Xylocaine

Action

Suppresses automaticity of ventricular cells, decreasing diastolic depolarization and increasing ventricular fibrillation threshold. Produces local anesthesia by reducing sodium permeability of sensory nerves, which blocks impulse generation and conduction.

Availability

Injection for I.M. use: 300 mg/3 ml (automatic injection device)

Injection for direct I.V. use: 1% and 2% in syringes and vials

Injection for I.V. infusion: 2 mg/ml, 4 mg/ml, 8 mg/ml

Injection for I.V injection admixtures: 40 mg/ml, 100 mg/ml, 200 mg/ml

Patch: 5%

Topical cream: 0.5%, 4%

Topical gel: 0.5%, 2.5%

Topical jelly: 2%

Topical liquid, ointment: 2.5%, 5%

Topical solution: 4%

Topical solution (viscous): 2%

Topical spray: 0.5%

Indications and dosages

➣ Ventricular arrhythmias

Adults: Initially, 50 to 100 mg I.V. bolus given at rate of 25 to 50 mg/minute. If desired response doesn't occur after 5 minutes, give repeat dose at 25 to 50 mg/minute; maximum dosage is 300 mg given over 1 hour. Maintenance dosage is 1 to 4 mg/minute by continuous I.V. infusion for no more than 24 hours.

Children: Initially, 1 mg/kg I.V. bolus, then repeated based on patient response; don't exceed 5 mg/kg. Maintenance dosage is 30 mcg/kg/minute by continuous I.V. infusion.

➣ Caudal anesthesia (without epinephrine)

Adults: For obstetric analgesia, 200 to 300 mg caudally as 1% solution. For surgical anesthesia, 225 to 300 mg as 1.5% solution. For continuous caudal anesthesia, don't repeat maximum dosage at intervals of less than 90 minutes.

➣ Epidural anesthesia (without epinephrine)

Adults: For lumbar analgesia, 250 to 300 mg epidurally as 1% solution, 225 to 300 mg as 1.5% solution, or 200 to 300 mg as 2% solution. For thoracic anesthesia, 200 to 300 mg as 1% solution. For continuous epidural anesthesia, don't repeat maximum dosage at intervals of less than 90 minutes.

➣ I.V. regional infiltration (without epinephrine)

Adults: 50 to 300 mg I.V. as 0.5% solution. For I.V. regional anesthesia, maximum dosage is 4 mg/kg.

➣ I.V. local infiltration (without epinephrine)

Children: Up to 4.5 mg/kg I.V. as 0.25% to 1% solution

➣ Spinal anesthesia (without epinephrine)

Adults: For obstetric low-spinal or saddle-block anesthesia (normal vaginal delivery), 50 mg of 5% Xylocaine-MPF with glucose 7.5%, or 9 to 15 mg of 1.5% Xylocaine-MPF with dextrose 7.5%. For cesarean section, 75 mg of 5% Xylocaine-MPF with glucose 7.5%. For surgical anesthesia, 75 to 100 mg of 5% Xylocaine-MPF with glucose 7.5%.

➣ Paracervical anesthesia (without epinephrine)

Adults: For obstetric analgesia, 100 mg paracervically as 1% solution (each side). For paracervical block, maximum dosage is 200 mg over each 90-minute period (half administered on each side).

➣ Peripheral nerve block

Adults: For brachial nerve block, 225 to 300 mg as 1.5% solution. For dental nerve block, 20 to 100 mg as 2% solution with epinephrine 1:100,000 or 1:50,000. For intercostal nerve block, 30 mg as 1% solution. For pudendal nerve block, 100 mg as 1% solution. For paravertebral nerve block, 30 mg to 50 mg as 1% solution.

➣ Sympathetic nerve block (without epinephrine)

Adults: For cervical nerve block, 50 mg as 1% solution. For lumbar nerve block, 50 to 100 mg as 1% solution.

➣ Dental anesthesia

Adults: 1 to 5 ml of lidocaine 2% with epinephrine 1:50,000 or 1:100,000. Maximum dosage is less than 500 mg (7 mg/kg).

Children: 20 to 30 mg as 2% solution with epinephrine 1:100,000

➣ Topical anesthesia for skin or mucous membranes

Adults: Apply thin layer of gel, jelly, or ointment to skin or mucous membranes as needed before procedure; or apply 5% patch to most painful areas and intact skin (up to three patches at a time for up to 12 hours within a 24-hour period). For new denture fittings, use 5-g ointment (250 mg) per single dose or 20 g/day. For oropharyngeal use, apply to desired area or to instrument before insertion.

Children: Apply thin layer of ointment to skin or mucous membranes p.r.n. before procedure. Maximum dosage is 2.5 g ointment per 6 hours or 4.5 mg/kg.

