Lidocaine/prilocaine

Lidocaine/prilocaine is a eutectic mixture of equal quantities (by weight) of lidocaine and prilocaine. A 5% emulsion preparation, containing 2.5% each of lidocaine/prilocaine, is marketed by APP Pharmaceuticals under the trade name EMLA (an abbreviation for Eutectic Mixture of Local Anesthetics).[1]

Lidocaine/prilocaine
Combination of
Lidocaineanesthetic
Prilocaineanesthetic
Clinical data
License data
Identifiers
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
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Eutectic mixture

Separately, lidocaine and prilocaine are solid bases. When mixed in equal quantities by weight, however, they form a eutectic mixture – that is the melting point of the mixture is lower than the melting points of the individual components. The lidocaine/prilocaine eutectic mixture is an oil with a melting point of 18 °C, known as emla cream thus can be formulated into preparations without the use of a non-aqueous solvent.[2] This allows higher concentrations of anaesthetic to be formulated into the preparation and maintained during application.

Clinical use

Indications

The lidocaine/prilocaine combination is indicated for dermal anaesthesia. Specifically it is applied to prevent pain associated with intravenous catheter insertion, blood sampling, superficial surgical procedures; and topical anaesthesia of leg ulcers for cleansing or debridement.[3] Also, it can be used to numb the skin before tattooing as well as electrolysis and laser hair removal. It is also sometimes used in advance of injected local anaesthetics for minor surgery and biopsies.

A topical spray consisting of an aerosol formulation of lidocaine and prilocaine was evaluated under the name PSD502 for use in treating premature ejaculation. The spray is applied on the penile skin prior to intercourse. While this formulation was not approved by the FDA,[4] a similar product, Promescent, is available over-the-counter in the U.S.

Dosage forms

Lidocaine/prilocaine eutectic mixture is marketed as a 5% oil-in-water emulsion incorporated in a cream base (EMLA cream) or a cellulose disk (EMLA patch). The cream is applied under an occlusive dressing, while the patch incorporates an occlusive dressing to facilitate absorption of lidocaine and prilocaine into the area where anaesthesia is required. Local dermal anaesthesia is achieved after approximately 60 minutes, whereupon the occlusive dressing (or patch) is removed. The duration of anaesthesia is approximately two hours following removal of the occlusive dressing.

E. Fougera & Co., makers of the generic cream widely used in the United States as Lidocaine and Prilocaine Cream, 2.5%/2.5%, recommends different timing for application of the cream as well as length of anesthesia. They state the cream must be applied at least one hour before the start of a routine procedure and for two hours before the start of a painful procedure. Additionally, they state that the duration of effective skin anesthesia will be at least one hour after removal of the occlusive dressing.[5]

Circumcision

Lidocaine/prilocaine eutectic mixture is used during circumcision in newborn boys and has been considered efficacious and safe to lessen pain from circumcision.[6]

The European Medicines Agency concludes in its latest (2014) statement on Emla: "Safety and efficacy for the use of EMLA on genital skin and genital mucosa have not been established in children younger than 12 years. Available paediatric data do not demonstrate adequate efficacy for circumcision."[7]

The Patient Information Leaflet of EMLA in the UK states: "EMLA Cream should not be applied to the genital skin (e.g. penis) and genital mucosa (e.g. in the ...) of children (below 12 years of age) owing to insufficient data on absorption of active substances."[8]

Compendial status
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See also

References
  1. Pesaturo KA, Matthews M (2009). "Topical Anesthesia Use in Children: Eutectic Mixture of Local Anesthetics". US Pharm. 34 (3): HS-4. Retrieved 2014-01-07.
  2. "EMLA Official FDA information, side effects and uses". Drugs.com. Retrieved 2014-01-07.
  3. Heinen MM, van Achterberg T, op Reimer WS, van de Kerkhof PC, de Laat E (March 2004). "Venous leg ulcer patients: a review of the literature on lifestyle and pain-related interventions". Journal of Clinical Nursing. 13 (3): 355–66. doi:10.1046/j.1365-2702.2003.00887.x. PMID 15009338.
  4. "PSD502 TEMPE Spray". Promescent.com. Retrieved 4 July 2014.
  5. Lidocaine and Prilocaine Cream, 2.5%/2.5%, package insert. E. Fougera & Co. package insert. Melville, New York, 9/2007.
  6. Taddio A, Ohlsson K, Ohlsson A (2000). Ohlsson A (ed.). "Lidocaine-prilocaine cream for analgesia during circumcision in newborn boys". The Cochrane Database of Systematic Reviews (2): CD000496. doi:10.1002/14651858.CD000496. PMID 10796371. (Retracted, see doi:10.1002/14651858.cd000496.pub2. If this is an intentional citation to a retracted paper, please replace {{Retracted}} with {{Retracted|intentional=yes}}.)
  7. "INN of the active substance(s): lidocaine/prilocaine" (PDF). Committee for Medicinal Products for Human Use (CHMP). European Medicines Agency.
  8. "Package leaflet: Information for the user EMLA Cream 5%" (PDF). AstraZeneca. 2017.
  9. The United States Pharmacopeial Convention. "Revision Bulletin: Lidocaine and Prilocaine Cream–Revision to Related Compounds Test". Archived from the original on 5 July 2010. Retrieved 10 July 2009.
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