lidocaine

Absorption: IV administration results in complete bioavailability; some absorption follows local use.

Distribution: Widely distributed. Concentrates in adipose tissue. Crosses the blood-brain barrier.

Metabolism/Excretion: Mostly metabolized by the liver; <10% excreted in urine as unchanged drug.

Half-Life: Biphasic—initial phase, 7–30 min; terminal phase, 90–120 min; ↑ in HF and hepatic impairment.

Time/Action Profile ⬆ ⬇

(IV = antiarrhythmic effects; local = anesthetic effects)

ROUTE	ONSET	PEAK	DURATION
IV	immediate	immediate	10–20 min (up to several hr after continuous infusion)
Local	rapid	unknown	1–3 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity; cross-sensitivity may occur;
Third-degree heart block;
Wolff-Parkinson-White syndrome;
Pedi: Children 3 yr ( risk of seizures, cardiac arrest and death with viscous lidocaine); viscous lidocaine should not be used for teething pain; should only be used for other indications when safer alternatives are not available or have failed.

Use Cautiously in:

Glucose–6–phosphate dehydrogenase deficiency, history of methemoglobinemia, cardiac or pulmonary disease, or concurrent exposure to oxidizing agents (or metabolites of these agents) (↑ risk of methemoglobinemia);
Liver disease, HF, patients weighing <50 kg, and geriatric patients (↓ bolus and/or maintenance dose);
Respiratory depression;
Shock;
Heart block;
OB: Use only if the potential benefit justifies the potential risk to the fetus;
Pedi: Infants 6 mo ( risk of methemoglobinemia); safety of topical patch not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: arrhythmias, bradycardia, CARDIAC ARREST, heart block, hypotension

EENT:

mucosal use

↓or absent gag reflex

GI: nausea, vomiting

Hemat: methemoglobinemia

Local: stinging, burning, contact dermatitis, erythema

MS: chondrolysis

Neuro: confusion, drowsiness, agitation, blurred vision, dizziness, paresthesia, SEIZURES, slurred speech, tremor

Resp: bronchospasm

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of acetaminophen, benzocaine, bupivacaine, chloroquine, cyclophosphamide, dapsone, flutamide, hydroxyurea, ifosfamide, metoclopramide, nitrofurantoin, nitroglycerin, nitroprusside, nitrous oxide, phenobarbital, phenytoin, prilocaine, primaquine, procaine, quinine, rasburicase, ropivacaine, sulfonamides, tetracaine, and valproate may ↑ risk of methemoglobinemia; monitor closely.
↑cardiac depression and toxicity with phenytoin, amiodarone, quinidine, procainamide, or propranolol.
Cimetidine, azole antifungals, clarithromycin, erythromycin, fluoxetine, fluvoxamine, nefazodone, paroxetine, protease inhibitors, propofol, ritonavir, verapamil, and propranolol may ↓ metabolism and ↑ risk of toxicity.
Lidocaine may ↑ levels of calcium channel blockers, certain benzodiazepines, cyclosporine, fluoxetine, lovastatin, simvastatin, mirtazapine, paroxetine, ritonavir, tacrolimus, theophylline, tricyclic antidepressants, and venlafaxine.
Effects of lidocaine may be ↓ by carbamazepine, phenobarbital, phenytoin, and rifampin.

Route/Dosage ⬆ ⬇

Ventricular Tachycardia (with a Pulse) or Pulseless Ventricular Tachycardia/Ventricular Fibrillation

IV (Adults ): 1–1.5 mg/kg bolus; may repeat doses of 0.5–0.75 mg/kg every 5–10 min up to a total dose of 3 mg/kg; may then start continuous infusion of 1–4 mg/min.
Endotracheal
(Adults ): Give 2–2.5 times the IV loading dose down the endotracheal tube, followed by a 10 mL saline flush.
IV (Children ): 1 mg/kg bolus (not to exceed 100 mg), followed by 20–50 mcg/kg/min continuous infusion (range 20–50 mcg/kg/min); may administer 2nd bolus of 0.5–1 mg/kg if delay between bolus and continuous infusion.
Endotracheal
(Children ): Give 2–3 mg/kg down the endotracheal tube followed by a 5 mL saline flush.

Local

Infiltration
(Adults and Children ): Infiltrate affected area as needed (increased amount and frequency of use increases likelihood of systemic absorption and adverse reactions).
(Adults ): Cream/ointment/gel/solution/jelly: Apply to affected area 2–3 times daily. Patch: Up to 3 patches may be applied once for up to 12 hr in any 24-hr period; consider smaller areas of application in geriatric or debilitated patients.
Mucosal
(Adults ): For anesthetizing oral surfaces: 20 mg as 2 sprays/quadrant (not to exceed 30 mg/quadrant) may be used. 15 mL of the viscous solution may be used every 3 hr for oral or pharyngeal pain. For anesthetizing the female urethra: 3–5 mL of the jelly or 20 mg as 2% solution may be used. For anesthetizing the male urethra: 5–10 mL of the jelly or 5–15 mL of 2% solution may be used before catheterization or 30 mL of jelly before cystoscopy or similar procedures. Topical solutions may be used to anesthetize mucous membranes of the larynx, trachea, or esophagus.
Mucosal
(Children ≥3 yr): Do not exceed 4.5 mg/kg/dose (or 300 mg/dose) of viscous solution; swish in the mouth and spit out no more frequently than every 3 hr (maximum: 4 doses per 12-hr period).
Mucosal
(Children <3 yr): ≤1.2 mL applied to area with a cotton-tipped applicator no more frequently than every 3 hr (maximum: 4 doses per 12-hr period); use only if the underlying condition requires treatment with product volume of ≤1.2 mL.