➣ Prevention or treatment of pain during procedures involving male or female urethra

Adults: For female urethral examination, apply 3 to 5 ml of 2% jelly topically several minutes before exam. For male sounding or cystoscopy, apply 5 to 10 ml of 2% jelly topically before procedure, or apply 30 ml to fill or dilate urethra in divided doses using penile clamp for several minutes between doses. For male catheterization, apply 5 to 10 ml of 2% jelly to anterior urethra before procedure. Don't use more than 600 mg/12 hours.

➣ Oral cavity disorders; pharyngeal disorders

Adults: For oral cavity disorders, 300 mg (15 ml) of viscous oral topical solution swished and then expelled, or applied with cotton swab q 3 hours p.r.n. For pharyngeal disorders, use same dosage, but solution may be swallowed.

Children older than age 3: Dosage individualized based on age, weight, and physical condition. Maximum dosage is 4.5 mg/kg q 3 hours.

Children up to age 3: 1.25 ml applied with swab q 3 hours

➣ Local anesthesia (oral or nasal mucosa)

Adults: 0.6 to 3 mg/kg or 40 to 200 mg of 4% topical solution, not to exceed 4.5 mg/kg or 300 mg (7.5 ml)

Children: Dosage individualized

Off-label uses

• Pediatric patients with cardiac arrest who develop frequent premature ventricular contractions

• Status epilepticus

Contraindications

• Hypersensitivity to drug, its components, or other amide local anesthetics

• Heart failure, cardiogenic shock, second- or third-degree heart block, intraventricular block in absence of a pacemaker

• Wolff-Parkinson-White or Adams-Stokes syndrome

• Severe hemorrhage, shock, or heart block (lidocaine with dextrose)

• Local infection at puncture site (lidocaine with dextrose)

• Septicemia (lidocaine with dextrose)

Precautions

Use cautiously in:

• renal or hepatic disorders, inflammation or sepsis in injection area

• labor or delivery

• breastfeeding patients.

Administration

☞ Know that I.V. lidocaine is a high-alert drug.

☞ Make sure resuscitation equipment and oxygen are available before giving I.V. lidocaine.

• Dilute injection in additive syringe and single-use vial according to manufacturer's instructions before administering as I.V. infusion.

• Add 1 g lidocaine to 1 L dextrose 5% in water to yield a solution of 1 mg/ml.

• For I.V. bolus injection, give doses of 25 to 50 mg over at least 1 minute. Deliver continuous infusion by infusion pump no faster than 4 mg/minute.

☞ Know that too-rapid infusion may cause seizures.

• Be aware that drug can be given I.M. using 10% parenteral solution only.

Adverse reactions

CNS: anxiety; confusion; difficulty speaking; dizziness; hallucinations; lethargy; paresthesia; light-headedness; fatigue; drowsiness; headache; persistent sensory, motor, or autonomic deficit of lower spinal segment; septic meningitis; seizures

CV: bradycardia, hypotension, new or worsening arrhythmias, cardiac arrest

EENT: diplopia, abnormal vision

GI: nausea, vomiting, dry mouth

GU: urinary retention

Metabolic: methemoglobinemia

Respiratory: suppressed cough reflex, respiratory depression, respiratory arrest

Skin: rash; urticaria; pruritus; erythema; contact dermatitis; cutaneous lesions; tissue irritation, sloughing, and necrosis

Other: fever; edema; infection, burning, stinging, tenderness, and swelling at injection site; anaphylaxis

Interactions

Drug-drug. Beta-adrenergic blockers, cimetidine: increased lidocaine blood level

MAO inhibitors, tricyclic antidepressants: prolonged hypertension

Mexiletine, tocainide: additive cardiac effects

Phenytoin, procainamide: increased cardiac depression

Drug-diagnostic tests. Creatine kinase: increased level (with I.M. use)

Patient monitoring

☞ Monitor vital signs and ECG continuously. Watch for cardiac depression.

☞ Evaluate level of consciousness closely.

☞ Watch for adverse reactions, particularly anaphylaxis.

☞ Stay alert for seizures.

☞ Monitor neurologic status for lower spinal segment deficits.

• Give supportive oxygen therapy, as indicated and prescribed.

• Monitor electrolyte, blood urea nitrogen, and creatinine levels.

• Assess topical site for adverse reactions.

Patient teaching

• Discuss reason for drug therapy with patient and family, when appropriate.

• Explain that patient will be monitored continuously during therapy.

☞ Instruct patient to promptly report discomfort at I.V. site as well as adverse effects, especially cardiovascular, respiratory, or neurologic problems or allergic reactions.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.