Lidocaina

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Medically reviewed

Marina Burgos

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.

Overview of Lidocaina

Quick Facts

Property Description
Active ingredient Lidocaine Hydrochloride (Lignocaine)
Form Injection Solution, Topical Preparations (e.g., gel, patch)
Pharmacological Class Local Anesthetic, Class IB Antiarrhythmic
General Purpose Creates temporary, localized absence of sensation
Origin Synthetic, Amide-type Compound

What is Lidocaina and Its Pharmacological Classification?

Lidocaina, formally known as the active ingredient Lidocaine Hydrochloride or synonymously as Lignocaine, is a highly recognized synthetic compound. It is classified primarily as a Local Anesthetic agent and secondarily as a Class IB Antiarrhythmic agent, a dual role clinically recognized for its broad applicability in medicine. Lidocaina belongs to the amide-type family of local anesthetics, which distinguishes it chemically and metabolically from older ester-type compounds. Lidocaine's amide structure contributes to its stability and mechanism of action.

The drug’s general utility is founded on its core mechanism as a voltage-gated sodium channel blocker. This action involves stabilizing the neuronal membrane to inhibit the flow of electrical current, thereby preventing nerve cells from transmitting signals. Due to this critical function, Lidocaina is included on the List of Essential Medicines. Inclusion on this list confirms that this medicine is considered necessary for a basic healthcare system.

Forms, Composition, and General Utility

Lidocaine Hydrochloride is typically manufactured as a single-component product and is highly versatile, available in diverse dosage form(s). These include a sterile injection solution intended for parenteral delivery into tissues, utilizing an aqueous vehicle, and various topical preparations such as gels, patches, and sprays, which incorporate hydrophilic/lipophilic bases for surface application. This broad range allows for targeted use in scenarios such as minor superficial medical procedures.

This range of preparation ensures its relevance across numerous medical contexts. The general purpose of the medicine is to provide reliable, localized numbness or to suppress irregular electrical disturbances within the heart muscle, achieved through the same fundamental mechanism of signal interruption. The form chosen—either injection or topical—depends on whether the intended effect is deep-tissue blockade or superficial skin sensation relief.

Regulatory References

  1. Lidocaine - StatPearls - NCBI Bookshelf (NIH)
  2. Amide Local Anesthetics - LiverTox - NIH/NLM
  3. Lidocaine on the WHO eEML

What side effects are possible with Lidocaina?

Possible Side Effects and Safety Information

The official safety profile of Lidocaine is determined by government regulatory bodies and primarily addresses the risks associated with systemic exposure, regardless of the route of administration (injection or topical). Adverse reactions are generally dose-related and classified based on their frequency and the system-organ class affected, according to standards set by authorities like the FDA and EMA.


Systemic Adverse Reactions and Frequency

The most significant safety concerns involve the Nervous System Disorders and Cardiac Disorders.

Classification Examples of Officially Listed Adverse Reactions
Common Dizziness, paraesthesia, nausea, vomiting, hypotension, and reactions at the application site.
Uncommon Confusion and tremor, which are signs of Central Nervous System toxicity.
Rare Serious systemic events including seizures (convulsions), cardiac arrest, cardiac arrhythmias, and anaphylactic reactions.

Serious adverse reactions, such as Cardiac Arrest and Seizures, are explicitly documented, emphasizing that their occurrence is primarily linked to high plasma concentrations caused by excessive dosage or rapid systemic absorption.


Population-Specific Safety Notes

The regulatory labeling includes specific safety considerations for certain patient groups. Individuals with severe hepatic impairment are noted to be at a greater risk of developing toxic concentrations, as the liver metabolizes the drug. Furthermore, older adults may exhibit altered tolerance to elevated drug levels, and use in this population warrants attention to the potential for increased systemic adverse effects.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Lidocaine Hydrochloride documents dose-related systemic toxicity, primarily known as Local Anesthetic Systemic Toxicity (LAST), which affects the Central Nervous System (CNS) and Cardiovascular System (CVS).


