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Ebastine in context. Introduction.

Abstract

The allergic reaction to a specific antigen is characterised by a series of complex immunological processes consisting of an early specific immune response and a late inflammatory reaction. The release of active substances (principally histamine) from cytoplasmic granules of mast cells and basophils in response to antigen challenge is responsible for many of the symptoms observed in the early phase of the allergic reaction. The late phase inflammatory reaction caused by the recruitment of inflammatory cells (mainly eosinophils) to the area of initial antigen challenge and the consequent release of soluble factors result in amplification and prolongation of allergic symptoms. Antihistamines are the most widely used drugs for the treatment of allergic conditions. These agents act on both the early immune response (by blocking the action of histamine at the H1 receptor) and also demonstrate anti-inflammatory effects. Second generation antihistamines are free of the sedative and anticholinergic effects characteristic of the first generation agents. Ebastine, the focus of this supplement, is a new second generation agent that has shown antihistamine activity in preclinical studies and clinical efficacy in providing relief from symptoms in patients with allergic disorders.

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BibTeXRIS

E Buendia. 1996. Ebastine in context. Introduction.. https://doi.org/10.2165/00003495-199600521-00003

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Does potency predict clinical efficacy? Illustration through an antihistamine model.

OBJECTIVE: The concepts of potency and efficacy are often confused and used interchangeably within the scientific and pharmaceutical industry. It is important that the distinction between the two is understood, and that the terms are defined within their correct context. After reading this article, readers should have an understanding of the relationships between receptor potency and clinical efficacy. DATA SOURCES: Following a comprehensive review of the literature using MEDLINE, the author observed a lack of relevant references that relate measurements of potency to clinical efficacy. Therefore, the author reviewed the basic pharmacologic principles of potency using examples from the recent antihistamine literature. RESULTS: Potency is an expression of the activity of a drug in terms of the concentration or amount of the drug required to produce a defined effect, whereas clinical efficacy judges the therapeutic effectiveness of the drug in humans. The differing methods of evaluating the activity of antihistamines in vitro and in vivo can lead to inconsistent results, which complicate the use of potency to predict clinical efficacy. Further, as therapeutic behavior is modulated by pharmacokinetic and pharmacodynamic parameters and by further interactions at sites other than the target receptor, it does not necessarily follow that more potent drugs have greater clinical efficacy. CONCLUSIONS: Although potency can be a good preclinical marker of the therapeutic potential of a drug, clinical efficacy should only be evaluated within the patient population using appropriate outcome measures.

Histamine Antagonists↗