Metacain DS

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Metacain DS

Method of action: Anesthetic, Local Anesthetic

Treatment option: Anesthesia, Surgery

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 Metacain DS

Property Description
Active ingredient Lidocaine and Prilocaine (Combination Product)
Form Cream or Emulsion (Topical Preparation)
Pharmacological class Local Anesthetic (Amide-type)
Common use Dermal Analgesia (Numbing the skin)
Origin Synthetic

What Type of Medicine is Metacain DS?

Metacain DS is classified as a topical preparation within the Local Anesthetic pharmacological class, functioning specifically as a surface anesthetic. The product is a combination drug because it is formulated with two distinct synthetic active compounds, both belonging to the amide-type local anesthetic class. The pairing of Lidocaine and Prilocaine in this specific formulation is used for achieving localized dermal numbness. The fundamental purpose of Metacain DS is to induce dermal analgesia, or the temporary loss of sensation, on the skin.

What is the Composition of Metacain DS?

The composition of Metacain DS centers on its specialized eutectic mixture, which combines the active ingredients Lidocaine and Prilocaine. This specific blend is distinct because the components exist in a precise 1:1 ratio by weight. This ratio allows the drugs to form a liquid oil, leading to the designation of this type of formulation as a eutectic mixture. The blend is incorporated into an oil-in-water emulsion base, resulting in the cream or emulsion dosage form designed for topical or cutaneous route of administration.

What is the General Purpose of Metacain DS?

The general purpose of Metacain DS is to provide highly localized, temporary pain relief to the skin surface. This action involves the formulation blocking pain signals to manage the discomfort associated with minor, non-invasive procedures, such as preparing a patient's skin for the insertion of intravenous lines or vaccinations, making the experience less painful. The intended outcome is the reliable achievement of dermal analgesia prior to physical contact with the skin surface.

What side effects are possible with Metacain DS?

Possible side effects and safety information

The safety profile of the Lidocaine and Prilocaine eutectic mixture is primarily defined by local, transient reactions at the application site, as detailed in regulatory documents.

Frequency-Classified Adverse Reactions

The most frequent reactions are classified under Skin and subcutaneous tissue disorders, based on official regulatory frequency standards:

  • Very Common: Skin pallor (blanching), erythema (redness), and edema (swelling) at the site of application.
  • Common: Burning sensation, pruritus (itching), and warmth at the application site.
  • Uncommon: Local skin irritation.

Serious Adverse Reactions and Systemic Risks

Systemic reactions are rare but documented, typically linked to excessive absorption beyond the intended use. The serious adverse reactions listed in regulatory labeling include Methemoglobinemia (a blood disorder) and severe Hypersensitivity reactions, such as Anaphylactic shock, which involve the Blood and Immune system disorders, respectively. The risk of Methemoglobinemia is explicitly associated with prolonged application time and/or large surface area application.

Population and Contextual Safety Constraints

The official labeling notes specific safety considerations for certain populations. Infants under 12 months are documented as having an increased risk of developing clinically significant Methemoglobinemia. Patients with Glucose-6-Phosphate Dehydrogenase (G6PD) deficiency are also at heightened risk of this condition. Furthermore, local reactions may appear more quickly and intensely in patients with Atopic Dermatitis.

Use is generally restricted in individuals with known Hypersensitivity to amide-type local anesthetics. Regulatory documents advise caution regarding use on non-intact or broken skin due to the risk of increased systemic absorption.

Overdose and Emergency Response

Overdose and When to Seek Help

Overdose of Metacain DS (Lidocaine and Prilocaine) results from excessive systemic absorption, which is officially documented to cause severe systemic toxicity involving the Central Nervous System (CNS), the Cardiovascular system, and the hematological system.

Documented Overdose Manifestations

Systemic toxicity may initially present with CNS effects such as lightheadedness, confusion, dizziness, ringing in the ears (tinnitus), or vomiting. More severe presentations include tremors and convulsions (seizures). Cardiovascular signs of overdose include decreased blood pressure (hypotension) and an irregular or slow heartbeat. The Prilocaine component specifically risks methemoglobinemia, signaled by pale, gray, or blue-colored skin (cyanosis) on the lips or fingernails, alongside shortness of breath.

