Lidocaine

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Lidocaine
Lidocaine.svg
Lidocaine-from-xtal-3D-balls.png
Clinical data
PronunciationLidocaine: /ˈlaɪdəkeɪn/ LY-də-kayn [1] [2]
Lignocaine: /ˈlɪɡnəkeɪn/ LIG-nə-kayn
Trade names Xylocaine, Ztlido, others
Other nameslignocaine
AHFS/Drugs.com Local Monograph

Systemic Monograph

Ophthalmic Professional Drug Facts
MedlinePlus a682701
License data
Pregnancy
category
  • AU:A
Routes of
administration 		Intravenous, subcutaneous, topical, by mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 35% (by mouth)
3% (topical)
Metabolism Liver, [7] 90% CYP3A4-mediated
Onset of action Within 1.5 min (IV) [7]
Elimination half-life 1.5 h to 2 h
Duration of action 10 min to 20 min (IV), [7] 0.5 h to 3 h (local) [8] [9]
Excretion Kidney [7]
Identifiers
  • 2-(diethylamino)-
    N-(2,6-dimethylphenyl)acetamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard 100.004.821 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C14H22N2O
Molar mass 234.343 g·mol−1
3D model (JSmol)
Melting point 68 °C (154 °F)
  • Cc1cccc(C)c1NC(=O)CN(CC)CC
  • InChI=1S/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17) Yes check.svgY
  • Key:NNJVILVZKWQKPM-UHFFFAOYSA-N Yes check.svgY
   (verify)

Lidocaine, also known as lignocaine and sold under the brand name Xylocaine among others, is a local anesthetic of the amino amide type. [10] It is also used to treat ventricular tachycardia and ventricular fibrillation. [7] [8] When used for local anaesthesia or in nerve blocks, lidocaine typically begins working within several minutes and lasts for half an hour to three hours. [8] [9] Lidocaine mixtures may also be applied directly to the skin or mucous membranes to numb the area. [10] [8] It is often used mixed with a small amount of adrenaline (epinephrine) to prolong its local effects and to decrease bleeding. [8]

Contents

If injected intravenously, it may cause cerebral effects such as confusion, changes in vision, numbness, tingling, and vomiting. [10] [7] It can cause low blood pressure and an irregular heart rate. [7] There are concerns that injecting it into a joint can cause problems with the cartilage. [8] It appears to be generally safe for use in pregnancy. [7] A lower dose may be required in those with liver problems. [7] It is generally safe to use in those allergic to tetracaine or benzocaine. [8] Lidocaine is an antiarrhythmic medication of the class Ib type. [7] This means it works by blocking sodium channels thus decreasing the rate of contractions of the heart. [10] [7] When injected near nerves, the nerves cannot conduct signals to or from the brain. [8]

Lidocaine was discovered in 1946 and went on sale in 1948. [11] It is on the World Health Organization's List of Essential Medicines. [12] It is available as a generic medication. [8] [13] In 2021, it was the 267th most commonly prescribed medication in the United States, with more than 1 million prescriptions. [14] [15]

Medical uses

Local numbing agent

The efficacy profile of lidocaine as a local anaesthetic is characterized by a rapid onset of action and intermediate duration of efficacy. [10] Therefore, lidocaine is suitable for infiltration, block, and surface anaesthesia. Longer-acting substances such as bupivacaine are sometimes given preference for spinal and epidural anaesthesias; lidocaine, though, has the advantage of a rapid onset of action. [10]

Lidocaine is one of the most commonly used local anaesthetics in dentistry. It can be administered in multiple ways, most often as a nerve block or infiltration, depending on the type of treatment carried out and the area of the mouth worked on. [10]

For surface anaesthesia, several formulations can be used for endoscopies, before intubations. Lidocaine drops can be used on the eyes for short ophthalmic procedures. There is tentative evidence for topical lidocaine for neuropathic pain and skin graft donor site pain. [10] [16] [17] As a local numbing agent, it is used for the treatment of premature ejaculation. [18]

An adhesive transdermal patch containing a 5% concentration of lidocaine in a hydrogel bandage, is approved by the US FDA for reducing nerve pain caused by shingles. [19] The transdermal patch is also used for pain from other causes, such as compressed nerves and persistent nerve pain after some surgeries.

Heart arrhythmia

Lidocaine is a common class-1b antiarrhythmic drug; it is used intravenously for the treatment of ventricular arrhythmias (for acute myocardial infarction, digoxin poisoning, cardioversion, or cardiac catheterization) if amiodarone is not available or contraindicated. [10] Lidocaine should be given for this indication after defibrillation, CPR, and vasopressors have been initiated. A routine preventive dose is no longer recommended after a myocardial infarction as the overall benefit is not convincing. [20]

Epilepsy

A 2013 review on treatment for neonatal seizures recommended intravenous lidocaine as a second-line treatment, if phenobarbital fails to stop seizures. [21]

Other

Intravenous lidocaine infusions are also used to treat chronic pain and acute surgical pain as an opiate sparing technique. The quality of evidence for this use is poor so it is difficult to compare it to placebo or an epidural. [22]

Inhaled lidocaine can be used as a cough suppressor acting peripherally to reduce the cough reflex. This application can be implemented as a safety and comfort measure for people needing intubation, as it reduces the incidence of coughing and any tracheal damage it might cause when emerging from anaesthesia. [23]

A 2019 systematic review of the literature found that intraurethral lidocaine reduces pain in men who undergo cystoscopic procedures. [24]

Lidocaine, along with ethanol, ammonia, and acetic acid, may also help in treating jellyfish stings, both numbing the affected area and preventing further nematocyst discharge. [25] [26]

For gastritis, drinking a viscous lidocaine formulation may help with the pain. [27]

A 2021 study found that lidocaine 5% spray on glans penis 10-20 minutes prior to sexual intercourse significantly improves premature ejaculation. [28] Another study found that lidocaine-prilocaine cream 5% is effective in premature ejaculation and 20 minutes of application time before sexual intercourse. [29]

Adverse effects

Adverse drug reactions (ADRs) are rare when lidocaine is used as a local anesthetic and is administered correctly. Most ADRs associated with lidocaine for anesthesia relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, and allergic reactions only rarely occur. [30] Systemic exposure to excessive quantities of lidocaine mainly results in central nervous system (CNS) and cardiovascular effects – CNS effects usually occur at lower blood plasma concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations. ADRs by individual organ systems are:

ADRs associated with the use of intravenous lidocaine are similar to the toxic effects of systemic exposure above. These are dose-related and more frequent at high infusion rates (≥3 mg/min). Common ADRs include headache, dizziness, drowsiness, confusion, visual disturbances, tinnitus, tremor, and/or paraesthesia. Infrequent ADRs associated with the use of lidocaine include: hypotension, bradycardia, arrhythmias, cardiac arrest, muscle twitching, seizures, coma, and/or respiratory depression. [31]

It is generally safe to use lidocaine with vasoconstrictors such as adrenaline, including in regions such as the nose, ears, fingers, and toes. [32] While concerns of tissue death, if used in these areas, have been raised, the evidence does not support these concerns. [32]

The use of lidocaine for spinal anesthesia may lead to an increased risk of transient neurological symptoms, a painful condition that is sometimes experienced immediately after surgery. [33] There is some weak evidence to suggest that the use of alternative anesthetic medications such as prilocaine, procaine, bupivacaine, ropivacaine, or levobupivacaine may decrease the risk of a person developing transient neurological symptoms. [33] Low-quality evidence suggests that 2‐chloroprocaine and mepivacaine when used for spinal anesthetic have a similar risk of the person developing transient neurological symptoms as lidocaine. [33]

Interactions

Any drugs that are also ligands of CYP3A4 and CYP1A2 can potentially increase serum levels and potential for toxicity or decrease serum levels and the efficacy, depending on whether they induce or inhibit the enzymes, respectively. Drugs that may increase the chance of methemoglobinemia should also be considered carefully. Dronedarone and liposomal morphine are both absolutely a contraindication, as they may increase the serum levels, but hundreds of other drugs require monitoring for interaction. [34]

