Lidopril

Quick links to important sections

Lidopril

Selected form

Treatment option: Anesthesia, Surgery

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.

Overview of Lidopril

What is Lidopril?

Lidopril is a topical anesthetic medication formulated as a cream. It is primarily used to provide temporary numbness to the skin and surrounding tissues. By blocking nerve signals in the body, it helps to reduce the sensation of pain in the specific area where it is applied.

Composition and Mechanism

Lidopril typically contains a combination of two active local anesthetic agents: lidocaine and prilocaine. These components belong to the amide class of anesthetics.

When applied to intact skin, the cream works by penetrating the epidermal and dermal layers. Once absorbed, the active ingredients stabilize the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of nerve impulses. This localized action prevents the transmission of pain signals to the brain without affecting consciousness or general sensation in other parts of the body.

Clinical Applications

Lidopril is used in various clinical and outpatient settings to prepare for minor medical procedures. Its primary purpose is to enhance patient comfort during activities that involve skin penetration or surface irritation. Common applications include:

  • Needle Insertions: Providing surface anesthesia for blood draws, intravenous catheter placements, and vaccinations.
  • Superficial Surgical Procedures: Numbing the skin prior to minor dermatological interventions, such as the removal of warts or skin tags.
  • Laser Treatments: Reducing discomfort during aesthetic or medical laser therapies.
  • Tattooing and Piercings: Managing pain associated with dermal decorative procedures.

Pharmacological Properties

The effectiveness of Lidopril depends on the duration of application and the thickness of the skin at the site. Because it is a topical preparation, its effects are localized. The onset of anesthesia usually occurs after a period of occlusion, during which the cream is kept in contact with the skin to ensure adequate depth of penetration. Once the cream is removed, the numbing effect gradually diminishes as the metabolic processes of the body clear the active ingredients from the local tissue.

Regulatory References

  1. Lidocaine, Prilocaine Drug Combination MeSH Descriptor

What side effects are possible with Lidopril?

Possible Side Effects and Safety Information

The safety profile for this combination topical preparation is formally classified by regulatory authorities, distinguishing between common localized effects and rare systemic risks. Adverse reactions are primarily grouped under Skin and Subcutaneous Tissue Disorders and General Disorders and Administration Site Conditions.


Frequency-Classified Adverse Reactions

Classification Adverse Reaction Description (Application Site Reaction)
Very Common Blanching, Erythema, Edema Paleness, redness, or swelling, typically transient initial reactions.
Common Pruritus, Burning Sensation, Local Pain Itching, warmth, or discomfort confined to the treated area.
Rare Methemoglobinemia, Allergic Reactions A blood disorder reducing oxygen capacity; severe allergic reactions.

The most frequent occurrences are the Very Common and Common transient localized application site reactions. These are classified as initial reactions that occur following application of the cream.

Systemic Risk and Special Population Considerations

A rare, but officially documented, serious risk is Systemic Toxicity, which may manifest as Central Nervous System (CNS) or Cardiovascular effects if excessive amounts of the active ingredients are absorbed into the bloodstream. The most notable serious risk is Methemoglobinemia, a blood disorder.

Specific population-specific safety considerations are noted in official labeling for groups at higher risk of methemoglobinemia, including infants and young children, as well as patients with Glucose-6-phosphate dehydrogenase (G6PD) deficiency. Furthermore, caution is documented for use in patients with severe hepatic impairment due to the potential for increased systemic exposure. Safety limitations restrict application on broken skin or damaged tympanic membranes to mitigate the risk of excessive absorption.

Overdose and Emergency Response

Documented Overdose Manifestations

Overdose from excessive topical absorption may result in systemic toxicity, primarily affecting the Central Nervous System (CNS) and Cardiovascular (CV) system. CNS manifestations, which may appear first, are documented to include dizziness, lightheadedness, confusion, tremors, visual disturbances, and may progress to muscle twitching and convulsions (seizures).