Availability ⬆ ⬇

(Generic available)

Solution for injection: 5 mg/mL (0.5%); 10 mg/mL (1%); 15 mg/mL (1.5%); 20 mg/mL (2%)
Premixed infusion: 1000 mg/250 mL D5W (0.4%); 2000 mg/500 mL D5W (0.4%); 2000 mg/250 mL D5W (0.8%)
Injection for local infiltration/nerve block: 0.5%; 1%; 2%; 4%
Topical cream: 4%^OTC; 5%
Topical gel: 2%^OTC; 3%; 4%; 5%^OTC
Topical jelly: 2%
Topical liquid: 2.5%
Topical ointment: 4%; 5%
Topical patch: 1.8%; 3.5%; 4%; 5%
Topical solution: 2%; 4%
Topical spray: 2%; 4%
Viscous solution: 2%
In combination with: diclofenac (Diclona); epinephrine (Xylocaine with Epinephrine); prilocaine (Oraquix).

Assessment ⬆ ⬇

Antiarrhythmic: Monitor ECG continuously and BP and respiratory status frequently during administration.
Anesthetic: Assess degree of numbness of affected part.
Monitor for pain intensity in affected area periodically during therapy.

Lab Test Considerations:

Serum electrolyte levels should be monitored periodically during prolonged therapy.

Toxicity and Overdose:

Monitor serum lidocaine levels periodically during prolonged or high-dose IV therapy. Therapeutic serum lidocaine levels range from 1.5–5 mcg/mL.
- Signs and symptoms of toxicity include confusion, excitation, blurred or double vision, nausea, vomiting, ringing in ears, tremors, twitching, seizures, difficulty breathing, severe dizziness or fainting, and unusually slow heart rate.
- If symptoms of overdose occur, stop infusion and monitor patient closely.

Implementation ⬆ ⬇

Lidocaine is readily absorbed through mucous membranes. Inadvertent overdose of lidocaine jelly and spray has resulted in patient harm or death from neurologic and/or cardiac toxicity. Do not exceed recommended doses.
Throat Spray: Ensure that gag reflex is intact before allowing patient to drink or eat.
Infiltration: Lidocaine with epinephrine may be used to minimize systemic absorption and prolong local anesthesia.
When used concomitantly with other products containing local anesthetic agents, consider amount absorbed from all formulations.
- Lidoderm and ZTLido are not interchangeable.

IV Administration:

Only 1% and 2% solutions are used for IV push injection. Diluent: Administer undiluted.
Diluent: Lidocaine vials need to be further diluted. Dilute 2 g of lidocaine in 250 mL or 500 mL of D5W or 0.9% NaCl. Admixed infusion stable for 24 hr at room temperature. Premixed infusions are already diluted and ready to use.Concentration: 4–8 mg/mL.
Rate: See Route/Dosage section. Administer via infusion pump for accurate dose.

Patient/Family Teaching ⬆ ⬇

Explain purpose of lidocaine to patient.
May cause drowsiness and dizziness. Advise patient to call for assistance during ambulation and transfer.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.
Apply Lidoderm Patch to intact skin to cover the most painful area. Patch may be cut to smaller sizes with scissors before removing release liner. Clothing may be worn over patch. Avoid contact with water (bathing, swimming, showering), may not stick if it gets wet. If irritation or burning sensation occurs during application, remove patch until irritation subsides. Wash hands after application; avoid contact with eyes. Dispose of used patch to avoid access by children or pets.
- Apply ZTLido to intact skin to cover the most painful area. Apply immediately after removing from envelope. System may be cut to smaller sizes with scissors before removing release liner. Clothing may be worn over patch. May be used during moderate exercise (biking for 30 min). May be exposed to water (showering for 10 min or immersion for 15 min). Dry by gently patting the skin, not by rubbing skin or topical system. If edges have lifted, press firmly on edges. If system detaches, may be reapplied as originally directed. If system will not stick, dispose by folding adhesive sides together and discard where children or pets cannot get to them. Apply a new system for total duration of 12 hr of used and new system together. If irritation or a burning sensation occurs during application, remove and reapply when irritation subsides.
- Caution women to consult health care professional before using a topical anesthetic for a mammogram or other procedures. If recommended, use lowest drug concentration, and apply sparingly. Do not apply to broken or irritated skin, do not wrap skin, and do not apply heat to area (heating pad/electric blanket), to decrease chance that drug may be absorbed into the body. May result in seizures, cardiac arrhythmias, respiratory failure, coma, and death.
- Advise patient referred for MRI test to discuss patch with referring health care professional and MRI facility to determine if removal of patch is necessary prior to test and for directions for replacing patch.
Mucosal: Caution parent to administer as directed, not to use more or more often than directed, and to use measuring device for accurate dose in children younger than 3 yr. Advise parent that if signs and symptoms of toxicity (lethargy, shallow breathing, seizure activity) occur to seek emergency attention and not to administer more lidocaine.
- Caution parents that oral lidocaine causes numbness and may impair swallowing; do not administer food and/or chewing gum for at least 60 min after administration.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