Lidocaine HCl (Xylocaine®, Zingo®, Lidoderm®, RectiCare®, LMX®, Akten®)

Overview

Lidocaine is a sodium channel blocker used as an anesthetic agent and in the treatment of ventricular arrhythmias.  It inhibits Na+ conduction through voltage-gated sodium channels in the membranes of neurons and cardiac myocytes, inhibiting action potential formation and propagation.

Lidocaine Visual Summary

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Indications and Dosing

Ventricular Arrhythmia

  • Stable VT: 1-1.5 mg/kg IV/IO + 0.5-0.75 mg/kg Q5-10min, then 1-4 mg/min infusion after rhythm corrected
  • Pulseless VT/VF: 1-1.5 mg/kg IV/IO + 0.5-0.75 mg/kg Q5-10min, then 1-4 mg/min infusion after return of perfusion

Local/Regional Anesthesia

  • Infiltration: 5-300 mg (percutaneous), 50-300 mg (IV regional), 0.5 mg (intradermal) prior to venipuncture
  • Nerve Block: 200-300 mg (brachial, caudal, lumbar), 20-100 mg (dental), 30-50 mg (intercostal, paravertebral), 100 mg (pudendal, paracervical), 50-100 mg (stellate ganglion, lumbar sympathetic), 20-30 mg/dermatome (epidural)

Topical Anesthesia

  • Dermal: 5 g 5% ointment BID-TID applied w/ swab
  • Endotracheal Intubation: 15 mL 2% jelly, or 5 g 5% ointment; applied to device before insertion
  • Ophthalmic: 2 drops/eye 3.5% gel, repeat PRN
  • Oronasopharyngeal: 1-5 mL Q3h PRN; spray or cotton swab 4% solution; or 5 g ointment Q3h for oral mucosa
  • Post-Herpetic Neuralgia: 1-3 5% patches up to 12h/day
  • Pruritic/Painful Dermatoses: Apply cream up to 6x/day PRN
  • Urethral: 3-5 mL (female) or 15 mL (male) 2% jelly into urethra

Interstitial Cystitis

  • Off-label: 200 mg 1x, Q1w, or QD intravesicular; alkalinized w/ sodium bicarbonate

Status Epilepticus

  • Off-label: 1 mg/kg IV, wait 2 min then 0.5 mg/kg IV, then 30 μg/kg/min continuous IV

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Pharmacology

Physiology: Lidocaine inhibits Na+ conduction through voltage-gated sodium channels in the membranes of neurons and cardiac myocytes, inhibiting action potential formation and propagation.  In the context of a ventricular arrhythmia, lidocaine will stabilize the cardiac membranes and increase the likelihood that the arrhythmia will resolve and return to sinus rhythm.  It is a class 1B antiarrhythmic in the Vaughan-Williams system. By inhibiting peripheral nerve impulse propagation, lidocaine also acts as a potent anesthetic agent.

lidocaine_mechanism
Lidocaine Mechanism of Action

Targets: NaV1.x (non-specific)

Half-life: 1.5 – 2h

Excretion: Renal

Metabolism: CYP1A2/3A4 Substrate, CYP2D6 Inhibitor

Other: topical forms not absorbed systemically unless skin/mucosa are compromised

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Safety

Serious Adverse Events

Injected Forms

  • Arrhythmia
  • Cardiovascular Depression
  • Respiratory Depression
  • Audiovisual Disturbance
  • Dizziness/Seizures
  • Malignant Hyperthermia
  • Methemoglobinemia
  • Lethargy/Nausea (common)

Topical Form

  • Hypertension
  • Nausea
  • Anxiety
  • Paresthesia
  • Lightheadedness
  • Local Erythema (common)
  • Local Edema (common)

Contraindications

  • Lidocaine Hypersensitivity
  • Amide Anesthetic Hypersensitivity
  • Adams-Stokes Syndrome  (injected form)
  • WPW Syndrome  (injected form)
  • Severe SA/AV/IV Block (injected form)
  • Skin Injury/Infection (topical)
  • Traumatized Mucosa (topical)

Pregnancy

  • FDA Pregnancy Category B (no good studies in pregnant women, animal studies have not demonstrated fetal toxicity)

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Evidence-Based Medicine

Foundational Studies

  • Lidocaine was originally developed in 1943 for use as a local anesthetic agent
  • Southworth, JAMA, 1950, first reported lidocaine administration during ventricular fibrillation
  • Hitchcock and Keown, Southern Medical Journal 1959, lidocaine use for arrythmia management during cardiac surgery

Recently Published Lidocaine Research

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Drug Cost

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Citations

  1. Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M. DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2017 Nov 8. doi: 10.1093/nar/gkx1037
  2. Epocrates Rx Online [Internet database]. San Mateo (CA): Epocrates, Inc. 2003. Retrieved at mobile.epocrates.com. Web-based; continuous content updates. Accessed 2018 May 21.
  3. “Prescription Prices, Coupons & Pharmacy Information – GoodRx.” Prescription Prices, Coupons & Pharmacy Information – GoodRxhttp://www.goodrx.com
  4. “DailyMed.” U.S. National Library of Medicine, National Institutes of Health, dailymed.nlm.nih.gov/dailymed/.
  5. Southworth, J. L. S., McKusick, U. A., Pierce, E. C., and Rawson, F. L. Ventricular
    fibrillation precipitated by cardiac catheterization. J.A.M.A. 143:717,
    1950

 

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