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Lidocaine and Prilocaine

Pronunciation

(LYE doe kane & PRIL oh kane)

Index Terms

  • Lidocaine/Prilocaine
  • Prilocaine and Lidocaine

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Cream, topical:

EMLA: Lidocaine 2.5% and prilocaine 2.5% (5 g [DSC], 30 g [DSC])

DermacinRx Prizopak: Lidocaine 2.5% and prilocaine 2.5% (3 x 30 g) [packaged with occlusive dressing]

Leva Set: Lidocaine 2.5% and prilocaine 2.5% (3 x 30 g [DSC]) [packaged with occlusive dressing]

Lidopril: Lidocaine 2.5% and prilocaine 2.5% (3 x 30 g) [packaged with occlusive dressing]

Lidopril XR: Lidocaine 2.5% and prilocaine 2.5% (2 x 30 g) [packaged with occlusive dressing]

Livixil Pak: Lidocaine 2.5% and prilocaine 2.5% (3 x 30 g) [packaged with occlusive dressing]

LP Lite Pak: Lidocaine 2.5% and prilocaine 2.5% (2 x 30 g) [packaged with occlusive dressing]

Medolor Pak: Lidocaine 2.5% and prilocaine 2.5% (3 x 30 g) [packaged with occlusive dressing]

Prilolid: Lidocaine 2.5% and prilocaine 2.5% (1 x 30 g) [packaged with occlusive dressing]

Relador Pak: Lidocaine 2.5% and prilocaine 2.5% (3 x 30 g) [packaged with occlusive dressing]

Venipuncture CPI: Lidocaine 2.5% and prilocaine 2.5% (5 g)

Generic: Lidocaine 2.5% and prilocaine 2.5% (5 g, 30 g, 5800 g, 18,000 g)

Gel, periodontal:

Oraqix: Lidocaine 2.5% and prilocaine 2.5% (1.7 g)

Brand Names: U.S.

  • DermacinRx Prizopak
  • EMLA [DSC]
  • Leva Set [DSC]
  • Lidopril
  • Lidopril XR
  • Livixil Pak
  • LP Lite Pak
  • Medolor Pak
  • Oraqix
  • Prilolid
  • Relador Pak
  • Venipuncture CPI

Pharmacologic Category

  • Local Anesthetic

Pharmacology

Local anesthetic action occurs by stabilization of neuronal membranes and inhibiting the ionic fluxes required for the initiation and conduction of impulses

Absorption

EMLA: Related to duration of application and area where applied

3-hour application: 3.6% lidocaine and 6.1% prilocaine

24-hour application: 16.2% lidocaine and 33.5% prilocaine

Onset of Action

EMLA: 1 hour (more rapid in genital mucosa: 5 to 10 minutes); Peak effect: 2 to 3 hours

Oraqix: ≤30 seconds

Duration of Action

EMLA: 1 to 2 hours after removal; Genital mucosa: 15 to 20 minutes after application (range: 5 to 45 minutes)

Oraqix: ~20 minutes

Use: Labeled Indications

US labeling:

Cream: Topical anesthetic for use on normal intact skin to provide local analgesia; for use on genital mucous membranes for superficial minor surgery; and as pretreatment for infiltration anesthesia.

Periodontal gel: Topical anesthetic for use in periodontal pockets during scaling and/or root planing procedures

Canadian labeling:

Cream: Topical anesthetic for use on intact skin in connection with: IV cannulation or venipuncture; superficial surgical procedures (eg, split skin grafting, electrolysis, removal of molluscum contagiosum); laser treatment for superficial skin surgery (eg, telangiectasia, port wine stains, warts, moles, skin nodules, scar tissue); surgical procedures of genital mucosa (≤10 minutes) on small superficial localized lesions (eg, removal of condylomata by laser or cautery, biopsies); local infiltration anesthesia in genital mucous membranes; mechanical cleansing/debridement of leg ulcers; vaccination with measles-mumps-rubella (MMR), diphtheria-pertussis-tetanus-poliovirus (DPTP), Haemophilus influenzae b, and hepatitis B.

Patch: Topical anesthetic for use on intact skin in connection with IV cannulation or venipuncture; vaccination with measles-mumps-rubella (MMR), diphtheria-pertussis-tetanus-poliovirus (DPTP), Haemophilus influenzae b, and hepatitis B.

Periodontal gel: Topical anesthetic for use in periodontal pockets during scaling and/or root planing procedures

Contraindications

Hypersensitivity to local anesthetics of the amide type or any component of the formulation

Canadian labeling: Additional contraindications (not in US labeling): Congenital or idiopathic methemoglobinemia.

Cream and patch only: Infants ≤12 months of age who require treatment with methemoglobin-inducing agents; preterm infants (gestational age <37 weeks); procedures requiring large amounts over a large body area that are not conducted in a facility with health care professionals trained in the diagnosis and management of dose-related toxicity and other acute emergencies, and with appropriate resuscitative treatments and equipment.

Dosing: Adult

Anesthetic: Topical:

Cream (intact skin): Note: Apply a thick layer to intact skin and cover with an occlusive dressing. Dermal analgesia can be expected to increase for up to 3 hours under occlusive dressing and persist for 1 to 2 hours after removal of the cream.

US labeling:

Minor dermal procedures (eg, IV cannulation or venipuncture): Apply 2.5 g (1/2 of the 5 g tube) over 20 to 25 cm2 of skin surface area) for at least 1 hour

Major dermal procedures (eg, more painful dermatological procedures involving a larger skin area such as split thickness skin graft harvesting): Apply 2 g per 10 cm2 of skin and allow to remain in contact with the skin for at least 2 hours.

Adult male genital skin (eg, pretreatment prior to local anesthetic infiltration): Apply 1 g per 10 cm2 to the skin surface for 15 minutes. Local anesthetic infiltration should be performed immediately after removal of cream.

Adult female genital mucous membranes: Minor procedures (eg, removal of condylomata acuminata, pretreatment for local anesthetic infiltration): Apply 5 to 10 g for 5 to 10 minutes. The local anesthetic infiltration or procedure should be performed immediately after removal of cream.

Canadian labeling:

Minor dermal procedures (eg, IV cannulation, venipuncture, surgical or laser treatment): Apply 2 g (~1/2 of the 5 g tube) over ~13.5 cm2 for at least 1 hour but no longer than 5 hours

Major dermal procedures (eg, split-skin grafting): 1.5 to 2 g per 10 cm2 (maximum: 60 g per 400 cm2) for at least 2 hours but no longer than 5 hours

Genital mucosa (eg, surgical procedures ≤10 minutes such as localized wart removal, and prior to local anesthetic infiltration): Apply 2 g (~1/2 of 5 g tube) per lesion (maximum: 10 g) for 5 to 10 minutes. Initiate procedure immediately after removing cream.

Leg ulcers (eg, mechanical cleansing/surgical debridement): Apply ~1 to 2 g per 10 cm2 (maximum: 10 g) for at least 30 minutes and up to 60 minutes for necrotic tissue that is more difficult to penetrate. Initiate procedure immediately after removing cream.

Periodontal gel (Oraqix): Apply on gingival margin around selected teeth using the blunt-tipped applicator included in package. Wait 30 seconds, then fill the periodontal pockets using the blunt-tipped applicator until gel becomes visible at the gingival margin. Wait another 30 seconds before starting treatment. May reapply; maximum recommended dose: One treatment session: 5 cartridges (8.5 g)

Transdermal patch [Canadian product]: Minor procedures (eg, needle insertion): Apply 1 or more patches to intact skin surface area <10 cm2 for at least 1 hour (maximum application time: 5 hours)

Dosing: Geriatric

Smaller areas of treatment may be necessary depending on status of patient (eg, debilitated, impaired hepatic function). Refer to adult dosing.

Dosing: Pediatric

Although the incidence of systemic adverse effects is very low, caution should be exercised, particularly when applying over large areas and leaving on for >2 hours

Local anesthetic (procedures): Infants and Children (intact skin): Topical: Note: If a patient >3 months of age does not meet the minimum weight requirement, the maximum total dose should be restricted to the corresponding maximum based on patient weight.

Cream: Should not be used in neonates with a gestation age <37 weeks nor in infants <12 months of age who are receiving treatment with methemoglobin-inducing agents

Dosing is based on child's age and weight:

Age 0 to 3 months or <5 kg: Apply a maximum of 1 g over no more than 10 cm2 of skin; leave on for no longer than 1 hour

Age 3 months to 12 months and >5 kg: Apply no more than a maximum 2 g total over no more than 20 cm2 of skin; leave on for no longer than 4 hours

Age 1 to 6 years and >10 kg: Apply no more than a maximum of 10 g total over no more than 100 cm2 of skin. US labeling recommends leaving on for no longer than 4 hours. Canadian labeling recommends leaving on for no longer than 5 hours.

Age 7 to 12 years and >20 kg: Apply no more than a maximum 20 g total over no more than 200 cm2 of skin. US labeling recommends leaving on for no longer than 4 hours. Canadian labeling recommends leaving on for no longer than 5 hours.

Transdermal patch [Canadian product]: Note: Should not be used in neonates with a gestation age <37 weeks nor in infants <12 months of age who are receiving treatment with methemoglobin-inducing agents

Dosing is based on child's age and weight: Apply patch(es) to skin area(s) <10 cm2:

Age 0 to 3 months or <5 kg: Apply 1 patch and leave on for ~1 hour (do not exceed 1-hour application time); do not apply more than 1 patch at same time; safety of repeated dosing not established

Age 3 months to 12 months and >5 kg: Apply 1 to 2 patches for ~1 hour (maximum application time: 4 hours); do not apply more than 2 patches at the same time

Age 1 to 6 years and >10 kg: Apply 1 or more patches for minimum of 1 hour (maximum application time: 5 hours); maximum dose: 10 patches

Age 7 to 12 years and >20 kg: Apply 1 or more patches for a minimum of 1 hour (maximum application time: 5 hours); maximum dose: 20 patches

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer labeling. Lidocaine and prilocaine primarily undergo hepatic metabolism and their pharmacokinetics are not expected to be changed significantly in renal impairment.

Dosing: Hepatic Impairment

Smaller areas of treatment are recommended for patients with severe hepatic impairment.

Administration

Cream: For external use only. Avoid application to open wounds or near the eyes. Avoid use in situations where penetration or migration past the tympanic membrane into the middle ear is possible. In small infants and children, observe patient to prevent accidental ingestion of cream or dressing. To obtain 1 g of cream, squeeze narrow strip ~1.5 inches long and 0.2 inches wide from tube. Repeat as necessary to obtain quantity needed for dose (eg, 2 strips = 2 g dose). Apply a thick layer of cream to designated site of intact skin. Cover site with occlusive dressing. Mark the time on the dressing. Allow at least 1 hour (mild dermatologic procedures) or at least 2 hours (major dermal procedures) for optimum therapeutic effect. Remove the dressing and wipe off excess cream (gloves should be worn). Smaller areas of treatment are recommended for small children, debilitated patients, or patients with severe hepatic impairment.

Transdermal patch [Canadian product]: Apply patch or patches to intact skin. Allow at least 1 hour for optimum therapeutic effect. After removing patch or patches, clean treated areas thoroughly prior to procedure.

Oraqix is a viscous liquid. Make sure it is in the liquid form before administration; if semisolid gel forms, refrigerate until becomes liquid again (do not freeze). Do not use dental cartridge warmers; heat will cause product to gel prematurely (product is a microemulsion which is intended to form a gel in the periodental pocket). Apply slowly and evenly on gingival margin around selected teeth using the provided blunt-tipped applicator. Wait 30 seconds, then fill the periodontal pockets using the blunt-tipped applicator until gel becomes visible at the gingival margin. Wait another 30 seconds before starting treatment.

Storage

Cream:

US labeling: Store between 20°C to 25°C (68°F to 77°F).

Canadian labeling: Store between 15°C to 30°C (59°F to 86°F).

Patch (Canadian availability; not available in the US): Store between 15°C to 30°C (59°F to 86°F); do not freeze.

Periodontal gel: Store at 25°C (77°F); excursions permitted between 15°C and 30°C (59°F and 86°F); do not freeze. May turn opaque at temperature of ≤5°C. Do not use dental cartridge warmers; heat will cause product to gel prematurely (product is a microemulsion that is intended to form a gel in the periodontal pocket).

Drug Interactions

Abiraterone Acetate: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Antiarrhythmic Agents (Class III): Lidocaine (Topical) may enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III). Antiarrhythmic Agents (Class III) may increase the serum concentration of Lidocaine (Topical). This mechanism specifically applies to amiodarone and dronedarone. Monitor therapy

Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Beta-Blockers: May increase the serum concentration of Lidocaine (Topical). Monitor therapy

Bupivacaine (Liposomal): Local Anesthetics may enhance the adverse/toxic effect of Bupivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with local anesthetics. Liposomal bupivacaine may be administered 20 minutes or more after the administration of lidocaine, but the optimal duration of dose separation for other local anesthetics is unknown Avoid combination

CloZAPine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of CloZAPine. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP1A2 Inhibitors (Moderate): May decrease the metabolism of CYP1A2 Substrates. Monitor therapy

CYP1A2 Inhibitors (Strong): May decrease the metabolism of CYP1A2 Substrates. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates. Consider therapy modification

Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferasirox: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Disopyramide: May enhance the arrhythmogenic effect of Lidocaine (Topical). Disopyramide may increase the serum concentration of Lidocaine (Topical). Specifically, the unbound/free fraction of lidocaine. Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Monitor therapy

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates. Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification

Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Nitric Oxide: May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when nitric oxide is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine. Monitor therapy

Obeticholic Acid: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Peginterferon Alfa-2b: May increase the serum concentration of CYP1A2 Substrates. Monitor therapy

Prilocaine: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents. Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Sodium Nitrite: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Monitor therapy

Tetracaine (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Monitor therapy

TiZANidine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use cannot be avoided, initiate tizanidine at an adult dose of 2 mg and increase in 2-4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification

Vemurafenib: May increase the serum concentration of CYP1A2 Substrates. Management: Consider alternatives to such combinations whenever possible, particularly if the CYP1A2 substrate has a relatively narrow therapeutic index. Consider therapy modification

Adverse Reactions

Cream/patch: Frequency not always defined.

Dermatologic: Hyperpigmentation, urticaria

Genitourinary: Blistering of foreskin (rare)

Local: Pallor (37%), erythema (21% to 30%), burning (17%), edema (6% to 10%), itching (2%), petechia, purpura, stinging

Miscellaneous: Alteration in temperature sensation (local: 7%)

<1% (Limited to important or life-threatening): Anaphylactic shock, angioedema, central nervous system depression, central nervous system stimulation, central nervous system toxicity (high dose), circulatory shock (high dose), hypersensitivity reactions, hypotension, methemoglobinemia (high dose)

Periodontal gel:

>10%: Local: Application site reaction (1%, includes abscess, edema, irritation, numbness, pain, ulceration, vesicles)

1% to 10%:

Central nervous system: Fatigue (1%)

Gastrointestinal: Bitter taste (2%), nausea (1%)

Respiratory: Infection (1%)

Miscellaneous: Flu-like syndrome (1%), allergic reactions

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity: Allergic and anaphylactic reactions may occur. Patients allergic to paraaminobenzoic acid derivatives (eg, procaine, tetracaine, benzocaine) have not shown cross sensitivity to lidocaine and/or prilocaine; use with caution in patients with a history of drug sensitivities.

• Methemoglobinemia: Has been reported in infants and children; associated with large doses, larger-than-recommended areas of application, neonates and infants <3 months of age, and concomitant use of methemoglobinemia-inducing agents (eg, acetaminophen, benzocaine, chloroquine, dapsone, nitrofurantoin, nitroglycerin, nitroprusside, phenobarbital, phenytoin, quinine, sulfonamides). Neonates and infants up to 3 months of age should be monitored for methemoglobinemia. Do not use in preterm neonates (gestational age <37 weeks), infants <12 months of age requiring treatment with methemoglobinemia-inducing agents, or in patients with congenital or idiopathic methemoglobinemia.

Disease-related concerns:

• Atopic dermatitis: Use with caution; rapid and greater absorption through the skin is observed in these patients; a shorter application time should be used.

• Cardiovascular disease: Use with caution in patients with severe impairment of impulse initiation and conduction in the heart (eg, grade II and III AV block, pronounced bradycardia).

• Glucose-6-phosphate dehydrogenase (G6PD) deficiency: Patients with G6PD may be more susceptible to drug-induced methemoglobinemia.

• Hepatic impairment: Use with caution in patients with severe hepatic impairment; risk of increased systemic exposure. Smaller treatment area may be required.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Acutely ill patients: Use with caution in acutely ill; smaller treatment area may be required consistent with age and physical status.

• Debilitated patients: Use with caution in debilitated patients; smaller treatment area may be required consistent with age and physical status.

• Elderly: Use with caution in elderly patients; smaller treatment area may be required consistent with age and physical status.

Dosage forms specific issues:

• Periodontal gel: Do not use with standard dental syringes; only use with the supplied blunt-tipped applicator.

Other warnings/precautions:

• Appropriate use: Although the incidence of systemic adverse reactions with use of the cream is very low, caution should be exercised, particularly when applying over large areas and leaving on for longer than 2 hours. When used prior to cosmetic or medical procedures, the smallest amount of cream necessary for pain relief should be applied. High systemic levels and toxic effects (eg, methemoglobinemia, irregular heartbeats, respiratory depression, seizures, death) have been reported in patients who (without supervision of a trained professional) have applied topical anesthetics in large amounts (or to large areas of the skin), left these products on for a prolonged time, or have used wraps/dressings to cover the skin following application. Do not apply to broken or inflamed skin, open wounds, or near the eyes. Avoid use in situations where penetration or migration past the tympanic membrane into the middle ear is possible; ototoxicity has been observed in animal studies. Avoid inadvertent trauma to the treated area (eg, scratching, rubbing, exposure to extreme hot or cold temperatures) until complete sensation has returned.

Monitoring Parameters

Serum methemoglobin before, during, and after use in neonates and infants up to 3 months of age. Consider ECG monitoring in patients treated with Class III antiarrhythmic drugs (eg, amiodarone).

Pregnancy Risk Factor

B

Pregnancy Considerations

Animal reproduction studies have not been conducted with this combination. Lidocaine and prilocaine cross the placenta. Their use is not contraindicated during labor and delivery. Refer to individual agents.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience redness, temperature sensitivity, pale skin, bad taste, or nausea. Have patient report immediately to prescriber signs of methemoglobinemia (blue or gray color of the lips, nails, or skin; abnormal heartbeat; seizures; severe dizziness or passing out; severe headache; fatigue; loss of strength and energy; or shortness of breath), or severe application site irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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