Xylocaina

Quick links to important sections

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 Xylocaina

Quick Facts

Property Description
Active Ingredient Lidocaine Hydrochloride
Pharmacological Class Local Anesthetic; Class Ib Antiarrhythmic
Key Forms Sterile Injection Solution, Topical Gel/Jelly, Ointment, Spray
Origin Type Synthetic (Amino Amide)
General Purpose To create temporary, localized numbness and stabilize specific heart rhythms

What Type of Medicine is Xylocaina? (Identity and Classification)

Xylocaina is the trade name for a medicinal product whose core active component is Lidocaine Hydrochloride, a potent, dual-action synthetic compound. It is fundamentally classified as a Local Anesthetic, but its molecular properties also establish it as a Class Ib Antiarrhythmic Agent. Lidocaine is an amino amide-type compound, a synthetic origin that defines its stability and its metabolism, which occurs primarily through the liver. This agent functions by interrupting pain transmission pathways and is a standard component in pharmacological practice worldwide.

Forms, Variations, and High-Level Composition

The active component, Lidocaine Hydrochloride, is formulated into multiple pharmaceutical preparations to enable either parenteral (injection) or topical administration, including a sterile aqueous solution, viscous solution, jelly, and ointment. Injectable forms are typically composed of the active ingredient dissolved in a sterile, nonpyrogenic aqueous solution. Lidocaine's chemical structure facilitates a rapid onset of action when delivered into local tissues. Additionally, it is often prepared as a combination product with a vasoconstrictor like Epinephrine, which prolongs the local numbing effect, a key differentiation for various procedures.

General Purpose and Function

The essential function of Xylocaina is derived from its ability to act as a reversible sodium channel blocker, preventing nerve impulses from transmitting electrical signals. This action provides effective prevention and relief from localized pain by creating temporary, reversible loss of sensation in a targeted area. Furthermore, intravenous Lidocaine is utilized to suppress certain abnormal electrical impulses in the heart, serving as a secondary function in managing acute cardiac instability.

Regulatory References

  1. WHO Model List of Essential Medicines

What side effects are possible with Xylocaina?

Possible Side Effects and Safety Information

The safety characteristics of Xylocaina (Lidocaine) are comprehensively documented across official regulatory labels, classifying potential adverse events primarily by frequency and the physiological system affected.

Systemic adverse reactions are chiefly a concern when high plasma concentrations are reached, which can occur due to excessive dosing or rapid absorption. The central safety focus in regulatory documentation involves the Nervous System and the Cardiovascular System.

System-Organ Class Common Side Effects (Official Classification) Serious Adverse Reactions (Label-Documented)
Nervous System Dizziness, Drowsiness, Nausea, Vomiting Convulsions/Seizures, Respiratory Arrest
Cardiovascular System Hypotension (low blood pressure), Bradycardia (slow heart rate) Cardiac Arrest, Cardiovascular Collapse

Official prescribing information classifies certain neurological signs, such as tremor or tinnitus, as Uncommon, while serious, potentially life-threatening events like Anaphylaxis (Hypersensitivity) and Cardiac Arrest are generally classified as Rare. The progression of systemic toxicity is a key safety pattern: excitatory CNS manifestations, such as lightheadedness, are officially documented to often precede signs of cardiovascular depression.

Specific Population-Specific Safety Considerations are detailed for individuals with compromised clearance mechanisms. Regulatory guidelines recommend caution and potential dose adjustments for Older Adults and patients with documented Hepatic or Renal Impairment due to the potential for reduced clearance and drug accumulation.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory profile for Xylocaina (Lidocaine Hydrochloride) overdose describes a progression of systemic toxicity affecting the Central Nervous System (CNS) and Cardiovascular System (CVS).

Documented Overdose Manifestations

System Documented Signs/Outcomes
Early CNS Restlessness, dizziness, tinnitus, blurred vision, circumoral paraesthesia.
Severe CNS Seizures, loss of consciousness, respiratory arrest.
Cardiovascular Marked hypotension, bradycardia, cardiovascular collapse, cardiac arrest.
Systemic Risk Development of methemoglobinemia (blue/gray skin, rapid heart rate, headache, shortness of breath).

