Dose-dependent competitive block by topical acetylsalicylic and salicylic acid of low pH-induced cutaneous pain

Pain
Kay H SteenHans W Kreysel

Abstract

In a human acid pain model, which uses continuous intradermal pressure infusion of a phosphate-buffered solution (pH 5.2) to induce localized non-adapting pain, the flow was adjusted to result in constant pain ratings of about 20% or 50% on a visual analog scale (VAS). Six volunteers in each group participated in 4 different placebo-controlled double-blind cross-over studies to measure rapidly evolving cutaneous analgesia from topically applied new ointment formulations of acetylsalicylic acid (ASA) and salicylic acid (SA) as well as of commercial ibuprofen and benzocain creams. Similar, log-linear dose-response curves were found for both ASA and SA, significant in effect at 3 g/kg and higher drug contents and reaching saturation level at 15 or 30 g/kg, respectively, which, 20 min after application, caused a mean pain suppression of 95% using ASA and 80% using SA. Half-maximal effects were achieved using 3 g/kg ASA or 15 g/kg SA. The SA action was also clearly slower to develop. With an increased flow of the acidic buffer, producing lower effective tissue pH and more intense pain, the effect of ASA and SA decreased to 73% pain suppression. A competitive mechanism of both drug effects was suggested by the fact that, with 15 g/kg...Continue Reading

References

Jan 1, 1976·Journal of Neurology, Neurosurgery, and Psychiatry·M J Harrison
Apr 1, 1990·Journal of Neurophysiology·E LangH O Handwerker
Jun 1, 1988·Pain·Peter N C WatsonVerna R Watt
Sep 1, 1989·Pain·M C Rowbotham, H L Fields
Feb 1, 1987·Acta Physiologica Scandinavica·E KuneschK E Hagbarth
Jul 1, 1987·Journal of the American Academy of Dermatology·J E BernsteinJ Y Roshal
May 1, 1970·The Journal of Investigative Dermatology·R J Feldmann, H I Maibach
Oct 1, 1956·The American Journal of Physiology·H K BEECHER

Citations

Sep 9, 2010·Digestive Diseases and Sciences·Yasutada Akiba, Jonathan D Kaunitz
Apr 26, 1996·Neuroscience Letters·U IssbernerKay H Steen
Jun 17, 1998·Life Sciences·S K SauerP W Reeh
Dec 15, 2015·CNS Neuroscience & Therapeutics·Milind M MuleyJason J McDougall
Sep 3, 2010·Pharmacology & Therapeutics·Emmanuel DevalEric Lingueglia
Sep 11, 2009·British Journal of Clinical Pharmacology·Camilla StaahlAsbjørn Mohr Drewes
May 25, 2002·Drug Development and Industrial Pharmacy·Pankaj DayalMandip Sing
Dec 7, 2007·Anesthesiology Clinics·Gary McCleane
Jun 23, 2012·Pharmacological Reviews·Anne Estrup OlesenAsbjørn Mohr Drewes
Mar 5, 2003·Pharmacological Reviews·Jana Sawynok

Related Concepts

Administration, Topical
Topical anesthetic
Analgesics, Anti-Inflammatory
Zorprin
Dose-Response Relationship, Drug
Hydrogen-Ion Concentration
Palliative Surgery
Salicylic Acids
Skin
Salicylic Acid

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