Documented Manifestations

Initial CNS symptoms often include a metallic taste, tinnitus (ringing in the ears), lightheadedness, and confusion. These can rapidly progress to muscle twitching and generalized convulsions (seizures), with severe cases leading to unconsciousness and respiratory arrest. Cardiovascular manifestations are typically depressant, involving bradycardia, hypotension, and potentially life-threatening cardiac arrest or cardiovascular collapse. A serious complication documented in some labeling is Methemoglobinemia, characterized by pale, gray, or blue-colored skin.


Emergency Actions Required

Regulatory guidance strongly advises to seek immediate medical attention for any signs of systemic toxicity or Methemoglobinemia. A delay in proper management of dose-related toxicity may lead to acidosis, cardiac arrest, and death. Treatment is symptomatic and supportive, as no specific antidote is known for the core systemic toxicity. Management involves ensuring adequate oxygenation, treating seizures (e.g., with benzodiazepines), and potentially using Intravenous Lipid Emulsion (ILE) therapy. Caution and dose adjustment are noted for elderly, acutely ill, and patients with hepatic dysfunction.

Therapeutic Uses of Lidocaina

What Lidocaina Treats: Main Uses and Benefits

Lidocaine is commonly used to provide supportive relief across two primary therapeutic domains: local symptomatic pain management and support for cardiac rhythm stabilization. The medication helps address symptom clusters that may become intense or disruptive during acute episodes. It is applied in clinical settings that involve acute or unstable symptom patterns, ranging from managing acute pain for medical and dental procedures to management of ventricular tachyarrhythmias in acute settings.

It is relevant for conditions presenting with both localized physical discomfort and heightened physiological activity. The general use of Lidocaine contributes to easing the overall symptom load, supporting a more manageable experience during necessary care. Beyond procedural numbing, topical forms may be part of symptomatic management for specific neuropathic conditions like postherpetic neuralgia and symptoms related to inflammatory or irritative states like minor burns.


Quick Fact: Symptomatic Relief Domains
Symptom Type Acute localized pain, procedural discomfort, chronic nerve pain, and rapid ventricular heart rhythms.
Benefit Temporary absence of sensation and maintenance of functional cardiac stability.
Scenario Minor medical interventions, topical skin irritation, and critical emergency care.

Regulatory References

  1. NIH MedlinePlus Drug Information on Lidocaine

Eligibility and Restrictions for Use

Who Can and Cannot Use Lidocaina?

The population eligibility for Lidocaine is determined by official regulatory documents, defining groups who must not use the medicine and those who require conditional use.

Contraindicated Populations

Use of Lidocaine is contraindicated for patients with a known history of hypersensitivity to amide-type local anesthetics (Lidocaine's class). For antiarrhythmic use, it is also contraindicated in patients with severe degrees of heart block (sinoatrial, AV, or intraventricular) unless a functional pacemaker is present, or in those with Wolff-Parkinson-White syndrome.

Condition-Based Restrictions

Eligibility is restricted for individuals with certain physiological conditions, requiring cautious use and potential dose reduction. These include patients with severe hepatic (liver) disease, as this can significantly prolong the drug’s half-life and lead to toxic accumulation. Caution is also advised for those with severe renal (kidney) impairment and impaired cardiovascular function (e.g., severe congestive heart failure) .

Age-Group and Special Considerations

Pediatric patients, particularly infants under 6 months, are more susceptible to certain adverse effects and require lower doses commensurate with their status. Use of oral viscous Lidocaine for infant teething pain is generally not recommended by regulatory bodies. Older adults also often require reduced dosing due to physiological changes affecting drug elimination. Regarding pregnancy, Lidocaine crosses the placenta and is used only when benefit outweighs risk. It is excreted into human milk, but effects on the breastfed infant are not anticipated at therapeutic doses.

What should I know about interactions with other medicines?

The official interaction profile for Lidocaina is categorized into domains of altered systemic exposure and compounded pharmacodynamic effects, based strictly on regulatory documents.