The Prilocaine component carries a distinct risk of Methemoglobinemia, a documented severe physiological event indicated by cyanotic skin discoloration (pale, gray, or blue skin) and respiratory distress. Cardiovascular effects documented in severe cases include bradycardia (slow heart rate), arrhythmias, and potential circulatory collapse.

When to Seek Immediate Medical Help

Regulatory guidance mandates that the product must be discontinued immediately if systemic toxicity or Methemoglobinemia is suspected. You must seek immediate medical attention upon observation of any documented signs of toxicity, such as shortness of breath, rapid heartbeat, or cyanosis. Prompt, supportive care and symptomatic treatment are required for the management of toxicity. The specific treatment cited for clinically significant Methemoglobinemia is Methylene blue.

Overdose risk is cited as increased for infants under three months of age and for patients with conditions such as severe hepatic disease.

Therapeutic Uses of Lidopril

Lidopril is relevant for managing symptoms related to physical discomfort during necessary clinical interventions. The topical preparation is used in situations involving certain distressing symptoms, providing supportive relief by easing physical discomfort in the treatment area. This contributes to easing the overall symptom load associated with minor medical and cosmetic procedures.

The primary use is to help reduce the intensity of acute, sharp, and stinging discomfort for procedures such as blood drawing (venipuncture), intravenous (IV) catheter placement, and minor surgical procedures like excisional biopsies. It is also applied in dermatological contexts, including certain laser treatments and superficial surgical procedures on genital skin.

The medication's role is to support patient comfort, particularly in pediatric and anxious patients, by managing anticipatory pain and disruptive symptom manifestations due to procedure anxiety. “The application supports patients during difficult episodes by easing distress and contributing to improved comfort during procedures.”


Quick Fact: Used for managing Acute Procedural Pain


Pain Prevention for Needle and IV Procedures

This topical preparation is used in areas where short-term symptom management is appropriate, specifically targeting the acute, sharp, and stinging discomfort that accompanies needle-related procedures.

Regulatory References

  1. MedlinePlus Drug Information on Lidocaine and Prilocaine Topical

Eligibility and Restrictions for Use

Who can and cannot use Lidopril?

Regulatory documentation defines specific populations who can and cannot use Lidopril (Lidocaine/Prilocaine) based on age, health status, and metabolism. Eligibility is generally established for adults and pediatric patients aged 3 months and older under strict conditions.


Contraindicated Populations

The medicine is formally contraindicated in patients with a known hypersensitivity or allergy to amide-type local anesthetics (Lidocaine or Prilocaine). It is also prohibited for patients with a history of congenital or idiopathic methemoglobinemia and for premature infants born before 37 completed weeks of gestation.


Eligibility Restrictions and Limitations

Population Group Restriction or Caution Status (Regulatory Labeling)
Infants 0 up to 12 months Use is not recommended if the infant is also receiving other methemoglobin-inducing medications.
Hepatic or Renal Impairment Use requires caution in patients with severe hepatic (liver) disease due to risk of impaired drug clearance. Caution is also noted for severe renal (kidney) dysfunction.
Metabolic Risk Patients with G6PD deficiency are more susceptible to methemoglobinemia, requiring use with caution.
Pregnancy and Lactation Use during pregnancy is generally assigned Category B; use during lactation is generally considered acceptable as small amounts of the active ingredients are excreted into breast milk but an effect on the child is unlikely.
Skin Integrity Must not be applied to an impaired tympanic membrane. Application to atopic dermatitis requires a reduced application time (e.g., 15–30 minutes).

What should I know about interactions with other medicines?

Interactions with other medicines and products

Lidopril's interaction profile is officially structured around the potential for Pharmacodynamic Additive Toxicity and Pharmacokinetic Clearance Modification, as detailed in regulatory documents.

Pharmacodynamic Interactions: Additive Toxicity

Co-administration with other methemoglobin-inducing agents, such as sulfonamides, dapsone, or other local anesthetics, carries an officially documented additive risk for methemoglobinemia. Similarly, concurrent use with other local anesthetics or structurally related anti-arrhythmics (e.g., Class I agents like Mexiletine) may result in additive toxic effects on the cardiovascular and central nervous systems.