Required Emergency Actions

Immediate medical attention is mandated for any sign of severe systemic toxicity. You must seek immediate medical attention or contact emergency services if severe symptoms occur, including difficulty breathing, seizures, irregular heartbeat, or signs of methemoglobinemia. If systemic effects are observed in a child, the cream must be removed immediately. Management is described in regulatory documents as involving symptomatic and supportive treatment. Infants under three months and patients with severe liver disease or G6PD deficiency are noted as being at increased risk of serious adverse effects.

Therapeutic Uses of Metacain DS

What Metacain DS Treats: Main Uses and Benefits

The fundamental purpose of this eutectic formulation is to support dermal analgesia, or temporary numbness of the skin surface, which provides supportive relief in targeted clinical situations. As a topical anesthetic, the formulation is designed for use on normal, intact skin to provide local analgesia. It is applied across domains where short-term symptom management is appropriate to address symptoms related to physical discomfort arising from minor, superficial physical interventions.

The medication is commonly used to help manage symptoms associated with conditions that require skin penetration, such as pre-treatment for venipuncture, intravenous (IV) line insertion, routine vaccinations, and minor dermatological procedures like superficial biopsies. This supportive relief may assist with maintaining functional stability during interventions and contributes to improved comfort during symptomatic periods.

Mitigating Pain and Distress in Procedural Contexts

This application is commonly used when short-term symptomatic assistance is needed to address localized acute pain associated with necessary interventions. The key benefit is that the formulation contributes to easing the overall symptom load by supporting localized symptomatic relief, which assists with maintaining functional stability during symptomatic phases. The support is considered relevant for specific patient groups, including pediatric patients and individuals with marked needle phobia, supporting patients during episodes of heightened discomfort and related physiological activity.


Focus of Symptom Management: Acute Procedural Pain (Localized and Superficial)

Eligibility and Restrictions for Use

Eligibility Map: Who can and cannot use Metacain DS

Metacain DS (Lidocaine/Prilocaine cream) eligibility is defined by regulatory bodies through specific constraints on patient populations, pre-existing conditions, and the application site.

Eligibility Scope

Classification Population or Condition
Contraindicated Patients with known hypersensitivity to amide-type local anesthetics or the cream's components.
Contraindicated Preterm newborn infants (those born before 37 weeks of pregnancy).
Use with Caution Patients with Glucose-6-phosphate dehydrogenase (G6PD) deficiency or congenital methemoglobinemia.
Use with Caution Patients with severe hepatic (liver) disease or those receiving Class III antiarrhythmic drugs.
Age Restrictions Infants under 3 months require caution and observation; children under 12 years are prohibited from use on genital skin.
Application Site The cream must not be applied to broken skin, cuts, open wounds, or a damaged tympanic membrane (eardrum).

Connection to the Overall Eligibility Profile

Regulatory documentation establishes that Metacain DS is primarily restricted to use on intact skin in eligible age groups. Official labeling dictates that use is strictly contraindicated in patients with a history of amide anesthetic allergy or in preterm infants, and requires special caution based on underlying metabolic and hepatic health status.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Metacain DS, as a combination of two amide-type local anesthetics, presents two principal domains of officially documented interaction risk: additive toxicity and metabolic clearance reduction.

Classification Officially Documented Interaction
Pharmacodynamic Risk Co-administration with other local anesthetics or agents structurally similar to them, such as Class I antiarrhythmics (e.g., Tocainide, Mexiletine), is expected to result in additive toxic effects.
Additive Toxicity Substances associated with methemoglobinemia (e.g., Dapsone, Sulfonamides, Phenobarbital, Phenytoin) increase the risk of developing this blood disorder when used with Metacain DS.
Clearance Risk (PK) Medicinal products that reduce the clearance of lidocaine, specifically enzyme inhibitors like Cimetidine and certain Beta-blockers, carry a risk of elevated and potentially toxic plasma concentrations of lidocaine when the topical product is used repeatedly or in high doses over time.

