Antileukotrienes in the Treatment of Asthma
- Paul M. O'Byrne, MB;
- Elliot Israel, MD; and
- Jeffrey M. Drazen, MD
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From McMaster University, Hamilton, Ontario, Canada; and Harvard Medical School, Boston, Massachusetts.
Requests for Reprints: Paul M. O'Byrne, MB, Asthma Research Group, Department of Medicine, Division of Respirology, McMaster University, 1200 Main
Street West, Hamilton, Ontario L8N 3Z5, Canada.
Current Author Addresses: Dr. O'Byrne: Asthma Research Group, Department of Medicine, Division of Respirology, McMaster University, 1200 Main Street
West, Hamilton, Ontario L8N 3Z5, Canada.
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Figure 1. In addition, 5-LO activating protein antagonists, such as BAYx1005 and MK-886; 5-LO inhibitors, such as zileuton;
and cysteinyl leukotriene receptor type 1 (CysL T ) receptor antagonists, such as zafirlukast, inhibit the production or action
of the cysteinylleukotrienes. 5-HPETE = 5-hydroperoxyeicosatetraenoic acid; LTA ( ) = leukotriene A ; LTD = leukotriene D
; LTE = leukotriene E . The 5-lipoxygenase (5-LO) pathway of arachidonic acid (AA) metabolism, showing the other enzymes (5-lipoxygenase activating
protein [FLAP] and leukotriene C4 [LTC4] synthetase) necessary for the production of the cysteinyl leukotrienes.1444444
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Figure 2. Pretreatment with MK-571 markedly attenuated the decrease in FEV after exercise. Reproduced from Impens and colleagues
with permission. The effect of a selective cysteinyl leukotriene receptor type 1 (CysLT1) receptor antagonist, MK-571, on the percentage decrease from baseline in the FEV1 after exercise in asthmatic patients.1[52]
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Figure 3. Groups are stratified by FEV as a percentage of predicted value at study entry. A total of 111 patients had an FEV
greater than 70%, 187 had an FEV of 50% to 70%, and 103 had an FEV ( ) less than 50%. * < 0.05 for comparison with placebo.
Reproduced from Israel and colleagues with permission. Percentage of patients who required corticosteroid treatment for exacerbations of asthma after receiving zileuton, 400 mg
or 600 mg four times daily, or placebo.1111P[106]
- Copyright ©2004 by the American College of Physicians
-
Ann Intern Med
September 15, 1997
vol. 127
no. 6
472-480
RSS Feeds
Figure 1. In addition, 5-LO activating protein antagonists, such as BAYx1005 and MK-886; 5-LO inhibitors, such as zileuton; and cysteinyl leukotriene receptor type 1 (CysL T ) receptor antagonists, such as zafirlukast, inhibit the production or action of the cysteinylleukotrienes. 5-HPETE = 5-hydroperoxyeicosatetraenoic acid; LTA ( ) = leukotriene A ; LTD = leukotriene D ; LTE = leukotriene E . The 5-lipoxygenase (5-LO) pathway of arachidonic acid (AA) metabolism, showing the other enzymes (5-lipoxygenase activating protein [FLAP] and leukotriene C4 [LTC4] synthetase) necessary for the production of the cysteinyl leukotrienes.1444444
Figure 2. Pretreatment with MK-571 markedly attenuated the decrease in FEV after exercise. Reproduced from Impens and colleagues with permission. The effect of a selective cysteinyl leukotriene receptor type 1 (CysLT1) receptor antagonist, MK-571, on the percentage decrease from baseline in the FEV1 after exercise in asthmatic patients.1[52]
Figure 3. Groups are stratified by FEV as a percentage of predicted value at study entry. A total of 111 patients had an FEV greater than 70%, 187 had an FEV of 50% to 70%, and 103 had an FEV ( ) less than 50%. * < 0.05 for comparison with placebo. Reproduced from Israel and colleagues with permission. Percentage of patients who required corticosteroid treatment for exacerbations of asthma after receiving zileuton, 400 mg or 600 mg four times daily, or placebo.1111P[106]
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