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Лидокаин

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Лидокаин

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

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Overview of Лидокаин

Quick Facts

Property Description
Active Ingredient Lidocaine Hydrochloride
Pharmacological Class Amide-type Local Anesthetic, Class Ib Antiarrhythmic
Common Use (General) Inducing local numbness and stabilizing heart rhythm
Origin Synthetic (Acetanilide Derivative)

What is Lidocaine: Definition and Pharmacological Class

Lidocaine is a synthetic medicinal agent that is chemically classified as a derivative of acetanilide. Its active ingredient is Lidocaine Hydrochloride, which is the internationally recognized INN (International Nonproprietary Name) for this substance. Lidocaine holds a dual pharmacological role, being categorized as both an amide-type local anesthetic and an antiarrhythmic agent of Class Ib.

This essential dual classification, which includes it on the WHO Model List of Essential Medicines, defines its core utility. The drug is clinically recognized for its ability to induce local numbness to alleviate pain and is also used to stabilize dangerous irregularities in heart rhythm, particularly ventricular arrhythmias.

Composition and Forms: The Versatility of Lidocaine

Lidocaine Hydrochloride is a highly versatile active component, supporting both regional pain control and systemic heart applications. It is manufactured in several key pharmaceutical forms to suit diverse therapeutic needs and routes of administration. These forms include a sterile solution for injection (used for parenteral administration in procedures like nerve blocks), as well as preparations for topical and external use such as a spray, gel, or transdermal patch.

The final composition of these medicinal products is based on the active ingredient combined with an appropriate aqueous or polymeric base. The broad availability of Lidocaine, from injectable solutions to topical gels, makes it a cornerstone of accessible and targeted pain management and cardiac instability control.

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What side effects are possible with Лидокаин?

Possible Side Effects and Safety Information

The safety profile of Lidocaine, as classified in official regulatory documents, primarily involves effects on the nervous system and cardiovascular function, which are related to systemic exposure. Adverse reactions are grouped by frequency and the body system affected.

Commonly Documented Adverse Reactions

Adverse effects listed as common in regulatory sources include dizziness, somnolence (drowsiness), and hypotension (low blood pressure). These are generally observed when systemic absorption occurs, such as with injectable forms. Uncommon effects may include signs of central nervous system (CNS) toxicity, such as tremor, tinnitus (ringing in the ears), and convulsions.

Serious Adverse Reactions and Constraints

Regulatory agencies document several rare but serious adverse reactions, including severe systemic toxicity that can lead to respiratory arrest and major cardiac depression that may result in cardiac arrest. The official safety profile also notes risks of Methemoglobinemia and severe anaphylactic reactions.

Lidocaine is officially contraindicated in patients with a history of hypersensitivity to amide-type local anesthetics and those with specific severe pre-existing cardiac conduction disturbances, such as severe heart block without a functioning pacemaker.

Population-Specific Safety Notes

Official labeling addresses specific populations: Older adults and individuals with severe hepatic (liver) impairment may require special considerations due to altered drug metabolism and increased risk of toxic blood concentrations. Similarly, pediatric patients are noted to be at increased risk of systemic toxicity. The risk of adverse effects, particularly CNS toxicity, is noted to be related to the total administered dose and the rate of injection.

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Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Lidocaine overdose describes systemic toxicity resulting from excessively high plasma concentrations. Manifestations primarily affect the Central Nervous System (CNS) and the Cardiovascular System.

Overdose often presents with a biphasic CNS pattern. Early signs may include sensory disturbances like tinnitus, a metallic taste, blurred vision, and nervousness. This can progress rapidly to more severe motor and depressive signs, including muscle twitching, seizures, and eventually unconsciousness.

The most serious outcomes are cardiovascular. Overdose may lead to severe events such as marked bradycardia, hypotension, cardiovascular collapse, and potentially cardiac arrest and respiratory arrest. A serious hematologic complication, Methemoglobinemia, is also documented, characterized by cyanotic skin discoloration.


When Immediate Medical Help is Required

The Prescribing Information mandates that patients must seek immediate medical attention for any signs of systemic toxicity, particularly if symptoms of methemoglobinemia (e.g., cyanotic skin, rapid heart rate) or progressive CNS effects are observed. Immediate treatment is required to avert life-threatening effects. Management is symptomatic and supportive, requiring the availability of resuscitative equipment and specific interventions like methylene blue for methemoglobinemia. Patients with severe hepatic disease and infants under 6 months of age are listed as having an increased susceptibility to toxic concentrations.