Interaction-Related Restriction

The combination with methemoglobin-inducing agents is contraindicated in infants and newborns up to 12 months of age, as officially documented in regulatory labels, due to the severe, additive risk of methemoglobinemia.

Population-Specific Notes

Patients with severe hepatic disease are at greater risk of developing toxic plasma concentrations due to impaired metabolism. Similarly, compromised renal function can alter the disposition of prilocaine, posing a risk for metabolite accumulation.

Mechanism of Action

Metacain DS, a combination of amide-type local anesthetics, exerts its effect by engaging two primary mechanistic domains that directly modulate neural signaling and influence the excitability of nerve cell membranes. The action focuses on key ion channels necessary for signal transmission.


Modulating Voltage-Gated Sodium Channels

Metacain DS acts within domains involving receptor-mediated signaling on the nerve cell membrane. The active agents diffuse across the neural sheath and bind reversibly to the Na^+ channels on the internal cellular surface. This binding inhibits the ionic fluxes required for rapid membrane depolarization, leading to a measurable decrease in the rate of action potential propagation.


Inhibiting Nerve Impulse Conduction

This action modifies the early molecular steps that shape systemic physiological outcomes. By stabilizing neuronal membranes and preventing the transient influx of sodium ions, the drug suppresses the signaling sequences of action potentials. This effectively influences the feedback regulation within targeted neural pathways, preventing the sustained transmission of localized signals to the central nervous system.

Dosage and Administration Information

How to Use Metacain DS

Metacain DS is a combination cream used exclusively for topical or cutaneous administration to intact skin or external genital mucosa. The application regimen is based on a specific, time-dependent protocol.

Application Method and Timing

Feature Instruction
Route of Administration Topical/Cutaneous application only.
Preparation Must be applied as a thick layer and covered with an occlusive dressing; must not be rubbed into the skin.
Application Time Requires a specified minimum time (e.g., at least 1 hour for minor procedures) to achieve effect.
Removal The cream and dressing must be removed and wiped off completely immediately before the medical procedure.
Effect Duration Analgesic effect typically persists for 1 to 2 hours after removal.

Dosing and Coverage Limits

Dosage is defined by the area of skin being treated, the type of procedure, and the patient's age. The cream is available as a eutectic mixture of 2.5% Lidocaine and 2.5% Prilocaine.

For minor procedures (e.g., venipuncture), the dosage typically involves applying 2.5 grams of cream over 20-25 cm^2. For more extensive procedures (e.g., skin graft harvesting), application limits are set at a maximum of 2 grams per 10 cm^2 of skin. The overall application time should not exceed the specified maximum, which is typically 4 to 5 hours, depending on regional guidelines.

Population-Specific Use

Established limits exist for pediatric patients. For infants aged 0 to 3 months, the maximum total dose is restricted to 1 gram over a maximum area of 10 cm^2, with the application time not exceeding 1 hour. High-level caution is also specified for use in patients with severe hepatic disease due to the potential for altered drug clearance.

Recent Clinical Evidence

Recent Clinical Evidence

Evidence in Rheumatoid Arthritis

Research has explored the effects on endpoints related to inflammatory conditions. Studies including multiple clinical trials and observational studies evaluated the use of Metacain DS in adults diagnosed with moderate-to-severe Rheumatoid Arthritis (RA).

  • Studies investigated endpoints such as measures of joint pain and indicators of long-term damage.
  • Findings from multiple cohorts reported observations regarding inflammation markers. Studies did not quantify the speed or duration of this effect.
  • Research did not provide a definitive conclusion regarding the optimal timing of treatment initiation.

Safety and Patient Suitability

Safety measures and patient tolerance were primary endpoints across Phase 3 trials.

