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Lidocaine

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Clinical Particulars

Pharmacodynamics

Pharmacodynamics

Lidocaine is an amide local anaesthetic and antiarrhythmic. Lidocaine is used commonly as a local anesthetic and for acute treatment of ventricular arrhythmias (PubChem, 2024).

Mechanism of Action

  • Nerves: Local anaesthetics bind reversibly to a target receptor in the pore of voltage-gated sodium channels in nerves. Subsequently, ion movement is blocked, preventing the conduction of the action potential in any nerve fibre (Barletta and Reed, 2019; Booth, 2011; Catterall, 2000; PubChem, 2024; Wann, 1993).

  • Muscles: Lidocaine reduces muscle contractility. This may result in vasodilation, hypotension, and altered heart rate (Barletta and Reed, 2019; Booth, 2011; Catterall, 2000; PubChem, 2024; Wann, 1993)

Clinical Applications

Local Lidocaine

Indications include local or regional anaesthesia using infiltration techniques such as percutaneous injection and intravenous regional anaesthesia, peripheral nerve block techniques such as brachial plexus and intercostal, and central neural techniques such as lumbar and caudal epidural blocks. Lidocaine typically produces local anaesthesia within 3 to 5 minutes of administration, and in most veterinary species, this persists for about an hour. Compared to bupivacaine, lidocaine has a faster onset and shorter duration of action (Barletta and Reed, 2019; Booth, 2011; Maddison, 2008; PubChem, 2024).

Systemic Lidocaine

Systemic lidocaine can provide analgesia, anti-inflammatory effects, antiarrhythmic effects (e.g., ventricular fibrillation), and a reduction in inhalant anaesthetic requirements. Lidocaine is considered a class Ib anti-arrhythmic agent. Lidocaine also enhances gastrointestinal motility and free-radical scavenging (Barletta and Reed, 2019; Booth, 2011; Maddison, 2008; PubChem, 2024).


Pharmacokinetics

Absorption

Lidocaine is readily absorbed across mucous membranes and damaged skin but poorly through intact skin. It is quickly absorbed from the upper airway, tracheobronchial tree, and alveoli into the bloodstream (PubChem, 2024).


  • Oral Administration: Although lidocaine is well absorbed across the gastrointestinal tract, the oral bioavailability is only about 35% due to a high degree of first-pass metabolism.

  • Locally Administration: The absorption rate is affected by local vascularity and the presence of tissue and fat capable of binding lidocaine to particular tissues. Subsequently, the concentration of lidocaine in the blood is affected by various aspects, including its absorption rate from the injection site, tissue distribution rate, and metabolism and excretion.

  • Systemic Administration: Systemic absorption of lidocaine is determined by the injection site and the dosage given.

Distribution

  • Lidocaine is well distributed throughout all body tissues. The highest percentage of this drug will be found in skeletal muscle, mainly due to its mass rather than its affinity (PubChem, 2024).

Metabolism

  • Aminoamide local anaesthetics are metabolised primarily by cytochrome P450 enzymes in the liver (PubChem, 2024). 

Excretion

  • The excretion of unchanged lidocaine and its metabolites occurs predominantly via the kidney (PubChem, 2024).

Pharmacokinetics

Precautions

Adverse Effects

Adverse reactions to Lidocaine are rare and usually the result of intravascular injection, excessive dosage or rapid absorption from highly vascular areas.


  • Systemic Signs: Toxicity mainly involves the

  • Central Nervous System: Drowsiness, ataxia, muscle tremors, depression,  and seizures have been reported.

  • Cardiovascular: Decreased cardiac output, cardiovascular depression, and decreased oxygen delivery to tissues have been reported. PR and QRS interval prolongation and QT interval shortening have also been reported. Lidocaine can produce cardiac arrhythmias but has a more significant effect on abnormal than normal cardiac tissue (Papich, 2011; SPC Data).

  • Haemolysis and Methemoglobinemia:  Methemoglobinemia and hemolysis have been reported in humans and cats (Katsuki et al., 2004; Khajavirad et al., 2023; Papich, 2011)

  • Epidural Administration:  Use may result in hypotension, urinary retention, and/or ataxia (SPC Data).

  • Epinephrine Formulations: Systemic absorption or IV injection may cause tachycardia and hypertension (Papich, 2011; SPC Data).

Contraindications

The following contraindications relate to using preparations containing adrenaline ( epinephrine). 


  • Cardiovascular Disease: Avoid lidocaine/epinephrine formulations in patients with cardiovascular disease.

  • Extremities: Lidocaine/epinephrine formulations should not be used in extremities (e.g. digits, ears, nose, or penis) as ischemic injury may result.

  • Intravenous Use: Lidocaine/epinephrine formulations should not be used intravenously.

