Relative potency of fexofenadine HCl 180 mg, loratadine 10 mg, and placebo using a skin test model of wheal-and-flare suppression

Assessment of Histamine Pharmacodynamics by Microvasculature Response of Histamine Using Histamine Iontophoresis Laser Doppler Flowimetry

“…In contrast, the HILD method appears to provide a more dynamic assessment of blood flow response over time and is devoid of subjectivity (ie, operator error) in the determination of pharmacodynamic parameters. It should be noted that there are no recommended guidelines for timing of measurement of skin response after EH application, and several different time intervals have been used in clinical evaluations 6 , 29 , 30 …”

“…T he pharmacodynamics and potency of orally administered H 1 antagonists are routinely investigated using bioassays that measure edema and suppression of the cutaneous wheal-and-flare response following administration of histamine by either the intradermal or epicutaneous (ie, skin prick test) route. [1][2][3][4][5][6][7] Epicutaneous histamine (EH) has been used successfully to characterize the onset, maximum activity, and duration of antihistamine effect relative to drug dose in both adults and children and presently is considered to be the "gold standard" for assessing antihistamine pharmacodynamics (PD). [8][9][10][11] Assessment of wheal-and-flare magnitude following EH testing has been shown to correlate with dermal concentrations of H 1 receptor antagonists and relief of symptoms of allergic rhinitis.…”

Inhibition of the histamine‐induced weal and flare response: a valid surrogate measure for antihistamine clinical efficacy?

“…Another approach to evaluating the relative potencies of antihistamines is to compare their inhibition of the flare reaction. In the great majority of studies (Table 1), such comparisons have found similar orders of potency for the antihistamines evaluated, regardless of the relative weal responses [37–48, 51, 52, 54–62, 64–83]. However, in the study by Frossard et al [51], which used the concentration–response curve method, ebastine (10 and 20 mg) and cetirizine inhibited flare response to a similar degree but differed significantly in their inhibition of weal development.…”

“…Numerous studies have compared the effects of a single dose of different antihistamines on histamine-induced weal and flare, with the majority enrolling healthy volunteers (Table 1). Loratadine was included in 15 of the 28 studies of healthy volunteers [37,38,40,41,44,45,[55][56][57][65][66][67][68][69][70] and caused less suppression of weal and flare than other second-generation antihistamines in all but three of the studies, usually when antihistamines were studied within 24 h after drug intake [37,69,70]. On the other hand, cetirizine, included in 20 studies of healthy volunteers, suppressed weal and flare to a greater extent than loratadine (nine studies) [ (four studies) [46,47,55,69], and desloratadine (one study) [60].…”

Antihistamines in Treatment of Chronic Urticaria. Review of Modern Recommendations

“…Simons изуча-лись концентрации в крови и коже (при биопсии) и пода-вление образования кожных реакций в гистамин-инду- Примечание. Адаптировано по ссылкам [45][46][47][48][49][50][51][52][53][54][55][56].…”