antileukotriene

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an·ti·leu·ko·tri·ene

(an'tē-lū'kō-trī'ēn),
A drug that prevents or alleviates bronchoconstriction in asthma by blocking the production or action of naturally occurring leukotrienes; may also be useful in psoriasis.

Leukotrienes are eicosanoids derived from arachidonic acid, which is present in cell membranes. The cysteinyl leukotrienes, which are elaborated by bronchopulmonary mast cells, eosinophils, and probably alveolar macrophages, have been shown to mediate bronchoconstriction induced by exercise, hyperventilation in cold air, aspirin, and inhaled allergens. They act by stimulating a specific receptor, known as cysteinyl leukotriene receptor type 1 (CysLT1). Antileukotrienes having clinical usefulness in asthma include zileuton, which inhibits 5-lipoxygenase, an enzyme critical in the biosynthesis of leukotrienes, and leukotriene receptor antagonists (cinalukast, montelukast, zarirlukast, and others). Antileukotrienes reverse bronchconstriction in asthma to a lesser degree than β2-adrenergic agonists, but their effects are additive to those of the latter agents. In chronic asthma, antileukotrienes improve peak flow and FEV1 and reduce the frequency and severity of acute asthmatic attacks, the need for β2-agonists, and the need for corticosteroid rescue. They are particularly effective in the prophylaxis of asthma induced by exercise and aspirin. In contrast, many people with allergic asthma show little or no response. Antileukotrienes are not indicated in the treatment of an acute asthmatic attack or in mild, intermittent asthma controlled adequately with occasional use of inhaled β2-agonists. They have not been recommended as a substitute for inhaled corticosteroids in prophylaxis of asthma. Antileukotrienes are administered orally or by inhalation. Both onset and waning of clinical effects are gradual. Side-effects are minimal, but drug interactions may occur because of interference with cytochrome P-450 enzymes. Rare transitory elevations of hepatic aminotransferase have been reported with some agents.

antileukotriene

Any of a class of agents that either interferes with leukotriene synthesis or antagonises leukotriene receptors, which are as effective as cromolyn or theophylline, and may reduce the amount of inhaled steroids needed to control inflammation.

Antileukotrienes 
LTD4 receptor antagonists (Zafirkulast-Accolate)
 
Pros
LTD4-induced bronchoconstriction, early and late responses, exercise challenge, cold-induced asthma, chronic asthma.
 
5-Lipoxygenase inhibitor (Zileutron-Zyflo)
 
Pros
Asthma induced by exercise, cold, aspirin, bronchial hyperresponsiveness.
 
FLAP inhibitors (5-lipoxygenase-activating protein inhibitor)

Pros
Early and late responses and cold-induced asthma.

antileukotriene

Any of a class of agents that either interfere with leukotriene synthesis or antagonize leukotriene receptors, which are as effective as cromolyn or theophylline, and may ↓ the amount of inhaled steroids needed to control inflammation See Asthma, Leukotrienes, Zafirlukast, Zileuton.
Antileukotrienes
LTD4 receptor antagonists
Zafirkulast-Accolate® Benefits LTD4-induced bronchoconstriction, early and late responses, exercise challenge, cold-induced asthma, chronic asthma
5-Lipoxygenase inhibitor
Zileutron-Zyflo®Benefits asthma induced by exercise, cold, aspirin, bronchial hyperresponsiveness
FLAP inhibitors
None are FDA-approved Benefits early and late responses and cold-induced asthma
.

an·ti·leu·ko·tri·ene

(an'tē-lū-ko-trī'ēn)
A drug that prevents or alleviates bronchoconstriction in asthma by blocking the production or action of naturally occurring leukotrienes; may also be useful in psoriasis.

an·ti·leu·ko·tri·ene

(an'tē-lū-ko-trī'ēn)
A drug that prevents or alleviates bronchoconstriction in asthma by blocking the production or action of naturally occurring leukotrienes; may also be useful in psoriasis.
References in periodicals archive ?
Leukotriene antagonists as well as cycloxygenase inhibitors (cox 2 inhibitors) are two classes of drugs recently synthesized from years of analyzing the exact participants in the inflammation cascade (see Figure 1).
Therefore, leukotriene antagonists could interfere with cytokine function.
There is very limited literature regarding the use of leukotriene antagonists in acute attack of bronchial asthma.
Table 1: Drugs primarily used for asthma therapy Category Name of drugs Corticosteroids Budesonide, methyl prednisolone Beta agonists Salbutamol, salmeterol, bambuterol, formoterol Methyl xanthine Doxophylline, etophylline, theophylline Leukotriene antagonists Montelukast Antiistaminics Levocetirizine Anticholinergic Ipratropium bromide, tiotropium bromide Table 2: Distribution of study population according to prescribed individual and combined drugs Antiasthmatic No.
10] Patients were excluded if they had significant co-morbidities, were receiving oral corticosteroids, LABAs, leukotriene antagonists or theophylline or had undergone an asthma exacerbation or lower respiratory tract infection within the four weeks prior to study entry.
Medications commonly used to treat asthma include corticosteroids (inhaled and oral), leukotriene antagonists (Singulair, Accolate, and Zyflo), theophylline, bronchodilators (both short- and long-acting), and xolair (Omalizumab).
Major Finding: Leukotriene antagonists showed equivalence with inhaled glucocorticoids as first-line therapy for asthma and with beta-agonists as add-on therapy for asthma at 2 months and at 2 years on several measures, but fell just short of demonstrating equivalence on the primary end point at 2 years.
In children leukotriene antagonists may be used as monotherapy in those with milder symptoms and are especially effective in exercise-induced asthma.
Leukotriene antagonists like Singulair have become a common adjuvant along with inhaled steroids and slow-acting, long-duration bronchodilators in the management of asthma.
Leukotriene antagonists have been recommended on a trial basis with follow-up to evaluate the treatment response.
In a systematic review comparing the use of inhaled glucocorticoids with leukotriene antagonists as monotherapy in the treatment of asthma, Ducharme (2003) concluded that leukotriene antagonists are less effective than inhaled glucocorticoids when used as a single agent in the treatment of asthma.