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Pharmacology of Leukotriene Receptor Antagonists and 5‐Lipoxygenase Inhibitors in the Management of Asthma
Author(s) -
Drazen Jeffrey M.
Publication year - 1997
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/j.1875-9114.1997.tb03698.x
Subject(s) - bronchoconstriction , asthma , arachidonate 5 lipoxygenase , leukotriene , receptor , inflammation , zileuton , lipid signaling , pharmacology , eicosanoid , medicine , immunology , arachidonic acid , effector , chemistry , enzyme , biochemistry
The leukotrienes (LTs), a family of inflammatory mediators arising from the metabolism of arachidonic acid via the 5‐lipoxygenase pathway, are prominently implicated in the pathobiology of asthma. Two classes of LTs, the cysteinyl LTs (LTC 4 , LTD 4 , and LTE 4 ) and the dihydroxy‐LT (LTB 4 ) have been identified, with each class acting via distinct receptors. Inhibition of LT‐mediated inflammation can be achieved by either interruption of 5‐lipoxygenase action, thereby preventing formation of the LTs, or inhibition at specific LT receptor sites in the airway. Both the 5‐lipoxygenase inhibitors and the cysLT receptor antagonists have thus far demonstrated the capacity to improve pulmonary function and reduce symptoms in clinical models of asthma, such as exercise‐, aspirin‐, or antigen‐induced bronchoconstriction, and to improve pulmonary function in patients with mild‐to‐moderate, chronic stable asthma. The LTs are therefore critical effector molecules in some patients with asthma and important targets in the pharmacologic management of this disease.