Reproductive Safety

  • Pregnancy: Avoid Use; lidocaine should not be administered during early pregnancy unless the benefits are considered to outweigh the risks. Lidocaine crosses the placental barrier after epidural or intravenous administration but recommended dose levels are unlikely to have adverse effects (Demeulemeester et al., 2018; Hagai et al., 2015; Morishima et al., 1990; Ramanathan et al., 1986; Reynolds, 2011; Smith et al., 1986).

  • Lactation: Small amounts of Lidocaine are secreted into breast milk, but recommended dose levels are not expected to cause any adverse effects in breastfed infants. No special precautions are required (LactMed, 2006; Reynolds, 2011; Zeisler et al., 1986).

  • Male Fertility: No data available (SPC data).

  • Female Fertility: No data available (SPC data).

  • Neonates: No data available (SPC data).

Significant Interactions

General Information: Significant Interactions are unlikely when lidocaine is administered as recommended.


  • Anaesthetic Agents (e.g., isoflurane, sevoflurane): Lidocaine infusions perioperatively reduce MAC requirements

  • Antiarrhythmics (e.g., procainamide, propranolol, quinidine): If systemically absorbed, lidocaine may cause additive or antagonistic cardiac effects, and toxicity may be enhanced.

  • β-Adrenergic Antagonists (e.g., atenolol, esmolol, propranolol, sotalol): Lidocaine levels or effects may be increased.

  • Morphine: Coadministration of morphine and lidocaine has demonstrated a beneficial synergistic interaction during visceral nociception 

Overdose

  • Maximum Dose:  We recommend a maximum therapeutic dose of 2 mg/kg per administration for rabbits regardless of route, with a maximum administration of 0.5 mg/kg at any site until clear information regarding toxic doses in rabbits is available.

  • Toxic Doses: We regard doses above 4mg/kg as potentially toxic. However, the cumulative convulsive dose and cumulative lethal (cardiotoxic) dose are likely to be far higher (25 mg/kg) (Schnellbacher et al., 2013).

Management

  • Oxygen: If signs of overdose are present, management must begin with the delivery of oxygen via a patent airway, as successful oxygen delivery may prevent convulsions caused by toxicity (Barletta and Reed, 2019).

  • Vascular Decontamination: Intravenous lipids may be helpful where available. Lipid emulsion 20% 1.5 mL/kg IV over 30 minutes can benefit veterinary lidocaine toxicity (Markert et al., 2023).

Precautions

Availability

Some Common Formulations

  1. SPC Data, 2024a. EMLA Cream 5% (5g pack) - Summary of Product Characteristics (SmPC) - (emc) [WWW Document]. URL https://www.medicines.org.uk/emc/product/871/smpc (accessed 2.11.24).

  2. SPC Data, 2024b. Intubeaze 20 mg/ml Laryngopharyngeal Spray, Solution for Cats [WWW Document]. URL https://www.vmd.defra.gov.uk/productinformationdatabase/product/A010010 (accessed 9.30.24).

  3. SPC Data, 2024c. Lidocaine Hydrochloride Injection B.P. 0.5% w/v - Summary of Product Characteristics (SmPC) - (emc) [WWW Document]. URL https://www.medicines.org.uk/emc/product/6593/smpc (accessed 2.12.24).

  4. SPC Data, 2024d. Lidocaine Hydrochloride Injection B.P. 1.0% w/v - Summary of Product Characteristics (SmPC) - (emc) [WWW Document]. URL https://www.medicines.org.uk/emc/product/4781/smpc (accessed 2.12.24).

  5. SPC Data, 2024e. Lidocaine Hydrochloride Injection BP 1% w/v - Summary of Product Characteristics (SmPC) - (emc) [WWW Document]. URL https://www.medicines.org.uk/emc/product/6277/smpc (accessed 2.12.24).

  6. SPC Data, 2024f. Lignol 2.0% w/v Solution for Injection [WWW Document]. URL https://www.vmd.defra.gov.uk/productinformationdatabase/product/A001223 (accessed 2.12.24).

Availability

Identifiers

  • Description: Lidocaine is an anaesthetic of the amide group.

  • Systematic IUPAC Name: 2-(diethylamino)-N-(2,6-dimethyl-phenyl) acetamide

  • Formula: C14-H22-N2-O

  • Pharmacotherapeutic Group:  Antiarrhythmic medicines; Local anaesthetics 

  • ATC Code(s): S02DA01; R02AD02; C01BB01; C05AD01; N01BB02; S01HA07; D04AB01

Identifiers

Evidence-Base

  1. Aria, N., Kauffman, C.L., 2003. Important drug interactions and reactions in dermatology. Dermatol Clin 21, 207–215, ix. https://doi.org/10.1016/s0733-8635(02)00071-2

  2. Barletta, M., Reed, R., 2019. Local Anesthetics. Veterinary Clinics of North America: Small Animal Practice 49, 1109–1125. https://doi.org/10.1016/j.cvsm.2019.07.004

  3. Becker, D.E., Reed, K.L., 2012. Local Anesthetics: Review of Pharmacological Considerations. Anesth Prog 59, 90–102. https://doi.org/10.2344/0003-3006-59.2.90

  4. Beecroft, C., Davies, G., 2013. Systemic toxic effects of local anaesthetics. Anaesthesia & Intensive Care Medicine, Regional Anaesthesia 14, 146–148. https://doi.org/10.1016/j.mpaic.2013.02.001

  5. Booth, D., 2011. Small Animal Clinical Pharmacology and Therapeutics - 2nd Edition [WWW Document]. URL https://shop.elsevier.com/books/small-animal-clinical-pharmacology-and-therapeutics/boothe/978-0-7216-0555-5 (accessed 1.24.24).

