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Effect time-course of the inhibition of histamine induced skin reactions by orally applied dimethindene maleate.
Rehn, D; Geissler, H; Schuster, O; Lukas, H; Hennings, G.
Afiliación
  • Rehn D; Zyma GmbH, Hauptabteilung Medizin und Entwicklung, München.
Agents Actions ; 33(1-2): 221-4, 1991 May.
Article en En | MEDLINE | ID: mdl-1680275
We have investigated the time-course of the flare inhibiting activity of dimethindene maleate in man and compared the resulting effect-kinetic data with those from pharmacokinetic investigations. The study was carried out in a double-blind, placebo-controlled cross-over design with randomly assigned healthy volunteers. Dimethindene maleate (4 mg) was orally applied, followed by intracutaneous histamine provocations (-1, 2, 5, 14, 17, 20, 23, 26, 29 h). The two cross-over periods were separated by a wash-out phase of 17 h. Flare areas were documented 5, 10, 20 and 30 min after provocation with histamine. A strong inhibition of the development of flares was observed. With regard to the time-course of the inhibiting effect, its maximum was observed at a provocation time of 5 h. The mean residence time of the inhibiting effect was calculated to be ca. 13 h. This is different from the mean residence time of ca. 8 h obtained from blood level data. Blood- and effect-levels are not linearly related under oral treatment conditions.
Asunto(s)
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urticaria / Histamina / Dimetindeno / Antagonistas de los Receptores Histamínicos H1 Tipo de estudio: Clinical_trials Límite: Adult / Humans / Male Idioma: En Revista: Agents Actions Año: 1991 Tipo del documento: Article Pais de publicación: Suiza
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urticaria / Histamina / Dimetindeno / Antagonistas de los Receptores Histamínicos H1 Tipo de estudio: Clinical_trials Límite: Adult / Humans / Male Idioma: En Revista: Agents Actions Año: 1991 Tipo del documento: Article Pais de publicación: Suiza