Anti-leukotrienes: here to stay?
Anti-leukotrienes, which are competitive antagonists of cysteinyl-leukotriene-1 receptors, are the first new class of anti-asthmatics introduced in over 30 years. There is a strong scientific rationale for their use, as cysteinyl-leukotrienes are increased in asthma and can mimic several of the pathophysiological features of asthma. In addition, there is often increased tissue responsiveness to these mediators. Anti-leukotrienes inhibit several bronchoconstrictor challenges, including allergens, exercise, irritants and aspirin. In clinical trials, they have significant benefit compared with placebo, but are less effective compared with low doses of inhaled corticosteroids. As an add-on therapy to inhaled corticosteroids, they are also disappointing and less effective than long-acting beta(2)-receptor agonists. In clinical practice, they have not proved to be very useful, and they are less cost-effective than other treatments. It is unlikely that this class of drug will be improved greatly in the future, and so will remain as a weak second-line therapy.
Barnes
Peter J
PJ
Department of Thoracic Medicine, National Heart and Lung Institute, Dovehouse Street, London SW3 6LY, UK. p.j.barnes@ic.ac.uk
D000305:Adrenal Cortex Hormones / Q000627:therapeutic use; D018927:Anti-Asthmatic Agents / Q000009:adverse effects / Q000627:therapeutic use*; D000893:Anti-Inflammatory Agents / Q000009:adverse effects / Q000627:therapeutic use; D001249:Asthma / Q000188:drug therapy / Q000378:metabolism; D003545:Cysteine / Q000096:biosynthesis; D004359:Drug Therapy, Combination; D006801:Humans; D020024:Leukotriene Antagonists / Q000009:adverse effects / Q000627:therapeutic use*; D015289:Leukotrienes / Q000096:biosynthesis; D008565:Membrane Proteins / Q000037:antagonists & inhibitors; D018077:Receptors, Leukotriene
D000305:Adrenal Cortex Hormones; D018927:Anti-Asthmatic Agents; D000893:Anti-Inflammatory Agents; D020024:Leukotriene Antagonists; D015289:Leukotrienes; D008565:Membrane Proteins; D018077:Receptors, Leukotriene; C112381:cysteinyl-leukotriene; D003545:Cysteine; C083169:leukotriene D4 receptor