• Gisèle Pickering, Nicolas Macian, Frédéric Libert, J Michel Cardot, Séverine Coissard, Philippe Perovitch, Marc Maury, and Claude Dubray.
• CHU Clermont-Ferrand, Centre de Pharmacologie Clinique, Clermont-Ferrand, France ; Inserm, Clermont-Ferrand, France ; Clermont Université, Laboratoire de Pharmacologie, Faculté de Médecine, Clermont-Ferrand, France.
• Drug Des Dev Ther. 2014 Jan 1;8:1621-7.

BackgroundAcetaminophen (APAP) by oral or intravenous (iv) routes is used for mild to moderate pain but may take time to be effective. When fast relief is required and/or oral or iv routes are not available because of the patient's condition, the transmucosal route may be an alternative.MethodologyA new transmucosal/buccal (b) pharmaceutical form of APAP dissolved in 50% wt alcohol is compared with other routes of administration. Two consecutive randomized, crossover, double-blind clinical trials (CT1: NCT00982215 and CT2: NCT01206985) included 16 healthy volunteers. CT1 compared the pharmacology of 250 mg bAPAP with 1 g iv APAP. CT2 compared the pharmacodynamics of 125 mg bAPAP with 1 g iv and 125 mg sublingual (s) APAP. Mechanical pain thresholds are recorded in response to mechanical stimuli applied on the forearm several times during 120 minutes. The objective is to compare the time of onset of antinociception and the antinociception (area under the curve) between the routes of administration with analysis of variance (significance P<0.05).ResultsbAPAP has a faster time of antinociception onset (15 minutes, P<0.01) and greater antinociception at 50 minutes (P<0.01, CT1) and 30 minutes (P<0.01, CT2) than ivAPAP and sAPAP. All routes are similar after 50 minutes.ConclusionbAPAP has a faster antinociceptive action in healthy volunteers. This attractive alternative to other routes would be useful in situations where oral or iv routes are not available. This finding must now be confirmed in patients suffering from acute pain of mild and moderate intensity.

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