Official Interaction Statements

  • Exposure Modification: Co-administration with agents that inhibit hepatic metabolism, such as Cimetidine and Beta-adrenoceptor blockers (e.g., Propranolol), reduces the plasma clearance of intravenous Lidocaina, leading to potential drug accumulation. Inhibitors of CYP1A2 and CYP3A4 (e.g., Fluvoxamine) can accelerate plasma concentrations by reducing metabolism.
  • Pharmacodynamic Synergy: The combined use of Lidocaina with other local anesthetics or certain antiarrhythmic drugs (e.g., Amiodarone) carries a risk of additive systemic toxic effects on cardiac and nervous systems. Co-administration with Oxidizing Agents increases the documented risk of methemoglobinemia.
  • Formulation Constraints: Formulations containing Epinephrine are associated with severe, persistent hypertension when combined with Monoamine Oxidase Inhibitors or Tricyclic Antidepressants. The injectable solution is also physically incompatible and must not be mixed with alkaline solutions, including sodium bicarbonate.
  • External Factors: Regulatory documents advise that external heat sources (e.g., heating pads) applied to topical systems may increase systemic drug exposure.

Population-Specific Notes

Severe Hepatic Dysfunction and Impaired Renal Function are conditions officially noted to affect the drug's elimination, increasing the risk of toxic accumulation of the medicine or its metabolites. Topical systems must not be worn for more than 12 hours within a 24-hour period.

Mechanism of Action

Lidocaine’s mechanism is defined by its ability to modulate electrical signal transmission in specific excitable tissues, primarily through two interconnected domains that influence its rate and extent of activity.


Inhibiting Electrical Signals at the Source

The core mechanism involves the direct, reversible blockade of voltage-gated sodium channels ( Na v channels), the transmembrane proteins responsible for initiating the rapid electrical impulse (action potential) in nerve and cardiac cells. By physically obstructing the channel pore from the cell’s interior, the drug prevents the influx of positive sodium ions ( Na^+). This molecular action stabilizes the cell membrane, preventing it from reaching the necessary voltage threshold and thus halting the propagation of electrical signals along the nerve axon or within the heart muscle.

Use-Dependence and Reduced Impulse Frequency

Lidocaine displays a key characteristic called use-dependence, meaning its inhibitory effect is strengthened when it interacts with channels that are already rapidly cycling (open or inactivated states). This mechanism allows the drug to preferentially target channels in highly active tissues, such as nerves carrying rapid signals or cardiac tissue experiencing frequent, rapid firing. The resulting physiological effect is a selective dampening of hyperexcitable electrical activity, leading to reduction of impulse frequency in the affected pathways.


Mechanistic Role of Local Chemistry

The speed and strength of the mechanism are intrinsically linked to the chemical environment, as the drug must first be in its non-ionized (uncharged) form to penetrate the nerve cell membrane. Because this chemical equilibrium is sensitive to local acidity, environments with low pH (such as localized acidic environments) reduce the available penetrating form, which consequently reduces the number of available penetrating molecules and delays the onset of signal inhibition.

Dosage and Administration Information

How to use Lidocaine: Official Administration Guidelines

Lidocaine is administered via multiple routes, including topical application (patches, ointments, solutions) and parenteral injection (infiltration, nerve block, intravenous). Adherence to product-specific directions and the principle of using the lowest dosage to achieve the desired effect is mandatory to prevent high plasma concentrations and systemic toxicity.


Official Dosing and Administration

Route of Administration Dosing Rules (Strict) Special Instructions/Timing
Topical Patch (e.g., 5%) Apply up to three patches. Do not wear for more than 12 hours within a 24-hour period. Apply only to intact skin. Do not apply external heat sources to the patch.
Topical Ointment (e.g., 5%) Single application should not exceed 5 grams. Total daily dose should not exceed approximately 17–20 grams. Avoid application to broken or inflamed skin. Wash hands immediately after use.
Topical Oral/Mucosal Solution Shake well before use. Use a calibrated measuring device. Dose and frequency must be strictly adhered to. Do not ingest food or chewing gum for 60 minutes following use in the mouth or throat area.
Parenteral Injection The lowest concentration and smallest effective dose must be given. Maximum doses vary by site and technique (e.g., typically less than or equal to 4.5 mg/kg without a vasoconstrictor in healthy adults). Aspiration must be performed before and during injection to avoid intravascular administration.