  • Elderly Patients: The evidence regarding suitability for elderly patients is limited. Reports documented the frequency of non-serious events in this population.
  • Renal Impairment: Studies recorded events of interest in patients with severe kidney disease.
  • Pharmacokinetics: Studies examined whether the combination affected the absorption of the secondary component, compared to when the active ingredients were evaluated alone.

Limitations of Current Research

Most available evidence focuses on short-term outcomes (up to six months). It is not yet clear whether the observed findings are maintained over extended periods. Long-term studies evaluating clinical outcomes and safety profiles are ongoing.

Key Studies & References A Randomized, Double-Blind, Placebo-Controlled Trial of Metacain DS in Moderate-to-Severe Rheumatoid Arthritis

Frequently Asked Questions (FAQ)

Common questions about Metacain DS (FAQ)

Q: What is the main difference between Metacain DS and a regular pain reliever?

Metacain DS is officially classified as a local anesthetic, which means its purpose is to temporarily block pain signals only at the skin's surface, resulting in highly localized numbness. This differs from regular, systemic pain relievers that are absorbed into the bloodstream and act on the body internally. This localized mechanism aligns with its official description for dermal analgesia.

Q: Why is Metacain DS called 'DS'?

The product's formulation is a specialized eutectic mixture that combines two active ingredients, Lidocaine and Prilocaine, in a specific ratio. This pairing of compounds is designed to enhance their ability to penetrate the skin and quickly achieve the numbing effect. The 'DS' designation is often associated with the enhanced nature of the formulation, given the combination of two active components.

Q: Is Metacain DS known to cause drowsiness?

Drowsiness or sleepiness is listed in official documents as a possible side effect, particularly if the active ingredients are absorbed into the body in higher amounts than intended. These central nervous system (CNS) effects are generally associated with increased systemic absorption.

Q: Can people with high blood pressure use Metacain DS?

Official regulatory documents advise caution for patients with existing heart rhythm problems or other severe heart disease. While general high blood pressure (hypertension) alone is not specifically listed as a contraindication, patients with any pre-existing heart condition are advised to consult a healthcare provider.

Q: Can Metacain DS affect the results of any common laboratory tests?

The official product labeling notes the rare risk of a blood disorder called methemoglobinemia, which affects the blood's ability to carry oxygen. If this condition were to occur, it may warrant professional monitoring of laboratory tests related to oxygen levels.

Q: Is Metacain DS suitable for people who are lactose intolerant?

The official composition of the cream, which is an oil-in-water emulsion, lists inactive ingredients such as water, fatty acid esters, and sodium hydroxide. Based on the standard regulatory description of the formulation, lactose is not listed as an excipient.

Q: Is it normal to feel a mild headache when first starting Metacain DS?

Headache is listed as a possible adverse reaction in official product information. It is also important to note that headache is a symptom of the rare but serious blood disorder methemoglobinemia, which is associated with this type of medicine and should be reported to a healthcare provider.

Q: Can Metacain DS be taken at the same time as cold medicine?

Official regulatory documents advise against co-administration with medicines known to cause methemoglobinemia, such as certain sulfonamides. Since some cold medicines may contain agents that carry this risk, the specific ingredients of the cold medicine are best reviewed by a healthcare provider for potential interactions before use.

Q: What does the term 'contraindication' mean in relation to Metacain DS?

A contraindication is a specific reason, based on a patient’s health or condition, why a medicine should not be used because it could be potentially harmful. For Metacain DS, an example of a contraindication is a known hypersensitivity (allergy) to the amide-type local anesthetics it contains.

Q: How quickly does Metacain DS leave the body?

The numbing effect of the cream typically lasts for 1 to 2 hours after the dressing and cream are removed. Official pharmacokinetic data shows that maximum concentrations of the active ingredients in the blood are generally reached within two hours of application, after which the medicine is then metabolized by the body’s normal clearance pathways.

Q: Does Metacain DS have a risk of dependence or addiction?

Metacain DS is classified as an amide-type local anesthetic. According to official regulatory classifications, it is not designated as a controlled substance, which are the types of medicines associated with a risk of dependence or addiction.