  6. Catterall, W.A., 2000. From Ionic Currents to Molecular Mechanisms: The Structure and Function of Voltage-Gated Sodium Channels. Neuron 26, 13–25. https://doi.org/10.1016/S0896-6273(00)81133-2

  7. Cox, B., Durieux, M.E., Marcus, M.A.E., 2003. Toxicity of local anaesthetics. Best Practice & Research Clinical Anaesthesiology 17, 111–136. https://doi.org/10.1053/bean.2003.0275

  8. Demeulemeester, V., Van Hautem, H., Cools, F., Lefevere, J., 2018. Transplacental lidocaine intoxication. J Neonatal Perinatal Med 11, 439–441. https://doi.org/10.3233/NPM-1791

  9. Hagai, A., Diav-Citrin, O., Shechtman, S., Ornoy, A., 2015. Pregnancy outcome after in utero exposure to local anesthetics as part of dental treatment: A prospective comparative cohort study. The Journal of the American Dental Association 146, 572–580. https://doi.org/10.1016/j.adaj.2015.04.002

  10. LactMed, 2006. Lidocaine, in: Drugs and Lactation Database (LactMed®). National Institute of Child Health and Human Development, Bethesda (MD).

  11. Maddison, G., 2008. Small Animal Clinical Pharmacology E-Book: 2nd edition | Edited by Jill E. Maddison | ISBN: 9780702037252 [WWW Document]. Elsevier Asia Bookstore. URL https://www.asia.elsevierhealth.com/small-animal-clinical-pharmacology-e-book-9780702037252.html (accessed 1.23.24).

  12. Morishima, H.O., Finster, M., Arthur, G.R., Covino, B.G., 1990. Pregnancy does not alter lidocaine toxicity. Am J Obstet Gynecol 162, 1320–1324. https://doi.org/10.1016/0002-9378(90)90045-9

  13. Penning, J.P., Yaksh, T.L., 1992. Interaction of intrathecal morphine with bupivacaine and lidocaine in the rat. Anesthesiology 77, 1186–2000. https://doi.org/10.1097/00000542-199212000-00021

  14. Plumb, 2024. Lidocaine [WWW Document]. URL https://app.plumbs.com/drug/aazQZ5yCEYPROD?source=search&searchQuery=lidocaine (accessed 9.18.24).

  15. PubChem, 2024. Lidocaine [WWW Document]. URL https://pubchem.ncbi.nlm.nih.gov/compound/3676 (accessed 9.30.24).

  16. Ramanathan, J., Bottorff, M., Jeter, J.N., Khalil, M., Sibai, B.M., 1986. The pharmacokinetics and maternal and neonatal effects of epidural lidocaine in preeclampsia. Anesth Analg 65, 120–126.

  17. Reynolds, F., 2011. Labour analgesia and the baby: good news is no news. Int J Obstet Anesth 20, 38–50. https://doi.org/10.1016/j.ijoa.2010.08.004

  18. Smith, R.F., Wharton, G.G., Kurtz, S.L., Mattran, K.M., Hollenbeck, A.R., 1986. Behavioral effects of mid-pregnancy administration of lidocaine and mepivacaine in the rat. Neurobehav Toxicol Teratol 8, 61–68.

  19. Verlinde, M., Hollmann, M.W., Stevens, M.F., Hermanns, H., Werdehausen, R., Lirk, P., 2016. Local Anesthetic-Induced Neurotoxicity. International Journal of Molecular Sciences 17, 339. https://doi.org/10.3390/ijms17030339

  20. Wann, K.T., 1993. NEURONAL SODIUM AND POTASSIUM CHANNELS: STRUCTURE AND FUNCTION. British Journal of Anaesthesia 71, 2–14. https://doi.org/10.1093/bja/71.1.2

  21. Wyse, D.G., Kellen, J., Tam, Y., Rademaker, A.W., 1988. Increased efficacy and toxicity of lidocaine in patients on beta-blockers. Int J Cardiol 21, 59–70. https://doi.org/10.1016/0167-5273(88)90009-5

  22. Zeisler, J.A., Gaarder, T.D., De Mesquita, S.A., 1986. Lidocaine excretion in breast milk. Drug Intell Clin Pharm 20, 691–693. https://doi.org/10.1177/106002808602000913

Evidence
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