Emergency Actions and Urgent Help

Upon recognizing any sign of systemic toxicity or overdose, the medicinal product must be discontinued immediately. The regulator explicitly states that users must seek immediate medical attention or call a Poison Control Centre immediately if signs of methemoglobinemia are observed, such as pale, gray, or blue-colored skin, headache, or shortness of breath.

There is no specific antidote for lidocaine overdose. Constant ECG monitoring is required during certain administrations to manage potential toxicity. Patients with severe hepatic disease and infants under six months of age are listed in official labeling as being at greater risk for toxic blood concentrations or methemoglobinemia, respectively.

Therapeutic Uses of Xylocaina

Xylocaina is a medicine relevant across therapeutic domains where additional symptomatic support is needed. Its use in local or regional anesthesia is a main therapeutic domain, and it is also commonly used in situations involving systemic functional stress and applications for local anesthesia.

Xylocaina is commonly used to help with symptoms related to physical discomfort during acute medical and dental interventions, is relevant for managing ventricular tachyarrhythmias in critical settings, and may assist with providing supportive relief for chronic nerve-related pain, such as post-herpetic neuralgia. Topical forms are generally applied in conditions involving inflammatory or irritative processes, including discomfort from minor burns or hemorrhoids. The primary therapeutic benefit is commonly used to help with the creation of temporary, localized loss of sensation, which may help patients experience less distress during procedures.

Quick Fact: Supports relief for Acute Pain, Chronic Symptoms, and Electrical Instability

“The medication provides support that helps ease the overall symptom burden during periods of heightened symptoms.”

In clinical scenarios where short-term symptomatic assistance is needed, Xylocaina supports a manageable experience of symptoms, addressing symptom clusters that may become intense or disruptive and assisting with managing symptoms that create noticeable physiological strain in critical care contexts.

Eligibility and Restrictions for Use

Eligibility Map: Who can and cannot use Xylocaina

Official regulatory documents define strict criteria for the use of Xylocaina (Lidocaine Hydrochloride), establishing both absolute exclusions and conditional restrictions.


Populations for whom use is contraindicated

  • Patients with a known history of hypersensitivity to lidocaine or any other amide-type local anesthetic are strictly contraindicated.
  • Intravenous administration is contraindicated in patients with severe cardiac conduction diseases, including Stokes-Adams syndrome or Wolff-Parkinson-White syndrome, unless a pacemaker is present.

Age-related eligibility rules

  • Pediatric Patients: Use is restricted; children should receive reduced dosages. The oral viscous solution is limited for children under three years of age to situations where safer alternatives have failed.
  • Children under 2 years: Use requires caution due to insufficient safety and efficacy data for some topical forms.
  • Elderly Patients: Should be given reduced doses commensurate with their physical condition.

Condition-specific eligibility rules

  • Patients with severe hepatic (liver) or renal (kidney) disease must use the medicine with caution due to the risk of impaired clearance and drug accumulation.
  • Use requires caution in patients with pre-existing cardiovascular compromise, including severe heart block, hypovolemia, or shock.

Pregnancy and lactation eligibility status

  • Pregnancy (Category B): Use is permitted only if clearly needed as there are no adequate studies in pregnant women.
  • Lactation: Caution should be exercised when administered to a nursing woman, as it is not confirmed whether the drug is excreted in human milk.

What should I know about interactions with other medicines?

Interactions with other medicines and products

The official regulatory profile for Xylocaina (Lidocaine) documents specific interaction patterns concerning its clearance and systemic effects. The metabolism of Xylocaina is primarily mediated by the liver enzymes CYP1A2 and CYP3A4. Agents that inhibit these enzymes, such as Cimetidine and Fluvoxamine, can reduce Xylocaina's clearance, which is officially stated to increase plasma concentrations and raise the risk of toxic accumulation.

Conversely, CYP inducers like Phenytoin may decrease Xylocaina's exposure. Other medicines that reduce hepatic blood flow, such as Propranolol, can also increase Xylocaina plasma levels by slowing its removal from the body.

