Lidocaine

Lidocaine
ATC Code A01AE01, C01BB01, C05AD01, D04AB01, N01BB02, R02AD02, S01HA07, S02DA01
Formula C14H22N2O
Molar Mass (g·mol−1) 234,34
Physical State solid
Melting Point (°C) 68,5
PKS Value 8,01[
CAS Number 73-78-9
PUB Number 6314
Drugbank ID DB00281
Solubility poorly soluble in water, very soluble in dichloromethane and ethanol

Basics

Lidocaine is a drug belonging to the class of local anesthetics. In addition to its use as a local anesthetic, lidocaine is used in some cases as a class Ib antiarrhythmic agent. Since its development in the 1940s, it has been one of the most widely used drugs in the world. For example, it is used for anesthesia during minor surgical procedures. Lidocaine is also on the WHO's list of essential medicines.

Lidocaine is usually administered in the form of injections (infiltration anaesthesia) or as a spray or ointment (surface anaesthesia). When used as an antiarrhythmic agent, it is administered exclusively intravenously.

Pharmacology

Pharmacodynamics

The effect of the substance is based on the blockade of voltage-dependent sodium channels located in the membranes of nerve cells. Sodium channels are significantly involved in the transmission of stimuli in the human body. If they are blocked at certain points in the body, no stimuli (e.g. pain) are transmitted from there to the brain. This is the reason for the local anaesthesia of Lidocaine. The antiarrhythmic effect is based on the same principle. Here, however, sodium channels in the heart muscle cells are blocked. This results in a prolongation of the action potential, whereby certain arrhythmias can be remedied. However, lidocaine itself can also cause arrhythmias, which is why it is now rarely considered for this application.

Pharmacokinetics

Lidocaine is well absorbed in the GI tract, but a large portion of the given dose is immediately cleared due to the significant "first pass effect," which is why oral bioavailability is only 35%. Therefore, lidocaine for systemic use (antiarrhythmic) is administered intravenously only. This circumvents the "first pass effect". Lidocaine is 60-80% bound to plasma proteins and is relatively rapidly cleared by the liver. The elimination half-life is 1.5-2 hours. The majority of the given dose is excreted via the kidneys.

Drug Interactions

Drug interactions are not expected when used as a topical anesthetic. When used as an antiarrhythmic agent, class III antiarrhythmic agents should not be given concomitantly under any circumstances.

Toxicity

Typical side effects (common and very common)

  • Hypotension
  • Nausea
  • Paresthesia
  • Dizziness
  • Bradycardia
  • Hypertension
  • Vomiting

Toxicological data

LD50 (rat, oral): 317 mg-kg-1

Sources

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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