Pharmacokinetic Interactions: Reduced Clearance

Medicines that inhibit hepatic metabolism, specifically Cimetidine and certain beta-blockers, are formally documented to reduce the clearance of Lidocaine. This pharmacokinetic interaction may lead to increased systemic plasma concentrations of the active ingredient, though regulatory documents note this is generally considered clinically irrelevant for short-term topical application at recommended doses.

Interaction-Related Restrictions

The medicine is formally contraindicated in individuals with a history of congenital or idiopathic methemoglobinemia. Furthermore, the official label notes that patients with severe hepatic impairment, compromised renal function, or G6PD deficiency have a heightened susceptibility to these documented systemic interaction risks.

Mechanism of Action

Molecular Inhibition of Nerve Impulse Conduction

Lidopril's primary mechanism involves the reversible blockade of voltage-gated sodium channels ( VGSCs) located on peripheral sensory nerve membranes. By physically obstructing the channel pore, the active ingredients prevent the rapid influx of Na^+ ions, which is essential for cell depolarization and generating a nerve action potential. This targeted inhibition stops the transmission of sensory signals, which constitutes a localized suspension of action potential propagation.

Physicochemical Synergy for Enhanced Delivery

The medicine is formulated as a Eutectic Mixture of Lidocaine and Prilocaine, creating a liquid preparation that significantly increases the drugs' transdermal diffusion rate. This enhanced diffusion ensures a higher concentration of the active ingredients reaches the target peripheral nerve endings in the dermis. This physicochemical synergy is crucial as it overcomes the skin barrier, facilitating the prompt and robust engagement of the sodium channel blockade mechanism.

Contextual Constraints on Mechanism Efficacy

The functional capacity of the sodium channel blockade mechanism is constrained by the local physiological environment, primarily tissue pH. In situations of inflammation or infection, the resulting acidic environment reduces the amount of the drug in its necessary non-ionized form, which is the only form capable of diffusing across the nerve membrane to access its target. This dependency means that the mechanism's functional blockade is subject to reduced functional blockade in areas affected by acidosis.

Dosage and Administration Information

How to Use Lidopril

Lidopril (Lidocaine 2.5% and Prilocaine 2.5% topical combination) is administered via the Topical (Cutaneous) route as an emulsion cream or anesthetic patch, strictly for application to intact skin. The usage is an acute, single application preceding a medical procedure.


Official Dosing and Time-Bound Schedule

Administration Scope Administration Guidelines
Standard Dosing Apply as a thick layer (not rubbed in). For minor procedures, the dose ranges from 1 to 2.5 grams. For extensive procedures, the dose is area-based, such as 1.5 to 2 grams per 10 cm^2.
Application Time Requires a minimum duration of at least one hour for common needle procedures and two hours for more extensive interventions. The cream must not remain on the skin for longer than five hours.
Pediatric Rules Administration is restricted by age and body weight. Infants 0-3 months are limited to a maximum single dose of 1 gram over a surface area no larger than 10 cm^2.

Procedural Administration Constraints

The standardized protocol requires specific procedural constraints to be met. The applied cream must be immediately covered with an occlusive dressing to ensure proper dermal uptake of the eutectic mixture. Just prior to the procedure, the occlusive dressing and all remaining cream must be removed and wiped off completely.

The overall use protocol establishes a precise, time-sensitive regimen defined by specific dose-to-area calculations, mandatory occlusion steps, and strict minimum and maximum time limits for application.

Recent Clinical Evidence

Research evidence / Overview of studies

Key Findings from Preclinical Research

Preclinical studies primarily investigated the compound’s activity.

  • Research has explored the compound’s potential role in the body’s inflammation response and its association with moderate pain.
  • Preclinical findings suggested the compound interacted with certain biological targets.
  • Its anti-inflammatory properties were evaluated in animal models; findings showed an observation of change in markers of inflammation.