Pharmacodynamic and Product-Specific Restrictions

Interaction Type Interacting Substances/Context Official Regulatory Statement
Additive Toxicity Other Local Anesthetics, Methemoglobinemia-Inducing Agents Co-administration results in additive toxic effects and increased systemic risk.
Vasoconstrictor-Dependent Ergot-type Oxytocic Drugs, MAOIs, Tricyclic Antidepressants Use of Xylocaina with a vasoconstrictor (e.g., Epinephrine) is noted to carry a risk of severe, prolonged hypertension.
Timing Restriction Food and Chewing Gum (Oral Forms) Ingestion is restricted for 60 minutes after using oral forms to mitigate the risk of aspiration.

Certain non-medicinal substances, including Grapefruit Juice (CYP inhibition) and Nicotine (CYP induction), are also documented to affect Xylocaina exposure. Patients with severe hepatic or renal disease are officially noted to be at greater risk from these clearance-altering interactions.

Mechanism of Action

Core Mechanism: Direct Nav Channel Blockade

Xylocaina’s mechanism is defined by its action as a reversible blocker of voltage-gated sodium channels (Nav channels), the molecular gates necessary for electrical signaling in excitable cells. By physically obstructing the channel pore, the drug prevents the rapid influx of positive sodium ions (Na^+) across the membrane, thereby halting the electrical impulse. This interaction is use-dependent, meaning it preferentially targets nerves or cardiac tissue that are undergoing high-frequency depolarization.

Dual System Modulation

The Nav channel blockade leads to two distinct physiological consequences. In the peripheral nervous system, it causes the complete interruption of electrical signal propagation along sensory nerve fibers, which results in the reversible loss of afferent electrical signal transmission. In the heart, this mechanism modulates electrical activity in the myocardium by suppressing abnormal automaticity and reducing erratic firing in specialized cardiac cells.

Synergy: Prolonged Mechanism via Vasoconstriction

In combination products, a secondary mechanism is engaged: alpha1-adrenergic agonism induces local vasoconstriction (narrowing of blood vessels). This reduces the blood flow near the site of administration, which slows the rate at which Xylocaina is removed from the tissue. The resulting physiological effect is the prolongation of the primary Nav channel blockade duration.

Dosage and Administration Information

Official Administration Guidelines: Xylocaina (Lidocaine)

Xylocaina (lidocaine) is administered strictly according to the specific formulation and procedure. Professional adherence to the dose and administration guidelines is required to avoid serious adverse effects.

Administration Scope

Feature Guideline
Route of Administration Parenteral (Injection for blocks/infiltration), Topical Instillation (Jelly for mucous membranes), Topical Solution (Swish/Gargle).
Dosing Schedule The lowest effective dosage must be used. Do not exceed 4.5 mg/kg of body weight for injections in healthy adults. Maximum total dose for the 2% Jelly is 600 mg in any 12-hour period.
Age-Group Rules Reduced doses are required for children, the elderly, and acutely ill patients, commensurate with their age and physical condition.

Procedural and Timing Requirements

For injections (e.g., nerve blocks), aspiration must be performed prior to administration to prevent unintended intravascular delivery. For epidural administration, a test dose is recommended. Multiple-dose vials containing methylparaben should not be used for epidural or spinal anesthesia.

For topical oral solutions, food and chewing gum should not be ingested for 60 minutes following application to the mouth or throat to prevent aspiration and accidental biting trauma. The oral viscous solution may be used as needed, but typically no more frequently than every 3 hours, not to exceed 8 doses in 24 hours.

This structured approach ensures that the medicine is used in the specific manner, at the appropriate dose, and under the precise conditions established for each indicated application.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Xylocaina


Evidence for Local and Regional Anesthesia Studies

Research has extensively examined the use of Xylocaina injections for exploring temporary, localized loss of sensation, a context that is relevant in trials assessing short-term or episodic symptom patterns related to outcomes related to physical discomfort during procedures. These short-term Randomized Controlled Trials (RCTs) and observational settings evaluated the product's use in adults undergoing minor and major medical, surgical, and dental procedures. Studies consistently described patterns related to the rapid onset of a temporary loss of sensation following administration. The evidence for this primary function is highly consistent across major reviews.


Evidence for Acute Ventricular Tachyarrhythmias

The intravenous use of Xylocaina was evaluated in acute medical settings, relevant in research contexts involving fluctuating or unstable symptoms related to heart rhythm. Historical clinical trials and systematic reviews focused on patients experiencing acute or disruptive episodes of abnormal heart rhythm. Researchers monitored measurements related to controlling rapid, unstable electrical activity in the ventricles. Findings were characterized by heterogeneity and often relied on smaller populations. Certainty remains low regarding definitive long-term or survival outcomes, and comparative evidence is lacking in large-scale modern RCTs. The evidence level for this use is generally considered moderate.


Evidence for Post-Herpetic Neuralgia and Chronic Pain Relief

Controlled crossover studies and long-term observational data have explored the topical patch formulation of Xylocaina in the context of localized, persistent nerve-related discomfort, specifically Post-Herpetic Neuralgia (PHN). Research examined the use of the patch in adults with PHN, monitoring patient-reported outcomes describing perceived discomfort. Long-term observational data described patterns related to the duration of product application. Data provides limited information regarding the consistency of pain relief patterns when applied to other localized neuropathic pain conditions beyond PHN.


What is Still Uncertain About Xylocaina Research

A significant gap in the evidence relates to its use as an intravenous infusion in the context of perioperative recovery following surgery. Systematic reviews found that trials in this area reported mixed findings related to pain scores and opioid consumption, leading to the conclusion that certainty remains low for clinically relevant benefits in this specific scenario. The evidence quality varies for this particular use due to differences in study designs and modest sample sizes. Furthermore, for all uses, the data for certain groups and the long-term effects are not fully established, particularly when looking at repeat usage or sustained benefit outside of the specific conditions studied.

Key Studies & References WHO Model List of Essential Medicines

Frequently Asked Questions (FAQ)

Common questions about Xylocaina (FAQ)


Q: How quickly does the numbing effect of Xylocaina usually begin to work?

A: According to official product information, the numbing effect from topical Xylocaina formulations, such as creams or jellies, is generally described as beginning within a time frame of 3 to 5 minutes. For an injection, the numbing effect is typically described as starting within the first few minutes after administration.


Q: What are the general signs of a potential allergic reaction to Xylocaina?

A: Regulatory documents state that signs of a potential allergic reaction may include the development of hives (urticaria), skin lesions, or swelling (edema). These reactions can potentially be associated with more serious events classified as anaphylactoid reactions.


Q: What is methemoglobinemia, and is it a known risk with Xylocaina?

A: Methemoglobinemia is described in official safety documents as a rare but serious condition. It is described as a condition where the hemoglobin in the blood is maintained in a form that is less efficient at carrying oxygen. This condition is documented in regulatory information as a possible adverse reaction.


Q: Is there a risk of accidental injury to the numb area while Xylocaina is still active?

A: Official regulatory guidance on the use of the oral solution restricts the ingestion of food and chewing gum for a time after application to prevent accidental biting trauma to the mouth or throat. In general, any area that has experienced a temporary loss of sensation due to Xylocaina may be at risk for accidental injury. The temporary loss of sensation may require careful attention until normal feeling is restored.


Q: Is Xylocaina associated with any known long-term effects on the body?

A: Official safety information notes that spinal administration can be associated with the development of long-lasting neurological symptoms, such as numbness or paralysis. Furthermore, regulatory guidelines note a concern regarding infusion into a joint after surgery due to potential for irreversible joint damage.


Q: Can symptoms like tingling or numbness around the mouth be a warning sign of an issue?

A: Official product information lists numbness and tingling of the mouth and lips (perioral numbness) as a potential early indication of Central Nervous System (CNS) toxicity. This is described as a sign that the concentration of the medicine in the blood may be increasing.


Q: What is the difference between Xylocaina and other common topical numbing products?

A: The active ingredient in Xylocaina, Lidocaine, is classified as an amino amide-type local anesthetic. This classification is significant in the safety profile, as official guidelines require avoiding use in individuals who have a known sensitivity or allergy to any medicine within the amide-type local anesthetic class.


Q: Is Xylocaina considered a narcotic or a controlled substance?

A: Regulatory agencies classify Xylocaina's active ingredient, Lidocaine, as a Local Anesthetic and a Class Ib Antiarrhythmic Agent. It is not listed as a narcotic or considered a federally controlled substance.


Q: What is the typical duration of effect for Xylocaina topical cream or ointment?

