine solution for relief of mouth discomfort; gargle for use in pharynx, may be swallowed (as prescribed).
  • Oral topical anesthetics (e.g., Xylocaine Viscous) may interfere with swallowing reflex. Do NOT ingest food within 60 min after drug application; especially pediatric, geriatric, or debilitated patients. Do not chew gum while buccal and throat membranes are anesthetized to prevent biting trauma.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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