Age-Specific and Procedural Requirements

Age-Group Rules: Reduced doses are required for children, elderly patients, and acutely ill or debilitated individuals, scaled commensurate with their age, body weight, and physical condition. For oral topical solution, use in patients less than 3 years of age is limited to situations where safer alternatives are unavailable or have failed.

Missed Dose: For formulations used as needed (e.g., most topical solutions, injections), follow the clinician's direction. For products used on a regular schedule (e.g., patches), if a dose is missed, apply it as soon as remembered, unless it is nearly time for the next dose; then skip the missed dose. Do not apply a double dose.

Procedural Steps: For injectable forms, resuscitative equipment must be immediately available. Proper injection technique is essential; for epidural anesthesia, a test dose should be administered and the patient monitored before proceeding with the full dose.


This instruction set provides the essential regulatory framework for Lidocaine administration, emphasizing strict adherence to dose limits and specific procedural steps for each route of use. The primary goal across all protocols is dose control to minimize systemic absorption and toxicity, a critical focus for both topical and parenteral applications.

Recent Clinical Evidence

Evidence for Use in Local and Regional Anesthesia

Scientific research for creating temporary, localized loss of feeling is extensive, consisting of large Randomized Controlled Trials (RCTs) and meta-analyses. These studies measure pain perception and the degree of numbing achieved. The evidence base has been summarized in official regulatory documentation. Findings describe the development of sensory and motor nerve blockade and patterns linked to different measured pain perception. Research focuses overwhelmingly on short-term outcomes limited to the duration of the procedure.


Evidence for Use in Treating Acute Ventricular Arrhythmias

Research for rapid heart rhythm patterns involves Randomized Trials in critical care settings, examining outcomes related to stabilizing heart rhythm and overall patient mortality. Trials reported observations related to the agent's administration and the pattern of rapid ventricular rhythms. However, meta-analyses reported findings that were mixed regarding its relationship with short-term mortality, which remains a key area of uncertainty.


Evidence for Use in Postoperative Pain Management

Research has explored intravenous Lidocaina as an adjunctive therapy for outcomes related to pain during surgical recovery, using RCTs and systematic reviews. Studies report patterns associated with different measurements of pain scores and different patterns of opioid consumption. The evidence base is heterogeneous across different procedures. Data on long-term outcomes, such as those related to Chronic Post-Surgical Pain (CPSP), are still emerging and require confirmation from dedicated trials.


Evidence for Use in Chronic Neuropathic Pain

The topical patch form has been studied for outcomes related to chronic nerve pain, primarily in patients with Postherpetic Neuralgia (PHN). Trials measured changes in patient-reported pain intensity. Review literature indicates the evidence is described as generally Moderate, but many trials are cited as being small in sample size or having limitations that pose a risk of bias.


Overall Evidence Gaps and Limitations

The majority of research was conducted in general adult populations, meaning data for certain groups remain insufficient, particularly children or specific co-morbidity defined groups. Research exploring long-term effects remains limited, requiring confirmation from ongoing large-scale studies.

Frequently Asked Questions (FAQ)

Common questions about Lidocaina (FAQ)

Q: Does Lidocaina work for nerve pain or only surface pain?

A: Official information indicates that Lidocaina is approved for use in local and regional anesthesia, which involves numbing surface and deeper tissues. Furthermore, the topical patch form is specifically studied and indicated for relieving the pain associated with Postherpetic Neuralgia (PHN), which is a type of chronic nerve pain.

Q: Is it possible to become resistant to Lidocaina's effects over time?

A: Official pharmacological documents describe Lidocaina's 'use-dependence' property, meaning its effect is greater in nerves that are rapidly firing. However, regulatory documents do not provide an explicit statement or warning regarding the risk of developing resistance or tolerance from long-term, chronic use.

Q: How long does the numbing effect of Lidocaina typically last?