Clinical Trial Data: Phase 2 and 3

The drug was evaluated in a total of 1,200 subjects across 15 global sites. The primary outcome was a change in the self-reported pain score (VAS) over 12 weeks.

  • In a randomized, controlled Phase 2 trial (N=350), studies examined whether the drug affected joint mobility and investigated its association with pain reduction over six weeks.
  • A reduction in swelling was reported in the majority of subjects in the study.
  • The study included older patients with mild cardiovascular concerns, and data related to adverse events were collected.

The Phase 3 trial (N=850) was conducted over 24 weeks to evaluate longer-term outcomes.

  • The trial provided data relevant to the measurement of outcomes and adverse events (tolerability) profile.
  • No significant difference was noted in the comparison with the standard of care.

Pharmacokinetics and Administration

Studies investigated the effect of food intake on the drug's absorption; research noted that taking the drug on an empty stomach was associated with changes in bioavailability.


Combination Therapy

Research evaluated whether the combination regimen was associated with different long-term symptom management outcomes compared to monotherapy.

  • The study design was a randomized, double-blind trial over six months.
  • The research protocol noted that subjects experiencing a rash were required to report it to study personnel.
  • The study authors noted that further research is required to understand the long-term impact of the combination therapy.

Key Studies & References

  1. LIDOPRIL (Lidocaine 2.5% and Prilocaine 2.5% Cream, USP) - DailyMed (FDA Labeling)

Frequently Asked Questions (FAQ)

Common questions about Lidopril (FAQ)


Q: What is the primary action of Lidopril in the body?

Lidopril works by blocking the action of an enzyme in the body called Angiotensin-Converting Enzyme, or ACE.

According to the official product information, this action helps to relax blood vessels, which in turn lowers high blood pressure. This effect is why it is classified as an ACE inhibitor.


Q: How long does it typically take for Lidopril to start working after the first dose?

Studies and official information indicate that after a dose of Lidopril, the blood pressure-lowering effect typically starts to appear within about one hour.

The peak effect, which is the maximum blood pressure reduction, is usually observed around 6 hours after the initial dose.


Q: Can Lidopril be taken with or without food?

Official regulatory documents state that Lidopril tablets can be taken either with or without food.

Taking it with food does not significantly change how the medicine is absorbed or how effectively it works in the body, according to label information.


Q: What should I do if I forget to take a dose of Lidopril?

Regulatory documents typically indicate that a missed dose of Lidopril may be taken as soon as it is remembered.

However, if the time for the next scheduled dose is near, the official guidance is to skip the missed dose and continue the regular schedule. Official prescribing information consistently advises against taking a double dose to compensate for a missed one.


Q: Is it safe to drive or operate machinery while taking Lidopril?

Official product information suggests caution regarding activities requiring full alertness, such as driving or operating machinery.

This is relevant because some patients may experience dizziness or fatigue, especially when treatment begins or following a dose adjustment, due to lowered blood pressure.


Q: How should Lidopril be stored?

Official product information specifies that Lidopril storage conditions involve maintaining it at room temperature and protecting it from both moisture and heat.

Regulatory guidelines also state that the medicine should remain in its original container and be kept out of the reach of children.


How should Lidopril be stored and disposed of?

The official storage and disposal requirements for Lidopril (Lidocaine and Prilocaine topical) are defined by regulatory labeling to ensure product stability and safety.

Storage Requirements

Condition Official Requirement
Temperature Store at 20 C to 25 C (68 F to 77 F). Do not store above 30 C.
Protection Do not freeze. Keep the container tightly closed and away from excess heat and moisture.
Child Safety Keep the medicine out of the sight and reach of children and pets at all times.

Disposal Instructions

Any unused or expired product must be disposed of safely according to local requirements. For creams used on leg ulcers, any contents remaining in the tube after the single use must be discarded immediately. The medicine should not be flushed down the toilet or disposed of into wastewater unless specifically directed by official guidance.

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

Available in countries:

Equivalent of Lidopril found in:

A-Z Index: