Topical Anesthetics

EMLA = eutectic mixture of local anesthetic (combination of lidocaine & prilocaine)

  • Pregnancy Category B
  • Most effective topical anesthetic 
  • Applied under occlusion with a 60-min application period
  • Block nerve conduction via reversible inhibition of sodium ion influx preventing depolarization
  • Smaller diameter nerves are most susceptible (C & Aδ fibers – pain & temperature) whereas large nerves are more resistant (Aβ fibers -pressure)
  • Most resistant nerves are proprioception & motor nerves
  • Amount of EMLA systemically absorbed is directly related to the surface area of application as well as duration of contact with skin, specifically, longer duration & occlusion increase EMLA penetration & efficacy 
  • Metabolism via hepatic microsomal CYP enzymes
FDA

  • Topical analgesia prior to surgery, laser, debridement of leg ulcers

Off-label

  • Mucosal analgesia, Pruritus, Postherpetic neuralgia, Hyperhidrosis

Absolute

  • Hypersensitivity, methemoglobinemia

Relative

  • Hypersensitivity to anesthetics other than lidocaine/prilocaine, Mucosal application, Application on broken skin, G6PD deficiency, age <1 month, Pregnancy, significant cardiac or hepatic impairment 
  • Methemoglobinemia (prilocaine)
  • Toxicity (very rare)
  • Local reactions: stinging, burning, pruritus, blanching, erythema, allergic contact dermatitis

Medications that may increase risk of methemoglobinemia with EMLA

  • Acetaminophen, Aminosalicylic acid, Phenobarbital, Phenytoin, Antimalarials, Nitrates, Sulfonamides

Methemoglobinemia: 

Risk due to prilocaine component of eutectic mixture of local anesthetic (EMLA), higher with: 

  • Patients with congenital or acquired methemoglobinemia
  • Patients on medications that may increase the risk of methemoglobinemia
  • G6PD deficiency 
  • Patients younger than 1 year of age 

Management of methemoglobinemia (acute)

  • Plasmapheresis, methylene blue

Other topical anesthetics

  • Lidocaine (Lidocaine 4% cream “LMX4”, lidocaine 5% cream ‘LMX5”), Benzocaine (higher risk of allergic reactions)