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Therapeutic Uses of Лидокаин

Lidocaine plays a role in managing two distinct categories of symptoms: pain and cardiac rhythm disturbances.


What Лидокаин treats: main uses and benefits

Lidocaine’s primary function is as a local anesthetic, which is applied across domains where additional symptomatic support is needed to help manage symptoms related to physical discomfort. It is commonly applied to facilitate local or regional anesthesia in clinical scenarios such as infiltration, nerve block, and epidural procedures. This use is relevant when supportive symptom management is appropriate to ease the overall symptom burden during medical or surgical procedures. The general patient benefit is captured by the principle: “provides support that helps ease the overall symptom burden.”

In a separate therapeutic domain, the injectable form of lidocaine is also applied in addressing acute ventricular arrhythmias. This use is relevant in conditions involving episodic or fluctuating manifestations of heart rhythm disturbances. It may assist with maintaining functional stability in settings marked by temporary physiological imbalance, providing short-term symptomatic assistance when warranted.

Quick Fact: Relief for Acute Discomfort

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Eligibility and Restrictions for Use

Who Can and Cannot Use Lidocaine

Official regulatory documents define strict eligibility criteria for Lidocaine, specifying absolute contraindications and populations requiring restricted use.


Absolute Non-Eligibility (Contraindications)

Lidocaine is contraindicated in patients with a known hypersensitivity to amide-type local anesthetics. Absolute exclusions also include individuals experiencing severe shock or those with severe degrees of heart block (second or third degree) that are not managed by a pacemaker.


Conditional and Restricted Use

Use is highly restricted and requires caution in several patient groups, often necessitating reduced doses:

Population Group Regulatory Condition
Organ Impairment Patients with severe hepatic or renal impairment require caution and dose reduction

. | | Age (Infants) | Infants under 6 months must be treated with extreme caution due to increased risk of methemoglobinemia. | | Age (Geriatric) | Elderly, debilitated, or acutely ill patients require doses commensurate with their physical status. | | Reproductive Status | During pregnancy (FDA Category B/AU Category A), use is recommended only if clearly needed. Use while breastfeeding requires caution. |

These restrictions ensure the medicine is only administered where official labeled conditions for use are met.

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What should I know about interactions with other medicines?

Interactions with other medicines and products

The interaction profile of Lidocaine is officially documented around two main types: Pharmacokinetic, involving altered clearance, and Pharmacodynamic, involving additive effects.


Pharmacokinetic Interactions: Altered Plasma Exposure

Lidocaine is primarily cleared by hepatic metabolism involving the CYP1A2 and CYP3A4 enzyme pathways. Interactions affecting these pathways can modify systemic exposure, as stated in regulatory documents.

  • Increased Exposure (Reduced Clearance): Co-administration with enzyme inhibitors, such as Fluvoxamine and Cimetidine, and substances that decrease hepatic blood flow like Propranolol, reduces Lidocaine's clearance and may significantly increase its plasma concentration. Fluvoxamine, specifically, is documented to increase the drug's systemic exposure (AUC) by approximately 1.7-fold.
  • Decreased Exposure (Increased Clearance): The anticonvulsant Phenytoin may stimulate Lidocaine's hepatic metabolism, potentially leading to decreased plasma levels.

Pharmacodynamic Interactions and Restrictions

These interactions result in additive physiological effects, primarily on cardiac and neurological function.

  • Additive Toxic Effects: Co-administration with other antiarrhythmic drugs (e.g., Amiodarone, Quinidine) or other local anesthetics results in documented additive toxicity, particularly regarding cardiac and systemic effects.
  • Neuromuscular Blockade: Concurrent use with muscle relaxants (e.g., Suxamethonium) carries an officially recognized risk of enhanced and prolonged neuromuscular blockade.
  • Prohibited Combination: Co-administration with Quinupristin/Dalfopristin should be avoided due to the potential for significantly increased Lidocaine plasma levels and a subsequent risk of ventricular arrhythmias.

Population and Substance Notes

Interaction risk may be higher in patients with hepatic impairment due to reduced clearance. Ingestion of grapefruit or grapefruit juice may also increase plasma concentrations by inhibiting CYP3A4.

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Mechanism of Action

How Лидокаин Works

The mechanism of action for Лидокаин centers on its ability to interrupt electrical signaling in excitable cells, exerting its effects across two distinct physiological systems through one core molecular action: the targeted blockade of sodium channels.