A: Official drug information indicates that the numbing effects of topical Xylocaina formulations, such as creams or jellies, is typically described as beginning to subside after a period of approximately 1.5 to 2 hours. However, the duration of the effect can be influenced by various factors.


Q: Does the duration of Xylocaina's effect depend on the area of the body it is applied to?

A: Yes, regulatory information describes the total duration of the numbing effect as being influenced by several factors, including where the product is applied on the body and the overall size of the treated area.


Q: Does the effect of Xylocaina last longer if a higher concentration is used?

A: Official product information notes that the duration of the numbing effect for topical Xylocaina is one of the factors that can depend on the concentration of the cream or jelly formulation used.


Q: Are there factors that can affect how quickly Xylocaina works for pain relief?

A: Yes, the rate at which Xylocaina begins to work is documented as being influenced by factors such as the specific formulation used (e.g., jelly vs. injection), the amount administered, and the patient's overall health status.


Q: If Xylocaina is administered as an injection, how long does the numbness typically last?

A: Regulatory sources indicate that the effects of a Xylocaina injection is generally described as beginning to subside after a period of approximately 1.5 to 2 hours. The actual duration can vary depending on the specific injection technique and whether a vasoconstrictor (like epinephrine) was included.


Q: Is it possible for Xylocaina's numbing effect to wear off too quickly during a procedure?

A: Yes, the duration of the numbing effect is directly linked to factors like the specific dosage and concentration used, as well as the site of application. These factors are central considerations in regulatory administration guidelines regarding the expected duration of effect.


Q: Why might some people experience a metallic taste after receiving Xylocaina?

A: A metallic taste is listed in official documents as a possible early warning sign of Central Nervous System (CNS) toxicity. This taste is noted as one of the signs associated with a potential increase in the concentration of the medicine in the bloodstream.


Q: Does Xylocaina affect a person's ability to drive or operate machinery?

A: Official regulatory agencies caution that Xylocaina use may result in side effects such as drowsiness, dizziness, or blurred vision. Such neurological effects may temporarily impact the ability to safely drive or operate machinery.


Q: Is mild skin irritation or temporary redness a normal reaction after topical Xylocaina application?

A: Official safety information classifies local irritation or redness (erythema) at the site of application as common reactions following the use of topical Xylocaina formulations.


Q: Are there restrictions on using Xylocaina if a person has epilepsy or a history of seizures?

A: The medicine is generally noted to require caution when used in patients with a history of seizure disorders. This is due to the drug’s potential effect on the central nervous system, which, at high concentrations, includes the risk of convulsions.


Q: Can Xylocaina interact with over-the-counter pain medications or supplements?

A: Yes, the medicine is documented to interact with certain medicines and supplements that influence the liver enzymes responsible for its clearance (CYP1A2 and CYP3A4). These interactions may slow the body's removal of the medicine, which could result in higher concentrations in the bloodstream.


Q: Can Xylocaina be used after the expiration date printed on the package?

A: Regulatory agencies define the expiration date as the time during which the product is guaranteed to retain its strength and quality. For this reason, official guidance recommends against using any medication past its printed expiration date due to the potential for loss of effectiveness.

How should Xylocaina be stored and disposed of?

Storage and Disposal of Xylocaina

The official storage conditions for Xylocaina (Lidocaine HCl) require adherence to specific temperature and handling rules, as determined by regulatory agencies.

Official Storage and Handling

  • Temperature: Store at 20 C to 25 C ( 68 F to 77 F), consistent with Controlled Room Temperature. Do not freeze the sterile injection solutions.
  • Protection: Injectable forms containing Epinephrine must be protected from light.
  • Stability Check: The solution must be visually inspected before use; do not administer if particulate matter or discoloration is observed.
  • Child Safety: All forms of the medicine must be stored out of the sight and reach of children.
  • Single-Dose Vials: Any unused portion of solution from single-dose containers must be discarded immediately after initial use.

Disposal

Unused or expired Xylocaina should be disposed of in accordance with local regulations for pharmaceutical waste. Avoid disposal into household trash or wastewater unless specific local instructions authorize it.

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

Available in countries:

Equivalent of Xylocaina found in:

A-Z Index: