Emla cream 2.5/2.5%
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EMLA Cream is a topical local anesthetic used to numb the skin in order to decrease pain sensations before minor medical procedures, injections, taking of blood samples, or inserting an intravenous catheter. EMLA Cream is often used before receiving a tattoo. Even after application of EMLA Cream, you will have some sensations of pressure and touch on the area.
How Does EMLA Cream Work
The ingredients in EMLA Cream, lidocaine and prilocaine, are mixed together with other ingredients that allow the anesthetics to pass through the skin so the numbing effect can take place. The lidocaine and prilocaine work together to act directly on the nerve cells in that are of the skin to stop electrical impulses that cause pain from being passed along the nerve to the skin.
When and How is EMLA Cream Applied?
- You should thoroughly wash and dry the area where the EMLA Cream is to be applied.
- A thick layer should be patted onto the skin.
- Be sure not to rub the EMLA Cream into the skin.
- Do not use EMLA Cream on damaged skin or an open wound.
- Keep EMLA Cream away from eyes, nose, and mouth. Rinse with water if this should happen.
- Wash your hands right away after using EMLA Cream.
Side Effects of EMLA Cream
The most common side effects from the use of EMLA Cream are:
- Unusual skin sensations
- Change in hot or cold sensation
- Pale skin
- Swelling and redness at the site of application
When experience, these side effects are normally mild.
A more rare but severe side effect is an allergic reaction like itching, rash, trouble breathing, tightness in the chest, and swelling in mouth, face, lips, or tongue. You should seek medical attention if this happens to you while using EMLA Cream
Other Brand Names
Other brand names for EMLA Cream are: Oraquix. The generic name for EMLA Cream is lidocaine/w prilocaine.
There are certain medical conditions that could interact negatively with EMLA Cream. Be sure you let you healthcare provider know of any conditions, like the following:
- If you are pregnant or breastfeeding.
- What prescription and non-prescription medications you are taking.
- What, if any, allergies you may have to food, medicine, or anything else.
- What medical conditions you may have or if you are currently ill.
EMLA Cream comes two different size tubes: 5 gram and 30 gram.
A tube of EMLA Cream contains 2.5% lidocaine and 2.5% prilocaine.
Your doctor will tell you how much cream to apply to the area. Do not apply more than what the doctor recommends. You should not use EMLA Cream longer than what the doctor prescribes.
EMLA Cream is packaged in white tube, with blue print.
About Emla cream
What Emla cream is used for
EMLA Cream is used to create a temporary loss of feeling or numbness of the skin, and can be used:
on healthy, unbroken skin before minor skin surgery, or when getting a needle or having blood taken;
prior to vaccination with only the following vaccines: MMR (Measles-Mumps-Rubella), DPTP (Diptheria-Pertussis-Tetanus-Poliovirus), H. influenzae b or Hepatitis B;
on the genital mucosa;
for the cleansing of leg ulcers.
For best results talk to your doctor before using the cream on the genital mucosa or for leg ulcers.
What Emla cream does
EMLA is the brand name for a topical anesthetic that contains the drugs lidocaine and prilocaine. Topical anesthetics are used to cause a temporary loss of feeling or numbness of the skin at the area where it is applied.
When Emla cream should not be used
if you/your child have methemoglobinemia (a blood disorder);
on infants who required methemoglobin-inducing agents (e.g., sulfanomides) and are 12 months of age or younger;
if you/your child are allergic to lidocaine, prilocaine, any other “-caine” type anesthetics, or any of the nonmedicinal ingredients in the product (see What the important nonmedicinal ingredients are:);
on infants less than 3 months of age, unless instructed by your doctor.
What the medicinal ingredient is
lidocaine 2.5% and prilocaine 2.5%.
What the important nonmedicinal ingredients for Emla cream are
EMLA Cream also contains carboxypolymethylene, polyoxyethylene hydrogenated castor oil, and sodium hydroxide.
Tegaderm dressings contain polyether polyurethane films, acrylate adhesives and paper liners. These dressings are hypoallergenic and do not contain latex. (Tegaderm dressings are supplied with the 5 g EMLA Cream tube only).
What dosage forms Emla cream comes in
EMLA Cream: 5 g and 30 g tubes.
Warnings and Precautions
Serious Warnings and Precautions
EMLA Cream is for use on healthy, unbroken skin. Do not apply to open wounds, nor to burns or rashes or other skin conditions, including diaper rash.
BEFORE you use EMLA Cream talk to your doctor or pharmacist if:
if you/your child have glucose-6-phosphate dehydrogenase deficiency;
if you/your child have ever had a bad, unusual or allergic reaction to lidocaine or prilocaine, also available under brand names such as Xylocaine (lidocaine) and Citanest (prilocaine);
if you think you/your child may be sensitive or allergic to other ingredients of the cream or Tegaderm dressing (see What the important nonmedicinal ingredients are:);
if there is an infection, skin rash or cut at, or near, the area where you want to apply EMLA Cream;
if you/your child have dermatitis or any other skin problems or diseases;
if you/your child have severe kidney or liver disease (see Proper Use of This Medication:);
if you are pregnant, trying to become pregnant or are breast-feeding;
if you would like to use EMLA Cream prior to treatment of a leg ulcer(s);
if you would like to use EMLA Cream on the genital area of children.
Interactions with Emla cream
Tell your doctor or pharmacist about any other drugs you take or have recently taken, including the ones you can buy without a prescription, including:
antiarrhythmic drugs for heart problems (e.g. mexilitine, amiodarone);
other drugs which may trigger methomoglobin formation, including: sulfonamides, acetanilide, aniline dyes, benzocaine (or other “-caine” type anesthetics), chloroquine, dapsone, naphthalene, nitrates or nitrites, nitrofurantoin, nitroglycerin, nitroprusside, pamaquine, para-aminosalicylic acid, phenacetin, phenobarbital, phenytoin, primaquine, quinine and high doses of acetaminophen.
Proper Use of Emla cream
If your doctor tells you to use EMLA Cream, follow your doctor's instructions for use. In any other situation, follow the directions below.
Do not put EMLA Cream near the eyes, as it may cause some irritation. If you accidentally get EMLA in the eye, rinse it well with lukewarm water and protect it until sensation returns.
Do not apply EMLA Cream inside the ear. Do not put EMLA Cream in the mouth, or swallow it. If EMLA Cream is accidentally swallowed, call your doctor.
Do not re-use EMLA Cream or dressings.
The numbing effect of EMLA starts working about 1 hour after it is applied. You may still feel pressure and touch in the area where you apply EMLA. The numbness of the skin may continue to increase after the cream is removed, and will last for at least 2 hours following a 1-2 hour application.
For minor procedures on skin such as surgical treatment of lesions or when getting a needle or having blood taken, apply a thick layer of cream, about half of a 5 g tube (2 g). After covering EMLA Cream with an air-tight dressing, leave on for at least 1 hour. It is important to cover EMLA Cream with an air-tight dressing to ensure that the cream penetrates the skin properly and numbness of the area is felt.
Your doctor may use EMLA Cream on larger areas for such procedures as split-skin grafting. If you are instructed by the doctor to apply EMLA Cream yourself for this procedure, apply a thick layer of cream to the area to be treated (about 1.5 to 2 g/10 cm2; a 10 cm2 area is a little larger than the size of a two dollar coin or "toonie"). Leave the EMLA Cream on for at least 2 hours.
You will not get any added benefit from leaving EMLA Cream on for longer than 5 hours.
Half a 5 g tube corresponds to about 2 g EMLA Cream.
1 g of EMLA Cream administered from the 30 g aluminium tube is equivalent to a ribbon of cream of approximately 3.5 cm (or approximately 1.5 inches).
Conditions where adjustments in dose may be required
acutely ill patients
patients with severe liver disease
patients with severe kidney disease
patients also treated with other anesthetics or certain antiarrhythmic drugs (e.g. mexilitine, amiodarone)
EMLA should be used with caution in these patients, who may be more sensitive to the effects of lidocaine and prilocaine.
For children under the age of 6: take care not to apply more EMLA Cream or give it more frequently than the doctor recommended. Please make sure that your child does not ingest any of the cream.
When using EMLA Cream for your child's pain relief, remember it is also very important to provide comfort and emotional support.
For minor skin procedures. It is important to cover EMLA Cream with an air-tight dressing to ensure that the cream penetrates the skin properly and numbness of the area is felt.
In children, EMLA Cream should only be applied to healthy, unbroken skin.
Do not apply EMLA Cream to infants under 3 months of age unless a doctor tells you to do so. Infants under 3 months of age are at a higher risk than older children for methemoglobinemia. This is a condition in which there is not enough oxygen in the blood, and it can be caused by an overdose of EMLA.
Be careful to apply no more than the maximum indicated dose of EMLA Cream.
Neonates Under the Age of 3 Months (ONLY IF INSTRUCTED BY A DOCTOR)
Apply up to 1 g of cream on a skin area not larger than 10 cm2 (a little larger than the size of a two dollar coin or “toonie”). After covering EMLA Cream with an air-tight dressing, leave on for 1 hour. DO NOT LEAVE EMLA ON THE SKIN FOR LONGER THAN 1 HOUR.
Infants Between 3 and 12 Months of Age
Apply up to 2 g of cream on a total skin area not larger than 20 cm2 (a little larger than the size of a credit card). After covering EMLA Cream with an air-tight dressing, leave on for at least 1 hour. Do not leave on the skin for more than 4 hours.
Children Between 1-6 Years
Apply up to 10 g of cream on a total skin area not larger than 100 cm2 (a little larger than the size of two credit cards). After covering EMLA Cream with an air-tight dressing, leave on for at least 1 hour. Do not leave on the skin for more than 5 hours.
Children Between 7-12 Years
Apply up to 20 g of cream on a total skin area not larger than 200 cm2 (a little larger than a standard postcard). After covering EMLA Cream with an air-tight dressing, leave on for at least 1 hour. Do not leave on the skin for more than 5 hours.
Dosage of EMLA Cream on Leg Ulcers
Talk to your doctor before using EMLA Cream on leg ulcers.
Large doses of EMLA Cream and EMLA Patch should be used with caution in patients receiving other local anesthetics or agents structurally related to amide-type local anesthetics (e.g. antiarrhythmics such as mexiletine), as the toxic effects are additive.
Prilocaine, a component of EMLA, accentuates the formation of methemoglobin (MetHb) by a mechanism involving metabolism of prilocaine to o-toluidine and subsequent oxidation of hemoglobin to MetHb. The in vivo reduction of MetHb back to O2Hb is dependent on the presence of MetHb reductase.
In patients treated concomitantly with EMLA and other methemoglobin-inducing agents including but not limited to sulfonamides, acetanilid, aniline dyes, benzocaine, chloroquine, dapsone, naphthalene, nitrates and nitrites, nitrofurantoin, nitroglycerin, nitroprusside, pamaquine, para-aminosalicylic acid, phenacetin, phenobarbital, phenytoin, primaquine and quinine, EMLA may induce the formation of methemoglobin and result in overt clinical signs of methemoglobinemia (see Contraindications and Overdosage).
Acetaminophen has been shown to induce methemoglobin formation in vitro and in animals. In humans, methemoglobin formation is very rare at therapeutic doses and overdoses of acetaminophen.
Caution is advised when using Class III antiarrhythmic drugs concomitantly with EMLA due to potential pharmacodynamic or pharmacokinetic interactions, or both. A drug interaction study has shown that the plasma concentration of lidocaine may be increased following administration of a therapeutic dose of intravenous lidocaine to patients treated with amiodarone (n=6). Case reports have described symptoms of lidocaine toxicity in patients treated concomitantly with lidocaine and amiodarone. Patients treated with Class III antiarrhythmic drugs (e.g. amiodarone) should be kept under close surveillance and ECG monitoring should be considered, since cardiac effects of these drugs and EMLA Cream may be additive.
Class 1 antiarrhythmic drugs (such as mexiletine) should be used with caution since toxic effects are additive and potentially synergistic (see Contraindications regarding infants, Adverse Reactions, and Overdosage).
Lidocaine is mainly metabolized in the liver to its two major pharmacologically active metabolites, monoethylglycinexylidine (MEGX) and glycinexylidine (GX), by CYP1A2 and CYP3A4 and has a high hepatic extraction ratio. Prilocaine is mainly metabolized to o-toluidine in the liver, by unestablished mechanisms. Only a small proportion (2-5%) of lidocaine and prilocaine is excreted unchanged in the urine. The hepatic clearance of lidocaine, and probably prilocaine, is expected to depend largely on blood flow.