Лидокаин acts directly on voltage-gated sodium channels (NaV channels), the critical molecular gatekeepers responsible for initiating electrical impulses. The molecule physically obstructs the inner pore of these channels, preventing the necessary influx of sodium ions (Na^+) across the cell membrane. This action raises the threshold needed to generate an electrical signal, stabilizing the membrane and functionally blocking the propagation of impulses along peripheral nerve fibers and within the cardiac tissue.

Лидокаин exhibits use-dependence, meaning its blocking effect intensifies in tissue that is firing rapidly or abnormally. This kinetic selectivity results in a reduction of excessive electrical discharges and ectopic activity. The drug’s efficacy is constrained by the local pH level; in acidic conditions (e.g., inflammation), a higher proportion of the molecule becomes charged, which limits its ability to cross the cell membrane and reach the intracellular binding site.

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Dosage and Administration Information

How to Use Lidocaine: Official Administration Guidelines

Lidocaine is utilized through several distinct administration protocols, which are dictated by the intended application and governed by official documents. Use patterns are strictly divided between parenteral administration for antiarrhythmic and local anesthetic purposes, and topical use for external pain relief.


Administration Routes and Dosing Patterns

Application Domain Key Administration Rules Official Dosing Principle
Antiarrhythmic Use Administered via Intravenous (IV) bolus followed by continuous infusion. Initial dose is typically 1 to 1.5 mg/kg, followed by a maintenance infusion of 1 to 4 mg per minute.
Local Anesthesia Administered via Infiltration, Nerve Block, or Epidural injection. The total maximum single dose for non-epinephrine solutions is generally 4.5 mg/kg (up to 300 mg total).
Topical Use Applied to the skin via transdermal patch or mucous membranes via gel/solution. The patch is used for intermittent, time-limited application, typically worn for a maximum of 8 to 12 hours within a 24-hour period.

Procedural and Population Requirements

All injection procedures mandate specific steps, such as aspiration prior to injection to ensure proper placement and visual inspection for particulate matter before use. For continuous IV infusion, the solution is often prepared by dilution with a fluid such as 5% Dextrose in Water. Dosage adjustments are a required principle for certain patient populations, with official instructions advising the use of reduced doses for older adults and individuals with severe hepatic impairment. Additionally, only preservative-free preparations must be used for administration via the central neural axis (spinal or epidural routes).

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Recent Clinical Evidence

Research Evidence / Overview of Studies for Лидокаин (Lidocaine)


Evidence for Use in Local and Regional Anesthesia

Research supporting the use of Lidocaine for local and regional anesthesia includes Randomized Controlled Trials (RCTs), comparative studies, and systematic reviews. This research examined how Lidocaine is used in research exploring how symptoms change over time when administered before or during various procedures, such as nerve blocks, infiltration, and topical applications to mucosal surfaces. Research explored outcomes related to physical discomfort, including measuring changes in pain intensity using standardized scales and the duration of the effect. Research explored outcomes related to physical discomfort, which included measured differences in pain scores compared to placebo injections in infiltration and nerve block settings.

What remains uncertain is the full picture regarding outcomes beyond the immediate procedural recovery period. While the short-term profile is well-characterized, follow-up durations were limited in many studies, focusing mainly on the minutes or hours during and immediately following the procedure. Furthermore, evidence quality varies across studies when comparing Lidocaine to the wide array of newer localized sensory agents.


Evidence for Use in Acute Heart Rhythm Stabilization

Intravenous Lidocaine was studied as a Class Ib antiarrhythmic agent, primarily in acute, critical settings. Research has explored outcomes related to systemic or functional imbalance, particularly in patients experiencing conditions characterized by acute or disruptive episodes of ventricular arrhythmias. The main endpoints studies monitored included the measured effect on the abnormal rhythm, the proportion of patients where spontaneous circulation was measured (ROSC), and short-term survival rates.

Findings data show patterns related to measurements of the heart's electrical rhythm in these acute scenarios. However, when comparing Lidocaine to other antiarrhythmic medications in this setting, findings were mixed across various studies, especially concerning major endpoints like long-term survival and favorable neurological outcomes. Long-term effects are not fully established, and comparative evidence is lacking for certain specific ventricular arrhythmia types, leading to ongoing research to clarify the drug’s use relative to other available therapies.


What is Still Uncertain about Лидокаин

A major area of uncertainty is the variability of findings in acute care settings, particularly when comparing intravenous Lidocaine to other antiarrhythmic agents, where findings were mixed regarding long-term outcomes like survival. For its anesthetic use, evidence quality varies across studies in comparing topical Lidocaine to other pain-relieving products. Overall, evidence is limited concerning long-term durability of effect for both indications. Follow-up durations were limited in many pivotal trials, and sample sizes were modest in some of the older or highly specific studies.