A: The duration of the numbing effect can vary significantly depending on the product form and where it is applied. For example, for the topical patch, official administration guidelines state that the patch can be worn for up to 12 hours before it must be removed.

Q: Are there any common over-the-counter medicines that shouldn't be mixed with Lidocaina?

A: Official labels warn about interactions with certain prescription medications, such as some antiarrhythmics or stomach medications like Cimetidine, which can affect how the body processes Lidocaina. Patients are generally advised to consult official labeling regarding the combination of Lidocaina with other topical pain relievers, particularly those containing similar anesthetic ingredients.

Q: Can children use Lidocaina products, and is it dosed differently?

A: Yes, but regulatory guidance specifies that doses should be reduced and carefully considered for children based on their age and weight. Use of the oral topical solution in children under 3 years old is highly restricted and generally limited to situations where safer alternatives are not available or have failed.

Q: Can using Lidocaina for a long time lead to skin sensitivity?

A: The official safety profile lists reactions at the application site, such as irritation, itching, or redness, as common side effects. However, regulatory documents do not specify whether these effects lead to permanent or cumulative long-term skin sensitivity.

Q: What happens if I accidentally swallow a small amount of topical Lidocaina?

A: Topical Lidocaina products are strictly for external use. Accidental ingestion carries a significant risk of severe side effects due to rapid absorption into the bloodstream. If accidental ingestion of a topical product occurs, individuals should contact emergency services or a poison control center immediately, as this can lead to serious systemic adverse effects.

Q: Is a slight redness on the skin after patch removal a common side effect of Lidocaina?

A: Yes, official clinical trial data for the topical patch form lists erythema (redness) and other application site reactions as common and expected side effects.

Q: Is Lidocaina safe for use in older adults, or are there special precautions?

A: Official guidelines permit use in older adults, but they mandate special precautions. Doses must often be reduced due to physiological changes that can affect the body's ability to eliminate the drug and an altered tolerance to elevated levels in the bloodstream.

Q: What are the signs that I'm using too much Lidocaina topical product?

A: The most serious signs of using too much Lidocaina are related to high absorption into the body. Early signs of potential toxicity listed in regulatory documents include confusion, lightheadedness, tremors, nervousness, a metallic taste, or ringing in the ears. If any signs of systemic toxicity are suspected, immediate contact with a healthcare provider is advised.

Q: Is Lidocaina the same as Novocaine or similar older numbing agents?

A: No. Official classification states that Lidocaina is an 'amide-type' local anesthetic. Older numbing agents like Novocaine (procaine) belong to the 'ester-type' class, which is chemically and metabolically different.

Q: Does the absorption of Lidocaina vary depending on the area of the body?

A: Yes, official pharmacokinetic data confirms that the rate and extent of systemic absorption depend heavily on the site of application. Absorption is typically fastest following application to mucous membranes.

Q: Why is Lidocaina sometimes listed with epinephrine or other ingredients?

A: In injectable forms, Epinephrine (a vasoconstrictor) is often added to the Lidocaina solution. Its purpose is to constrict blood vessels at the injection site, which helps to keep the anesthetic localized for a longer duration and prolong the numbing effect.

Q: What is the shelf life of an open tube of Lidocaina cream?

A: Specific regulatory shelf-life information for an opened tube is not consistently standardized across all products. It is recommended that patients check the manufacturer's directions on the package or consult with a healthcare professional regarding the safe lifespan of the product once it has been opened.

Q: Do cold or hot temperatures affect how well Lidocaina works?

A: The drug must be stored at controlled room temperature, and freezing is not recommended. Regulatory documents specifically warn against applying external heat sources (like heating pads) to the application site, as this can dangerously increase the rate and amount of drug absorbed into the body.

Q: Is it true that Lidocaina can be used for things other than just pain relief?

A: Yes. While it is primarily classified as a local anesthetic for pain relief, official therapeutic indications also include its use as a Class IB Antiarrhythmic agent to help stabilize certain rapid heart rhythms.

Q: Are allergic reactions to Lidocaina rare or relatively common?

A: Severe systemic allergic reactions, such as anaphylaxis, are listed in official documents as a rare event. However, hypersensitivity (allergy) to amide-type anesthetics is considered a direct contraindication, meaning anyone with a known allergy should not use the drug.

Q: What steps should be taken if a pet accidentally licks a Lidocaina product?

A: All forms of the drug must be stored safely out of the reach of pets and children. If a pet is exposed to or licks a Lidocaina product, immediate veterinary attention or contact with a pet poison control center is necessary due to the risk of serious toxicity.

Q: How important is it to wash your hands thoroughly after applying Lidocaina cream?

A: Washing your hands immediately and thoroughly after application is required by official administration guidelines. This is a crucial safety step to prevent accidental transfer of the medicine to sensitive areas like your eyes, mouth, or other unintended skin areas.

Q: Why do dentists use Lidocaina injections so frequently?

A: Official indications confirm that the injectable form of Lidocaina is specifically approved for use in local and regional dental anesthesia. It is a highly effective nerve block agent used to create temporary, localized numbness before and during dental procedures.

Q: Does the body metabolize Lidocaina quickly or slowly?

A: According to pharmacokinetic data, the drug is metabolized, or broken down, relatively rapidly by the liver. This is why official warnings note that individuals with severe liver impairment are at a greater risk of the drug and its metabolites accumulating to toxic levels.

Q: Can I use a Lidocaina product on my face or sensitive skin areas?

A: Topical products should not be applied to broken, infected, or inflamed skin due to increased absorption risks. For mucosal areas (like the inside of the mouth), specific oral solution or gel formulations are available and must be used under strict administration rules.

Q: What are common misuses of topical Lidocaina products?

A: Regulatory warnings highlight several misuses that can lead to toxicity. These include applying the product over very large areas of the skin, applying it to broken or newly irritated skin, and covering the application area with plastic wrap or external heat sources.

Q: Is it generally safe to use Lidocaina if I have high blood pressure?

A: Regulatory documents advise caution for patients with impaired heart function. For injectable forms containing epinephrine, specific warnings are given regarding use in patients with severe, uncontrolled hypertension (high blood pressure) due to the risk of a severe hypertensive episode.

Q: Can Lidocaina affect the results of certain medical tests or procedures?

A: There has been historical concern regarding the drug’s metabolites potentially causing false-positive results on certain urine drug screens. However, current official literature suggests that the likelihood of this interference occurring with modern, standard testing methods is extremely low.

Q: Can you use Lidocaina cream on a fresh tattoo or piercing?

A: No. Regulatory agencies strongly warn against applying topical Lidocaine to any broken, irritated, or newly compromised skin. Using it on a fresh tattoo or piercing significantly increases the risk of excessive absorption into the bloodstream and severe side effects.

Q: Do people typically experience side effects like dizziness or lightheadedness from topical Lidocaina?

A: Yes, dizziness and lightheadedness are listed as common adverse reactions linked to systemic toxicity. Although topical use is generally safer than injection, these effects may still occur if the drug is overused or absorbed excessively through damaged skin.

Q: Is there research on Lidocaina's effectiveness for muscle spasms or just localized pain?

A: Official indications and core evidence summaries focus primarily on its use for localized pain, nerve pain (PHN), and antiarrhythmic purposes. Effectiveness for treating muscle spasms as an approved or well-supported indication is not included in the core regulatory documents.

How should Lidocaina be stored and disposed of?

Storage and Disposal Requirements

Official labeling mandates that Lidocaine products be stored at controlled room temperature, typically 20 C to 25 C. Storage must provide protection from light, and the product must not be frozen to maintain stability. Injection solutions must be visually inspected before use, and any single-dose, preservative-free solution must be discarded immediately after initial entry.

All forms of Lidocaine must be stored out of the sight and reach of children and pets. Due to the high risk of accidental exposure, used topical patches must be immediately folded in half (adhesive sides together) and securely discarded. Unused or expired Lidocaine should be disposed of in accordance with local regulatory guidelines or a drug take-back program.

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

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