Contraindications

Absolute contraindications for the use of lidocaine include:

Exercise caution in people with any of these:

Overdosage

Overdoses of lidocaine may result from excessive administration by topical or parenteral routes, accidental oral ingestion of topical preparations by children (who are more susceptible to overdose), accidental intravenous (rather than subcutaneous, intrathecal, or paracervical) injection, or from prolonged use of subcutaneous infiltration anesthesia during cosmetic surgery.[ citation needed ] The maximum safe dose is 3 mg per kg. [10]

Such overdoses have often led to severe toxicity or death in both children and adults (local anesthetic systemic toxicity). [41] Symptoms include central nervous system manifestations such as numbness of the tongue, dizziness, tinnitus, visual disturbances, convulsions, reduced consciousness progressing to coma, as well as respiratory arrest and cardiovascular disturbances. [42] Lidocaine and its two major metabolites may be quantified in blood, plasma, or serum to confirm the diagnosis in potential poisoning victims or to assist forensic investigation in a case of fatal overdose. [ citation needed ]

Lidocaine is often given intravenously as an antiarrhythmic agent in critical cardiac-care situations. [43] Treatment with intravenous lipid emulsions (used for parenteral feeding) to reverse the effects of local anaesthetic toxicity is becoming more common. [44] [45]

Postarthroscopic glenohumeral chondrolysis

Lidocaine in large amounts may be toxic to cartilage and intra-articular infusions can lead to postarthroscopic glenohumeral chondrolysis. [46]

Pharmacology

Mechanism of action

Lidocaine alters signal conduction in neurons by prolonging the inactivation of the fast voltage-gated Na+ channels in the neuronal cell membrane responsible for action potential propagation. [10] [47] With sufficient blockage, the voltage-gated sodium channels will not open and an action potential will not be generated. Careful titration allows for a high degree of selectivity in the blockage of sensory neurons, whereas higher concentrations also affect other types of neurons.[ citation needed ]

The same principle applies to this drug's actions in the heart. Blocking sodium channels in the conduction system, as well as the muscle cells of the heart, raises the depolarization threshold, making the heart less likely to initiate or conduct early action potentials that may cause an arrhythmia. [48]

Pharmacokinetics

When used as an injectable it typically begins working within four minutes and lasts for half an hour to three hours. [8] [9] Lidocaine is about 95% metabolized (dealkylated) in the liver mainly by CYP3A4 to the pharmacologically active metabolites monoethylglycinexylidide (MEGX) and then subsequently to the inactive glycine xylidide. MEGX has a longer half-life than lidocaine, but also is a less potent sodium channel blocker. [49] The volume of distribution is 1.1 L/kg to 2.1 L/kg, but congestive heart failure can decrease it. About 60% to 80% circulates bound to the protein alpha1 acid glycoprotein. The oral bioavailability is 35% and the topical bioavailability is 3%. Lidocaine efficacy may be reduced in tissues that are inflamed, due to competing inflammatory mediators. [10]

The elimination half-life of lidocaine is biphasic and around 90 min to 120 min in most people. This may be prolonged in people with hepatic impairment (average 343 min) or congestive heart failure (average 136 min). [50] Lidocaine is excreted in the urine (90% as metabolites and 10% as unchanged drug). [51]

Chemistry

Molecular structure and conformational flexibility

Lidocaine's 1,5-dimethylbenzene group gives it hydrophobic properties. In addition to this aromatic unit, lidocaine has an aliphatic section comprising amide, carbonyl, and enyl groups.

Lidocaine exhibits a remarkable degree of conformational flexibility, resulting in more than 60 probable conformers. [52] This adaptability arises from the high lability of the amide and ethyl groups within the molecule. These groups can undergo shifts in their positions, leading to significant variations in the overall molecular configuration.

