A critical review of the topical local anesthetic amethocaine (Ametop) for pediatric pain

Lisa O'Brien, Anna Taddio, Dorothy A Lyszkiewicz, Gideon Koren
Paediatric Drugs 2005, 7 (1): 41-54
A topical formulation of the ester-type local anesthetic amethocaine (tetracaine) [Ametop ] is currently available for reducing pain from cutaneous procedures such as venipuncture. The Ametop mark preparation contains 40 mg of amethocaine base (4% w/w) and produces anesthesia within 30-45 minutes of application; duration of action ranges from 4 to 6 hours. Clinical studies have demonstrated the superiority of the 4% amethocaine preparation over placebo in pediatric populations for indications such as intravenous cannulation, vaccination, and venipuncture. Amethocaine has been shown to produce anesthesia comparable to that of 5% lidocaine-prilocaine for procedures such as venipuncture and accessing centrally placed devices; in general, anesthesia was achieved more rapidly with amethocaine than lidocaine-prilocaine. In the neonatal population amethocaine was found to be ineffective at reducing the pain of heel prick and peripherally inserted central catheters. Depending on the type of procedure, amethocaine application times between 30 and 60 minutes have produced clinically acceptable anesthesia; application times <30 minutes have not been associated with reliable anesthesia. The 4% amethocaine preparation is well tolerated; the most commonly reported local skin reaction is transient local erythema while local edema and itching have been reported more rarely. There have been no accounts of systemic toxicity with topical use of the preparation. Several cases of sensitization have been described in adults upon repeated exposure to topical amethocaine. In summary, the novel preparation of 4% amethocaine gel has been shown to be clinically effective for managing pain associated with minor cutaneous procedures while maintaining a good tolerability profile. Amethocaine has also demonstrated similar efficacy to lidocaine-prilocaine when appropriate application times are used; the more rapid onset of action and extended duration of action of amethocaine may make it more useful than lidocaine-prilocaine in busy clinical settings.

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