With the low systemic exposure to lidocaine and prilocaine and short duration of topical application of EMLA (lidocaine and prilocaine), metabolic drug-drug interactions of clinical significance with lidocaine or prilocaine are unlikely.
Clinically relevant pharmacodynamic drug interactions may occur with EMLA and other local anesthetics or structurally related drugs, and Class I and Class III antiarrhythmic drugs due to additive effects.
Metabolism of prilocaine can accentuate the formation of methemoglobin. Co-administration of EMLA and other methemoglobin-inducing agents to patients 12 months of age or younger may result in clinical signs of methemoglobinemia (see Contraindications, Warnings and Precautions, Drug Interactions, Adverse Reactions).
Information for the Patient
Dosage and Administration
Conditions where dosing may require adjustment:
in acutely ill, debilitated or elderly patients, and patients with severe hepatic impairment who are more sensitive to systemic effects due to increased blood levels of lidocaine and prilocaine from repeated doses of EMLA (lidocaine and prilocaine)
in patients who are administered other local anesthetics or amide type local anesthetics (see Drug Interactions)
in debilitated patients, or those with impaired elimination, smaller application areas are recommended to avoid toxicity. Decreased duration of application is not recommended as this may decrease the analgesic effect
|Apply patch(es) only to selected skin area(s) <10 cm2 a. Remove patch and clean the area thoroughly prior to procedure.|
|Neonates 0 up to 3 months or <5 kgb , c||1 patch applied for approx. 1 hour. Maximum 1-hour applicationd. No more than 1 patch applied at the same time. The safety of repeated dosing has not been established.|
|Infants 3 up to 12 monthsc and >5 kg||Patch applied for approx. 1 hourd. Maximum 4-hour application. No more than 2 patches applied at the same timee.|
|Children 1–6 years and >10 kg||One or more patches applied for a minimum of 1 hour. Maximum 5-hour applicationf. Maximum dose is 10 g (10 patches).|
|Children 7–12 years and >20 kg||One or more patches applied for a minimum of 1 hour. Maximum 5-hour applicationf. Maximum dose is 20 g (20 patches).|
b. Infants less than 3 months of age are at higher risk of methemoglobinemia due to immature reductase enzyme pathways.
c. Until further clinical data is available, EMLA should not be used in infants who require treatment with methemoglobin-inducing agents, i.e., sulfonamides, and are 12 months of age or younger.
d. The safety of a longer application time has not been established.
e. No clinically significant increase in methemoglobin levels has been observed after an application time of up to 4 hours on 16 cm2.
f. There is no benefit to application times longer than 5 hours, as the analgesic effectiveness of the cream in the patch dissipates over time.
Please note: If a patient greater than 3 months old does not meet the minimum weight requirement, the maximum total dose of EMLA Patch should be restricted to that which corresponds to the patient's weight.
See Information for the Patient—Instructions for Application.
The adverse drug reactions included below for EMLA (lidocaine and prilocaine) represent data from both clinical and post-marketing experience (see Table 1).
Indications and Clinical Use
EMLA CREAM (Lidocaine 2.5% and Prilocaine 2.5%) is indicated for use in:
Topical analgesia of intact skin in connection with:
needle insertion, e.g., i.v. catheters or prior to blood sampling;
vaccination with only the following vaccines that have been shown not to interact with EMLA in clinical trials: MMR, DPTP, H. influenzae b and Hepatitis B. Since the effect of EMLA on the immune response to any other vaccine is unknown, it cannot be recommended for use with other vaccines;
superficial surgical procedures, e.g., removal of molluscum contagiosum, split skin grafting, electrolysis;
Topical analgesia of genital mucosa in connection with:
local infiltration anesthesia;
surgical procedures lasting not longer than 10 minutes on small superficial localized lesions, e.g., removal of condylomata by laser or cautery, and biopsies.
Topical analgesia of leg ulcers in connection with:
mechanical/sharp cleansing/debridement, e.g., the removal of necrotic tissue and debris by curettes, scissors, tweezers, etc.
EMLA PATCH (Lidocaine 2.5% and Prilocaine 2.5%) is indicated for use in:
Topical analgesia of intact skin in connection with:
needle insertion, e.g., i.v. catheters or prior to blood sampling;
vaccination with only the following vaccines that have been shown not to interact with EMLA in clinical trials: MMR, DPTP, H. influenzae b and Hepatitis B. Since the effect of EMLA on the immune response to any other vaccine is unknown, it cannot be recommended for use with other vaccines.
Local anesthetic toxicity is manifested by symptoms of nervous system excitation and in severe cases, central nervous and cardiovascular depression.
In the unlikely event of toxicity following epidermal application of EMLA (lidocaine and prilocaine), signs of systemic toxicity anticipated would be similar in nature to those observed following other routes of administration of local anesthetics.
Rare cases of methemoglobinemia have been reported.
Mild methemoglobinemia is characterized by tissue cyanosis, a bluish-grey or brownish discoloration of the skin, especially around the lips and nail beds, which is not reversed by breathing 100% oxygen. Clinical signs may also include pallor and marbleization.
Severe methemoglobinemia (MetHb concentrations above approximately 25%) is associated with signs of hypoxemia, ie. dyspnea, tachycardia and depression of consciousness.
Drug-induced methemoglobinemia may occur with the use of drugs including but not limited to sulfonamides, acetanilid, aniline dyes, benzocaine, chloroquine, dapsone, naphthalene, nitrates and nitrites, nitrofurantoin, nitroglycerin, nitroprusside, pamaquine, para-aminosalicylic acid, phenacetin, phenobarbital, phenytoin, primaquine and quinine.
Acetaminophen has been shown to induce methemoglobin formation in vitro and in animals. In humans, methemoglobin formation is very rare at therapeutic doses and overdoses of acetaminophen.
It should be kept in mind that EMLA is contraindicated for patients with congenital or idiopathic methemoglobinemia and for infants 12 months of age or younger who require treatment with methemoglobin-inducing drugs. Patients with glucose-6-phosphate dehydrogenase deficiency are more susceptible to drug-induced methemoglobinemia (see also Contraindications, Warnings and Precautions).
Severe neurological symptoms (convulsions, CNS depression) must be treated symptomatically by respiratory support and the administration of anticonvulsive drugs.
In neonates, methemoglobin concentrations of up to 5-6% are not considered to be of clinical significance, with treatment of symptomatic methemoglobinemia not typically necessary unless methemoglobin concentrations are above 25-30%. However, the severity of clinical symptoms should be the primary consideration in the decision to initiate treatment, rather than the level of methemoglobin. Most patients recovered spontaneously after removal of the cream. Methemoglobinemia may be treated with a slow intravenous injection of methylene blue. It has been reported in published literature that methylene blue should be used cautiously as a treatment for methemoglobinemia in patients with glucose-6-phosphate dehydrogenase deficiency because it may not be effective for these patients and may cause hemolytic anemia.
There are anecdotal reports of patients consuming EMLA Cream or Patches; all cases resolved without serious injury. Such patients should be monitored for symptoms of systemic toxicity.
Class 1 antiarrhythmic drugs (such as mexiletine) should be used with caution since the toxic effects are additive and potentially synergistic.
Dosage Forms, Composition and Packaging
Each g of cream (5%) contains: lidocaine 25 mg and prilocaine 25 mg as a 1:1 oil/water emulsion. Nonmedicinal ingredients: carboxypolymethylene, polyoxyethylene hydrogenated castor oil, purified water and sodium hydroxide to adjust pH to 8.7 to 9.7. Aluminum tubes of 5 g with 2 occlusive dressings and tubes of 30 g without dressings.
Each single dose unit patch in the form of an occlusive dressing contains: lidocaine 25 mg and prilocaine 25 mg. It is composed of a laminate backing, an absorbent cellulose disc, and an adhesive tape ring. The disc contains 1 g of the EMLA emulsion, the active contact surface area being approximately 10 cm2. The surface area of the entire patch is approximately 40 cm2. Nonmedicinal ingredients: carboxypolymethylene, polyoxyethylene hydrogenated castor oil, purified water and sodium hydroxide to adjust pH to 8.7-9.7; patch components: cellulose and cotton disc, polyethylene foam with acrylate adhesive, polyamide/aluminium/plastic and polypropylene/aluminium/plastic laminates. Boxes of 2 and 20 single-use patches.
Warnings and Precautions
Greater sensitivity of some older individuals cannot be ruled out. There are insufficient data to evaluate quantitative differences in systemic plasma levels of lidocaine and prilocaine between geriatric and non-geriatric patients following application of EMLA.
During intravenous studies, the elimination half-life of lidocaine was statistically significantly longer in elderly patients (2.5 hours) than in younger patients (1.5 hours).
No studies are available on the intravenous pharmacokinetics of prilocaine in elderly patients (see Action and Clinical Pharmacology).
In individuals with normal renal function, the extent of systemic absorption of lidocaine and prilocaine is low, 5-14% after cutaneous application, higher on genital mucosa and leg ulcer. Only a small fraction of lidocaine and prilocaine (2-5%) is excreted unchanged in the urine, as the primary metabolism occurs in the liver (see Action and Clinical Pharmacology). The pharmacokinetics of lidocaine and its main metabolite were not altered significantly in haemodialysis patients (n=4) who received an intravenous dose of lidocaine. Therefore, renal impairment is not expected to significantly affect the pharmacokinetics of lidocaine and prilocaine when EMLA is used according to dosage instructions (see Dosage and Administration).
Should EMLA be used concomitantly with other products containing lidocaine and/or priolocaine during labor and delivery, the total dose contributed by all formulations should be considered.
EMLA is contraindicated for patients with congenital or idiopathic methemoglobinemia and for infants 12 months of age or younger who require treatment with methemoglobin-inducing drugs (see also Contraindications). Patients with glucose-6-phosphate dehydrogenase deficiency are more susceptible to drug-induced methemoglobinemia.
Patients who are acutely ill, debilitated or elderly, and patients with severe hepatic impairment may require dosing adjustments commensurate with age, weight and physical condition, because they may be more sensitive to systemic effects due to increased blood levels of lidocaine and prilocaine following repeated doses of EMLA (see also Dosage and Administration).
The active substances in EMLA, lidocaine and prilocaine, have not been evaluated for carcinogenicity in animal studies following topical application; neither has EMLA the eutectic mixture of lidocaine and prilocaine bases. Metabolites of prilocaine have been shown to be carcinogenic after life-time, once-daily oral exposure in laboratory animals.
Chronic oral toxicity studies of o-toluidine, a metabolite of prilocaine, in mice (150-2400 mg/kg) and rats (150-800 mg/kg) have shown that o-toluidine is a carcinogen in both species at all doses tested. A non-carcinogenic dose in rats or mice has not been established. The lowest tumor-inducing dose tested in animals (150 mg/kg) corresponds to approximately 30 times the amount of o-toluidine to which a 50 kg subject would be exposed following the application of 60 g of EMLA Cream for 24 hours on the intact skin, assuming an extent of absorption of 30%, and 100% conversion to o-toluidine. Based on a yearly exposure (once daily dosing with o-toluidine in animals and 5 treatment sessions with 60 g EMLA Cream in humans), the safety margins would be approximately 2200 times when comparing the exposure in animals to man.
Genotoxicity tests with lidocaine showed no evidence of mutagenic potential. A metabolite of lidocaine, 2,6-xylidine, showed weak evidence of activity in some genotoxicity tests. A chronic oral toxicity study of the metabolite 2,6-xylidine (0, 14, 45, 135 mg/kg) administered in feed to rats showed that there was a significantly greater incidence of nasal cavity tumors in male and female animals that had daily oral exposure to the highest dose of 2,6-xylidine for 2 years. The lowest tumor-inducing dose tested in animals (135 mg/kg) corresponds to approximately 60 times the amount of 2,6-xylidine to which a 50 kg subject would be exposed following the application of 60 g of EMLA Cream for 24 hours on the intact skin, assuming an extent of absorption of 15%, and 80% conversion to 2,6-xylidine. Based on a yearly exposure (once daily dosing with 2,6-xylidine in animals and 5 treatment sessions with 60 g EMLA Cream in humans), the safety margins would be approximately 4700 times when comparing the exposure in animals to man.
Repeated doses of EMLA (lidocaine and prilocaine) may increase blood levels of lidocaine and prilocaine. EMLA should be used with caution in patients who may be more sensitive to the systemic effects of lidocaine and prilocaine including acutely ill, debilitated, or elderly patients, and patients with severe hepatic impairment (see Dosage and Administration).
Due to insufficient data on absorption, EMLA should not be applied to open wounds as a result of trauma. Note: Leg ulcers often follow a slight trauma but are not classified as traumatic wounds.
Special care should also be employed to ensure the occlusive bandage or patch is secure. This will avoid accidental dislocation and exposure of EMLA, especially in young children.
EMLA is not recommended in any clinical situation where it can penetrate or migrate into the middle ear. Tests on laboratory animals (guinea pigs) have shown that EMLA has an ototoxic effect when instilled into the middle ear. When the same animals were exposed to EMLA in the external auditory canal, no abnormalities were seen. EMLA causes minor structural damage to the tympanic membrane in rats when applied directly to the membrane.
Care should be taken when applying EMLA to patients with atopic dermatitis. A more rapid and greater absorption through the skin is observed in these patients. A shorter application time should be used (see Action and Clinical Pharmacology). There have been two reports of purpura at the application site after 60 minutes. After a repeated application of 30 minutes in one of these patients, no reaction was seen. There are not sufficient data available to characterize absorption or local reactions, nor to permit dosing recommendations.
EMLA should not be applied to, or near to, the eyes as it causes corneal irritation if it comes into contact with the cornea. This reaction may be reversible. In addition, the loss of protective reflexes may allow corneal irritation and potential abrasion. Take care to avoid accidental contact of EMLA with the eyes (e.g., rubbing the eyes after using fingers to apply EMLA elsewhere), as the analgesic effect may result in damage from undetected foreign bodies. If eye contact does occur, immediately rinse the eye in water or sodium chloride solution and protect the eye until sensation returns.
EMLA should not be applied to the genital mucosa of children or infants due to insufficient data on absorption.
In infants below the age of 3 months, the capacity of the MetHb reductase is lower than in older children and in adults. A transient, clinically insignificant increase in methemoglobin levels is commonly observed up to 12 hours after an application of EMLA.
EMLA should not be used:
in patients with congenital or idiopathic methemoglobinemia;
in infants who require treatment with methemoglobin-inducing agents such as sulfonamides, and are 12 months of age or younger (see also Contraindications, Warnings and Precautions, Drug Interactions, Adverse Reactions);
in preterm infants (defined as a gestational age less than 37 weeks).
Parents should be reminded of the importance of emotional and psychological support of younger children undergoing medical or surgical procedures.
When using EMLA in younger children, especially infants under the age of 3 months, care must be taken to ensure that the caregiver understands the need to limit the dose and area of application and to prevent accidental ingestion (see Dosage and Administration).
In neonates (minimum gestation age: 37 weeks) and children weighing less than 20 kg, the area and duration of application should be limited (see Dosage and Administration, EMLA Cream).
The safety of EMLA during pregnancy has not been established in humans. Lidocaine and prilocaine cross the placental barrier and may be absorbed by the fetal tissues. It is reasonable to assume that lidocaine and prilocaine have been used in a large number of pregnant women and women of child-bearing age. No specific disturbances to the reproductive process have so far been reported, e.g., an increased incidence of malformations or other directly or indirectly harmful effects on the fetus. However, care should be given during early pregnancy when maximum organogenesis takes place.
Lidocaine and, in all probability, prilocaine, are excreted in human milk, but in such small quantities that there is generally no risk of the infant being affected at therapeutic dose levels due to low systemic absorption.
Because amide-type local anesthetics are metabolized by the liver, these drugs, especially repeated doses, should be used cautiously in patients with hepatic disease. For patients with severe hepatic disease, a reduced capacity to metabolize local anesthetics may increase the risk of developing toxic plasma concentrations (see Dosage and Administration).
Lidocaine and prilocaine have been shown to inhibit viral and bacterial growth. The effect of EMLA on intradermal injections of live vaccines has not been determined.
Storage and Stability
EMLA Cream (lidocaine and prilocaine) in aluminium tubes should be stored at room temperature (15-30°C). Protect from freezing.
EMLA Patch (lidocaine and prilocaine) should be stored at room temperature (15-30°C). Protect from freezing. Single use. Do not reuse.
Action and Clinical Pharmacology
EMLA (Eutectic Mixture of Local Anesthetics) (lidocaine and prilocaine) is a 1:1 oil/water emulsion of a eutectic mixture of lidocaine and prilocaine bases. Dermal analgesia is a result of the migration of lidocaine and prilocaine into the epidermal and dermal layers of the skin followed by the accumulation of these agents in the vicinity of dermal pain receptors and nerve endings. Lidocaine and prilocaine are both amide-type local anesthetic agents. They stabilize the neuronal membrane preventing the initiation and conduction of nerve impulses, thereby effecting local anesthetic action. EMLA provides dermal analgesia; the depth of which depends upon the application time and the applied dose. Analgesia may be less for deeper structures.
EMLA may produce a transient biphasic vascular response involving initial vasoconstriction followed by vasodilation at the application site (see Adverse Reactions). In patients with atopic dermatitis, a shorter biphasic response involving initial vasoconstriction followed by vasodilation may be seen. Erythema may be observed after 30 to 60 minutes.
Systemic absorption of lidocaine and prilocaine from EMLA is dependent upon several factors, including: the applied dose, duration of application, the thickness and vascularity of the skin in the area of application, and the presence of any condition in which the skin is not healthy and intact (e.g. sunburn, rash or leg ulcers).
Prilocaine has a larger distribution volume than lidocaine which results in lower plasma concentrations of prilocaine when equal amounts of prilocaine and lidocaine are administered. At concentrations produced by application of EMLA, lidocaine is approximately 60-80% bound to plasma proteins, primarily alpha-1-acid glycoprotein. At much higher plasma concentrations (1 to 4 µg/mL of free base), the plasma protein binding of lidocaine is concentration dependent. Prilocaine is 55% bound to plasma proteins.
It is not known if lidocaine or prilocaine are metabolized in the skin. Lidocaine is metabolized rapidly by the liver to a number of metabolites including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both of which have pharmacologic activity similar to, but less potent than that of lidocaine. Prilocaine is metabolized in both the liver and kidneys by amidases to various metabolites including ortho-toluidine and N-n-propylalanine.
There is considerable inter-subject variability in lidocaine and prilocaine plasma levels. In pre-marketing studies, all plasma levels of lidocaine and prilocaine after topical administration of EMLA products have been found to be below 1.2 μg/mL. These are below the levels associated with systemic toxicity (5 μg/mL).
It is well known that patients with atopic dermatitis show abnormal vascular reactions to pharmacological stimuli. In patients with atopic dermatitis, percutaneous absorption of EMLA is more rapid and greater than in normal skin. In two patients, within one hour after application of 4-6 g EMLA to a 25 cm2 area of the forearm, lidocaine and prilocaine plasma levels were higher than those observed in normal skin. However, in these patients, the systemic plasma levels were 100 times lower than those associated with toxicity. In patients with atopic dermatitis, a shorter application time should be used (see Warnings and Precautions, Skin). It should be noted, however, that dermatological procedures were not performed in the above patients. Clinical data are not available at present to permit dosage recommendations.
The half-life of lidocaine elimination from the plasma following IV administration is approximately 65 to 150 minutes (mean 110,±24 SD, n=13). More than 98% of an absorbed dose of lidocaine can be recovered in the urine as metabolites or parent drug. The systemic clearance is 10 to 20 mL/min/kg (mean 13,±3 SD, n=13). The elimination half-life of prilocaine is approximately 10 to 150 minutes (mean 70,±48 SD, n=13). The systemic clearance is 18 to 64 mL/min/kg (mean 38,±15 SD, n=13).
During intravenous studies, the elimination half-life of lidocaine was statistically significantly longer in elderly patients (2.5 hours) than in younger patients (1.5 hours). No studies are available on the intravenous pharmacokinetics of prilocaine in elderly patients (see Warnings and Precautions, Geriatrics).
EMLA (lidocaine and prilocaine) is contraindicated in:
patients who are hypersensitive to local anesthetics of the amide type or to any ingredients in the formulation (see Dosage Forms, Composition and Packaging);
patients with congenital or idiopathic methemoglobinemia;
infants who require treatment with methemoglobin-inducing agents, e.g., sulfonamides, and are 12 months of age or younger (see Drug Interactions);
preterm infants (defined as gestational age less than 37 weeks).