Influence of temperature and pressure on conformational preference

The dynamic transformation of lidocaine conformers in supercritical carbon dioxide (scCO2) highly depends on external factors such as pressure [52] and temperature. [53] Alterations in these conditions can lead to distinct conformations, impacting the molecule's physicochemical properties. One notable consequence of these variations is the particle size of lidocaine when produced through micronization using scCO2. Changes in the position of the amide group within the molecule can trigger a redistribution of intra- and intermolecular hydrogen bonds, affecting the outcome of the micronization process and the resultant particle size. [54]

Veterinary use

Lidocaine is commonly used in veterinary medicine in both companion and production animals around the world and is listed as an essential veterinary medicine by the World Veterinary Association and also the World Small Animal Veterinary Association. [55]

In veterinary medicine, it is commonly used as a local anaesthetic both as an injectable or topical product. It provides excellent local anaesthesia when given by local infiltration into a tissue or via specific nerve blocks. These are commonly applied to nerves of the head, limbs, thorax, and spine. It can also be used to treat ventricular arrhythmias when given intravenously. In most veterinary species, when given via injection, it has a rapid onset of action (2-10 minutes) with a duration of action of 30-60 minutes. [56]

In veterinary species, its metabolism is much the same as humans with rapid metabolism in the liver to the major metabolites MEGX (monoethylglycine xylidide) and GX (glycine xylidide) that retain partial activity against sodium channels. These compounds are further metabolized to monoethylglycine and xylidide, respectively. [56]

Toxicity in animals is similar to that seen in humans with both toxicity to the central nervous system (CNS) and cardiovascular system observed. General the CNS signs are seen first with agitation and muscle twitching seen before the cardiovascular signs of hypotension, myocardial depression, and arrhythmias. Further CNS depression will result from higher doses with seizures and convulsions and eventually apnea and death. [56]

It is a component of the veterinary drug Tributame along with embutramide and chloroquine used to carry out euthanasia on horses and dogs. [57] [58]

History

Lidocaine, the first amino amide–type local anesthetic (previous were amino esters), was first synthesized under the name 'xylocaine' by Swedish chemist Nils Löfgren in 1943. [59] [60] [61] His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself. [59] It was first marketed in 1949.

Society and culture

Dosage forms

Lidocaine, usually in the form of its hydrochloride salt, is available in various forms including many topical formulations and solutions for injection or infusion. [62] It is also available as a transdermal patch, which is applied directly to the skin.[ citation needed ]

Names

Lidocaine is the International Nonproprietary Name (INN), British Approved Name (BAN), and Australian Approved Name (AAN), [63] while lignocaine is the former BAN[ citation needed ] and AAN. Both the old and new names will be displayed on the product label in Australia until at least 2023. [64]

Xylocaine is a brand name, referring to the major synthetic building block 2,6-xylidine. The "ligno" prefix is chosen because "xylo" means wood in Greek while "ligno" means the same in Latin. The "lido" prefix instead refers to the fact that the drug is chemically related to acetanilide. [61]

Recreational use

As of 2021, lidocaine is not listed by the World Anti-Doping Agency as a substance whose use is banned in sport. [65] It is used as an adjuvant, adulterant, and diluent to street drugs such as cocaine and heroin. [66] It is one of the three common ingredients in site enhancement oil used by bodybuilders. [67]

Adulterant in cocaine

Lidocaine is often added to cocaine as a diluent. [68] [69] Cocaine and lidocaine both numb the gums when applied. This gives the user the impression of high-quality cocaine when in actuality the user is receiving a diluted product. [70]

Compendial status

Related Research Articles

Local anesthesia is any technique to induce the absence of sensation in a specific part of the body, generally for the aim of inducing local analgesia, i.e. local insensitivity to pain, although other local senses may be affected as well. It allows patients to undergo surgical and dental procedures with reduced pain and distress. In many situations, such as cesarean section, it is safer and therefore superior to general anesthesia.

<span class="mw-page-title-main">Local anesthetic</span> Medications to reversibly block pain

A local anesthetic (LA) is a medication that causes absence of all sensation in a specific body part without loss of consciousness, providing local anesthesia, as opposed to a general anesthetic, which eliminates all sensation in the entire body and causes unconsciousness. Local anesthetics are most commonly used to eliminate pain during or after surgery. When it is used on specific nerve pathways, paralysis also can be induced.