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Frequently Asked Questions (FAQ)

Common questions about Лидокаин (FAQ)


Q: What is the main difference between an anesthetic and an analgesic, in the context of Лидокаин?

A: Лидокаин is officially classified as a local anesthetic, meaning it works by causing a temporary loss of feeling or numbness in a specific, targeted area. An analgesic, by comparison, is a type of medicine used to relieve or reduce pain without causing a complete loss of sensation or numbness. This distinction is based on how the drug affects the body’s nerve signals.

Q: Is the sensation of tingling or burning after application described as a normal effect?

A: Regulatory documents mention temporary effects at the application site for topical forms. These can include sensations like minor itching, tingling, or mild burning, as well as common observations of redness or paleness. These local reactions are generally expected to resolve quickly once the application is finished or removed.

Q: Is it true that different strengths of Лидокаин cream exist?

A: Yes. Official product information confirms that Лидокаин is manufactured in various topical forms, including creams and ointments, with multiple concentration strengths available. These concentrations are formulated to suit different therapeutic needs, with some being available over-the-counter and others requiring a prescription.

Q: Why is Лидокаин sometimes referred to as Xylocaine?

A: Лидокаин is the official, internationally recognized generic (nonproprietary) name for the active drug component. Xylocaine is one of the original and common brand names under which this medicine is marketed and officially recognized in many regulatory documents. Both names refer to the same active ingredient.

Q: Is it common for people to misunderstand the difference between local and general anesthesia?

A: The medicine is a local anesthetic which is designed to block pain signals only in a targeted area of the body. This mechanism is distinct from general anesthesia, which is used to cause a reversible state of unconsciousness. Regulatory information emphasizes the drug's localized effect.

Q: How does the onset time of Лидокаин generally compare when applied to the skin versus when injected?

A: According to official clinical information, solutions that are injected directly into tissue typically have a very rapid onset of action, often within minutes. In contrast, topical applications (such as patches or creams) require a longer duration of contact time on the skin to be adequately absorbed and produce their full numbing effect.

Q: How is the duration of effect for injected Лидокаин described in official documents?

A: Official labeling for injectable solutions classifies their duration of effect as intermediate. For example, in a specific formulation used for spinal anesthesia, the duration of surgical numbness averages about two hours, though this can vary by specific formulation.

Q: What is the role of epinephrine when sometimes included with injected Лидокаин?

A: Some injectable formulations of Лидокаин include the medicine epinephrine. Regulatory documents describe this substance as a vasoconstrictor, which works to tighten local blood vessels. This action is used to help prolong the duration of the anesthetic effect in the targeted area and reduce the amount of Лидокаин that enters the bloodstream too quickly.

Q: Why is a small patch test sometimes mentioned before using a larger amount of topical Лидокаин?

A: The official contraindications state that Лидокаин should not be used in individuals with a known hypersensitivity (severe allergic reaction) to local anesthetics of the amide type. Procedures like a small patch test may be used in clinical settings to assess a patient's risk of a reaction, which is a required safety consideration before applying the full dose.

Q: Is Лидокаин commonly used for pain relief that is not related to a procedure?

A: Yes. Regulatory documents describe the use of certain topical forms, such as the 5% patch, for treating pain associated with specific chronic conditions. The medicine is indicated for the relief of pain associated with post-herpetic neuralgia, which is nerve pain that can persist after a shingles outbreak.

Q: Do certain forms of Лидокаин, like gels or patches, work faster than others?

A: Official information does not provide a direct comparison of onset time between gels, creams, and patches. The rate of onset for any topical application depends on the specific product's formulation, concentration, and the particular site of application on the body.

Q: Can the feeling of numbness from Лидокаин last longer than expected?

A: While the expected duration is generally outlined in the product information, official safety profiles caution against certain conditions. Using excessive amounts or covering the application site with a tight, occlusive dressing can increase the amount of medicine absorbed into the body, which may lead to more intense or prolonged effects.

Q: How does the term 'systemic absorption' relate to topical Лидокаин use?

A: Systemic absorption is the process where the medicine passes from the skin into the bloodstream and then travels throughout the body. Regulatory documents warn that when a topical dose is absorbed systemically, it raises the potential for side effects that affect the entire body, such as those involving the nervous system or heart.

Q: Is there a maximum amount of topical Лидокаин that can be applied per day, according to regulatory documents?