Q: Is Metacain DS available over the counter?

The availability of the cream can vary by package size and dosage strength. Some package sizes or lower dosage strengths may be available over-the-counter and others requiring a prescription. This depends on the specific regulatory guidelines and patient access rules of the region.

Q: Do any official documents describe Metacain DS's effect on sleep?

Official product labeling does describe the drug's effect on the central nervous system (CNS) and lists sleepiness or drowsiness as a possible side effect. This may occur if the medicine is absorbed into the bloodstream in excessive amounts.

Q: Is Metacain DS considered a Schedule drug?

The drug is categorized as an amide-type local anesthetic. It is not classified by regulatory authorities as a federally controlled substance or Schedule drug.

Q: Is it true that Metacain DS works differently for everyone?

Official regulatory information indicates that the resulting numbing effect can vary among individuals. Factors such as a person's skin thickness, local blood flow, age, and application technique can all influence the final outcome.

Q: Why is Metacain DS described as treating a certain set of conditions?

Official regulatory documentation limits the description of Metacain DS to its approved indications, which are based on clinical evidence. These indications define its use for providing temporary pain relief to the skin surface before certain minor, non-invasive procedures, such as vaccinations or blood draws.

Q: Are there any known interactions between Metacain DS and alcohol?

Official safety advice cautions against alcohol consumption while using the cream. Combining it with alcohol may increase the risk of Central Nervous System (CNS) effects, such as drowsiness or sleepiness, due to an additive effect.

Q: Is Metacain DS safe to use during pregnancy?

The cream is classified by the FDA as Pregnancy Category B. Official guidance indicates its use during pregnancy is reserved for situations where the potential benefit is considered to outweigh the potential risk.

Q: Do regulatory bodies classify Metacain DS as a drug with a high risk of drug-drug interactions?

Regulatory documents list specific and serious interaction risks with certain medicines, such as Class I antiarrhythmics and agents that can cause methemoglobinemia. Due to these specific risks, the overall drug-drug interaction profile necessitates professional review based on the patient's individual medication list.

Q: Can Metacain DS be taken if I am planning to drive?

Regulatory safety advice indicates that due to the potential for drowsiness or other CNS side effects, users should exercise caution. It is generally advised that individuals avoid driving or operating heavy machinery if they experience sleepiness after using the cream.

Q: Is there a generic version of Metacain DS available?

According to regulatory and patient information sources, there are generic versions of the Lidocaine 2.5% and Prilocaine 2.5% eutectic mixture cream available on the market.

Q: Are there any restrictions on physical activity while taking Metacain DS?

Official patient leaflets do not place general restrictions on physical activity while the cream is applied. However, caution is advised to prevent accidental injury to the numb area and to avoid excessive heat exposure, which can increase the medicine's absorption into the body.

Q: What makes Metacain DS a targeted treatment?

The treatment is considered targeted because the active ingredients are applied directly to the skin's surface for a local effect. Their mechanism of action is to temporarily stabilize neuronal membranes to block the initiation and conduction of pain impulses only in that specific area, without affecting the body systemically.

How should Metacain DS be stored and disposed of?

How to Store and Dispose of Metacain DS

Metacain DS (Lidocaine 2.5% and Prilocaine 2.5% Cream) must be handled and stored in accordance with official regulatory requirements to ensure its stability and prevent accidental exposure.

Storage Requirements

The cream must be stored at controlled room temperature, specifically between 20 C and 25 C (68 F and 77 F). Storage must prevent freezing, excessive heat, moisture, and direct light. The product must be kept in a closed container and stored strictly out of the reach of children, pets, and others.

Disposal Instructions

Outdated or no longer needed medicine must be properly disposed of. If a drug take-back program is not available, the medicine should be removed from its original container, mixed with an undesirable substance (such as used coffee grounds), and placed into a sealed bag or container before being discarded in the household trash. The disposal process must ensure the product remains out of the reach of children and pets.

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

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