Lidocain

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Lidocain

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Medically reviewed

Marina Burgos

Last updated on 10/01/2026

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 Lidocain

What is Lidocaine?

Property Description
Active Ingredient Lidocaine Hydrochloride
Pharmacological Class Local Anesthetic; Antiarrhythmic (Class 1B)
Common Use Type Temporary Numbing and Pain Relief
Primary Forms Topical (cream, gel, patch), Injectable Solution
Origin Synthetic (Amino Amide)

Lidocaine is a powerful medication chemically classified as an amino amide, primarily used as a local anesthetic to numb specific areas of the body and as an antiarrhythmic agent to stabilize heart rhythms. It is the International Nonproprietary Name (INN) for the active pharmaceutical ingredient, meaning it is the globally recognized generic name.

Lidocaine is available in various pharmaceutical formulations, including sterile solutions for injection and several topical forms such as creams, gels, and transdermal patches. Its primary purpose is to temporarily block nerve signals in the area of application or injection, providing reliable relief from discomfort.


Pharmacological Class and Origin

Lidocaine belongs to the pharmacological class of local anesthetics and is specifically classified as a Class 1B antiarrhythmic agent. It was first synthesized in 1943 by Swedish chemist Nils Löfgren, making it a synthetic organic compound (a derivative of acetanilide).

This dual classification is clinically important. The compound's critical role in providing essential pain management and addressing specific cardiac issues has led to its inclusion on the World Health Organization's List of Essential Medicines.

As an amino amide, Lidocaine is metabolically distinct from older anesthetic types, which contributes to its proven safety and efficacy profile in routine medical settings.

What side effects are possible with Lidocain?

Possible Side Effects and Safety Information

Lidocaine’s official safety profile is primarily structured around the risk of systemic toxicity, as documented by regulatory bodies. Adverse reactions are generally considered dose-dependent, meaning they are a consequence of the concentration reaching the bloodstream, often due to excessive dosage or rapid absorption.

System-Organ Classes and Frequency

Regulatory documentation classifies potential effects by the physiological system impacted. When higher systemic levels are achieved, the most significant effects relate to the Central Nervous System (CNS) and the Cardiovascular System.

Classification System-Organ Class (SOC) Examples of Officially Listed Effects
Common Nervous System Disorders Dizziness, somnolence, headache
Common Cardiac Disorders Bradycardia, hypotension
Rare Immune System Disorders Hypersensitivity reactions, anaphylaxis

Serious Adverse Reactions and Safety Constraints

The label explicitly documents serious adverse reactions, which are often the result of high plasma concentrations. These include potential events such as convulsions/seizures, cardiac arrest, and severe hypotension. The risk of methemoglobinemia, a blood disorder, is also cited as a rare potential adverse reaction.

Certain safety considerations are outlined for specific patient groups. Individuals with severe hepatic (liver) impairment and older adults are cited in official labeling as groups that may have reduced clearance, which increases the potential for higher blood concentrations and systemic toxicity. Early neurological effects, such as lightheadedness or nervousness, are documented as potential warning signs associated with rising plasma concentrations.

Overdose and Emergency Response

Lidocaine overdose is officially documented to involve progressive systemic toxicity primarily affecting the Central Nervous System (CNS) and the Cardiovascular System (CVS). Initial signs of CNS toxicity may include light-headedness, confusion, tinnitus, tremors, and twitching, which can rapidly escalate to severe manifestations such as seizures, followed by profound CNS depression resulting in unconsciousness and respiratory arrest. The regulatory profile also details life-threatening cardiovascular depression, including bradycardia, severe hypotension, and serious ventricular arrhythmias, which may lead directly to cardiovascular collapse and cardiac arrest.

The official regulatory guidance mandates that immediate medical attention must be sought upon observing any symptom of systemic toxicity. This urgency is also required for signs of methemoglobinemia, a documented complication presenting as cyanosis (pale, gray, or blue-colored skin or lips), headache, or rapid heart rate. The treatment approach is defined as symptomatic and supportive care. Specific official management protocols require immediate availability of resuscitative equipment, securing the airway, administering oxygen, and utilizing specific agents such as Methylene Blue for methemoglobinemia. Furthermore, official labeling notes that elderly, acutely ill, and patients with severe hepatic disease are at increased risk of developing toxic plasma concentrations.