<span class="mw-page-title-main">Procaine</span> Local anesthetic drug

Procaine is a local anesthetic drug of the amino ester group. It is most commonly used in dental procedures to numb the area around a tooth and is also used to reduce the pain of intramuscular injection of penicillin. Owing to the ubiquity of the trade name Novocain or Novocaine, in some regions, procaine is referred to generically as novocaine. It acts mainly as a sodium channel blocker. Today, it is used therapeutically in some countries due to its sympatholytic, anti-inflammatory, perfusion-enhancing, and mood-enhancing effects.

Lidocaine/prilocaine is a eutectic mixture of equal quantities of lidocaine and prilocaine. A 5% emulsion preparation, containing 2.5% each of lidocaine/prilocaine, is marketed by APP Pharmaceuticals under the trade name EMLA. As a spray, it is marketed under the name Tempe (PSD502) that can be used by men to help with premature ejaculation. The spray is manufactured by Plethora Solutions and branded as Fortacin in the UK and Recordati in the EU.

<span class="mw-page-title-main">Bupivacaine</span> Local anaesthetic drug

Bupivacaine, marketed under the brand name Marcaine among others, is a medication used to decrease sensation in a specific small area. In nerve blocks, it is injected around a nerve that supplies the area, or into the spinal canal's epidural space. It is available mixed with a small amount of epinephrine to increase the duration of its action. It typically begins working within 15 minutes and lasts for 2 to 8 hours.

<span class="mw-page-title-main">Ropivacaine</span> Local anaesthetic drug

Ropivacaine (rINN) is a local anaesthetic drug belonging to the amino amide group. The name ropivacaine refers to both the racemate and the marketed S-enantiomer. Ropivacaine hydrochloride is commonly marketed by AstraZeneca under the brand name Naropin.

<span class="mw-page-title-main">Nerve block</span> Deliberate inhibition of nerve impulses

Nerve block or regional nerve blockade is any deliberate interruption of signals traveling along a nerve, often for the purpose of pain relief. Local anesthetic nerve block is a short-term block, usually lasting hours or days, involving the injection of an anesthetic, a corticosteroid, and other agents onto or near a nerve. Neurolytic block, the deliberate temporary degeneration of nerve fibers through the application of chemicals, heat, or freezing, produces a block that may persist for weeks, months, or indefinitely. Neurectomy, the cutting through or removal of a nerve or a section of a nerve, usually produces a permanent block. Because neurectomy of a sensory nerve is often followed, months later, by the emergence of new, more intense pain, sensory nerve neurectomy is rarely performed.

<span class="mw-page-title-main">Proxymetacaine</span> Chemical compound

Proxymetacaine (INN) or proparacaine (USAN) is a topical anesthetic drug of the aminoester group.

<span class="mw-page-title-main">Articaine</span> Chemical compound

Articaine is a dental amide-type local anesthetic. It is the most widely used local anesthetic in a number of European countries and is available in many countries. It is the only local anaesthetic to contain a thiophene ring, meaning it can be described as 'thiophenic'; this conveys lipid solubility.

<span class="mw-page-title-main">Prilocaine</span> Local anesthetic of the amino amide type

Prilocaine is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils Löfgren. In its injectable form, it is often used in dentistry. It is also often combined with lidocaine as a topical preparation for dermal anesthesia, for treatment of conditions like paresthesia. As it has low cardiac toxicity, it is commonly used for intravenous regional anaesthesia (IVRA).

<span class="mw-page-title-main">Chloroprocaine</span> Local anaesthetic drug

Chloroprocaine is a local anesthetic given by injection during surgical procedures and labor and delivery. Chloroprocaine vasodilates; this is in contrast to cocaine which vasoconstricts. Chloroprocaine is an ester anesthetic.

<span class="mw-page-title-main">Levobupivacaine</span> Chemical compound

Levobupivacaine (rINN) is a local anaesthetic drug indicated for minor and major surgical anaesthesia and pain management. It is a long-acting amide-type local anaesthetic that blocks nerve impulses by inhibiting sodium ion influx into the nerve cells. Levobupivacaine is the S-enantiomer of racemic bupivacaine and therefore similar in pharmacological effects. The drug typically starts taking effect within 15 minutes and can last up to 16 hours depending on factors such as site of administration and dosage.

