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- Title
The apparent volumes of distribution of H<sub>1</sub> receptor antagonists.
- Authors
Tillement, Jean-Paul; Albengres, Edith; Barré, Jérôme; Rihoux, Jean-Pierre
- Abstract
ABSTRACT: The apparent volume of distribution (VD) of a drug estimates its distribution into the body. Referring to the volume of exchangeable water (0.6 L/kg body weight), it indicates if tissue distribution is extensive when VD is greater than 0.6 L/kg or poor if VD is less than 0.6 L/kg. Its interest in the selection of an appropriate drug is found after comparing the map of selected targets (mainly receptors) to be reached by the drug, the accessibility of these targets by the drug, and the VD necessary and sufficient to reach them. This analysis is here applied to H1 receptor antagonists, a pharmacologic class, where target cells, endothelial cells such as eosinophils, mastocytes, basophils, and smooth fibers have receptors on the external side of cell membranes and thus are more readily accessible from blood than toxic sites located inside cells (heart, brain, liver). Of the H1 receptor antagonists marketed today, cetirizine has the lowest VD, 0.4 L/kg, enough to reach selected targets without extensive distribution in organs where it would be useless. These characteristics are related to its chemical amphoteric structure.
- Subjects
ANTIHISTAMINES; CHEMICAL inhibitors; ASTEMIZOLE
- Publication
Dermatologic Therapy, 2000, Vol 13, Issue 4, p337
- ISSN
1396-0296
- Publication type
Article
- DOI
10.1046/j.1529-8019.2000.00041.x