A: Yes, regulatory documents specify maximum limits to control systemic exposure. For the 5% topical patch, the application is limited to a maximum of four patches at one time for up to 12 hours within a 24-hour period. For other topical forms, the total daily dose is typically limited to prevent toxicity.

Q: Are there different classifications of Лидокаин use for children versus adults?

A: Yes, official warnings address special patient populations. Children under 6 months are noted to require extreme caution due to specific risks like methemoglobinemia. For older children, doses are typically determined based on age and weight to minimize the risk of drug toxicity.

Q: Is Лидокаин the same type of medicine as Novocaine?

A: No, they belong to different chemical categories. Лидокаин is classified as an amide-type local anesthetic. Novocaine (procaine) is classified as an ester-type local anesthetic. While both are used to numb specific areas, they have distinct chemical structures.

Q: Does the application of heat or cold affect how quickly topical Лидокаин is absorbed?

A: Regulatory warnings caution against conditions that might increase the rate of absorption. While heat and cold are not explicitly listed, the guidance warns that anything that significantly increases skin temperature or moisture could potentially lead to increased systemic absorption of the drug and a higher risk of adverse effects.

Q: Are there specific body areas where the absorption of topical Лидокаин is greater?

A: Official dosing guidelines caution that application to skin areas with higher vascularity (meaning greater blood flow) can result in a higher rate of drug uptake. This increased systemic absorption is a risk that may require the use of lower doses in those areas.

Q: How is the risk of accidental ingestion of topical Лидокаин described?

A: Official warnings emphasize that all formulations must be stored out of the reach of children and pets to prevent accidental exposure. Used topical patches must be specially folded and disposed of to avoid access, as ingestion carries a serious risk of systemic toxicity.

Q: Has Лидокаин been studied for use in people with specific nerve conditions?

A: Yes, official regulatory indications are often based on research. The topical 5% patch is specifically indicated and supported by evidence for the relief of pain associated with a particular type of nerve condition called post-herpetic neuralgia.

Q: Are there specific sports or activities mentioned in warnings related to the use of Лидокаин?

A: Official labeling for certain injectable formulations notes the potential for an ingredient (such as sodium metabisulfite) to cause a false-positive result in drug tests. This is a point of consideration relevant to professional athletes and others subject to such testing.

Q: Do regulatory agencies issue special warnings about using Лидокаин near the eyes or mouth?

A: Yes. Official safety and administration instructions for topical forms of Лидокаин strongly advise users to avoid contact with the eyes. Caution is also required when applying the drug to the mouth or mucous membranes to minimize the risk of severe local irritation or increased systemic absorption.

Q: Are there common patterns of misuse of Лидокаин that official sources warn against?

A: Regulatory advisories warn consumers against several misuse patterns that increase risk. These include applying topical products to large areas of the body, using them on irritated or broken skin, or covering them with tight bandages or occlusion for longer than specified.

Q: Is the effectiveness of Лидокаин described as being reduced by any specific substances?

A: Official documents describe that the drug’s effectiveness is constrained by the local pH level of the tissue. If the area is acidic (such as in an area of infection or inflammation), a higher proportion of the molecule is inhibited, which can reduce its ability to work at the site of action.

Q: Does official guidance mention a required waiting time between topical applications?

A: Yes. For products like the 5% transdermal patch, the official guidance requires that the skin application site be given a 12-hour rest period (a drug-free interval) after the patch is removed and before a new patch is applied.

Q: What are the concerns about using Лидокаин on broken or damaged skin?

A: Regulatory documents explicitly advise users not to apply topical products to areas of broken, damaged, or irritated skin, or on burns. This is because application to compromised skin allows for rapid and increased systemic absorption, which significantly raises the risk of serious side effects and drug toxicity.

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How should Лидокаин be stored and disposed of?

Storage and Disposal of Lidocaine

Official regulatory guidelines define specific conditions for storing and disposing of Lidocaine formulations to maintain product stability and safety.

Storage Requirements

Most Lidocaine solutions and patches must be stored at Controlled Room Temperature, typically 20 C to 25 C (68 F to 77 F). The product must be protected from extreme heat, and injection solutions should not be frozen. Containers for viscous solutions must be kept tightly closed immediately after use.

Handling and Disposal

All Lidocaine products must be stored out of the reach of children and pets. For disposal, single-dose injection vials require that any unused portion be discarded immediately. Used topical patches must be folded so the adhesive side sticks to itself before being safely disposed of in a manner that prevents access by children and pets.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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