Veterinary anesthesia is a specialization in the veterinary medicine field dedicated to the proper administration of anesthetic agents to non-human animals to control their consciousness during procedures. A veterinarian or a Registered Veterinary Technician administers these drugs to minimize stress, destructive behavior, and the threat of injury to both the patient and the doctor. The duration of the anesthesia process goes from the time before an animal leaves for the visit to the time after the animal reaches home after the visit, meaning it includes care from both the owner and the veterinary staff. Generally, anesthesia is used for a wider range of circumstances in animals than in people not only due to their inability to cooperate with certain diagnostic or therapeutic procedures, but also due to their species, breed, size, and corresponding anatomy. Veterinary anesthesia includes anesthesia of the major species: dogs, cats, horses, cattle, sheep, goats, and pigs, as well as all other animals requiring veterinary care such as birds, pocket pets, and wildlife.

Dental anesthesia is the application of anesthesia to dentistry. It includes local anesthetics, sedation, and general anesthesia.

Topical tac is a topical anesthetic solution introduced by Pryor et al. in 1980. It is a mixture of 5 to 12% tetracaine, 0.05% adrenaline, and 4 or 10% cocaine hydrochloride. It has been used in ear, nose, and throat surgery and in the emergency department where numbing of the surface is needed rapidly. Use in the pediatric patient cohort has been documented, including when children have been injured in the eye, ear, or other sensitive locations.

<span class="mw-page-title-main">Intravenous regional anesthesia</span>

Intravenous regional anesthesia (IVRA) or Bier's block anesthesia is an anesthetic technique on the body's extremities where a local anesthetic is injected intravenously and isolated from circulation in a target area. The technique usually involves exsanguination of the target region, which forces blood out of the extremity, followed by the application of pneumatic tourniquets to safely stop blood flow. The anesthetic agent is intravenously introduced into the limb and allowed to diffuse into the surrounding tissue while tourniquets retain the agent within the desired area.

Ocular surgery may be performed under topical, local or general anesthesia. Local anaesthesia is more preferred because it is economical, easy to perform and the risk involved is less. Local anaesthesia has a rapid onset of action and provides a dilated pupil with low intraocular pressure.

Balanced anesthesia, also known as multimodal anesthesia, is a technique used to induce and maintain anesthesia in patients undergoing surgery or certain medical procedures. This method employs a combination of anesthetic agents and other drugs – and techniques – to selectively target various aspects of the central nervous system, allowing for a tailored anesthetic experience based on the individual patient's needs and the specific requirements of the procedure.

Total intravenous anesthesia (TIVA) refers to the intravenous administration of anesthetic agents to induce a temporary loss of sensation or awareness. The first study of TIVA was done in 1872 using chloral hydrate, and the common anesthetic agent propofol was licensed in 1986. TIVA is currently employed in various procedures as an alternative technique of general anesthesia in order to improve post-operative recovery.

References

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  5. ↑ "Xylocaine MPF- lidocaine hydrochloride injection, solution Xylocaine- lidocaine hydrochloride injection, solution Xylocaine- lidocaine hydrochloride,epinephrine bitartrate injection, solution". DailyMed. Retrieved 11 April 2021.
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  20. ↑ Martí-Carvajal AJ, Simancas-Racines D, Anand V, Bangdiwala S (August 2015). "Prophylactic lidocaine for myocardial infarction". The Cochrane Database of Systematic Reviews. 8 (8): CD008553. doi:10.1002/14651858.CD008553.pub2. PMC   8454263 . PMID   26295202.
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  23. ↑ Biller JA (2007). "Airway obstruction, bronchospasm, and cough". In Berger AM, Shuster JL, Von Roenn JH (eds.). Principles and practice of palliative care and supportive oncology. Hagerstwon, MD: Lippincott Williams & Wilkins. pp. 297–307. ISBN   978-0-7817-9595-1. Inhaled lidocaine is used to suppress cough during bronchoscopy. Animal studies and a few human studies suggest that lidocaine has an antitussive effect…
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