PubMed · 6152833
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G R Hervey. Motion illness.. https://pubmed.ncbi.nlm.nih.gov/6152833/
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Histamine H1-receptor antagonists are reversible, competitive inhibitors of the actions of histamine, a critical mediator in the pathophysiology of the allergic response. This review is mainly devoted to second generation antihistamines that possess a low sedation potential compared with first generation compounds. The pharmacokinetic and pharmacodynamic data of 10 compounds have been updated. Some values are lacking for drugs under development, but also for older antihistamines. Thereafter, pharmacokinetic-pharmacodynamic relationships are reported from published or original documents. A linear pharmacokinetic-pharmacodynamic relationship has been found for acrivastine, astemizole, cetirizine, ebastine and terfenadine, whereas nonlinear relationships have been calculated for ebastine (in the dog), levocabastine, mizolastine, noberastine and terfenadine. It must be concluded that this type of approach for therapeutic optimisation is very fruitful and may enable large numbers of clinical studies to be avoided. Trends for the future include: (i) in vitro binding studies with the human H1-receptor obtained by molecular biology; (ii) the characterisation of the cytochromes P450 responsible for the biotransformation of antihistamine; (iii) the calculation of the pharmacokinetic-pharmacodynamic relationship in healthy individuals; and (iv) prospective effect-controlled clinical studies.
This article reviews the effect of H1 antihistamines on the pruritus of urticaria, from articles in which their therapeutic effect on chronic idiopathic and physical urticaria is assessed. In limited studies available pruritus improved concomitantly with wealing by an average of two thirds, though the response in individual patients was variable. In some physical urticarias the pruritus and wealing showed disproportionate improvement compared to erythema. The minimally sedating H1 antihistamines were as effective or more effective than classical H1 antihistamines. The dose of antihistamines that totally abolished a histamine weal only partly reduced urticarial weals (therefore by inference also of the associated pruritus). Additional therapy aimed at pruritogenic mediators other than histamine would be expected to improve urticarial pruritus.