Therapeutic Uses of Lidocain

What Lidocaine Treats: Main Uses and Benefits

Lidocaine is primarily used to offer temporary symptomatic support across various clinical domains. The use of this medication is commonly applied across domains where additional symptomatic support is needed.

It is relevant in settings requiring short-term symptomatic assistance for conditions presenting with symptoms related to physical discomfort, irritation, and temporary functional strain. It provides support that helps ease the overall symptom burden during periods of heightened symptoms.


Key Therapeutic Domains

Lidocaine is utilized for managing symptom clusters that may become intense or disruptive, easing episodes of symptomatic discomfort, and supports the patient during difficult episodes by easing distress. The medication is relevant in conditions characterized by episodic or fluctuating manifestations.

This medication is commonly used to help with symptoms that interfere with daily functioning. It is applied in addressing symptoms related to inflammatory or irritative states, or symptoms associated with acute or episodic changes.


Quick Fact

Quick Fact: Relief for Localized Physical Discomfort – Lidocaine is considered relevant for easing symptoms related to localized physical discomfort, and may assist with maintaining functional stability when symptoms are more noticeable.

Regulatory References

  1. NIH MedlinePlus overview

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Lidocaine

The official regulatory profile for Lidocaine establishes strict eligibility rules based on patient health status and age. Absolute non-eligibility is determined by pre-existing conditions and known allergies.

Eligibility Status Applicable Population/Condition
Contraindicated Patients with known hypersensitivity to Lidocaine or any other amide-type local anesthetic must not use the medicine. Additionally, for antiarrhythmic purposes, it is contraindicated in patients with severe cardiac conduction disorders (e.g., severe heart block, WPW syndrome) who do not have a functional pacemaker.
Restricted Use/Caution Use requires caution and monitoring in patients with severe hepatic (liver) impairment or severe renal (kidney) disease due to the risk of drug accumulation and toxicity. Older adults and acutely ill patients must receive reduced, cautious doses commensurate with their physical status.
Age Limitations The oral viscous solution is not recommended by regulatory bodies for use in infants and young children, such as for teething pain. Infants under 6 months of age are officially listed as being more susceptible to methemoglobinemia.
Pregnancy/Lactation Pregnancy: Classified as Category B; its use is advised only if clearly needed and the benefit outweighs the risk. Lactation: Lidocaine is excreted into human milk in small amounts; caution is advised for nursing women, as stated in regulatory documents.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Lidocaine is subject to officially documented pharmacokinetic and pharmacodynamic interactions with several medicines, as detailed in regulatory labeling.


Interactions Affecting Lidocaine Exposure

Lidocaine is primarily metabolized by cytochrome P450 (CYP) enzymes, notably CYP1A2 and CYP3A4. Co-administration with strong inhibitors of these enzymes, such as fluvoxamine or itraconazole, reduces the clearance of Lidocaine. This reduction leads to increased systemic plasma concentrations (elevated AUC and C max) of Lidocaine and its active metabolite, potentially elevating the risk of toxicity. Medicines that decrease hepatic blood flow, such as cimetidine and propranolol, are also documented to reduce Lidocaine clearance.


Pharmacodynamic and Additive Effects

  • Additive Systemic Toxicity: The systemic toxic effects of Lidocaine are additive with other local anesthetics (e.g., bupivacaine) and Class I antiarrhythmics (e.g., mexiletine), necessitating careful attention to potential cardiotoxicity or neurotoxicity.
  • Methemoglobinemia Risk: Concurrent use with other oxidizing medicinal products and agents known to induce methemoglobinemia, such as certain nitrates/nitrites or dapsone, increases the established risk of methemoglobin formation.

Interaction-Related Administration Rules

  • Timing Restriction (Oral Forms): For oral or mucosal Lidocaine forms, labeling advises avoiding eating or chewing gum while the area is anesthetized to prevent accidental trauma.
  • Heat Restriction (Topical Patches): The application of external heat sources directly over topical Lidocaine patches is restricted, as it may result in increased systemic drug exposure.

Interaction classifications may vary by region; this information is based on official government documentation (FDA, EMA, NIH).

Mechanism of Action

Lidocaine functions as a use-dependent inhibitor that targets the intracellular pore of voltage-gated sodium channels ( Na v) found on excitable membranes, particularly those of peripheral sensory neurons. By stabilizing the channel in its open or inactivated state, the drug physically blocks the influx of Na^+ ions required to initiate membrane depolarization and action potential generation .

This molecular blockade results in the stabilization of the neuronal membrane, suppressing electrical signal conduction along nerve axons. The primary effect occurs in the peripheral nervous system, where the inhibition of action potential transmission along A-delta and C sensory fibers leads to the inhibition of sensory impulse transmission from the periphery toward the central nervous system. Due to its non-selective nature, the mechanism also extends to the cardiac conduction system, supporting the modulation of impulse conduction velocity in cardiomyocytes.

Dosage and Administration Information

Lidocaine is used through several routes depending on its intended application, including intravenous (IV) administration, parenteral injection for local and regional anesthesia, and topical/cutaneous application via patches or gels.

For acute management of ventricular arrhythmias, adult IV administration involves an initial bolus of 50 mg to 100 mg administered over 2 to 3 minutes. This may be followed by a continuous maintenance infusion typically ranging from 1 to 4 mg/minute, with a cumulative limit generally not exceeding 300 mg in one hour. IV use requires constant ECG monitoring during administration to guide flow rate adjustments and ensure proper use.

In local infiltration anesthesia, the total dose is restricted, generally not exceeding 4.5 mg/kg of body weight. For transdermal patches (e.g., 5% formulations), the usage pattern is cyclic: a maximum of three patches can be applied once daily, but they must be worn for no more than 12 hours, followed by a 12-hour patch-free interval.

Administration requires specific procedural precautions. For central neural blocks like epidural anesthesia, an initial test dose is mandated before the total volume is injected. Furthermore, guidelines specify reduced dosages for older adults, debilitated patients, and those with underlying cardiac or hepatic impairment, reflecting modifications necessary for populations with altered drug clearance.

Recent Clinical Evidence

Research evidence / Overview of studies for Lidocaine

Evidence for Local Anesthesia and Procedural Numbing

This section will summarize the structure of Randomized Controlled Trials (RCTs), controlled clinical studies, and meta-analyses that have evaluated the local anesthetic evaluation of both injectable and topical Lidocaine formulations for minor medical and dental procedures. The overview will cover what outcomes (such as pain perception and onset time) were measured and which healthy adult and pediatric populations were included in the research.

The research exploring the use of Lidocaine for local numbing involves numerous short-term RCTs where investigators measured outcomes related to physical discomfort during dental work or minor surgical procedures. Findings describe patterns observed in the studies indicating a measured change in pain perception and a specific duration of the measured change in anesthetic status in the observed populations. Research has explored the speed at which physiological changes in nerve conduction were observed following administration. Long-term effects are not fully established because the evidence mainly focused on this immediate, short-term observation period.

Evidence for Systemic Pain Management (Intravenous and Topical)

This block will detail the research base, including systematic reviews and controlled trials, that examined the use of intravenous Lidocaine infusions for post-surgical pain and topical patches for certain chronic pain conditions. It will focus on the variety of outcomes studied, such as functional recovery markers and the measurement of opioid consumption in these trials.

Studies monitored postoperative pain intensity and the amount of stronger pain medication was observed in the patient populations. However, the pooled findings from reviews have often been mixed or reported inconsistent findings across the different surgical types studied. Certainty remains low regarding the optimal amount of intravenous Lidocaine needed to consistently relate to measurements of postsurgical pain outcomes, as protocols varied significantly. Follow-up durations were limited in many key trials, providing limited information for long-term outcomes.

Evidence for Antiarrhythmic Use in Cardiac Conditions

Intravenous Lidocaine was evaluated in large, controlled trials and systematic reviews for use in adult patients experiencing out-of-hospital cardiac arrest (OHCA). Research examined survival to hospital discharge and whether the patient achieved a favorable neurological outcome upon discharge. Research describes patterns of survival outcomes in specific subgroups, such as those where the arrest was witnessed by a bystander. However, when examining the overall study population, data show patterns related to survival outcomes where the findings were often mixed, and the results lacked sufficient statistical certainty.

Key Studies & References

  1. Lidocaine Hydrochloride Injection USP (Antiarrhythmic and Anesthetic Indications)

Frequently Asked Questions (FAQ)

Common questions about Lidocain (FAQ)

Q: Is Lidocain the same thing as Novocain or marcaine?

A: Official sources classify Lidocaine as an amino amide local anesthetic. This is a chemical distinction that separates it from Novocain (Procaine), which is an ester-type anesthetic, and Marcaine (Bupivacaine), which is a different amide-type compound.

Q: Can children use Lidocain products, and is there a different dosage rule for them?

A: Official documentation advises that, when administering the drug, children should generally be given reduced dosages appropriate for their age and overall physical condition. This approach is generally used to accommodate potential differences in how children process the drug.

Q: Is Lidocain safe to use during pregnancy or while breastfeeding?

A: The drug is classified by regulatory authorities as Pregnancy Category B. This classification means that while animal studies have not shown harm to the fetus, controlled studies in pregnant women are lacking. Regulatory documents indicate that its use during pregnancy is considered appropriate only when the clinical need has been clearly established.

Q: Can applying heat or ice affect how Lidocain works on the skin?

A: Official product labeling includes restrictions against the application of external heat sources over a topical patch due to the risk of increased systemic absorption. Patient instructions for some formulations also advise against exposing the treated, numb area to hot or cold temperatures to prevent accidental injury.

Q: Can Lidocain be used on broken skin or open wounds?

A: Regulatory documents advise against applying certain topical formulations to skin that is cut, scratched, or significantly red. The presence of existing infections or open wounds in the application area is noted as a situation where use must proceed with caution.

Q: Does being older or having a lower body weight affect how Lidocain works?

A: Official labeling indicates that reduced dosages are generally necessary for older adults and acutely ill patients. This is due to the potential for reduced drug clearance, which can lead to higher systemic plasma concentrations and an increased risk of toxicity.

Q: How quickly does Lidocain start working when used for pain relief?

A: The time to onset varies by the form used. Following an intravenous bolus injection, the onset of action is described as rapid in official documents. For certain topical patches, the numbing effects are typically described as starting within 30 minutes of application.

Q: How long do the numbing effects of Lidocain usually last?

A: The duration of effect depends on the route of administration. For intravenous antiarrhythmic use, the effect following a single bolus is described in official documents as lasting approximately 15 to 20 minutes.

Q: Can Lidocain be used for long-term chronic pain, or just for short procedures?

A: Official documents describe certain topical formulations, such as the 5% patch, as approved by the FDA for the treatment of specific chronic conditions. Specifically, it is indicated for the management of pain associated with post-herpetic neuralgia (PHN), which is a long-term nerve pain condition.

Q: Why do doctors sometimes mix Lidocain with epinephrine (adrenaline)?

A: Lidocaine solutions used for injection are often combined with epinephrine (also known as adrenaline). This combination is used to prolong the duration of the numbing effect and to help reduce the rate of systemic absorption of Lidocaine from the site of injection.

Q: Can Lidocain cause a tingling or buzzing feeling before it goes numb?

A: Official documentation lists tingling or itching at the application site as a common side effect of topical use. In certain situations, tingling around the mouth (known as perioral paresthesia) is cited as an early sign that the drug's concentration in the bloodstream may be rising too high.

Q: What is the risk of having an allergic reaction to Lidocain?

A: The drug is contraindicated in anyone with a known history of hypersensitivity or allergy to Lidocaine or other similar amide-type anesthetics. While serious allergic reactions, like anaphylaxis, are cited in documentation, they are described as extremely rare events.

Q: Does using too much Lidocain at once increase the risk of side effects?

A: Regulatory documents indicate that the potential for adverse reactions is generally dose-dependent, meaning it correlates with the amount of drug that enters the bloodstream. Therefore, using excessive amounts increases the potential for higher systemic plasma concentrations and the related risk of toxicity.

Q: What are the signs that too much Lidocain has been absorbed into the body?

A: Early neurological signs associated with rising systemic concentrations may include dizziness, lightheadedness, nervousness, or tingling around the mouth. The more severe effects listed in official documents, which occur at very high concentrations, include convulsions/seizures, severe hypotension, and cardiac arrest.

Q: Does Lidocain show up on drug tests?

A: Scientific research has demonstrated that Lidocaine and its primary metabolite can be detected in plasma and urine following its administration. This detection is part of pharmacokinetic studies that examine how the body processes the drug.

Q: Are there certain skin conditions that make using Lidocain less appropriate?

A: Official documents note that the presence of existing skin infections or open wounds in the area of administration is a situation where caution is recommended.

Q: Is there any research on using Lidocain for chronic headaches or migraines?

A: Research has examined the use of Lidocaine for various types of chronic pain. While research has examined its use for chronic pain conditions, some specific applications, such as infusions for chronic headaches or migraines, are described in research documents as investigational.

Q: Can Lidocain affect my ability to drive or operate machinery?

A: Official patient information advises caution regarding driving or operating machinery. This is because the drug may cause effects such as drowsiness or dizziness, which have the potential to slow a person’s reflexes.

Q: Is it possible to become 'resistant' or tolerant to the effects of Lidocain over time?

A: Official prescribing information indicates that tolerance to elevated blood levels of the drug can develop. The degree of tolerance that may be observed is noted to vary depending on the patient’s overall physical status.

Q: Do official sources describe any specific instructions for removing Lidocain patches safely?

A: Official patient instructions advise specific steps for safe removal. These include avoiding contact with the sticky side, folding the used patch in half, placing it back in the original pouch, and washing hands immediately after handling.

Q: Are there any studies examining the use of Lidocain for pain after shingles (postherpetic neuralgia)?

A: Studies, including controlled trials, have examined the use of the 5% topical patch for pain relief. This research supported the FDA approval of this formulation specifically for use in treating pain associated with post-herpetic neuralgia (PHN), a complication of shingles.

Q: What is the risk of accidental exposure to pets or small children?

A: Official patient safety warnings strictly advise keeping the medication out of reach of children and pets. The warnings explicitly state that a new or used patch, if chewed or eaten, may cause harm to children or pets due to the concentrated drug content.

Q: Can Lidocain be used on sensitive areas like the face or mucous membranes?

A: Official formulations are available that are specifically indicated for use on certain sensitive areas, including the mucous membranes of the mouth and throat, to provide topical anesthesia.

Q: Is Lidocain a controlled substance or habit-forming?

A: Regulatory authorities do not classify Lidocaine as a controlled substance.

Q: Do official documents mention any potential interactions with alcohol?

A: Official patient information for Lidocaine injections includes warnings related to the use of alcohol during administration. This is because the combination may cause a drop in blood pressure, which can lead to feelings of dizziness and fainting.

Q: Are there reported cases of Lidocain-related systemic toxicity and what does that mean?

A: Systemic toxicity is a term used in regulatory documents to describe a rare but serious condition. It occurs when the concentration of the drug absorbed into the bloodstream is too high, potentially affecting the central nervous system (e.g., brain) and the cardiovascular system (e.g., heart).

Q: Can Lidocain be used before getting a vaccination or blood test?

A: Some topical formulations are indicated in official documents for use in providing local anesthesia prior to minor medical procedures. This includes numbing the skin before procedures such as venipuncture (blood tests).

Q: What does it mean if a product has Lidocain HCL versus just Lidocain?

A: Lidocaine HCl (hydrochloride) is a chemical salt form that is water-soluble and is often used in injectable solutions. Lidocaine (free base) is the non-ionized form, which is used in certain topical applications.

Q: Is it safe to exercise or sweat heavily while using a Lidocain patch?

A: Official administration instructions for certain patches advise avoiding activities like bathing or swimming due to the risk of poor adhesion or increased absorption. This suggests that activities causing heavy sweating may also be a limiting factor in patch use.

Q: Can Lidocain interfere with certain laboratory test results?

A: Official labeling for the drug may include information regarding interference with laboratory tests. It is generally noted that some metabolites of the drug may interfere with the results of certain diagnostic assays.

Q: What is the difference between a prescription Lidocain product and an over-the-counter one?

A: The difference is primarily based on concentration and regulatory classification. Prescription products are available in higher concentrations (e.g., 5%) for specific chronic conditions, while over-the-counter products are available in lower concentrations (e.g., 4%) for temporary minor pain relief.

How should Lidocain be stored and disposed of?

How to Store and Dispose of Lidocain?

Lidocaine preparations must be stored in a cool, dry place, away from excessive heat and moisture, and kept out of the reach of children and pets. Always check the specific temperature requirements on the product's packaging or patient information leaflet.

Proper disposal of unused or expired lidocaine is critical to prevent accidental ingestion and environmental contamination. The best disposal method is utilizing a community-based drug take-back program or a medication disposal kiosk, often found at pharmacies or police stations.

If a take-back option is unavailable, most non-injectable lidocaine forms (e.g., creams, patches) can be disposed of in the household trash. First, mix the medication (do not crush tablets) with an undesirable, inedible substance like used coffee grounds or cat litter, then place the mixture in a sealed plastic bag or container before discarding. Always remove or scratch out personal information on the prescription label before discarding empty packaging.

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

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